CGRP antagonists

摘要

Substituted 3-amino-benzaldehyde compounds (I), and their tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures, salts, or the hydrates of the salts, preferably salts with inorganic or organic acids or bases, are new. Substituted 3-amino-benzaldehyde compounds of formula (I), and their tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures, salts, or the hydrates of the salts, preferably salts with inorganic or organic acids or bases, are new. Either R 1>spiro[indane-2,3'-pyrrolidine]-2'-one group; and R 2>H or 1-3C-alkyl; or R 1>R 2>N : 2,8-diazaspiro[4.5]decane group or piperidine group; R 3>e.g. 5-membered heteroaryl group; 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 the preparation of a medicament comprising mixing (I) with one or more inert carrier 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; Vasotropic; Antibacterial; Immunosuppressive; Gynecological; Endocrine-Gen.; Antilichen; Antipruritic; Osteopathic; Antirheumatic; Muscular-Gen.; Gastrointestinal-Gen.; Cytostatic. MECHANISM OF ACTION : Calcitonin gene-related peptide antagonist. The ability of (I) to antagonise calcitonin gene-related peptide was tested using SK-N-MC cell. The results showed that 1-(6-(1-methyl-1H-indol-3-carbonyl)pyrimidin-4-yl)-1'H-spiro[piperidin-4,4'-quinazolin]-2'(3'H)-one exhibited an inhibitory constant value of 81 nM.