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Aminophosphinic derivatives that can be used in the treatment of pain
专利权人:
PHARMALEADS
发明人:
申请号:
IL21076011
公开号:
IL210760A
申请日:
2011.01.20
申请国别(地区):
IL
年份:
2014
代理人:
摘要:
The present invention relates to a compound of the following general formula (I): R1-NH-CH(R2)-P(=O)(OR3)-CH2-C(R4)(R5)-CONH-CH(R6)-COOR7 (I) or a pharmaceutically acceptable salt of the latter, an isomer or a mixture of isomers in any proportions, especially a mixture of enantiomers, and in particular a racemic mixture, for which R1 represents a ‑C(=O)‑O‑C(R8)(R9)‑OC(=O)‑R10 group R2 represents an optionally substituted hydrocarbon-based chain, an aryl or heteroaryl group or a methylene group substituted by a heterocycle R3 represents a hydrogen atom or a ‑C(R12)(R13)‑OC(=O)‑R14 group R4 and R5 form, together with the carbon that bears them, a saturated hydrocarbon-based ring or an optionally substituted piperidine ring or R4 represents a hydrogen atom and R5 represents a phenyl or a benzyl that is optionally substituted, a heteroaromatic ring or a methylene group substituted by a heterocycle R6 represents an optionally substituted hydrocarbon-based chain or a phenyl or a benzyl that is optionally substituted and R7 represents a hydrogen atom or a benzyl, alkyl, heteroaryl, alkylheteroaryl, –CHMe-COOR18, ‑CHR19-OC(=O)R20 and -CHR19-OC(=O)OR20 group. The present invention also relates to the use of these compounds as a medicinal product, and in particular for the treatment of pain, more advantageously neuropathic and neuroinflammatory pain, to their method of synthesis and also to the compositions containing them.La présente invention concerne un composé de formule générale (I) suivante: R1 -NH-CH(R2)-P(=O)(OR3)-CH2-C(R4)(R5)-CONH-CH(R6)-COOR7 (I) ou un sel pharmaceutiquement acceptable de celui-ci, un isomère ou un mélange disomères en toutes proportions, notamment un mélange dénantiomères, et en particulier, un mélange racémique, pour laquelle R1 représente un groupement –C(=O)-O-C(R8)(R9)-OC(=O)-R10 R2 représente une chaîne hydrocarbonée éventuellement substituée, un groupe aryle ou hétéroaryle ou un groupe méthylène substitué par un hétérocycle R3 représente un
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