Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-02-06
1996-10-22
Davis, Zinna Northington
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546306, C07D21375, A61K 3144
Patent
active
055677223
ABSTRACT:
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.
REFERENCES:
patent: 4057636 (1977-11-01), Petersen
Smallwood, JK, J. Card. Pharm., 12-:102-9 (1988).
Peterson HJ, J. Med. Chem., 21(8):773-781 (1978).
Robertson DW, et al., Annual Reports in Medicinal Chemistry 24, Ch 10, 91-100 (1989).
Petersen, Journal of Medicinal Chemistry, vol. 21, No. 8, 1978, pp. 773-781 .
Hester, Jr. Jackson B.
Humphrey Stephen J.
Ludens James H.
Meisheri Kaushik D.
Corneglio Donald L.
Davis Zinna Northington
The Upjohn Company
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