[EN] SUBSTITUTED BICYCLIC HETEROCYCLIC COMPOUNDS AS NADPH OXIDASE INHIBITORS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES BICYCLIQUES SUBSTITUÉS UTILISÉS EN TANT QU'INHIBITEURS DE NADPH OXYDASE
申请人:GLENMARK PHARMACEUTICALS SA
公开号:WO2018203298A1
公开(公告)日:2018-11-08
The present application relates to substituted fused heteroaryl and heterocyclic compounds, useful as nicotinamide adenine dinucleotide phosphate oxidase inhibitors (NADPH oxidase inhibitors), processes for their preparation, pharmaceutical compositions comprising the compounds, and the use of the compounds or the compositions in the treatment or prevention of various diseases, conditions and/or disorders mediated by NADPH oxidase. (Formula I)
Substituted 2H-[1]benzopyrano[4,3,2-cd]indazoles, 2H-[1]benzothiopyrano[4,3,2-cd]indazoles, and 2H-[1]benzoselenino[4,3,2-cd]indazoles have demonstrated pharmacological activity against a broad spectrum of Gram-positive and Gram-negative bacteria, yeasts, and fungi, as well as activity against the L1210 and P388 murine leukemia cells lines. Pharmaceutical compositions containing the compounds and methods of employing the compounds in methods of treating bacterial or fungal infections and of inhibiting the growth of neoplasms in mammals are also disclosed.
A series of 12-aminotetrahydroisoquinocarbazoles and relatedcompounds were synthesized using an intramolecular Diels-Alder reaction and screened for antiarrhythmic activity in chloroform-induced ventricular arrhythmias in mice. Several compounds showed more potent activity than disopyramide. There was some correlation between substituents on aromatic ring and angular position, and antiarrhythmic activity
[EN] PIPERIDINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF METABOLIC DISORDERS<br/>[FR] DÉRIVÉS DE PIPÉRIDINE ET LEUR UTILISATION POUR LE TRAITEMENT DE TROUBLES MÉTABOLIQUES
申请人:BOEHRINGER INGELHEIM INT
公开号:WO2012001107A1
公开(公告)日:2012-01-05
The invention relates to new piperidine derivatives of the formula (I) to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
The present invention relates to 2-substituted cephem compounds of Formula (I) having a quaternary ammonium group on the 3-side chain, preferably together with a cathechol group, or pharmaceutically acceptable salts thereof, which exhibit potent antimicrobial spectrum against a variety of bacteria including Gram negative bacteria and/or Gram positive bacteria, corresponding pharmaceutical compositions, methods of making, treatment methods for bacterial infections or uses thereof.