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New histone deacetylase inhibitors and their use in therapy
专利权人:
Karus Therapeutics Limited
发明人:
SHUTTLEWORTH, Stephen Joseph,TOMASSI, Cyrille Davy,CECIL, Alexander Richard Liam,MACCORMICK, Somhairle,NODES, William John,SILVA, Franck Alexandre
申请号:
ES13792060
公开号:
ES2672701T3
申请日:
2013.11.06
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
A compound of formula ** Formula ** where: it is a single bond and X is N; and where: R is H; each R 'is independently selected from H and QR1; each Q is independently selected from a link, 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- heterocycloalkyl C10 or trifluoromethyl; L is a 5-membered nitrogen-containing heteroaryl, optionally condensed to a benzene, with the proviso that L is not pyrrole or benzo-condensed pyrrole; Y is a pyridyl; W is the zinc -CONHOH binding group of the structure: each aryl or heteroaryl may be substituted with up to five substituents selected from C1-C6 alkyl, hydroxy, C1-C3 hydroxyalkyl, C1-C3 alkoxy, C1-C3 haloalkoxy, amino , mono C1-C3 alkylamino, bis C1-C3 alkylamino, C1-C3 acylamino, C1-C3 aminoalkyl, mono (C1-C3 alkyl) amino C1-C3 alkyl, bis (C1-C3 alkyl) amino C1-C3 alkyl, acylamino C1-C3, C1-C3 alkyl sulfonylamino, halo, nitro, cyano, trifluoromethyl, carboxy, C1-C3 alkoxycarbonyl, aminocarbonyl, mono C1-C3 alkylcarbonyl, bis C1-C3 alkylcarbonyl, -SO3H, C1-C3 alkylsulfonyl, aminosulfonyl , mono C1-C3 alkyl aminosulfonyl and bis C1-C3 alkyl aminosulfonyl; each alkyl, alkenyl or alkynyl may be optionally substituted with aryl, C3-C10 cycloalkyl, heteroaryl, halogen, NH2, NO2 or hydroxyl, or its pharmaceutically acceptable salt; wherein in at least one, preferably in both, of L and Y, the atom that is directly bonded to X is a carbon, and at least one nitrogen atom is directly bonded to said carbon; wherein in addition to an N atom, L contains at least one more heteroatom in the heteroaryl ring selected from N, O or S; and where n is 5 to 7.Un compuesto de fórmula**Fórmula** en donde: es un enlace sencillo y X es N; y en donde: R es H; cada R' se selecciona en forma independiente entre H y QR1; cada Q se selecciona en forma independiente entre un enlace, CO, CO2, NH, S
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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