公开(公告)号：US08173669B2

公开(公告)日：2012-05-08

申请号：US12535156

申请日：2009-08-04

申请人： Omar Ben Ayad ,  Odile Leclerc ,  Alistair Lochead ,  Mourad Saady ,  Franck Slowinski ,  Julien Vache

发明人： Omar Ben Ayad ,  Odile Leclerc ,  Alistair Lochead ,  Mourad Saady ,  Franck Slowinski ,  Julien Vache

IPC分类号： A01N43/42 ,  A61K31/44 ,  C07D221/02

CPC分类号： C07D487/08 ,  C07D471/08

摘要： The invention relates to compounds of the general formula (I): Wherein R, m, n and o are as defined herein. The invention also relates to a method for preparing the same and to the application in therapy.

摘要翻译： 本发明涉及通式（I）的化合物：其中R，m，n和o如本文所定义。 本发明还涉及其制备方法及其在治疗中的应用。

公开(公告)号：US08759343B2

公开(公告)日：2014-06-24

申请号：US13422296

申请日：2012-03-16

申请人： Omar Ben Ayad ,  Odile LeClerc ,  Alistair Lochead ,  Mourad Saady ,  Franck Slowinski ,  Julien Vache

发明人： Omar Ben Ayad ,  Odile LeClerc ,  Alistair Lochead ,  Mourad Saady ,  Franck Slowinski ,  Julien Vache

IPC分类号： A61K31/4439 ,  C07D401/14 ,  C07D413/14 ,  C07D401/04 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377

CPC分类号： C07D487/08 ,  C07D471/08

摘要： The invention relates to compounds of the general formula (I): wherein R, m, n and o are as defined herein. The invention also relates to a method for preparing the same and to the application in therapy.

摘要翻译： 本发明涉及通式（I）的化合物：其中R，m，n和o如本文所定义。 本发明还涉及其制备方法及其在治疗中的应用。

公开(公告)号：US07388005B2

公开(公告)日：2008-06-17

申请号：US10490136

申请日：2002-09-19

申请人： Thierry Gallet ,  Patrick Lardenois ,  Alistair Lochead ,  Séverine Marguerie ,  Alain Nedelec ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

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

IPC分类号： A61K31/551 ,  A61K31/519 ,  C07D487/04 ,  A61P25/28

CPC分类号： A61K31/519 ,  A61K31/551 ,  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 C1-2 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 nitrogen atom being optionally; or a methylene group optionally substituted; R1 represents a pyrimidine group optionally substituted; R2 may represent a C1-6 alkyl group optionally substituted by a C6,10 aryloxy or a C6,10 arylamino group; a C3-6 cycloalkyl group, a C1-4 alkylthio group, a C1-4 alkoxy group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a phenylthio group, a benzyl group, a benzene ring, an indan ring, a 5,6,7,8-tetrahydronaphthalene ring, a naphthalene 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, C1-6 alkyl group, a hydroxy group, a C1-4 alkoxy group or a halogen atom; R5 represents a hydrogen atom, a C1-6 alkyl 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 GSK3β3 or GSK3β3 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 1-12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，任选的氮原子; 或任选取代的亚甲基; R1表示任选取代的嘧啶基团; R 2可以表示任选被C 6,10芳氧基或C 6,10芳基氨基取代的C 1-6烷基; C 3-6环烷基，C 1-4烷硫基，C 1-4烷氧基，C 1 -C 4烷氧基， 1-2个全卤代烷基，C 1-3卤代烷基，苯硫基，苄基，苯环，茚满环，5,6,7， 8-四氢萘环，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，C 1-6烷基或卤素原子。 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GSK3β3或GSK3β3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 。

公开(公告)号：US07247638B2

公开(公告)日：2007-07-24

申请号：US11225218

申请日：2005-09-13

申请人： Alistair Lochead ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

发明人： Alistair Lochead ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

IPC分类号： C07D487/04 ,  A61K31/519

CPC分类号： A61K31/519 ,  C07D487/04

摘要： The invention relates to substituted-pyrimidone derivatives represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as defined herein. 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's disease.

摘要翻译： 本发明涉及由式（I）表示的取代嘧啶酮衍生物或其盐：其中X，Y，R 1，R 2，R 3，R 4，R 5，n，p和q如本文所定义。 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如阿尔茨海默病异常活动引起的神经变性疾病。

公开(公告)号：US07462621B2

公开(公告)日：2008-12-09

申请号：US11696982

申请日：2007-04-05

申请人： Thierry Gallet ,  Patrick Lardenois ,  Alistair Lochead ,  Severine Marguerie ,  Alain Nedelec ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

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

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P25/28 ,  A61K31/55

CPC分类号： A01N43/90 ,  C07D213/50 ,  C07D213/60 ,  C07D487/04

摘要： The invention relates to an use of pyrimidone derivative represented by formula (I) or a salt thereof: wherein m, n, p, X, Y, R1, R2, R3, R4 and R5 are as defined herein for treating a variety of disease states. More specifically, the invention relates 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's 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的用途：其中m，n，p，X，Y，R 1，R 2，R 3，R 4和R 5如本文所定义，用于治疗各种疾病 状态。 更具体地，本发明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 阿尔茨海默氏病。

公开(公告)号：US07217715B2

公开(公告)日：2007-05-15

申请号：US11224873

申请日：2005-09-13

申请人： Alistair Lochead ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

发明人： Alistair Lochead ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

IPC分类号： C07D487/04 ,  A61K31/519

CPC分类号： A61K31/519 ,  C07D487/04

摘要： The invention relates to a substituted-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as described herein. 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）表示的取代嘧啶酮衍生物或其盐：其中X，Y，R 1，R 2，R 3，R 4，R 5，n，p和q如本文所述。 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，所述活性成分用于预防和/或治疗由GSK3β如阿尔茨海默病异常活动引起的神经变性疾病。

公开(公告)号：US07214682B2

公开(公告)日：2007-05-08

申请号：US10490135

申请日：2002-09-19

申请人： Thierry Gallet ,  Patrick Lardenois ,  Alistair Lochead ,  Séverine Marguerie ,  Alain Nedelec ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

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

IPC分类号： A01N43/90 ,  A61K31/519 ,  A01N43/62 ,  A61K31/55 ,  C07D471/00 ,  C07D487/00

CPC分类号： A01N43/90 ,  C07D213/50 ,  C07D213/60 ,  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 sulfur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, an ethenylene group, an ethynylene group an oxygen atom, a sulfur 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; or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring optionally substituted; R2 may represent a C1-6 alkyl group optionally; a C3-6 cycloalkyl group, a C1-4 alkythio group, a C1-4 alkoxy group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a phenylthio group, a benzyl group, a benzene ring, an indan ring, a 5,6,7,8-tetrahydronaphthalene ring, a naphthalene ring, a pyridine ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring; R3 and R4 represent, each independently, a hydrogen atom, a C1-6 alkyl group, a hydroxy group, a C1-4 alkoxy group or a halogen atom; R5 represents a hydrogen atom, a C1-6 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

公开(公告)号：US20060025431A1

公开(公告)日：2006-02-02

申请号：US11220999

申请日：2005-09-07

申请人： Pascal George ,  Alistair Lochead ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

发明人： Pascal George ,  Alistair Lochead ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

IPC分类号： A61K31/519 ,  C07D487/10

CPC分类号： C07D487/10

摘要： The invention relates to a dihydrospiro-[cycloalkyl]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, m, n, p and q are as described herein. 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）表示的二氢螺环 - [环烷基] - 嘧啶酮衍生物或其盐：其中X，Y，R 1，R 2，R 3，m，n，p和q如本文所述。 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，所述活性成分用于预防和/或治疗由GSK3β如阿尔茨海默病异常活动引起的神经变性疾病。

公开(公告)号：US08093256B2

公开(公告)日：2012-01-10

申请号：US11764374

申请日：2007-06-18

申请人： Alistair Lochead ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

发明人： Alistair Lochead ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

IPC分类号： A61K31/519 ,  C07D487/04

CPC分类号： A61K31/519 ,  C07D487/04

摘要： The invention relates to use of substituted-pyrimidone derivatives represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as defined herein. More specifically, the invention relates 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 disease caused by abnormal activity of GSK3β, such as Pick's disease among various other diseases as claimed herein.

摘要翻译： 本发明涉及由式（I）表示的取代嘧啶酮衍生物或其盐的用途：其中X，Y，R 1，R 2，R 3，R 4，R 5，n，p和q如本文所定义。 更具体地，本发明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GSK3＆bgr异常活性引起的疾病，例如各种其他疾病中的皮克病 如本文所要求的。

公开(公告)号：US07507743B2

公开(公告)日：2009-03-24

申请号：US11866142

申请日：2007-10-02

申请人： Pascal George ,  Alistair Lochead ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

发明人： Pascal George ,  Alistair Lochead ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

IPC分类号： A61P25/28 ,  A61K31/519

CPC分类号： C07D487/10

摘要： The invention relates to therapeutic uses of a dihydrospiro-[cycloalkyl]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, m, n, p and q are as described herein. Specifically, the invention relates 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）表示的二氢螺环 - [环烷基] - 嘧啶酮衍生物或其盐的治疗用途：其中X，Y，R 1，R 2，R 3，m，n，p和q如本文所述。 具体地说，本发明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如阿尔茨海默病异常活动引起的神经变性疾病。