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    Peptides and therapeutic applications thereof
    4.
    发明授权
    Peptides and therapeutic applications thereof 失效
    肽及其治疗应用

    公开(公告)号：US4407794A

    公开(公告)日：1983-10-04

    申请号：US289383

    申请日：1981-08-03

    申请人： Bernard Roques ,  Jeanne-Marie Lecomte

    发明人： Bernard Roques ,  Jeanne-Marie Lecomte

    IPC分类号： C07K14/655 ,  A61K38/00 ,  A61P25/00 ,  C07K7/06 ,  C07K14/575 ,  C07K14/67 ,  C07K14/70 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K14/672 ,  C07K14/702 ,  A61K38/00 ,  Y10S514/809

    摘要： This invention relates to peptide derivatives of the formula:Tyr--A--Gly--B--C--D (I)in which:A is a D.Ala, AzaGly, Aib, D.Ser., D.Thr, D.Cys, homo Serine, .beta.Phe Ser, .beta.OH Leu, 4OH Ile, .alpha.,.beta.,.gamma. OHNor Val or OH Val residue in which the side-chain OH or SH groups, when same exist, may be free or protected (i) by a straight- or branched-chain alkyl containing 1-6 carbon atoms, (ii) by an unsubstituted phenyl radical or a phenyl radical substituted with one or more fluorine atoms, (iii) by an unsubstituted benzyl radical or a benzyl radical substituted with one or more fluorine atoms, (iv) by an aliphatic acyl radical having 1-6 carbon atoms or an acyl radical COX in which X is a phenyl, benzyl or benzhydryl radical, optionally substituted with one or more fluorine atoms,B is a L.Phe, pF.L.Phe or pentafluoro L.Phe residue,C is a Leu, N.Leu or Ile residue of D or L configuration,D is hydrogen or a group of the formula: ##STR1## in which n=0, 1 or 2, R is a hydrogen atom or a radical as defined for the protection of group OH of residue A,Y is a hydrogen atom, a group hydroxy, carboxy, carbamoyl, a group OR.sub.1, COOR.sub.1 or CONHR.sub.1 in which R.sub.1 represents a radical as defined for the protection of group OH of residue A, a phosphatidylethanolamine chain or a chain ##STR2## in which n is an integer from 0 to 3, R.sub.2 is a hydrogen atom or a straight alkyl radical containing 1-4 carbon atoms, and R.sub.3 is a hydrogen or oxygen atom or a straight alkyl residue containing 1-4 carbon atoms,and their pharmaceutically acceptable salts.Said compounds are therapeutically useful, typically an analgesic, psychotropic and anti-diarrheic agents.

    摘要翻译： 本发明涉及下式的肽衍生物：Tyr-A-Gly-BCD（I），其中：A为D.Ala，AzaGly，Aib，D.Ser。，D.Thr，D.Cys，高丝氨酸， βPhe Ser，βOH Leu，4OH Ile，α，β，γOHNor Val或OH Val残基，其中侧链OH或SH基团当存在时可以是游离的或受保护的（i）通过直链或 含有1-6个碳原子的支链烷基，（ii）未取代的苯基或被一个或多个氟原子取代的苯基，（iii）未取代的苄基或被一个或多个氟原子取代的苄基 ，（iv）具有1-6个碳原子的脂族酰基或酰基COX，其中X是苯基，苄基或二苯甲基，任选被一个或多个氟原子取代，B是L.Phe，pF。 L.Phe或五氟L.Phe残基，C是D或L构型的Leu，N.Leu或Ile残基，D是氢或下式的基团：其中n = 0,1或2， R是氢原子 如保护残基A的OH基团所定义的基团，Y是氢原子，羟基，羧基，氨基甲酰基，基团OR1，COOR1或CONHR1，其中R1表示为保护基团OH定义的基团 残基A，磷脂酰乙醇胺链或NH（CH2）nR3NR2R2 + RF，其中n为0-3的整数，R2为氢原子或含有1-4个碳原子的直链烷基，R3为氢或 氧原子或含有1-4个碳原子的直链烷基，及其药学上可接受的盐。 所述化合物是治疗上有用的，通常是镇痛药，精神药物和抗腹泻剂。

    Aminophosphinic derivatives that can be used in the treatment of pain
    5.
    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
    6.
    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。

    SAFETY AND CONTROL DEVICE FOR A DOMESTIC ELECTRICAL APPLIANCE
    7.
    发明申请
    SAFETY AND CONTROL DEVICE FOR A DOMESTIC ELECTRICAL APPLIANCE 审中-公开
    家用电器的安全和控制装置

    公开(公告)号：US20080230617A1

    公开(公告)日：2008-09-25

    申请号：US12052754

    申请日：2008-03-21

    申请人： Bernard Roques

    发明人： Bernard Roques

    IPC分类号： F24H9/20

    CPC分类号： H05K3/306 ,  H05K2201/10409 ,  H05K2203/167

    摘要： The safety and control device for a domestic electrical appliance according to the present invention comprises an electronic card (2) which comprises an insulating plate (4) comprising a printed circuit (15) supplying an electronic control system (5) for driving a domestic electrical appliance and an electromechanical safety device (3) connected to the printed circuit (15) and comprising an insulating body (8) joined to a capillary or to a safety bimetallic disk (9).

    摘要翻译： 根据本发明的用于家用电器的安全和控制装置包括电子卡（2），其包括绝缘板（4），所述绝缘板（4）包括印刷电路（15），所述印刷电路（15）提供用于驱动家用电器 连接到印刷电路（15）并且包括连接到毛细管或安全双金属盘（9）的绝缘体（8）的机电安全装置（3）。

    AMINOPHOSPHINIC DERIVATIVES THAT CAN BE USED IN THE TREATMENT OF PAIN
    8.
    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。

    Wall feedthrough
    9.
    发明授权
    Wall feedthrough 有权
    墙壁馈通

    公开(公告)号：US06617512B2

    公开(公告)日：2003-09-09

    申请号：US09987429

    申请日：2001-11-14

    申请人： Bernard Roques

    发明人： Bernard Roques

    IPC分类号： H02G318

    CPC分类号： H01B17/308

    摘要： The invention relates to a wall feedthrough, in particular for a metal wall and for a high-voltage coaxial cable, said feedthrough comprising an insulating socket which is affixed to the wall and which includes a central segment, an upstream end and a downstream end, said ends each projecting on its side from the wall. The insulating socket allows passing a cable inner conductor through it, and the feedthrough furthermore includes primary mechanical fasteners at the downstream socket end which cooperate with secondary mechanical fasteners affixed to the sheathed part of the cable. This feedthrough is characterized in that the cable's inner conductor is electrically insulated from the wall by pre-stressed electric insulators.

    摘要翻译： 本发明涉及壁馈通，特别是用于金属壁和用于高压同轴电缆的壁馈通，所述馈通包括固定在壁上并包括中心段，上游端和下游端的绝缘插座， 所述端部各自从其侧壁突出。绝缘插座允许电缆内部导体穿过其中，并且馈通还包括在下游插座端处的主要机械紧固件，其与固定到电缆的护套部分的次级机械紧固件配合 该馈通的特征在于，电缆的内导体通过预应力电绝缘体与壁电绝缘。

    Amino acid derivatives and their therapeutical applications
    10.
    发明授权
    Amino acid derivatives and their therapeutical applications 失效
    氨基酸衍生物及其治疗应用

    公开(公告)号：US5491169A

    公开(公告)日：1996-02-13

    申请号：US312117

    申请日：1994-09-26

    申请人： Bernard Roques ,  Marie C. Fournie-Zaluski

    发明人： Bernard Roques ,  Marie C. Fournie-Zaluski

    IPC分类号： C07D213/71 ,  A61K31/00 ,  A61K31/16 ,  A61P25/24 ,  C07C319/22 ,  C07C323/60 ,  C07C323/64 ,  C07C323/65 ,  C07D295/22 ,  C07D295/32 ,  C07C321/14

    CPC分类号： C07D295/32 ,  C07C323/60 ,  C07C323/65 ,  C07C2101/14

    摘要： Compounds having the properties of morphinic substances, particularly anasia, with beneficial effects on behaviour and with peripheral effects without their major drawbacks (tolerence, addiction), the blood-brain barrier and having the following formula :H.sub.2 N--CH(R.sub.1)--CH(R.sub.2)--S--S--CH(R.sub.3)--CH(R.sub.4)--A--B--Zwherein: AB preferably represents a CO amide bond, R.sub.2 et R.sub.3 preferably represent a hydrogen atom, R.sub.1 et R.sub.4 preferably represent, independently of each other, a benzyl grouping, --CH.sub.2 CH.sub.2 SCH.sub.3, --CH.sub.2 --CH.sub.2 --S(O)--CH.sub.3 or --CH.sub.2 --CH(CH.sub.3) .sub.2, Z may represent a --CH(R.sub.5)[CH(R.sub.6)].sub.n --COO(R.sub.7) grouping wherein: R.sub.5 may represent a hydrogen atom, a methyl grouping, a benzyl grouping or a phenyl grouping, R.sub.6 may represent a hydrogen atom and may also form a hydrocarbon cycle with R.sub.5, or Z may represent a heterocyclic grouping, and preferably a morpholinyl grouping. No drawings.

    摘要翻译： 具有吗啡物质特性的化合物，特别是镇痛，具有对行为和外周作用的有益作用而没有其主要缺点（过敏，成瘾），血脑屏障并具有以下分子式：H2N-CH（R1）-CH（ R 2）-SS-CH（R 3）-CH（R 4）-ABZ其中：AB优选表示CO酰胺键，R 2和R 3优选表示氢原子，R 1和R 4优选彼此独立地表示苄基， -CH 2 CH 2 SCH 3，-CH 2 -CH 2 -S（O）-CH 3或-CH 2 -CH（CH 3）2，Z可以表示-CH（R 5）[CH（R 6）] n -COOH（R7） 代表氢原子，甲基，苄基或苯基，R6可以表示氢原子，也可以与R5形成烃循环，或Z可以表示杂环基，优选吗啉基。 没有图纸