会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 3. 发明申请
    • AMINOPHOSPHINIC DERIVATIVES THAT CAN BE USED IN THE TREATMENT OF PAIN
    • 可用于治疗疼痛的氨基磷酸衍生物
    • US20110124601A1
    • 2011-05-26
    • US13055096
    • 2009-07-22
    • Bernard RoquesHervé PorasMarie-Claude Fournie-Zaluski
    • Bernard RoquesHervé PorasMarie-Claude Fournie-Zaluski
    • A61K31/662C07F9/30C07F9/32C07F9/6553A61K31/67C07F9/59A61K31/675A61P29/00A61P25/04
    • 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。
    • 4. 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。
    • 5. 发明授权
    • Aminoacid derivatives containing a disulfanyl group in the form of mixed disulfanyl and aminopeptidase N inhibitors
    • 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
    • US08247608B2
    • 2012-08-21
    • US12084091
    • 2006-10-24
    • Bernard RoquesMarie-Claude Fournie-Zaluski
    • Bernard RoquesMarie-Claude Fournie-Zaluski
    • C07C321/00C07C323/00C07C381/00C07C211/00A61K31/38
    • C07C323/60C07D333/24
    • 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.
    • 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。
    • 6. 发明授权
    • (&agr;-aminophosphino) peptide derivatives, method for making same and therapeutic applications thereof
    • (α-氨基膦基)肽衍生物,其制备方法和治疗应用
    • US06518260B1
    • 2003-02-11
    • US09284882
    • 1999-04-22
    • Marie-Claude Fournie-ZaluskiHuixiong ChenBernard Pierre Roques
    • Marie-Claude Fournie-ZaluskiHuixiong ChenBernard Pierre Roques
    • A61K3166
    • C07F9/301C07F9/3211
    • The invention concerns compounds derived from (&agr;-aminophosphino) peptides, of general formula (I), in which R1 and R2 each represents a hydrogen atom or taken together form an imine with the adjacent nitrogen atom; R3 represents an alkyl group, an alkenyl group, a phenyl group, a benzyl group, all these groups capable of being substituted or not, a hydrogen atom, a cycloalkyl group, a cycloalkylmethyl group or finally, a methyl group substituted by a heterocyclic, aromatic or saturated group; R4 represents a phenyl group, a benzyl group, these groups capable of being substituted or not, a hydrogen atom, an alkyl group, analkenyl group or a cycloalkyl group; R5 represents an alkyl group, an alkenyl group, a phenyl group, a benzyl group, all these groups capable of being substituted or not, a hydrogen atom, a cycloalkyl, cycloalkylmethyl group or finally a methyl group substituted by a heterocyclic, aromatic or saturated group; R6, R7 and R8 can in particular represent a hydrogen atom, an alkyl group, a phenyl group substituted or not . . . n is equal to 0 or 1, in the form of enantiomers, diastereoisomers or racemic mixtures, their salts, their method of preparation and their therapeutic applications.
    • 本发明涉及衍生自通式(I)的(α-氨基膦基)肽的化合物,其中R 1和R 2各自代表氢原子或与其相邻的氮原子一起形成亚胺; R3表示烷基,烯基,苯基,苄基,所有这些能够被取代的基团,氢原子,环烷基,环烷基甲基或最后被杂环取代的甲基, 芳族或饱和基团; R4表示苯基,苄基,这些能够被取代的基团,氢原子,烷基,断链基或环烷基; R5表示烷基,烯基,苯基,苄基,所有这些能够被取代的基团,氢原子,环烷基,环烷基甲基或最后被杂环,芳族或饱和的取代的甲基 组; R6,R7和R8可以特别表示氢原子,烷基,被取代的苯基。 。 。 n等于0或1,以对映异构体,非对映异构体或外消旋混合物,其盐,其制备方法及其治疗应用的形式。
    • 8. 发明授权
    • Amino acid derivatives, method for preparing same, and therapeutic use thereof
    • 氨基酸衍生物,其制备方法及其治疗用途
    • US08466309B2
    • 2013-06-18
    • US12991999
    • 2009-05-13
    • Marie-Claude Fournie-ZaluskiHervé PorasBernard Roques
    • Marie-Claude Fournie-ZaluskiHervé PorasBernard Roques
    • C07C69/74C07C321/00C07C323/00C07C381/00A01N43/16
    • C07C323/65C07C323/60
    • 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).
    • 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。
    • 9. 发明申请
    • Aminoacid Derivatives Containing a Disulfanyl Group in the form of Mixed Disulfanyl and Aminopeptidase N Inhibitors
    • 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
    • US20090131509A1
    • 2009-05-21
    • US12084091
    • 2006-10-24
    • Bernard RoquesMarie-Claude Fournie-Zaluski
    • Bernard RoquesMarie-Claude Fournie-Zaluski
    • A61K31/381C07D333/24C07D409/02A61P25/24A61P25/00A61P29/00A61K31/215C07C69/66
    • C07C323/60C07D333/24
    • 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.
    • 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。
    • 10. 发明申请
    • AMINOACID DERIVATIVES CONTAINING A DISULFANYL GROUP IN THE FORM OF MIXED DISULFANYL AND AMINOPEPTIDASE N INHIBITORS
    • 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
    • US20090012153A1
    • 2009-01-08
    • US12146941
    • 2008-06-26
    • Bernard RoquesMarie-Claude Fournie-Zaluski
    • Bernard RoquesMarie-Claude Fournie-Zaluski
    • A61K31/16C07C233/01C07D333/22A61K31/381C07D309/00A61K31/35A61K31/195A61P25/00A61P25/24
    • C07D285/135C07C323/52C07D333/22
    • 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.
    • 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。