Pyrimidine, cyanoguandines as k-channel blockers

Details Pyrimidine, cyanoguandines as k-channel blockers Pyrimidine, cyanoguandines as k-channel blockers

C - Chemistry, Metallurgy

07

D

C07D 239/28 (2006.01) A61K 31/505 (2006.01) C07D 239/42 (2006.01) C07D 239/48 (2006.01)

Patent

CA 2161325

Pyrimidine-cyanoguanidine compounds Formula (I) and its pharmaceutically acceptable acid addition salts wherein R1 is hydrogen or methyl; R2 is C1-C6 alkyl, C2-C6 alkenyl, C21-C6 alkynyl, C3-C5 cycloalkyl, C3-C5 cycloalkenyl, hydroxy methyl, methoxy C1-C5 alkyl, or R1 and R2 are combined to form a C3-C6 carbocyclic ring; R3 and R4 are each independently selected to be hydrogen, C1-C4 alkyl, F. Cl, Br, I or CF3; R5 is hydrogen, F or Cl; R6 is hydrogen, -NH2, -NHCH3, -NHC2H5, -NHCH(CH3)2, -N(CH3)2, -N(C2H5)2, NH(CH2)m-OC1-C3 alkyl (where m is 2 or 3), -NHC(O)C1-C3 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.

L'invention concerne des composés de cyanoguanidine-pyrimidine de formule I et leurs sels d'addition d'acide pharmaceutiquement acceptables, formule dans laquelle R1 représente hydrogène ou méthyle; R2 représente alkyle C1-C6, alcényle C2-C6, alkynyle C2-C6, cycloalkyle C3-C5, cycloalcényle C3-C5, hydroxyméthyle, méthoxy-alkyle C1-C5, ou R1 et R2 sont combinés pour former un noyau carbocyclique C3-C6; R3 et R4 représentent indépendamment hydrogène, alkyle C1-C4, F, Cl, Br, I ou CF3; R5 représente hydrogène, F or Cl; R6 représente hydrogène, -NH2, -NHCH3, -NHC2H5, -NHCH(CH3)2, -N(CH3)2, -N(C2H5)2, NH(CH2)m-OC1-C3 alkyle (m correspond à 2 ou 3), -NHC(O)C1-C3 alkyle, Cl ou Br; et n correspond à 0 ou 1. Les composés de formule I sont des agents bloquants des vannes à potassium utilisés dans le traitement de troubles cardiovasculaires tels que l'insuffisance cardiaque congestive et l'hypertension, ainsi qu'en tant qu'agents diurétiques.

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