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    Acylaminothiazole derivatives, their preparation and their therapeutic use
    1.
    发明授权
    Acylaminothiazole derivatives, their preparation and their therapeutic use 失效
    酰氨基噻唑衍生物，其制备及其治疗用途

    公开(公告)号：US07563903B2

    公开(公告)日：2009-07-21

    申请号：US11186507

    申请日：2005-07-21

    申请人： Pierre Despeyroux ,  Daniel Frehel ,  Bruno Schoentjes ,  Viviane Van Dorsselaer

    发明人： Pierre Despeyroux ,  Daniel Frehel ,  Bruno Schoentjes ,  Viviane Van Dorsselaer

    IPC分类号： A61K31/426 ,  C07D277/46

    CPC分类号： C07D417/12 ,  C07D277/46

    摘要： Compound corresponding to the general formula (I): in which, X represents an oxygen or sulphur atom; R1 represents a C1-10 alkyl group optionally substituted, a C3-7 cycloalkyl, thienyl, pyridinyl or pyrimidinyl group; the thienyl groups being optionally substituted; the phenyl group being optionally substituted; R2 represents a C1-6 alkyl group optionally substituted, a C3-7 cycloalkyl, piperidinyl, phenyl or pyridinyl group; the C3-7 cycloalkyl and piperidinyl groups being optionally substituted; the phenyl and pyridinyl groups being optionally substituted; R3 represents a hydrogen atom or a C1-6 alkyl group optionally substituted with a C3-7 cycloalkyl group; R4 represents a hydrogen atom or a C1-6 alkyl group; R5 and R5′ represent, independently of each other, a hydrogen or halogen atom, a hydroxyl or C1-3 alkyl group; or R5 and R5′ form together an oxo or oxime group such as: where R7 represents a hydrogen atom or a C1-3 alkyl; n represents an integer ranging from 0 to 3; and R6 represents, independently of each other when n=2 or 3, a hydrogen or halogen atom, a hydroxyl, C1-3 alkyl, C1-3 alkoxy, C1-3 fluoroalkyl or C1-3 fluoroalkoxy group; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. therapeutic application.

    摘要翻译： 对应于通式（I）的化合物：其中X表示氧或硫原子; R 1表示任选取代的C 1-10烷基，C 3-7环烷基，噻吩基，吡啶基或嘧啶基; 噻吩基任选被取代; 苯基任选被取代; R 2表示任选取代的C 1-6烷基，C 3-7环烷基，哌啶基，苯基或吡啶基; C3-7环烷基和哌啶基任选被取代; 苯基和吡啶基任选被取代; R3表示氢原子或任选被C 3-7环烷基取代的C 1-6烷基; R4表示氢原子或C1-6烷基; R5和R5'彼此独立地表示氢或卤素原子，羟基或C1-3烷基; 或R 5和R 5'一起形成氧基或肟基，例如：其中R 7表示氢原子或C 1-3烷基; n表示0〜3的整数， 当n = 2或3时，R 6表示独立地为氢或卤原子，羟基，C 1-3烷基，C 1-3烷氧基，C 1-3氟烷基或C 1-3氟烷氧基; 以碱的形式，与酸的加成盐，水合物或溶剂合物的治疗应用。

    Acylaminothiazole derivatives, their preparation and their therapeutic use
    2.
    发明申请
    Acylaminothiazole derivatives, their preparation and their therapeutic use 失效
    酰氨基噻唑衍生物，其制备及其治疗用途

    公开(公告)号：US20060052426A1

    公开(公告)日：2006-03-09

    申请号：US11186507

    申请日：2005-07-21

    申请人： Pierre Despeyroux ,  Daniel Frehel ,  Bruno Schoentjes ,  Viviane Van Dorsselaer

    发明人： Pierre Despeyroux ,  Daniel Frehel ,  Bruno Schoentjes ,  Viviane Van Dorsselaer

    IPC分类号： C07D277/18 ,  A61K31/426

    CPC分类号： C07D417/12 ,  C07D277/46

    摘要： Compound corresponding to the general formula (I): in which, X represents an oxygen or sulphur atom; R1 represents a C1-10 alkyl group optionally substituted, a C3-7 cycloalkyl, thienyl, pyridinyl or pyrimidinyl group; the thienyl groups being optionally substituted; the phenyl group being optionally substituted; R2 represents a C1-6 alkyl group optionally substituted, a C3-7 cycloalkyl, piperidinyl, phenyl or pyridinyl group; the C3-7 cycloalkyl and piperidinyl groups being optionally substituted; the phenyl and pyridinyl groups being optionally substituted; R3 represents a hydrogen atom or a C1-6 alkyl group optionally substituted with a C3-7 cycloalkyl group; R4 represents a hydrogen atom or a C1-6 alkyl group; R5 and R5′ represent, independently of each other, a hydrogen or halogen atom, a hydroxyl or C1-3 alkyl group; or R5 and R5′ form together an oxo or oxime group such as: where R7 represents a hydrogen atom or a C1-3 alkyl; n represents an integer ranging from 0 to 3; and R6 represents, independently of each other when n=2 or 3, a hydrogen or halogen atom, a hydroxyl, C1-3 alkyl, C1-3 alkoxy, C1-3 fluoroalkyl or C1-3 fluoroalkoxy group; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. therapeutic application.

    摘要翻译： 对应于通式（I）的化合物：

    Use of acylaminothiazole derivatives as therapeutic agents
    4.
    发明授权
    Use of acylaminothiazole derivatives as therapeutic agents 失效
    酰基氨基噻唑衍生物作为治疗剂的用途

    公开(公告)号：US07795289B2

    公开(公告)日：2010-09-14

    申请号：US11859443

    申请日：2007-09-21

    申请人： Sylvie Baltzer ,  Bruno Schoentjes ,  Viviane Van Dorsselaer

    发明人： Sylvie Baltzer ,  Bruno Schoentjes ,  Viviane Van Dorsselaer

    IPC分类号： A61K31/426

    CPC分类号： C07D417/12 ,  C07D277/56

    摘要： This invention discloses and claims a method of treatment of a disease as defined herein using a compound conforming to the general formula (I): Wherein R1, R2, R′2, R3, R4 and R5 are as described herein. Specifically, the compounds of the present invention exhibit an inhibitory effect on the production of β-amyloid peptide (β-A4) by inhibition of gamma protease. Therefore, the compounds of the present invention are useful in the treatment of pathologies such as senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, amyloid angiopathy and/or cerebrovascular disorders.

    摘要翻译： 本发明公开并要求使用符合通式（I）的化合物治疗本文定义的疾病的方法：其中R 1，R 2，R'2，R 3，R 4和R 5如本文所述。 具体地，本发明的化合物通过抑制γ蛋白酶表现出对β-淀粉样蛋白肽（＆bgr; -A4）的产生的抑制作用。 因此，本发明的化合物可用于治疗老年性痴呆，阿尔茨海默氏病，唐氏综合征，帕金森病，淀粉样血管病和/或脑血管障碍等病态。

    Acylaminothiazole derivatives, preparation and therapeutic use thereof
    5.
    发明授权
    Acylaminothiazole derivatives, preparation and therapeutic use thereof 失效
    酰氨基噻唑衍生物，其制备和治疗用途

    公开(公告)号：US07291636B2

    公开(公告)日：2007-11-06

    申请号：US11035803

    申请日：2005-01-14

    申请人： Sylvie Baltzer ,  Bruno Schoentjes ,  Viviane Van Dorsselaer

    发明人： Sylvie Baltzer ,  Bruno Schoentjes ,  Viviane Van Dorsselaer

    IPC分类号： A61K31/426 ,  C07D277/46

    CPC分类号： C07D417/12 ,  C07D277/56

    摘要： This invention discloses and claims a compound conforming to the general formula (I): Wherein R1, R2, R′2, R3, R4 and R5 are as described herein. The compounds of the present invention exhibit an inhibitory effect on the production of β-amyloid peptide (β-A4) by inhibition of gamma protease. Therefore, the compounds of the present invention are useful in the treatment of pathologies such as senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, amyloid angiopathy and/or cerebrovascular disorders.

    摘要翻译： 本发明公开了一种符合通式（I）的化合物：其中R 1，R 2，R 2，R 2， R 3，R 4和R 5如本文所述。 本发明的化合物通过抑制γ蛋白酶对β-淀粉样蛋白肽（β-A4）的产生具有抑制作用。 因此，本发明的化合物可用于治疗老年性痴呆，阿尔茨海默氏病，唐氏综合征，帕金森病，淀粉样血管病和/或脑血管障碍等病态。

    Benzimidazole derivatives, preparation and therapeutic use thereof
    7.
    发明授权
    Benzimidazole derivatives, preparation and therapeutic use thereof 失效
    苯并咪唑衍生物，其制备和治疗用途

    公开(公告)号：US06979683B2

    公开(公告)日：2005-12-27

    申请号：US10432672

    申请日：2001-11-21

    申请人： Francis Barth ,  Daniel Bichon ,  Frank Bolkenius ,  Viviane Van Dorsselaer

    发明人： Francis Barth ,  Daniel Bichon ,  Frank Bolkenius ,  Viviane Van Dorsselaer

    IPC分类号： A61K31/5517 ,  A61P1/04 ,  A61P1/16 ,  A61P1/18 ,  A61P3/10 ,  A61P7/00 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P13/12 ,  A61P17/06 ,  A61P21/04 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/18 ,  A61P35/00 ,  A61P35/04 ,  A61P37/04 ,  A61P37/06 ,  A61P43/00 ,  C07D487/06

    CPC分类号： C07D487/06

    摘要： The invention relates to benzimidazole derivatives of general formula (I) in which X represents a nitrogen atom or a carbon atom; and 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-tetrahydroisoquinoline; —(CH2)p-heteroaryl; heteroarylcarbonyl; phenylcarbonyl; (C1-C6)alkylcarbonyl; —(CH2)p—COOR′; or phenylsulphonyl group; and when X represents a carbon atom R3 represents a hydrogen atom; a group —NR5R6; —NHCOR7; —CONHR5; —COR7; —NHCONH2; —OH or —CH2OH, R4 represents in particular a hydrogen atom; an optionally substituted group —(CH2)p-phenyl; a group —(CH2)p-heteroaryl; or a group —(CH2)tNR7R8. Preparation process and therapeutic application.

    摘要翻译： 本发明涉及通式（I）的苯并咪唑衍生物，其中X表示氮原子或碳原子; 当X表示氮原子时，R 3特别表示氢原子或（C 1 -C 4）烷基，R 4表示氢原子， （C1-C6）烷基; （C 3 -C 7）环烷基; 4-哌啶基; - （CH 2）2 -NR 5 R 6; - （CH 2 CH 2）p -CONR 5 R 6; -CO - （CH 2 CH 2）n -NR 5 R 6; - （CH 2）2 - 苯基; - （CH 2）2 - 吗啉基; - （CH 2）2 - 吡咯烷基; - （CH 2）2 - 四氢异喹啉; - （CH 2）2 - 杂芳基; 杂芳基羰基; 苯基羰基 （C 1 -C 6）烷基羰基; - （CH 2）2 -COOR'; 或苯基磺酰基; 当X表示碳原子时，R 3表示氢原子; 基团-NR5R6; -NHCOR7; -CONHR5; -COR7; -NHCONH 2; -OH或-CH 2 OH，R 4特别表示氢原子; 任选取代的基团 - （CH 2 CH 2）p - 苯基; 基团 - （CH 2）2 - 杂芳基; 或基团 - （CH 2 CH 2）NR 7 R 8。 制备工艺及治疗应用。

    Acylaminothiazole derivatives and use thereof as beta-amyloid inhibitors
    9.
    发明授权
    Acylaminothiazole derivatives and use thereof as beta-amyloid inhibitors 失效
    酰氨基噻唑衍生物及其作为β-淀粉样蛋白抑制剂的用途

    公开(公告)号：US07759377B2

    公开(公告)日：2010-07-20

    申请号：US12051924

    申请日：2008-03-20

    申请人： Sylvie Baltzer ,  Marc Pascal ,  Viviane Van Dorsselaer

    发明人： Sylvie Baltzer ,  Marc Pascal ,  Viviane Van Dorsselaer

    IPC分类号： A61K31/426 ,  C07D277/38

    CPC分类号： C07D277/56 ,  C07D277/36 ,  C07D417/04 ,  C07D417/12

    摘要： Compounds of formula (I) as defined herein: inhibit the formation of the β-amyloid peptide (β-A4) and are, therefore, useful in the treatment of pathologies in which a β-amyloid peptide (β-A4) formation inhibitor provides a therapeutic benefit. Particular such pathologies are senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, amyloid angiopathy, cerebrovascular disorders, frontotemporal dementias and Pick's disease, post-traumatic dementias, pathologies linked to neuroinflammatory processes, Huntington's disease and Korsakov's syndrome.

    摘要翻译： 本文定义的式（I）化合物：抑制β-淀粉样蛋白肽（＆bgr; -A4）的形成，因此可用于治疗其中一种淀粉样蛋白肽（＆bgr; -A4 ）形成抑制剂提供治疗益处。 特别的这种病症是老年性痴呆，阿尔茨海默病，唐氏综合征，帕金森病，淀粉样血管病，脑血管病，额颞痴呆和皮克病，创伤后痴呆，与神经炎症过程相关的病症，亨廷顿病和科萨科夫综合征。

    ACYLAMINOTHIAZOLE DERIVATIVES AND USE THEREOF AS BETA-AMYLOID INHIBITORS
    10.
    发明申请
    ACYLAMINOTHIAZOLE DERIVATIVES AND USE THEREOF AS BETA-AMYLOID INHIBITORS 失效
    ACYLAMINOTH唑唑衍生物及其作为β-淀粉样抑制剂的用途

    公开(公告)号：US20060293366A1

    公开(公告)日：2006-12-28

    申请号：US11457490

    申请日：2006-07-14

    申请人： Sylvie Baltzer ,  Marc Pascal ,  Viviane Van Dorsselaer

    发明人： Sylvie Baltzer ,  Marc Pascal ,  Viviane Van Dorsselaer

    IPC分类号： A61K31/4439 ,  A61K31/427 ,  A61K31/426 ,  C07D417/02

    CPC分类号： C07D277/56 ,  C07D277/36 ,  C07D417/04 ,  C07D417/12

    摘要： Compounds of formula (I) as defined herein: inhibit the formation of the β-amyloid peptide (β-A4) and are, therefore, useful in the treatment of pathologies in which a β-amyloid peptide (β-A4) formation inhibitor provides a therapeutic benefit. Particular such pathologies are senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, amyloid angiopathy, cerebrovascular disorders, frontotemporal dementias and Pick's disease, post-traumatic dementias, pathologies linked to neuroinflammatory processes, Huntington's disease and Korsakov's syndrome.

    摘要翻译： 如本文所定义的式（I）化合物：抑制β-淀粉样蛋白肽（β-A4）的形成，因此可用于治疗β-淀粉状蛋白肽（β-A4）形成抑制剂提供的病理学 治疗好处。 特别的这种病症是老年性痴呆，阿尔茨海默病，唐氏综合征，帕金森病，淀粉样血管病，脑血管病，额颞痴呆和皮克病，创伤后痴呆，与神经炎症过程相关的病症，亨廷顿病和科萨科夫综合征。