首页> 外国专利> NOVEL O-SUBSTITUTED DERIVATIVES OF BENZOYLGUANIDINE, METHOD OF OBTAINING THEM, THEIR APPLICATION IN PRODUCTION OF PHARMACEUTIC AND DIAGNOSTIC AGENTS AND PHARMACEUTIC GAENT AS SUCH

NOVEL O-SUBSTITUTED DERIVATIVES OF BENZOYLGUANIDINE, METHOD OF OBTAINING THEM, THEIR APPLICATION IN PRODUCTION OF PHARMACEUTIC AND DIAGNOSTIC AGENTS AND PHARMACEUTIC GAENT AS SUCH

机译:苯甲酰胍的新型O取代衍生物,获得它们的方法,其在生产制药和诊断试剂以及制药中间体中的应用

摘要

Benzoylguanidine compounds of formula (I) and their salts are new. R1 = R13-SOm or R14R15N-SO2; m = 1 or 2; R13 = 1-8C alkyl or perfluoroalkyl, 3-8C alkenyl or CnH2n-R16; n = 0-4; R16 = 3-8C cycloalkyl or phenyl, biphenyl or naphthyl (each optionally substituted by 1-3 F, Cl, CF3, CH3, OCH3 or NR25R26); R25, R26 = H or 1-4C alkyl or perfluoroalkyl; R14 = H, 1-8C alkyl or perfluoroalkyl, 3-8C alkenyl or CnH2n-R27; R27 = 3-8C cycloalkyl or phenyl, biphenyl or naphthyl (each optionally substituted by 1-3 F, Cl, CF3, CH3, OCH3 or NR28R29); R28, R29, R15 = H, or 1-4C alkyl or perfluoroalkyl; or R14+R15 = (CH2)a where one CH2 group may be replaced by O, S, NH, N-CH3 or N-benzyl; a = 4-5; one of R2, R3 = H and the other = CHR30R31 or C(OH)R33R34; R30 = (CH2)g-(CHOH)h-(CH2)i-(CHOH)k-R32 or (CH2)g-O-(CH2-CH2O)h-R24; R24, R32 = H or Me; g, h, i = 0-4; k = 1-4; R31, R33, R34 = H or 1-4C alkyl; or R33+R34 = 3-6C cycloalkyl; or R33 = CH2OH; R4 = 1-4C alkyl or alkoxy or F, Cl, Br, I, CN, (CH2)n'-(CF2)o-CF3; n' = 0-1; and o = 0-2.
机译:式(I)的苯甲酰胍化合物及其盐是新的。 R1 = R13-SOm或R14R15N-SO2; m = 1或2; R13 = 1-8C烷基或全氟烷基,3-8C烯基或CnH2n-R16; n = 0-4; R16 = 3-8C环烷基或苯基,联苯基或萘基(各自任选被1-3个F,Cl,CF3,CH3,OCH3或NR25R26取代); R25,R26 = H或1-4C烷基或全氟烷基; R14 = H,1-8C烷基或全氟烷基,3-8C烯基或CnH2n-R27; R27 = 3-8C环烷基或苯基,联苯基或萘基(各自任选地被1-3个F,Cl,CF3,CH3,OCH3或NR28R29取代); R28,R29,R15 = H或1-4C烷基或全氟烷基;或R 14 + R 15 =(CH 2)a,其中一个CH 2基团可以被O,S,NH,N-CH 3或N-苄基取代; a = 4-5; R2中的一个,R3 = H,另一个= CHR30R31或C(OH)R33R34; R30 =(CH2)g-(CHOH)h-(CH2)i-(CHOH)k-R32或(CH2)g-O-(CH2-CH2O)h-R24; R24,R32 = H或Me; g,h,i = 0-4; k = 1-4; R31,R33,R34 = H或1-4C烷基;或R33 + R34 = 3-6C环烷基;或或R33 = CH2OH; R4 = 1-4C烷基或烷氧基或F,Cl,Br,I,CN,(CH2)n’-(CF2)o-CF3; n'= 0-1;并且o = 0-2。

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