- BENZAZOLE DERIVATIVES, COMPOSITIONS, AND METHODS OF USE AS AURORA KINASE INHIBITORS
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The present invention relates to compounds and methods from the treatment of cancer. The invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising compounds that inhibit Aurora kinase, and methods for the treatment of cancer using the compounds of the presentation invention or pharmaceutical compositions comprising compounds of the present invention.
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Page/Page column 62-63
(2010/11/28)
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- Lactam inhibitors of factor Xa and method
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Lactam inhibitors are provided which have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, and prodrug esters thereof, wherein n is 1 to 5; and and R1, R2, R3, R4, R5 , R6, R7, R8, R9, R10, R10a, 1011 and R12 are as defined herein. These compounds are inhibitors of Factor Xa and thus are useful as anticoagulants. A method for treating cardiovascular diseases associated with thromboses is also provided.
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- SYNTHESIS OF SUBSTITUTED PYRAZOLO- AND PYRAZOLOPHENOTHIAZINE DERIVATIVES
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The synthesis of new pyrazolo- and phenothiazines by the Bernthsen thionation of N-arylindazoles obtained using organometalic compounds is reported.
- Boyer, Gerard,Galy, Jean Pierre,Barbe, Jacques
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p. 487 - 496
(2007/10/02)
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- Synthesis of Pyrazoloacridin-9(10H)-ones
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Eight pyrazoloacridin-9(10H)-ones were prepared in a three step procedure from 5- and 6-nitroindazoles.Palladium catalysed hydrogenation of nitroindazoles afforded the corresponding 5- and 6-aminoindazoles.These, in turn, reacted with o-chlorobenzoic acid under the conditions of the Ullman reaction to give anthranilic acids.Cyclisation of these acids by means of sulfuric acid led to the title compounds.If phosphoryl chloride was used, instead of sulfuric acid, a 9-chloroacridine derivative was obtained.All the compounds were characterised by 1H NMR spectroscopy.
- Boyer, Gerard,Galy, Jean-Pierre,Faure, Robert,Elguero, Jose,Barbe, Jacques
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p. 2601 - 2615
(2007/10/02)
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