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。

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：US07001902B2

公开(公告)日：2006-02-21

申请号：US10276822

申请日：2001-05-29

申请人： Thierry Gallet ,  Frédéric Galli ,  Odile Leclerc ,  Alistair Lochead

发明人： Thierry Gallet ,  Frédéric Galli ,  Odile Leclerc ,  Alistair Lochead

IPC分类号： A61P25/00 ,  A61K31/55 ,  C07D471/08

CPC分类号： C07D471/08

摘要： Compound corresponding to the general formula (I) in which R1, R2, R3, R4 and R5 each represent a hydrogen or halogen atom or a nitro, amino, trifluoromethyl, trifluoroalkoxy, cyano, hydroxyl, (C1–C6)alkyl or (C1–C6)alkoxy group and R6 represents a (C1–C6)alkyl group. Therapeutic application.

摘要翻译： 对应于通式（I）的化合物<化学式id =“CHEM-US-00001”num =“000

公开(公告)号：US08198287B2

公开(公告)日：2012-06-12

申请号：US12487270

申请日：2009-06-18

申请人： Aude Fayol ,  Thierry Gallet ,  Alistair Lochead ,  Mourad Saady ,  Corinne Veronique ,  Philippe Yaiche

发明人： Aude Fayol ,  Thierry Gallet ,  Alistair Lochead ,  Mourad Saady ,  Corinne Veronique ,  Philippe Yaiche

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D239/70

CPC分类号： A01N43/90 ,  C07D239/70

摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof are disclosed and claimed. Wherein m, n, o, Y, Z, R1, R2, R3, R4, R5 R6 and R7 are as described herein. Also disclosed are the salts of compounds of formula (I). 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： 公开并要求保护由式（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m，n，o，Y，Z，R 1，R 2，R 3，R 4，R 5，R 6和R 7如本文所述。 还公开了式（I）化合物的盐。 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：US20090306088A1

公开(公告)日：2009-12-10

申请号：US12487270

申请日：2009-06-18

申请人： Aude FAYOL ,  Thierry GALLET ,  Alistair LOCHEAD ,  Mourad SAADY ,  Corinne VERONIQUE ,  Philippe YAICHE

发明人： Aude FAYOL ,  Thierry GALLET ,  Alistair LOCHEAD ,  Mourad SAADY ,  Corinne VERONIQUE ,  Philippe YAICHE

IPC分类号： A61K31/519 ,  C07D471/04 ,  A61P25/00

CPC分类号： A01N43/90 ,  C07D239/70

摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof are disclosed and claimed. Wherein m, n, o, Y, Z, R1, R2, R3, R4, R5 R6 and R7 are as described herein. Also disclosed are the salts of compounds of formula (I). 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： 公开并要求保护由式（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m，n，o，Y，Z，R 1，R 2，R 3，R 4，R 5，R 6和R 7如本文所述。 还公开了式（I）化合物的盐。 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：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 。

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：US06974819B2

公开(公告)日：2005-12-13

申请号：US10362850

申请日：2001-08-31

申请人： Antonio Almario Garcia ,  Thierry Gallet ,  Adrien Tak Li ,  Alistair Lochead ,  Séverine Marguerie ,  Alain Nedelec ,  Mourad Saady ,  Philippe Yaiche

发明人： Antonio Almario Garcia ,  Thierry Gallet ,  Adrien Tak Li ,  Alistair Lochead ,  Séverine Marguerie ,  Alain Nedelec ,  Mourad Saady ,  Philippe Yaiche

IPC分类号： A61K31/519 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P17/14 ,  A61P23/02 ,  A61P25/00 ,  A61P25/02 ,  A61P25/16 ,  A61P25/24 ,  A61P25/28 ,  A61P27/06 ,  A61P35/00 ,  A61P35/02 ,  C07D487/04

CPC分类号： C07D487/04 ,  A61K31/519

摘要： Imidazo[1,2-α]pyrimidinones and pyrimido[1,2-α]pyrimidinones useful for preventive and/or therapeutic treatment of neurodegenerative diseases, such as Alzheimer's disease, caused by abnormal GSK3β activity.

摘要翻译： 咪唑并[1,2-α]嘧啶酮和嘧啶并[1,2-α]嘧啶酮，用于预防和/或治疗由异常GSK3β活性引起的神经变性疾病，如阿尔茨海默病。

公开(公告)号：US06255319B1

公开(公告)日：2001-07-03

申请号：US09403003

申请日：1999-10-15

申请人： Samir Jegham ,  Alistair Lochead ,  Frédéric Galli ,  Alain Nedelec ,  Axelle Samson ,  Thierry Gallet

发明人： Samir Jegham ,  Alistair Lochead ,  Frédéric Galli ,  Alain Nedelec ,  Axelle Samson ,  Thierry Gallet

IPC分类号： A61K3146

CPC分类号： C07D451/04

摘要： Compound of general formula (I) in which R1 represents an alkyl or cycloalkylmethyl group, X1 represents a hydrogen or halogen atom or an alkoxy group, or alternatively OR1 and X1 together represent an —OCH2O—, —O(CH2)2—, —O(CH2)3—, —O(CH2)2O— or —(CH2)3O— group, X2 represents a hydrogen atom or an amino group, X3 represents a hydrogen or halogen atom, and R2 represents a hydrogen atom, an optionally substituted alkyl group, an optionally substituted phenylalkyl group or a group —(CH2)nCO—Z in which n represents a number from 1 to 6 and Z represents a 1-piperidyl group. Therapeutic application.

摘要翻译： 通式（I）的化合物，其中R 1表示烷基或环烷基甲基，X 1表示氢或卤素原子或烷氧基，或者OR 1和X 1一起表示-OCH 2 O-，-O（CH 2）2 - O（CH 2）3 - ， - O（CH 2）2 O-或 - （CH 2）3 O-基，X 2表示氢原子或氨基，X 3表示氢或卤素原子，R 2表示氢原子， 取代的烷基，任选取代的苯基烷基或基团 - （CH 2）n CO-Z，其中n表示1至6的数，Z表示1-哌啶基。 治疗应用。

公开(公告)号：US6143761A

公开(公告)日：2000-11-07

申请号：US381098

申请日：1999-09-15

申请人： Alistair Lochead ,  Samir Jegham ,  Frederic Galli ,  Thierry Gallet

发明人： Alistair Lochead ,  Samir Jegham ,  Frederic Galli ,  Thierry Gallet

IPC分类号： A61K31/4355 ,  A61P1/00 ,  A61P25/00 ,  A61P43/00 ,  C07D491/04 ,  C07D491/048 ,  A61K31/435

CPC分类号： C07D491/04

摘要： Compounds corresponding to the general formula (I) ##STR1## in which R.sub.1 represents a hydrogen atom, a (C.sub.1 -C.sub.6)alkyl group or a phenyl(C.sub.1 -C.sub.4)alkyl group, R.sub.2 represents a hydrogen atom or a (C.sub.1 -C.sub.6)alkyl group and R.sub.3, R.sub.4 and R.sub.5 each represent, independently of one another, a hydrogen or halogen atom or a trifluoromethyl, cyano, hydroxyl, (C.sub.1 -C.sub.6)alkyl or (C.sub.1 -C.sub.6)alkoxy group. Application in therapeutics.

摘要翻译： PCT No.PCT / FR98 / 00531 Sec。 371日期1999年9月15日 102（e）1999年9月15日PCT提交1998年3月17日PCT公布。 出版物WO98 / 42713 日期：1998年10月1日对应于通式（I）的化合物，其中R1表示氢原子，（C1-C6）烷基或苯基（C1-C4）烷基，R2表示氢原子或（C1 -C 6）烷基，R 3，R 4和R 5各自独立地表示氢或卤素原子或三氟甲基，氰基，羟基，（C 1 -C 6）烷基或（C 1 -C 6）烷氧基。 在治疗中的应用。