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Title:
リジン特異的脱メチル化酵素1阻害薬およびその使用
Document Type and Number:
Japanese Patent JP5868948
Kind Code:
B2
Abstract:
The present invention relates to a compound of Formula 1, wherein: (A) is heteroaryl or aryl; each (A'), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A') is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, haloalkoxy, aryl, arylalkoxy, alkyl, alkoxy, amido, -CH 2 C(=O)NH 2 , heteroaryl, cyano, sulfonyl, and sulfinyl; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is -NH-; (L) is chosen from a single bond, -CH 2 -, -CH 2 CH 2 -, -CH 2 CH 2 CH 2 -, and -CH 2 CH 2 CH 2 CH 2 -; and (D) is an aliphatic carbocyclic group or benzocycloalkyl, wherein said aliphatic carbocyclic group or said benzocycloalkyl has 0, 1, 2, or 3 substituents independently chosen from - NH 2 , -NH(C 1 -C 6 alkyl), -N(C 1 -C 6 alkyl)(C 1 -C 6 alkyl), alkyl, halo, amido, cyano, alkoxy, haloalkyl, and haloalkoxy. A €² x ˆ’ A ˆ’ B ˆ’ Z ˆ’ L ˆ’ D The compounds of the invention show activity for inhibiting LSD1, which makes them useful in the treatment or prevention of diseases such as cancer.

Inventors:
Albert Ortega Munoz
Julio Castro-Palomino Laria
Matthew Colin Thor Fife
Application Number:
JP2013505467A
Publication Date:
February 24, 2016
Filing Date:
April 19, 2011
Export Citation:
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Assignee:
ORYZON GENOMICS S.A.
International Classes:
C07C211/40; A61K31/135; A61K31/16; A61P31/12; A61P31/18; A61P31/22; A61P35/00; A61P43/00; C07C211/42; C07C217/56; C07C237/24
Domestic Patent References:
JP2001503013A
Foreign References:
WO1999067203A1
Other References:
Indian Journal of Chemistry,Vol.16B, No.3,p.220-225 (1978).
BOLESOV I G,CYCLOPROPANES AND CYCLOBUTANES LXVIII. N-MONO- AND N,N-DISUBSTITUTED 1-AMINO-2-PHENYLCYCLOPROPANES,JOURNAL OF ORGANIC CHEMISTRY OF THE USSR,ロシア,M A I K NAUKA - INTERPERIODICA,1974年 6月 1日,V10 N6,P1678-1684
Bioorganic & Medicinal Chemistry Letters,Vol.18,p.3047-3051 (2008).
Journal of Medicinal and Pharmaceutical Chemistry,Vol.5, No.6 ,p.1265-1284 (1962).
Attorney, Agent or Firm:
Aoyama Aoi
Takuji Yamada
Michiko Matsutani
Yasushi Ochiai
Mizuhara Masahiro