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    AMINOPHOSPHINIC DERIVATIVES THAT CAN BE USED IN THE TREATMENT OF PAIN
    5.
    发明申请
    AMINOPHOSPHINIC DERIVATIVES THAT CAN BE USED IN THE TREATMENT OF PAIN 有权
    可用于治疗疼痛的氨基磷酸衍生物

    公开(公告)号：US20110124601A1

    公开(公告)日：2011-05-26

    申请号：US13055096

    申请日：2009-07-22

    申请人： Bernard Roques ,  Hervé Poras ,  Marie-Claude Fournie-Zaluski

    发明人： Bernard Roques ,  Hervé Poras ,  Marie-Claude Fournie-Zaluski

    IPC分类号： A61K31/662 ,  C07F9/30 ,  C07F9/32 ,  C07F9/6553 ,  A61K31/67 ,  C07F9/59 ,  A61K31/675 ,  A61P29/00 ,  A61P25/04

    CPC分类号： C07F9/306 ,  A61K31/662 ,  A61K31/67 ,  A61K31/675 ,  A61K39/08 ,  A61K45/06 ,  C07F9/301 ,  C07F9/303 ,  C07F9/3211 ,  C07F9/3241 ,  C07F9/4816 ,  C07F9/59 ,  C07F9/655345

    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)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.

    摘要翻译： 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。

    Aminophosphinic derivatives that can be used in the treatment of pain
    6.
    发明授权
    Aminophosphinic derivatives that can be used in the treatment of pain 有权
    可用于治疗疼痛的氨基亚磷酸衍生物

    公开(公告)号：US08703747B2

    公开(公告)日：2014-04-22

    申请号：US13055096

    申请日：2009-07-22

    申请人： Bernard Roques ,  Hervé Poras ,  Marie-Claude Fournie-Zaluski

    发明人： Bernard Roques ,  Hervé Poras ,  Marie-Claude Fournie-Zaluski

    IPC分类号： A61K31/66 ,  A01N57/00 ,  A01N57/18

    CPC分类号： C07F9/306 ,  A61K31/662 ,  A61K31/67 ,  A61K31/675 ,  A61K39/08 ,  A61K45/06 ,  C07F9/301 ,  C07F9/303 ,  C07F9/3211 ,  C07F9/3241 ,  C07F9/4816 ,  C07F9/59 ,  C07F9/655345

    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)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.

    摘要翻译： 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。

    Aminoacid derivatives containing a disulfanyl group in the form of mixed disulfanyl and aminopeptidase N inhibitors
    7.
    发明授权
    Aminoacid derivatives containing a disulfanyl group in the form of mixed disulfanyl and aminopeptidase N inhibitors 有权
    含有以二硫烷基和氨基肽酶N抑制剂形式的二硫烷基的氨基酸衍生物

    公开(公告)号：US08247608B2

    公开(公告)日：2012-08-21

    申请号：US12084091

    申请日：2006-10-24

    申请人： Bernard Roques ,  Marie-Claude Fournie-Zaluski

    发明人： Bernard Roques ,  Marie-Claude Fournie-Zaluski

    IPC分类号： C07C321/00 ,  C07C323/00 ,  C07C381/00 ,  C07C211/00 ,  A61K31/38

    CPC分类号： C07C323/60 ,  C07D333/24

    摘要： The invention relates to novel compounds of formula (I): H2N—CH(R1)—CH2—S—S—CH2—CH(R2)—CONH—R5, wherein R1 is a hydrocarbon chain, phenyl or benzyl radical, methylene radical substituted by a 5 or 6 atom heterocycle; R2 is a phenyl or benzyl radical, a 5 or 6 atom aromatic heterocycle, methylene group substituted by a 5 or 6 atom heterocycle; R5 is a CH(R3)—COOR4 radical, wherein R3 is hydrogen, an OH or OR group, a saturated hydrocarbon group, a phenyl or benzyl radical and OR4 is hydrophile ester, or 5 or 6 membered heterocycle comprising several heteroatoms selected from a group consisting of nitrogen, sulphur and oxygen, with at least two nitrogene atoms, wherein said heterocycle is substitutable by an alkyl C1-C6, phenyl or benzyl radical. The use of the inventive compounds in the form of drugs, a pharmaceutical composition comprising said compounds, a pharmaceutically acceptable excipient, the use in conjunction of at least one type of cannabinoid derivative for potentiating the analgesic and antidepressant effect of the novel compounds of formula (I) and/or morphine or the derivatives thereof are also disclosed.

    摘要翻译： 本发明涉及新的式（I）化合物：H 2 N-CH（R 1）-CH 2 -S-S-CH 2 -CH（R 2）-CONH-R 5，其中R 1是烃链，苯基或苄基，亚甲基 被5或6个原子杂环取代; R2是苯基或苄基，5或6个芳族杂环，被5或6个杂原子取代的亚甲基; R 5是CH（R 3）-COOR 4基团，其中R 3是氢，OH或OR基团，饱和烃基，苯基或苄基，OR 4是亲水酯，或包含若干个杂原子的5或6元杂环， 由氮，硫和氧组成的组，具有至少两个氮原子，其中所述杂环可被C 1 -C 6烷基，苯基或苄基取代。 药物形式的本发明化合物的使用，包含所述化合物的药物组合物，药学上可接受的赋形剂，联合至少一种类型的大麻素衍生物的用途，用于增强新型式（III）化合物的镇痛作用和抗抑郁作用 I）和/或吗啡或其衍生物也被公开。

    Amino acid derivatives, method for preparing same, and therapeutic use thereof
    8.
    发明授权
    Amino acid derivatives, method for preparing same, and therapeutic use thereof 有权
    氨基酸衍生物，其制备方法及其治疗用途

    公开(公告)号：US08466309B2

    公开(公告)日：2013-06-18

    申请号：US12991999

    申请日：2009-05-13

    申请人： Marie-Claude Fournie-Zaluski ,  Hervé Poras ,  Bernard Roques

    发明人： Marie-Claude Fournie-Zaluski ,  Hervé Poras ,  Bernard Roques

    IPC分类号： C07C69/74 ,  C07C321/00 ,  C07C323/00 ,  C07C381/00 ,  A01N43/16

    CPC分类号： C07C323/65 ,  C07C323/60

    摘要： The disclosure relates to novel compounds of the formula (I) R1NH—CH(R2)CH2—S—S—CH2—C(R3)(R4)—CONH—C(R5)(R6)—COOR7, in which R1 is a (acyloxy)alkyl carbamate-C(O)—O—C(R8)(R9)—OC(O)—R10 group; R2 is a hydrocarbon chain, a methylene radical substituted by a heterocycle, R4 is a hydrogen atom and R3 is a phenyl or benzyl radical, a heteroaryl, a methylene group substituted by a heterocycle or R3 and R4 form together a saturated cycle; R5 and R6 are hydrogen, a hydrocarbon chain, a phenyl or benzyl radical or R5 and R6 form together a saturated cycle; R7 is hydrogen, a phenyl or benzyl radical, a group of the formula CR12(R13)C(O)OR14 or OCR12(R13)OC(O)R14 or OCR12(R13)OC(O)OR14. The disclosure also relates to the use of these compounds as a drug, and to a pharmaceutical composition containing said compounds and a pharmaceutically acceptable carrier. The disclosure further relates to the combined use of at least one cannabinoid derivative and/or morphine or one derivative thereof and/or Gaba derivatives for enhancing the analgesic and anti-depressive effect of the compounds of the formula (I).

    摘要翻译： 本发明涉及式（I）的新化合物：R1NH-CH（R2）CH2-SS-CH2-C（R3）（R4）-CONH-C（R5）（R6）-COOR7，其中R1是（ 酰氧基）烷基氨基甲酸酯-C（O）-OC（R 8）（R 9）-OC（O）-R 10基团; R2是烃链，被杂环取代的亚甲基，R4是氢原子，R3是苯基或苄基，杂芳基，被杂环取代的亚甲基或R3和R4一起形成饱和环; R5和R6是氢，烃链，苯基或苄基或R5和R6一起形成饱和循环; R 7是氢，苯基或苄基，式CR 12（R 13）C（O）OR 14或OCR 12（R 13）OC（O）R 14或OCR 12（R 13）OC（O）OR 14的基团。 本公开还涉及这些化合物作为药物的用途，以及含有所述化合物和药学上可接受的载体的药物组合物。 本公开还涉及至少一种大麻素衍生物和/或吗啡或其一种衍生物和/或Gaba衍生物用于增强式（I）化合物的止痛和抗抑郁作用的组合使用。

    Aminoacid Derivatives Containing a Disulfanyl Group in the form of Mixed Disulfanyl and Aminopeptidase N Inhibitors
    9.
    发明申请
    Aminoacid Derivatives Containing a Disulfanyl Group in the form of Mixed Disulfanyl and Aminopeptidase N Inhibitors 有权
    含二硫烷基和氨基肽酶N抑制剂形式的二硫烷基的氨基酸衍生物

    公开(公告)号：US20090131509A1

    公开(公告)日：2009-05-21

    申请号：US12084091

    申请日：2006-10-24

    申请人： Bernard Roques ,  Marie-Claude Fournie-Zaluski

    发明人： Bernard Roques ,  Marie-Claude Fournie-Zaluski

    IPC分类号： A61K31/381 ,  C07D333/24 ,  C07D409/02 ,  A61P25/24 ,  A61P25/00 ,  A61P29/00 ,  A61K31/215 ,  C07C69/66

    CPC分类号： C07C323/60 ,  C07D333/24

    摘要： The invention relates to novel compounds of formula (I): H2N—CH(R1)—CH2—S—S—CH2—CH(R2)—COONH—R5, wherein R1 is a hydrocarbon chain, phenyl or benzyl radical, methylene radical substituted by a 5 or 6 atom heterocycle; R2 is a phenyl or benzyl radical, a 5 or 6 atom aromatic heterocycle, methylene group substituted by a 5 or 6 atom heterocycle; R5 is a CH(R3)—COOR4 radical, wherein R3 is hydrogen, an OH or OR group, a saturated hydrocarbon group, a phenyl or benzyl radical and OR4 is hydrophile ester, or 5 or 6 membered heterocycle comprising several heteroatoms selected from a group consisting of nitrogen, sulphur and oxygen, with at least two nitrogene atoms, wherein said heterocycle is substitutable by an alkyl C1-C6, phenyl or benzyl radical. The use of the inventive compounds in the form of drugs, a pharmaceutical composition comprising said compounds, a pharmaceutically acceptable excipient, the use in conjunction of at least one type of cannabinoid derivative for potentiating the analgesic and antidepressant effect of the novel compounds of formula (I) and/or morphine or the derivatives thereof are also disclosed.

    摘要翻译： 本发明涉及新的式（I）化合物：H 2 N-CH（R 1）-CH 2 -S-CH 2 -CH（R 2）-COONH-R 5，其中R 1是烃链，苯基或苄基，被 5或6原子杂环; R2是苯基或苄基，5或6个芳族杂环，被5或6个原子杂环取代的亚甲基; R 5是CH（R 3）-COOR 4基团，其中R 3是氢，OH或OR基团，饱和烃基，苯基或苄基，OR 4是亲水酯，或包含若干个杂原子的5或6元杂环， 由氮，硫和氧组成的组，具有至少两个氮原子，其中所述杂环可被C 1 -C 6烷基，苯基或苄基取代。 药物形式的本发明化合物的使用，包含所述化合物的药物组合物，药学上可接受的赋形剂，联合至少一种类型的大麻素衍生物的用途，用于增强新型式（III）化合物的镇痛作用和抗抑郁作用 I）和/或吗啡或其衍生物也被公开。

    AMINOACID DERIVATIVES CONTAINING A DISULFANYL GROUP IN THE FORM OF MIXED DISULFANYL AND AMINOPEPTIDASE N INHIBITORS
    10.
    发明申请
    AMINOACID DERIVATIVES CONTAINING A DISULFANYL GROUP IN THE FORM OF MIXED DISULFANYL AND AMINOPEPTIDASE N INHIBITORS 有权
    含有不同组合的混合衍生物和氨基酸N抑制剂的氨基酸衍生物

    公开(公告)号：US20090012153A1

    公开(公告)日：2009-01-08

    申请号：US12146941

    申请日：2008-06-26

    申请人： Bernard Roques ,  Marie-Claude Fournie-Zaluski

    发明人： Bernard Roques ,  Marie-Claude Fournie-Zaluski

    IPC分类号： A61K31/16 ,  C07C233/01 ,  C07D333/22 ,  A61K31/381 ,  C07D309/00 ,  A61K31/35 ,  A61K31/195 ,  A61P25/00 ,  A61P25/24

    CPC分类号： C07D285/135 ,  C07C323/52 ,  C07D333/22

    摘要： The invention relates to novel compounds of formula (I): H2N—CH(R1)—CH2—S—S—CH2—CH(R2)—CONH—R5, wherein R1 is a hydrocarbon chain, phenyl or benzyl radical, methylene radical substituted by a 5 or 6 atom heterocycle; R2 is a phenyl or benzyl radical, a 5 or 6 atom aromatic heterocycle, methylene group substituted by a 5 or 6 atom heterocycle; R5 is a CH(R3)—COOR4 radical, wherein R3 is hydrogen, an OH or OR group, a saturated hydrocarbon group, a phenyl or benzyl radical and OR4 is hydrophile ester, or 5 or 6 membered heterocycle comprising several heteroatoms selected from a group consisting of nitrogen, sulphur and oxygen, with at least two nitrogene atoms, wherein said heterocycle is substitutable by an alkyl C1-C6, phenyl or benzyl radical. The use of the inventive compounds in the form of drugs, a pharmaceutical composition comprising said compounds, a pharmaceutically acceptable excipient, the use in conjunction of at least one type of cannabinoid derivative for potentiating the analgesic and antidepressant effect of the novel compounds of formula (I) and/or morphine or the derivatives thereof are also disclosed.

    摘要翻译： 本发明涉及新的式（I）化合物：H 2 N-CH（R 1）-CH 2 -S-CH 2 -CH（R 2）-CONH-R 5，其中R 1是烃链，苯基或苄基，被 5或6原子杂环; R2是苯基或苄基，5或6个芳族杂环，被5或6个杂原子取代的亚甲基; R 5是CH（R 3）-COOR 4基团，其中R 3是氢，OH或OR基团，饱和烃基，苯基或苄基，OR 4是亲水酯，或包含若干个杂原子的5或6元杂环， 由氮，硫和氧组成的组，具有至少两个氮原子，其中所述杂环可被C 1 -C 6烷基，苯基或苄基取代。 药物形式的本发明化合物的使用，包含所述化合物的药物组合物，药学上可接受的赋形剂，联合至少一种类型的大麻素衍生物的用途，用于增强新型式（III）化合物的镇痛作用和抗抑郁作用 I）和/或吗啡或其衍生物也被公开。