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55 条记录 (耗时 0.173 秒)

    2-aminopyrazine-5-carboxamide derivatives, their preparation and their application in therapeutics
    31.
    发明授权
    2-aminopyrazine-5-carboxamide derivatives, their preparation and their application in therapeutics 失效
    2-氨基吡嗪-5-甲酰胺衍生物，其制备及其在治疗中的应用

    公开(公告)号：US5420130A

    公开(公告)日：1995-05-30

    申请号：US243315

    申请日：1994-05-16

    申请人： Pascal George ,  Benoit Marabout ,  Jacques Froissant

    发明人： Pascal George ,  Benoit Marabout ,  Jacques Froissant

    IPC分类号： A61K31/495 ,  A61K31/4965 ,  A61P13/02 ,  A61P13/08 ,  A61P15/00 ,  C07D241/26 ,  C07D241/28 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14

    CPC分类号： C07D401/12 ,  C07D241/26

    摘要： Compounds corresponding to the general formula (I) ##STR1## in which n represents 0 or 1, R.sub.1 represents a methyl group, in which case R.sub.2 represents a phenoxy(C.sub.1 -C.sub.4)alkyl group (in which the phenoxy group is optionally substituted), or else R.sub.1 and R.sub.2 together form, and with the nitrogen atom which carries them, a 4-(phenoxymethyl)piperid-1-yl group (in which the phenoxy group is optionally substituted) or a 4-phenylpiperazin-1-yl group (in which the phenyl group is optionally substituted), R.sub.3 represents a hydrogen atom or a methyl group, R.sub.4 represents a hydrogen atom and R.sub.5 represents a hydrogen atom or a group of general formula -CH.sub.2 -CH.sub.2 -NH-R.sub.6, R.sub.6 being a hydrogen atom or a tert-butyloxycarbonyl, 4-carbamoylpyrimidin-2-yl or 5-carbamoylpyrazin-2-yl group, are useful in the treatment of diseases and complaints involving hyperactivity of the .alpha.-adrenergic system at the level of the lower urinary apparatus.

    摘要翻译： 对应于通式（I）的化合物其中n表示0或1，R1表示甲基，其中R2表示苯氧基（C1-C4）烷基（其中苯氧基为 任选取代），或者R1和R2一起形成，并且与携带它们的氮原子一起形成4-（苯氧基甲基）哌啶-1-基（其中苯氧基任选被取代）或4-苯基哌嗪-1-基 - 基（其中苯基任选被取代），R 3表示氢原子或甲基，R 4表示氢原子，R 5表示氢原子或通式-CH 2 -CH 2 -NH-R 6基团， R6是氢原子或叔丁氧基羰基，4-氨基甲酰基嘧啶-2-基或5-氨基甲酰基吡嗪-2-基可用于治疗涉及α-肾上腺素能系统的多动症的疾病和投诉， 下尿路器

    Imidazopyridine for use as an anaesthetic
    33.
    发明授权
    Imidazopyridine for use as an anaesthetic 失效
    咪唑并吡啶用作麻醉剂

    公开(公告)号：US5064836A

    公开(公告)日：1991-11-12

    申请号：US619428

    申请日：1990-11-29

    申请人： Henri Depoortere ,  Pascal George

    发明人： Henri Depoortere ,  Pascal George

    IPC分类号： C07D471/04 ,  A61K31/435 ,  A61K31/44 ,  A61P23/00

    CPC分类号： A61K31/44

    摘要： A method of anaesthetizing a subject in need of anaesthetizing, which comprises administering to the subject an anaesthetically effective amount of N-[[2-(4-ethylphenyl)-3-imidazo[1,2-a]pyridinyl]methyl] N,3-dimethylbutanamide or a pharmaceutically acceptable salt thereof.

    摘要翻译： 一种麻醉需要麻醉的受试者的方法，其包括向所述受试者施用麻醉有效量的N - [[2-（4-乙基苯基）-3-咪唑并[1,2-a]吡啶基]甲基] 3-二甲基丁酰胺或其药学上可接受的盐。

    Imidazo(1,2-a)quinoline derivatives useful as anxiolytic agents
    34.
    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。

    3-acylaminomethylimidazo[1,2-a]pyridine derivatives and pharmaceutical compositions containing them
    38.
    发明授权
    3-acylaminomethylimidazo[1,2-a]pyridine derivatives and pharmaceutical compositions containing them 失效
    3-酰氨基甲基咪唑并[1,2-a]吡啶衍生物和含有它们的药物组合物

    公开(公告)号：US4650796A

    公开(公告)日：1987-03-17

    申请号：US826966

    申请日：1986-02-07

    申请人： Pascal George ,  Claude Giron

    发明人： Pascal George ,  Claude Giron

    IPC分类号： C07D487/04 ,  A61K31/435 ,  A61K31/44 ,  A61P25/08 ,  A61P25/20 ,  A61P25/28 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： Compounds which are imidazo[1,2-a]pyridine derivatives of general formula (I) ##STR1## in which each of X.sub.1, X.sub.2, X.sub.3, independently of each other, is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, methoxy, methylthio, ethylthio, methylsulphonyl, nitro, amino, methylamino, dimethylamino, acetylamino or diacethylamino, Y is hydrogen, chlorine or methyl, R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl or benzyl, R.sub.2 is C.sub.1 -C.sub.6 alkyl, cyclohexyl, trichloromethyl, 1-propenyl, allyl, phenyl, 4-chlorophenyl or benzyl, or R.sub.1 and R.sub.2 together represent a divalent C.sub.3 -C.sub.5 alipathic group and their pharmaceutically acceptable acid salts have anxiolytic, sleep-inducing, hypnotic, anticonvulsant, analgesic and anti-ulcer properties.

    摘要翻译： 作为其中X 1，X 2，X 3各自独立的通式（I）的咪唑并[1,2-a]吡啶衍生物的化合物是氢，卤素，C 1 -C 4烷基， 甲氧基，甲硫基，乙硫基，甲基磺酰基，硝基，氨基，甲基氨基，二甲基氨基，乙酰氨基或二乙基氨基，Y是氢，氯或甲基，R1是氢，C1-C4烷基或苄基，R2是C1-C6烷基，环己基，三氯甲基， 1-丙烯基，烯丙基，苯基，4-氯苯基或苄基，或R 1和R 2一起代表二价C 3 -C 5脂酰基，其药学上可接受的酸盐具有抗焦虑，睡眠诱导，催眠，抗惊厥，镇痛和抗溃疡性质 。

    Therapeutically useful imidazo[1,2-a]pyridine derivatives
    39.
    发明授权
    Therapeutically useful imidazo[1,2-a]pyridine derivatives 失效
    治疗上有用的咪唑并[1,2-a]吡啶衍生物

    公开(公告)号：US4492695A

    公开(公告)日：1985-01-08

    申请号：US484611

    申请日：1983-04-13

    申请人： Jean-Pierre Kaplan ,  Pascal George ,  Jean-Michel Bernardon

    发明人： Jean-Pierre Kaplan ,  Pascal George ,  Jean-Michel Bernardon

    IPC分类号： A61K31/435 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54 ,  A61P25/08 ,  A61P25/20 ,  A61P25/28 ,  A61P43/00 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： An imidazo[1,2-a]pyridine derivative of the formula: ##STR1## wherein Y represents a hydrogen or halogen atom or a C.sub.1-4 alkyl radical, Z represents a furan-2-yl, thien-2-yl or pyridin-2-yl radical optionally carrying a halogen atom or a methyl or ethyl radical in the 5-position, and R represents the hydroxy radical, a C.sub.1-4 alkoxy radical or a group --NR.sub.1 R.sub.2 in which R.sub.1 and R.sub.2 independently of one another each represent a hydrogen atom; a straight- or branched-chain C.sub.1-5 alkyl radical optionally carrying one or more halogen atoms or a hydroxy radical, a group --N(C.sub.1-4 alkyl).sub.2, a carbamoyl radical or a C.sub.1-4 alkoxy radical; the allyl radical; the propargyl radical; a C.sub.3-6 cycloalkyl radical; the benzyl radical; or the phenyl radical, or alternatively --NR.sub.1 R.sub.2 together represent a heterocyclic ring containing from 3 to 6 carbon atoms, or a heterocyclic ring of the formula ##STR2## in which X is O, S, CHOR' or N-R", R' being a hydrogen atom or the benzyl radical and R" being a hydrogen atom, a C.sub.1-4 alkyl radical or the phenyl radical optionally carrying a methoxy radical or a halogen atom, are new compounds. They are therapeutically useful as they possess anxiolytic, antianoxic, sleep-inducing, hypnotic and anticonvulsant properties.

    摘要翻译： 下式的咪唑并[1,2-a]吡啶衍生物：其中Y表示氢或卤素原子或C1-4烷基，Z表示呋喃-2-基，噻吩-2-基或吡啶 -2-基任选地在5-位上带有卤素原子或甲基或乙基，R表示羟基，C 1-4烷氧基或-NR 1 R 2，其中R 1和R 2各自独立地为 表示氢原子; 任选携带一个或多个卤素原子或羟基的直链或支链C 1-5烷基，基团-N（C 1-4烷基）2，氨基甲酰基或C 1-4烷氧基; 烯丙基; 炔丙基; C3-6环烷基; 苄基; 或苯基，或者-NR1R2一起代表含有3至6个碳原子的杂环，或其中X为O，S，CHOR'或N-R“的式”IMAGE“的杂环，R “是氢原子或苄基，R”是氢原子，C1-4烷基或任选带有甲氧基或卤素原子的苯基是新的化合物。 它们是治疗有用的，因为它们具有抗焦虑，抗癫痫，睡眠诱导，催眠和抗惊厥性质。

    Imidazo[1,2-a] pyridine derivatives and their application as pharmaceuticals
    40.
    发明授权
    Imidazo[1,2-a] pyridine derivatives and their application as pharmaceuticals 失效
    咪唑并[1,2-a]吡啶衍生物及其作为药物的应用

    公开(公告)号：US4382938A

    公开(公告)日：1983-05-10

    申请号：US313601

    申请日：1981-10-21

    申请人： Jean-Pierre Kaplan ,  Pascal George

    发明人： Jean-Pierre Kaplan ,  Pascal George

    IPC分类号： A61K31/435 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54 ,  A61P9/00 ,  A61P25/08 ,  A61P25/20 ,  A61P25/28 ,  C07D471/04 ,  C07D487/02

    CPC分类号： C07D471/04

    摘要： Imidazo[1,2-a] pyridines of the formula: ##STR1## and their acid addition salts in which Y represents a hydrogen or halogen atom or a C.sub.1-4 alkyl radical, Z represents a naphthyl radical or a radical ##STR2## in which each of X.sub.1 and X.sub.2 independently of one another is a hydrogen or halogen atom, a C.sub.1-4 alkoxy radical, a C.sub.1-6 alkyl radical or CF.sub.3, CH.sub.3 S--, CH.sub.3 SO.sub.2 --, --NO.sub.2, --NH.sub.2 or --NHCOCH.sub.3, and each of R.sub.1 and R.sub.2 independently of one another represents a hydrogen atom, a straight or branched C.sub.1-5 alkyl radical which is unsubstituted or substituted by one or more halogen atoms or hydroxyl, --N(C.sub.1-4 alkyl).sub.2, carbamoyl or C.sub.1-4 alkoxy radicals, allyl, propargyl, a C.sub.3-6 cycloalkyl radical, benzyl, or phenyl, not both R.sub.1 and R.sub.2 being hydrogen, or --NR.sub.1 R.sub.2 represents a heterocyclic ring containing from 3 to 6 carbon atoms, or a heterocyclic ring of the formula ##STR3## in which X is O, S, CHOR' or >N--R, R' being hydrogen or benzyl and R being hydrogen, a C.sub.1-4 alkyl radical, or phenyl which is unsubstituted or substituted by methoxy or a halogen atom, which may be made from the corresponding acids, have valuable pharmacological properties, especially anxiolytic, anti-anoxic, sleep-inducing, hypnotic and anticonvulsant properties.

    摘要翻译： 下式的咪唑并[1,2-a]吡啶及其酸加成盐，其中Y表示氢或卤素原子或C1-4烷基，Z表示萘基或基团， 其中X1和X2各自独立地为氢或卤素原子，C1-4烷氧基，C1-6烷基或CF3，CH3S-，CH3SO2-，-NO2，-NH2或-NHCOCH3，各自为 R 1和R 2彼此独立地表示氢原子，未被取代或被一个或多个卤素原子或羟基取代的直链或支链C 1-5烷基，-N（C 1-4烷基）2，氨基甲酰基或C1- 4个烷氧基，烯丙基，炔丙基，C 3-6环烷基，苄基或苯基，不同时R 1和R 2均为氢，或-NR 1 R 2表示含有3至6个碳原子的杂环，或式 其中X为O，S，CHOR'或> NR，R'为氢或苄基，R为氢，C1-4烷基或未取代的苯基 或由相应的酸制成的甲氧基或卤原子取代，具有有价值的药理学特性，特别是抗焦虑，抗缺氧，睡眠诱导，催眠和抗惊厥性质。