[EN] DIAZACARBAZOLES AND METHODS OF USE<br/>[FR] DIAZACARBAZOLES ET PROCÉDÉS D'UTILISATION
申请人:GENENTECH INC
公开号:WO2009151589A1
公开(公告)日:2009-12-17
The invention relates to 1,5-diazacarbazole compounds of Formula (I), (I-a), (I-b), (I-c), (I-d), (I-e), (I-f), (I-g) and (I-h) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chkl) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
本发明涉及式(I)、(I-a)、(I-b)、(I-c)、(I-d)、(I-e)、(I-f)、(I-g)和(I-h)的1,5-二氮杂咯化合物,其作为激酶抑制剂具有用途,更具体地作为检查点激酶1(chkl)抑制剂,因此作为癌症治疗剂具有用途。本发明还涉及包含这些化合物的组合物,更具体地是包含这些化合物的药物组合物以及使用这些化合物治疗各种癌症和高增殖性疾病的方法,以及使用这些化合物进行哺乳动物细胞的体内、体外和原位诊断或治疗,或相关的病理条件的方法。