METHODS FOR TREATING HUNTINGTON' S DISEASE

The present description relates to compounds, forms, and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease. In particular, the present description relates to substituted monocyclic heteroaryl compounds, forms and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating

Huntington's disease.

BACKGROUND

Huntington's Disease (HD) is a progressive, autosomal dominant neurodegenerative disorder of the brain, having symptoms characterized by involuntary movements, cognitive impairment, and mental deterioration. Death, typically caused by pneumonia or coronary artery disease, usually occurs 13 to 15 years after the onset of symptoms. The prevalence of HD is between three and seven individuals per 100,000 in populations of western European descent. In North America, an estimated 30,000 people have HD, while an additional 200,000 people are at risk of inheriting the disease from an affected parent. The disease is caused by an expansion of uninterrupted trinucleotide CAG repeats in the "mutant" huntingtin (Htt) gene, leading to production of HTT (Htt protein) with an expanded poly-glutamine (polyQ) stretch, also known as a "CAG repeat" sequence. There are no current small molecule therapies targeting the underlying cause of the disease, leaving a high unmet need for medications that can be used for treating or ameliorating HD. Consequently, there remains a need to identify and provide a small molecule compound for use in treating or ameliorating HD.

All other documents referred to herein are incorporated by reference into the present application as though fully set forth herein.

SUMMARY

The present description relates to a method or use of a compound for treating or ameliorating HD (Huntington's Disease) in a subject in need thereof comprising administering to the subject an effective amount of a compound of Formula (I):

(I) or a form thereof, wherein wi, w ₂ , w ₃ , w ₄ , w ₅ , w ₆ and w ₇ are as defined herein. In particular, the present description relates to a method of use of a compound of Formula (I) or a form or composition thereof for treating or ameliorating HD in a subject in need thereof comprising, administering an effective amount of the compound or a form or composition thereof, to the subject.

DETAILED DESCRIPTION

The present description relates to a method or use of a compound for treating or ameliorating HD (Huntington's Disease) in a subject in need thereof comprising administering to the subject an effective amount of a compound of Formula (I):

(I)

or a form thereof, wherein:

wi and w ₅ are independently C-Ra or N;

W2 is C-Rb or N;

W3, W4 and w ₇ are independently C-Ri, C-R ₂ , C-Ra or N;

we is C-Ri, C-R ₂ , C-Rc or N;

wherein one of w ₃ , w ₄ , w ₆ and w ₇ is C-Ri and one other of w ₃ , w ₄ , w ₆ and w ₇ is C-R ₂ , provided that,

when W3 is C-Ri, then w ₆ is C-R ₂ and w ₄ and w ₇ are independently C-R _a or N; or,

when W3 is C-R ₂ , then w ₆ is C-Ri and w ₄ and w ₇ are independently C-R _a or N; or,

when w ₄ is C-Ri, then w ₇ is C-R ₂ and W3 is C-Ra or N and w ₆ is C-Rc or N; or,

when w ₄ is C-R ₂ , then w ₇ is C-Ri and W3 is C-Ra or N and w ₆ is C-Rc or N; and,

wherein any one, two or three of wi, w ₂ , w ₃ , w ₄ , w ₅ , w ₆ and w ₇ may optionally be N;

Ri is Ci-8alkyl, amino, Ci-salkyl-amino, (Ci-8alkyl) ₂ -amino, Ci-salkoxy-Ci-salkyl-amino,

(Ci-8alkoxy-Ci-8alkyl) ₂ -amino, (Ci-8alkoxy-Ci-8alkyl)(Ci-8alkyl)amino, amino-Ci-salkyl,

Ci-8alkyl-amino-Ci-8alkyl, (Ci-8alkyl) ₂ -amino-Ci-8alkyl,

Ci-salkoxy-Ci-salkyl-amino-Ci-salkyl, (Ci-8alkoxy-Ci-8alkyl) ₂ -amino-Ci-8alkyl,

(Ci-8alkoxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, amino-Ci-salkyl -amino,

(amino-Ci-8alkyl) ₂ -amino, (amino-Ci-8alkyl)(Ci-8alkyl)amino, Ci-8alkyl-amino-Ci-8alkyl-amino, (Ci-8alkyl-amino-Ci-8alkyl)2-amino, (Ci-8alkyl-amino-Ci-8alkyl)(Ci-8alkyl)amino, (Ci-8alkyl)2-amino-Ci-8alkyl-amino,

[(Ci-8alkyl)2-amino-Ci-8alkyl](Ci-8alkyl)amino, amino-Ci-salkoxy,

Ci-8alkyl-amino-Ci-8alkoxy, (Ci-8alkyl)2-amino-Ci-8alkoxy,

Ci-salkoxy-Ci-salkyl-amino-Ci-salkoxy, Ci-salkoxy-Ci-salkyl-amino-Ci-salkoxy,

(Ci-8alkoxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkoxy, amino-C2-8alkenyl,

Ci-8alkyl-amino-C2-8alkenyl, (Ci-8alkyl)2-amino-C2-8alkenyl, amino-C2-8alkynyl,

Ci-8alkyl-amino-C2-8alkynyl, (Ci-8alkyl)2-amino-C2-8alkynyl, halo-Ci-salkyl -amino, (halo-Ci-8alkyl)2-amino, (halo-Ci-8alkyl)(Ci-8alkyl)amino, hydroxy-Ci-salkyl,

hydroxy-Ci-8alkoxy-Ci-8alkyl, hydroxy-Ci-salkyl-amino, (hydroxy-Ci-8alkyl)2-amino, (hydroxy-Ci-8alkyl)(Ci-8alkyl)amino, hydroxy-Ci-salkyl-amino-Ci-salkyl,

(hydroxy-Ci-8alkyl)2-amino-Ci-8alkyl, (hydroxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, hydroxy-Ci-8alkyl-amino-Ci-8alkoxy, (hydroxy-Ci-8alkyl)2-amino-Ci-8alkoxy,

(hydroxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkoxy,

hydroxy-Ci-8alkyl-amino-Ci-8alkyl-amino, (hydroxy-Ci-8alkyl-amino-Ci-8alkyl)2-amino, (hydroxy-Ci-8alkyl)2-amino-Ci-8alkyl-amino,

(hydroxy-Ci-8alkyl-amino-Ci-8alkyl)(Ci-8alkyl)amino,

(hydroxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl-amino,

[(hydroxy-Ci-8alkyl)2-amino-Ci-8alkyl](Ci-8alkyl)amino,

[(hydroxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl](Ci-8alkyl )amino, heterocyclyl, heterocyclyl-Ci-8alkyl, heterocyclyl -Ci-salkoxy, heterocyclyl-amino,

(heterocyclyl)(Ci-8alkyl)amino, heterocyclyl -amino-Ci-salkyl,

heterocyclyl-Ci-8alkyl-amino, (heterocyclyl -Ci-8alkyl)2-amino,

(heterocyclyl-Ci-8alkyl)(Ci-8alkyl)amino, heterocyclyl -Ci-salkyl-amino-Ci-salkyl, (heterocyclyl-Ci-8alkyl)2-amino-Ci-8alkyl,

(heterocyclyl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, heterocyclyl-oxy,

heterocyclyl-carbonyl, heterocyclyl-carbonyl-oxy, C3-i4cycloalkyl, aryl-Ci-salkyl-amino, (aryl-Ci-8alkyl)2-amino, (aryl-Ci-8alkyl)(Ci-8alkyl)amino, aryl-Ci-salkyl-amino-Ci-salkyl, (aryl-Ci-8alkyl)2-amino-Ci-8alkyl, (aryl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, heteroaryl, heteroaryl-Ci-salkyl, heteroaryl-C ι-salkoxy, heteroaryl -amino, heteroaryl-C l-salkyl-amino, (heteroaryl-Ci-8alkyl)2-amino, (heteroaryl-Ci-8alkyl)(Ci-8alkyl)amino, heteroaryl -Ci-8alkyl-amino-Ci-8alkyl, (heteroaryl-Ci-8alkyl)2-amino-Ci-8alkyl or

(heteroaryl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl;

wherein, each instance of heterocyclyl, C3-i4cycloalkyl, aryl and heteroaryl is optionally

substituted with one, two or three R ₃ substituents and optionally, with one additional R ₄ substituent; or,

wherein, each instance of heterocyclyl, C _3- i4cycloalkyl, aryl and heteroaryl is optionally

substituted with one, two, three or four R ₃ substituents;

R ₂ is aryl, aryl-amino, aryl-amino-carbonyl, heterocyclyl, heteroaryl or heteroaryl-amino;

wherein, each instance of aryl, heterocyclyl and heteroaryl is optionally substituted with one, two or three R ₆ substituents and optionally, with one additional R7 substituent;

R _a is, in each instance, independently selected from hydrogen, halogen or Ci-salkyl;

Rb is hydrogen, halogen, Ci-salkyl or Ci-salkoxy;

R _c is hydrogen, halogen or Ci-salkyl;

R ₃ is, in each instance, independently selected from cyano, halogen, hydroxy, oxo, Ci-salkyl, halo-Ci-salkyl, Ci-salkyl-carbonyl, Ci-salkoxy, halo-Ci-salkoxy, Ci-salkoxy-Ci-salkyl, Ci-salkoxy-carbonyl, amino, Ci-salkyl-amino, (Ci-8alkyl) ₂ -amino, amino-Ci-salkyl, Ci-8alkyl-amino-Ci-8alkyl, (Ci-8alkyl) ₂ -amino-Ci-8alkyl, amino-Ci-salkyl-amino,

Ci-8alkyl-amino-Ci-8alkyl-amino, (Ci-8alkyl-amino-Ci-8alkyl) ₂ -amino,

(Ci-8alkyl) ₂ -amino-Ci-8alkyl-amino, [(Ci-8alkyl) ₂ -amino-Ci-8alkyl] ₂ -amino,

(Ci-8alkyl-amino-Ci-8alkyl)(Ci-8alkyl)amino,

[(Ci-8alkyl) ₂ -amino-Ci-8alkyl](Ci-8alkyl)amino, Ci-salkoxy-Ci-salkyl-amino,

(Ci-8alkoxy-Ci-8alkyl) ₂ -amino, (Ci-8alkoxy-Ci-8alkyl)(Ci-8alkyl)amino,

Ci-8alkyl-carbonyl-amino, Ci-salkoxy-carbonyl-amino, hydroxy-Ci-salkyl,

hydroxy-Ci-salkoxy-Ci-salkyl, hydroxy-Ci-salkyl-amino, (hydroxy-Ci-8alkyl) ₂ -amino or (hydroxy-Ci-8alkyl)(Ci-8alkyl)amino;

R4 is C _3- i4cycloalkyl, C _3- i4cycloalkyl-Ci-8alkyl, C _3- i4cycloalkyl-amino, aryl-Ci-salkyl,

aryl-Ci-salkoxy-carbonyl, aryl-sulfonyloxy-Ci-salkyl, heterocyclyl or

heterocyclyl-Ci-salkyl; wherein, each instance of C _3- i4cycloalkyl, aryl and heterocyclyl is optionally substituted with one, two or three R5 substituents; R.5 is, in each instance, independently selected from halogen, hydroxy, cyano, nitro, Ci-salkyl, halo-Ci-8alkyl, Ci-salkoxy, halo-Ci-salkoxy, amino, Ci-salkyl-amino, (Ci-8alkyl)2-amino or Ci-salkyl-thio;

R ₆ is, in each instance, independently selected from halogen, hydroxy, cyano, nitro, Ci-salkyl, C ₂ -8alkenyl, halo-Ci-salkyl, hydroxy-Ci-salkyl, Ci-salkoxy, halo-Ci-salkoxy,

Ci-salkoxy-Ci-salkyl, amino, Ci-salkyl-amino, (Ci-8alkyl) ₂ -amino or Ci-salkyl-thio; and, R7 is C3-i4cycloalkyl, C3-i4cycloalkyl-oxy, aryl, heterocyclyl or heteroaryl; and,

wherein the form of the compound is selected from the group consisting of a salt, prodrug,

hydrate, solvate, clathrate, isotopologue, racemate, enantiomer, diastereomer,

stereoisomer, polymorph and tautomer form thereof.

In one aspect of the use of a compound of Formula (I), wi is C-Ra.

In another aspect of the use of a compound of Formula (I), wi is N.

In one aspect of the use of a compound of Formula (I), w ₂ is C-Rb.

In another aspect of the use of a compound of Formula (I), w ₂ is N.

In one aspect of the use of a compound of Formula (I), w ₃ is C-Ra.

In another aspect of the use of a compound of Formula (I), w ₃ is N.

In one aspect of the use of a compound of Formula (I), w ₄ is C-Ra.

In another aspect of the use of a compound of Formula (I), w ₄ is N.

In one aspect of the use of a compound of Formula (I), w ₅ is C-Ra.

In another aspect of the use of a compound of Formula (I), w ₅ is N.

In one aspect of the use of a compound of Formula (I), w ₆ is C-Rc.

In another aspect of the use of a compound of Formula (I), w ₆ is N.

In one aspect of the use of a compound of Formula (I), w ₇ is C-Ra.

In another aspect of the use of a compound of Formula (I), w ₇ is N.

In one aspect of the use of a compound of Formula (I), w ₃ is C-Ri and w ₆ is C-R ₂ .

In another aspect of the use of a compound of Formula (I), w ₃ is C-R ₂ and w ₆ is C-Ri.

In one aspect of the use of a compound of Formula (I), w ₄ is C-Ri and w ₇ is C-R ₂ .

In another aspect of the use of a compound of Formula (I), w ₄ is C-R ₂ and w ₇ is C-Ri.

In one aspect of the use of a compound of Formula (I), w ₃ is C-Ri, w ₆ is C-R ₂ and wi, w ₄ , w ₅ and w ₇ are independently C-Ra or N and w ₂ is C-Rb or N. In another aspect of the use of a compound of Formula (I), w ₃ is C-R ₂ , w ₆ is C-Ri and wi, w ₄ , w ₅ and W7 are independently C-Ra or N and w ₂ is C-Rb or N.

In one aspect of the use of a compound of Formula (I), w ₄ is C-Ri, w ₇ is C-R ₂ , wi, w ₃ and w ₅ are independently C-Ra or N, w ₂ is C-Rb or N and w ₆ is C-R _c or N.

In another aspect of the use of a compound of Formula (I), w ₄ is C-R ₂ , w ₇ is C-Ri, wi, w ₃ and w ₅ are independently C-R _a or N, w ₂ is C-Rb or N and w ₆ is C-R _c or N.

In one aspect of the use of a compound of Formula (I), wi and w ₂ are N.

In one aspect of the use of a compound of Formula (I), wi and w ₃ are N.

In one aspect of the use of a compound of Formula (I), wi and w ₄ are N.

In one aspect of the use of a compound of Formula (I), wi and w ₅ are N.

In one aspect of the use of a compound of Formula (I), wi and w ₆ are N.

In one aspect of the use of a compound of Formula (I), wi and w ₇ are N.

In one aspect of the use of a compound of Formula (I),

Ri is Ci-8alkyl, amino, Ci-salkyl-amino, (Ci-8alkyl) ₂ -amino, Ci-salkoxy-Ci-salkyl-amino,

(Ci-8alkoxy-Ci-8alkyl) ₂ -amino, (Ci-8alkoxy-Ci-8alkyl)(Ci-8alkyl)amino, amino-Ci-salkyl, Ci-8alkyl-amino-Ci-8alkyl, (Ci-8alkyl) ₂ -amino-Ci-8alkyl,

Ci-salkoxy-Ci-salkyl-amino-Ci-salkyl, (Ci-8alkoxy-Ci-8alkyl) ₂ -amino-Ci-8alkyl,

(Ci-8alkoxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, amino-Ci-salkyl -amino,

(amino-Ci-8alkyl) ₂ -amino, (amino-Ci-8alkyl)(Ci-8alkyl)amino,

Ci-8alkyl-amino-Ci-8alkyl-amino, (Ci-8alkyl-amino-Ci-8alkyl) ₂ -amino,

(Ci-8alkyl-amino-Ci-8alkyl)(Ci-8alkyl)amino, (Ci-8alkyl) ₂ -amino-Ci-8alkyl-amino,

[(Ci-8alkyl) ₂ -amino-Ci-8alkyl](Ci-8alkyl)amino, amino-Ci-salkoxy,

Ci-8alkyl-amino-Ci-8alkoxy, (Ci-8alkyl) ₂ -amino-Ci-8alkoxy,

Ci-salkoxy-Ci-salkyl-amino-Ci-salkoxy, (Ci-8alkoxy-Ci-8alkyl) ₂ -amino-Ci-8alkoxy, (Ci-8alkoxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkoxy, amino-C ₂ -8alkenyl,

Ci-8alkyl-amino-C ₂ -8alkenyl, (Ci-8alkyl) ₂ -amino-C ₂ -8alkenyl, amino-C ₂ -8alkynyl,

Ci-8alkyl-amino-C ₂ -8alkynyl, (Ci-8alkyl) ₂ -amino-C ₂ -8alkynyl, halo-Ci-salkyl -amino, (halo-Ci-8alkyl) ₂ -amino, (halo-Ci-8alkyl)(Ci-8alkyl)amino, hydroxy-Ci-salkyl, hydroxy-Ci-salkoxy-Ci-salkyl, hydroxy-Ci-salkyl-amino, (hydroxy-Ci-8alkyl) ₂ -amino, (hydroxy-Ci-8alkyl)(Ci-8alkyl)amino, hydroxy-Ci-salkyl-amino-Ci-salkyl,

(hydroxy-Ci-8alkyl) ₂ -amino-Ci-8alkyl, (hydroxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, hydroxy-Ci-8alkyl-amino-Ci-8alkoxy, (hydroxy-Ci-8alkyl)2-amino-Ci-8alkoxy,

(hydroxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkoxy,

hydroxy-Ci-8alkyl-amino-Ci-8alkyl-amino, (hydroxy-Ci-8alkyl-amino-Ci-8alkyl)2-amino, (hydroxy-Ci-8alkyl)2-amino-Ci-8alkyl-amino,

(hydroxy-Ci-8alkyl-amino-Ci-8alkyl)(Ci-8alkyl)amino,

(hydroxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl-amino,

[(hydroxy-Ci-8alkyl)2-amino-Ci-8alkyl](Ci-8alkyl)amino,

[(hydroxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl](Ci-8alkyl )amino, heterocyclyl, heterocyclyl-Ci-8alkyl, heterocyclyl -Ci-salkoxy, heterocyclyl-amino,

(heterocyclyl)(Ci-8alkyl)amino, heterocyclyl -amino-Ci-salkyl,

heterocyclyl-Ci-8alkyl-amino, (heterocyclyl -Ci-8alkyl)2-amino,

(heterocyclyl-Ci-8alkyl)(Ci-8alkyl)amino, heterocyclyl -Ci-salkyl-amino-Ci-salkyl, (heterocyclyl-Ci-8alkyl)2-amino-Ci-8alkyl,

(heterocyclyl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, heterocyclyl-oxy,

heterocyclyl-carbonyl, heterocyclyl-carbonyl-oxy, C3-i4cycloalkyl, aryl-Ci-salkyl-amino, (aryl-Ci-8alkyl)2-amino, (aryl-Ci-8alkyl)(Ci-8alkyl)amino, aryl-Ci-salkyl-amino-Ci-salkyl, (aryl-Ci-8alkyl)2-amino-Ci-8alkyl, (aryl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, heteroaryl, heteroaryl-Ci-salkyl, heteroaryl-Ci-salkoxy, heteroaryl -amino, heteroaryl-Ci-salkyl-amino, (heteroaryl-Ci-8alkyl)2-amino, (heteroaryl-Ci-8alkyl)(Ci-8alkyl)amino,

heteroaryl -Ci-8alkyl-amino-Ci-8alkyl, (heteroaryl-Ci-8alkyl)2-amino-Ci-8alkyl or

(heteroaryl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl; wherein, each instance of heterocyclyl, C3-i4cycloalkyl, aryl and heteroaryl is optionally substituted with R3 and R4 substituents. er aspect of the use of a compound of Formula (I),

ino, (Ci-8alkyl)2-amino, Ci-salkoxy-Ci-salkyl-amino, (Ci-8alkoxy-Ci-8alkyl)2-amino, amino-Ci-8alkyl, Ci-salkyl-amino-Ci-salkyl, (Ci-8alkyl)2-amino-Ci-8alkyl,

Ci-salkoxy-Ci-salkyl-amino-Ci-salkyl, (Ci-8alkoxy-Ci-8alkyl)2-amino-Ci-8alkyl,

(Ci-8alkoxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, amino-Ci-salkyl -amino,

(amino-Ci-8alkyl)2-amino, (amino-Ci-8alkyl)(Ci-8alkyl)amino,

Ci-8alkyl-amino-Ci-8alkyl-amino, (Ci-8alkyl-amino-Ci-8alkyl)2-amino,

(Ci-8alkyl-amino-Ci-8alkyl)(Ci-8alkyl)amino, (Ci-8alkyl)2-amino-Ci-8alkyl-amino,

[(Ci-8alkyl)2-amino-Ci-8alkyl](Ci-8alkyl)amino, amino-Ci-salkoxy, Ci-8alkyl-amino-Ci-8alkoxy, (Ci-8alkyl)2-amino-Ci-8alkoxy,

Ci-salkoxy-Ci-salkyl-amino-Ci-salkoxy, (Ci-8alkoxy-Ci-8alkyl)2-amino-Ci-8alkoxy, (Ci-8alkoxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkoxy, amino-C2-8alkenyl,

Ci-8alkyl-amino-C2-8alkenyl, (Ci-8alkyl)2-amino-C2-8alkenyl, amino-C2-8alkynyl, Ci-8alkyl-amino-C2-8alkynyl, (Ci-8alkyl)2-amino-C2-8alkynyl, halo-Ci-salkyl -amino, (halo-Ci-8alkyl)2-amino, (halo-Ci-8alkyl)(Ci-8alkyl)amino, hydroxy-Ci-salkyl, hydroxy-Ci-8alkoxy-Ci-8alkyl, hydroxy-Ci-salkyl-amino, (hydroxy-Ci-8alkyl)2-amino, (hydroxy-Ci-8alkyl)(Ci-8alkyl)amino, hydroxy-Ci-salkyl-amino-Ci-salkyl,

(hydroxy-Ci-8alkyl)2-amino-Ci-8alkyl, (hydroxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, hydroxy-Ci-8alkyl-amino-Ci-8alkoxy, (hydroxy-Ci-8alkyl)2-amino-Ci-8alkoxy,

(hydroxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkoxy,

hydroxy-Ci-8alkyl-amino-Ci-8alkyl-amino, (hydroxy-Ci-8alkyl-amino-Ci-8alkyl)2-amino, (hydroxy-Ci-8alkyl)2-amino-Ci-8alkyl-amino,

(hydroxy-Ci-8alkyl-amino-Ci-8alkyl)(Ci-8alkyl)amino,

(hydroxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl-amino,

[(hydroxy-Ci-8alkyl)2-amino-Ci-8alkyl](Ci-8alkyl)amino,

[(hydroxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl](Ci-8alkyl )amino, heterocyclyl, heterocyclyl-Ci-salkyl, heterocyclyl -Ci-salkoxy, heterocyclyl-amino,

(heterocyclyl)(Ci-8alkyl)amino, heterocyclyl -amino-Ci-salkyl,

heterocyclyl-Ci-8alkyl-amino, (heterocyclyl -Ci-8alkyl)2-amino,

(heterocyclyl-Ci-8alkyl)(Ci-8alkyl)amino, heterocyclyl -Ci-salkyl-amino-Ci-salkyl, (heterocyclyl-Ci-8alkyl)2-amino-Ci-8alkyl,

(heterocyclyl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, heterocyclyl-oxy,

heterocyclyl-carbonyl, heterocyclyl-carbonyl-oxy, C3-i4cycloalkyl, aryl-Ci-salkyl-amino, (aryl-Ci-8alkyl)2-amino, (aryl-Ci-8alkyl)(Ci-8alkyl)amino, aryl-Ci-salkyl-amino-Ci-salkyl, (aryl-Ci-8alkyl)2-amino-Ci-8alkyl, (aryl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, heteroaryl, heteroaryl-Ci-salkyl, heteroaryl-Ci-salkoxy, heteroaryl-Ci-salkyl -amino,

(heteroaryl-Ci-8alkyl)2-amino, (heteroaryl-Ci-8alkyl)(Ci-8alkyl)amino,

heteroaryl -Ci-8alkyl-amino-Ci-8alkyl, (heteroaryl-Ci-8alkyl)2-amino-Ci-8alkyl or

(heteroaryl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl; wherein, each instance of heterocyclyl, C3-i4cycloalkyl, aryl and heteroaryl is optionally substituted with R3 and R4 substituents. In another aspect of the use of a compound of Formula (I),

Ri is Ci-8alkyl, amino, Ci-salkyl-amino, (Ci-8alkyl)2-amino, Ci-salkoxy-Ci-salkyl-amino,

(Ci-8alkoxy-Ci-8alkyl)2-amino, (Ci-8alkoxy-Ci-8alkyl)(Ci-8alkyl)amino, amino-Ci-salkyl, Ci-8alkyl-amino-Ci-8alkyl, (Ci-8alkyl)2-amino-Ci-8alkyl,

Ci-salkoxy-Ci-salkyl-amino-Ci-salkyl, (Ci-8alkoxy-Ci-8alkyl)2-amino-Ci-8alkyl,

(Ci-8alkoxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, amino-Ci-salkyl -amino,

(amino-Ci-8alkyl)2-amino, (amino-Ci-8alkyl)(Ci-8alkyl)amino,

Ci-8alkyl-amino-Ci-8alkyl-amino, (Ci-8alkyl-amino-Ci-8alkyl)2-amino,

(Ci-8alkyl-amino-Ci-8alkyl)(Ci-8alkyl)amino, (Ci-8alkyl)2-amino-Ci-8alkyl-amino,

[(Ci-8alkyl)2-amino-Ci-8alkyl](Ci-8alkyl)amino, amino-Ci-salkoxy,

Ci-8alkyl-amino-Ci-8alkoxy, (Ci-8alkyl)2-amino-Ci-8alkoxy,

Ci-salkoxy-Ci-salkyl-amino-Ci-salkoxy, (Ci-8alkoxy-Ci-8alkyl)2-amino-Ci-8alkoxy, (Ci-8alkoxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkoxy, amino-C2-8alkenyl,

Ci-8alkyl-amino-C2-8alkenyl, (Ci-8alkyl)2-amino-C2-8alkenyl, amino-C2-8alkynyl, Ci-8alkyl-amino-C2-8alkynyl, (Ci-8alkyl)2-amino-C2-8alkynyl, halo-Ci-salkyl -amino, (halo-Ci-8alkyl)2-amino, (halo-Ci-8alkyl)(Ci-8alkyl)amino, hydroxy-Ci-salkyl, hydroxy-Ci-salkoxy-Ci-salkyl, hydroxy-Ci-salkyl-amino, (hydroxy-Ci-8alkyl)2-amino, (hydroxy-Ci-8alkyl)(Ci-8alkyl)amino, hydroxy-Ci-salkyl-amino-Ci-salkyl,

(hydroxy-Ci-8alkyl)2-amino-Ci-8alkyl, (hydroxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, hydroxy-Ci-8alkyl-amino-Ci-8alkoxy, (hydroxy-Ci-8alkyl)2-amino-Ci-8alkoxy,

(hydroxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkoxy,

hydroxy-Ci-8alkyl-amino-Ci-8alkyl-amino, (hydroxy-Ci-8alkyl-amino-Ci-8alkyl)2-amino, (hydroxy-Ci-8alkyl)2-amino-Ci-8alkyl-amino,

(hydroxy-Ci-8alkyl-amino-Ci-8alkyl)(Ci-8alkyl)amino,

(hydroxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl-amino,

[(hydroxy-Ci-8alkyl)2-amino-Ci-8alkyl](Ci-8alkyl)amino or

[(hydroxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl](Ci-8alkyl)am ino.

In another aspect of the use of a compound of Formula (I),

Ri is heterocyclyl, heterocyclyl-Ci-salkyl, heterocyclyl-Ci-salkoxy, heterocyclyl-amino,

(heterocyclyl)(Ci-8alkyl)amino, heterocyclyl -amino-Ci-salkyl,

heterocyclyl-Ci-8alkyl-amino, (heterocyclyl -Ci-8alkyl)2-amino, (heterocyclyl-Ci-8alkyl)(Ci-8alkyl)amino, heterocyclyl -Ci-salkyl-amino-Ci-salkyl, (heterocyclyl-Ci-8alkyl)2-amino-Ci-8alkyl,

(heterocyclyl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, heterocyclyl-oxy,

heterocyclyl-carbonyl, heterocyclyl-carbonyl-oxy, C3-i4cycloalkyl, aryl-Ci-salkyl-amino, (aryl-Ci-8alkyl)2-amino, (aryl-Ci-8alkyl)(Ci-8alkyl)amino, aryl-Ci-salkyl-amino-Ci-salkyl, (aryl-Ci-8alkyl)2-amino-Ci-8alkyl, (aryl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, heteroaryl, heteroaryl-Ci-salkyl, heteroaryl-Ci-salkoxy, heteroaryl -amino, heteroaryl-Ci-salkyl-amino, (heteroaryl-Ci-8alkyl)2-amino, (heteroaryl-Ci-8alkyl)(Ci-8alkyl)amino,

heteroaryl -Ci-8alkyl-amino-Ci-8alkyl, (heteroaryl-Ci-8alkyl)2-amino-Ci-8alkyl or

(heteroaryl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl; wherein, each instance of heterocyclyl, C3-i4cycloalkyl, aryl and heteroaryl is optionally substituted with R3 and R ₄ substituents. In another aspect of the use of a compound of Formula (I),

Ri is heterocyclyl, heterocyclyl-Ci-salkyl, heterocyclyl-Ci-salkoxy, heterocyclyl-amino,

(heterocyclyl)(Ci-8alkyl)amino, heterocyclyl -amino-Ci-salkyl,

heterocyclyl-Ci-8alkyl-amino, (heterocyclyl -Ci-8alkyl)2-amino,

(heterocyclyl-Ci-8alkyl)(Ci-8alkyl)amino, heterocyclyl -Ci-salkyl-amino-Ci-salkyl, (heterocyclyl-Ci-8alkyl)2-amino-Ci-8alkyl,

(heterocyclyl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, heterocyclyl-oxy,

heterocyclyl-carbonyl or heterocyclyl-carbonyl-oxy; wherein, each instance of heterocyclyl is optionally substituted with R3 and R ₄ substituents.

In another aspect of the use of a compound of Formula (I), Ri is heterocyclyl optionally

substituted with one, two or three R3 substituents and optionally, with one additional R ₄ substituents; or, optionally, with one, two, three or four R3 substituents.

In another aspect of the use of a compound of Formula (I), Ri is C3-i ₄ cycloalkyl optionally

substituted with R3 and R ₄ substituents.

In another aspect of the use of a compound of Formula (I),

Ri is aryl-Ci-8alkyl-amino, (aryl-Ci-8alkyl)2-amino, (aryl-Ci-8alkyl)(Ci-8alkyl)amino,

aryl-Ci-8alkyl-amino-Ci-8alkyl, (aryl-Ci-8alkyl)2-amino-Ci-8alkyl or

(aryl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl; wherein, each instance of aryl is optionally substituted with R3 and R ₄ substituents. In another aspect of the use of a compound of Formula (I), Ri is aryl-Ci-salkyl-amino optionally substituted with R ₃ and R ₄ substituents.

In another aspect of the use of a compound of Formula (I),

Ri is heteroaryl, heteroaryl-Ci-salkyl, heteroaryl-Ci-salkoxy, heteroaryl-amino,

heteroaryl -Ci-salkyl-amino, (heteroaryl-Ci-8alkyl)2-amino,

(heteroaryl-Ci-8alkyl)(Ci-8alkyl)amino, heteroaryl-Ci-salkyl-amino-Ci-salkyl,

(heteroaryl-Ci-8alkyl)2-amino-Ci-8alkyl or

(heteroaryl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl; wherein, each instance of heterocyclyl, C _3- i4cycloalkyl, aryl and heteroaryl is optionally substituted with R ₃ and R ₄ substituents.

In another aspect of the use of a compound of Formula (I), Ri is heteroaryl optionally substituted with R ₃ and R ₄ substituents.

In one aspect of the use of a compound of Formula (I),

Ri is heterocyclyl selected from azetidinyl, tetrahydrofuranyl, pyrrolidinyl, piperidinyl,

piperazinyl, 1,4-diazepanyl, 3,6-dihydropyridinyl, 1,2,5,6-tetrahydropyridinyl,

1,2,3,6-tetrahydropyridinyl, hexahydropyrrolo[3,4-£]pyirol-(lH)-yl,

(3a,S',6a ₎ S)-hexahydropyrrolo[3,4-^]pyrrol-(lH)-yl,

(3aR,6aR)-hexahydropyrrolo[3,4-£]pyrrol-(lH)-yl,

hexahydropyrrolo[3,4-£]pyrrol-(2H)-yl, (3a,S',6a ₎ S)-hexahydropyrrolo[3,4-^]pyrrol-(2H)-yl, hexahydropyrrolo[3,4-c]pyrrol-(lH)-yl, (3aR,6a,S)-hexahydropyrrolo[3,4-c]pyrrol-(lH)-yl, l,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrolyl, octahydro-5H-pyrrolo[3,2-c]pyridinyl, octahydro-6H-pyrrolo[3,4-£]pyridinyl, (4aR,7aR)-octahydro-6H-pyirolo[3,4-£]pyridinyl, (4a,S',7a ₎ S)-octahydro-6H-pyrrolo[3,4-^]pyridinyl,

hexahydropyrrolo[ 1 ,2-a]pyrazin-(2H)-one, hexahydropyrrolo[ 1 ,2-a]pyrazin-( lH)-yl,

(7R, 8 a^-hexahy dropyrrol o [ 1 , 2-a] pyrazin-( lH)-yl ,

(8a,S)-hexahydropyrrolo[l,2-a]pyrazin-(lH)-yl,

(8aR)-hexahydropyrrolo[l,2-a]pyrazin-(lH)-yl,

(8a,S)-3,4,6,7,8,8a-hexahydro-lH-pyrrolo[l,2-a]pyrazinyl,

(8aR)-3, 4,6,7,8, 8a-hexahydro-lH-pyrrolo[l,2-a]pyrazinyl,

(8a,S)-l,3,4,6,7,8-hexahydropyrrolo[l,2-a]pyrazinyl,

(8aR)-l,3,4,6,7,8-hexahydropyrrolo[l,2-a]pyrazinyl,

(8a,S)-octahydropyrrolo[l,2-a]pyrazin-(lH)-yl, (8aR)-octahydropyrrolo[ 1 ,2-a]pyrazin-(lH)-yl, octahydro-2H-pyrido[ 1 ,2-a]pyrazinyl, (3aR,4aR,7aS)-hexahydro-lH-cyclobuta[l,2-c: l,4-c']dipyrrol-(3H)-yl,

3-azabicyclo[3.1.0]hexyl, (lR,5,S)-3-azabicyclo[3.1.0]hexyl, 8-azabicyclo[3.2.1]octyl, (lR,55)-8-azabicyclo[3.2.1]octyl, 8-azabicyclo[3.2.1]oct-2-enyl,

(li?,5,S)-8-azabicyclo[3.2.1]oct-2-enyl, 9-azabicyclo[3.3.1]nonyl,

(li?,5,S)-9-azabicyclo[3.3.1]nonyl, 2,5-diazabicyclo[2.2.1]heptyl,

(l,S 4,S 2,5-diazabicyclo[2.2.1]heptyl, 2,5-diazabicyclo[2.2.2]octyl,

3,6-diazabicyclo[3.2.0]heptyl, 3,8-diazabicyclo[3.2.1]octyl,

(li?,5,S)-3,8-diazabicyclo[3.2.1]octyl, l,4-diazabicyclo[3.2.2]nonyl, azaspiro[3.3]heptyl,

2.6- diazaspiro[3.3]heptyl, 4,7-diazaspiro[2.5]octyl, 2,6-diazaspiro[3.4]octyl,

2.7- diazaspiro[3.5]nonyl, 5,8-diazaspiro[3.5]nonyl, 2,7-diazaspiro[4.4]nonyl or

6,9-diazaspiro[4.5]decyl; wherein, each instance of heterocyclyl is optionally substituted with one, two or three R ₃ substituents and optionally, with one additional R ₄ substituent; or, optionally, with one, two, three or four R ₃ substituents.

er aspect of the use of a compound of Formula (I),

terocyclyl selected from azetidin-l-yl, tetrahydrofuran-3-yl, pyrrolidin-l-yl,

piperidin-l-yl, piped din-4-yl, piperazin-l-yl, 1,4-diazepan-l-yl, 3,6-dihydropyridin-4-yl, l,2,5,6-tetrahydropyridin-5-yl, 1,2,3, 6-tetrahydropyridin-4-yl,

hexahydropyrrolo[3,4-£]pyrrol-l(2H)-yl,

(3a,S',6a ₎ S)-hexahydropyrrolo[3,4-^]pyrrol-l(2H)-yl,

(3a,S',6a ₎ S)-hexahydropyrrolo[3,4-^]pyrrol-5(lH)-yl,

(3aR,6aR)-hexahydropyrrolo[3,4-£]pyrrol-5(lH)-yl,

hexahydropyrrolo[3,4-c]pyrrol-2(lH)-yl,

(3aR,6a,S)-hexahydropyrrolo[3,4-c]pyrrol-2(lH)-yl,

octahydro-5H-pyrrolo[3,2-c]pyridin-5-yl, octahydro-6H-pyrrolo[3,4-£]pyridin-6-yl,

(4aR,7aR)-octahydro-6H-pyrrolo[3,4-£]pyridin-6-yl,

(4a,S',7a ₎ S)-octahydro-6H-pyrrolo[3,4-^]pyridin-6-yl,

hexahydropyrrolo[ 1 ,2-a]pyrazin-6(2H)-one, hexahydropyrrolo[ 1 ,2-a]pyrazin-2( lH)-yl, (7R,8a,S)-hexahydropyrrolo[l,2-a]pyrazin-2(lH)-yl,

(8a,S)-hexahydropyrrolo[l,2-a]pyrazin-2(lH)-yl,

(8aR)-hexahydropyrrolo[l,2-a]pyrazin-2(lH)-yl, (8a,S)-3,4,6,7,8,8a-hexahydro-lH-pyrrolo[l,2-a]pyrazin-2-yl,

(8aR)-3, 4,6,7,8, 8a-hexahydro-lH-pyrrolo[l,2-a]pyrazin-2-yl,

(8aS)- 1 ,3 ,4,6,7,8-hexahydropyrrolo[ 1 ,2-a]pyrazin-2-yl,

(8aR)-l,3,4,6,7,8-hexahydropyrrolo[l,2-a]pyrazin-2-yl,

(8a,S)-octahydropyrrolo[l,2-a]pyrazin-2(lH)-yl,

(8aR)-octahydropyrrolo[ 1 ,2-a]pyrazin-2(lH)-yl, octahydro-2H-pyrido[ 1 ,2-a]pyrazin-2-yl, (3aR,4aR,7aS)-hexahydro-lH-cyclobuta[l,2-c: l,4-c']dipyrrol-2(3H)-yl,

3-azabicyclo[3.1.0]hex-3-yl, 8-azabicyclo[3.2.1]oct-3-yl,

(lR,5S)-8-azabicyclo[3.2.1]oct-3-yl, 8-azabicyclo[3.2.1]oct-2-en-3-yl,

(li?,5,S)-8-azabicyclo[3.2.1]oct-2-en-3-yl, 9-azabicyclo[3.3.1]non-3-yl,

(lR,55)-9-azabicyclo[3.3.1]non-3-yl, 2,5-diazabicyclo[2.2.1]hept-2-yl,

(l,S 4,S 2,5-diazabicyclo[2.2.1]hept-2-yl, 2,5-diazabicyclo[2.2.2]oct-2-yl,

3,6-diazabicyclo[3.2.0]hept-3-yl, 3,8-diazabicyclo[3.2.1]oct-3-yl,

(lR,55)-3,8-diazabicyclo[3.2.1]oct-3-yl, l,4-diazabicyclo[3.2.2]non-4-yl,

azaspiro[3.3]hept-2-yl, 2,6-diazaspiro[3.3]hept-2-yl, 4,7-diazaspiro[2.5]oct-7-yl,

2,6-diazaspiro[3.4]oct-2-yl, 2,7-diazaspiro[3.5]non-2-yl, 2,7-diazaspiro[3.5]non-7-yl, 5,8-diazaspiro[3.5]non-8-yl, 2,7-diazaspiro[4.4]non-2-yl or 6,9-diazaspiro[4.5]dec-9-yl; wherein, each instance of heterocyclyl is optionally substituted with one, two or three R ₃ substituents and optionally, with one additional R ₄ substituent; or, optionally, with one, two, three or four R ₃ substituents.

er aspect of the use of a compound of Formula (I),

bstituted heterocyclyl selected from (3R)-3-pyrrolidin-l-ylpyrrolidin-l-yl,

l-methylpiperidin-4-yl, l-ethylpiperidin-4-yl, 2,2,6,6-tetramethylpiperidin-4-yl,

(3 S)-3 -methylpiperazin- 1 -yl, 4-methylpiperazin- 1 -yl, 4-ethylpiperazin- 1 -yl,

3- (trifluoromethyl)piperazin-l-yl, l-tert-butoxy-carbonyl-3,6-dihydropyridin-4-yl, l-ethyl-l,2,3,6-tetrahydropyridin-4-yl, 2,2,6,6-tetramethyl-l,2,3,6-tetrahydropyridin-4-yl,

4- methyl- 1 ,4-diazepan- 1 -yl, (3 aS,6aS)- 1 -methylhexahydropyrrolo[3 ,4-£]pyrrol-5(lH)-yl, (3a,S',6a ₎ S)-5-methylhexahydropyrrolo[3,4-^]pyrrol-l(2H)-yl,

(3aR,6aR)-l-methylhexahydropyrrolo[3,4-^]pyrrol-5(lH)-yl,

(3aR,6a,S)-5-methylhexahydropyrrolo[3,4-c]pyrrol-2(lH)-yl ,

(3aR,6a,S)-5-(2-hydroxyethyl)hexahydropyrrolo[3,4-c]pyrro l-2(lH)-yl, (3aR,6a,S)-5-(propan-2-yl)hexahydropyrrolo[3,4-c]pyrrol-2(lH )-yl,

(3aR,6a,S)-5-ethylhexahydropyrrolo[3,4-c]pyrrol-2(lH)-yl,

(4aR,7aR)-l-methyloctahydro-6H-pyrrolo[3,4-^]pyridin-6-yl,

(4aR,7aR)-l-ethyloctahydro-6H-pyrrolo[3,4-^]pyridin-6-yl,

(4aR,7aR)-l-(2-hydroxyethyl)octahydro-6H-pyrrolo[3,4-^]pyrid in-6-yl,

(4a,S',7a ₎ S)-l-methyloctahydro-6H-pyrrolo[3,4-^]pyridin-6-yl,

(4a,S',7a ₎ S)-l-(2-hydroxyethyl)octahydro-6H-pyrrolo[3,4-^]pyridi n-6-yl,

(7R,8a,S)-7-hydroxyhexahydropyrrolo[l,2-a]pyrazin-2(lH)-yl,

(8a,S)-8a-methyl-l,3,4,6,7,8-hexahydropyrrolo[l,2-a]pyrazin- 2-yl,

(8aR)-8a-m ethyl- 1 ,3 ,4,6,7, 8-hexahydropyrrolo[ 1 ,2-a]pyrazin-2-yl,

(8a,S)-8a-methyloctahydropyrrolo[ 1 ,2-a]pyrazin-2(lH)-yl,

(8aR)-8a-methyloctahydropyrrolo[l,2-a]pyrazin-2(lH)-yl,

(lR,5,S',6s)-6-(dimethylamino)-3-azabicyclo[3.1.0]hex-3-yl,

(lR,5,S)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl, 9-methyl-9-azabicyclo[3.3.1]non-3-yl, (3-exo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl,

(lR,55)-9-methyl-9-azabicyclo[3.3.1]non-3-yl,

(l-S'^^-S-methyl^^-diazabicycloP^. ^hept^-yl,

(l-S^-S-ethyl^S-diazabicycloP^. l]hept-2-yl or 6-methyl-2,6-diazaspiro[3.3]hept-2-yl. In one aspect of the use of a compound of Formula (I), Ri is heterocyclyl-C l-salkyl, wherein

heterocyclyl is selected from morpholinyl, piperidinyl, piperazinyl, imidazolyl or pyrrolidinyl; and, wherein, each instance of heterocyclyl is optionally substituted with R ₃ and R ₄ substituents.

In another aspect of the use of a compound of Formula (I), Ri is heterocyclyl-Ci-salkyl selected from morpholin-4-yl-methyl, morpholin-4-yl-ethyl, morpholin-4-yl-propyl,

piperi din- 1-yl -methyl, piperazin-l-yl-methyl, piperazin-l-yl-ethyl, piperazin-l-yl-propyl, piperazin-l-yl -butyl, imidazol-l-yl -methyl, imidazol-l-yl-ethyl, imidazol-l-yl-propyl, imidazol-l-yl -butyl, pyrrolidin- 1-yl -methyl, pyrrolidin-l-yl-ethyl, pyrrolidin-l-yl-propyl or pyrrolidin- 1-yl -butyl; wherein, each instance of heterocyclyl is optionally substituted with R ₃ and R ₄ substituents. In one aspect of the use of a compound of Formula (I), Ri is heterocyclyl-Ci-salkoxy, wherein heterocyclyl is selected from pyrrolidinyl, piperidinyl or morpholinyl; and, wherein, each instance of heterocyclyl is optionally substituted with R ₃ and R ₄ substituents.

In another aspect of the use of a compound of Formula (I), Ri is heterocyclyl-Ci-salkoxy selected from pyrrolidin-2-yl-methoxy, pyrrolidin-2-yl-ethoxy, pyrrolidin-l-yl-methoxy, pyrrolidin- 1 -yl-ethoxy, piperidin- 1 -yl-methoxy, piped din- 1 -yl-ethoxy,

morpholin-4-yl-methoxy or morpholin-4-yl-ethoxy; wherein, each instance of heterocyclyl is optionally substituted with R ₃ and R ₄ substituents.

In one aspect of the use of a compound of Formula (I), Ri is heterocyclyl-amino, wherein

heterocyclyl is selected from azetidinyl, pyrrolidinyl, piperidinyl,

9-azabicyclo[3.3.1]nonyl or (li?,5,S)-9-azabicyclo[3.3.1]nonyl; and, wherein, each instance of heterocyclyl is optionally substituted with R ₃ and R ₄ substituents.

In another aspect of the use of a compound of Formula (I), Ri is heterocyclyl-amino selected from azetidin-3-yl-amino, pyrrolidin-3-yl-amino, piperidin-4-yl-amino,

9-azabicyclo[3.3.1]non-3-yl-amino, (lR,5,S)-9-azabicyclo[3.3.1]non-3-yl-amino,

9-methyl-9-azabicyclo[3.3.1]non-3-yl-amino,

(3-exo)-9-methyl-9-azabicyclo[3.3. l]non-3-yl-amino or (lR,5S)-9-methyl-9- azabicyclo[3.3.1]non-3-yl-amino; wherein, each instance of heterocyclyl is optionally substituted with R ₃ and R ₄ substituents.

In one aspect of the use of a compound of Formula (I), Ri is (heterocyclyl)(Ci-8alkyl)amino, wherein heterocyclyl is selected from pyrrolidinyl or piperidinyl; and, wherein, each instance of heterocyclyl is optionally substituted with R ₃ and R ₄ substituents.

In another aspect of the use of a compound of Formula (I), Ri is (heterocyclyl)(Ci-8alkyl)amino selected from (pyrrolidin-3-yl)(methyl)amino or (piperidin-4-yl)(methyl)amino; wherein, each instance of heterocyclyl is optionally substituted with R ₃ and R ₄ substituents.

In one aspect of the use of a compound of Formula (I), Ri is heterocyclyl-amino-Ci-salkyl,

wherein heterocyclyl is selected from tetrahydrofuranyl; and, wherein, each instance of heterocyclyl is optionally substituted with R ₃ and R ₄ substituents.

In another aspect of the use of a compound of Formula (I), Ri is heterocyclyl -amino-Ci-salkyl, selected from 3-(tetrahydrofuran-3-yl-amino)propyl; wherein, each instance of

heterocyclyl is optionally substituted with R ₃ and R ₄ substituents. In one aspect of the use of a compound of Formula (I), Ri is

heterocyclyl-Ci-8alkyl-amino-Ci-8alkyl, wherein heterocyclyl is selected from

tetrahydrofuranyl, thienyl or pyridinyl; and, wherein, each instance of heterocyclyl is optionally substituted with R ₃ and R ₄ substituents.

In another aspect of the use of a compound of Formula (I), Ri is

heterocyclyl-Ci-8alkyl-amino-Ci-8alkyl, selected from 3-[(tetrahydrofuran-2- ylmethyl)amino]propyl, 3-[(thienyl-3-ylmethyl)amino]propyl, 3-[(pyridin-2- ylmethyl)amino]propyl or 3-[(pyridin-4-ylmethyl)amino]propyl; wherein, each instance of heterocyclyl is optionally substituted with R ₃ and R ₄ substituents.

In one aspect of the use of a compound of Formula (I), Ri is heterocyclyl-oxy, wherein

heterocyclyl is selected from pyrrolidinyl or piperidinyl; and, wherein, each instance of heterocyclyl is optionally substituted with R ₃ and R ₄ substituents.

In another aspect of the use of a compound of Formula (I), Ri is heterocyclyl-oxy selected from pyrrolidin-3-yl-oxy or piperidin-4-yl-oxy; wherein, each instance of heterocyclyl is optionally substituted with R ₃ and R ₄ substituents.

In one aspect of the use of a compound of Formula (I), Ri is heterocyclyl-carbonyl, wherein

heterocyclyl is selected from piperazinyl; and, wherein, each instance of heterocyclyl is optionally substituted with R ₃ and R ₄ substituents.

In another aspect of the use of a compound of Formula (I), Ri is heterocyclyl-carbonyl selected from piperazin-l-yl-carbonyl; wherein, each instance of heterocyclyl is optionally substituted with R ₃ and R ₄ substituents.

In one aspect of the use of a compound of Formula (I), Ri is heterocyclyl-carbonyl-oxy, wherein heterocyclyl is selected from piperazinyl; and, wherein, each instance of heterocyclyl is optionally substituted with R ₃ and R ₄ substituents.

In another aspect of the use of a compound of Formula (I), Ri is heterocyclyl-carbonyl-oxy

selected from piperazin-l-yl-carbonyl-oxy; wherein, each instance of heterocyclyl is optionally substituted with R ₃ and R ₄ substituents.

In one aspect of the use of a compound of Formula (I), Ri is C _3- i ₄ cycloalkyl selected from

cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl or cycloheptyl; wherein, each instance of C _3- i ₄ cycloalkyl is optionally substituted with R ₃ and R ₄ substituents. In another aspect of the use of a compound of Formula (I), Ri is C3-8cycloalkyl selected from cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl or cycloheptyl; wherein, each instance of C3-8cycloalkyl is optionally substituted with R ₃ and R ₄ substituents.

In one aspect of the use of a compound of Formula (I), Ri is aiyl-Ci-salkyl-amino-Ci-salkyl,

wherein aryl is selected from phenyl; and, wherein, each instance of aryl is optionally substituted with R ₃ and R ₄ substituents.

In another aspect of the use of a compound of Formula (I), Ri is aiyl-Ci-salkyl-amino-Ci-salkyl selected from 3-(benzylamino)propyl; wherein, each instance of aryl is optionally substituted with R ₃ and R ₄ substituents.

In one aspect of the use of a compound of Formula (I), Ri is heteroaryl, wherein heteroaryl is selected from pyridinyl; and, wherein, each instance of heteroaryl is optionally substituted with R ₃ and R ₄ substituents.

In another aspect of the use of a compound of Formula (I), Ri is heteroaryl selected from pyridin-

4-yl; wherein, each instance of heteroaryl is optionally substituted with R ₃ and R ₄ substituents.

In one aspect of the use of a compound of Formula (I), Ri is heteroaryl-Ci-salkyl, wherein

heteroaryl is selected from lH-imidazolyl; and, wherein, each instance of heteroaryl is optionally substituted with R ₃ and R ₄ substituents.

In another aspect of the use of a compound of Formula (I), Ri is heteroaryl-Ci-salkyl selected from lH-imidazol-l-yl -methyl; wherein, each instance of heteroaryl is optionally substituted with R ₃ and R ₄ substituents.

In one aspect of the use of a compound of Formula (I), Ri is

(heteroaryl-Ci-8alkyl)(Ci-8alkyl)amino, wherein heteroaryl is selected from pyridinyl; and, wherein, each instance of heteroaryl is optionally substituted with R ₃ and R ₄ substituents. In another aspect of the use of a compound of Formula (I), Ri is

(heteroaryl-Ci-8alkyl)(Ci-8alkyl)amino selected from (pyridin-3-ylmethyl)(methyl)amino; wherein, each instance of heteroaryl is optionally substituted with R ₃ and R ₄ substituents. In one aspect of the use of a compound of Formula (I), Ri is heteroaryl-Ci-salkyl-amino-Ci-salkyl, wherein heteroaryl is selected from thienyl or pyridinyl; and, wherein, each instance of heteroaryl is optionally substituted with R ₃ and R ₄ substituents. In another aspect of the use of a compound of Formula (I), Ri is

heteroaryl-Ci-8alkyl-amino-Ci-8alkyl selected from thien-3-yl-methyl-amino-propyl, pyridin-2-yl-methyl-amino-propyl, pyridin-3-yl-methyl-amino-propyl or

pyridin-4-yl-methyl-amino-propyl; wherein, each instance of heteroaryl is optionally substituted with R ₃ and R ₄ substituents.

In one aspect of the use of a compound of Formula (I), R ₃ is selected from cyano, halogen,

hydroxy, oxo, Ci-salkyl, halo-Ci-salkyl, Ci-salkyl-carbonyl, Ci-salkoxy, halo-Ci-salkoxy, Ci-salkoxy-Ci-salkyl, Ci-salkoxy-carbonyl, amino, Ci-salkyl-amino, (Ci-8alkyl)2-amino, amino-Ci-8alkyl, Ci-salkyl-amino-Ci-salkyl, (Ci-8alkyl)2-amino-Ci-8alkyl,

amino-Ci-8alkyl-amino, Ci-salkyl-amino-Ci-salkyl-amino,

(Ci-8alkyl)2-amino-Ci-8alkyl-amino, Ci-salkoxy-Ci-salkyl-amino,

Ci-8alkyl-carbonyl-amino, Ci-salkoxy-carbonyl-amino, hydroxy-Ci-salkyl,

hydroxy-Ci-salkoxy-Ci-salkyl, hydroxy-Ci-salkyl-amino, (hydroxy-Ci-8alkyl)2-amino or (hydroxy-Ci-8alkyl)(Ci-8alkyl)amino.

In another aspect of the use of a compound of Formula (I), R ₃ is selected from cyano, halogen, hydroxy, oxo, Ci-salkyl, halo-Ci-salkyl, Ci-salkoxy, Ci-salkoxy-Ci-salkyl,

Ci-salkoxy-carbonyl, amino, Ci-salkyl-amino, (Ci-8alkyl)2-amino, amino-Ci-salkyl, Ci-8alkyl-amino-Ci-8alkyl, (Ci-8alkyl)2-amino-Ci-8alkyl, Ci-salkyl-amino-Ci-salkyl-amino, Ci-8alkoxy-Ci-8alkyl-amino, Ci-salkoxy-carbonyl-amino, hydroxy-Ci-salkyl,

hydroxy-Ci-salkoxy-Ci-salkyl, hydroxy-Ci-salkyl-amino, (hydroxy-Ci-8alkyl)2-amino or (hydroxy-Ci-8alkyl)(Ci-8alkyl)amino.

In one aspect of the use of a compound of Formula (I), R ₃ is Ci-salkyl selected from methyl, ethyl, propyl, isopropyl or tert-butyl.

In another aspect of the use of a compound of Formula (I), R ₃ is Ci-salkyl selected from ethyl, propyl, isopropyl or tert-butyl.

In one aspect of the use of a compound of Formula (I), R ₃ is halo-Ci-salkyl selected from

trihalo-methyl, dihalo-methyl, halo-methyl, trihalo-ethyl, dihalo-ethyl, halo-ethyl, trihalo-propyl, dihalo-propyl or halo-propyl; wherein, halo is selected from fluoro, chloro, bromo or iodo. In another aspect of the use of a compound of Formula (I), R ₃ is halo-Ci-salkyl selected from trihalo-methyl, dihalo-methyl, halo-methyl, trihalo-ethyl, dihalo-ethyl, trihalo-propyl or dihalo-propyl; wherein, halo is selected from fluoro, chloro, bromo or iodo.

In one aspect of the use of a compound of Formula (I), R ₃ is hydroxy-Ci-salkyl selected from

hydroxy-methyl, hydroxy-ethyl, hydroxy-propyl, dihydroxy-propyl, hydroxy-butyl or dihydroxy-butyl.

In another aspect of the use of a compound of Formula (I), R ₃ is hydroxy-Ci-salkyl selected from hydroxy-methyl, dihydroxy-propyl, hydroxy-butyl or dihydroxy-butyl.

In one aspect of the use of a compound of Formula (I), R ₃ is Ci-salkoxy selected from methoxy, ethoxy, propoxy or isopropoxy.

In one aspect of the use of a compound of Formula (I), R ₃ is halo-Ci-salkoxy selected from

trihalo-methoxy, dihalo-methoxy, halo-methoxy, trihalo-ethoxy, dihalo-ethoxy, halo-ethoxy, trihalo-propoxy, dihalo-propoxy or halo-propoxy; wherein, halo is selected from fluoro, chloro, bromo or iodo.

In one aspect of the use of a compound of Formula (I), R ₃ is Ci-salkoxy-carbonyl-amino selected from methoxy-carbonyl-amino, ethoxy-carbonyl-amino, propoxy-carbonyl-amino, isopropoxy-carbonyl -amino, tert-butoxy-carbonyl-amino.

In one aspect of the use of a compound of Formula (I), R ₄ is C _3- i4cycloalkyl selected from

cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; wherein, each instance of

C _3- i4cycloalkyl is optionally substituted with R ₅ substituents.

In another aspect of the use of a compound of Formula (I), R4 is C _3- 8cycloalkyl selected from

cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; wherein, each instance of

C _3- 8cycloalkyl is optionally substituted with R5 substituents.

In one aspect of the use of a compound of Formula (I), R4 is C _3- i4cycloalkyl-Ci-8alkyl, wherein

C _3- i4cycloalkyl is selected from cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; and, wherein, each instance of C _3- i4cycloalkyl is optionally substituted with

R5 substituents.

In another aspect of the use of a compound of Formula (I), R4 is C _3- 8cycloalkyl-Ci-8alkyl, wherein C _3- 8cycloalkyl is selected from cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; and, wherein, each instance of C _3- 8cycloalkyl is optionally substituted with R5 substituents. In one aspect of the use of a compound of Formula (I), R ₄ is C3-i4cycloalkyl -amino, wherein C3-i4cycloalkyl is selected from cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; and, wherein, each instance of C3-i4cycloalkyl is optionally substituted with R ₅ substituents.

In another aspect of the use of a compound of Formula (I), R4 is C3-8cycloalkyl-amino, wherein C3- ₈ cycloalkyl is selected from cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; and, wherein, each instance of C3- ₈ cycloalkyl is optionally substituted with R5 substituents.

In one aspect of the use of a compound of Formula (I), R4 is aryl-Ci _-8 alkyl,

aryl-Ci _-8 alkoxy-carbonyl or aryl-sulfonyloxy-Ci _-8 alkyl, wherein aryl is selected from phenyl; and, wherein, each instance of aryl is optionally substituted with R5 substituents.

In another aspect of the use of a compound of Formula (I), R4 is aryl-Ci _-8 alkyl or

aryl-Ci _-8 alkoxy-carbonyl, wherein each instance of aryl is optionally substituted with R5 substituents.

In one aspect of the use of a compound of Formula (I), R4 is heterocyclyl selected from oxetanyl, pyrrolidinyl, piped dinyl, piperazinyl, 1,3-dioxanyl or morpholinyl, wherein each instance of heterocyclyl is optionally substituted with R5 substituents.

In another aspect of the use of a compound of Formula (I), R4 is heterocyclyl selected from

oxetan-3-yl, pyrrolidin-l-yl, piperidin-l-yl, piperazin-l-yl, l,3-dioxan-5-yl or

morpholin-4-yl, wherein each instance of heterocyclyl is optionally substituted with R5 substituents.

In one aspect of the use of a compound of Formula (I), R4 is heterocyclyl-Ci _-8 alkyl, wherein each instance of heterocyclyl is selected from pyrrolidinyl or piperidinyl; and, wherein, each instance of heterocyclyl is optionally substituted with R5 substituents.

In another aspect of the use of a compound of Formula (I), R4 is heterocyclyl-Ci _-8 alkyl selected from pyrrolidin-l-yl-Ci _-8 alkyl or piperidin-l-yl-Ci _-8 alkyl, wherein each instance of heterocyclyl is optionally substituted with R5 substituents.

In one aspect of the use of a compound of Formula (I), R5 is selected from halogen, hydroxy, cyano, nitro, halo-Ci _-8 alkyl, Ci _-8 alkoxy, halo-Ci _-8 alkoxy, amino, Ci _-8 alkyl-amino,

(Ci _-8 alkyl)2-amino or Ci _-8 alkyl-thio; wherein, halogen and halo is selected from fluoro, chloro, bromo or iodo. In one aspect of the use of a compound of Formula (I), R5 is hydroxy.

In one aspect of the use of a compound of Formula (I), R5 is Ci-salkyl selected from methyl, ethyl, propyl, isopropyl, n-butyl or tert-butyl.

In another aspect of the use of a compound of Formula (I), R5 is Ci-salkyl selected from ethyl, propyl, isopropyl or tert-butyl.

In one aspect of the use of a compound of Formula (I), R ₅ is halo-Ci-salkyl selected from

trihalo-methyl, dihalo-methyl, halo-methyl, trihalo-ethyl, dihalo-ethyl, halo-ethyl, trihalo-propyl, dihalo-propyl or halo-propyl; wherein, halo is selected from fluoro, chloro, bromo or iodo.

In one aspect of the use of a compound of Formula (I), R ₅ is Ci-salkoxy selected from methoxy, ethoxy, propoxy or isopropoxy.

In one aspect of the use of a compound of Formula (I), R ₅ is halo-Ci-salkoxy selected from

trihalo-methoxy, dihalo-methoxy, halo-methoxy, trihalo-ethoxy, dihalo-ethoxy, halo-ethoxy, trihalo-propoxy, dihalo-propoxy or halo-propoxy; wherein, halo is selected from fluoro, chloro, bromo or iodo.

In one aspect of the use of a compound of Formula (I), R ₂ is aryl selected from phenyl optionally substituted with one, two or three R ₆ substituents and optionally, with one additional R ₇ substituent.

In one aspect of the use of a compound of Formula (I), R ₂ is aryl-amino, wherein aryl is selected from phenyl; and, wherein, each instance of aryl is optionally substituted with R ₆ and R ₇ substituents.

In another aspect of the use of a compound of Formula (I), R ₂ is aryl-amino selected from

phenyl-amino; wherein, each instance of aryl is optionally substituted with R ₆ and R ₇ substituents.

In one aspect of the use of a compound of Formula (I), R ₂ is aryl-amino-carbonyl, wherein aryl is selected from phenyl; and, wherein, each instance of aryl is optionally substituted with 5 and R ₇ substituents.

In another aspect of the use of a compound of Formula (I), R ₂ is aryl-amino-carbonyl selected from phenyl -amino-carbonyl; wherein, each instance of aryl is optionally substituted with R ₆ and R ₇ substituents. In one aspect of the use of a compound of Formula (I),

R ₂ is heterocyclyl selected from 1,2,3, 6-tetrahydropyridinyl, 1,3-benzodioxolyl or

2,3-dihydro-l,4-benzodioxinyl; wherein, each instance of heterocyclyl is optionally substituted with R6 and R ₇ substituents.

In another aspect of the use of a compound of Formula (I),

R ₂ is heterocyclyl selected from 1,2,3, 6-tetrahydropyridin-4-yl, l,3-benzodioxol-5-yl or

2,3-dihydro-l,4-benzodioxin-6-yl; wherein, each instance of heterocyclyl is optionally substituted with Rs and R ₇ substituents.

In one aspect of the use of a compound of Formula (I),

R ₂ is heteroaryl optionally substituted with one, two or three R ₆ substituents and optionally, with one additional R ₇ substituent.

In one aspect of the use of a compound of Formula (I),

R ₂ is heteroaryl selected from thienyl, lH-pyrazolyl, lH-imidazolyl, 1,3-thiazolyl,

1,2,4-oxadiazolyl, 1,3,4-oxadiazolyl, pyridinyl, pyrimidinyl, lH-indolyl, 2H-indolyl, lH-indazolyl, 2H-indazolyl, indolizinyl, benzofuranyl, benzothienyl, lH-benzimidazolyl, 1,3-benzothiazolyl, 1,3-benzoxazolyl, 9H-purinyl, quinazolinyl, quinoxalinyl, furo[3,2-£]pyridinyl, furo[3,2-c]pyridinyl, furo[2,3-c]pyridinyl, thieno[3,2-c]pyridinyl, thieno[2,3-<i]pyrimidinyl, lH-pyrrolo[2,3-£]pyridinyl, lH-pyrrolo[2,3-c]pyridinyl, pyrrolo[ 1 ,2-a]pyrimidinyl, pyrrolo[ 1 ,2-a]pyrazinyl, pyrrolo[ 1 ,2-£]pyridazinyl, pyrazolo[l,5-a]pyridinyl, pyrazolo[l,5-a]pyrazinyl, pyrazolo[4,3-b]pyridinyl, pyrazolo[3,4-c]pyridinyl, imidazo[l,2-a]pyridinyl, 3H-imidazo[4,5-£]pyridinyl, imidazo[ 1 ,2-a]pyrimidinyl, imidazo[ 1 ,2-c]pyrimidinyl, imidazo[ 1 ,2-£]pyridazinyl, imidazo[ 1 ,2-a]pyrazinyl, imidazo[2, 1 -b] [ 1 ,3 Jthiazolyl, imidazo[2, 1 -b] [ 1 ,3 ,4]thiadiazolyl, [l,3]oxazolo[4,5-£]pyridinyl, [l,2,4]triazolo[l,5-a]pyridinyl,

[ 1 ,2,4]triazolo[4,3 -ajpyridinyl, [ 1 ,2,4]triazolo[ 1 ,5-a]pyrimidinyl,

[l,2,4]triazolo[l,5-b]pyridazinyl, pyrido[l,2-a]pyrimidinyl or pyrido[l,2-a]pyrimidinone; wherein, each instance of heteroaryl is optionally substituted with one, two or three R ₆ substituents and optionally, with one additional R ₇ substituent.

In another aspect of the use of a compound of Formula (I),

R ₂ is heteroaryl selected from thien-2-yl, thien-3-yl, lH-pyrazol-3-yl, lH-pyrazol-4-yl,

lH-pyrazol-5-yl, lH-imidazol-l-yl, lH-imidazol-4-yl, l,3-thiazol-2-yl, l,2,4-oxadiazol-3-yl, l,3,4-oxadiazol-2-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyrimidin-4-yl, lH-indol-3-yl, lH-indol-4-yl, lH-indol-5-yl, lH-indol-6-yl,

lH-indazol-5-yl, 2H-indazol-5-yl, indolizin-2-yl, benzofuran-2-yl, benzofuran-5-yl, benzothien-2-yl, benzothien-3-yl, lH-benzimidazol-2-yl, lH-benzimidazol-6-yl, l,3-benzoxazol-2-yl, l,3-benzoxazol-5-yl, l,3-benzoxazol-6-yl, l,3-benzothiazol-2-yl, l,3-benzothiazol-5-yl, l,3-benzothiazol-6-yl, 9H-purin-8-yl, quinazolin-6-yl,

quinoxalin-2-yl, furo[3,2-£]pyridin-2-yl, furo[3,2-c]pyridin-2-yl, furo[2,3-c]pyridin-2-yl, thieno[3,2-c]pyridin-2-yl, thieno[2,3-<i]pyrimidin-6-yl, lH-pyrrolo[2,3-£]pyridin-5-yl, lH-pyrrolo[2,3 -c]pyridin-4-yl, pyrrolo[ 1 ,2-a]pyrimidin-7-yl, pyrrolo[ 1 ,2-a]pyrazin-7-yl, pyrrolo[l,2-£]pyridazin-2-yl, pyrazolo[l,5-a]pyridin-2-yl, pyrazolo[l,5-a]pyridin-5-yl, pyrazolo[l,5-a]pyrazin-2-yl, pyrazolo[4,3-b]pyridin-5-yl, pyrazolo[3,4-c]pyridin-5-yl, imidazo[ 1 ,2-a]pyridin-2-yl, imidazo[ 1 ,2-a]pyridin-6-yl, imidazo[ 1 ,2-a]pyrimidin-2-yl, imidazo[ 1 ,2-a]pyrimidin-6-yl, imidazo[ 1 ,2-c]pyrimidin-2-yl,

imidazo[ 1 ,2-£]pyridazin-2-yl, imidazo[ 1 ,2-£]pyridazin-6-yl, imidazo[ 1 ,2-a]pyrazin-2-yl, imidazo[2, 1 -b] [ 1 ,3 ]thiazol-6-yl, imidazo[2, 1 -b] [ 1 ,3 ,4]thiadiazol-6-yl,

[l,3]oxazolo[4,5-£]pyridin-2-yl, [l,2,4]triazolo[l,5-a]pyridin-6-yl,

[ 1 ,2,4]triazolo[ 1 ,5-a]pyrimidin-6-yl, [ 1 ,2,4]triazolo[ 1 ,5-b]pyridazin-6-yl,

pyrido[l,2-a]pyrimidin-4-yl or pyrido[l,2-a]pyrimidin-4-one; wherein, each instance of heteroaryl is optionally substituted with one, two or three R ₆ substituents and optionally, with one additional R ₇ substituent.

In another aspect of the use of a compound of Formula (I),

R.2 is substituted heteroaryl selected from 4-methylthien-2-yl, l-methyl-lH-pyrazol-3-yl,

4-methyl-lH-pyrazol-3-yl, l-phenyl-lH-pyrazol-3-yl,

1- (tetrahydro-2H-pyran-2-yl)-lH-pyrazol-4-yl, l-phenyl-lH-imidazol-4-yl,

2- methyl- 1 -(pyridin-2-yl)- lH-imidazol-4-yl, 4-methyl- 1 ,3 -thiazol-2-yl,

4- (trifluorom ethyl)- 1 ,3 -thiazol-2-yl, 4-phenyl- 1 ,3 -thiazol-2-yl,

5- phenyl-l,2,4-oxadiazol-3-yl, 3-fluoropyridin-4-yl, 6-fluoropyridin-2-yl,

2-chloropyridin-4-yl, 4-chloropyridin-3-yl, 5-chloropyridin-2-yl, 6-methylpyridin-3-yl, 2-(trifluoromethyl)pyridin-3-yl, 4-(trifluorom ethyl )pyridin-2-yl,

6- (trifluoromethyl)pyridin-2-yl, 2-methoxypyridin-4-yl, 4-methoxypyridin-3-yl, 6-methoxypyridin-2-yl, 2-ethoxypyridin-3-yl, 6-ethoxypyridin-2-yl, 6-(propan-2-yloxy)pyridin-2-yl, 6-(dimethylamino)pyridin-3-yl,

6-(methylsulfanyl)pyridin-2-yl, 6-(cyclobutyloxy)pyridin-2-yl,

6- (pyrrolidin-l-yl)pyridin-2-yl, (5-fluoro-6-hydroxy)pyridin-3-yl, 2-methylpyrimidin-4-yl, 2-(propan-2-yl)pyrimidin-4-yl, 2-cyclopropylpyrimidin-4-yl, 1 -methyl- lH-indol-3-yl, l,7-dimethyl-lH-indazol-5-yl, 2 -methyl -2H-indazol-5-yl, 2,7-dimethyl-2H-indazol-5-yl,

7- fluoro-2-methyl-2H-indazol-5-yl, 2-methyl-l-benzofuran-5-yl,

1 -methyl- lH-benzimidazol -2 -yl, 4-methyl-lH-benzimidazol-2-yl

5-fluoro-lH-benzimidazol-2-yl, 4-fluoro-l,3-benzoxazol-2-yl,

5- fluoro-l,3-benzoxazol-2-yl, 4-chloro-l,3-benzoxazol-2-yl, 4-iodo-l,3-benzoxazol-2-yl, 2-methyl- 1 ,3 -benzoxazol-6-yl, 4-methyl- 1 ,3 -benzoxazol-2-yl,

4-(trifluoromethyl)-l,3-benzoxazol-2-yl, 7-(trifluoromethyl)-l,3-benzoxazol-2-yl, 2-methyl- 1, 3 -benzothiazol-2-yl, 2-methyl-l,3-benzothiazol-5-yl,

2-methyl- 1 ,3 -benzothiazol-6-yl, 4-chloro- 1 ,3 -benzothiazol-2-yl,

7- chloro-l,3-benzothiazol-2-yl, 4-(trifluoromethyl)-l,3-benzothiazol-2-yl,

(4-hydroxy-2-methyl)quinazolin-6-yl, 5-methylfuro[3,2-£]pyridin-2-yl,

4,6-dimethylfuro[3,2-c]pyridin-2-yl, 5,7-dimethylfuro[2,3-c]pyridin-2-yl,

4,6-dimethylthieno[3,2-c]pyridin-2-yl, 2,4-dimethylthieno[2,3-<i]pyrimidin-6-yl,

1 -methylpyrrolo[ 1 ,2-a]pyrazin-7-yl, 3 -methylpyrrolo[ 1 ,2-a]pyrazin-7-yl,

1 ,3 -dimethylpyrrolo[ 1 ,2-a]pyrazin-7-yl, 2-m ethyl pyrrolo[ 1 ,2-£]pyridazin-2-yl,

2-methylpyrazolo[l,5-a]pyridin-5-yl, 5-methylpyrazolo[l,5-a]pyridin-2-yl,

4-(dimethylamino)-6-methylpyrazolo[l,5-a]pyrazin-2-yl,

4.6- dimethylpyrazolo[l,5-a]pyrazin-2-yl, 4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl,

1.7- dimethyl-lH-pyrazolo[4,3-b]pyridin-5-yl,

l,7-dimethyl-lH-pyrazolo[3,4-c]pyridin-5-yl,

2,7-dimethyl-2H-pyrazolo[3,4-c]pyridin-5-yl,

2,7-dimethyl-2H-pyrazolo[4,3-b]pyridin-5-yl, 2-chloroimidazo[2, l-£][l,3]thiazol-6-yl, 2-methylimidazo[2, l-£][l,3]thiazol-6-yl, 3-methylimidazo[2, l-£][l,3]thiazol-6-yl, 2-ethylimidazo[2, 1 -b] [ 1 ,3 ]thiazol-6-yl, 2-methylimidazo[2, 1 -b] [ 1 ,3 ,4]thiadiazol-6-yl,

6- cyanoimidazo[l,2-a]pyridin-2-yl (also referred to as

2-imidazo[ 1 ,2-a]pyridine-6-carbonitrile), 6-fluoroimidazo[ 1 ,2-a]pyridin-2-yl,

8- fluoroimidazo[l,2-a]pyridin-2-yl, 6,8-difluoroimidazo[l,2-a]pyridin-2-yl, - (trifluoromethyl)imidazo[ 1 ,2-a]pyridin-2-yl,

- (trifluoromethyl)imidazo[ 1 ,2-a]pyridin-2-yl, 6-chloroimidazo[ 1 ,2-a]pyridin-2-yl,- chloroimidazo[ 1 ,2-a]pyridin-2-yl, 8-chloroimidazo[ 1 ,2-a]pyridin-2-yl,

- bromoimidazo[ 1 ,2-a]pyridin-2-yl, 2-methylimidazo[ 1 ,2-a]pyridin-2-yl,

- methylimidazo[ 1 ,2-a]pyridin-2-yl, 6-methylimidazo[ 1 ,2-a]pyridin-2-yl,

-methylimidazo[ 1 ,2-a]pyridin-2-yl, 8-methylimidazo[ 1 ,2-a]pyridin-2-yl,

-ethylimidazo[ 1 ,2-a]pyridin-2-yl, 8-ethylimidazo[ 1 ,2-a]pyridin-2-yl,

, 8-dimethylimidazo[ 1 ,2-a]pyridin-2-yl, 8-ethyl-6-methylimidazo[ 1 ,2-a]pyridin-2-yl,- methoxyimidazo[ 1 ,2-a]pyridin-2-yl, 8-methoxyimidazo[ 1 ,2-a]pyridin-2-yl,

- fluoro-8-methylimidazo[ 1 ,2-a]pyridin-2-yl,

- fluoro-6-methylimidazo[ 1 ,2-a]pyridin-2-yl,

-chloro-6-methylimidazo[ 1 ,2-a]pyridin-2-yl, 6-methyl-8-nitroimidazo[ 1 ,2-a]pyridin-2-yl,-cyclopropylimidazo[ 1 ,2-a]pyridin-2-yl, 2-methylimidazo[ 1 ,2-a]pyridin-6-yl,

-ethylimidazo[ 1 ,2-a]pyridin-6-yl, 2,3 -dimethylimidazo[ 1 ,2-a]pyridin-6-yl,

, 8-dimethylimidazo[ 1 ,2-a]pyridin-6-yl, 2-(trifluorom ethyl )imidazo[ 1 ,2-a]pyridin-6-yl,-chloro-2-methylimidazo[ 1 ,2-a]pyridin-6-yl,

-fluoro-2-methylimidazo[ 1 ,2-a]pyridin-6-yl, 6-fluoroimidazo[ 1 ,2-a]pyrimidin-2-yl,- chloroimidazo[ 1 ,2-a]pyrimidin-2-yl, 6-methylimidazo[ 1 ,2-a]pyrimidin-2-yl,

- methylimidazo[ 1 ,2-a]pyrimidin-2-yl, 2-methylimidazo[ 1 ,2-a]pyrimidin-6-yl,

-methylimidazo[ 1 ,2-£]pyridazin-2-yl, 2-methylimidazo[ 1 ,2- ]pyridazin-6-yl,

- methyl-3-(l,2,3,6-tetrahydropyridin-4-yl)imidazo[l,2-^]pyrid azin-6-yl,

-methylimidazo[ 1 ,2-a]pyrazin-2-yl, 8-methylimidazo[ 1 ,2-a]pyrazin-2-yl,

,8-dimethylimidazo[l,2-a]pyrazin-2-yl, 6-chloro-8-methylimidazo[l,2-a]pyrazin-2-yl,-methyl-8-(trifl uoromethyl)imidazo[ 1 ,2-a]pyrazin-2-yl,

- (methylsulfanyl)imidazo[ 1 ,2-a]pyrazin-2-yl, 2-methylimidazo[2, 1 -b] [ 1 ,3 ]thiazol-6-yl,- methylimidazo[2, l- ][l,3]thiazol-6-yl, 2-methylimidazo[2, l- ][l,3,4]thiadiazol-6-yl,-methyl-[l,2,4]triazolo[l,5-a]pyridi n-6-yl, 2-methyl-[l,2,4]triazolo[l,5-a]pyrimidin-6-yl,-methyl-[l,2,4 ]triazolo[l,5-b]pyridazin-6-yl or

H,4'H-2,7'-bipyrido[l,2-a]pyrimidine-4,4'-dione. In another aspect of the use of a compound of Formula (I),

R ₂ is heteroaryl selected from thienyl, lH-pyrazolyl, lH-imidazolyl, 1,3-thiazolyl,

1,2,4-oxadiazolyl, 1,3,4-oxadiazolyl, pyridinyl, pyrimidinyl, lH-indolyl, 2H-indolyl, lH-indazolyl, 2H-indazolyl, indolizinyl, benzofuranyl, benzothienyl, lH-benzimidazolyl, 1,3-benzothiazolyl, 1,3-benzoxazolyl, 9H-purinyl, quinazolinyl or quinoxalinyl; wherein, each instance of heteroaryl is optionally substituted with one, two or three R ₆ substituents and optionally, with one additional R ₇ substituent.

In another aspect of the use of a compound of Formula (I),

R ₂ is heteroaryl selected from furo[3,2-£]pyridinyl, furo[3,2-c]pyridinyl, furo[2,3-c]pyridinyl, thieno[3,2-c]pyridinyl, thieno[2,3 -^pyrimidinyl, lH-pyrrolo[2,3-£]pyridinyl,

lH-pyrrolo[2,3 -cjpyridinyl, pyrrolo[ 1 ,2-a]pyrimidinyl, pyrrolo[ 1 ,2-a]pyrazinyl, pyrrolo[ 1 ,2-£]pyridazinyl, pyrazolo[ 1 ,5-a]pyridinyl, pyrazolo[ 1 , 5-a]pyrazinyl, pyrazolo[4,3-b]pyridinyl, pyrazolo[3,4-c]pyridinyl, imidazo[l,2-a]pyridinyl,

3H-imidazo[4,5-£]pyridinyl, imidazo[ 1 ,2-a]pyrimidinyl, imidazo[ 1 ,2-c]pyrimidinyl, imidazo[ 1 ,2-£]pyridazinyl, imidazo[ 1 ,2-a]pyrazinyl, imidazo[2, 1 -b] [ 1 ,3]thiazolyl, imidazo[2,l-£][l,3,4]thiadiazolyl, [l,3]oxazolo[4,5-^]pyridinyl,

[ 1 ,2,4]triazolo[ 1 ,5-a]pyridinyl, [ 1 ,2,4]triazolo[4,3 -ajpyridinyl,

[ 1 ,2,4]triazolo[ 1 ,5-a]pyrimidinyl, [ 1 ,2,4]triazolo[ 1 , 5-b]pyridazinyl,

pyrido[l,2-a]pyrimidinyl or pyrido[l,2-a]pyrimidinone; wherein, each instance of heteroaryl is optionally substituted with one, two or three R ₆ substituents and optionally, with one additional R ₇ substituent.

In one aspect of the use of a compound of Formula (I), R ₂ is heteroaryl-amino, wherein heteroaryl is selected from pyridinyl or pyrimidinyl; and, wherein, each instance of heteroaryl is optionally substituted with R ₆ and R ₇ substituents.

In another aspect of the use of a compound of Formula (I), R ₂ is heteroaryl-amino selected from pyridin-2-yl -amino, pyridin-3-yl-amino or pyrimidin-2-yl-amino; wherein, each instance of heteroaryl is optionally substituted with R ₆ and R ₇ substituents.

In one aspect of the use of a compound of Formula (I), R ₆ is selected from halogen, hydroxy, cyano, nitro, Ci-salkyl, halo-Ci-salkyl, hydroxy-Ci-salkyl, Ci-salkoxy, halo-Ci-salkoxy, Ci-salkoxy-Ci-salkyl, (Ci-8alkyl) ₂ -amino or Ci-salkyl-thio; wherein, halogen and halo is selected from fluoro, chloro, bromo or iodo. In one aspect of the use of a compound of Formula (I), R ₆ is Ci-salkyl selected from methyl, ethyl, propyl, isopropyl or tert-butyl.

In another aspect of the use of a compound of Formula (I), R ₆ is Ci-salkyl selected from ethyl, propyl, isopropyl or tert-butyl.

In one aspect of the use of a compound of Formula (I), R ₆ is C ₂ -8alkenyl selected from ethenyl, allyl or buta-l,3-dienyl.

In another aspect of the use of a compound of Formula (I), R ₆ is C _2- 8alkenyl selected from ethenyl or allyl.

In one aspect of the use of a compound of Formula (I), R ₆ is halo-Ci-salkyl selected from

trihalo-methyl, dihalo-methyl, halo-methyl, trihalo-ethyl, dihalo-ethyl, halo-ethyl, trihalo-propyl, dihalo-propyl or halo-propyl; wherein, halo is selected from fluoro, chloro, bromo or iodo.

In one aspect of the use of a compound of Formula (I), R ₆ is hydroxy-Ci-salkyl selected from

hydroxy-methyl, hydroxy-ethyl, hydroxy-propyl, dihydroxy-propyl, hydroxy-butyl or dihydroxy-butyl.

In another aspect of the use of a compound of Formula (I), R ₆ is hydroxy-Ci-salkyl selected from hydroxy-methyl, dihydroxy-propyl, hydroxy-butyl or dihydroxy-butyl.

In one aspect of the use of a compound of Formula (I), R ₆ is Ci-salkoxy selected from methoxy, ethoxy, propoxy or isopropoxy.

In one aspect of the use of a compound of Formula (I), R ₆ is halo-Ci-salkoxy selected from

trihalo-methoxy, dihalo-methoxy, halo-methoxy, trihalo-ethoxy, dihalo-ethoxy, halo-ethoxy, trihalo-propoxy, dihalo-propoxy or halo-propoxy; wherein, halo is selected from fluoro, chloro, bromo or iodo.

In one aspect of the use of a compound of Formula (I), R ₇ is C3-i4cycloalkyl, C3-i4cycloalkyl-oxy, aryl, heterocyclyl or heteroaryl; wherein C3-i4cycloalkyl is selected from cyclopropyl or cyclobutoxy; wherein aryl is selected from phenyl; wherein heterocyclyl is selected from oxetanyl, pyrrolidinyl or 1,2,3,6-tetrahydropyridinyl; and, wherein heteroaryl is selected from thienyl or pyridinyl.

In another aspect of the use of a compound of Formula (I), R ₇ is C3-i4cycloalkyl or

C3-i4cycloalkyl-oxy, wherein each instance of C3-i4cycloalkyl is selected from

cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl. In another aspect of the use of a compound of Formula (I), R ₇ is C3-8cycloalkyl or

C3-8cycloalkyl-oxy, wherein each instance of C3-8cycloalkyl is selected from cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl.

In one aspect of the use of a compound of Formula (I), R ₇ is aryl selected from phenyl.

In one aspect of the use of a compound of Formula (I), R ₇ is heterocyclyl selected from oxetanyl, pyrrolidinyl or 1,2,3, 6-tetrahydropyridinyl.

In another aspect of the use of a compound of Formula (I), R ₇ is heterocyclyl selected from

oxetan-3-yl, pyrrolidin-l-yl or l,2,3,6-tetrahydropyridin-4-yl.

In one aspect of the use of a compound of Formula (I), R ₇ is heteroaryl selected from thienyl or pyridinyl.

In another aspect of the use of a compound of Formula (I), R ₇ is heteroaryl selected from

pyridinyl.

In one aspect of the use of a compound of Formula (I), R ₇ is heteroaryl selected from thien-2-yl or pyridin-2-yl.

In another aspect of the use of a compound of Formula (I), R ₇ is heteroaryl selected from

pyridin-2-yl.

In one aspect of the use of a compound of Formula (I), R _c is hydrogen or Ci-salkyl.

In another aspect of the use of a compound of Formula (I),

Ri is heterocyclyl, heterocyclyl-Ci-salkyl, heterocyclyl-Ci-salkoxy, heterocyclyl-amino,

(heterocyclyl)(Ci-8alkyl)amino, heterocyclyl -amino-Ci-salkyl,

heterocyclyl-Ci-8alkyl-amino, (heterocyclyl -Ci-8alkyl)2-amino,

(heterocyclyl-Ci-8alkyl)(Ci-8alkyl)amino, heterocyclyl -Ci-salkyl-amino-Ci-salkyl,

(heterocyclyl-Ci-8alkyl)2-amino-Ci-8alkyl,

(heterocyclyl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, heterocyclyl-oxy,

heterocyclyl-carbonyl, heterocyclyl-carbonyl-oxy, C3-i4cycloalkyl, aryl-Ci-salkyl-amino, (aryl-Ci-8alkyl)2-amino, (aryl-Ci-8alkyl)(Ci-8alkyl)amino, aryl-Ci-salkyl-amino-Ci-salkyl, (aryl-Ci-8alkyl)2-amino-Ci-8alkyl, (aryl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, heteroaryl, heteroaryl -Ci-salkyl, heteroaryl-Ci-salkoxy, heteroaryl -amino, heteroaryl-Ci-salkyl-amino, (heteroaryl-Ci-8alkyl)2-amino, (heteroaryl-Ci-8alkyl)(Ci-8alkyl)amino,

heteroaryl -Ci-8alkyl-amino-Ci-8alkyl, (heteroaryl-Ci-8alkyl)2-amino-Ci-8alkyl or

(heteroaryl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl; wherein, each instance of heterocyclyl, C3-i4cycloalkyl, aryl and heteroaryl is optionally substituted with R ₃ and R ₄ substituents; and,

wherein, heterocyclyl is selected from azetidinyl, tetrahydrofuranyl, pyrrolidinyl, piperidinyl, piperazinyl, 1,4-diazepanyl, 3,6-dihydropyridinyl, 1,2,5,6-tetrahydropyridinyl,

1,2,3,6-tetrahydropyridinyl, hexahydropyrrolo[3,4-£]pyirol-(lH)-yl,

(3a,S',6a ₎ S)-hexahydropyrrolo[3,4-^]pyrrol-(lH)-yl,

(3aR,6aR)-hexahydropyrrolo[3,4-£]pyrrol-(lH)-yl,

hexahydropyrrolo[3,4-£]pyrrol-(2H)-yl, (3a,S',6a ₎ S)-hexahydropyrrolo[3,4-^]pyrrol-(2H)-yl, hexahydropyrrolo[3,4-c]pyrrol-(lH)-yl, (3aR,6a,S)-hexahydropyrrolo[3,4-c]pyrrol-(lH)-yl, octahydro-5H-pyrrolo[3,2-c]pyridinyl, octahydro-6H-pyrrolo[3,4-£]pyridinyl,

(4aR,7aR)-octahydro-6H-pyirolo[3,4-£]pyridinyl,

(4a,S',7a ₎ S)-octahydro-6H-pyrrolo[3,4-^]pyridinyl,

hexahydropyrrolo[ 1 ,2-a]pyrazin-(2H)-one, hexahydropyrrolo[ 1 ,2-a]pyrazin-( lH)-yl,

(7R, 8 a^-hexahy dropyrrol o [ 1 , 2-a] pyrazin-( lH)-yl ,

(8a,S)-hexahydropyrrolo[l,2-a]pyrazin-(lH)-yl,

(8aR)-hexahydropyrrolo[l,2-a]pyrazin-(lH)-yl,

(8a,S)-3,4,6,7,8,8a-hexahydro-lH-pyrrolo[l,2-a]pyrazinyl,

(8aR)-3, 4,6,7,8, 8a-hexahydro-lH-pyrrolo[l,2-a]pyrazinyl,

(8a,S)-l,3,4,6,7,8-hexahydropyrrolo[l,2-a]pyrazinyl,

(8aR)-l,3,4,6,7,8-hexahydropyrrolo[l,2-a]pyrazinyl,

(8a,S)-octahydropyrrolo[l,2-a]pyrazin-(lH)-yl,

(8aR)-octahydropyrrolo[ 1 ,2-a]pyrazin-(lH)-yl, octahydro-2H-pyrido[ 1 ,2-a]pyrazinyl, (3aR,4aR,7aS)-hexahydro-lH-cyclobuta[l,2-c: l,4-c']dipyrrol-(3H)-yl,

3-azabicyclo[3.1.0]hexyl, (li?,5,S)-3-azabicyclo[3.1.0]hexyl, 8-azabicyclo[3.2.1]octyl, (lR,55)-8-azabicyclo[3.2.1]octyl, 8-azabicyclo[3.2.1]oct-2-enyl,

(li?,5,S)-8-azabicyclo[3.2.1]oct-2-enyl, 9-azabicyclo[3.3.1]nonyl,

(li?,5,S)-9-azabicyclo[3.3.1]nonyl, 2,5-diazabicyclo[2.2.1]heptyl,

(l,S 4,S 2,5-diazabicyclo[2.2.1]heptyl, 2,5-diazabicyclo[2.2.2]octyl,

3,6-diazabicyclo[3.2.0]hept-3-yl, 3,8-diazabicyclo[3.2.1]octyl,

(li?,5,S)-3,8-diazabicyclo[3.2.1]octyl, l,4-diazabicyclo[3.2.2]nonyl, azaspiro[3.3]heptyl, 2,6-diazaspiro[3.3]heptyl, 4,7-diazaspiro[2.5]oct-7-yl, 2,6-diazaspiro[3.4]oct-2-yl, 2,7-diazaspiro[3.5]nonyl, 5,8-diazaspiro[3.5]nonyl, 2,7-diazaspiro[4.4]nonyl or

6, 9-diazaspiro[4.5 ] decyl .

In another aspect of the use of a compound of Formula (I),

R.2 is aryl, aryl-amino, aryl-amino-carbonyl, heterocyclyl, heteroaryl or heteroaryl-amino;

wherein, aryl is phenyl;

wherein, heterocyclyl is selected from 1,2,3,6-tetrahydropyridinyl, 1,3-benzodioxolyl or

2,3-dihydro-l,4-benzodioxinyl;

wherein, heteroaryl is selected from thienyl, lH-pyrazolyl, lH-imidazolyl, 1,3-thiazolyl,

1,2,4-oxadiazolyl, 1,3,4-oxadiazolyl, pyridinyl, pyrimidinyl, lH-indolyl, 2H-indolyl, lH-indazolyl, 2H-indazolyl, indolizinyl, benzofuranyl, benzothienyl, lH-benzimidazolyl, 1,3-benzothiazolyl, 1,3-benzoxazolyl, 9H-purinyl, quinazolinyl, quinoxalinyl, furo[3,2-£]pyridinyl, furo[3,2-c]pyridinyl, furo[2,3-c]pyridinyl, thieno[3,2-c]pyridinyl, thieno[2,3 -^pyrimidinyl, lH-pyrrolo[2,3-£]pyridinyl, lH-pyrrolo[2,3-c]pyridinyl, pyrrolo[ 1 ,2-a]pyrimidinyl, pyrrolo[ 1 ,2-a]pyrazinyl, pyrrolo[ 1 ,2-£]pyridazinyl, pyrazolo[l,5-a]pyridinyl, pyrazolo[l,5-a]pyrazinyl, pyrazolo[4,3-b]pyridinyl, pyrazolo[3 ,4-c]pyridinyl, imidazo[ 1 ,2-a]pyridinyl, imidazo[ 1 ,2-a]pyrimidinyl, imidazo[ 1 ,2-c]pyrimidinyl, imidazo[ 1 ,2- )]pyridazinyl, imidazo[ 1 ,2-a]pyrazinyl, imidazo[2, 1 -b] [ 1 ,3 Jthiazolyl, imidazo[2, 1 -b] [ 1 ,3 ,4]thiadiazolyl,

[l,3]oxazolo[4,5-£]pyridinyl, [l,2,4]triazolo[l,5-a]pyridinyl,

[ 1 ,2,4]triazolo[ 1 ,5-a]pyrimidinyl, [ 1 ,2,4]triazolo[ 1 , 5-b]pyridazinyl,

pyrido[l,2-a]pyrimidinyl or pyrido[l,2-a]pyrimidinone; and, wherein, each instance of aryl, heterocyclyl and heteroaryl is optionally substituted with R6 and R ₇ substituents.

In another aspect of the use of a compound of Formula (I),

Ri is heterocyclyl, heterocyclyl-Ci-salkyl, heterocyclyl-Ci-salkoxy, heterocyclyl-amino,

(heterocyclyl)(Ci-8alkyl)amino, heterocyclyl -amino-Ci-salkyl,

heterocyclyl-Ci-8alkyl-amino, (heterocyclyl -Ci-8alkyl)2-amino,

(heterocyclyl-Ci-8alkyl)(Ci-8alkyl)amino, heterocyclyl -Ci-salkyl-amino-Ci-salkyl, (heterocyclyl-Ci-8alkyl)2-amino-Ci-8alkyl,

(heterocyclyl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, heterocyclyl-oxy,

heterocyclyl-carbonyl, heterocyclyl-carbonyl-oxy, C3-i4cycloalkyl, aryl-Ci-salkyl-amino, (aryl-Ci-8alkyl)2-amino, (aryl-Ci-8alkyl)(Ci-8alkyl)amino, aryl-Ci-salkyl-amino-Ci-salkyl, (aryl-Ci-8alkyl)2-amino-Ci-8alkyl, (aryl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, heteroaryl, heteroaryl-Ci-8alkyl, heteroaryl-Ci-salkoxy, heteroaryl -amino, heteroaryl-Ci-salkyl-amino, (heteroaryl-Ci-8alkyl)2-amino, (heteroaryl-Ci-8alkyl)(Ci-8alkyl)amino,

heteroaryl -Ci-8alkyl-amino-Ci-8alkyl, (heteroaryl-Ci-8alkyl)2-amino-Ci-8alkyl or

(heteroaryl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl;

wherein, heterocyclyl is selected from azetidinyl, tetrahydrofuranyl, pyrrolidinyl, piperidinyl, piperazinyl, 1,4-diazepanyl, 3,6-dihydropyridinyl, 1,2,5,6-tetrahydropyridinyl,

1,2,3,6-tetrahydropyridinyl, hexahydropyrrolo[3,4-£]pyirol-(lH)-yl,

(3a,S',6a ₎ S)-hexahydropyrrolo[3,4-^]pyrrol-(lH)-yl,

(3aR,6aR)-hexahydropyrrolo[3,4-£]pyrrol-(lH)-yl,

hexahydropyrrolo[3,4-£]pyrrol-(2H)-yl, (3a,S',6a ₎ S)-hexahydropyrrolo[3,4-^]pyrrol-(2H)-yl, hexahydropyrrolo[3,4-c]pyrrol-(lH)-yl, l,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrolyl, (3aR,6a,S)-hexahydropyrrolo[3,4-c]pyrrol-(lH)-yl, octahydro-5H-pyrrolo[3,2-c]pyridinyl, octahydro-6H-pyrrolo[3,4-£]pyridinyl, (4aR,7aR)-octahydro-6H-pyirolo[3,4-£]pyridinyl, (4a,S',7a ₎ S)-octahydro-6H-pyrrolo[3,4-^]pyridinyl,

hexahydropyrrolo[ 1 ,2-a]pyrazin-(2H)-one, hexahydropyrrolo[ 1 ,2-a]pyrazin-( lH)-yl,

(7R, 8 a^-hexahy dropyrrol o [ 1 , 2-a] pyrazin-( lH)-yl ,

(8a,S)-hexahydropyrrolo[l,2-a]pyrazin-(lH)-yl,

(8aR)-hexahydropyrrolo[l,2-a]pyrazin-(lH)-yl,

(8a,S)-3,4,6,7,8,8a-hexahydro-lH-pyrrolo[l,2-a]pyrazinyl,

(8aR)-3, 4,6,7,8, 8a-hexahydro-lH-pyrrolo[l,2-a]pyrazinyl,

(8a,S)-l,3,4,6,7,8-hexahydropyrrolo[l,2-a]pyrazinyl,

(8aR)-l,3,4,6,7,8-hexahydropyrrolo[l,2-a]pyrazinyl,

(8a,S)-octahydropyrrolo[l,2-a]pyrazin-(lH)-yl,

(8aR)-octahydropyrrolo[ 1 ,2-a]pyrazin-(lH)-yl, octahydro-2H-pyrido[ 1 ,2-a]pyrazinyl, (3aR,4aR,7aS)-hexahydro-lH-cyclobuta[l,2-c: l,4-c']dipyrrol-(3H)-yl,

3-azabicyclo[3.1.0]hexyl, (li?,5,S)-3-azabicyclo[3.1.0]hexyl, 8-azabicyclo[3.2.1]octyl, (lR,55)-8-azabicyclo[3.2.1]octyl, 8-azabicyclo[3.2.1]oct-2-enyl,

(li?,5,S)-8-azabicyclo[3.2.1]oct-2-enyl, 9-azabicyclo[3.3.1]nonyl,

(li?,5,S)-9-azabicyclo[3.3.1]nonyl, 2,5-diazabicyclo[2.2.1]heptyl,

(l-S'^^^^-diazabicycloP^. ^heptyl, 2,5-diazabicyclo[2.2.2]octyl, 3,6-diazabicyclo[3.2.0]heptyl, 3,8-diazabicyclo[3.2.1]octyl,

(lR,5,S)-3,8-diazabicyclo[3.2.1]octyl, l,4-diazabicyclo[3.2.2]nonyl, azaspiro[3.3]heptyl,

2.6- diazaspiro[3.3]heptyl, 4,7-diazaspiro[2.5]octyl, 2,6-diazaspiro[3.4]octyl,

2.7- diazaspiro[3.5]nonyl, 5,8-diazaspiro[3.5]nonyl, 2,7-diazaspiro[4.4]nonyl or

6,9-diazaspiro[4.5]decyl; and, wherein, each instance of heterocyclyl, C3-i4cycloalkyl, aryl and heteroaryl is optionally substituted with R ₃ and R ₄ substituents; and

R ₂ is aryl, aryl-amino, aryl-amino-carbonyl, heterocyclyl, heteroaryl or heteroaryl-amino;

wherein, heterocyclyl is selected from l,2,3,6-tetrahydropyridin-4-yl, l,3-benzodioxol-5-yl or 2,3-dihydro-l,4-benzodioxin-6-yl;

wherein, heteroaryl is selected from thienyl, lH-pyrazolyl, lH-imidazolyl, 1,3-thiazolyl,

1,2,4-oxadiazolyl, 1,3,4-oxadiazolyl, pyridinyl, pyrimidinyl, lH-indolyl, 2H-indolyl, lH-indazolyl, 2H-indazolyl, indolizinyl, benzofuranyl, benzothienyl, lH-benzimidazolyl, 1,3-benzothiazolyl, 1,3-benzoxazolyl, 9H-purinyl, quinazolinyl, quinoxalinyl,

furo[3,2-£]pyridinyl, furo[3,2-c]pyridinyl, furo[2,3-c]pyridinyl, thieno[3,2-c]pyridinyl, thieno[2,3-<i]pyrimidinyl, lH-pyrrolo[2,3-£]pyridinyl, lH-pyrrolo[2,3-c]pyridinyl, pyrrolo[ 1 ,2-a]pyrimidinyl, pyrrolo[ 1 ,2-a]pyrazinyl, pyrrolo[ 1 ,2-£]pyridazinyl, pyrazolo[l,5-a]pyridinyl, pyrazolo[l,5-a]pyrazinyl, pyrazolo[4,3-b]pyridinyl,

pyrazolo[3,4-c]pyridinyl, imidazo[l,2-a]pyridinyl, 3H-imidazo[4,5- )]pyridinyl, imidazo[ 1 ,2-a]pyrimidinyl, imidazo[ 1 ,2-c]pyrimidinyl, imidazo[ 1 ,2- )]pyridazinyl, imidazo[ 1 ,2-a]pyrazinyl, imidazo[2, 1 -b] [ 1 ,3 Jthiazolyl, imidazo[2, 1 -b] [ 1 ,3 ,4]thiadiazolyl, [l,3]oxazolo[4,5-£]pyridinyl, [l,2,4]triazolo[l,5-a]pyridinyl,

[ 1 ,2,4]triazolo[4,3 -ajpyridinyl, [ 1 ,2,4]triazolo[ 1 ,5-a]pyrimidinyl,

[l,2,4]triazolo[l,5-b]pyridazinyl, pyrido[l,2-a]pyrimidinyl or pyrido[l,2-a]pyrimidinone; and, wherein, each instance of heterocyclyl and heteroaryl is optionally substituted with R ₆ and R ₇ substituents.

In another aspect of the use of a compound of Formula (I),

Ri is Ci-8alkyl, amino, Ci-salkyl-amino, (Ci-8alkyl) ₂ -amino, Ci-salkoxy-Ci-salkyl-amino,

(Ci-8alkoxy-Ci-8alkyl) ₂ -amino, (Ci-8alkoxy-Ci-8alkyl)(Ci-8alkyl)amino, amino-Ci-salkyl, Ci-8alkyl-amino-Ci-8alkyl, (Ci-8alkyl) ₂ -amino-Ci-8alkyl,

Ci-salkoxy-Ci-salkyl-amino-Ci-salkyl, (Ci-8alkoxy-Ci-8alkyl) ₂ -amino-Ci-8alkyl,

(Ci-8alkoxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, amino-Ci-salkyl -amino, (amino-Ci-8alkyl)2-amino, (amino-Ci-8alkyl)(Ci-8alkyl)amino,

Ci-8alkyl-amino-Ci-8alkyl-amino, (Ci-8alkyl-amino-Ci-8alkyl)2-amino,

(Ci-8alkyl-amino-Ci-8alkyl)(Ci-8alkyl)amino, (Ci-8alkyl)2-amino-Ci-8alkyl-amino,

[(Ci-8alkyl)2-amino-Ci-8alkyl](Ci-8alkyl)amino, amino-Ci-salkoxy,

Ci-8alkyl-amino-Ci-8alkoxy, (Ci-8alkyl)2-amino-Ci-8alkoxy,

Ci-salkoxy-Ci-salkyl-amino-Ci-salkoxy, (Ci-8alkoxy-Ci-8alkyl)2-amino-Ci-8alkoxy, (Ci-8alkoxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkoxy, amino-C2-8alkenyl,

Ci-8alkyl-amino-C2-8alkenyl, (Ci-8alkyl)2-amino-C2-8alkenyl, amino-C2-8alkynyl, Ci-8alkyl-amino-C2-8alkynyl, (Ci-8alkyl)2-amino-C2-8alkynyl, halo-Ci-salkyl -amino, (halo-Ci-8alkyl)2-amino, (halo-Ci-8alkyl)(Ci-8alkyl)amino, hydroxy-Ci-salkyl, hydroxy-Ci-8alkoxy-Ci-8alkyl, hydroxy-Ci-salkyl-amino, (hydroxy-Ci-8alkyl)2-amino, (hydroxy-Ci-8alkyl)(Ci-8alkyl)amino, hydroxy-Ci-salkyl-amino-Ci-salkyl,

(hydroxy-Ci-8alkyl)2-amino-Ci-8alkyl, (hydroxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, hydroxy-Ci-8alkyl-amino-Ci-8alkoxy, (hydroxy-Ci-8alkyl)2-amino-Ci-8alkoxy,

(hydroxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkoxy,

hydroxy-Ci-8alkyl-amino-Ci-8alkyl-amino, (hydroxy-Ci-8alkyl-amino-Ci-8alkyl)2-amino,

(hydroxy-Ci-8alkyl)2-amino-Ci-8alkyl-amino,

(hydroxy-Ci-8alkyl-amino-Ci-8alkyl)(Ci-8alkyl)amino,

(hydroxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl-amino,

[(hydroxy-Ci-8alkyl)2-amino-Ci-8alkyl](Ci-8alkyl)amino or

[(hydroxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl](Ci-8alkyl)am ino; and

R.2 is aryl, aryl-amino, aryl-amino-carbonyl, heterocyclyl, heteroaryl or heteroaryl-amino,

wherein, each instance of aryl, heterocyclyl and heteroaryl is optionally substituted with

R.6 and R ₇ substituents.

In another aspect of the use of a compound of Formula (I),

Ri is heterocyclyl, heterocyclyl-Ci-salkyl, heterocyclyl-Ci-salkoxy, heterocyclyl-amino,

(heterocyclyl)(Ci-8alkyl)amino, heterocyclyl -amino-Ci-salkyl,

heterocyclyl-Ci-8alkyl-amino, (heterocyclyl -Ci-8alkyl)2-amino,

(heterocyclyl-Ci-8alkyl)(Ci-8alkyl)amino, heterocyclyl -Ci-salkyl-amino-Ci-salkyl, (heterocyclyl-Ci-8alkyl)2-amino-Ci-8alkyl,

(heterocyclyl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, heterocyclyl-oxy, heterocyclyl-carbonyl, heterocyclyl-carbonyl-oxy, C3-i4cycloalkyl, aryl-Ci-salkyl-amino, (aryl-Ci-8alkyl)2-amino, (aryl-Ci-8alkyl)(Ci-8alkyl)amino, aryl-Ci-salkyl-amino-Ci-salkyl, (aryl-Ci-8alkyl)2-amino-Ci-8alkyl, (aryl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, heteroaryl, heteroaryl-Ci-salkyl, heteroaryl-Ci-salkoxy, heteroaryl -amino, heteroaryl-Ci-salkyl-amino, (heteroaryl-Ci-8alkyl)2-amino, (heteroaryl-Ci-8alkyl)(Ci-8alkyl)amino,

heteroaryl -Ci-8alkyl-amino-Ci-8alkyl, (heteroaryl-Ci-8alkyl)2-amino-Ci-8alkyl or

(heteroaryl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl; wherein, each instance of heterocyclyl, C3-i4cycloalkyl, aryl and heteroaryl is optionally substituted with R3 and R4 substituents; and

R2 is aryl, aryl-amino, aryl-amino-carbonyl, heterocyclyl, heteroaryl or heteroaryl-amino,

wherein, each instance of aryl, heterocyclyl and heteroaryl is optionally substituted with R ₆ and R7 substituents.

In another aspect of the use of a compound of Formula (I),

Ri is heterocyclyl, heterocyclyl-Ci-salkyl, heterocyclyl-Ci-salkoxy, heterocyclyl-amino,

(heterocyclyl)(Ci-8alkyl)amino, heterocyclyl -amino-Ci-salkyl,

heterocyclyl-Ci-8alkyl-amino, (heterocyclyl -Ci-8alkyl)2-amino,

(heterocyclyl-Ci-8alkyl)(Ci-8alkyl)amino, heterocyclyl -Ci-salkyl-amino-Ci-salkyl, (heterocyclyl-Ci-8alkyl)2-amino-Ci-8alkyl,

(heterocyclyl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl, heterocyclyl-oxy,

heterocyclyl-carbonyl or heterocyclyl-carbonyl-oxy; wherein, each instance of heterocyclyl is optionally substituted with R3 and R4 substituents; and

R2 is aryl, aryl-amino, aryl-amino-carbonyl, heterocyclyl, heteroaryl or heteroaryl-amino,

wherein, each instance of aryl, heterocyclyl and heteroaryl is optionally substituted with R ₆ and R7 substituents.

In another aspect of the use of a compound of Formula (I),

Ri is heterocyclyl optionally substituted with one, two or three R3 substituents and optionally, with one additional R4 substituents; or, optionally, with one, two, three or four R3 substituents; and

R2 is aryl, aryl-amino, aryl-amino-carbonyl, heterocyclyl, heteroaryl or heteroaryl-amino,

wherein, each instance of aryl, heterocyclyl and heteroaryl is optionally substituted with R ₆ and R7 substituents. In another aspect of the use of a compound of Formula (I),

Ri is C3-i4cycloalkyl optionally substituted with R ₃ and R ₄ substituents; and

R ₂ is aryl, aryl-amino, aryl-amino-carbonyl, heterocyclyl, heteroaryl or heteroaryl-amino,

wherein, each instance of aryl, heterocyclyl and heteroaryl is optionally substituted with

R ₆ and R ₇ substituents.

In another aspect of the use of a compound of Formula (I),

Ri is aryl-Ci-8alkyl-amino, (aryl-Ci-8alkyl) ₂ -amino, (aryl-Ci-8alkyl)(Ci-8alkyl)amino,

aryl-Ci-8alkyl-amino-Ci-8alkyl, (aryl-Ci-8alkyl) ₂ -amino-Ci-8alkyl or

(aryl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl; wherein, each instance of aryl is optionally substituted with R ₃ and R ₄ substituents; and

R ₂ is aryl, aryl-amino, aryl-amino-carbonyl, heterocyclyl, heteroaryl or heteroaryl-amino,

wherein, each instance of aryl, heterocyclyl and heteroaryl is optionally substituted with

R ₆ and R ₇ substituents.

In another aspect of the use of a compound of Formula (I),

Ri is aryl-Ci-8alkyl-amino optionally substituted with R ₃ and R ₄ substituents; and

R ₂ is aryl, aryl-amino, aryl-amino-carbonyl, heterocyclyl, heteroaryl or heteroaryl-amino,

wherein, each instance of aryl, heterocyclyl and heteroaryl is optionally substituted with

R ₆ and R ₇ substituents.

In another aspect of the use of a compound of Formula (I),

Ri is heteroaryl, heteroaryl-Ci-salkyl, heteroaryl-Ci-salkoxy, heteroaryl-amino,

heteroaryl -Ci-salkyl-amino, (heteroaryl-Ci-8alkyl) ₂ -amino,

(heteroaryl-Ci-8alkyl)(Ci-8alkyl)amino, heteroaryl-Ci-salkyl-amino-Ci-salkyl,

(heteroaryl-Ci-8alkyl) ₂ -amino-Ci-8alkyl or

(heteroaryl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl; wherein, each instance of heterocyclyl, C _3- i ₄ cycloalkyl, aryl and heteroaryl is optionally substituted with R ₃ and R ₄ substituents; and

R ₂ is aryl, aryl-amino, aryl-amino-carbonyl, heterocyclyl, heteroaryl or heteroaryl-amino,

wherein, each instance of aryl, heterocyclyl and heteroaryl is optionally substituted with R ₆ and R ₇ substituents.

In another aspect of the use of a compound of Formula (I),

Ri is heteroaryl optionally substituted with R ₃ and R ₄ substituents; and R ₂ is aryl, aryl-amino, aryl-amino-carbonyl, heterocyclyl, heteroaryl or heteroaryl-amino, wherein, each instance of aryl, heterocyclyl and heteroaryl is optionally substituted with R.6 and R ₇ substituents.

An aspect of the use of the compound of Formula (I) is the use of a compound selected from

Formula (II), Formula (III), Formula (IV), Formula (V), Formula (VI), Formula (VII), Formula (VIII), Formula (IX), Formula (X), Formula (XI), Formula (XII), Formula (XIII) or Formula (XIV):

(Π), (HI), (IV),

(V), (VI), (VII),

(VIII), (IX), (X),

(XI), (XII), (XIII) or (XIV) or a form thereof.

In an aspect of the use of the compound of Formula (I), w ₃ is C-Ri, w ₆ is C-R ₂ , wi, w ₄ , w ₅ and w ₇ are independently C-R _a or N and w ₂ is C-Rb or N.

In another aspect of the use of the compound of Formula (I), w ₃ is C-R ₂ , w ₆ is C-Ri, wi, w ₄ , w ₅ and w ₇ are independently C-Ra or N and w ₂ is C-Rb or N. In another aspect of the use of the compound of Formula (I), w ₄ is C-Ri, w ₇ is C-R ₂ , wi, w ₃ and

W5 are independently C-Ra or N, w ₂ is C-Rb or N and w ₆ is C-R _c or N.

In another aspect of the use of the compound of Formula (I), w ₄ is C-R ₂ , w ₇ is C-Ri, wi, w ₃ and

W5 are independently C-Ra or N, w ₂ is C-Rb or N and w ₆ is C-R _c or N.

In an aspect of the use of the compound of Formula (II), w ₃ is C-Ri, w ₆ is C-R ₂ , w ₄ , w ₅ and w ₇ are independently C-Ra or N and w ₂ is C-Rb or N.

In another aspect of the use of the compound of Formula (II), w ₃ is C-R ₂ , w ₆ is C-Ri, w ₄ , w ₅ and w ₇ are independently C-Ra or N and w ₂ is C-Rb or N.

In another aspect of the use of the compound of Formula (II), w ₄ is C-Ri, w ₇ is C-R ₂ , w ₃ and w ₅ are independently C-R _a or N, w ₂ is C-Rb or N and w ₆ is C-R _c or N.

In another aspect of the use of the compound of Formula (II), w ₄ is C-R ₂ , w ₇ is C-Ri, w ₃ and w ₅ are independently C-R _a or N, w ₂ is C-Rb or N and w ₆ is C-R _c or N.

In an aspect of the use of the compound of Formula (III), w ₃ is C-Ri, w ₆ is C-R ₂ and wi, w ₄ , w ₅ and w ₇ are independently C-Ra or N.

In another aspect of the use of the compound of Formula (III), w ₃ is C-R ₂ , w ₆ is C-Ri and wi, w ₄ ,

W5 and w ₇ are independently C-Ra or N.

In another aspect of the use of the compound of Formula (III), w ₄ is C-Ri, w ₇ is C-R ₂ , wi, w ₃ and

W5 are independently C-Ra or N and w ₆ is C-R _c or N.

In another aspect of the use of the compound of Formula (III), w ₄ is C-R ₂ , w ₇ is C-Ri, wi, w ₃ and

W5 are independently C-Ra or N and w ₆ is C-R _c or N.

In an aspect of the use of the compound of Formula (IV), w ₄ is C-Ri, w ₇ is C-R ₂ , wi and w ₅ are independently C-Ra or N, w ₂ is C-Rb or N and w ₆ is C-R _c or N.

In another aspect of the use of the compound of Formula (IV), w ₄ is C-R ₂ , w ₇ is C-Ri, wi and w ₅ are independently C-R _a or N, w ₂ is C-Rb or N and w ₆ is C-R _c or N.

In an aspect of the use of the compound of Formula (V), w ₃ is C-Ri, w ₆ is C-R ₂ , wi, w ₅ and w ₇ are independently C-Ra or N and w ₂ is C-Rb or N.

In another aspect of the use of the compound of Formula (V), w ₃ is C-R ₂ , w ₆ is C-Ri, wi, w ₅ and w ₇ are independently C-Ra or N and w ₂ is C-Rb or N.

In an aspect of the use of the compound of Formula (VI), w ₃ is C-Ri, w ₆ is C-R ₂ , wi, w ₄ and w ₇ are independently C-R _a or N and w ₂ is C-Rb or N. In another aspect of the use of the compound of Formula (VI), w ₃ is C-R ₂ , w ₆ is C-Ri, wi, w ₄ and

W7 are independently C-Ra or N and w ₂ is C-Rb or N.

In another aspect of the use of the compound of Formula (VI), w ₄ is C-Ri, w ₇ is C-R ₂ , wi and w ₃ are independently C-R _a or N, w ₂ is C-Rb or N and w ₆ is C-R _c or N.

In another aspect of the use of the compound of Formula (VI), w ₄ is C-R ₂ , w ₇ is C-Ri, wi and w ₃ are independently C-R _a or N, w ₂ is C-Rb or N and w ₆ is C-R _c or N.

In another aspect of the use of the compound of Formula (VII), w ₄ is C-Ri, w ₇ is C-R ₂ , wi, w ₃ and

W5 are C-Ra or N and w ₂ is C-Rb or N.

In another aspect of the use of the compound of Formula (VII), w ₄ is C-R ₂ , w ₇ is C-Ri, wi, w ₃ and

W5 are C-Ra or N and w ₂ is C-Rb or N.

In another aspect of the use of the compound of Formula (VIII), w ₃ is C-Ri, w ₆ is C-R ₂ , wi, w ₄ and W5 are C-R _a or N and w ₂ is C-Rb or N.

In another aspect of the use of the compound of Formula (VIII), w ₃ is C-R ₂ , w ₆ is C-Ri, wi, w ₄ and W5 are C-R _a or N and w ₂ is C-Rb or N.

In an aspect of the use of the compound of Formula (IX), w ₃ is C-Ri, w ₆ is C-R ₂ , w ₄ and w ₇ are independently C-Ra or N and w ₂ is C-Rb or N.

In another aspect of the use of the compound of Formula (IX), w ₃ is C-R ₂ , w ₆ is C-Ri, w ₄ and w ₇ are independently C-R _a or N and w ₂ is C-Rb or N.

In another aspect of the use of the compound of Formula (IX), w ₄ is C-Ri, w ₇ is C-R ₂ , w ₂ is C-Rb or N, w ₃ is C-Ra or N and w ₆ is C-R _c or N.

In another aspect of the use of the compound of Formula (IX), w ₄ is C-R ₂ , w ₇ is C-Ri, w ₂ is C-Rb or N, w ₃ is C-Ra or N and w ₆ is C-R _c or N.

In an aspect of the use of the compound of Formula (X), w ₃ is C-Ri, w ₆ is C-R ₂ , w ₂ is C-Rb or N and W5 and w ₇ are independently C-R _a or N.

In another aspect of the use of the compound of Formula (X), w ₃ is C-R ₂ , w ₆ is C-Ri, w ₂ is C-Rb or N and w ₅ and w ₇ are independently C-Ra or N.

In an aspect of the use of the compound of Formula (XI), w ₄ is C-Ri, w ₇ is C-R ₂ , w ₂ is C-Rb or N,

W5 is C-Ra or N and w ₆ is C-Rc or N.

In another aspect of the use of the compound of Formula (XI), w ₄ is C-R ₂ , w ₇ is C-Ri, w ₂ is C-Rb or N, W5 is C-Ra or N and w ₆ is C-R _c or N. In an aspect of the use of the compound of Formula (XII), w ₃ is C-Ri, w ₆ is C-R ₂ and w ₄ , w ₅ and

W7 are independently C-Ra or N.

In another aspect of the use of the compound of Formula (XII), w ₃ is C-R ₂ , w ₆ is C-Ri and w ₄ , w ₅ and W7 are independently C-Ra or N.

In another aspect of the use of the compound of Formula (XII), w ₄ is C-Ri, w ₇ is C-R ₂ , w ₃ and w ₅ are independently C-R _a or N and w ₆ is C-Rc or N.

In another aspect of the use of the compound of Formula (XII), w ₄ is C-R ₂ , w ₇ is C-Ri, w ₃ and w ₅ are independently C-R _a or N and w ₆ is C-Rc or N.

In an aspect of the use of the compound of Formula (XIII), w ₃ is C-Ri, w ₆ is C-R ₂ , w ₂ is C-Rb or

N and w ₄ and w ₅ are independently C-R _a or N.

In another aspect of the use of the compound of Formula (XIII), w ₃ is C-R ₂ , w ₆ is C-Ri, w ₂ is

C-Rb or N and w ₄ and w ₅ are independently C-R _a or N.

In an aspect of the use of the compound of Formula (XIV), w ₄ is C-Ri, w ₇ is C-R ₂ , w ₂ is C-Rb or

N and w ₃ and w ₅ are independently C-R _a or N.

In another aspect of the use of the compound of Formula (XIV), w ₄ is C-R ₂ , w ₇ is C-Ri, w ₂ is

C-Rb or N and w ₃ and w ₅ are independently C-R _a or N.

Another aspect of the use of the compound of Formula (I) is the use of the compound selected from Formula II), Formula (III), Formula (IX), Formula (XI) or Formula (XII):

(IX), (XI), or (XII) or a form thereof. Another aspect of the use of the compound of Formula (I) is the use of the compound of Formula (II):

(Π)

or a form thereof.

Another aspect of the use of the compound of Formula (I) is the use of the compound of Formula (III):

(III)

or a form thereof.

Another aspect of the use of the compound of Formula (I) is the use of the compound of Formula (IV):

or a form thereof.

Another aspect of the use of the compound of Formula (I) is the use of the compound of Formula (V):

or a form thereof. Another aspect of the use of the compound of Formula (I) is the use of the compound of Formula (VI):

(VI)

or a form thereof.

Another aspect of the use of the compound of Formula (I) is the use of the compound of Formula (VII):

or a form thereof.

Another aspect of the use of the compound of Formula (I) is the use of the compound of Formula (VIII):

or a form thereof.

Another aspect of the use of the compound of Formula (I) is the use of the compound of Formula (IX):

or a form thereof. Another aspect of the use of the compound of Formula (I) is the use of the compound of Formula (X):

(X)

or a form thereof.

Another aspect of the use of the compound of Formula (I) is the use of the compound of Formula (XI):

(XI)

or a form thereof.

Another aspect of the compound of Formula (I) is the use of the compound of Formula (XII):

or a form thereof.

Another aspect of the use of the compound of Formula (I) is the use of the compound of Formula (XIII):

(XIII)

or a form thereof. Another aspect of the use of the compound of Formula (I) is the use of the compound of Formula (XIV):

or a form thereof.

An aspect of the use of the compound of Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V), Formula (VI), Formula (VII), Formula (VIII), Formula (IX), Formula (X), Formula (XI), Formula (XII), Formula (XIII) or Formula (XIV) is the use of a compound selected from Formula (la), Formula (Ha), Formula (Ilia), Formula (IVa), Formula (Va), Formula (Via), Formula (Vila), Formula (Villa), Formula (IXa), Formula (Xa), Formula (XIa), Formula (Xlla), Formula (XHIa) or Formula (XlVa), respectively:

(Via) (Vila), (Villa),

(Xlla), (XHIa), or (XlVa) or a form thereof.

In an aspect of the use of the compound of Formula (la), one of w ₃ , w ₄ , w ₆ and w ₇ is C-Ri and one other of w ₃ , w ₄ , w ₆ and w ₇ is C-R ₂ , provided that,

when W3 is C-Ri, then w ₆ is C-R ₂ and w ₄ and w ₇ are independently C-R _a or N; or,

when W3 is C-R ₂ , then w ₆ is C-Ri and w ₄ and w ₇ are independently C-R _a or N; or,

when w ₄ is C-Ri, then w ₇ is C-R ₂ and w ₃ is C-Ra or N and w ₆ is C-Rc or N; or,

when w ₄ is C-R ₂ , then w ₇ is C-Ri and W3 is C-Ra or N and w ₆ is C-Rc or N.

In an aspect of the use of the compound of Formula (Ila), one of w ₃ , w ₄ , w ₆ and w ₇ is C-Ri and one other of w ₃ , w ₄ , w ₆ and w ₇ is C-R ₂ , provided that,

when W3 is C-Ri, then w ₆ is C-R ₂ and w ₄ and w ₇ are independently C-R _a or N; or,

when W3 is C-R ₂ , then w ₆ is C-Ri and w ₄ and w ₇ are independently C-R _a or N; or,

when w ₄ is C-Ri, then w ₇ is C-R ₂ and W3 is C-Ra or N and w ₆ is C-Rc or N; or,

when w ₄ is C-R ₂ , then w ₇ is C-Ri and W3 is C-Ra or N and w ₆ is C-Rc or N.

In an aspect of the use of the compound of Formula (Ilia), one of w ₃ , w ₄ , w ₆ and w ₇ is C-Ri and one other of w ₃ , w ₄ , w ₆ and w ₇ is C-R ₂ , provided that,

when W3 is C-Ri, then w ₆ is C-R ₂ and w ₄ and w ₇ are independently C-R _a or N; or,

when W3 is C-R ₂ , then w ₆ is C-Ri and w ₄ and w ₇ are independently C-R _a or N; or,

when w ₄ is C-Ri, then w ₇ is C-R ₂ and W3 is C-Ra or N and w ₆ is C-Rc or N; or,

when w ₄ is C-R ₂ , then w ₇ is C-Ri and W3 is C-Ra or N and w ₆ is C-Rc or N. In an aspect of the use of the compound of Formula (IVa), one of w ₄ and w ₇ is C-Ri and the other is C-R ₂ , provided that, when w ₄ is C-Ri, then w ₇ is C-R ₂ ; or, when w ₄ is C-R ₂ , then w ₇ is

In an aspect of the use of the compound of Formula (Va), one of w ₃ and w ₆ is C-Ri and the other is C-R ₂ , provided that, when w ₃ is C-Ri, then w ₆ is C-R ₂ ; or, when w ₃ is C-R ₂ , then w ₆ is

In an aspect of the use of the compound of Formula (Via), one of w ₃ , w ₄ , w ₆ and w ₇ is C-Ri and one other of w ₃ , w ₄ , w ₆ and w ₇ is C-R ₂ , provided that,

when w ₃ is C-Ri, then w ₆ is C-R ₂ and w ₄ and w ₇ are independently C-R _a or N; or,

when w ₃ is C-R ₂ , then w ₆ is C-Ri and w ₄ and w ₇ are independently C-R _a or N; or,

when w ₄ is C-Ri, then w ₇ is C-R ₂ and w ₃ is C-Ra or N and w ₆ is C-Rc or N; or,

when w ₄ is C-R ₂ , then w ₇ is C-Ri and w ₃ is C-Ra or N and w ₆ is C-Rc or N.

In an aspect of the use of the compound of Formula (Vila), one of w ₄ and w ₇ is C-Ri and the other is C-R ₂ , provided that, when w ₄ is C-Ri, then w ₇ is C-R ₂ ; or, when w ₄ is C-R ₂ , then

In an aspect of the use of the compound of Formula (Villa), one of w ₃ and w ₆ is C-Ri and the other is C-R ₂ , provided that, when w ₃ is C-Ri, then w ₆ is C-R ₂ ; or, when w ₃ is C-R ₂ , then

In an aspect of the use of the compound of Formula (IXa), one of w ₃ , w ₄ , w ₆ and w ₇ is C-Ri and one other of w ₃ , w ₄ , w ₆ and w ₇ is C-R ₂ , provided that,

when w ₃ is C-Ri, then w ₆ is C-R ₂ and w ₄ and w ₇ are independently C-R _a or N; or,

when w ₃ is C-R ₂ , then w ₆ is C-Ri and w ₄ and w ₇ are independently C-R _a or N; or,

when w ₄ is C-Ri, then w ₇ is C-R ₂ and w ₃ is C-Ra or N and w ₆ is C-Rc or N; or,

when w ₄ is C-R ₂ , then w ₇ is C-Ri and w ₃ is C-Ra or N and w ₆ is C-Rc or N.

In an aspect of the use of the compound of Formula (Xa), one of w ₃ and w ₆ is C-Ri and the other is C-R ₂ , provided that, when w ₃ is C-Ri, then w ₆ is C-R ₂ ; or, when w ₃ is C-R ₂ , then w ₆ is

In an aspect of the use of the compound of Formula (XIa), one of w ₄ and w ₇ is C-Ri and the other is C-R ₂ , provided that, when w ₄ is C-Ri, then w ₇ is C-R ₂ ; or, when w ₄ is C-R ₂ , then w ₇ is In an aspect of the use of the compound of Formula (Xlla), one of w ₃ , w ₄ , w ₆ and w ₇ is C-Ri and one other of w ₃ , w ₄ , w ₆ and w ₇ is C-R ₂ , provided that,

when W3 is C-Ri, then w ₆ is C-R ₂ and w ₄ and w ₇ are independently C-R _a or N; or,

when W3 is C-R ₂ , then w ₆ is C-Ri and w ₄ and w ₇ are independently C-R _a or N; or,

when w ₄ is C-Ri, then w ₇ is C-R ₂ and w ₃ is C-Ra or N and w ₆ is C-Rc or N; or,

when w ₄ is C-R ₂ , then w ₇ is C-Ri and w ₃ is C-Ra or N and w ₆ is C-Rc or N.

In an aspect of the use of the compound of Formula (XHIa), one of w ₃ and w ₆ is C-Ri and the other is C-R ₂ , provided that, when w ₃ is C-Ri, then w ₆ is C-R ₂ ; or, when w ₃ is C-R ₂ , then

In an aspect of the use of the compound of Formula (XlVa), one of w ₄ and w ₇ is C-Ri and the other is C-R ₂ , provided that, when w ₄ is C-Ri, then w ₇ is C-R ₂ ; or, when w ₄ is C-R ₂ , then

An aspect of the use of the compound of Formula (I), Formula (II), Formula (III), Formula (IX), Formula (XI) or Formula (XII) is the use of the compound selected from Formula (la), Formula (Ila), Formula (Ilia), Formula (IXa), Formula (XIa) or Formula (Xlla), respectivel :

(la), (Ila), (Ilia),

(IXa), (XIa), or (Xlla) or a form thereof. Another aspect of the use of the compound of Formula (I) is the use of the compound of Formula (la):

(la)

or a form thereof.

Another aspect of the use of the compound of Formula (II) is the use of the compound of Formula (Ila):

(Ila)

or a form thereof.

Another aspect of the use of the compound of Formula (III) is the use of the compound of

Formula (Ilia):

(Ilia)

or a form thereof.

Another aspect of the use of the compound of Formula (IV) is the use of the compound of

Formula (IVa):

(IVa)

or a form thereof. Another aspect of the use of the compound of Formula (V) is the use of the compound of Formula (Va):

(Va)

or a form thereof.

Another aspect of the use of the compound of Formula (VI) is the use of the compound of

Formula (Via):

(Via)

or a form thereof.

Another aspect of the use of the compound of Formula (VII) is the use of the compound of

Formula (Vila):

(Vila)

or a form thereof.

Another aspect of the use of the compound of Formula (VIII) is the use of the compound of

Formula (Villa):

(Villa)

or a form thereof. Another aspect of the use of the compound of Formula (IX) is the use of the compound of Formula (IXa):

(IXa)

or a form thereof.

Another aspect of the use of the compound of Formula (X) is the use of the compound of Formula (Xa):

(Xa)

or a form thereof.

Another aspect of the use of the compound of Formula (XI) is the use of the compound of

Formula (XIa):

(XIa)

or a form thereof.

Another aspect of the use of the compound of Formula (XII) is the use of the compound of

Formula (Xlla):

(Xlla)

or a form thereof. Another aspect of the use of the compound of Formula (XIII) is the use of the compound of Formula (XHIa):

(XHIa)

or a form thereof.

Another aspect of the use of the compound of Formula (XIV) is the use of the compound of Formula (XI Va):

(XlVa)

or a form thereof.

An aspect of the use of the compound of Formula (la) is the use of a compound of Formula (lal), Formula (Ia2), Formula (Ia3) or Formula (Ia4):

or a form thereof. An aspect of the use of the compound of Formula (Ila) is the use of a compound of Formula (Hal), Formula (IIa2), Formula (IIa3) or Formula (IIa4):

(IIa3) or (IIa4)

or a form thereof.

An aspect of the use of the compound of Formula (Ilia) is the use of a compound of Formula (Illal), Formula (IIIa2), Formula (IIIa3) or Formula (IIIa4):

(IIIa3) or (IIIa4)

or a form thereof. An aspect of the use of the compound of Formula (IVa) is the use of a compound of Formula (IVal) or Formul

(IVal) or (IVa2)

or a form thereof.

An aspect of the use of the compound of Formula (Va) is the use of a compound of Formula (Val) or Formula (Va2):

or a form thereof.

An aspect of the use of the compound of Formula (Via) is the use of a compound of Formula (Vial), Formula (VIa2), Formula (VIa3) or Formula (VIa2):

(VIa3) or (VIa4)

or a form thereof. An aspect of the use of the compound of Formula (Vila) is the use of a compound of Formula

(Vllal) or Formula (VIIa2):

or a form thereof.

An aspect of the use of the compound of Formula (Villa) is the use of a compound of Formula (VHIal) or Formula (VIIIa2):

or a form thereof.

An aspect of the use of the compound of Formula (IXa) is the use of a compound of Formula (IXal), Formula (IXa2), Formula (IXa3) or Formula (IXa4):

(IXa3) or (IXa4)

or a form thereof. An aspect of the use of the compound of Formula (Xa) is the use of a compound of Formula (Xal) or Formul

or a form thereof.

An aspect of the use of the compound of Formula (XIa) is the use of a compound of Formula (Xlal) or Formul

(XIal) or (XIa2)

or a form thereof.

An aspect of the use of the compound of Formula (Xlla) is the use of a compound of Formula

(Xllal), Formula (XIIa2), Formula (XIIa3) or Formula (XIIa4):

(XIIa3) or (XIIa4)

or a form thereof. An aspect of the use of the compound of Formula (Xllla) is the use of a compound of Formula (XHIal) or Formula (XIIIa2):

(XHIal) or (XIIIa2)

or a form thereof.

An aspect of the use of the compound of Formula (XlVa) is the use of a compound of Formula (XlVal) or Formula (XIVa2):

or a form thereof.

An aspect of the use of the compound of Formula (la) is the use of the compound of Formula (lal):

(lal)

or a form thereof.

An aspect of the use of the compound of Formula (la) is the use of the compound of Formula (Ia2):

(Ia2)

or a form thereof. An aspect of the use of the compound of Formula (la) is the use of the compound of Formula (Ia3):

(Ia3)

or a form thereof.

An aspect of the use of the compound of Formula (la) is the use of the compound of Formula (Ia4):

or a form thereof.

An aspect of the use of the compound of Formula (Ila) is the use of the compound of Formula (Hal):

or a form thereof.

An aspect of the use of the compound of Formula (Ila) is the use of the compound of Formula (IIa2):

(IIa2)

or a form thereof. An aspect of the use of the compound of Formula (Ila) is the use of the compound of Formula (IIa3):

(IIa3)

or a form thereof.

An aspect of the use of the compound of Formula (Ila) is the use of the compound of Formula (IIa4):

(IIa4)

or a form thereof.

An aspect of the use of the compound of Formula (Ilia) is the use of the compound of Formula (Illal):

(Illal)

or a form thereof.

An aspect of the use of the compound of Formula (Ilia) is the use of the compound of Formula (IIIa2):

(IIIa2)

or a form thereof. An aspect of the use of the compound of Formula (Ilia) is the use of the compound of Formula (IIIa3):

(IIIa3)

or a form thereof.

An aspect of the use of the compound of Formula (Ilia) is the use of the compound of Formula (IIIa4):

(IIIa4)

or a form thereof.

An aspect of the use of the compound of Formula (IVa) is the use of the compound of Formula (IVal):

or a form thereof.

An aspect of the use of the compound of Formula (IVa) is the use of the compound of Formula (IVa2):

(IVa2)

or a form thereof. An aspect of the use of the compound of Formula (Va) is the use of the compound of Formula (Val):

(Val)

or a form thereof.

An aspect of the use of the compound of Formula (Va) is the use of the compound of Formula (Va2):

or a form thereof.

An aspect of the use of the compound of Formula (Via) is the use of the compound of Formula (Vial):

(Vial)

or a form thereof.

An aspect of the use of the compound of Formula (Via) is the use of the compound of Formula (VIa2):

(VIa2)

or a form thereof. An aspect of the use of the compound of Formula (Via) is the use of the compound of Formula Formula (VIa3):

(VIa3)

or a form thereof.

An aspect of the use of the compound of Formula (Via) is the use of the compound of Formula (VIa4):

(VIa4)

or a form thereof.

An aspect of the use of the compound of Formula (Vila) is the use of the compound of Formula (Vllal):

or a form thereof.

An aspect of the use of the compound of Formula (Vila) is the use of the compound of Formula (VIIa2):

(VIIa2)

or a form thereof. An aspect of the use of the compound of Formula (Villa) is the use of the compound of Formula (VHIal):

or a form thereof.

An aspect of the use of the compound of Formula (Villa) is the use of the compound of Formula (VIIIa2):

or a form thereof.

An aspect of the use of the compound of Formula (IXa) is the use of the compound of Formula (IXal):

(IXal)

or a form thereof.

An aspect of the use of the compound of Formula (IXa) is the use of the compound of Formula (IXa2):

(IXa2)

or a form thereof. An aspect of the use of the compound of Formula (IXa) is the use of the compound of Formula (IXa3):

(IXa3)

or a form thereof.

An aspect of the use of the compound of Formula (IXa) is the use of the compound of Formula (IXa4):

(IXa4)

or a form thereof.

An aspect of the use of the compound of Formula (Xa) is the use of the compound of Formula (Xal):

(Xal)

or a form thereof.

An aspect of the use of the compound of Formula (Xa) is the use of the compound of Formula (Xa2):

(Xa2)

or a form thereof. An aspect of the use of the compound of Formula (XIa) is the use of the compound of Formula (XIal):

(XIal)

or a form thereof.

An aspect of the use of the compound of Formula (XIa) is the use of the compound of Formula (XIa2):

(XIa2)

or a form thereof.

An aspect of the use of the compound of Formula (Xlla) is the use of the compound of Formula (Xllal):

(Xllal)

or a form thereof.

An aspect of the use of the compound of Formula (Xlla) is the use of the compound of Formula (XIIa2):

(XIIa2)

or a form thereof. An aspect of the use of the compound of Formula (Xlla) is the use of the compound of Formula (XIIa3):

(XIIa3)

or a form thereof.

An aspect of the use of the compound of Formula (Xlla) is the use of the compound of Formula (XIIa4):

(XIIa4)

or a form thereof.

An aspect of the use of the compound of Formula (Xllla) is the use of the compound of Formula (XHIal):

(XHIal)

or a form thereof.

An aspect of the use of the compound of Formula (Xllla) is the use of the compound of Formula (XIIIa2):

(XIIIa2)

or a form thereof. An aspect of the use of the compound of Formula (XlVa) is the use of the compound of Formula (XlVal):

(XlVal)

or a form thereof.

An aspect of the use of the compound of Formula (XlVa) is the use of the compound of Formula (XIVa2):

(XIVa2)

or a form thereof.

An aspect of the use of the compound of Formula (I) or a form thereof is a compound selected from the group consisting of:

70

631 632 633

667 669

703 704 705

739 740 741

757 758 759

793 794 795

846 847 848

876, or 877

wherein the form of the compound is selected from the group consisting of a salt, prodrug, hydrate, solvate, clathrate, isotopologue, racemate, enantiomer, diastereomer, stereoisomer, polymorph and tautomer form thereof.

An aspect of the use of the compound of Formula (I) or a form thereof is a compound selected from the group consisting of (where compound number (#*) indicates that a salt form of the compound was isolated):

Cpd Name

1 2-(4-methoxyphenyl)-7-(piperazin-l-yl)-4H-pyrido[l,2-a]pyrim idin-4-one

2 2-(4-methoxyphenyl)-7-(4-methylpiperazin-l-yl)-4H-pyrido[l,2 -a]pyrimidin-4-one

3 2-(4-methoxyphenyl)-7-[(3R)-3-methylpiperazin-l-yl]-4H-pyrid o[l,2-a]pyrimidin-4-one Cpd Name

4 7-[(3R,5S)-3,5-dimethylpiperazin-l-yl]-2-(4-methoxy

one

5 7-(l,4-diazepan-l-yl)-2-(4-methoxyphenyl)-4H-pyrido[l,2-a]py rimidin-4-one

6 2-(3,4-dimethoxyphenyl)-7-(piperazin-l-yl)-4H-pyrido[l,2-a]p yrimidin-4-one

7 2-(3,4-dimethoxyphenyl)-7-(3,3-dimethylpiperazin-l-yl)-4H-py rido[l,2-a]pyrimidin-4-one

8 2-(3,4-dimethoxyphenyl)-7-[(3R)-3-methylpiperazin-l-yl]-4H-p yrido[l,2-a]pyrimidin-4-one

9 2-(3,4-dimethoxyphenyl)-7-(4-ethylpiperazin-l-yl)-4H-pyrido[ l,2-a]pyrimidin-4-one

10 7-(l,4-diazepan-l-yl)-2-(3,4-dimethoxyphenyl)-4H-pyrido[l,2- a]pyrimidin-4-one

11 2-(3 ,4-dimethoxyphenyl)-7-(4-methyl- 1 ,4-diazepan- 1 -yl)-4H-pyrido [ 1 ,2-a]pyrimidin-4-one

12 2-(4-methoxyphenyl)-7-[(3S)-3-methylpiperazin-l-yl]-4H-pyrid o[l,2-a]pyrimidin-4-one

13 2-(3,4-dimethoxyphenyl)-7-(4-methylpiperazin-l-yl)-4H-pyrido [l,2-a]pyrimidin-4-one

14 2-(3,4-dimethoxyphenyl)-7-[(3R,5S)-3,5-dimethylpiperazin-l-y l]-4H-pyrido[l,2-a]pyrimidin- 4-one

15 2-(3,4-dimethoxyphenyl)-7-(4-propylpiperazin-l-yl)-4H-pyrido [l,2-a]pyrimidin-4-one

16 2-(4-methoxyphenyl)-7-(4-methyl-l,4-diazepan-l-yl)-4H-pyrido [l,2-a]pyrimidin-4-one

17 7-(3,3-dimethylpiperazin-l-yl)-2-(4-methoxyphenyl)-4H-pyrido [l,2-a]pyrimidin-4-one

18 2-(l,3-benzodioxol-5-yl)-7-(piperazin-l-yl)-4H-pyrido[l,2-a] pyrimidin-4-one

19 2-(l,3-benzodioxol-5-yl)-7-(4-methylpiperazin-l-yl)-4H-pyrid o[l,2-a]pyrimidin-4-one

20 2-(l,3-benzodioxol-5-yl)-7-[(3R)-3-methylpiperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

21 2-(l,3-benzodioxol-5-yl)-7-[(3R,5S)-3,5-dimethylpiperazin-l- yl]-4H-pyrido[l,2-a]pyrimidin- 4-one

22 2-(3-methoxyphenyl)-7-(piperazin-l-yl)-4H-pyrido[l,2-a]pyrim idin-4-one

23 2-(3-methoxyphenyl)-7-(4-methylpiperazin-l-yl)-4H-pyrido[l,2 -a]pyrimidin-4-one

24 2-(3-methoxyphenyl)-7-[(3R)-3-methylpiperazin-l-yl]-4H-pyrid o[l,2-a]pyrimidin-4-one

25 7-[(3R,5S)-3,5-dimethylpiperazin-l-yl]-2-(3-methoxyphenyl)-4 H-pyrido[l,2-a]pyrimidin-4- one

26 7-(4-ethylpiperazin- 1 -yl)-2-(3 -methoxyphenyl)-4H-pyrido [ 1 ,2-a]pyrimidin-4-one

27 7-(l,4-diazepan-l-yl)-2-(3-methoxyphenyl)-4H-pyrido[l,2-a]py rimidin-4-one

28 2-(3-methoxyphenyl)-7-(4-methyl-l,4-diazepan-l-yl)-4H-pyrido [l,2-a]pyrimidin-4-one

29 2-(6-methylimidazo[l,2-a]pyridin-2-yl)-7-(piperazin-l-yl)-4H -pyrido[l,2-a]pyrimidin-4-one

30 2-(3,4-dimethoxyphenyl)-7-[(3S)-3-methylpiperazin-l-yl]-4H-p yrido[l,2-a]pyrimidin-4-one

31 2-(2,3-dihydro-l,4-benzodioxin-6-yl)-7-(piperazin-l-yl)-4H-p yrido[l,2-a]pyrimidin-4-one

32 2-(2,3 -dihydro- 1 ,4-benzodioxin-6-yl)-7- [(3 S)-3 -methylpiperazin- 1 -yl] -4H-pyrido [1,2- a]pyrimidin-4-one

33 2-phenyl-7-(piperazin-l-yl)-4H-pyrido[l,2-a]pyrimidin-4-one Cpd Name

34 7-[(3S)-3-methylpiperazin-l-yl]-2-phenyl-4H-pyrido[l,2-a]pyr imidin-4-one

35 2-(2,3-dihydro-l,4-benzodioxin-6-yl)-7-[(3R)-3-methylpiperaz in-l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

36 2-(2,3 -dihydro- 1 ,4-benzodioxin-6-yl)-7-(3 ,3 -dimethylpiperazin- 1 -yl)-4H-pyrido [1,2- a]pyrimidin-4-one

37 2-(2,3-dihydro-l,4-benzodioxin-6-yl)-7-[(3R,5S)-3,5-dimethyl piperazin-l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

38 7-( 1 ,4-diazepan- 1 -yl)-2-(2,3 -dihydro- 1 ,4-benzodioxin-6-yl)-4H-pyrido [ 1 ,2-a]pyrimidin-4-one

39 2-(2,3 -dihydro- 1 ,4-benzodioxin-6-yl)-7-(4-methyl- 1 ,4-diazepan- 1 -yl)-4H-pyrido [1,2- a]pyrimidin-4-one

40 2-(3,4-dimethoxyphenyl)-9-fluoro-7-(4-methylpiperazin-l-yl)- 4H-pyrido[l,2-a]pyrimidin-4- one

41 2-(3-chlorophenyl)-7-(piperazin-l-yl)-4H-pyrido[l,2-a]pyrimi din-4-one

42 2-(4-chlorophenyl)-7-(piperazin-l-yl)-4H-pyrido[l,2-a]pyrimi din-4-one

43 7-(piperazin-l-yl)-2-[3-(trifluoromethyl)phenyl]-4H-pyrido[l ,2-a]pyrimidin-4-one

44 7-(piperazin-l-yl)-2-[4-(trifluoromethyl)phenyl]-4H-pyrido[l ,2-a]pyrimidin-4-one

45 2-(3 -methylphenyl)-7-(piperazin- 1 -yl)-4H-pyrido [ 1 ,2-a]pyrimidin-4-one

46 2-(4-fluorophenyl)-7-(piperazin- 1 -yl)-4H-pyrido [ 1 ,2-a]pyrimidin-4-one

47 2-(4-nitrophenyl)-7-(piperazin-l-yl)-4H-pyrido[l,2-a]pyrimid in-4-one

48 2-(3,4-dimethoxyphenyl)-9-fluoro-7-(piperidin-4-ylamino)-4H- pyrido[l,2-a]pyrimidin-4-one

49 2-[4-(dimethylamino)phenyl]-9-fluoro-7-(piperazin-l-yl)-4H-p yrido[l,2-a]pyrimidin-4-one

50 2-[4-(dimethylamino)phenyl]-9-fluoro-7-[(3R)-3-methylpiperaz in-l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

51 2-(2-fluorophenyl)-7-(piperazin-l-yl)-4H-pyrido[l,2-a]pyrimi din-4-one

52 3-(3,4-dimethoxyphenyl)-8-(piperazin-l-yl)-4H-pyrido[l,2-a]p yrimidin-4-one

53 2-[4-(dimethylamino)phenyl]-7-(piperazin-l-yl)-4H-pyrido[l,2 -a]pyrimidin-4-one

54 2-[4-(dimethylamino)phenyl]-7-[(3S)-3-methylpiperazin-l-yl]- 4H-pyrido[l,2-a]pyrimidin-4- one

55 2-(3,4-dimethylphenyl)-7-(piperazin-l-yl)-4H-pyrido[l,2-a]py rimidin-4-one

56 2-(3 ,4-dimethylphenyl)-7- [(3 S)-3 -methylpiperazin- 1 -yl] -4H-pyrido [ 1 ,2-a]pyrimidin-4-one

57 2-[3-(dimethylamino)phenyl]-7-(piperazin-l-yl)-4H-pyrido[l,2 -a]pyrimidin-4-one

58 2-[3-(dimethylamino)phenyl]-7-[(3S)-3-methylpiperazin-l-yl]- 4H-pyrido[l,2-a]pyrimidin-4- one

59 2-[4-(difluoromethoxy)phenyl]-7-(piperazin-l-yl)-4H-pyrido[l ,2-a]pyrimidin-4-one

60 2-[4-(difluoromethoxy)phenyl]-7-[(3S)-3-methylpiperazin-l-yl ]-4H-pyrido[l,2-a]pyrimidin-4- one Cpd Name

61 2-(3-fluorophenyl)-7-(piperazin-l-yl)-4H-pyrido[l,2-a]pyrimi din-4-one

62 2-(3-nitrophenyl)-7-(piperazin-l-yl)-4H-pyrido[l,2-a]pyrimid in-4-one

63 2-(4-methylphenyl)-7-(piperazin-l-yl)-4H-pyrido[l,2-a]pyrimi din-4-one

64 2-(2-fluoro-4,5-dimethoxyphenyl)-7-(piperazin-l-yl)-4H-pyrid o[l,2-a]pyrimidin-4-one

65 2-(2-fluoro-4,5-dimethoxyphenyl)-7-[(3S)-3-methylpiperazin-l -yl]-4H-pyrido[l,2- a]pyrimidin-4-one

66 7-(3,8-diazabicyclo[3.2.1]oct-3-yl)-2-(3,4-dimethoxyphenyl)- 4H-pyrido[l,2-a]pyrimidin-4- one

67 2-[4-methoxy-3-(trifluoromethyl)phenyl]-7-(piperazin-l-yl)-4 H-pyrido[l,2-a]pyrimidin-4-on

68 2-[4-methoxy-3 -(trifluoromethyl)phenyl] -7-[(3R)-3 -methylpiperazin- 1 -yl] -4H-pyrido[ 1 ,2- a]pyrimidin-4-one

69 2-[4-methoxy-3-(trifluoromethyl)phenyl]-7-[(3S)-3-methylpipe razin-l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

70 2-(3,4-dimethoxyphenyl)-9-methoxy-7-(piperazin-l-yl)-4H-pyri do[l,2-a]pyrimidin-4-one 71 ¹ 2-(3,5-difluoro-4-hydroxyphenyl)-7-(piperazin-l-yl)-4H-pyrid o[l,2-a]pyrimidin-4-one

72 2-(3-fluoro-4-methoxyphenyl)-7-(piperazin-l-yl)-4H-pyrido[l, 2-a]pyrimidin-4-one

73 4-[4-oxo-7-(piperazin-l-yl)-4H-pyrido[l,2-a]pyrimidin-2-yl]b enzonitrile

74 2-(6-methylimidazo[l,2-a]pyrazin-2-yl)-7-(piperazin-l-yl)-4H -pyrido[l,2-a]pyrimidin-4-one

75 2-(6-methylimidazo [ 1 ,2-a]pyrazin-2-yl)-7-[(3 S)-3 -methylpiperazin- 1 -yl] -4H-pyrido [1,2- a]pyrimidin-4-one

76 2-[3-fluoro-5-(trifluoromethyl)phenyl]-7-(piperazin-l-yl)-4H -pyrido[l,2-a]pyrimidin-4-one

77 2-[4-fluoro-3-(trifluoromethyl)phenyl]-7-(piperazin-l-yl)-4H -pyrido[l,2-a]pyrimidin-4-one

78 2-[2-methoxy-3-(trifluoromethyl)phenyl]-7-(piperazin-l-yl)-4 H-pyrido[l,2-a]pyrimidin-4-one

79 2-(3 , 5 -difluorophenyl)-7-(piperazin- 1 -yl)-4H-pyrido [ 1 ,2-a]pyrimidin-4-one

80 7-(piperazin-l-yl)-2-[3-(trifluoromethoxy)phenyl]-4H-pyrido[ l,2-a]pyrimidin-4-one

81 2-[4-methoxy-3-(trifluoromethoxy)phenyl]-7-(piperazin-l-yl)- 4H-pyrido[l,2-a]pyrimidin one

82 2-[4-hydroxy-3-(trifluoromethoxy)phenyl]-7-(piperazin-l-yl)- 4H-pyrido[l,2-a]pyrimidin-4- one

83 2-[4-methoxy-3-(trifluoromethoxy)phenyl]-7-[(3S)-3-methylpip erazin-l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

84 2-[4-hydroxy-3-(trifluoromethoxy)phenyl]-7-[(3S)-3-methylpip erazin-l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

85 2-(3 ,4-dimethoxyphenyl)-4-oxo-7-(piperazin- 1 -yl)-4H-quinolizine- 1 -carbonitrile

86 2-(3-fluoro-4-methoxyphenyl)-7-[(3R)-3-methylpiperazin-l-yl] -4H-pyrido[l,2-a]pyrimidin-4- one Cpd Name

87 2-(3 -fluoro-4-methoxyphenyl)-7- [(3 S)-3 -methylpiperazin- 1 -yl] -4H-pyrido [ 1 ,2-a]pyrimidin-4- one

88 2-(6-methoxypyridin-3-yl)-7-(piperazin-l-yl)-4H-pyrido[l,2-a ]pyrimidin-4-one

89 2-(2,4-dimethoxyphenyl)-7-(piperazin-l-yl)-4H-pyrido[l,2-a]p yrimidin-4-one

90 2-(2,4-dimethoxyphenyl)-7-[(3S)-3-methylpiperazin-l-yl]-4H-p yrido[l,2-a]pyrimidin-4-one

91 2-(3,4-dimethoxyphenyl)-7-[(3S)-3-methylpiperazin-l-yl]-4H-q uinolizin-4-one

92 2-(5-fluoropyridin-3-yl)-7-(piperazin-l-yl)-4H-pyrido[l,2-a] pyrimidin-4-one

93 2-(5-fluoropyridin-3-yl)-7-[(3S)-3-methylpiperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

94 2-(5-chloropyridin-3-yl)-7-(piperazin-l-yl)-4H-pyrido[l,2-a] pyrimidin-4-one

95 2-(5-chloropyridin-3-yl)-7-[(3S)-3-methylpiperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

96 2-(5-chloro-6-methoxypyridin-3-yl)-7-(piperazin-l-yl)-4H-pyr ido[l,2-a]pyrimidin-4-one

97 2-(lH-indol-6-yl)-7-(piperazin-l-yl)-4H-pyrido[l,2-a]pyrimid in-4-one

98 2-(lH-indol-5-yl)-7-(piperazin-l-yl)-4H-pyrido[l,2-a]pyrimid in-4-one

99 2-[3-(difluoromethoxy)-4-methoxyphenyl]-7-(piperazin-l-yl)-4 H-pyrido[l,2-a]pyrimidin one

100 2-[3-(difluoromethoxy)-4-hydroxyphenyl]-7-(piperazin-l-yl)-4 H-pyrido[l,2-a]pyrimidin-4- one

101 2-[3-(difluoromethoxy)-4-methoxyphenyl]-7-[(3S)-3-methylpipe razin-l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

102 2-[3-(difluoromethoxy)-4-hydroxyphenyl]-7-[(3S)-3-methylpipe razin-l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

103 2-(3-fluoro-4-methoxyphenyl)-7-(piperazin-l-yl)-4H-quinolizi n-4-one

104 2-(3-fluoro-4-methoxyphenyl)-7- [(3 S)-3 -methylpiperazin- l-yl]-4H-quinolizin-4-one

105 2-(3,5-difluorophenyl)-7-[(3S)-3-methylpiperazin-l-yl]-4H-py rido[l,2-a]pyrimidin-4-one

106 2-(3,4-dimethoxyphenyl)-7-(piperazin-l-yl)-4H-quinolizin-4-o ne

107 2-(imidazo[l,2-a]pyridin-7-yl)-7-(piperazin-l-yl)-4H-pyrido[ l,2-a]pyrimidin-4-one

108 2-(imidazo[l,2-a]pyridin-6-yl)-7-(piperazin-l-yl)-4H-pyrido[ l,2-a]pyrimidin-4-one

109 2-(2-methylimidazo[l,2-a]pyridin-6-yl)-7-(piperazin-l-yl)-4H -pyrido[l,2-a]pyrimidin-4-one

110 2-(3-chloro-4-methoxyphenyl)-7-(piperazin-l-yl)-4H-pyrido[l, 2-a]pyrimidin-4-one

111 2-(3 -chloro-4-methoxyphenyl)-7-[(3 S)-3 -methylpiperazin- 1 -yl]-4H-pyrido[ 1 ,2-a]pyrimidin-4- one

112 2-(3-ethoxy-4-methoxyphenyl)-7-(piperazin-l-yl)-4H-pyrido[l, 2-a]pyrimidin-4-one

113 2-(3-ethoxy-4-methoxyphenyl)-7-[(3S)-3-methylpiperazin-l-yl] -4H-pyrido[l,2-a]pyrimidin-4- one

114 2-(2-methylimidazo[l,2-a]pyridin-6-yl)-7-(4-methylpiperazin- l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one Cpd Name

115 2-(2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3S)-3-methylpiper azin-l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

116 7-(l,4-diazepan-l-yl)-2-(2-methylimidazo[l,2-a]pyridin-6-yl) -4H-pyrido[l,2-a]pyrimidin-4- one

117 7-[(3R,5S)-3,5-dimethylpiperazin-l-yl]-2-(2-methylimidazo[l, 2-a]pyridin-6-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

118 2-(6,8-dimethylimidazo[l,2-a]pyrazin-2-yl)-7-(piperazin-l-yl )-4H-pyrido[l,2-a]pyrimidin-4- one

119 2-(6, 8-dimethylimidazo [ 1 ,2-a]pyrazin-2-yl)-7-[(3 S)-3 -methylpiperazin- 1 -yl] -4H-pyrido [1,2- a]pyrimidin-4-one

120 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(piperazin-l-y l)-4H-pyrido[l,2-a]pyrimidin-4- one

121 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(3S)-3-methyl piperazin-l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

122 2-(3,4-dimethoxyphenyl)-7-(2-methylpyridin-4-yl)-4H-pyrido[l ,2-a]pyrimidin-4-one

123 7-(piperazin-l-yl)-2-[2-(trifluoromethyl)imidazo[l,2-a]pyrid in-6-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

124 2-(2-ethylimidazo[l,2-a]pyridin-6-yl)-7-(piperazin-l-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

125 2-(2,3-dimethylimidazo[l,2-a]pyridin-6-yl)-7-(piperazin-l-yl )-4H-pyrido[l,2-a]pyrimidi one

126 2-(3,4-dimethoxyphenyl)-7-[(3aR,6aS)-hexahydropyrrolo[3,4-c] pyrrol-2(lH)-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

127 7-(4-aminopiperidin-l-yl)-2-(3,4-dimethoxyphenyl)-4H-pyrido[ l,2-a]pyrimidin-4-one

128 7-(piperazin-l-yl)-2-(lH-pyrrolo[2,3-b]pyridin-5-yl)-4H-pyri do[l,2-a]pyrimidin-4-one

129 2-(l-methyl-lH-pyrrolo[2,3-b]pyridin-5-yl)-7-(piperazin-l-yl )-4H-pyrido[l,2-a]pyrimidin-4- one

130 7-[(3R,5S)-3,5-dimethylpiperazin-l-yl]-2-(l-methyl-lH-pyrrol o[2,3-b]pyndin-5-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

131 7-[(3R,5S)-3,5-dimethylpiperazin-l-yl]-2-(4,6-dimethylpyrazo lo[l,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

132 7-(l,4-diazepan-l-yl)-2-(4,6-dimethylpyrazolo[l,5-a]pyrazin- 2-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

133 2-(2-methyl-l,3-benzoxazol-6-yl)-7-(piperazin-l-yl)-4H-pyrid o[l,2-a]pyrimidin-4-one

134 2-(2-methyl-l,3-benzoxazol-6-yl)-7-[(3S)-3-methylpiperazin-l -yl]-4H-pyrido[l,2- a]pyrimidin-4-one

135 2-(2-methyl-l,3-benzothiazol-5-yl)-7-[(3S)-3-methylpiperazin -l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

136 2-(2-methyl-l,3-benzothiazol-5-yl)-7-(piperazin-l-yl)-4H-pyr ido[l,2-a]pyrimidin-4-one

137 2-(2-methyl-2H-indazol-5-yl)-7-(piperazin-l-yl)-4H-pyrido[l, 2-a]pyrimidin-4-one Cpd Name

138 2-(2-methyl-2H-indazol-5-yl)-7-[(3S)-3-methylpiperazin-l-yl] -4H-pyrido[l,2-a]pyrimii one

139 2-(3-fluoro-5-methoxyphenyl)-7-(piperazin-l-yl)-4H-pyrido[l, 2-a]pyrimidin-4-one

140 2-(3-fluoro-5-methoxyphenyl)-7-[(3S)-3-methylpiperazin-l-yl] -4H-pyrido[l,2-a]pyrimidin-4- one

141 2-(2,8-dimethylimidazo[l,2-a]pyridin-6-yl)-7-(pi

one

142 2-(3,4-dimethoxyphenyl)-9-methyl-7-[(3S)-3-methylpiperazin-l -yl]-4H-pyrido[l,2- a]pyrimidin-4-one

143 2-(3,4-dimethoxyphenyl)-7-(l,2,3,6 etrahydropyridin-4-yl)-4H-pyrido[l,2-a]pyrimidin-4-one

144 2-(3,4-dimethoxyphenyl)-7-(piperidin-4-yl)-4H-pyrido[l,2-a]p yrimidin-4-one

145 2-(3-fluoro-4,5-dimethoxyphenyl)-7-(piperazin-l-yl)-4H-pyrid o[l,2-a]pyrimidin-4-one

146 2-(3,4-dimethoxyphenyl)-7-(4-hydroxypiperazin-l-yl)-4H-pyrid o[l,2-a]pyrimidin-4-one

147 2-(3,4-dimethoxyphenyl)-7-[(3S)-3-(dimethylamino)pyrrolidin- l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

148 2-(3,4-dimethoxyphenyl)-7-[4-(dimethylamin^

one

149 2-(4-methoxy-3-methylphenyl)-7-(piperazin-l-yl)-4H-pyrido[l, 2-a]pyrimidin-4-one

150 3-[4-oxo-7-(piperazin-l-yl)-4H-pyrido[l,2-a]pyrimidin-2-yl]b enzonitrile

151 2-methoxy-5-[4-oxo-7-(piperazin-l-yl)-4H-pyrido[l,2-a]pyrimi din-2-yl]benzonitrile

152 2-(3-fluoro-4-hydroxyphenyl)-7-(piperazin-l-yl)-4H-pyrido[l, 2-a]pyrimidin-4-one

153 2-(4-ethoxy-3 -fluorophenyl)-7-(piperazin- 1 -yl)-4H-pyrido [ 1 ,2-a]pyrimidin-4-one

154 2-[3-fluoro-4-(2,2,2 rifluoroethoxy)phenyl]-7-(piperazin-l-yl)-4H-pyrido[l,2-a]py rimidin-4- one

155 2-(2-methyl-l,3-benzoxazol-5-yl)-7-(piperazin-l-yl)-4H-pyrid o[l,2-a]pyrimidin-4-one

156 2-(2-methyl-l,3-benzoxazol-5-yl)-7-[(3S)-3-methylpiperazin-l -yl]-4H-pyrido[l,2- a]pyrimidin-4-one

157 2-(3-fluoro-4-methylphenyl)-7-(piperazin-l-yl)-4H-pyrido[l,2 -a]pyrimidin-4-one

158 2-(3-fluoro-4-methylphenyl)-7-[(3S)-3-methylpiperazin-l-yl]- 4H-pyrido[l,2-a]pyrimidin-4- one

159 7-[(3S)-3-aminopyrrolidin-l-yl]-2-(3,4-dimethoxyphenyl)-4H-p yrido[l,2-a]pyrimidin-4-one

160 2-(3,4-dimethoxyphenyl)-9-methyl-7-(piperazin-l-yl)-4H-pyrid o[l,2-a]pyrimidin-4-one

161 7-(l,4-diazepan-l-yl)-2-(2-methyl-l,3-benzothiazol-5-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

162 7-[(3S)-3-methylpiperazin-l-yl]-2-(4-methyl-l,3 hiazol-2-yl)-4H-pyrido[l,2-a]pyrimidin-4- one

163 2-(4-methyl-l,3-thiazol-2-yl)-7-(piperazin-l-yl)-4H-pyrido[l ,2-a]pyrimidin-4-one

164 2-(3,4-dimethoxyphenyl)-7-(l-methylpiperidin-4-yl)-4H-pyrido [l,2-a]pyrimidin-4-one Cpd Name

165 2-(3 ,4-dimethoxyphenyl)-7-[(3 S)-3 -(propan-2-ylamino)pyrrolidin- 1 -yl] -4H-pyrido [1,2- a]pyrimidin-4-one

166 2-(3 -fluoro-4-methoxyphenyl)-7-(4-methyl- 1 ,4-diazepan- 1 -yl)-4H-pyrido [ 1 ,2-a]pyrimidin-4- one

167 2-(4-methoxy-3-nitrophenyl)-7-(piperazin-l-yl)-4H-pyrido[l,2 -a]pyrimidin-4-one

168 2-[3-fluoro-4-(methylsulfanyl)phenyl]-7-(piperazin-l-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

169 7-(4-methyl- 1 ,4-diazepan- 1 -yl)-2-(2-methylimidazo [ 1 ,2-a]pyridin-6-yl)-4H-pyrido [1,2- a]pyrimidin-4-one

170 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(4-methylpiper azin-l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

171 2-(2-methyl-l,3-benzoxazol-6-yl)-7-(4-methylpiperazin-l-yl)- 4H-pyrido[l,2-a]pyrimidin-4- one

172 7-[(3R,5S)-3,5-dimethylpiperazin-l-yl]-2-(2-methyl-l,3-benzo xazol-6-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

173 2-(5-fluoro-6-methoxypyridin-3-yl)-7-[(3S)-3-methylpiperazin -l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

174 7-[(3R,5S)-3,5-dimethylpiperazin-l-yl]-2-(5-fluoro-6-methoxy pyridin-3-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

175 7-[(3R,5S)-3,5-dimethylpiperazin-l-yl]-2-(2-methyl-l,3-benzo thiazol-5-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

176 2-(2-methyl-l,3-benzothiazol-5-yl)-7-(4-methylpiperazin-l-yl )-4H-pyrido[l,2-a]pyrimidin-4- one

177 2-(2-methyl-l,3-benzothiazol-5-yl)-7-(4-methyl-l,4-diazepan- l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

178 7-[(8aS)-hexahydropyrrolo[l,2-a]pyrazin-2(lH)-yl]-2-(2-methy l-l,3-benzothiazol-5-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

179 2-(4-methyl-lH-imidazol-l-yl)-7-(piperazin-l-yl)-4H-pyrido[l ,2-a]pyrimidin-4-one

180 2-(4-methyl-lH-imidazol-l-yl)-7-[(3S)-3-methylpiperazin-l-yl ]-4H-pyrido[l,2-a]pyrimidin-4^ one

181 2-(3,4-dimethoxyphenyl)-7-{[2-(methylamino)ethyl]amino}-4H-p yrido[l,2-a]pyrimidin-4-one

182 2-(5-fluoro-6-methoxypyridin-3-yl)-7-(piperazin-l-yl)-4H-pyr ido[l,2-a]pyrimidin-4-one

183 2-(3,5-difluoro-4-methoxyphenyl)-7-(piperazin-l-yl)-4H-pyrid o[l,2-a]pyrimidin-4-one

184 2-(3 , 5 -difluoro-4-methoxyphenyl)-7- [(3 S)-3 -methylpiperazin- 1 -yl] -4H-pyrido [1,2- a]pyrimidin-4-one

185 7-[4-(dimethylamino)piperidin-l-yl]-2-(3-fluoro-4-methoxyphe nyl)-4H-pyrido[l,2- a]pyrimidin-4-one

186 2-(3-fluoro-4-methoxyphenyl)-7-(l,2,3,6-tetrahydropyridin-4- yl)-4H-pyrido[l,2-a]pyrimidin- 4-one

187 2-(3,4-dimethoxyphenyl)-7-(piperidin-4-ylamino)-4H-pyrido[l, 2-a]pyrimidin-4-one Cpd Name

188 2-(3,4-dimethoxyphenyl)-7-(l-methyl-l,2,3,6 etrahydropyridin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

189 2-(3-chloro-5-fluorophenyl)-7-[(3S)-3-methylpiperazin-l-yl]- 4H-pyrido[l,2-a]pyrimidin-4- one

190 2-(3-chloro-5-fluorophenyl)-7-(piperazin-l-yl)-4H-pyrido[l,2 -a]pyrimidin-4-one

191 7-[(3S)-3-methylpiperazin-l-yl]-2-(l-methyl-lH-pyrazol-4-yl) -4H-pyrido[l,2-a]pyrimidin-4- one

192 2-(l-methyl-lH-pyrazol-4-yl)-7-(piperazin-l-yl)-4H-pyrido[l, 2-a]pyrimidin-4-one

193 2-(2-methyl- 1 ,3 -benzoxazol-6-yl)-7- [(3R)-3 -methylpiperazin- 1 -yl] -4H-pyrido [1,2- a]pyrimidin-4-one

194 7-(3,3-dimethylpiperazin-l-yl)-2-(2-methyl-l,3-benzoxazol-6- yl)-4H-pyrido[l,2-a]pyrimidin- 4-one

195 7-(l,4-diazepan-l-yl)-2-(2-methyl-l,3-benzoxazol-6-yl)-4H-py rido[l,2-a]pyrimidin-4-one

196 2-(2-methyl-l,3-benzoxazol-6-yl)-7-(4-methyl-l,4-diazepan-l- yl)-4H-pyrido[l,2-a]pyrimidin- 4-one

197 7-[(8aS)-hexahydropyrrolo[l,2-a]pyrazin-2(lH)-yl]-2-(2-methy l-l,3-benzoxazol-6-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

198 7-[(8aR)-hexahydropyrrolo[l,2-a]pyrazin-2(lH)-yl]-2-(2-methy l-l,3-benzoxazol-6-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

199 2-(4,5-dimethoxypyridin-2-yl)-7-(piperazin-l-yl)-4H-pyrido[l ,2-a]pyrimidin-4-one

200 7-[3-(dimethylamino)pyrrolidin-l-yl]-2-(3-fluoro-4-methoxyph enyl)-4H-quinolizin-4-one

201 7-(4-aminopiperidin-l-yl)-2-(3-fluoro-4-methoxyphenyl)-4H-qu inolizin-4-one

202 7-(4-ethylpiperazin-l-yl)-2-(2-methyl-l,3-benzoxazol-6-yl)-4 H-pyrido[l,2-a]pyrimidin-4-one 203 ¹ 7-[4-(dimethylamino)piperidin-l-yl]-2-(3-fluoro-4-methoxyphe nyl)-4H-quinolizin-4-one

204 2-(3-fluoro-4-methoxyphenyl)-7-(l-methyl-l,2,3,6-tetrahydrop yridin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

205 7-[(3S)-3 -(dimethyl amino)pyrrolidin- 1 -yl] -2-(3 -fluoro-4-methoxyphenyl)-4H-pyrido [1,2- a]pyrimidin-4-one

206 7-[(3R,4R)-3-(dimethylamino)-4-hydroxypyrrolidin-l-yl]-2-(3- fluoro-4-methoxyphenyl)-4H- pyrido[l,2-a]pyrimidin-4-one

207 7-(4-aminopiperidin- 1 -yl)-2-(3 -fluoro-4-methoxyphenyl)-4H-pyrido [ 1 ,2-a]pyrimidin-4-one

208 2-(3-fluoro-4-methoxyphenyl)-7-[4-(methylamino)piperidin-l-y l]-4H-pyrido[l,2-a]pyrimidi 4-one

209 2-(8-fluoro-2-methylimidazo [ 1 ,2-a]pyridin-6-yl)-7-(piperazin- 1 -yl)-4H-pyrido [1,2- a]pyrimidin-4-one

210 7-[(3R,5S)-3,5-dimethylpiperazin-l-yl]-2-(8-fluoro-2-methyli midazo[l,2-a]pyridin-6-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

211 2-(8-fluoro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-(4-methyl- l,4-diazepan-l-yl)-4H- pyrido[l,2-a]pyrimidin-4-one Cpd Name

212 2-(3-fluoro-4-methoxyphenyl)-7-[(3aR,6aS)-hexahydropyrrolo[3 ,4-c]pyrrol-2(lH)-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

213 2-(3-fluoro-4-methoxyphenyl)-7-[(3aR,6aS)-5-methylhexahydrop yrrolo[3,4-c]pyrrol-2(lH)- yl]-4H-pyrido[l,2-a]pyrimidin-4-one

214 2-(3,4-dimethoxyphenyl)-7-[l-(2-hydroxyethyl)piperidin-4-yl] -4H-pyrido[l,2-a]pyrimidin-4- one

215 2-(4-fluoro-3-methoxyphenyl)-7-[(3S)-3-methylpiperazin-l-yl] -4H-pyrido[l,2-a]pyrimidin-4- one

216 2-(4-fluoro-3-methoxyphenyl)-7-(piperazin-l-yl)-4H-pyrido[l, 2-a]pyrimidin-4-one

217 2-(3,4-difluoro-5-methoxyphenyl)-7-[(3S)-3-methylpiperazin-l -yl]-4H-pyrido[l,2- a]pyrimidin-4-one

218 2-(3,4-difluoro-5-methoxyphenyl)-7-(piperazin-l-yl)-4H-pyrid o[l,2-a]pyrimidin-4-one

219 2-(2-methyl-l,3-benzothiazol-6-yl)-7-(piperazin-l-yl)-4H-pyr ido[l,2-a]pyrimidin-4-one

220 7-(3-fluoro-4-methoxyphenyl)-2-(piperazin-l-yl)-4H-pyrido[l, 2-a]pyrimidin-4-one

221 2-(2-methyl-l,3-benzothiazol-6-yl)-7-[(3S)-3-methylpiperazin -l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

222 2-(3-fluoro-4-methoxyphenyl)-7-[(3S)-3-(methylamino)pyrrolid in-l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

223 2-(3-fluoro-4-methoxyphenyl)-7-{4-[(methylamm^

a]pyrimidin-4-one

224 7-[(3S)-3-aminopyrrolidin-l-yl]-2-(3-fluoro-4-methoxyphenyl) -4H-pyrido[l,2-a]pyrimidin-4- one

225 2-(3 -fluoro-4-methoxyphenyl)-7- { [(3R)- 1 -methylpyrrolidin-3 -yl] amino } -4H-pyrido [1,2- a]pyrimidin-4-one

226 7-{4-[(dimethylamino)methyl]piperidin-l-yl}-2-(3-fluoro-4-me thoxyphenyl)-4H-pyrido[l,2- a]pyrimidin-4-one

227 2-(6-methoxypyridin-2-yl)-7-(piperazin-l-yl)-4H-pyrido[l,2-a ]pyrimidin-4-one

228 7-(piperazin-l-yl)-2-(pyridin-3-yl)-4H-pyrido[l,2-a]pyrimidi n-4-one

229 2-(5-methoxypyridin-3-yl)-7-(piperazin-l-yl)-4H-pyrido[l,2-a ]pyrimidin-4-one

230 3-fluoro-5-{7-[(3S)-3-methylpiperazin-l-yl]-4-oxo-4H-pyrido[ l,2-a]pyrimidin-2- yljbenzonitrile

231 3-fluoro-5-[4-oxo-7-(piperazin-l-yl)-4H-pyrido[l,2-a]pyrimid in-2-yl]benzonitrile

232 2-(3-fluoro-4-methoxyphenyl)-7-[(3'S,4'S)-4'-hydroxy-l,3'-bi pyrrolidin-r-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

233 2-(3-fluoro-4-methoxyphenyl)-7-{methyl[(3R)-pyrrolidin-3-yl] amino}-4H-pyrido[l,2- a]pyrimidin-4-one

234 7-[(3S)-3,4-dimethylpiperazin-l-yl]-2-(2-methyl-l,3-benzoxaz ol-6-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

235 2-(3,4-dimethoxyphenyl)-7-[(l-methylpiperidin-4-yl)oxy]-4H-p yrido[l,2-a]pyrimidin-4-one Cpd Name

236 2-(3,4-dimethoxyphenyl)-7-[(3S)-pyrrolidin-3-yloxy]-4H-pyrid o[l,2-a]pyrimidin-4-one

237 2-(3,4-dimethoxyphenyl)-7-(piperidin-4-yloxy)-4H-pyrido[l,2- a]pyrimidin-4-one

238 7-(l,4-diazepan-l-yl)-2-(3,4-dimethoxyphenyl)-9-methyl-4H-py rido[l,2-a]pyrimidin-4-one

239 2-(3-fluoro-4-methoxyphenyl)-7-{methyl[(3R)-l-methylpyrrolid in-3-yl]amino}-4H- pyrido[l,2-a]pyrimidin-4-one

240 7-[4-(dimethylamino)piperidin-l-yl]-2-(2-methyl-l,3-benzoxaz ol-6-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

241 7-[(3S)-3-(dimethylamino)pyrrolidin-l-yl]-2-(2-methyl-l,3-be nzoxazol-6-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

242 7-(4-aminopiperidin-l-yl)-2-(2-methyl-l,3-benzoxazol-6-yl)-4 H-pyrido[l,2-a]pyrimidin-4-one

243 7-[(3aR,6aS)-hexahydropyrrolo[3,4-c]pyrrol-2(lH)-yl]-2-(2-me thyl-l,3-benzoxazol-6-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

244 7-[(3R)-3,4-dimethylpiperazin-l-yl]-2-(2-methyl-l,3-benzoxaz ol-6-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

245 2-(3,4-dimethoxyphenyl)-7-(l,2,3,6-tetrahydropyridin-4-yl)-4 H-quinolizin-4-one

246 2-(3-fluoro-4-methoxyphenyl)-7-[(3aR,6aR)-l-methylhexahydrop yrrolo[3,4-b]pyrrol-5(lH)- yl]-4H-pyrido[l,2-a]pyrimidin-4-one

247 2-(3,4-dimethoxyphenyl)-9-methyl-7-(l,2,3,6-tetrahydropyridi n-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

248 2-(3,4-dimethoxyphenyl)-7-[l-(2-hydroxyethyl)-l,2,3,6-tetrah ydropyridin-4-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

249 2-(3,4-dimethoxyphenyl)-7-(l-methyl-l,2,3,6 etrahydropyridin-4-yl)-4H-quinolizin-4-one

250 2-(3,4-dimethoxyphenyl)-9-methyl-7-(piperidin-4-yl)-4H-pyrid o[l,2-a]pyrimidin-4-one

251 2-(3,4-dimethoxyphenyl)-9-methyl-7-(l-methyl-l,2,3,6-tetrahy dropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

252 2-(3,4-dimethoxyphenyl)-9-methyl-7-(l-methylpiperidin-4-yl)- 4H-pyrido[l,2-a]pyrimidm one

253 7-(l,4-diazepan-l-yl)-2-(2-methyl-l,3-benzothiazol-6-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

254 2-(2-methyl- 1 ,3 -benzothiazol-6-yl)-7-(4-methyl-l ,4-diazepan-l -yl)-4H-pyrido[ 1 ,2- a]pyrimidin-4-one

255 7-[(8aS)-hexahydropyrrolo[l,2-a]pyrazin-2(lH)-yl]-2-(2-methy l-l,3-benzothiazol-6-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

256 2-(2-methyl-l,3-benzothiazol-6-yl)-7-(4-methylpiperazin-l-yl )-4H-pyrido[l,2-a]pyrimidin-4- one

257 2-(3,4-dimethoxyphenyl)-7-[(3aR,6aS)-hexahydropyrrolo[3,4-c] pyrrol-2(lH)-yl]-9-methyl- 4H-pyrido[l,2-a]pyrimidin-4-one

258 7-[(3S)-3,4-dimethylpiperazin-l-yl]-2-(4,6-dimethylpyrazolo[ l,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one Cpd Name

259 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(3R,5S)-3,4,5 rimethylpiperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

260 2-(3,4-dimethoxyphenyl)-9-methyl-7-[(3aR,6aS)-5-methylhexahy dropyrrolo[3,4-c]pyrrol- 2(lH)-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

261 2-(3,4-dimethoxyphenyl)-7-[4-(dimethylamino)piperidin-l-yl]- 9-methyl-4H-pyrido[l,^

a]pyrimidin-4-one

262 7-[(lR,5S)-8-azabicyclo[3.2.1]oct-2-en-3-yl]-2-(3,4-dimethox yphenyl)-4H-pyndo[l,2- a]pyrimidin-4-one

263 2-(3,4-dimethoxyphenyl)-7-(l,2,5,6 etrahydropyridin-3-yl)-4H-pyrido[l,2-a]pyrimidin-4-one

264 7-[(3R)-3-(dimethylamino)pyrrolidin-l-yl]-2-(2-methyl-l,3-be nzoxazol-6-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

265 2-(2-ethyl- 1 ,3 -benzoxazol-6-yl)-7-(piperazin- 1 -yl)-4H-pyrido [ 1 ,2-a]pyrimidin-4-one

266 2-(2-ethyl-l,3-benzoxazol-6-yl)-7-[(3S)-3-methylpiperazin-l- yl]-4H-pyrido[l,2-a]pyrimidin- 4-one

267 2-(2-methyl-l,3-benzoxazol-6-yl)-7-[(3aR,6aS)-5-methylhexahy dropyrrolo[3,4-c]pyrrol- 2(lH)-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

268 7-(8-fluoro-2-methylimidazo [ 1 ,2-a]pyridin-6-yl)-2-(piperazin- 1 -yl)-4H-pyrido [1,2- a]pyrimidin-4-one

269 2-(8-fluoro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-(4-methylp iperazin-l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

270 2-(8-fluoro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3R)-3-me thylpiperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

271 2-(8-fluoro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(8aS)-hex ahydropyrrolo[l,2-a]pyrazin- 2(lH)-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

272 2-(8-fluoro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(8aR)-hex ahydropyrrolo[l,2-a]pyrazin- 2(lH)-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

273 7-(4-aminopiperidin-l-yl)-2-(8-fluoro-2-methylimidazo[l,2-a] pyridin-6-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

274 7-[(3R)-3-(dimethylamino)pyrrolidin-l-yl]-2-(8-fl^

4H-pyrido[l,2-a]pyrimidin-4-one

275 7-[(3S)-3-(dimethylamino)pyrrolidin-l-yl]-2-(8-fluoro-2-meth ylimidazo[l,2-a]pyridin-6-yl^ 4H-pyrido[l,2-a]pyrimidin-4-one

276 2-(4-aminopiperidin- 1 -yl)-7-(3 -fluoro-4-methoxyphenyl)-4H-pyrido [ 1 ,2-a]pyrimidin-4-one

277 2-[(3S)-3 -(dimethyl amino)pyrrolidin- 1 -yl] -7-(3 -fluoro-4-methoxyphenyl)-4H-pyrido [1,2- a]pyrimidin-4-one

278 2-[(3R)-3 -(dimethyl amino)pyrrolidin- 1 -yl] -7-(3 -fluoro-4-methoxyphenyl)-4H-pyrido [1,2- a]pyrimidin-4-one

279 2-(3-fluoro-4-methoxyphenyl)-7-[(3aR,6aS)-5-(2-hydroxyethyl) hexahydropyrrolo[3,4- c]pyrrol-2(lH)-yl]-4H-pyrido[l,2-a]pyrimidin-4-one Cpd Name

280 2-(3-fluoro-4-methoxyphenyl)-7-[(3aS,6aS)-l-methylhexahydrop yrrolo[3,4-b]pyrrol-5(lH)- yl]-4H-pyrido[l,2-a]pyrimidin-4-one

281 2-(3-fluoro-4-methoxyphenyl)-7-[(3aR,6aS)-5-(propan-2-yl)hex ahydropyrrolo[3,4-c]pyrrol- 2(lH)-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

282 7-[(3R)-3 -(dimethyl amino)pyrrolidin- 1 -yl] -2-(3 -fluoro-4-methoxyphenyl)-4H-pyrido [1,2- a]pyrimidin-4-one

283 7-(3,3-dimethylpiperazin-l-yl)-2-(2-methyl-l,3-benzothiazol- 6-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

284 7-[(8aR)-hexahydropyrrolo[l,2-a]pyrazin-2(lH)-yl]-2-(2-methy l-l,3-benzothiazol-6-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

285 7-[4-(dimethylamino)piperidin-l-yl]-2-(2-methyl-l,3-benzothi azol-6-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

286 2-(2-methyl-l,3-benzothiazol-6-yl)-7-(piperidin-4-yloxy)-4H- pyrido[l,2-a]pyrimidin-4-one

287 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-(piperazin -l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

288 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3R,5S)-3 ,5-dimethylpiperazin-l-yl]-4H^ pyrido[l,2-a]pyrimidin-4-one

289 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-(4-methyl- l,4-diazepan-l-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

290 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3R)-3-me thylpiperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

291 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3S)-3-me thylpiperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

292 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(8aR)-hex ahydropyrrolo[l,2-a]pyrazin- 2(lH)-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

293 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(8aS)-hex ahydropyrrolo[l,2-a]pyrazin- 2(lH)-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

294 7-(3-fluoro-4-methoxyphenyl)-2-(l,2,3,6 etrahydropyridin-4-yl)-4H-pyrido[l,2-a]pyrimidin- 4-one

295 7-[(3S)-3,4-dimethylpiperazin-l-yl]-2-(8-fluoro-2-methylimid azo[l,2-a]pyridin-6-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

296 7-[(3R)-3,4-dimethylpiperazin-l-yl]-2-(8-fluoro-2-methylimid azo[l,2-a]pyridin-6-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

297 7-[4-(dimethylamino)piperidin-l-yl]-2-(8-fluoro-2-methylimid azo[l,2-a]pyridin-6-yl)-4H^ pyrido[l,2-a]pyrimidin-4-one

298 2-[4-(dimethylamino)piperidin-l-yl]-7-(3-fluoro-4-methoxyphe nyl)-4H-pyrido[l,2- a]pyrimidin-4-one

299 2-(4-fluoro-2-methyl-l,3-benzoxazol-6-yl)-7-(l,2,3,6-tetrahy dropyridin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

300 2-(4-fluoro-2-methyl-l,3-benzoxazol-6-yl)-7-(l-methyl-l,2,3, 6 etrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one Cpd Name

301 2-(3-fluoro-4-methoxyphenyl)-7-[(4aR,7aR)-octahydro-6H-pyrro lo[3,4-b]pyridin-6-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

302 2-(2-methyl-l,3-benzoxazol-6-yl)-7-(l,2,3,6-tetrahydropyridi n-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

303 2-(2-methyl-l,3-benzoxazol-6-yl)-7-(l-methyl-l,2,3,6 etrahydropyridin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

304 7-(l-ethyl-l,2,3,6 etrahydropyridin-4-yl)-2-(2-methyl-l,3-benzoxazol-6-yl)-4H-p yrido[l,2- a]pyrimidin-4-one

305 2-(4-fluoro-2-methyl-l,3-benzoxazol-6-yl)-7-(piperazin-l-yl) -4H-pyrido[l,2-a]pyrimidin-4- one

306 2-(4-fluoro-2-methyl-l,3-benzoxazol-6-yl)-7-[(3S)-3-methylpi perazin-l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

307 7-[(3S)-3,4-dimethylpiperazin-l-yl]-2-(4-fluoro-2-methyl-l,3 -benzoxazol-6-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

308 2-(4-fluoro-2-methyl-l,3-benzoxazol-6-yl)-7-(4-methylpiperaz in-l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

309 7-(4-ethylpiperazin-l-yl)-2-(4-fluoro-2-methyl-l,3-benzoxazo l-6-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

310 2-(4-fluoro-2-methyl-l,3-benzoxazol-6-yl)-7-(4-propylpiperaz in-l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

311 7-[(3aR,6aS)-5-ethylhexahydropyrrolo[3,4-c]pyrrol-2(lH)-yl]- 2-(3-fluoro-4-methoxyphenyl)- 4H-pyrido[l,2-a]pyrimidin-4-one

312 2-(3-fluoro-4-methoxyphenyl)-9-methyl-7-(l,2,3,6-tetrahydrop yridin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

313 2-(3-fluoro-4-methoxyphenyl)-7-[(4aR,7aR)-l-methyloctahydro- 6H-pyrrolo[3,4-b]pyridin-6- yl]-4H-pyrido[l,2-a]pyrimidin-4-one

314 2-(3,4-dimethoxyphenyl)-9-methyl-7-[(3R)-3-methylpiperazin-l -yl]-4H-pyrido[l,2- a]pyrimidin-4-one

315 2-(3-fluoro-4-methoxyphenyl)-9-methyl-7-(l-methyl-l,2,3,6-te trahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

316 7-(3-fluoro-4-methoxyphenyl)-2-(piperidin-4-yl)-4H-pyrido[l, 2-a]pyrimidin-4-one

317 7-(3-fluoro-4-methoxyphenyl)-2-(l-methylpiperidin-4-yl)-4H-p yrido[l,2-a]pyrimidin-4-one

318 7-(l-ethyl-l,2,3,6-tetrahydropyridin-4-yl)-2-(4-fluoro-2-met hyl-l,3-benzoxazol-6-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

319 2-(4-fluoro-2-methyl-l,3-benzoxazol-6-yl)-7-(l-propyl-l,2,3, 6-tetrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

320 2-(3,4-dimethoxyphenyl)-7-[(lR,5S)-8-methyl-8-azabicyclo[3.2 .1]oct-3-yl]-4H-pyndo[l,2- a]pyrimidin-4-one

321 2-(3,4-dimethoxyphenyl)-7-[(2R)-2-methylpiperazin-l-yl]-4H-p yrido[l,2-a]pyrimidin-4-one

322 2-(2-methyl- 1 ,3 -benzoxazol-6-yl)-7- [(3 S)-3 -methylpiperazin- 1 -yl] -4H-quinolizin-4-one Cpd Name

323 2-(2-methyl-l,3-benzoxazol-6-yl)-7-(4-methylpiperazin-l-yl)- 4H-quinolizin-4-one

324 7-[(3S)-4-ethyl-3-methylpiperazin-l-yl]-2-(2-methyl-l,3-benz oxazol-6-yl)-4H-quinolizin-4- one

325 7-[(3S)-3,4-dimethylpiperazin-l-yl]-2-(2-methyl-l,3-benzoxaz ol-6-yl)-4H-quinolizin-4-one

326 7-(4-aminopiperidin-l-yl)-2-(2-methyl-l,3-benzoxazol-6-yl)-4 H-quinolizin-4-one

327 2-(3-fluoro-4-methoxyphenyl)-9-methyl-7-[(3S)-3-methylpipera zin-l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

328 7-[4-(dimethylamino)piperidin-l-yl]-2-(3-fluoro-4-methoxyphe nyl)-9-methyl-4H-pyrid

a]pyrimidin-4-one

329 2-(3-fluoro-4-methoxyphenyl)-9-methyl-7-(l-methylpiperidin-4 -yl)-4H-pyrido[l,2- a]pyrimidin-4-one

330 7-[4-(cyclopropylamino)piperidin-l-yl]-2-(3,4-dimethoxypheny l)-9-methyl-4H-pyrido[l,2- a]pyrimidin-4-one

331 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3S)-3,4- dimethylpiperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

332 2-(3,4-dimethoxyphenyl)-7-[(3R,5S)-3,5-dimethylpiperazin-l-y l]-9-methyl-4H-pyrido[l,2- a]pyrimidin-4-one

333 2-(3,4-dimethoxyphenyl)-7-[(3R)-3,4-dimethylpiperazin-l-yl]- 9-methyl-4H-pyrido[l,2- a]pyrimidin-4-one

334 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(4-methyl-l,4- diazepan-l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

335 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(3R)-3-methyl piperazin-l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

336 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(8aS)-hexahyd ropyrrolo[l,2-a]pyrazin-2(lH)- yl]-4H-pyrido[l,2-a]pyrimidin-4-one

337 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(8aR)-hexahyd ropyrrolo[l,2-a]pyrazin-2(lH)- yl]-4H-pyrido[l,2-a]pyrimidin-4-one

338 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(4-ethylpipera zin-l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

339 7-[4-(dimethylamino)piperidin-l-yl]-2-(4,6-dimethylpyrazolo[ l,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

340 7-(3,3-dimethylpiperazin-l-yl)-2-(4,6-dimethylpyrazolo[l,5-a ]pyrazin-2-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

341 7-(4-cyclopropylpiperazin-l-yl)-2-(4,6-dimethylpyrazolo[l,5- a]pyrazin-2-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

342 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l,2,3,6-tetra hydropyridin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

343 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(3R)-4-ethyl- 3-methylpiperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one Cpd Name

344 2-(3,4-dimethoxyphenyl)-9-methyl-7-(4-methylpiperazin-l-yl)- 4H-pyrido[l,2-a]pyrimi

one

345 2-(3,4-dimethoxyphenyl)-7-[4-(dimethylamino)piperidin-l-yl]- 9-ethyl-4H-pyrido[l,2- a]pyrimidin-4-one

346 2-(3,4-dimethoxyphenyl)-7-[l-(2-hydroxyethyl)-l,2,3,6 etrahydropyridin-4-yl]-9-methyl-4H- pyrido[l,2-a]pyrimidin-4-one

347 7-[4-(dimethylamino)piperidin-l-yl]-2-(2-methyl-l,3-benzothi azol-5-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

348 7-(4-aminopiperidin-l-yl)-2-(2-methyl-l,3-benzothiazol-5-yl) -4H-pyrido[l,2-a]pyrimidin-4 one

349 7-[(3aR,6aS)-hexahydropyrrolo[3,4-c]pyrrol-2(lH)-yl]-2-(2-me thyl-l,3-benzothiazol-5-yl)- 4H-pyrido[l,2-a]pyrimidin-4-one

350 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l-methyl-l,2, 3,6-tetrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

351 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l-ethyl-l,2,3 ,6-tetrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

352 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l-propyl-l,2, 3,6-tetrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

353 2-(3,4-dimethoxyphenyl)-7-(l,2,3,6 etrahydropyridin-4-yl)-4H-pyrimido[l,2-a]pyrimidin-4- one

354 7-(l-cyclopropyl-l,2,3,6-tetrahydropyridin-4-yl)-2-(4,6-dime thylpyrazolo[l,5-a]pyrazin-2-yl)- 4H-pyrido[l,2-a]pyrimidin-4-one

355 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[l-(propan-2-y l)-l,2,3,6-tetrahydropyridin-4- yl]-4H-pyrido[l,2-a]pyrimidin-4-one

356 7-(l-cyclobutyl-l,2,3,6-tetrahydropyridin-4-yl)-2-(4,6-dimet hylpyrazolo[l,5-a]pyrazin-2-yl)- 4H-pyrido[l,2-a]pyrimidin-4-one

357 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[l-(oxetan-3-y l)-l,2,3,6-tetrahydropyridin-4- yl]-4H-pyrido[l,2-a]pyrimidin-4-one

358 2-(3,4-dimethoxyphenyl)-9-methyl-7-[4-(methylamino)piperidin -l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

359 2-(3,4-dimethoxyphenyl)-7-[4-(ethylamino)piperidin-l-yl]-9-m ethyl-4H-pyrido[l,2- a]pyrimidin-4-one

360 2-(3,4-dimethoxyphenyl)-8-methyl-7-(piperazin-l-yl)-4H-pyrid o[l,2-a]pyrimidin-4-one

361 2-(3,4-dimethoxyphenyl)-7-[4-(propan-2-ylamino)piperidin-l-y l]-4H-pyrido[l,2-a]pyrimidin- 4-one

362 7-(l-cyclobutyl-l,2,3,6-tetrahydropyridin-4-yl)-2-(3,4-dimet hoxyphenyl)-4H-pyrido[l,2- a]pyrimidin-4-one

363 2-(3,4-dimethoxyphenyl)-7-[l-(propan-2-yl)-l,2,3,6-tetrahydr opyridin-4-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

364 2-(3,4-dimethoxyphenyl)-7-[l-(oxetan-3-yl)-l,2,3,6-tetrahydr opyridin-4-yl]-4H-pyrido[l,2- a]pyrimidin-4-one Cpd Name

365 2-(3,4-dimethoxyphenyl)-7-(l-propyl-l,2,3,6-tetrahydropyridi n-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

366 2-(3,4-dimethoxyphenyl)-7-[4-(methylamino)cyclohex-l-en-l-yl ]-4H-pyrido[l,2-a]pyrimidin- 4-one

367 2-(3,4-dimethoxyphenyl)-7-[4-(dimethylamino)cyclohex-l-en-l- yl]-4H-pyrido[l,2- a]pyrimidin-4-one

368 2-(3 ,4-dimethoxyphenyl)-7- {4- [ethyl (methyl)amino] cyclohex- 1 -en- 1 -yl } -4H-pyrido [1,2- a]pyrimidin-4-one

369 2-(3 ,4-dimethoxyphenyl)-7- {4- [methyl (propyl)amino] cyclohex- 1 -en- 1 -yl } -4H-pyrido [1,2- a]pyrimidin-4-one

370 2-(3,4-dimethoxyphenyl)-7-(l-ethyl-l,2,3,6-tetrahydropyridin -4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

371 7-(3,4-dimethoxyphenyl)-2-(l,2,3,6-tetrahydropyridin-4-yl)-4 H-pyrido[l,2-a]pyrimidin-4-one

372 7-(8-fluoro-2-methylimidazo[l,2-a]pyridin-6-yl)-2-(l,2,3,6-t etrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

373 2-(8-fluoro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[4-(propan -2-yl)piperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

374 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[4-(propan -2-yl)piperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

375 7-(2-methylimidazo[l,2-a]pyridin-6-yl)-2-(l,2,3,6-tetrahydro pyridin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

376 7-(2-methylimidazo[l,2-a]pyridin-6-yl)-2-(l-methyl-l,2,3,6-t etrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

377 7-(3,4-dimethoxyphenyl)-2-(l-methyl-l,2,3,6-tetrahydropyridi n-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

378 2-(3,4-dimethoxyphenyl)-9-methyl-7-(l-propyl-l,2,3,6-tetrahy dropyridin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

379 7-(l-cyclobutyl-l,2,3,6-tetrahydropyridin-4-yl)-2-(3,4-dimet hoxyphenyl)-9-methyl-4H- pyrido[l,2-a]pyrimidin-4-one

380 ¹ 2-(2-methyl-l,3-benzothiazol-6-yl)-7-(piperidin-4-yl)-4H-pyr imido[l,2-b]pyridazin-4-one

381 7-(4-aminopiperidin-l-yl)-2-(2-methyl-l,3-benzothiazol-6-yl) -4H-pyrido[l,2-a]pyrimidin-4- one

382 7-(3-aminopyrrolidin-l-yl)-2-(2-methyl-l,3-benzothiazol-6-yl )-4H-pyrido[l,2-a]pyrimidin-4- one

383 7-[(3R)-3-(dimethylamino)pyrrolidin-l-yl]-2-(2-methyl-l,3-be nzothiazol-6-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

384 2-(2-methyl-l,3-benzothiazol-6-yl)-7-(l,2,3,6-tetrahydropyri din-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

385 2-(8-fluoro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[4-(2-meth oxyethyl)piperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one Cpd Name

386 2-(3,4-dimethoxyphenyl)-9-methyl-7-[l-(o^

pyrido[l,2-a]pyrimidin-4-one

387 2-(3,4-dimethoxyphenyl)-9-methyl-7-[l-(propan-2-yl)-l,2,3,6 etrahydropyridin-4-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

388 2-(3,4-dimethoxyphenyl)-7-(l-ethyl-l,2,3,6 etrahydropyridin-4-yl)-9-methyl-4H-pyrido[l,^ a]pyrimidin-4-one

389 2-(3,4-dimethoxyphenyl)-8-methyl-7-(l,2,3,6-tetrahydropyridi n-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

390 7-(l-cyclopropyl-l,2,3,6 etrahydropyridin-4-yl)-2-(3,4-dimethoxyphenyl)-9-methyl-4H- pyrido[l,2-a]pyrimidin-4-one

391 2-(3,4-dimethoxyphenyl)-8-methyl-7-(l-methyl-l,2,3,6 etrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

392 2-(2-methyl-l,3-benzothiazol-6-yl)-7-(l-methyl-l,2,3,6-tetra hydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

393 7-[l-(2-hydroxyethyl)-l,2,3,6 etrahydropyridin-4-yl]-2-(2-methyl-l,3-benzothiazol-6-yl)-4H ^ pyrido[l,2-a]pyrimidin-4-one

394 2-(2-methyl-l,3-benzothiazol-6-yl)-7-[l-(propan-2-yl)-l,2,3, 6 etrahydropyridin-4-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

395 7-(l-cyclopropyl-l,2,3,6 etrahydropyridin-4-yl)-2-(2-methyl-l,3-benzothiazol-6-yl)-4H - pyrido[l,2-a]pyrimidin-4-one

396 7-(l-ethyl-l,2,3,6 etrahydropyridin-4-yl)-2-(2-methyl-l,3-benzothiazol-6-yl)-4H -pyrido[l,2- a]pyrimidin-4-one

397 7-[(3R)-3,4-dimethylpiperazin-l-yl]-2-(4,6-dimethylpyrazolo[ l,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

398 2-(3,4-dimethoxyphenyl)-7-(l,2,3,6 etrahydropyridin-4-yl)-4H-pyrimido[l,2-b]pyridazin-4- one

399 7-[(lS,4S)-2,5-diazabicyclo[2.2.1]hept-2-yl]-2-(4,6-dimethyl pyrazolo[l,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

400 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(lS,4S)-5-met hyl-2,5-diazabicyclo[2.2.1]hept- 2-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

401 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(lS,4S)-5-eth yl-2,5-diazabicyclo[2.2 ]hept-2- yl]-4H-pyrido[l,2-a]pyrimidin-4-one

402 2-(3,4-dimethoxyphenyl)-7-(l,2,3,6 etrahydropyridin-4-yl)-4H-pyrazino[l,2-a]pyrimidin-4- one

403 2-(3-fluoro-4-methoxyphenyl)-7-(piperidin-4-yl)-4H-pyrido[l, 2-a]pyrimidin-4-one

404 2-(3,4-dimethoxyphenyl)-7-(l-ethylpiperidin-4-yl)-4H-pyrido[ l,2-a]pyrimidin-4-one

405 2-(3,4-dimethoxyphenyl)-7-[cis-4-(methylamino)cyclohexyl]-4H -pyrido[l,2-a]pyrimidin

one

406 2-(3,4-dimethoxyphenyl)-7-(piperidin-3-yl)-4H-pyrido[l,2-a]p yrimidin-4-one Cpd Name

407 2-(3,4-dimethoxyphenyl)-9-methyl-7-[4-(propylamino)piperidin -l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

408 2-(3,4-dimethoxyphenyl)-9-ethyl-7-(l,2,3,6-tetrahydropyridin -4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

409 7-(2-methylimidazo[l,2-a]pyridin-6-yl)-2-(piperidin-4-yl)-4H -pyrido[l,2-a]pyrimidin-4-on^

410 7-(8-fluoro-2-methylimidazo[l,2-a]pyridin-6-yl)-2-(piperidin -4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

411 7-(8-fluoro-2-methylimidazo[l,2-a]pyridin-6-yl)-2^

4H-pyrido[l,2-a]pyrimidin-4-one

412 7-(4-cyclopropylpiperazin-l-yl)-2-(8-fluoro-2-methylimidazo[ l,2-a]pyridin-6-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

413 ¹ 2-(l,3-dimethylpyrrolo[l,2-a]pyrazin-7-yl)-7-(l,2,3,6-tetrah ydropyridin-4-yl)-4H- pyrazino[l,2-a]pyrimidin-4-one

414 2-(3,4-dimethoxyphenyl)-7-[(8aR)-hexahydropyrrolo[l,2-a]pyra zin-2(lH)-yl]-9-methyl-4H- pyrido[l,2-a]pyrimidin-4-one

415 2-(3,4-dimethoxyphenyl)-9-ethyl-7-(l-methyl-l,2,3,6 etrahydropyridin-4-yl)-4H-pyrido[l,2 a]pyrimidin-4-one

416 2-(3,4-dimethoxyphenyl)-9-methyl-7-[4-(propan-2-ylamino)pipe ridin-l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

417 2-(3,4-dimethoxyphenyl)-7-[(8aS)-hexahydropyrrolo[l,2-a]pyra zin-2(lH)-yl]-9-methyl-4H- pyrido[l,2-a]pyrimidin-4-one

418 2-(3,4-dimethoxyphenyl)-9-ethyl-7-(l-ethyl-l,2,3,6 etrahydropyridin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

419 2-(3,4-dimethoxyphenyl)-9-methyl-7-[4-(moφholin-4-yl)piperi din-l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

420 2-(6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(piperazin-l-yl)-4 H-pyrido[l,2-a]pyrimidin-4-one

421 2-(2-methyl-l,3-benzoxazol-6-yl)-7-(l,2,3,6-tetrahydropyridi n-4-yl)-4H-pyrazino[l,2- a]pyrimidin-4-one hydrochloride (1 : 1)

422 2-(2-methyl-l,3-benzoxazol-6-yl)-7-(l-methyl-l,2,3,6-tetrahy dropyridin-4-yl)-4H- pyrazino[l,2-a]pyrimidin-4-one

423 7-(l -ethyl-l,2,3,6-tetrahydropyridin-4-yl)-2-(2-methyl-l,3-benzo xazol-6-yl)-4H-pyrazino[l,2- a]pyrimidin-4-one

424 2-(2-methyl-l,3-benzothiazol-6-yl)-7-(piperidin-4-yl)-4H-pyr ido[l,2-a]pyrimidin-4-one

425 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[4-(pyrrolidin -l-yl)piperidin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

426 7-(l,4'-bipiperidin- -yl)-2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-4H-pyrido[l ,2- a]pyrimidin-4-one

427 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[4-(4-methylpi perazin-l-yl)piperidin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one Cpd Name

428 2-(4,6-dimethyl yrazolo[l,5-a] yrazin-2-yl)-7-[4-(moφholin-4-yl) i eridin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

429 2-(2-methylimidazo[l,2-a]pyridin-6-yl)-7-(l,2,3,6-tetrahydro pyridin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

430 2-(2-methylimidazo[l,2-a]pyridin-6-yl)-7-(l-methyl-l,2,3,64e trahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

431 7-(l-ethyl-l,2,3,6 etrahydropyridin-4-yl)-2-(2-methylimidazo[l,2-a]pyridin-6-yl )-4H- pyrido[l,2-a]pyrimidin-4-one

432 7-[4-(dimethylamino)piperidin-l-yl]-2-(2-methylimidazo[l,2-a ]pyridin-6-yl)-4H^yrido

a]pyrimidin-4-one

433 2-(3,4-dimethoxyphenyl)-7-{4-[(2-hydroxyethyl)amino]piperidi n-l-yl}-9-methyl-4H- pyrido[l,2-a]pyrimidin-4-one

434 2-(3,4-dimethoxyphenyl)-9-ethyl-7-(l-methylpiperidin-4-yl)-4 H^yrido[l,2-a]pyrimidin-4-

435 7-[4-(diethylamino)piperidin-l-yl]-2-(3,4-dimethoxyphenyl)-9 -methyl-4H-pyrido[l,2- a]pyrimidin-4-one

436 2-(3,4-dimethoxyphenyl)-9-ethyl-7-(l-ethylpiperidin-4-yl)-4H -pyrido[l,2-a]pyrimidin-4-one

437 2-(2-methylimidazo[l,2-a]pyridin-6-yl)-7-[4-(pyrrolidin-l-yl )piperidin-l-yl]-4H^yrido[l,2- a]pyrimidin-4-one

438 2-(2-methylimidazo[l,2-a]pyridin-6-yl)-7-(piperidin-4-yl)-4H ^yrido[l,2-a]pyrimidin-4-one

439 2-(2-methyl-l,3-benzothiazol-6-yl)-7-(l-methylpiperidin-4-yl )-4H^yrido[l,2-a]pyrimidin- one

440 7-(4-methylpiperazin-l-yl)-2-(6-methylpyrazolo[l,5-a]pyrazin -2-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

441 7-[(3S)-3-methylpiperazin-l-yl]-2-(6-methylpyrazolo[l,5-a]py razin-2-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

442 7-[(3R,5S)-3,5-dimethylpiperazin-l-yl]-2-(6-methylpyrazolo[l ,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

443 2-(l-methyl-lH-indazol-5-yl)-7-(l,2,3,6 etrahydropyridin-4-yl)-4H^yrido[l,2-a]pyrimidin-4- one

444 2-[6-(dimethylamino)pyridin-3-yl]-7-(l,2,3,6-tetrahydropyrid in-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

445 7-[4-(diethylamino)piperidin-l-yl]-2-(2-m^

a]pyrimidin-4-one

446 2-(3,4-dimethoxyphenyl)-7-{4-[(2-hydroxyethyl)(methyl)amino] piperidin-l-yl}-9-methyl-4H^ pyrido[l,2-a]pyrimidin-4-one

447 2-(3,4-dimethoxyphenyl)-9-ethyl-7-[(3R)-3-m

4-one

448 2-(2-methylimidazo[l,2-a]pyridin-6-yl)-7-(l-methylpiperidin- 4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one Cpd Name

449 2-(l-methyl-lH-indazol-5-yl)-7-(l-me ^

a]pyrimidin-4-one

450 2-[6-(dimethylamino)pyridin-3-yl]-7-(l-methyl-l,2,3,6 etrahydropyridin-4-yl)-4H-pyrido[l _^ a]pyrimidin-4-one

451 7-[4-(diethylamino)piperidin-l-yl]-2-(4,6-dimethylpyrazolo[l ,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

452 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(piperidin-4-y l)-4H-pyrido[l,2-a]pyrimidin-4- one

453 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l-methylpiper idin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

454 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l-ethylpiperi din-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

455 2-(3,4-dimethoxyphenyl)-9-ethyl-7-[(8aR)-hexahydropyrrolo[l, 2-a]pyrazin-2(lH)-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

456 2-(3,4-dimethoxyphenyl)-7-{4-[(2-methoxyethyl)amino]piperidi n-l-yl}-9-methyl-4H- pyrido[l,2-a]pyrimidin-4-one

457 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-(4-me thylpiperazin-l-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

458 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(8aR)-hexahyd ropyrrolo[l,2-a]pyrazin-2(lH)- yl]-9-methyl-4H-pyrido[l,2-a]pyrimidin-4-one

459 7-[4-(dimethylamino)piperidin-l-yl]-2-(4,6-dim

4H-pyrido[l,2-a]pyrimidin-4-one

460 7-(2-methylimidazo[l,2-a]pyridin-6-yl)-2-(l-methylpiperidin- 4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

461 7-(2-methylimidazo[l,2-a]pyridin-6-yl)-2-[l-(propan-2-yl)pip eridin-4-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

462 7-(8-fluoro-2-methylimidazo[l,2-a]pyridin-6-yl)-2-(l-methylp iperidin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

463 7-(l-ethyl-l,2,3,6 etrahydropyridin-4-yl)-2-(l-methyl-lH-indazol-5-yl)-4H-pyrid o[l,2- a]pyrimidin-4-one

464 2-(l-methyl-lH-indazol-5-yl)-7-(l-propyl-l,2,3,6-tetrahydrop yridin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

465 2-[6-(dimethylamino)pyridin-3-yl]-7-(piperidin-4-yl)-4H-pyri do[l,2-a]pyrimidin-4-

466 7-(4-ethylpiperazin-l-yl)-2-(6-methylpyrazolo[l,5-a]pyrazin- 2-yl)-4H-pyrido[l,2-a]pyrimidin- 4-one

467 7-[(8aR)-hexahydropyrrolo[l,2-a]pyrazin-2(lH)-yl]-2-(6-methy lpyrazolo[l,5-a]pyrazin-2-yl)- 4H-pyrido[l,2-a]pyrimidin-4-one

468 7-[4-(dimethylamino)piperidin-l-yl]-2-(6-methylpyrazolo[l,5- a]pyrazin-2-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

469 7-[4-(2-hydroxyethyl)piperazin-l-yl]-2-(6-methylpyrazolo[l,5 -a]pyrazin-2-yl)-4H-pyrido[l,2- a]pyrimidin-4-one Cpd Name

470 2-(2-methylimidazo[l,2-a]pyridin-6-yl)-7-(l-propylpiperidin- 4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

471 7-[l-(2-hydroxyethyl)-l,2,3,6 etrahydropyridin-4-yl]-2-(l-methyl-lH-indazol-5-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

472 7-[(3R)-3-methylpiperazin-l-yl]-2-(6-methylpyrazolo[l,5-a]py razin-2-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

473 2-(6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l,2,3,6-tetrahydr opyridin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

474 2-(2-methyl-2H-indazol-5-yl)-7-(l,2,3,6 etrahydropyridin-4-yl)-4H-pyrido[l,2-a]pyrimidin-4- one

475 2-(l-methyl-lH-indazol-5-yl)-7-(l-methylpiperidin-4-yl)-4H-p yrido[l,2-a]pyrimidin

476 2-(2-methyl-2H-indazol-5-yl)-7-(l-methyl-l,2,3,6 etrahydropyridin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

477 7-(l-ethyl-l,2,3,6 etrahydropyridin-4-yl)-2-(2-methyl-2H-indazol-5-yl)-4H-pyrid o[l,2- a]pyrimidin-4-one

478 7-(l-ethylpiperidin-4-yl)-2-(2-methylimidazo[l,2-a]pyridin-6 -yl)-4H-pyrido[l,2-a]pyrimi 4-one

479 2-(l,3-dimethylpyrrolo[l,2-a]pyrazin-7-yl)-7-[l-(propan-2-yl )-l,2,3,6-tetrahydropyridin-4-yl]- 4H-pyrazino[l,2-a]pyrimidin-4-one

480 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-(l,2, 3,6-tetrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

481 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-(l-me thyl-l,2,3,6 etrahydropyridin- 4-yl)-4H-pyrido[l,2-a]pyrimidin-4-one

482 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l-ethyl-l,2,3 ,6-tetrahydropyridin-4-yl)-9- methyl-4H-pyrido[l,2-a]pyri mi din -4-one

483 7-(l-cyclopropyl-l,2,3,6-tetrahydropyridin-4-yl)-2-(4,6-dime thylpyrazolo[l,5-a]pyrazin-2-yl)- 9-methyl-4H-pyrido[l,2-a]pyrimidin-4-one

484 2-(6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l-methyl-l,2,3,6- tetrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

485 7-(l-ethyl-l,2,3,6-tetrahydropyridin-4-yl)-2-(6-methylpyrazo lo[l,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

486 2-(5,7-dimethylfuro[2,3-c]pyridin-2-yl)-7-(piperazin-l-yl)-4 H-pyrido[l,2-a]pyrimidin-4-one

487 2-(5,7-dimethylfuro[2,3-c]pyridin-2-yl)-7-(4-methylpiperazin -l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

488 2-(5,7-dimethylfuro[2,3-c]pyridin-2-yl)-7-[(3S)-3-methylpipe razin-l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

489 2-(l-methyl-lH-indazol-5-yl)-7-(4-methylpiperazin-l-yl)-4H-p yrido[l,2-a]pyrimidin-4-one

490 2-(l-methyl-lH-indazol-5-yl)-7-(piperazin-l-yl)-4H-pyrido[l, 2-a]pyrimidin-4-one

491 7-[4-(dimethylamino)piperidin-l-yl]-2-(l-methyl-lH-indazol-5 -yl)-4H-pyrido[l,2- a]pyrimidin-4-one Cpd Name

492 7-(4-methyl-l,4-diazepan-l-yl)-2-(l-methyl-lH-indazol-5-yl)- 4H-pyrido[l,2-a]pyrimidin one

493 7-(l-ethyl-l,2,3,6 etrahydropyridin-4-yl)-2-(2-methyl-l,3-benzoxazol-6-yl)-4H-p yrimido[l,2- b]pyridazin-4-one

494 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-(4-ethylpi perazin-l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

495 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3R)-4-et hyl-3-methylpiperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

496 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3S)-4-et hyl-3-methylpiperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

497 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3R)-3-me thyl-4-(propan-2-yl)piperazin- 1 -yl]-4H-pyrido[l ,2-a]pyrimidin-4-one

498 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3S)-3-me thyl-4-(propan-2-yl)piperazin- 1 -yl]-4H-pyrido[l ,2-a]pyrimidin-4-one

499 2-(2-methyl-l,3-benzoxazol-6-yl)-7-(piperidin-4-yl)-4H-pyrim ido[l,2-b]pyridazin-4-one

500 2-(2-methyl-l,3-benzoxazol-6-yl)-7-(l-methylpiperidin-4-yl)- 4H-pyrimido[l,2-b]pyridazin-4- one

501 7-(l-ethylpiperidin-4-yl)-2-(2-methyl-l,3-benzoxazol-6-yl)-4 H-pyrimido[l,2-b]pyridazin-4- one

502 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(piperidin-4-y l)-4H-pyrazino[l,2-a]pyrimidin- 4-one

503 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l-methylpiper idin-4-yl)-4H-pyrazino[l,2- a]pyrimidin-4-one

504 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l-ethylpiperi din-4-yl)-4H-pyrazino[l,2- a]pyrimidin-4-one

505 2-(l-methyl-lH-indazol-5-yl)-7-(l,2,3,6 etrahydropyridin-4-yl)-4H-pyrazino[l,2-a]pyrimidm 4-one

506 2-(l-methyl-lH-indazol-5-yl)-7-(l-methyl-l,2,3,6 etrahydropyridin-4-yl)-4H-pyrazino[l,2- a]pyrimidin-4-one

507 7-(l-ethyl-l,2,3,6 etrahydropyridin-4-yl)-2-(l-methyl-lH-indazol-5-yl)-4H-pyraz ino[l,2^ a]pyrimidin-4-one

508 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(4-ethylpipera zin-l-yl)-9-methyl-4H- pyrido[l,2-a]pyrimidin-4-one

509 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-[(3R) -3-methylpiperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

510 7-[(3R)-3,4-dimethylpiperazin-l-yl]-2-(4,6-dimethylpyrazolo[ l,5-a]pyrazin-2-yl)-9-methyl- 4H-pyrido[l,2-a]pyrimidin-4-one

511 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(3R)-4-ethyl- 3-methylpiperazin-l-yl]-9- methyl-4H-pyrido[l,2-a]pyri mi din -4-one

512 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(piperidin-4-y l)-4H-pyrimido[l,2-b]pyridazin- 4-one Cpd Name

513 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7^

b]pyridazin-4-one

514 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l-ethylpiperi din-4-yl)-4H-pyrimido[l,2- b]pyridazin-4-one

515 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(octahydro-5H- pyrrolo[3,2-c]pyridin-5-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

516 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-(piperidin -4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

517 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-(l-methylp iperidin-4-yl)-4H-pyrido[l _^ a]pyrimidin-4-one

518 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-(l-ethylpi peridin-4-yl)-4H-pyrido[l,2- a] pyrimidin-4-one

519 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[l-(propan -2-yl)piperidin-4-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

520 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-(4-me thyl-l,4-diazepan-l-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

521 2-(2-methyl-2H-indazol-5-yl)-7-(piperidin-4-yl)-4H-pyrimido[ l,2-b]pyridazin-4-one

522 2-(2-methyl-2H-indazol-5-yl)-7-(l-methylpiperidin-4-yl)-4H-p yrimido[l,2-b]pyridazin-

523 7-(l-ethylpiperidin-4-yl)-2-(2-methyl-2H-indazol-5-yl)-4H-py rimido[l,2-b]pyridazin-4-one

524 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-(l-methylp iperidin-4-yl)-4H-pyrimi

b] pyridazin-4-one

525 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-(l-ethylpi peridin-4-yl)-4H-pyrimi

b]pyridazin-4-one

526 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[l-(2-hydr oxyethyl)piperidin-4-yl]-4H- pyrimido[l,2-b]pyridazin-4-one

527 2-(5,7-dimethylfuro[2,3-c]pyndin-2-yl)-7-[(3R,5S)-3,5-dimeth ylpiperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

528 7-[4-(dimethylamino)piperidin-l-yl]-2-(5,7-dim

a]pyrimidin-4-one

529 2-(5,7-dimethylfuro[2,3-c]pyridin-2-yl)-7-[4-(2-hydroxyethyl )piperazin-l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

530 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[l-(2-hydroxye thyl)piperidin-4-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

531 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[4-(2-hydroxye thyl)piperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

532 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(3R)-4-(2-hyd roxyethyl)-3-methylpiperazin-l- yl]-4H-pyrido[l,2-a]pyrimidin-4-one

533 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3S)-4-(2 -methoxyethyl)-3- methylpiperazin-l-yl]-4H-pyrido[l,2-a]pyrimidin-4-one Cpd Name

534 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-{(3S)-4-[2 -(2-hydroxyethoxy)ethyl]-3- methylpiperazin-l-yl}-4H-pyrido[l,2-a]pyrimidin-4-one

535 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3S)-4-cy clopropyl-3-methylpiperazin-l- yl]-4H-pyrido[l,2-a]pyrimidin-4-one

536 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3S)-4-cy clobutyl-3-methylpiperazin-l- yl]-4H-pyrido[l,2-a]pyrimidin-4-one

537 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3S)-4-(2 -hydroxyethyl)-3- methylpiperazin-l-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

538 2-(8-fluoro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3S)-4-(2 -methoxyethyl)-3- methylpiperazin-l-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

539 2-(8-fluoro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3S)-4-(2 -hydroxyethyl)-3- methylpiperazin-l-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

540 2-(8-fluoro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-{(3S)-4-[2 -(2-hydroxyethoxy)ethyl]-3- methylpiperazin-l-yl}-4H-pyrido[l,2-a]pyrimidin-4-one

541 2-(8-fluoro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3S)-3-me thyl-4-(propan-2-yl)piperazin-l- yl]-4H-pyrido[l,2-a]pyrimidin-4-one

542 7-[(3S)-4-cyclopropyl-3-methylpiperazin-l-yl]-2-(8-fluoro-2- methylimidazo[l,2-a]pyridin-6- yl)-4H-pyrido[l,2-a]pyrimidin-4-one

543 7-[(3S)-4-cyclobutyl-3-methylpiperazin-l-yl]-2-(8-fluoro-2-m ethylimidazo[l,2-a]pyridin-6- yl)-4H-pyrido[l,2-a]pyrimidin-4-one

544 7-(3,3-dimethylpiperazin-l-yl)-2-(4,6-dimethylpyrazolo[l,5-a ]pyrazin-2-yl)-9-methyl-4H- pyrido[l,2-a]pyrimidin-4-one

545 2-(l-methyl-lH-indazol-5-yl)-7-[(3R)-3-methylpiperazin-l-yl] -4H-pyrido[l,2-a]pyrimidin-4- one

546 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(piperazin -l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

547 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(4-methylp iperazin-l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

548 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(4-ethylpi perazin-l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

549 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-[4-(2-hydr oxyethyl)piperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

550 7-[4-(dimethylamino)piperidin-l-yl]-2-(4-ethyl-6-methylpyraz olo[l,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

551 7-[4-(diethylamino)piperidin-l-yl]-2-(4-ethyl-6-methylpyrazo lo[l,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

552 7-[(3R,5S)-3,5-dimethylpiperazin-l-yl]-2-(l-methyl-lH-indazo l-5-yl)-4H-pyndo[l,2- a]pyrimidin-4-one

553 2-(l-methyl-lH-indazol-5-yl)-7-[(3S)-3-methylpiperazin-l-yl] -4H-pyrido[l,2-a]pyrimidin-4- one Cpd Name

554 2-(2-methylimidazo[l,2-a]pyridin-6-yl)-7-[l-(^

a]pyrimidin-4-one

555 2-(2-methylimidazo[l,2-a]pyridin-7-yl)-7-(piperazin-l-yl)-4H -pyrido[l,2-a]pyrimidin-4-one

556 2-(2-methylimidazo[l,2-a]pyridin-7-yl)-7-(piperidin-4-yl)-4H -pyrido[l,2-a]pyrimidin-4-one

557 2-(2-methylimidazo[l,2-a]pyridin-7-yl)-7-(4-methylpiperazin- l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

558 7-(4-ethylpiperazin-l-yl)-2-(2-methylimida

4-one

559 2-(2-methylimidazo[l,2-a]pyridin-7-yl)-7-(l-methylpiperidin- 4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

560 7-(l-ethylpiperidin-4-yl)-2-(2-methylimidazo[l,2-a]pyridin-7 -yl)-4H-pyrido[l,2-a]pyrimi 4-one

561 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-[(3S) -3-methylpiperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

562 7-[(3R,5S)-3,5-dimethylpiperazin-l-yl]-2-(4,6-dimethylpyrazo lo[l,5-a]pyrazin-2-yl)-9- methyl-4H-pyrido[l,2-a]pyri mi din -4-one

563 7-[(3S)-3,4-dimethylpiperazin-l-yl]-2-(4,6-dimethylpyrazolo[ l,5-a]pyrazin-2-yl)-9-methyl- 4H-pyrido[l,2-a]pyrimidin-4-one

564 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-[(3R, 5S)-3,4,5-trimethylpiperazin-l- yl]-4H-pyrido[l,2-a]pyrimidin-4-one

565 2-(2-methylimidazo[l,2-a]pyridin-6-yl)-7-[l-(propan-2-yl)-l, 2,3,6-tetrahydropyridin-4-yl]- 4H-pyrido[l,2-a]pyrimidin-4-one

566 2-(2-methyl-2H-indazol-5-yl)-7-(piperidin-4-yl)-4H-pyrazino[ l,2-a]pyrimidin-4-one

567 2-(2-methyl-2H-indazol-5-yl)-7-(l-methylpiperidin-4-yl)-4H-p yrazino[l,2-a]pyrimidin-4-one

568 7-(l-ethylpiperidin-4-yl)-2-(2-methyl-2H-indazol-5-yl)-4H-py razino[l,2-a]pyrimidin-4-one

569 7-[l-(2-hydroxyethyl)piperidin-4-yl]-2-(2-methyl-2H-indazol- 5-yl)-4H-pyrazino[l,2- a]pyrimidin-4-one

570 7-{4-[(dimethylamino)methyl]piperidin-l-yl}-2-(4,6-dimethylp yrazolo[l,5-a]pyrazin-2-yl)- 4H-pyrido[l,2-a]pyrimidin-4-one

571 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[4-(pyrrolidin -l-ylmethyl)piperidin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

572 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[4-(piperidin- l-ylmethyl)piperidin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

573 2-(3,4-dimethoxyphenyl)-7-{4-[(dimethylamino)methyl]piperidi n-l-yl}-4H-pyrido[l,2- a]pyrimidin-4-one

574 2-(3,4-dimethoxyphenyl)-7-[4-(pyrrolidin-l-ylmethyl)piperidi n-l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

575 2-(3,4-dimethoxyphenyl)-7-[4-(piperidin-l-ylmethyl)piperidin -l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one Cpd Name

576 7-[l-(2-hydroxyethyl)piperidin-4-yl]-2-(2-m

a]pyrimidin-4-one

577 7-[l-(2-hydroxyethyl)-l,2,3,6 etrahydropyridin-4-yl]-2-(2-methylimidazo[l,2-a]pyridin-6-yl )- 4H-pyrido[l,2-a]pyrimidin-4-one

578 2-(2-methyl-2H-indazol-5-yl)-7-(l-methylpiperidin-4-yl)-4H-p yrido[l,2-a]pyrimidin-4-

579 2-(2-methylimidazo[l,2-a]pyridin-6-yl)-7-(l-methylpiperidin- 4-yl)-4H-pyrazino[l,2- a]pyrimidin-4-one

580 7-(l-ethylpiperidin-4-yl)-2-(2-methylimidazo[l,2-a]pyridin-6 -yl)-4H-pyrazino[l,2- a]pyrimidin-4-one

581 7-[l-(2-hydroxyethyl)piperidin-4-yl]-2-(2-methylimidazo[l,2- a]pyridin-6-yl)-4H- pyrazino[l,2-a]pyrimidin-4-one

582 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-{4-[(2-hydroxy ethyl)(methyl)amino]piperidin- 1 -yl } -9-methyl-4H-pyrido [ 1 ,2-a]pyrimidin-4-one

583 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-[4-(p ropylamino)piperidin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

584 7-(4-amino-4-methylpiperidin-l-yl)-2-(4,6-dimethylpyrazolo[l ,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

585 2-(2-methylimidazo[l,2-a]pyridin-6-yl)-7-(piperidin-4-yl)-4H -pyrazino[l,2-a]pyrimidin-4-

586 2-(2-methyl-2H-indazol-5-yl)-7-(piperazin-l-yl)-4H-pyrazino[ l,2-a]pyrimidin-4-one

587 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-(piperidin -4-yl)-4H-pyrazino[l,2- a]pyrimidin-4-one

588 2-(2,8-dimethylimidazo[l,2-a]pyridin-6-yl)-7-(piperidin-4-yl )-4H-pyrazino[l,2-a]pyrimidm one

589 2-(2-methyl-2H-indazol-5-yl)-7-(4-methylpiperazin-l-yl)-4H-p yrazino[l,2-a]pyrimidin-4-on^

590 7-(4-ethylpiperazin-l-yl)-2-(2-methyl-2H-indazol-5-yl)-4H-py razino[l,2-a]pyrimidin-4-

591 7-[4-(2-hydroxyethyl)piperazin-l-yl]-2-(2-methyl-2H-indazol- 5-yl)-4H-pyrazino[l,2- a]pyrimidin-4-one

592 2-(2,8-dimethylimidazo[l,2-a]pyridin-6-yl)-7-(l-methylpiperi din-4-yl)-4H-pyrazino[l,2- a]pyrimidin-4-one

593 2-(2,8-dimethylimidazo[l,2-a]pyridin-6-yl)-7-(l-ethylpiperid in-4-yl)-4H-pyrazino[l,2- a]pyrimidin-4-one

594 2-(2,8-dimethylimidazo[l,2-a]pyridin-6-yl)-7-[l-(2-hydroxyet hyl)piperidin-4-yl]-4H- pyrazino[l,2-a]pyrimidin-4-one

595 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[l-(propan -2-yl)piperidin-4-yl]-4H- pyrazino[l,2-a]pyrimidin-4-one

596 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[4-(ethylamino )piperidin-l-yl]-9-methyl-4H- pyrido[l,2-a]pyrimidin-4-one

597 7-{4-[bis(2-hydroxyethyl)amino]piperidin-l-yl}-2-(4,6-dimeth ylpyrazolo[l,5-a]pyrazin-2-yl)- 9-methyl-4H-pyrido[l,2-a]pyrimidin-4-one Cpd Name

598 7-[l-(2-hydroxyethyl)piperidin-4-yl]-2-(2-methyl-l,3-benzoxa zol-6-yl)-4H-pyrimido[l,2- b]pyridazin-4-one

599 2-(8-chloro-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[l-(2-hydr oxyethyl)piperidin-4-yl]-4H- pyrazino[l,2-a]pyrimidin-4-one

600 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[l-(oxetan-3-y l)piperidin-4-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

601 2-(5,7-dimethylfuro[2,3-c]pyridin-2-yl)-7-(4-ethylpiperazin- l-yl)-4H-pyrido[l,2-a]pyrimidi

4- one

602 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l-methyloctah ydro-5H-pyrrolo[3,2-c]pyridin-

5- yl)-4H-pyrido[l,2-a]pyrimidin-4-one

603 2-(l-methyl-lH-indazol-5-yl)-7-(piperidin-4-yl)-4H-pyrido[l, 2-a]pyrimidin-4-one

604 7-(l-ethylpiperidin-4-yl)-2-(l-methyl-lH-indazol-5-yl)-4H-py rido[l,2-a]pyrimidin-4-one

605 7-[l-(2-hydroxyethyl)piperidin-4-yl]-2-(l-methyl-lH-indazol- 5-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

606 2-(2-methyl-2H-indazol-5-yl)-7-(piperidin-4-yl)-4H-pyrido[l, 2-a]pyrimidin-4-one

607 2-(2,8-dimethylimidazo[l,2-a]pyridin-6-yl)-7-(piperidin-4-yl )-4H-pyrido[l,2-a]pyrimidin- one

608 2-(2-methyl-2H-indazol-5-yl)-7-[l-(propan-2-yl)piperidin-4-y l]-4H-pyrido[l,2-a]pyrimidin-4 one

609 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-{4-[(2-hydroxy ethyl)amino]piperidin-l-yl}-9- methyl-4H-pyrido[l,2-a]pyri mi din -4-one

610 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-[4-(m ethylamino)piperidin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

611 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-[4-(p ropan-2-ylamino)piperidin-l- yl]-4H-pyrido[l,2-a]pyrimidin-4-one

612 7-(l-ethylpiperidin-4-yl)-2-(2-methyl-2H-indazol-5-yl)-4H-py rido[l,2-a]pyrimidin-4-one

613 7-[l-(2-hydroxyethyl)piperidin-4-yl]-2-(2-methyl-2H-indazol- 5-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

614 2-(2,8-dimethylimidazo[l,2-a]pyridin-6-yl)-7-(l-methylpiperi din-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

615 2-(2,8-dimethylimidazo[l,2-a]pyridin-6-yl)-7-(l-ethylpiperid in-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

616 2-(2,8-dimethylimidazo[l,2-a]pyridin-6-yl)-7-[l-(propan-2-yl )piperidin-4-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

617 2-(2,8-dimethylimidazo[l,2-a]pyridin-6-yl)-7-[l-(2-hydroxyet hyl)piperidin-4-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

618 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(4-propylp iperazin-l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

619 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-[4-(propan -2-yl)piperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one Cpd Name

620 7-(4-cyclopropylpiperazin-l-yl)-2-(4-ethyl-6-methylpyrazolo[ l,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

621 7-(4-cyclobutylpiperazin-l-yl)-2-(4-ethyl-6-methylpyrazolo[l ,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

622 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-[4-(oxetan -3-yl)piperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

623 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l-ethyloctahy dro-5H-pyrrolo[3,2-c]pyridin-5- yl)-4H-pyrido[l,2-a]pyrimidin-4-one

624 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[l-(2-hydroxye thyl)octahydro-5H-pyrrolo[3,2- c]pyridin-5-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

625 2-(4-methoxy-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(4-methy lpiperazin-l-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

626 2-(4-hydroxy-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(4-methy lpiperazin-l-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

627 2-(2-methylimidazo[l,2-a]pyridin-6-yl)-7-[l-(propan-2-yl)pip eridin-4-yl]-4H-pyrazino[l,2- a]pyrimidin-4-one

628 7-(l-cyclobutylpiperidin-4-yl)-2-(2-methylimidazo[l,2-a]pyri din-6-yl)-4H-pyrazino[l,2- a]pyrimidin-4-one

629 7-[(3R)-3,4-dimethylpiperazin-l-yl]-2-(4-ethyl-6-methylpyraz olo[l,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

630 7-[(3R)-4-ethyl-3-methylpiperazin-l-yl]-2-(4-ethyl-6-methylp yrazolo[l,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

631 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(3R)-3-me thyl-4-propylpiperazin-l-yl]- 4H-pyrido[l,2-a]pyrimidin-4-one

632 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(3R)-4-(2 -hydroxyethyl)-3- methylpiperazin-l-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

633 7-[(3R,5S)-3,5-dimethylpiperazin-l-yl]-2-(4-ethyl-6-methylpy razolo[l,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

634 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-[4-(pyrrol idin-l-yl)piperidin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

635 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(3S)-3-me thylpiperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

636 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(4-methyl- l,4-diazepan-l-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

637 2-(8-ethyl-2-methylimidazo[l,2-a]pyridin-6-yl)-7-(piperazin- l-yl)-4H-pyrido[l,2-a]pyrimi 4-one

638 2-(8-ethyl-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3R)-3-met hylpiperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

639 2-(8-ethyl-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3S)-3-met hylpiperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one Cpd Name

640 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[l-(propan-2-y l)piperidin-4-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

641 7-(l-cyclopropylpiperidin-4-yl)-2-(4,6-dimethylpyrazolo[l,5- a]pyrazin-2-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

642 7-(l-cyclobutylpiperidin-4-yl)-2-(4,6-dimethylpyrazolo[l,5-a ]pyrazin-2-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

643 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(3R)-3-me thyl-4-(propan-2-yl)piperazin- 1 -yl]-4H-pyrido[l ,2-a]pyrimidin-4-one

644 7-[(3R)-4-cyclopropyl-3-methylpiperazin-l-yl]-2-(4-ethyl-6-m ethylpyrazolo[l,5-a]pyrazin-2- yl)-4H-pyrido[l,2-a]pyrimidin-4-one

645 7-[(3R)-4-cyclobutyl-3-methylpiperazin-l-yl]-2-(4-ethyl-6-me thylpyrazolo[l,5-a]pyrazin-2- yl)-4H-pyrido[l,2-a]pyrimidin-4-one

646 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(3R)-3-me thyl-4-(oxetan-3-yl)piperazin-l- yl]-4H-pyrido[l,2-a]pyrimidin-4-one

647 2-(8-ethyl-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[4-(2-hydro xyethyl)piperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

648 7-(4-cyclobutylpiperazin-l-yl)-2-(8-ethyl-2-methylimidazo[l, 2-a]pyridin-6-yl)-4H-pyrido[l,2^ a]pyrimidin-4-one

649 2-(8-ethyl-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3R)-4-(2- hydroxyethyl)-3- methylpiperazin-l-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

650 7-[(3R)-4-cyclobutyl-3-methylpiperazin-l-yl]-2-(8-ethyl-2-me thylimidazo[l,2-a]pyridin-6-yl)- 4H-pyrido[l,2-a]pyrimidin-4-one

651 2-(8-ethyl-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3S)-4-(2- hydroxyethyl)-3- methylpiperazin-l-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

652 7-[(3S)-4-cyclobutyl-3-methylpiperazin-l-yl]-2-(8-ethyl-2-me thylimidazo[l,2-a]pyridin-6-yl)- 4H-pyrido[l,2-a]pyrimidin-4-one

653 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(piperidin -4-yl)-4H-pyrazino[l,2- a]pyrimidin-4-one

654 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l-methylp iperidin-4-yl)-4H-pyrazino[l,2- a]pyrimidin-4-one

655 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l-ethylpi peridin-4-yl)-4H-pyrazino[l,2- a]pyrimidin-4-one

656 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(piperidin -4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

657 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l-methylp iperidin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

658 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l-ethylpi peridin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

659 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-[l-(2-hydr oxyethyl)piperidin-4-yl]-4H- pyrido[l,2-a]pyrimidin-4-one Cpd Name

660 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l-propylp iperidin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

661 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(3R)-3-me thylpiperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

662 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[l-(2-fluoroet hyl)piperidin-4-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

663 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[l-(3-fluoropr opyl)piperidin-4-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

664 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-[4-(2-fluo roethyl)piperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

665 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-[4-(3-fluo ropropyl)piperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

666 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(3R)-4-(2 -fluoroethyl)-3-methylpiperazin- 1 -yl]-4H-pyrido[l ,2-a]pyrimidin-4-one

667 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(3R)-4-(3 -fluoropropyl)-3- methylpiperazin-l-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

668 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-[l-(2-fluo roethyl)piperidin-4-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

669 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-[l-(3-fluo ropropyl)piperidin-4-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

670 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-{(3R)-4-[2-(2- hydroxyethoxy)ethyl]-3- methylpiperazin-l-yl}-9-methyl-4H-pyrido[l,2-a]pyrimidin-4-o ne

671 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-(pipe ridin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

672 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-(l-me thylpiperidin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

673 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(3R)-4-(2-hyd roxyethyl)-3-methylpiperazin-l- yl]-9-methyl-4H-pyrido[l,2-a]pyrimidin-4-one

674 2-[8-(hydroxymethyl)-2-methylimidazo[l,2^

a]pyrimidin-4-one

675 7-[(3R,5S)-3,5-dimethylpiperazin-l-yl]-2-(8-ethyl-2-methylim idazo[l,2-a]pyridin-6-yl)-4H^ pyrido[l,2-a]pyrimidin-4-one

676 2-(8-ethyl-2-methylimidazo[l,2-a]pyridin-6-yl)-7-(4-methyl-l ,4-diazepan-l-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

677 2-[8-(hydroxymethyl)-2-methylimidazo[l,2-a]pyridin-6-yl]-7-( 4-methylpiperazin-l-yl)-4H^ pyrido[l,2-a]pyrimidin-4-one

678 7-(4-ethylpiperazin-l-yl)-2-[8-(hydroxymethyl)-2-methylimida zo[l,2-a]pyridin-6-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

679 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-[l-(propan -2-yl)piperidin-4-yl]-4H- pyrido[l,2-a]pyrimidin-4-one Cpd Name

680 7-(l-cyclopropylpiperidin-4-yl)-2-(4-ethyl-6-methylpyrazolo[ l,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

681 7-(l-cyclobutylpiperidin-4-yl)-2-(4-ethyl-6-methylpyrazolo[l ,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

682 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-[l-(oxetan -3-yl)piperidin-4-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

683 2-(4-cyclopropyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(pip erazin-l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

684 2-(4-cyclopropyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(4-m ethylpiperazin-l-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

685 2-(4-cyclopropyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(4-e thylpiperazin-l-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

686 2-(4-cyclopropyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-[4-( 2-hydroxyethyl)piperazin-l-yl]- 4H-pyrido[l,2-a]pyrimidin-4-one

687 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l-propylpiper idin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

688 2-[4-(dimethylamino)-6-methylpyrazolo[l,5-a]pyrazin-2-yl]-7- (piperazin-l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

689 2-(2-methyl-lH-benzimidazol-6-yl)-7-(4-methylpiperazin-l-yl) -4H-pyrido[l,2-a]pyrimidi one

690 7-(4-ethylpiperazin-l-yl)-2-(2-methyl-lH-benzimidazol-6-yl)- 4H-pyrido[l,2-a]pyrimidin one

691 2-(2,8-dimethylimidazo[l,2-a]pyridin-6-yl)-7-(piperidin-4-yl )-4H-pyrimido[l,2-b]pyridazi one

692 2-(2-methylimidazo[l,2-a]pyridin-6-yl)-7-(piperidin-4-yl)-4H -pyrimido[l,2-b]pyridazin-4-one

693 7-[l-(2,2-dimethyl-l,3-dioxan-5-yl)piperidin-4-yl]-2-(4-ethy l-6-methylpyrazolo[l,5-a]pyrazin- 2-yl)-4H-pyrido[l,2-a]pyrimidin-4-one

694 7-[l-(l,3-dihydroxypropan-2-yl)piperidin-4-yl]-2-(4-ethyl-6- methylpyrazolo[l,5-a]pyrazin-2- yl)-4H-pyrido[l,2-a]pyrimidin-4-one

695 7-[(3R,5S)-3,5-dimethylpiperazin-l-yl]-2-(l,3-dimethylpyrrol o[l,2-a]pyrazin-7-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

696 2-(8-ethyl-2-methylimidazo[l,2-a]pyridin-6-yl)-7-(piperidin- 4-yl)-4H-pyrido[l,2-a]pyrimidi 4-one

697 2-(8-ethyl-2-methylimidazo[l,2-a]pyridin-6-yl)-7-(l-methylpi peridin-4-yl)-4H-pyrido[l,2 a]pyrimidin-4-one

698 2-(8-ethyl-2-methylimidazo[l,2-a]pyridin-6-yl)-7-(l-ethylpip eridin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

699 2-(8-ethyl-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[l-(2-hydro xyethyl)piperidin-4-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

700 7-[(3R)-3,4-dimethylpiperazin-l-yl]-2-(8-ethyl-2-methylimida zo[l,2-a]pyridin-6-yl)-4H- pyrido[l,2-a]pyrimidin-4-one Cpd Name

701 2-(8-ethyl-2-methylimidazo[l,2-a]py^

pyrido[l,2-a]pyrimidin-4-one

702 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l-ethylpiperi din-4-yl)-9-methyl-4H- pyrido[l,2-a]pyrimidin-4-one

703 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[l-(2-hydroxye thyl)piperidin-4-yl]-9-methyl- 4H-pyrido[l,2-a]pyrimidin-4-one

704 7-(l-cyclobutylpiperidin-4-yl)-2-(4,6-dimethylpyrazolo[l,5-a ]pyrazin-2-yl)-9-methyl-4H- pyrido[l,2-a]pyrimidin-4-one

705 9-methyl-2-(2-methyl-2H-indazol-5-yl)-7-(l-methylpiperidin-4 -yl)-4H-pyrido[l,2- a]pyrimidin-4-one

706 7-[4-(dimethylamino)-4-methylpiperidin-l-yl]-2-(4,6-dimethyl pyrazolo[l,5-a]pyrazin-2-yl)- 4H-pyrido[l,2-a]pyrimidin-4-one

707 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[4-(ethylamino )-4-methylpiperidin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

708 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[4-methyl-4-(p ropylamino)piperidin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

709 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-{4-[(2-hydroxy ethyl)amino]-4- methylpiperidin- 1 -yl } -4H-pyrido [ 1 ,2-a]pyrimidin-4-one

710 7-(l-cyclobutylpiperidin-4-yl)-9-methyl-2-(2-methyl-2H-indaz ol-5-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

711 7-[l-(2-hydroxyethyl)piperidin-4-yl]-9-methyl-2-(2-methyl-2H -indazol-5-yl)-4H-pyrido[ a]pyrimidin-4-one

712 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-(l-pr opylpiperidin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

713 2-(l,3-dimethylpyrrolo[l,2-a]pyrazin-7-yl)-7-[(3R)-3-methylp iperazin-l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

714 2-(8-cyclopropyl-2-methylimidazo[l,2-a]pyridin-6-yl)-7-(pipe razin-l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

715 2-(8-cyclopropyl-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3R) -3-methylpiperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

716 2-(8-cyclopropyl-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3S) -3-methylpiperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

717 2-(8-cyclopropyl-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(3R, 5S)-3,5-dimethylpiperazin-l- yl]-4H-pyrido[l,2-a]pyrimidin-4-one

718 7-(l-cyclopropylpiperidin-4-yl)-9-methyl-2-(2-methyl-2H-inda zol-5-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

719 7-(l -ethylpiperidin-4-yl)-9-methyl-2-(2-methyl-2H-indazol-5-yl)- 4H-pyrido[l,2-a]pyrimidi^ 4-one

720 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-(pipe razin-l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

721 9-methyl-2-(2-methyl-2H-indazol-5-yl)-7-(piperidin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4 Cpd Name

722 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(l-methylpipe ridin-4-yl)oxy]-4H-pyrido[l,2- a]pyrimidin-4-one

723 2-(6-methyl-4-propylpyrazolo[l,5-a]pyrazin-2-yl)-7-(piperazi n-l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

724 7-(4-methylpiperazin-l-yl)-2-(6-methyl-4-propylpyrazolo[l,5- a]pyrazin-2-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

725 7-(4-ethylpiperazin-l-yl)-2-(6-methyl-4-propylpyrazolo[l,5-a ]pyrazin-2-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

726 7-[4-(2-hydroxyethyl)piperazin-l-yl]-2-(6-methyl-4-propylpyr azolo[l,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

727 7-[(3R)-3-methylpiperazin-l-yl]-2-(6-methyl-4-propylpyrazolo [l,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

728 7-[(3S)-3-methylpiperazin-l-yl]-2-(6-methyl-4-propylpyrazolo [l,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

729 7-[(3R,5S)-3,5-dimethylpiperazin-l-yl]-2-(6-methyl-4-propylp yrazolo[l,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

730 2-(l,3-dimethylpyrrolo[l,2-a]pyrazin-7-yl)-7-[(3R)-3-methyl- 4-(propan-2-yl)piperazin-l-yl]- 4H-pyrido[l,2-a]pyrimidin-4-one

731 7-(4-amino-4-methylpiperidin-l-yl)-2-(l,3-dimethylpyrrolo[l, 2-a]pyrazin-7-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

732 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(3S)-3-ethylp iperazin-l-yl]-9-methyl-4H- pyrido[l,2-a]pyrimidin-4-one

733 2-[2-methyl-8-(trifluoromethyl)imidazo[l,2-a]pyridin-6-yl]-7 -(piperazin-l-yl)-4H-pyri

a]pyrimidin-4-one

734 7-[(3R)-3-methylpiperazin-l-yl]-2-[2-methyl-8-(trifluorometh yl)imidazo[l,2-a]pyridin

4H-pyrido[l,2-a]pyrimidin-4-one

735 7-[(3S)-3-methylpiperazin-l-yl]-2-[2-methyl-8-(ta

4H-pyrido[l,2-a]pyrimidin-4-one

736 7-[(3R,5S)-3,5-dimethylpiperazin-l-yl]-2-[2-methyl-8-(triflu oromethyl)imidazo[l,2-a]pyri 6-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

737 7-(4-amino-4-methylpiperidin-l-yl)-2-(4-ethyl-6-methylpyrazo lo[l,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

738 2-(2,7-dimethyl-2H-indazol-5-yl)-7-(piperazin-l-yl)-4H-pyrid o[l,2-a]pyrimidin-4-one

739 2-(2,7-dimethyl-2H-indazol-5-yl)-7-(piperidin-4-yl)-4H-pyrid o[l,2-a]pyrimidin-4-one

740 7-(3-aminoprop-l-yn-l-yl)-2-(4,6-dimethylpyrazolo[l,5-a]pyra zin-2-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

741 2-(2,7-dimethyl-2H-indazol-5-yl)-7-[(3R)-3-methylpiperazin-l -yl]-4H-pyndo[l,2- a]pyrimidin-4-one

742 7-(3-aminopropyl)-2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl )-4H-pyrido[l,2-a]pyrimidin-4- one Cpd Name

743 2-(l,3-dimethylpyrrolo[l,2-a]pyrazin-7-yl)-7-(l,2,3,6 etrahydropyridin-4-yl)-4H-pyrido[l,2^ a]pyrimidin-4-one

744 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-(2,2,6,6 etramethyl-l,2,3,6-tetrahydropyridin- 4-yl)-4H-pyrido[l,2-a]pyrimidin-4-one

745 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(2,2,6,6-t etramethyl-l,2,3,6- tetrahydropyridin-4-yl)-4H-pyrido[l,2-a]pyrimidin-4-one

746 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(3aR,6aS)-hex ahydropyrrolo[3,4-c]pyrrol- 2(lH)-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

747 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(3aR,6aS) -hexahydropyrrolo[3,4-c]pyrrol- 2(lH)-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

748 7-[(3R,5S)-3,5-dimethylpiperazin-l-yl]-2-(l -ethyl-3-methylpyrrolo[l,2-a]pyrazin-7-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

749 7-(l,4-diazepan-l-yl)-2-(l-ethyl-3-methylpyrrolo[l,2-a]pyraz in-7-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

750 2-(2,7-dimethyl-2H-indazol-5-yl)-7-[(3S)-3-methylpiperazin-l -yl]-4H-pyrido[l,2-a]pyrimidin- 4-one

751 2-(2,7-dimethyl-2H-indazol-5-yl)-7-[(3S)-3,4-dimethylpiperaz in-l-yl]-4H-pyndo[l,2- a]pyrimidin-4-one

752 2-(2,7-dimethyl-2H-indazol-5-yl)-7-(l-methylpiperidin-4-yl)- 4H-pyrido[l,2-a]pyrimidin

one

753 2-(2,7-dimethyl-2H-indazol-5-yl)-7-(l-ethylpiperidin-4-yl)-4 H-pyrido[l,2-a]pyrimidin-4-one

754 9-methyl-2-(2-methyl-2H-indazol-5-yl)-7-(piperazin-l-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

755 9-me l-2-(2-methyl-2H-indazol-5-yl)-7-[(3R)-3-methylpiperazin-l-y l]-4H-pyrido[l,2- a]pyrimidin-4-one

756 9-methyl-2-(2-methyl-2H-indazol-5-yl)-7-[(3S)-3-methylpipera zin-l-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

757 7-[3-(dimethylamino)azetidin-l-yl]-2-(4,6-dimethylpyrazolo[l ,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

758 7-[3-(diethylamino)azetidin-l-yl]-2-(4,6-dimethylpyrazolo[l, 5-a]pyrazin-2-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

759 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[3-(pyrrolidin -l-yl)azetidin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

760 7-(l,4-diazepan-l-yl)-2-(4-ethyl-6-methylpyrazolo[l ,5-a]pyrazin-2-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

761 7-[(3aR,6aS)-hexahydropyrrolo[3,4-c]pyrrol-2(lH)-yl]-2-(6-me thyl-4-propylpyrazolo[l,5- a]pyrazin-2-yl)-4H-pyrido[l,2-a]pyrimidin-4-one

762 2-(6-methyl-4-propylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l,2,3,6- tetrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

763 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l,2,3,6-t etrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one Cpd Name

764 7-[(3S)-3-(aminomethyl)pyrrolidin-l-yl]-2-(4,6-dimethylpyraz olo[l,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

765 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[3-(piperidin- l-yl)azetidin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

766 2-(6-methyl-4-propylpyrazolo[l,5-a]pyrazin-2-yl)-7-(piperidi n-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

767 7-(2,7-diazaspiro[4.4]non-2-yl)-2-(4,6-dimethylpyrazolo[l,5- a]pyrazin-2-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

768 2-(2,7-dimethyl-2H-indazol-5-yl)-7-(4-methylpiperazin-l-yl)- 4H-pyrido[l,2-a]pyrimidin-4 one

769 7-[3-(dimethylamino)propyl]-2-(4,6-dimethylpyrazolo[l,5-a]py razin-2-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

770 7-{(3S)-3-[(dimethylamino)methyl]pyrrolidin-l-yl}-2-(4,6-dim ethylpyrazolo[l,5-a]pyrazin-2- yl)-4H-pyrido[l,2-a]pyrimidin-4-one

771 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-( piperidin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

772 9-methyl-2-(l-methyl-lH-indazol-5-yl)-7-(piperidin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-o

773 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-( l,2,3,6-tetrahydropyridin-4-yl)- 4H-pyrido[l,2-a]pyrimidin-4-one

774 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-( l-methylpiperidin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

775 2-(l,7-dimethyl-lH-indazol-5-yl)-7-(piperidin-4-yl)-4H-pyrid o[l,2-a]pyrimidin-4-one

776 2-(l,7-dimethyl-lH-indazol-5-yl)-7-(piperazin-l-yl)-4H-pyrid o[l,2-a]pyrimidin-4-one

777 2-(l,7-dimethyl-lH-indazol-5-yl)-7-[(3S)-3-methylpiperazin-l -yl]-4H-pyrido[l,2-a]pyrimidin- 4-one

778 7-{(3S)-3-[(diethylamino)methyl]pyrrolidin-l-yl}-2-(4,6-dime thylpyrazolo[l,5-a]pyrazin-2- yl)-4H-pyrido[l,2-a]pyrimidin-4-one

779 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-{(3S)-3-[(ethy lamino)methyl]pyrrolidin-l-yl}- 4H-pyrido[l,2-a]pyrimidin-4-one

780 7-{3-[(dimethylamino)methyl]azetidm^

pyrido[l,2-a]pyrimidin-4-one

781 7-{3-[(diethylamino)methyl]azetidin-l-yl}-2-(4,6-dimethylpyr azolo[l,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

782 2-(l-ethyl-3-methylpyrrolo[l,2-a]pyrazin-7-yl)-7-[(8aS)-hexa hydropyrrolo[l,2-a]pyrazin- 2(lH)-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

783 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-[ (3R)-3-methylpiperazin-l-yl]- 4H-pyrido[l,2-a]pyrimidin-4-one

784 9-me l-2-(l-methyl-lH-indazol-5-yl)-7-(l-methylpiperidin-4-yl)-4H -pyrido[l,2- a]pyrimidin-4-one Cpd Name

785 7-[(3R)-3,4-dimethylpiperazin-l-yl]-2-(4-ethyl-6-methylpyraz olo[l,5-a]pyrazin-2-yl)-9- methyl-4H-pyrido[l,2-a]pyrimidin-4-one

786 7-(l-ethylpiperidin-4-yl)-9-methyl-2-(l-m

4-one

787 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-[ (3S)-3-methylpiperazin-l-yl]- 4H-pyrido[l,2-a]pyrimidin-4-one

788 7-[l-(2-hydroxyethyl)piperidin-4-yl]-9-methyl-2-(l-methyl-lH -indazol-5-yl)-4H-pyrido

a]pyrimidin-4-one

789 7-[(3S)-3,4-dimethylpiperazin-l-yl]-2-(4-ethyl-6-methylpyraz olo[l,5-a]pyrazin-2-yl)-9- methyl-4H-pyrido[l,2-a]pyri mi din -4-one

790 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-(l-ethylpi peridin-4-yl)-9-methyl-4H- pyrido[l,2-a]pyrimidin-4-one

791 9-methyl-2-(2-methyl-2H-indazol-5-yl)-7-(l,2,3,6-tetrahydrop yridin-4-yl)-4H-pyrazino[l,2- a]pyrimidin-4-one

792 7-(l-cyclobutylpiperidin-4-yl)-2-(4-ethyl-6-methylpyrazolo[l ,5-a]pyrazin-2-yl)-9-methyl-4H- pyrido[l,2-a]pyrimidin-4-one

793 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-7-[l-(2-hydr oxyethyl)piperidin-4-yl]-9- methyl-4H-pyrido[l,2-a]pyrimidin-4-one

794 2-(8-ethyl-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(8aR)-hexa hydropyrrolo[l,2-a]pyrazin- 2(lH)-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

795 2-(8-ethyl-2-methylimidazo[l,2-a]pyridin-6-yl)-7-[(8aS)-hexa hydropyrrolo[l,2-a]pyrazin- 2(lH)-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

796 9-methyl-2-(2-methyl-2H-indazol-5-yl)-7-(piperidin-4-yl)-4H- pyrazino[l,2-a]pyrimidin-4-one

797 7-[(3R)-3-(aminomethyl)pyrrolidin-l-yl]-2-(4,6-dimethylpyraz olo[l,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

798 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[(2S,6S)-2,6-d imethyl-l,2,3,6- tetrahydropyridin-4-yl]-4H-pyrido[l,2-a]pyrimidin-4-one

799 7-{(3R)-3-[(dimethylamino)methyl]pyrrolidin-l-yl}-2-(4,6-dim ethylpyrazolo[l,5-a]pyrazin-2- yl)-4H-pyrido[l,2-a]pyrimidin-4-one

800 7-[(2S,6S)-2,6-dimethylpiperidin-4-yl]-2-(4,6-dimethylpyrazo lo[l,5-a]pyrazin-2-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

836 2-(6-methylimidazo[l,2-a]pyridin-2-yl)-7-(4-methylpiperazin- l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

837 2'-methyl-7-(piperazin-l-yl)-4H,4'H-2,7'-bipyrido[l,2-a]pyri midine-4,4'-dione

838 2-[4-(difluoromethoxy)-3-fluorophenyl]-7-(piperazin-l-yl)-4H -pyrido[l,2-a]pyrimidin-4-one

839 2-(5-fluoro-6-hydroxypyridin-3-yl)-7-(piperazin-l-yl)-4H-pyr ido[l,2-a]pyrimidin-4-one

840 2-(4-hydroxy-2-methylquinazolin-6-yl)-7-(piperazin-l-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

841 2-[6-(dimethylamino)pyridin-3-yl]-7-(l-methylpiperidin-4-yl) -4H-pyrido[l,2-a]pyrimidm one Cpd Name

842 7-(l-ethyl-l,2,3,6 etrahydropyridin-4-yl)-2-(2-methylimidazo[l,2-b]pyridazin-6- yl)-4H^ pyrazino[l,2-a]pyrimidin-4-one

843 2-[4-(dimethylamino)-6-methylpyrazolo[l,5-a]pyrazin-2-yl]-7- (4-methylpiperazin-l-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

844 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[3-(trifluorom ethyl)piperazin-l-yl]-4H- pyrido[l,2-a]pyrimidin-4-one

845 2-(l,7-dimethyl-lH-indazol-5-yl)-7-(4-ethylpiperazin-l-yl)-4 H-pyrido[l,2-a]pyrimidin-4-one

846 2-(l,7-dimethyl-lH-indazol-5-yl)-7-(4-methylpiperazin-l-yl)- 4H-pyrido[l,2-a]pyrimidin-4- one

847 tert-butyl 4-[2-(4-hydroxy-2-methoxyphenyl)-4-oxo-4H-pyrido[l,2-a]pyrim idin-7-yl]-3,6- dihydropyridine- 1 (2H)-carboxylate

848 tert-butyl 4-[2-(2-methoxy-4-{[(trifluoromethyl)sulfonyl]oxy}phenyl)-4- oxo-4H-pyrido[l,2- a]pyrimidin-7-yl]-3,6-dihydropyridine-l(2H)-carboxylate

849 ¹ 2-[4-(2-hydroxypyridin-4-yl)-2-methoxyphenyl]-7-(l,2,3,6 etrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

850 ¹ 2-[2-hydroxy-4-(2-hydroxypyridin-4-yl)phenyl]-7-(l,2,3,6-tet rahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

851 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-[ methyl(2,2,6,6- tetramethylpiperidin-4-yl)amino]-4H-pyrido[l,2-a]pyrimidin-4 -one

852 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-[meth yl(2,2,6,6 etramethyl^

4-yl)amino]-4H-pyrido[l,2-a]pyrimidin-4-one

853 9-methyl-2-(2-methyl-2H-indazol-5-yl)-7-[m

4H-pyrido[l,2-a]pyrimidin-4-one

854 7-(piperazin-l-yl)-2-[l-(tetrahydro-2H-pyran-2-yl)-lH-pyrazo l-4-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

855 ¹ 7-(piperazin-l-yl)-2-(lH-pyrazol-4-yl)-4H-pyrido[l,2-a]pyrim idin-4-one

856 ¹ 7-[(3S)-3-methylpiperazin-l-yl]-2-(2-methylpyrazolo[l,5-a]py ridin-5-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

857 2-(2-methylpyrazolo[l,5-a]pyridin-5-yl)-7-(l,2,3,6-tetrahydr opyridin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

858 7-(l-ethyl-l,2,3,6 etrahydropyridin-4-yl)-2-(2-methylpyrazolo[l,5-a]pyridin-5-y l)-4H- pyrido[l,2-a]pyrimidin-4-one

859 ¹ 2-(2-methylpyrazolo[l,5-a]pyridin-5-yl)-7-(piperazin-l-yl)-4 H-pyrido[l,2-a]pyrimidin-4-one

860 ¹ 2-(l,7-dimethyl H-pyrazolo[4,3-b]pyridin-5-yl)-7-(l,2,3,6 etrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

861 ¹ 2-(l,7-dimethyl H-pyrazolo[3,4-c]pyridin-5-yl)-7-(l,2,3,6 etrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

862 ¹ 2-(2,7-dimethyl-2H-pyrazolo[3,4-c]pyridin-5-yl)-7-(l,2,3,6 etrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one Cpd Name

863 ¹ 2-(2,7-dimethyl-2H-pyrazolo[4,3-b]pyridin-5-yl)-7-(l,2,3,6 etrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

864 7-(l-ethylpiperidin-4-yl)-9-methyl-2-(2-methyl-2H-indazol-5- yl)-4H-pyrazino[l,2- a]pyrimidin-4-one

865 9-methyl-2-(2-methyl-2H-indazol-5-yl)-7-(2,2,6,6 etramethyl-l,2,3,6 etrahydropyridin-4-yl^ 4H-pyrido[l,2-a]pyrimidin-4-one

866 2-(2,7-dimethyl-2H-indazol-5-yl)-9-methyl-7-(2,2,6,6 etramethylpiperidin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one

867 9-methyl-2-(2-methyl-2H-indazol-5-yl)-7-(2,2,6,6 etramethylpiperidin-4-yl)-4H-pyrido[l _^ a]pyrimidin-4-one

868 2-(2,8-dimethylimidazo[l,2-a]pyridin-6-yl)-7-(4-methylpipera zin-l-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

869 2-(7-fluoro-2-methyl-2H-indazol-5-yl)-9-methyl-7-(piperidin- 4-yl)-4H-pyrazino[l,2- a]pyrimidin-4-one

870 ¹ 9-methyl-2-(2-methylimidazo[l,2-b]pyridazin-6-yl)-7^

a]pyrimidin-4-one

871 ¹ 2-(2,7-dimethyl-2H-indazol-5-yl)-9-methyl-7-(piperidin-4-yl) -4H-pyrazino[l,2-a]pyrimidm one

872 7-(l-ethylpiperidin-4-yl)-2-(7-fluoro-2-methyl-2H-indazol-5- yl)-9-methyl-4H-pyrazino[l _^ a]pyrimidin-4-one

873 7-(l-ethylpiperidin-4-yl)-9-methyl-2-(2-methylimidazo[l,2-b] pyridazin-6-yl)-4H- pyrazino[l,2-a]pyrimidin-4-one

874 ¹ 2-(2,7-dimethyl-2H-indazol-5-yl)-7-(l-ethylpiperidin-4-yl)-9 -methyl-4H-pyrazino[l,2- a]pyrimidin-4-one

875 ¹ 2-(8-fluoro-2-methylimidazo[l,2-a]pyridin-6-yl)-9-methyl-7-( piperidin-4-yl)-4H-pyrazin^ a]pyrimidin-4-one

876 2-(l,3-dimethylpyrrolo[l,2-a]pyrazin-7-yl)-7-(l-ethylpiperid in-4-yl)-9-methyl-4H- pyrazino[l,2-a]pyrimidin-4-one, or

877 7-(l -ethylpiperidin-4-yl)-2-(8-fluoro-2-methylim^

pyrazino[l,2-a]pyrimidin-4-one wherein the form of the compound is selected from the group consisting of a salt, prodrug, hydrate, solvate, clathrate, isotopologue, racemate, enantiomer, diastereomer, stereoisomer, polymorph and tautomer form thereof. An aspect of the compound of Formula (I) or a form thereof is a compound selected from the group consisting of (where compound number (#*) indicates that a salt form of the compound was isolated):

Cpd Name

836 2-(6-methylimidazo[ 1 ,2-a]pyridin-2-yl)-7-(4-methylpiperazin- 1 -yl)-4H-pyrido[ 1 ,2- a]pyrimidin-4-one

837 2'-methyl-7-(piperazin- 1 -yl)-4H,4'H-2,7'-bipyrido[ 1 ,2-a]pyrimidine-4,4'-dione

838 2-[4-(difluoromethoxy)-3 -fluorophenyl]-7-(piperazin- 1 -yl)-4H-pyrido[ 1 ,2-a]pyrimidin-4- one

839 2-(5-fluoro-6-hydroxypyridin-3-yl)-7-(piperazin-l-yl)-4H-pyr ido[l,2-a]pyrimidin-4-one

840 2-(4-hydroxy-2-m ethyl quinazolin-6-yl)-7-(piperazin- 1 -yl)-4H-pyrido[ 1 ,2-a]pyrimidin-4- one

841 2-[6-(dimethylamino)pyridin-3-yl]-7-(l-methylpiperidin-4-yl) -4H-pyrido[l,2-a]pyrimidin- 4-one

842 7-( 1 -ethyl- 1 ,2,3 ,6-tetrahydropyridin-4-yl)-2-(2-methylimidazo[ 1 ,2-b]pyridazin-6-yl)-4H- pyrazino[ 1 ,2-a]pyrimidin-4-one

843 2-[4-(dimethylamino)-6-methylpyrazolo[l,5-a]pyrazin-2-yl]-7- (4-methylpiperazin-l-yl)- 4H-pyrido[ 1 ,2-a]pyrimidin-4-one

844 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-7-[3-(trifluorom ethyl)piperazin-l-yl]-4H- pyrido[ 1 ,2-a]pyrimidin-4-one

845 2-(l,7-dimethyl-lH-indazol-5-yl)-7-(4-ethylpiperazin-l-yl)-4 H-pyrido[l,2-a]pyrimidin-4- one

846 2-(l,7-dimethyl-lH-indazol-5-yl)-7-(4-methylpiperazin-l-yl)- 4H-pyrido[l,2-a]pyrimidin- 4-one

847 tert-butyl 4-[2-(4-hydroxy-2-methoxyphenyl)-4-oxo-4H-pyrido[l,2-a]pyrim idin-7-yl]-3,6- dihydropyridine-l(2H)-carboxylate

848 tert-butyl 4-[2-(2-methoxy-4-{ [(trifluoromethyl)sulfonyl]oxy}phenyl)-4-oxo-4H- pyrido[ 1 ,2-a]pyrimidin-7-yl]-3 ,6-dihydropyridine- 1 (2H)-carboxylate

849 ¹ 2-[4-(2-hydroxypyridin-4-yl)-2-methoxyphenyl]-7-(l,2,3,6-tet rahydropyridin-4-yl)-4H- pyrido[ 1 ,2-a]pyrimidin-4-one

850 ¹ 2-[2-hydroxy-4-(2-hydroxypyridin-4-yl)phenyl]-7-(l,2,3,6-tet rahydropyridin-4-yl)-4H- pyrido[ 1 ,2-a]pyrimidin-4-one

851 2-(4-ethyl-6-methylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-[ methyl(2,2,6,6- tetramethylpiperidin-4-yl)amino]-4H-pyrido[l,2-a]pyrimidin-4 -one

852 2-(4,6-dimethylpyrazolo[l,5-a]pyrazin-2-yl)-9-methyl-7-[meth yl(2,2,6,6- tetramethylpiperidin-4-yl)amino]-4H-pyrido[l,2-a]pyrimidin-4 -one

853 9-methyl-2-(2-methyl-2H-indazol-5-yl)-7-[methyl(2,2,6,6-tetr amethylpiperidin-4- yl)amino]-4H-pyrido[l,2-a]pyrimidin-4-one Cpd Name

854 7-(piperazin-l-yl)-2-[l-(tetrahydro-2H-pyran-2-yl)-lH-pyrazo l-4-yl]-4H-pyrido[l,2- a]pyrimidin-4-one

855 ¹ 7-(piperazin-l-yl)-2-(lH-pyrazol-4-yl)-4H-pyrido[l,2-a]pyrim idin-4-one

856 ¹ 7-[(3 S)-3 -methylpiperazin- 1 -yl]-2-(2-methylpyrazolo[ 1 , 5-a]pyridin-5-yl)-4H-pyrido[ 1 ,2- a]pyrimidin-4-one

857 2-(2-methylpyrazolo[l,5-a]pyridin-5-yl)-7-(l,2,3,6-tetrahydr opyridin-4-yl)-4H-pyrido[l,2- a]pyrimidin-4-one

858 7-(l-ethyl-l,2,3,6-tetrahydropyridin-4-yl)-2-(2-methylpyrazo lo[l,5-a]pyridin-5-yl)-4H- pyrido[ 1 ,2-a]pyrimidin-4-one

859 ¹ 2-(2-methylpyrazolo[ 1 ,5 -a]pyridin-5-yl)-7-(piperazin- 1 -yl)-4H-pyrido[ 1 ,2-a]pyrimidin-4- one

860 ¹ 2-(l,7-dimethyl-lH-pyrazolo[4,3-b]pyridin-5-yl)-7-(l,2,3,6-t etrahydropyridin-4-yl)-4H- pyrido[ 1 ,2-a]pyrimidin-4-one

861 ¹ 2 l,7-dimethyl-lH-pyrazolo[3,4-c]pyridin-5-yl)-7-(l,2,3,6-tetr ahydropyridin-4-yl)-4H- pyrido[ 1 ,2-a]pyrimidin-4-one

862 ¹ 2-(2,7-dimethyl-2H-pyrazolo[3,4-c]pyridin-5-yl)-7-(l,2,3,6-t etrahydropyridin-4-yl)-4H- pyrido[ 1 ,2-a]pyrimidin-4-one

863 ¹ 2-(2,7-dimethyl-2H-pyrazolo[4,3-b]pyridin-5-yl)-7-(l,2,3,6-t etrahydropyridin-4-yl)-4H- pyrido[ 1 ,2-a]pyrimidin-4-one

864 7-(l-ethylpiperidin-4-yl)-9-methyl-2-(2-methyl-2H-indazol-5- yl)-4H-pyrazino[l,2- a]pyrimidin-4-one

865 9-methyl-2 2-methyl-2H-indazol-5-yl)-7-(2,2,6,64etramethyl-l,2,3,6-tetr ahydropyridin- 4-yl)-4H-pyrido[ 1 ,2-a]pyrimidin-4-one

866 2 2,7-dimethyl-2H-indazol-5-yl)-9-methyl-7-(2,2,6,6-tetramethy lpiperidin-4-yl)-4H- pyrido[ 1 ,2-a]pyrimidin-4-one

867 9-methyl-2 2-methyl-2H-indazol-5-yl)-7-(2,2,6,6-tetramethylpiperidin-4- yl)-4H- pyrido[ 1 ,2-a]pyrimidin-4-one

868 2-(2,8-dimethylimidazo[ 1 ,2-a]pyridin-6-yl)-7-(4-methylpiperazin- 1 -yl)-4H-pyrido[ 1 ,2- a]pyrimidin-4-one

869 2-(7-fluoro-2-methyl-2H-indazol-5-yl)-9-methyl-7-(piperidin- 4-yl)-4H-pyrazino[l,2- a]pyrimidin-4-one

870 ¹ 9-methyl-2-(2-methylimidazo[ 1 ,2-b]pyridazin-6-yl)-7-(piperidin-4-yl)-4H-pyrazino[ 1 ,2- a]pyrimidin-4-one

871 ¹ 2-(2,7-dimethyl-2H-indazol-5-yl)-9-methyl-7-(piperidin-4-yl) -4H-pyrazino[l,2- a]pyrimidin-4-one

872 7-(l-ethylpiperidin-4-yl)-2-(7-fluoro-2-methyl-2H-indazol-5- yl)-9-methyl-4H- pyrazino[ 1 ,2-a]pyrimidin-4-one

873 7-(l-ethylpiperidin-4-yl)-9-methyl-2-(2-methylimidazo[l,2-b] pyridazin-6-yl)-4H- pyrazino[ 1 ,2-a]pyrimidin-4-one Cpd Name

874 ¹ 2-(2,7-dimethyl-2H-indazol-5-yl)-7-(l-ethylpiperidin-4-yl)-9 -methyl-4H-pyrazino[l,2- a]pyrimidin-4-one

875 ¹ 2-(8-fluoro-2-methylimidazo[ 1 ,2-a]pyridin-6-yl)-9-methyl-7-(piperidin-4-yl)-4H- pyrazino[ 1 ,2-a]pyrimidin-4-one

876 2 l,3-dimethylpyrrolo[l,2-a]pyrazin-7-yl)-7-(l-ethylpiperidin- 4-yl)-9-methyl-4H- pyrazino[ 1 ,2-a]pyrimidin-4-one, or

877 7-(l-ethylpiperidin-4-yl)-2-(8-fluoro-2-methylimidazo[l,2-a] pyridin-6-yl)-9-methyl-4H- pyrazino[ 1 ,2-a]pyrimidin-4-one wherein the form of the compound is selected from the group consisting of a salt, prodrug, hydrate, solvate, clathrate, isotopologue, racemate, enantiomer, diastereomer, stereoisomer, polymorph and tautomer form thereof.

Another aspect of the present description includes a method of use of a compound of Formula (I) or a form thereof for treating or ameliorating FID in a subject in need thereof, comprising administering an effective amount of the compound of Formula (I) or a form thereof to the subject.

Another aspect of the present description includes a use of the compound of Formula (I) or a form thereof for treating or ameliorating FID in a subject in need thereof, comprising

administering an effective amount of the compound of Formula (I) or a form thereof to the subject.

Another aspect of the present description includes a use of the compound salt of Formula (I) or a form thereof for treating or ameliorating HD in a subject in need thereof, comprising administering an effective amount of the compound salt of Formula (I) or a form thereof to the subject.

Another aspect of the present description includes a method of use of a compound salt of Formula (I) or a form thereof for treating or ameliorating HD in a subject in need thereof, comprising administering an effective amount of the compound salt of Formula (I) thereof to the subject, wherein the compound salt is selected from the group consisting of:

Cpd Name

2-(3,5-difluoro-4-hydroxyphenyl)-7-(piperazin-l-yl)-4H-pyrid o[l,2-a]pyrimidin-4-one 71 hy drochl ori de ( 1 : 1 ) Cpd Name

7-[4-(dimethylamino)piperidin-l-yl]-2-(3-fluoro-4-methoxyphe nyl)-4H-quinolizin-4-one 203 acetate (1 : 1)

380 2-(2 -methyl- 1 ,3 -benzothiazol-6-yl)-7-(piperidin-4-yl)-4H-pyrimido[ 1 ,2-b]pyridazin-4-one trifluoroacetate (1 : 1)

413 2-(l,3-dimethylpyrrolo[l,2-a]pyrazin-7-yl)-7-(l,2,3,6-tetrah ydropyridin-4-yl)-4H- pyrazino[l,2-a]pyrimidin-4-one hydrochloride (1 :2)

849 2-[4-(2-hydroxypyridin-4-yl)-2-methoxyphenyl]-7-(l,2,3,6-tet rahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one hydrochloride (1 : 1)

850 2-[2-hydroxy-4-(2-hydroxypyridin-4-yl)phenyl]-7-(l,2,3,6-tet rahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one trifluoroacetate (1 : 1)

855 7-(piperazin-l-yl)-2-(lH-pyrazol-4-yl)-4H-pyrido[l,2-a]pyrim idin-4-one

hydrochloride (1 : 1)

856 7-[(3 S)-3 -methylpiperazin- 1 -yl]-2-(2-methylpyrazolo[ 1 , 5-a]pyridin-5-yl)-4H-pyrido[ 1 ,2- a]pyrimidin-4-one hydrochloride (1 :2)

859 2-(2-methylpyrazolo[ 1 ,5 -a]pyridin-5-yl)-7-(piperazin- 1 -yl)-4H-pyrido[ 1 ,2-a]pyrimidin-4- one hydrochloride (1 :2)

860 2-(l,7-dimethyl-lH-pyrazolo[4,3-b]pyridin-5-yl)-7-(l,2,3,6-t etrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one hydrochloride (1 :2)

861 2-(l,7-dimethyl-lH-pyrazolo[3,4-c]pyridin-5-yl)-7-(l,2,3,6-t etrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one hydrochloride (1 :2)

862 2-(2,7-dimethyl-2H-pyrazolo[3,4-c]pyridin-5-yl)-7-(l,2,3,6-t etrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one hydrochloride (1 :2)

863 2-(2,7-dimethyl-2H-pyrazolo[4,3-b]pyridin-5-yl)-7-(l,2,3,6-t etrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one hydrochloride (1 :2)

870 9-methyl-2-(2-methylimidazo[ 1 ,2-b]pyridazin-6-yl)-7-(piperidin-4-yl)-4H-pyrazino[ 1 ,2- a]pyrimidin-4-one hydrochloride (1 :2)

871 2-(2,7-dimethyl-2H-indazol-5-yl)-9-methyl-7-(piperidin-4-yl) -4H-pyrazino[l,2- a]pyrimidin-4-one hydrochloride (1 : 1)

874 2-(2,7-dimethyl-2H-indazol-5-yl)-7-(l-ethylpiperidin-4-yl)-9 -methyl-4H-pyrazino[l,2- a]pyrimidin-4-one hydrochloride (1 : 1), or

875 2-(8-fluoro-2-methylimidazo[ 1 ,2-a]pyridin-6-yl)-9-methyl-7-(piperidin-4-yl)-4H- pyrazino[l,2-a]pyrimidin-4-one hydrochloride (1 :2) wherein the form of the compound salt is selected from the group consisting of a prodrug, hydrate, solvate, clathrate, isotopologue, racemate, enantiomer, diastereomer, stereoisomer, polymorph and tautomer form thereof. An aspect of the compound of Formula (I) or a form thereof is a compound salt selected from the group consisting of:

Cpd Name

849 2-[4-(2-hydroxypyridin-4-yl)-2-methoxyphenyl]-7-(l,2,3,6-tet rahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one hydrochloride (1 : 1)

850 2-[2-hydroxy-4-(2-hydroxypyridin-4-yl)phenyl]-7-(l,2,3,6-tet rahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one trifluoroacetate (1 : 1)

855 7-(piperazin-l-yl)-2-(lH-pyrazol-4-yl)-4H-pyrido[l,2-a]pyrim idin-4-one

hydrochloride (1 : 1)

856 7-[(3 S)-3 -methylpiperazin- 1 -yl]-2-(2-methylpyrazolo[ 1 , 5-a]pyridin-5-yl)-4H-pyrido[ 1 ,2- a]pyrimidin-4-one hydrochloride (1 :2)

859 2-(2-methylpyrazolo[ 1 ,5 -a]pyridin-5-yl)-7-(piperazin- 1 -yl)-4H-pyrido[ 1 ,2-a]pyrimidin-4- one hydrochloride (1 :2)

860 2-(l,7-dimethyl-lH-pyrazolo[4,3-b]pyridin-5-yl)-7-(l,2,3,6-t etrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one hydrochloride (1 :2)

861 2-(l,7-dimethyl-lH-pyrazolo[3,4-c]pyridin-5-yl)-7-(l,2,3,6-t etrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one hydrochloride (1 :2)

862 2-(2,7-dimethyl-2H-pyrazolo[3,4-c]pyridin-5-yl)-7-(l,2,3,6-t etrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one hydrochloride (1 :2)

863 2-(2,7-dimethyl-2H-pyrazolo[4,3-b]pyridin-5-yl)-7-(l,2,3,6-t etrahydropyridin-4-yl)-4H- pyrido[l,2-a]pyrimidin-4-one hydrochloride (1 :2)

870 9-m ethyl -2-(2-methylimidazo[ 1 ,2-b]pyridazin-6-yl)-7-(piperidin-4-yl)-4H-pyrazino[ 1 ,2- a]pyrimidin-4-one hydrochloride (1 :2)

871 2-(2,7-dimethyl-2H-indazol-5-yl)-9-methyl-7-(piperidin-4-yl) -4H-pyrazino[l,2- a]pyrimidin-4-one hydrochloride (1 : 1)

874 2-(2,7-dimethyl-2H-indazol-5-yl)-7-(l-ethylpiperidin-4-yl)-9 -methyl-4H-pyrazino[l,2- a]pyrimidin-4-one hydrochloride (1 : 1), or

875 2-(8-fluoro-2-methylimidazo[ 1 ,2-a]pyridin-6-yl)-9-methyl-7-(piperidin-4-yl)-4H- pyrazino[l,2-a]pyrimidin-4-one hydrochloride (1 :2) wherein the form of the compound salt is selected from the group consisting of a prodrug, hydrate, solvate, clathrate, isotopologue, racemate, enantiomer, diastereomer, stereoisomer, polymorph and tautomer form thereof.

CHEMICAL DEFINITIONS

The chemical terms used above and throughout the description herein, unless specifically defined otherwise, shall be understood by one of ordinary skill in the art to have the following indicated meanings. As used herein, the term "Ci-salkyl" generally refers to saturated hydrocarbon radicals having from one to eight carbon atoms in a straight or branched chain configuration, including, but not limited to, methyl, ethyl, n-propyl (also referred to as propyl or propanyl), isopropyl, n-butyl (also referred to as butyl or butanyl), isobutyl, sec-butyl, tert-butyl, n-pentyl (also referred to as pentyl or pentanyl), n-hexyl (also referred to as hexyl or hexanyl), n-heptyl (also referred to as heptyl or heptanyl), n-octyl and the like. In some aspects, Ci-salkyl includes, but is not limited to, Ci-6alkyl, Ci-4alkyl and the like. A Ci-salkyl radical is optionally substituted with substituent species as described herein where allowed by available valences.

As used herein, the term "C2-8alkenyl" generally refers to partially unsaturated

hydrocarbon radicals having from two to eight carbon atoms in a straight or branched chain configuration and one or more carbon-carbon double bonds therein, including, but not limited to, ethenyl (also referred to as vinyl), allyl, propenyl and the like. In some aspects, C ₂ -8alkenyl includes, but is not limited to, C ₂ -6alkenyl, C ₂ -4alkenyl and the like. A C ₂ -8alkenyl radical is optionally substituted with substituent species as described herein where allowed by available valences.

As used herein, the term "C ₂ -8alkynyl" generally refers to partially unsaturated

hydrocarbon radicals having from two to eight carbon atoms in a straight or branched chain configuration and one or more carbon-carbon triple bonds therein, including, but not limited to, ethynyl, propynyl, butynyl and the like. In some aspects, C ₂ -8alkynyl includes, but is not limited to, C ₂ -6alkynyl, C ₂ -4alkynyl and the like. A C ₂ -8alkynyl radical is optionally substituted with substituent species as described herein where allowed by available valences.

As used herein, the term "Ci-salkoxy" generally refers to saturated hydrocarbon radicals having from one to eight carbon atoms in a straight or branched chain configuration of the formula: -O-Ci-salkyl, including, but not limited to, methoxy, ethoxy, n-propoxy, isopropoxy, n-butoxy, isobutoxy, sec-butoxy, tert-butoxy, n-pentoxy, n-hexoxy and the like. In some aspects, Ci-salkoxy includes, but is not limited to, Ci-6alkoxy, Ci-4alkoxy and the like. A Ci-salkoxy radical is optionally substituted with substituent species as described herein where allowed by available valences.

As used herein, the term "C3-i4cycloalkyl" generally refers to a saturated or partially unsaturated monocyclic, bicyclic or polycyclic hydrocarbon radical, including, but not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, cycloheptyl, cyclooctyl, lH-indanyl, indenyl, tetrahydro-naphthalenyl and the like. In some aspects, C3-i4cycloalkyl includes, but is not limited to, C3- ₈ cycloalkyl, Cs-scycloalkyl, C3-iocycloalkyl and the like. A C3-i4cycloalkyl radical is optionally substituted with substituent species as described herein where allowed by available valences.

As used herein, the term "aryl" generally refers to a monocyclic, bicyclic or polycyclic aromatic carbon atom ring structure radical, including, but not limited to, phenyl, naphthyl, anthracenyl, fluorenyl, azulenyl, phenanthrenyl and the like. An aryl radical is optionally substituted with substituent species as described herein where allowed by available valences.

As used herein, the term "heteroaryl" generally refers to a monocyclic, bicyclic or polycyclic aromatic carbon atom ring structure radical in which one or more carbon atom ring members have been replaced, where allowed by structural stability, with one or more

heteroatoms, such as an O, S or N atom, including, but not limited to, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, isoxazolyl, isothiazolyl, oxazolyl, 1,3-thiazolyl, triazolyl, oxadiazolyl, thiadiazolyl, tetrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, triazinyl, indolyl, indazolyl, indolizinyl, isoindolyl, benzofuranyl, benzothienyl, benzoimidazolyl, 1,3-benzothiazolyl,

1,3-benzoxazolyl, purinyl, quinolinyl, isoquinolinyl, quinazolinyl, quinoxalinyl, 1,3-diazinyl, 1,2-diazinyl, 1,2-diazolyl, 1,4-diazanaphthalenyl, acridinyl, furo[3,2-£]pyridinyl,

furo[3,2-c]pyridinyl, furo[2,3-c]pyridinyl, 6H-thieno[2,3-£]pyrrolyl, thieno[3,2-c]pyridinyl, thieno[2,3-<i]pyrimidinyl, lH-pyrrolo[2,3-£]pyridinyl, lH-pyrrolo[2,3-c]pyridinyl,

lH-pyrrolo[3 ,2-£]pyridinyl, pyrrolo[ 1 ,2-a]pyrazinyl, pyrrolo[ 1 ,2-£]pyridazinyl,

pyrazolo[l,5-a]pyridinyl, pyrazolo[l,5-a]pyrazinyl, pyrazolo[4,3-b]pyridinyl,

pyrazolo[3,4-c]pyridinyl, imidazo[l,2-a]pyridinyl, 3H-imidazo[4,5-£]pyridinyl,

imidazo[ 1 ,2-a]pyrimidinyl, imidazo[ 1 ,2-c]pyrimidinyl, imidazo[ 1 ,2-£]pyridazinyl,

imidazo[ 1 ,2-a]pyrazinyl, imidazo[2, 1 -b] [ 1 ,3 Jthiazolyl, imidazo[2, 1 -b] [ 1 ,3 ,4]thiadiazolyl,

[l,3]oxazolo[4,5-£]pyridinyl, [l,2,4]triazolo[l,5-a]pyridinyl, [l,2,4]triazolo[4,3-a]pyridinyl, [ 1 ,2,4]triazolo[ 1 ,5-a]pyrimidinyl, [ 1 ,2,4]triazolo[ 1 , 5-b]pyridazinyl, pyrido[ 1 ,2-a]pyrimidinyl or pyrido[l,2-a]pyrimidinone and the like. A heteroaryl radical is optionally substituted on a carbon or nitrogen atom ring member with substituent species as described herein where allowed by available valences.

In certain aspects, the nomenclature for a heteroaryl radical may differ, such as in non- limiting examples where furanyl may also be referred to as furyl, thienyl may also be referred to as thiophenyl, pyridinyl may also be referred to as pyridyl, benzothienyl may also be referred to as benzothiophenyl and 1,3-benzoxazolyl may also be referred to as 1,3-benzooxazolyl.

In certain other aspects, the term for a heteroaryl radical may also include other regioisomers, such as in non-limiting examples where the term pyrrolyl may also include

2H-pyrrolyl, 3H-pyrrolyl and the like, the term pyrazolyl may also include lH-pyrazolyl and the like, the term imidazolyl may also include lH-imidazolyl and the like, the term triazolyl may also include IH- 1,2,3 -triazolyl and the like, the term oxadiazolyl may also include 1,2,4-oxadiazolyl, 1,3,4-oxadiazolyl and the like, the term tetrazolyl may also include lH-tetrazolyl, 2H-tetrazolyl and the like, the term indolyl may also include lH-indolyl and the like, the term indazolyl may also include lH-indazolyl, 2H-indazolyl and the like, the term benzoimidazolyl may also include lH-benzoimidazolyl and the term purinyl may also include 9H-purinyl and the like.

As used herein, the term "heterocyclyl" generally refers to a saturated or partially unsaturated monocyclic, bicyclic or polycyclic carbon atom ring structure radical in which one or more carbon atom ring members have been replaced, where allowed by structural stability, with a heteroatom, such as an O, S or N atom, including, but not limited to, oxiranyl, oxetanyl, azetidinyl, tetrahydrofuranyl, pyrrolinyl, pyrrolidinyl, pyrazolinyl, pyrazolidinyl, imidazolinyl, imidazolidinyl, isoxazolinyl, isoxazolidinyl, isothiazolinyl, isothiazolidinyl, oxazolinyl, oxazolidinyl, thiazolinyl, thiazolidinyl, triazolinyl, triazolidinyl, oxadiazolinyl, oxadiazolidinyl, thiadiazolinyl, thiadiazolidinyl, tetrazolinyl, tetrazolidinyl, pyranyl, dihydro-2H-pyranyl, thiopyranyl, 1,3-dioxanyl, 3,6-dihydropyridinyl, 1,2,5,6-tetrahydropyridinyl,

1,2,3,6-tetrahydropyridinyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl,

1,4-diazepanyl, 1,3-benzodioxolyl, 1,4-benzodioxanyl, 2,3-dihydro-l,4-benzodioxinyl, hexahydropyrrolo[3,4-£]pyrrol-(lH)-yl, (3a,S',6a ₎ S)-hexahydropyrrolo[3,4-^]pyrrol-(lH)-yl, (3aR,6aR)-hexahydropyrrolo[3,4-£]pyrrol-(lH)-yl, hexahydropyrrolo[3,4-£]pyrrol-(2H)-yl, (3a,S',6a ₎ S)-hexahydropyrrolo[3,4-^]pyrrol-(2H)-yl,

(3aR,6aR)-hexahydropyrrolo[3,4-£]pyrrol-(2H)-yl, hexahydropyrrolo[3,4-c]pyrrol-(lH)-yl, l,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrolyl, (3aR,6a,S)-hexahydropyrrolo[3,4-c]pyrrol-(lH)-yl, (3aR,6aR)-hexahydropyrrolo[3,4-c]pyrrol-(lH)-yl, octahydro-5H-pyrrolo[3,2-c]pyridinyl, octahydro-6H-pyrrolo[3,4-£]pyridinyl, (4aR,7aR)-octahydro-6H-pyirolo[3,4-£]pyridinyl,

(4a,S',7a ₎ S)-octahydro-6H-pyrrolo[3,4-^]pyridinyl, hexahydropyrrolo[l,2-a]pyrazin-(lH)-yl, (7R, 8 a^-hexahy dropyrrol o [ 1 , 2-a] pyrazin-( lH)-yl , (8a,S)-hexahydropyrrolo[l,2-a]pyrazin-(lH)-yl, (8aR)-hexahydropyrrolo[l,2-a]pyrazin-(lH)-yl,

(8a,S)-3,4,6,7,8,8a-hexahydro-lH-pyrrolo[l,2-a]pyrazinyl,

(8aR)-3, 4,6,7,8, 8a-hexahydro-lH-pyrrolo[l,2-a]pyrazinyl,

(8a,S)-l,3,4,6,7,8-hexahydropyrrolo[l,2-a]pyrazinyl,

(8aR)-l,3,4,6,7,8-hexahydropyrrolo[l,2-a]pyrazinyl,

(8a,S)-octahydropyrrolo[l,2-a]pyrazin-(lH)-yl, (8aR)-octahydropyrrolo[l,2-a]pyrazin-(lH)-yl, hexahydropyrrolo[ 1 ,2-a]pyrazin-(2H)-one, octahydro-2H-pyrido[ 1 ,2-a]pyrazinyl,

(3aR,4aR,7aS)-hexahydro-lH-cyclobuta[l,2-c: l,4-c']dipyrrol-(3H)-yl, 3-azabicyclo[3.1.0]hexyl, (lR,55)-3-azabicyclo[3.1.0]hexyl, 8-azabicyclo[3.2.1]octyl, (lR,55)-8-azabicyclo[3.2.1]octyl, 8-azabicyclo[3.2.1]oct-2-enyl, (li?,5,S)-8-azabicyclo[3.2.1]oct-2-enyl, 9-azabicyclo[3.3.1]nonyl, (li?,5,S)-9-azabicyclo[3.3.1]nonyl, 2,5-diazabicyclo[2.2.1]heptyl,

(l,S 4,S 2,5-diazabicyclo[2.2.1]heptyl, 2,5-diazabicyclo[2.2.2]octyl,

3.6- diazabicyclo[3.2.0]heptyl, 3,8-diazabicyclo[3.2.1]octyl, (li?,5,S)-3,8-diazabicyclo[3.2.1]octyl, l,4-diazabicyclo[3.2.2]nonyl, azaspiro[3.3]heptyl, 2,6-diazaspiro[3.3]heptyl,

4.7- diazaspiro[2.5]octyl, 2,6-diazaspiro[3.4]octyl, 2,7-diazaspiro[3.5]nonyl,

5.8- diazaspiro[3.5]nonyl, 2,7-diazaspiro[4.4]nonyl, 6,9-diazaspiro[4.5]decyl and the like. A heterocyclyl radical is optionally substituted on a carbon or nitrogen atom ring member with substituent species as described herein where allowed by available valences.

In certain aspects, the nomenclature for a heterocyclyl radical may differ, such as in non- limiting examples where 1,3-benzodioxolyl may also be referred to as benzo[<i][l,3]dioxolyl; 2,3-dihydro-l,4-benzodioxinyl may also be referred to as 2,3-dihydrobenzo[£][l,4]dioxinyl;

2.6- diazaspiro[3.3]heptyl may also be referred to as 2,6-diazaspiro[3.3]heptanyl;

4.7- diazaspiro[2.5]octyl may also be referred to as 4,7-diazaspiro[2.5]octanyl;

2,7-diazaspiro[3.5]nonyl may also be referred to as 2,7-diazaspiro[3.5]nonanyl; and, the like.

As used herein, the term "Ci-salkoxy-Ci-salkyl" refers to a radical of the

formula: -Ci-salkyl-O-Ci-salkyl.

As used herein, the term "Ci-salkoxy-Ci-salkyl-amino" refers to a radical of the formula: - H-Ci-salkyl-O-Ci-salkyl.

As used herein, the term "(Ci-8alkoxy-Ci-8alkyl)2-amino" refers to a radical of the formula: -N(Ci-8alkyl-0-Ci-8alkyl) ₂ . As used herein, the term "Ci-salkoxy-Ci-salkyl-amino-Ci-salkoxy" refers to a radical of the formula: -O-Ci-salkyl- H-Ci-salkyl-O-Ci-salkyl.

As used herein, the term "(Ci-8alkoxy-Ci-8alkyl)2-amino-Ci-8alkoxy" refers to a radical of the formula: -0-Ci-8alkyl-N(Ci.8alkyl-0-Ci. ₈ alkyl)2.

As used herein, the term "(Ci-8alkoxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkoxy" refers to a radical of the formula: -0-Ci-8alkyl-N(Ci-8alkyl)(Ci-8alkyl-0-Ci-8alkyl).

As used herein, the term "Ci-salkoxy-Ci-salkyl-amino-Ci-salkyl" refers to a radical of the formula: -Ci-salkyl- H-Ci-salkyl-O-Ci-salkyl.

As used herein, the term "(Ci-salkoxy-Ci-salkyl^-amino-Ci-salkyl" refers to a radical of the formula: -Ci-8alkyl-N(Ci-8alkyl-0-Ci-8alkyl)2.

As used herein, the term "(Ci-8alkoxy-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl" refers to a radical of the formula: -Ci-8alkyl-N(Ci-8alkyl)(Ci-8alkyl-0-Ci-8alkyl).

As used herein, the term "Ci-salkoxy-carbonyl" refers to a radical of the

formula: -C(0)-0-Ci- ₈ alkyl.

As used herein, the term "Ci-8alkoxy-carbonyl-C2-8alkenyl" refers to a radical of the formula: -C2-8alkenyl-C(0)-0-Ci-8alkyl.

As used herein, the term "Ci-salkoxy-carbonyl-amino" refers to a radical of the formula: -NH-C(0)-0-Ci- ₈ alkyl.

As used herein, the term "Ci-salkyl-amino" refers to a radical of the

formula: -NH-Ci-salkyl.

As used herein, the term "(Ci-8alkyl)2-amino" refers to a radical of the

formula: -N(Ci-8alkyl)2.

As used herein, the term "Ci-8alkyl-amino-C2-8alkenyl" refers to a radical of the formula: -C2-8alkenyl- H-Ci-8alkyl.

As used herein, the term "(Ci-8alkyl)2-amino-C2-8alkenyl" refers to a radical of the formula: -C2-8alkenyl-N(Ci-8alkyl)2.

As used herein, the term "Ci-salkyl-amino-Ci-salkoxy" refers to a radical of the formula: -O-Ci-salkyl-NH-Ci-salkyl.

As used herein, the term "(Ci-8alkyl)2-amino-Ci-8alkoxy" refers to a radical of the formula: -0-Ci-8alkyl-N(Ci-8alkyl) ₂ . As used herein, the term "Ci-salkyl-amino-Ci-salkyl" refers to a radical of the formula: -Ci _-8 alkyl-NH-Ci _-8 alkyl.

As used herein, the term "(Ci- ₈ alkyl) ₂ -amino-Ci- ₈ alkyr refers to a radical of the formula: -Ci-8alkyl-N(Ci-8alkyl)2.

As used herein, the term "Ci- ₈ alkyl-amino-Ci _-8 alkyl-amino" refers to a radical of the formula: - H-Ci _-8 alkyl- H-Ci _-8 alkyl.

As used herein, the term "(Ci-8alkyl)2-amino-Ci-8alkyl-amino" refers to a radical of the formula: - H-Ci-8alkyl-N(Ci-8alkyl) ₂ .

As used herein, the term "(Ci-8alkyl-amino-Ci-8alkyl) ₂ -amino" refers to a radical of the formula: -N(Ci-8alkyl- H-Ci-8alkyl) ₂ .

As used herein, the term "[(Ci-8alkyl) ₂ -amino-Ci-8alkyl] ₂ -amino" refers to a radical of the formula: -N[Ci-8alkyl-N(Ci-8alkyl) ₂ ]2.

As used herein, the term "(Ci-8alkyl-amino-Ci-8alkyl)(Ci-8alkyl)amino" refers to a radical of the formula: -N(Ci- ₈ alkyl)(Ci- ₈ alkyl- H-Ci _-8 alkyl).

As used herein, the term "[(Ci-8alkyl) ₂ -amino-Ci-8alkyl](Ci-8alkyl)amino" refers to a radical of the formula: -N(Ci-8alkyl)[Ci-8alkyl-N(Ci-8alkyl) ₂ ].

As used herein, the term "Ci-8alkyl-amino-C2-8alkynyl" refers to a radical of the formula: -C ₂ -8alkynyl- H-Ci-8alkyl.

As used herein, the term "(Ci-8alkyl)2-amino-C2-8alkynyl" refers to a radical of the formula: -C ₂ -8alkynyl-N(Ci-8alkyl) ₂ .

As used herein, the term "Ci- ₈ alkyl-carbonyl" refers to a radical of the

formula: -C(0)-Ci- ₈ alkyl.

As used herein, the term "Ci _-8 alkyl-carbonyl-amino" refers to a radical of the

formula: -NH-C(0)-Ci- ₈ alkyl.

As used herein, the term "Ci _-8 alkyl-thio" refers to a radical of the formula: -S-Ci _-8 alkyl.

As used herein, the term "amino-C ₂ - ₈ alkenyl" refers to a radical of the

formula: -C ₂ - ₈ alkenyl- H ₂ .

As used herein, the term "amino-Ci _-8 alkoxy" refers to a radical of the

formula: -0-Ci _-8 alkyl- H ₂ .

As used herein, the term "amino-Ci _-8 alkyl" refers to a radical of the

formula: -Ci _-8 alkyl- H ₂ . As used herein, the term "amino-Ci _-8 alkyl -amino" refers to a radical of the

formula: - H-Ci _-8 alkyl- H ₂ .

As used herein, the term "(amino-Ci _-8 alkyl) ₂ -amino" refers to a radical of the

formula: -N(Ci _-8 alkyl- H ₂ ) ₂ .

As used herein, the term "(amino-Ci _-8 alkyl)(Ci _-8 alkyl)amino" refers to a radical of the formula: -N(Ci _-8 alkyl)(Ci _-8 alkyl- H ₂ ).

As used herein, the term "amino-C _2-8 alkynyl" refers to a radical of the

formula: -C _2-8 alkynyl- H ₂ .

As used herein, the term "aryl-Ci _-8 alkoxy-carbonyl" refers to a radical of the

formula: -C(0)-0-Ci- ₈ alkyl-aryl.

As used herein, the term "aryl-Ci _-8 alkyl" refers to a radical of the formula: -Ci _-8 alkyl-aryl.

As used herein, the term "aryl-Ci _-8 alkyl-amino" refers to a radical of the

formula: - H-Ci _-8 alkyl-aryl.

As used herein, the term "(aryl-Ci _-8 alkyl) ₂ -amino" refers to a radical of the

formula: -N(Ci _-8 alkyl-aryl) ₂ .

As used herein, the term "(aryl-Ci _-8 alkyl)(Ci _-8 alkyl)amino" refers to a radical of the formula: -N(Ci _-8 alkyl)(Ci _-8 alkyl-aryl).

As used herein, the term "aryl-Ci- ₈ alkyl-amino-Ci- ₈ alkyl" refers to a radical of the formula: -Ci _-8 alkyl- H-Ci _-8 alkyl-aryl.

As used herein, the term "(aryl-Ci- ₈ alkyl) ₂ -amino-Ci- ₈ alkyl" refers to a radical of the formula: -Ci _-8 alkyl-N(Ci _-8 alkyl-aryl) ₂ .

As used herein, the term "(aryl-Ci- ₈ alkyl)(Ci- ₈ alkyl)amino-Ci- ₈ alkyl" refers to a radical of the formula: -Ci- ₈ alkyl-N(Ci- ₈ alkyl)(Ci _-8 alkyl-aryl).

As used herein, the term "aryl-amino" refers to a radical of the formula: - H-aryl.

As used herein, the term "aryl-amino-carbonyl" refers to a radical of the

formula: -C(0)- H-aryl.

As used herein, the term "aryl-sulfonyloxy-Ci _-8 alkyl" refers to a radical of the

formula: -Ci- ₈ alkyl-0-S0 ₂ -aryl.

As used herein, the term "benzoxy-carbonyl" refers to a radical of the

formula: -C(0)-0-CH ₂ -phenyl. As used herein, the term "C3-i4cycloalkyl-Ci-8alkyl" refers to a radical of the formula: -Ci-8alkyl-C3-i4cycloalkyl.

As used herein, the term "C3-i4cycloalkyl-amino" refers to a radical of the

formula: - H-C3-i4cycloalkyl.

As used herein, the term "C3-i4cycloalkyl-oxy" refers to a radical of the

formula: -0-C3-i4cycloalkyl.

As used herein, the term "halo" or "halogen" generally refers to a halogen atom radical, including fluoro, chloro, bromo and iodo.

As used herein, the term "halo-Ci-salkoxy" refers to a radical of the

formula: -O-Ci-salkyl-halo, wherein Ci-salkyl is partially or completely substituted with one or more halogen atoms where allowed by available valences.

As used herein, the term "halo-Ci-salkyl" refers to a radical of the

formula: -Ci-salkyl-halo, wherein Ci-salkyl is partially or completely substituted with one or more halogen atoms where allowed by available valences.

As used herein, the term "halo-Ci-salkyl -amino" refers to a radical of the

formula: -NH-Ci-salkyl-halo.

As used herein, the term "(halo-Ci-8alkyl)(Ci-8alkyl)amino" refers to a radical of the formula: -N(Ci-8alkyl)(Ci-8alkyl-halo).

As used herein, the term "(halo-Ci-8alkyl)2-amino" refers to a radical of the

formula: -N(Ci-8alkyl-halo)2.

As used herein, the term "heteroaryl-Ci-salkoxy" refers to a radical of the

formula: -O-Ci-salkyl-heteroaryl.

As used herein, the term "heteroaryl-Ci-salkyl" refers to a radical of the

formula: -Ci-salkyl-heteroaryl.

As used herein, the term "heteroaryl-Ci-salkyl-amino" refers to a radical of the formula: - H-Ci-salkyl-heteroaryl.

As used herein, the term "(heteroaryl-Ci-8alkyl)2-amino" refers to a radical of the formul a : -N(C i -salkyl -heteroaryl) ₂ .

As used herein, the term "(heteroaryl-Ci-8alkyl)(Ci-8alkyl)amino" refers to a radical of the formula: -N(Ci-8alkyl)(Ci-8alkyl-heteroaryl). As used herein, the term "heteroaryl-Ci-salkyl-amino-Ci-salkyl" refers to a radical of the formula: -Ci-salkyl-NH-Ci-salkyl-heteroaryl.

As used herein, the term "(heteroaryl-Ci-8alkyl)2-amino-Ci-8alkyl" refers to a radical of the formula: -Ci-8alkyl-N(Ci-8alkyl-heteroaryl)2.

As used herein, the term "(heteroaryl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl" refers to a radical of the formula: -Ci-8alkyl-N(Ci-8alkyl)(Ci-8alkyl-heteroaryl).

As used herein, the term "heteroaryl -amino" refers to a radical of the

formul a : - H-heteroaryl .

As used herein, the term "heterocyclyl-Ci-salkoxy" refers to a radical of the

formula: -O-Ci-salkyl-heterocyclyl.

As used herein, the term "heterocyclyl-Ci-salkyl" refers to a radical of the

formula: -Ci-salkyl-heterocyclyl.

As used herein, the term "heterocyclyl-Ci-salkyl -amino" refers to a radical of the formula: -NH-Ci-salkyl-heterocyclyl.

As used herein, the term "(heterocyclyl-Ci-8alkyl)2-amino" refers to a radical of the formula: -N(Ci-8alkyl-heterocyclyl)2.

As used herein, the term "(heterocyclyl-Ci-8alkyl)(Ci-8alkyl)amino" refers to a radical of the formula: -N(Ci-8alkyl)(Ci-8alkyl-heterocyclyl).

As used herein, the term "heterocyclyl-Ci-salkyl-amino-Ci-salkyl" refers to a radical of the formula: -Ci-salkyl-NH-Ci-salkyl-heterocyclyl.

As used herein, the term "(heterocyclyl-Ci-salkyl^-amino-Ci-salkyl" refers to a radical of the formula: -Ci-8alkyl-N(Ci-8alkyl-heterocyclyl)2.

As used herein, the term "(heterocyclyl-Ci-8alkyl)(Ci-8alkyl)amino-Ci-8alkyl" refers to a radical of the formula: -Ci-8alkyl-N(Ci-8alkyl)(Ci-8alkyl-heterocyclyl).

As used herein, the term "heterocyclyl-amino" refers to a radical of the

formula: - H-heterocyclyl.

As used herein, the term "(heterocyclyl)(Ci-8alkyl)amino" refers to a radical of the formula: -N(Ci-8alkyl)(heterocyclyl).

As used herein, the term "heterocyclyl-amino-C l-salkyl" refers to a radical of the formula: -Ci-salkyl -NH-heterocyclyl. As used herein, the term "heterocyclyl-carbonyl" refers to a radical of the

formula: -C(0)-heterocyclyl.

As used herein, the term "heterocyclyl-carbonyl-oxy" refers to a radical of the

formula: -0-C(0)-heterocyclyl.

As used herein, the term "heterocyclyl-oxy" refers to a radical of the

formula: -O-heterocyclyl.

As used herein, the term "hydroxy" refers to a radical of the formula: -OH.

As used herein, the term "hydroxy-Ci-salkoxy-Ci-salkyl" refers to a radical of the formula: -Ci _-8 alkyl-0-Ci _-8 alkyl-OH.

As used herein, the term "hydroxy-Ci- ₈ alkyl" refers to a radical of the

formula: -Ci _-8 alkyl-OH, wherein Ci _-8 alkyl is partially or completely substituted with one or more hydroxy radicals where allowed by available valences.

As used herein, the term "hydroxy-Ci _-8 alkyl-amino" refers to a radical of the

formula: - H-Ci-salkyl-OH.

As used herein, the term "(hydroxy-Ci-8alkyl)2-amino" refers to a radical of the formula: -N(Ci- ₈ alkyl-OH) ₂ .

As used herein, the term "(hydroxy-Ci-8alkyl)(Ci-8alkyl)amino" refers to a radical of the formula: -N(Ci- ₈ alkyl)(Ci _-8 alkyl-OH).

As used herein, the term "hydroxy-Ci-salkyl-amino-Ci-salkyl" refers to a radical of the formula: -Ci _-8 alkyl- H-Ci _-8 alkyl-OH.

As used herein, the term "(hydroxy-Ci- ₈ alkyl)2-amino-Ci _-8 alkyl" refers to a radical of the formula: -Ci _-8 alkyl-N(Ci- ₈ alkyl-OH) ₂ .

As used herein, the term "(hydroxy-Ci- ₈ alkyl)(Ci- ₈ alkyl)amino-Ci _-8 alkyl" refers to a radical of the formula: -Ci- ₈ alkyl-N(Ci- ₈ alkyl)(Ci _-8 alkyl-OH).

As used herein, the term "hydroxy-Ci _-8 alkyl-amino-Ci _-8 alkoxy" refers to a radical of the formula: -0-Ci _-8 alkyl- H-Ci _-8 alkyl-OH.

As used herein, the term "(hydroxy-Ci- ₈ alkyl) ₂ -amino-Ci- ₈ alkoxy" refers to a radical of the formula: -0-Ci _-8 alkyl-N(Ci- ₈ alkyl-OH) ₂ .

As used herein, the term "(hydroxy-Ci- ₈ alkyl)(Ci- ₈ alkyl)amino-Ci _-8 alkoxy" refers to a radical of the formula: -0-Ci _-8 alkyl-N(Ci _-8 alkyl)(Ci _-8 alkyl-OH). As used herein, the term "hydroxy-Ci- ₈ alkyl-amino-Ci _-8 alkyl-amino" refers to a radical of the formula: - I-Ci- ₈ alkyl- H-Ci _-8 alkyl-OH.

As used herein, the term "(hydroxy-Ci _-8 alkyl-amino-Ci _-8 alkyl)2-amino" refers to a radical of the formula: -N(Ci _-8 alkyl- H-Ci- ₈ alkyl-OH) ₂ .

As used herein, the term "(hydroxy-Ci- ₈ alkyl) ₂ -amino-Ci- ₈ alkyl-amino" refers to a radical of the formula: - H-Ci _-8 alkyl-N(Ci- ₈ alkyl-OH) ₂ .

As used herein, the term "(hydroxy-Ci- ₈ alkyl-amino-Ci- ₈ alkyl)(Ci _-8 alkyl)amino" refers to a radical of the formula: -N(Ci- ₈ alkyl)(Ci _-8 alkyl- H-Ci _-8 alkyl-OH).

As used herein, the term "[(hydroxy-Ci- ₈ alkyl) ₂ -amino-Ci- ₈ alkyl](Ci- ₈ alkyl)amino" refers to a radical of the formula: -N(Ci- ₈ alkyl)[Ci _-8 alkyl-N(Ci- ₈ alkyl-OH) ₂ ].

As used herein, the term "(hydroxy-Ci- ₈ alkyl)(Ci- ₈ alkyl)amino-Ci _-8 alkyl-amino" refers to a radical of the formula: - H-Ci _-8 alkyl-N(Ci _-8 alkyl,Ci _-8 alkyl-OH).

As used herein, the term

"[(hydroxy-Ci- ₈ alkyl)(Ci- ₈ alkyl)amino-Ci- ₈ alkyl](Ci _-8 alkyl)amino" refers to a radical of the formula: -N(Ci- ₈ alkyl)[Ci- ₈ alkyl-N(Ci- ₈ alkyl)(Ci _-8 alkyl-OH)].

As used herein, the term "substituent" means positional variables on the atoms of a core molecule that are substituted at a designated atom position, replacing one or more hydrogens on the designated atom, provided that the designated atom's normal valency is not exceeded, and that the substitution results in a stable compound. Combinations of substituents and/or variables are permissible only if such combinations result in stable compounds. A person of ordinary skill in the art should note that any carbon as well as heteroatom with valences that appear to be unsatisfied as described or shown herein is assumed to have a sufficient number of hydrogen atom(s) to satisfy the valences described or shown. In certain instances one or more substituents having a double bond (e.g., "oxo" or "=0") as the point of attachment may be described, shown or listed herein within a substituent group, wherein the structure may only show a single bond as the point of attachment to the core structure of Formula (I). A person of ordinary skill in the art would understand that, while only a single bond is shown, a double bond is intended for those substituents.

As used herein, the term "and the like," with reference to the definitions of chemical terms provided herein, means that variations in chemical structures that could be expected by one skilled in the art include, without limitation, isomers (including chain, branching or positional structural isomers), hydration of ring systems (including saturation or partial unsaturation of monocyclic, bicyclic or polycyclic ring structures) and all other variations where allowed by available valences which result in a stable compound.

For the purposes of this description, where one or more substituent variables for a compound of Formula (I) or a form thereof encompass functionalities incorporated into a compound of Formula (I), each functionality appearing at any location within the disclosed compound may be independently selected, and as appropriate, independently and/or optionally substituted.

As used herein, the terms "independently selected," or "each selected" refer to functional variables in a substituent list that may occur more than once on the structure of Formula (I), the pattern of substitution at each occurrence is independent of the pattern at any other occurrence. Further, the use of a generic substituent variable on any formula or structure for a compound described herein is understood to include the replacement of the generic substituent with species substituents that are included within the particular genus, e.g., aryl may be replaced with phenyl or naphthalenyl and the like, and that the resulting compound is to be included within the scope of the compounds described herein.

As used herein, the terms "each instance of or "in each instance, when present," when used preceding a phrase such as "... C3-i4cycloalkyl, C3-i4cycloalkyl-Ci-4alkyl, aryl, aryl-Ci-4alkyl, heteroaryl, heteroaryl-Ci-4alkyl, heterocyclyl and heterocyclyl-Ci-4alkyl," are intended to refer to the C3-i4cycloalkyl, aryl, heteroaryl and heterocyclyl ring systems when each are present either alone or as a substituent.

As used herein, the term "optionally substituted" means optional substitution with the specified substituent variables, groups, radicals or moieties.

COMPOUND FORMS

As used herein, the term "form" means a compound of Formula (I) having a form selected from the group consisting of a free acid, free base, prodrug, salt, hydrate, solvate, clathrate, isotopologue, racemate, enantiomer, diastereomer, stereoisomer, polymorph and tautomer form thereof.

In certain aspects described herein, the form of the compound of Formula (I) is a free acid, free base or salt thereof. In certain aspects described herein, the form of the compound of Formula (I) is a salt thereof.

In certain aspects described herein, the form of the compound of Formula (I) is an isotopologue thereof.

In certain aspects described herein, the form of the compound of Formula (I) is a stereoisomer, racemate, enantiomer or diastereomer thereof.

In certain aspects described herein, the form of the compound of Formula (I) is a tautomer thereof.

In certain aspects described herein, the form of the compound of Formula (I) is a pharmaceutically acceptable form.

In certain aspects described herein, the compound of Formula (I) or a form thereof is isolated for use.

As used herein, the term "isolated" means the physical state of a compound of Formula (I) or a form thereof after being isolated and/or purified from a synthetic process (e.g., from a reaction mixture) or natural source or combination thereof according to an isolation or purification process or processes described herein or which are well known to the skilled artisan (e.g., chromatography, recrystallization and the like) in sufficient purity to be characterized by standard analytical techniques described herein or well known to the skilled artisan.

As used herein, the term "protected" means that a functional group in a compound of Formula (I) or a form thereof is in a form modified to preclude undesired side reactions at the protected site when the compound is subjected to a reaction. Suitable protecting groups will be recognized by those with ordinary skill in the art as well as by reference to standard textbooks such as, for example, T.W. Greene et al, Protective Groups in organic Synthesis (1991), Wiley, New York. Such functional groups include hydroxy, phenol, amino and carboxylic acid. Suitable protecting groups for hydroxy or phenol include trialkylsilyl or diarylalkylsilyl (e.g.,

t-butyldimethylsilyl, t-butyldiphenylsilyl or trimethylsilyl), tetrahydropyranyl, benzyl, substituted benzyl, methyl, methoxymethanol, and the like. Suitable protecting groups for amino, amidino and guanidino include t-butoxycarbonyl, benzyl oxycarbonyl, and the like. Suitable protecting groups for carboxylic acid include alkyl, aryl or arylalkyl esters. In certain instances, the protecting group may also be a polymer resin, such as a Wang resin or a 2-chlorotrityl-chloride resin. Protecting groups may be added or removed in accordance with standard techniques, which are well-known to those skilled in the art and as described herein. It will also be appreciated by those skilled in the art, although such protected derivatives of compounds described herein may not possess pharmacological activity as such, they may be administered to a subject and thereafter metabolized in the body to form compounds described herein which are pharmacologically active. Such derivatives may therefore be described as "prodrugs". All prodrugs of compounds described herein are included within the scope of the use described herein.

As used herein, the term "prodrug" means a form of an instant compound (e.g., a drug precursor) that is transformed in vivo to yield an active compound of Formula (I) or a form thereof. The transformation may occur by various mechanisms {e.g., by metabolic and/or non-metabolic chemical processes), such as, for example, by hydrolysis and/or metabolism in blood, liver and/or other organs and tissues. A discussion of the use of prodrugs is provided by T. Higuchi and W. Stella, "Pro-drugs as Novel Delivery Systems," Vol. 14 of the A.C.S. Symposium Series, and in Bioreversible Carriers in Drug Design, ed. Edward B. Roche, American

Pharmaceutical Association and Pergamon Press, 1987.

In one example, when a compound of Formula (I) or a form thereof contains a carboxylic acid functional group, a prodrug can comprise an ester formed by the replacement of the hydrogen atom of the acid group with a functional group such as alkyl and the like. In another example, when a compound of Formula (I) or a form thereof contains a hydroxyl functional group, a prodrug form can be prepared by replacing the hydrogen atom of the hydroxyl with another functional group such as alkyl, alkylcarbonyl or a phosphonate ester and the like. In another example, when a compound of Formula (I) or a form thereof contains an amine functional group, a prodrug form can be prepared by replacing one or more amine hydrogen atoms with a functional group such as alkyl or substituted carbonyl. Pharmaceutically acceptable prodrugs of compounds of Formula (I) or a form thereof include those compounds substituted with one or more of the following groups: carboxylic acid esters, sulfonate esters, amino acid esters, phosphonate esters and mono-, di- or triphosphate esters or alkyl substituents, where appropriate. As described herein, it is understood by a person of ordinary skill in the art that one or more of such

substituents may be used to provide a compound of Formula (I) or a form thereof as a prodrug.

One or more compounds described herein may exist in unsolvated as well as solvated forms with pharmaceutically acceptable solvents such as water, ethanol, and the like, and the description herein is intended to embrace both solvated and unsolvated forms. As used herein, the term "solvate" means a physical association of a compound described herein with one or more solvent molecules. This physical association involves varying degrees of ionic and covalent bonding, including hydrogen bonding. In certain instances the solvate will be capable of isolation, for example when one or more solvent molecules are incorporated in the crystal lattice of the crystalline solid. As used herein, "solvate" encompasses both solution-phase and isolatable solvates. Non-limiting examples of suitable solvates include ethanolates, methanolates, and the like.

As used herein, the term "hydrate" means a solvate wherein the solvent molecule is water.

The compounds of Formula (I) can form salts, which are intended to be included within the scope of this description. Reference to a compound of Formula (I) or a form thereof herein is understood to include reference to salt forms thereof, unless otherwise indicated. The term "salt(s)", as employed herein, denotes acidic salts formed with inorganic and/or organic acids, as well as basic salts formed with inorganic and/or organic bases. In addition, when a compound of Formula (I) or a form thereof contains both a basic moiety, such as, without limitation an amine moiety, and an acidic moiety, such as, but not limited to a carboxylic acid, zwitterions ("inner salts") may be formed and are included within the term "salt(s)" as used herein.

The term "pharmaceutically acceptable salt(s)", as used herein, means those salts of compounds described herein that are safe and effective (i.e., non-toxic, physiologically acceptable) for use in mammals and that possess biological activity, although other salts are also useful. Salts of the compounds of the Formula (I) may be formed, for example, by reacting a compound of Formula (I) or a form thereof with an amount of acid or base, such as an equivalent amount, in a medium such as one in which the salt precipitates or in an aqueous medium followed by lyophilization.

Pharmaceutically acceptable salts include one or more salts of acidic or basic groups present in compounds described herein. Aspects of acid addition salts include, and are not limited to, acetate, ascorbate, benzoate, benzenesulfonate, bisulfate, bitartrate, borate, bromide, butyrate, chloride, citrate, camphorate, camphorsulfonate, ethanesulfonate, formate, fumarate, gentisinate, gluconate, glucaronate, glutamate, iodide, isonicotinate, lactate, maleate, methanesulfonate, naphthalenesulfonate, nitrate, oxalate, pamoate, pantothenate, phosphate, propionate, saccharate, salicylate, succinate, sulfate, tartrate, thiocyanate, toluenesulfonate (also known as tosylate), trifluoroacetate salts and the like. Certain aspects of acid addition salts include chloride, dichloride, trichloride, bromide, acetate, formate or trifluoroacetate salts.

Additionally, acids which are generally considered suitable for the formation of pharmaceutically useful salts from basic pharmaceutical compounds are discussed, for example, by P. Stahl et al, Camille G. (eds.) Handbook of Pharmaceutical Salts. Properties, Selection and Use. (2002) Zurich: Wiley-VCH; S. Berge et al, Journal of Pharmaceutical Sciences (1977) 66(1) 1-19; P. Gould, International J. of Pharmaceutics (1986) 33, 201-217; Anderson et al, The Practice of Medicinal Chemistry (1996), Academic Press, New York; and in The Orange Book (Food & Drug Administration, Washington, D.C. on their website). These disclosures are incorporated herein by reference thereto.

Suitable basic salts include, but are not limited to, aluminum, ammonium, calcium, lithium, magnesium, potassium, sodium and zinc salts.

All such acid salts and base salts are intended to be included within the scope of pharmaceutically acceptable salts as described herein. In addition, all such acid and base salts are considered equivalent to the free forms of the corresponding compounds for purposes of this description.

Compounds of Formula (I) and forms thereof, may further exist in a tautomeric form. All such tautomeric forms are contemplated and intended to be included within the scope of the compounds of Formula (I) or a form thereof as described herein.

The compounds of Formula (I) or a form thereof may contain asymmetric or chiral centers, and, therefore, exist in different stereoisomeric forms. The present description is intended to include all stereoisomeric forms of the compounds of Formula (I) as well as mixtures thereof, including racemic mixtures.

The compounds described herein may include one or more chiral centers, and as such may exist as racemic mixtures (R/S) or as substantially pure enantiomers and diastereomers. The compounds may also exist as substantially pure (R) or (S) enantiomers (when one chiral center is present). In one aspect, the compounds described herein are (S) isomers and may exist as enantiomerically pure compositions substantially comprising only the (S) isomer. In another aspect, the compounds described herein are (R) isomers and may exist as enantiomerically pure compositions substantially comprising only the (R) isomer. As one of skill in the art will recognize, when more than one chiral center is present, the compounds described herein may also exist as a (R,R), (R,S), (S,R) or (S,S) isomer, as defined by IUPAC Nomenclature

Recommendations.

As used herein, the term "substantially pure" refers to compounds consisting substantially of a single isomer in an amount greater than or equal to 90%, in an amount greater than or equal to 92%, in an amount greater than or equal to 95%, in an amount greater than or equal to 98%, in an amount greater than or equal to 99%, or in an amount equal to 100%) of the single isomer.

In one aspect of the description, a compound of Formula (I) or a form thereof is a substantially pure (S) enantiomer form present in an amount greater than or equal to 90%, in an amount greater than or equal to 92%, in an amount greater than or equal to 95%, in an amount greater than or equal to 98%, in an amount greater than or equal to 99%, or in an amount equal to 100%.

In one aspect of the description, a compound of Formula (I) or a form thereof is a substantially pure (R) enantiomer form present in an amount greater than or equal to 90%, in an amount greater than or equal to 92%, in an amount greater than or equal to 95%, in an amount greater than or equal to 98%, in an amount greater than or equal to 99%, or in an amount equal to 100%.

As used herein, a "racemate" is any mixture of isometric forms that are not

"enantiomerically pure", including mixtures such as, without limitation, in a ratio of about 50/50, about 60/40, about 70/30, or about 80/20.

In addition, the present description embraces all geometric and positional isomers. For example, if a compound of Formula (I) or a form thereof incorporates a double bond or a fused ring, both the cis- and trans-forms, as well as mixtures, are embraced within the scope of the description. Diastereomeric mixtures can be separated into their individual diastereomers on the basis of their physical chemical differences by methods well known to those skilled in the art, such as, for example, by chromatography and/or fractional crystallization. Enantiomers can be separated by use of chiral UPLC column or other chromatographic methods known to those skilled in the art. Enantiomers can also be separated by converting the enantiomeric mixture into a diastereomeric mixture by reaction with an appropriate optically active compound (e.g., chiral auxiliary such as a chiral alcohol or Mosher's acid chloride), separating the diastereomers and converting (e.g., hydrolyzing) the individual diastereomers to the corresponding pure enantiomers. Also, some of the compounds of Formula (I) may be atropisomers (e.g., substituted biaryls) and are considered as part of this description.

All stereoisomers (for example, geometric isomers, optical isomers and the like) of the present compounds (including those of the salts, solvates, esters and prodrugs of the compounds as well as the salts, solvates and esters of the prodrugs), such as those which may exist due to asymmetric carbons on various substituents, including enantiomeric forms (which may exist even in the absence of asymmetric carbons), rotameric forms, atropisomers, and diastereomeric forms, are contemplated within the scope of this description, as are positional isomers (such as, for example, 4-pyridyl and 3-pyridyl). Individual stereoisomers of the compounds described herein may, for example, be substantially free of other isomers, or may be present in a racemic mixture, as described supra.

The use of the terms "salt", "solvate", "ester", "prodrug" and the like, is intended to equally apply to the salt, solvate, ester and prodrug of enantiomers, stereoisomers, rotamers, tautomers, positional isomers, racemates or isotopologues of the instant compounds.

The term "isotopologue" refers to isotopically-enriched compounds described herein which are identical to those recited herein, but for the fact that one or more atoms are replaced by an atom having an atomic mass or mass number different from the atomic mass or mass number usually found in nature. Examples of isotopes that can be incorporated into compounds described herein include isotopes of hydrogen, carbon, nitrogen, oxygen, phosphorus, fluorine and chlorine, such as ² H, ¾, ¹³ C, ¹⁴ C, ¹⁵ N, ¹⁸ 0, ¹⁷ 0, ³¹ P, ³² P, ³⁵ S, ¹⁸ F, ³⁵ C1 and ³⁶ C1, respectively, each of which are also within the scope of this description.

Certain isotopically-enriched compounds described herein (e.g., those labeled with ³ H and ¹⁴ C) are useful in compound and/or substrate tissue distribution assays. Tritiated (i.e., ³ H) and carbon-14 (i.e., ¹⁴ C) isotopes are particularly preferred for their ease of preparation and detectability. Further, substitution with heavier isotopes such as deuterium (i.e., ² H) may afford certain therapeutic advantages resulting from greater metabolic stability (e.g., increased in vivo half-life or reduced dosage requirements) and hence may be preferred in some circumstances.

Polymorphic crystalline and amorphous forms of the compounds of Formula (I) and of the salts, solvates, hydrates, esters and prodrugs of the compounds of Formula (I) are further intended to be included in the present description. COMPOUND USES

The present description relates to a method or use of a compound of Formula (I) or a form thereof for treating or ameliorating HD in a subject in need thereof, comprising administering an effective amount of the compound or a form thereof to the subject.

The present description also relates to a method of use of the compound of Formula (I) or a form thereof for treating or ameliorating FID in a subject in need thereof.

The present description further relates to use of the compound of Formula (I) or a form thereof for treating or ameliorating FID in a subject in need thereof.

The present description further relates to use of the compound of Formula (I) or a form thereof having activity toward HD.

The present description further relates to use of the compound of Formula (I) or a form thereof in a combination therapy to provide additive or synergistic activity, thus enabling the development of a combination product for treating or ameliorating HD.

In addition to monotherapeutic use, the instant compounds are useful in a combination therapy with current standard of agents, having additive or synergistic activity with one or more known agents.

A combination therapy comprising compounds described herein in combination with one or more known drugs may be used to treat HD regardless of whether HD is responsive to the known drug.

Aspects of the present description include the use of a compound of Formula (I) or a form thereof in a combination therapy for treating or ameliorating HD in a subject in need thereof, comprising administering an effective amount of the compound of Formula (I) or a form thereof and an effective amount of one or more agent(s).

Aspects of the present description include the use of a compound of Formula (I) or a form thereof in a combination therapy for treating or ameliorating HD in a subject in need thereof, comprising administering an effective amount of the compound of Formula (I) or a form thereof and an effective amount of one or more agent(s).

In an aspect of a use or method provided herein, compounds of Formula (I) or a form thereof used in combination with one or more additional agents can be administered to a subject or contacted with a subject or patient cell(s) prior to, concurrently with, or subsequent to administering to the subject or patient or contacting the cell with an additional agent(s). A compound(s) of Formula (I) or a form thereof and an additional agent(s) can be administered to a subject or contacted with a cell in single composition or different compositions. In a specific aspect, a compound(s) of Formula (I) or a form thereof is used in combination with gene therapy to inhibit HTT expression (using, e.g., viral delivery vectors) or the administration of another small molecule HTT inhibitor. In another specific aspect, a compound(s) of Formula (I) or a form thereof are used in combination with cell replacement using differentiated non-mutant HTT stem cells. In another specific aspect, a compound(s) of Formula (I) or a form thereof are used in combination with cell replacement using differentiated HTT stem cells.

In one aspect, provided herein is the use of compounds of Formula (I) or a form thereof in combination with supportive standard of care therapies, including palliative care.

An aspect of the present description includes the use of a compound of Formula (I) or a form thereof in the preparation of a kit comprising the compound of Formula (I) or a form thereof and instructions for administering an effective amount of the compound of Formula (I) or a form thereof and an effective amount of one or more agent(s) in a combination therapy for treating or ameliorating HD in a subject in need thereof.

Accordingly, the present description relates to use of a compound of Formula (I) or a form thereof for treating or ameliorating HD. In accordance with the use of the present description, compounds that are useful in selectively treating or ameliorating HD, have been identified and use of these compounds for treating or ameliorating HD has been provided.

One aspect of the use of the present description relates to use of a compound of Formula (I) or a form thereof for treating or ameliorating HD in a subject in need thereof, comprising administering an effective amount of the compound of Formula (I) or a form thereof to the subject.

One aspect of the use of the present description relates to a method of use of a compound of Formula (I) or a form thereof for treating or ameliorating HD in a subject in need thereof, comprising administering an effective amount of the compound to the subject.

An aspect of the use of the present description relates to use of a compound of Formula (I) or a form thereof in the manufacture of a medicament for treating or ameliorating HD in a subject in need thereof, comprising administering an effective amount of the medicament to the subject.

An aspect of the use of the present description relates to use of a compound of Formula (I) or a form thereof in the preparation of a kit comprising the compound of Formula (I) or a form thereof and instructions for administering the compound for treating or ameliorating HD in a subject in need thereof.

In one respect, for each of such aspects, the subject is treatment naive. In another respect, for each of such aspects, the subject is not treatment naive.

As used herein, the phrases "a method or use for a compound for treating or ameliorating HD (Huntington's Disease)," "a method of use for a compound for treating or ameliorating HD" or "a use for a compound for treating or ameliorating HD" coextensively refer to a plurality of potential uses of a compound which would be known to those of skill in the art including, without limitation: (i) a method of use of a compound for treating or ameliorating HD; (ii) a use of a compound for treating or ameliorating HD; (iii) a use of a compound in the preparation of a medicament for treating or ameliorating HD; (iv) a use of a compound in the preparation of a pharmaceutical composition for treating or ameliorating HD; (iv) a use of a compound in the preparation of a kit for treating or ameliorating HD; and, the like.

As used herein, the term "treating" refers to: (i) preventing a disease, disorder or condition from occurring in a subject that may be predisposed to the disease, disorder and/or condition but has not yet been diagnosed as having the disease, disorder and/or condition; (ii) inhibiting a disease, disorder or condition, i.e., arresting the development thereof; and/or (iii) relieving a disease, disorder or condition, i.e., causing regression of the disease, disorder and/or condition.

As used herein, the term "subject" refers to an animal or any living organism having sensation and the power of voluntary movement, and which requires oxygen and organic food. Nonlimiting examples include members of the human, primate, equine, porcine, bovine, murine, rattus, canine and feline specie. In some aspects, the subject is a mammal or a warm-blooded vertebrate animal. In other aspects, the subject is a human. As used herein, the term "patient" may be used interchangeably with "subject" and "human".

As used herein, the terms "effective amount" or "therapeutically effective amount" mean an amount of compound of Formula (I) or a form, composition or medicament thereof effective in inhibiting the above-noted diseases and thus producing the desired therapeutic, ameliorative, inhibitory or preventative effect in a subject in need thereof.

The dose administered to achieve an effective target plasma concentration may also be administered based upon the weight of the subject or patient. Doses administered on a weight basis may be in the range of about 0.001 mg/kg/day to about 3500 mg/kg/day, or about 0.001 mg/kg/day to about 3000 mg/kg/day, or about 0.001 mg/kg/day to about 2500 mg/kg/day, or about 0.001 mg/kg/day to about 2000 mg/kg/day, or about 0.001 mg/kg/day to about 1500 mg/kg/day, or about 0.001 mg/kg/day to about 1000 mg/kg/day, or about 0.001 mg/kg/day to about 500 mg/kg/day, or about 0.001 mg/kg/day to about 250 mg/kg/day, or about 0.001 mg/kg/day to about 100 mg/kg/day, or about 0.001 mg/kg/day to about 75 mg/kg/day, or about 0.001 mg/kg/day to about 50 mg/kg/day, or about 0.001 mg/kg/day to about 40 mg/kg/day, or about 0.001 mg/kg/day to about 30 mg/kg/day, or about 0.001 mg/kg/day to about 20 mg/kg/day, or about 0.001 mg/kg/day to about 10 mg/kg/day, or about 0.01 mg/kg/day to about 2000 mg/kg/day, or about 0.01 mg/kg/day to about 1500 mg/kg/day, or about 0.01 mg/kg/day to about 1000 mg/kg/day, or about 0.01 mg/kg/day to about 600 mg/kg/day, or about 0.01 mg/kg/day to about 500 mg/kg/day, or about 0.01 mg/kg/day to about 300 mg/kg/day, or about 0.015 mg/kg/day to about 200 mg/kg/day, or about 0.02 mg/kg/day to about 100 mg/kg/day, or about 0.025 mg/kg/day to about 100 mg/kg/day, or about 0.03 mg/kg/day to about 100 mg/kg/day, wherein said amount is orally administered once (once in approximately a 24 hour period), twice (once in approximately a 12 hour period) or thrice (once in approximately an 8 hour period) daily according to subject weight.

In certain aspects, the effective amount will be in a range of from about 0.001 mg/kg/day to about 500 mg/kg/day, or about 0.01 mg/kg/day to about 500 mg/kg/day, or about 0.1 mg to about 500 mg/kg/day, or about 1.0 mg/day to about 500 mg/kg/day, in single, divided, or a continuous dose for a patient or subject having a weight in a range of between about 40 to about 200 kg (which dose may be adjusted for patients or subjects above or below this range, particularly children under 40 kg). The typical adult subject is expected to have a median weight in a range of about 70 kg.

In another aspect, where daily doses are adjusted based upon the weight of the subject or patient, compounds described herein may be formulated for delivery at about 0.02, 0.025, 0.03, 0.05, 0.06, 0.075, 0.08, 0.09, 0.10, 0.20, 0.25, 0.30, 0.50, 0.60, 0.75, 0.80, 0.90, 1.0, 1.10, 1.20, 1.25, 1.50, 1.75, 2.0, 3.0, 5.0, 10, 20, 30, 40, 50, 100, 150, 200, 250, 300, 400 or 500 mg/kg/day. Daily doses adjusted based upon the weight of the subject or patient may be administered as a single, divided, or continuous dose. In aspects where a dose of compound is given more than once per day, the dose may be administered twice, thrice, or more times per day. Within the scope of the present description, the "effective amount" of a compound of Formula (I) or a form thereof for use in the manufacture of a medicament, for use in the preparation of a pharmaceutical kit or in a method of use for treating or ameliorating FID in a subject in need thereof is intended to include an amount in a range of from about 0.001 mg/kg/day to about 3500 mg/kg/day, or about 0.001 mg/kg/day to about 3000 mg/kg/day, or about 0.001 mg/kg/day to about 2500 mg/kg/day, or about 0.001 mg/kg/day to about 2000 mg/kg/day, or about 0.001 mg/kg/day to about 1500 mg/kg/day, or about 0.001 mg/kg/day to about 1000 mg/kg/day, or about 0.001 mg/kg/day to about 500 mg/kg/day, or about 0.001 mg/kg/day to about 250 mg/kg/day, or about 0.001 mg/kg/day to about 100 mg/kg/day, or about 0.001 mg/kg/day to about 75 mg/kg/day, or about 0.001 mg/kg/day to about 50 mg/kg/day, or about 0.001 mg/kg/day to about 40 mg/kg/day, or about 0.001 mg/kg/day to about 30 mg/kg/day, or about 0.001 mg/kg/day to about 20 mg/kg/day, or about 0.001 mg/kg/day to about 10 mg/kg/day, or about 0.01 mg/kg/day to about 2000 mg/kg/day, or about 0.01 mg/kg/day to about 1500 mg/kg/day, or about 0.01 mg/kg/day to about 1000 mg/kg/day, or about 0.01 mg/kg/day to about 600

mg/kg/day, or about 0.01 mg/kg/day to about 500 mg/kg/day, or about 0.01 mg/kg/day to about 300 mg/kg/day, or about 0.015 mg/kg/day to about 200 mg/kg/day, or about 0.02 mg/kg/day to about 100 mg/kg/day, or about 0.025 mg/kg/day to about 100 mg/kg/day, or about 0.03 mg/kg/day to about 100 mg/kg/day, wherein said amount is administered once (once in approximately a 24 hour period; i.e., "q.d."), twice (once in approximately a 12 hour period; i.e., "b.i.d." or "q. l2h"), thrice (once in approximately an 8 hour period; i.e., "t.i.d." or "q.8h"), or four times (once in approximately a 6 hour period; i.e., "q.d.s.", "q.i.d." or "q.6h") daily according to subject weight.

Such amounts may further include an amount in a range of from about 0.001 mg to about 3500 mg administered daily; 0.001 mg to about 3000 mg administered daily; 0.001 mg to about 2500 mg administered daily; 0.001 mg to about 2000 mg administered daily; 0.001 mg to about 1500 mg administered daily; 0.001 mg to about 1000 mg administered daily; 0.001 mg to about 500 mg administered daily; 0.001 mg to about 250 mg administered daily; 1.0 mg to about 3500 mg administered daily; 1.0 mg to about 1500 mg administered daily; 1.0 mg to about 1000 mg administered daily; 10.0 mg to about 600 mg administered daily; 0.5 mg to about 2000 mg administered daily; or, an amount in a range of from about 5.0 mg to about 300 mg administered daily. For example, the effective amount may be the amount required to treat HD in a subject or, more specifically, in a human. The effective amount for a subject will depend upon various factors, including the subject's body weight, size and health. Effective amounts for a given patient can be determined by routine experimentation that is within the skill and judgment of the clinician.

For any compound, the effective amount can be estimated initially either in cell culture assays or in relevant animal models, such as a mouse, chimpanzee, marmoset or tamarin animal model. Relevant animal models may also be used to determine the appropriate concentration range and route of administration. Such information can then be used to determine useful doses and routes for administration in humans. Therapeutic efficacy and toxicity may be determined by standard pharmaceutical procedures in cell cultures or experimental animals, e.g., ED50 (the dose therapeutically effective in 50% of the population) and LD50 (the dose lethal to 50% of the population). The dose ratio between therapeutic and toxic effects is therapeutic index, and can be expressed as the ratio, LD50/ED50. In some aspects, the effective amount is such that a large therapeutic index is achieved. In further aspects, the dosage is within a range of circulating concentrations that include an ED50 with little or no toxicity. The dosage may vary within this range depending upon the dosage form employed, sensitivity of the patient, and the route of administration.

More specifically, the concentration-biological effect relationships observed with regard to a compound of Formula (I) or a form thereof indicate a target plasma concentration ranging from approximately 0.001 μg/mL to approximately 50 μg/mL, from approximately 0.01 μg/mL to approximately 20 μg/mL, from approximately 0.05 μg/mL to approximately 10 μg/mL, or from approximately 0.1 μg/mL to approximately 5 μg/mL. To achieve such plasma concentrations, the compounds described herein may be administered at doses that vary, such as, for example, without limitation, from 0.1 ng to 10,000 mg, depending upon the route of administration in single, divided, or continuous doses for a patient weighing between about 10 to about 100 kg (which dose may be adjusted for patients within this weight range, particularly for children under 40 kg).

The exact dosage will be determined by the practitioner, in light of factors related to the subject. Dosage and administration may be adjusted to provide sufficient levels of the active agent(s) or to maintain the desired effect. Factors which may be taken into account include the severity of the disease state, general health of the subject, ethnicity, age, weight, gender, diet, time of day and frequency of administration, drug combination(s), reaction sensitivities, experience with other therapies, and tolerance/response to therapy. Long-acting pharmaceutical

compositions may be administered every 2, 3 or 4 days, once every week, or once every two weeks depending on half-life and clearance rate of the particular formulation.

The compounds and compositions described herein may be administered to the subject via any drug delivery route known in the art. Nonlimiting examples include oral, ocular, rectal, buccal, topical, nasal, sublingual, transdermal, subcutaneous, intramuscular, intraveneous (bolus and infusion), intracerebral, and pulmonary routes of administration.

In one aspect, provided herein are methods for modulating the amount of HTT (huntingtin protein), comprising contacting a human cell with a compound of Formula (I) or a form thereof. In a specific aspect, provided herein are methods for modulating the amount of HTT, comprising contacting a human cell with a compound of Formula (I) or a form thereof that modulates the expression of HTT. The human cell can be contacted with a compound of Formula (I) or a form thereof in vitro, or in vivo, e.g., in a non-human animal or in a human. In a specific aspect, the human cell is from or in a human. In another specific aspect, the human cell is from or in a human with HD. In another specific aspect, the human cell is from or in a human with HD, caused by a CAG repeat in the Htt gene, resulting in a loss of HTT expression and/or function. In another aspect, the human cell is from a human with HD. In another aspect, the human cell is in a human with HD. In one aspect, the compound is a form of the compound of Formula (I).

In a specific aspect, provided herein is a method for enhancing the inhibition of mutant HTT transcribed from the Htt gene, comprising contacting a human cell with a compound of Formula (I) or a form thereof. The human cell can be contacted with a compound of Formula (I) or a form thereof in vitro, or in vivo, e.g., in a non-human animal or in a human. In a specific aspect, the human cell is from or in a human. In another specific aspect, the human cell is from or in a human with HD. In another specific aspect, the human cell is from or in a human with HD, caused by a CAG repeat in the Htt gene, resulting in a loss of wild-type "normal" HTT expression and/or function. In another aspect, the human cell is from a human with HD. In another aspect, the human cell is in a human with HD. In one aspect, the compound is a form of the compound of Formula (I). In another aspect, provided herein is a method for modulating the inhibition of mutant HTT transcribed from the Htt gene, comprising administering to a non-human animal model for HD a compound of Formula (I) or a form thereof. In a specific aspect, provided herein is a method for modulating the inhibition of mutant HTT transcribed from the Htt gene, comprising administering to a non-human animal model for HD a compound of Formula (I) or a form thereof. In a specific aspect, the compound is a form of the compound of Formula (I).

In another aspect, provided herein is a method for decreasing the amount of mutant HTT, comprising contacting a human cell with a compound of Formula (I) or a form thereof. In a specific aspect, provided herein is a method for decreasing the amount of mutant HTT, comprising contacting a human cell with a compound of Formula (I) that inhibits the transcription of mutant HTT (huntingtin mRNA) from the Htt gene. In another specific aspect, provided herein is a method for decreasing the amount of HTT, comprising contacting a human cell with a compound of Formula (I) that inhibits the expression of mutant HTT transcribed from the Htt gene. The human cell can be contacted with a compound of Formula (I) or a form thereof in vitro, or in vivo, e.g., in a non-human animal or in a human. In a specific aspect, the human cell is from or in a human. In another specific aspect, the human cell is from or in a human with HD. In another specific aspect, the human cell is from or in a human with HD, caused by a CAG repeat in the Htt gene, resulting in a loss of HTT expression and/or function. In another aspect, the human cell is from a human with HD. In another aspect, the human cell is in a human with HD. In one aspect, the compound is a form of the compound of Formula (I).

In certain aspects, treating or ameliorating HD with a compound of Formula (I) or a form thereof (alone or in combination with an additional agent) has a therapeutic effect and/or beneficial effect. In a specific aspect, treating HD with a compound of Formula (I) or a form thereof (alone or in combination with an additional agent) results in one, two or more of the following effects: (i) reduces or ameliorates the severity of HD; (ii) delays onset of HD; (iii) inhibits the progression of HD; (iv) reduces hospitalization of a subject; (v) reduces

hospitalization length for a subject; (vi) increases the survival of a subject; (vii) improves the quality of life for a subject; (viii) reduces the number of symptoms associated with HD; (ix) reduces or ameliorates the severity of a symptom(s) associated with HD; (x) reduces the duration of a symptom associated with HD; (xi) prevents the recurrence of a symptom associated with HD; (xii) inhibits the development or onset of a symptom of HD; and/or (xiii) inhibits of the progression of a symptom associated with HD.

METABOLITES

Also included within the scope of the present description are the use of in vivo metabolic products of the compounds described herein. Such products may result, for example, from the oxidation, reduction, hydrolysis, amidation, esterification and the like of the administered compound, primarily due to enzymatic processes. Accordingly, the description includes the use of compounds produced by a process comprising contacting a compound described herein with a mammalian tissue or a mammal for a period of time sufficient to yield a metabolic product thereof.

Such products typically are identified by preparing a radio-labeled isotopologue {e.g., ¹⁴ C or ¾) of a compound described herein, administering the radio-labeled compound in a detectable dose {e.g., greater than about 0.5 mg/kg) to a mammal such as a rat, mouse, guinea pig, dog, monkey or human, allowing sufficient time for metabolism to occur (typically about 30 seconds to about 30 hours), and identifying the metabolic conversion products from urine, bile, blood or other biological samples. The conversion products are easily isolated since they are

"radiolabeled" by virtue of being isotopically-enriched (others are isolated by the use of antibodies capable of binding epitopes surviving in the metabolite). The metabolite structures are determined in conventional fashion, e.g., by MS or MR analysis. In general, analysis of metabolites may be done in the same way as conventional drug metabolism studies well-known to those skilled in the art. The conversion products, so long as they are not otherwise found in vivo, are useful in diagnostic assays for therapeutic dosing of the compounds described herein even if they possess no biological activity of their own.

PHARMACEUTICAL COMPOSITIONS

Aspects of the present description include the use of a compound of Formula (I) or a form thereof in a pharmaceutical composition for treating or ameliorating HD in a subject in need thereof, comprising administering an effective amount of the compound of Formula (I) or a form thereof in admixture with one or more pharmaceutically acceptable excipient(s).

An aspect of the present description includes the use of a pharmaceutical composition of the compound of Formula (I) or a form thereof in the preparation of a kit comprising the pharmaceutical composition of the compound of Formula (I) or a form thereof and instructions for administering the compound for treating or ameliorating HD in a subject in need thereof.

As used herein, the term "composition" means a product comprising the specified ingredients in the specified amounts, as well as any product which results, directly or indirectly, from combination of the specified ingredients in the specified amounts.

The pharmaceutical composition may be formulated to achieve a physiologically compatible pH, ranging from about pH 3 to about pH 11. In some aspects, the pharmaceutical composition is formulated to achieve a pH of from about pH 3 to about pH 7. In other aspects, the pharmaceutical composition is formulated to achieve a pH of from about pH 5 to about pH 8.

The term "pharmaceutically acceptable excipient" refers to an excipient for administration of a pharmaceutical agent, such as the compounds described herein. The term refers to any pharmaceutical excipient that may be administered without undue toxicity. Pharmaceutically acceptable excipients may be determined in part by the particular composition being

administered, as well as by the particular mode of administration and/or dosage form.

Nonlimiting examples of pharmaceutically acceptable excipients include carriers, solvents, stabilizers, adjuvants, diluents, etc. Accordingly, there exists a wide variety of suitable formulations of pharmaceutical compositions for the instant compounds described herein {see, e.g., Remington's Pharmaceutical Sciences).

Suitable excipients may be carrier molecules that include large, slowly metabolized macromolecules such as proteins, polysaccharides, polylactic acids, polyglycolic acids, polymeric amino acids, amino acid copolymers, and inactive antibodies. Other exemplary excipients include antioxidants such as ascorbic acid; chelating agents such as EDTA; carbohydrates such as dextrin, hydroxyalkylcellulose, hydroxyalkylmethylcellulose {e.g., hydroxypropylmethylcellulose, also known as HPMC), stearic acid; liquids such as oils, water, saline, glycerol and ethanol; wetting or emulsifying agents; pH buffering substances; and the like. Liposomes are also included within the definition of pharmaceutically acceptable excipients.

The pharmaceutical compositions described herein may be formulated in any form suitable for the intended use described herein. Suitable formulations for oral administration include solids, liquid solutions, emulsions and suspensions, while suitable inhalable formulations for pulmonary administration include liquids and powders. Alternative formulations include syrups, creams, ointments, tablets, and lyophilized solids which can be reconstituted with a physiologically compatible solvent prior to administration.

When intended for oral use for example, tablets, troches, lozenges, aqueous or oil suspensions, non-aqueous solutions, dispersible powders or granules (including micronized particles or nanoparticles), emulsions, hard or soft capsules, syrups or elixirs may be prepared. Compositions intended for oral use may be prepared according to any method known to the art for the manufacture of pharmaceutical compositions, and such compositions may contain one or more agents including sweetening agents, flavoring agents, coloring agents, and preserving agents, in order to provide a palatable preparation.

Pharmaceutically acceptable excipients suitable for use in conjunction with tablets include, for example, inert diluents, such as celluloses, calcium or sodium carbonate, lactose, calcium or sodium phosphate; disintegrating agents, such as croscarmellose sodium, cross-linked povidone, maize starch, or alginic acid; binding agents, such as povidone, starch, gelatin or acacia; and lubricating agents, such as magnesium stearate, stearic acid, or talc. Tablets may be uncoated or may be coated by known techniques including microencapsulation to delay disintegration and adsorption in the gastrointestinal tract and thereby provide a sustained action over a longer period. For example, a time delay material such as glyceryl monostearate or glyceryl distearate alone or with a wax may be employed.

Formulations for oral use may be also presented as hard gelatin capsules where the active ingredient is mixed with an inert solid diluent, for example celluloses, lactose, calcium phosphate, or kaolin, or as soft gelatin capsules wherein the active ingredient is mixed with non-aqueous or oil medium, such as glycerin, propylene glycol, polyethylene glycol, peanut oil, liquid paraffin, or olive oil.

In other aspects, pharmaceutical compositions described herein may be formulated as suspensions comprising a compound of Formula (I) or a form thereof in admixture with one or more pharmaceutically acceptable excipient(s) suitable for the manufacture of a suspension. In yet other aspects, pharmaceutical compositions described herein may be formulated as dispersible powders and granules suitable for preparation of a suspension by the addition of one or more excipient(s).

Excipients suitable for use in connection with suspensions include suspending agents, such as sodium carboxymethylcellulose, methylcellulose, hydroxypropyl methylcelluose, sodium alginate, polyvinylpyrrolidone, gum tragacanth, gum acacia, dispersing or wetting agents such as a naturally occurring phosphatide (e.g., lecithin), a condensation product of an alkylene oxide with a fatty acid (e.g., polyoxyethylene stearate), a condensation product of ethylene oxide with a long chain aliphatic alcohol (e.g., heptadecaethyleneoxycethanol), a condensation product of ethylene oxide with a partial ester derived from a fatty acid and a hexitol anhydride (e.g., polyoxyethylene sorbitan monooleate); and thickening agents, such as carbomer, beeswax, hard paraffin, or cetyl alcohol. The suspensions may also contain one or more preservatives such as acetic acid, methyl and/or n-propyl p-hydroxy-benzoate; one or more coloring agents; one or more flavoring agents; and one or more sweetening agents such as sucrose or saccharin.

The pharmaceutical compositions described herein may also be in the form of oil-in-water emulsions. The oily phase may be a vegetable oil, such as olive oil or arachis oil, a mineral oil, such as liquid paraffin, or a mixture of these. Suitable emulsifying agents include naturally- occurring gums, such as gum acacia and gum tragacanth; naturally occurring phosphatides, such as soybean lecithin, esters or partial esters derived from fatty acids; hexitol anhydrides, such as sorbitan monooleate; and condensation products of these partial esters with ethylene oxide, such as polyoxyethylene sorbitan monooleate. The emulsion may also contain sweetening and flavoring agents. Syrups and elixirs may be formulated with sweetening agents, such as glycerol, sorbitol or sucrose. Such formulations may also contain a demulcent, a preservative, a flavoring or a coloring agent.

Additionally, the pharmaceutical compositions described herein may be in the form of a sterile injectable preparation, such as a sterile injectable aqueous emulsion or oleaginous suspension. Such emulsion or suspension may be formulated according to the known art using those suitable dispersing or wetting agents and suspending agents which have been mentioned above. The sterile injectable preparation may also be a sterile injectable solution or suspension in a non-toxic parenterally acceptable diluent or solvent, such as a solution in 1,2-propanediol. The sterile injectable preparation may also be prepared as a lyophilized powder. Among the acceptable vehicles and solvents that may be employed are water, Ringer' s solution and isotonic sodium chloride solution. In addition, sterile fixed oils may be employed as a solvent or suspending medium. For this purpose any bland fixed oil may be employed including synthetic mono- or di-glycerides. In addition, fatty acids such as oleic acid may likewise be used in the preparation of injectables. The compounds described herein may be substantially insoluble in water and sparingly soluble in most pharmaceutically acceptable protic solvents and vegetable oils, but generally soluble in medium-chain fatty acids (e.g., caprylic and capric acids) or triglycerides and in propylene glycol esters of medium-chain fatty acids. Thus, contemplated in the description are compounds which have been modified by substitutions or additions of chemical or biochemical moieties which make them more suitable for delivery (e.g., increase solubility, bioactivity, palatability, decrease adverse reactions, etc.), for example by esterification, glycosylation, PEGylation, etc.

In some aspects, the compound described herein is formulated for oral administration in a lipid-based composition suitable for low solubility compounds. Lipid-based formulations can generally enhance the oral bioavailability of such compounds. As such, pharmaceutical compositions described herein may comprise a effective amount of a compound of Formula (I) or a form thereof, together with at least one pharmaceutically acceptable excipient selected from medium chain fatty acids or propylene glycol esters thereof (e.g., propylene glycol esters of edible fatty acids such as caprylic and capric fatty acids) and pharmaceutically acceptable surfactants, such as polysorbate 20 or 80 (also referred to as Tween® 20 or Tween® 80, respectively) or polyoxyl 40 hydrogenated castor oil.

In other aspects, the bioavailability of low solubility compounds may be enhanced using particle size optimization techniques including the preparation of nanoparticles or

nanosuspensions using techniques known to those skilled in the art. The compound forms present in such preparations include amorphous, partially amorphous, partially crystalline or crystalline forms.

In alternative aspects, the pharmaceutical composition may further comprise one or more aqueous solubility enhancer(s), such as a cyclodextrin. Nonlimiting examples of cyclodextrin include hydroxypropyl, hydroxyethyl, glucosyl, maltosyl and maltotriosyl derivatives of α-, β-, and γ-cyclodextrin, and hydroxypropyl-P-cyclodextrin (HPBC). In some aspects, the

pharmaceutical composition further comprises HPBC in a range of from about 0.1% to about 20%, from about 1% to about 15%, or from about 2.5% to about 10%. The amount of solubility enhancer employed may depend on the amount of the compound in the composition.

PREPARATION OF COMPOUNDS

Compounds of Formula (I) can be prepared using reagents and methods known in the art, including the methods provided in International Application No. PCT/US2013/025292, filed on February 8, 2013, and published as International Publication No. WO 2013/119916 on August 15, 2013, the entire contents of which are incorporated herein by reference (see in particular, General Synthetic Methods, Schemes A-J, at paragraphs [001126] to [001159]; and Specific Synthetic Examples, at paragraphs [001160] to [001573] and Table 1).

BIOLOGICAL EXAMPLES

The following in vitro biological examples demonstrate the usefulness of the compounds of the present description for treating Huntington's disease.

To describe in more detail and assist in understanding the present description, the following non-limiting biological examples are offered to more fully illustrate the scope of the description and are not to be construed as specifically limiting the scope thereof. Such variations of the present description that may be now known or later developed, which would be within the purview of one skilled in the art to ascertain, are considered to fall within the scope of the present description and as hereinafter claimed.

Compounds of Formula (I) were tested using the Meso Scale Discovery (MSD) Assay provided in International Application No. PCT/US2016/066042, filed on December 11, 2016 and claiming priority to United States Provisional Application U.S. 62/265,652 filed on December 10, 2015, published as International Publication No. WO 2017/100726 on June 15, 2017, the entire contents of which are incorporated herein by reference.

The Endogenous Huntingtin Protein assay used in Example 1 was developed using the ELISA-based MSD electrochemiluminescence assay platform.

Example 1

Endogenous Huntingtin Protein Assay

Meso Scale Discovery (MSD) 96-well or 384-well plates were coated overnight at 4°C with MW1 (expanded polyglutamine) or MAB2166 monoclonal antibody (for capture) at a concentration of 1 μg/mL in PBS (30 μΕ per well). Plates were then washed three times with 300 μL· wash buffer (0.05% Tween-20 in PBS) and blocked (100 μL· blocking buffer; 5% BSA in PBS) for 4-5 hours at room temperature with rotational shaking and then washed three times with wash buffer.

Samples (25 μΕ) were transferred to the antibody-coated MSD plate and incubated overnight at 4°C. After removal of the lysates, the plate was washed three times with wash buffer, and 25 μΙ_, of #5656S (Cell signaling; rabbit monoclonal) secondary antibody (diluted to 0.25 μg/mL in 0.05% Tween-20 in blocking buffer) was added to each well and incubated with shaking for lHour at room temperature. Following incubation with the secondary antibody, the wells were rinsed with wash buffer after which 25 μΙ_, of goat anti-rabbit SULFO TAG secondary detection antibody (required aspect of the MSD system) (diluted to 0.25 μg/mL in 0.05% Tween- 20 in blocking buffer) was added to each well and incubated with shaking for 1 hour at room temperature. After rinsing three times with wash buffer, 150 μΙ_, of read buffer T with surfactant (MSD) were added to each empty well, and the plate was imaged on a SI 6000 imager (MSD) according to manufacturers' instructions provided for 96- or 384-well plates. The resulting IC50 values (μΜ) for compounds tested are shown in Table 1.

As shown in Table 1, test compounds described herein had the following IC50 values, an IC50 value between > 3 μΜ and < 33 μΜ is indicated by a single star (*), an IC50 value between > 1 μΜ and < 3 μΜ is indicated by two stars (**), an IC50 value between > 0.5 μΜ and < 1 μΜ is indicated by three stars (***), an IC50 value between > 0.1 μΜ and < 0.5 μΜ is indicated by four stars (****) and an IC ₅₀ value of < 0.1 μΜ is indicated by five stars (*****).

Table 1

Cpd ICso Cpd ICso Cpd IC50

29 * 481 * 706 *

72 * 482 * 709 *

74 ** 486 *** 710 ****

75 ** 487 *** 711 ****

88 * 489 * 713 ****

94 * 490 * 714 *

96 * 502 ***** 718 ****

107 * 503 ** 719 *****

108 * 504 **** 720 *

109 ** 505 * 721 ***

114 * 506 * 723 *

118 * 507 * 727 *

120 ** 516 ***** 733 **

121 * 530 * 734 *

123 * 531 * 735 *

124 * 532 ** 736 * Cpd ICso Cpd ICso Cpd ICso

125 * 540 ** 738 ****

128 * 545 * 739 ***

129 * 546 ** 741 ***

131 * 549 * 748 ***

133 *** 550 * 749 *

135 ** 552 * 750 *

136 * 553 * 751 *

137 ** 555 * 752 ****

138 ** 556 * 753 ****

141 ** 557 * 754 ***

162 * 566 **** 755 **

163 * 567 * 756 ****

170 * 568 ** 763 ****

179 * 569 ** 766 ***

191 * 578 * 768 **

192 * 579 * 770 *

194 * 580 * 771 ***

199 * 581 ** 773 *

209 **** 582 * 774 *

219 * 584 * 776 *

228 * 585 *** 777 *

229 * 586 * 780 **

258 * 587 **** 787 *

259 * 588 *** 791 *****

261 * 589 * 793 **

268 * 590 * 796 *****

269 *** 591 * 836 *

271 ** 592 * 837 *

272 *** 593 ** 838 *

287 **** 594 ** 839 *

302 **** 595 ** 840 *

305 **** 599 ** 841 *

306 **** 606 * 842 *

308 *** 608 *** 843 *

309 ** 609 * 844 * Cpd ICso Cpd ICso Cpd ICso

318 ** 612 ** 845 *

336 * 613 ** 846 *

337 * 624 *** 847 *

350 * 627 ** 848 *

351 * 628 * 849 *

356 * 632 ** 850 *

400 * 633 * 851 *

401 * 635 ** 852 *

409 ** 636 * 853 *

410 *** 637 *** 854 *

412 * 639 * 855 *

413 ***** 641 * 856 **

420 ** 649 *** 857 ***

421 * 653 ***** 858 **

422 **** 654 ***** 859 **

423 * 655 **** 860 *

428 * 656 **** 861 *

438 *** 662 *** 862 **

441 ** 665 * 863 **

442 * 667 ** 864 *****

444 * 668 *** 865 *

450 * 671 ** 866 *

451 * 673 * 867 *

452 **** 674 * 868 **

460 * 677 * 869 *****

461 * 679 * 870 *****

462 ** 683 * 871 *****

463 * 684 * 872 *****

465 * 685 * 873 ****

474 *** 688 * 874 ****

476 * 696 ***** 875 *****

477 ** 702 ** 876 **

479 * 705 *** 877 *****

480 **** Without regard to whether a document cited herein was specifically and individually indicated as being incorporated by reference, all documents referred to herein are incorporated by reference into the present application for any and all purposes to the same extent as if each individual reference was fully set forth herein.

Having now fully described the subject matter of the claims, it will be understood by those having ordinary skill in the art that the same can be performed within a wide range of equivalents without affecting the scope of the subject matter or aspects described herein. It is intended that the appended claims be interpreted to include all such equivalents.