Biosource Pharm, Inc.

Micrologix Biotech Inc.

American Cyanamid Company

Cubist Pharmaceuticals, Incorporated

Biowest Therapeutics Inc.

Richard A Leese

William V Curran

Donald B Borders

Howard Jarolmen

Blaise S Lippa

Amedeo A Fantini

You Seok Hwang

Christopher Matthew Liu

Yanzhi Zhang

Noreen D Francis

Amy C D Bombardier

Dale R Cameron

Qi Jia

Bart J Zoltan

Lalitha Krishnan

Matthew B Nodwell

Yuchen Chen

Vincent A Boyd

Raghavan Krishnan

Noreen Francis

Shirley A Wacowich-Sgarbi

Dominique Dugourd

Paulo W M Sgarbi

Provided herein is an antibacterial compound of the following formula: or a pharmaceutically acceptable salt thereof. The antibacterial compound has antibacterial properties against a diverse range of gram negative bacteria and reduced toxicity compared to polymyxins such as polymyxin B. Also provided are antibacterial pharmaceutical compositions containing the antibacterial compound, as well as methods for preparing the antibacterial compound.

Antibiotic compositions for the treatment of gram negative infections

Provided herein are novel compounds and novel protected compounds that can be derived from polymyxin, including, e.g., polymyxin A. The novel compounds have antibacterial properties against a diverse range of Gram negative bacteria and reduced toxicity compared to polymyxins such as polymyxin A. Also provided are antibacterial pharmaceutical compositions containing the novel compounds and novel protected compounds, as well as methods for preparing the antibacterial compounds and protected compounds.

Disclosed herein are novel peptides and protected peptides. These compounds can be derived from naturally occurring peptides, such as those selected from colistin, circulin A, polymyxin A, polymyxin B, polymyxin D, octapeptin B, octapeptin C, and [Ile]polymyxin B. Also disclosed are pharmaceutical compositions containing the new peptides, as well as methods for preparing the novel peptides and protected peptides.

Peptide antibiotics and methods for making same

The present invention provides derivatives of lipopeptide antibiotics that display antimicrobial activity against microorganisms, methods and compounds for synthesizing such antimicrobial derivatives and analogues, and methods of using the compounds in a variety of contexts, including in the treatment and prevention of microbial infections.

Compositions of lipopeptide antibiotic derivatives and methods of use thereof

Novel cyclodepsipeptide intermediates have been prepared from the A21978 complex and used to synthesize new lipodepsipeptide antibiotics. The three intermediates can be readily derivatized to give new families of antibiotics that have potent antibacterial activity against gram positive bacteria.

Lipodepsipeptide antibiotics and methods of preparation

The present invention provides antimicrobial sulfonamide derivatives of lipopeptide antibiotics, pharmaceutical compositions of antimicrobial sulfonamide derivatives, methods for making antimicrobial sulfonamide derivatives, methods for inhibiting microbial growth with antimicrobial sulfonamide derivatives and methods for treating or preventing microbial infections in a subject with antimicrobial sulfonamide derivatives. Antimicrobial sulfonamide derivatives are generally an amino core antibiotic that has been further modified with a lipophilic sulfonyl group.

Antimicrobial sulfonamide derivatives of lipopeptide antibiotics

The present invention provides laspartomycin core peptides, laspartomycin core peptide derivatives, antimicrobial laspartomycin derivatives, methods for making laspartomycin core peptides, methods for making laspartomycin core peptide derivatives, methods for making antimicrobial laspartomycin derivatives, pharmaceutical compositions of antimicrobial laspartomycin derivatives, methods of inhibiting microbial growth and methods for treating and/or preventing microbial infections in a subject.

Derivatives of laspartomycin and preparation and use thereof

The present invention provides a laspartomycin core peptide, a laspartomycin core peptide derivative, a antimicrobial laspartomycin derivative, a method for making laspartomycin core peptides, methods for making laspartomycin core peptide derivatives, methods for making antimicrobial laspartomycin derivatives, pharmaceutical compositions of antimicrobial laspartomycin derivatives, methods of inhibiting microbial growth and methods for treating and/or preventing microbial infections in a subject.

The invention provides a method for selectively extracting a compound of formula I: ##STR1## wherein: R is hydrogen or --NR.sub.3 R.sub.4 ; and when R=--NR.sub.3 R.sub.4, R.sub.3 and R.sub.4 may be the same or different and are selected from hydrogen and straight or branched (C.sub.1 -C.sub.4)alkyl; R.sub.1 and R.sub.2 may be the same or different and are selected from straight or branched (C.sub.1 -C.sub.6)alkyl; from an aqueous mixture containing a compound of Formula I, its C-4 epimer and its oxidative degradation by-products by adding methylene at a concentration of 2-4 ml of methylene chloride per gram of compound of Formula I and at a pH between pH 6.5-8.0; and obtaining an extract containing methylene chloride, a compound of Formula I, and its C-4 epimer, said epimer being present in an amount of less than 3% of the amount of the compound of Formula I.

Method for selective extracting a 7-(hydrogen or substituted

A Peltier effect thermal control sample containment means for an automatic sample holding apparatus used in conjunction with a liquid chromatograph analysis. The apparatus provides for the cooling or heating of a plurality of liquid chromatography samples and the maintenance of said samples at specific temperatures for extended periods of time.

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Suffern, NY, United States of America

Richard A Leese