Peptide derivatives as thrombin inhibitors

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

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514 18, 530331, 548535, A61K 3805

Patent

active

056144997

ABSTRACT:
The invention relates to new competitive inhibitors of thrombin, pharmaceutical compositions containing the compounds as active ingredients, and the use of the compounds as anticoagulants for prophylaxis and treatment of thromboembolic diseases, according to the formula ##STR1## wherein A represents a methylene group, an ethylene group or a propylene group, which may be substituted or
A represents --CH.sub.2 --O--CH.sub.2 --, --CH.sub.2 --S--CH.sub.2 --, --CH.sub.2 --SO--CH.sub.2 --, or
A represents --CH.sub.2 --O--, --CH.sub.2 --S--, --CH.sub.2 --SO--, with the heteroatom functionality in position 4;
n is an integer 2 to 6; and
B represents --N(R.sup.6)--C(NH)--NH.sub.2, wherein R.sup.6 is H or a methyl group, or
B represents --S--C(NH)--NH.sub.2, or --C(NH)--NH.sub.2.

REFERENCES:
patent: 4568636 (1986-02-01), Svendsen
patent: 5037819 (1991-08-01), Han
patent: 5110812 (1992-05-01), Han
Chemical Abstracts, vol. 99, No. 25, 19 Dec. 1983 (Columbus, Ohio, USA), Bajusz, Sandor et al, "Inhibition of Thrombin with H- and Boc-D-Phe-Pro-Agm," p. 21, Abstract No. 205609.

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