The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Oct. 13, 1998

Filed:

Apr. 11, 1997
Applicant:
Inventors:

Guangcheng Jiang, San Diego, CA (US);

Graeme Semple, Hamphire, GB;

Assignee:

Ferring BV, Hoofddorp, NL;

Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
A61K / ; C07K / ;
U.S. Cl.
CPC ...
514 15 ; 530328 ;
Abstract

Peptides are provided which have improved duration of GnRH antagonistic properties and/or which can be synthesized more economically. These antagonists may be used in the same manner as the compounds of which they are analogs to regulate fertility and to treat steroid-dependent tumors and for other short-term and long-term treatment indications. One particularly effective peptide, a decapeptide analog of the GnRH antagonist Acyline, has the formula: Ac-D-2Nal-D-4Cpa-D-Dpr(methylcarbamoyl)-Ser-4Aph(acetyl)-D-4Aph(acetyl)-Le u-Lys(isopropyl)-Pro-D-Ala-NH.sub.2. It continues to exhibit very substantial suppression of LH secretion at 96 hours following injection. Other economically attractive and pharmacologically effective analogs have the formulas: Ac-D-2Nal-D-4Cpa-Xaa.sub.3 -Ser-4Aph(acetyl)-D-4Aph(acetyl)-Leu-Lys(isopropyl)-Pro-D-Ala-NH.sub.2 ; and Ac-D-2Nal-D-4Cpa-Xaa.sub.3 -Ser-4Aph(hydroorotyl)-D-4Aph(acetyl)-Leu-Lys(isopropyl)-Pro-D-Ala-NH.sub. 2, wherein Xaa.sub.3 is D-Gln or Gln.


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