| 摘要 |
<p>Substituted piperidine compounds (I) and their tautomers and salts are new. Substituted piperidine compounds of formula (I) and their tautomers and salts are new. R 1>substituted 3,4-dihydro-1H-quinazolin-2-one compound of formula (1a), substituted 1,3,4,5-tetrahydro-benzo[d][1,3]diazepin-2-one compound of formula (2a) or 5-phenyl-2,4-dihydro-[1,2,4]triazol-3-one compound of formula (3a); R 1> 1>H or H 3C-O-; R 2>substituted toluene compound of formula (4a); R 2> 1>HO, H 3CO, H-C(O)-O or H 3C-C(O)-O-; R 2> 2>1-2C alkyl or H 3CO-; R 3>R4a-2-8C alkylene-NH- or heterocyclic compounds of formulae (5a-6a); R4a : H, H 2N, 13C-alkyl-NH, (1-3C alkyl) 2-N or 1-6C alkyl-O-C(O)-NH-; R 3> 2>, R 3> 4>H or 1-3C alkyl; R 3> 3>free electron pair or oxygen atom; R4b : H, 1-6C alkyl, H 2N-2-6C alkylene, 1-3C alkyl-NH-2-6C alkylene, (1-3C alkyl) 2-N-1-6C-alkylene, 3-6C cycloalkyl-1-3C-alkylene, NH 2, 1-3C alkyl-NH or (1-3C alkyl) 2-N; R 4>7 cyclic compounds e.g. heterocyclic compounds of formulae (7a-10a); and R 4> 2>R 3> 2>. Provided that: when X is C, R 4> 1> is H, OH or 1-3C alkyl; when X is N, R 4> 1> is a free electron pair or an oxygen atom; if X is N, then Y 1> is O, S, S(O), S(O) 2; if X is C, then Y 1> is S, S(O), S(O) 2; and provided that R 3> and R 4> are not bound to one another simultaneously via an N atom. [Image] [Image] [Image] [Image] ACTIVITY : Analgesic; Antidiabetic; Antiarthritic; Osteopathic; Antirheumatic; Antiallergic; Antiinflammatory; Antiasthmatic; Gastrointestinal-Gen.; Vasotropic; Antibacterial; Immunosuppressive; Dermatological; Vulnerary; Antipruritic; Cardiovascular-Gen. MECHANISM OF ACTION : Calcitonin gene related peptide (CGRP) receptor-antagonist. The ability of (I) to antagonize CGRP receptor was tested in SK-N-MC cells. The result showed that the IC 5 0 value of (I) was >= 10000 nM.</p> |
