GnRH Antagonists IV

  • US 4,569,927 A
  • Filed: 05/21/1984
  • Issued: 02/11/1986
  • Est. Priority Date: 02/23/1984
  • Status: Expired due to Fees
First Claim
Patent Images

1. A peptide or a nontoxic salt thereof, said peptide having the formula:

  • X-R1 -(W)D-Phe-R3 -R4 -R5 -R6 -R7 -Arg-Pro-R10 wherein X is hydrogen or an acyl group having 7 or less carbon atoms;

    R1 is dehydro-Pro, D-pGlu, D-Phe, D-Trp or β

    -D-NAL;

    W is 4F, 4Cl, 2,4Cl2, 3,4Cl2, 4Br, 4NO2 or C.sup.α

    Me-4Cl;

    R3 is (Nin For) D-Trp or D-Trp which is substituted in the 5- or 6-position with NO2, NH2, OCH3, F, Cl, Br or CH3 ;

    R4 is Ser, Orn, AAL or aBu;

    R5 is Tyr, Arg, (3F)Phe, (2F)Phe, (3I)Tyr, (3CH3)Phe, (2CH3)Phe, (3Cl)Phe or (2Cl)Phe;

    R6 is (4NH2)D-Phe, D-Lys, D-Orn, D-Har, D-His, (4gua)D-Phe, D-Tyr, D-Trp, D-Phe, D-Leu, D-Ile, D-Nle, D-Val, D-Ala, D-Ser(OtBu), β

    -D-2NAL, (imBzl)D-His, or D-Arg;

    R7 is Leu, NML, Nle or Nva; and

    R10 is Gly-NH2, D-Ala-NH2 or NH-Y, with Y being lower alkyl, cycloalkyl, fluoro lower alkyl or NHCONHQ, where Q is H or lower alkyl, provided however that when R5 is Arg, R6 is D-Tyr.

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