Syntex (u.s.a.) Inc.

Pfizer Corporation

Syntex LLC

Robin W Spencer

Alexander Krantz

Heinz W Pauls

Roger A Smith

Arthur A Nagel

Fredric J Vinick

Tim F Tam

W Stephen Faraci

A series of aromatic pyrrolidine derivatives and suitable pharmaceutically acceptable salts thereof are disclosed. These compounds are useful as PEP inhibitors in the treatment of Alzheimer's disease, amnesia, dementia, anxiety ischemia, or stroke.

Aromatic pyrrolidine amide prolyl endopeptidase inhibitors

Thiol protease inhibitors are disclosed having the formula: ##STR1## or an optical isomer thereof, or a pharmaceutically acceptable salt thereof, wherein:

Aryloxy and arylacyloxy methyl ketones as thiol protease inhibitors

Compounds of the formula ##STR1## wherein n is 1-3; R.sup.1, R.sup.2 and R.sup.3 are the same or different and are hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl or aryl lower alkyl wherein when aryl is phenyl it is unsubstituted or independently substituted with one or more halo, lower alkyl or lower alkoxy groups; and R.sup.4 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, trialkylsilyl, aryl or aryl lower alkyl wherein when aryl is phenyl it is unsubstituted or independently substituted by one or more halo, lower alkyl or lower alkoxy groups; excluding those compounds wherein R.sup.1 and R.sup.2 are hydrogen and R.sup.4 is ethyl, propyl or butyl. These compounds are useful as protease inhibitors.

Ynenolactone protease inhibitors

Growing community of inventors

East Lyme, CT, United States of America

Robin W Spencer