SUBSTITUTED 5,6,7,8-TETRAHYDROQUINOLINE DERIVATIVES, COMPOSITIONS, AND METHODS OF USE THEREOF
申请人:Barbay Joseph Kent
公开号:US20090048295A1
公开(公告)日:2009-02-19
Substituted 5,6,7,8-tetrahydroquinoline derivatives, which are C5
a
receptor modulators, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, immune and inflammatory diseases and conditions, are disclosed.
[EN] SUBSTITUTED 5,6,7,8-TETRAHYDROQUINOLINE DERIVATIVES, COMPOSITIONS, AND METHODS OF USE THEREOF<br/>[FR] DÉRIVÉS DE 5,6,7,8-TÉTRAHYDROQUINOLÉINES SUBSTITUÉES, COMPOSITIONS ET PROCÉDÉS D'UTILISATION DE CEUX-CI
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2009023669A1
公开(公告)日:2009-02-19
Substituted 5,6,7,8-tetrahydroquinoline derivatives, which are C5a receptor modulators, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, immune and inflammatory diseases and conditions, are disclosed.
Synthesis and characterization of 5,6,7,8-tetrahydroquinoline C5a receptor antagonists
作者:J. Kent Barbay、Yong Gong、Mieke Buntinx、Jian Li、Concha Claes、Pamela J. Hornby、Guy Van Lommen、Jean Van Wauwe、Wei He
DOI:10.1016/j.bmcl.2008.03.049
日期:2008.4
A novel series of substituted 2-aryl-5-amino-5,6,7,8-tetrahydroquinoline C5a receptor antagonists is reported. Synthetic routes were developed that allow the substituents on the tetrahydroquinoline core to be efficiently varied, facilitating determination of structure-activity relationships. Members of the series display high binding affinity for the C5a receptor and are potent functional antagonists. (c) 2008 Elsevier Ltd. All rights reserved.