Boehringer Ingelheim (Canada) Ltd.

Bio-mega/boehringer Ingelheim Research Inc.

Biomega, Inc.

Boehringer Ingelheim Gmbh

Dominik M Wernic

Jean Rancourt

Youla S Tsantrizos

Montse Llinas-Brunet

Murray D Bailey

Nathalie Goudreau

Teddy Halmos

Elise Ghiro

Anne-Marie Faucher

Dale R Cameron

Marc-Andre Poupart

Bruno Simoneau

Marc-Andr&eacute; Poupart

Dale Cameron

Yvan Guindon

Pierre Louis Beaulieu

Marc-André Poupart

John DiMaio

Jorge Jaramillo

Ellse Ghiro

Racemates, diastereoisomers and optical isomers of a compound of formula (I):wherein

Hepatitis C inhibitor tri-peptides

Racemates, diastereolsomers and optical isomers of a compound of formula (I):wherein B is H, a Cor Caryl, Caralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with Calkyl; Calkoxy; Calkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with Calkyl; amido; or (lower alkyl)amide; or

A racemate diastereoisomer and optical isomer of a compound of formula (I):wherein B is H, a Cor Caryl, Caralkyl; Het or (lower alkyl)-Het, all of which may be optionally substituted with Calkyl; Calkoxy; Calkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with Calkyl; amido; or (lower alkyl)amide; or

Hepatitis C inhibitor peptides

Racemates, diastereolsomers and optical isomers of a compound of formula (I):

Hepatitis C inhibitor tri-pepitides

Racemates, diastereoisomers and optical isomers of a compound of formula (I):

A racemate, diastereoisomer and optical isomer of a compound of formula (I):

Disclosed herein is a stereospecific synthesis amenable to the large scale preparation of a hydrochloric acid addition salt of a chlorohydrin of the formula ##STR1## wherein R.sup.1 and R.sup.2 are amino protective groups and R.sup.3 is an amino acid side chain or a protected amino acid side chain. The synthesis involves reacting an aldehyde of the formula ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined hereinbefore with (chloromethyl)lithium at -20.degree. C. or below and contacting the resulting diastereoisomeric mixture of lithium alcoholates with aqueous hydrochloric acid to obtain a separable mixture of the hydrochloric acid addition salts of the chlorohydrin and its corresponding hydroxy diastereoisomer. The hydrochloric acid addition salt of the chlorohydrin is transformed readily into corresponding optionally amino-protected aminoepoxides; for example, 3(S)-(tert-butyloxycarbonylamino)-l,2(S)-epoxy-4-phenyl-butane.

Process for key intermediates for HIV protease inhibitors

Disclosed herein are derivatives of atrial natriuretic peptides wherein the exocyclic N-terminal peptide segment is deleted and the two cysteinyl residues (at positions 105 and 121) of the natural sequence are replaced with a trivalent unit, --NHCH(CO--)--Q--X--Y--CH.sub.2 CH.sub.2 CO-- wherein Q is methylene, ethylene or CR'R' wherein R' and R' each independently is lower alkyl, X is oxy or thio, and Y is methylene or des-Y. The derivatives may be optionally substituted at various positions including positions 106, 107 and 124. The derivatives possess ANF-like activity and are indicated for treating hypertension and for treating pathological conditions resulting from an imbalance of body fluids and electrolytes.

Growing community of inventors

Laval, Canada

Dominik M Wernic