US4500467A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Benzoylthio compounds, their preparation and their use as drugs
Assignee: BASF SE
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Filing: 1983-11-21
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Granted: 1985-02-19
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Expires: 2003-11-21
Abstract
Abstract Benzoylthio compounds of the formula I ##STR1## where R 1 and R 3 are identical or different and are each hydrogen or C 1 -C 4 -alkyl, R 2 and R 4 are identical or different and are each hydrogen or C 1 -C 6 -alkyl which is unsubstituted or substituted by hydroxyl, mercapto, C 1 -C 4 -alkylthio, a carboxylic ester group, carboxamido or acylamino or are each an aryl, hetaryl, arylalkylene or hetarylalkylene radical which is unsubstituted or substituted in the aryl moiety by hydroxyl, C 1 -C 4 -alkoxy, arylalkoxy or halogen, R 1 and R 2 and/or R 3 and R 4 together may furthermore be a radical --(CH 2 ) p -- (p=2, 3, 4), --CH 2 --S--CH 2 -- or --CH 2 --C 6 H 4 --CH 2 --(ortho), X is NH or sulfur, m and n are identical or different and are each 0 or 1, and q is 0 or 1 where X is S, and is 0 where X is NH, and their salts with physiologically tolerated bases, their preparation, drugs containing these compounds and the use of these drugs in treating disorders.
Inventors
- 👤 Hugo Kubinyi
- 👤 Martin Traut
- 👤 Josef Gries
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 14:54
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/08; C07K5/0802; C07K5/0804; C07K5/0806; A; A61; A61P; A61P43/00; A61P9/00; A61P9/12; C07C; C07C327/00; C07D; C07D205/00; C07D205/02; C07D205/04; C07D209/00; C07D209/02; C07D209/04; C07D209/10; C07D209/18; C07D209/20; C07D211/00; C07D211/04; C07D211/06; C07D211/36; C07D211/60; C07D217/00; C07D217/22; C07D217/26; C07D277/00; C07D277/02; C07D277/04; C07D277/06; C07K5/06; C07K5/06008; C07K5/06017; C07K5/06026; C07K5/06034; C07K5/06052; C07K5/0606; C07K5/06078; C07K5/06139; C07K5/06156; C07K5/06165
Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
183 words
An angiotensin converting enzyme inhibitor which is selected from the group consisting of benzoylthio compounds of the formula ##STR7## wherein R 1 and R 3 are identical or different and are each hydrogen or C 1 -C 4 alkyl; R 2 and R 4 are identical or different and are each hydrogen; C 1 -C 6 alkyl which is unsubstituted or substituted by hydroxyl, mercapto, C 1 -C 4 alkylthio, a carboxylic ester group, carboxamido, or acylamino; aryl; hetaryl; arylakylene; or hetarylalkylene radical which is unsubstituted or substituted in the aryl moiety by hydroxyl, C 1 -C 4 alkoxy, arylalkoxy, or halogen; with the proviso that R 1 and R 4 together or R 3 and R 4 together may furthermore be a radical selected from --(CH 2 ) p --, wherein p is 2-4, --CH 2 --S--CH 2 --, or ortho--CH 2 --C 6 H 4 --CH 2 --; X is NH or sulfur; m and n are identical or different and are each 0 or 1; and q is 0; or a salt of said inhibitor with a physiologically acceptable base.
Claim 2
Dependent Claim
183 words
An angiotensin converting enzyme inhibitor which is selected from the group consisting of benzoylthio compounds of the formula ##STR7## wherein R 1 and R 3 are identical or different and are each hydrogen or C 1 -C 4 alkyl; R 2 and R 4 are identical or different and are each hydrogen; C 1 -C 6 alkyl which is unsubstituted or substituted by hydroxyl, mercapto, C 1 -C 4 alkylthio, a carboxylic ester group, carboxamido, or acylamino; aryl; hetaryl; arylakylene; or hetarylalkylene radical which is unsubstituted or substituted in the aryl moiety by hydroxyl, C 1 -C 4 alkoxy, arylalkoxy, or halogen; with the proviso that R 1 and R 4 together or R 3 and R 4 together may furthermore be a radical selected from --(CH 2 ) p --, wherein p is 2-4, --CH 2 --S--CH 2 --, or ortho--CH 2 --C 6 H 4 --CH 2 --; X is NH or sulfur; m and n are identical or different and are each 0 or 1; and q is 0; or a salt of said inhibitor with a physiologically acceptable base.
Claim 3
Dependent Claim
101 words
The inhibitor of claim 1, wherein R 1 and R 3 are each hydrogen; R 2 is hydrogen, C 1 -C 4 alkyl, benzyl, naphthylmethylene, or indol-3-ylmethylene; R 4 is C 1 -C 4 alkyl, benzyl, or indol-3-ylmethylene; with the proviso that R 1 and R 2 together or R 3 and R 4 together may furthermore be --(CH 2 ) 3 -- or --CH 2 --S--CH 2 --; X is sulfur; and n and m are identical or different and are each 0 or 1, and q is 0, or a salt of said inhibitor with a physiologically acceptable base.
Claim 4
Dependent Claim
93 words
The inhibitor of claim 1 wherein R 4 is hydrogen, C 1 -C 4 alkyl, benzyl or indol-3-ylmethylene, and R 2 is an alkyl group selected from the group consisting of methyl, ethyl, propyl, isopropyl, n-butyl, isobutyl, and sec-butyl; said alkyl group being optionally substituted with a substituent selected from the group consisting of methylthio, ethylthio, methoxycarbonyl, ethoxycarbonyl, benzyloxycarbonyl, formamido, acetamido, benzamido, and benzyloxycarbamido; or R 2 is an aryl, hetaryl, alkylalkylene or an hetarylalkylene group selected from the group consisting of phenyl, naphthyl, thienyl, pyrrolyl, benzyl, naphthylmethylene, indolylmethylene, pyrrolylmethylene, imidazoylmethylene, and thienylmethylene.
Claim 5
Dependent Claim
24 words
A therapeutic composition comprising a pharmaceutical excipient and an antihypertension effective amount of a benzoylthio compound according to claim 1 as the active compound.
Claim 6
Dependent Claim
24 words
The method of treating hypertension in a patient suffering therefrom, which comprises administering an effective amount of a benzoylthio compound according to 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) | 1988-02-19 | 1988-08-20 | 1989-02-19 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-02-19 | 1992-08-20 | 1993-02-19 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-02-19 | 1996-08-20 | 1997-02-19 | $7700.00 | Window Closed / Lapsed |