Patent EP0536164B1 successfully refreshed from Google Patents.
US4304782A
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Psychotropic deuterated derivatives of phenylhydantoin and pharmaceutical compositions comprising such derivatives
Assignee: REGION WELLONNE REPRESENTEE PAR I'EXECUTIF REGIONAL WALLON
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Filing: 1980-02-20
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Granted: 1981-12-08
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Expires: 2000-02-20
Abstract
Abstract Psychotropic composition comprising as an active constituent, a pharmaceutical composition, more particularly a psychotropic composition, characterized in that it comprises as an active constituent, a deuterated phenylhydantoin corresponding to the general formula ##STR1## wherein radicals R 1 are identical or different and represent hydrogen or methyl, R 2 is ethyl or a substituted or unsubstituted phenyl group, which is deuterated or not, R 3 is hydrogen, halogen or a linear or ramified alkyl radical comprising 1 to 4 carbon atoms, a linear or ramified alkoxy radical comprising 1 to 4 carbon atoms, a trifluoromethyl, hydroxy, nitro or amino radical, X is an oxo, thio or methylene group and x is an integer of 1-5, one of its enantioners or one of its salts with a physiologically acceptable base, in combination with a pharmaceutically acceptable vehicle.
Inventors
- 👤 Pierre A. Dumont
- 👤 Jacques H. Poupaert
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 23:28
CPC Classifications
C; C07; C07D; C07D233/00; C07D233/54; C07D233/66; C07D233/72; C07D233/74; A; A61; A61P; A61P25/00
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
179 words
A psychotropic pharmaceutical composition, which comprises as an active constituent, a therapeutically effective amount of a deuterated phenylhydantoin corresponding to the formula ##STR5## wherein R 1 , which may be the same or different, represents hydrogen or methyl, R 2 is ethyl, unsubstituted phenyl or phenyl substituted by halogen, straight chain or branched chain alkyl comprising 1 to 4 carbon atoms, straight or branched chain alkoxy comprising 1 to 4 carbon atoms, trifluoromethyl, nitro or amino, which phenyl or substituted phenyl may be deuterated, R 3 is hydrogen, halogen, straight chain or branched chain alkyl comprising 1 to 4 carbon atoms, straight or branched chain alkoxy comprising 1 to 4 carbon atoms, trifluoromethyl, nitro or amino, X is oxo, thio or methylene and x is an integer, with the proviso that the deuteration in R 2 and due to d x is such that said deuterated phenylhydantoin corresponding to the formula (I) is a mono- or penta-deuterated phenylhydantoin, one of its enantiomers or one of its salts with a physiologically acceptable base, in combination with a pharmaceutically acceptable vehicle.
Claim 2
Dependent Claim
179 words
A psychotropic pharmaceutical composition, which comprises as an active constituent, a therapeutically effective amount of a deuterated phenylhydantoin corresponding to the formula ##STR5## wherein R 1 , which may be the same or different, represents hydrogen or methyl, R 2 is ethyl, unsubstituted phenyl or phenyl substituted by halogen, straight chain or branched chain alkyl comprising 1 to 4 carbon atoms, straight or branched chain alkoxy comprising 1 to 4 carbon atoms, trifluoromethyl, nitro or amino, which phenyl or substituted phenyl may be deuterated, R 3 is hydrogen, halogen, straight chain or branched chain alkyl comprising 1 to 4 carbon atoms, straight or branched chain alkoxy comprising 1 to 4 carbon atoms, trifluoromethyl, nitro or amino, X is oxo, thio or methylene and x is an integer, with the proviso that the deuteration in R 2 and due to d x is such that said deuterated phenylhydantoin corresponding to the formula (I) is a mono- or penta-deuterated phenylhydantoin, one of its enantiomers or one of its salts with a physiologically acceptable base, in combination with a pharmaceutically acceptable vehicle.
Claim 3
Dependent Claim
51 words
A composition according to claim 1, wherein the phenylhydantoin is a deuterated diphenylhydantoin of the formula: ##STR6## wherein R 3 , which may be the same or different has the same meaning as defined in claim 1, R 1 and X are as defined in claim 1 and x+y=1 or 5.
Claim 4
Dependent Claim
27 words
A composition according to either of claims 1 or 2, wherein, in formulae I or II, said halogen for R 3 is chlorine, fluorine, bromine or iodine.
Claim 5
Dependent Claim
21 words
A composition according to claim 2, wherein said deuterated diphenylhydantoin is selected from the group consisting of (R,S)-5-(paradeuterophenyl)-5-phenylhydantoin, (R)-5-(paradeuterophenyl)-5-phenylhydantoin and (S)-5-(paradeuterophenyl)-5-phenylhydantoin.
Claim 6
Dependent Claim
27 words
A composition according to claim 2, wherein said deuterated diphenylhydantoin is selected from the group consisting of (R,S)-5-phenyl-d 5 -5-phenylhydantoin, (R)-5-phenyl-d 5 -5-phenylhydantoin and (S)-5-phenyl-d 5 -5-phenylhydantoin.
Claim 7
Dependent Claim
13 words
A composition according to claim 1, in the form of a unit dosage.
Claim 8
Dependent Claim
18 words
A composition according to claim 6, in the form of a tablet, wafer, capsule, coated pill or solution.
Claim 9
Dependent Claim
23 words
A method for treating epilepsy, comprising administering a psychotropic composition according to claim 1 to humans or animals in need of such treatment.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-12-07 | 1985-06-08 | 1985-12-08 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-12-07 | 1989-06-08 | 1989-12-08 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-12-07 | 1993-06-08 | 1993-12-08 | $7700.00 | Window Closed / Lapsed |