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    • 80. 发明授权
    • Aminophosphinic derivatives that can be used in the treatment of pain
    • 可用于治疗疼痛的氨基亚磷酸衍生物
    • US08703747B2
    • 2014-04-22
    • US13055096
    • 2009-07-22
    • Bernard RoquesHervé PorasMarie-Claude Fournie-Zaluski
    • Bernard RoquesHervé PorasMarie-Claude Fournie-Zaluski
    • A61K31/66A01N57/00A01N57/18
    • C07F9/306A61K31/662A61K31/67A61K31/675A61K39/08A61K45/06C07F9/301C07F9/303C07F9/3211C07F9/3241C07F9/4816C07F9/59C07F9/655345
    • 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)OR20 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.
    • 本发明涉及以下通式(I)的化合物:R1-NH-CH(R2)-P(= O)(OR3)-CH2-C(R4)(R5)-CONH-CH(R6) -COOR7(I)或其后者的药学上可接受的盐,任何比例的异构体或异构体混合物,特别是对映异构体的混合物,特别是外消旋混合物,其中R1表示-C(= O) - O-C(R 8)(R 9)-OC(= O)-R 10基; R2表示任选取代的烃基链,芳基或杂芳基或被杂环取代的亚甲基; R3表示氢原子或-C(R12)(R13)-OC(= O)-R14基团; R4和R5与带有它们的碳一起形成饱和烃基环或任选取代的哌啶环,或R4表示氢原子,R 5表示任选取代的苯基或苄基,杂芳环或亚甲基 被杂环取代的基团; R6表示任选取代的烃基链或任选取代的苯基或苄基; 并且R 7表示氢原子或苄基,烷基,杂芳基,烷基杂芳基,-CHMe-COOR 18,-CHR 19 -OC(= O)OR 20和-CHR 19 -OC(= O)OR 20基团。 本发明还涉及这些化合物作为药用产品的用途,特别是用于治疗其合成方法的疼痛,更有利的是神经性和神经炎性疼痛,以及含有它们的组合物。