Cyanoguanidines as k-channel blockers

Details Cyanoguanidines as k-channel blockers Cyanoguanidines as k-channel blockers

C - Chemistry, Metallurgy

07

D

C07D 213/75 (2006.01) A61K 31/44 (2006.01) C07D 213/78 (2006.01) C07D 213/89 (2006.01) C07D 401/04 (2006.01)

Patent

CA 2179036

Cyanoguanidine compounds of Formula (I) and their pharmaceutically acceptable acid addition salts where R1 is hydrogen or methyl; R2 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl C3-C5 cycloalkyl, C3-C5 cycloalkenyl, hydroxymethyl, methoxy C1-C5 alkyl, or R1 and R2 are combined to form a C3-C6 carboxyclic 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)mOC1-C3 alkyl, NHC(O)C1-C3 alkyl, F, Cl, Br, C1-C3 alkyl, NH(CH2)mF, 1-imidazolyl, NHOC1-C3 alkyl, NHOH, NHSO2C1-C3 alkyl, SH, SC1-C3 alkyl, NHC(O)OC1-C3 alkyl, NHC(O)NHC1-C3 alkyl, NHSO2NHC1-C3 alkyl, NHSO2N(C1-C3 alkyl)2 or amino acid amide; R7 is C1-C7 alkyl, NH2, NHC1-C3 alkyl, N(C1-C3 alkyl)2, CF3, F, Cl, Br, I, OC1-C3 alkyl, OH, COOH, C(O)OC1-C3 alkyl, C(O)NH2, C(O)NHC1-C3 alkyl, C(O)C1-C3 alkyl, C(O)N(C1-C3 alkyl)2, SO2NH2, SO2NHC1-C3 alkyl, CN, SO2N(C1-C3 alkyl)2, NHC(O)C1-C3 alkyl, NHC(O)NHC1-C3 alkyl, NHC(O)N(C1-C3 alkyl)2, NHSO2NHC1-C3 alkyl, NHSO2N(C1-C3 alkyl)2, SH, SC1-C3 alkyl, NO2, SO2C1-C3 alkyl, NHC(O)OC1- C3 alkyl, amino acid amide or hydrogen; R8 is hydrogen, C1-C6 alkyl, NH2, NHC1- C3 alkyl, N(CH3)2, N(C2H5)2, F, Cl, Br, OC1-C3 alkyl or OH; and where m is 2 or 3 and n is 0 or 1 (except for those compounds where R8 is hydrogen and R6 is hydrogen, NH2, NHCH3, NHC2H5, NHCH(CH3)2, N(CH3)2, N(C2H5)2, NH(CH2)m-OC1- C3 alkyl, NHC(O)C1-C3 alkyl, Cl or Br). 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 se rapporte à des composés de cyanoguanidine de la formule (I) et à leurs sels d'addition acides pharmaceutiquement acceptables, formule dans laquelle R¿1? représente hydrogène or méthyle; R¿2? représente alkyle C¿1?-C¿6?, alcényle C¿2?-C¿6?, alkynyle C¿2?-C¿6?, cycloalkyle C¿3?-C¿5?, cycloalcényle C¿3?-C¿5?, hydroxyméthyle, méthoxy C¿1?-C¿5? alkyle, ou bien R¿1? et R¿2? sont combinés pour former un cycle carbocyclique C¿3?-C¿6?; R¿3? et R¿4? sont chacun, indépendamment, sélectionnés parmi hydrogène, alkyle C¿1?-C¿4?, F, Cl, Br, I ou CF¿3?; R¿5? représente hydrogène, F ou Cl; R¿6? représente hydrogène, NH¿2?, NHCH¿3?, NHC¿2?H¿5?, NHCH(CH¿3?)¿2?, N(CH¿3?)¿2?, N(C¿2?H¿5?)¿2?, NH(CH¿2?)¿m?OC¿1?-C¿3? alkyle, NHC(O)C¿1?-C¿3? alkyle, F, Cl, Br, alkyle C¿1?-C¿3? , NH(CH¿2?)¿m?F, 1-imidazolyle, NHOC¿1?-C¿3? alkyle, NHOH, NHSO¿2?C¿1?-C¿3? alkyle, SH, SC¿1?-C¿3? alkyle, NHC(O)OC¿1?-C¿3? alkyle, NHC(O)NHC¿1?-C¿3? alkyle, NHSO¿2?NHC¿1?-C¿3? alkyle, NHSO¿2?N(alkyle C¿1?-C¿3?)¿2? ou un amide d'acide aminé; R¿7? représente alkyle C¿1?-C¿7?, NH¿2?, NHC¿1?-C¿3? alkyle, N(alkyle C¿1?-C¿3?)¿2?, CF¿3?, F, Cl, Br, I, OC¿1?-C¿3? alkyle, OH, COOH, C(O)OC¿1?-C¿3? alkyle, C(O)NH¿2?, C(O)NHC¿1?-C¿3? alkyle, C(O)C¿1?-C¿3? alkyle, C(O)N(alkyle C¿1?-C¿3?)¿2?, SO¿2?NH¿2?, SO¿2?NHC¿1?-C¿3? alkyle, CN, SO¿2?N(alkyle C¿1?-C¿3?)¿2?, NHC(O)C¿1?-C¿3? alkyle, NHC(O)NHC¿1?-C¿3? alkyle, NHC(O)N(alkyle C¿1?-C¿3?)¿2?, NHSO¿2?NHC¿1?-C¿3? alkyle, NHSO¿2?N(alkyle C¿1?-C¿3?)¿2?, SH, SC¿1?-C¿3? alkyle, NO¿2?, SO¿2?C¿1?-C¿3? alkyle, NHC(O)OC¿1?-C¿3? alkyle, un amide d'acide aminé ou hydrogène; R¿8? représente hydrogène, alkyle C¿1?-C¿6?, NH¿2?, NHC¿1?-C¿3? alkyle, N(CH¿3?)¿2?, N(C¿2?H¿5?)¿2?, F, Cl, Br, OC¿1?-C¿3? alkyle ou OH; et où m vaut 2 ou 3 et n vaut 0 ou 1 (excepté pour les composés où R¿8? représente hydrogène et R¿6? représente hydrogène, NH¿2?, NHCH¿3?, NHC¿2?H¿5?, NHCH(CH¿3?)¿2?, N(CH¿3?)¿2?, N(C¿2?H¿5?)¿2?, NH(CH¿2?)¿m?-OC¿1?-C¿3? alkyle, NHC(O)C¿1?-C¿3? alkyle, Cl ou Br). Les composés de la formule (I) sont des agents bloquants des canaux de potassium utiles dans le traitement de troubles cardiovasculaires, tels que l'insuffisance cardiaque congestive et l'hypertension, et agissent également comme diurétiques.

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