US4458076A
Expired / Lapsed
US
⏱️ 0.0 years remaining
3-(4-Piperidinyl)-1,2-benzisothiazoles
Assignee: Aventis Pharmaceuticals Inc
•
Filing: 1983-05-31
•
Granted: 1984-07-03
•
Expires: 2003-05-31
Abstract
Abstract Novel 3-(4-piperidinyl)-1,2-benzisothiazoles, processes for the preparation thereof, and method of treating psychoses and alleviating pain employing compounds or compositions thereof are disclosed.
Inventors
- 👤 Joseph T. Strupczewski
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 14:39
CPC Classifications
C; C07; C07D; C07D417/00; C07D417/02; C07D417/04; A; A61; A61P; A61P1/00; A61P1/08; A61P25/00; A61P25/04; A61P25/20; C07D417/14
Claims Analysis
Total Claims: 25
Claim 1
Independent Claim
171 words
A compound of the formula ##STR34## wherein R is hydrogen, loweralkyl, loweralkenyl, cycloalkylloweralkyl, phenylloweralkyl, hydroxy, diloweralkyaminoloweralkyl, cyano, cyanomethyl, ##STR35## a group of the formula ##STR36## wherein R 1 is hydrogen, loweralkyl or a group of the formula OR 2 wherein R 2 is phenyl or benzyl; a group of the formula ##STR37## wherein n is 2 or 3; a group of the formula ##STR38## wherein n is 2 or 3; a group of the formula ##STR39## wherein n is 2 or 3; a group of the formula ##STR40## wherein R 3 and R 4 are each independently hydrogen or loweralkyl, R 5 is hydrogen, halogen or loweralkyl, and n is 2 or 3; a group of the formula ##STR41## wherein R 6 is hydrogen or loweralkyl, R 7 is hydrogen, halogen or loweralkyl, and n is 2 or 3; or a group of the formula ##STR42## X is hydrogen, halogen, loweralkyl, loweralkoxy or hydroxy; and m is 1 or 2; the optical antipodes thereof; or pharmaceutically acceptable acid addition salts thereof.
Claim 2
Dependent Claim
171 words
A compound of the formula ##STR34## wherein R is hydrogen, loweralkyl, loweralkenyl, cycloalkylloweralkyl, phenylloweralkyl, hydroxy, diloweralkyaminoloweralkyl, cyano, cyanomethyl, ##STR35## a group of the formula ##STR36## wherein R 1 is hydrogen, loweralkyl or a group of the formula OR 2 wherein R 2 is phenyl or benzyl; a group of the formula ##STR37## wherein n is 2 or 3; a group of the formula ##STR38## wherein n is 2 or 3; a group of the formula ##STR39## wherein n is 2 or 3; a group of the formula ##STR40## wherein R 3 and R 4 are each independently hydrogen or loweralkyl, R 5 is hydrogen, halogen or loweralkyl, and n is 2 or 3; a group of the formula ##STR41## wherein R 6 is hydrogen or loweralkyl, R 7 is hydrogen, halogen or loweralkyl, and n is 2 or 3; or a group of the formula ##STR42## X is hydrogen, halogen, loweralkyl, loweralkoxy or hydroxy; and m is 1 or 2; the optical antipodes thereof; or pharmaceutically acceptable acid addition salts 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
10 words
A compound according to claim 2 wherein R is loweralkyl.
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 ##STR43##
Claim 7
Dependent Claim
10 words
A compound according to claim 1 wherein R is diloweralkylaminoloweralkyl.
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 ##STR44## 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
21 words
A compound according to claim 1 wherein R is a group of the formula ##STR45## wherein n is 2 or 3.
Claim 11
Dependent Claim
21 words
A compound according to claim 1 wherein R is a group of the formula ##STR46## wherein n is 2 or 3.
Claim 12
Dependent Claim
21 words
A compound according to claim 1 wherein R is a group of the formula ##STR47## wherein n is 2 or 3.
Claim 13
Dependent Claim
40 words
A compound according to claim 1 wherein R is a group of the formula ##STR48## wherein R 3 and R 4 are each independently hydrogen or loweralkyl; R 5 is hydrogen, halogen or loweralkyl; and n is 2 or 3.
Claim 14
Dependent Claim
35 words
A compound according to claim 1 wherein R is a group of the formula ##STR49## wherein R 6 is hydrogen or loweralkyl; R 7 is hydrogen, halogen or loweralkyl; and n is 2 or 3.
Claim 15
Dependent Claim
15 words
A compound according to claim 1 wherein R is a group of the formula ##STR50##
Claim 16
Dependent Claim
8 words
The compound of claim 2 which is 3-(1-methyl-4-piperidinyl)-1,2-benzisothiazole.
Claim 17
Dependent Claim
8 words
The compound of claim 2 which is 3-(1-cyano-4-piperidinyl)-1,2-benzisothiazole.
Claim 18
Dependent Claim
8 words
The compound of claim 2 which is 3-(4-piperidinyl)-1,2-benzoisothiazole.
Claim 19
Dependent Claim
8 words
The compound of claim 2 which is 3-{1-(cyclopropylmethyl)-4-piperidinyl}-1,2-benzisothiazole.
Claim 20
Dependent Claim
8 words
The compound of claim 4 which is 3-{1-[phenethyl]-4-piperidinyl}-1,2-benzisothiazole.
Claim 21
Dependent Claim
8 words
The compound of claim 5 which is 3-(1-benzoyloxy-4-piperidinyl)-1,2-benzisothiazole.
Claim 22
Dependent Claim
8 words
The compound of claim 11 which is 3-[1-(6-fluoro-1,2-benzisoxazole-3-propyl)-4-piperidinyl]-1,2-benzisothiazole.
Claim 23
Dependent Claim
8 words
The compound of claim 12 which is 3-{3-[4-(1,2-benzisothiazole-3-yl)piperidinyl]propyl}-2-methylindole.
Claim 24
Dependent Claim
8 words
The compound of claim 13 which is 3-[1-(1,3-dihydro-2-oxo-2H-benzimidazol-1-ylpropyl)-4-piperidinyl]-1,2-benzisothiazole.
Claim 25
Dependent Claim
8 words
The compound of claim 14 which is 3-{1-[4,4-bis)4-fluorophenyl)-1-butyl]-4-piperidinyl]-1,2-benzisothiazole.
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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) | 1987-07-03 | 1988-01-02 | 1988-07-03 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-07-03 | 1992-01-02 | 1992-07-03 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-07-03 | 1996-01-02 | 1996-07-03 | $7700.00 | Window Closed / Lapsed |