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1. 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。

2. 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

3. 发明申请

WO2008078196A2 SUBSTITUTED HETEROARYL PYRIDOPYRIMIDONE DERIVATIVES 审中-公开
标题翻译：取代的杂芳基吡啶并嘧啶酮衍生物
公开(公告)号：WO2008078196A2
公开(公告)日：2008-07-03
申请号：PCT/IB2007004409
申请日：2007-12-20
申请人： SANOFI AVENTIS , MITSUBISHI TANABE PHARMA CORP , FAYOL AUDE , GALLET THIERRY , LOCHEAD ALISTAIR , SAADY MOURAD , VERONIQUE CORINNE , YAICHE PHILIPPE
发明人： FAYOL AUDE , GALLET THIERRY , LOCHEAD ALISTAIR , SAADY MOURAD , VERONIQUE CORINNE , YAICHE PHILIPPE
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 GSK3ß, such as Alzheimer disease.
摘要翻译：式（I）代表的嘧啶酮衍生物或其盐，或其溶剂合物或其水合物：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代表键，氧原子，氮原子，硫原子，任选被选自C 1-6烷基基团，羟基，C 1-6烷氧基的组中选择一个或两个基团取代的亚甲基，C 1-2氟烷全卤代烷基或氨基; R1代表2,3或4-吡啶环或2,4或5-嘧啶环; R2代表任选取代的4-15元杂环基; R 3代表氢原子，C 1-6烷基或卤素原子; R 4和R 5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代表氢原子，C1-6烷基; 环烷基或卤素原子; 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; 以游离碱或与酸加成盐的形式存在。本发明还涉及包含其所述衍生物或其盐作为用于引起GSK3ß的异常活性，如阿尔茨海默病的神经变性疾病的预防性和/或治疗性治疗的有效成分的药物。

4. 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。

5. 发明专利

BRPI0914301A2 derivados de pirimidin-4-ona substituída 未知
公开(公告)号：BRPI0914301A2
公开(公告)日：2015-10-13
申请号：BRPI0914301
申请日：2009-06-25
申请人： MITSUBISHI TANABE PHARMA CORP , SANOFI AVENTIS
发明人： LOCHEAD ALISTAIR , FAYOL AUDE , VACHE JULIEN , SAADY MOURAD , YAICHE PHILIPPE
IPC分类号： C07D471/04 , A61K31/519 , A61P25/00

6. 发明专利

ZA201009272B SUBSTITUTED ALKYL PYRIMIDIN-4-ONE DERIVATIVES 未知
公开(公告)号：ZA201009272B
公开(公告)日：2012-03-28
申请号：ZA201009272
申请日：2010-12-23
申请人： MITSUBISHI TANABE PHARMA CORP , SANOFI-AVENTIS
发明人： FAYOL AUDE , LOCHEAD ALISTAIR , SAADY MOURAD , VACHE JULIEN , YAICHE PHILIPPE
IPC分类号： C07D20060101 , A61K20060101 , A61P20060101
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

7. 发明专利

NZ587068A SUBSTITUTED HETEROARYLAMIDE DIAZEPINOPYRIMIDONE DERIVATIVES 未知
公开(公告)号：NZ587068A
公开(公告)日：2011-12-22
申请号：NZ58706809
申请日：2009-01-27
申请人： SANOFI AVENTIS , MITSUBISHI TANABE PHARMA CORP
发明人： FAYOL AUDE , LOCHEAD ALISTAIR , SAADY MOURAD , VACHE JULIEN , YAICHE PHILIPPE
IPC分类号： A61K31/519 , C07D403/04 , C07D487/04
摘要： Disclosed are triaza-benzocycloheptene derivatives represented by general formula (I). Processes for preparing the compounds are also disclosed. Also disclosed is the use of the compounds of formula (I) for treating Alzheimer's disease, Parkinson's disease, tauopathies, vascular dementia; acute stroke, traumatic injuries; cerebrovascular accidents, brain cord trauma, spinal cord trauma; peripheral neuropathies, retinopathies, glaucoma, non-insulin dependent diabetes; obesity; manic depressive illness; schizophrenia; alopecia; cancers; parenchymal renal diseases, muscle atrophy or diseases caused by abnormal GSK3-beta activity.

8. 发明专利

AR072962A1 DERIVADOS DE PIRIMIDIN-4-ONA SUSTITUIDOS 未知
公开(公告)号：AR072962A1
公开(公告)日：2010-10-06
申请号：ARP090102311
申请日：2009-06-24
申请人： MITSUBISHI TANABE PHARMA CORP , SANOFI AVENTIS
发明人： LOCHEAD ALISTAIR , SAADY MOURAD , YAICHE PHILIPPE , VACHE JULIEN , FAYOL AUDE
IPC分类号： C07D471/04 , A61K31/519 , A61P25/00
摘要： Composiciones farmacéuticas y usos en el tratamiento de enfermedades neurodegenerativas. Reivindicacion 1: Un derivado de pirimidona representado por la formula (1) o una sal del mismo, en al que: Y representa dos átomos de hidrogeno, un átomo de azufre o un átomo de oxígeno; R1 representa un anillo de 2, 3 o 4-piridina o un anillo de 2, 4 o 5-pirimidina, estando el anillo opcionalmente sustituido con un grupo alquilo C1-6, un grupo alcoxi C1-6 o un átomo de halogeno; R2 representa un átomo de hidrogeno, un grupo alquilo C1-6 o un átomo de halogeno; R3 representa un grupo fenil-, un grupo fenil-CH2-, un grupo alquil C1-6-O-C(O)-, un grupo fenil-C(O)-, un grupo heterocíclico de 5-10 miembros, un grupo fenil-CH2-O-C(O)- o un grupo -C(O)-heterocíclico de 5-10 miembros, estando estos grupos opcionalmente sustituidos con 1 a 4 sustituyentes seleccionados entre un grupo alquilo C1-6, un átomo de halogeno, un grupo alquilo C1-2 perhalogenado, un grupo alquilo C1-3 halogenado, un gripo hidroxilo, un grupo alcoxi C1-6, un grupo alcoxi C1-2 perhalogenado, un grupo alquil C1-6-sulfonilo, un nitro, un ciano, un amino, un grupo monoalquil C1-6-amino o un grupo dialquil C2-12-amino, u grupo acetoxi o un grupo aminosulfonilo; R4 representa un átomo de hidrogeno, un átomo de halogeno, un grupo hidroxilo o un grupo alquilo C1-6; m representa de 0 a 2; en forma de una base libre o una sal de adicion con un ácido. Reivindicacion 6: Un inhibidor de GSK3beta seleccionado entre el grupo de un derivado de pirimidona representado por la formula (1) o sales del mismo, o un solvato del mismo o un hidrato del mismo de acuerdo con la reivindicacion 1.

9. 发明专利

CA2713248A1 SUBSTITUTED HETEROARYLAMIDE OXAZEPINOPYRIMIDONE DERIVATIVES 未知
公开(公告)号：CA2713248A1
公开(公告)日：2009-08-06
申请号：CA2713248
申请日：2009-01-27
申请人： SANOFI AVENTIS , MITSUBISHI TANABE PHARMA CORP
发明人： FAYOL AUDE , LOCHEAD ALISTAIR , SAADY MOURAD , VACHE JULIEN , YAICHE PHILIPPE
IPC分类号： C07D498/04 , A61K31/33 , A61P25/00 , 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.

10. 发明专利

AU2009208727A1 Substituted arylamide oxazepinopyrimidone derivatives 未知
公开(公告)号：AU2009208727A1
公开(公告)日：2009-08-06
申请号：AU2009208727
申请日：2009-01-27
申请人： MITSUBISHI TANABE PHARMA CORP , SANOFI AVENTIS
发明人： SAADY MOURAD , VACHE JULIEN , LOCHEAD ALISTAIR , FAYOL AUDE , YAICHE PHILIPPE
IPC分类号： C07D498/04 , A61K31/33 , A61P25/00
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 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 benzene ring or a naphthalene ring; the rings being optionally substituted R4 represents a hydrogen atom or a C 1-6 alkyl group; and n represents 0 to 3 and their therapeutic use.

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