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    5-PHENYLPYRAZOLOPYRIDINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
    7.
    发明申请
    5-PHENYLPYRAZOLOPYRIDINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF 有权

    公开(公告)号：US20130023554A1

    公开(公告)日：2013-01-24

    申请号：US13496118

    申请日：2010-09-17

    申请人： Florian Auger ,  Danielle De Peretti ,  Luc Even

    发明人： Florian Auger ,  Danielle De Peretti ,  Luc Even

    IPC分类号： C07D471/04 ,  C07F5/02 ,  A61P25/28 ,  A61P25/08 ,  A61P29/00 ,  A61P25/30 ,  A61P19/10 ,  A61P35/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61K31/437 ,  A61P25/00

    CPC分类号： C07D471/06

    摘要： Compounds of formula (I): in which:R1 represents a phenyl group or naphthyl group, optionally substituted by one or more atoms or groups chosen, independently of one another, from: halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkoxy, (C1-C6)thioalkyl, —S(O)(C1-C6)alkyl, —S(O)2(C1-C6)alkyl, hydroxyl, hydroxy(C1-C6)alkylene, CHO, COOH, (C1-C6)alkoxy(C1-C6)alkyleneoxy, NRaRb, CONRaRb, SO2NRaRb, NRcCORd, OC(O)NRaRb, OCO(C1-C6)alkyl, NRcC(O)ORe or NRcSO2Re; X represents from 1 to 4 substituents which are identical to or different from one another and which are chosen from hydrogen, halogen, (C1-C6)alkyl or (C1-C6)alkoxy, it being possible for the (C1-C6)alkyl to be optionally substituted by one or more groups chosen from a halogen, (C1-C6)alkoxy or hydroxyl; R2 and R3 represent, independently of one another, a hydrogen atom, a (C1-C6)alkyl group optionally substituted by an Rf group, or a CHO or COOH group; X and R3 can together form, with the carbon atoms which carry them, a carbocycle of 5 to 7 carbon atoms; R4 represents a hydrogen atom or a (C1-C6)alkyl group; Ra and Rb represent, independently of one another, a hydrogen atom or a (C1-C6)alkyl, aryl(C1-C6)alkylene or aryl group; or Ra and Rb together form, with the nitrogen atom which carries them, an azetidine, pyrrolidine, piperidine, azepine, morpholine, thiomorpholine, piperazine or homopiperazine group, this group being optionally substituted by a (C1-C6)alkyl, aryl or aryl(C1-C6)alkylene group; Rc and Rd represent, independently of one another, a hydrogen atom or a (C1-C6)alkyl, aryl(C1-C6)alkylene or aryl group; or Rc and Rd together form a (C2-C5)alkylene group; Re represents a (C1-C6)alkyl, aryl(C1-C6)alkylene or aryl group; or Rc and Re together form a (C2-C5)alkylene group; Rf represents a hydroxyl, oxo, CHO or COOH group, in the form of the base or of an addition salt with an acid.Therapeutic use and synthetic process.

    9H-imidazo[1,2-A]benzimidazole-3-acetamide derivatives, their preparation and their therapeutic application
    8.
    发明授权
    9H-imidazo[1,2-A]benzimidazole-3-acetamide derivatives, their preparation and their therapeutic application 失效
    9H-咪唑并[1,2-A]苯并咪唑-3-乙酰胺衍生物，其制备及其治疗应用

    公开(公告)号：US5466706A

    公开(公告)日：1995-11-14

    申请号：US180998

    申请日：1994-01-14

    申请人： Pascal George ,  Danielle De Peretti ,  Jocelyne Roy ,  Jean-Paul Schmitt ,  Mireille Sevrin

    发明人： Pascal George ,  Danielle De Peretti ,  Jocelyne Roy ,  Jean-Paul Schmitt ,  Mireille Sevrin

    IPC分类号： A61K31/415 ,  A61P25/08 ,  A61P25/20 ,  A61P43/00 ,  C07D233/68 ,  C07D235/00 ,  C07D487/04 ,  C07D519/00 ,  A61K

    CPC分类号： C07D487/04

    摘要： Compound corresponding to the formula: ##STR1## in which X represents one or more of hydrogen, halogen, alkyl, trifluoromethyl, alkoxy, alkylthio, methylsulphonyl, cyano, ethoxycarbonyl, aminocarbonyl and carboxy, Y represents one or more of hydrogen, halogens, alkyl, trifluoromethyl, methoxy and trifluoromethoxy, R.sub.1 represents hydrogen, alkyl, phenylmethyl, 2-phenylethyl, acetyl or alkoxycarbonyl, R.sub.2 and R.sub.3 each represent hydrogen, alkyl which is optionally substituted, prop-2-enyl, prop-2-ynyl, phenyl, 1-(phenylmethyl)piperidin-4-yl, or 1-[(cyclohexen-1-yl)methyl]piperidin-4-yl, or alternatively R.sub.2 and R.sub.3 form, with the nitrogen atom carrying them, an optionally substituted heterocycle. These compounds are useful as hypnotic, anxiolytic and anticonvulsant agents.

    摘要翻译： 对应于下式的化合物：其中X表示氢，卤素，烷基，三氟甲基，烷氧基，烷硫基，甲基磺酰基，氰基，乙氧基羰基，氨基羰基和羧基中的一个或多个，Y表示一个或多个氢， 卤素，烷基，三氟甲基，甲氧基和三氟甲氧基，R1代表氢，烷基，苯基甲基，2-苯基乙基，乙酰基或烷氧基羰基，R2和R3各自表示氢，任选取代的烷基，丙-2-烯基，丙-2-炔基 ，苯基，1-（苯基甲基）哌啶-4-基或1 - [（环己烯-1-基）甲基]哌啶-4-基，或者R2和R3与带有氮原子一起形成任选取代的 杂环。 这些化合物可用作催眠，抗焦虑药和抗惊厥剂。

    Imidazo(1,2-a)quinoline derivatives useful as anxiolytic agents
    9.
    发明授权
    Imidazo(1,2-a)quinoline derivatives useful as anxiolytic agents 失效
    咪唑（1,2-a）喹啉衍生物，可用作抗焦虑剂

    公开(公告)号：US4675323A

    公开(公告)日：1987-06-23

    申请号：US826981

    申请日：1986-02-07

    申请人： Pascal George ,  Danielle De Peretti

    发明人： Pascal George ,  Danielle De Peretti

    IPC分类号： C07D471/04 ,  A61K31/395 ,  C07D401/14 ,  C07D411/14

    CPC分类号： C07D471/04

    摘要： Compounds which are imidazo[1,2-a]quinoline derivatives of general formula (I) ##STR1## in which X is hydrogen, halogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, (C.sub.1-4) alkylthio, methylsulphonyl, amino, (C.sub.1-4)alkylamino, di-(C.sub.1-4)alkylamino, nitro or trifluoromethyl, Y is hydrogen, halogen or methyl in position 6, 7 or 8, R.sub.1 and R.sub.2, which may be the same or different, are hydrogen or (C.sub.1-6) alkyl, or R.sub.1 and R.sub.2 together form a tetramethylene, pentamethylene, 3-methyl-3-azapentamethylene, 3-ethoxycarbonyl-3-azapentamethylene group, and A and B both are hydrogen or together form a carbon-carbon bond, and their pharmacologically acceptable acid addition salts have anxiolytic, sleep-inducing, hypnotic, anticonvulsant, analgesic and anti-ulcer properties.

    摘要翻译： 作为通式（I）的咪唑并[1,2-a]喹啉衍生物的化合物，其中X是氢，卤素，（C 1-4）烷基，（C 1-4）烷氧基，（C 1-4）烷硫基 ，甲基磺酰基，氨基，（C 1-4）烷基氨基，二 - （C 1-4）烷基氨基，硝基或三氟甲基，Y是6或7或8位的氢，卤素或甲基，R 1和R 2可以相同或 不同的是氢或（C 1-6）烷基，或者R 1和R 2一起形成四亚甲基，五亚甲基，3-甲基-3-氮杂萘基，3-乙氧基羰基-3-氮杂萘基，A和B都是氢或一起形成 碳 - 碳键，其药理学上可接受的酸加成盐具有抗焦虑，睡眠诱导，催眠，抗惊厥，止痛和抗溃疡等特性。