US4426391A
Expired / Lapsed
US
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[(Alkoxycarbonyl)oxy]alkyl esters of methyldopa
Assignee: Merck and Co Inc
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Filing: 1982-09-15
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Granted: 1984-01-17
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Expires: 2002-09-15
Abstract
Abstract Novel prodrugs of methyldopa which are [(alkoxycarbonyl)oxy]alkyl esters of methyldopa are disclosed. Also, pharmaceutical compositions containing these compounds are disclosed. Upon administration to warm-blooded animals, these prodrugs liberate methyldopa along with innocuous side products.
Inventors
- 👤 Jose Alexander
- 👤 Chung Shih
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 11:49
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/21; A61K31/215; A61K31/235; A61K31/24
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
42 words
A compound of the formula: ##STR3## wherein R 1 and R 2 are independently hydrogen or alkyl having from 1 to 10 carbon atoms; R 3 is alkyl having from 1-10 carbon atoms or a non-toxic pharmaceutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim
42 words
A compound of the formula: ##STR3## wherein R 1 and R 2 are independently hydrogen or alkyl having from 1 to 10 carbon atoms; R 3 is alkyl having from 1-10 carbon atoms or a non-toxic pharmaceutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim
37 words
A compound of the formula: ##STR4## wherein R 1 and R 2 are independently hydrogen or methyl R 3 is alkyl having from 1 to 5 carbon atoms or a non-toxic pharmaceutically acceptable acid addition salt thereof.
Claim 4
Dependent Claim
37 words
A compound of the formula: ##STR4## wherein R 1 and R 2 are independently hydrogen or methyl R 3 is alkyl having from 1 to 5 carbon atoms or a non-toxic pharmaceutically acceptable acid addition salt thereof.
Claim 5
Dependent Claim
12 words
A compound of claim 1 which is [(3-Methyl-1-butyloxycarbonyl)oxy]methyl (3,4-dihydroxyphenyl)-2-methylalanine ester acetate salt.
Claim 6
Independent Claim
63 words
A method of treating hypertension which comprises administering to a patient in need of such treatment a pharmaceutically effective amount of a compound of the formula: ##STR5## wherein R 1 and R 2 are independently hydrogen or alkyl having up to 10 carbon atoms; R 3 is alkyl having 1 to 10 carbon atoms or a pharmaceutically acceptable non-toxic acid addition salt thereof.
Claim 7
Independent Claim
63 words
A method of treating hypertension which comprises administering to a patient in need of such treatment a pharmaceutically effective amount of a compound of the formula: ##STR5## wherein R 1 and R 2 are independently hydrogen or alkyl having up to 10 carbon atoms; R 3 is alkyl having 1 to 10 carbon atoms or a pharmaceutically acceptable non-toxic acid addition salt thereof.
Claim 8
Dependent Claim
52 words
An antihypertensive pharmaceutical composition comprising an effective amount of a compound of the formula: ##STR6## wherein R 1 and R 2 are independently hydrogen or alkyl having up to 10 carbon atoms; R 3 is alkyl having from 1 to 10 carbon atoms or a non-toxic pharmaceutically acceptable acid addition salt thereof.
Claim 9
Dependent Claim
52 words
An antihypertensive pharmaceutical composition comprising an effective amount of a compound of the formula: ##STR6## wherein R 1 and R 2 are independently hydrogen or alkyl having up to 10 carbon atoms; R 3 is alkyl having from 1 to 10 carbon atoms or a non-toxic pharmaceutically acceptable acid addition salt thereof.
References Cited (Backward Citations)
US3939270A
Cited
US3983138A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-01-16 | 1987-07-18 | 1988-01-17 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-01-16 | 1991-07-18 | 1992-01-17 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-01-16 | 1995-07-18 | 1996-01-17 | $7700.00 | Window Closed / Lapsed |