EP0282971A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Substituted 2-aminobenzothiazoles and derivatives useful as cerebrovascular agents
Assignee: Warner Lambert Co LLC
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Filing: 1988-03-15
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Granted: —
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Expires: 2008-03-15
Abstract
Abstract Use of a compound of the general formula I or of a pharmaceutically acceptable salt thereof wherein R¹ and R² are the same or different and are hydrogen straight or branched alkyl of from one to six carbon atoms, lower alkylaryl, lower alkenyl, phenyl, CF₃, hydroxy, lower alkoxy, lower alkylthio, lower alkylsulphonyl, CF₃O at the six position, halogen, nitro, carboxy, lower alkoxycarbonyl, NR⁵R⁶CO, NR⁵R⁶ R⁵CONR⁵, CN, NR⁵R⁶SO₂, wherein R⁵ and R⁶ may be the same or different and are hydrogen, lower alkyl or aryl; R¹ and R² may together form a carbocyclic or methylenedioxy ring; R³ is hydrogen; R⁴ is hydrogen, lower alkyl, lower alkyl substituted by a substituted or unsubstituted heterocyclic group, methylcycloalkyl, benzyl, phenethyl, phenyl, substituted phenyl, alkyl, propargyl, with the proviso that R¹, R², and R³ must be hydrogen when R⁴ is not hydrogen, for the preparation of a pharmaceutical for treating cerebrovascular disorders.
Inventors
- 👤 Graham Johnson
- 👤 Michael Raymond Pavia
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-06 07:55
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/41; A61K31/425; A61P; A61P23/00; A61P25/00; A61P25/28; A61P9/00
Claims Analysis
Total Claims: 8
Claim 1
Independent Claim
147 words
Use of a compound of the general formula I or of a pharmaceutically acceptable salt thereof wherein R¹ and R² are the same or different and are hydrogen, straight or branched alkyl of from one to six carbon atoms, lower alkylaryl, lower alkenyl, phenyl, CF₃, hydroxy, lower alkoxy, lower alkylthio, lower alkylsulphonyl, CF₃O at the six position, halogen, nitro, carboxy, lower alkoxycarbonyl, NR⁵R⁶CO, NR⁵R⁶, R⁵CONR⁵, CN, NR⁵R⁶SO₂, wherein R⁵ and R⁶ may be the same or different and are hydrogen, lower alkyl, or aryl; R¹ and R² may together form a carbocyclic or methylenedioxy ring; R³ is hydrogen; R⁴ is hydrogen, lower alkyl, lower alkyl substituted by a substituted or unsubstituted heterocyclic group, methylcycloalkyl, benzyl, phenethyl, phenyl, substituted phenyl, alkyl, propargyl with the proviso that R¹, R², and R³ must be hydrogen when R⁴ is not hydrogen, for the preparation of a pharmaceutical for treating cerebrovascular disorders.
Claim 2
Dependent Claim
147 words
Use of a compound of the general formula I or of a pharmaceutically acceptable salt thereof wherein R¹ and R² are the same or different and are hydrogen, straight or branched alkyl of from one to six carbon atoms, lower alkylaryl, lower alkenyl, phenyl, CF₃, hydroxy, lower alkoxy, lower alkylthio, lower alkylsulphonyl, CF₃O at the six position, halogen, nitro, carboxy, lower alkoxycarbonyl, NR⁵R⁶CO, NR⁵R⁶, R⁵CONR⁵, CN, NR⁵R⁶SO₂, wherein R⁵ and R⁶ may be the same or different and are hydrogen, lower alkyl, or aryl; R¹ and R² may together form a carbocyclic or methylenedioxy ring; R³ is hydrogen; R⁴ is hydrogen, lower alkyl, lower alkyl substituted by a substituted or unsubstituted heterocyclic group, methylcycloalkyl, benzyl, phenethyl, phenyl, substituted phenyl, alkyl, propargyl with the proviso that R¹, R², and R³ must be hydrogen when R⁴ is not hydrogen, for the preparation of a pharmaceutical for treating cerebrovascular disorders.
Claim 3
Dependent Claim
14 words
Use according to Claim 1 wherein the cerebrovascular disorder is cerebral infarction or stroke.
Claim 4
Dependent Claim
44 words
Use according to Claim 1 or 2 wherein the compound I is a member selected from the group consisting of 2-amino-6-methylbenzothiazole, 2-amino-6-trifluoromethoxybenzothiazole, 2-amino-6-trifluoromethylbenzothiazole, 2-aminobenzothiazole, 2-amino-4-methylbenzothiazole, 2-amino-6-ethoxybenzothiazole, 2-amino-6-nitrobenzothiazole, 2-amino-5-methoxybenzothiazole, 2-amino-6-methylsulphonylbenzothiazole, 2-amino-4,6-dimethylbenzothiazole, ethylaminobenzothiazole, 2-benzylaminobenzothiazole, 2-amino-4-trifluoromethylbenzothiazole, 2-amino-5-trifluoromethylbenzothiazole, 2-amino-6-bromobenzothiazole, 2-amino-6-chlorobenzothiazole, 2-amino-4-chlorobenzothiazole, 2-amino-6-fluorobenzothiazole, 2-amino-5-methoxybenzothiazole, 2-amino-4,6-difluorobenzothiazole, 2-amino-6-methylthiobenzothiazole, 2-amino-naptho[1,2-d]thiazole, and 2-[[2-(1-methyl-2-pyrrolidinyl)ethyl]amino]-benzothiazole.
Claim 5
Dependent Claim
144 words
Use of a compound of the general Formula I or a pharmaceutically acceptable salt thereof wherein R¹ and R² are the same or different and are hydrogen, straight or branched alkyl of from one to six carbon atoms, lower alkylaryl, lower alkenyl, phenyl, CF₃, hydroxy, lower alkoxy, lower alkylthio, lower alkylsulphonyl, CF₃O, at the six position, halogen, nitro, carboxy, lower alkoxycarbonyl, NR⁵R⁶CO, NR⁵6⁶, R⁵CONR⁵, CN, NR⁵R⁶SO₂ wherein R⁵ and R⁶ may be the same or different and are hydrogen, lower alkyl, or aryl; R¹ and R² may together form a carbocyclic or methylenedioxy ring; R³ is hydrogen; R⁴ is hydrogen, lower alkyl, lower alkyl substituted by a heterocyclic or a substituted heterocyclic group, methylcycloalkyl, benzyl, phenethyl, phenyl, substituted phenyl, alkyl, propargyl with the proviso that R¹, R², and R³ must be hydrogen when R⁴ is not hydrogen for the preparation of an anesthetic pharmaceutical.
Claim 6
Dependent Claim
144 words
Use of a compound of the general Formula I or a pharmaceutically acceptable salt thereof wherein R¹ and R² are the same or different and are hydrogen, straight or branched alkyl of from one to six carbon atoms, lower alkylaryl, lower alkenyl, phenyl, CF₃, hydroxy, lower alkoxy, lower alkylthio, lower alkylsulphonyl, CF₃O, at the six position, halogen, nitro, carboxy, lower alkoxycarbonyl, NR⁵R⁶CO, NR⁵6⁶, R⁵CONR⁵, CN, NR⁵R⁶SO₂ wherein R⁵ and R⁶ may be the same or different and are hydrogen, lower alkyl, or aryl; R¹ and R² may together form a carbocyclic or methylenedioxy ring; R³ is hydrogen; R⁴ is hydrogen, lower alkyl, lower alkyl substituted by a heterocyclic or a substituted heterocyclic group, methylcycloalkyl, benzyl, phenethyl, phenyl, substituted phenyl, alkyl, propargyl with the proviso that R¹, R², and R³ must be hydrogen when R⁴ is not hydrogen for the preparation of an anesthetic pharmaceutical.
Claim 7
Dependent Claim
28 words
Use according to Claim 4 wherein the compound is used for the preparation of anesthetic pharmaceuticals to be used in surgical operations where risk of cerebrovascular damage exists.
Claim 8
Dependent Claim
25 words
A pharmaceutical composition comprising a cerebrovascularly effective amount of a compound as defined in Claim 1 and 4 in combination with a pharmaceutically acceptable carrier.
References Cited (Backward Citations)
No citation records indexed.
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