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1. 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

2. 发明专利

JP2010209089A METHOD FOR PRODUCING INTERMEDIATE OF DERIVATIVE OF 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 审中-公开
标题翻译：用于制备取代的2-吡啶基-6,7,8,9-四氢吡啶并[1,2-a]吡啶并[4']和7-吡啶-2,3-二氢吲哚并[1,2-a]的衍生物的中间体的方法，嘧啶-5（1H） - 酮
公开(公告)号：JP2010209089A
公开(公告)日：2010-09-24
申请号：JP2010098978
申请日：2010-04-22
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： C07D487/04 , 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
CPC分类号： A01N43/90 , C07D213/50 , C07D213/60 , C07D487/04
摘要： PROBLEM TO BE SOLVED: To provide a method for producing a compound to be used for medicines for preventive and/or therapeutic treatment of diseases caused by abnormal activity of GSK3β or GSK3β and cdk5/p25, more particularly, caused by neurodegenerative disorders.
SOLUTION: Substituted 2-pyridinyl-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one and 2,3-dihydro-1H-imidazo[1,2-a]pyrimidin-5-one are produced using a compound represented by general formula (IV), [wherein, R1 indicates a 2, 3 or 4-pyridine ring that may be optionally substituted by a 3-6C cycloalkyl group, a 1-4C alkyl group, a 1-4C alkoxy group, a benzyl group or a halogen atom; R5 indicates a hydrogen atom, a methyl group or a halogen atom; and R indicates an ethyl group].
COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：要解决的问题：提供一种用于制备用于预防和/或治疗由GSK3β或GSK3β和cdk5 / p25的异常活性引起的疾病的药物的化合物的方法，更特别是由神经变性疾病引起的疾病。解决方案：将取代的2-吡啶基-6,7,8,9-四氢-4H-嘧啶并[1,2-a]嘧啶-4-酮和2,3-二氢-1H-咪唑并[1,2- a]嘧啶-5-酮使用由通式（IV）表示的化合物制备，[其中，R 1表示可任选被3-6C环烷基取代的2,3或4-吡啶环， 4C烷基，1-4C烷氧基，苄基或卤素原子; R5表示氢原子，甲基或卤素原子; R表示乙基]。版权所有（C）2010，JPO＆INPIT

3. 发明专利

JP2010159303A Medicinal composition containing 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 derivative 审中-公开
标题翻译：含有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，m）的药物组合物）-ONE衍生
公开(公告)号：JP2010159303A
公开(公告)日：2010-07-22
申请号：JP2010098977
申请日：2010-04-22
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 , A61P17/14 , A61P21/00 , A61P25/00 , A61P25/02 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P25/34 , A61P27/02 , A61P27/06 , A61P35/00 , A61P35/02 , A61P43/00 , C07D213/50 , C07D213/60 , C07D487/04
CPC分类号： A01N43/90 , C07D213/50 , C07D213/60 , C07D487/04
摘要： PROBLEM TO BE SOLVED: To provide a medicinal composition useful as an effective component of a medicine for prevention and/or treatment of abnormal GSK3β, or GSK3β and cdk5/p25 activity, in greater details, disorders caused by neurodegenerative disorder. SOLUTION: This medicinal composition includes as an effective component a material selected from the group consisting of pyrimidon derivatives represented by formula (I) or salts thereof, or their solvates or their hydrates. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：更详细地提供可用作用于预防和/或治疗异常GSK3β或GSK3β和cdk5 / p25活性的药物的有效成分的药物组合物，其由神经变性疾病引起的疾病。解决方案：该药物组合物包括选自由式（I）表示的嘧啶衍生物或其盐或其溶剂化物或其水合物的材料作为有效成分。版权所有（C）2010，JPO＆INPIT

4. 发明申请

WO2008110699A3 AZABICYCLOALKANE DERIVATIVES, PREPARATION THEREOF AND USE THEREOF IN THERAPY 审中-公开
标题翻译：化学药剂衍生物，其制剂及其在治疗中的应用
公开(公告)号：WO2008110699A3
公开(公告)日：2009-01-15
申请号：PCT/FR2008000137
申请日：2008-02-04
申请人： SANOFI AVENTIS , BEN AYAD OMAR , LECLERC ODILE , LOCHEAD ALISTAIR , SAADY MOURAD , SLOWINSKI FRANCK , VACHE JULIEN
发明人： BEN AYAD OMAR , LECLERC ODILE , LOCHEAD ALISTAIR , SAADY MOURAD , SLOWINSKI FRANCK , VACHE JULIEN
IPC分类号： C07D471/08 , A61K31/4748 , A61P9/00 , A61P25/00 , A61P29/00 , C07D487/08
CPC分类号： C07D487/08 , C07D471/08
摘要： The invention relates to compounds of the general formula (I) in which: R is a hydrogen or halogen atom; or a hydroxyl, (C1C6)alkoxy, (C3-C7)cycloalkyl-O- or (C3-C7)cycloalkyl-(C-1- C3)alkylene-O- group; or a heterocycloalkyl, aryl ou heteroaryl group; wherein said group can optionally be substituted by one or more groups selected from halogen atoms, (C1C6)alkyl, (C3-C7)cycloalkyl, (C3- C7)cycloalkyl-(C1-C3)alkylene, (C1-C6)alkoxy, (C3-C7)cycloalkyl-O-, (C3- C7)cycloalkyl-(C1C3)alkylene-O-, (C1-C6)fluoroalkyl, (C1C6)fluoroalkoxy, nitro, cyano, hydroxyl, amino, (C1C6)alkylamino or di(C1-C6)alkylamino, heterocycloalkyl, aryl, aryl-(C1C6)alkylene, heteroaryl, heteroaryl-(C1- C6)alkylene, aryl-O-, -C(O)-(C1C6)alkyl groups, the heterocycloalkyl group being optionally substituted by -C(O)O(CH3)3; n is 1 or 2; m is 1 or 2; o is 1 or 2; in the state of a base or an addition salt to an acid, as well as in the hydrate or solvate state. The invention also relates to a method for preparing the same and to the application in therapy.
摘要翻译：本发明涉及通式（I）的化合物，其中：R为氢或卤素原子; 或羟基，（C 1 -C 6）烷氧基，（C 3 -C 7）环烷基-O-或（C 3 -C 7）环烷基 - （C 1 -C 3）亚烷基-O-基团; 或杂环烷基，芳基杂芳基; 其中所述基团可任选被一个或多个选自卤素原子，（C 1 -C 6）烷基，（C 3 -C 7）环烷基，（C 3 -C 7）环烷基 - （C 1 -C 3）亚烷基，（C 1 -C 6）烷氧基，（C 3 -C 7）环烷基-O-，（C 3 -C 7）环烷基 - （C 1 -C 3）亚烷基-O-，（C 1 -C 6）氟烷基，（C 1 -C 6）氟烷氧基，硝基，氰基，羟基，氨基，（C 1 -C 6）烷基氨基或二（C1-C6）烷基氨基，杂环烷基，芳基，芳基 - （C1C6）亚烷基，杂芳基，杂芳基 - （C1- C6）亚烷基，芳基-O-，-C（O） - （C1C6）烷基，杂环烷基任选被-C（O）O（CH 3）3取代; n为1或2; m为1或2; o是1或2; 以碱的形式或与酸的加成盐以及水合物或溶剂合物状态。本发明还涉及其制备方法及其在治疗中的应用。

5. 发明申请

WO2007057790A2 SUBSTITUTED BICYCLIC PYRIMIDONE DERIVATIVES 审中-公开
标题翻译：取代的双环嘧啶酮衍生物
公开(公告)号：WO2007057790A2
公开(公告)日：2007-05-24
申请号：PCT/IB2006004046
申请日：2006-11-21
申请人： SANOFI AVENTIS , MITSUBISHI PHARMA CORP , CHEREZE NATHALIE , LOCHEAD ALISTAIR , SAADY MOURAD , SLOWINSKI FRANCK , YAICHE PHILIPPE
发明人： CHEREZE NATHALIE , LOCHEAD ALISTAIR , SAADY MOURAD , SLOWINSKI FRANCK , YAICHE PHILIPPE
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 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 substituted by a hydrogen atom or a C 1- 3 alkyl group, a sulphur atom, a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine 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 or a C- 1-6 alkyl group; R5 represents a hydrogen atom, a C 1-6 alkyl group optionally substituted; R6 represents a hydrogen atom, a C 1-6 alkyl 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. 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，或其溶剂化物或其水合物：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表示键，氧原子，被氢原子或C 1〜3烷基取代的氮原子，硫原子，任选被取代的亚甲基; R1代表2,3或4-吡啶环或2,4或5-嘧啶环，所述环任选被取代; R2代表苯环或萘环; 该环任选被取代; R 3表示氢原子，C 1-6烷基或卤素原子; R4代表氢原子或C1-6烷基; R 5表示氢原子，任选取代的C 1-6烷基; R6代表氢原子，C1-6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.本发明还涉及一种药物，其包含所述衍生物或其盐作为活性成分，其用于预防和/或治疗由GSK3β的异常活性引起的神经退行性疾病，如阿尔茨海默病。

6. 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。

7. 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。

8. 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

9. 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。

10. 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。

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