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

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：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。

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。

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。

公开(公告)号：US08202874B2

公开(公告)日：2012-06-19

申请号：US12968958

申请日：2010-12-15

申请人： Alistair Lochead ,  Mourad Saady ,  Philippe Yaiche

发明人： Alistair Lochead ,  Mourad Saady ,  Philippe Yaiche

IPC分类号： A61K31/497

CPC分类号： A61K31/497 ,  C07D241/52 ,  C07D401/04

摘要： N-oxide pyrazine derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: R1, R2, R3, R4, and R5 are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I) and their use in therapeutics.

摘要翻译： 式（I）表示的N-氧化吡嗪衍生物或其盐，或其溶剂合物或其水合物：其中：R1，R2，R3，R4和R5如本公开所定义。 还公开了制备式（I）化合物及其在治疗中的用途的方法。

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。

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。