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：EP2321313A1

公开(公告)日：2011-05-18

申请号：EP09769670.2

申请日：2009-06-25

申请人： Mitsubishi Tanabe Pharma Corporation ,  Sanofi-Aventis

发明人： LOCHEAD, Alistair ,  SAADY, Mourad ,  YAICHE, Philippe

IPC分类号： C07D471/04 ,  A61K31/519 ,  A61P31/10 ,  A61P17/14 ,  A61P25/00

CPC分类号： A01N43/54 ,  C07D471/04

摘要： A pyrimido isoquinoline derivative represented by formula (I) : wherein: R1 represents a 4-pyridine ring or a 4-pyrimidine ring; R2 represents a hydrogen atom: R3 represents a hydrogen atom; R4 represents: a hydrogen atom; a halogen atom; R7, RB, R9. R10 represent independently from each other a hydrogen atom, a halogen atom, a C
1-6 alkoxy group, a nitro, a hydroxyl or an amino; Formula (II) represents a single or a double bond, in form of a free base or of an addition salt with an acid. The compounds of formula (I) are useful for the treatment of neurodegenerative diseases caused by abnormal activity of GSK3ß.

摘要翻译： 由式（I）表示的嘧啶异喹啉衍生物：其中：R1表示4-吡啶环或4-嘧啶环; R2表示氢原子; R3表示氢原子; R4表示：氢原子; 卤素原子; R 7，R 8，R 9，R 10彼此独立地表示氢原子，卤素原子，C 1-6烷氧基，硝基，羟基或氨基; 表示单一或双键，其形式为游离碱或与酸形成的加成盐。 式（I）化合物是可用于治疗各种疾病如癌症，神经变性疾病或糖尿病的GSK3抑制剂。

公开(公告)号：EP2321295A2

公开(公告)日：2011-05-18

申请号：EP09769671.0

申请日：2009-06-25

申请人： Mitsubishi Tanabe Pharma Corporation ,  Sanofi-Aventis

发明人： LOCHEAD, Alistair ,  SAADY, Mourad ,  YAICHE, Philippe

IPC分类号： C07D401/04 ,  C07D487/04 ,  A61K31/53 ,  A61P25/28 ,  A61P3/10 ,  A61P35/00 ,  A61P33/06

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 C
1-6 alkyl group, a hydroxyl group, a C
1-6 alkoxy group; R1 represents a 4-pyridine ring; R2 represents a hydrogen atom, a C
1-6 alkyl; R3 represents a hydrogen atom, a C
1-6 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. Use in therapeutic.

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; R1表示4-吡啶环; R 2表示氢原子，C 1-6烷基; R 3表示氢原子，C 1-6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。 这些化合物可用作GSK3-²抑制剂。

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：EP2162443A2

公开(公告)日：2010-03-17

申请号：EP08807106.3

申请日：2008-05-14

申请人： Sanofi-Aventis ,  Mitsubishi Tanabe Pharma Corporation

发明人： CHEREZE, Nathalie ,  GALLET, Thierry ,  LOCHEAD, Alistair ,  SAADY, Mourad ,  VERONIQUE, Corinne ,  YAICHE, Philippe

IPC分类号： C07D239/38 ,  C07D471/04 ,  A61P35/00

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：化合物（I）适用于治疗神经变性疾病。

公开(公告)号：EP1957492A2

公开(公告)日：2008-08-20

申请号：EP06847275.2

申请日：2006-11-21

申请人： sanofi-aventis ,  Mitsubishi Tanabe Pharma Corporation

发明人： CHEREZE, Nathalie ,  LOCHEAD, Alistair ,  SAADY, Mourad ,  SLOWINSKI, Franck ,  YAICHE, Philippe

IPC分类号： C07D471/04 ,  A61K31/519

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 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; 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 C1-6 alkyl group or a halogen atom; R4 represents a hydrogen atom or a C-1-6 alkyl group; R5 represents a hydrogen atom, a C1-6 alkyl group optionally substituted; R6 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R7 represents a hydrogen atom or a C1-6 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 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，被氢原子或C 1-3烷基取代的氮原子，硫原子，任选取代的亚甲基; 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; R2代表苯环或萘环; 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表示氢原子或C 1-6烷基; R5表示氢原子，C 1-6烷氧基羰基或任选取代的C 1-6烷基; R6表示氢原子，C 1-6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至2.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异常活动引起的神经变性疾病，例如阿尔茨海默病 。

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：EP2321286A1

公开(公告)日：2011-05-18

申请号：EP09769668.6

申请日：2009-06-25

申请人： Mitsubishi Tanabe Pharma Corporation ,  Sanofi-Aventis

发明人： LOCHEAD, Alistair ,  SAADY, Mourad ,  YAICHE, Philippe

IPC分类号： C07D241/52 ,  C07D401/04 ,  A61K31/497 ,  A61P25/28

CPC分类号： A61K31/497 ,  C07D241/52 ,  C07D401/04

摘要： A N-oxide pyrazine derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: (I) wherein: R1 represents a 4-pyridine ring, a halogen atom; R2 represents a hydrogen atom; R3 represents a hydrogen atom; R4 represents: a phenylCi-3alkyl group, this group being optionally substituted; R5 represents a hydrogen atom; in the form of a free base or of an addition salt with an acid. Use in Therapy

摘要翻译： 由式（I）表示的N-氧化吡嗪衍生物或其盐，或其溶剂化物或其水合物：（I）其中：R 1表示4-吡啶环，卤素原子; R2代表氢原子; R3代表氢原子; R 4代表：苯基C 1-3烷基，该基团任选被取代; R5代表氢原子; 以游离碱或与酸加成盐的形式存在。 用于治疗

公开(公告)号：EP2321314A2

公开(公告)日：2011-05-18

申请号：EP09769672.8

申请日：2009-06-25

申请人： Mitsubishi Tanabe Pharma Corporation ,  Sanofi-Aventis

发明人： LOCHEAD, Alistair ,  SAADY, Mourad ,  YAICHE, Philippe

IPC分类号： C07D471/04 ,  A61K31/519 ,  A61P25/00

CPC分类号： C07D471/04 ,  A61K31/519 ,  Y02A50/411

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 C 1-6 alkyl group, a halogen atom, a C 1-2 halogenated alkyl group, a hydroxyl group, a C 1-6 alkoxy group, a C 1-2 halogenated alkoxy group, R5 represents a hydrogen atom, a C 1-6 alkyl group, a 4-pyridine group, a phenyl group, these groups being optionally substituted, R6 represents a hydrogen atom, a C 1-6 alkyl group, a benzyloxy group, a phenyl C 1-6 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 1-6烷氧基， C 1-2卤代烷氧基，R 5表示氢原子，C 1-6烷基，4-吡啶基，苯基，这些基团任选被取代，R 6表示氢原子，C 1-6烷基 基团，苄氧基，苯基C 1-6烷基，这些基团任选被取代，形式为游离碱或与酸形成的加成盐。 用于治疗。

公开(公告)号：EP2307416A2

公开(公告)日：2011-04-13

申请号：EP09769674.4

申请日：2009-06-25

申请人： Mitsubishi Tanabe Pharma Corporation ,  Sanofi-Aventis

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-ι-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