[EN] PYRROLIDINYL UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS<br/>[FR] COMPOSÉS DE N-PYRROLIDINYLE URÉE, THIO-URÉE,GUANIDINE ET CYANOGUANIDINE EN TANT QU'INHIBITEURS DE LA KINASE TRKA
申请人:ARRAY BIOPHARMA INC
公开号:WO2014078372A1
公开(公告)日:2014-05-22
Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R1, R2, Ra, Rb, Rc, Rd, X, Ring B, and Ring C are as defined herein, and wherein Ring B moiety and the NH-C(=X)-NH moiety are in the trans configuration, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.
化合物的公式I:或其立体异构体、互变异构体、药用可接受的盐、溶剂合物或前药,其中R1、R2、Ra、Rb、Rc、Rd、X、环B和环C的定义如本文所述,并且环B基团和NH-C(=X)-NH基团处于反式构型,是TrkA激酶的抑制剂,对可以用TrkA激酶抑制剂治疗的疾病具有用处,如疼痛、癌症、炎症/炎症性疾病、神经退行性疾病、某些传染病、干燥综合征、子宫内膜异位症、糖尿病周围神经病变、前列腺炎和盆腔疼痛综合征。