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EP0077029A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Renin inhibitory peptides

Assignee: Merck and Co Inc
•
Filing: 1982-10-07
•
Granted: —
•
Expires: 2002-10-07
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Abstract

Abstract Renin inhibitory peptides of the formula:

Inventors

  • 👤 Daniel F. Veber
  • 👤 Daniel H. Rich

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-26 15:53
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/02; C07K5/0227; A; A61; A61P; A61P43/00; A61P9/00; A61P9/12; Y; Y10; Y10S; Y10S530/00; Y10S530/86

Claims Analysis

Total Claims: 7
Claim 1
Independent Claim 96 words
l. A peptide of the formula: wherein: A is hydrogen; or phenoxyacetyl; R 1 is C 3-6 straight or branched alkyl; C 3-7 cycloalkyl; phenyl; or phenyl monosubstituted with hydroxyl, fluoro, chloro, bromo, methyl, or trifluoromethyl; R 2 is hydrogen; or methyl; R 3 is methyl; or isopropyl ; R 4 is phenyl; or 4-hydroxyphenyl; and B is OR; NHR; or NR 2 , where each R may be the same or different and is hydrogen or C 1-4 alkyl; and a pharmaceutically acceptable salt thereof; all of the asymmetric carbon atoms having an S configuration.
Claim 2
Dependent Claim 21 words
A peptide according to Claim 1 wherein the peptide is N-phenoxyacetyl-L-leucyl-(3S,4S)-statyl-L-valyl-L-phenylalanine, or the amide or C 1-4 alkyl ester form thereof.
Claim 3
Dependent Claim 21 words
A peptide according to Claim 1 wherein the peptide is N-phenoxyacetyl-L-leucyl-(3S,4S)-statyl-L-leucyl-L-phenylalanine, or the amide or C 1-4 alkyl ester form thereof.
Claim 4
Dependent Claim 21 words
A peptide according to Claim 1 wherein the peptide is N-phenoxyacetyl-L-leucyl-4(S)-amino-3(S)-hydroxy-5-phenylpentanoyl-L-leucyl-L-phenylalanine, or the amide or C 1-4 alkyl ester form thereof.
Claim 5
Dependent Claim 21 words
A peptide according to Claim 1 wherein the peptide is L-leucyl-(3S,4S)-statyl-L-valyl-L-phenylalanine, or the amide or C 1-4 alkyl ester form thereof.
Claim 6
Dependent Claim 110 words
A pharmaceutical composition for treating renin-associated hypertension, comprising a pharmaceutical carrier and a therapeutically effective amount of a peptide of the formula: wherein: A is hydrogen; or phenoxyacetyl; R 1 is C 3-6 straight or branched alkyl; C 3-7 cycloalkyl; phenyl; or phenyl monosubstituted with hydroxyl, fluoro, chloro, bromo, methyl, or trifluoromethyl; R 2 is hydrogen; or methyl; R 3 is methyl; or isopropyl;1R 4 is phenyl; or 4-hydroxyphenyl; and B is OR; NHR; or NR 2 , where each R may be the same or different and is hydrogen or C 1-4 alkyl; and a pharmaceutically acceptable salt thereof; all of the asymmetric carbon atoms having an S configuration.
Claim 7
Dependent Claim 114 words
7 _ A pharmaceutical composition for treating renin-associated hyperaldosteronism, comprising a pharmaceutical carrier and a therapeutically effective amount of a peptide of the formula: wherein: A is hydrogen; or phenoxyacetyl; R 1 is C 3-6 straight or branched alkyl; C 3-7 cycloalkyl; phenyl; or phenyl monosubstituted with hydroxyl, fluoro, chloro, bromo, methyl, or trifluoromethyl; R 2 is hydrogen ; or methyl; R 3 is methyl; or isopropyl; R 4 is phenyl; or 4-hydroxyphenyl; and B is OR; NHR; or NR 2 , where each R may be the same or different and is hydrogen or C 1-4 alkyl; and a pharmaceutically acceptable salt thereof; all of the asymmetric carbon atoms having an S configuration.

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