The design, synthesis and in vitro immunosuppressive evaluation of novel isobenzofuran derivatives
摘要:
The synthesis and biological evaluation of a series of novel isobenzofuran-based compounds are described. The compounds were evaluated for their immunosuppressive effects of T-cell proliferation and IMPDH type II inhibitor activity in vitro, as well as their structure-activity relationships were assessed. Several compounds demonstrated highly efficacious immunosuppressive properties, especially compounds 2d, 2e, 2h and 2j, which were superior to MPA, while compounds 2k, 2m, 2n, 4c and 5d exhibited an equipotent inhibitory activity compared to MPA. Generally, it was obviously demonstrated that alpha,beta-unsaturated amides proved more potent than the diamide and urea series. The present study provides a guide for further research on development of safe and effective immunosuppressive agents. (C) 2011 Elsevier Ltd. All rights reserved.
Compounds of the formula ##STR1## wherein X, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, A, B, D and E are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
The invention provides a compound which exhibits satisfactory peroral absorbability and excellent antagonistic activity against NK-1 receptor or NK-2 receptor. The compound is a benzylamine derivative represented by formula (1) or a salt thereof.
Biphenyl-substituted quinoline and naphthyridines derivatives as angiotensine II antagonists
申请人:E.R. SQUIBB & SONS, INC.
公开号:EP0556060A1
公开(公告)日:1993-08-18
Compounds of the formula
wherein X, R₁, R₂, R₃, R₄, R₅, R₆, A, B, D and E are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
式中的化合物
其中 X、R₁、R₂、R₃、R₄、R₅、R₆、A、B、D 和 E 如本文所定义。这些化合物可抑制血管紧张素 II 的作用,因此可用作降压药等。
BENZYLAMINE DERIVATIVE
申请人:ZERIA PHARMACEUTICAL CO., LTD.
公开号:EP1650189A1
公开(公告)日:2006-04-26
The invention provides a compound which exhibits satisfactory peroral absorbability and excellent antagonistic activity against NK-1 receptor or NK-2 receptor. The compound is a benzylamine derivative represented by formula (1) or a salt thereof.