US4316896A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Aminoacid derivatives as antihypertensives
Assignee: Merck and Co Inc
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Filing: 1978-09-07
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Granted: 1982-02-23
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Expires: 1998-09-07
Abstract
Abstract The invention relates to new phosphoryl aminoacid derivatives and related compounds which are useful as antihypertensives.
Inventors
- 👤 Eugene D. Thorsett
- 👤 Arthur A. Patchett
- 👤 Elbert E. Harris
- 👤 Alan L. Maycock
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-25 21:14
CPC Classifications
C; C07; C07F; C07F9/00; C07F9/02; C07F9/06; C07F9/08; C07F9/09; C07F9/091; A; A61; A61K; A61K31/00; A61K31/66; A61P; A61P9/00; A61P9/12; C07F9/16; C07F9/165; C07F9/1651; C07F9/22; C07F9/24; C07F9/2454; C07F9/2458; C07F9/547; C07F9/553; C07F9/572; C07F9/6536; C07F9/6539; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06191; A61K38/00
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
145 words
A compound of the formula: ##STR14## wherein n is 0 or 1 R is lower alkyl, phenyl lower alkyl, hydroxyphenyl lower alkyl, hydroxy lower alkyl, aminoloweralkyl, guanidino lower alkyl, imidazoyl lower alkyl, indolyl lower alkyl, mercapto lower alkyl, lower alkyl mercapto lower alkyl; R 3 and R 4 may be connected together to form an alkylene bridge of from 2 to 4 carbon atoms or an alkylene bridge of from 2 to 3 carbon atoms and one sulfur atom; X is NR 5 , S where R 5 =H or lower alkyl; R 1 is hydrogen, lower alkyl, phenyl lower alkyl or phenyl or substituted phenyl wherein the substituent is halo, lower alkoxy or lower alkyl; R 2 is hydrogen, lower alkyl, phenyl lower alkyl, or phenyl or substituted phenyl wherein the substituent is halo, lower alkoxy or lower alkyl and pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
145 words
A compound of the formula: ##STR14## wherein n is 0 or 1 R is lower alkyl, phenyl lower alkyl, hydroxyphenyl lower alkyl, hydroxy lower alkyl, aminoloweralkyl, guanidino lower alkyl, imidazoyl lower alkyl, indolyl lower alkyl, mercapto lower alkyl, lower alkyl mercapto lower alkyl; R 3 and R 4 may be connected together to form an alkylene bridge of from 2 to 4 carbon atoms or an alkylene bridge of from 2 to 3 carbon atoms and one sulfur atom; X is NR 5 , S where R 5 =H or lower alkyl; R 1 is hydrogen, lower alkyl, phenyl lower alkyl or phenyl or substituted phenyl wherein the substituent is halo, lower alkoxy or lower alkyl; R 2 is hydrogen, lower alkyl, phenyl lower alkyl, or phenyl or substituted phenyl wherein the substituent is halo, lower alkoxy or lower alkyl and pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
38 words
A compound of claim 1 wherein R 3 and R 4 are joined to form ##STR15## wherein Y is CH 2 or S; X is NR 5 and R is lower alkyl or phenyl (C 1-4 )lower alkyl.
Claim 4
Dependent Claim
14 words
A compound of claim 2 wherein R is methyl, X is NH and n=0.
Claim 5
Dependent Claim
15 words
A compound of claim 3 having the formula ##STR16## and the pharmaceutically acceptable salts thereof.
Claim 6
Dependent Claim
15 words
A compound of claim 3 having the formula ##STR17## and the pharmaceutically acceptable salts thereof.
Claim 7
Dependent Claim
15 words
A compound of claim 3 having the formula: ##STR18## and the pharmaceutically acceptable salts thereof.
Claim 8
Dependent Claim
15 words
A compound of claim 3 having the formula: ##STR19## and the pharmaceutically acceptable salts thereof.
Claim 9
Dependent Claim
12 words
A compound of claim 3 with X=NH of the L-amino acid configurations.
Claim 10
Dependent Claim
22 words
A pharmaceutical composition for treating hypertension comprising a pharmaceutically acceptable carrier and an antihypertensively effective amount of a compound of claim 1.
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) | 1985-02-22 | 1985-08-24 | 1986-02-23 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-02-22 | 1989-08-24 | 1990-02-23 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-02-22 | 1993-08-24 | 1994-02-23 | $7700.00 | Window Closed / Lapsed |