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1. 发明授权

US08173669B2 Azabicycloalkane derivatives, preparation thereof and use thereof in therapy 有权
标题翻译：氮杂双环烷烃衍生物，其制备方法及其在治疗中的用途
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。

2. 发明授权

US08759343B2 Azabicycloalkane derivatives, preparation thereof and use thereof in therapy 有权
标题翻译：氮杂双环烷烃衍生物，其制备方法及其在治疗中的用途
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。

3. 发明授权

US07388005B2 Substituted 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyrimidinyl-2,3-dihydroimidazo [1,2-a]pyrimidin-5(1H)one derivatives for neurodegenerative disorders 失效
标题翻译：取代的2-嘧啶基-6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮和7-嘧啶基-2,3-二氢咪唑并[1,2-a]嘧啶-5（1H）神经变性疾病的衍生物
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。

4. 发明授权

US07247638B2 8-Substituted-6,7,8,9-tetrahydropyrimido [1,2-a] pyrimidin-4-one derivatives. 失效
标题翻译： 8-取代的6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮衍生物。
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。

5. 发明授权

US08093256B2 Use of 8-substituted-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives 失效
标题翻译： 8-取代-6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮衍生物的用途
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。

6. 发明授权

US07507743B2 Substituted 8′-pyridinyl-dihydrospiro-[cycloalkyl]-pyrimido[1,2-a] pyrimidin-6-one and 8′-pyrimidinyl-dihydrospiro-[cycloalkyl]-pyrimido[1,2-a] pyrimidin-6-one derivatives 失效
标题翻译：取代的8'-吡啶基 - 二氢螺 - [环烷基] - 嘧啶并[1,2-a]嘧啶-6-酮和8'-嘧啶基 - 二氢螺 - [环烷基] - 嘧啶并[1,2-a]嘧啶-6-酮衍生品
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。

7. 发明申请

US20080269257A1 Use of Substituted 2-Pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-A] Pyrimidin-4-one and 7-Pyrimidinyl-2,3-dihydroimidazo[1,2-A] Pyrimidin-5(1H)one Derivatives 失效
标题翻译：使用取代的2-嘧啶基-6,7,8,9-四氢嘧啶并[1,2-A]嘧啶-4-酮和7-嘧啶基-2,3-二氢咪唑并[1,2-A]嘧啶-5（1H ）一个衍生品
公开(公告)号：US20080269257A1
公开(公告)日：2008-10-30
申请号：US12120496
申请日：2008-05-14
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： A61K31/519 , C07D487/02 , A61P25/28 , A61P25/00
CPC分类号： A61K31/519 , A61K31/551 , C07D487/04
摘要： The invention relates to use of a pyrimidone derivative represented by formula (I) or a salt thereof as therapeutic agents: Wherein m, n, p, X, Y, R1, R2, R3, R4 R5, are as defined herein. The invention specifically 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 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作为治疗剂的用途：其中m，n，p，X，Y，R 1，R 2，R 3，R 4 R5如本文所定义。本发明具体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例如阿尔茨海默病异常活动引起的神经变性疾病。

8. 发明授权

US07294631B2 Substituted 8′-pyri(MI)dinyl-dihydrospiro-[cycloalkylamine]-pyrimido[1,2-a]pyrimidin-6-one derivatives 失效
标题翻译：取代的8'-吡啶（MI）二乙基 - 二氢螺环 - [环烷基胺] - 嘧啶并[1,2-a]嘧啶-6-酮衍生物
公开(公告)号：US07294631B2
公开(公告)日：2007-11-13
申请号：US11423557
申请日：2006-06-12
申请人： Nathalie Chereze , Alistair Lochead , Mourad Saady , Franck Slowinski , Philippe Yaiche
发明人： Nathalie Chereze , Alistair Lochead , Mourad Saady , Franck Slowinski , Philippe Yaiche
IPC分类号： A61K31/527 , A61K31/551 , C07D225/08 , C07D239/20 , C07D487/20 , C07D495/10
CPC分类号： A61K31/527 , A61K31/397 , C07D487/04 , Y02P20/142
摘要： The invention relates to a dihydrospiro-[cycloalkylamine]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, o, m, 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 disease.
摘要翻译：本发明涉及由式（I）表示的二氢螺环 - [环烷基胺] - 嘧啶酮衍生物或其盐：其中X，Y，R 1，R 2，R 3，R 4，o，m，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，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。

9. 发明申请

US20050049261A1 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 失效
标题翻译：取代的2-吡啶基-6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮和7-吡啶基-2,3-二氢咪唑并[1,2-a]嘧啶-5（1h）衍生品
公开(公告)号：US20050049261A1
公开(公告)日：2005-03-03
申请号：US10490135
申请日：2002-09-19
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： A61K31/519 , A61P3/04 , A61P3/10 , A61P9/10 , A61P17/14 , A61P25/00 , A61P25/02 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/06 , A61P35/00 , A61P43/00 , C07D213/50 , C07D213/60 , C07D487/04
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.
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，二氧戊环基，任选取代的氮原子; 或任选取代的亚甲基; 或任选取代的亚甲基; R1表示任选取代的2,3或4-吡啶环; R 2可以任选地表示C 1-6烷基; C 3-6环烷基，C 1-4链炔基，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，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，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GSK3beta以及cdk5 / p25例如阿尔茨海默病的异常活动引起的神经退行性疾病疾病。

10. 发明授权

US08148364B2 Substituted bicyclic pyrimidone derivatives 失效
标题翻译：取代的双环嘧啶酮衍生物
公开(公告)号：US08148364B2
公开(公告)日：2012-04-03
申请号：US12122111
申请日：2008-05-16
申请人： Nathalie Chereze , Alistair Lochead , Mourad Saady , Franck Slowinski , Philippe Yaiche
发明人： Nathalie Chereze , Alistair Lochead , Mourad Saady , Franck Slowinski , Philippe Yaiche
IPC分类号： C07D239/00 , C07D223/00 , A61K31/55 , A61K31/519 , A61P25/28
CPC分类号： C07D239/00 , C07D471/04
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Wherein Y, Z, R1, R2, R3, R4, R5, R6, R7, n, m, and o 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：由式（I）表示的嘧啶酮衍生物或其盐或其溶剂合物或其水合物：其中Y，Z，R1，R2，R3，R4，R5，R6，R7，n，m和o分别为在此描述。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，其用于预防和/或治疗由GSK3和bgr的异常活性如阿尔茨海默病引起的神经退行性疾病。

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