发明名称 Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as PARP inhibitors
摘要 Provided are certain fused tetra or penta-cyclic compounds and salts thereof, compositions thereof, and methods of use thereof.
申请公布号 US9617273(B2) 申请公布日期 2017.04.11
申请号 US201614988484 申请日期 2016.01.05
申请人 BeiGene, Ltd. 发明人 Zhou Changyou;Ren Bo;Wang Hexiang
分类号 C07D487/06;C07D487/14;C07D487/04;C07D471/16;C07D471/22 主分类号 C07D487/06
代理机构 Cooley LLP 代理人 Cooley LLP
主权项 1. A compound of Formula (I): or a stereoisomer or a pharmaceutically acceptable salt thereof, wherein: RN is hydrogen or alkyl, wherein the alkyl is optionally substituted with at least one of hydroxyl or C1-C12 alkoxyl;X is C or N;m and n are each 1 or 2;t is 0 or 1;R1 at each occurrence, is independently selected from halogen, CN, NO2, OR9, NR9R10, NR9COR10, NR9SO2R10, CONR9R10, COOR9, SO2R9, alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl;R2 is hydrogen or alkyl;R3, R4, R5, R6, R7 and R8, which may be the same or different, are each independently selected from hydrogen, —OR9, —COR9, —CO2R9, alkyl, cycloalkyl, or aryl,or (R3 and R4), and/or (R4 and R5), and/or (R5 and R6), and/or (R6 and R7), and/or (R7 and R8), together with the atom(s) they are attached, form a 3- to 8-membered saturated, partially or fully unsaturated ring having 0, 1 or 2 heteroatoms independently selected from —NR13—, —O—, —S—, —SO— or —SO2—;provided that when X is N, R6 is absent,R9 and R10, which may be the same or different, are each selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl;R13 is selected from hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, and heterocyclyl,wherein the cycloalkyl is a hydrocarbon group selected from saturated and partially unsaturated cyclic hydrocarbon groups, comprising monocyclic, bicyclic and tricyclic groups, and comprising from 3 to 12 carbon atoms;wherein the heteroaryl is a group selected from: 5- to 7-membered aromatic, monocyclic rings comprising at least one heteroatom selected from N, O, and S, with the remaining ring atoms being carbon;8- to 12-membered bicyclic rings comprising at least one heteroatom selected from N, O, and S, with the remaining ring atoms being carbon and wherein at least one ring is aromatic and at least one heteroatom is present in the aromatic ring; and11- to 14-membered tricyclic rings comprising at least one heteroatom selected from N, O, and S, with the remaining ring atoms being carbon and wherein at least one ring is aromatic and at least one heteroatom is present in an aromatic ring; andwherein the heterocyclyl is a ring selected from 4- to 12-membered monocyclic, bicyclic and tricyclic, saturated and partially unsaturated rings, comprising at least one carbon atoms in addition to at least one heteroatom selected from oxygen, sulfur, and nitrogen.
地址 Grand Cayman KY