The Procter Gamble Company

Kelly Lynn McDow-Dunham

Biswanath De

Stanislaw Pikul

Yetunde Olabisi Taiwo

Neil Gregory Almstead

Michael G Natchus

Thomas L Cupps

Rimma Sandler Bradley

1,3-diheterocyclic metalloprotease inhibitors

Diheterocyclic metalloprotease inhibitors

Disclosed are compounds which are inhibitors of metalloproteases having the following structure: ##STR1## where Ar, W, X, Y, Z, R.sub.1 and R.sub.2 have the meanings described in the specification and optical isomers, diastereomers, and enantiomers thereof or a pharmaceutically-acceptable salt, or biohydrolyzable amides, esters, or imides thereof. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by unwanted metalloprotease activity using these compounds or pharmaceutical compositions.

The invention provides compounds of formula ##STR1## as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.

1,5-heterocyclic metalloprotease inhibitors

The invention provides compounds which are useful as inhibitors of matrix metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I) ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are described in the claims, a stereoisomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable alkoxyamide, ester acyloxyamide, imide or derivative thereof. Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by matrix metalloprotease activity using these compounds or the pharmaceutical compositions containing them.

Phosphinic acid amides as matrix metalloprotease inhibitors

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Loveland, OH, United States of America

Kelly Lynn McDow-Dunham