Pharmaceutical compositions for headache, migraine, nausea and emesis
AssigneeMeditor Pharmaceuticals Ltd.
InventorsRaphael Barkan, Alexander Mirimsky
Life of this patent
Estimating the term…
Abstract
S-alkylsiothiouronium derivatives such as S-ethylisothiouronium diethylphosphate are used for the treatment of headaches, in particular, migraines, as well as for the prevention or treatment of nausea and vomiting. The compositions of the invention are also effective in preventing or alleviating emesis associated with migraines or other medical conditions such as chemotherapy or radiotherapy, as well as other symptoms of migraines including phonophobia and photophobia.
Claims47
A pharmaceutical composition for the treatment of headache, migraine, nausea or vomiting comprising, as an active ingredient, a compound having the general formula:
- 7
- wherein,
- R1 is a linear or branched saturated or unsaturated alkylene, comprising one to eight carbon atoms optionally substituted with one or more substituent selected from the group consisting of halogen, primary, secondary or tertiary amine, primary, secondary or tertiary alcohol, or interrupted by one or more heteroatom selected from the group consisting of O, N, and S;
- R2, R3, R4 and R5 are each independently a hydrogen, hydroxy, linear or branched lower alkyl, linear or branched lower alkenyl, linear or branched lower alkynyl, lower alkoxy, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, lower thioalkoxy, nitro, amino, cyano, sulfonyl, haloalkyl, carboaryloxy, carboalkylaryloxy, alkyl sulfoxide, aryl sulfoxide, alkyl sulfone, aryl sulfone, alkyl sulfate, aryl sulfate, sulfonamide, thioalkyl, optionally substituted by halogen;
- A− is a physiologically acceptable anion;
- together with and a pharmaceutically acceptable carrier or diluent.
Use for the preparation of a medicament for treatment of headache migraine or nausea and vomiting, of a compound having the general formula:
- 8
- wherein,
- R1 is a linear or branched saturated or unsaturated alkylene, comprising one to eight carbon atoms optionally substituted with one or more substituent selected from the group consisting of halogen, primary, secondary or tertiary amine, primary, secondary or tertiary alcohol, or interrupted by one or more heteroatom selected from the group consisting of O, N, and S;
- R2, R3, R4 and R5 are each independently a hydrogen, hydroxy, linear or branched lower alkyl, linear or branched lower alkenyl, linear or branched lower alkynyl, lower alkoxy, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, lower thioalkoxy, nitro, amino, cyano, sulfonyl, haloalkyl, carboaryloxy, carboalkylaryloxy, alkyl sulfoxide, aryl sulfoxide, alkyl sulfone, aryl sulfone, alkyl sulfate, aryl sulfate, sulfonamide, thioalkyl, optionally substituted by halogen;
- A− is a physiologically acceptable anion;
- together with and a pharmaceutically acceptable carrier or diluent.
18 Use according to claim 15, wherein each of said tablets, capsules or ampoules comprises between 40 and 80 mg of the compound.
A method of treating headache or migraine, the method comprising the step of administering to a subject a therapeutically effective amount of a compound having the general formula:
- 9
- wherein, R1 is a linear or branched saturated or unsaturated alkylene, comprising one to eight carbon atoms optionally substituted with one or more substituent selected from the group consisting of halogen, primary, secondary or tertiary amine, primary, secondary or tertiary alcohol, or interrupted by one or more heteroatom selected from the group consisting of O, N, and S;
- R2, R3, R4 and R5 are each independently a hydrogen, hydroxy, linear or branched lower alkyl, linear or branched lower alkenyl, linear or branched lower alkynyl, lower alkoxy, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, lower thioalkoxy, nitro, amino, cyano, sulfonyl, haloalkyl, carboaryloxy, carboalkylaryloxy, alkyl sulfoxide, aryl sulfoxide, alkyl sulfone, aryl sulfone, alkyl sulfate, aryl sulfate, sulfonamide, thioalkyl, optionally substituted by halogen;
- A− is a physiologically acceptable anion;
- together with and a pharmaceutically acceptable carrier or diluent.
A method of preventing or alleviating nausea or vomiting, the method comprising the step of administering to a subject a therapeutically effective amount of a compound having the general formula:
- 10
- wherein, R1 is a linear or branched saturated or unsaturated alkylene, comprising one to eight carbon atoms optionally substituted with one or more substituent selected from the group consisting of halogen, primary secondary or tertiary amine, primary secondary or tertiary alcohol, or interrupted by one or more heteroatom selected from the group consisting of O, N, and S;
- R2, R3, R4 and R5 are each independently a hydrogen, hydroxy, linear or branched lower alkyl, linear or branched lower alkenyl, linear or branched lower alkynyl, lower alkoxy, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, lower thioalkoxy, nitro, amino, cyano, sulfonyl, haloalkyl, carboaryloxy, carboalkylaryloxy, alkyl sulfoxide, aryl sulfoxide, alkyl sulfone, aryl sulfone, alkyl sulfate, aryl sulfate, sulfonamide, thioalkyl, optionally substituted by halogen;
- A− is a physiologically acceptable anion;
- together with and a pharmaceutically acceptable carrier or diluent.
Dependencies are inferred from the claim text.