申请人:Pharmacia & Upjohn Company
公开号:US05668157A1
公开(公告)日:1997-09-16
Cyanoguanidine compounds of formula (I) and its pharmaceutically acceptable acid addition salts wherein R.sub.1 is hydrogen or methyl; R.sub.2 is C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.5 cycloalkyl, C.sub.3 -C.sub.5 cycloalkenyl hydroxy methyl, methoxy-C.sub.1 -C.sub.5 alkyl, or R.sub.1 and R.sub.2 are combined to form a C.sub.3 -C.sub.6 carbocyclic ring; R.sub.3 and R.sub.4 are each independently selected to be hydrogen, C.sub.1 -C.sub.4 alkyl, F, Cl, Br, I or CF.sub.3 ; R.sub.5 is hydrogen, F or Cl; R.sub.6 is hydrogen, --NH.sub.2, --NHCH.sub.3, --NHC.sub.2 H.sub.5, --NHCH(CH.sub.3).sub.2, --N(CH.sub.3).sub.2, --N(C.sub.2 H.sub.5).sub.2, NH(CH.sub.2).sub.m, --OC.sub.1 -C.sub.3 alkyl (where m is 2 or 3), --NHC(O)C.sub.1 -C.sub.3 alkyl, Cl or Br; and n is 0 or 1. The compounds of formula (I) are potassium channel blockers useful in the treatment of cardiovascular disorders such as congestive heart failure and hypertension and as a diuretic. ##STR1##
式(I)的氰脲基化合物及其药学上可接受的酸盐,其中R.sub.1为氢或甲基;R.sub.2为C.sub.1-C.sub.6烷基,C.sub.2-C.sub.6烯基,C.sub.2-C.sub.6炔基,C.sub.3-C.sub.5环烷基,C.sub.3-C.sub.5环烯基羟甲基,甲氧基-C.sub.1-C.sub.5烷基,或R.sub.1和R.sub.2结合形成C.sub.3-C.sub.6碳环;R.sub.3和R.sub.4各自独立选择为氢,C.sub.1-C.sub.4烷基,F,Cl,Br,I或CF.sub.3;R.sub.5为氢,F或Cl;R.sub.6为氢,--NH.sub.2,--NHCH.sub.3,--NHC.sub.2 H.sub.5,--NHCH(CH.sub.3).sub.2,--N(CH.sub.3).sub.2,--N(C.sub.2 H.sub.5).sub.2,NH(CH.sub.2).sub.m,--OC.sub.1-C.sub.3烷基(其中m为2或3),--NHC(O)C.sub.1-C.sub.3烷基,Cl或Br;n为0或1。式(I)的化合物是钾通道阻滞剂,可用于治疗心血管疾病,如充血性心力衰竭和高血压,以及作为利尿剂。