公开(公告)号：US5721231A

公开(公告)日：1998-02-24

申请号：US535913

申请日：1995-09-28

Applicant: Minoru Moriwaki ,  Hiroyuki Kitani ,  Syuji Ehara ,  Hirotsugu Komatsu ,  Mariko Amano

Inventor： Minoru Moriwaki ,  Hiroyuki Kitani ,  Syuji Ehara ,  Hirotsugu Komatsu ,  Mariko Amano

IPC: C07D495/14 ,  A61K31/55

CPC classification number: C07D495/14

Abstract: N-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno �3,2-f!�1,2,4!triazolo�4,3-a!�1,4!diazepin-6-yl )-N'- (2-methoxyphenyl)urea, optical isomers thereof and pharmaceutically acceptable salts thereof. The compounds of the present invention strongly and selectively inhibit the expression of VCAM-1 and have an inhibitory effect on leukocyte adhesion to vascular endothelial cells. Accordingly, the compounds of the present invention can be used as cell adhesion inhibitors for prophylaxis or treatment of various diseases in which cell adhesion is involved in the onset and progress thereof.

Abstract translation: N-（4-（4-氯苯基）-2,3,9-三甲基-6H-噻吩并〔3,2-f〕〔1,2,4〕三唑并〔4,3-a〕〔1,4〕二氮杂 -6-基）-N'-（2-甲氧基苯基）脲，其旋光异构体和其药学上可接受的盐。 本发明化合物强烈和选择性地抑制VCAM-1的表达，并且对白细胞对血管内皮细胞的粘附具有抑制作用。 因此，本发明的化合物可以用作细胞粘附抑制剂，用于预防或治疗其起因和进展中涉及细胞粘附的各种疾病。