公开(公告)号：WO9919306A3

公开(公告)日：1999-07-29

申请号：PCT/US9821327

申请日：1998-10-09

Applicant: UNIV TEXAS ,  UNIV CALIFORNIA ,  BUDDE RAYMOND J A ,  ELLMAN JONATHAN A ,  LEVIN VICTOR A ,  GALLICK GARY E ,  NEWMAN ROBERT A

Inventor： BUDDE RAYMOND J A ,  ELLMAN JONATHAN A ,  LEVIN VICTOR A ,  GALLICK GARY E ,  NEWMAN ROBERT A

IPC: A61P25/00 ,  C07D243/24 ,  A61K31/55

CPC classification number: C07D243/24

Abstract: Disclosed herein are small molecule, non-peptidyl inhibitors of protein tyrosine kinases, and methods for their use. The instant inhibitors are based on a 1,4-benzodiazepin-2-one nucleus. A compound represented by structural formula (I), where R1, R2 and R3 are independently described as Y bonded to W, where Y is a 0-6 atom straight or branched saturated or unsaturated chain group comprising C, N, O or S as shown in Table 1, and W is hydrogen or any three membered, four membered, five membered, six membered or fused bicyclic ring system comprising C, N, O or S as shown in Tables 4-9; X is separately and independently selected from Table 2; and salts of said compound. Methods are provided for inhibition of specific protein tyrosine kinases, for example pp60 . Methods are further provided for the use of these inhibitors in situations where the inhibition of a protein tyrosine kinase is indicated, for example, in the treatment of certain diseases in mammals, including humans.

Abstract translation: 本文公开了蛋白酪氨酸激酶的小分子非肽基抑制剂及其使用方法。 本发明抑制剂基于1,4-苯并二氮杂-2-酮核。 由结构式（I）表示的化合物，其中R 1，R 2和R 3独立地描述为与W键合的Y，其中Y是包含C，N，O或S的0-6原子直链或支链饱和或不饱和链基团，如 如表1所示，且W为氢或包含C，N，O或S的任何三元，四元，五元，六元或稠合双环体系，如表4-9所示; X分别独立地选自表2; 和所述化合物的盐。 提供了抑制特定蛋白酪氨酸激酶的方法，例如pp60 。 进一步提供了将这些抑制剂用于其中抑制蛋白酪氨酸激酶的情况，例如用于治疗哺乳动物（包括人）的某些疾病的方法。