US4423049A
Expired / Lapsed
US
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2-[4-[(4,4-Dialkyl-2,6-piperidinedion-1-yl)butyl]-1-piperazinyl]pyrimidines
Assignee: Mead Johnson and Co LLC
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Filing: 1981-12-28
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Granted: 1983-12-27
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Expires: 2001-12-28
Abstract
Abstract 1-[4-(4,4-Dialkyl-2,6-piperidinedion-1-yl)butyl]piperazines with 2-pyrimidyl substituents in the 4- position have been synthesized and demonstrate useful anxiolytic properties. The compound 4,4-dimethyl-1-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,6-piperidi nedione, which has selective anxiolytic activity, constitutes the preferred embodiment of the invention.
Inventors
- 👤 Davis L. Temple, Jr.
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-10 01:59
CPC Classifications
C; C07; C07D; C07D403/00; C07D403/14; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/32; C07D239/42; A; A61; A61P; A61P25/00; A61P25/18; A61P25/20; C07C; C07C51/00; C07D211/00; C07D211/04; C07D211/80; C07D211/84; C07D211/86; C07D211/88; C07D211/90; C07D239/46; C07D239/47; C07D239/56; C07D309/00; C07D309/32; C07D401/00; C07D401/02; C07D401/12; C07D487/00; C07D487/02; C07D487/10
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
48 words
A compound selected from the group consisting of a compound having Formula (I) ##STR18## wherein R 1 and R 2 are independently selected from C 1 to C 4 alkyl groups; with Z being hydrogen, hydroxyl, halogen, or trifluoromethyl; and the non-toxic pharmaceutically acceptable acid addition salts thereof.
Claim 2
Dependent Claim
48 words
A compound selected from the group consisting of a compound having Formula (I) ##STR18## wherein R 1 and R 2 are independently selected from C 1 to C 4 alkyl groups; with Z being hydrogen, hydroxyl, halogen, or trifluoromethyl; and the non-toxic pharmaceutically acceptable acid addition salts thereof.
Claim 3
Dependent Claim
9 words
A compound of claim 1 wherein Z is 5-fluoro.
Claim 4
Dependent Claim
9 words
A compound of claim 1 wherein Z is 5-hydroxy.
Claim 5
Dependent Claim
14 words
The compound of claim 1, 4,4-dimethyl-1-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,6-piperidinedione or a pharmaceutically acceptable acid addition salt thereof.
Claim 6
Dependent Claim
14 words
The compound of claim 1, 4-ethyl-4-methyl-1-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,6-piperidinedione or a pharmaceutically acceptable acid addition salt thereof.
Claim 7
Dependent Claim
14 words
The compound of claim 1, 4,4-diethyl-1-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,6-piperidinedione or a pharmaceutically acceptable acid addition salt thereof.
Claim 8
Dependent Claim
13 words
The compound of claim 1, 4-methyl-4-propyl-1-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,6-piperidinedione or pharmaceutically acceptable acid addition salt thereof.
Claim 9
Dependent Claim
14 words
The compound of claim 1, 4,4-dimethyl-1-[4-[4-(5-fluoro-2-pyrimidinyl)-1-piperazinyl]butyl]-2,6-piperidinedione or a pharmaceutically acceptable acid addition salt thereof.
Claim 10
Dependent Claim
37 words
The process for ameliorating an undesirable anxiety state in a manual comprising systemic administration to said mammal of an effective anxiolytic dose of from 0.01 to 40 mg/kg body weight of a compound claimed in claim 1.
Claim 11
Dependent Claim
20 words
The process of claim 9 wherein the Formula (I) compound is 4,4-dimethyl-1-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,6-piperidinedione or a pharmaceutically acceptable acid addition salt thereof.
Claim 12
Dependent Claim
46 words
A pharmaceutical composition in dosage unit form suitable for systemic administration to a mammalian host comprising a pharmaceutical carrier and an amount of a compound claimed in claim 1 to provide an effective non-toxic dose of from 0.01 to 40 mg/kg body weight of said host.
Claim 13
Dependent Claim
21 words
The pharmaceutical composition of claim 11 wherein the Formula (I) compound is 4,4-dimethyl-1-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,6-piperidinedione or a pharmaceutically acceptable acid addition salt thereof.
References Cited (Backward Citations)
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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) | 1986-12-26 | 1987-06-27 | 1987-12-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1990-12-26 | 1991-06-27 | 1991-12-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1994-12-26 | 1995-06-27 | 1995-12-27 | $7700.00 | Window Closed / Lapsed |