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41. 发明授权

US07608624B2 1-[alkyl], 1-[(heteroaryl)alkyl] and 1-[(aryl)alkyl]-7-pyridinyl-imidazo[1,2-a]pyrimidin-5(1h)-one derivatives 失效
标题翻译： 1- [烷基]，1 - [（杂芳基）烷基]和1 - [（芳基）烷基] -7-吡啶基 - 咪唑并[1,2-a]嘧啶-5（1h）
公开(公告)号：US07608624B2
公开(公告)日：2009-10-27
申请号：US11370451
申请日：2006-03-08
申请人： Alistair Lochead , Severine Marguerie , Mourad Saady , Philippe Yaiche
发明人： Alistair Lochead , Severine Marguerie , Mourad Saady , Philippe Yaiche
IPC分类号： A61K31/519
CPC分类号： A61K31/519 , C07D487/04
摘要： The invention relates to a method of treatment of a variety of neurodegenerative diseases such as Alzheimer disease using a imidazo[1,2-a]pyrimidone derivative represented by formula (I) or a salt thereof: Wherein X, R1, R2, and n are as defined herein.
摘要翻译：本发明涉及使用由式（I）表示的咪唑并[1,2-a]嘧啶酮衍生物或其盐治疗多种神经变性疾病如阿尔茨海默病的方法：其中X，R1，R2和n 如本文所定义。

42. 发明授权

US07566720B2 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： 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）
公开(公告)号：US07566720B2
公开(公告)日：2009-07-28
申请号：US11841285
申请日：2007-08-20
申请人： Antonio Almario Garcia , Thierry Gallet , Adrien Tak Li , Alistair Lochead , Severine Marguerie , Alain Nedelec , Mourad Saady , Philippe Yaiche
发明人： Antonio Almario Garcia , Thierry Gallet , Adrien Tak Li , Alistair Lochead , Severine Marguerie , Alain Nedelec , Mourad Saady , Philippe Yaiche
IPC分类号： A61P25/00 , A61P25/28 , A61P3/04 , C07D471/04 , C07D487/04 , A61K31/519
CPC分类号： C07D487/04 , A61K31/519
摘要： The invention relates to therapeutic uses of a pyrimidone derivative represented by formula (I) or a salt thereof: Wherein X, Y, R1, R2, m and n are as defined herein. Specifically, a medicament comprising the said derivative or a salt thereof as an active ingredient is used for preventive and/or therapeutic treatment of a neurodegenerative diseases caused by abnormal activity of GSK3β such as Alzheimer's disease.
摘要翻译：本发明涉及由式（I）表示的嘧啶酮衍生物或其盐的治疗用途：其中X，Y，R 1，R 2，m和n如本文所定义。具体地说，包含所述衍生物或其盐作为活性成分的药物用于预防和/或治疗由诸如阿尔茨海默病的GSK3β的异常活性引起的神经变性疾病。

43. 发明授权

US07547705B2 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：US07547705B2
公开(公告)日：2009-06-16
申请号：US11866687
申请日：2007-10-03
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： A61K31/397 , A61K31/551 , A61K31/527 , A61K31/4162 , C07D225/00 , C07D223/00 , C07D487/20 , C07D239/00 , A61P3/10 , A61P25/28 , A61P25/16 , A61P25/18
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，R1，R2，R3，R4，o，m，n，p和q如上所定义这里。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。

44. 发明授权

US07465737B2 Heteroaryl substituted 2-pyridinyl and 2-pyrimidinyl -6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives 失效
标题翻译：杂芳基取代的2-吡啶基和2-嘧啶基-6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮衍生物
公开(公告)号：US07465737B2
公开(公告)日：2008-12-16
申请号：US11749349
申请日：2007-05-16
申请人： Alistair Lochead , Alain Nedelec , Mourad Saady , Philippe Yaiche
发明人： Alistair Lochead , Alain Nedelec , Mourad Saady , Philippe Yaiche
IPC分类号： A61K31/519
CPC分类号： A61K31/519 , A01N43/90 , C07D487/04
摘要： The invention relates to use of a pyrimidone derivative represented by formula (I)or a salt thereof wherein: X, Y, R1, R2, R3, R4, R5, m, n and p are as defined herein. In particular, 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 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，Y，R 1，R 2，R 3，R 4，R 5，m，n和p如本文所定义。特别地，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，例如阿尔茨海默病。

45. 发明授权

US07393853B2 Use of substituted 8-Perfluoroalkyl-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives as therapeutic agents 失效
标题翻译：取代的8-全氟烷基-6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮衍生物作为治疗剂
公开(公告)号：US07393853B2
公开(公告)日：2008-07-01
申请号：US11696256
申请日：2007-04-04
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
CPC分类号： A61K31/519 , C07D487/04
摘要： The invention relates to use of 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 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 disease caused by abnormal activity of GSK3β, such as Pick'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如本文所述用于处理多种的疾病状态。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的异常活性如皮克病引起的疾病。

46. 发明授权

US07211581B2 Substituted 2-(diaza-bicyclo-alkyl)-pyrimidone derivatives 失效
公开(公告)号：US07211581B2
公开(公告)日：2007-05-01
申请号：US11219923
申请日：2005-09-06
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： C07D401/14 , C07D403/14 , A61K31/506 , A61K31/444 , A61P3/10
CPC分类号： A61K31/506 , C07D401/14 , C07D487/08
摘要： The invention relates to a 2-(diaza-bicyclo-alkyl)-pyrimidone derivative represented by formula (I): wherein: R1 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R2 represents a hydrogen atom, a C1-6 alkyl group optionally substituted by 1 to 4 substituents selected from a halogen atom, a hydroxyl group, a C1-4 alkoxy group; a C1-2 perhalogenated alkyl group, a benzyl group, a phenethyl group, a benzyloxycarbonyl group, a C1-4 alkoxy carbonyl group, a benzene ring, a naphthalene ring, a quinoline ring, a phthalazine ring, a 5,6,7,8-tetrahydronaphthalene ring, a pyridine ring, an indole ring, a pyrrole ring, a thiophene ring, a benzenesulfonyl group, a benzoyl group, a pyridazine ring, a furan ring and an imidazole ring; each of the benzyl group, the phenethyl group, the benzyloxycarbonyl group, the benzenesulfonyl group, the benzoyl group and the benzene, naphthalene, quinoline, phthalazine, 5,6,7,8-tetrehydronaphthalene, pyridine, indole, pyrrole and thiophene rings being optionally substituted by 1 to 4 substituents selected from a C1-6 alkyl group, a benzene ring, a halogen atom, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a hydroxyl group, a C1-4 alkoxy group, a nitro group, a cyano group, an amino group, a C1-6 monoalkylamino group and a C2-10 dialkylamino group; R3 represents a 2, 4 or 5-pyrimidine ring or a 2, 3 or 4-pyridine ring, the rings being optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or a halogen atom; R4 represents a C1-4 alkyl group optionally substituted by a hydroxyl group, a C1-4 alkoxy group or a halogen atom and n represents 1 or 2; or a salt thereof, or a solvate thereof or a hydrate thereof. 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.

47. 发明申请

US20060014762A1 2-Pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-A]pyrimidin-4-one and 7-pyridinyl-2,3-dihydoimidazo[1,2-A]pyrimidin-5(1H)one derivatives 审中-公开
公开(公告)号：US20060014762A1
公开(公告)日：2006-01-19
申请号：US11227007
申请日：2005-09-15
申请人： Antonio Almario Garcia , Thierry Gallet , Adrien Ll , Alistair Lochead , Severine Marguerie , Alain Nedelec , Mourad Saady , Philippe Yaiche
发明人： Antonio Almario Garcia , Thierry Gallet , Adrien Ll , Alistair Lochead , Severine Marguerie , Alain Nedelec , Mourad Saady , Philippe Yaiche
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04 , A61K31/519
摘要： The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof: wherein: X represents 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, a 1,2-cyclopropylene, an oxygen atom, a sulphur atom, a sulfonyl group, a sulfoxyde group, a carbonyl group, a nitrogen atom being optionally substituted; or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridyl group optionally substituted by a C3-6 cycloalkyl group a C1-4 alkyl group, a C1-4 alkoxy group, a benzyl group or a halogen atom; when Y represents a bond, a methylene group optionally substituted or a carbonyl group then R2 represents a C1-6 alkyl 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 5,6,7,8-tetrahydronaphthyl ring, a naphthyl ring, a phenylthio group, a benzyl group, a phenyl ring, a pyridyl ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring; when Y represents an ethenylene group, an ethynylene group, an oxygen atom, a sulphur atom, a sulfonyl group, a sulfoxyde group or a nitrogen atom being optionally substituted then R2 represents a C1-6 alkyl group, a C3-6 cycloalkyl group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a naphthyl ring, a 5,6,7,8-tetrahydronaphthyl ring, a benzyl group, a phenyl ring, a pyridyl ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring. 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 diseases caused by abnormal activity of GSK3β such as Alzheimer's disease.

48. 发明授权

US06908927B2 Pyridopyranoazepine derivatives, their preparation and their therapeutic application 有权
标题翻译：吡啶吡喃并氮衍生物，其制备及其治疗应用
公开(公告)号：US06908927B2
公开(公告)日：2005-06-21
申请号：US10359881
申请日：2003-02-06
申请人： Frédéric Galli , Samir Jegham , Alistair Lochead , Axelle Samson
发明人： Frédéric Galli , Samir Jegham , Alistair Lochead , Axelle Samson
IPC分类号： A61K31/436 , A61K31/439 , A61P1/00 , A61P1/04 , A61P3/04 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P25/36 , A61P29/00 , C07D209/00 , C07D221/00 , C07D311/00 , C07D491/22 , A61K31/44 , A61P25/04
CPC分类号： C07D491/22
摘要： The invention relates to pyridopyranoazepine derivatives, to pharmaceutical compositions containing them, to process for preparing them, and to the method of use thereof in the treatment or prevention of disorders associated with a dysfunction of the nicotine receptors.
摘要翻译：本发明涉及吡啶吡喃并氮衍生物，含有它们的药物组合物，其制备方法及其在治疗或预防与尼古丁受体功能障碍相关的疾病中的应用方法。

49. 发明授权

US06057321A 1,4-diazabicyclo [2.2.2] oct-2-ylmethyl derivatives, their preparation and therapeutic application 失效
标题翻译： 1,4-二氮杂双环[2.2.2]辛-2-基甲基衍生物，其制备和治疗应用
公开(公告)号：US06057321A
公开(公告)日：2000-05-02
申请号：US319413
申请日：1999-06-04
申请人： Alistair Lochead , Samir Jegham , Alain Nedelec , Axelle Solignac
发明人： Alistair Lochead , Samir Jegham , Alain Nedelec , Axelle Solignac
IPC分类号： A61K31/4995 , A61P1/00 , A61P1/08 , A61P9/00 , A61P13/00 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D487/08 , A61K31/529
CPC分类号： C07D487/08
摘要： The invention concerns compounds of general formula (I) ##STR1## in which R.sub.1 represents a methyl group, X.sub.1 represents a hydrogen atom, or OR.sub.1 and X.sub.1 together form a group of formula --O(CH.sub.2).sub.2 --,--O(CH.sub.2).sub.3 --, --O(CH.sub.2).sub.2 O-- or --O(CH.sub.2).sub.3 O--, X.sub.2 represents a hydrogen atom or an amino group, and X.sub.3 representing a halogen atom. The compounds are ligands of serotoninergic receptors of the 5-HT.sub.3 and/or 5-HT.sub.4 types, and act as 5-HT.sub.4 agonists and/or 5-HT.sub.3 antogonists.
摘要翻译： PCT No.PCT / FR97 / 02174 Sec。 371日期1999年6月4日第 102（e）1999年6月4日PCT 1997年12月2日PCT PCT。公开号WO98 / 24790 日期1998年6月11日本发明涉及通式（I）的化合物，其中R1表示甲基，X1表示氢原子，或OR1和X1一起形成式-O（CH 2）2 - ， - O（ CH2）3-，-O（CH2）2O-或-O（CH2）3O-，X2表示氢原子或氨基，X3表示卤素原子。这些化合物是5-HT3和/或5-HT4类型的5-羟色胺能受体的配体，并且作为5-HT4激动剂和/或5-HT3绝种子。

50. 发明授权

US07462621B2 Use of 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 as therapeutic agents 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 ）一种衍生物作为治疗剂
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。

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