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1. 发明申请

WO2008155669A2 ARYLAMIDE PYRIMIDONE DERIVATIVES 审中-公开
标题翻译：亚胺酰吡咯烷酮衍生物
公开(公告)号：WO2008155669A2
公开(公告)日：2008-12-24
申请号：PCT/IB2008/002446
申请日：2008-05-14
申请人： SANOFI-AVENTIS , MITSUBISHI TANABE PHARMA CORPORATION , CHEREZE, Nathalie , GALLET, Thierry , LOCHEAD, Alistair , SAADY, Mourad , VERONIQUE, Corinne , YAICHE, Philippe
发明人： CHEREZE, Nathalie , GALLET, Thierry , LOCHEAD, Alistair , SAADY, Mourad , VERONIQUE, Corinne , YAICHE, Philippe
CPC分类号： C07D239/36
摘要： A pyrimidone derivative represented by Formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C 1-2 alkyl group and a hydrogen atom; Z represents a bond, an oxygen atom, a nitrogen atom substituted by a hydrogen atom or a C 1-3 alkyl group, a sulphur atom, a methylene group optionally substituted by one or two groups chosen from a C 1-6 alkyl group, a hydroxyl group, a C 1-6 alkoxy group, a C 1-2 perhalogenated alkyl group or an amino group; R1 represents a 2, 4 or 5-pyrimidine ring or a 4-pyridine ring, the ring being optionally substituted by a C 1-6 alkyl group, a C 1-6 alkoxy group or a halogen atom; R2 represents a benzene ring, a naphthalene ring or a benzyl group; the rings being optionally substituted by 1 to 4 substituents selected from a C 1-6 alkyl group, C 3-7 cycloalkyl group, a C 3-7 cycloalkyl-C 1-6 alkyl group, a halogen atom, a C 1-2 perhalogenated alkyl group, a C 1-3 halogenated alkyl group, a hydroxyl group, an heteroaryl group optionally substituted by a C 1-6 alkyl group, C 3-7 cycloalkyl group, a C 3-7 cycloalkyl-C 1-6 alkyl group, C 1-6 alkoxy group optionally substituted by a C 3-5 cycloalkyl group, a C 1-2 perhalogenated alkoxy group, a C 1-6 alkylsulfonyl group, a nitro, a cyano, an amino, a C 1-6 monoalkylamino group or a C 2-12 dialkylamino group, an acetoxy group or an aminosulfonyl group; R3 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; R4 represents a hydrogen atom or a C 1-6 alkyl group; R5 represents a hydrogen atom, a C 1-6 alkyl group; R6 represents a hydrogen atom, a C 1-6 alkyl group; R7 represents a hydrogen atom or a C 1-6 alkyl group; n represents 0 to 3 and m represents 0 in the form of a free base or of an addition salt with an acid.
摘要翻译：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表示2个氢原子，硫原子，氧原子或C 1-2烷基和氢原子; Z表示键，氧原子，被氢原子或C1-3烷基取代的氮原子，硫原子，任选被一个或两个选自C 1-6烷基，羟基的基团取代的亚甲基基团，C1-6烷氧基，C1-2全卤代烷基或氨基; R1表示2,4或5-嘧啶环或4-吡啶环，该环任选被C 1-6烷基，C 1-6烷氧基或卤素原子取代; R2表示苯环，萘环或苄基; 该环任选被1至4个选自C 1-6烷基，C 3-7环烷基，C 3-7环烷基-C 1-6烷基，卤素原子，C 1-2全卤代烷基， C 1-3卤代烷基，羟基，任选被C 1-6烷基取代的杂芳基，C 3-7环烷基，C 3-7环烷基-C 1-6烷基，任选被 C3-5环烷基，C1-2全卤代烷氧基，C1-6烷基磺酰基，硝基，氰基，氨基，C1-6单烷基氨基或C2-12二烷基氨基，乙酰氧基或氨基磺酰基; R3表示氢原子，C1-6烷基或卤素原子; R4表示氢原子或C1-6烷基; R5表示氢原子，C1-6烷基; R6表示氢原子，C1-6烷基; R7表示氢原子或C1-6烷基; n表示0〜3，m表示0以游离碱或与酸形成的加成盐形式。

2. 发明申请

WO2008078196A3 SUBSTITUTED HETEROARYL PYRIDOPYRIMIDONE DERIVATIVES 审中-公开
公开(公告)号：WO2008078196A3
公开(公告)日：2008-07-03
申请号：PCT/IB2007/004409
申请日：2007-12-20
申请人： SANOFI-AVENTIS , MITSUBISHI TANABE PHARMA CORPORATION , FAYOL, Aude , GALLET, Thierry , LOCHEAD, Alistair , SAADY, Mourad , VERONIQUE, Corinne , YAICHE, Philippe
发明人： FAYOL, Aude , GALLET, Thierry , LOCHEAD, Alistair , SAADY, Mourad , VERONIQUE, Corinne , YAICHE, Philippe
IPC分类号： C07D239/70 , A61K31/517 , A61P25/00
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: Y represents two hydrogen atoms, a sulfur atom, an oxygen atom or a Ci-2 alkyl group and a hydrogen atom; Z represents a bond, an oxygen atom, a nitrogen atom, a sulphur atom, a methylene group optionally substituted by one or two groups chosen from a Ci-6 alkyl group, a hydroxyl group, a Ci-6 alkoxy group, a Ci_2 perhalogenated alkyl group or an amino group; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring; R2 represents an optionally substituted 4-15 membered heterocyclic group; R3 represents a hydrogen atom, a Ci-6 alkyl group or a halogen atom; R4 and R5 represent, each independently, a hydrogen atom, a Ci-6 alkyl group, optionally substituted by 1 to 4 substituents selected from a halogen atom, a phenyl group, a hydroxyl group or a Ci-6 alkoxy group; R6 represents a hydrogen atom, a Ci-6 alkyl group; a cycloalkyl group, or a halogen atom; R7 represents a hydrogen atom or a Ci-6 alkyl group; n represents 0 to 3; m represents 0 to 1; o represents 0 to 2; in the form of a free base or of an addition salt with an acid. 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.

3. 发明申请

WO2003027116A3 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 审中-公开
公开(公告)号：WO2003027116A3
公开(公告)日：2003-04-03
申请号：PCT/EP2002/011128
申请日：2002-09-19
申请人： SANOFI-SYNTHELABO , MITSUBISHI PHARMA CORPORATION , GALLET, Thierry , LARDENOIS, Patrick , LOCHEAD, Alistair , MARGUERIE, Séverine , NEDELEC, Alain , SAADY, Mourad , SLOWINSKI, Franck , YAICHE, Philippe
发明人： GALLET, Thierry , LARDENOIS, Patrick , LOCHEAD, Alistair , MARGUERIE, Séverine , NEDELEC, Alain , SAADY, Mourad , SLOWINSKI, Franck , YAICHE, Philippe
IPC分类号： 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 C 1-2 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 C 1-6 alkyl group optionally; a C 3-6 cycloalkyl group, a C 1-4 alkythio group, a C 1-4 alkoxy group, a C 1-2 perhalogenated alkyl group, a C 1-3 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 C 1-6 alkyl group, a hydroxy group, a C 1-4 alkoxy group or a halogen atom; R5 represents a hydrogen atom, a C 1-6 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.

4. 发明申请

WO03027116A2 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 审中-公开
标题翻译：取代的2-吡啶基-6,7,8,9-四氢吡啶并[1,2-A]嘧啶-4-酮和7-吡啶-2,3-二氢吲哚并[1,2-A]嘧啶-5（1H）酮衍生物
公开(公告)号：WO03027116A2
公开(公告)日：2003-04-03
申请号：PCT/EP0211128
申请日：2002-09-19
申请人： SANOFI SYNTHELABO , MITSUBISHI PHARMA CORP , GALLET THIERRY , LARDENOIS PATRICK , LOCHEAD ALISTAIR , MARGUERIE SEVERINE , NEDELEC ALAIN , SAADY MOURAD , SLOWINSKI FRANCK , YAICHE PHILIPPE
发明人： GALLET THIERRY , LARDENOIS PATRICK , LOCHEAD ALISTAIR , MARGUERIE SEVERINE , NEDELEC ALAIN , SAADY MOURAD , SLOWINSKI FRANCK , YAICHE PHILIPPE
IPC分类号： A61K31/519 , A61P3/04 , A61P3/10 , A61P9/10 , A61P17/14 , A61P25/00 , A61P25/02 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/06 , A61P35/00 , A61P43/00 , C07D213/50 , C07D213/60 , C07D487/04
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 GSK3 beta or GSK3 beta 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 1-2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，羟基亚氨基亚甲基，二氧戊环基，任选取代的氮原子; 或任选取代的亚甲基; 或任选取代的亚甲基; R1表示任选取代的2,3或4-吡啶环; R 2可以任选地表示C 1-6烷基; C 3-6环烷基，C 1-4链炔基，C 1-4烷氧基，C1-2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，C1-6烷基或卤素原子; 条件是当R 3和R 4各自表示氢原子时，R 5不是氢原子。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的预防和/或治疗，例如阿尔茨海默病。

5. 发明申请

WO2008155669A3 ARYLAMIDE PYRIMIDONE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES 审中-公开
标题翻译：用于治疗神经损伤性疾病的亚胺酰吡咯烷酮衍生物
公开(公告)号：WO2008155669A3
公开(公告)日：2009-06-04
申请号：PCT/IB2008002446
申请日：2008-05-14
申请人： SANOFI AVENTIS , MITSUBISHI TANABE PHARMA CORP , CHEREZE NATHALIE , GALLET THIERRY , LOCHEAD ALISTAIR , SAADY MOURAD , VERONIQUE CORINNE , YAICHE PHILIPPE
发明人： CHEREZE NATHALIE , GALLET THIERRY , LOCHEAD ALISTAIR , SAADY MOURAD , VERONIQUE CORINNE , YAICHE PHILIPPE
IPC分类号： C07D239/36 , A61K31/513 , A61P25/00
CPC分类号： C07D239/36
摘要： A pyrimidone derivative represented by Formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Z represents a bond, an oxygen atom, a nitrogen atom substituted by a hydrogen atom or a C1-3 alkyl group, a sulphur atom, a methylene group optionally substituted by one or two groups chosen from a C1-6 alkyl group, a hydroxyl group, a C1-6 alkoxy group, a C1-2 perhalogenated alkyl group or an amino group; R1 represents a 2, 4 or 5-pyrimidine ring or a 4-pyridine ring, the ring being optionally substituted by a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom; R2 represents a benzene ring, a naphthalene ring or a benzyl group; the rings being optionally substituted by 1 to 4 substituents selected from a C1-6 alkyl group, C3-7 cycloalkyl group, a C3-7 cycloalkyl-C1-6 alkyl group, a halogen atom, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a hydroxyl group, an heteroaryl group optionally substituted by a C1-6 alkyl group, C3-7 cycloalkyl group, a C3-7 cycloalkyl-C1-6 alkyl group, C1-6 alkoxy group optionally substituted by a C3-5 cycloalkyl group, a C1-2 perhalogenated alkoxy group, a C1-6 alkylsulfonyl group, a nitro, a cyano, an amino, a C1-6 monoalkylamino group or a C2-12 dialkylamino group, an acetoxy group or an aminosulfonyl group; R3 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R4 represents a hydrogen atom or a C1-6 alkyl group; R5 represents a hydrogen atom, a C1-6 alkyl group; R6 represents a hydrogen atom, a C1-6 alkyl group; R7 represents a hydrogen atom or a C1-6 alkyl group; n represents 0 to 3 and m represents 0 in the form of a free base or of an addition salt with an acid.
摘要翻译：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表示2个氢原子，硫原子，氧原子或C 1-2烷基和氢原子; Z表示键，氧原子，被氢原子或C1-3烷基取代的氮原子，硫原子，任选被一个或两个选自C 1-6烷基，羟基的基团取代的亚甲基基团，C1-6烷氧基，C1-2全卤代烷基或氨基; R1表示2,4或5-嘧啶环或4-吡啶环，该环任选被C 1-6烷基，C 1-6烷氧基或卤素原子取代; R2表示苯环，萘环或苄基; 该环任选被1至4个选自C 1-6烷基，C 3-7环烷基，C 3-7环烷基-C 1-6烷基，卤素原子，C 1-2全卤代烷基， C 1-3卤代烷基，羟基，任选被C 1-6烷基取代的杂芳基，C 3-7环烷基，C 3-7环烷基-C 1-6烷基，任选被 C3-5环烷基，C1-2全卤代烷氧基，C1-6烷基磺酰基，硝基，氰基，氨基，C1-6单烷基氨基或C2-12二烷基氨基，乙酰氧基或氨基磺酰基; R3表示氢原子，C1-6烷基或卤素原子; R4表示氢原子或C1-6烷基; R5表示氢原子，C1-6烷基; R6表示氢原子，C1-6烷基; R7表示氢原子或C1-6烷基; n表示0〜3，m表示0以游离碱或与酸形成的加成盐形式。

6. 发明申请

WO2008155666A2 HETEROARYLAMIDE PYRIMIDONE DERIVATIVES 审中-公开
标题翻译：异烟酰胺吡咯烷酮衍生物
公开(公告)号：WO2008155666A2
公开(公告)日：2008-12-24
申请号：PCT/IB2008/002429
申请日：2008-05-14
申请人： SANOFI-AVENTIS , MITSUBISHI TANABE PHARMA CORPORATION , CHEREZE, Nathalie , GALLET, Thierry , LOCHEAD, Alistair , SAADY, Mourad , VERONIQUE, Corinne , YAICHE, Philippe
发明人： CHEREZE, Nathalie , GALLET, Thierry , LOCHEAD, Alistair , SAADY, Mourad , VERONIQUE, Corinne , YAICHE, Philippe
CPC分类号： C07D403/14 , C07D239/38 , C07D401/14 , C07D409/14 , C07D417/14 , C07D471/04
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C 1-2 alkyl group and a hydrogen atom; Z represents a bond, an oxygen atom, a nitrogen atom substituted by a hydrogen atom or a C 1-3 alkyl group, a sulphur atom, a methylene group optionally substituted by one or two groups chosen from a C 1-6 alkyl group, a hydroxyl group, a C 1-6 alkoxy group, a C 1-2 perhalogenated alkyl group or an amino group; R1 represents a 2, 4 or 5-pyrimidine ring or a 4- pyridine ring, the ring being optionally substituted by a C 1-6 alkyl group, a C 1-6 alkoxy group or a halogen atom; R2 represents a 4-15 membered heterocyclic group, this group being optionally substituted by 1 to 4 substituents selected from a C 1-6 alkyl group, a halogen atom, a C 1-2 perhalogenated alkyl group, a C 1-6 halogenated alkyl group, a hydroxyl group, a C 1-6 alkoxy group, a C 1-2 perhalogenated alkoxy group, a C 1-6 halogenated alkoxy group, a nitro, a cyano, an amino, a C 1-6 monoalkylamino group, a C 2-12 dialkylamino group, a S-(C 1-6 - alkyl) group, an heterocyclic group, an aryl group, an heteroaryl group, a O-aryl group or a S-aryl group, the above-mentioned groups being optionally substituted by 1 to 4 substituents selected from a C 1-6 alkyl group, a halogen atom, a C 1-6 alcoxy group, a C(O)O (C 1-6 -alkyl) or a C(O)O (aryl) group, the aryl optionally substituted by 1 to 4 substituents selected from a C 1-6 alkyl group, a halogen atom, a C 1-6 alcoxy group; R3 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; R4 represents a hydrogen atom or a C 1-6 alkyl group; R5 represents a hydrogen atom, a C 1-6 alkyl group; R6 represents a hydrogen atom, a C 1-6 alkyl group; R7 represents a hydrogen atom or a C 1-6 alkyl group; and n represents 0 to 3 and m represents 0 in the form of a free base or of an addition salt with an acid.
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：X表示两个氢原子，硫原子，氧原子或C 1-2烷基和氢原子; Z表示键，氧原子，被氢原子或C1-3烷基取代的氮原子，硫原子，任选被一个或两个选自C 1-6烷基，羟基的基团取代的亚甲基基团，C 1-6烷氧基，C1-2全卤代烷基或氨基; R1表示2,4或5-嘧啶环或4-吡啶环，该环任选被C 1-6烷基，C 1-6烷氧基或卤素原子取代; R2表示4-15元杂环基，该基团任选被1至4个选自C 1-6烷基，卤素原子，C 1-2烷基卤代烷基，C 1-6卤代烷基，C 1-6卤代烷基，羟基，C1-6烷氧基，C1-2全卤代烷氧基，C1-6卤代烷氧基，硝基，氰基，氨基，C1-6一烷基氨基，C2-12二烷基氨基， S-（C 1-6 - 烷基）基，杂环基，芳基，杂芳基，O-芳基或S-芳基，上述基团任选被1至4个选自 C 1-6烷基，卤素原子，C 1-6烷氧基，C（O）O（C 1-6 - 烷基）或C（O）O（芳基）），任选地被1〜选自C 1-6烷基，卤素原子，C 1-6烷氧基的4个取代基; R3表示氢原子，C1-6烷基或卤素原子; R4表示氢原子或C1-6烷基; R5表示氢原子，C1-6烷基; R6表示氢原子，C1-6烷基; R7表示氢原子或C1-6烷基; n表示0〜3，m表示0以游离碱或与酸形成的加成盐。

7. 发明申请

WO9850383A8 5-PHENYL-1,3,4-OXADIAZOL-2(3H)-ONE DERIVATIVES AND THEIR USE AS 5-HT4 LIGANDS 审中-公开
标题翻译： 5-苯基-1,3,4-氧杂双酚-2（3H） - 酮衍生物及其作为5-HT 4配体的用途
公开(公告)号：WO9850383A8
公开(公告)日：1999-04-22
申请号：PCT/FR9800886
申请日：1998-05-04
申请人： SYNTHELABO , JEGHAM SAMIR , LOCHEAD ALISTAIR , NEDELEC ALAIN , GALLI FREDERIC , GALLET THIERRY
发明人： JEGHAM SAMIR , LOCHEAD ALISTAIR , NEDELEC ALAIN , GALLI FREDERIC , GALLET THIERRY
IPC分类号： C07D405/14 , A61K31/4245 , A61K31/439 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/551 , A61P1/00 , A61P9/00 , A61P25/00 , A61P43/00 , C07D413/04 , C07D413/06 , C07D413/14 , C07D453/02 , A61K31/41 , A61K31/435 , A61K31/445 , A61K31/46 , A61K31/47 , A61K31/495 , A61K31/55 , C07D271/113 , C07D451/02
CPC分类号： C07D413/06 , C07D413/14 , C07D453/02
摘要： The invention concerns compounds of general formula (I) in which R1 represents H, an alkyl or a cycloalkylmethyl, X1 represents H or an alkoxy, or OR1 and X1 together represent a -OCH2O-, -O(CH2)2-, -O(CH2)3-, O(CH2)2O- or -O(CH2)3O- group, X2 represents H, an amino group or a -NHCO2R group in which R represents an alkyl or a phenylalkyl, X3 represents H or a halogen, n represents number 0, 1, 2, or 3, and Het represents either a pyrrolidin-1-yl group, or a piperidin-1-yl group optionally substituted, or a 1H-hexahydroazepin-1-yl group, or an 8-azabicyclo{3.2.1}oct-8-yl group, or a 4-(phenylmethyl)piperazin-1-yl group, or a 4-methyl-hexahydro-1,4-diazepin-1-yl group, or a 1,2,3,4-tetrahydrisoquinolin-2-yl group, or a 1-azabicyclo{2.2.2}oct-3-yl group. The invention is applicable in therapy. Said compounds are useful for preventing disorders in which 5-HT4 receptors are involved, whether in the central nervous, the gastrointestinal, the cardiovascular or the urinary system.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1表示H，烷基或环烷基甲基，X 1表示H或烷氧基，或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-O（CH 2）3 O-基，X 2表示H，其中R表示烷基或苯基烷基的氨基或-NHCO 2 R基，X 3表示H或卤素，n表示数0,1,2或3，Het表示任选取代的吡咯烷-1-基或哌啶-1-基，或1H-六氢氮杂-1-基或8 - 氮杂双环{3.2.1}辛-8-基或4-（苯基甲基）哌嗪-1-基或4-甲基 - 六氢-1,4-二氮杂-1-基或1 ，2,3,4-四氢化喹啉-2-基或1-氮杂双环{2.2.2}辛-3-基。本发明适用于治疗。所述化合物可用于预防5-HT 4受体参与的疾病，无论是在中枢神经，胃肠道，心血管或泌尿系统中。

8. 发明申请

WO2008155666A3 HETEROARYLAMIDE-SUBSTITUTED PYRIMIDONE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES 审中-公开
标题翻译：用于治疗神经损伤性疾病的异氟醚取代的吡咯烷酮衍生物
公开(公告)号：WO2008155666A3
公开(公告)日：2009-04-09
申请号：PCT/IB2008002429
申请日：2008-05-14
申请人： SANOFI AVENTIS , MITSUBISHI TANABE PHARMA CORP , CHEREZE NATHALIE , GALLET THIERRY , LOCHEAD ALISTAIR , SAADY MOURAD , VERONIQUE CORINNE , YAICHE PHILIPPE
发明人： CHEREZE NATHALIE , GALLET THIERRY , LOCHEAD ALISTAIR , SAADY MOURAD , VERONIQUE CORINNE , YAICHE PHILIPPE
IPC分类号： C07D239/38 , A61K31/495 , A61P3/00 , A61P25/00 , A61P35/00 , C07D401/14 , C07D403/14 , C07D409/14 , C07D417/14 , C07D471/04
CPC分类号： C07D403/14 , C07D239/38 , C07D401/14 , C07D409/14 , C07D417/14 , C07D471/04
摘要： A pyrimidone derivative represented by Formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Formula (I). The compounds (I) are suitable for the treatment of neurodegenerative diseases.
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：式（I）。化合物（I）适用于治疗神经变性疾病。

9. 发明申请

WO2008078196A2 SUBSTITUTED HETEROARYL PYRIDOPYRIMIDONE DERIVATIVES 审中-公开
标题翻译：取代的杂芳基吡啶并嘧啶酮衍生物
公开(公告)号：WO2008078196A2
公开(公告)日：2008-07-03
申请号：PCT/IB2007004409
申请日：2007-12-20
申请人： SANOFI AVENTIS , MITSUBISHI TANABE PHARMA CORP , FAYOL AUDE , GALLET THIERRY , LOCHEAD ALISTAIR , SAADY MOURAD , VERONIQUE CORINNE , YAICHE PHILIPPE
发明人： FAYOL AUDE , GALLET THIERRY , LOCHEAD ALISTAIR , SAADY MOURAD , VERONIQUE CORINNE , YAICHE PHILIPPE
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: wherein: Y represents two hydrogen atoms, a sulfur atom, an oxygen atom or a Ci-2 alkyl group and a hydrogen atom; Z represents a bond, an oxygen atom, a nitrogen atom, a sulphur atom, a methylene group optionally substituted by one or two groups chosen from a Ci-6 alkyl group, a hydroxyl group, a Ci-6 alkoxy group, a Ci_2 perhalogenated alkyl group or an amino group; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring; R2 represents an optionally substituted 4-15 membered heterocyclic group; R3 represents a hydrogen atom, a Ci-6 alkyl group or a halogen atom; R4 and R5 represent, each independently, a hydrogen atom, a Ci-6 alkyl group, optionally substituted by 1 to 4 substituents selected from a halogen atom, a phenyl group, a hydroxyl group or a Ci-6 alkoxy group; R6 represents a hydrogen atom, a Ci-6 alkyl group; a cycloalkyl group, or a halogen atom; R7 represents a hydrogen atom or a Ci-6 alkyl group; n represents 0 to 3; m represents 0 to 1; o represents 0 to 2; in the form of a free base or of an addition salt with an acid. 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 GSK3ß, such as Alzheimer disease.
摘要翻译：式（I）代表的嘧啶酮衍生物或其盐，或其溶剂合物或其水合物：其中：Y代表两个氢原子，硫原子，氧原子或C 1-2烷基和氢原子; Z代表键，氧原子，氮原子，硫原子，任选被选自C 1-6烷基基团，羟基，C 1-6烷氧基的组中选择一个或两个基团取代的亚甲基，C 1-2氟烷全卤代烷基或氨基; R1代表2,3或4-吡啶环或2,4或5-嘧啶环; R2代表任选取代的4-15元杂环基; R 3代表氢原子，C 1-6烷基或卤素原子; R 4和R 5各自独立地表示氢原子，任选被1至4个选自卤素原子，苯基，羟基或C 1-6烷氧基的取代基取代的C 1-6烷基; R6代表氢原子，C1-6烷基; 环烷基或卤素原子; R 7代表氢原子或C 1-6烷基; n表示0至3; m代表0至1; o代表0至2; 以游离碱或与酸加成盐的形式存在。本发明还涉及包含其所述衍生物或其盐作为用于引起GSK3ß的异常活性，如阿尔茨海默病的神经变性疾病的预防性和/或治疗性治疗的有效成分的药物。

10. 发明申请

WO2003027115A1 SUBSTITUTED 2-PYRIMIDINYL-6,7,8,9-TETRAHYDROPYRIMIDO[1,2-A]PYRIMIDIN-4-ONE AND 7-PYRIMIDINYL-2,3-DIHYDROIMIDAZO[1,2-A]PYRIMIDIN-5(1H)ONE DERIVATIVES FOR NEURODEGENERATIVE DISORDERS 审中-公开
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-嘧啶基-2,3-二氢吲哚并[1,2-A]嘧啶-5（1H）酮神经损伤性疾病的衍生物
公开(公告)号：WO2003027115A1
公开(公告)日：2003-04-03
申请号：PCT/EP2002/011127
申请日：2002-09-19
申请人： SANOFI-SYNTHELABO , MITSUBISHI PHARMA CORPORATION , GALLET Thierry , LARDENOIS, Patrick , LOCHEAD, Alistair , MARGUERIE, Séverine , NEDELEC, Alain , SAADY, Mourad , SLOWINSKI, Franck , YAICHE, Philippe
发明人： GALLET Thierry , LARDENOIS, Patrick , LOCHEAD, Alistair , MARGUERIE, Séverine , NEDELEC, Alain , SAADY, Mourad , SLOWINSKI, Franck , YAICHE, Philippe
IPC分类号： C07D487/04
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 C 1-2 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 C 1-6 alkyl group optionally substituted by a C 6,10 aryloxy or a C 6,10 arylamino group; a C 3-6 cycloalkyl group, a C 1-4 alkylthio group, a C 1-4 alkoxy group, a C 1-2 perhalogenated alkyl group, a C 1-3 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, C 1-6 alkyl group, a hydroxy group, a C 1- 4 alkoxy group or a halogen atom; R5 represents a hydrogen atom, a C 1-6 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 1-2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; R2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，C1-2全卤代烷基，C1-3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; R3和R4各自独立地表示氢原子，C1-6烷基，羟基，C1-4烷氧基或卤素原子; R5表示氢原子，C1-6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，如阿尔茨海默病。

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