U.S. patents available from 1976 to present.
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Camptothecin analogues, preparation methods therefor, use thereof as drugs, and pharmaceutical compositions containing said analogues

Patent 5981542 Issued on November 9, 1999. Estimated Expiration Date: Icon_subject December 2, 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.

Inventors

Application

No. 973561 filed on 12/02/1997

US Classes:

514/283, Ring nitrogen in the pentacyclo ring system is shared by five-membered cyclo and six-membered cyclo (e.g., vincamine, etc.)514/280, Pentacyclo ring system having the six-membered hetero ring as one of the cyclos546/48Three or more ring hetero atoms in the pentacyclo ring system

Examiners

Primary: Shah, Mukund J.
Assistant: Kifle, Bruck

Attorney, Agent or Firm

Foreign Patent References

  • WO 94/11376 WO. 05/22/1994

International Classes

C07D 491/14
C07D 491/22
C07D 471/04
A61K 031/47

Foreign Application Priority Data

1995-06-21 GB

Abstract

A camptothecin analog characterized in that the hydroxy lactone of the camptothecin is a ଲ-hydroxy lactone or the corresponding ଲ-hydroxyacid, resulting from the opening of said lactone, or a derivative of said ଲ-hydroxyacid, or a Pharmaceutically acceptable salt thereof, is disclosed. In particular, compounds of formulae (I) and (II) are disclosed. Methods for preparing the compounds of formulae (I) and (II), pharmaceutical compositions containing said containing said compounds, and their use, particularly as topoisomerase inhibitors and antitumoral drugs, are also disclosed.

Other References

  • Journal of Medicinal Chemistry, vol. 32, No. 3, 1989 pp. 715-720
  • Journal of Medicinal Chemistry, vol. 19, No. 5, May 1976 pp. 675-67
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