11-04-2013 дата публикации
Номер: US20130090386A1
Принадлежит:
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, —CHC(=0)NH, 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—, —CHCH—, —CHCHCH—, and —CHCHCHCH—; 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, —NH(C-Calkyl), —N(C-Calkyl)(C-Calkyl), alkyl, halo, amido, cyano, alkoxy, haloalkyl, and haloalkoxy. (A′)X-(A)-(B)—(Z)-(L)-(D) formula (I) The compounds of the invention show activity for inhibiting LSD1, which makes them useful in the treatment or prevention of diseases such as cancer. 1. A compound of Formula 1{'br': None, 'sub': 'X', '(A′)-(A)-(B)—(Z)-(L)-(D)\u2003\u20031'} (A) is heteroaryl or aryl;', {'sub': 2', '2, '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, —CHC(═O)NH, 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—;', {'sub': 2', '2', '2', '2', '2', '2', '2', '2', '2', '2, '(L) is chosen from a single bond, —CH—, —CHCH—, —CHCHCH—, and —CHCHCHCH—; and'}, {'sub': 2', '1', '6', '1', '6', '1', ...
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