- IMIDAZOLYL MODULATORS OF 5-HT3 RECEPTORS
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The present invention relates to new imidazolyl modulators of 5-HT3 receptors, pharmaceutical compositions thereof, and methods of use thereof.
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- Process for preparing 1,2,3,9-tetrahydro-9-methyl-3-methylene-4H-carbazol-4-one and ondansetron therefrom
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The present invention provides a rapid, high-yielding process for preparing 1,2,3,9-tetrahydro-9-methyl-3-methylene-4H-carbazol-4-one from 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one without using a secondary amine as a catalyst, and without using glacial acetic acid as a solvent. The present invention further provides a rapid, high-yielding process for preparing ondansetron from 1,2,3,9-tetrahydro-9-methyl-3-methylene-4H-carbazol-4-one without using alumina as a catalyst.
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- PROCESS FOR PREPARING 1,2,3,9-TETRAHYDRO-9-METHYL-3-[(2-METHYL-1H-IMIDAZOLE-1-YL)METHYL]-4H-CARBAZOL-4-ONE OR ITS SALT
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1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]- 4H-carbazol-4-one or its salt is prepared in high yield by reacting a compound of formula 2 with a compound of formula 3 and a compound of formula 4 in the presence of an acid, an alkylsilylhalide compound or an acylhalide compound, in an solvent, and thus, such an inventive process can be favorably applied to a large-scale mass production thereof.
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- PROCESS FOR PREPARING 1,2,3,9-TETRAHYDRO-9-METHYL-3-[(2-METHYL-1H-IMIDAZOLE-1-YL)METHYL]-4H-CARBAZOL-4-ONE OR ITS SALT
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The present invention provides an improved process for preparing 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-carbazol-4-one or its salt, which is useful as an anti-vomiting agent, in a high yield under a mild condition, so as to be favorably applied to a large-scale mass production thereof.
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- HIGH PURITY ONDANSETRON HYDROCHLORIDE DIHYDRATE AND PROCESS FOR ITS SYNTHESIS
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The invention relates to high purity ondansetron hydrochloride dihydrate containing not more than 0.10 w/w % chemical impurities as well as to the process for its synthesis.
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- Novel crystal and solvate forms of ondansetron hydrochloride and processes for their preparation
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The present invention provides novel ondansetron hydrochloride crystalline polymorphic forms and solvates. Processes for making and interconverting the polymorphic forms are also provided. Further provided are pharmaceutical compositions and therapeutic methods using the novel polymorphic forms and hydrates.
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- Method for treating nausea and vomiting
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The invention relates to the use of compounds of the general formula (I) STR1 wherein R1 represents a hydrogen atom or a C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycoalkyl-(C1-4) alkyl, C3-6 alkenyl, C3-10 alkynyl, phenyl or phenyl-C1-3 alkyl group, and one of the groups represented by R2,R3 and R4 is a hydrogen atom or a C1-6 alkyl, C3-7 cycloalkyl, C2-6 alkenyl or phenyl - C1-3 alkyl group and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C1-6 alkyl group; and physiologically acceptable salts and solvates thereof, for the relief of nausea and vomiting and/or the promotion of gastric emptying and for the manufacture of a medicament for this purpose. Promotion of gastric emptying may be for the relief of gastro-intestinal disorders associated with gastric stasis or may be of advantage of radiological examination procedures. The invention also relates to a product containing a therapeutic agent liable to induce nausea and vomiting, e.g. a cytostatic agent such as a cyclophosphamide, an alkylating agent or a platinum complex, and a compound of the general formula (I) as a combined preparation for simultaneous separate or sequential use in therapy.
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- 1,2,3,9-tetrahydro-3-imidazol-1-ylmethyl-4H-carbazol-4-ones, composition containing them, and method of using them to treat neuronal 5HT function disturbances
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The invention relates to compounds of formula (I). STR1 wherein R 1 represents a hydrogen atom or a C 1-10 alkyl, C 3-7 cycloalkyl, C 3-6 alkenyl, C 3-7 cycloalkyl-(C 1-4) alkyl, C 3-10 alkynyl, phenyl or phenyl-C 1-3 alkyl group, and one of the groups represented by R 2, R 3 and R 4 is a hydrogen atom or a C 1-6 alkyl, C 3-7 cycloalkyl, C 2-6 alkenyl or phenyl-(C 1-3) alkyl group and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C 1-6 alkyl group; and physiologically acceptable salts and solvates, e.g. hydrates thereof.The compounds are potent selective antagonists at ""neuronal"" 5-hydroxytryptamine receptors and are useful in the treatment of migraine and psychotic disorders such as schizophrenia.
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