Nucleic Acid Related Compounds. 87. Nucleophilic Functionalization of Cytidine and 2'-Deoxycytidine Derivatives via Elaboration of the 4-Amino Group into a Readily Displaced 1,2,4-Triazol-4-yl Substituent
Structure-activity relationship studies indicated that the antibacterial potency was better when the 6,8-substituents were fluorine atoms and the 7-substituent was either 1-imidazolyl, 20, or 4-methyl-1-imidazolyl, 25. From the results of studies on pharmacokinetic profile and toxicity, 20 and 25 were found to possess excellent antibacterial activities and to show high blood levels after oral administration
[EN] SUBSTITUTED PIPERIDINES AS RENIN INHIBITORS<br/>[FR] PIPÉRIDINES SUBSTITUÉES EN TANT QU'INHIBITEURS DE LA RÉNINE
申请人:NOVARTIS AG
公开号:WO2009098275A1
公开(公告)日:2009-08-13
The present invention relates to compounds of the general formula (I) and the salts thereof, preferably the pharmaceutically acceptable salts thereof; in which R has the meaning explained in the description, a process for their preparation and the use of these compounds as medicines, especially as renin inhibitors.
[EN] BENZENE-FUSED 6-MEMBERED OXYGEN-CONTAINING HETEROCYCLIC DERIVATIVES OF BICYCLIC HETEROARYLS<br/>[FR] DÉRIVÉS HÉTÉROCYCLIQUES D'HÉTÉROARYLES BICYCLIQUES À 6 CYCLES BENZÉNIQUES ACCOLÉS DE BENZÈNE CONTENANT DE L'OXYGÈNE
申请人:NOVARTIS AG
公开号:WO2011064211A1
公开(公告)日:2011-06-03
The invention relates to new derivatives of formula I, wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a proliferative disease.
[EN] SUBSTITUTED PIPERIDINES AS RENIN INHIBITORS<br/>[FR] PIPÉRIDINES SUBSTITUÉES UTILISÉES COMME INHIBITEURS DE LA RÉNINE
申请人:NOVARTIS AG
公开号:WO2009098276A1
公开(公告)日:2009-08-13
The present invention relates to compounds of the general formula (I) and the salts thereof, preferably the pharmaceutically acceptable salts thereof; in which R has the meaning explained in the description, a process for their preparation and the use of these compounds as medicines, especially as renin inhibitors.
Pyrazolo-pyridine derivatives as ligands for GABA receptors
申请人:Merck Sharp & Dohme Ltd.
公开号:US06333336B1
公开(公告)日:2001-12-25
Pyrazolo[4,3-c]pyridin-3-one derivatives substituted at the 2-position by an optionally substituted aryl or heteroaryl moiety, and having pendant substituents at the 7-position and optionally also at the 6-position, are selective ligands for GABAA receptors, particularly having high affinity for the &agr;2 and/or &agr;3 subunit, and are useful in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.