Heterodiazinon compound

Details Heterodiazinon compound Heterodiazinon compound

C - Chemistry, Metallurgy

07

D

C07D 413/04 (2006.01) A61K 31/5395 (2006.01) A61P 25/28 (2006.01) C07D 273/04 (2006.01)

Patent

CA 2362385

The present invention provides a novel compound having an excellent 2-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor antagonistic action, particularly a therapeutic, preventing and ameliorating action useful for cerebral ischemia, cerebrospinal injuries, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's chorea, epilepsy, pain, spastic paralysis, multiple sclerosis etc. That is, the present invention provides a heterodiazinon compound represented by the following formula (I), a pharmacologically acceptable salt thereof or hydrates thereof. (see formula I) Wherein A represents an oxygen atom, a sulfur atom or a group represented by the formula >NR3 (wherein R3 represents hydrogen atom or a lower alkyl group); R1 and R2 are the same as or different from each other and each represents an optionally substituted aryl group, an optionally substituted heteroaryl group, an optionally substituted aralkyl group, an optionally substituted heteroaryl alkyl group, an optionally substituted aryl alkenyl group, an optionally substituted heteroaryl alkenyl group, an optionally substituted piperidyl group, an optionally substituted piperazinyl group; a morpholinyl group, an optionally substituted lower cycloalkyl group, a tetrahydrofuranyl group, a tetrahydropyranyl group, an adamantyl group, an optionally substituted amino group or an optionally substituted amide group; and R4 and R5 are the same as or different from each other and each represents hydrogen atom, hydroxy, a halogen atom, nitrile group, nitro group, a lower alkyl group, an aryl group or a heteroaryl group, provided that the compounds represented by the following formula (II): (see formula II) (wherein R11 and R12 are the same as or different from each other and each represents hydrogen atom, fluorine, chlorine, bromine, iodine, a C1-C2 fluoroalkyl group, a C1-C2 chloroalkyl group, a C1-C2 bromoalkyl group, a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a C7-C9 aralkyl group, phenyl group, a C1-C6 alkoxy group, a C1-C6 alkylthio group, a C1-C6 alkylsulfinyl group, a C7-C9 aralkoxy group, phenoxy group, phenylthio group, phenylsulfonyl group, alkali metal carboxylate C2-C5 alkoxycarbonyl group or a group represented by the formula -N(R15)R16 (wherein R15 and R16 are the same as or different from each other and each represents hydrogen atom or a C1-C2 alkyl group); and R13 and R14 are the same as or different from each other and each represents a C1-4 alkylsulfonyl group, nitro group, a group represented by the formula -OCH n X3-n (wherein X represents fluorine, chlorine, bromine or iodine; and n is any of integers 1 to 3) or a group having the same meanings as the definitions of R11 and R12) are excluded.

L'invention concerne des dérivés d'hérétodiazinone représentés par la formule générale (1), des sels de ceux-ci, acceptables au plan pharmaceutique, ou des hydrates desdits dérivés et sels, présentant un antagonisme au récepteur de l'acide 2-amino-3-hydroxy-5-méthyl-4-isoxazolepropionique (AMPA). Dans ladite formule (1), A représente O, S ou NR<3> (R<3> représentant hydrogène ou alkyle inférieur); R<1> et R<2> représentent chacun séparément (hétéro)a ryle éventuellement substitué ou similaire; et R<4> et R<5> repr ésentent chacun séparément hydrogène, hydroxyle, halogéno, nitro, alkyle inférieur, (hétéro)aryle ou similaire.

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