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1. 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。

2. 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。

3. 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。

4. 发明申请

WO2008155668A3 HETEROARYLAMIDE PYRIMIDONE COMPOUNDS 审中-公开
标题翻译：异丁酰胺吡咯烷酮化合物
公开(公告)号：WO2008155668A3
公开(公告)日：2009-03-12
申请号：PCT/IB2008002445
申请日：2008-05-14
申请人： SANOFI AVENTIS , MITSUBISHI TANABE PHARMA CORP , LOCHEAD ALISTAIR , SAADY MOURAD , VERONIQUE CORINNE , YAICHE PHILIPPE
发明人： LOCHEAD ALISTAIR , SAADY MOURAD , VERONIQUE CORINNE , YAICHE PHILIPPE
IPC分类号： C07D401/12 , A61K31/513 , A61P3/00 , A61P25/00 , C07D239/36 , C07D403/12 , C07D405/12 , C07D409/12
CPC分类号： C07D403/12 , C07D239/36 , C07D401/14 , C07D405/14 , C07D409/14 , C07D471/04
摘要： A pyrimidone derivative represented by Formula (I) or a salt, solvate 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 4-15 membered heterocyclic, group, this group being optionally substituted by 1 to 4 substituents as defined in claim 1; 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; and n represents 0 to 3 and m represents 1 in the form of a free base or of an addition salt with an acid. and a medicament containing the same as a GSKk inhibitor.
摘要翻译：由式（I）表示的嘧啶酮衍生物或其盐，溶剂合物或水合物，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，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4-15元杂环基，该基团任选被1至4个如权利要求1所定义的取代基取代; 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1以游离碱或与酸形成的加成盐的形式。和含有与GSKk抑制剂相同的药物。

5. 发明申请

WO2008155670A2 ARYLAMIDE PYRIMIDONE COMPOUNDS 审中-公开
标题翻译： ARYLAMIDE PYRIMIDONE化合物
公开(公告)号：WO2008155670A2
公开(公告)日：2008-12-24
申请号：PCT/IB2008002458
申请日：2008-05-14
申请人： SANOFI AVENTIS , MITSUBISHI TANABE PHARMA CORP , LOCHEAD ALISTAIR , SAADY MOURAD , VERONIQUE CORINNE , YAICHE PHILIPPE
发明人： LOCHEAD ALISTAIR , SAADY MOURAD , VERONIQUE CORINNE , YAICHE PHILIPPE
CPC分类号： C07D403/04 , A61K9/0019 , A61K9/2018 , A61K9/4858 , C07D413/14
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 C1-6alkyl 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 1 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，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1以游离碱或与酸的加成盐形式的1。

6. 发明申请

WO2005037782A3 DERIVATIVES OF N-[PHENYL(ALKYLPIPERIDINE-2-YL)METHYL]BENZAMIDE, PREPARATION METHOD THEREOF AND APPLICATION OF SAME IN THERAPEUTICS 审中-公开
标题翻译： N- [苯基（阿基哌啶-2-基）甲基]苯甲酰胺的衍生物，其制备方法及其在治疗中的应用
公开(公告)号：WO2005037782A3
公开(公告)日：2005-07-07
申请号：PCT/FR2004002642
申请日：2004-10-15
申请人： SANOFI AVENTIS , DARGAZANLI GIHAD , ESTENNE-BOUHTOU GENEVIEVE , VERONIQUE CORINNE
发明人： DARGAZANLI GIHAD , ESTENNE-BOUHTOU GENEVIEVE , VERONIQUE CORINNE
IPC分类号： A61P25/00 , C07D211/28 , A61K31/445
CPC分类号： C07D211/28
摘要： The invention relates to compounds having general formula (I), wherein: R1 represents a hydrogen atom, an alkyl group, a cycloalkyl group, a cycloalkylalkyl group, a phenylalkyl group, an alkenyl group, or an alkynyl group; R2 represents an alkyl group, a cycloalkyl group, or a cycloalkylalkyl group; X represents a hydrogen atom or one or more halogen atoms and/or trifluoromethyl, alkyl or alkoxy groups; R3 represents a hydrogen atom, or one or more halogen atoms and/or trifluoromethyl, alkyl cycloalkyl, alkoxy, phenyl, cyano, acetyl, benzoyl, thioalkyl, alkylsulfonyl, carboxy or alkoxycarbonyl groups, or a group having formula NR4R5 or SO2NR4R5 or CONR4R5 in which R4 and R5 each represent a hydrogen atom or an alkyl or cycloalkyl group or NR4R5 represents a pyrrolidine, piperidine or morpholine ring. The invention also relates to the use of said compounds in therapeutics.
摘要翻译：本发明涉及具有通式（I）的化合物，其中：R1表示氢原子，烷基，环烷基，环烷基烷基，苯基烷基，烯基或炔基; R2表示烷基，环烷基或环烷基烷基; X表示氢原子或一个或多个卤素原子和/或三氟甲基，烷基或烷氧基; R 3表示氢原子或一个或多个卤素原子和/或三氟甲基，烷基环烷基，烷氧基，苯基，氰基，乙酰基，苯甲酰基，硫代烷基，烷基磺酰基，羧基或烷氧基羰基，或具有式NR4R5或SO2NR4R5或CONR4R5的基团其中R4和R5各自表示氢原子或烷基或环烷基，或NR4R5表示吡咯烷，哌啶或吗啉环。本发明还涉及所述化合物在治疗中的用途。

7. 发明专利

BRPI0811527A2 未知
公开(公告)号：BRPI0811527A2
公开(公告)日：2014-11-18
申请号：BRPI0811527
申请日：2008-05-14
申请人： SANOFI AVENTIS , MITSUBISHI TANABE PHARMA CORP
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
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.

8. 发明专利

NZ581165A HETEROARYLAMIDE PYRIMIDONE COMPOUNDS 未知
公开(公告)号：NZ581165A
公开(公告)日：2011-09-30
申请号：NZ58116508
申请日：2008-05-14
申请人： SANOFI AVENTIS , MITSUBISHI TANABE PHARMA CORP
发明人： LOCHEAD ALISTAIR , SAADY MOURAD , VERONIQUE CORINNE , YAICHE PHILIPPE
IPC分类号： C07D403/12 , A61K31/513 , A61P3/00 , A61P25/00 , C07D239/36 , C07D401/12 , C07D405/12 , C07D409/12
摘要： Disclosed is 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 an alkyl group and a hydrogen atom; Z represents a bond, an oxygen atom, a nitrogen atom substituted by a hydrogen atom or an alkyl group, a sulphur atom, a methylene group; R1 represents a 2, 4 or 5-pyrimidine ring or a 4-pyridine ring; R2 represents a heterocyclic group, R3 represents a hydrogen atom, an alkyl group or a halogen atom; R4 represents a hydrogen atom or an alkyl group; R5 represents a hydrogen atom, an alkyl group; R7 represents a hydrogen atom or an alkyl group; and n represents 0 to 3 and m represents 1 in the form of a free base or of an addition salt with an acid exemplified by [1,5]Naphthyridine-2-carboxylic acid [Z-(1-methyl-6-oxo-1,6-dihydro- [4,4']bipyrimidinyl-2-yl)-ethyl]-amide, 6-Chloro-pyridine-2-carboxylic acid [Z-(1-methyl-6-oxo-1,6-dihydro- [4,4']bipyrimidinyl-2-yl)-ethyl]-amide and 2-Methoxy-N-[2-( 1-methyl-6-oxo-1 ,6-dihydro-[4,4']bipyrimidinyl-2-yl)-ethyl]-amide in treating Alzheimer's disease, Parkinson's disease, tauopathies, vascular dementia; acute stroke, traumatic injuries; cerebrovascular accidents, brain cord trauma, spinal cord trauma; peripheral neuropathies; retinopathies or glaucoma, noninsulin dependent diabetes; obesity; manic depressive illness; schizophrenia; cancers; parenchymal renal diseases or muscle atrophy and malaria. Also disclosed is a process to make said derivative by coupling a pyrimidone amine with a carboxylic acid derivative in basic conditions.

9. 发明专利

AU2007337826A1 Substituted heteroaryl pyridopyrimidone derivatives 未知
公开(公告)号：AU2007337826A1
公开(公告)日：2008-07-03
申请号：AU2007337826
申请日：2007-12-20
申请人： MITSUBISHI TANABE PHARMA CORP , SANOFI AVENTIS
发明人： FAYOL AUDE , VERONIQUE CORINNE , SAADY MOURAD , YAICHE PHILIPPE , GALLET THIERRY , LOCHEAD ALISTAIR
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 C 1-2 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 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, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring; R2 represents a 4-15 membered heterocyclic group , R3 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; R4 and R5 represent, each independently, a hydrogen atom, a C 1-6 alkyl group, optionally substituted by 1 to 4 substituents selected from a halogen atom, a phenyl group, a hydroxyl group or a C 1-6 alkoxy group; R6 represents a hydrogen atom, a C 1-6 alkyl group ; a cycloalkyl group, or a halogen atom; R7 represents a hydrogen atom or a C 1-6 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 GSK3², such as Alzheimer disease.

10. 发明专利

BRPI0811115A2 未知
公开(公告)号：BRPI0811115A2
公开(公告)日：2014-12-23
申请号：BRPI0811115
申请日：2008-05-14
申请人： SANOFI AVENTIS , MITSUBISHI TANABE PHARMA CORP
发明人： LOCHEAD ALISTAIR , SAADY MOURAD , VERONIQUE CORINNE , YAICHE PHILIPPE
IPC分类号： C07D401/12 , A61K31/513 , A61P3/00 , A61P25/00 , C07D239/36 , C07D403/12 , C07D405/12 , C07D409/12
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 1 in the form of a free base or of an addition salt with an acid, and a medicament containing the same as a GSK3² inhibitor.

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