Polium Technologies, Inc.

Mikhail Y Gololobov

Victor Ilyashenko

Hamilton J Lenox

Elena Terentieva

(R)-6F-phenylephrine, essentially free of (S)-6F-phenylephrine, and an anesthetic formulation comprising (R)-6F-epinephrin or (R)-6F-phenylephrine and having improved stability compared to formulations containing their non-fluorinated analog, are disclosed. Further disclosed is a method of providing vasoconstriction in a mammal by administering the anesthetic formulation. The anesthetic composition can include an anesthetic, an (R)-chiral compound having the structure:wherein R, R, and Rare independently selected from &#x2014;H or &#x2014;F, at least one of R, R, and Ris &#x2014;F, and Ris selected from &#x2014;OH, &#x2014;H or &#x2014;F, or a pharmaceutically acceptable salt or ester thereof, said vasoconstrictor being essentially free of the (S)-chiral form. Also, a method of chiral addition of cyanide to a ring-fluorinated phenaldehyde, employing an almond hydroxynitrile lyase enzyme, provided in the form of a reversibly soluble polymer conjugate ((R)-Finezyme&#x2122;-H series biocatalysts) is disclosed. Several such biocatalysts are disclosed.

Optically active fluorinated vasoconstrictors, methods for making them, and anesthetic formulations comprising them

The present invention is directed to a method for producing reversibly soluble, catalytically active enzyme-polymer conjugates and the products thereof. In particular, the invention is directed to reversibly soluble catalytically active enzyme-polymer conjugates made by incorporating enzymes modified to contain free vinyl double bonds into reversibly soluble polymers i.e., polymers that reversibly respond to slight changes in the environment, such as temperature, ionic strength, pH, electric fields, etc., during the polymerization reaction. Thus, when modified enzymes are incorporated into reversibly soluble polymers, the biocatalysts obtained can be precipitated without destroying the delicate enzyme(s). Moreover, these biocatalysts can be solubilized again and reused at the initial environmental conditions.

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Hoffman Estates, IL, United States of America

Mikhail Y Gololobov