US5162362A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Octahydroindole-2-carboxylic acids
Assignee: Sanofi Aventis Deutschland GmbH
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Filing: 1983-12-27
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Granted: 1992-11-10
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Expires: 2003-12-27
Abstract
Abstract What are disclosed are aminoacid compounds of the formula ##STR1## wherein n is 0 or 1, and salts thereof, said compounds and salts having hypotensive properties; methods for making the compounds; pharmaceutical compositions containing the compounds or salts; and use of the compounds and salts for treating hypertension.
Inventors
- 👤 Rolf Geiger
- 👤 Volker Teetz
- 👤 Hansjorg Urbach
- 👤 Bernward Scholkens
- 👤 Rainer Henning
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 03:43
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/02; C07K5/022; C07K5/0222; C07D; C07D217/00; C07D217/22; C07D217/26; A; A61; A61K; A61K38/00
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
174 words
A compound of the formula or a physiologically tolerated salt thereof, wherein R 1 is (a) (C 1 -C 6 )-alkyl or (b) (C 1 -C 6 )-alkyl substituted by 1) (C 5 -C 7 )-cycloalkyl 2) amino, 3) (C 1 -C 6 )-alkoxycarbonylamino, 4) (C 1 -C 6 )-alkanoylamino, or 5) (C 1 -C 6 )-alkoxyphenyl; R 2 is (a) (C 1 -C 6 )-alkyl, (b) (C 1 -C 6 )-alkyl substituted by 1) (C 5 -C 7 )-cycloalkyl, 2) phenoxy, 3) phenoxy substituted by 3.1 halogen, 3.2 methyl, or 3.3 methoxy, 4) amino, 5) (C 1 -C 6 )-alkylureido, 6) cyclohexylureido, 7) phenylureido, 8) (C 1 -C 6 )-alkylmercapto, (C 1 -C 6 )-alkylsulfinyl, or (C 1 -C 6 )-alkylsulfonyl, 9) phenylmercapto, phenylsulfinyl, or phenylsulfonyl, 10) benzylmercapto, benzylsulfinyl, or benzylsulfonyl, 11) a heterocycle selected from the group consisting of indole, imidazole, pyrrole, pyrazole, thiophene, thiazole, or 12) such a heterocycle substituted by 12.1 halogen, 12.2 methyl, or 12.3 amino; and wherein R 3 is hydrogen, (C 1 -C 6 )-alkyl, or benzyl.
Claim 2
Dependent Claim
174 words
A compound of the formula or a physiologically tolerated salt thereof, wherein R 1 is (a) (C 1 -C 6 )-alkyl or (b) (C 1 -C 6 )-alkyl substituted by 1) (C 5 -C 7 )-cycloalkyl 2) amino, 3) (C 1 -C 6 )-alkoxycarbonylamino, 4) (C 1 -C 6 )-alkanoylamino, or 5) (C 1 -C 6 )-alkoxyphenyl; R 2 is (a) (C 1 -C 6 )-alkyl, (b) (C 1 -C 6 )-alkyl substituted by 1) (C 5 -C 7 )-cycloalkyl, 2) phenoxy, 3) phenoxy substituted by 3.1 halogen, 3.2 methyl, or 3.3 methoxy, 4) amino, 5) (C 1 -C 6 )-alkylureido, 6) cyclohexylureido, 7) phenylureido, 8) (C 1 -C 6 )-alkylmercapto, (C 1 -C 6 )-alkylsulfinyl, or (C 1 -C 6 )-alkylsulfonyl, 9) phenylmercapto, phenylsulfinyl, or phenylsulfonyl, 10) benzylmercapto, benzylsulfinyl, or benzylsulfonyl, 11) a heterocycle selected from the group consisting of indole, imidazole, pyrrole, pyrazole, thiophene, thiazole, or 12) such a heterocycle substituted by 12.1 halogen, 12.2 methyl, or 12.3 amino; and wherein R 3 is hydrogen, (C 1 -C 6 )-alkyl, or benzyl.
Claim 3
Dependent Claim
10 words
A compound as in claim 1 which is N-(1-S-carboethoxy-2-phenoxy-ethyl)-S-alanyl-octahydroindole-2-S-carboxylic acid.
Claim 4
Dependent Claim
10 words
A compound as in claim 1 which is N-[1-S-carboethoxy-3-(3-indolyl)-propyl]-S-alanyl-octahydroindole-2-S-carboxylic acid.
Claim 5
Dependent Claim
10 words
A compound as in claim 1 which is N-[1-S-carboethoxy-3-(3-indolyl)-ethyl]-S-alanyl-octahydroindole-2-S-carboxylic acid.
Claim 6
Dependent Claim
10 words
A compound as in claim 1 which is N-[1-S-carboethoxy-3-(2-thienyl)-propyl]-S-alanyl-octahydroindole-2-S-carboxylic acid.
Claim 7
Dependent Claim
10 words
A compound as in claim 1 which is N-(1-S-carboethoxy-2-phenylthioethyl)-S-alanyl-octahydroindole-2-S-carboxylic acid.
Claim 8
Dependent Claim
30 words
A pharmaceutical preparation for the treatment of hypertension, said preparation comprising a hypotensively effective amount of a compound or salt as in claim 1 and a pharmaceutically acceptable carrier therefor.
Claim 9
Dependent Claim
32 words
A method for treating hypertension in a patient suffering therefrom, which method comprises orally, intravenously, or subcutaneously administering to said patient a hypotensively effective amount of a compound as in claim 1.
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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) | 1995-11-10 | 1996-05-11 | 1996-11-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1999-11-10 | 2000-05-11 | 2000-11-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2003-11-10 | 2004-05-11 | 2004-11-10 | $7700.00 | Window Closed / Lapsed |