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    2-((4-Piperidyl)methyl)-1,2,3,4-tetrahydroisoquinoline derivatives, their preparation and their application in therapy
    2.
    发明授权
    2-((4-Piperidyl)methyl)-1,2,3,4-tetrahydroisoquinoline derivatives, their preparation and their application in therapy 失效
    2 - （（4-哌啶基）甲基）-1,2,3,4-四氢异喹啉衍生物，其制备及其在治疗中的应用

    公开(公告)号：US4885302A

    公开(公告)日：1989-12-05

    申请号：US228748

    申请日：1988-08-05

    申请人： Pascal George ,  Mireille Sevrin ,  Christian Maloizel

    发明人： Pascal George ,  Mireille Sevrin ,  Christian Maloizel

    IPC分类号： A61K31/47 ,  A61K31/475 ,  A61P9/00 ,  A61P9/12 ,  A61P25/04 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

    CPC分类号： C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

    摘要： A compound of formula (I) ##STR1## in which R is (a) a hydrogen atom;(b) a linear or branched (C.sub.1 -C.sub.6) alkyl group; an allyl group; a cycloalkylmethyl group in which the cycloalkyl moiety has from 3 to 6 carbon atoms; a phenylmethyl group unsubstituted or substituted with one to three substituents chosen from halogen atoms and trifluoromethyl, nitro, amino, dimethylamino, cyano, aminocarbonyl, linear or branched (C.sub.1 -C.sub.3) alkyl, linear or branched (C.sub.1 -C.sub.3) alkoxy and linear or branched (C.sub.1 -C.sub.3) alkylthio groups; a 2-phenylethyl group; a 3-phenylpropyl group; a 3-phenyl-2-propenyl group; a phenylcarbonylmethyl group; a naphthylmethyl group; a pyridylmethyl group; a furylmethyl group; or a thienylmethyl group; or(c) a linear or branched (C.sub.2 -C.sub.6) alkanoyl group; a cycloalkylcarbonyl group in which the cycloalkyl moiety has from 3 to 6 carbon atoms; a trifluoroacetyl group; a phenyl-carbonyl group unsubstituted or substituted with one to three substituents chosen from halogen atoms and trifluoromethyl, nitro, linear or branched (C.sub.1 -C.sub.3) alkyl, linear or branched (C.sub.1 -C.sub.3) alkoxy and linear or branched (C.sub.1 -C.sub.3) alkylthio groups; a 1-oxo-3-phenyl-2-propenyl group; a naphthylcarbonyl group; a pyridylcarbonyl group; a furylcarbonyl group; a thienylcarbonyl group; a (2-indolyl)-carbonyl group; or a (5-indolyl)carbonyl group; or a pharmacologically acceptable acid addition salt thereof.

    摘要翻译： 式（I）化合物其中R为（a）氢原子; （b）直链或支链（C1-C6）烷基; 烯丙基; 环烷基甲基，其中环烷基部分具有3至6个碳原子; 未取代或被一至三个选自卤素原子和三氟甲基，硝基，氨基，二甲基氨基，氰基，氨基羰基，直链或支链（C 1 -C 3）烷基，直链或支链（C 1 -C 3）烷氧基和直链或支链 支链（C1-C3）烷硫基; 2-苯基乙基; 3-苯基丙基; 3-苯基-2-丙烯基; 苯基羰基甲基; 萘基甲基; 吡啶基甲基; 呋喃甲基; 或噻吩甲基; 或（c）直链或支链（C 2 -C 6）烷酰基; 环烷基部分具有3至6个碳原子的环烷基羰基; 三氟乙酰基; 直链或支链（C1-C3）烷基，直链或支链（C1-C3）烷氧基和直链或支链的（C1-C3）烷基， 烷硫基; 1-氧代-3-苯基-2-丙烯基; 萘基羰基; 吡啶基羰基; 呋喃基羰基; 噻吩基羰基; （2-吲哚基） - 羰基; 或（5-吲哚基）羰基; 或其药理学上可接受的酸加成盐。

    8-azabicyclo[3.2.1] octane-3-methanamine derivatives as ligands of D2 and D3 dopamine and 5HT1A and 5HT2 serotonin receptors
    3.
    发明授权
    8-azabicyclo[3.2.1] octane-3-methanamine derivatives as ligands of D2 and D3 dopamine and 5HT1A and 5HT2 serotonin receptors 失效
    8-氮杂双环[3.2.1]辛烷-3-甲胺衍生物作为D2和D3多巴胺和5HT1A和5HT2血清素受体的配体

    公开(公告)号：US06221879B1

    公开(公告)日：2001-04-24

    申请号：US09529077

    申请日：2000-07-14

    申请人： Benoit Marabout ,  Mireille Sevrin ,  Pascal George ,  Jean-Pierre Merly ,  Daniele De Peretti ,  Jocelyne Roy ,  David Machnik

    发明人： Benoit Marabout ,  Mireille Sevrin ,  Pascal George ,  Jean-Pierre Merly ,  Daniele De Peretti ,  Jocelyne Roy ,  David Machnik

    IPC分类号： A61K3146

    CPC分类号： C07D451/02 ,  A61K31/36 ,  A61K31/46

    摘要： Compounds of general formula (I) in which U represents a group of general formula (A) or (B) in which formulae V represents a hydrogen or halogen atom, a (C1-C3)alkyl group or one or two (C1-C3)alkoxy groups, W and X each represent, respectively, either two oxygen atoms, or an oxygen atom and a CH2 group, or a CH2 group and an oxygen atom, or an oxygen atom and a CO group, n represents the number 0 or 1, R represents either a propyl group when U represents a group of general formula (A), or a hydrogen atom or a (C1-C3)alkyl group when U represents a group of general formula (B), Y represents one or more atoms or groups chosen from the following: hydrogen, halogen, (C1-C3)alkyl and (C1-C3)alkoxy, Z represents two hydrogen atoms or an oxygen atom.

    摘要翻译： 其中U表示通式（A）或（B）的基团的通式（I）的化合物，其中式V表示氢或卤素原子，（C1-C3）烷基或一个或两个（C1-C3 ）烷氧基，W和X分别表示两个氧原子，或氧原子和CH2基团，或CH2基团和氧原子，或氧原子和CO基团，n表示数字0或 1，当U表示通式（A）的基团时，当U表示通式（A）的基团时，R表示丙基，或者当U表示通式（B）的基团时，R表示氢原子或（C1-C3）烷基），Y表示一个或多个 原子或基团：氢，卤素，（C1-C3）烷基和（C1-C3）烷氧基，Z表示两个氢原子或氧原子。

    9H-imidazo[1,2-A]benzimidazole-3-acetamide derivatives, their preparation and their therapeutic application
    4.
    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。

    (4-piperidyl)methyl-2,3-dihydro-1H-isoindole and -2,3,4,5-tetrahydro-1H-benzazepine derivatives, their preparation and their application in therapy
    8.
    发明授权
    (4-piperidyl)methyl-2,3-dihydro-1H-isoindole and -2,3,4,5-tetrahydro-1H-benzazepine derivatives, their preparation and their application in therapy 失效
    （4-哌啶基）甲基-2,3-二氢-1H-茚并-2,3,4,5-四氢-1H-苯并恶嗪衍生物及其制备及其在治疗中的应用

    公开(公告)号：US5096900A

    公开(公告)日：1992-03-17

    申请号：US503941

    申请日：1990-02-08

    申请人： Pascal George ,  Mireille Sevrin ,  Michel Mangane

    发明人： Pascal George ,  Mireille Sevrin ,  Michel Mangane

    IPC分类号： C07D401/06

    CPC分类号： C07D401/06

    摘要： A benzazepine derivative which is a compound of formula (I): ##STR1## in which: each of m and n denotes the number 1, oreach of m and n denoted the number 2, orm denotes the number 3 and n denoted the number 1; andR denotes hydrogen or a group of formula --Z--R' in which Z denotes a --CO-- or --CH.sub.2 -- group and R' denotes a phenyl group which is unsubstituted or substituted with from one to three substituents selected from halogen atoms, linear or branch (C.sub.1 -C.sub.3) groups and linear or branched (C.sub.1 -C.sub.3) alkoxy groups,or a pharmacologically acceptable acid addition salt.

    摘要翻译： 作为式（I）的化合物的苯并氮杂衍生物：其中：m和n分别表示数1，或m和n分别表示数2，或m表示数3，n表示 1号; 并且R表示氢或式-ZR'的基团，其中Z表示-CO-或-CH2-基团，R'表示未取代的或被1至3个选自以下的取代基取代的苯基：卤原子，直链或 支链（C1-C3）基团和直链或支链（C1-C3）烷氧基，或药理学上可接受的酸加成盐。

    2,3-dihydro-1H-isoindole derivatives and their application in therapy
    9.
    发明授权
    2,3-dihydro-1H-isoindole derivatives and their application in therapy 失效
    2,3-二氢-1H-茚-2-酮衍生物及其在治疗中的应用

    公开(公告)号：US5081128A

    公开(公告)日：1992-01-14

    申请号：US377929

    申请日：1989-07-11

    申请人： Pascal George ,  Mireille Sevrin ,  Michel Mangane ,  Jean-Pierre Merly ,  Dennis Bigg

    发明人： Pascal George ,  Mireille Sevrin ,  Michel Mangane ,  Jean-Pierre Merly ,  Dennis Bigg

    IPC分类号： A61K31/4427 ,  A61K31/445 ,  A61K31/55 ,  A61P43/00 ,  C07D401/06

    CPC分类号： C07D401/06

    摘要： A benzazepine derivative which is a compound of formula (I): ##STR1## in which each of m and n denotes the number 1, oreach of m and n denotes the number 2, orm denotes the number 3 and n denotes the number 1; and R denotes hydrogen or a group of formula --Z--R' in which Z denotes a --CO-- or --CH.sub.2 -- group and R' denotes a phenyl group which is unsubtituted or substituted with from one to three substituents selected from halogen atoms, linear or branch (C.sub.1 -C.sub.3) alkyl groups and linear or branched (C.sub.1 -C.sub.3) alkoxy groups, or a pharmacologically acceptable acid addition salt.

    摘要翻译： 作为式（I）的化合物的苯并吖庚因衍生物：其中m和n各自表示数1，或m和n各自表示数2，或m表示数3，n表示数 1; 并且R表示氢或式-ZR'的基团，其中Z表示-CO-或-CH2-基，R'表示未取代或被一至三个选自以下的取代基取代的苯基：卤原子，直链或 支链（C1-C3）烷基和直链或支链（C1-C3）烷氧基，或药理学上可接受的酸加成盐。

    2-[(4-piperidyl)methyl]-1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indole derivatives, and their application in treating depressive state, anxiety state or hypertension
    10.
    发明授权
    2-[(4-piperidyl)methyl]-1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indole derivatives, and their application in treating depressive state, anxiety state or hypertension 失效
    2 - [（4-哌啶基）甲基] -1,2,3,4-四氢-9H-吡啶并[3,4-b]吲哚衍生物及其在治疗抑郁状态，焦虑状态或高血压中的应用

    公开(公告)号：US4977159A

    公开(公告)日：1990-12-11

    申请号：US228751

    申请日：1988-08-05

    申请人： Mireille Sevrin ,  Pascal George ,  Jacques Menin ,  Claude Morel ,  Dennis Bigg

    发明人： Mireille Sevrin ,  Pascal George ,  Jacques Menin ,  Claude Morel ,  Dennis Bigg

    IPC分类号： A61K31/445 ,  A61P9/00 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P43/00 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： A compound which is a pyrido[3,4-b]derivative of formula (I) ##STR1## in which R is a hydrogen atom or an alkyl carbonyl, arylalkylcarbonyl or arylcarbonyl group of formula COR.sub.1 wherein R.sub.1 is a C.sub.1 -C.sub.6 alkyl group, a benzyl group or a phenyl group unsubstituted or substituted with 1 to 3 substituents chosen from halogen atoms and trifluoromethyl, C.sub.1 -C.sub.3 alkyl and C.sub.1 -C.sub.3 alkoxy groups or R is an alkoxycarbonyl or benzyloxycarbonyl group of formula COOR.sub.2 wherein R.sub.2 is a C.sub.1 -C.sub.6 alkyl group or a benzyl group, or R is a substituted aminocarbonyl group of formula CONHR.sub.3 wherein R.sub.3 is a C.sub.1 -C.sub.6 alkyl group or a phenyl group, or R is an arylsulphonyl group of formula SO.sub.2 R.sub.4 wherein R.sub.4 is a phenyl group, or a pharmacologically acceptable acid addition salt thereof useful for treating hypertension, depressive state or anxiety state.

    摘要翻译： 化合物，其是式（I）的吡啶并[3,4-b]衍生物，其中R是氢原子或式COR1的烷基羰基，芳基烷基羰基或芳基羰基，其中R1是C1- C6烷基，苄基或未取代的或被1至3个选自卤素原子和三氟甲基，C1-C3烷基和C1-C3烷氧基的取代基取代的苯基，或者R是式COOR2的烷氧基羰基或苄氧基羰基，其中R2是 C 1 -C 6烷基或苄基，或R是式CONHR 3的取代的氨基羰基，其中R 3是C 1 -C 6烷基或苯基，或R是式SO 2 R 4的芳基磺酰基，其中R 4是苯基 ，或其可用于治疗高血压，抑郁状态或焦虑状态的药理学上可接受的酸加成盐。