发明名称 Protein kinase C inhibitors and uses thereof
摘要 This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
申请公布号 US9321763(B2) 申请公布日期 2016.04.26
申请号 US201313857028 申请日期 2013.04.04
申请人 Rigel Pharmaceuticals, Inc. 发明人 Singh Rajinder;Duncton Matthew;Zhang Jing;Alvarez Salvador;Tso Kin;Holland Sacha;Yen Rose;Kolluri Rao;Heckrodt Thilo;Chen Yan;Masuda Esteban;Li Hui;Payan Donald G.;Kelley Ryan
分类号 A61K31/506;A61K31/505;A61K31/535;A61K31/553;C07D471/04;C07D519/00;C07D295/00 主分类号 A61K31/506
代理机构 Bozicevic, Field & Francis LLP 代理人 Ng Rudy J.;Francis Carol L.;Bozicevic, Field & Francis LLP
主权项 1. A compound of formula (VI): wherein R1, R2, R3, R4, R5, and R6 are independently selected from hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, acyl, acylamino, acyloxy, amino, substituted amino, aminoacyl, aminoacyloxy, oxyaminoacyl, azido, cyano, halogen, hydroxyl, carboxyl, carboxylalkyl, thiol, thioalkoxy, substituted thioalkoxy, aryl, aryloxy, hydroxyamino, alkoxyamino, nitro, —SO-alkyl, —SO— substituted alkyl, —SO-aryl, —SO-heteroaryl, —SO2-alkyl, —SO2-substituted alkyl, —SO2-aryl and —SO2-heteroaryl; or R1 and R2 together form an oxo group; or R3 and R4 together form an oxo group; or R5 and R6 together form an oxo group; R7, R8, R9, and R10 are independently selected from hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, acyl, acylamino, acyloxy, amino, substituted amino, aminoacyl, aminoacyloxy, oxyaminoacyl, azido, cyano, halogen, hydroxyl, carboxyl, carboxylalkyl, thiol, thioalkoxy, substituted thioalkoxy, aryl, aryloxy, hydroxyamino, alkoxyamino, nitro, —SO-alkyl, —SO-substituted alkyl, —SO-aryl, —SO-heteroaryl, —SO2-alkyl, —SO2-substituted alkyl, —SO2-aryl and —SO2-heteroaryl; or R7 and R8 together form an oxo group; or R9 and R10 together form an oxo group; R11 is selected from alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, hydroxy, alkoxy, substituted alkoxy, amino, substituted amino, carboxyl, carboxyl ester, cyano, halogen, thiol, thioalkoxy, substituted thioalkoxy, acyl, aminoacyl, nitro, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, —SO-alkyl, —SO-substituted alkyl, —SO-aryl, —SO-heteroaryl, —SO2-alkyl, —SO2-substituted alkyl, —SO2-aryl and —SO2-heteroaryl; R20 is selected from hydrogen, alkyl, and substituted alkyl; G is halogen or —NY2Ar1; Y1 and Y2 are independently selected from hydrogen, alkyl and substituted alkyl; and Ar1 is selected from aryl, substituted aryl, heteroaryl, and substituted heteroaryl; or a salt or stereoisomer thereof.
地址 South San Francisco CA US