Design and Synthesis of 4-Substituted Benzamides as Potent, Selective, and Orally Bioavailable IKs Blockers
摘要:
Multiple delayed rectifier potassium currents, including I-Ks are responsible for the repolarization and termination of the cardiac action potential, and blockers of these currents may be useful as antiarrhythmic agents. Modification of compound 5 produced 19(S) that is the most potent IF, blocker reported to date with > 5000-fold selectivity over other cardiac ion channels. Further modification produced 24A with 23% oral bioavailability.
[EN] PYRROLIDINE DERIVATIVES AND THEIR USE AS COMPLEMENT PATHWAY MODULATORS<br/>[FR] DÉRIVÉS PYRROLIDINE ET LEUR UTILISATION EN TANT QUE MODULATEURS DE LA VOIE DU COMPLÉMENT
申请人:NOVARTIS AG
公开号:WO2014002054A1
公开(公告)日:2014-01-03
The present invention provides a compound of formula (I) a method for manufacturing the compounds of the invention, and its therapeutic uses as complement pathway modulators for the treatment of ocular diseases. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
PYRROLIDINE DERIVATIVES AND THEIR USE AS COMPLEMENT PATHWAY MODULATORS
申请人:NOVARTIS AG
公开号:US20150190457A1
公开(公告)日:2015-07-09
The present invention provides a compound of formula (I) a method for manufacturing the compounds of the invention, and its therapeutic uses as complement pathway modulators for the treatment of ocular diseases. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
[EN] PYRAZOLO[3,4-B]PYRAZINE DERIVATIVES AS SHP2 PHOSPHATASE INHIBITORS<br/>[FR] DÉRIVÉS DE PYRAZOLO[3,4-B]PYRAZINE UTILISÉS EN TANT QU'INHIBITEURS DE LA PHOSPHATASE SHP2
申请人:RELAY THERAPEUTICS INC
公开号:WO2019067843A1
公开(公告)日:2019-04-04
Disclosed herein are novel compounds of formula (I) and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds ad compositions of the disclosure.