The dehydration is known and may be carried out, for example, by refluxing with heating, in an organic solvent erg. The deprotection of R Y is known and may be carried out, for example, in a solvent e. As a result, the present inventors have found that the purpose may be achieved with aryl sulfide, sulfoxide, sulfone derivatives of the formula I. Clinical investigations have identified activated ras genes in a wide variety of human neoplasms, including carcinomas, sarcomas, leukemias, and lymphomas. Finally, the instant compounds may be usefully employed as metal ion and metalloprotein chelators.
Arylalkylamines, process for preparing them and pharmaceutical compositions containing them. Peptidyl derivatives and their use as metalloproteinases inhibitors.
Purification may be carried out after each reaction, or after a series of reactions. The following examples were prepared similarly to above syntheses. The reaction mixture was concentrated. Hydroxamic acid derivatives as inhibitors of cytokine production. The layers were separated, and the organic extract was washed with dilute sodium bicarbonate, then was dried over sodium sulfate.
The oxidation is known and may be carried out, for example, in an organic solvent e. This reaction is known and may be carried out, for example, in an organic solvent e. For preparation of such spray compositions, for example, the method described in the U. The organic extract was dried over sodium sulfate and evaporated. The diastereomers may be separated by chromatography.
Triton soluble fractions lanes and the same fractions following immunoprecipitation with an anti-ras monoclonal antibody lanes are also shown. The compounds of the present invention of the formula I may be converted into the corresponding salts by known method.
Purified and analyzed as above. Toluene mL was added, the solution was concentrated to a slurry, and the product collected on a filter. The organic layer was dried over anhydrous magnesium sulfate, filterd and concentrated.
The residue was washed with ether to give the title compound mg having the following physical data. Novel benzodiazepinone derivatives, preparation method and intermediates thereof, medicament application and pharmaceutical compositions comprising the same. For example, C carbocyclic aryl includes benzene, pentalene, indene, naphthalene, azulene etc. And further, coating may include containment within capsules of absorbable materials such as gelatin. When an acid is used, a salt thereof may be used.
In the present invention, non-toxic salts includes all such salts. Methods and compositions for the identification, characterization, and inhibition of farnesyltransferase. The deprotection under alkali or acidic conditions, or hydrogenolysis, may be carried out by the methods as hereinbefore described. Capsules include hard capsules and soft capsules.
Thiophene and thiazole substituted trifluoroethanone derivatives as histone deacetylase hdac inhibitors. Use of inhibitors of prenyltransferases for the preparation of a medicament for the treatment of diseases resulting from the membrane fixation of the heterotrimeric g protein.
The resulting product is subsequently purified by chromatography or crystallization. Recombinant enzyme was produced in a baculovirus expression system as in O'Reilly, D. Method of determining acute myeloid leukemia response to treatment with farnesyltransferase inhibitors. The following reference examples and examples illustrate the present invention, but do not limit the present invention. However, these substrate-analogous inhibitors might have various problems.
When racemic starting materials are employed, diastereomeric products are obtained. Hydroxyalkanoylaminolactams and related structures as inhibitors of Alphabeta protein production. Oxidant sensitive and insensitive aromatic esters as inhibitors of human neutrophil elastase. Candida geranylgeranyl-protein transferase polypetide, compositions and methods related thereto.
This reaction is known and may be carried out, for example, by refluxing with heating, in an organic solvent e. Mobile communication terminal and multimedia message processing method using the same. Further examples of these groups are found in E.
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As shown in the panels A, C, and E, all three cell lines grew logarithmically with no added inhibitor. Arylsulfonamido-substituted hydroxamic acids.
The reaction mixture was diluted with ethyl acetate. Also, the following compounds are already known. Aqueous solutions and suspensions may include distilled water for injection or physiological salt solution. The alkyl, aryl, or heterocycle moieties may be substituted with protected -P.
As shown for some peptides, several inhibitors tightly bind the enzyme and inhibit its activity, yet are not a substrate for the enzyme. Hydroxyalkanoylaminolactams and related structures as inhibitors of a beta protein production. The reaction solution was extracted with ethyl acetate. The reaction solution was concentrated and benzene was added to the residue, and then the solution was concentrated again.
Methods of determining acute myeloid leukemia response to treatment with farnesyltransferase inhibitors. The organic phase was washed with brine, dried over magnesium sulfate, filtered, english handwriting practice book pdf and concentrated. Cells transformed in this way grow and differentiate in an abnormal way.
The molecule was then cleaved, purified and analyzed as above. Non toxic and water-soluble salts are preferable.
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