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93 条记录 (耗时 0.03 秒)

    2,3-dihydrofuro [3,2-.beta.]pyridin, preparation and application thereof in therapy
    43.
    发明授权
    2,3-dihydrofuro [3,2-.beta.]pyridin, preparation and application thereof in therapy 失效
    2,3-二氢呋喃并[3,2-b]吡啶，其制备及其在治疗中的应用

    公开(公告)号：US6143761A

    公开(公告)日：2000-11-07

    申请号：US381098

    申请日：1999-09-15

    申请人： Alistair Lochead ,  Samir Jegham ,  Frederic Galli ,  Thierry Gallet

    发明人： Alistair Lochead ,  Samir Jegham ,  Frederic Galli ,  Thierry Gallet

    IPC分类号： A61K31/4355 ,  A61P1/00 ,  A61P25/00 ,  A61P43/00 ,  C07D491/04 ,  C07D491/048 ,  A61K31/435

    CPC分类号： C07D491/04

    摘要： Compounds corresponding to the general formula (I) ##STR1## in which R.sub.1 represents a hydrogen atom, a (C.sub.1 -C.sub.6)alkyl group or a phenyl(C.sub.1 -C.sub.4)alkyl group, R.sub.2 represents a hydrogen atom or a (C.sub.1 -C.sub.6)alkyl group and R.sub.3, R.sub.4 and R.sub.5 each represent, independently of one another, a hydrogen or halogen atom or a trifluoromethyl, cyano, hydroxyl, (C.sub.1 -C.sub.6)alkyl or (C.sub.1 -C.sub.6)alkoxy group. Application in therapeutics.

    摘要翻译： PCT No.PCT / FR98 / 00531 Sec。 371日期1999年9月15日 102（e）1999年9月15日PCT提交1998年3月17日PCT公布。 出版物WO98 / 42713 日期：1998年10月1日对应于通式（I）的化合物，其中R1表示氢原子，（C1-C6）烷基或苯基（C1-C4）烷基，R2表示氢原子或（C1 -C 6）烷基，R 3，R 4和R 5各自独立地表示氢或卤素原子或三氟甲基，氰基，羟基，（C 1 -C 6）烷基或（C 1 -C 6）烷氧基。 在治疗中的应用。

    7-(Pyrimidin-4-yl)-Imidazo[1,2-a]Pyrimidin-5(1H)-ones as GSK3β inhibitors
    49.
    发明授权
    7-(Pyrimidin-4-yl)-Imidazo[1,2-a]Pyrimidin-5(1H)-ones as GSK3β inhibitors 失效
    7-（嘧啶-4-基） - 咪唑并[1,2-a]嘧啶-5（1H） - 酮作为GSK3beta抑制剂

    公开(公告)号：US07429663B2

    公开(公告)日：2008-09-30

    申请号：US10504679

    申请日：2003-02-26

    申请人： Alistair Lochead ,  Mourad Saady ,  Philippe Yaiche

    发明人： Alistair Lochead ,  Mourad Saady ,  Philippe Yaiche

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/04 ,  A61P3/10 ,  A61P25/28

    CPC分类号： C07D487/04

    摘要： The invention relates to a imidazo[1,2-a]pyrimidone derivative represented by formula (I) or a salt thereof: R1 wherein X represents a bond, an ethenylene group, an ethenylene group, a methylene group optionally substituted; a carbonyl group, an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group or a nitrogen atom being optionally substituted; R1 represents a 2, 4 or 5-pyrimidinyl optionally substituted; R2 represents a C1-6 alkyl group, a C1-2 perhalogenated alkyl group,a C1-3 halogenated alkyl group, a benzyl group, a benzene ring, a naphthalene ring, 5,6,7,8-tetrahydronaphthalene ring, a pyridine ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring, the benzyl group and the rings being optionally substituted; and n represents 0 to 3. 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 GSK3β, such as Alzheimer disease.

    摘要翻译： 本发明涉及由式（I）表示的咪唑并[1,2-a]嘧啶酮衍生物或其盐：R 1其中X表示键，亚乙烯基，亚乙烯基， 任选取代的亚甲基; 羰基，氧原子，硫原子，磺酰基，亚砜基或任选取代的氮原子; R 1表示任选取代的2,4或5-嘧啶基; R 2表示C 1-6烷基，C 1-12全卤代烷基，C 1-3烷基， 卤代烷基，苄基，苯环，萘环，5,6,7,8-四氢萘环，吡啶环，吲哚环，吡咯环，噻吩环，呋喃环或呋喃环 咪唑环，苄基和环任选被取代; 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GSK3beta异常活动引起的神经变性疾病，例如阿尔茨海默氏症 疾病。

    Heteroaryl substituted 2-pyridinyl and 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one derivatives
    50.
    发明授权
    Heteroaryl substituted 2-pyridinyl and 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one derivatives 失效
    杂芳基取代的2-吡啶基和2-嘧啶基-6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮衍生物

    公开(公告)号：US07232827B2

    公开(公告)日：2007-06-19

    申请号：US10504677

    申请日：2003-02-26

    申请人： Alistair Lochead ,  Alain Nedelec ,  Mourad Saady ,  Philippe Yaiche

    发明人： Alistair Lochead ,  Alain Nedelec ,  Mourad Saady ,  Philippe Yaiche

    IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D471/00 ,  C07D487/00

    CPC分类号： A61K31/519 ,  A01N43/90 ,  C07D487/04

    摘要： The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein: (I) 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 or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring optionally substituted; R2 represents a heterocyclic bicyclic rings, having 1–4 heteroatoms selected from an oxygen atom, a sulfur atom and a nitrogen atom and having 5–9 carbon atoms, of formula (II) R3 represents a hydrogen atom, a C1-6 alkyl group, a hydroxy group, a C1-4 alkoxy group or a halogen atom; R4 represents a hydrogen atom, a C1-6 alkyl group, a C1-4 alkoxy 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 GSK3β or GSK3β 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：（I）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，亚乙炔基或任选取代的亚甲基; R1表示2,3或4-吡啶环或任选取代的2,4或5-嘧啶环; R 2表示具有1-4个选自氧原子，硫原子和氮原子并且具有5-9个碳原子的杂原子的式（II）的杂环双环，R 3表示氢原子，C 1 -C 1-6烷基，羟基，C 1-4烷氧基或卤素原子; R 4表示氢原子，C 1-6烷基，C 1-4烷氧基或卤素原子。 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GSK3β或GSK3β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