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filingDate 1998-04-13-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2001-11-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber JP-2001523229-A
titleOfInvention GnRH antagonists modified at positions 5 and 6
abstract (57) Abstract: Peptides having improved duration of GnRH antagonism are provided. These antagonists can be used to modulate fertility and treat steroid dependent tumors, and can be used for both short and long term therapeutic indications. These antagonists have an amino Phe derivative or its equivalent at position 5 or at positions 5 and 6. This derivative is modified to include a heterocycle containing a urea moiety in the carbamoyl group or side chain. A particularly effective decapeptide that continues to exert significant LH secretion inhibition over 96 hours after injection is of the formula: Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-4Aph (L-hydrooroto) -D-4Aph ( acetyl) -Leu-Lys (isopropyl) -Pro-D-Ala-NH 2, and Ac-D-2Nal-D- 4Cpa-D-3Pal-Ser-4Aph (L- Hidorooroto) -D-4Amf (Q 2) having -Leu-Lys (isopropyl) -Pro-Xaa 10. In the formula, Q 2 is Cbm or MeCbm, and Xaa 10 is D-Ala-NH 2 , D-Ala-ol, or Ala-ol.
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priorityDate 1997-04-11-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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