U.S. patents available from 1976 to present.
U.S. patent applications available from 2005 to present.

Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol derivative

Patent 5840890 Issued on November 24, 1998. Estimated Expiration Date: Icon_subject January 9, 2017. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.

Patent References

9-(1,3-Dihydroxy-2-propoxymethyl)guanine as antiviral agent
Patent #: 4355032
Issued on: 10/19/1982
Inventor: Verheyden ,   et al.

Antiviral compounds Patent #: 5043339
Issued on: 08/27/1991
Inventor: Beauchamp

Inventors

Application

No. 775424 filed on 01/09/1997

US Classes:

544/276, Nitrogen attached directly or indirectly to the purine ring system by nonionic bonding435/119Containing at least two hetero rings bridged or fused among themselves or bridged or fused with a common carbocyclic ring system, (e.g., rifamycin, etc.)

Examiners

Primary: Berch, Mark L.

Attorney, Agent or Firm

Foreign Patent References

  • 0 158 847 EP. 10/13/1985
  • 0 308 065 EP. 03/13/1989
  • 0 375 329 EP. 06/13/1990
  • 1 523 865 GB. 06/13/1978
  • 2 104 070 GB. 03/13/1983
  • 2 122 618 GB. 01/13/1984
  • 8829571 GB. 06/13/1990
  • WO 94/29311 WO. 12/13/1994

International Classes

C07D 473/18
C07B 051/00

Abstract

Process and novel intermediates for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol ganciclovir) and its pharmaceutically acceptable salts. The present process and monoester intermediates provide for mono-esterification by an L-valine derivative, resulting in a monocarboxylate-monovalinate which is then selectively hydrolyzed under basic or enzymatic conditions to give the monovaline ester of ganciclovir in high yield and purity. These products are of value as antiviral agents with improved absorption.

Other References

  • E. Jensen, et al., Acta Pharm. Nord. 3(4) 243-247 (1991)
  • John C. Martin, et al., J. Pharm. Sci. 76(2), pp. 180-184 (1987)
  • P.C. Maudgal, et al., Arch. Ophthalmol. 1984; 102:140-142
  • Leon Colla, et al., J. Med. Chem., 98, 3, 26, 602-604 (1983)
  • L.M. Beauchamp, et al., Antiviral Chemistry & Chemotherapy (1992), 3(3), 157-16
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