Patent US4350704A successfully refreshed from Google Patents.
US4350704A
Expired / Lapsed
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Substituted acyl derivatives of octahydro-1H-indole-2-carboxylic acids
Assignee: Warner Lambert Co LLC
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Filing: 1981-02-17
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Granted: 1982-09-21
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Expires: 2001-02-17
Abstract
Abstract Substituted acyl derivatives of octahydro-1H-indole-2-carboxylic acid and the pharmaceutically acceptable salts thereof are produced by acylating a suitably substituted octahydro-1H-indole with a suitably activated substituted carboxylic acid and when desired hydrolyzing the resulting product. The compounds of the invention, their salts and pharmaceutical compositions thereof are useful as antihypertensive agents.
Inventors
- 👤 Milton L. Hoefle
- 👤 George Bobowski
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 04:45
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/02; C07K5/022; C07K5/0222; C07D; C07D209/00; C07D209/02; C07D209/04; C07D209/30; C07D209/42; A; A61; A61K; A61K38/00
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
90 words
A octahydro-1-(ω-mercaptoalkanoyl)-1H-indole-2-carboxylic acid compound having the formula ##STR25## wherein R is hydrogen or lower alkyl; R 1 is hydrogen, lower alkyl, or benzyl; R 2 is hydrogen or ##STR26## where R 3 is lower alkyl, phenyl, substituted phenyl having 1 or 2 substituents selected from the group consisting of fluorine, chlorine, bromine, lower alkyl or alkoxy; and n is 0 or 1; wherein lower alkyl and lower alkoxy include straight or branched groups having 1 to 4 carbon atoms and pharmaceutically acceptable salts of the compounds when R is hydrogen.
Claim 2
Dependent Claim
90 words
A octahydro-1-(ω-mercaptoalkanoyl)-1H-indole-2-carboxylic acid compound having the formula ##STR25## wherein R is hydrogen or lower alkyl; R 1 is hydrogen, lower alkyl, or benzyl; R 2 is hydrogen or ##STR26## where R 3 is lower alkyl, phenyl, substituted phenyl having 1 or 2 substituents selected from the group consisting of fluorine, chlorine, bromine, lower alkyl or alkoxy; and n is 0 or 1; wherein lower alkyl and lower alkoxy include straight or branched groups having 1 to 4 carbon atoms and pharmaceutically acceptable salts of the compounds when R is hydrogen.
Claim 3
Dependent Claim
57 words
A substituted octahydro-1-(3-mercaptoalkanoyl)-1H-indole-2-carboxylic acid compound according to claim 1 having the formula ##STR27## and pharmaceutically acceptable salts thereof; where R 1 is hydrogen, or lower alkyl having 1 to 3 carbon atoms; R 2 is hydrogen or ##STR28## where R 3 is lower alkyl having 1 to 3 carbon atoms, phenyl, and n is 0 or 1.
Claim 4
Dependent Claim
35 words
A substituted octahydro-1-(3-mercaptopropanoyl)-1H-indole-2-carboxylic acid compound according to claim 2 wherein R 1 is hydrogen or methyl; R 2 is hydrogen or ##STR29## where R 3 is methyl, or phenyl and pharmaceutically acceptable basic salts thereof.
Claim 5
Dependent Claim
16 words
The compound according to claim 3 which is octahydro-1-[3-(acetylthio)-2-methylpropanoyl]-1H-indole-2-carboxylic acid and pharmaceutically acceptable basic salts thereof.
Claim 6
Dependent Claim
16 words
The compound according to claim 3 which is octahydro-1-(3-mercapto-2-methylpropanoyl)-1H-indole-2-carboxylic acid and pharmaceutically acceptable basic salts thereof.
Claim 7
Dependent Claim
17 words
The compound according to claim 5 which is (2α,3aβ,7aβ)-octahydro-1-(3-mercapto-2-methylpropanoyl)-1H-indole-2-carboxylic acid and the pharmaceutically acceptable basic salts thereof.
Claim 8
Dependent Claim
19 words
The compond according to claim 6 which is (2α,3aβ,7aβ)-octahydro-1-(3-mercapto-2-methylpropanoyl)-1H-indole-2-carboxylic acid, diastereomer A and the pharmaceutically acceptable basic salts thereof.
Claim 9
Dependent Claim
19 words
The compound according to claim 6 which is (1)-(2α,3aβ,7aβ)-octahydro-1-(3-mercapto-2-methylpropanoyl)-1H-indole-2-carboxylic acid, diastereomer A and the pharmaceutically acceptable basic salts thereof.
Claim 10
Dependent Claim
16 words
The compound according to claim 3 which is octahydro-1-(3-mercaptopropanoyl)-1H-indole-2-carboxylic acid and pharmaceutically acceptable basic salts thereof.
Claim 11
Dependent Claim
16 words
The compound according to claim 3 which is octahydro-1-[3-(acetylthio)propanoyl]-1H-indole-2-carboxylic acid and pharmaceutically acceptable basic salts thereof.
Claim 12
Dependent Claim
25 words
A hypertensive pharmaceutical composition comprising a substituted octahydro-1-(3-mercaptoalkanoyl)1-indole-2-carboxylic acid compound according to claim 1 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
Claim 13
Dependent Claim
26 words
A method of treating hypertension by administering an effective amount of a substituted octahydro-1-(3-mercaptoalkanoyl)-1-indole-2-carboxylic acid compound according to claim 1 or a pharmaceutically acceptable salt thereof.
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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) | 1985-09-20 | 1986-03-22 | 1986-09-21 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-09-20 | 1990-03-22 | 1990-09-21 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-09-20 | 1994-03-22 | 1994-09-21 | $7700.00 | Window Closed / Lapsed |