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60 条记录 (耗时 0.032 秒)

    Carbamate derivatives of alkyl-heterocycles, preparation thereof and therapeutic use thereof
    54.
    发明授权
    Carbamate derivatives of alkyl-heterocycles, preparation thereof and therapeutic use thereof 有权
    烷基杂环氨基甲酸酯衍生物，其制备及其治疗用途

    公开(公告)号：US08716289B2

    公开(公告)日：2014-05-06

    申请号：US13129235

    申请日：2009-11-13

    申请人： Ahmed Abouabdellah ,  Nathalie Chereze ,  Aude Fayol ,  Mourad Saady ,  Julien Vache ,  Corinne Veronique ,  Philippe Yaiche

    发明人： Ahmed Abouabdellah ,  Nathalie Chereze ,  Aude Fayol ,  Mourad Saady ,  Julien Vache ,  Corinne Veronique ,  Philippe Yaiche

    IPC分类号： A61K31/47 ,  A61K31/497 ,  A61K31/498 ,  A61K31/501 ,  A61K31/502 ,  A61K31/506

    CPC分类号： C07D417/14 ,  C07D401/14 ,  C07D403/14 ,  C07D407/14 ,  C07D413/12 ,  C07D413/14

    摘要： Compound corresponding to general formula (I): in which R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or NR8R9 group; n is an integer equal to 1, 2 or 3 and m is an integer equal to 1 or 2; A is a covalent bond or a C1-8-alkylene group; R1 is a phenyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, triazinyl, naphthyl, quinolinyl, isoquinolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, cinnolinyl or naphthyridinyl group, this group being optionally substituted; R3 is a hydrogen or fluorine atom, a C1-6-alkyl group or a tritluoromethyl group; R4 is a group selected from furanyl, pyrrolyl, thienyl, isothiazolyl, oxazolyl, isoxazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, imidazole, triazolyl, tetrazolyl, oxazolone, oxazolidinone, isoxazolone, isoxazolidinone, isothiazolone, isothiazolidinone, imidazolone, imidazolidinone, pyrazolone, pyrazolidinone, oxadiazolone, thiadiazolone and triazolone, this group being optionally substituted; in the form of a base or of an addition salt with an acid. Therapeutic use.

    摘要翻译： 对应于通式（I）的化合物：其中R 2为氢或氟原子或羟基，氰基，三氟甲基，C 1-6 - 烷基，C 1-6 - 烷氧基或NR 8 R 9基团; n是等于1,2或3的整数，m是等于1或2的整数; A是共价键或C 1-8亚烷基; R 1是苯基，吡啶基，哒嗪基，嘧啶基，吡嗪基，三嗪基，萘基，喹啉基，异喹啉基，酞嗪基，喹唑啉基，喹喔啉基，噌啉基或萘啶基， R3是氢或氟原子，C1-6烷基或三氟甲基; R4是选自呋喃基，吡咯基，噻吩基，异噻唑基，恶唑基，异恶唑基，吡唑基，恶二唑基，噻二唑基，咪唑，三唑基，四唑基，恶唑酮，恶唑烷酮，异恶唑酮，异恶唑烷酮，异噻唑酮，异噻唑烷酮，咪唑啉酮，咪唑烷酮，吡唑啉酮，吡唑烷酮， 恶二唑酮，噻二唑酮和三唑酮，该基团任选被取代; 以碱的形式或与酸的加成盐形式。 治疗用途。

    Heteroaryl substituted 2-pyridinyl and 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one derivatives
    59.
    发明申请
    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：US20050222172A1

    公开(公告)日：2005-10-06

    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： A61K31/519 ,  A61P3/04 ,  A61P3/10 ,  A61P9/10 ,  A61P17/14 ,  A61P21/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P25/34 ,  A61P27/02 ,  A61P27/06 ,  A61P35/00 ,  A61P43/00 ,  C07D487/04 ,  C07D519/00

    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: (1) 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：（1）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 。

    1-[alkyl 1-[heteroaryl )alkyl] and 1-[ aryl) alkyl]-7-( pyrimidin-4-yl) imadazo [1,2-a] pyrimidin-5(1h)-one derivatives
    60.
    发明申请
    1-[alkyl 1-[heteroaryl )alkyl] and 1-[ aryl) alkyl]-7-( pyrimidin-4-yl) imadazo [1,2-a] pyrimidin-5(1h)-one derivatives 失效
    1- [烷基1- [杂芳基]烷基]和1- [芳基]烷基] -7-（嘧啶-4-基）咪唑并[1,2-a]嘧啶-5（1h） - 酮衍生物

    公开(公告)号：US20050119280A1

    公开(公告)日：2005-06-02

    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： A61K31/437 ,  A61K31/519 ,  A61P3/04 ,  A61P3/10 ,  A61P9/10 ,  A61P17/14 ,  A61P25/02 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P27/06 ,  A61P35/00 ,  C07D487/04

    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。