Substituted thiazoles and the use thereof as inhibitors of plasminogen activator inhibitor-1
申请人:3-Dimensional Pharmaceuticals, Inc.
公开号:US20010044545A1
公开(公告)日:2001-11-22
The present invention relates to the use of aminothiazole derivatives of Formula I of as inhibitors of PAI-1, and to novel classes of aminothiazole derivatives, their synthesis and their use as inhibitors of PAI-1. It has been discovered that compounds of Formula I:
1
or a solvate, hydrate or a pharmaceutically acceptable salt thereof, wherein
Y, Ar
1
, Ar
2
, R
1
, R
2
, Z, m and n are described in the specification, inhibit plasminogen activator inhibitor-1 (PAI-1). These compounds can be used in the prophylaxis or for the treatment of thrombosis, angina pectoris, cerebral infarction, myocardial infarction, pulmonary infarction, intra-atrial thrombus in atrial fibrillation, deep venous thrombus, disseminated intravascular coagulation syndrome, diabetic complications, restenosis and stroke.
本发明涉及使用公式I的氨基噻唑衍生物作为PAI-1的抑制剂,以及新型氨基噻唑衍生物类、它们的合成和作为PAI-1抑制剂的应用。发现公式I的化合物:1或其溶剂化物、水合物或药学上可接受的盐,其中Y、Ar1、Ar2、R1、R2、Z、m和n在说明书中有所描述,能够抑制纤溶酶原激活抑制剂-1(PAI-1)。这些化合物可用于预防或治疗血栓形成、心绞痛、脑梗死、心肌梗死、肺梗死、房颤中的心房内血栓、深静脉血栓、弥散性血管内凝血综合征、糖尿病并发症、再狭窄和中风。