Claims
- 1. (R)-6F-phenylephrine, essentially free of (S)-6F-phenylephrine.
- 2. An anesthetic formulation comprising (R)-6F-epinephrin or (R)-6F-phenylephrine and having improved stability compared to formulations containing their non-fluorinated analogs.
- 3. A method of providing vasoconstriction in a mammal, comprising the step of administering to said mammal an amount of (R)-6F-epinephrin or (R)-6F-phenylephrine effective to provide vasoconstricting activity.
- 4. A composition comprising:
an amount of an anesthetic effective to provide local anesthetic activity; an amount of an (R)-chiral compound having the structure: 34wherein r1, r2, and r4 are independently selected from −H or −F, at least one of r1, r2, and r4 is −F, and R3 is selected from −OH, −H or −F, or a pharmaceutically acceptable salt or ester thereof, said vasoconstrictor being essentially free of the (S)-chiral form, effective to provide vasoconstrictive activity.
- 5. A local anesthetic composition comprising:
from 0.1% to 20% by weight of an anesthetic agent; from 0.0001% to 0.01% of a vasoconstrictor comprising an (R)-chiral compound having the structure: 35wherein R1, R2, and R4 are independently selected from —H or —F, at least one of R1, R2, and R4 is —F, and R3 is selected from —OH, —H or —F, or a pharmaceutically acceptable salt or ester thereof, said vasoconstrictor being essentially free of the (S)-chiral form, and as the balance, adjuvants and an excipient in a predominant quantity.
- 6. The local anesthetic composition of claim 4, wherein said anesthetic agent is lidocaine hydrochloride.
- 7. The local anesthetic composition of claim 4, wherein said vasoconstrictor comprises (R)-6F-phenylephrin.
- 8. The local anesthetic composition of claim 4, wherein said vasoconstrictor comprises (R)-6F-epinephrin.
- 9. A method of chiral addition of cyanide to a ring-fluorinated phenaldehyde, comprising the steps of:
Providing a ring-fluorinated phenaldehyde; and Reacting said ring-fluorinated phenaldehyde with a source of cyanide in the presence of a catalytic amount of an almond hydroxynitrile lyase enzyme, provided in the form of a reversibly soluble polymer conjugate ((R)-Finezyme™-H series biocatalysts).
- 10. A method of chiral addition of cyanide to a ring-fluorinated phenaldehyde, comprising the steps of:
Providing a ring-fluorinated phenaldehyde; and Reacting said ring-fluorinated phenaldehyde with a source of cyanide in the presence of a catalytic amount of free hydroxynitrile lyase enzyme.
- 11. The method of claim 9, comprising the subsequent steps of separating said ring-fluorinated cyanohydrin and said almond hydroxynitrillyase enzyme, and recovering at least a substantial portion of said almond hydroxynitrillyase enzyme in a form suitable for re-use in said reaction.
- 12. PaHNL-poly-N-isopropylacrylamide (Finezyme™-H1).
- 13. PaHNL-poly(N-isopropylacrylamide-co-N-tert-butylacrylamide) (Finezyme™-H2).
- 14. PaHNL-Eudragit L-100 (Finezyme™-H3).
- 15. PaHNL-Eudragit S-100 (Finezyme™-H4).
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] Priority is claimed from provisional application Attorney Docket No. 13738US01, filed Jun. 19, 2002, by Hamilton J. Lenox, Elena Terentieva and Mikhail Y. Gololobov, now pending. The entire specification and all the claims of the provisional application referred to above are hereby incorporated by reference to provide continuity of disclosure.
Provisional Applications (1)
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Number |
Date |
Country |
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60389839 |
Jun 2002 |
US |