公开(公告)号：US20070167461A1

公开(公告)日：2007-07-19

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： A61K31/519

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：US20080027078A1

公开(公告)日：2008-01-31

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： A61K31/519 ,  A61P25/00 ,  A61P25/28 ,  A61P3/04

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。

公开(公告)号：US20110294786A1

公开(公告)日：2011-12-01

申请号：US13197228

申请日：2011-08-03

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： A61K31/55 ,  A61K31/519 ,  A61P25/18 ,  A61P25/16 ,  A61P3/10 ,  A61P3/04 ,  C07D471/04 ,  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：US20080081819A1

公开(公告)日：2008-04-03

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： A61K31/519 ,  A61P25/00 ,  A61P3/04

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。

公开(公告)号：US20090281121A1

公开(公告)日：2009-11-12

申请号：US12434053

申请日：2009-05-01

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 ,  A61P3/00 ,  A61P25/00

CPC分类号： C07D487/04

摘要： The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof: Wherein X, Y, R1, R2, R3, R4, n, p, q, o and m 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）表示的嘧啶酮衍生物或其盐：其中X，Y，R 1，R 2，R 3，R 4，n，p，q，o和m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：US20090036427A1

公开(公告)日：2009-02-05

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： A61K31/55 ,  A61K31/519 ,  C07D487/04 ,  A61P25/28 ,  A61P25/16 ,  C07D471/04

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，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：US20070191384A1

公开(公告)日：2007-08-16

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。

公开(公告)号：US20080021046A1

公开(公告)日：2008-01-24

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 ,  A61P25/00 ,  A61P35/00

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/或治疗由GSK3β的异常活性引起的疾病，例如各种其他疾病中的皮克病，例如 在此。

公开(公告)号：US20070010539A1

公开(公告)日：2007-01-11

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： A61K31/519 ,  C07D487/14

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。

公开(公告)号：US20070167455A1

公开(公告)日：2007-07-19

申请号：US11693345

申请日：2007-03-29

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： A61K31/513

CPC分类号： A61K31/506 ,  C07D401/14 ,  C07D487/08

摘要： The invention relates to therapeutic uses of a 2-(diaza-bicyclo-alkyl)-pyrimidone derivative represented by formula (I): Wherein R1, R2, R3, R4 and n are as defined herein. Specifically, the compounds of formula (I) are used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β, such as Alzheimer's disease. The invention relates also to intermediates for the preparation of compound of formula (I).

摘要翻译： 本发明涉及由式（I）表示的2-（二氮杂 - 双环烷基） - 嘧啶酮衍生物的治疗用途：其中R1，R2，R3，R4和n如本文所定义。 具体来说，式（I）化合物可用于预防和/或治疗由诸如阿尔茨海默病的GSK3β异常活动引起的神经变性疾病。 本发明还涉及制备式（I）化合物的中间体。