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INDICAL DERIVATIVES, THEIR PREPARATION PROCESS AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
专利权人:
LES LABORATOIRES SERVIER
发明人:
PASCAL MARCHAND,VINCENT BABONNEAU,SYLVIE PIESSARD,MURIEL DUFLOS,JEAN-ALBERT BOUTIN,VALERIE AUDINOT,PHILIPPE DELAGRANGE,DANIEL-HENRI CAIGNARD
申请号:
BRPI0717528
公开号:
BRPI0717528A2
申请日:
2007.10.17
申请国别(地区):
BR
年份:
2013
代理人:
摘要:
Indole derivatives (I), their enantiomers, diastereomers and their acid/base addition salts are new. Indole derivatives of formula (I), their enantiomers, diastereomers and their acid/base addition salts are new. R 11-6C alkyl, 3-8C cycloalkyl or 3-8C cycloalkyl-1-6C alkyl, preferably alkyl; NR 2R 35-8 membered heterocycle, preferably piperidinyl; and n : 2-6, preferably 2. An independent claim is included for the preparation of (I). [Image] ACTIVITY : Hypnotic; Tranquilizer; Antidepressant; Cardiovascular-Gen; Gastrointestinal-Gen; Neuroleptic; Anorectic; Anticonvulsant; Antidiabetic; Antiparkinsonian; Nootropic; Antimigraine; Neuroprotective; Endocrine-Gen; Contraceptive; Immunomodulator; Cytostatic. MECHANISM OF ACTION : Melatonin receptor binder. The affinity of (I) to bind with melatonin receptors MT1 and MT2 was tested using 2-[ 1>; 2>; 5>;I]-iodomelatonin as reference radioligand. The results showed that (I) exhibited an inhibition constant value of less than 1 mu M.
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