首页> 外国专利> SUBTITUTED DIARYL-DICARBOXYLIC-DI-GUANIDINES, PROCESS FOR PRODUCING THEM, THEIR USE FOR PREPARING PHARMACEUTICALS, AND DIAGNOSTICS AND PHARMACEUTCAL COMPOSITIONS CONTAINING THEM

SUBTITUTED DIARYL-DICARBOXYLIC-DI-GUANIDINES, PROCESS FOR PRODUCING THEM, THEIR USE FOR PREPARING PHARMACEUTICALS, AND DIAGNOSTICS AND PHARMACEUTCAL COMPOSITIONS CONTAINING THEM

机译:取代的二芳基-二羧酸基-二胍类化合物,其制备过程,其在制备药物中的用途以及诊断药和包含它们的药物和药物组合物

摘要

Diaryl dicarboxylic acid diguanidines of formula (I) and their salts are new. One of R1-R5 and one of R6-R10 = CON=C(NH2)2; of the others, R1, R5, R6, R10 = H, 1-4C alkyl, F, Cl, OR32, NR33R34 or CF3; R32-R34 = H or 1-4C alkyl; R2, R4, R7, R9 = H, F, Cl, Br, I, OH, CN, CF3, CON=C(NH2)2, 1-8C alkyl, 2-8C alkenyl, (CH2)mR14, pyrrol-(1, 2 or 3)-yl (optionally mono- to tetra-substituted by F, Cl, Br, I, CN, 2-8C alkanoyl, 2-8C alkoxycarbonyl, formyl, carboxy, CF3, methyl or methoxy), SO2R22, CONR23R24, COR28, SO2N(R29)R30, OR35 or N(R35)R36; m = 0-2; R14 = 3-8C cycloalkyl or phenyl (optionally mono- - tri-substituted with F, Cl, CF3, methyl, methoxy or N(R15)R16); R15, R16, R23, R24, R29, R30 = H or CH3; R22, R28 = methyl or CF3; R35, R36 = H or 1-6C alkyl; or R35+R36 = 4-7 methylene (optionally with one group substituted by O, S, NH, NCH3 or N-benzyl); R3 = H, SR25, OR25, N(R25)R26, C(R25)(R26)R27; R25 = H, 1-8C alkyl, phenyl (optionally mono- to tri-substituted with F, Cl, CF3, CH3, methoxy, hydroxy, amino, methylamino or dimethylamino), or 1-9C heteroaryl (optionally mono- to tri-substituted by F, Cl, CF3, CH3, OMe, OH, NH2, NHCH3, N(CH3)2); R26, R27 = as R25, or H or 1-8C alkyl; A = bond, N(R11)CO, N(R12)CON(R13), N(R17)CON(R18)SO2, N(R19)SO2, SO2, SO2N(R19)CO, OCON(R19)SO2 or C(R20)=C(R21); and R11 - R21 = H or 1-8C alkyl.
机译:式(I)的二芳基二羧酸二胍及其盐是新的。 R1-R5之一和R6-R10之一= CON = C(NH2)2;其中,R1,R5,R6,R10 = H,1-4C烷基,F,Cl,OR32,NR33R34或CF3; R32-R34 = H或1-4C烷基; R2,R4,R7,R9 = H,F,Cl,Br,I,OH,CN,CF3,CON = C(NH2)2、1-8C烷基,2-8C烯基,(CH2)mR14,吡咯-( 1、2或3)-基(可选被F,Cl,Br,I,CN,2-8C烷酰基,2-8C烷氧羰基,甲酰基,羧基,CF3,甲基或甲氧基单取代或四取代),SO2R22, CONR23R24,COR28,SO2N(R29)R30,OR35或N(R35)R36; m = 0-2; R14 = 3-8C环烷基或苯基(任选被F,Cl,CF3,甲基,甲氧基或N(R15)R16单-三取代); R15,R16,R23,R24,R29,R30 = H或CH3; R22,R28 =甲基或CF3; R35,R36 = H或1-6C烷基;或R35 + R36 = 4-7亚甲基(任选地被一个被O,S,NH,NCH3或N-苄基取代的基团);或R3 = H,SR25,OR25,N(R25)R26,C(R25)(R26)R27; R 25 = H,1-8C烷基,苯基(可选被F,Cl,CF3,CH3,甲氧基,羟基,氨基,甲基氨基或二甲基氨基单取代或三取代)或1-9C杂芳基(可选单取代至三被F,Cl,CF3,CH3,OMe,OH,NH2,NHCH3,N(CH3)2取代); R26,R27 = R25或H或1-8C烷基; A =键,N(R11)CO,N(R12)CON(R13),N(R17)CON(R18)SO2,N(R19)SO2,SO2,SO2N(R19)CO,OCON(R19)SO2或C (R20)= C(R21);和R11-R21 = H或1-8C烷基。

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