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1. 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。

2. 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。

3. 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。

4. 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。

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

WO2004082577A3 8-SUBSTITUTED-6, 7, 8, 9-TETRAHYDROPYRIMIDO[1,2-a] PYRIMIDIN-4-ONE DERIVATIVES 审中-公开
标题翻译： 8-取代-6,7,8,9-四氢嘧啶并[1,2-a]吡啶并[4-a]衍生物
公开(公告)号：WO2004082577A3
公开(公告)日：2004-11-04
申请号：PCT/EP2004004014
申请日：2004-03-19
申请人： SANOFI AVENTIS , MITSUBISHI 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： A61K20060101 , A61K31/519 , A61P25/00 , C07D20060101 , C07D487/04
CPC分类号： A61K31/519 , C07D487/04
摘要： The invention relates to substituted-pyrimidone derivatives 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, a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the rings being optionally substituted; R2 represents a phenyl group or a naphthalene ring; the phenyl group and the naphthalene ring being optionally substituted; R3 represents a hydrogen atom or a C1-6 alkyl group; R4 represents a phenyl group, a pyridinyl group or a naphthalene ring, the groups and the ring being optionally substituted; R5 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; n represents 0 to 3; and p+q=0-3. 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.

7. 发明申请

WO2010089510A3 DERIVATIVES OF AZASPIRANYL-ALKYLCARBAMATES OF 5-MEMBER HETEROCYCLIC COMPOUNDS, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF 审中-公开
标题翻译：五元杂环化合物的五氢化偶氮烷 - 烷基氨基甲酸酯的衍生物及其制备和治疗用途
公开(公告)号：WO2010089510A3
公开(公告)日：2010-09-30
申请号：PCT/FR2010050183
申请日：2010-02-04
申请人： SANOFI AVENTIS , ABOUABDELLAH AHMED , CHEREZE NATHALIE , FAYOL AUDE , LOCHEAD ALISTAIR , SAADY MOURAD , VACHE JULIEN , YAICHE PHILIPPE
发明人： ABOUABDELLAH AHMED , CHEREZE NATHALIE , FAYOL AUDE , LOCHEAD ALISTAIR , SAADY MOURAD , VACHE JULIEN , YAICHE PHILIPPE
IPC分类号： C07D413/14 , A61K31/438 , A61P1/00 , A61P9/00 , A61P25/00 , A61P29/00 , A61P31/00 , A61P35/00 , A61P37/00 , C07D417/14
CPC分类号： C07D417/14 , C07D413/14
摘要： The invention relates to a compound of the general formula (I) in which R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, NR8R9 group; m, n, o and p are independently an integer equal to 0, 1, 2 or 3; A is a covalent bond or a C1-8-alkylene group; R1 is an optionally substituted aryl or heteroaryl group; R3 is a hydrogen or fluorine atom or a C1-6-alkyl group or a trifluoromethyl group; R4 is an optionally substituted 5-member heterocyclic compound; the compound being in the form of a base or acid addition salt. The invention also relates to the therapeutic use thereof.
摘要翻译：本发明涉及通式（I）的化合物，其中R2是氢或氟原子或羟基，氰基，三氟甲基，C1-6-烷基，C1-6-烷氧基，NR8R9基团; m，n，o和p独立地为等于0,1,2或3的整数; A是共价键或C 1-8 - 亚烷基; R1是任选取代的芳基或杂芳基; R3是氢或氟原子或C1-6-烷基或三氟甲基; R4是任选取代的5元杂环化合物; 该化合物为碱或酸加成盐的形式。本发明还涉及其治疗用途。

8. 发明申请

WO2009156864A3 SUBSTITUTED ALKYL PYRIMIDIN-4-ONE DERIVATIVES 审中-公开
标题翻译：取代的烷基吡啶-4-酮衍生物
公开(公告)号：WO2009156864A3
公开(公告)日：2010-04-01
申请号：PCT/IB2009006568
申请日：2009-06-25
申请人： MITSUBISHI TANABE PHARMA CORP , SANOFI AVANTIS , 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： C07D471/04 , A61K31/519 , A61P25/00
CPC分类号： C07D471/04 , A61K31/517 , A61K31/519 , C07D487/04
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof (I), wherein, X represents a methylene, NH, a nitrogen atom substituted by a C(O)-O- (C1-6-alkyl) 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 C1-6 alkyl group optionally substituted, R4 represents a hydrogen atom, a halogen atom, a hydroxyl group, a C1-6 alkyl group; m represents 1 to 2 when X is a methylene or m represents 2 when X is NH, a nitrogen atom substituted by a C(O)-O-(C1- 6-alkyl) group; in the form of a free base or of an addition salt with an acid. Use in therapeutic
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（I），其中X表示亚甲基，NH，被C（O）-O-（C1 -6-烷基）基团; 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; R 3表示任选取代的C 1-6烷基，R 4表示氢原子，卤素原子，羟基，C 1-6烷基; 当X为亚甲基时，m表示1〜2，X表示NH时，m表示2，C（O）-O-（C1-6 - 烷基）取代的氮原子。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

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。

10. 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

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