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373 条记录 (耗时 0.02 秒)

    PROCEDE DE PREPARATION DE DERIVES DE BROMOMETHYL-BIPHENYLE
    15.
    发明授权
    PROCEDE DE PREPARATION DE DERIVES DE BROMOMETHYL-BIPHENYLE 有权
    PROCESS FOR溴联苯联系衍生物的制备

    公开(公告)号：EP1032557B1

    公开(公告)日：2003-09-10

    申请号：EP98954537.1

    申请日：1998-11-09

    申请人： SANOFI-SYNTHELABO

    发明人： BIARD, Michel ,  CASTRO, Bertrand

    IPC分类号： C07C253/30 ,  C07C255/50

    CPC分类号： C07C253/30 ,  Y02P20/55 ,  C07C255/50

    摘要： The invention concerns a method for preparing 4'-bromomethyl-biphenyl derivatives of general formula (I) in which R is as defined in Claim 1, characterised in that it consists in reacting in a biphasic medium and under the effect of light irradiation, a bromination agent selected among bromine, N-bromoacetamide, N-bromophtalimide, N-bromomaleimide, a N-bromosulphonamide, N-bromosuccinimide, 1,3-dibromo-5,5-dimehtylhydantoin and an alkaline metal bromhydric/bromate acid system with a biphenyl derivative of general formula (II) in which R has the same meaning as above, thereby obtaining the desired compound.

    Substituted 2-pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyridinyl-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)one derivatives
    16.
    发明公开
    Substituted 2-pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyridinyl-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)one derivatives 审中-公开
    取代基2-吡啶基-6,7,8,9-四氢嘧啶并[1,2-a嘧啶-4-基]和7-吡啶基-2,3-二氢咪唑并[1,2-a嘧啶-5（1H）

    公开(公告)号：EP1340761A1

    公开(公告)日：2003-09-03

    申请号：EP02290489.0

    申请日：2002-02-28

    申请人： SANOFI-SYNTHELABO ,  MITSUBISHI PHARMA CORPORATION

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

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P25/00

    CPC分类号： 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 C 1-2 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 hydroxyiminomethylene group, a dioxolan group, a nitrogen atom being optionally substituted; or a methylene group optionally substituted;
    R1 represents a 2, 3 or 4-pyridine ring optionally substituted;
    R2 may represent a C 1-6 alkyl group optionally; a C 3-6 cycloalkyl group, a C 1-4 alkylthio group, a C 1-4 alkoxy group, a C 1-2 perhalogenated alkyl group, a C 1-3 halogenated alkyl group, a phenylthio group, a benzyl group, a phenyl ring, a 5,6,7,8-tetrahydronaphthyl ring, a naphthyl 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, a C 1-6 alkyl group, a hydroxy group, a C 1-4 alkoxy group or a halogen atom;
    R5 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; with the proviso that when R3 and R4 represent each a hydrogen atom then R5 is not a hydrogen 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：X表示两个氢原子，硫原子，氧原子或C 1-2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，羟基亚氨基亚甲基，二氧戊环，任选取代的氮原子; 或任选取代的亚甲基; R1表示任选取代的2,3或4-吡啶环; 任选地，R 2可以表示C 1-6烷基; C 3-6环烷基，C 1-4烷硫基，C 1-4烷氧基，C1-2全卤代烷基，C 1-3卤代烷基，苯硫基，苄基，苯环， 5,6,7,8-四氢萘基环，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，C1-6烷基或卤素原子; 条件是当R 3和R 4各自表示氢原子时，R 5不是氢原子。 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的预防和/或治疗，例如 阿尔茨海默病。

    DERIVES DE BENZIMIDAZOLE, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE
    17.
    发明公开
    DERIVES DE BENZIMIDAZOLE, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE 有权
    DEIV苯并咪唑，LEUR制剂和LEUR应用EN THERAPEUQUE

    公开(公告)号：EP1339719A1

    公开(公告)日：2003-09-03

    申请号：EP01997491.4

    申请日：2001-11-21

    申请人： SANOFI-SYNTHELABO

    发明人： BARTH, Francis ,  BICHON, Daniel ,  BOLKENIUS, Frank ,  VAN DORSSELAER, Viviane

    IPC分类号： C07D487/06 ,  A61K31/5517 ,  A61P9/00 ,  A61P25/00 ,  A61P29/00

    CPC分类号： C07D487/06

    摘要： The invention concerns benzimidazole derivatives of general formula (I), wherein: X represents a nitrogen atom or a carbon atom; when X represents a nitrogen atom, R3 represents in particular a hydrogen atom or a C1-C4 alkyl group; R4 represents in particular a hydrogen atom, a C1-C6 alkyl, C3-C7 cycloalkyl, 4-piperidyl, -(CH2)p-NR5R6, -(CH2)p-CONR5R6, -CO-(CH2)p-NR5R6, -(CH2)p-phenyl, -(CH2)p-morpholinyl, -(CH2)p-pyrrolidinyl, -(CH2)p-tetrahydro-isoquinoline, -(CH2)p-heteoraryl, heteroarylcarbonyl, phenylcarbonyl, C1-C6 alkylcarbonyl, -(-CH2)p-COOR', or phenylsulphonyl group; and when X represents a carbon atom, R3 represents a hydrogen atom, a -NR5R6, -NHCOR7, -CONHR5, -COR7, -NHCONH2, -OH or -CH2OH; R4 represents in particular a hydrogen atom, a -(CH2)p-phenyl group optionally substituted, a -(CH2)p-heteroaryl or a (CH2)tNR7R8 group. The compounds of formula (I) of the invention can be used for preparing a medicine for treating or preventing disorders wherein the PARP enzyme is involved.

    摘要翻译： 本发明涉及通式（I）的苯并咪唑衍生物，其中：X代表氮原子或碳原子; 当X代表氮原子时，R3特别代表氢原子或C1-C4烷基; R 4特别代表氢原子，C 1 -C 6烷基，C 3 -C 7环烷基，4-哌啶基， - （CH 2）p -NR 5 R 6， - （CH 2）p -CONR 5 R 6，-CO-（CH 2）p -NR 5 R 6， - （CH2）p-苯基， - （CH2）p-吗啉基， - （CH2）p-吡咯烷基， - （CH2）p-四氢异喹啉， - （CH2）p-杂芳酰基，杂芳基羰基，苯基羰基， - （ - CH 2）p -COOR'或苯磺酰基; 当X代表碳原子时，R 3代表氢原子，-NR 5 R 6，-NHCOR 7，-CONHR 5，-COR 7，-NHCONH 2，-OH或-CH 2 OH; R4特别表示氢原子，任选取代的 - （CH2）p-苯基， - （CH2）p-杂芳基或（CH2）tNR7R8基团。 本发明的式（I）化合物可用于制备用于治疗或预防PARP酶参与的病症的药物。

    Thiadiazolylalkoxyphenyl derivatives, their preparation and their use anti-picornaviral agents
    20.
    发明授权
    Thiadiazolylalkoxyphenyl derivatives, their preparation and their use anti-picornaviral agents 失效
    Thiadiazolylalkoxyphenyl衍生物，它们的制备以及它们作为抗小核糖核酸病毒装置

    公开(公告)号：EP0759755B1

    公开(公告)日：2003-08-13

    申请号：EP95919773.2

    申请日：1995-05-10

    申请人： SANOFI-SYNTHELABO

    发明人： ALDOUS, David J. ,  BAILEY, Thomas R. ,  DIANA, Guy Dominic ,  NITZ, Theodore J.

    IPC分类号： C07D417/12 ,  A61K31/41

    CPC分类号： C07D417/12

    摘要： Compounds of formula (I) wherein Thi is thiadiazolyl or thiadiazolyl substituted with alcoxy, fluoromethyl, difluoromethyl, trifluoromethyl, 1,1-difluoroethyl, halo, alkyl, cycloalkyl, hydroxyalkyl, or alkoxyalkyl; Y is alkylene bridge of 3-9 carbon atoms; R1 and R2 are each independently chosen from hydrogen, halo, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl, or cyano; R3 is alkoxycarbonyl, phenyl, alkyltetrazolyl or heterocyclyl chosen from benzoxazolyl, benzathiazolyl, thiadioazolyl, imidazolyl, dihydroimidazolyl, oxazolyl, thiazolyl, oxadiazolyl, pyrazolyl, isoxazolyl, isothiazolyl, furyl, triazolyl, thienyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, or substituted phenyl, or substituted heterocyclyl wherein the substitution is with alkyl, alkoxyalkyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, furyl, thienyl, or fluoroalkyl; or a pharmaceutically acceptable salt thereof are effective antipicornaviral agents.