US4411901A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Benzisothiazole and benzisoxazole piperazine derivatives
Assignee: Mead Johnson and Co LLC
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Filing: 1981-12-23
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Granted: 1983-10-25
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Expires: 2001-12-23
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-azaspior[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
2026-11-07 02:47
CPC Classifications
C; C07; C07D; C07D417/00; C07D417/14; C07D275/00; C07D275/04; A; A61; A61P; A61P25/00; 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; C07D417/02; C07D417/12; C07D487/00; C07D487/02; C07D487/10
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
52 words
A compound of Formula (I) ##STR43## wherein R represents the radical ##STR44## wherein n is 3 or 4, R 1 and R 2 are independently lower alkyl of 1 to 4 carbon atoms, Y is oxygen or sulfur, Z is hydrogen or halogen or a pharmaceutically acceptable non-toxic acid addition salt thereof.
Claim 2
Dependent Claim
52 words
A compound of Formula (I) ##STR43## wherein R represents the radical ##STR44## wherein n is 3 or 4, R 1 and R 2 are independently lower alkyl of 1 to 4 carbon atoms, 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 8-azaspiro[4.5]decane-7,9-dione radical (a) or a pharmaceutically acceptable acid addition salt thereof.
Claim 4
Dependent Claim
16 words
The compound of claim 2 which is 8-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione or a pharmaceutically acceptable acid addition salt thereof.
Claim 5
Dependent Claim
16 words
The compound of claim 2 which is 8-[4-[4-(1,2-benzisoxazol-3-yl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione or a pharmaceutically acceptable acid addition salt thereof.
Claim 6
Dependent Claim
23 words
The compound of claim 1 wherein R is the R 1 ,R 2 -glutarimide (b) or a pharmaceutically acceptable acid addition salt thereof.
Claim 7
Dependent Claim
16 words
The compound of claim 5 which is 1-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-4-methyl-4-propyl-2,6-piperidinedione or a pharmaceutically acceptable acid addition salt thereof.
Claim 8
Dependent Claim
16 words
The compound of claim 5 which is 1-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-4,4-dimethyl-2,6-piperidinedione or a pharmaceutically acceptable acid addition salt thereof.
Claim 9
Dependent Claim
16 words
The compound of claim 5 which is 1-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-4,4-diethyl-2,6-piperidinedione or a pharmaceutically acceptable acid addition salt thereof.
Claim 10
Dependent Claim
14 words
The compound of claim 2 which is 8-[4-[4-(6-chloro-1,2-benzisoxazol-3-yl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione or a pharmaceutically acceptable salt thereof.
Claim 11
Dependent Claim
40 words
The process for ameliorating a psychotic state in a mammal in need of such treatment which comprises systemic administration to said mammal an effective dose of from about 0.01 to 40 mg/kg body weight of a compound of claim 1.
Claim 12
Dependent Claim
11 words
The process of claim 10 in which the compound is 8-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione.
Claim 13
Dependent Claim
1 words
8-[4-[4-(2,1-Benzisothiazol-3-yl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione.
Claim 14
Dependent Claim
1 words
8-[4-[4-(2,1-Benzisothiazol-3-yl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione.
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) | 1986-10-24 | 1987-04-25 | 1987-10-25 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1990-10-24 | 1991-04-25 | 1991-10-25 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1994-10-24 | 1995-04-25 | 1995-10-25 | $7700.00 | Window Closed / Lapsed |