US4352811A
Expired / Lapsed
US
⏱️ 0.0 years remaining
3-(1-Substituted-4-piperidyl)-1,2-benzisoxazoles
Assignee: Aventis Pharmaceuticals Inc
•
Filing: 1981-11-12
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Granted: 1982-10-05
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Expires: 2001-11-12
Abstract
Abstract Novel 3-(1-substituted-4-piperidyl)-1,2-benzisoxazoles, processes for the preparation thereof, and methods of treating psychoses employing compounds and compositions thereof are disclosed.
Inventors
- 👤 Joseph T. Strupczewski
- 👤 Richard C. Allen
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 22:25
CPC Classifications
C; C07; C07C; C07C17/00; C07C17/35; A; A61; A61P; A61P25/00; A61P25/02; A61P25/20; C07C17/354; C07D; C07D209/00; C07D209/02; C07D209/04; C07D209/10; C07D209/12
Claims Analysis
Total Claims: 50
Claim 1
Independent Claim
134 words
A compound of the formula ##STR29## wherein R is a group of the formula ##STR30## wherein n is 2 or 3; a group of the formula ##STR31## wherein n is 2 or 3; a group of the formula ##STR32## wherein n is 2 or 3; a group of the formula ##STR33## wherein R 1 and R 2 are each independently hydrogen or loweralkyl, R 3 is hydrogen, halogen or loweralkyl and n is 2 or 3; a group of the formula ##STR34## wherein R 4 is hydrogen or loweralkyl, R 5 is hydrogen, halogen or loweralkyl; and n is 2 or 3; and a group of the formula ##STR35## X is hydroen, 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
134 words
A compound of the formula ##STR29## wherein R is a group of the formula ##STR30## wherein n is 2 or 3; a group of the formula ##STR31## wherein n is 2 or 3; a group of the formula ##STR32## wherein n is 2 or 3; a group of the formula ##STR33## wherein R 1 and R 2 are each independently hydrogen or loweralkyl, R 3 is hydrogen, halogen or loweralkyl and n is 2 or 3; a group of the formula ##STR34## wherein R 4 is hydrogen or loweralkyl, R 5 is hydrogen, halogen or loweralkyl; and n is 2 or 3; and a group of the formula ##STR35## X is hydroen, 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
21 words
A compound according to claim 1 wherein R is a group of the formula ##STR36## wherein n is 2 or 3.
Claim 4
Dependent Claim
10 words
A compound according to claim 2 wherein n is 3.
Claim 5
Dependent Claim
21 words
A compound according to claim 1 wherein R is a group of the formula ##STR37## wherein n is 2 or 3.
Claim 6
Dependent Claim
10 words
A compound according to claim 4 wherein n is 3.
Claim 7
Dependent Claim
21 words
A compound according to claim 1 wherein R is a group of the formula ##STR38## wherein n is 2 or 3.
Claim 8
Dependent Claim
10 words
A compound according to claim 6 wherein n is 3.
Claim 9
Dependent Claim
40 words
A compound according to claim 1 wherein R is a group of the formula ##STR39## wherein R 1 and R 2 are each independently hydrogen or loweralkyl, R 3 is hydrogen, halogen or loweralkyl, and n is 2 or 3.
Claim 10
Dependent Claim
19 words
A compound according to claim 8 wherein R 1 is lowerallkyl, R 2 is hydrogen and n is 3.
Claim 11
Dependent Claim
35 words
A compound according to claim 1 wherein R is a group of the formula ##STR40## wherein R 4 is hydrogen or loweralkyl, R 5 is hydrogen, halogen or loweralkyl and n is 2 or 3.
Claim 12
Dependent Claim
11 words
A compound according to claim 10 wherein R 4 is hydrogen.
Claim 13
Dependent Claim
15 words
A compound according to claim 1 wherein R is a group of the formula ##STR41##
Claim 14
Dependent Claim
10 words
The compound of claim 3 which is 3-[1-(4-fluorobenzoylpropyl)-4-piperidyl]-1,2-benzisoxazole ethylene ketal.
Claim 15
Dependent Claim
10 words
The compound of claim 3 which is 3-[1-(4-fluorobenzoylpropyl)-4-piperidyl]-6-fluoro-1,2-benzisoxazole ethylene ketal.
Claim 16
Dependent Claim
10 words
The compound of claim 3 which is 3-[1-(4-fluorobenzoylpropyl)-4-piperidyl]-6-chloro-1,2-benzisoxazole ethylene ketal.
Claim 17
Dependent Claim
8 words
The compound of claim 5 which is 3-[1-(4-fluorobenzoylpropyl)-4-piperidyl]-1,2-benzisoxazole.
Claim 18
Dependent Claim
8 words
The compound of claim 5 which is 3-[1-(4-fluorobenzoylpropyl)-4-piperidyl]-6-fluoro-1,2-benzisoxazole.
Claim 19
Dependent Claim
8 words
The compound of claim 5 which is 3-[1-(4-fluorobenzoylpropyl)-4-piperidyl]-6-chloro-1,2-benzisoxazole.
Claim 20
Dependent Claim
8 words
The compound of claim 7 which is 3-[1-(6-fluoro-1,2-benzisoxazol-3-propyl)-4-piperidyl]-1,2-benzisoxazole.
Claim 21
Dependent Claim
8 words
The compound of claim 7 which is 3-[1-(6-fluoro-1,2-benzisoxazol-3-propyl)-4-piperidyl]-5-fluoro-1,2-benzisoxazole.
Claim 22
Dependent Claim
8 words
The compound of claim 7 which is 3-[1-(6-fluoro-1,2-benzisoxazol-3-propyl)-4-piperidyl]-6-fluoro-1,2-benzisoxazole.
Claim 23
Dependent Claim
8 words
The compound of claim 7 which is 3-[1-(6-fluoro-1,2-benzisoxazol-3-propyl)-4-piperidyl]-5-methoxy-1,2-benzisoxazole.
Claim 24
Dependent Claim
8 words
The compound of claim 7 which is 3-[1-(6-fluoro-1,2-benzisoxazol-3-propyl)-4-piperidyl]-6-chloro-1,2-benzisoxazole.
Claim 25
Dependent Claim
8 words
The compound of claim 9 which is 3-{3-[4-1,2-benzisoxazol-3-yl)piperidyl]propyl}-2-methylindole.
Claim 26
Dependent Claim
8 words
The compound of claim 9 which is 3-{3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidyl]propyl}-2-methylindole.
Claim 27
Dependent Claim
8 words
The compound of claim 9 which is 3-{3-[4-(6-chloro-1,2-benzisoxazol-3-yl)piperidyl]propyl}-2-methylindole.
Claim 28
Dependent Claim
8 words
The compound of claim 9 which is 3-{3-[4-(5-methoxy-1,2-benzisoxazol-3-yl)piperidyl]propyl}-2-methylindole.
Claim 29
Dependent Claim
8 words
The compound of claim 9 which is 3-{3-[4-(5-hydroxy-1,2-benzisoxazol-3-yl)piperidyl]propyl}-2-methylindole.
Claim 30
Dependent Claim
8 words
The compound of claim 9 which is 3-{3-[4-(5-fluoro-1,2-benzisoxazol-3-yl)piperidyl]propyl}-2-methylindole.
Claim 31
Dependent Claim
8 words
The compound of claim 11 which is 3-{[1,3-dihydro-2-oxo-2H-benzimidizol-1-yl]propyl-4-piperidyl}-1,2-benzisoxazole.
Claim 32
Dependent Claim
8 words
The compound of claim 11 which is 3-{1-[1,3-dihydro-2-oxo-2H-benzimidazol-1-ylethyl]-4-piperidinyl}-1,2-benzisoxazole.
Claim 33
Dependent Claim
8 words
The compound of claim 11 which is 6-chloro-3-{1-[1,3-dihydro-2-oxo-2H-benzimidazol-1-ylpropyl]-4-piperidyl}-1,2-benzisoxazole.
Claim 34
Dependent Claim
8 words
The compound of claim 11 which is 6-chloro-3-{1-[1,3-dihydro-2-oxo-2H-benzimidazol-1-ylethyl]-4-piperidyl}-1,2-benzisoxazole.
Claim 35
Dependent Claim
8 words
The compound of claim 11 which is 5-fluoro-3-{1-[1,3-dihydro-2-oxo-2H-benzimidazol-1-ylpropyl]-4-piperidyl}-1,2-benzisoxazole.
Claim 36
Dependent Claim
8 words
The compound of claim 11 which is 6-fluoro-3-{1-[1,3-dihydro-2-oxo-2H-benzimidazol-1-ylpropyl]-4-piperidyl}-1,2-benzisoxazole.
Claim 37
Dependent Claim
8 words
The compound of claim 11 which is 6-methoxy-3-{1-[1,3-dihydro-2-oxo-2H-benzimidazol-1-ylpropyl]-4-piperidyl}-1,2-benzisoxazole.
Claim 38
Dependent Claim
9 words
The compound of claim 12 which is 3-{1-[4,4-bis(4-Fluorophenyl)-1-butyl]-4-piperidyl}-1,2-benzisoxazole hydrochloride.
Claim 39
Dependent Claim
8 words
The compound of claim 12 which is 3-{1-[4,4-bis(4-fluorophenyl)-1-butyl]-4-piperidyl}-6-fluoro-1,2-benzisoxazole.
Claim 40
Dependent Claim
8 words
The compound of claim 12 which is 3-{1-[4,4-bis(4-fluorophenyl)-1-butyl]-4-piperidyl}-5-fluoro-1,2-benzisoxazole.
Claim 41
Dependent Claim
8 words
The compound of claim 12 which is 3-{1-[4,4-bis(4-fluorophenyl)-1-butyl]-4-piperidyl}-5-methoxy-1,2-benzisoxazole.
Claim 42
Dependent Claim
8 words
The compound of claim 12 which is 3-{1-[4,4-bis(4-fluorophenyl)-1-butyl]-4-piperidyl}-5-hydroxy-1,2-benzisoxazole.
Claim 43
Dependent Claim
8 words
The compound of claim 12 which is 6-chloro-3-{1-[4,4-bis(4-fluorophenyl)-1-butyl]-4-piperidyl}-1,2-benzisoxable.
Claim 44
Dependent Claim
8 words
The compound of claim 12 which is 5,6-dimethoxy-3-{1-[4,4-bis(4-fluorophenyl)-1-butyl]-4-piperidyl}-5-methoxy-1,2-benzisoxazole.
Claim 45
Dependent Claim
8 words
The compound of claim 7 which is 3-[1-(6-fluoro-1,2-benzisoxazol-3-propyl)-4-piperidyl]-5,6-dimethoxy-1,2-benzisoxazole.
Claim 46
Dependent Claim
9 words
The compound of claim 9 which is 3-{3-(4-[5,6-dimethoxy-1,2-benzisoxazol-3-yl]piperidyl)propyl}-2-methyl indole.
Claim 47
Dependent Claim
9 words
The compound of claim 11 which is 5,6-dimethoxy-3-{1-[1,3-dihydro-2-oxo-2H-benzimidazole-1-yl-propyl]-4-piperidinyl}-1,2-benzisoxazole hydrobromide.
Claim 48
Dependent Claim
8 words
The compound of claim 11 which is 4-fluoro-3-{[1,3-dihydro-2-oxo-2H-benzimidazole-1-yl-propyl]-4-piperdinyl}-1,2-benzisoxazole.
Claim 49
Dependent Claim
27 words
A method of treating psychoses comprising administering to a mammal in need of psychoses treatment a psychoses-treating, effective amount of a compound as defined in claim 1.
Claim 50
Dependent Claim
27 words
A psychoses-treating composition comprising an inert psychoses-treating adjuvant and, as the active ingredient, an amount effective in treating psychoses of a compound as defined in 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) | 1985-10-04 | 1986-04-05 | 1986-10-05 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-10-04 | 1990-04-05 | 1990-10-05 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-10-04 | 1994-04-05 | 1994-10-05 | $7700.00 | Window Closed / Lapsed |