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    • 1. 发明申请
    • SUBSTITUTED BICYCLIC PYRIMIDONE DERIVATIVES
    • 取代的双环嘧啶酮衍生物
    • WO2007057790A2
    • 2007-05-24
    • PCT/IB2006004046
    • 2006-11-21
    • SANOFI AVENTISMITSUBISHI PHARMA CORPCHEREZE NATHALIELOCHEAD ALISTAIRSAADY MOURADSLOWINSKI FRANCKYAICHE PHILIPPE
    • CHEREZE NATHALIELOCHEAD ALISTAIRSAADY MOURADSLOWINSKI FRANCKYAICHE PHILIPPE
    • C07D239/00C07D471/04
    • 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.
    • 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 。
    • 2. 发明申请
    • ARYLAMIDE PYRIMIDONE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
    • 用于治疗神经损伤性疾病的亚胺酰吡咯烷酮衍生物
    • WO2008155669A3
    • 2009-06-04
    • PCT/IB2008002446
    • 2008-05-14
    • SANOFI AVENTISMITSUBISHI TANABE PHARMA CORPCHEREZE NATHALIEGALLET THIERRYLOCHEAD ALISTAIRSAADY MOURADVERONIQUE CORINNEYAICHE PHILIPPE
    • CHEREZE NATHALIEGALLET THIERRYLOCHEAD ALISTAIRSAADY MOURADVERONIQUE CORINNEYAICHE PHILIPPE
    • C07D239/36A61K31/513A61P25/00
    • C07D239/36
    • 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 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, 4 or 5-pyrimidine ring or a 4-pyridine ring, the ring being optionally substituted by a C1-6 alkyl group, a C1-6 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 C1-6 alkyl group, C3-7 cycloalkyl group, a C3-7 cycloalkyl-C1-6 alkyl group, a halogen atom, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a hydroxyl group, an heteroaryl group optionally substituted by a C1-6 alkyl group, C3-7 cycloalkyl group, a C3-7 cycloalkyl-C1-6 alkyl group, C1-6 alkoxy group optionally substituted by a C3-5 cycloalkyl group, a C1-2 perhalogenated alkoxy group, a C1-6 alkylsulfonyl group, a nitro, a cyano, an amino, a C1-6 monoalkylamino group or a C2-12 dialkylamino group, an acetoxy group or an aminosulfonyl group; R3 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R4 represents a hydrogen atom or a C1-6 alkyl group; R5 represents a hydrogen atom, a C1-6 alkyl group; R6 represents a hydrogen atom, a C1-6 alkyl group; R7 represents a hydrogen atom or a C1-6 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.
    • 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. 发明专利
    • BRPI0811527A2
    • 2014-11-18
    • BRPI0811527
    • 2008-05-14
    • SANOFI AVENTISMITSUBISHI TANABE PHARMA CORP
    • CHEREZE NATHALIEGALLET THIERRYLOCHEAD ALISTAIRSAADY MOURADVERONIQUE CORINNEYAICHE PHILIPPE
    • C07D239/36A61K31/513A61P25/00
    • 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.
    • 7. 发明专利
    • ΥΠΟΚΑΤΕΣΤΗΜΕΝΑ ΠΑΡΑΓΩΓΑ 8’-ΠΥΡΙ(ΜΙ)ΔΙΝΥΛΟ-ΔΙΫΔΡΟΣΠΕΙΡΟ-[ΚΥΚΛΟΑΛΚΥΛΑΜΙΝΟ]-ΠΥΡΙΜΙΔΟ[1,2-A]ΠΥΡΙΜΙΔΙΝ-6ΟΝΗΣ.
    • CY1107982T1
    • 2013-09-04
    • CY071100987
    • 2007-07-24
    • SANOFI AVENTIS
    • CHEREZE NATHALIELOCHEAD ALISTAIRSAADY MOURADSLOWINSKI FRANCKYAICHE PHILIPPE
    • C07D487/04A61K31/505A61P25/28
    • Ηεφεύρεσηαφοράσεέναπαράγωγοδιυδροσπειρο-[κυκλοαλκυλαμινο]-πυριμιδόνηςπουπαριστάνεταιμετοντύπο (I) ήέναάλαςαυτού, όπου: τοΧ παριστάνειδύοάτομαυδρογόνου, έναάτομοθείου, έναάτομοοξυγόνουή μια C1-2 αλκυλο-ομάδακαιέναάτομουδρογόνου, τοΥ παριστάνειένανδεσμό, μιακαρβονυλο-ομάδα, μιαμεθυλενο-ομάδαπροαιρετικάυποκατεστημένη, το R1 παριστάνειένανδακτύλιο 2-, 3- ή 4-πυριδίνηςή ένανδακτύλιο 2-, 4- ή 5-πυριμιδίνης, όπουο δακτύλιοςείναιπροαιρετικάυποκατεστημένος, το R2 παριστάνειένανδακτύλιοβενζολίουή ένανδακτύλιοναφθαλενίου, όπουοιδακτύλιοιείναιπροαιρετικάυποκατεστημένοι, το R3 παριστάνειέναάτομουδρογόνου, μια C1-6 αλκυλο-ομάδαή έναάτομοαλογόνου, το R4 παριστάνειέναάτομουδρογόνου, μια C1-4 αλκοξυκαρβονυλο-ομάδα, μια C3-6 κυκλοαλκυλοκαρβονυλο-ομάδα, μιαβενζοϋλο-ομάδα, μια C1-6 αλκυλο-ομάδα, όπουοιομάδεςείναιπροαιρετικάυποκατεστημενες, ταο και m παριστάνουν 1 έως 2, το n παριστάνει 0 έως 3, το p παριστάνει 0 έως 2, καιτο q παριστάνει 0 έως 2. Ηεφεύρεσηαφοράεπίσηςσεέναφάρμακοτοοποίοπεριέχειτοενλόγωπαράγωγοή έναάλαςαυτούωςδραστικόσυστατικότοοποίοχρησιμοποιείταιγιατηνπροληπτικήκαι/ήθεραπευτικήαντιμετώπισημιαςνευροεκφυλιστικήςνόσουη οποίαπροκαλείταιαπότηνμηφυσιολογικήδραστηριότητατης GSK3β, όπωςτηςνόσουτου Alzheimer.