wherein R(1) and R(2) mean independently C1-C3-alkyl or in common they mean alkylene chain with 2, 3, 4 carbon atoms or pentamethylene; R(3) - R(9) are CnH2n/NR(11)/m; R(9) is hydrogen atom; n = 0, 1, 2, 3, 4, 5, 6; R(11) is hydrogen atom, C1-C4-alkyl; m = 0 or 1; R(4) - R(12) are C1H2 being one CH2-group in the group CnH2r can be replaced for O-, - CO-O- or NR(10) wherein R(10) is methyl; R(12) is hydrogen atom, cycloalkyl with 3 carbon atoms, piperidyl, pyridyl, CpF2p+1 or phenyl; r = 1, 2, 3, 4, 5 or 6; p = 1; R(5), R(6), R(7), R(8) mean independently each of other hydrogen, fluorine, chlorine atom, C1-C2-alkyl, -CN, -NO2, -CONR(13) R(14), -COOR(15), R(16)-CsH2s-Y wherein their phenyl can be unsubstituted or substituted with bromine atom wherein R(16) is hydrogen atom, C1F2t+1; s = 0, 1, 2, 3 or 4; t = 1, 2 or 3; R(13) and R(14) mean independently hydrogen atom of in common mean alkylene chain with 5 carbon atoms; R(15) is hydrogen atom, CH3; Y is NH-, -O-, SO3- being, however, R(6) can not mean -OCF3,-OC2F5, and their physiologically acceptable salts also; and formula (1a): wherein R(A) is hydrogen atom; R(B) is hydrogen atom; R(1)-R(4) have values indicated in claim 1; R(C) is CN that are used for preparing a medicinal agent to block K+-channel that is opened by cyclic adenosine monophosphate (cAMP). EFFECT: improved preparing method, valuable medicinal and biochemical properties of compounds. 19 cl, 2 tbl, 124 ex"/> SULFONAMIDE-SUBSTITUTED CHROMANS, METHODS FOR THEIR PREPARING, THEIR APPLICATION AS MEDICINAL AND DIAGNOSTIC AGENT AND MEDICINAL AGENT CONTAINING THEREOF
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SULFONAMIDE-SUBSTITUTED CHROMANS, METHODS FOR THEIR PREPARING, THEIR APPLICATION AS MEDICINAL AND DIAGNOSTIC AGENT AND MEDICINAL AGENT CONTAINING THEREOF

机译:磺酰胺取代的铬酸酯,其制备方法,其作为药用和诊断剂以及包含其的药用剂的应用

摘要

FIELD: organic chemistry, medicine, biochemistry. SUBSTANCE: invention relates to novel derivatives of chroman of the formula (I) wherein R(1) and R(2) mean independently C1-C3-alkyl or in common they mean alkylene chain with 2, 3, 4 carbon atoms or pentamethylene; R(3) - R(9) are CnH2n/NR(11)/m; R(9) is hydrogen atom; n = 0, 1, 2, 3, 4, 5, 6; R(11) is hydrogen atom, C1-C4-alkyl; m = 0 or 1; R(4) - R(12) are C1H2 being one CH2-group in the group CnH2r can be replaced for O-, - CO-O- or NR(10) wherein R(10) is methyl; R(12) is hydrogen atom, cycloalkyl with 3 carbon atoms, piperidyl, pyridyl, CpF2p+1 or phenyl; r = 1, 2, 3, 4, 5 or 6; p = 1; R(5), R(6), R(7), R(8) mean independently each of other hydrogen, fluorine, chlorine atom, C1-C2-alkyl, -CN, -NO2, -CONR(13) R(14), -COOR(15), R(16)-CsH2s-Y wherein their phenyl can be unsubstituted or substituted with bromine atom wherein R(16) is hydrogen atom, C1F2t+1; s = 0, 1, 2, 3 or 4; t = 1, 2 or 3; R(13) and R(14) mean independently hydrogen atom of in common mean alkylene chain with 5 carbon atoms; R(15) is hydrogen atom, CH3; Y is NH-, -O-, SO3- being, however, R(6) can not mean -OCF3,-OC2F5, and their physiologically acceptable salts also; and formula (1a): wherein R(A) is hydrogen atom; R(B) is hydrogen atom; R(1)-R(4) have values indicated in claim 1; R(C) is CN that are used for preparing a medicinal agent to block K+-channel that is opened by cyclic adenosine monophosphate (cAMP). EFFECT: improved preparing method, valuable medicinal and biochemical properties of compounds. 19 cl, 2 tbl, 124 ex
机译:领域:有机化学,医学,生物化学。物质:本发明涉及式(I)的苯并二氢吡喃的新型衍生物。<图像文件=“ 00000003.GIF” he =“ 39” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 41” />其中R(1 )和R(2)独立地表示C 1 -C 3 -烷基,或共同地表示具有2、3、4个碳原子的亚烷基链或五亚甲基; R(3)-R(9)是C n H 2n / NR(11)/ m ; R(9)是氢原子; n = 0、1、2、3、4、5、6; R(11)是氢原子,C 1 -C 4 -烷基; m = 0或1; R(4)-R(12)是C 1 H 2 是C n <组中的一个CH 2 -基团/ Sub> H 2r 可以替换为O-,-CO-O-或NR(10),其中R(10)是甲基; R(12)是氢原子,具有3个碳原子的环烷基,哌啶基,吡啶基,C p F 2p + 1 或苯基; r = 1、2、3、4、5或6; p = 1; R(5),R(6),R(7),R(8)分别独立地表示氢,氟,氯原子,C 1 -C 2 -烷基,-CN,-NO 2 ,-CONR(13)R(14),-COOR(15),R(16)-C s H 2s -Y,其中它们的苯基可以未被取代或被溴原子取代,其中R(16)是氢原子,C 1 F 2t + 1 ; s = 0、1、2、3或4; t = 1、2或3; R(13)和R(14)独立地表示具有5个碳原子的共同平均亚烷基链的氢原子; R(15)为氢原子,CH 3 ; Y是NH-,-O-,SO 3 -,但是R(6)不能表示-OCF 3 ,-OC 2 F 5 及其生理上可接受的盐;和公式(1a):<图像文件=“ 00000004.GIF” he =“ 30” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 49” />其中R(A)是氢原子; R(B)是氢原子; R(1)-R(4)具有权利要求1中指示的值; R(C)是CN,用于制备药物以阻断由环一磷酸腺苷(cAMP)打开的K + 通道。效果:改进的制备方法,化合物的重要药用和生化特性。 19厘升,2汤匙,124前

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