US5236940A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Pharmaceutical compositions, 2-benzothiazolamine derivatives, and their preparation
Assignee: Rhone Poulenc Sante SA
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Filing: 1991-09-03
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Granted: 1993-08-17
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Expires: 2011-09-03
Abstract
Abstract Pharmaceutical compositions are disclosed. They are useful for the treatment of medical conditions associated with the effects of glutamate, comprise as active principle, at least one compound of formula: ##STR1## or a salt thereof, in which either R 1 represents polyfluoroalkoxy, 2,2,2-trifluoroethyl, pentafluoroethyl, tert-butyl, trimethylsilyl or trifluoromethylthio and R 2 and R 3 represent hydrogen, or R 1 represents polyfluoroalkoxy, R 2 represents hydrogen and R 3 represents alkyl, amino, alkoxy, phenyl, phenylalkyl, dimethylamino or dialkylaminoakylthio, or R 1 represents polyfluoroalkoxy, R 2 represents amino and R 3 represents hydrogen, with the exception of 6-trifluoromethoxy-2-benzothiazolamine.
Inventors
- 👤 Francois Audiau
- 👤 Claude James
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 23:19
CPC Classifications
C; C07; C07D; C07D277/00; C07D277/60; C07D277/62; C07D277/68; C07D277/82
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
113 words
A compound of formula: ##STR5## in which either: (1) - R 1 represents polyfluoroalkoxy, tert-butyl, or trimethylsilyl, and R 2 and R 3 represent hydrogen, with the proviso that, when R 1 represents trifluoromethoxy, R 2 and R 3 are not both hydrogen; (2) - or R 1 represents polyfluoroalkoxy, R 2 represents hydrogen, and R 3 represents amino or phenylalkyl; (3) - or R 1 represents polyfluoroalkoxy, R 2 represents amino and R 3 represents hydrogen, provided that said alkyl and alkoxy radicals or portions contain 1to 4 carbon atoms each in a straight or branched chain, or a pharmaceutically acceptable salt of a said compound with an inorganic or organic acid.
Claim 2
Dependent Claim
113 words
A compound of formula: ##STR5## in which either: (1) - R 1 represents polyfluoroalkoxy, tert-butyl, or trimethylsilyl, and R 2 and R 3 represent hydrogen, with the proviso that, when R 1 represents trifluoromethoxy, R 2 and R 3 are not both hydrogen; (2) - or R 1 represents polyfluoroalkoxy, R 2 represents hydrogen, and R 3 represents amino or phenylalkyl; (3) - or R 1 represents polyfluoroalkoxy, R 2 represents amino and R 3 represents hydrogen, provided that said alkyl and alkoxy radicals or portions contain 1to 4 carbon atoms each in a straight or branched chain, or a pharmaceutically acceptable salt of a said compound with an inorganic or organic acid.
Claim 3
Dependent Claim
58 words
A compound as claimed in claim 1, in which either: (1) - R 1 represents pentafluoroethoxy, 2,2,2-trifluoroethoxy, 1,1,2,2-tetrafluoroethoxy, or 2,2,3,3,3-pentafluoropropoxy, and R 2 and R 3 represent hydrogen; (2) - R 1 represents trifluoromethoxy, R 2 represents hydrogen, and R 3 represents amino; (3) - R 1 represents trifluoromethoxy, R 2 represents amino, and R 3 represents hydrogen.
Claim 4
Dependent Claim
15 words
A compound as claimed in claim 1 which is 6-pentafluoroethoxy-2-benzothiazolamine and its acid addition salts.
Claim 5
Dependent Claim
15 words
A compound as claimed in claim 1 which is 6-tertbutyl-2-benzothiazolamine, and its acid addition salts.
Claim 6
Dependent Claim
15 words
A compound as claimed in claim 1 which is 6-trifluoromethoxy-2,5-benzothiazolediamine and its acid addition salts.
Claim 7
Dependent Claim
15 words
A compound as claimed in claim 1 which is 6-trifluoromethoxy-2,4-benzothiazolediamine and its acid addition salts.
Claim 8
Dependent Claim
135 words
A pharmaceutical composition comprising, as active principle, in association with a compatible pharmaceutically acceptable carrier, an effective amount of at least one compound of formula: ##STR6## in which either (1) - R 1 represents polyfluoroalkoxy, tert-butyl, or trimethylsilyl and R 2 and R 3 represent hydrogen, with the proviso that, when R 1 represents trifluoromethoxy, R 2 and R 3 are not both hydrogen; (2) - or R 1 represents polyfluoroalkoxy, R 2 represents hydrogen and R 3 represents amino or phenylalkyl; (3) - or R 1 represents polyfluoroalkoxy, R 2 represents amino and R 3 represents hydrogen, provided that said alkyl and alkoxy radicals or portions contain 1 to 4 carbon atoms each in a straight or branched chain, or a pharmaceutically acceptable salt of a said compound with an inorganic or organic acid.
Claim 9
Dependent Claim
135 words
A pharmaceutical composition comprising, as active principle, in association with a compatible pharmaceutically acceptable carrier, an effective amount of at least one compound of formula: ##STR6## in which either (1) - R 1 represents polyfluoroalkoxy, tert-butyl, or trimethylsilyl and R 2 and R 3 represent hydrogen, with the proviso that, when R 1 represents trifluoromethoxy, R 2 and R 3 are not both hydrogen; (2) - or R 1 represents polyfluoroalkoxy, R 2 represents hydrogen and R 3 represents amino or phenylalkyl; (3) - or R 1 represents polyfluoroalkoxy, R 2 represents amino and R 3 represents hydrogen, provided that said alkyl and alkoxy radicals or portions contain 1 to 4 carbon atoms each in a straight or branched chain, or a pharmaceutically acceptable salt of a said compound with an inorganic or organic acid.
Claim 10
Dependent Claim
60 words
A pharmaceutical composition according to claim 7, in which either: (1) - R 1 represents pentafluoroethoxy, 2,2,2-trifluoroethoxy, 1,1,2,2-tetrafluoroethoxy, or 2,2,3,3,3-pentafluoropropoxy, and R 2 and R 3 represent hydrogen; (2) - or R 1 represents trifluoromethoxy, R 2 represents hydrogen, and R 3 represents amino; (3) - or R 1 represents trifluoromethoxy, R 2 represents amino, and R 3 represents hydrogen.
Claim 11
Dependent Claim
18 words
A pharmaceutical composition according to claim 7 in which the active ingredient is 6-pentafluoroethoxy-2-benzothiazolamine, 6-tert-butyl-2-benzothiazolamine, 6-trifluoromethoxy-2,5-benzothiazolediamine, or 6-trifluoromethoxy-2,4-benzothiazolediamine.
Claim 12
Dependent Claim
44 words
A method for the treatment of a medical condition associated with the effects of glutamate which comprises administering to a subject in need of such treatment an amount of a compound of formula (I) as defined in claim 7 sufficient to inhibit such effects.
Claim 13
Dependent Claim
44 words
A method for the treatment of a medical condition associated with the effects of glutamate which comprises administering to a subject in need of such treatment an amount of a compound of formula (I) as defined in claim 8, sufficient to inhibit such effects.
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) | 1996-08-16 | 1997-02-15 | 1997-08-17 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2000-08-16 | 2001-02-15 | 2001-08-17 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2004-08-16 | 2005-02-15 | 2005-08-17 | $7700.00 | Window Closed / Lapsed |