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1. 发明公开

EP1716141A1 BENZOPYRAN DERIVATIVES, METHOD OF PRODUCTION AND USE THEREOF 有权
标题翻译：苯并吡喃衍生物，方法和应用
公开(公告)号：EP1716141A1
公开(公告)日：2006-11-02
申请号：EP05707824.8
申请日：2005-01-21
申请人： Université de Liège , UNIVERSITE LIBRE DE BRUXELLES
发明人： SEBILLE, Sophie , PIROTTE, Bernard , BOVERIE, Stéphane , DE TULLIO, Pascal , LEBRUN, Philippe , ANTOINE, Marie-Hélène
IPC分类号： C07D405/12 , C07D409/12 , C07D311/58 , A61K31/352
CPC分类号： C07D311/68 , C07D405/12 , C07D409/12
摘要： The invention relates to novel benzopyran derivatives of formula (I), to their method of production, to composition comprising the derivatives and use thereof. Formula (I) wherein: R1, R2, R3 and R4 are independently hydrogen, halogen, C1-6-alkyl. C3-8-cycloalkyl, hydroxy, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, nitro, amino, cyano, cyanomethyl, perhalomethyl, C1-6-monoalkyl- or dialkylamino, sulfamoyl, C1-6-alkylthio, C1-6-alkylsulfonyl, C1-6-alkylsulfinyl, formyl, C1-6-alkylcarbonylamino, R8arylthio, R8arylsulfinyl, R8arylsulfonyl, C1-6-alkoxycarbonyl, C1-6-alkoxycarbonyl-C1-6-alkyl, carbamoyl, carbamoylmethyl, C1-6-monoalkyl- or dialkylaminocarbonyl, C1-6-monoalkyl- or dialkylaminothiocarbonyl, ureido, C1-6-monoalkyl- or dialkylaminocarbonylamino, thioureido, C1-6-monoalkyl- or dialkylaminothiocarbonylamino, C1-6-monoalkyl- or dialkylaminosulfonyl, carboxy, carboxy-C1-6-alkyl, acyl, R8aryl, R8aryl-C1-6-alkyl, R8aryloxy; R5 and R6 are each independently hydrogen, C1-6-alkyl or, R5 and R6 taken together with the carbon atom to which they are attached form a 3- to 6-membered carbocyclic ring; R7 is 2-, 3- or 4-pyridyl optionally mono- or polysubstituted by R1; R7 is 2- or 3-thienyl optionally mono- or polysubstituted substituted by R1 or R7 is phenyl optionally mono- or polysubstituted by R1 with the exception of or R7 representing C6H5 ; R8 is hydrogen, halogen, C1-6-alkyl, C3-8-cycloalkyl, hydroxy, C1-6-alkoxy, nitro, amino, cyano, cyanomethyl, perhalomethyl; or a salt thereof with a pharmaceutically acceptable acid or base, or any optical isomer or mixture of optical isomers, including a racemic mixture or any polymorphic and tautomeric form.

2. 发明申请

WO2005075463A1 BENZOPYRAN DERIVATIVES, METHOD OF PRODUCTION AND USE THEREOF 审中-公开
标题翻译：苯并吡喃衍生物，生产方法及其用途
公开(公告)号：WO2005075463A1
公开(公告)日：2005-08-18
申请号：PCT/EP2005/050275
申请日：2005-01-21
申请人： UNIVERSITE DE LIEGE , UNIVERSITE LIBRE DE BRUXELLES , SEBILLE, Sophie , PIROTTE, Bernard , BOVERIE, Stéphane , DE TULLIO, Pascal , LEBRUN, Philippe , ANTOINE, Marie-Hélène
发明人： SEBILLE, Sophie , PIROTTE, Bernard , BOVERIE, Stéphane , DE TULLIO, Pascal , LEBRUN, Philippe , ANTOINE, Marie-Hélène
IPC分类号： C07D405/12
CPC分类号： C07D311/68 , C07D405/12 , C07D409/12
摘要： The invention relates to novel benzopyran derivatives of formula (I), to their method of production, to composition comprising the derivatives and use thereof. Formula (I) wherein: R 1 , R 2 , R 3 and R 4 are independently hydrogen, halogen, C 1-6 -alkyl. C 3-8 -cycloalkyl, hydroxy, C 1-6 -alkoxy, C 1-6 -alkoxy-C 1-6 -alkyl, nitro, amino, cyano, cyanomethyl, perhalomethyl, C 1-6 -monoalkyl- or dialkylamino, sulfamoyl, C 1-6 -alkylthio, C 1-6 -alkylsulfonyl, C 1-6 -alkylsulfinyl, formyl, C 1-6 -alkylcarbonylamino, R 8 arylthio, R 8 arylsulfinyl, R 8 arylsulfonyl, C 1-6 -alkoxycarbonyl, C 1-6 -alkoxycarbonyl-C 1-6 -alkyl, carbamoyl, carbamoylmethyl, C 1-6 -monoalkyl- or dialkylaminocarbonyl, C 1-6 -monoalkyl- or dialkylaminothiocarbonyl, ureido, C 1-6 -monoalkyl- or dialkylaminocarbonylamino, thioureido, C 1-6 -monoalkyl- or dialkylaminothiocarbonylamino, C 1-6 -monoalkyl- or dialkylaminosulfonyl, carboxy, carboxy-C 1-6 -alkyl, acyl, R 8 aryl, R 8 aryl-C 1-6 -alkyl, R 8 aryloxy; R 5 and R 6 are each independently hydrogen, C 1-6 -alkyl or, R 5 and R 6 taken together with the carbon atom to which they are attached form a 3- to 6-membered carbocyclic ring; R 7 is 2-, 3- or 4-pyridyl optionally mono- or polysubstituted by R 1 ; R 7 is 2- or 3-thienyl optionally mono- or polysubstituted substituted by R 1 or R 7 is phenyl optionally mono- or polysubstituted by R 1 with the exception of or R 7 representing C 6 H 5 ; R 8 is hydrogen, halogen, C 1-6 -alkyl, C 3-8 -cycloalkyl, hydroxy, C 1-6 -alkoxy, nitro, amino, cyano, cyanomethyl, perhalomethyl; or a salt thereof with a pharmaceutically acceptable acid or base, or any optical isomer or mixture of optical isomers, including a racemic mixture or any polymorphic and tautomeric form.
摘要翻译：本发明涉及式（I）的新型苯并吡喃衍生物，其制备方法，包含衍生物和其用途的组合物。式（I）其中：R 1，R 2，R 3和R 4独立地为氢，卤素，C 1-6 - 烷基。 C 3-8 - 环烷基，羟基，C 1-6 - 烷氧基，C 1-6 - 烷氧基-C 1-6 - 烷基，硝基，氨基，氰基，氰基甲基，全卤甲基，C 1-6 - 单烷基 - 或二烷基氨基，氨磺酰基， - 烷硫基，C 1-6 - 烷基磺酰基，C 1-6 - 烷基亚磺酰基，甲酰基，C 1-6 - 烷基羰基氨基，R 8芳硫基，R 8芳基亚磺酰基，R 8芳基磺酰基，C 1-6 - 烷氧基羰基，C 1-6 - 烷氧基羰基-C 1-6 - 烷基，氨基甲酰基，氨基甲酰基甲基 C 1-6单烷基 - 或二烷基氨基羰基，C 1-6 - 单烷基 - 或二烷基氨基硫代羰基，脲基，C 1-6 - 单烷基 - 或二烷基氨基羰基氨基，硫脲基，C 1-6 - 单烷基 - 或二烷基氨基硫代羰基氨基，C 1-6 - 单烷基 - 或二烷基氨基磺酰基，羧基，羧基-C 1-6 - 烷基，酰基，R 8芳基，R 8芳基-C 1-6烷基，R 8芳氧基; R 5和R 6各自独立地为氢，C 1-6 - 烷基或者R 5和R 6与它们所连接的碳原子一起形成3-至6-元碳环; R7是任选被R1单取代或多取代的2-，3-或4-吡啶基; R 7是任选被R 1或R 7取代的单或多取代的2-或3-噻吩基，R 3是任选被R1单取代或多取代的苯基，或者R 7代表C 6 H 5; R 8为氢，卤素，C 1-6 - 烷基，C 3-8 - 环烷基，羟基，C 1-6 - 烷氧基，硝基，氨基，氰基，氰基甲基，全卤代甲基。或其盐与药学上可接受的酸或碱，或任何光学异构体或光学异构体的混合物，包括外消旋混合物或任何多晶型和互变异构形式。

3. 发明授权

EP1716141B1 BENZOPYRAN DERIVATIVES, METHOD OF PRODUCTION AND USE THEREOF 有权
标题翻译：苯并吡喃衍生物，方法和应用
公开(公告)号：EP1716141B1
公开(公告)日：2016-01-20
申请号：EP05707824.8
申请日：2005-01-21
申请人： Université de Liège , Université Libre de Bruxelles
发明人： SEBILLE, Sophie , PIROTTE, Bernard , BOVERIE, Stéphane , DE TULLIO, Pascal , LEBRUN, Philippe , ANTOINE, Marie-Hélène
IPC分类号： C07D405/12 , C07D409/12 , C07D311/58 , A61K31/352
CPC分类号： C07D311/68 , C07D405/12 , C07D409/12

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