U.S. patents available from 1976 to present.
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Non-peptide GnRH agents

Patent 6218426 Issued on April 17, 2001. Estimated Expiration Date: Icon_subject March 1, 2019. 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

GnRH Antagonists VI
Patent #: 4565804
Issued on: 01/21/1986
Inventor: Rivier ,   et al.

GNRH antagonists XIII Patent #: 5506207
Issued on: 04/09/1996
Inventor: Rivier, et al.

Inventors

Assignee

Application

No. 259206 filed on 03/01/1999

US Classes:

514/448, C=O bonded directly to the hetero ring (X is chalcogen)514/471, Nitrogen containing514/613, Carboxamides (i.e., R-C(=O)-N, wherein R is a radical having carbon bonded directly to the C(=O)-N or is hydrogen and wherein any substituent attached to nitrogen will be referred to as E)514/634, Guanidines (i.e., N=C(-N)-N)549/72, Nitrogen or chalcogen attached indirectly to the hetero ring by nonionic bonding549/461, Having -C(=X)-, wherein X is chalcogen, attached directly or indirectly to the tricyclo ring system by nonionic bonding549/483, Having -C(=X)-, wherein X is chalcogen, bonded directly to the hetero ring549/487, Nitrogen bonded directly to the -C(=X)- group560/190, Polycarboxylic acid564/161, Substituent Q contains benzene ring564/170, Hydroxy, bonded directly to carbon, or ether in substituent Q (H of -OH may be replaced by a substituted or unsubstituted ammonium ion or a Group IA or IIA light metal)564/237Benzene ring containing

Examiners

Primary: Killos, Paul J.

Foreign Patent References

  • 9303058 WO. 02/08/1993
  • 9500474 WO. 01/08/1995
  • 9721703 WO. 06/08/1997

International Classes

A01N 043/06
C07C 069/34

Abstract

Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are of the following general formula, where X1, X2, Y, and are defined variables: ##STR1##Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.

Other References

  • Mitchinson et al., "Discrimination of Spermidine Amino Functions by a New Protecting Group Strategy; Application to the Synthesis of Guanidinylated Polyamines, Including Hirudonine," J. Chem. Soc. Commun., 1994, 2613-2614
  • Yorke et al., "Synthesis of Acarnidines: Guanidinated Spermidine Homologues Through Imine Intermediates," Aust. J. Chem., vol. 39, 1986, 447-45
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