US4684660A
Expired / Lapsed
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Mercaptoacyldepeptides
Assignee: ER Squibb and Sons LLC
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Filing: 1980-05-01
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Granted: 1987-08-04
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Expires: 2000-05-01
Abstract
Abstract Compounds having the formula ##STR1## and alkyl esters and salts thereof. R 1 is hydrogen, alkanoyl or ##STR2## R 2 is hydrogen, alkyl, or phenylalkyl; n is 0 or 1; and A 1 and A 2 each is an α-amino or α-imino acid residue joined through a peptide bond, have useful hypotensive activity.
Inventors
- 👤 Miquel A. Ondetti
- 👤 Josip Pluscec
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 21:11
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06139; C07K5/06165; A; A61; A61K; A61K38/00
Claims Analysis
Total Claims: 26
Claim 1
Independent Claim
47 words
A compound having the formula ##STR12## or an alkyl ester or a salt thereof, wherein R 1 is hydrogen, or ##STR13## R 2 is hydrogen, alkyl or phenylalkyl; and A 1 and A 2 each is an α-amino or α-imino acid residue joined through a peptide bond.
Claim 2
Dependent Claim
47 words
A compound having the formula ##STR12## or an alkyl ester or a salt thereof, wherein R 1 is hydrogen, or ##STR13## R 2 is hydrogen, alkyl or phenylalkyl; and A 1 and A 2 each is an α-amino or α-imino acid residue joined through a peptide bond.
Claim 3
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 1 is hydrogen.
Claim 4
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 1 is ##STR14##
Claim 5
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 2 is hydrogen.
Claim 6
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 2 is alkyl.
Claim 7
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 2 is phenylalkyl.
Claim 8
Dependent Claim
23 words
A compound in accordance with claim 1 wherein A 1 is an α-amino acid residue and A 2 is an α-imino acid residue.
Claim 9
Dependent Claim
12 words
A compound in accordance with claim 7 wherein A 2 is L-proline.
Claim 10
Dependent Claim
59 words
A compound having the formula ##STR15## or an alkyl ester or a salt thereof, wherein R 1 is hydrogen, or ##STR16## or an alkyl ester or a salt thereof, wherein R 2 is hydrogen, alkyl or phenylalkyl; and A 1 and A 2 each is independently proline, 4-hydroxyproline, 4,4-ethylenedioxyproline, 4-methoxyproline, 4-thiazolidinecarboxylic acid, tryptophane, glycine, alanine, leucine, isoleucine or valine.
Claim 11
Dependent Claim
59 words
A compound having the formula ##STR15## or an alkyl ester or a salt thereof, wherein R 1 is hydrogen, or ##STR16## or an alkyl ester or a salt thereof, wherein R 2 is hydrogen, alkyl or phenylalkyl; and A 1 and A 2 each is independently proline, 4-hydroxyproline, 4,4-ethylenedioxyproline, 4-methoxyproline, 4-thiazolidinecarboxylic acid, tryptophane, glycine, alanine, leucine, isoleucine or valine.
Claim 12
Dependent Claim
8 words
The compound in accordance with claim 9, 1-(S-3-mercapto-2-methyl-1-oxopropyl)-L-prolyl-L-proline.
Claim 13
Dependent Claim
10 words
The compound in accordance with claim 9, 1-(S-3-mercapto-2-methyl-1-oxopropyl)-L-prolyl-glycine, lithium salt.
Claim 14
Dependent Claim
8 words
The compound in accordance with claim 9, (S)-1-(3-mercapto-2-methyl-1-oxopropyl)-L-prolyl-L-alanine.
Claim 15
Dependent Claim
8 words
The compound in accordance with claim 9, (S)-(3-mercapto-2-methyl-1-oxopropyl)-L-propyl-D-alanine.
Claim 16
Dependent Claim
12 words
A compound in accordance with claim 9 wherein R 1 is hydrogen.
Claim 17
Dependent Claim
12 words
A compound in accordance with claim 9 wherein R 1 is ##STR17##
Claim 18
Dependent Claim
12 words
A compound in accordance with claim 9 wherein R 2 is hydrogen.
Claim 19
Dependent Claim
12 words
A compound in accordance with claim 9 wherein R 2 is alkyl.
Claim 20
Dependent Claim
12 words
A compound in accordance with claim 9 wherein R 2 is phenylalkyl.
Claim 21
Dependent Claim
23 words
A compound in accordance with claim 9 wherein A 1 is an α-amino acid residue and A 2 is an α-imino acid residue.
Claim 22
Dependent Claim
12 words
A compound in accordance with claim 9 wherein A 2 is L-proline.
Claim 23
Dependent Claim
67 words
A pharmaceutically acceptable compound having the formula ##STR18## or an alkyl ester or a salt thereof, wherein R 1 is hydrogen, or ##STR19## R 2 is hydrogen, alkyl or phenylalkyl; and A 1 and A 2 each is an α-amino or α-imino acid residue joined through a peptide bond; said compound when administered to a mammal with elevated blood pressure being capable of reducing the blood pressure.
Claim 24
Dependent Claim
67 words
A pharmaceutically acceptable compound having the formula ##STR18## or an alkyl ester or a salt thereof, wherein R 1 is hydrogen, or ##STR19## R 2 is hydrogen, alkyl or phenylalkyl; and A 1 and A 2 each is an α-amino or α-imino acid residue joined through a peptide bond; said compound when administered to a mammal with elevated blood pressure being capable of reducing the blood pressure.
Claim 25
Independent Claim
75 words
A method for reducing blood pressure in mammals which comprises administering to a mammal in need thereof, an effective amount of a compound having the formula ##STR20## or an alkyl ester or a physiologically acceptable salt thereof, wherein R 1 is hydrogen, or ##STR21## R 2 is hydrogen, alkyl or phenylalkyl, n is 0 or 1; and A 1 and A 2 each is an α-amino or, α-imino acid residue joined through a peptide bond.
Claim 26
Independent Claim
75 words
A method for reducing blood pressure in mammals which comprises administering to a mammal in need thereof, an effective amount of a compound having the formula ##STR20## or an alkyl ester or a physiologically acceptable salt thereof, wherein R 1 is hydrogen, or ##STR21## R 2 is hydrogen, alkyl or phenylalkyl, n is 0 or 1; and A 1 and A 2 each is an α-amino or, α-imino acid residue joined through a peptide bond.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1990-08-03 | 1991-02-02 | 1991-08-04 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-08-03 | 1995-02-02 | 1995-08-04 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-08-03 | 1999-02-02 | 1999-08-04 | $7700.00 | Window Closed / Lapsed |