American Cyanamid Company

Biosource Pharm, Inc.

Micrologix Biotech Inc.

Cubist Pharmaceuticals, Incorporated

Biowest Therapeutics Inc.

William V Curran

Richard A Leese

Donald B Borders

Carl B Ziegler

Gregg Brian Feigelson

Adma S Ross

Ving J Lee

Howard Jarolmen

Andrew S Tomcufcik

Blaise S Lippa

Amedeo A Fantini

You Seok Hwang

Christopher Matthew Liu

Yanzhi Zhang

Noreen D Francis

Amy C D Bombardier

Ransom B Conrow

Dale R Cameron

Qi Jia

Robert Herman Lenhard

David Michael Blum

Martin L Sassiver

Matthew B Nodwell

James H Boothe

Yuchen Chen

Robert E Babine

Vincent A Boyd

Noreen Francis

Raghavan Krishnan

Dominique Dugourd

Jesse Gamble

Paulo W M Sgarbi

Shirley A Wacowich-Sgarbi

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.

Antibiotic compositions for the treatment of gram negative infections

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

This method is for preparing salts of amphotericin B methyl ester and other polyene macrolide esters. The steps of the process involve methylation by use of cesium carbonate for converting to methyl ester and significantly reducing side products, which are over methylation products. The free base-Schiff base mixture is converted to amphotericin B methyl ester hydrochloride or some other salt form, by using tetrahydrofuran-water to dissolve the mixture for acid treatment to obtain the salt. The aldehyde liberated during salt formation is removed by centrifuging, as to any precipitated aldehyde, and the aldehyde remaining in solution is removed by eluting the solution through a reverse phase adsorbent to obtain amphotericin B methyl ester hydrochloride as a yellow powder.

Method for preparing salts of polyene macrolide esters

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.

New 4-substituted azetidinones having the formulae I and II: ##STR1## wherein X is oxygen, sulfur or a moiety of the formula NR.sup.6 where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are defined hereafter, which are intermediates for the preparation of carbapenem and carbacephem antibacterials and processes for producing such antibacterials through the utilization of an acid mediated ring closure reaction.

4-substituted azetidinones as precursors to 2-substituted-3-carboxy

Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.4, R.sup.5, R.sup.12, R.sup.16 and R.sup.17 are defined in the specification are provided. These compounds are useful as intermediates for the preparation of carbapenem antibacterials.

The invention provides substituted allylazetidinone compounds having the formula: ##STR1## and propargyl azetidinone compounds having the formula: ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.30, X, Y and Q are defined in the specification.

2-substituted alkyl-3-carboxy carbapenems as antibiotics and a method of

The invention relates to new 2-substituted alkyl-3-carboxy carbapenems having the formula: ##STR1## with R.sup.1, R.sup.2, R.sup.3, X and Y defined hereafter as antibiotics and beta lactamase inhibitors produced by a novel Michael addition-elimination reaction of a substituted allyl azetidinone in the reaction shown: ##STR2## with R.sup.1, R.sup.2, Q, X and Y defined hereafter.

2-substituted alkyl-3-carboxy carbopenems as antibiotics and a method of

New 4-substituted azetidinones having the formulea I and II: ##STR1## with R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and X defined hereafter, which are intermediates for the preparation of carbapenem and carbacephem antibacterials and processes for producing such antibacterials through the utilization of an acid mediated ring closure reaction.

Growing community of inventors

Pearl River, NY, United States of America

William V Curran