Trimeris, Inc.

Glaxo Group Limited

Glaxo Inc.

Other

Glaxo Wellcome Inc.

Brian L Bray

John Joseph Partridge

Myung-Chol Kang

Paul Erickson Friedrich

Huyi Zhang

Marc W Andersen

Stephen E Schneider

Maynard Emanuel Lichty

John P Turnbull

Nicolai A Tvermoes

Barbara E Johnston

Maynard Lichty

John Dwyer

Catherine Mader

Gene Merutka

John William Lackey

Daniel S Kinder

David Heilman

Jie Di

Nikolai A Tvermores

Paul E Friedrich

Provided is an HIV fusion inhibitor peptide having an amino acid sequence of any one of SEQ ID NO:9, SEQ ID NO:10, SEQ ID NO:11, SEQ ID NO:12, SEQ ID NO:13, SEQ ID NO:14, or SEQ ID NO:15; and provided is a pharmaceutical composition comprising a HIV fusion inhibitor peptide and one or more of a pharmaceutically acceptable carrier and macromolecular carrier, and uses and methods of treatment provided by these compositions.

HIV fusion inhibitor peptides with improved biological properties

Provided are conjugates comprising a polymer having operably bound thereto no less than two molecules of synthetic peptide derived from HIV gp41; methods of using these conjugates to inhibit transmission of HIV to a target cell by adding an amount of effective to inhibit infection of the cell by the virus; and methods of producing the conjugates by operably binding each molecule of synthetic peptide, via a reactive functionality, to the polymer.

Antiviral peptide-polymer conjugate comprising a polymer covalently attached to two or more synthetic HIV gp41 HR1 and/or HR2 peptides

Provided is a pharmaceutical composition comprising a solution comprised of synthetic peptide in a final concentration of not less than 70 mg/ml in admixture with a polyol; wherein the synthetic peptide is an HIV fusion inhibitor, and wherein the polyol is in a final concentration of no less than 5 weight % and no more than 75 weight % of the pharmaceutical composition. Also provided is a synthetic peptide-containing pharmaceutical composition as a unit dose comprising an aqueous formulation comprised of synthetic peptide in a final concentration of not less than 70 mg/ml in admixture with a polyol; wherein the synthetic peptide is an HIV fusion inhibitor, and wherein the polyol is in a final concentration of no less than 5 weight % and no more than 75 weight % of the pharmaceutical composition. Further provided is a method of treating HIV infection by administering to an HIV-infected individual a pharmaceutical composition according to the present invention.

Pharmaceutical composition for improved administration of HIV gp41-derived peptides, and its use in therapy

The present invention relates, first, to methods for the synthesis of peptides referred to as T-1249 and T-1249-like peptides. Such methods utilize solid and liquid phase synthesis procedures to synthesize and combine groups of specific peptide fragments to yield the peptide of interest. The present invention further relates to individual peptide fragments which act as intermediates in the synthesis of the peptides on interest (e.g., T-1249). The present invention still further relates to groups of such peptide intermediate fragments which can be utilized together to produce full-length T-1249 and T-1249-like peptides.

Methods and compositions for peptide synthesis

Methods and composition for peptide synthesis

The present invention relates, first, to methods for the synthesis of peptides, in particular T-20 (also referred to as &ldquo;DP-178&rdquo;; SEQ ID NO:1) and T-20-like peptides. Such methods utilize solid and liquid phase synthesis procedures to synthesize and combine groups of specific peptide fragments to yield the peptide of interest. The present invention further relates to individual peptide fragments which act as intermediates in the synthesis of the peptides of interest (e.g., T-20). The present invention still further relates to groups of such peptide intermediate fragments which can be utilized together to produce full length T-20 and T-20-like peptides.

The present invention relates, first, to methods for the synthesis of peptides, in particular T-20 (also referred to as 'DP-178'; SEQ ID NO:1) and T-20-like peptides. Such methods utilize solid and liquid phase synthesis procedures to synthesize and combine groups of specific peptide fragments to yield the peptide of interest. The present invention further relates to individual peptide fragments which act as intermediates in the synthesis of the peptides of interest (e.g., T-20). The present invention still further relates to groups of such peptide intermediate fragments which can be utilized together to produce full length T-20 and T-20-like peptides.

The compound 1,8-diazabicyclo[5.4.0]undec-1(7)-enium cyanide is the reaction product of acetone cyanohydrin and 1,8-diazabicyclo [5.4.0]undec-7-ene.

1,8-diazabicyclo[5.4.0]undec-1(7)-enium cyanide and method of making

A process for removing osmium from an aqueous solution of nucleosides comprising adding hydrogen sulfide, an aromatic pi base such as pyridine, and a mineral acid. The osmium is precipitated out of solution.

Method for removing osmium from nucleosides

Synthesis of the triol of the following formula (I) from an alcohol of the formula (IV): ##STR1## via steps including protecting and then cyanating the alcohol to yield a cyanide, isomerization of the double bond, hydrolysis followed by reduction of the cyanide back to an alcohol and cis-dihydroxylation of the double bond.

Synthesis of a 3,4-dihydroxy-1-cyclopentanylpurinone

Synthesis of the triol of formula (I) or its amine-protected derivative from a cyclopentene of the formula (II) or its amine-protected derivative: ##STR1## via steps including oxidation to the aldehyde, migration of the double bond, reduction of the aldehyde moiety back to the alcohol grouping and 1,2-cis-dihydroxylation of the double bond.

Synthesis of a 3,4-dihydroxy-1-cyclopentanylpurinone from a

A kinetic resolution of pyridazinones of the following formula (A): ##STR1## where R.sup.1 is alkyl by enzymatic hydrolysis results in good optical purity of the phenolic product. This is significant considering the distance in the molecule (A) from the C-5 chiral center to the site of hydrolysis.

Growing community of inventors

Graham, NC, United States of America

Brian L Bray