US4396772A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Phosphinylalkanoyl amino acids
Assignee: ER Squibb and Sons LLC
•
Filing: 1981-11-23
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Granted: 1983-08-02
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Expires: 2001-11-23
Abstract
Abstract Angiotensin converting enzyme activity is inhibited by compounds having the formula ##STR1## and salts thereof wherein R 1 is alkyl, aryl, arylalkyl, cycloalkyl, or cycloalkyl(alkyl); R 2 and R 4 each is independently hydrogen, alkyl, arylalkyl or ##STR2## wherein X is hydrogen, alkyl, or phenyl and Y is hydrogen, alkyl, phenyl or alkoxy, or together X and Y are --(CH 2 ) 2 --, --(CH 2 ) 3 --, --CH═CH--or ##STR3## R 3 is hydrogen or alkyl; ##STR4## is a residue of an amino acid selected from the group consisting of glycine, alanine, valine, norvaline, leucine, N-methylleucine, norleucine, isoleucine, phenylalanine, tyrosine, serine, threonine, cysteine, methionine, aspartic acid, glutamic acid, arginine, lysine, asparagine, glutamine, histidine, or tryptophane; and n is 0 or 1.
Inventors
- 👤 Edward W. Petrillo, Jr.
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 12:22
CPC Classifications
C; C07; C07F; C07F9/00; C07F9/02; C07F9/28; C07F9/30; C07F9/32; C07F9/3205; C07F9/3211; A; A61; A61P; A61P9/00; A61P9/12; C07F9/301; C07F9/547; C07F9/553; C07F9/572; C07F9/5728; C07F9/645; C07F9/6503; C07F9/6506
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
135 words
A compound having the formula ##STR18## or a salt thereof, wherein R 1 is alkyl, aryl, arylalkyl, cycloalkyl, or cycloalkyl(alkyl); R 2 and R 4 each is independently hydrogen, alkyl, arylalkyl or ##STR19## wherein X is hydrogen, alkyl, or phenyl and Y is hydrogen, alkyl, phenyl or alkoxy, or together X and Y are --(CH 2 )-- 2 , --(CH 2 ) 3 --, --CH═CH-- or ##STR20## R 3 is hydrogen or alkyl; ##STR21## is a residue of an amino acid selected from the group consisting of glycine, alanine, valine, norvaline, leucine, N-methylleucine, norleucine, isoleucine, phenylalanine, tyrosine, serine, threonine, cysteine, methionine, aspartic acid, glutamic acid, arginine, lysine, asparagine, glutamine, histidine, or tryptophane; and n is 0 or 1; wherein the amino acid residue ##STR22## is linked to the adjacent carbonyl group by an amide bond.
Claim 2
Dependent Claim
135 words
A compound having the formula ##STR18## or a salt thereof, wherein R 1 is alkyl, aryl, arylalkyl, cycloalkyl, or cycloalkyl(alkyl); R 2 and R 4 each is independently hydrogen, alkyl, arylalkyl or ##STR19## wherein X is hydrogen, alkyl, or phenyl and Y is hydrogen, alkyl, phenyl or alkoxy, or together X and Y are --(CH 2 )-- 2 , --(CH 2 ) 3 --, --CH═CH-- or ##STR20## R 3 is hydrogen or alkyl; ##STR21## is a residue of an amino acid selected from the group consisting of glycine, alanine, valine, norvaline, leucine, N-methylleucine, norleucine, isoleucine, phenylalanine, tyrosine, serine, threonine, cysteine, methionine, aspartic acid, glutamic acid, arginine, lysine, asparagine, glutamine, histidine, or tryptophane; and n is 0 or 1; wherein the amino acid residue ##STR22## is linked to the adjacent carbonyl group by an amide bond.
Claim 3
Dependent Claim
11 words
A compound in accordance with claim 1 wherein n is 1.
Claim 4
Dependent Claim
16 words
A compound in accordance with claim 1 wherein R 2 and R 4 each is hydrogen.
Claim 5
Dependent Claim
22 words
A compound in accordance with claim 1 wherein one of R 2 and R 4 is hydrogen and the other is ##STR23##
Claim 6
Dependent Claim
10 words
The compound in accordance with claim 1 N-[[ethoxy(4-phenylbutyl)phosphinyl]acetyl]-L-tyrosine, methyl ester.
Claim 7
Dependent Claim
10 words
The compound in accordance with claim 1 N-[[hydroxy(4-phenylbutyl)phosphinyl]acetyl]-L-tyrosine, methyl ester.
Claim 8
Dependent Claim
8 words
The compound in accordance with claim 1 N-[[hydroxy(4-phenylbutyl)phosphinyl]acetyl]-L-tyrosine.
Claim 9
Dependent Claim
10 words
The compound in accordance with claim 1 N 2 -[[ethoxy(4-phenylbutyl)phosphinyl]acetyl]-L-arginine.
Claim 10
Dependent Claim
10 words
The compound in accordance with claim 1 N 2 -[[hydroxy(4-phenylbutyl)phosphinyl]acetyl]-L-arginine.
Claim 11
Dependent Claim
10 words
The compound in accordance with claim 1 N-[[(2-phenylethyl)(phenylmethoxy)phosphinyl]-acetyl]-L-tryptophan, phenylmethyl ester.
Claim 12
Dependent Claim
10 words
The compound in accordance with claim 1 N-[[hydroxy(2-phenylethyl)phosphinyl]acetyl]-L-tryptophan, ammonia salt.
References Cited (Backward Citations)
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US4179464A
Cited
US4316896A
Cited
US4168267A
Cited
US4371526A
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1986-08-01 | 1987-01-31 | 1987-08-02 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1990-08-01 | 1991-01-31 | 1991-08-02 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1994-08-01 | 1995-01-31 | 1995-08-02 | $7700.00 | Window Closed / Lapsed |