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.
COMPOUNDS FOR THE TREATMENT AND PREVENTION OF INFLUENZA
申请人:Chen Li
公开号:US20110195979A1
公开(公告)日:2011-08-11
A compound of formula (I)
as well as pharmaceutically acceptable salt thereof, wherein R
1
to R
4
and Ar are as defined in description and in claims, can be used as a medicament.
化合物的化学式(I)及其药用盐,其中R1至R4和Ar如描述和权利要求中所定义,可用作药物。
[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.
[EN] COMPOUNDS FOR THE TREATMENT AND PREVENTION OF INFLUENZA<br/>[FR] COMPOSÉS POUR LE TRAITEMENT ET LA PRÉVENTION DE LA GRIPPE
申请人:HOFFMANN LA ROCHE
公开号:WO2011095576A1
公开(公告)日:2011-08-11
A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 and Ar are as defined in description and in claims, can be used as a medicament.
式(I)的化合物及其药学上可接受的盐,其中R1至R4和Ar如描述和索赔中定义的,可用作药物。
METHOD OF TREATMENT USING NOVEL ANTAGONISTS OR INVERSE AGONISTS AT OPIOID RECEPTORS
申请人:IGNAR DIANE MICHELE
公开号:US20100113512A1
公开(公告)日:2010-05-06
A method of treatment using pharmaceutical compositions containing novel antagonists or inverse agonists at opioid receptors for the treatment of binge eating disorder, anorexia nervosa, bulimia nervosa, excess drug or alcohol use, or eating disorder not otherwise specified.
NOVEL COMPOUNDS AS ANTAGONISTS OR INVERSE AGONISTS AT OPIOID RECEPTORS
申请人:Cowan David John
公开号:US20110124559A1
公开(公告)日:2011-05-26
Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.