Eschem Inc.

Unitech Chemical Inc.

Achillion Pharmaceuticals, Inc.

Advanced Life Sciences, Inc.

Ralph M Schure

John H Kooi

John M Brown

Gerald H Steele

Michael T Flavin

David E Zembower

Yuh-Meei Lin

Zhao Lei

Lisa Dunkle

Bo Kowalczyk

Geng-Xian Zhao

The invention provides a method of synthesizing &#x3b2;-L-5-fluoro-2',3&#x2032;-dideoxy-2&#x2032;,3&#x2032;-didehydrocytidine (&#x3b2;-L-FD4C). The method allows for large-scale production of &#x3b2;-L-FD4C in an efficient, cost-effective, and environmentally sound manner.

Method for synthesizing &#x3b2;-L-5-fluoro-2',3&#x2032;-dideoxy-2&#x2032;,3&#x2032;-didehydrocytidine (&#x3b2;-L-FD4C)

Substantially purified antiviral biflavanoids robustaflavone, hinokiflavone, amentoflavone, agathisflavone, volkensiflavone, morelloflavone, rhusflavanone, succedaneaflavanone, GB-1a, and GB-2a are provided. Antiviral biflavanoid derivatives and salt forms thereof, e.g., robustaflavone tetrasulfate potassium salt, and methods for preparing the same are also disclosed. Pharmaceutical compositions which include the antiviral biflavanoids, derivatives or salts thereof are also provided alone or in combination with at least one antiviral agent such as 3TC. Also disclosed is an improved method for obtaining substantially pure robustaflavone from plant material. The biflavanoid compounds, derivatives or salts thereof of the invention may be used in a method for treating and/or preventing viral infections caused by viral agents such as influenza, e.g., influenza A and B; hepatitis, e.g., hepatitis B; human immunodeficiency virus, e.g., HIV-1; Herpes viruses (HSV-1 and HSV-2); Varicella Zoster virus (VZV); and measles. For instance, semi-synthetic hexa-O-acetate and hexa-O-methyl ether derivatives of robustaflavone have been found to be effective in a method for treating or preventing hepatitis B viral infections. Compositions which include these robustaflavone derivatives along with methods for preparing and using the same are also provided. These compositions may be used alone or in combination with at least one antiviral agent such as 3TC.

Biflavanoids and derivatives thereof as antiviral agents

Adhesives and coatings, especially two-compartment epoxy laminating adhesives, are prepared so as to be flame-resistant in the so-called part B or polyamide component thereof by including in that compartment a chlorinated hydrocarbon solvent together with an adduct of a polyamide and an aromatic hydroxy or epoxy compound. By this approach, the amine is tied up and is rendered resistant to premature reaction with the chlorinated hydrocarbon solvent within the part B component, which premature reaction would lead to the formation of undesirable crystals within the part B component and reduce its pot life. When the part B component is blended with an epoxy-containing art B component, the polyamine adduct gradually disassociates in order to free the polyamine to catalyze setting of the two-component system, particularly the epoxy resin of the part A component.

Stabilization of epoxy systems in non-flammable solvents

Adhesives and coatings, especially two-component epoxy laminating adhesives, are prepared so as to be flame-resistant in the so-called part B or polyamide component thereof by including in that component a chlorinated hydrocarbon solvent together with an adduct of a polyamide and an aromatic hydroxy or epoxy compound. By this approach, the amine is tied up and is rendered resistant to premature reaction with the chlorinated hydrocarbon solvent within the part B component, which premature reaction would lead to the formation of undesirable crystals within the part B component and reduce its pot life. When the part B component is blended with an epoxy-containing part B component, the polyamine adduct gradually disassociates in order to free the polyamine to catalyze setting of the two-component system, particularly the epoxy resin of the part A component.

Blends of certain block copolymers and epoxy resins, which have superior thermoplastic adhesive properties are disclosed. The blends are prepared by mixing hydroxy-terminated poly(ester/ether) block copolymers with epoxy resins. These unreacted blends are useful as hot melt thermoplastic adhesives having very high peel strength, high tensile shear strength, creep resistance at elevated temperatures, and good viscosity stability.

Hot melt adhesive having both high peel and tensile shear strength

A polymeric compound having superior thermoplastic adhesive properties is disclosed. The compound is a poly(ester/ether) block copolymer which is extended with an anhydride to introduce carboxyl groups thereinto. Also disclosed are thermoset adhesives having superior properties and which are such carboxylated copolymers that have been crosslinked with a suitable resin.

Growing community of inventors

Darien, IL, United States of America

Ralph M Schure