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    Benzimidazole derivatives and pharmaceutical compositions containing them
    1.
    发明授权
    Benzimidazole derivatives and pharmaceutical compositions containing them 失效
    苯并咪唑衍生物和含有它们的药物组合物

    公开(公告)号：US4820710A

    公开(公告)日：1989-04-11

    申请号：US906279

    申请日：1986-09-10

    申请人： Philippe Manoury ,  Jean Binet ,  Gerard Defosse

    发明人： Philippe Manoury ,  Jean Binet ,  Gerard Defosse

    IPC分类号： A61K31/415 ,  A61K31/44 ,  A61K31/505 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  C07D239/04

    CPC分类号： C07D401/14

    摘要： Benzimidazole derivatives corresponding to the formula (1) ##STR1## in which X is CH or N,R.sub.1 is either a hydrogen atom, or a benzyl radical which can bear 1 to 3 substituents chosen from halogen atoms and trifluoromethyl, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, cyano, methylthio, methylsulphinyl and methylsulphonyl radicals, or a methyl radical bearing a heterocyclic substituent in which the heterocyclic system can be a pyridyl, thienyl or furyl radical and can bear one or more substituents, R.sub.2 is a hydrogen atom or a (C.sub.1-4)alkyl radical, R.sub.3 is a hydrogen atom or a hydroxy radical, and R.sub.4 is a hydrogen atom or a (C.sub.1-4)alkyl radical, where appropriate, in tautomeric form when R.sub.3 is OH.The compounds may be used in treating allergy and histamine-induced inflammation.

    摘要翻译： 对应于式（1）的苯并咪唑衍生物其中X是CH或N，R 1是氢原子或可以带有1-3个选自卤素原子和三氟甲基的取代基的苄基，（C1 -4）烷基，（C 1-4）烷氧基，氰基，甲硫基，甲基亚磺酰基和甲基磺酰基，或具有杂环取代基的甲基，其中杂环体系可以是吡啶基，噻吩基或呋喃基，并且可以具有一个或多个取代基 ，R 2为氢原子或（C 1-4）烷基，R 3为氢原子或羟基，R 4为氢原子或（C 1-4）烷基，当R 3为 是OH。 该化合物可用于治疗过敏和组胺诱导的炎症。

    Indolone derivatives, their preparation and their application in therapy
    6.
    发明授权
    Indolone derivatives, their preparation and their application in therapy 失效
    吲哚酮衍生物，其制备及其在治疗中的应用

    公开(公告)号：US5010079A

    公开(公告)日：1991-04-23

    申请号：US388373

    申请日：1989-08-02

    申请人： Philippe Manoury ,  Jean Binet ,  Daniel Obitz ,  Gerard Defosse ,  Elisabeth Dewitte ,  Corinne Veronique

    发明人： Philippe Manoury ,  Jean Binet ,  Daniel Obitz ,  Gerard Defosse ,  Elisabeth Dewitte ,  Corinne Veronique

    IPC分类号： A61K31/495 ,  A61P43/00 ,  C07D209/34 ,  C07D401/12

    CPC分类号： C07D401/12 ,  C07D209/34

    摘要： An indolone derivative is useful for the treatment of anxiety, depression and schizophrenia and is a 5HT.sub.1A agonist and 5HT.sub.2 antagonist, which is a compound of formula (I): ##STR1## in which R.sub.1 is a hydrogen or halogen atom or a (C.sub.1-4)alkyl radical,R.sub.2 is a hydrogen atom or a (C.sub.1-4)alkyl radical,R.sub.3 is a hydrogen atom, a (C.sub.1-4)alkyl radical or an S-(C.sub.1-4) alkyl radical; andR.sub.4 is a phenyl, chlorophenyl, naphthyl, 7-methoxy-1-naphthyl, 6-methoxy-1-indanyl, 2-methoxy-6-pyridyl, 3-methoxy-2-pyridyl, isoquinolyl, 7-methoxy-1-isoquinolyl, 7-methoxy-1,2,3,4-tetrahydro-1-naphthyl or 7-fluoro-1-naphthyl radical;or a pharmaceutically acceptable acid addition salt thereof.

    摘要翻译： 吲哚酮衍生物可用于治疗焦虑，抑郁和精神分裂症，并且是5HT1A激动剂和5HT2拮抗剂，其为式（I）的化合物：其中R 1为氢或卤素原子或（C1- 4）烷基，R 2是氢原子或（C 1-4）烷基，R 3是氢原子，（C 1-4）烷基或S-（C 1-4）烷基; 并且R 4是苯基，氯苯基，萘基，7-甲氧基-1-萘基，6-甲氧基-1-二氢化茚基，2-甲氧基-6-吡啶基，3-甲氧基-2-吡啶基，异喹啉基，7-甲氧基-1- 异喹啉基，7-甲氧基-1,2,3,4-四氢-1-萘基或7-氟-1-萘基; 或其药学上可接受的酸加成盐。

    Piperidine derivatives, their preparation and their application in therapeutics
    7.
    发明授权
    Piperidine derivatives, their preparation and their application in therapeutics 失效
    哌啶衍生物，其制备及其在治疗中的应用

    公开(公告)号：US5418241A

    公开(公告)日：1995-05-23

    申请号：US127058

    申请日：1993-09-27

    申请人： Samir Jegham ,  Gerard Defosse ,  Thomas Purcell

    发明人： Samir Jegham ,  Gerard Defosse ,  Thomas Purcell

    IPC分类号： A61K31/445 ,  A61K31/4427 ,  A61P1/08 ,  A61P25/04 ,  A61P25/06 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  C07D211/60 ,  C07D233/64 ,  C07D235/30 ,  C07D401/14

    CPC分类号： C07D401/14

    摘要： The invention provides a compound which is a piperidine derivative of formula (I) ##STR1## in which R.sub.1 is hydrogen or straight or branched (C.sub.1 -C.sub.6) alkyl, R.sub.2 is hydrogen or straight or branched (C.sub.1 -C.sub.8) alkyl, Z and Z.sub.1 which may be the same or different, each is hydrogen, chlorine, hydroxyl, amino, nitro, hydroxymethyl, (C.sub.1 -C.sub.2) alkyl, (C.sub.1 -C.sub.8) alkoxy straight or branched (C.sub.1 -C.sub.5) alkoxycarbonyl or aryl (C.sub.1 -C.sub.2) alkoxy, Z is in position 4, 6 or 7 and Z and Z.sub.1 cannot both be hydrogen, or its addition salt with a pharmaceutically acceptable acid and its therapeutic application.

    摘要翻译： 本发明提供了式（I）哌啶衍生物（Ⅰ）的化合物，其中R 1是氢或直链或支链（C 1 -C 6）烷基，R 2是氢或直链或支链（C 1 -C 8）烷基 ，可以相同或不同的Z和Z 1各自为氢，氯，羟基，氨基，硝基，羟甲基，（C1-C2）烷基，（C1-C8）烷氧基直链或支链（C1-C5）烷氧基羰基或芳基 （C1-C2）烷氧基，Z在4,6或7位，Z和Z1不能都是氢，或其加药盐与药学上可接受的酸及其治疗应用。

    Piperidine derivatives, their preparation and their therapeutic application
    8.
    发明授权
    Piperidine derivatives, their preparation and their therapeutic application 失效
    哌啶衍生物，其制备及其治疗应用

    公开(公告)号：US5280030A

    公开(公告)日：1994-01-18

    申请号：US862376

    申请日：1992-04-02

    申请人： Samir Jegham ,  Gerard DeFosse ,  Thomas Purcell ,  Johannes Schoemaker

    发明人： Samir Jegham ,  Gerard DeFosse ,  Thomas Purcell ,  Johannes Schoemaker

    IPC分类号： A61K31/445 ,  A61K31/4427 ,  A61P1/08 ,  A61P25/00 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

    CPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/14

    摘要： A compound which is a piperidine derivative of general formula (I) ##STR1## in which R.sub.1 represents a hydrogen atom, a linear or branched (C.sub.1-6)alkyl group or a cyclo(C.sub.3-8)alkyl group, X represents an oxygen atom, a sulphur atom or a group of general formula N--R.sub.3 in which R.sub.3 is a hydrogen atom, or a linear or branched (C.sub.1-8)alkyl, cyclo(C.sub.3-6)alkyl, cyclo(C.sub.3-6)alkylmethyl, (C.sub.1-4)alkoxy-(C.sub.1-4)alkyl, phenyl, pyridin-4-yl, pyridin-3-yl, pyridin-4-ylmethyl or pyridin-3-ylmethyl group and Z represents a hydrogen or fluorine atom and acid addition salts thereof with pharmaceutically acceptable acids, can be used for the treatment and prevention of disorders in which 5-HT receptors are involved.

    摘要翻译： 对应于通式（I）的化合物，其中R 1表示氢原子或直链或支链（C 1-6）烷基或环（C 3-8）烷基，X表示 氧原子或硫原子或其中R3是氢原子的通式为N-R3的基团，直链或支链（C1-8）烷基，环（C3-6）烷基，环（C3 -6）烷基甲基，（C 1-4）烷氧基（C 1-4）烷基，苯基，4-吡啶基或3-吡啶基，Z表示氢或氟原子，以及它们的加成盐 与药学上可接受的酸。 应用于治疗。