发明名称 METHODS OF USING PHTHALAZINONE KETONE DERIVATIVES
摘要 A phthalazinone ketone derivative as represented by formula (I), a preparation method thereof, a pharmaceutical composition containing the derivative, a use thereof as a poly (ADP-ribose) polymerase (PARP) inhibitor, and a cancer treatment method thereof are described.;
申请公布号 US2016151367(A1) 申请公布日期 2016.06.02
申请号 US201615016986 申请日期 2016.02.05
申请人 Jiangsu Hansoh Pharmaceutical Co., Ltd. 发明人 TANG Peng Cho;LI Xin;LI Xiangqin;CHEN Yang;WANG Bin;ZHU Zhe
分类号 A61K31/502;A61K31/495;A61K31/5377 主分类号 A61K31/502
代理机构 代理人
主权项 1. A method for inhibiting poly (ADP-ribose) polymerase (PARP) in a subject in need thereof, comprising administering to the subject a pharmaceutical composition comprising one or more pharmaceutically acceptable carriers or excipients, and a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein A and B are taken together with the attached carbon atoms to form an aryl or heteroaryl, wherein the aryl or heteroaryl is each independently and optionally substituted with one or more groups selected from the group consisting of an alkyl, halogen, hydroxyl, alkoxyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, —C(O)OR5, —OC(O)R5, —O(CH2)nC(O)OR5, —C(O)R5, —NHC(O)R5, —NR6R7, —OC(O)NR6R7 and —C(O)NR6R7; R1, R2, R3 and R4 are each independently selected from the group consisting of hydrogen, a halogen, alkyl, cyano and alkoxyl, wherein the alkyl or alkoxyl is each independently and optionally substituted with one or more groups selected from the group consisting of a halogen, hydroxyl, alkyl and alkoxyl; D, E, and G are each independently selected from the group consisting of a nitrogen atom and C(R8); R5 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein the alkyl, cycloalkyl, heterocyclyl, aryl or heteroaryl is each independently and optionally substituted with one or more groups selected from the group consisting of an alkyl, halogen, hydroxyl, alkoxyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, carboxyl and alkoxycarbonyl; R6 and R7 are each independently selected from the group consisting of hydrogen, alkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein the alkyl, cycloalkyl, heterocyclyl, aryl or heteroaryl is each independently and optionally substituted with one or more groups selected from the group consisting of an alkyl, halogen, hydroxyl, alkoxyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, carboxyl and alkoxycarbonyl; alternatively, R6 and R7 are taken together with the attached N atom to form a heterocyclyl, wherein the heterocyclyl contains one or more N, O or S(O)m heteratoms, and the heterocyclyl is optionally substituted with one or more groups selected from the group consisting of an alkyl, halogen, hydroxyl, alkoxyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, carboxyl and alkoxycarbonyl; R8 is selected from the group consisting of hydrogen, alkyl, halogen, hydroxyl, cyano, alkoxyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, benzyl, —C(O)OR5, —OC(O)R5, —O(CH2)nC(O)OR5, —(CH2)nNR6R7, —C(O)R5, —NHC(O)R5, —NR6R7, —OC(O)NR6R7 and —C(O)NR6R7, wherein the alkyl, alkoxyl, cycloalkyl, heterocyclyl, aryl, heteroaryl or benzyl is each independently and optionally substituted with one or more groups selected from the group consisting of an alkyl, halogen, hydroxyl, alkoxyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, oxo, —C(O)OR5, —OC(O)R5, —O(CH2)nC(O)OR5, —C(O)R5, —NHC(O)R5, —NR6R7, —OC(O)NR6R7 and —C(O)NR6R7; m is selected from the group consisting of 0, 1 and 2; and n is selected from the group consisting of 0, 1 and 2.
地址 Lianyungang CN