发明名称 Compounds and pharmaceutical compositions that have powerful non-NMDA antagonist properties with reduced nephrotoxicity
摘要 Compounds of formula (I) wherein: R1 represents a halogen atom or a trifluoromethyl group, R2 represents a hydrogen atom or an alkyl or cycloalkyl group; R3 represents an alkyl, cycloalkyl, aryl, arylalkyl, alkoxy, aryloxy, arylalkoxy, hydroxy, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkylcarbonyl, arylcarbonyl, or arylalkylcarbonyl group or an NHR6 group (wherein R6 represents a hydrogen atom or an alkyl, cycloalkyl, aryl, alkylcarbonyl, arylcarbonyl, arylalkyl, arylalkylcarbonyl group), or R2 and R3 together form with the nitrogen atom carrying them a ring having 5 or 6 carbon atoms, in which one of the carbon atoms can be replaced by an oxygen, nitrogen or sulphur atom or by an SO or SO2 group or by an NRa group (wherein Ra represents a hydrogen atom or an alkyl, cycloalkyl, aryl, or arylalkyl group, R4 and R5, which may be identical or different, represent a hydrogen atom or an alkyl, cycloalkyl, aryl or arylalkyl group or a group with the formula R7-CH-O-CO-R8 (wherein R7 and R8, which may be identical or different, represent a hydrogen atom or an alkyl, cycloalkyl or aryl group). These compounds are found to be powerful non-NMDA (N-methyl-D aspartate) antagonists with reduced associated nephrotoxicity. They are used as therapeutic agents for the acute and chronic treatment of neurological and psychological disorders such as cerebrovascular accident, cerebral or spinal traumatism, epilepsy, chronic neurodegenerative diseases such as Alzheimer's disease, schizophrenia, lateral amyotrophic sclerosis and Huntington's chorea.
申请公布号 NZ510000(A) 申请公布日期 2001.12.21
申请号 NZ20010510000 申请日期 2001.02.16
申请人 ADIR ET COMPAGNIE 发明人 LESTAGE, PIERRE;CORDI, ALEX;DESOS, PATRICE
分类号 A61K31/675;A61P9/10;A61P25/00;A61P25/08;A61P25/14;A61P25/18;A61P25/28;C07B61/00;C07F9/38;C07F9/60;(IPC1-7):C07D215/227;C07D215/18;C07F9/40;C07F9/50 主分类号 A61K31/675
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