Boehringer Ingelheim Pharmaceuticals, Inc.

Bio-mega/boehringer Ingelheim Research Inc.

Boehringer Ingelheim (canada) Ltd.

Biomega, Inc.

Julian Adams

Karl D Hargrave

Karl G Grozinger

John Robert Proudfoot

Kollol Pal

Pierre Louis Beaulieu

John DiMaio

Raymond Plante

Ernest Cullen

Wolfgang Eberlein

Wolfhard Engel

Neil Moss

Edward S Lazer

Gunther Schmidt, Deceased

Clara K Miao

Gunther Trummlitz

Peter Farina

Sumanas Rakhit

Pierre Lavallee

Robert D&eacute;ziel

Pierre Lavalle/ E

Louis Grenier

Robert De/ Ziel

Mark Behnke

Disclosed herein are tetrapeptide derivatives of the formula X&mdash;NH&mdash;CHR,&mdash;C(W,)&mdash;NR,&mdash;CH&lsqb;CH,C(O)&mdash;Y&rsqb;&mdash;C(W,)&mdash;NH&mdash;CH&lsqb;CR,(R,)&mdash;COOH&rsqb;&mdash;C(W,)&mdash;NH&mdash;CHR,&mdash;Z wherein X is a terminal group, for example, alkanoyl or phenylalkanoyl radicals, R,and R,are selected from amino acid or derived amino acid residues, R,is hydrogen, alkyl or phenylalkyl, R,and R,are hydrogen or alkyl or R,and R,are joined to form a cycloalkyl, W,, W,and W,are oxo or thioxo, Y is, for example, an alkoxy or a monosubstituted or disubstituted amino, and Z is a terminal unit, for example, hydrogen, COOH or CH,OH. The derivatives are useful for treating herpes infections.

Antiherpes tetrapeptide derivatives having a substituted aspartic acid side chain

A process for the preparation of a 3-amino-2-chloro-4-alkylpyridine of the formula: ##STR1## wherein R is alkyl of from one to three carbon atoms, an intermediate in the preparation of certain 5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepine compounds useful in the prevention and treatment of HIV infection.

Method for the preparation of 3-amino-2-chloro-4-methylpyridines

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.

Antiherpes pentapeptides

Disclosed are novel 5,11-dihydro-6H-dipyrido[3,2-b; 2',3'-e][1,4]diazepines. These are useful in the prevention or treatment of HIV infection.

5,11-dihyro-6H-dipyrido[3,2-B:2',3'-e][1,3]diazepines and their use in

Disclosed are novel pyrido[2,3,-b][1,5]benzodiazepines. These compounds are useful in the treatment of AIDS, ARC and related disorders associated with HIV infection. ##STR1##

Pyridobenzo- and pyridiothieno-diazepines useful for the treatment of

Disclosed are novel pyrido[2,3-b][1,4]benzodiazepines. These compounds are useful in the treatment of AIDS, ARC and related disorders associated with HIV infection. The compounds are of the class having the structure: ##STR1##

Pyridobenzo-and pyridiothieno-diazepines useful for the treatment of HIV

2-(1-pyrrolidino)-benzoxazoles of general formula ##STR1## are disclosed which are inhibitors of leukotriene biosynthesis.

Pyrrolidine derivatives inhibitors of leukotriene biosynthesis

This invention relates to a novel method for preparing certain dipyrido-diazepines.

Method for the preparation of 5,11-dihydro-6h-dipyrido

Various substituted benzoxazoles and benzothiazoles, are described and disclosed, which are potent inhibitors of leukotriene synthesis in warm-blooded animals.

Leukotriene biosynthesis inhibitors

Disclosed are novel dipyrido[3,2-b:2',3'-e][1,4]diazepines and their use in the treatment of HIV-1 infection. An exemplary species is 6-chloro-11-cyclopropyl-4-methyl-11H-dipyrido[3,2-b:2',3'-e][1,4]diazepine , which has the following chemical structure: ##STR1##

Dipyrido[3,2-B:2 ',3'-E][1,4]Diaqzepines and their use in the treatment

Disclosed herein are pentapeptide derivatives of the formula X--NR.sup.1 --CH(R.sup.2)--C(W)--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 are 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 alkoxy or a mono or disubstituted amino, and Z is a terminal group, for example, COOH or CH.sub.2 OH. The derivatives are useful for treating herpes infections.

Antiherpes pentapeptide derivatives having a substituted aspartic acid

5,11-dihydro-6H-dipyrido(3,2-B:2',3'-E)(1,4)diazepines and their use in

Various substituted benzoxazoles, benzothiazoles, oxazolopyridines and thiazolopyridines are described and disclosed, compounds that are potent inhibitors of leukotriene synthesis in warm-blooded animals.

Disclosed herein are cyclic peptide derivatives of the formula ##STR1## wherein A is absent or the tripeptide radical Thr.rarw.Gly.rarw.Ala, R.sup.1 is benzyl or benzyl monosubstituted at position 4 of the aromatic ring with halo, hydroxy, lower alkyl or lower alkoxy, R.sup.2 and R.sup.4 each independently is hydrogen or lower alkyl, R.sup.3 is lower alkyl or lower alkyl monosubstituted with a hydroxy, R.sup.5 is lower alkyl, Y is oxo or thioxo and Z is hydroxy or NR.sup.6 R.sup.7 wherein R.sup.6 and R.sup.7 each independently is hydrogen or lower alkyl. The derivatives are useful for treating herpes infections.

Growing community of inventors

Ridgefield, CT, United States of America

Julian Adams