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US4816443A Expired / Lapsed US ⏱️ 0.0 years remaining

Piptides having ANF activity

Assignee: Merck and Co Inc
•
Filing: 1987-05-19
•
Granted: 1989-03-28
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Expires: 2007-05-19
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Abstract

Abstract Novel peptides having potent natriuretic activity are disclosed with the following amino acid sequence: ##STR1## wherein Z is H, acetyl, Boc or Ser-Leu, E is Phe, NMP, OMT, ChA, F is Gly or DAl, G is Ala or Gly, H is Arg or DAr, Pro, Lys or Dly, I is Ile, Met, MeO, MO 2 , Leu, Nle, or Val, J is Aib, αMG or αMA, K is Arg or Lys, L is Ile or Val, M is Aib, Gly, Ala or DAl, N is Ala, NMA, Pro, Phe or NMP, O is Gln, DGl, Ala or DAl, P is Ser, His, Arg or Lys, Q is Gly, Pro, Ala or Dal, R is Leu, Phe or ChA, S is Gly, Ala or Dal, Arg or DAr, T is Asn DAs, Ala or Dal, U is Ser, DSe, Ala or DAl, V is Phe, DPh, Ala or DAl, Y is -OH or -NH 2 and n is 0 or 1. Also included are the lower alkyl esters and the physiologically acceptable metal salts and acid addition salts of the foregoing peptides. Unless indicated otherwise all optically active amino acids have the L-configuration.

Inventors

  • 👤 Stephen F. Brady
  • 👤 Ruth F. Nutt

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-05 18:03
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/575; C07K14/58; A; A61; A61P; A61P7/00; A61P7/10; A61P9/00; A61P9/12; A61K; A61K38/00

Claims Analysis

Total Claims: 9
Claim 1
Independent Claim 167 words
A peptide of the formula: ##STR4## wherein Z is H, acetyl, Boc or Ser-Leu, E is Phe, NMP, OMT, ChA, F is Gly or D-Ala, G is Ala or Gly, H is Arg or D-Arg, Pro, Lys or D-Lys, I is Ile, Met, MeO, MO 2 , Leu, Nle, or Val, J is Aib, αMG or αMA, K is Arg or Lys, L is Ile or Val, M is Aib, Gly, Ala or D-Ala, N is Ala, NMA, Pro, Phe or NMP, O is Gln, D-Gln, Ala or D-Ala, P is Ser, His, Arg or Lys, Q is Gly, Pro, Ala or D-Ala, R is Leu, Phe or ChA, S is Gly, Ala or D-Ala, Arg or D-Arg, T is Asn DAs, Ala or D-Ala, U is Ser, D-Ser, Ala or D-Ala, V is Phe, D-Phe, Ala or D-Ala, Y is --OH or --NH 2 and n is 0 or 1, and the lower alkyl esters and the physiologically acceptable metal salts and acid addition salts thereof.
Claim 2
Dependent Claim 167 words
A peptide of the formula: ##STR4## wherein Z is H, acetyl, Boc or Ser-Leu, E is Phe, NMP, OMT, ChA, F is Gly or D-Ala, G is Ala or Gly, H is Arg or D-Arg, Pro, Lys or D-Lys, I is Ile, Met, MeO, MO 2 , Leu, Nle, or Val, J is Aib, αMG or αMA, K is Arg or Lys, L is Ile or Val, M is Aib, Gly, Ala or D-Ala, N is Ala, NMA, Pro, Phe or NMP, O is Gln, D-Gln, Ala or D-Ala, P is Ser, His, Arg or Lys, Q is Gly, Pro, Ala or D-Ala, R is Leu, Phe or ChA, S is Gly, Ala or D-Ala, Arg or D-Arg, T is Asn DAs, Ala or D-Ala, U is Ser, D-Ser, Ala or D-Ala, V is Phe, D-Phe, Ala or D-Ala, Y is --OH or --NH 2 and n is 0 or 1, and the lower alkyl esters and the physiologically acceptable metal salts and acid addition salts thereof.
Claim 3
Dependent Claim 11 words
A peptide of claim 1 wherein the C-terminal group is --COOH.
Claim 4
Dependent Claim 13 words
A peptide of claim 1 wherein the C-terminal group is --CONH 2 .
Claim 5
Dependent Claim 12 words
A peptide of claim 1 in combination with a pharmaceutically acceptable carrier.
Claim 6
Dependent Claim 26 words
A method of treating a disorder of electrolyte balance which comprises administering to a mammalian species a therapeutically active amount of a peptide of claim 1.
Claim 7
Dependent Claim 27 words
A method of treating a disorder of altered vacular resistance which comprises administering to a mammalian species a therapeutically active amount of a peptide of claim 1.
Claim 8
Dependent Claim 23 words
A method of treating essential hypertension which comprises administering to a mammalian species a therapeutically active amount of a peptide of claim 1.
Claim 9
Dependent Claim 24 words
A method of treating congestive heart failure which comprises administering to a mammalian species a therapeutically active amount of a peptide of claim 1.

References Cited (Backward Citations)

US4607023A Cited
US4557864A Cited
US4618600A Cited
US4673732A Cited
US4609725A Cited
US4716147A Cited
US4721704A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1992-03-27 1992-09-26 1993-03-28 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1996-03-27 1996-09-26 1997-03-28 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2000-03-27 2000-09-26 2001-03-28 $7700.00 Window Closed / Lapsed

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