NOVEL HISTONE DEACETYLASE INHIBITORS AND THEIR USE IN THERAPY

摘要

A compound of the formula: (I) or a pharmaceutically acceptable salt thereof, wherein: L is a 5-membered nitrogen-containing heteroaryl which is optionally fused to a benzene; Y is a 5, 6 or 7-membered nitrogen-containing heteroaryl, which is optionally fused to a benzene; and W is a zinc-binding group. The compounds are HDAC inhibitors and therefore have potential utility in therapy.;

主权项

1. A compound of the formula wherein:
is a double bond and X is C; or is a single bond and X is N, CH or CQR1; and wherein:
n is 1 to 10;R is H or QR1;each R/ is independently selected from H and QR1;each Q is independently selected from a bond, CO, CO2, NH, S, SO, SO2 or O;each R1 is independently selected from H, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heteroaryl, C1-C10 cycloalkyl, halogen, C1-C10 alkylaryl, C1-C10 alkyl heteroaryl, C1-C10 heterocycloalkyl or trifluoromethyl,L is a 5-membered nitrogen-containing heteroaryl which is optionally fused to a benzene;Y is a 5, 6 or 7-membered nitrogen-containing heteroaryl, which is optionally fused to a benzene;W is a zinc-binding group;each aryl or heteroaryl may be substituted by up to five substituents selected from C1-C5 alkyl, hydroxy, C1-C3 hydroxyalkyl, C1-C3 alkoxy, C1-C3 haloalkoxy, amino, C1-C3 mono alkylamino, C1-C3 bis alkylamino, C1-C3 acylamino, C1-C3 aminoalkyl, mono(C1-C3 alkyl)amino C1-C3 alkyl, bis(C1-C3 alkyl)amino C1-C3 alkyl, C1-C3-acylamino, C1-C3 alkyl sulfonylamino, halo, nitro, cyano, trifluoromethyl, carboxy, C1-C3 alkoxycarbonyl, aminocarbonyl, mono C1-C3 alkyl aminocarbonyl, bis C1-C3 alkyl aminocarbonyl, —SO3H, C1-C3 alkylsulfonyl, aminosulfonyl, mono C1-C3 alkyl aminosulfonyl and bis C1-C3-alkyl aminosulfonyl; andeach alkyl, alkenyl or alkynyl may be optionally substituted with halogen, NH2, NO2 or hydroxyl,or a pharmaceutically acceptable salt thereof.