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    Derivatives of dioxan-2-alkyl carbamates, preparation thereof and application thereof in therapeutics
    7.
    发明授权
    Derivatives of dioxan-2-alkyl carbamates, preparation thereof and application thereof in therapeutics 有权
    二烷基-2-烷基氨基甲酸酯的衍生物，其制备及其在治疗中的应用

    公开(公告)号：US08119687B2

    公开(公告)日：2012-02-21

    申请号：US12834268

    申请日：2010-07-12

    申请人： Ahmed Abouabdellah ,  Michele Bas ,  Gihad Dargazanli ,  Christian Hoornaert ,  Adrien Tak Li ,  Florence Medaisko

    发明人： Ahmed Abouabdellah ,  Michele Bas ,  Gihad Dargazanli ,  Christian Hoornaert ,  Adrien Tak Li ,  Florence Medaisko

    IPC分类号： A61K31/351

    CPC分类号： C07D319/06 ,  C07C235/06 ,  C07D405/12

    摘要： A compound corresponding to general formula (I): in which R1 represents a phenyl or naphthalenyl group optionally substituted with one or more halogen atoms or hydroxyl, cyano, nitro, (C1-C3)alkyl, (C1-C3)alkoxy, trifluoromethyl, trifluoromethoxy, benzyloxy, (C3-C6)cycloalkyl-O— or (C3-C6)cycloalkyl(C1-C3)alkoxy groups; R2 represents either a group of general formula CHR3CONHR4 in which R3 represents a hydrogen atom or a methyl group and R4 represents a hydrogen atom or a (C1-C3)alkyl, (C3-C5) cycloalkyl or (pyridin-4-yl)methyl group; or a 2,2,2-trifluoroethyl group; or an (imidazol-2-yl)methyl group; or a (benzimidazol-2-yl)methyl group; or a phenyl group optionally substituted with one or more halogen atoms or cyano, nitro, (C1-C3)alkyl, (C1-C3)alkoxy, trifluoromethyl or trifluoromethoxy groups; and n represents a number ranging from 1 to 3; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. Also disclosed and claimed are the pharmaceutical compositions derived therefrom and their therapeutic use in treating a wide variety of diseases.

    摘要翻译： 氰基，硝基，（C1-C3）烷基，（C1-C3）烷氧基，三氟甲基，（C1-C3）烷氧基， 三氟甲氧基，苄氧基，（C3-C6）环烷基-O-或（C3-C6）环烷基（C1-C3）烷氧基; R 2表示通式CHR 3 CONHR 4的基团，其中R 3表示氢原子或甲基，R 4表示氢原子或（C 1 -C 3）烷基，（C 3 -C 5）环烷基或（吡啶-4-基）甲基 组; 或2,2,2-三氟乙基; 或（咪唑-2-基）甲基; 或（苯并咪唑-2-基）甲基; 或任选被一个或多个卤素原子取代的苯基或氰基，硝基，（C 1 -C 3）烷基，（C 1 -C 3）烷氧基，三氟甲基或三氟甲氧基; n表示1〜3的数; 以碱的形式，与酸的加成盐，水合物或溶剂合物的形式。 还公开并要求保护的是由其衍生的药物组合物及其治疗各种疾病的治疗用途。

    DERIVATIVES OF DIOXAN-2-ALKYL CARBAMATES, PREPARATION THEREOF AND APPLICATION THEREOF IN THERAPEUTICS
    8.
    发明申请
    DERIVATIVES OF DIOXAN-2-ALKYL CARBAMATES, PREPARATION THEREOF AND APPLICATION THEREOF IN THERAPEUTICS 有权
    二氧化-2-烷基碳酸酯的衍生物，其制备方法及其在治疗中的应用

    公开(公告)号：US20090286868A1

    公开(公告)日：2009-11-19

    申请号：US12510326

    申请日：2009-07-28

    申请人： Ahmed Abouabdellah ,  Michele Bas ,  Gihad Dargazanli ,  Christian Hoornaert ,  Adrien Tak Li ,  Florence Medaisko

    发明人： Ahmed Abouabdellah ,  Michele Bas ,  Gihad Dargazanli ,  Christian Hoornaert ,  Adrien Tak Li ,  Florence Medaisko

    IPC分类号： A61K31/335 ,  C07D319/06

    CPC分类号： C07D319/06 ,  C07C235/06 ,  C07D405/12

    摘要： A compound corresponding to general formula (I): in which R1 represents a phenyl or naphthalenyl group optionally substituted with one or more halogen atoms or hydroxyl, cyano, nitro, (C1-C3)alkyl, (C1-C3)alkoxy, trifluoromethyl, trifluoromethoxy, benzyloxy, (C3-C6)cycloalkyl-O— or (C3-C6)cycloalkyl(C1-C3)alkoxy groups; R2 represents either a group of general formula CHR3CONHR4 in which R3 represents a hydrogen atom or a methyl group and R4 represents a hydrogen atom or a (C1-C3)alkyl, (C3-C5)cycloalkyl or (pyridin-4-yl)methyl group; or a 2,2,2-trifluoroethyl group; or an (imidazol-2-yl)methyl group; or a (benzimidazol-2-yl)methyl group; or a phenyl group optionally substituted with one or more halogen atoms or cyano, nitro, (C1-C3)alkyl, (C1-C3)alkoxy, trifluoromethyl or trifluoromethoxy groups; and n represents a number ranging from 1 to 3; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. Also disclosed and claimed are the pharmaceutical compositions derived therefrom and their therapeutic use in treating a wide variety of diseases.

    摘要翻译： 氰基，硝基，（C1-C3）烷基，（C1-C3）烷氧基，三氟甲基，（C1-C3）烷氧基， 三氟甲氧基，苄氧基，（C3-C6）环烷基-O-或（C3-C6）环烷基（C1-C3）烷氧基; R 2表示通式CHR 3 CONHR 4的基团，其中R 3表示氢原子或甲基，R 4表示氢原子或（C 1 -C 3）烷基，（C 3 -C 5）环烷基或（吡啶-4-基）甲基 组; 或2,2,2-三氟乙基; 或（咪唑-2-基）甲基; 或（苯并咪唑-2-基）甲基; 或任选被一个或多个卤素原子取代的苯基或氰基，硝基，（C 1 -C 3）烷基，（C 1 -C 3）烷氧基，三氟甲基或三氟甲氧基; n表示1〜3的数; 以碱的形式，与酸的加成盐，水合物或溶剂合物的形式。 还公开并要求保护的是由其衍生的药物组合物及其治疗各种疾病的治疗用途。

    2-amino-3-(alkyl)-pyrimidone derivatives
    9.
    发明授权
    2-amino-3-(alkyl)-pyrimidone derivatives 失效
    2-氨基-3-（烷基） - 嘧啶酮衍生物

    公开(公告)号：US07378413B2

    公开(公告)日：2008-05-27

    申请号：US11035264

    申请日：2005-01-13

    申请人： Antonio Almario Carcia ,  Ryoichi Ando ,  Keiichi Arimoto ,  Fumiaki Uehara ,  Adrien Tak Li ,  Aya Shoda ,  Jonathan Reid Frost ,  Kazutoshi Watanabe

    发明人： Antonio Almario Carcia ,  Ryoichi Ando ,  Keiichi Arimoto ,  Fumiaki Uehara ,  Adrien Tak Li ,  Aya Shoda ,  Jonathan Reid Frost ,  Kazutoshi Watanabe

    IPC分类号： A61K31/505 ,  C07D401/04

    CPC分类号： A61K31/505 ,  C07D401/04 ,  C07D401/14 ,  C07D409/14

    摘要： A pyrimidone derivative represented by formula (I) or a salt thereof: Wherein: R1 represents a hydrogen atom or a C1-6 alkyl group which may be substituted by a C6,10 aryl group; R2 represents a C1-10 alkyl group which may be substituted, a C2-6 alkenyl group which may be substituted, a C3-6 alkynyl group which may be substituted, a C3-6 cycloalkyl group which may be substituted, or a C6-10 ARYL group which may be substituted; or R1 and R2 form together a C2-6 alkylene group which may be substituted; or R1 and R2 form together a chain of formula —(CH2)2—X—(CH2)2— or —(CH2)2—X—(CH2)3— where X represents a oxygen atom, a sulfur atom, or a nitrogen atom which may be substituted; R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or halogen atom; and R4 represents a C1-10 alkyl group optionally substituted by a hydroxyl group, amino, C1-6 monoalkylamino group, C2-12 dialkylamino group or C6,10 aryl group which may be substituted. And 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's disease.

    摘要翻译： 由式（I）表示的嘧啶酮衍生物或其盐：其中R1表示氢原子或可以被C 6-10取代的C 1-6烷基， / SUB>芳基; R 2表示可以被取代的C 1-10烷基，可以被取代的C 2-6亚烷基，C 3-6亚烷基， 可以被取代的亚炔基，可被取代的C 3-6亚烷基或可以被取代的C 6〜6-亚芳基; 或者R 1和R 2一起形成可以被取代的C 2-6亚烷基; 或者R 1和R 2一起形成式 - （CH 2 CH 2）2 - （CH 2）2 - 或 - （CH 2）2 -X-（CH 2）3 - - 其中X表示 氧原子，硫原子或可被取代的氮原子; R 3表示任选被C 1-4烷基，C 1-4烷氧基或卤素原子取代的2,3或4-吡啶基; 并且R 4表示任选被羟基，氨基，C 1-6 - 单烷基氨基，C 2-12-12任意取代的C 1-10烷基。 >可以被取代的二烷基氨基或C 6,10 芳基。 以及包含所述衍生物或其盐作为活性成分的药物，其用于由GSK3β如阿尔茨海默氏病的异常活性引起的神经变性疾病的预防和/或治疗性治疗。

    DERIVATIVES OF DIOXAN-2-ALKYL CARBAMATES, PREPARATION THEREOF AND APPLICATION THEREOF IN THERAPEUTICS
    10.
    发明申请
    DERIVATIVES OF DIOXAN-2-ALKYL CARBAMATES, PREPARATION THEREOF AND APPLICATION THEREOF IN THERAPEUTICS 有权
    二氧化-2-烷基碳酸酯的衍生物，其制备方法及其在治疗中的应用

    公开(公告)号：US20100280076A1

    公开(公告)日：2010-11-04

    申请号：US12834268

    申请日：2010-07-12

    申请人： Ahmed ABOUABDELLAH ,  Michele Bas ,  Gihad Dargazanli ,  Christian Hoornaert ,  Adrien Tak Li ,  Florence Medaisko

    发明人： Ahmed ABOUABDELLAH ,  Michele Bas ,  Gihad Dargazanli ,  Christian Hoornaert ,  Adrien Tak Li ,  Florence Medaisko

    IPC分类号： A61K31/4433 ,  A61K31/357 ,  A61K31/4184 ,  A61P19/02 ,  A61P19/06 ,  A61P1/00 ,  A61P25/06 ,  A61P25/14 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28

    CPC分类号： C07D319/06 ,  C07C235/06 ,  C07D405/12

    摘要： A compound corresponding to general formula (I): in which R1 represents a phenyl or naphthalenyl group optionally substituted with one or more halogen atoms or hydroxyl, cyano, nitro, (C1-C3)alkyl, (C1-C3)alkoxy, trifluoromethyl, trifluoromethoxy, benzyloxy, (C3-C6)cycloalkyl-O— or (C3-C6)cycloalkyl(C1-C3)alkoxy groups; R2 represents either a group of general formula CHR3CONHR4 in which R3 represents a hydrogen atom or a methyl group and R4 represents a hydrogen atom or a (C1-C3)alkyl, (C3-C5) cycloalkyl or (pyridin-4-yl)methyl group; or a 2,2,2-trifluoroethyl group; or an (imidazol-2-yl)methyl group; or a (benzimidazol-2-yl)methyl group; or a phenyl group optionally substituted with one or more halogen atoms or cyano, nitro, (C1-C3)alkyl, (C1-C3)alkoxy, trifluoromethyl or trifluoromethoxy groups; and n represents a number ranging from 1 to 3; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. Also disclosed and claimed are the pharmaceutical compositions derived therefrom and their therapeutic use in treating a wide variety of diseases.

    摘要翻译： 氰基，硝基，（C1-C3）烷基，（C1-C3）烷氧基，三氟甲基，（C1-C3）烷氧基， 三氟甲氧基，苄氧基，（C3-C6）环烷基-O-或（C3-C6）环烷基（C1-C3）烷氧基; R 2表示通式CHR 3 CONHR 4的基团，其中R 3表示氢原子或甲基，R 4表示氢原子或（C 1 -C 3）烷基，（C 3 -C 5）环烷基或（吡啶-4-基）甲基 组; 或2,2,2-三氟乙基; 或（咪唑-2-基）甲基; 或（苯并咪唑-2-基）甲基; 或任选被一个或多个卤素原子取代的苯基或氰基，硝基，（C 1 -C 3）烷基，（C 1 -C 3）烷氧基，三氟甲基或三氟甲氧基; n表示1〜3的数; 以碱的形式，与酸的加成盐，水合物或溶剂合物的形式。 还公开并要求保护的是由其衍生的药物组合物及其治疗各种疾病的治疗用途。