The Upjohn Co.

Pharmacia & Upjohn Company

Stephen J Humphrey

Jackson B Hester, Jr

James H Ludens

Kaushik D Meisheri

E Jon Jacobsen

James Taylor Curry

A diuretic compound of Formula I ##STR1## or pharmaceutically acceptable salt thereof where R.sup.1 is a C.sub.1-6 alkyl; R.sup.2 is halogen, C.sub.1-4 alkyl; and R.sup.3 is C.sub.1-4 alkoxy are disclosed, preferably, benzamide, 3-chloro-N-(2-ethyl-2-(3-methoxyphenyl)-4-(1-piperidinyl)butyl), monohydrochloride. The compounds are effective diuretics which increase the excretion of water with little increase in electrolyte excretion.

Diuretic compound

Cyanoguanidines as K-channel blockers

Pyrimidine, cyanoguanidines as K-channel blockers

Cyanoguanidine compounds of Formula I and its pharmaceutically acceptable acid addition salts ##STR1## 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.

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Kalamazoo, MI, United States of America

Stephen J Humphrey