Arylsulfonylaminobenzene derivatives and the use thereof as factor Xa inhibitors

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United States of America Patent

PATENT NO 5741819
SERIAL NO

08488196

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Abstract

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The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds of structure: ##STR1## or pharmaceutically acceptable salts thereof; wherein R.sup.1 is alkyl, substituted alkyl, cycloalkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl; R.sup.2 is one of hydrogen, alkyl, cycloalkyl or aryl; R.sup.3 is one of hydrogen, hydroxy or alkoxy; R.sup.4 is one of --NH.sub.2, phenyl or pyridyl, wherein said phenyl and said pyridyl are optionally substituted with one or two of halogen, hydroxy, hydroxyalkyl, alkoxy, amino, monoalkylamino, dialkylamino, aminoalkyl, monoalkylaminoalkyl and/or dialkylaminoalkyl; X is one of --CH.sub.2 -- or --C(O)--; and n is from zero to eleven; provided that when R.sup.4 is --NH.sub.2, then R.sup.3 is hydrogen and n is other than zero; and also provided that when R.sup.3 is hydroxy or alkoxy, then R.sup.4 is other than --NH.sub.2, and n is other than zero.

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Patent Owner(s)

Patent OwnerAddress
3-DIMENSIONAL PHARMACEUTICALS INCEAGLEVIEW CORPORATE CENTER SUITE 104 665 STOCKTON DRIVE EXTON PA 19341 UNITED STATES OF AMERICA

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Illig, Carl R Phoenixville, PA 91 982
Lu, Tianbao Exton, PA 79 551
Salvino, Joseph M Schwenksville, PA 57 302
Soll, Richard M Lawrenceville, NJ 56 1558
Subasinghe, Nalin L West Chester, PA 13 130
Tomczuk, Bruce E Collegeville, PA 49 377

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