Merrell Pharmaceuticals, Inc.

Merrell Dow Pharmaceuticals

H Michael Kolb

Joseph P Burkhart

Daniel G Schirlin

Eugene L Giroux

Bernhard Neises

Fritz E Gerhart, Deceased

Michel J Jung

Philippe Bey

Michael J Jung

This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.

Peptidase inhibitors

The present invention relates to a novel enantiospecific processes for preparing (S)-4-amino-hepta-5,6-dienoic acid and pharmaceutically acceptable salts thereof, which is useful as an irreversible inhibitor of GABA-T, to novel intermediates thereof, and a process for preparing an intermediate thereof.

(S)-4-amino-hepta-5,6-dienoic acid and intermediates therof

Processes for preparing (S)-4-amino-hepta-5,6-dienoic acid and

This invention relates to certain conjugates of folates and antifolates with difluoroglutamic acid which are useful in the treatment of patients suffering from certain neoplastic diseases including leukemia, melanomas, carcinomas, sarcomas and mixed neoplasias.

Difluoroglutamic acid conjugates with folates and anti-folates for the

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Cincinnati, OH, United States of America

H Michael Kolb