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1. 发明授权

US08507476B2 Substituted arylamide diazepinopyrimidone derivatives 有权
标题翻译：取代的芳基酰胺二氮杂吡啶并吡啶酮衍生物
公开(公告)号：US08507476B2
公开(公告)日：2013-08-13
申请号：US12844278
申请日：2010-07-27
申请人： Aude Fayol , Alistair Lochead , Mourad Saady , Julien Vache , Philippe Yaiche
发明人： Aude Fayol , Alistair Lochead , Mourad Saady , Julien Vache , Philippe Yaiche
IPC分类号： A61P25/00 , A61K31/55 , C07D491/00
CPC分类号： C07D487/04 , C07D243/08 , C07D403/12
摘要： The disclosure relates to a series pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: Y, Z, R1, R2, R3, R4, R5 and n are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.
摘要翻译：本发明涉及由式（I）表示的一系列嘧啶酮衍生物或其盐或其溶剂合物或其水合物：其中：Y，Z，R 1，R 2，R 3，R 4，R 5和n如披露还公开了制备式（I）化合物，其中间体及其在治疗各种疾病状况中的用途的方法。

2. 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。

3. 发明授权

US07429663B2 7-(Pyrimidin-4-yl)-Imidazo[1,2-a]Pyrimidin-5(1H)-ones as GSK3β inhibitors 失效
标题翻译： 7-（嘧啶-4-基） - 咪唑并[1,2-a]嘧啶-5（1H） - 酮作为GSK3beta抑制剂
公开(公告)号：US07429663B2
公开(公告)日：2008-09-30
申请号：US10504679
申请日：2003-02-26
申请人： Alistair Lochead , Mourad Saady , Philippe Yaiche
发明人： Alistair Lochead , Mourad Saady , Philippe Yaiche
IPC分类号： C07D487/04 , A61K31/519 , A61P35/04 , A61P3/10 , A61P25/28
CPC分类号： C07D487/04
摘要： The invention relates to a imidazo[1,2-a]pyrimidone derivative represented by formula (I) or a salt thereof: R1 wherein X represents a bond, an ethenylene group, an ethenylene group, a methylene group optionally substituted; a carbonyl group, an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group or a nitrogen atom being optionally substituted; R1 represents a 2, 4 or 5-pyrimidinyl optionally substituted; R2 represents a C1-6 alkyl group, a C1-2 perhalogenated alkyl group,a C1-3 halogenated alkyl group, a benzyl group, a benzene ring, a naphthalene ring, 5,6,7,8-tetrahydronaphthalene ring, a pyridine ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring, the benzyl group and the rings being optionally substituted; and n represents 0 to 3. 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）表示的咪唑并[1,2-a]嘧啶酮衍生物或其盐：R 1其中X表示键，亚乙烯基，亚乙烯基，任选取代的亚甲基; 羰基，氧原子，硫原子，磺酰基，亚砜基或任选取代的氮原子; R 1表示任选取代的2,4或5-嘧啶基; R 2表示C 1-6烷基，C 1-12全卤代烷基，C 1-3烷基，卤代烷基，苄基，苯环，萘环，5,6,7,8-四氢萘环，吡啶环，吲哚环，吡咯环，噻吩环，呋喃环或呋喃环咪唑环，苄基和环任选被取代; 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GSK3beta异常活动引起的神经变性疾病，例如阿尔茨海默氏症疾病。

4. 发明授权

US07232827B2 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：US07232827B2
公开(公告)日：2007-06-19
申请号：US10504677
申请日：2003-02-26
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： A01N43/90 , A61K31/519 , C07D471/00 , C07D487/00
CPC分类号： A61K31/519 , A01N43/90 , C07D487/04
摘要： The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein: (I) 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 or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring optionally substituted; R2 represents a heterocyclic bicyclic rings, having 1–4 heteroatoms selected from an oxygen atom, a sulfur atom and a nitrogen atom and having 5–9 carbon atoms, of formula (II) R3 represents a hydrogen atom, a C1-6 alkyl group, a hydroxy group, a C1-4 alkoxy group or a halogen atom; R4 represents a hydrogen atom, a C1-6 alkyl group, a C1-4 alkoxy 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 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：（I）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，亚乙炔基或任选取代的亚甲基; R1表示2,3或4-吡啶环或任选取代的2,4或5-嘧啶环; R 2表示具有1-4个选自氧原子，硫原子和氮原子并且具有5-9个碳原子的杂原子的式（II）的杂环双环，R 3表示氢原子，C 1 -C 1-6烷基，羟基，C 1-4烷氧基或卤素原子; R 4表示氢原子，C 1-6烷基，C 1-4烷氧基或卤素原子。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GSK3β或GSK3β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

5. 发明授权

US07217715B2 Substituted 8-perfluoroalkyl-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives 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
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。

6. 发明授权

US07214682B2 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
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

7. 发明申请

US20060025431A1 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：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。

8. 发明授权

US08592437B2 Heteroarylamide pyrimidone compounds 有权
标题翻译：杂芳基酰胺嘧啶酮化合物
公开(公告)号：US08592437B2
公开(公告)日：2013-11-26
申请号：US12606680
申请日：2009-10-27
申请人： Alistair Lochead , Mourad Saady , Corinne Veronique , Philippe Yaiche
发明人： Alistair Lochead , Mourad Saady , Corinne Veronique , Philippe Yaiche
IPC分类号： C07D403/12 , C07D239/36 , A61K31/513
CPC分类号： C07D403/12 , C07D239/36 , C07D401/14 , C07D405/14 , C07D409/14 , C07D471/04
摘要： The present invention discloses a series of pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Wherein X, Z, R1, R2, R3, R4, R5, R6, R7, n and m are as defined herein. Also disclosed herein are the methods of preparation of compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.
摘要翻译：本发明公开了一系列由式（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X，Z，R1，R2，R3，R4，R5，R6，R7，n和 m如本文所定义。本文还公开了制备式（I）化合物，其中间体及其在治疗各种疾病状况中的用途的方法。

9. 发明授权

US08507470B2 Substituted arylamide oxazepinopyrimidone derivatives 有权
标题翻译：取代的芳酰胺氧氮杂嘧啶衍生物
公开(公告)号：US08507470B2
公开(公告)日：2013-08-13
申请号：US12844275
申请日：2010-07-27
申请人： Aude Fayol , Alistair Lochead , Mourad Saady , Julien Vache , Philippe Yaiche
发明人： Aude Fayol , Alistair Lochead , Mourad Saady , Julien Vache , Philippe Yaiche
IPC分类号： C07D498/04
CPC分类号： C07D498/04
摘要： The disclosure relates to a series pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: Y, Z, R1, R2, R3, R4 and n are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.
摘要翻译：本发明涉及由式（I）表示的一系列嘧啶酮衍生物或其盐，或其溶剂合物或其水合物：其中：Y，Z，R 1，R 2，R 3，R 4和n如本公开所定义。还公开了制备式（I）化合物，其中间体及其在治疗各种疾病状况中的用途的方法。

10. 发明授权

US08501728B2 Substituted heteroarylamide oxazepinopyrimidone derivatives 有权
标题翻译：取代的杂芳基酰胺氧氮杂并嘧啶衍生物
公开(公告)号：US08501728B2
公开(公告)日：2013-08-06
申请号：US12844270
申请日：2010-07-27
申请人： Aude Fayol , Alistair Lochead , Mourad Saady , Julien Vache , Philippe Yaiche
发明人： Aude Fayol , Alistair Lochead , Mourad Saady , Julien Vache , Philippe Yaiche
IPC分类号： A61P3/00 , A61P25/00 , A61P35/00 , A61K31/553 , C07D498/04
CPC分类号： C07D498/04 , C07D519/00
摘要： The disclosure relates to a series pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: Y, Z, R1, R2, R3, R4 and n are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.
摘要翻译：本发明涉及由式（I）表示的一系列嘧啶酮衍生物或其盐，或其溶剂合物或其水合物：其中：Y，Z，R 1，R 2，R 3，R 4和n如本公开所定义。还公开了制备式（I）化合物，其中间体及其在治疗各种疾病状况中的用途的方法。

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