发明名称 Protein kinase inhibitors
摘要 The present invention relates to a novel family of inhibitors of protein kinases of Formula (1) wherein X is selected from CH2, O, S(0)n, or NR6; and process for their production and pharmaceutical compositions thereof. In particular, the present invention relates to inhibitors of the members of the Tec, Src, Btk and Lck protein kinase families.;
申请公布号 US9624239(B2) 申请公布日期 2017.04.18
申请号 US201214009635 申请日期 2012.04.03
申请人 Pharmascience Inc. 发明人 Laurent Alain;Rose Yannick;Morris Stephen;Jaquith James
分类号 A61K31/519;C07D487/04;C07D491/147;C07D495/14;C12Q1/48;C07D487/14;C07K14/47;C12N9/12 主分类号 A61K31/519
代理机构 Leydig, Voit & Mayer, Ltd. 代理人 Leydig, Voit & Mayer, Ltd.
主权项 1. A compound of Formula 1: m is 0; X is CH2 or O; n is an integer from 0 to 2; R1 is wherein Y is selected from O or CH2; wherein X2, X3, X5, X6, X2′, X3′, X4′, X5′, X6′ are independently selected from CR and N; each R is independently selected from hydrogen, halogen, —NO2, —CN, alkyl, alkenyl, alkynyl, —OR3, —OC(O)R3, —OC(O)NR4R5, —NR4R5, —S(O)nR3, —C(O)R3, —C(O)OR3, —C(O)NR4R5, —S(O)2NR4R5, —NR2C(O)R3, —NR2S(O)nR3, —NR2C(O)NR4R5, —NR2S(O)2NR4R5, aryl, heteroaryl, carbocyclyl, and heterocyclyl; R2 is selected from hydrogen, alkyl, alkenyl, alkynyl, heteroalkyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl, R2a, R2b, R2c, R2d, R2e, R2f are independently selected from hydrogen, alkyl, heteroalkyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl; R3 is selected from hydrogen, alkyl, alkenyl, alkynyl, heteroalkyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl; and R4 and R5 are independently selected from hydrogen, alkyl, heteroalkyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl; or R4 and R5 can be fused to form a 3 to 8 membered heterocyclyl ring system.
地址 Montreal, Quebec CA