National Institutes of Health, a Component of the US Dept. of Health & Human Services

The United States of America As Represented by the Department of Health

The United States of America As Represented by the Secretary of

USA As Represented by Secretary of the Navy

University of Illinois

The Trustees of Boston College

Nektar Therapeutics Al, Corporation

The United States of America As Represented by the Secretary, Department

Other

Brigham Young University

National Institute of Heatlh

Nektar Therapeutics

Michael R Boyd

Kirk R Gustafson

James Brislin McMahon

Gerhard Bringmann

John H Cardellina, Ii

Gordon M Cragg

Barry R O'Keefe

Robert H Shoemaker

Lewis K Pannell

Richard W Fuller

Charles L Cantrell

Yoel Kashman

Laurent A Decosterd

Michael James Roberts

Toshiyuki Mori

Kirk P Manfredi

Doel Soejarto

John A Beutler

John W Blunt

T Ross Kelly

Roland Gotz

Duncan Thomas

Johnson Jato

Guido Francois

Roland G Otz

J David Phillipson

Sven Harmsen

Ian Parsons

Robert J Gulakowski

Christoph Schneider

Georges Timperman

M Elizabeth Snell

Matthias Wenzel

Tawnya C McKee

Peter M Blumberg

Paul Alan Cox

Jon C Clardy

Heidi R Bokesch

Karen L Erickson

Angela M Gronenborn

Kenneth M Snader

Yaii F Hallock

Guido Fran&ccedil;ois

Junichi Ishitoya

Laurent Ak&eacute; Assi

Nancy A Sharkey

Krik R Gustafson

Owen S Weislow

Ian Parson

Laurent Ake Assi

John H Cardelina, Ii

Deborah Galinis

Barry R O'keefe

Tawnya C Mckee

The present invention provides a compound of the formula (I) or (II), wherein Ris H, alkyl, alkenyl or aryl, Ris H, alkyl or aryl, Ris H, a alkyl, alkenyl or aryl, Rand R-Rare independently R, C(O)Ror SOR, wherein Ris H, alkyl, alkenyl or aryl, and Ris R, C(O)Ror SOR, wherein Ris H, alkyl, alkenyl or aryl. Rcan be unsubstituted or substituted with one or more oxo(&#x2550;O), OR, OC(O)R, OSOR, NHR, NHC(O)Rand NHSORgroups. Ris H, alkyl, alkenyl, or aryl. Rcan be unsubstituted or substituted with one or more groups such as oxo(&#x2550;O), OR, COR, CORand OC(O)R. Ris H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent. The present invention further provides a method of treating a condition treatable by the inhibition of vacuolar-type (H+)-ATPase and a method of treating cancer. 

Biologically active macrolides, compositions, and uses thereof

The present invention provides a compound of the formula (I) or (II, wherein Ris H, alkyl, alkenyl or aryl, Ris H, alkyl or aryl, Ris H, a alkyl, alkenyl or aryl, Rand R-Rare independently R, C(O)Ror SOR, wherein Ris H, alkyl, alkenyl or aryl, and Ris R, C(O)Ror SOR, wherein Ris H, alkyl, alkenyl or aryl. Rcan be unsubstituted or substituted with one or more oxo(&#x2550;O), OR, OC(O)R, OSOR, NHR, NHC(O)Rand NHSORgroups. Ris H, alkyl, alkenyl, or aryl. Rcan be unsubstituted or substituted with one or more groups such as oxo(&#x2550;O), OR, COR, CORand OC(O)R. Ris H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent. The present invention further provides a method of treating a condition treatable by the inhibition of vacuolar-type (H+)-ATPase and a method of treating cancer. 

A composition comprising a substantially purified compound of the formula: in combination with at least one additional therapeutic agent, and methods of preventing or treating cancer and a condition treatable by the inhibition of vacuolar-type (H+)-ATPase.

Chondropsin-class antitumor V-ATPase inhibitor compounds, compositions and methods of use thereof

An isolated and purified nucleic acid molecule that encodes a polypeptide comprising at least eight contiguous amino acids of SEQ ID NO: 3, wherein the at least eight contiguous amino acids have anti-viral activity, as well as an isolated and purified nucleic acid molecule that encodes a polypeptide comprising at least eight contiguous amino acids of SEQ ID NO: 3, wherein the at least eight contiguous amino acids have anti-viral activity, and, when the at least eight contiguous amino acids comprise amino acids 1-121 of SEQ ID NO: 3, the at least eight contiguous amino acids have been rendered glycosylation-resistant, a vector comprising such an isolated and purified nucleic acid molecule, a host cell comprising the nucleic acid molecule, optionally in the form of a vector, a method of producing an anti-viral polypeptide or conjugate thereof, the anti-viral polypeptide itself, a conjugate or fusion protein comprising the anti-viral polypeptide, and compositions comprising an effective amount of the anti-viral polypeptide or conjugate or fusion protein thereof. Further provided are methods of inhibiting prophylactically or therapeutically a viral infection of a host.

Griffithsin, glycosylation-resistant griffithsin, and related conjugates, compositions, nucleic acids, vectors, host cells, methods of production and methods of use

Chondropsin-class antitumor V-atpase inhibitor compounds, compositions and methods of use thereof

The present invention provides a compound of formula (II). The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent. The present invention further provides a method of treating a condition treatable by the inhibition of vacuolar-type (H+)-ATPase and a method of treating cancer.

The present invention provides methods of treating a viral infection of a host using antiviral proteins (collectively referred to as cyanovirins).

Methods of using cyanovirins to inhibit viral infection

The present invention provides variants of cyanovirin-N and water-soluble polymer conjugates thereof, and methods of preparing such conjugates. The cyanovirin-N of the invention are particularly suited for site-selective covalent attachment of one or more water soluble polymers, to provide polymer conjugates of cyanovirin-N variants exhibiting antiviral activity.

Cyanovirin variant-polymer conjugates

An isolated or purified antiviral protein of SEQ ID NO: 1, nucleic acids encoding the antiviral protein, cells comprising the nucleic acids, and methods of inhibiting viral infection comprising contacting the virus with the antiviral protein.

Scytovirins and related conjugates, fusion proteins, nucleic acids, vectors, host cells, compositions, antibodies and methods of using scytovirins

The present invention provides vacuolar-type (H+)-ATPase-inhibiting compounds, compositions thereof, and methods of using them to treat or prevent a condition treatable by the inhibition of a vacuolar-type (H+)-ATPase. The composition of the present invention comprises a compound of the present invention and a carrier. The method of the present invention includes administering a vacuolar-type (H+)-ATPase inhibiting-effective amount of a compound of the present invention. The compound of the present invention has formula (I) wherein Rand Rare H, saturated or unsaturated alkyl, aryl, RCH&#x2014;, RCO&#x2014;, or RSO&#x2014;, wherein Ris H, saturated or unsaturated alkyl, or aryl; Ris H, alkyl, aryl, an oxime, or an oxime methyl ether; the aromatic ring is unsubstituted or substituted; and Z is a contiguous linker comprising a chain of 0-10 atoms which, together with the five atoms beginning with the carbon of the aromatic ring in meta-relationship with ORand ending with the carbon directly attached to the alkyl oxygen of the lactone, integrally form a 5-17 membered ring; or a pharmaceutically acceptable salt, an ester, or a prodrug thereof.

Method of treating osteoporosis comprising vacuolar-type (H+)-ATPase-inhibiting compounds

The invention provides a method of inhibiting prophylactically or therapeutically an influenza viral infection in a host. The method comprises instilling into or onto a host a cell producing an antiviral protein, antiviral peptide, or antiviral conjugate comprising at least nine contiguous amino acids of SEQ ID NO: 2, wherein the at least nine contiguous amino acids are nonglycosylated and have antiviral activity, whereupon the influenza viral infection is inhibited.

Glycosylation-resistant cyanovirins and related conjugates, compositions, nucleic acids, vectors, host cells, methods of production and methods of using nonglycosylated cyanovirins

The present invention provides variants of cyanovirin-N and water-soluble polymer conjugates thereof. The cyanovirin-N of the invention are particularly suited for site-selective covalent attachment of one or more water soluble polymers, to provide polymer conjugates of cyanovirin-N variants exhibiting antiviral activity.

Growing community of inventors

Ijamsville, MD, United States of America

Michael R Boyd