Antithrombotic amidinophenylalanine and amidinopyridylalanine de

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

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540594, C07D40112, A61K 3155

Patent

active

058613935

ABSTRACT:
This invention relates to compounds of formula (I), ##STR1## pharmaceutically acceptable salt thereof, and pharmaceutically acceptable solvates of either entity, wherein X is CH or N; Y is optionally monousaturated C.sub.3 -C.sub.5 alkylene optionally substituted with C.sub.1 -C.sub.4 allyl or methylene; R.sup.1 is H; C.sub.1 -C.sub.4 alkyl optionally substituted with C.sub.1 -C.sub.4 alkoxy, OH, NR.sup.5 R.sup.6, CONR.sup.5 R.sup.6, C.sub.3 -C.sub.6 cycloalkyl or aryl; or C.sub.3 -C.sub.6 alkenyl; R.sup.2 is H; C.sub.1 -C.sub.4 alkyl optionally substituted with C.sub.1 -C.sub.4 alkoxy, OH, NR.sup.5 R.sup.6, CONR.sup.5 R.sup.6, C.sub.3 -C.sub.6 cycloalkyl or aryl; or CONR.sup.5 R.sup.6 ; R.sup.3 and R.sup.4 are each independently selected from H; C.sub.1 -C.sub.4 alkyl optionally substituted with NR.sup.5 R.sup.6 ; C.sub.1 -C.sub.4 alkoxy; halo; CONR.sup.5 R.sup.6 and aryl; and R.sup.5 and R.sup.6 are each independently selected from H and C.sub.1 -C.sub.4 alkyl; are potent and selective thrombin inhibitors useful in the treatment of, inter alia, deep vein thrombosis; reocclusion following thrombolytic therapy; chronic arterial obstruction; peripheral vascular disease; acute myocardial infarction; unstable angina; atrial fibrillation; thrombotic stroke; transient ischaemic attacks; restenosis and occlusion following angioplasty; or neurodegenerative disorders.

REFERENCES:
Chemical Abstracts, vol. 123, No. 23, Abstract No. 314,532a pp. 962-963, Dec. 4, 1995.

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