发明名称 INDAZOLES
摘要 Herein are disclosed indazoles of formula (I);;where the various groups are defined herein, and which are useful for treating cancer.
申请公布号 US2014350013(A1) 申请公布日期 2014.11.27
申请号 US201414458305 申请日期 2014.08.13
申请人 GlaxoSmithKline LLC 发明人 DUQUENNE Celine;Johnson Neil;Knight Steven D.;Lafrance Louis;Miller William H.;Newlander Kenneth;Romeril Stuart;Rouse Meagan B.;Tian Xinrong;Verma Sharad Kumar
分类号 C07D409/14;C07D401/14;C07D401/12 主分类号 C07D409/14
代理机构 代理人
主权项 1. A compound of formula (I):wherein X and Z are selected independently from the group consisting of hydrogen, (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, unsubstituted or substituted (C3-C8)cycloalkyl, unsubstituted or substituted (C3-C8)cycloalkyl-(C1-C8)alkyl or -(C2-C8)alkenyl, unsubstituted or substituted (C5-C8)cycloalkenyl, unsubstituted or substituted (C5-C8)cycloalkenyl-(C1-C8)alkyl or -(C2-C8)alkenyl, (C6-C10)bicycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryl-(C1-C8)alkyl or -(C2-C8)alkenyl, halo, cyano, —CORa, CO2Ra, —CONRaRb, —CONRaNRaRb, —SRa, —SORa, —SO2Ra, —SO2NRaRb, nitro, —NRaRb, —NRaC(O)Rb, —NRaC(O)NRaRb, —NRaC(O)ORa, —NRaSO2Rb, —NRaSO2NRaRb, —NRaNRaRb, —NRaNRaC(O)Rb, —NRaNRaC(O)NRaRb, —NRaNRaC(O)ORa, —ORa, —OC(O)Ra, and —OC(O)NRaRb; Y is H or halo; R1 is (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, unsubstituted or substituted (C3-C8)cycloalkyl, unsubstituted or substituted (C3-C8)cycloalkyl-(C1-C8)alkyl or -(C2-C8)alkenyl, unsubstituted or substituted (C5-C8)cycloalkenyl, unsubstituted or substituted (C5-C8)cycloalkenyl-(C1-C8)alkyl or -(C2-C8)alkenyl, unsubstituted or substituted (C6-C10)bicycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryl-(C1-C8)alkyl or -(C2-C8)alkenyl, —CORa, —CO2Ra, —CONRaRb, or —CONRaNRaRb; R3 is hydrogen, (C1-C8)alkyl, cyano, trifluoromethyl, —NRaRb, or halo; R6 is selected from the group consisting of hydrogen, halo, (C1-C8)alkyl, (C2-C8)alkenyl, —B(OH)2, substituted or unsubstituted (C2-C8)alkynyl, unsubstituted or substituted (C3-C8)cycloalkyl, unsubstituted or substituted (C3-C8)cycloalkyl-(C1-C8)alkyl, unsubstituted or substituted (C5-C8)cycloalkenyl, unsubstituted or substituted (C5-C8)cycloalkenyl-(C1-C8)alkyl, (C6-C10)bicycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryl-(C1-C8)alkyl, cyano, —CORa, —CO2Ra, —CONRaRb, —CONRaNRaRb, —SRa, —SORa, —SO2Ra, —SO2NRaRb nitro, —NRaRb, —NRaC(O)Rb, —NRaC(O)NRaRb, —NRaC(O)ORa, —NRaSO2Rb, —NRaSO2NRaRb, —NRaNRaRb, —NRaNRaC(O)Rb, —NRaNRaC(O)NRaRb, —NRaNRaC(O)ORa, —ORa, —OC(O)Ra, and —OC(O)NRaRb; wherein any (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, or aryl group is optionally substituted by 1, 2, or 3 groups independently selected from the group consisting of —O(C1-C6)alkyl(Rc)1-2, —S(C1-C6)alkyl(Rc)1-2, —(C1-C6)alkyl(Rc)1-2, halo, (C1-C6)alkyl, (C3-C8)cycloalkyl, (C5-C8)cycloalkenyl, (C1-C6)haloalkyl, cyano, —CORa, —CO2Ra, —CONRaRb, —SRa, —SORa, —SO2Ra, —SO2NRaRb, nitro, —NRaRb, —NRaC(O)Rb, —NRaC(O)NRaRb, —NRaC(O)ORa, —NRaSO2Rb, —NRaSO2NRaRb, —ORa, —OC(O)Ra, —OC(O)NRaRb, aryl, and aryl(C1-C4)alkyl; wherein any aryl moiety of said aryl or aryl(C1-C4)alkyl is optionally substituted by 1, 2, or 3 groups independently selected from the group consisting of halo, (C1-C6)alkyl, (C3-C8)cycloalkyl, (C5-C8)cycloalkenyl, (C1-C6)haloalkyl, cyano, —CORa, —CO2Ra, —CONRaRb, —SRa, —SORa, —SO2Ra, —SO2NRaRb, nitro, —NRaRb, —NRaC(O)Rb, —NRaC(O)NRaRb, —NRaC(O)ORa, —NRaSO2Rb, —NRaSO2NRaRb, —ORa, —OC(O)Ra, and —OC(O)NRaRb; Ra and Rb are each independently hydrogen, (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, (C3-C8)cycloalkyl, (C5-C8)cycloalkenyl, (C6-C10)bicycloalkyl, or aryl, wherein said (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, or aryl group is optionally substituted by 1, 2, or 3 groups independently selected from halo, hydroxyl, (C1-C4)alkoxy, amino, (C1-C4)alkylamino, ((C1-C4)alkyl)((C1-C4)alkyl)amino, —CO2H, —CO2(C1-C4)alkyl, —CONH2, —CONH(C1-C4)alkyl, —CON((C1-C4)alkyl)((C1-C4)alkyl), —SO2(C1-C4)alkyl, —SO2NH2, —SO2NH(C1-C4)alkyl, and —SO2N((C1-C4)alkyl)((C1-C4)alkyl); or Ra and Rb taken together with the nitrogen to which they are attached represent a 5-8 membered saturated or unsaturated ring, optionally containing an additional heteroatom selected from oxygen, nitrogen, and sulfur, wherein said ring is optionally substituted by 1, 2, or 3 groups independently selected from (C1-C4)alkyl, (C1-C4)haloalkyl, amino, (C1-C4)alkylamino, ((C1-C4)alkyl)((C1-C4)alkyl)amino, hydroxyl, oxo, (C1-C4)alkoxy, and (C1-C4)alkoxy(C1-C4)alkyl, wherein said ring is optionally fused to a (C3-C8)cycloalkyl or aryl ring; or Ra and Rb taken together with the nitrogen to which they are attached represent a 6- to 10-membered bridged bicyclic ring system optionally fused to a (C3-C8)cycloalkyl or aryl ring; and each Rc is independently —NRaSO2Rb, —SORa, —SO2Ra, —NRaC(O)ORa, —NRaRb, or —CO2Ra; or a pharmaceutically acceptable salt thereof.
地址 Wilmington DE US