US4255432A
Expired / Lapsed
US
⏱️ 0.0 years remaining
8-[2-3-Indolyl)ethyl]-1-oxa-3-,8-diazaspiro[4.5]decan-2-ones, pharmaceutical compositions thereof and methods of use thereof
Assignee: Syntex USA LLC
•
Filing: 1979-09-06
•
Granted: 1981-03-10
•
Expires: 1999-09-06
Abstract
Abstract Compounds of the formula ##STR1## wherein R 1 , R 2 and R 3 are the same or different and are hydrogen, C 1 to C 6 alkyl, C 6 to C 12 carbocyclic aryl or aralkyl of 1 to 6 carbon atoms in the alkyl moiety and 6 to 12 carbon atoms in the carbocyclic aryl moiety; R 4 and R 5 are the same or different and are hydrogen or C 1 to C 6 alkyl; and R 6 and R 7 are the same or different and are hydrogen, C 1 to C 6 alkyl or C 1 to C 6 alkoxy. Methods for preparing these compounds are also disclosed. The compounds are useful as antihypertensives and as diuretics. They also function as antihistamines and as bronchodilating agents and are therefore effective in inhibiting the effects of allergic reactions. They are also of use in the treatment of migraine and in the treatment of vasospastic disorders.
Inventors
- 👤 Arthur F. Kluge
- 👤 Arthur M. Strosberg
- 👤 Stefan H. Unger
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-28 21:30
CPC Classifications
C; C07; C07D; C07D211/00; C07D211/04; C07D211/06; C07D211/36; C07D211/40; C07D211/44; C07D211/48
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
48 words
A compound chosen from those represented by the formula ##STR6## wherein R 1 is C 1 to C 6 alkyl and R 6 and R 7 are the same or different and are hydrogen or C 1 to C 6 alkoxy and the pharmaceutically acceptable, non-toxic salts thereof.
Claim 2
Dependent Claim
48 words
A compound chosen from those represented by the formula ##STR6## wherein R 1 is C 1 to C 6 alkyl and R 6 and R 7 are the same or different and are hydrogen or C 1 to C 6 alkoxy and the pharmaceutically acceptable, non-toxic salts thereof.
Claim 3
Dependent Claim
24 words
The compound of claim 1 wherein R 1 is hydrogen, methyl, ethyl, i-propyl, n-propyl, or n-butyl and R 6 and R 7 are hydrogen.
Claim 4
Dependent Claim
12 words
The compound in accordance with claim 2 wherein R 1 is methyl.
Claim 5
Independent Claim
66 words
A method for relieving the symptoms of hypertension which comprises administering to an individual afflicted with such, an anti-hypertensive effective amount of a compound of the formula: ##STR7## wherein R 1 is C 1 to C 6 alkyl and R 6 and R 7 are the same or different and are hydrogen or C 1 to C 6 alkoxy and the pharmaceutically acceptable, non-toxic salts thereof.
Claim 6
Independent Claim
66 words
A method for relieving the symptoms of hypertension which comprises administering to an individual afflicted with such, an anti-hypertensive effective amount of a compound of the formula: ##STR7## wherein R 1 is C 1 to C 6 alkyl and R 6 and R 7 are the same or different and are hydrogen or C 1 to C 6 alkoxy and the pharmaceutically acceptable, non-toxic salts thereof.
Claim 7
Dependent Claim
66 words
A pharmaceutical composition useful for relieving the symptoms of hypertension which comprises a pharmaceutically acceptable carrier and an anti-hypertensive effective amount of the compound of the formula: ##STR8## wherein R 1 is C 1 to C 6 alkyl and R 6 and R 7 are the same or different and are hydrogen or C 1 to C 6 alkoxy and the pharmaceutically acceptable, non-toxic salts thereof.
Claim 8
Dependent Claim
66 words
A pharmaceutical composition useful for relieving the symptoms of hypertension which comprises a pharmaceutically acceptable carrier and an anti-hypertensive effective amount of the compound of the formula: ##STR8## wherein R 1 is C 1 to C 6 alkyl and R 6 and R 7 are the same or different and are hydrogen or C 1 to C 6 alkoxy and the pharmaceutically acceptable, non-toxic salts thereof.
Claim 9
Independent Claim
62 words
A method useful for inhibiting the effects of allergic reaction which comprises administering an anti-allergic effective amount of a compound of the formula: ##STR9## wherein R 1 is C 1 to C 6 alkyl and R 6 and R 7 are the same or different and are hydrogen or C 1 to C 6 alkoxy and the pharmaceutically acceptable, non-toxic salts thereof.
Claim 10
Independent Claim
62 words
A method useful for inhibiting the effects of allergic reaction which comprises administering an anti-allergic effective amount of a compound of the formula: ##STR9## wherein R 1 is C 1 to C 6 alkyl and R 6 and R 7 are the same or different and are hydrogen or C 1 to C 6 alkoxy and the pharmaceutically acceptable, non-toxic salts thereof.
Claim 11
Dependent Claim
67 words
A pharmaceutical composition useful for inhibiting the effects of allergic reactions which comprises a pharmaceutically acceptable carrier and an anti-allergic effective amount of a compound of the formula: ##STR10## wherein R 1 is C 1 to C 6 alkyl and R 6 and R 7 are the same or different and are hydrogen or C 1 to C 6 alkoxy and the pharmaceutically acceptable, non-toxic salts thereof.
Claim 12
Dependent Claim
67 words
A pharmaceutical composition useful for inhibiting the effects of allergic reactions which comprises a pharmaceutically acceptable carrier and an anti-allergic effective amount of a compound of the formula: ##STR10## wherein R 1 is C 1 to C 6 alkyl and R 6 and R 7 are the same or different and are hydrogen or C 1 to C 6 alkoxy and the pharmaceutically acceptable, non-toxic salts thereof.
Claim 13
Independent Claim
60 words
A method for the treatment of vasospastic disorders which comprises administering an anti-vasospastic effective amount of the compound of the formula: ##STR11## wherein R 1 is C 1 to C 6 alkyl and R 6 and R 7 are the same or different and are hydrogen or C 1 to C 6 alkoxy and the pharmaceutically acceptable, non-toxic salts thereof.
Claim 14
Independent Claim
60 words
A method for the treatment of vasospastic disorders which comprises administering an anti-vasospastic effective amount of the compound of the formula: ##STR11## wherein R 1 is C 1 to C 6 alkyl and R 6 and R 7 are the same or different and are hydrogen or C 1 to C 6 alkoxy and the pharmaceutically acceptable, non-toxic salts thereof.
Claim 15
Dependent Claim
65 words
A pharmaceutical composition useful for treating vaso spastic disorders which comprises a pharmaceutically acceptable carrier and an anti-vasospastic effective amount of the compound of the formula: ##STR12## wherein R 1 is C 1 to C 6 alkyl and R 6 and R 7 are the same or different and are hydrogen or C 1 to C 6 alkoxy and the pharmaceutically acceptable, non-toxic salts thereof.
Claim 16
Dependent Claim
65 words
A pharmaceutical composition useful for treating vaso spastic disorders which comprises a pharmaceutically acceptable carrier and an anti-vasospastic effective amount of the compound of the formula: ##STR12## wherein R 1 is C 1 to C 6 alkyl and R 6 and R 7 are the same or different and are hydrogen or C 1 to C 6 alkoxy and the pharmaceutically acceptable, non-toxic salts thereof.
Claim 17
Independent Claim
58 words
A method for treatment of migraine which comprises administering an anti-migraine effective amount of the compound of the formula: ##STR13## wherein R 1 is C 1 to C 6 alkyl and R 6 and R 7 are the same or different and are hydrogen or C 1 to C 6 alkoxy and the pharmaceutically acceptable, non-toxic salts thereof.
Claim 18
Independent Claim
58 words
A method for treatment of migraine which comprises administering an anti-migraine effective amount of the compound of the formula: ##STR13## wherein R 1 is C 1 to C 6 alkyl and R 6 and R 7 are the same or different and are hydrogen or C 1 to C 6 alkoxy and the pharmaceutically acceptable, non-toxic salts thereof.
Claim 19
Dependent Claim
63 words
A pharmaceutical composition useful for treating migraine which comprises a pharmaceutically acceptable carrier and an anti-migraine effective amount of a compound of the formula: ##STR14## wherein R 1 is C 1 to C 6 alkyl and R 6 and R 7 are the same or different and are hydrogen or C 1 to C 6 alkoxy and the pharmaceutically acceptable, non-toxic salts thereof.
Claim 20
Dependent Claim
63 words
A pharmaceutical composition useful for treating migraine which comprises a pharmaceutically acceptable carrier and an anti-migraine effective amount of a compound of the formula: ##STR14## wherein R 1 is C 1 to C 6 alkyl and R 6 and R 7 are the same or different and are hydrogen or C 1 to C 6 alkoxy and the pharmaceutically acceptable, non-toxic salts thereof.
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) | 1984-03-09 | 1984-09-08 | 1985-03-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-03-09 | 1988-09-08 | 1989-03-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-03-09 | 1992-09-08 | 1993-03-10 | $7700.00 | Window Closed / Lapsed |