Chimerix, Inc.

Other

Emory University

Gilead Sciences, Inc.

University of California

Burroughs Wellcome Co.

Triangle Pharmaceuticals, Inc.

Altus Pharmaceuticals Inc.

Althea Technologies, Inc.

Dennis C. Liotta

George R. Painter

Jose Soria

Merrick Almond

Marcos Sznaidman

Darryl Cleary

Merrick R Almond

George R Painter

Darryl G Cleary

Dennis C Liotta

Roy Wendell Ware

Bernhard Lampert

Ernest Randall Lanier, Jr

Jos&egrave; D Soria

Karl Y Hostetler

Janet L Rideout

James R Beadle

Timothy A Riley

Yao Yiming

Wang Yi Fong

Paula Francom

Jacqueline Ruiz

Amir Pesyan

Jeffrey D Wilson

George A Freeman

Yi Fong Wang

Ernest Randall Lanier

José D Soria

Darryl G Gleary

Steven A Short

Jon L Collins

Bernhard M Lampert

Marcos L Sznaidman

Yiming Yao

The present invention relates to compounds and methods for treating viral diseases. Some compounds of the invention are described by Formula I: 

Nucleoside phosphonate salts

The disclosure describes methods of synthesis of phosphonate ester derivatives. Preferred methods according to the disclosure allow for large-scale preparation of phosphonate ester compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of phosphonate ester derivatives without the use of chromatographic purification methods and in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of phosphonate ester derivatives.

Phosphonate ester derivatives and methods of synthesis thereof

The present invention relates to compounds and methods for treating viral diseases. Some compounds of the invention are described by Formula I: (I), wherein Mis Na, Li, K, Ca, Mg, or NRRRRand R, R, Rand Rare each independently hydrogen or Calkyl, or a stereoisomer, a diastereomer, an enantiomer or racemate thereof. 

The present invention provides methods of treating human immunodeficiency virus (HIV) and/or hepatitis B virus (HBV) infection, including administering a compound described in the invention in an amount effective treat the HIV and/or HBV infection and at least substantially inhibit the development of resistance to said antiviral compounds in the subject. Pharmaceutical compositions are also provided.

Methods of treating viral infections

The present application provides methods and compositions for combination therapy with antiviral compounds for the treatment of poxvirus infections, such as orthopox virus infections. In one embodiment, a method of treatment of a poxvirus infection is provided that comprises administering to a host in need thereof cidofovir, cyclic cidofovir, or a salt, ester, or prodrug thereof in combination or alternation with at least a second anti-poxvirus agent. The second anti-poxvirus agent is, for example, a biologic, such as a pegylated interferon.

Compounds, compositions and methods for the treatment of poxvirus infections

The present invention provides methods of treating viral infection of the eye or posterior ocular condition including administering a pharmaceutical composition comprising a compound described in the present application. In some embodiments, the pharmaceutical composition is topically administered. In another embodiment, the pharmaceutical composition is orally administered or intraocularly administered.

Compounds, compositions and methods for treating ocular conditions

This application provides a process for preparing enantiomerically pure &#x3b2;-D-dioxolane nucleosides. In particular, a new synthesis of (&#x2212;)-DAPD, suitable for large scale development, is described. In one embodiment the invention provides a process for preparing a substantially pure &#x3b2;-D- or &#x3b2;-L-1,3-dioxolane nucleosides comprising a) preparing or obtaining an esterified 2,2-dialkoxy ethanol; b) cyclizing the esterified 2,2-dialkoxy ethanol with glycolic acid to obtain a 1,3-dioxolane lactone; c) resolving the 1,3-dioxolane lactone to obtain a substantially pure D- or L-lactone; d) selectively reducing and activating the D- or L-chiral lactone to obtain a substantially pure D- or L-1,3-dioxolane; e) coupling the D- or L-1,3-dioxolane to an activated and/or protected purine or pyrimidine base; and f) optionally purifying the nucleoside to obtain a substantially pure protected &#x3b2;-D- or &#x3b2;-L-1,3-dioxolane nucleoside.

Methods to manufacture 1,3-dioxolane nucleosides

The present invention relates to phosphonate, nucleoside phosphonate or nucleoside phosphate compounds, compositions containing them, processes for obtaining them, and their use in treating a variety of medical disorders, in particular viral infections, cancers and the like.

Metabolically stable alkoxyalkyl esters of antiviral or antiproliferative phosphonates, nucleoside phosphonates and nucleoside phosphates

The present invention relates to a process for the biocatalyst-mediated enantioselective conversion of enantiomeric mixtures of hydrophobic esters using a biphasic solvent system. More particularly, the present invention relates to the enzyme-mediated enantioselective synthesis of anti-viral compounds, such as 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane (FTC) and its analogues, in a non-homogenous reaction system.

Non-homogeneous systems for the resolution of enantiomeric mixtures

The present invention relates to a process for the biocatalyst-mediated enantioselective conversion of enantiomeric mixtures of hydrophobic esters uing a biphasic solvent system. More particularly, the present invention relates to the enzyme-mediated enantioselective synthesis of anti-viral compounds, such as 2-hydroxymethyl-5-(5-flurocytosin-1-yl)-1,3-oxathiolane (FTC) and its analogues, in a non-homogenous reaction system.

Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include reacting a 5-O-protected-oxymethyl-1,3-oxathiolane with a silylated nucleoside in the presence of (Cl)Ti(isopropoxide). Using the processes described herein, the compounds can be provided as isolated enantiomers.

Process of manufacture of 1,3-oxathiolane nucleosides using titanium trichloride mono-isopropoxide

Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.

Method of manufacture of 1,3-oxathiolane nucleosides

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Apex, NC, United States of America

Merrick R Almond