EP0067770A2
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EP
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Treatment of migraine with tropyl benzoate derivatives
Assignee: Sanofi Aventis France
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Filing: 1982-06-11
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Granted: —
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Expires: 2002-06-11
Abstract
Abstract Migraine is treated with a tropyl benzoate derivative of the following general Formula 1:-wherein:-R, represents C<sub>1</sub>-C<sub>4</sub> alkyl, C<sub>1</sub>-C<sub>4</sub> alkoxy; or halogen;R<sub>2</sub> represents hydrogen, C<sub>1</sub>-C<sub>4</sub> alkyl, C<sub>1</sub>-C<sub>4</sub> alkoxy or halogen; andR<sub>3</sub> represents hydrogen, C<sub>1</sub>-C<sub>4</sub> alkyl, C<sub>1</sub>-C<sub>4</sub> alkoxy, or halogen provided that R<sub>3</sub> is hydrogen when R<sub>2</sub> is hydrogen.Some of the tropyl benzoate derivatives of Formula I are novel compounds.
Inventors
- 👤 John Richard Fozard
- 👤 Maurice Ward Gittos
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-09 21:15
CPC Classifications
C; C07; C07D; C07D451/00; C07D451/02; C07D451/04; C07D451/06; C07D451/12; A; A61; A61P; A61P25/00; A61P25/04; A61P43/00
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
111 words
A pharmaceutical composition in unit dose form for the treatment of migraine comprising, in admixture or otherwise associated with a pharmaceutically acceptable diluent or carrier, an amount of 0.5 to 100mg per unit dose of a tropyl benzoate derivative of the following general Formula I:- wherein:- R 1 represents C 1 -C 4 alkyl, C 1 -C 4 alkoxy; or halogen; R 2 represents hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy or halogen; and R 3 represents hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, or halogen provided that R 3 is hydrogen when R 2 is hydrogen; or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
111 words
A pharmaceutical composition in unit dose form for the treatment of migraine comprising, in admixture or otherwise associated with a pharmaceutically acceptable diluent or carrier, an amount of 0.5 to 100mg per unit dose of a tropyl benzoate derivative of the following general Formula I:- wherein:- R 1 represents C 1 -C 4 alkyl, C 1 -C 4 alkoxy; or halogen; R 2 represents hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy or halogen; and R 3 represents hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, or halogen provided that R 3 is hydrogen when R 2 is hydrogen; or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
18 words
A composition as claimed in Claim 1 containing 1 to 50 mg of said compound per unit dose.
Claim 4
Dependent Claim
18 words
A composition as claimed in Claim 2 containing 3 to 30 mg of said compound per unit dose.
Claim 5
Dependent Claim
28 words
A composition as claimed in any one of the preceding Claims wherein R 1 represents methyl, methoxy or chlorine, R 2 represents hydrogen, and R 3 represents hydrogen.
Claim 6
Dependent Claim
33 words
A composition as claimed in any one of Claims 1 to 3 wherein R 1 and R 2 are the same and each represents methyl, methoxy or chlorine, and R 3 represents hydrogen.
Claim 7
Dependent Claim
32 words
A composition as claimed in any one of Claims 1 to 3 wherein R 1 , R 2 and R 3 are all the same and each represents methyl, methoxy or chlorine.
Claim 8
Dependent Claim
28 words
A composition as claimed in any one of Claims 1 to 3 wherein the tropylbenzoate derivative is selected from tropyl-3-methoxybenzoate, tropyl-3,5-dimethoxybenzoate, tropyl-3,4,5-trimethoxybenzoate and pharmaceutically acceptable salts thereof. t
Claim 9
Dependent Claim
27 words
A composition as claimed in any one of Claims 1 to 3 wherein the tropylbenzoate derivative is selected from tropyl-3-chlorobenzoate, tropyl-3,4-dichlorobenzoate, tropyl-3,4,5-trichlorobenzoate, and pharmaceutically acceptable salts thereof.
Claim 10
Dependent Claim
28 words
A composition as claimed in any one of Claims 1 to 3 wherein the tropylbenzoate derivative is selected from tropyl- 3-methylbenzoate, tropyl-3,5-dimethylbenzoate, tropyl-3,4,5-trimethylbenzoate, and pharmaceutically acceptable salts thereof.
Claim 11
Dependent Claim
99 words
A tropyl benzoate derivative of the following general Formula I: - wherein:- R 1 represents C l -C 4 alkyl, C 1 - C 4 alkoxy; or halogen; R 2 represents hydrogen, C l -C 4 alkyl, C 1 -C 4 alkoxy or halogen; and R 3 represents hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, or halogen provided that R 3 is hydrogen when R 2 is hydrogen excluding those in which R 1 , R 2 and R 3 are in a combination specified in Table I hereinbefore, or a pharmaceutically acceptable salt thereof.
Claim 12
Dependent Claim
99 words
A tropyl benzoate derivative of the following general Formula I: - wherein:- R 1 represents C l -C 4 alkyl, C 1 - C 4 alkoxy; or halogen; R 2 represents hydrogen, C l -C 4 alkyl, C 1 -C 4 alkoxy or halogen; and R 3 represents hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, or halogen provided that R 3 is hydrogen when R 2 is hydrogen excluding those in which R 1 , R 2 and R 3 are in a combination specified in Table I hereinbefore, or a pharmaceutically acceptable salt thereof.
Claim 13
Dependent Claim
14 words
A compound selected from tropyl-3,5-dimethoxybenzoate, tropyl-3-methylbenzoate, tropyl-3,5-dimethylbenzoate, tropyl-3,4,5-trimethylbenzoate, tropyl-3,4,5-trichlorobenzoate and pharmaceutically acceptable salts thereof.
Claim 14
Dependent Claim
14 words
A compound selected from tropyl-3,5-dimethoxybenzoate, tropyl-3-methylbenzoate, tropyl-3,5-dimethylbenzoate, tropyl-3,4,5-trimethylbenzoate, tropyl-3,4,5-trichlorobenzoate and pharmaceutically acceptable salts thereof.
Claim 15
Dependent Claim
34 words
An analogous process for preparing a compound as claimed in Claim 10 which comprises the reaction in manner known per se of tropine and the corresponding acid halide of the following general Formula IV
Claim 16
Dependent Claim
104 words
A tropyl benzoate derivative of the following general Formula I:- wherein:- R 1 represents C 1 -C 4 alkyl, C 1 -C 4 alkoxy; or halogen; R 2 represents hydrogen, C l -C 4 alkyl, C 1 -C 4 alkoxy or halogen; and R 3 represents hydrogen, C 1 -C 4 alkyl, C1 - C4 alko xy, or halogen provided that R 3 is hydrogen when R 2 is hydrogen excluding those in which R l , R 2 and R 3 are in a combination specified in Table I hereinbefore, or a pharmaceutically acceptable salt thereof for use in the treatment of migraine.
Claim 17
Dependent Claim
104 words
A tropyl benzoate derivative of the following general Formula I:- wherein:- R 1 represents C 1 -C 4 alkyl, C 1 -C 4 alkoxy; or halogen; R 2 represents hydrogen, C l -C 4 alkyl, C 1 -C 4 alkoxy or halogen; and R 3 represents hydrogen, C 1 -C 4 alkyl, C1 - C4 alko xy, or halogen provided that R 3 is hydrogen when R 2 is hydrogen excluding those in which R l , R 2 and R 3 are in a combination specified in Table I hereinbefore, or a pharmaceutically acceptable salt thereof for use in the treatment of migraine.
Claim 18
Dependent Claim
21 words
A compound selected from tropyl-3,5-dimethoxybenzoate, tropyl-3-methylbenzoate, tropyl-3,5-dimethylbenzoate, tropyl-3,4,5-trimethylbenzoate, tropyl-3,4,5-trichlorobenzoate and pharmaceutically acceptable salts thereof for use in the treatment of migraine.
Claim 19
Dependent Claim
21 words
A compound selected from tropyl-3,5-dimethoxybenzoate, tropyl-3-methylbenzoate, tropyl-3,5-dimethylbenzoate, tropyl-3,4,5-trimethylbenzoate, tropyl-3,4,5-trichlorobenzoate and pharmaceutically acceptable salts thereof for use in the treatment of migraine.
References Cited (Backward Citations)
No citation records indexed.
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