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Sulfonamidsubstituerte kondenserte 5-ringforbindelser, deres anvendelse som medikament samt farmas°ytiske preparater inneholdende forbindelsene

机译:磺酰胺取代的稠合5环化合物,其用作包含该化合物的药物和药物制剂的用途

摘要

3-Sulfonamido-indene, benzofuran, indole or benzothiophene derivatives (I) are new. Sulfonamides of formula (I) and their salts are new: X = CR22R23, O, NR24, S, SO or SO2; R1,R2 = H, CF3 or alkyl; R2 may also = OR10a if X = CR22R23; R9 = H; or R2 + R9 = bond; R10a = H, acetyl or 1-3C alkyl; R3 = R10b-CnH2n-N(R11) or R10b-CnH2n (in which one CH2 of CnH2n is optionally replaced by O, CO, S, SO, SO2 or NR12a); R4 = R13-CrH2r (in which one CH2 of CrH2r is optionally replaced by O, CH=CH, C equivalent to C, CO, COO, OCO, S, SO, SO2, NR14 or CONR14); or R3 + R4 = 3-8C alkylene (in which one CH2 is optionally replaced by O, CO, S, SO, SO2 or NR12a); n = 0-10; r = 0-20; R12a = H, Me or Et; R10b = Me, cycloalkyl, CF3, C2F5 or C3F7; R11 = H or alkyl; or or R10b + R11 = bond if n = 3-10; R14 = H, 1-3C alkyl, CyH2yOR12b or CyH2yN(R12b)2; R12b = H, Me or Et; y = 2 or 3; R13 = Me, CF3, C2F5, C3F7, cycloalkyl, NR15R16, CONR15R16, OR17 or COOR17; or phenyl or 1-9C N-containing heterocycle (both optionally mono- or disubstituted by Q); Q = F, Cl, Br, I, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SONH2, SO2Me or NHSO2Me; R15,R16 = H or 1-4C alkyl; or R15+R16 = (CH2)4 or (CH2)5 (in which one CH2 is optionally replaced by O, S, NH, NMe or N(CH2Ph)); R17 = H, 1-3C alkyl or CzH2zR12c; R12c = H, Me or Et; z = 2 or 3; R5-R8 = H, F, Cl, Br, I, 1-5C alkyl, cycloalkyl, CN, CF3, C2F5, C3F7, N3, NO2 or -Y-CsH2s-R18; or phenyl, thienyl, furyl or 1-9C N-containing heterocycle (all optionally mono- or disubstituted by Q); Y = O, CO, COO, OCO, S, SO, SO2, OSO2, SO2NR10c or CONR10c (all bonded to the basic structure via the left-hand atom); R10c = H or 1-3C alkyl; s = 1-6; R18 = H, Me, CF3, C2F5, cycloalkyl, OR21, COOR21, NR15R16 or CONR15R16; or phenyl or 1-9C N-containing heterocycle (both optionally mono- or disubstituted by Q); R21 = H or 1-3C alkyl; R22,R23 = H, CF3 or alkyl; R24 = H, alkyl or phenyl (optionally mono- or disubstituted by Q); and alkyl moities = 1-6C and cycloalkyl 3-8C unless specified otherwise.
机译:3-磺酰胺基茚,苯并呋喃,吲哚或苯并噻吩衍生物(I)是新的。式(I)的磺酰胺及其盐是新的:X = CR22R23,O,NR24,S,SO或SO2; R1,R2 = H,CF3或烷基;如果X = CR22R23,则R2也可以= OR10a; R9 = H;或R2 + R9 =键; R10a = H,乙酰基或1-3C烷基; R3 = R10b-CnH2n-N(R11)或R10b-CnH2n(其中CnH2n的一个CH2可选地被O,CO,S,SO,SO2或NR12a代替); R4 = R13-CrH2r(其中CrH2r的一个CH2任选地被O,CH = CH,等于C,CO,COO,OCO,S,SO,SO2,NR14或CONR14的C取代);或R 3 + R 4 = 3-8C亚烷基(其中一个CH 2任选地被O,CO,S,SO,SO 2或NR 12a取代);或n = 0-10; r = 0-20; R12a = H,Me或Et; R10b = Me,环烷基,CF3,C2F5或C3F7; R11 = H或烷基;或如果n = 3-10,则R10b + R11 =键; R14 = H,1-3C烷基,CyH2yOR12b或CyH2yN(R12b)2; R12b = H,Me或Et; y = 2或3; R13 = Me,CF3,C2F5,C3F7,环烷基,NR15R16,CONR15R16,OR17或COOR17;或苯基或含1-9C N的杂环(均被Q单或双取代); Q = F,Cl,Br,I,CF3,NO2,CN,NH2,OH,Me,Et,OMe,NMe2,SONH2,SO2Me或NHSO2Me; R15,R16 = H或1-4C烷基;或R 15 + R 16 =(CH 2)4或(CH 2)5(其中一个CH 2任选地被O,S,NH,NMe或N(CH 2 Ph)取代);或R17 = H,1-3C烷基或CzH2zR12c; R12c = H,Me或Et; z = 2或3; R5-R8 = H,F,Cl,Br,I,1-5C烷基,环烷基,CN,CF3,C2F5,C3F7,N3,NO2或-Y-CsH2s-R18;或苯基,噻吩基,呋喃基或1-9C个含N的杂环(全部任选被Q单或双取代); Y = O,CO,COO,OCO,S,SO,SO2,OSO2,SO2NR10c或CONR10c(均通过左侧原子键合到基本结构上); R10c = H或1-3C烷基; s = 1-6; R18 = H,Me,CF3,C2F5,环烷基,OR21,COOR21,NR15R16或CONR15R16;或苯基或含1-9C N的杂环(均被Q单或双取代); R21 = H或1-3C烷基; R22,R23 = H,CF3或烷基; R24 = H,烷基或苯基(任选被Q单或双取代);除非另有说明,否则烷基部分= 1-6C和环烷基3-8C。

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