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    Pyridoindole derivatives
    2.
    发明授权
    Pyridoindole derivatives 失效
    吡啶并吲哚衍生物

    公开(公告)号：US4272539A

    公开(公告)日：1981-06-09

    申请号：US112212

    申请日：1980-01-15

    申请人： Gabor I. Koletar ,  Jonathan R. Frost ,  Regis Dupont ,  Patrick Lardenois ,  Claude Morel ,  Henry Najer

    发明人： Gabor I. Koletar ,  Jonathan R. Frost ,  Regis Dupont ,  Patrick Lardenois ,  Claude Morel ,  Henry Najer

    IPC分类号： A61K31/435 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  C07D471/04

    CPC分类号： C07D471/04 ,  Y10S514/923

    摘要： Pyridoindole derivatives of formula ##STR1## n=0 or 1; R.sub.1 =H, Hal, alk, alk-O-, CF.sub.3 ; R.sub.2 =--COOalk; --CONHR.sub.5 (R.sub.5 =H or various substituents); R.sub.3 =H, alk, --COOalk; R.sub.4 =H, Ac, alk, --CONHR.sub.6 (R.sub.6 =H or various substituents), and acid addition salts, except certain known compounds, are useful in treating anoxia and depression and in psychotropic therapy. They are prepared from tryptamine or a derivative thereof by reaction thereof with a pyruvic ester or 3-ethoxycarbonyl-1,2-dioxo-1-ethoxypropane to form compounds in which R.sub.4 is H and R.sub.2 is --COOalk. These compounds are reacted with amines, isocyanates or usual N-acylating or N-alkylating reagents to prepare the other compounds.

    摘要翻译： 式（I）的吡啶并吲哚衍生物n = 0或1; R1 = H，Hal，alk，alk-O-，CF3; R2 = -COOalk; -CONHR5（R5 = H或各种取代基）; R3 = H，alk，-COOalk; R4 = H，Ac，alk，-CONHR6（R6 = H或各种取代基），除了某些已知化合物之外，酸加成盐可用于治疗缺氧和抑郁症以及精神药物治疗。 它们由色胺或其衍生物通过与丙酮酸酯或3-乙氧基羰基-1,2-二氧代-1-乙氧基丙烷的反应制备，以形成其中R 4为H且R 2为-COOalk的化合物。 这些化合物与胺，异氰酸酯或通常的N-酰化或N-烷基化试剂反应以制备其它化合物。

    Alpha.sub.2 -antagonistic 2-(4,5-dihydro-1H-imidazol-2-yl)-pyrrolo[3,2,1-hi]indoles
    5.
    发明授权
    Alpha.sub.2 -antagonistic 2-(4,5-dihydro-1H-imidazol-2-yl)-pyrrolo[3,2,1-hi]indoles 失效
    α2-拮抗性2-（4,5-二氢-1H-咪唑-2-基） - 吡咯并[3,2,1-hi]吲哚

    公开(公告)号：US4617313A

    公开(公告)日：1986-10-14

    申请号：US770079

    申请日：1985-08-28

    申请人： Dennis Bigg ,  Claude Morel ,  Mireille Sevrin

    发明人： Dennis Bigg ,  Claude Morel ,  Mireille Sevrin

    IPC分类号： C07D209/08 ,  C07D487/06 ,  A61K31/415

    CPC分类号： C07D487/06 ,  C07D209/08

    摘要： Pyrrolo[3,2,1-hi]indole derivatives, in the form of racemates or optically active isomers, of formula (I) ##STR1## in which R is a hydrogen atom or C.sub.1 -C.sub.4 alkyl and R.sub.1 and R.sub.2, which may be the same or different, are hydrogen, halogen or C.sub.1 -C.sub.4 alkyl and their pharmaceutically acceptable acid addition salts are useful as .alpha..sub.2 -antagonists.

    摘要翻译： 吡咯并[3,2,1-hi]吲哚衍生物，其为式（I）的外消旋物或光学活性异构体，其中R是氢原子或C 1 -C 4烷基，R 1和R 2 可以相同或不同的是氢，卤素或C 1 -C 4烷基及其药学上可接受的酸加成盐可用作α2拮抗剂。

    Derivatives of fluorenes and fluoranthenes and process for their preparation
    6.
    发明授权
    Derivatives of fluorenes and fluoranthenes and process for their preparation 失效
    芴和荧蒽的衍生物及其制备方法

    公开(公告)号：US4277476A

    公开(公告)日：1981-07-07

    申请号：US60857

    申请日：1979-07-26

    申请人： Regis DuPont ,  Patrick Lardenois ,  Claude Morel ,  Jonathan Frost ,  Gabor I. Koletar

    发明人： Regis DuPont ,  Patrick Lardenois ,  Claude Morel ,  Jonathan Frost ,  Gabor I. Koletar

    IPC分类号： C07D471/04 ,  C07D471/14 ,  C07D471/16 ,  A01N43/48 ,  A61K31/495

    CPC分类号： C07D471/04 ,  C07D471/14

    摘要： Derivatives of fluorenes and fluoranthenes, in the form of racemates or of enantiomers, of the formula (I) ##STR1## in which n is 1 or 2, R.sub.1 is a hydrogen or halogen atom or an alkyl or alkoxy radical, R.sub.2 is a hydrogen atom or an alkyl, cycloalkyl, cycloalkylalkyl, benzyl, halogenobenzyl, alkylbenzyl, alkoxybenzyl, acyl, alkoxycarbonyl or alkylaminocarbonyl radical, R.sub.3 is a hydrogen atom or an alkyl radical, R.sub.4 is a hydrogen atom or an alkyl, acyl or aroyl radical, the alkyl and alkoxy radicals or parts of radicals having from 1 to 4 carbon atoms and pharmaceutically acceptable acid addition salts thereof, are therapeutically valuable as anti-anoxia and psychotropic agents.

    摘要翻译： 式（I）其中n为1或2的式（I）的外消旋物或对映异构体的芴和荧蒽衍生物，R1为氢或卤素原子或烷基或烷氧基，R2 是氢原子或烷基，环烷基，环烷基烷基，苄基，卤代苄基，烷基苄基，烷氧基苄基，酰基，烷氧基羰基或烷基氨基羰基，R3是氢原子或烷基，R4是氢原子或烷基，酰基或芳酰基 ，烷基和烷氧基或具有1至4个碳原子的基团部分及其药学上可接受的酸加成盐作为抗缺氧和精神药物具有治疗价值。

    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
    7.
    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。

    2-thienylimidazo[2,1-.beta.]benzothiazole-3-acetic acid derivatives, their preparation and their use
    8.
    发明授权
    2-thienylimidazo[2,1-.beta.]benzothiazole-3-acetic acid derivatives, their preparation and their use 失效
    2-噻吩基咪唑并[2,1-β]苯并噻唑-3-乙酸衍生物，其制备及其应用

    公开(公告)号：US5418248A

    公开(公告)日：1995-05-23

    申请号：US175249

    申请日：1993-12-29

    申请人： Mireille Sevrin ,  Claude Morel ,  Michel Mangane ,  Pascal George

    发明人： Mireille Sevrin ,  Claude Morel ,  Michel Mangane ,  Pascal George

    IPC分类号： A61K31/425 ,  A61P25/08 ,  A61P25/20 ,  C07D233/84 ,  C07D277/82 ,  C07D513/04

    CPC分类号： C07D513/04

    摘要： Compounds of the formula: ##STR1## in which R.sub.1 represents a hydroxy group, a C.sub.1 -C.sub.4 alkoxy group or an amino group of general formula --NR.sub.4 R.sub.5 in which R.sub.4 and R.sub.5 each represent, independently of each other, a hydrogen atom, a straight or branched C.sub.1 -C.sub.4 alkyl group, an allyl group or a methoxyethyl group, or alternatively --NR.sub.4 R.sub.5 represents a heterocycle containing 3 to 6 carbon atoms,Y represents a thienyl group optionally substituted by an alkyl group, andX represents a hydrogen or halogen atom,are useful as anticonvulsants and auxiolytics.

    摘要翻译： 下式的化合物：其中R 1表示羟基，C 1 -C 4烷氧基或通式-NR 4 R 5的氨基，其中R 4和R 5各自独立地表示氢原子 直链或支链C 1 -C 4烷基，烯丙基或甲氧基乙基，或者-NR4R5表示含有3至6个碳原子的杂环，Y表示任选被烷基取代的噻吩基，X表示氢 或卤素原子，可用作抗惊厥药和辅助溶剂。

    Pyridoindole derivatives
    10.
    发明授权
    Pyridoindole derivatives 失效
    吡啶并吲哚衍生物

    公开(公告)号：US4336256A

    公开(公告)日：1982-06-22

    申请号：US184070

    申请日：1980-09-04

    申请人： Gabor I. Koletar ,  Jonathan B. Frost ,  Regis DuPont ,  Patrick Lardenois ,  Claude Morel ,  Henry Najer

    发明人： Gabor I. Koletar ,  Jonathan B. Frost ,  Regis DuPont ,  Patrick Lardenois ,  Claude Morel ,  Henry Najer

    IPC分类号： A61K31/435 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  C07D471/04

    CPC分类号： C07D471/04 ,  Y10S514/923

    摘要： Pyridoindole derivatives of formula ##STR1## n=0 or 1; R.sub.1 =H, Hal, alk, alk--O--, CF.sub.3 ; R.sub.2 =--COOalk; --CONHR.sub.5 (R.sub.5 =H or various substituents); R.sub.3 =H, alk, --COOalk; R.sub.4 =H, Ac, alk, --CONHR.sub.6 (R.sub.6 =H or various substituents), and acid addition salts, except certain known compounds, are useful in treating anoxia and depression and in psychotropic therapy. They are prepared from tryptamine or a derivative thereof by reaction thereof with a pyruvic ester or 3-ethoxycarbonyl-1,2-dioxo-1-ethoxypropane to form compounds in which R.sub.4 is H and R.sub.2 is --COOalk. These compounds are reacted with amines, isocyanates or usual N-acylating or N-alkylating reagents to prepare the other compounds.

    摘要翻译： 式（I）的吡啶并吲哚衍生物n = 0或1; R1 = H，Hal，alk，alk-O-，CF3; R2 = -COOalk; -CONHR5（R5 = H或各种取代基）; R3 = H，alk，-COOalk; R4 = H，Ac，alk，-CONHR6（R6 = H或各种取代基），除了某些已知化合物之外，酸加成盐可用于治疗缺氧和抑郁症以及精神药物治疗。 它们由色胺或其衍生物通过与丙酮酸酯或3-乙氧基羰基-1,2-二氧代-1-乙氧基丙烷的反应制备，以形成其中R 4为H且R 2为-COOalk的化合物。 这些化合物与胺，异氰酸酯或通常的N-酰化或N-烷基化试剂反应以制备其它化合物。