CGRP antagonists

摘要

Substituted 3-piperidin-1-yl-benzaldehyde compounds (I), and their tautomers, diastereomers, enantiomers, hydrates, mixtures, salts, or hydrates of the salts, preferably salts with inorganic or organic acids or bases, are new. Substituted 3-piperidin-1-yl-benzaldehyde compounds of formula (I), and their tautomers, diastereomers, enantiomers, hydrates, mixtures, salts, or hydrates of the salts, preferably salts with inorganic or organic acids or bases, are new. R 1>substituted piperidin-2-one moiety; R 2>e.g. H, F or -CN; R 3>e.g. a 5-membered heteroaryl; ring A : a six membered ring consisting of U 1>, V 1>, X and Y 1>; U 1>, V 1>, X : e.g. N,N-oxide; and Y 1>e.g. N. With conditions. Full Definitions are given in the DEFINITIONS (Full Definitions) Field. An independent claim is included for preparing a medicament comprising mixing (I) with an inert carrier material and/or diluent by a non-chemical way. [Image] ACTIVITY : Analgesic; Antimigraine; Antidiabetic; Cardiovascular-Gen.; Antidiarrheic; Dermatological; Vulnerary; Antiinflammatory; Antiarthritic; Respiratory-Gen.; Neuroprotective; Antiallergic; Antiasthmatic; Antibacterial; Immunosuppressive; Gynecological; Endocrine-Gen.; Antilichen; Antipruritic; Osteopathic; Antirheumatic; Muscular-Gen.; Gastrointestinal-Gen.; Vasotropic; Cytostatic. MECHANISM OF ACTION : Calcitonin gene-related peptide antagonist. The ability of (I) to antagonist calcitonin gene-related peptide was tested using SK-N-MC cell. The results showed that 1-{1-[6-(6-fluoro-1-methyl-1H-indol-3-carbonyl)-pyrimidin-4-yl]-piperidin-4-yl}-1,3-dihydro-imidazo[4,5-b]pyridin-2-one exhibited an inhibitory constant value of 4 nM.