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    2-Thiohydantoine derivative compounds and use thereof for the treatment of diabetes
    1.
    发明申请
    2-Thiohydantoine derivative compounds and use thereof for the treatment of diabetes 审中-公开
    2-硫代乙内酰脲衍生物及其用于治疗糖尿病的用途

    公开(公告)号：US20060025589A1

    公开(公告)日：2006-02-02

    申请号：US10529817

    申请日：2003-10-03

    申请人： Jean Binet ,  Benaissa Boubia ,  Evelyne Chaput ,  Alan Edgar ,  Khan Ou ,  Philippe Ratel ,  Soth Samreth ,  Didier Thomas

    发明人： Jean Binet ,  Benaissa Boubia ,  Evelyne Chaput ,  Alan Edgar ,  Khan Ou ,  Philippe Ratel ,  Soth Samreth ,  Didier Thomas

    IPC分类号： C07D413/02 ,  C07D405/02 ,  C07D403/02

    CPC分类号： C07D401/04 ,  C07D233/86 ,  C07D401/12 ,  C07D405/04

    摘要： The invention relates to 2-thiohydantoin compounds selected from compounds of general formula (I): in which, in particular, one of the radicals R1 and R2 comprises two aromatic rings in the structure or is the dibenzofuranyl group, R3 is a hydrogen atom, a halogen atom, a C1-C4 alkyl group, a C1-C4 alkoxy group, a hydroxyl group, a phenyl group or a benzyl group, R4 is a hydrogen atom, a halogen atom or a C1-C4 alkyl group, and their addition salts with a non-toxic acid, especially the pharmaceutically acceptable salts. It further relates to the process for their preparation, to the pharmaceutical compositions in which they are present, and to their use as pharmacologically active substances, especially in the case of the treatment of diabetes, diseases due to hyperglycemia, hypertriglyceridemia, dyslipidemia or obesity.

    摘要翻译： 本发明涉及选自通式（I）的化合物的2-硫代乙内酰脲化合物：其中特别地，基团R 1和R 2中的一个包含两个芳族 结构中的环或是二苯并呋喃基，R 3是氢原子，卤素原子，C 1 -C 4烷基 C 1 -C 4烷氧基，羟基，苯基或苄基，R 4是氢原子， 卤素原子或C 1 -C 4烷基，以及它们与无毒酸，特别是药学上可接受的盐的加成盐。 其进一步涉及其制备方法，其存在的药物组合物及其作为药理活性物质的用途，特别是在治疗糖尿病，由于高血糖症，高甘油三酯血症，血脂异常或肥胖症引起的疾病的情况下。

    Imidazo[4,5-b]pyridin-2-one derivatives
    2.
    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。

    Indolone derivatives, their preparation and their application in therapy
    5.
    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
    6.
    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。