Patent US4452799A successfully refreshed from Google Patents.
US4452799A
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Benzisothiazole and benzisoxazole piperazine derivatives
Assignee: Mead Johnson and Co LLC
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Filing: 1983-08-05
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Granted: 1984-06-05
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Expires: 2003-08-05
Abstract
Abstract Disubstituted N,N-piperazinyl derivatives are disclosed wherein one substituent is benzisothiazol-3-yl or benzisoxazol-3-yl and the other is alkylene attached to heterocycles such as azaspiro[4.5]decanedione, dialkylglutarimide, thiazolidinedione and spirocyclopentylthiazolidinedione or butyrophenone-like groups. The compounds have psychotropic properties and 8-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione is a typical embodiment having selective antipsychotic activity.
Inventors
- 👤 Davis L. Temple, Jr.
- 👤 Joseph P. Yevich
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 12:55
CPC Classifications
C; C07; C07D; C07D275/00; C07D275/04; C07D211/00; C07D211/04; C07D211/80; C07D211/84; C07D211/86; C07D211/88; C07D261/00; C07D261/20; C07D277/00; C07D277/02; C07D277/20; C07D277/32; C07D277/34; C07D277/60; C07D319/00; C07D319/04; C07D319/06; C07D413/00; C07D413/02; C07D413/12; C07D417/00; C07D417/02; C07D417/12; C07D487/00; C07D487/02; C07D487/10
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
37 words
A compound of Formula (I) ##STR43## wherein R represents the radical ##STR44## wherein n is 3 or 4, Y is oxygen or sulfur, Z is hydrogen or halogen or a pharmaceutically acceptable non-toxic acid addition salt thereof.
Claim 2
Dependent Claim
37 words
A compound of Formula (I) ##STR43## wherein R represents the radical ##STR44## wherein n is 3 or 4, Y is oxygen or sulfur, Z is hydrogen or halogen or a pharmaceutically acceptable non-toxic acid addition salt thereof.
Claim 3
Dependent Claim
20 words
The compound of claim 1 wherein R is the 2,4-thiazolidinedione radical (c) or a pharmaceutically acceptable acid addition salt thereof.
Claim 4
Dependent Claim
16 words
The compound of claim 2 which is 3-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-2,4-thiazolidinedione or a pharmaceutically acceptable acid addition salt thereof.
Claim 5
Dependent Claim
16 words
The compound of claim 2 which is 3-[4-[4-(1,2-benzisoxazol-3-yl)-1-piperazinyl]butyl]-2,4-thiazolidinedione or a pharmaceutically acceptable acid addition salt thereof.
Claim 6
Dependent Claim
20 words
The compound of claim 1 wherein R is the spirocyclopentyl-2,4-thiazolidinedione radical (d) or a pharmaceutically acceptable acid addition salt thereof.
Claim 7
Dependent Claim
16 words
The compound of claim 5 which is 8-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-6-thia-8-azaspiro[4.4]nonane-7,9-dione or a pharmaceutically acceptable acid addition salt thereof.
Claim 8
Dependent Claim
16 words
The compound of claim 5 which is 8-[4-[4-(1,2-benzisoxazol-3-yl)-1-piperazinyl]butyl]-6-thia-8-azaspiro[4.4]nonane-7,9-dione or a pharmaceutically acceptable acid addition salt thereof.
Claim 9
Dependent Claim
18 words
The compound of claim 1 wherein R is radical (e) or a pharmaceutically acceptable acid addition salt thereof.
Claim 10
Dependent Claim
16 words
The compound of claim 8 which is 4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-1-(4-fluorophenyl)-1-butanone or a pharmaceutically acceptable acid addition salt thereof.
Claim 11
Dependent Claim
16 words
The compound of claim 8 which is 4-[4-(1,2-benzisoxazol-3-yl)-1-piperazinyl]-1-(4-fluorophenyl)-1-butanone or a pharmaceutically acceptable acid addition salt thereof.
Claim 12
Dependent Claim
18 words
The compound of claim 1 wherein R is radical (f) or a pharmaceutically acceptable acid addition salt thereof.
Claim 13
Dependent Claim
16 words
The compound of claim 11 which is α-[3-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]propyl]-4-fluorobenzenemethanol or a pharmaceutically acceptable acid addition salt thereof.
Claim 14
Dependent Claim
16 words
The compound of claim 11 which is α-[3-[4-(1,2-benzisoxazol3-yl)-1-piperazinyl]propyl]-4-fluorobenzenemethanol or a pharmaceutically acceptable acid addition salt thereof.
Claim 15
Dependent Claim
33 words
A neuroleptic process which comprises systemic administration to a mammal in need of such treatment an effective dose of from about 0.01 to 40 mg/kg body weight of a compound of claim 1.
Claim 16
Dependent Claim
19 words
A piperazine heterocycle of Formula (III) ##STR45## wherein Y is oxygen or sulfur and Z is hydrogen or halogen.
Claim 17
Dependent Claim
19 words
A piperazine heterocycle of Formula (III) ##STR45## wherein Y is oxygen or sulfur and Z is hydrogen or halogen.
Claim 18
Dependent Claim
8 words
The compound of claim 15 which is 3-(1-piperazinyl)-1,2-benzisothiazole.
Claim 19
Dependent Claim
8 words
The compound of claim 15 which is 3-(1-piperazinyl)-1,2-benzisoxazole.
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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) | 1987-06-05 | 1987-12-05 | 1988-06-05 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-06-05 | 1991-12-05 | 1992-06-05 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-06-05 | 1995-12-05 | 1996-06-05 | $7700.00 | Window Closed / Lapsed |