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    2-naphthamide derivatives and their therapeutic applications
    62.
    发明授权
    2-naphthamide derivatives and their therapeutic applications 失效
    2-萘甲酰胺衍生物及其治疗应用

    公开(公告)号：US5985895A

    公开(公告)日：1999-11-16

    申请号：US105575

    申请日：1998-06-26

    申请人： Camille-Georges Wermuth ,  Andre Mann ,  Fabrice Garrido ,  Jeanne-Marie Lecomte ,  Jean-Charles Schwartz ,  Pierre Sokoloff

    发明人： Camille-Georges Wermuth ,  Andre Mann ,  Fabrice Garrido ,  Jeanne-Marie Lecomte ,  Jean-Charles Schwartz ,  Pierre Sokoloff

    IPC分类号： C07D295/12 ,  A61K31/445 ,  A61K31/451 ,  A61K31/495 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  A61P25/30 ,  A61P39/02 ,  A61P43/00 ,  C07D211/14 ,  C07D211/70 ,  C07D295/13 ,  C07D211/06 ,  C07D211/20

    CPC分类号： C07D295/13 ,  C07D211/14 ,  C07D211/70

    摘要： The invention relates to 2-naphthamide derivatives, in the form of bases or of salts, corresponding to the following general formula (I): ##STR1## in which: the Z-Y entity represents an N--CH.sub.2, C.dbd.CH or CH--CH.sub.2 group;R.sup.1 represents a hydrogen, fluorine, bromine or iodine atom or a hydroxyl, methoxy, nitrile or nitro group;R.sup.2 represents a hydrogen or bromine atom or a hydroxyl, methoxy, nitrile or nitro group;the R.sub.1 and R.sub.2 substituents both being situated on the same ring of the naphthamide unit or each being situated on one of the rings;R.sup.3 and R.sup.4 can be identical or different and each independently represent a hydrogen or chlorine atom or a methoxy or methyl group or an electron-withdrawing group.The invention also relates to their therapeutic applications as partial agonists of the dopamine D.sub.3 receptor.The invention applies more particularly to the treatment of neuropsychiatric conditions involving the dopamine D.sub.3 receptor, in particular psychotic and depressive states, to the treatment of drug-dependence states or to the treatment of disorders of a sexual nature.

    摘要翻译： 本发明涉及对应于以下通式（I）的碱或盐形式的2-萘甲酰胺衍生物：其中：Z-Y实体代表N-CH 2，C = CH或CH-CH 2基团; R1表示氢，氟，溴或碘原子或羟基，甲氧基，腈或硝基; R2表示氢或溴原子或羟基，甲氧基，腈或硝基; R1和R2取代基都位于萘甲酰胺单元的相同环上，或者各自位于其中一个环上; R3和R4可以相同或不同，并且各自独立地表示氢或氯原子或甲氧基或甲基或吸电子基团。 本发明还涉及其作为多巴胺D3受体的部分激动剂的治疗应用。 本发明更具体地涉及治疗涉及多巴胺D3受体，特别是精神病和抑郁状态的治疗药物依赖状态或治疗性性疾病的神经精神病学条件。

    Peptides and therapeutic applications thereof
    67.
    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。