PHENANTHRIDINE DERIVATIVES AS BRADYKININ ANTAGONISTS
申请人:Beke Gyula
公开号:US20090270411A1
公开(公告)日:2009-10-29
The present invention relates to new phenanthridine derivatives of formula (I), wherein the variables are as defined in the specification, to processes for producing the same, to pharmacological compositions containing the same and to their use in therapy or prevention of painful and inflammatory processes.
The present invention relates to new sulfonamide derivatives of formula (I)
wherein
R
1
-R
5
and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
A new series of quinolinyl- and phenantridinyl-acetamides were synthesizer and evaluated against bradykinin B1 receptor. In vitro metabolic stability data were reported for the key compounds. The analgesic effect of compound 20 from the phenantridine series was proved in-vivo. (C) 2012 Elsevier Ltd. All rights reserved.
[EN] NEW PHENANTHRIDINE DERIVATIVES AS BRADYKININ ANTAGONISTS<br/>[FR] NOUVEAUX DERIVES DE PHENANTHRIDINE UTILISES COMME ANTAGONISTES DE LA BRADYKININE
申请人:RICHTER GEDEON VEGYESZET
公开号:WO2007072092A3
公开(公告)日:2007-11-01
NEW PHENANTHRIDINE DERIVATIVES AS BRADYKININ ANTAGONISTS