3,5-substituted aminobenzoylguanidines, their use as a medicamen

Details 3,5-substituted aminobenzoylguanidines, their use as a medicamen 3,5-substituted aminobenzoylguanidines, their use as a medicamen

1995-05-25

1996-05-14

Haley, Jacqueline

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Nitrogen containing other than solely as a nitrogen in an...

564164, 564165, C07C31116, A61K 31165

Patent

active

055168051

ABSTRACT:
3,5-Substituted aminobenzoylguanidines, process for their preparation, their use as a medicament or diagnostic and medicament containing them
There are described benzoylguanidines of the formula I ##STR1## where one of the substituents R(1), R(2), R(3) or R(4) is: an amino group ##STR2## where R(5), R(6)=inter alia, H or alkyl, or alternatively R(5) and R(6), together with the nitrogen atom, are a 5-7-membered ring, and the other substituents R(1), R(2), R(3) and R(4) in each case are: H, Hal, CN, CF.sub.3, NO.sub.2, CF.sub.3 --O--, C.sub.m F.sub.2m+1 --CH.sub.2 --O--, R(11)--C.sub.q H.sub.2q --X.sub.p --, X=O or NR(12), R(11)=H, (cyclo)alkyl, phenyl, and where R(1) and R(4) are not simultaneously hydrogen.
The compounds I have very good antiarrhythmic and cardio-protective properties, but no undesired salidiuretic properties. They additionally exhibit protective properties against is chemically induced damage in vivo and in vitro in different organs and gastroprotective properties as a result of inhibition of gastric acid secretion. Moreover, they are distinguished by inhibitory action on the proliferation of cells.

REFERENCES:
patent: 3780027 (1973-12-01), Cragoe, Jr. et al.
patent: 5091394 (1992-02-01), Englert et al.
M. S. Glitzer et al., "N-Amidino-3-Amino-6-Chloropyrazinecarboxamide: A New Diuretic Which Antagonizes the Renal Actions of Aldosterone", Proceedings of the Society for Experimental Biology and Medicine, 120:364-367 (1965).
P. Mildner et al., Inhibition of Urease by some Triazole, Urea, and Guanidine Derivatives, Chemical Abstracts, 81(23):168, 147547g (1974).

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