发明名称 THIAZOLOPYRIMIDINONES AND METHODS OF USE THEREOF
摘要 The present invention relates to certain thiazolopyrimidinone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
申请公布号 US2016222033(A1) 申请公布日期 2016.08.04
申请号 US201615094687 申请日期 2016.04.08
申请人 Genentech, Inc. 发明人 Yu Jiang;Wu Guosheng;Yuen Po-Wai;Villemure Elisia;Schwarz Jacob;Ly Cuong;Sellers Benjamin;Matthew Volgraf
分类号 C07D513/14;C07D513/10;C07D519/00;C07D513/04 主分类号 C07D513/14
代理机构 代理人
主权项 1. A compound of Formula (II): wherein Ra is C1-6alkyl or C2-6alkenyl, each optionally substituted with one or more Rb substituents; C2-6alkynyl; halo; —C(O)Rc; —NRdRe; —C(O)NRdRe; —C(S)NRdRe; —C(═N—OH)—C1-4alkyl; —OC1-4alkyl; —OC1-4haloalkyl; —SC1-4alkyl; —SO2C1-4alkyl; cyano; C3-6cycloalkyl optionally substituted with one or more Rf substituents; or a phenyl, monocyclic heteroaryl, or heterocycloalkyl ring, each ring optionally substituted with one or more Rg substituents; wherein each Rb substituent is independently selected from the group consisting of —OH, —C1-4alkoxy, —NRdRe, —C(O)NRdRe, —SC1-4alkyl, —SO2C1-4alkyl, cyano, halo, C3-6cycloalkyl, and monocyclic heteroaryl;Rc is C1-4alkyl, —C1-4haloalkyl, C3-6cycloalkyl, or a monocyclic, carbon-linked heterocycloalkyl;Rd is H or C1-4alkyl;Re is H; C1-4alkyl optionally substituted with —CN, —CF3, —OH, or a monocyclic heterocycloalkyl; C3-6cycloalkyl; —OH; or —OC1-4alkoxy;or Rd and Re taken together with the nitrogen to which they are attached form a heterocycloalkyl, optionally substituted with C1-4alkyl or —OH;each Rf substituent is independently selected from the group consisting of: C1-4alkyl optionally substituted with —OH, cyano, or C1-4alkoxy; —OH; halo; C1-4haloalkyl; —CONH2; and cyano; andeach Rg substituent is independently selected from the group consisting of C1-4alkyl, —CF3, halo, —NH2, —OCH3, cyano, and —OH; R1 is selected from the group consisting of H, C1-6alkyl, C1-4haloalkyl, C3-6cycloalkyl, halo, —OC1-4alkyl, —OC1-4haloalkyl, cyano, and —C(O)C1-4alkyl; or Ra and R1 taken together with the carbons to which they are attached form a 5- to 7-membered ring, optionally containing an O or NH, and optionally substituted with one or more Rh substituents; wherein each Rh substituent is independently —C(O)NRiRj, cyano, or is C1-4alkyl optionally substituted with —OH, —OCH3, cyano, or —C(O)NRiRj; or two Rh groups attached to the same carbon and taken together with the carbon to which they are attached form a carbonyl or a C3-6cycloalkyl; wherein Ri and Rj are each independently H or C1-4alkyl; R2 is —Rm, —ORm, or —NRmRn; wherein Rm is aryl or heteroaryl, each optionally substituted with one or more Rs substituents; wherein each Rs substituent is independently selected from the group consisting of C1-4alkyl, C2-4alkenyl (optionally substituted with halo), C2-4alkynyl, C1-4haloalkyl, C1-4alkoxy, C1-4alkyl-OH, C1-4haloalkoxy, halo, cyano, C3-6cycloalkyl (optionally substituted with —OH or halo), monocyclic heteroaryl, —NH2, —NO2, —NHSO2C1-4alkyl, and —SO2C1-4alkyl;Rn is H, C1-4haloalkyl, or C1-4alkyl optionally substituted with —OH or C1-4alkoxy; or Rm and Rn taken together with the nitrogen to which they are attached form a pyrrolidine or piperidine ring, optionally substituted with C1-4alkyl and optionally fused to phenyl, wherein said phenyl is optionally substituted with halo; R3 is H or methyl; and R4 is H or fluoro; or a pharmaceutically acceptable salt thereof.
地址 South San Francisco CA US