Title:
ＴＡＡＲリガンドとしての置換アゼチジン誘導体
Document Type and Number:
Japanese Patent JP6539724
Kind Code:
B2
Abstract:
The present invention relates to a compound of formula I wherein R1 is hydrogen, methoxy or fluoro; R2/R2' are independently from each other hydrogen, methoxy or fluoro; R3/R4 are independently from each other hydrogen or halogen; R is hydrogen or fluoro; L1 is -CH2-, -NR'-, -0-, -S-, CF2- or CH=; R' is hydrogen or lower alkyl; L2 is a bond, -C(0)NH-, -NH-, -CH2NHC(O)-, -NHC(O)- or -NHC(0)NH-; R is hydrogen, halogen, lower alkoxy, cyano or is phenyl optionally substituted by one or more substituents, selected from halogen, lower alkyl substituted by halogen or lower alkoxy, or is a five or six membered heteroaryl, selected from pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl or pyrazolyl, which heteroaryls are optionally substituted by one or more substituents, selected from halogen, lower alkyl, lower alkoxy, cyano, cycloalkyl, lower alkyl substituted by halogen, lower alkoxy substituted by halogen or by phenyl substituted by halogen; N is a ring nitrogen atom in position 1 or 2; or to a pharmaceutically suitable acid addition salt thereof. The compounds of formulas I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
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Inventors:
Cecele, Giuseppe
Flounder, Guido
Norcross, Roger
Friger, Philip
Robel, Etienne
Flounder, Guido
Norcross, Roger
Friger, Philip
Robel, Etienne
Application Number:
JP2017505642A
Publication Date:
July 03, 2019
Filing Date:
August 24, 2015
Export Citation:
Assignee:
F. HOFFMANN-LA ROCHE AKTIENGESELLSCHAFT
International Classes:
C07D205/04; A61K31/397; A61K31/4155; A61K31/4427; A61K31/497; A61K31/501; A61K31/506; A61P3/04; A61P3/06; A61P3/10; A61P9/00; A61P9/06; A61P9/12; A61P25/08; A61P25/14; A61P25/16; A61P25/18; A61P25/20; A61P25/22; A61P25/24; A61P25/28; A61P25/30; A61P43/00; C07D205/06; C07D401/12; C07D403/12
Domestic Patent References:
| JP2012515761A | ||||
| JP2010527980A | ||||
| JP2012509925A | ||||
| JP2003528845A | ||||
| JP2010534701A |
Foreign References:
| DE102004061748A1 | ||||
| WO2013170072A2 |
Other References:
RN 1203683-27-5 REGISTRY,DATABASE REGISTRY [ONLINE] Retrieved from STN,2010年 1月27日,検索日: 13 DEC 2017
HODGSON, D. M. ET AL,Lithiation-Electrophilic Substitution of N-Thiopivaloylazetidine,Angewandte Chemie (International ed.),2010年,49(16),2900-2903
TESTA, E. ET AL,Auf das Zentralnervensystem wirkende Substanzen, XXI. Zur Chemie der Azetidine, V 3-Monosubstituierte Azetidine,Justus Liebigs Annalen der Chemie,1961年,647(1),92-100
HODGSON, D. M. ET AL,Lithiation-Electrophilic Substitution of N-Thiopivaloylazetidine,Angewandte Chemie (International ed.),2010年,49(16),2900-2903
TESTA, E. ET AL,Auf das Zentralnervensystem wirkende Substanzen, XXI. Zur Chemie der Azetidine, V 3-Monosubstituierte Azetidine,Justus Liebigs Annalen der Chemie,1961年,647(1),92-100
Attorney, Agent or Firm:
Patent business corporation Tsukuni