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1. 发明申请

WO2009156861A3 SUBSTITUTED PYRIMIDONE DERIVATIVES 审中-公开
标题翻译：取代的吡咯烷酮衍生物
公开(公告)号：WO2009156861A3
公开(公告)日：2010-04-01
申请号：PCT/IB2009006486
申请日：2009-06-25
申请人： MITSUBISHI TANABE PHARMA CORP , SANOFI AVENTIS , LOCHEAD ALISTAIR , SAADY MOURAD , YAICHE PHILIPPE
发明人： LOCHEAD ALISTAIR , SAADY MOURAD , YAICHE PHILIPPE
IPC分类号： A61K31/519 , A61P25/00 , C07D471/04
CPC分类号： C07D471/04 , A61K31/519
摘要： Pyrimidone derivatives of formula (I) wherein: R1 represents a 4-pyridine ring; R2 represents a hydrogen atom; R3 represents a hydrogen atom; R4 represents : a hydrogen atom; a phenyl ring, this ring being optionally substituted by 1 to 4 substituents selected from a C1-6 alkyl group, a halogen atom, a C1-2 halogenated alkyl group, a hydroxyl group, a C1-6 alkoxy group, a C1-2 halogenated alkoxy group, R5 represents a hydrogen atom, a C1-6 alkyl group, a 4-pyridine group, a phenyl group, these groups being optionally substituted, R6 represents a hydrogen atom, a C1-6 alkyl group, a benzyloxy group, a phenyl C1-6 alkyl group, these groups being optionally substituted, in form of a free base or of an addition salt with an acid. Use in therapeutic.
摘要翻译：式（I）的嘧啶酮衍生物其中：R1表示4-吡啶环; R2表示氢原子; R3表示氢原子; R4表示：氢原子; 苯环，该环任选被1至4个选自C 1-6烷基，卤素原子，C 1-2卤代烷基，羟基，C 1-6烷氧基，C 1-2 卤代烷氧基，R5表示氢原子，C1-6烷基，4-吡啶基，苯基，这些基团任意取代，R6表示氢原子，C1-6烷基，苄氧基，苯基C 1-6烷基，这些基团任选被取代，以游离碱的形式或与酸的加成盐形式。用于治疗。

2. 发明申请

WO2009156861A2 SUBSTITUTED PYRIMIDONE DERIVATIVES 审中-公开
标题翻译：取代的吡咯烷酮衍生物
公开(公告)号：WO2009156861A2
公开(公告)日：2009-12-30
申请号：PCT/IB2009006486
申请日：2009-06-25
申请人： MITSUBISHI TANABE PHARMA CORP , SANOFI AVENTIS , LOCHEAD ALISTAIR , SAADY MOURAD , YAICHE PHILIPPE
发明人： LOCHEAD ALISTAIR , SAADY MOURAD , YAICHE PHILIPPE
IPC分类号： A61K31/519 , A61P25/00 , C07D471/04
CPC分类号： C07D471/04 , A61K31/519
摘要： Pyrimidone derivatives of formula (I) wherein: R1 represents a 4-pyridine ring; R2 represents a hydrogen atom; R3 represents a hydrogen atom; R4 represents : a hydrogen atom; a phenyl ring, this ring being optionally substituted by 1 to 4 substituents selected from a C1-6 alkyl group, a halogen atom, a C1-2 halogenated alkyl group, a hydroxyl group, a C1-6 alkoxy group, a C1-2 halogenated alkoxy group, R5 represents a hydrogen atom, a C1-6 alkyl group, a 4-pyridine group, a phenyl group, these groups being optionally substituted, R6 represents a hydrogen atom, a C1-6 alkyl group, a benzyloxy group, a phenyl C1-6 alkyl group, these groups being optionally substituted, in form of a free base or of an addition salt with an acid. Use in therapeutic.
摘要翻译：式（I）的嘧啶酮衍生物其中：R1表示4-吡啶环; R2表示氢原子; R3表示氢原子; R4表示：氢原子; 苯环，该环任选被1至4个选自C 1-6烷基，卤素原子，C 1-2卤代烷基，羟基，C 1-6烷氧基，C 1-2 卤代烷氧基，R5表示氢原子，C1-6烷基，4-吡啶基，苯基，这些基团任意取代，R6表示氢原子，C1-6烷基，苄氧基，苯基C 1-6烷基，这些基团任选被取代，以游离碱的形式或与酸的加成盐形式。用于治疗。

3. 发明专利

JP2010189422A PHARMACEUTICAL COMPOSITION CONTAINING 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 DERIVATIVE 审中-公开
标题翻译：含有2-嘧啶基-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]吡啶二酮-5（1H，m）的药物组合物）一个衍生物
公开(公告)号：JP2010189422A
公开(公告)日：2010-09-02
申请号：JP2010097989
申请日：2010-04-21
申请人： Mitsubishi Tanabe Pharma Corp , Sanofi-Aventis , サノフィ−アベンティス , 田辺三菱製薬株式会社
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 , A61P9/00 , A61P9/10 , A61P11/00 , A61P15/00 , A61P17/02 , A61P17/14 , A61P19/08 , A61P21/04 , A61P25/00 , A61P25/02 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/28 , A61P25/34 , A61P27/02 , A61P27/06 , A61P35/00 , A61P35/02 , A61P43/00 , C07D487/04
CPC分类号： A61K31/519 , A61K31/551 , C07D487/04
摘要： PROBLEM TO BE SOLVED: To provide a pharmaceutical composition containing a compound useful as an active component of a drug for preventing and/or treating neurodegenerative diseases such as Alzheimer disease. SOLUTION: The pharmaceutical composition contains a substance selected from a group consisting of pyrimidone derivatives represented by formula (I), their salts, their solvates and their hydrates as an active component. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供含有用作预防和/或治疗诸如阿尔茨海默病的神经变性疾病的药物的活性成分的化合物的药物组合物。解决方案：药物组合物含有选自由式（I）表示的嘧啶酮衍生物，其盐，其溶剂合物及其水合物作为活性成分的物质。版权所有（C）2010，JPO＆INPIT

4. 发明申请

WO2009156863A3 SUBSTITUTED TRICYCLIC DERIVATIVES AGAINST NEURODEGENERATIVE DISEASES 审中-公开
标题翻译：针对神经源性疾病的取代三氯甲苯胺衍生物
公开(公告)号：WO2009156863A3
公开(公告)日：2010-03-18
申请号：PCT/IB2009006553
申请日：2009-06-25
申请人： MITSUBISHI TANABE PHARMA CORP , SANOFI AVENTIS , ALMARIO GARCIA ANTONIO , LOCHEAD ALISTAIR , SAADY MOURAD , YAICHE PHILIPPE
发明人： ALMARIO GARCIA ANTONIO , LOCHEAD ALISTAIR , SAADY MOURAD , YAICHE PHILIPPE
IPC分类号： C07D487/04 , A61K31/519 , A61P25/00 , A61P35/00 , C07D519/00
CPC分类号： A01N43/54 , C07D487/04 , C07D519/00
摘要： Substituted Tricyclic Derivatives, Formula (I) wherein: Z represents a bond, a carbonyl group, a methylene group optionally substituted by one or two groups chosen from a Ci-6 alkyl group, a hydroxyl group, a C-?-6 alkoxy group; R1 represents a 4-pyridine ring, a 4-pyrimidine ring; R2 represents a hydrogen atom; R3 represents: a hydrogen atom; a phenyl or a naphthyl group, these groups being optionally substituted, a 5, 6 or 5-6 membered heteroaromatic group, this group being optionally substituted, n represents 0 to 3; m represents 0 to 1, in form of a free base or of an addition salt with an acid. Use in therapeutic
摘要翻译：取代的三环衍生物，式（I）其中：Z表示键，羰基，任选被一个或两个选自C 1-6烷基，羟基，C 1-6烷氧基的基团取代的亚甲基 ; R1代表4-吡啶环，4-嘧啶环; R2表示氢原子; R3表示：氢原子; 苯基或萘基，这些基团任选被取代，5,6或5-6元杂芳基，该基团任选被取代，n代表0至3; m表示0至1，以游离碱的形式或与酸的加成盐形式。用于治疗

5. 发明申请

WO2009095792A3 SUBSTITUTED HETEROARYLAMIDE DIAZEPINOPYRIMIDONE DERIVATIVES 审中-公开
标题翻译：取代的异丁酰胺二氮丙啶衍生物
公开(公告)号：WO2009095792A3
公开(公告)日：2009-10-08
申请号：PCT/IB2009000397
申请日：2009-01-27
申请人： SANOFI AVENTIS , MITSUBISHI TANABE PHARMA CORP , FAYOL AUDE , LOCHEAD ALISTAIR , SAADY MOURAD , VACHE JULIEN , YAICHE PHILIPPE
发明人： FAYOL AUDE , LOCHEAD ALISTAIR , SAADY MOURAD , VACHE JULIEN , YAICHE PHILIPPE
IPC分类号： A61K31/519 , C07D403/04 , C07D487/04
CPC分类号： C07D487/04 , C07D519/00
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof, Formula (I): wherein: Y 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, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the ring being optionally substituted by a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom; R2 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R3 represents a 4-15 membered heterocyclic group, this group being optionally substituted R4 represents a hydrogen atom, a C1-6 alkyl group optionally substituted by 1 to 4 substituents R5 represents a hydrogen atom or a C1-6 alkyl group; and n represents 0 to 3 and their therapeutic use.
摘要翻译：式（I）表示的嘧啶酮衍生物或其盐，或其溶剂化物或其水合物，式（I）：其中：Y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2,3或4-吡啶环或2,4或5-嘧啶环，该环任选被C 1-6烷基，C 1-6烷氧基或卤素原子取代; R2表示氢原子，C1-6烷基或卤素原子; R3表示4-15元杂环基，该基团任选被取代，R 4表示氢原子，任选被1至4个取代基取代的C 1-6烷基表示氢原子或C 1-6烷基; n表示0〜3，其治疗用途。

6. 发明申请

WO2008056266A8 SUBSTITUTED 8-PIPERIDINYL-2-PYRIDINYL-PYRIMIDO [1,2-A]PYRIMIDIN-6-ONE AND 8-PIPERIDINYL-2-PYRIMIDINYL-PYRIMIDO[1,2-A]PYRIMIDIN-6-ONE DERIVATIVES 审中-公开
标题翻译：取代的8-哌啶-2-基 - 吡啶并[1,2-A]嘧啶-6-酮和8-哌啶-2-基]嘧啶并[1,2-A]吡啶-6-酮衍生物
公开(公告)号：WO2008056266A8
公开(公告)日：2009-06-18
申请号：PCT/IB2007004272
申请日：2007-11-06
申请人： SANOFI AVENTIS , MITSUBISHI TANABE PHARMA CORP , LOCHEAD ALISTAIR , SAADY MOURAD , SLOWINSKI FRANCK , YAICHE PHILIPPE
发明人： LOCHEAD ALISTAIR , SAADY MOURAD , SLOWINSKI FRANCK , YAICHE PHILIPPE
IPC分类号： C07D487/04 , A61K31/519 , A61P25/28 , A61P33/06 , A61P35/00 , A61P37/00
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 represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, a carbonyl group or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrirhidine ring, the ring being optionally substituted; R2 represents a benzene ring or a naphthalene ring; the rings being optionally substituted; R3 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R4 represents a hydrogen atom, a C1-6 alkoxy carbonyl group or a C1-6 alkyl group optionally substituted; n represents 0 to 3; p represents 2; q represents 0; o represents 0, 1 or 2 and m represents respectively 4, 3 or 2, o+m being equal to 4. 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：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表示任选取代的键，羰基或亚甲基; R1表示2,3或4-吡啶环或2,4或5-吡啶环，该环任选被取代; R2表示苯环或萘环; 所述环任选被取代; R3表示氢原子，C1-6烷基或卤素原子; R4表示氢原子，C1-6烷氧基羰基或任选取代的C 1-6烷基; n表示0〜3; p表示2; q表示0; o表示0,1或2，m表示4或3或2，o + m等于4.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异常活动引起的神经变性疾病，如阿尔茨海默病。

7. 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。

8. 发明申请

WO2008056266A3 SUBSTITUTED 8-PIPERIDINYL-2-PYRIDINYL-PYRIMIDO [1,2-A]PYRIMIDIN-6-ONE AND 8-PIPERIDINYL-2-PYRIMIDINYL-PYRIMIDO[1,2-A]PYRIMIDIN-6-ONE DERIVATIVES 审中-公开
标题翻译：取代的8-哌啶-2-基 - 吡啶并[1,2-A]嘧啶-6-酮和8-哌啶-2-基]嘧啶并[1,2-A]吡啶-6-酮衍生物
公开(公告)号：WO2008056266A3
公开(公告)日：2008-07-10
申请号：PCT/IB2007004272
申请日：2007-11-06
申请人： SANOFI AVENTIS , MITSUBISHI TANABE PHARMA CORP , LOCHEAD ALISTAIR , SAADY MOURAD , SLOWINSKI FRANCK , YAICHE PHILIPPE
发明人： LOCHEAD ALISTAIR , SAADY MOURAD , SLOWINSKI FRANCK , YAICHE PHILIPPE
IPC分类号： C07D487/04 , A61K31/519 , A61P25/28 , A61P33/06 , A61P35/00 , A61P37/00
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 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, a carbonyl group or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrirhidine ring, the ring being optionally substituted; R2 represents a benzene ring or a naphthalene ring; the rings being optionally substituted; R3 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; R4 represents a hydrogen atom, a C 1-6 alkoxy carbonyl group or a C 1-6 alkyl group optionally substituted; n represents 0 to 3; p represents 2; q represents 0; o represents 0, 1 or 2 and m represents respectively 4, 3 or 2, o+m being equal to 4. 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：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表示任选取代的键，羰基或亚甲基; R1表示2,3或4-吡啶环或2,4或5-吡啶环，该环任选被取代; R2表示苯环或萘环; 所述环任选被取代; R 3表示氢原子，C 1-6烷基或卤素原子; R 4表示氢原子，C 1-6烷氧基羰基或任选取代的C 1-6烷基; n表示0〜3; p表示2; q表示0; o表示0,1或2，m表示4或3或2，o + m等于4.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异常活动引起的神经变性疾病，如阿尔茨海默病。

9. 发明申请

WO2009156860A3 4-(PYRIDIN-4-YL)-1H-(1, 3, 5)TRIAZIN-2-ONE DERIVATIVES AS GSK3-BETA INHIBITORS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES 审中-公开
标题翻译： 4-（PYRIDIN-4-YL）-1H-（1,3,5）TRIAZIN-2-ONE衍生物作为用于治疗神经损伤性疾病的GSK3-β抑制剂
公开(公告)号：WO2009156860A3
公开(公告)日：2010-03-04
申请号：PCT/IB2009006463
申请日：2009-06-25
申请人： MITSUBISHI TANABE PHARMA CORP , SANOFI AVENTIS , LOCHEAD ALISTAIR , SAADY MOURAD , YAICHE PHILIPPE
发明人： LOCHEAD ALISTAIR , SAADY MOURAD , YAICHE PHILIPPE
IPC分类号： C07D401/04 , A61K31/53 , A61P3/10 , A61P25/28 , A61P33/06 , A61P35/00 , C07D487/04
CPC分类号： C07D401/04 , C07D487/04
摘要： A triazinone derivative represented by formula (I) wherein: Z represents a bond, a carbonyl group, a methylene group optionally substituted by one or two groups chosen from a C1-6 alkyl group, a hydroxyl group, a Ci-ß alkoxy group; R1 represents a 4-pyridine ring; R2 represents a hydrogen atom, a C1-6 alkyl; R3 represents a hydrogen atom, a C1-6 alkyl group; R2 and R3 may form together a 6 membered cycle with the nitrogens caring R2 and R3 optionally substituted; R4 represents: a phenyl ring, being optionally substituted; n represents 0 to 2; in form of a free base or of an addition salt with an acid. The compounds of the present invention have GSK3ß inhibitory activity and are useful as an active ingredient of a medicament for preventive and/or therapeutic treatment of diseases caused by abnormal activity of GSK3ß and more particularly of neurodegenerative diseases.
摘要翻译：由式（I）表示的三嗪酮衍生物，其中：Z表示键，羰基，任选被一个或两个选自C 1-6烷基，羟基，C 1-6烷氧基的基团取代的亚甲基; R1表示4-吡啶环; R2表示氢原子，C1-6烷基; R3表示氢原子，C1-6烷基; R2和R3可以一起形成6元环与关心R2和R3任选取代的氮; R4表示：任选被取代的苯环; n表示0〜2; 以游离碱的形式或与酸形成的加成盐。本发明的化合物具有GSK3β抑制活性，可用作用于预防和/或治疗由GSK3β的异常活性引起的疾病，特别是神经变性疾病的药物的活性成分。

10. 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。

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