Heteroaryl amidines, methylamidines and guanidines, and the use thereof as protease inhibitors

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United States of America Patent

PATENT NO 6562840
SERIAL NO

10082127

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Abstract

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The present invention is directed to compounds of Formula I: ##STR1## wherein X is O, S or NR.sup.7 and R.sup.1 --R.sup.7, Y and Z are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, plasmin and urokinase. Certain of the compounds exhibit direct, selective inhibition of urokinase, or are intermediates useful for forming compounds having such activity.

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Patent Owner(s)

Patent OwnerAddress
3-DIMENSIONAL PHARMACEUTICALS INC665 STOCKTON DRIVE SUITE 104 EXTON PA 19341

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Hoffman, James B Ardmore, PA 8 88
Illig, Carl R Phoenixville, PA 91 982
Marugan, Juan Jose Exton, PA 32 144
Rudolph, M Jonathan Doylestown, PA 13 188
Subasinghe, Nalin L West Chester, PA 13 130
Wilson, Kenneth J Exton, PA 43 549

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