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    DERIVES D'AMINO-ACIDES CONTENANT UN GROUPEMENT DISULFANYLE COMME INHIBITEURS MIXTES DE LA NEPRILYSINE ET DE L 'AMINOPEPTIDASE N
    2.
    发明公开
    DERIVES D'AMINO-ACIDES CONTENANT UN GROUPEMENT DISULFANYLE COMME INHIBITEURS MIXTES DE LA NEPRILYSINE ET DE L 'AMINOPEPTIDASE N 有权
    EINE DISULFANYLGRUPPE ENTHALTENDE AMINOSAUREDERIVATE ALS GEMISCHTE INHIBITOREN VON NEPRILYSIN UND AMINOPEPTIDASE N

    公开(公告)号：EP1940818A1

    公开(公告)日：2008-07-09

    申请号：EP06807506.8

    申请日：2006-10-24

    申请人： Pharmaleads

    发明人： ROQUES, Bernard ,  FOURNIE-ZALUSKI, Marie-Claude

    IPC分类号： C07D333/24 ,  C07H3/02 ,  C07C323/65 ,  A61K31/381 ,  A61P29/00 ,  A61P25/00 ,  C07C323/60

    CPC分类号： C07D333/24 ,  C07C323/60 ,  C07C2601/14 ,  C07D285/12

    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： 本发明涉及式（I）的新化合物：H 2 N-CH（R 1） - CH 2 -SS-CH 其中R 1是烃链，苯基或（Ⅳ） 苄基，被5或6个原子杂环取代的亚甲基; R 2是苯基或苄基，5或6个原子的芳族杂环，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，或包含若干选自氮，硫和氧的杂原子的5或6元杂环，与 至少两个氮原子，其中所述杂环可被烷基C 1 -C 6烷基取代，苯基或苄基。 药物形式的本发明化合物的用途，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。

    NOUVEAUX DÉRIVÉS D'AMINO-ACIDES, LEUR PROCÉDÉ DE PRÉPARATION ET LEUR UTILISATION THÉRAPEUTIQUE
    5.
    发明公开
    NOUVEAUX DÉRIVÉS D'AMINO-ACIDES, LEUR PROCÉDÉ DE PRÉPARATION ET LEUR UTILISATION THÉRAPEUTIQUE 有权
    新的氨基酸衍生物，其制备方法及其食疗

    公开(公告)号：EP2297095A1

    公开(公告)日：2011-03-23

    申请号：EP09745768.3

    申请日：2009-05-13

    申请人： Pharmaleads

    发明人： FOURNIE-ZALUSKI, Marie-Claude ,  PORAS, Hervé ,  ROQUES, Bernard

    IPC分类号： C07C323/60 ,  C07C323/65

    CPC分类号： C07C323/65 ,  C07C323/60

    摘要： The invention relates to novel compounds of the formula (I) R
    1 NH-CH(R
    2 )-CH
    2 -S- S-CH
    2 -C(R
    3 )(R
    4 )-CONH-C(R
    5 )(R
    6 )-COOR
    7 , in which R
    1 is a (acyloxy)alkyl carbamate -C(O)-O-C(R
    8 )(R
    9 )-OC(O)-R
    10 group; R
    2 is a hydrocarbon chain, a methylene radical substituted by a heterocycle; R
    4 is a hydrogen atom and R
    3 is a phenyl or benzyl radical, a heteroaryl, a methylene group substituted by a heterocycle or R
    3 and R
    4 form together a saturated cycle; R
    5 and R
    6 are hydrogen, a hydrocarbon chain, a phenyl or benzyl radical or R
    5 and R
    6 form together a saturated cycle; R
    7 is hydrogen, a phenyl or benzyl radical, a group of the formula CR
    12 (R
    13 )C(O)OR
    14 or OCR
    12 (R
    13 )OC(O)R
    14 or OCR
    12 (R
    13 )OC(O)OR
    14 . The invention 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 invention 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 novel compounds of the formula (I).

    NOUVEAUX DÉRIVÉS D'AMINO-ACIDES, LEUR PROCÉDÉ DE PRÉPARATION ET LEUR UTILISATION THÉRAPEUTIQUE
    9.
    发明授权
    NOUVEAUX DÉRIVÉS D'AMINO-ACIDES, LEUR PROCÉDÉ DE PRÉPARATION ET LEUR UTILISATION THÉRAPEUTIQUE 有权
    新的氨基酸衍生物，其制备方法及其食疗

    公开(公告)号：EP2297095B1

    公开(公告)日：2012-04-25

    申请号：EP09745768.3

    申请日：2009-05-13

    申请人： Pharmaleads

    发明人： FOURNIE-ZALUSKI, Marie-Claude ,  PORAS, Hervé ,  ROQUES, Bernard

    IPC分类号： C07C323/60 ,  C07C323/65

    CPC分类号： C07C323/65 ,  C07C323/60

    摘要： The invention relates to novel compounds of the formula (I) R
    1 NH-CH(R
    2 )-CH
    2 -S- S-CH
    2 -C(R
    3 )(R
    4 )-CONH-C(R
    5 )(R
    6 )-COOR
    7 , in which R
    1 is a (acyloxy)alkyl carbamate -C(O)-O-C(R
    8 )(R
    9 )-OC(O)-R
    10 group; R
    2 is a hydrocarbon chain, a methylene radical substituted by a heterocycle; R
    4 is a hydrogen atom and R
    3 is a phenyl or benzyl radical, a heteroaryl, a methylene group substituted by a heterocycle or R
    3 and R
    4 form together a saturated cycle; R
    5 and R
    6 are hydrogen, a hydrocarbon chain, a phenyl or benzyl radical or R
    5 and R
    6 form together a saturated cycle; R
    7 is hydrogen, a phenyl or benzyl radical, a group of the formula CR
    12 (R
    13 )C(O)OR
    14 or OCR
    12 (R
    13 )OC(O)R
    14 or OCR
    12 (R
    13 )OC(O)OR
    14 . The invention 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 invention 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 novel compounds of the formula (I).

    SUBSTRATS PEPTIDIQUES RECONNUS PAR LA TOXINE BOTULIQUE DE TYPE A, BONT/A ET LEURS UTILISATIONS
    10.
    发明授权
    SUBSTRATS PEPTIDIQUES RECONNUS PAR LA TOXINE BOTULIQUE DE TYPE A, BONT/A ET LEURS UTILISATIONS 有权
    亚洲太平洋地区公司重新定位巴勒斯坦权力机构毒品犯罪的类型A，BONT / A和EL LEURS UTILISATIONS

    公开(公告)号：EP1743034B1

    公开(公告)日：2007-12-12

    申请号：EP05769759.1

    申请日：2005-05-04

    申请人： Pharmaleads

    发明人： FOURNIE-ZALUSKI, Marie-Claude ,  ROQUES, Bernard, Pierre

    IPC分类号： C12Q1/37

    CPC分类号： C07K14/705 ,  C07K5/0812 ,  C07K5/1016 ,  C12Q1/37 ,  G01N2333/96486

    摘要： The invention relates to a peptide substrate selectively recognisable by a botulinum toxin A, BoNT/A comprising a Nop-(Z)-Pya fragment in the peptide structure thereof, wherein Z is an aminoacid chain, preferably RA and said fragment is cleaved by the toxin. Said invention also relates to the substrate use, in particular for carrying out methods for detecting, identifying and/or dosing the botulinum toxin A at very low concentrations (of order of 20 pg) or the inhibitors and/or activators of the toxin metallopeptidase activity, thereby making it possible to quantify the power thereof.

    摘要翻译： 本发明涉及可由肉毒杆菌毒素A选择性识别的肽底物，在其肽结构中包含Nop-（Z）-Pya片段的BoNT / A，其中Z是氨基酸链，优选RA，并且所述片段被 毒素。 所述发明还涉及底物用途，特别是用于实施用于检测，鉴定和/或定量施用非常低浓度（20pg左右）的肉毒杆菌毒素A或毒素金属肽酶活性的抑制剂和/或活化剂的方法 从而可以量化其功率。