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    • 7. 发明申请
    • BENZOPYRAN DERIVATIVES, METHOD OF PRODUCTION AND USE THEREOF
    • 苯并吡喃衍生物,生产方法及其用途
    • WO2005075463A1
    • 2005-08-18
    • PCT/EP2005/050275
    • 2005-01-21
    • UNIVERSITE DE LIEGEUNIVERSITE LIBRE DE BRUXELLESSEBILLE, SophiePIROTTE, BernardBOVERIE, StéphaneDE TULLIO, PascalLEBRUN, PhilippeANTOINE, Marie-Hélène
    • SEBILLE, SophiePIROTTE, BernardBOVERIE, StéphaneDE TULLIO, PascalLEBRUN, PhilippeANTOINE, Marie-Hélène
    • C07D405/12
    • C07D311/68C07D405/12C07D409/12
    • 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.
    • 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。
    • 8. 发明申请
    • PYRIDINIC SULFONAMIDE DERIVATIVES, METHOD OF PRODUCTION AND USE THEREOF
    • 吡啶磺酰胺衍生物,其生产方法和用途
    • WO2003029217A2
    • 2003-04-10
    • PCT/EP2002/010532
    • 2002-09-19
    • UNIVERSITE DE LIEGEDELARGE, JacquesPIROTTE, BernardDOGNE, Jean-Michelde LEVAL, XavierJULEMONT, Fabien
    • DELARGE, JacquesPIROTTE, BernardDOGNE, Jean-Michelde LEVAL, XavierJULEMONT, Fabien
    • C07D213/00
    • C07D213/76C07D213/89
    • New pyridinic sulfonamide derivatives represented by a general formula (I), wherein A represents a Nitrogen or a -N = O group; X represents Oxygen, Sulphur or an element selected from the group consisting of ( -NR 3 , -CR 3 R 4 , -SO, -SO 2 , or -CO); wherein R 3 and R 4 which can be identical or different, denotes each independently one element selected from the group consisting of (hydrogen , a mono- or polyhalogenated C l-12 -alkyl, a mono- or polyhalogenated C 3-8 -cycloalkyl , a C 1-12 -alkyl or a C 3-8 -cycloalkyl); R 1 , represents a mono- or polyhalogenated C l-12 -alkyl or a mono- or poly-halogenated C 3-8 -cycloalkyl group; R 2 represents a C 3-8 -cycloalkyl group or an aryl group substituted or not by one or several elements selected from the group consisting of (halogen, C l-12 -alkyl, C 3-8 -cycloalkyl, R 1 , hydroxy, C 1-6 -alkoxy, C 1-6 -alkoxy-C l-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 5 arylthio, R 5 arylsulfinyl, R 5 arylsulfonyl, C 1-6 -alkoxycarbonyl, C 1-6 -alkoxycarbonyl-C 1-6 -alkyl, carbamyl, carbamylmethyl, 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 5 aryl, R 5 arylalkyl, R 5 aryloxy); where R 5 denotes one or several elements selected from the group consisting of (hydrogen, C 1-6 -alkyl, halogen, hydroxy or C 1-6 -alkoxy). The method of production of such derivatives and their use as active therapeutic substance in the treatment of diseases such as inflammation, arthrosis, cancer, angiogenesis and asthma are also reported.
    • 通式(I)表示的新的吡啶磺酰胺衍生物,其中A代表氮或-N = O基团; X代表氧,硫或选自下列的元素:(-NR 3,-CR 3 R 4,-SO 3 - , - SO 2或-CO); 其中R 3和R 4可以相同或不同,各自独立地表示选自(氢,一或多卤代C 1 -C 4烷基, 1-12-烷基,单卤代或多卤代C 3-8 - 环烷基,C 1-12 - 烷基或C 3-12 - -8 - 环烷基); R 1表示单卤代或多卤代C 1-12烷基或单卤代或多卤代C 3-8环烷基 组; R 2代表C 3-8 - 环烷基或取代或不取代一个或多个选自(卤素,C 1 -C 4)烷基, C 1 -C 12 - 烷基,C 3-8 - 环烷基,R 1,羟基,C 1-6烷氧基,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 - 烷基,C 1-6烷基, 单烷基或二烷基氨基,氨磺酰基,C 1-6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 5芳基硫基,R 5芳基亚磺酰基,R 5芳基磺酰基,C 1 -C 6烷基磺酰基, 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烷氧基羰基,C 1-6烷氧基羰基-C 1-6烷基, 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 - 单烷基氨基磺酰基或二烷基氨基磺酰基,羧基,羧基-C 1-6烷基,酰基,R 5 5芳基,R 5 5芳基烷基 ,R5 =芳氧基); 其中R 5表示选自(氢,C 1-6 - 烷基,卤素,羟基或C 1-6 - /子> - 烷氧基)。 还报道了这类衍生物的制备方法及其在治疗疾病如炎症,关节病,癌症,血管生成和哮喘中作为活性治疗物质的用途。