发明名称 SUBSTITUTED HETERO-AZEPINONES
摘要 There are provided compounds of the formula;;wherein:;V, W, X, Y, Z, R1, R2, R3, R4, R5 and R6 are described herein. The compounds are useful for the treatment of proliferative diseases, including cancer.
申请公布号 US2015361059(A1) 申请公布日期 2015.12.17
申请号 US201314418383 申请日期 2013.08.06
申请人 Hoffman-La Roche Inc. 发明人 Donnell Andrew F.;Han Xiaochun;Kester Robert Francis;Kong Norman;Le Kang;Lou Yan;Michoud Christophe;Moliterni John Anthony;Remiszewski Stacy;Rupert Kenneth Carey;Yun Weiya
分类号 C07D267/14;C07D267/12;C07D281/10;C07D417/06;C07D413/12;C07D413/14;C07D413/06;C07D498/10;C07D417/12 主分类号 C07D267/14
代理机构 代理人
主权项 1. A compound of the formula wherein: W and X are the same or different and are independently selected from H, C1-6-alkyl, hydoxy-C1-6-alkyl, aryl-C1-6-alkyl, C3-7-cycloalkyl-C1-6-alkyl, C2-6-alkenyl-C1-6-alkyl, C2-6-alkynyl-C1-6-alkyl and heterocycle or X and W together with the nitrogen to which they are bound can form a C2-9-heterocycle, or W together with the nitrogen to which it is bound and Y together with the carbon to which it is bound can form a C3-9-heterocycle; Y is C1-6-alkyl, hydoxy-C1-6-alkyl or C3-7-cycloalkyl-C1-6-alkyl; R1 is selected from H, halo, C1-6-alkyl, halo-C1-6-alkyl, aryl-C1-6-alkyl, C3-7-cycloalkyl-C1-6-alkyl, COOH, C(O)NR8′R9′, acyl, OR7, SR7, NR8R9, N-acyl, N-sulfonyl, cyano and SO2R10; R2 is selected from H, halo, C1-6-alkyl, aryl-C1-6-alkyl, C3-7-cycloalkyl-C1-6-alkyl, acyl, OR7, SR7, NR8R9, N-acyl, N-sulfonyl, cyano and SO2R10; R3 is selected from H, halo, C1-6-alkyl, halo-C1-6-alkyl, aryl-C1-6-alkyl, C3-7-cycloalkyl-C1-6-alkyl, acyl, OR7, SR7, NR8R9, N-acyl, N-sulfonyl, cyano and SO2R10; R4 is H or C1-6-alkyl; R5 and R6 are the same or different and are independently selected from H, C1-6-alkyl, C1-6-alkyl-S—C1-6-alkyl, C1-6-alkyl-O—C1-6-alkyl, aryl and C3-7-cycloalkyl, or R5 and R6 together with the carbon to which they are bound can form a C4-7-carbocycle or heterocycle, which is optionally substituted by C1-6-alkyl-SO2; V is S, O or SO2 Z is selected from C1-6-alkyl, aryl, optionally substituted by C3-7-cycloalkyl, C1-6-alkyl, C1-6-alkoxy, halo, halo-C1-6-alkoxy, C(O)N(C1-6-alkyl,C1-6-alkyl), C(O)NHSO2—C1-6-alkyl, C(O)N(C1-6-alkyl,hydroxy-C1-6-alkyl), C(O)N(C1-6-alkyl,COOH—C1-6-alkyl), phenyl optionally substituted by cyano, COO—C1-6-alkyl or COOH; aryl-C1-6-alkyl, heteroaryl optionally substituted by cyano, C1-6-alkoxy or phenyl optionally substituted by C(O)N(H,C1-6-alkyl), cyano or COOH, polycyclic aromatics, polycyclic heteroaromatics, optionally substituted by halo, SO2-phenyl, C1-6-alkyl-phenyl or phenyl optionally substituted by cyano; mixed aryl and non-aryl polycycles and mixed aryl and non-aryl polyheterocycles; optionally substituted by SO2—C1-6-alkyl, oxo, halo or C1-6-alkyl; R7 is C1-6-alkyl, aryl, heteroaryl or sulfonyl; R8 and R9 are the same or different and independently selected from H, C1-6-alkyl, aryl, aryl-C1-6-alkyl, whereby the alkyl portion is optionally substituted by oxo; and heteroaryl-C1-6-alkyl, R8′ is selected from H and C1-6-alkyl R9′ is selected from HOOC—C1-6-alkyl, hydroxy-C1-6-alkyl and aryl-C1-6-alkyl, wherein the aryl portion is substituted by COOH, or R8′ and R9′ form together with the nitrogen to which they are attached a heterocyclyl, substituted by hydroxy-C1-6-alkyl; and R10 is C1-6-alkyl, aryl, heterocyclyl or aryl-C1-6-alkyl or a pharmaceutically acceptable salt thereof.
地址 Little Falls NJ US