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    Indolone derivatives, their preparation and their application in therapy
    3.
    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 and pharmaceutical compositions containing them
    4.
    发明授权
    Piperidine derivatives and pharmaceutical compositions containing them 失效
    哌啶衍生物和含有它们的药物组合物

    公开(公告)号：US4680296A

    公开(公告)日：1987-07-14

    申请号：US787971

    申请日：1985-10-15

    申请人： Philippe Manoury ,  Jean Binet ,  Elisabeth Dewitte

    发明人： Philippe Manoury ,  Jean Binet ,  Elisabeth Dewitte

    IPC分类号： C07D401/06 ,  C07D401/14 ,  C07D409/14 ,  A61K31/505 ,  C07D401/04

    CPC分类号： C07D401/06 ,  C07D401/14 ,  C07D409/14

    摘要： Piperidine derivatives which are compounds of formula (I) ##STR1## wherein Ar.sub.1 and Ar.sub.2 independently represent a phenyl group optionally substituted by a halogen atom, a thienyl group or a pyridinyl group, A represents an alkylene group of 2 to 6 carbon atoms, X represents a CO group or a bond, R.sub.1 represents a hydrogen atom or an alkyl group of 1 to 4 carbon atoms, either R.sub.2 represents a hydrogen atom and R.sub.3 represents a hydrogen atom or a hydroxy group, or R.sub.2 and R.sub.3 together represent a bond, and R.sub.4 represents a hydrogen or halogen atom, or pharmaceutically acceptable acid addition salts thereof are useful as antiallergics and antipruritics.

    摘要翻译： 作为式（I）化合物的哌啶衍生物其中Ar 1和Ar 2独立地表示任选被卤素原子，噻吩基或吡啶基取代的苯基，A表示2〜6个碳的亚烷基 原子，X表示CO基或键，R1表示氢原子或1-4个碳原子的烷基，R2表示氢原子，R3表示氢原子或羟基，R2或R3表示 R 4表示氢或卤素原子，或其药学上可接受的酸加成盐可用作抗过敏药和止痒药。

    Imidazo[4,5-b]pyridin-2-one derivatives
    5.
    发明授权
    Imidazo[4,5-b]pyridin-2-one derivatives 失效
    咪唑并[4,5-b]吡啶-2-酮衍生物

    公开(公告)号：US4806560A

    公开(公告)日：1989-02-21

    申请号：US105243

    申请日：1987-10-07

    申请人： Philippe Manoury ,  Jean Binet ,  Elisabeth Dewitte

    发明人： Philippe Manoury ,  Jean Binet ,  Elisabeth Dewitte

    IPC分类号： A61K31/44 ,  A61P37/08 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： Imidazo[4,5-b]pyridin-2-one derivatives of the formula (I) ##STR1## in which n is 2, 3 or 4, x is .dbd.CH-- or .dbd.N--, R.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen, halogen or (C.sub.1-4) alkoxy and either R.sub.3 is H or OH and R.sub.4 is H, or R.sub.3 and R.sub.4 together form a direct bond, their enantiomers and their addition salts with pharmaceutically acceptable acids are pharmacologically active, for example as antagonists to histamine and serotonin.

    摘要翻译： 式（I）的咪唑并[4,5-b]吡啶-2-酮衍生物其中n为2,3或4，x为= CH-或= N-，R1和R2， 其可以相同或不同，各自表示氢，卤素或（C 1-4）烷氧基，且R 3为H或OH且R 4为H，或者R 3和R 4一起形成直接键，其对映异构体及其加成盐与药学上 可接受的酸是药理活性的，例如作为组胺和5-羟色胺的拮抗剂。

    Benzimidazole derivatives and pharmaceutical compositions containing them
    7.
    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。