Boehringer Ingelheim (canada) Ltd.

Bio-mega/boehringer Ingelheim Research Inc.

Biomega, Inc.

Boehringer Ingelheim Gmbh

UniversitÈ Laval

Pierre Lavallee

Pierre Louis Beaulieu

Bruno Simoneau

Sumanas Rakhit

Paul C Anderson

Yvan Guindon

Christiane Yoakim

Murray D Bailey

Marc-Andre Poupart

Julian Adams

Gulrez Fazal

Yvon Cormier

Evelyne Israel-Assayag

Raymond Plante

Robert Deziel

Grace L Jung

Francedillaois Soucy

Bildad Nyambura

Gregory P Cosentino

Gary W Bantle

William Ogilvie

The present disclosure relates to a novel active compound having the formula Ia: solid preparations, uses and methods for the treatment or prevention of respiratory diseases comprising said compound as well as process of preparation thereof.

Preparation and method for use in the treatment of respiratory diseases

Peptidomimetic inhibitors of the human cytomegalovirus protease

Disclosed herein are compounds of formula 1 ##STR1## wherein X is a terminal group, for example, an aryloxycarbonyl, an alkanoyl or an optionally mono- or disubstituted carbamoyl; B is absent or an amino acid residue, for example, Val or Asn; R.sup.1 is hydrogen or a ring substituent, for example, fluoro or methyl; R.sup.2 is alkyl; and Y is a ring substituent, for example, phenoxy, 2-pyridinylmethoxy, phenylthio or 2-pyridinylthio. The compounds inhibit the activity of human immunodeficiency virus (HIV) protease and interfere with HIV induced cytopathogenic effects in human cells. These properties render the compounds useful for combating HIV infections.

Substituted pipecolinic acid derivatives as HIV protease inhibitors

Disclosed herein are peptide derivatives of the formula X�--NR.sup.1 --CH(R.sup.2)--C(W.sup.1)!.sub.n --NH--CR.sup.3 (R.sup.4)--C(W.sup.2)--NR.sup.5 --CH�CH.sub.2 C(O)--Y!--C(W.sup.3)--NH--CR.sup.6 --�CR.sup.7 --(R.sup.8)--COOH!--C(W.sup.4)--NH--CR.sup.9 (R.sup.10)--Z wherein X is a terminal group, for example, alkanoyl or phenylalkanoyl radicals, R.sup.1 is hydrogen, alkyl or phenylalkyl, R.sup.2, R.sup.4 and R.sup.10 am selected from amino acid or derived amino acid residues, R.sup.3, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are hydrogen or alkyl, or R.sup.7 and R.sup.8 are joined to form a cycloalkyl, W.sup.1, W.sup.2, W.sup.3 and W.sup.4 are oxo or thioxo, Y is, for example, an alkyl or a cycloalkyl, Z is a terminal group, for example, COOH or CH.sub.2 OH, and n is 0 or 1. The derivatives are useful for treating herpes infections.

Antiviral peptide derivatives having a 2-oxoalkyl amino acid side chain

Disclosed herein is a method of using compounds of the formula:

Method of using renin inhibiting N-(2-amino-2-oxoethyl) butanediamide

Disclosed herein are pentapeptide derivatives of the formula (SEQ ID NO: 24) XNR.sup.1 --CH(R.sup.2)--C(O)--NH--CH(R.sup.3 --C(O)--NR.sup.4 --CH(CH.sub.2 Y)--CO--NH--CH[CR.sup.5 (R.sup.6)--COOH]--C(W)--NH--CH(R.sup.7)--Z wherein X is a terminal group, for example, alkanoyl or phenylalkanoyl radicals, R.sup.1 is alkyl or phenylalkyl, R.sup.2, R.sup.3 and R.sup.7 are selected from the side chains of amino acid or derived amino acid residues, R.sup.4, R.sup.5, and R.sup.6 are hydrogen or lower alkyl, W is oxo or thioxo, Y is carboxy, carbamyl or 5-1H-tetrazolyl and Z is carboxy or 5-1H-tetrazolyl. The derivatives are useful for treating herpes infections.

Growing community of inventors

Rosemere, Canada

Pierre Lavallee