Abbott Laboratories Corporation

Anthony K Fung

Jacob J Plattner

Saul H Rosenberg

William R Baker

Daniel T Chu

Steven Armen Boyd

Curt S Cooper

Herman H Stein

Zhenkun Ma

David S Garvey

Dale J Kempf

Jay R Luly

Biswanath De

Wang Shen

Gerard M Sullivan

Todd Warren Rockway

Stephen J O'Connor

Qun Li

Cheuk M Lee

Stephen A Fakhoury

Rajnandan N Prasad

Hing L Sham

Charles W Hutchins

John K Pratt

Martin Winn

John F DeBernardis

Howard E Morton

William J McClellan

Thomas W Von Geldern

David M Stout

Daniel Joseph Kerkman

Fatima Z Basha

Daniel J Plata

Jaroslav Kyncl

Andre G Pernet

Peter Hadley Jones

Diane M Yamamoto

Wei-Bo Wang

Thomas M Zydowsky

Kazumi Shiosaki

Jon F Denissen

Yvonne Connolly Martin

Dilbagh Singh Bariana

Yoek-Lin Armiger

B Gregory Donner

Amrit Lall

Yat Sun Or

Andrew Stewart Tasker

David John Augeri

Robert A Mantei

M Robert Leanna

David L Arendsen

Jeffrey A Kester

Raj Nandan Prasad

Robert M Leanna

Joseph F Dellaria

Hollis D Kleinert

Karin Rosemarie Tietje

Kenneth P Spina

John Hans Biel

Dilbagh S Bariana

Donald E Morrison

Antibacterial compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, as well as pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.

Pyridone antibiotic with improved safety profile

The present invention provides a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, which are useful for inhibiting protein farnesyltransferase and the farnesylation of the oncogene protein Ras or inhibiting de novo squalene production resulting in the inhibition of cholesterol biosynthesis, processes for the preparation of the compounds of the invention in addition to intermediates useful in these processes, a pharmaceutical composition, and to methods of using such compounds.

Inhibitors of squalene synthase and protein farnesyltransferase

The present invention provides a compound of the formula ##STR1## which inhibit squalene synthetase and cholesterol biosynthesis and are useful in the treatment of e.g., hyperlipidaemia, atherosclerosis, or fungal infections, processes for the preparation of the compounds of the invention, intermediates useful in these processes, and pharmaceutical compositions containing the compounds.

Inhibitors of squalene synthetase and protein farnesyltransferase

Antibacterial compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, selected preferred examples of which include those compounds wherein

Quinolizinone type compounds

Process for preparation of chiral cis-3,4-substituted pyrrolidine compounds having the formulas: ##STR1## and chiral 3,4-trans-substituted pyrrolidine compounds having the formulas: ##STR2## with the assistance of a streochemically directing chiral oxazolidinone moiety having the formula: ##STR3## wherein P, R and R.sup.1 are specifically defined, by sequential reaction of the compound or subsequent intermediates with an a,b-unsaturated add chloride, reaction with N-benzyl-N-(methoxymethyl)trimethyl-silylmethylamine and separating isomers by chromatography, hydrolytic removal of the oxazolidinone moiety, reaction with diphenylphosphoryl azide and triethylamine, and debenzylating; and novel intermediates of the process.

Process for synthesis of chiral cis-and trans-3-amino-4 substituted

The present invention provides a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, which are useful in inhibiting protein farnesyltransferase and the farnesylation of the oncogene protein Ras or inhibiting de novo squalene production resulting in the inhibition of cholesterol biosynthesis, processes for the preparation of the compounds of the invention in addition to intermediates useful in these processes, a pharmaceutical composition, and to methods of using such compounds.

Inhibitors of protein farnesyltransferase and squalene synthase

Process for preparation of chiral cis-3,4-substituted pyrrolidine compounds having the formulas ##STR1## and chiral 3,4-trans-substituted pyrrolidine compounds having the formulas ##STR2## with the assistance of a stereochemically directing chiral oxazolidinone moiety having the formula ##STR3## wherein P, R and R.sup.1 are specifically defined, by sequential reaction of the compound or subsequent intermediates with an a,b-unsaturated acid chloride, reaction with N-benzyl-N-(methoxymethyl)trimethylsilylmethylamine and separating isomers by chromatography, hydrolytic removal of the oxazolidinone moiety, reaction with diphenylphosphoryl azide and triethylamine, and debenzylating; and novel intermediates of the process.

Process for synthesis of chiral cis- and trans-3-amino-4-substituted

Antibacterial compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, preferred examples of which include those compounds wherein A is .dbd.CR.sup.6 --; R.sup.1 is cycloalkyl of from three to eight carbon atoms or substituted phenyl; R.sup.2 is selected from the group consisting of ##STR2## R.sup.3 is halogen; R.sup.4 is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group; R.sup.5 is hydrogen, loweralkyl, halo(loweralkyl), or --NR.sup.13 R.sup.14 ; and R.sup.6 is halogen, loweralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy, or amino(loweralkyl), as well as pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.

A renin inhibiting compound of the formula: ##STR1## wherein X is O, NH or S and G is a mimic of the Leu-Val cleavage site of angiotensinogen; or a pharmaceutically acceptable salt, ester or prodrug thereof; with the proviso that the compound is not N-(3-(4-Morpholino)propyl)-5(S)-(2(S)-(1(S)-(4-methoxymethoxy)piperidin-1- yl)carbonyl-2-phenyl)ethoxyhexanamido)-6-cyclohexyl-4(S)-hydroxy-2(S)-isopr opylhexanamide.

Renin inhibitors

The present invention relates to intermediates useful in a process for the preparation of a compound of the formula: ##STR1## wherein R.sub.2a is hydrogen or loweralkyl, R.sub.2b is hydrogen, loweralkyl, cycloalkyl or phenyl and R.sub.1 is cycloalkyl, cycloalkylalkyl, phenyl or benzyl. These intermediates are compounds of the formula: ##STR2## wherein P.sub.2 is an O-protecting group, P.sub.3 is an N-protecting group and R.sub.1, R.sub.2a and R.sub.2b are defined as above.

Substantially isomerically pure hexane or hexene compounds

Compounds are disclosed having the formula: ##STR1## wherein the substituents are defined herein. The compounds of the invention are angiotensin II receptor antagonists.

Angiotensin II receptor antagonists

The present invention relates to renin inhibiting compounds of the formula: ##STR1##

Non-peptide renin inhibitors

Compounds are disclosed having the formula: ##STR1## The compounds of the invention are angiotensin II receptor antagonists.

A renin inhibiting compound of the formula: ##STR1## wherein X is O NH or S and G is a mimic of the Leu-Val cleavage site of angiotensinogen; or a pharmaceutically acceptable salt, ester or prodrug thereof; with the proviso that the compound is not N-(3-(4-Morpholino)propyl)-5(S)-(2(S)-(1(S)-(4-(methoxymethoxy)piperidin-1 -yl)carbonyl-2- phenyl)ethoxyhexanamido)-6-cyclohexyl-4(S)-hydroxy-2(S)-isopropylhexanamid e.

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Gurnee, IL, United States of America

Anthony K Fung