Substituted imidazole derivatives and their use as anti-thrombos

Details Substituted imidazole derivatives and their use as anti-thrombos Substituted imidazole derivatives and their use as anti-thrombos

1982-02-03

1985-04-30

Jiles, Henry R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

548342, 548343, 548235, A61K 31415, C07D23354, C07D23366

Patent

active

045144125

ABSTRACT:
Compounds of the formula: ##STR1## wherein each of R.sub.1, R.sub.2 and R.sub.3, which can be the same or different, is hydrogen, chloro, bromo, fluoro, methyl, ethyl, methoxy, amino, hydroxy or nitro; R.sub.4 is hydrogen or alkyl of 1 to 7 carbon atoms; R.sub.5 is hydrogen or a straight or branched alkyl group of 1 to 5 carbon atoms or a phenyl group; and R.sub.6 is hydrogen or an alkyl group of 1 to 7 carbon atoms or a substituted or unsubstituted benzyl, X is --CH.sub.2 --, --CHOH-- or --CH.dbd.CH-- and n is 0-4; provided that R.sub.5 and R.sub.6 are simultaneously hydrogen only when n is 4 and X is --CH.dbd.CH--; and their non-toxic pharmaceutically acceptable acid addition salts and mixtures thereof exhibit valuable pharmacological activity and are useful in the treatment of mammals, especially as antithrombotic agents. Furthermore, some of the compounds have proved to possess antihypertensive or .beta.-blocking activity. Antimicrobial and antifungal properties have also been found. Processes for the preparation of these compounds are described, as are novel pharmaceutical compositions comprising at least one of the compounds or their salts.

REFERENCES:
Schubert, et al., CA 60:14495c.
Wegner, et al., CA 85:46504a.
Iwasaki, CA 86:106471z.
J. Am. Chem. Soc., 95:1, 1973, pp. 284-285, Wuonola, et al.
J. Org. Chem., 39, pp. 2301-2302, Noyce, et al.
Chem. Abs., 71:124547u; Soniun, et al.
Chem. Abs., 52:4494i, Lawson.

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