Julio Castro-Palomino Laria;Matthew Colin Thor Fyfe;Alberto Ortega Muñoz
发明人:
Alberto Ortega Muñoz,Julio Castro-Palomino Laria,Matthew Colin Thor Fyfe
申请号：
US13497994
公开号：
US20120283266A1
申请日:
2010.04.19
申请国别(地区):
US
年份:
2012
代理人:
摘要：
The invention relates to a compound of Formula (I): (A′)x-(A)-(B)-(Z)-(L)-(D), 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, aryl, arylalkoxy, alkyl, alkoxy, cyano, sulfonyl, amido, 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 —CH2CH2—, —CH2CH2CH2—, and —CH2CH2CH2CH2—； and (D) is chosen from —N(—R1)—R2, —O—R3, and —S—R3, wherein: R1 and R2 are mutually linked to form a heterocyclic ring together with the nitrogen atom that R1 and R2 are attached to, wherein said heterocyclic ring has 0, 1, 2, or 3 substituents independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), alkyl, halo, cyano, alkoxy, haloalkyl, and haloalkoxy, or R1 and R2 are independently chosen from —H, alkyl, cycloalkyl, haloalkyl, and heterocyclyl, wherein the sum of substituents on R1 and R2 together is 0, 1, 2, or 3, and the substituents are independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), and fluoro； and R3 is chosen from —H, alkyl, cycloalkyl, haloalkyl, and heterocyclyl, wherein R3 has 0, 1, 2, or 3 substituents independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), and fluoro； or an enantiomer, diastereomer, or mixture thereof, or a pharmaceutically acceptable salt or solvate thereof. The compounds of the invention show inhibitory LSD1 activity, which makes them useful in the treatment or prevention of diseases such as cancer.
