首页> 外国专利> Sulfonamidsubstituerte forbindelser, fremgangsmÕter for deres fremstilling, deres anvendelse som medikament eller diagnostikum, samt medikament inneholdende forbindelsen

Sulfonamidsubstituerte forbindelser, fremgangsmÕter for deres fremstilling, deres anvendelse som medikament eller diagnostikum, samt medikament inneholdende forbindelsen

机译:磺酰胺取代的化合物,其制备方法,作为药物或诊断剂的用途以及含有该化合物的药物

摘要

Pyranopyridine derivatives of formula (I) and their salts are new. R1, R2 = H, CF3, C2F5, C3F7, 1-6C alkyl or phenyl (optionally substituted by 1 or 2 F, Cl, Br, I, CF3, CH3, OCH3, sulphamoyl or methanesulphonyl); or R1+R2 = 2-10C alkylene (with one CH2 group optionally replaced by O, CO, S, SO, SO2 or NR10); R10 = H or 1-3C alkyl; R3 = R12-CaH2aÄNR13)Üm-; R12 = H, 3-8C cycloalkyl, CF3, C2H5 or C3H7; a = 0-10; m = 0 or 1; R13 = H or 1-6C alkyl; or R12+R13 = 4-8C alkylene (with one CH2 group optionally replaced by O, S, SO, SO2, CO or NR10); R4 = R14-CrH2r-; r = 0-20; R14 = H, 3-8C cycloalkyl, piperidyl, 1-pyrrolidinyl, N-morpholino, N-methylpiperazino, CF3, C2H5, C3H7, pyridyl, thienyl, imidazolyl or phenyl (optionally substituted by 1 or 2 F, Cl, Br, I, CF3, CH3, OCH3, sulphamoyl, methanesulphonyl or methanesulphonylamino); one CH2 group in CrH2r may be replaced by O, CH=CH, CC, CO, COO, OCO, CO-R11, S, SO, SO2 or NR11; or R3+R4 = 3-8C alkylene (with one CH2 group optionally replaced by O, S, SO, SO2, CO or NR11); R11 = H or -(CaH2a)-R10 (with one CH2 group optionally replaced by O, CH=CH, CC, CO, COO, OCO, S, SO, SO2, NR10 or CONR10); R5+R6 = -CR15=CR16-CR17=N-, -CR15=CR16-N=CR17-, -CR15=N-CR17=N-, -CR15=N-N=CR17-, -N=CR16-CR17=N- or -S-CR15=CR16; R15, R16, R17 = H, F, Cl, Br, I, 1-4C alkyl, 3-8C cycloalkyl, CN, CF3, C2H5, C3H7, NO2, CONR19R21, COOR21, R22-CsH2s-Z or phenyl (optionally substituted by 1 or 2 F, Cl, Br, I, CF3, CH3, OCH3, sulphamoyl or methanesulphonyl); R21 = H, methyl, ethyl, phenyl (optionally substituted by 1 or 2 F, Cl, Br, I, CF3, CH3, OCH3, sulphamoyl or methanesulphonyl) or CuH2uNR19R20 ; R19, R20 = H or 1-3C alkyl; u = 2 or 3; R22 = H, 3-8C cycloalkyl, COOR21, CONR19R21, thienyl, imidazolyl, pyridyl, quinolyl, isoquinolyl, piperidyl, 1-pyrrolidinyl, N-morpholino, N-methylpiperazino, CF3, C2H5, C3H7 or phenyl (optionally substituted by 1 or 2 F, Cl, Br, I, CF3, CH3, OCH3, sulphamoyl or methanesulphonyl); s = 0-6; Z = S, SO, SO2, CO, S-NR11, SO-NR11, SO2-NR11, SO2-O, O, NR11 or CO-NR11; R7 = H, OH, 1-4C alkoxy, 1-4C acyloxy, Cl, Br, F or 1-4C alkyl; and R8 = H or 1-6C alkyl.
机译:式(I)的吡喃吡啶衍生物及其盐是新的。 R1,R2 = H,CF3,C2F5,C3F7、1-6C烷基或苯基(任选地被1或2个F,Cl,Br,I,CF3,CH3,OCH3,氨磺酰基或甲磺酰基取代);或R 1 + R 2 = 2-10C亚烷基(带有一个CH 2基团,可选地被O,CO,S,SO,SO 2或NR 10取代);或R10 = H或1-3C烷基; R3 =R12-CaH2aÄNR13)Üm-; R12 = H,3-8C环烷基,CF3,C2H5或C3H7; a = 0-10; m = 0或1; R13 = H或1-6C烷基;或R 12 + R 13 = 4-8C亚烷基(带有一个CH 2基团,可选地被O,S,SO,SO 2,CO或NR 10取代);或R4 = R14-CrH2r-; r = 0-20; R14 = H,3-8C环烷基,哌啶基,1-吡咯烷基,N-吗啉代,N-甲基哌嗪子,CF3,C2H5,C3H7,吡啶基,噻吩基,咪唑基或苯基(可选被1或2 F,Cl,Br,I取代,CF3,CH3,OCH3,氨磺酰基,甲磺酰基或甲磺酰基氨基); CrH2r中的一个CH2基团可以被O,CH = CH,CC,CO,COO,OCO,CO-R11,S,SO,SO2或NR11取代;或R 3 + R 4 = 3-8C亚烷基(带有一个CH 2基团,可选地被O,S,SO,SO 2,CO或NR 11取代);或R11 = H或-(CaH2a)-R10(其中一个CH2基团可选地被O,CH = CH,CC,CO,COO,OCO,S,SO,SO2,NR10或CONR10取代); R5 + R6 = -CR15 = CR16-CR17 = N-,-CR15 = CR16-N = CR17-,-CR15 = N-CR17 = N-,-CR15 = NN = CR17-,-N = CR16-CR17 = N -或-S-CR15 = CR16; R15,R16,R17 = H,F,Cl,Br,I,1-4C烷基,3-8C环烷基,CN,CF3,C2H5,C3H7,NO2,CONR19R21,COOR21,R22-CsH2s-Z或苯基(可选地被取代1或2 F,Cl,Br,I,CF3,CH3,OCH3,氨磺酰基或甲磺酰基); R21 = H,甲基,乙基,苯基(任选地被1或2个F,Cl,Br,I,CF 3,CH 3,OCH 3,氨磺酰基或甲磺酰基取代)或CuH 2 uNR 19 R 20; R19,R20 = H或1-3C烷基; u = 2或3; R22 = H,3-8C环烷基,COOR21,CONR19R21,噻吩基,咪唑基,吡啶基,喹啉基,异喹啉基,哌啶基,1-吡咯烷基,N-吗啉代,N-甲基哌嗪基,CF3,C2H5,C3H7或苯基(可选被1或1取代) 2 F,Cl,Br,I,CF3,CH3,OCH3,氨磺酰基或甲磺酰基); s = 0-6; Z = S,SO,SO2,CO,S-NR11,SO-NR11,SO2-NR11,SO2-O,O,NR11或CO-NR11; R7 = H,OH,1-4C烷氧基,1-4C烷氧基,Cl,Br,F或1-4C烷基; R 8 = H或1-6C烷基。

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