Substituted indoles

Details Substituted indoles Substituted indoles

C - Chemistry, Metallurgy

07

D

C07D 401/06 (2006.01) A61K 31/404 (2006.01) A61P 43/00 (2006.01) C07D 209/42 (2006.01) C07D 221/00 (2006.01) C07D 235/00 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 417/12 (2006.01) C07D 417/14 (2006.01) C07D 471/04 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2482655

The invention relates to a compound of formula Ia, (see formula Ia) or a pharmaceutically usable salt, solvate or stereoisomer or a mixture thereof in which R1, R12, R13, D-E, X1, X2, Y, Z, p and r are as defined therein. These substituted indoles and their physiologically safe derivatives and salts have particular effects on the central nervous system, above all, effects that inhibit 5HT-resumption and 5HTx-agonistic and/or antagonistic effects and, in particular, serotonin, agonistic and antagonistic properties, and can be used as antipsychotics, antidepressants, anxiolytics and/or antihypertensives. These compositions can also be used as excitatory amino acid antagonists for fighting neurodegenerative diseases including cerebrovascular diseases, epilepsy, schizophrenia, Alzheimer's disease, Parkinson's disease or Huntington's disease, cerebral ischemias, infarcts or psychoses.

L'invention concerne des indoles substitués de formule (I), ainsi que leurs dérivés et sels physiologiquement tolérables. Dans ladite formule, R?1¿, D, E, R?12¿, p, X?1¿, E, G, X?2¿ et Z ont la signification indiquée dans la revendication 1. Lesdits indoles substitués, leurs dérivés et sels agissent en particulier sur le système nerveux central. Ils présentent notamment un effet inhibiteur de la recapture de la 5HT et un effet agoniste et/ou antagoniste 5 HTx, et en particulier des propriétés agonistes et antagonistes de la sérotonine. Ils peuvent être utilisés comme antipsychotiques, neuroleptiques, antidépresseurs, anxiolytiques et/ou antihypertoniques. Ils peuvent en outre être utilisés comme antagonistes des acides aminés excitateurs pour lutter contre les maladies neurodégénératives, y compris les maladies cérébrovasculaires, l'épilepsie, la schizophrénie, la maladie d'Alzheimer, la maladie de Parkinson et la maladie de Huntington, les ischémies cérébrales, les infarctus ou les psychoses.

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