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1. 发明申请

WO2008155666A2 HETEROARYLAMIDE PYRIMIDONE DERIVATIVES 审中-公开
标题翻译：异烟酰胺吡咯烷酮衍生物
公开(公告)号：WO2008155666A2
公开(公告)日：2008-12-24
申请号：PCT/IB2008/002429
申请日：2008-05-14
申请人： SANOFI-AVENTIS , MITSUBISHI TANABE PHARMA CORPORATION , CHEREZE, Nathalie , GALLET, Thierry , LOCHEAD, Alistair , SAADY, Mourad , VERONIQUE, Corinne , YAICHE, Philippe
发明人： CHEREZE, Nathalie , GALLET, Thierry , LOCHEAD, Alistair , SAADY, Mourad , VERONIQUE, Corinne , YAICHE, Philippe
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: wherein: X 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, 4 or 5-pyrimidine ring or a 4- pyridine 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 4-15 membered heterocyclic group, this group being optionally 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 1-6 halogenated alkyl group, a hydroxyl group, a C 1-6 alkoxy group, a C 1-2 perhalogenated alkoxy group, a C 1-6 halogenated alkoxy group, a nitro, a cyano, an amino, a C 1-6 monoalkylamino group, a C 2-12 dialkylamino group, a S-(C 1-6 - alkyl) group, an heterocyclic group, an aryl group, an heteroaryl group, a O-aryl group or a S-aryl group, the above-mentioned groups being optionally substituted by 1 to 4 substituents selected from a C 1-6 alkyl group, a halogen atom, a C 1-6 alcoxy group, a C(O)O (C 1-6 -alkyl) or a C(O)O (aryl) group, the aryl optionally substituted by 1 to 4 substituents selected from a C 1-6 alkyl group, a halogen atom, a C 1-6 alcoxy group; 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; R6 represents a hydrogen atom, a C 1-6 alkyl group; R7 represents a hydrogen atom or a C 1-6 alkyl group; and n represents 0 to 3 and m represents 0 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：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; 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，C 1-6烷氧基，C1-2全卤代烷基或氨基; R1表示2,4或5-嘧啶环或4-吡啶环，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4-15元杂环基，该基团任选被1至4个选自C 1-6烷基，卤素原子，C 1-2烷基卤代烷基，C 1-6卤代烷基，C 1-6卤代烷基，羟基，C1-6烷氧基，C1-2全卤代烷氧基，C1-6卤代烷氧基，硝基，氰基，氨基，C1-6一烷基氨基，C2-12二烷基氨基， S-（C 1-6 - 烷基）基，杂环基，芳基，杂芳基，O-芳基或S-芳基，上述基团任选被1至4个选自 C 1-6烷基，卤素原子，C 1-6烷氧基，C（O）O（C 1-6 - 烷基）或C（O）O（芳基）），任选地被1〜选自C 1-6烷基，卤素原子，C 1-6烷氧基的4个取代基; R3表示氢原子，C1-6烷基或卤素原子; R4表示氢原子或C1-6烷基; R5表示氢原子，C1-6烷基; R6表示氢原子，C1-6烷基; R7表示氢原子或C1-6烷基; n表示0〜3，m表示0以游离碱或与酸形成的加成盐。

2. 发明申请

WO2010055267A1 DERIVES DE CARBAMATES D'ALKYL-HETEROCYCLES, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE 审中-公开
标题翻译：烷基化合物的氨基甲酸酯衍生物，其制备方法及其治疗用途
公开(公告)号：WO2010055267A1
公开(公告)日：2010-05-20
申请号：PCT/FR2009/052179
申请日：2009-11-13
申请人： SANOFI-AVENTIS , ABOUABDELLAH, Ahmed , CHEREZE, Nathalie , FAYOL, Aude , SAADY, Mourad , VACHE, Julien , VERONIQUE, Corinne , YAICHE, Philippe
发明人： ABOUABDELLAH, Ahmed , CHEREZE, Nathalie , FAYOL, Aude , SAADY, Mourad , VACHE, Julien , VERONIQUE, Corinne , YAICHE, Philippe
IPC分类号： C07D401/14 , C07D403/14 , C07D407/14 , C07D413/12 , C07D413/14 , C07D417/14 , A61P25/00 , A61K31/445 , A61K31/497 , A61K31/506 , A61K31/501 , A61K31/498 , A61K31/4709 , A61K31/502 , A61P29/00
CPC分类号： C07D417/14 , C07D401/14 , C07D403/14 , C07D407/14 , C07D413/12 , C07D413/14
摘要： Composé répondant à la formule (I) dans laquelle R 2 représente un atome d'hydrogène, de fluor ou un groupe hydroxyle, cyano, trifluorométhyle, C 1-6 -alkyle, C 1-6 - alcoxy, NR 8 R 9 ; n représente un nombre entier égal à 1, 2 ou 3 et m représente un nombre entier égal à 1 ou 2; A représente une liaison covalente ou un groupe C 1-8 -alkylène; R 1 représente un groupe phényle, pyridinyle, pyridazinyle, pyrimidinyle, pyrazinyle, triazinyle, naphtalènyle, quinolinyle, isoquinolinyle, phtalazinyle, quinazolinyle, quinoxalinyle, cinnolinyle, naphthyridinyle, ce groupe étant éventuellement substitué; R3 représente un atome d'hydrogène, de fluor, un groupe C 1-6 -alkyle ou un groupe trif luorométhyle; R 4 représente un groupe choisi parmi un furanyle, pyrrolyle, thiènyle, isothiazolyle, oxazolyle, isoxazolyle, pyrazolyle, oxadiazolyle, thiadiazolyle, imidazole, triazolyle, tétrazolyle, oxazolone, oxazolidinone, isoxazolone, isoxazolidinone, isothiazolone, isothiazolidinone, imidazolone, imidazolidinone, pyrazolone, pyrazolidinone, oxadiazolone, thiadiazolone, triazolone, ce groupe étant éventuellement substitué; à l'état de base ou de sel d'addition à un acide. Application en thérapeutique.
摘要翻译：对应于通式（I）的化合物：其中R 2是氢或氟原子或羟基，氰基，三氟甲基，C 1-6 - 烷基，C 1-6 - 烷氧基或NR 8 R 9基团; n是等于1,2或3的整数，m是等于1或2的整数; A是共价键或C 1-8亚烷基; R 1是苯基，吡啶基，哒嗪基，嘧啶基，吡嗪基，三嗪基，萘基，喹啉基，异喹啉基，酞嗪基，喹唑啉基，喹喔啉基，噌啉基或萘啶基， R3是氢或氟原子，C1-6烷基或三氟甲基; R4是选自呋喃基，吡咯基，噻吩基，异噻唑基，恶唑基，异恶唑基，吡唑基，恶二唑基，噻二唑基，咪唑，三唑基，四唑基，恶唑酮，恶唑烷酮，异恶唑酮，异恶唑烷酮，异噻唑酮，异噻唑烷酮，咪唑啉酮，咪唑烷酮，吡唑啉酮，吡唑烷酮，恶二唑酮，噻二唑酮和三唑酮，该基团任选被取代; 以碱的形式或与酸的加成盐形式。治疗用途。

3. 发明申请

WO2010089510A2 DÉRIVÉS D'AZASPIRANYL-ALKYLCARBAMATES D'HÉTÉROCYCLES À 5 CHAÎNONS, LEUR PRÉPARATION ET LEUR APPLICATION EN THÉRAPEUTIQUE 审中-公开
标题翻译： 5-甲基杂环化合物的AZASPIRANYL-ALKYLCARBAMATES的衍生物，其制备方法及其治疗用途
公开(公告)号：WO2010089510A2
公开(公告)日：2010-08-12
申请号：PCT/FR2010/050183
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 , C07D417/14 , A61K31/438 , A61P37/00 , A61P29/00 , A61P1/00 , A61P25/00 , A61P9/00 , A61P35/00 , A61P31/00 , C07D277/24 , C07D261/12 , C07D221/20 , C07D215/38 , C07D213/74 , C07D209/54 , C07D205/12 , A61K31/4709 , A61K31/444 , A61P31/12
CPC分类号： C07D417/14 , C07D413/14
摘要： Composé répondant à la formule générale (I) : dans laquelle R 2 représente un atome d'hydrogène, de fluor ou un groupe hydroxyle, cyano, trif luorométhyle, C 1-6 -alkyle, C 1-6 - alcoxy, NR 8 R 9 ; m, n, o et p représentent, indépendamment l'un de l'autre, un nombre entier égal à 0, 1, 2 ou 3;A représente une liaison covalente ou un groupe C 1-8 -alkylène; R 1 représente un groupe de type aryle ou hétéroaryle éventuellement substitué; R 3 représente un atome d'hydrogène, de fluor, un groupe C 1-6 -alkyle ou un groupe trif luorométhyle; R 4 représente un hétérocycle à cinq chaînons éventuellement substitué; à l'état de base ou de sel d'addition à un acide. Application en thérapeutique.
摘要翻译：本发明涉及其中R 2为氢或氟原子或羟基，氰基，三氟甲基，C 1-6 - 烷基，C 1-6 - 烷氧基，NR 8 R 9基团的通式（I）的化合物; 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。

4. 发明申请

WO2010130945A1 DÉRIVÉS DE 7-AZA-SPIRO[3.5]NONANE-7-CARBOXYLATES, LEUR PRÉPRARATION ET LEUR APPLICATION EN THÉRAPEUTIQUE 审中-公开
标题翻译： 7-AZA-SPIRO [3.5] NONANE-7-羧酸酯衍生物，其制备方法及其治疗方法
公开(公告)号：WO2010130945A1
公开(公告)日：2010-11-18
申请号：PCT/FR2010/050914
申请日：2010-05-11
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： C07D401/12 , C07D413/12 , C07D417/12 , A61K31/4523 , A61P29/00 , A61P25/00
CPC分类号： C07D263/32 , C07D209/54 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12
摘要： Composés répondent à la formule générale (I) dans laquelle R 2 représente un atome d'hydrogène, de fluor ou un groupe hydroxyle, cyano, trifluorométhyle, Ci-6-alkyle, C 1-6 - alcoxy, NR 8 R 9 ; m, n, o et p représentent indépendamment l'un de l'autre un nombre allant de 0 à 3; étant entendu que m+n ≤ 7 et que o+p ≤ 7; A représente une liaison covalente, un atome d'oxygène, un groupe C 1-6 -alkylène ou un groupe -O-C 1-6 - alkylène dans lequel l'extrémité représentée par un atome d'oxygène est liée au groupe R 1 et l'extrémité représentée par un groupe alkylène est liée au carbone du bicycle; R 1 représente un groupe aryle ou hétéroaryle éventuellement substitué; R 3 représente un atome d'hydrogène, de fluor, un groupe C 1-6 -alkyle ou un groupe trifluorométhyle; R 4 représente un hétérocycle à cinq chaînons éventuellement substitué; à l'état de base ou de sel d'addition à un acide. Application en thérapeutique.
摘要翻译：本发明涉及通式（I）的化合物，其中：R 2是氢或氟原子或羟基，氰基，三氟甲基，C 1-6 - 烷基，C 1-6 - 烷氧基或NR 8 R 9基团; m，n，o和p独立地为0至3的数，条件是m + n = 7，o + p = 7; A是共价键，氧原子，C 1-6 - 亚烷基或-O-C 1-6 - 亚烷基，其中作为氧原子的末端键合到R 1基团，末端是亚烷基基团与双环化合物的碳键合; 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; 其中所述化合物可以是碱或酸加成盐的状态。本发明可用于治疗。

5. 发明申请

WO2008155669A2 ARYLAMIDE PYRIMIDONE DERIVATIVES 审中-公开
标题翻译：亚胺酰吡咯烷酮衍生物
公开(公告)号：WO2008155669A2
公开(公告)日：2008-12-24
申请号：PCT/IB2008/002446
申请日：2008-05-14
申请人： SANOFI-AVENTIS , MITSUBISHI TANABE PHARMA CORPORATION , CHEREZE, Nathalie , GALLET, Thierry , LOCHEAD, Alistair , SAADY, Mourad , VERONIQUE, Corinne , YAICHE, Philippe
发明人： CHEREZE, Nathalie , GALLET, Thierry , LOCHEAD, Alistair , SAADY, Mourad , VERONIQUE, Corinne , YAICHE, Philippe
CPC分类号： C07D239/36
摘要： A pyrimidone derivative represented by Formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: X 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, 4 or 5-pyrimidine ring or a 4-pyridine 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 benzene ring, a naphthalene ring or a benzyl group; the rings being optionally substituted by 1 to 4 substituents selected from a C 1-6 alkyl group, C 3-7 cycloalkyl group, a C 3-7 cycloalkyl-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, an heteroaryl group optionally substituted by a C 1-6 alkyl group, C 3-7 cycloalkyl group, a C 3-7 cycloalkyl-C 1-6 alkyl group, C 1-6 alkoxy group optionally substituted by a C 3-5 cycloalkyl 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 or an aminosulfonyl group; 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; R6 represents a hydrogen atom, a C 1-6 alkyl group; R7 represents a hydrogen atom or a C 1-6 alkyl group; n represents 0 to 3 and m represents 0 in the form of a free base or of an addition salt with an acid.
摘要翻译：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：X表示2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2,4或5-嘧啶环或4-吡啶环，该环任选被C 1-6烷基，C 1-6烷氧基或卤素原子取代; R2表示苯环，萘环或苄基; 该环任选被1至4个选自C 1-6烷基，C 3-7环烷基，C 3-7环烷基-C 1-6烷基，卤素原子，C 1-2全卤代烷基， C 1-3卤代烷基，羟基，任选被C 1-6烷基取代的杂芳基，C 3-7环烷基，C 3-7环烷基-C 1-6烷基，任选被 C3-5环烷基，C1-2全卤代烷氧基，C1-6烷基磺酰基，硝基，氰基，氨基，C1-6单烷基氨基或C2-12二烷基氨基，乙酰氧基或氨基磺酰基; R3表示氢原子，C1-6烷基或卤素原子; R4表示氢原子或C1-6烷基; R5表示氢原子，C1-6烷基; R6表示氢原子，C1-6烷基; R7表示氢原子或C1-6烷基; n表示0〜3，m表示0以游离碱或与酸形成的加成盐形式。

6. 发明申请

WO2007057790A3 SUBSTITUTED BICYCLIC PYRIMIDONE DERIVATIVES 审中-公开
公开(公告)号：WO2007057790A3
公开(公告)日：2007-05-24
申请号：PCT/IB2006/004046
申请日：2006-11-21
申请人： SANOFI-AVENTIS , MITSUBISHI PHARMA CORPORATION , CHEREZE, Nathalie , LOCHEAD, Alistair , SAADY, Mourad , SLOWINSKI, Franck , YAICHE, Philippe
发明人： CHEREZE, Nathalie , LOCHEAD, Alistair , SAADY, Mourad , SLOWINSKI, Franck , YAICHE, Philippe
IPC分类号： C07D471/04 , A61K31/519
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 GSK3β, such as Alzheimer disease.

7. 发明申请

WO2005058908A1 SUBSTITUTED 8’-PYRI(MI)DINYL-DIHYDROSPIRO-[CYCLOALKYLAMINE]-PYRIMIDO[1,2-a]PYRIMIDIN-6-ONE DERIVATIVES 审中-公开
标题翻译：取代的8'-哌嗪（MI）十二烷基二 - [环己基] - 吡咯并[1,2-a]吡啶-6-酮衍生物
公开(公告)号：WO2005058908A1
公开(公告)日：2005-06-30
申请号：PCT/EP2004/014846
申请日：2004-12-17
申请人： SANOFI-AVENTIS , MITSUBISHI PHARMA CORPORATION , CHEREZE, Nathalie , LOCHEAD, Alistair , SAADY, Mourad , SLOWINSKI, Franck , YAICHE, Philippe
发明人： CHEREZE, Nathalie , LOCHEAD, Alistair , SAADY, Mourad , SLOWINSKI, Franck , YAICHE, Philippe
IPC分类号： C07D487/04
CPC分类号： A61K31/527 , A61K31/397 , C07D487/04 , Y02P20/142
摘要： The invention relates to a dihydrospiro-[cycloalkylamine]-pyrimidone derivative represented by formula (I) or a salt thereof: (I) 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, 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, a C 1-4 alkoxy carbonyl group, a C 3-6 cycloalkyl carbonyl group, a benzoyl group, a C 1-6 alkyl group, the groups being optionally substituted; o and m represent 1 to 2; n represents 0 to 3; p represents 0 to 2; and q 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：本发明涉及由式（I）表示的二氢螺环 - [环烷基胺] - 嘧啶酮衍生物或其盐：（I）其中：X表示两个氢原子，硫原子，氧原子或C 1-2烷基，氢原子; Y表示键，羰基，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，C1-4烷氧基羰基，C3-6环烷基羰基，苯甲酰基，C1-6烷基，该基团任选被取代; o和m表示1〜2; n表示0〜3; p表示0〜2; 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，所述活性成分用于预防和/或治疗由GSK3β如异常活动引起的神经变性疾病，例如阿尔茨海默氏症疾病。

8. 发明公开

EP2356108A1 DERIVES DE CARBAMATES D'ALKYL-HETEROCYCLES, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE 有权
标题翻译：氨基甲酸酯alkylheterocycles，其制备方法及其食疗的
公开(公告)号：EP2356108A1
公开(公告)日：2011-08-17
申请号：EP09768186.0
申请日：2009-11-13
申请人： SANOFI
发明人： ABOUABDELLAH, Ahmed , CHEREZE, Nathalie , FAYOL, Aude , SAADY, Mourad , VACHE, Julien , VERONIQUE, Corinne , YAICHE, Philippe
IPC分类号： C07D401/14 , C07D403/14 , C07D407/14 , C07D413/12 , C07D413/14 , C07D417/14 , A61P25/00 , A61K31/445 , A61K31/497 , A61K31/506 , A61K31/501 , A61K31/498 , A61K31/4709 , A61K31/502 , A61P29/00
CPC分类号： C07D417/14 , C07D401/14 , C07D403/14 , C07D407/14 , C07D413/12 , C07D413/14
摘要： Compound corresponding to general formula (I): in which R
2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C
1-6 -alkyl, C
1-6 - alkoxy or NR
8 R
9 group; n is an integer equal to 1, 2 or 3 and m is an integer equal to 1 or 2; A is a covalent bond or a C
1-8 -alkylene group; R
1 is a phenyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, triazinyl, naphthyl, quinolinyl, isoquinolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, cinnolinyl or naphthyridinyl group, this group being optionally substituted; R
3 is a hydrogen or fluorine atom, a C
1-6 -alkyl group or a trifluoromethyl group; R
4 is a group selected from furanyl, pyrrolyl, thienyl, isothiazolyl, oxazolyl, isoxazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, imidazole, triazolyl, tetrazolyl, oxazolone, oxazolidinone, isoxazolone, isoxazolidinone, isothiazolone, isothiazolidinone, imidazolone, imidazolidinone, pyrazolone, pyrazolidinone, oxadiazolone, thiadiazolone and triazolone, this group being optionally substituted; in the form of a base or of an addition salt with an acid. Therapeutic use.

9. 发明授权

EP1699795B1 SUBSTITUTED 8'-PYRI(MI)DINYL-DIHYDROSPIRO-[CYCLOALKLYMINE]-PYRIMIDO[1,2A]PYRIMIDIN-6-ONE DERIVATIVES 有权
标题翻译： SUBSTITUIERTE 8'-哌嗪（MI）十二烷基 - [环己基] - 吡咯并[1,2A]嘧啶-6-胺
公开(公告)号：EP1699795B1
公开(公告)日：2007-04-25
申请号：EP04804431.7
申请日：2004-12-17
申请人： Sanofi-Aventis , Mitsubishi Pharma Corporation
发明人： CHEREZE, Nathalie , LOCHEAD, Alistair , SAADY, Mourad , SLOWINSKI, Franck , YAICHE, Philippe
IPC分类号： C07D487/04 , A61K31/505 , A61P25/28
CPC分类号： A61K31/527 , A61K31/397 , C07D487/04 , Y02P20/142
摘要： The invention relates to a dihydrospiro-[cycloalkylamine]-pyrimidone derivative represented by formula (I) or a salt thereof: (I) 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 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 C1-4 alkoxy carbonyl group, a C3-6 cycloalkyl carbonyl group, a benzoyl group, a C1-6 alkyl group, the groups being optionally substituted; o and m represent 1 to 2; n represents 0 to 3; p represents 0 to 2; and q 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：本发明涉及由式（I）表示的二氢螺环Ä环烷基胺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，羰基，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; R3表示氢原子，C1-6烷基或卤素原子; R4表示氢原子，C1-4烷氧基羰基，任选取代的C 1-6烷基; o和m表示1〜2; n表示0〜3; p表示0〜2; 并且q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的异常活性引起的神经变性疾病 beta，如阿尔茨海默病。

10. 发明授权

EP2430012B1 DÉRIVÉS DE 7-AZA-SPIRO[3.5]NONANE-7-CARBOXYLATES, LEUR PRÉPRARATION ET LEUR APPLICATION EN THÉRAPEUTIQUE 无效转让
标题翻译： 7-氮杂 - 螺[3.5]壬烷-7-羧酸酯衍生物，其制备方法及其治疗用途
公开(公告)号：EP2430012B1
公开(公告)日：2014-11-05
申请号：EP10728742.7
申请日：2010-05-11
申请人： SANOFI
发明人： ABOUABDELLAH, Ahmed , CHEREZE, Nathalie , FAYOL, Aude , LOCHEAD, Alistair , SAADY, Mourad , VACHE, Julien , YAICHE, Philippe
IPC分类号： C07D401/12 , C07D413/12 , C07D417/12 , A61K31/4523 , A61P29/00 , A61P25/00
CPC分类号： C07D263/32 , C07D209/54 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12

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