发明名称 Selective histone deactylase 6 inhibitors
摘要 Disclosed are selective histone deactylase inhibitors (HDACi) that having Formula (I). Methods of making and using these inhibitors for the treatment of cancer, in particular melanoma are also disclosed.;
申请公布号 US9409858(B2) 申请公布日期 2016.08.09
申请号 US201314383418 申请日期 2013.03.07
申请人 H. Lee Moffitt Cancer Center and Research Institute, Inc.;Board of Trustees of the University of Illinois 发明人 Sotomayor Eduardo M.;Bergman Joel;Kozikowski Alan;Woan Karrune Veeraprasert;Villagra Alejandro V.
分类号 C07C275/28;A61K31/505;A61K31/44;A61K31/4045;A61K31/167;C07D239/42;C07D213/75;C07D209/14;C07C275/34;A61K45/06;A61K31/422;A61K31/437;A61K31/454;A61K31/69;A61K38/00 主分类号 C07C275/28
代理机构 Meunier Carlin & Curfman LLC 代理人 Meunier Carlin & Curfman LLC
主权项 1. A compound having Formula I: wherein A is C1-C8 alkyl, phenyl, pyridyl, oxazolidyl, or pyrimidyl optionally substituted with one or more groups chosen from C1-C5 alkyl, C1-C4 alkoxy, or halo; and R1 and R2 are independently chosen from hydrogen, C1-C8 alkyl, C1-C8 alkenyl, C1-C8 alkynyl, C1-C8 haloalkyl, C5-C6 cycloalkyl, C5-C6 heterocycloalkyl, C1-C3 alkylaryl, aryl, C1-C3 alkylheteroaryl, or heteroaryl, any of which is optionally substituted with acetyl, C1-C5 alkyl, amino, —NR6R7, —C(O)NR6R7, C1-C4 alkoxy, C1-C4 alkylhydroxy, C5-C6 cycloalkyl, C5-C6 heterocycloalkyl, aryl, heteroaryl, carbonyl, halo, hydroxy, thiol, cyano, or nitro; or R1 and R2 are joined such that together they form an alkylene bridge comprising 2 atoms so that a 5-membered ring is formed with the —NC(O)N— moiety, in which case A is as defined above or hydrogen, and which 5-membered ring is optionally substituted with R1′, R2′, R1″, and R2″, which are independently, hydrogen, or are C1-C8 alkyl, C5-C6 cycloalkyl, C5-C6 heterocycloalkyl, C1-C3 alkylaryl, aryl, C1-C3 alkylheteroaryl, or heteroaryl any of which is optionally substituted with amino, aryl, C1-C4 alkoxy, halo, or hydroxy; or R1′and R1″ together or R2″ and R2′ together form a carbonyl; or R1′ and R2′ are null and R1″and R2″ together form a fused phenyl group; and R6 and R7 are independently H, C1-C4 alkyl, or are joined such that together they form an alkylene bridge comprising 4 or 5 atoms so that a 5 or 6-membered ring is formed with the nitrogen; or a pharmaceutically acceptable salt or hydrate thereof.
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