US4355037A
Expired / Lapsed
US
⏱️ 0.0 years remaining
3-(4-Piperidyl)-1,2-benzisoxales
Assignee: Aventis Pharmaceuticals Inc
•
Filing: 1981-11-12
•
Granted: 1982-10-19
•
Expires: 2001-11-12
Abstract
Abstract Novel 3-(4-piperidyl)-1,2-benzisoxazoles, intermediates and processes for the preparation thereof, and methods for alleviating pain utilizing compounds or compositions thereof are disclosed.
Inventors
- 👤 Joseph T. Strupczewski
- 👤 Beth Ann Gardner
- 👤 Richard C. Allen
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 23:46
CPC Classifications
C; C07; C07D; C07D413/00; C07D413/02; C07D413/04; A; A61; A61P; A61P25/00; A61P25/04; C07D211/00; C07D211/04; C07D211/06; C07D211/08; C07D211/18; C07D211/26; C07D211/28; C07D211/30; C07D211/32; C07D211/36; C07D211/60; C07D211/62
Claims Analysis
Total Claims: 44
Claim 1
Independent Claim
74 words
A compound of the formula ##STR13## wherein R is hydrogen, loweralkyl, loweralkenyl, cycloalkylloweralkyl, phenyloweralkyl, hydroxy, diloweralkylaminoloweralkyl, cyano, cyanomethyl, ##STR14## or a group of the formula ##STR15## wherein R 1 is hydrogen, loweralkyl or a group of the formula OR 2 wherein R 2 is phenyl or benzyl; X is hydrogen, loweralkyl, loweralkoxy, halogen or hydroxy; m is 1 or 2; the geometrical isomers and optical antipodes thereof; or the pharmaceutically acceptable acid addition thereof.
Claim 2
Dependent Claim
74 words
A compound of the formula ##STR13## wherein R is hydrogen, loweralkyl, loweralkenyl, cycloalkylloweralkyl, phenyloweralkyl, hydroxy, diloweralkylaminoloweralkyl, cyano, cyanomethyl, ##STR14## or a group of the formula ##STR15## wherein R 1 is hydrogen, loweralkyl or a group of the formula OR 2 wherein R 2 is phenyl or benzyl; X is hydrogen, loweralkyl, loweralkoxy, halogen or hydroxy; m is 1 or 2; the geometrical isomers and optical antipodes thereof; or the pharmaceutically acceptable acid addition thereof.
Claim 3
Dependent Claim
14 words
A compound according to claim 1 wherein R is hydrogen, loweralkyl, loweralkenyl or cycloalkylloweralkyl.
Claim 4
Dependent Claim
12 words
A compound according to claim 2 wherein R is loweralkenyl or cycloalkylloweralkyl.
Claim 5
Dependent Claim
10 words
A compound according to claim 1 wherein R is phenylloweralkyl.
Claim 6
Dependent Claim
12 words
A compound according to claim 1 wherein R is hydroxy or ##STR16##
Claim 7
Dependent Claim
10 words
A compound according to claim 1 wherein R is diloweralkylaminoalkyl.
Claim 8
Dependent Claim
12 words
A compound according to claim 1 wherein R is cyano or cyanomethyl.
Claim 9
Dependent Claim
36 words
A compound according to claim 1 wherein R is a group of the formula ##STR17## wherein R 1 is hydrogen, loweralkyl or a group of the formula OR 2 wherein R 2 is phenyl or benzyl.
Claim 10
Dependent Claim
8 words
The compound of claim 2 which is 3-(4-piperidyl)-6-fluoro-1,2-benzisoxazole.
Claim 11
Dependent Claim
8 words
The compound of claim 2 which is 5-methoxy-3-(4-piperidyl)-1,2-benzisoxazole.
Claim 12
Dependent Claim
8 words
The compound of claim 2 which is 5,6-dimethoxy-3-(4-piperidyl)-1,2-benzisoxazole.
Claim 13
Dependent Claim
8 words
The compound of claim 2 which is 5-fluoro-3-(4-piperidyl)-1,2-benzisoxazole.
Claim 14
Dependent Claim
8 words
The compound of claim 2 which is 6-methoxy-3-(4-piperidyl)-1,2-benzisoxazole.
Claim 15
Dependent Claim
8 words
The compound of claim 2 which is 3-(4-piperidyl)-6-chloro-1,2-benzisoxazole.
Claim 16
Dependent Claim
8 words
The compound of claim 2 which is 5-hydroxy-3-(4-piperidyl)-1,2-benzisoxazole.
Claim 17
Dependent Claim
8 words
The compound of claim 2 which is 3-(4-piperidyl)-1,2-benzisoxazole.
Claim 18
Dependent Claim
8 words
The compound of claim 2 which is 3-(1-methyl-4-piperidyl)-5-methyl-1,2-benzisoxazole.
Claim 19
Dependent Claim
8 words
The compound of claim 2 which is 4-fluoro-3-(1-methyl-4-piperidyl)-1,2-benzisoxazole.
Claim 20
Dependent Claim
8 words
The compound of claim 2 which is 3-(1-methyl-4-piperidyl)-1,2-benzisoxazole.
Claim 21
Dependent Claim
8 words
The compound of claim 3 which is 3-(1-allyl-4-piperidyl)-6-fluoro-1,2-benzisoxazole.
Claim 22
Dependent Claim
8 words
The compound of claim 3 which is 3-(1-allyl-4-piperidyl)-6-chloro-1,2-benzisoxazole.
Claim 23
Dependent Claim
8 words
The compound of claim 3 which is 3-(1-allyl-4-piperidyl)-1,2-benzisoxazole.
Claim 24
Dependent Claim
8 words
The compound of claim 4 which is 3-1-(cyclopropylmethyl-4-piperidyl)-1,2-benzisoxazole.
Claim 25
Dependent Claim
8 words
The compound of claim 4 which is 3[1-(β-phenylethyl)-4-piperidyl]-1,2-benzisoxazole.
Claim 26
Dependent Claim
8 words
The compound of claim 5 which is 3-[1-hydroxy-4-piperidyl]-1,2-benzisoxazole.
Claim 27
Dependent Claim
8 words
The compound of claim 5 which is 3-(1-benzoyloxy-4-piperidyl)-1,2-benzisoxazole.
Claim 28
Dependent Claim
8 words
The compound of claim 6 which is 3-[1-(3-dimethylaminopropyl)-4-piperidyl]-1,2-benzisoxazole.
Claim 29
Dependent Claim
8 words
The compound of claim 6 which is 3-[1-3-(diethylaminopropyl)-4-piperidyl]-1,2-benzisoxazole.
Claim 30
Dependent Claim
8 words
The compound of claim 6 which is 3-[1-2-dimethylaminoethyl)-4-piperidyl]-1,2-benzisoxazole.
Claim 31
Dependent Claim
8 words
The compound of claim 6 which is 3-[1-(2-diethylaminoethyl)-4-piperidyl]-1,2-benzisoxazole.
Claim 32
Dependent Claim
8 words
The compound of claim 7 which is 3-(1-cyano-4-piperidyl)-1,2-benzisoxazole.
Claim 33
Dependent Claim
8 words
The compound of claim 7 which is 3-(1-cyano-4-piperidyl)-5-methyl-1,2-benzisoxazole.
Claim 34
Dependent Claim
8 words
The compound of claim 7 which is 6-fluoro-3-(1-cyanomethyl-4-piperidyl)-1,2-benzisoxazole.
Claim 35
Dependent Claim
8 words
The compound of claim 8 which is 6-methoxy-3-(1-acetyl-4-piperidyl)-1,2-benzisoxazole.
Claim 36
Dependent Claim
12 words
The compound of claim 8 which is 4-(6-methoxy-1,2-benzisoxazol-3-yl)-1-piperidine carboxylic acid phenylmethyl ester.
Claim 37
Dependent Claim
8 words
The compound of claim 8 which is 5-methoxy-3-(1-acetyl-4-piperidyl)-1,2-benzisoxazole.
Claim 38
Dependent Claim
8 words
The compound of claim 8 which is 5,6-dimethoxy-3-(1-acetyl-4-piperidyl)-1,2-benzisoxazole.
Claim 39
Dependent Claim
8 words
The compound of claim 8 which is 3-(1-acetyl-4-piperidyl)-5-fluoro-1,2-benzisoxazole.
Claim 40
Dependent Claim
12 words
The compound of claim 8 which is 4-(4-fluoro-1,2-benzisoxazol-3-yl)-1-piperidine carboxylic acid phenyl ester.
Claim 41
Dependent Claim
12 words
The compound of claim 8 which is 4-(1,2-benzisoxazol-3-yl)-1-piperidine carboxylic acid phenyl ester.
Claim 42
Dependent Claim
8 words
The compound of claim 8 which is 3-(1-formyl-4-piperidyl)-6-chloro-1,2-benzisoxazole.
Claim 43
Dependent Claim
29 words
A method of alleviating pain comprising administering to a mammal in need of pain alleviation a pain-alleviating, effective amount of a compound as defined in claim 1 or 2.
Claim 44
Dependent Claim
30 words
A pain alleviating composition comprising an inert, pain-alleviating adjuvant and, as the active ingredient, an amount effective in alleviating pain of a compound as defined in claim 1 or 2.
References Cited (Backward Citations)
US4217349A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1985-10-18 | 1986-04-19 | 1986-10-19 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-10-18 | 1990-04-19 | 1990-10-19 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-10-18 | 1994-04-19 | 1994-10-19 | $7700.00 | Window Closed / Lapsed |