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US4293481A Expired / Lapsed US ⏱️ 0.0 years remaining

Tripeptide inhibitors of angiotensin-converting enzyme

Assignee: ER Squibb and Sons LLC
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Filing: 1980-07-24
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Granted: 1981-10-06
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Expires: 2000-07-24
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Abstract

Abstract Peptides having the formula ##STR1## wherein R 1 is hydrogen and R 2 is hydroxyl, alkyl, aryl, arylalkyl, alkoxy, alkylthio, aryloxy, arylthio, halogen or azido, or R 1 and R 2 are the same and each is hydrogen, halogen, alkoxy or alkylthio, or R 1 and R 2 together are oxo, --O--(CH 2 ) n --O--, or --S--(CH 2 ) n --S--, wherein n is 1 or 2; R 3 is hydrogen, alkyl or trifluoromethyl; R 4 is hydrogen or an acyl protecting group; and R 5 is hydrogen or alkyl; are inhibitors of angiotensin converting enzyme and can be used for the treatment of hypertension in mammals.

Inventors

  • 👤 Michael E. Condon
  • 👤 Miguel A. Ondetti

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-08 13:12
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/08; C07K5/0802; C07K5/0812; A; A61; A61K; A61K38/00; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55

Claims Analysis

Total Claims: 8
Claim 1
Independent Claim 96 words
A tripeptide having the formula ##STR8## or a salt thereof, wherein R 1 is hydrogen and R 2 is hydroxyl, alkyl, aryl, arylalkyl, alkoxy, alkylthio, aryloxy, arylthio, halogen, or azido, or R 1 and R 2 are the same and each is hydrogen, halogen, alkoxy or alkylthio, or R 1 and R 2 together are oxo, --O--(CH 2 ) n --O--, or --S--(CH 2 ) n --S--, wherein n is 1 or 2; R 3 is hydrogen, alkyl or trifluoromethyl; R 4 is hydrogen or an acyl protecting group; and R 5 is hydrogen or alkyl.
Claim 2
Dependent Claim 96 words
A tripeptide having the formula ##STR8## or a salt thereof, wherein R 1 is hydrogen and R 2 is hydroxyl, alkyl, aryl, arylalkyl, alkoxy, alkylthio, aryloxy, arylthio, halogen, or azido, or R 1 and R 2 are the same and each is hydrogen, halogen, alkoxy or alkylthio, or R 1 and R 2 together are oxo, --O--(CH 2 ) n --O--, or --S--(CH 2 ) n --S--, wherein n is 1 or 2; R 3 is hydrogen, alkyl or trifluoromethyl; R 4 is hydrogen or an acyl protecting group; and R 5 is hydrogen or alkyl.
Claim 3
Dependent Claim 16 words
A tripeptide in accordance with claim 1 wherein R 4 and R 5 each is hydrogen.
Claim 4
Dependent Claim 12 words
A tripeptide in accordance with claim 2 wherein R 3 is methyl.
Claim 5
Dependent Claim 15 words
A tripeptide in accordance with claim 2 wherein R 1 and R 2 are hydrogen.
Claim 6
Dependent Claim 10 words
The tripeptide in accordance with claim 1 (S,S)-1-[N-[3-[(benzyloxycarbonyl)amino]-2-hydroxy-1-oxo-4-phenylbutyl]-L-alanyl]-L-proline, t-butyl ester.
Claim 7
Dependent Claim 8 words
The tripeptide in accordance with claim 1 (S,S)-1-[N-[3-[(benzyloxycarbonyl)amino]-2-hydroxy-1-oxo-4-phenylbutyl]-L-alanyl]-L-proline.
Claim 8
Dependent Claim 8 words
The tripeptide in accordance with claim 1 (S,S)-1-[N-(3-amino-2-hydroxy-1-oxo-4-phenylbutyl)-L-alanyl]-L-proline.

References Cited (Backward Citations)

US4191753A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1984-10-05 1985-04-06 1985-10-06 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1988-10-05 1989-04-06 1989-10-06 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1992-10-05 1993-04-06 1993-10-06 $7700.00 Window Closed / Lapsed

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