公开(公告)号：EP2247598A1

公开(公告)日：2010-11-10

申请号：EP09706447.1

申请日：2009-01-27

申请人： Sanofi-Aventis ,  Mitsubishi Tanabe Pharma Corporation

发明人： FAYOL, Aude ,  LOCHEAD, Alistair ,  SAADY, Mourad ,  VACHE, Julien ,  YAICHE, Philippe

IPC分类号： C07D498/04 ,  C07D519/00 ,  A61K31/33 ,  A61P25/00

CPC分类号： C07D498/04 ,  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 Ci-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 or a C1-6 alkyl group; and n represents 0 to 3 and their therapeutic use.

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：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C 1-3烷基取代的氮原子，硫原子，任选被一个或两个选自C 1-6烷基的基团取代的亚甲基， 羟基，C 1-6烷氧基，C 1-2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; R 2表示氢原子，C 1-6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表示氢原子或C 1-6烷基; n表示0〜3，其治疗用途。

公开(公告)号：EP2321315A2

公开(公告)日：2011-05-18

申请号：EP09769675.1

申请日：2009-06-25

申请人： Mitsubishi Tanabe Pharma Corporation ,  Sanofi-Aventis

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 ,  Y02A50/411

摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein : X represents a methylene, NH, a nitrogen atom substituted by a C(O)-O-(C 1-6 -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 C 1-6 alkyl group, a C 1-6 alkoxy group or a halogen atom; R2 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; R3 represents a C 1-6 alkyl group optionally substituted, R4 represents a hydrogen atom, a halogen atom, a hydroxyl group, a C 1-6 alkyl group; m represents 1 to 2 when X is a methylene or m represents2 when X is NH, a nitrogen atom substituted by a C(O)-O-(C 1-6 -alkyl) group ; in the form of a free base or of an addition salt with an acid. Use in therapeutic

公开(公告)号：EP2238141A1

公开(公告)日：2010-10-13

申请号：EP09706634.4

申请日：2009-01-27

申请人： Sanofi-Aventis ,  Mitsubishi Tanabe Pharma Corporation

发明人： FAYOL, Aude ,  LOCHEAD, Alistair ,  SAADY, Mourad ,  VACHE, Julien ,  YAICHE, Philippe

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P25/00

CPC分类号： C07D487/04 ,  C07D243/08 ,  C07D403/12

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 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 benzene ring or a naphthalene ring; the rings being optionally substituted R4 represents a hydrogen atom, a C1-6 alkyl group, a C3-7 cycloalkyl group, a C3-7 cycloalkyl-C1-6 alkyl group, a COO (C1-6-alkyl) group, these group being optionally substituted; R5 represents a hydrogen atom or a C1-6 alkyl group and n represents 0 to 3 and their therapeutic use for the treatment of neurodegenerative diseases caused by abnormal activity of GSK3β.

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：Y代表两个氢原子，硫原子，氧原子或一个C 1-2烷基和氢原子 ; 其中Z表示键，以氧原子，被取代的氢原子或C 1-3烷基，硫原子的氮原子，亚甲基基团通过从C 1-6烷基选择一个或两个基团任选取代， 一个羟基，C 1-6烷氧基，C 1-2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，所述环任选被C 1-6烷基substituiertem，一个C 1-6烷氧基或卤素原子; R2 darstellt氢原子，C 1-6烷基或卤素原子; R3表示苯环或萘环; 所述环任选substituiertem R 4表示氢原子，C 1-4烷基，C 3-7环烷基，C 3-7环烷基-C 1-6烷基，COO一（C 1-6烷基 ）基团，本文基团任选被substituiertem; R5 darstellt氢原子或C 1-6烷基，n darstellt 0〜3，它们在由GSK3²的异常活性引起的神经变性疾病的治疗中的治疗用途。

公开(公告)号：EP2321316A1

公开(公告)日：2011-05-18

申请号：EP09769676.9

申请日：2009-06-25

申请人： Mitsubishi Tanabe Pharma Corporation ,  Sanofi-Aventis

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

摘要： A pyrimidone derivative represented by formula (I) or a salt thereof: wherein: Y represents two hydrogen atoms, a sulphur atom, an oxygen atom; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine 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 hydrogen atom, a C
1-6 alkyl group or a halogen atom; R3 represents a phenyl-group, a phenyl-CH
2 - group, a C
1-6 alkyl-O-C(O)- group, a phenyl-C(O)- group, a 5-10 membered heterocyclic group, a phenyl-CH
2 -O-C(O)- group, a -C(O)-5-10 membered heterocyclic group, these groups being optionnally 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
1-3 halogenated alkyl group, a hydroxyl group, a C
1-6 alkoxy 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, an aminosulfonyl group; R4 represents a hydrogen atom, a halogen atom, a hydroxyl group, a C
1-6 alkyl group; m represents 0 to 2, 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：Y表示两个氢原子，硫原子，氧原子，羟基和氢原子，羟基和 C 1-2烷基，羟基和C 1-2全卤代烷基; 卤素原子和氢原子或 - （CH 2）p - ; Z表示键，氧原子，NH，被氢原子或C 1-3烷基取代的氮原子，硫原子，亚甲基 基团任选取代; R1表示2,3或4-吡啶环或2,4或5-嘧啶环，该环任选被取代; R 2表示氢原子，C 1-6烷基或卤素原子; R3表示氢原子; 苯基或萘基，这些基团任选地被任选取代任选取代的-C（O）O（C 1-6 - 烷基）基团的4-15元杂环基团; -C（O） - 苯基，-C（O）O-苯基或-C（O）O-CH 2 - 苯基，上述基团的苯环任选被取代; 任选取代的-C（O）-4-15元杂环基; R4表示氢原子，卤素原子，羟基，任选取代的C 1-6烷基; n表示0〜3; m表示0〜3; p表示2〜7; 以游离碱的形式或与酸的加成盐形式。 用于治疗

公开(公告)号：EP2247599A1

公开(公告)日：2010-11-10

申请号：EP09706539.5

申请日：2009-01-27

申请人： Sanofi-Aventis ,  Mitsubishi Tanabe Pharma Corporation

发明人： FAYOL, Aude ,  LOCHEAD, Alistair ,  SAADY, Mourad ,  VACHE, Julien ,  YAICHE, Philippe

IPC分类号： C07D498/04 ,  A61K31/33 ,  A61P25/00

CPC分类号： C07D498/04

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 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 benzene ring or a naphthalene ring; the rings being optionally substituted R4 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）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C1-2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，任选被选自C1-6烷基，羟基 基团，C1-6烷氧基，C1-2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，所述环任选被C1-6烷基，C1-6烷氧基或卤素原子取代; R2代表氢原子，C1-6烷基或卤素原子; R3代表苯环或萘环; 该环任选被取代; R4表示氢原子或C1-6烷基; n代表0至3及其治疗用途。

公开(公告)号：EP2238140A2

公开(公告)日：2010-10-13

申请号：EP09705869.7

申请日：2009-01-27

申请人： Sanofi-Aventis ,  Mitsubishi Tanabe Pharma Corporation

发明人： FAYOL, Aude ,  LOCHEAD, Alistair ,  SAADY, Mourad ,  VACHE, Julien ,  YAICHE, Philippe

IPC分类号： 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 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, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine 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 hydrogen atom, a C
1-6 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 C
1-6 alkyl group optionally substituted by 1 to 4 substituents R5 represents a hydrogen atom or a C
1-6 alkyl group; and n represents 0 to 3 and their therapeutic use.

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：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C 1-3烷基取代的氮原子，硫原子，任选被一个或两个选自C 1-6烷基的基团取代的亚甲基， 羟基，C 1-6烷氧基，C 1-2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; R 2表示氢原子，C 1-6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。

公开(公告)号：EP2121635A2

公开(公告)日：2009-11-25

申请号：EP07870445.9

申请日：2007-12-20

申请人： Sanofi-Aventis ,  Mitsubishi Tanabe Pharma Corporation

发明人： FAYOL, Aude ,  GALLET, Thierry ,  LOCHEAD, Alistair ,  SAADY, Mourad ,  VERONIQUE, Corinne ,  YAICHE, Philippe

IPC分类号： C07D239/70

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 GSK3β, such as Alzheimer disease.

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：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，氮原子，硫原子，任选被一个或两个选自C 1-6烷基，羟基，C 1-6烷氧基，C 1-6烷氧基， C 1-2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; R2表示4-15元杂环基，R3表示氢原子，C1-6烷基或卤素原子; R4和R5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表示氢原子，C 1-6烷基; 环烷基或卤素原子; R 7表示氢原子或C 1-6烷基; n表示0〜3; m表示0〜1; o表示0〜2; 以游离碱的形式或与酸的加成盐形式。 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GSK3 2异常活动（例如阿尔茨海默病）引起的神经变性疾病。

公开(公告)号：EP2321315B1

公开(公告)日：2015-06-03

申请号：EP09769675.1

申请日：2009-06-25

申请人： Mitsubishi Tanabe Pharma Corporation ,  SANOFI

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 ,  Y02A50/411

摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein : X represents a methylene, NH, a nitrogen atom substituted by a C(O)-O-(C 1-6 -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 C 1-6 alkyl group, a C 1-6 alkoxy group or a halogen atom; R2 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; R3 represents a C 1-6 alkyl group optionally substituted, R4 represents a hydrogen atom, a halogen atom, a hydroxyl group, a C 1-6 alkyl group; m represents 1 to 2 when X is a methylene or m represents2 when X is NH, a nitrogen atom substituted by a C(O)-O-(C 1-6 -alkyl) group ; in the form of a free base or of an addition salt with an acid. Use in therapeutic

公开(公告)号：EP2321316B1

公开(公告)日：2014-03-12

申请号：EP09769676.9

申请日：2009-06-25

申请人： Mitsubishi Tanabe Pharma Corporation ,  SANOFI

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

公开(公告)号：EP2238140B1

公开(公告)日：2013-07-17

申请号：EP09705869.7

申请日：2009-01-27

申请人： SANOFI ,  Mitsubishi Tanabe Pharma Corporation

发明人： FAYOL, Aude ,  LOCHEAD, Alistair ,  SAADY, Mourad ,  VACHE, Julien ,  YAICHE, Philippe

IPC分类号： C07D487/04 ,  C07D519/00 ,  A61K31/519

CPC分类号： C07D487/04 ,  C07D519/00