US4171373A
Expired / Lapsed
US
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Ethynylbenzene compounds and derivatives thereof to treat pain, fever and inflammation
Assignee: William H Rorer Inc
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Filing: 1977-12-06
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Granted: 1979-10-16
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Expires: 1997-12-06
Abstract
Abstract The method of treating patients by administering an effective amount of a mercapto, lower acyl thio or lower alkyl thio substituted ethynylbenzene compound, and the pharmaceutical preparation thereof.
Inventors
- 👤 Julius Diamond
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 04:47
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/095; A61K31/10; C; C07; C07C; C07C205/00; C07C205/49; C07C205/56; C07C2601/00; C07C2601/12; C07C2601/14
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
117 words
A method of treating inflammation, pain or fever in a warm-blooded animal which comprises administering to the animal an effective non-toxic amount of an active compound of the formula ##STR8## wherein R is hydrogen, alkyl of 1 to 7 carbon atoms, cycloalkyl of 5 to 7 carbon atoms, 1to 7 carbon atoms alkyl substituted cycloalkenyl of 5 to 7 carbon atoms, phenyl or substituted phenyl where the substituent is Y", Y and Y' are each selected from the group consisting of hydrogen, mercapto, lower acylthio and lower alkyl thio; Y" is selected from the group consisting of: Y, lower alkyl, and trifluoromethyl, with the proviso that at least one of Y and Y' is other than hydrogen.
Claim 2
Independent Claim
117 words
A method of treating inflammation, pain or fever in a warm-blooded animal which comprises administering to the animal an effective non-toxic amount of an active compound of the formula ##STR8## wherein R is hydrogen, alkyl of 1 to 7 carbon atoms, cycloalkyl of 5 to 7 carbon atoms, 1to 7 carbon atoms alkyl substituted cycloalkenyl of 5 to 7 carbon atoms, phenyl or substituted phenyl where the substituent is Y", Y and Y' are each selected from the group consisting of hydrogen, mercapto, lower acylthio and lower alkyl thio; Y" is selected from the group consisting of: Y, lower alkyl, and trifluoromethyl, with the proviso that at least one of Y and Y' is other than hydrogen.
Claim 3
Dependent Claim
33 words
The method of claim 1, wherein the active compound is of the formula ##STR9## wherein x is 0-2, and R' is selected from the group consisting of hydrogen, lower alkyl and lower acyl.
Claim 4
Dependent Claim
11 words
The method of claim 2, wherein the active compound is 3-acetylthio-4-cyclohexylethynylbenzene.
Claim 5
Dependent Claim
11 words
The method of claim 2, wherein the active compound is 3-methylthio-4-cyclohexylethynylbenzene.
Claim 6
Dependent Claim
11 words
The method of claim 2, wherein the active compound is 3-mercapto-4-cyclohexylethynylbenzene.
Claim 7
Independent Claim
113 words
A method of treating inflammation, pain or fever in a warm-blooded animal which comprises administering to the animal an effective non-toxic amount of an active compound of the formula ##STR10## wherein R is hydrogen, alkyl of 1 to 7 carbon atoms, cycloalkyl of 5 to 7 carbon atoms, 1to 7 carbon atoms alkyl substituted cycloalkenyl of 5 to 7 carbon atoms, phenyl or substituted phenyl where the substituent is Y", Y and Y' are each selected from the group consisting of hydrogen, and lower acylthio; Y" is selected from the group consisting of: Y, lower alkyl, and trifluoromethyl, with the proviso that at least one of Y and Y' is other than hydrogen.
Claim 8
Independent Claim
113 words
A method of treating inflammation, pain or fever in a warm-blooded animal which comprises administering to the animal an effective non-toxic amount of an active compound of the formula ##STR10## wherein R is hydrogen, alkyl of 1 to 7 carbon atoms, cycloalkyl of 5 to 7 carbon atoms, 1to 7 carbon atoms alkyl substituted cycloalkenyl of 5 to 7 carbon atoms, phenyl or substituted phenyl where the substituent is Y", Y and Y' are each selected from the group consisting of hydrogen, and lower acylthio; Y" is selected from the group consisting of: Y, lower alkyl, and trifluoromethyl, with the proviso that at least one of Y and Y' is other than hydrogen.
Claim 9
Dependent Claim
23 words
The method of claim 6 wherein the active compound is of the formula ##STR11## wherein x is 0-2, and R' is lower acyl.
Claim 10
Dependent Claim
134 words
A pharmaceutical preparation in a dosage unit form adapted for administration to warm-blooded animals for the treatment of inflammation, pain or fever, comprising an effective non-toxic amount of an active compound of the formula ##STR12## where R is hydrogen, alkyl of 1 to 7 carbon atoms, cycloalkyl of 5 to 7 carbon atoms, 1to 7 carbon atoms alkyl substituted cycloalkyl of 5 to 7 carbon atoms, cycloalkenyl of 5 to 7 carbon atoms, phenyl or substituted phenyl where the substituent is Y"; Y and Y' are each selected from the group consisting of hydrogen, mercapto, lower acylthio and lower alkyl thio; Y" is selected from the group consisting of Y, lower alkyl and trifluoromethyl, with the proviso that at least one of Y and Y' is other than hydrogen, and a suitable pharmaceutical carrier.
Claim 11
Dependent Claim
134 words
A pharmaceutical preparation in a dosage unit form adapted for administration to warm-blooded animals for the treatment of inflammation, pain or fever, comprising an effective non-toxic amount of an active compound of the formula ##STR12## where R is hydrogen, alkyl of 1 to 7 carbon atoms, cycloalkyl of 5 to 7 carbon atoms, 1to 7 carbon atoms alkyl substituted cycloalkyl of 5 to 7 carbon atoms, cycloalkenyl of 5 to 7 carbon atoms, phenyl or substituted phenyl where the substituent is Y"; Y and Y' are each selected from the group consisting of hydrogen, mercapto, lower acylthio and lower alkyl thio; Y" is selected from the group consisting of Y, lower alkyl and trifluoromethyl, with the proviso that at least one of Y and Y' is other than hydrogen, and a suitable pharmaceutical carrier.
Claim 12
Dependent Claim
33 words
The method of claim 2, wherein the active compound is of the formula ##STR13## wherein x is 0-2, and R' is selected from the group consisting of hydrogen, lower alkyl and lower acyl.
Claim 13
Dependent Claim
11 words
The method of claim 9, wherein the active compound is 3-acetylthio-4-cyclohexylethynylbenzene.
Claim 14
Dependent Claim
11 words
The method of claim 9, wherein the active compound is 3-methylthio-4-cyclohexylethynylbenzene.
Claim 15
Dependent Claim
11 words
The method of claim 9, wherein the active compound is 3-mercapto-4-cyclohexylethynylbenzene.
Claim 16
Dependent Claim
130 words
A pharmaceutical preparation in a dosage unit form adapted for administration to warm-blooded animals for the treatment of inflammation, pain or fever, comprising an effective non-toxic amount of an active compound of the formula ##STR14## where R is hydrogen, alkyl of 1 to 7 carbon atoms, cycloalkyl of 5 to 7 carbon atoms, 1to 7 carbon atoms alkyl substituted cycloalkyl of 5 to 7 carbon atoms, cycloalkenyl of 5 to 7 carbon atoms, phenyl or substituted phenyl where the substituent is Y"; Y and Y' are each selected from the group consisting of hydrogen and lower acylthio; Y" is selected from the group consisting of Y, lower alkyl and trifluoromethyl, with the proviso that at least one of Y and Y' is other than hydrogen, and a suitable pharmaceutical carrier.
Claim 17
Dependent Claim
130 words
A pharmaceutical preparation in a dosage unit form adapted for administration to warm-blooded animals for the treatment of inflammation, pain or fever, comprising an effective non-toxic amount of an active compound of the formula ##STR14## where R is hydrogen, alkyl of 1 to 7 carbon atoms, cycloalkyl of 5 to 7 carbon atoms, 1to 7 carbon atoms alkyl substituted cycloalkyl of 5 to 7 carbon atoms, cycloalkenyl of 5 to 7 carbon atoms, phenyl or substituted phenyl where the substituent is Y"; Y and Y' are each selected from the group consisting of hydrogen and lower acylthio; Y" is selected from the group consisting of Y, lower alkyl and trifluoromethyl, with the proviso that at least one of Y and Y' is other than hydrogen, and a suitable pharmaceutical carrier.
Claim 18
Dependent Claim
23 words
The method of claim 7 wherein the active compound is of the formula ##STR15## wherein x is 0-2 and R' is lower acyl.
References Cited (Backward Citations)
US3821289A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-10-15 | 1983-04-16 | 1983-10-16 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-10-15 | 1987-04-16 | 1987-10-16 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-10-15 | 1991-04-16 | 1991-10-16 | $7700.00 | Window Closed / Lapsed |