Bicyclic pyrimidine derivatives and their use as anti-coagulants

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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544105, A61K 31535, C07D26536, C07D49802

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active

058469729

ABSTRACT:
This invention is directed to bicyclic pyrimidine derivatives of the following formulae: ##STR1## where A is --O--and Z.sup.1,Z.sup.2,R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6,R.sup.7 are defined herein. These compounds are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing these compounds and methods of using the compounds to treat disease-states characterized by thrombotic activity.

REFERENCES:
patent: 5332822 (1994-07-01), Misra
Tidwell, R. et al., "Strategies for Anticoagulation with Synthetic Protease Inhibitors, Xa Inhibitors Versus Thrombin Inhibitors," Thrombosis Research, (1980) 19:339-349.
Sturzebecher, J. et al., "Cyclic Amides of N.alpha.-arysulfonylaminoacylated 4-amidinophenylalanine-Tight Binding Inhibitors of Thrombin," Thrombosis Research, (1983) 29:635-642.
Kikumoto, R. et al., "Selective inhibition of Thrombin by dinecarboxylic Acid," Biochemistry, (1984) 23:85-90.
Sturzebecher, J. et al., "Synthetic Inhibitors of Serine Proteinases XXIII, Inhibition of Factor Xa by Diamidines", Thrombosis Research, (1980) 17:545:548.

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