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23 条记录 (耗时 0.03 秒)

    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。

    Pyridoindole derivatives
    3.
    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。

    Derivatives of fluorenes and fluoranthenes and process for their preparation
    4.
    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。

    Substituted 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyrimidinyl-2,3-dihydroimidazo [1,2-a]pyrimidin-5(1H)one derivatives for neurodegenerative disorders
    7.
    发明授权
    Substituted 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyrimidinyl-2,3-dihydroimidazo [1,2-a]pyrimidin-5(1H)one derivatives for neurodegenerative disorders 失效
    取代的2-嘧啶基-6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮和7-嘧啶基-2,3-二氢咪唑并[1,2-a]嘧啶-5（1H） 神经变性疾病的衍生物

    公开(公告)号：US07388005B2

    公开(公告)日：2008-06-17

    申请号：US10490136

    申请日：2002-09-19

    申请人： Thierry Gallet ,  Patrick Lardenois ,  Alistair Lochead ,  Séverine Marguerie ,  Alain Nedelec ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

    发明人： Thierry Gallet ,  Patrick Lardenois ,  Alistair Lochead ,  Séverine Marguerie ,  Alain Nedelec ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

    IPC分类号： A61K31/551 ,  A61K31/519 ,  C07D487/04 ,  A61P25/28

    CPC分类号： A61K31/519 ,  A61K31/551 ,  C07D487/04

    摘要： The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein: X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; y represents a bond, an ethenylene group, an ethynylene group, an oxygen atom, a sulphur atom, a sulfonyl group, a sulfoxide group, a carbonyl group, a nitrogen atom being optionally; or a methylene group optionally substituted; R1 represents a pyrimidine group optionally substituted; R2 may represent a C1-6 alkyl group optionally substituted by a C6,10 aryloxy or a C6,10 arylamino group; a C3-6 cycloalkyl group, a C1-4 alkylthio group, a C1-4 alkoxy group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a phenylthio group, a benzyl group, a benzene ring, an indan ring, a 5,6,7,8-tetrahydronaphthalene ring, a naphthalene ring, a pyridine ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring; R3 and R4 represents each independently a hydrogen atom, C1-6 alkyl group, a hydroxy group, a C1-4 alkoxy group or a halogen atom; R5 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β3 or GSK3β3 and cdk5/p25, such as Alzheimer disease.

    摘要翻译： 本发明涉及由式（I）表示的嘧啶酮衍生物或其盐，其中：X表示两个氢原子，硫原子，氧原子或C 1-12烷基和氢 原子; y表示键，亚乙烯基，亚乙炔基，氧原子，硫原子，磺酰基，亚砜基，羰基，任选的氮原子; 或任选取代的亚甲基; R1表示任选取代的嘧啶基团; R 2可以表示任选被C 6,10芳氧基或C 6,10芳基氨基取代的C 1-6烷基; C 3-6环烷基，C 1-4烷硫基，C 1-4烷氧基，C 1 -C 4烷氧基， 1-2个全卤代烷基，C 1-3卤代烷基，苯硫基，苄基，苯环，茚满环，5,6,7， 8-四氢萘环，萘环，吡啶环，吡咯环，噻吩环，呋喃环或咪唑环; R 3和R 4各自独立地表示氢原子，C 1-6烷基，羟基，C 1-4烷氧基或卤素原子; R5表示氢原子，C 1-6烷基或卤素原子。 本发明还涉及包含所述衍生物或其盐作为活性成分的药物，其用于预防和/或治疗由GSK3β3或GSK3β3和cdk5 / p25的异常活性引起的神经变性疾病，例如阿尔茨海默病 。