Novartis Ag

Entasis Therapeutics, Inc.

Pharmacia & Upjohn Company

Other

Novartis Pharma Gmbh

Ruben Alberto Tommasi

Leslie Wighton McQuire

Michael David Shultz

Olivier Rogel

Paul A Aristoff

Harvey I Skulnick

Suvit Thaisrivongs

Claus Ehrhardt

Pascal Rigollier

Thomas Francois Durand-Reville

Gordon L Bundy

Jeroen Cunera Verheijen

John Henry Van Duzer

Joseph Walter Strohbach

Ronald B Gammill

David John Anderson

Ayako Honda

Paul D Johnson

Steven Ronald Turner

Sven Weiler

Joel Morris

Louis L Skaletzky

Karen Rene Romines

Xiaoyun Wu

W Jeffrey Howe

Janelle Comita-Prevoir

Linda Louise Maggiora

Jonathan E Grob

Paul David Greenspan

Robert Alan Chrusciel

Eva Altmann

Claudia Betschart

Frank Wu

Junichi Sakaki

Rene Lattmann

Martin Missbach

Leo Widler

Naoki Teno

Satenig Guler

Erin Keaney

Leslie Ann Robinson

Clark W Smith

Thomas Leutert

Jan Romero

Theresa M Schwartz

John Mueller

George P Luke

Boudewijn Lodewijk Maria DeJonge

James M Tustin

Scott Douglas Cowen

Jing Zhang

Robert A Chruscial

Mark Sylvester

Keigo Gohda

Miyuki Horiuchi

Michihiro Takai

Erin E Pusateri

René Beerli

Lise Gauthier

John O'Donnell

Camilo Velez-Vega

Philippe Nantermet

Jerry W Skiles

Roger Aki Fujimoto

Leslie Wighton Mcquire

Boudewijn Lodewijk Maria Dejonge

Bill Moss

Gregory S Basarab

Boudewijn Lodewijk Dejonge

Provided herein are antibacterial compounds represented by Formula I, or a pharmaceutically acceptable salt thereof, wherein X, Y, R, R, and Rare as defined herein. Also provided are pharmaceutical compositions comprising the compounds of Formula I. 

Compounds and methods for treating bacterial infections

The present invention is directed to compounds which are beta-lactamase inhibitors. The compounds and their pharmaceutically acceptable salts are useful in combination with beta-lactam antibiotics, for the treatment of bacterial infections, including infections caused by drug resistant organisms, including multi-drug resistant organisms. The present invention includes compounds according to Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of R, R, R, R, Rand Rare described herein. 

Beta-lactamase inhibitor compounds

The present invention is directed to combinations of a &#x3b2;-lactamase inhibitor with sulbactam and, optionally, imipenem/cilastatin. The combinations are useful for the treatment of bacterial infections, including infections caused by drug resistant organisms, including multi-drug resistant pathogens. More particularly, the invention relates to a combination of &#x3b2;-lactamase inhibitor compound 1: or a pharmaceutically acceptable salt thereof, with sulbactam, or a pharmaceutically acceptable salt thereof, and, optionally, imipenem/cilastatin, or a pharmaceutically acceptable salt thereof. 

Combination therapy for treatment of resistant bacterial infections

The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.

ArylSulfonamide-based matrix metalloprotease inhibitors

Arylsulfonamide based matrix metalloprotease inhibitors

The present invention provides a compound of formula (I): said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).

Selective hydroxamic acid based MMP-12 and MMP-13 inhibitors

Use of compound of formula (I), wherein, is, or, and wherein the symbols are as defined, or a pharmaceutically-acceptable and -cleavable ester, or acid addition salt thereof, for the preparation of a medicament for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable. 

Quinazoline derivatives which promote the release of parathyroid hormone

The present invention provides a compound of formula (I): said compound is inhibitor of MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-9, and/or MMP-12 and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition. 

Selective hydroxamate based MMP inhibitors

The present invention provides a compound of formula (I): said compound is inhibitor of MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-9, and/or MMP-12 and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.

Arylsulfonamide-based matrix metalloprotease inhibitors

Compounds of the formula (I), wherein R is aryl or biaryl; R is aryl-lower alkyl, biaryl-lower alkyl, benzo-fused cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, aryloxy-lower alkyl, or aryl-C -C -alkyl in which C -C -alkyl is interrupted by Y; Y is O, S, SO, SO , CO or NR ; R is hydrogen or lower alkyl; or R and R combined are C -C -alkylene or C -C -alkylene interrupted by Y; R is hydrogen or lower alkyl; R is hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, biaryl-lower alkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, aryloxy-lower alkyl, or aryl-C -C -alkyl in which C -C -alkyl is interrupted by Y; R is hydrogen, lower alkyl or aryl-lower alkyl; and pharmaceutically acceptable salts thereof, which are useful as cysteine cathepsin inhibitors

N-substituted peptidyl nitriles as cysteine cathepsin inhibitors

Dipeptide nitriles

This invention refers to a microsplitter in flow systems especially used for separation techniques in analytical chemistry such as microliquid chromatography (MLC), high pressure liquid chromatography (HPLC) and ancillary techniques. The splitter system comprises a microsplitter and a micromixer which are connected by a microbore tubing. A high collection rate and high resolution of the sample peak are achieved by the proper choice of tubing length and diameters and the use of a back pressure regulator to obtain a controlled split ratio.

Microflow splitter

Growing community of inventors

Whitehouse Station, NJ, United States of America

Ruben Alberto Tommasi