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US 4,377,515 AGranted
Long lasting agonists and antagonists of LH-RH
AssigneeMerck & Co., Inc.
InventorsDaniel F. Veber, Roger M. Freidinger
Life of this patent
Estimating the term…
Abstract
Novel peptides of the formula: ##STR1## where A through G, X and Y are various amino acids and substituents; having long lasting LHRH agonist and antagonist activity; useful in promoting fertility, reducing fertility, respectively.
Claims6
A novel peptide of the formula:
- ##STR15## wherein for A the L- or D- N-acetyl or N-pyroGlu imino acid is a member selected from the group consisting of N-acetyl-Pro, N-acetyl-Hyp, N-pyroGlu-Pro, and N-pyroGlu-Hyp;
- for B the L- or D-aromatic amino acid is a member selected from the group consisting of Phe, Trp, Tyr, and His, and the L- or D- aliphatic amino acid is a member selected from the group consisting of Ala, Leu, Ile, and Val;
- for C the L- or D- aromatic amino acid is a member selected from the group consisting of Phe, Trp, Tyr, and His, and the L- or D- aliphatic amino acid is a member selected from the group consisting of Ala, Leu, Ile, and Val;
- for E the aromatic amino acid is a member selected from the group consisting of Phe, Trp, Tyr, and His;
- for F the amino acid with a basic side chain is a member selected from the group consisting of Lys, Arg, and Orn;
- and for G the imino acid is a member selected from the group consisting of Pro and Hyp, and the aliphatic amino acid is a member selected from the group consisting of Ala, Leu, Ile, and Val.
3 more elements
A novel peptide of the formula:
- ##STR16## wherein:
- A is L- or D- pyroGlu;
- L- or D-N-acetyl- or N-pyroGlu-Pro;
- acetyl D-Phe;
- or C.sub.3-7 cycloalkyl acyl;
- B is His;
- Gly;
- L- or D-:
- Phe, Tyr, Ala, Leu, Ile or Val;
- or is absent;
- C is L- or D-:
- Phe, Tyr, Ala, Leu, Ile, or Val;
- D is Ser;
- Thr;
- or Ala;
- E is Phe;
- or Tyr;
- F is Lys;
- or Arg;
- G is Pro;
- Ala;
- Leu;
- Ile;
- or Val;
- X is GlyNH.sub.2 ;
- AlaNH.sub.2 ;
- aminoethyl;
- aminopropyl;
- or aminohydroxyethyl;
- Y is hydrogen;
- or C.sub.1-4 alkyl;
- and
- n is 2 or 3.
30 more elements
Dependencies are inferred from the claim text.