5-membered heterocycle derivatives, their preparation and...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 233/54 (2006.01) A61K 31/395 (2006.01) A61K 31/417 (2006.01) A61K 31/421 (2006.01) A61K 31/426 (2006.01) A61K 31/454 (2006.01) A61K 31/496 (2006.01) A61P 25/00 (2006.01) C07D 261/04 (2006.01) C07D 263/32 (2006.01) C07D 277/24 (2006.01) C07D 277/28 (2006.01) C07D 403/04 (2006.01) C07D 403/06 (2006.01) C07D 405/06 (2006.01) C07D 409/06 (2006.01) C07D 413/06 (2006.01) C07D 417/04 (2006.01) C07D 417/06 (2006.01)

Patent

CA 2388505

The invention relates to compounds of general formula (I) which can be used for producing a medicament for inhibiting monoamine oxydases (MAO) and/or for lipidic peroxydation and/or for acting as modulators of sodium channels. The resulting medicament is particularly for use for treating Parkinson's disease, senile dementure, Alzheimer's disease, Huntington's chorea, amytrophic lateral sclerosis, schizophrenia, depression, psychosis, pain and epilepsy. The inventive compounds correspond to general formula (I), wherein Het is a 5-membered heterocycle comprising 2 heteroatoms and is such that general formula (I) corresponds exclusively to one of the following sub-formulae: (I)¿1?, (I)¿2?, (I)¿3? and (I)¿4?, wherein A represents especially a substituted phenyl or biphenyl radical, B represents especially H or an alkyl radical, X represents especially NH or S, Y represents O or S, n is a whole number from 0 to 6, R?1¿ and R?2¿ represent, independently of each other, especially radicals chosen from the following: a hydrogen atom or an alkyl or cycloalkyl radical; and .OMEGA. represents NR?46¿R?47¿ or OR?48¿, R?46¿ and R?47¿ representing especially radicals chosen from the following: an atom of hydrogen and an alkyl, cycloalkyl, alkynyl, cyanoalkyl alkoxycarbonyl, aralkoxycarbonyl or (cycloalkyl)oxycarbonyl radical and R?48¿ representing a hydrogen atom or an alkyl, alkynyl or cyanoylkynyl radical.

Les composés répondant à la formule générale (I) peuvent être utilisés pour préparer un médicament destiné à inhiber les monoamine oxydases (MAO) et/ou peroxydation lipidique et/ou à agir en tant que modulateurs des canaux sodiques. En particulier le médicament préparé sera destiné à traiter la maladie de Parkinson, les démences séniles, la maladie d'Alzheimer, la chorée de Huntington, la sclérose latérale amyotrophique, la schizophrénie, les dépressions, les psychoses, la douleur et l'épilepsie. Les composés de l'invention répondent à la formule générale (I) dans laquelle Het est un hétérocycle à 5 chaînons comportant 2 hétéroatomes et tel que la formule générale (I) corresponde exclusivement à l'une des sous-formules (I)1, (I)2, (I)3 et (I)4 dans lesquelles A représente notamment un radical phényle ou biphényle substitué, B représente notamment H ou un radical alkyle, X représente notamment NH ou S, Y représente O ou S, n est un entier de 0 à 6, R1 et R2 représentent indépendamment, notamment, des radicaux choisis parmi un atome d'hydrogène ou radical alkyle ou cycloalkyle, et .OMEGA. représente NR46R47 ou OR48, R46 et R47 représentant, notamment, des radicaux choisis parmi un atome d'hydrogène et un radical alkyle, cycloalkyle, alkynyle, cyanoalkyle alkoxycarbonyle, aralkoxycarbonyle ou (cycloalkyl)oxycarbonyle et R48 représentant un atome d'hydrogène ou un radical alkyle, alkynyle ou cyanoalkyle.

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