申请人:——
公开号:US20030153755A1
公开(公告)日:2003-08-14
Fused bicyclic amines of formula (1) are described wherein Ar is an aryl or heteroaryl group; Y is a —S(O
2
)— or —C(O)— group; R
1
is a hydrogen or halogen atom or an alkyl, haloalkyl, alkoxy, haloalkoxy or cyano group; X is a nitrogen atom or a C(R
1a
) group where R
1a
is as defined for R
1
and may be the same or different; W and Z are each a carbon atom and together with U form an optionally substituted five- or six-membered monocyclic aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the activity of Class I receptor tyrosine kinases and are of use in the prophylaxis and treatment of hyperproliferative disorders such as cancer, psoriasis, restenosis, atherosclerosis and fibrosis.
公式(1)中描述了Ar为芳基或杂芳基基团;Y为—S(O2)—或—C(O)—基团;R1为氢原子或卤素原子或烷基、卤代烷基、烷氧基、卤代烷氧基或氰基;X为氮原子或C(R1a)基团,其中R1a如R1所定义,可以相同也可以不同;W和Z各自为碳原子,并与U一起形成一个可选择取代的五元或六元单环芳香或杂芳基团;以及它们的盐、溶剂合物、水合物和N-氧化物。这些化合物能够抑制I类受体酪氨酸激酶的活性,并可用于预防和治疗癌症、银屑病、再狭窄、动脉粥样硬化和纤维化等过度增殖性疾病。