The Dupont Merck Pharmaceutical Company

Dupont Pharmaceuticals Company

Gregory James Pacofsky

Eugene Cruz Amparo

William Henry Miller

Patricia C Weber

John Wityak

Michael J Orwat

Robert J Cherney

John Matthew Fevig

Steven P Seitz

John J Duncia

Matthew M Abelman

Joseph Cacciola

Robert F Kaltenbach

Arthur D Patten

Emeka A Akamike

Joseph B Santella

Robert A Galemmo, Jr

Charles A Kettner

Chia-Lin J Wang

Robert M Knabb

Joseph Basil Santella, Iii

This invention relates to electrophilic dipeptide analogs conjugated to an N,N-disubstituted .alpha.-amino acid as inhibitors of trypsin-like serine protease enzymes.

Electrophilic peptide analogs as inhibitors of trypsin-like enzymes

Novel boronic acid and ester and carboxyl-modified amino acid compounds of the Formula I, which are inhibitors of trypsin-like enzymes, are disclosed :

Boronic acid and ester inhibitors of thrombin

Anticancer compounds of formula I: ##STR1## and pharmaceutically acceptable salts thereof, wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.9 and R.sup.10 are independently selected from the group H, C.sub.1 -C.sub.4 alkyl, OR.sup.4, N(R.sup.4).sub.2, NO.sub.2, CN, F, Cl, Br, I, Ph, and CF.sub.3, and NHC(O)R.sup.4 ;

Polycyclic and heterocyclic chromophores for bis-imide tumoricidals

The present invention relates to the discovery of new C-terminal boronic acid dipeptide inhibitors of trypsin-like enzymes such as thrombin and pharmaceutical compositions thereof.

Dipeptide boronic acid inhibitors of trypsin-like enzymes

Anticancer compounds of formula I: ##STR1## and pharmaceutically acceptable salts thereof, wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected H, CH.sub.3, NH.sub.2, NO.sub.2, and CN;

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Raleigh, NC, United States of America

Gregory James Pacofsky