发明名称 HISTONE DEACETYLASE INHIBITORS AND COMPOSITIONS AND METHODS OF USE THEREOF
摘要 Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use.;
申请公布号 US2016333001(A1) 申请公布日期 2016.11.17
申请号 US201615148884 申请日期 2016.05.06
申请人 CHDI Foundation, Inc. 发明人 Dominguez Celia;Maillard Michel C.;Breccia Perla;Haughan Alan F.;Jarvis Rebecca E.;Luckhurst Christopher A.;Saville-Stones Elizabeth A.;Stott Andrew J.;Van de Poël Amanda;Wall Michael;Wishart Grant
分类号 C07D413/12;C07D491/107 主分类号 C07D413/12
代理机构 代理人
主权项 1. A compound of Formula I: or a pharmaceutically acceptable salt thereof, an optical isomer, or a mixture of optical isomers thereof; wherein: R1 is selected from: H and C1-C3 alkyl;p is 0; and R2 and R3, together with the carbon to which they are attached, form a 3 to 6-membered cycloalkyl group, optionally substituted with one or two C1-C2 alkyl, C1-C2 haloalkyl or halo; orp is 1; R2 is H; and R3 and R4, together with the carbon atoms to which they are each attached, form a cyclopropyl group, wherein said cyclopropyl group is optionally substituted with one or two halo groups;R5 is C0-C3 alkylene;R6 is selected from: H, C1-C3 alkyl, and C1-C3 haloalkyl; andR7 is selected from: aryl, aryl-C1-C4-alkyl, heteroaryl, and heteroaryl-C1-C4-alkyl, each of which is optionally substituted on the aromatic moiety with one to five substituents each independently selected from: C1-C4alkylamino, C2-C8dialkylamino, C1-C4alkoxy, amino, cyano, halo, and hydroxyl; orR6 and R7, together with the nitrogen atom to which they are both attached, form a 5, 6, or 7-membered heteromonocyclic group, or a 6, 7, 8, 9, or 10-membered heterobicyclic group, each of which is optionally substituted with one to five substituents each independently selected from: C1-C4 alkoxy, C1-C3 alkyl, C1-C3 haloalkoxy, C1-C3 haloalkyl, 3 or 4-membered cycloalkoxy, 3 or 4-membered cycloalkyl, 3 or 4-membered heterocycloalkyl, aryl, cyano, halo, and heteroaryl, wherein aryl, 3 or 4-membered cycloalkyl, and heteroaryl are optionally further substituted with one to five substituents each independently selected from: C1-C3 alkoxy, C1-C3 alkyl, C1-C3 haloalkyl, cyano, and halo;W is N or CR8; X is N or CR9; Y is N or CR10; and Z is N or CR11; provided not more than two of W, X, Y, and Z are N; andR8, R9, R10 and R11 are each independently selected from: H, C1-C4alkyl, C1-C4 haloalkyl, and halo.
地址 New York NY US