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US4929641A
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Mercapto-acylamino acid antihypertensives
Assignee: Merck Sharp & Dohme LLC
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Filing: 1988-05-11
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Granted: 1990-05-29
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Expires: 2008-05-11
Abstract
Abstract Novel mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension are disclosed.
Inventors
- 👤 Martin F. Haslanger
- 👤 Bernard R. Neustadt
- 👤 Elizabeth M. Smith
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 05:02
CPC Classifications
C; C07; C07C; C07C323/00; C07C323/50; C07C323/51; C07C323/57; C07C323/58; C07C323/59; C07C327/00; C07C327/20; C07C327/32
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
55 words
A compound having the structural formula ##STR54## wherein R 1 is phenyl substituted by alkyl, R 2 is alkyl-S(O) 0-2 (CH 2 )q, R 3 is OR 7 wherein R 7 is hydrogen or lower alkyl, Q is hydrogen or R 10 CO-- wherein R 10 is alkyl, n is 0-2 and q is 1-4.
Claim 2
Dependent Claim
55 words
A compound having the structural formula ##STR54## wherein R 1 is phenyl substituted by alkyl, R 2 is alkyl-S(O) 0-2 (CH 2 )q, R 3 is OR 7 wherein R 7 is hydrogen or lower alkyl, Q is hydrogen or R 10 CO-- wherein R 10 is alkyl, n is 0-2 and q is 1-4.
Claim 3
Dependent Claim
12 words
A compound of claim 1 wherein R 2 is alkyl-S(CH 2 )q.
Claim 4
Dependent Claim
9 words
A compound of claim 2 wherein n is 1.
Claim 5
Dependent Claim
9 words
A compound of claim 2 wherein q is 2.
Claim 6
Dependent Claim
9 words
A compound of claim 3 wherein q is 2.
Claim 7
Dependent Claim
13 words
A compound of claim 5 wherein R 1 is 2-, 3- or 4-methylphenyl.
Claim 8
Dependent Claim
10 words
A compound of claim 6 wherein R 1 is 2-methylphenyl.
Claim 9
Dependent Claim
10 words
A compound of claim 6 wherein R 10 is methyl.
Claim 10
Dependent Claim
25 words
A compound of claim 6 which is selected from: N-[2-acetylthiomethyl-3-(2-methylphenyl)propionyl]-methionine ethyl ester; N-[2-acetylthiomethyl-3-(2-methylphenyl)propionyl]-methionine; N-[2-mercaptomethyl-3-(2-methylphenyl)propionyl]-methionine; N-[2-mercaptomethyl-3-(4-methylphenyl)propionyl]-methionine; N-[2-acetylthiomethyl-3-(2-methylphenyl)propionyl]-methionine methyl ester; N-[2-acetylthiomethyl-3-(4-methylphenyl)propionyl]-methionine methyl ester; and N-[2-acetylthiomethyl-3-(3-methylphenyl)propionyl]-methionine ethyl ester.
Claim 11
Dependent Claim
9 words
A compound of claim 9 which is the (S,S)-diastereomer.
Claim 12
Dependent Claim
10 words
A compound of claim 10 which is N-[2(S)-acetylthiomethyl-3-(2-methylphenyl)propionyl]-(S)-methionine ethyl ester.
Claim 13
Dependent Claim
9 words
A compound of claim 9 which is the (R,S)-diastereomer.
Claim 14
Dependent Claim
13 words
A compound of claim 9 which is a mixture of (S,S) and (R,S)-diastereomers.
Claim 15
Dependent Claim
19 words
An antihypertensive composition comprising an antihypertensive effective amount of a compound of claim 9 in a pharmaceutically acceptable carrier.
Claim 16
Dependent Claim
25 words
A method of treating hypertension or congestive heart failure comprising administering to a hypertensive human an antihypertensive effective amount of a compound of claim 1.
Claim 17
Dependent Claim
27 words
A method of claim 15 wherein the compound is selected from N-[2-acetylthiomethyl-3-(2-methylphenyl)propionyl]-methionine ethyl ester; N-[2-acetylthiomethyl-3-(2-methylphenyl)propionyl]-methionine; N-[2-mercaptomethyl-3-(2-methylphenyl)propionyl]-methionine; N-[2-mercaptomethyl-3-(4-methylphenyl)propionyl]-methionine; N-[2-acetylthiomethyl-3-(2-methylphenyl)propionyl]-methionine methyl ester; N-[2-acetylthiomethyl-3-(4-methylphenyl)propionyl]-methionine methyl ester; and N-[2-acetylthiomethyl-3-(3-methylphenyl)propionyl]-methionine ethyl ester.
Claim 18
Dependent Claim
12 words
A method of claim 16 wherein the compound is N-[2(S)-acetylthiomethyl-3-(2-methylphenyl)-propionyl]-(S)-methionine ethyl ester.
Claim 19
Dependent Claim
31 words
A method of treating congestive heart failure comprising administering to a human in need of such treatment an amount of a compound of claim 1 effective to treat congestive heart failure.
Claim 20
Dependent Claim
27 words
A method of claim 18 wherein the compound is selected from: N-[2-acetylthiomethyl-3-(2-methylphenyl)propionyl]-methionine ethyl ester; N-[2-acetylthiomethyl-3-(2-methylphenyl)propionyl]-methionine; N-[2-mercaptomethyl-3-(2-methylphenyl)propionyl]-methionine: N-[2-mercaptomethyl-3-(4-methylphenyl)propionyl]-methionine; N-[2-acetylthiomethyl-3-(2-methylphenyl)propionyl]-methionine methyl ester; N-[2-acetylthiomethyl-3-(4-methylphenyl)propionyl]-methionine methyl ester; and N-[2-acetylthiomethyl-3-(3-methylphenyl)propionyl]-methionine ethyl ester.
Claim 21
Dependent Claim
12 words
A method of claim 16 wherein the compound is N-[2(S)-acetylthiomethyl-3-(2-methylphenyl)propionyl]-(S)-methionine ethyl ester.
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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) | 1993-05-28 | 1993-11-27 | 1994-05-29 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-05-28 | 1997-11-27 | 1998-05-29 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-05-28 | 2001-11-27 | 2002-05-29 | $7700.00 | Window Closed / Lapsed |