- 1,1-Diarylalkenes as anticancer agents: Dual inhibitors of tubulin polymerization and phosphodiesterase 4
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A series of 1,1-diarylalkene derivatives were prepared to optimize the properties of CC-5079 (1), a dual inhibitor of tubulin polymerization and phosphodiesterase 4 (PDE4). By using the 3-ethoxy-4-methoxyphenyl PDE4 pharmacophore as one of the aromatic ri
- Ruchelman, Alexander L.,Man, Hon-Wah,Chen, Roger,Liu, Wei,Lu, Ling,Cedzik, Dorota,Zhang, Ling,Leisten, Jim,Collette, Alice,Narla, Rama Krishna,Raymon, Heather K.,Muller, George W.
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p. 6356 - 6374
(2011/12/02)
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- RELEASE-CONTROL COMPOSITION
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The present invention relates to a controlled release capsule preparation for oral administration, which contains (i) a granule containing a physiologically active substance which is a compound represented by the formula: wherein n is an integer of 1 to 3, and Ar is an aromatic ring optionally having substituent(s), or a salt thereof, and a hydrophilic polymer, and coated with an enteric coating agent and the like, and (ii) a fluidizer. According to the present invention, a controlled release composition for oral administration of an imidazole derivative, which has steroid C17,20-lyase inhibiting activity and which has remarkably improved sustainability of the blood concentration, is provided.
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Page/Page column 29-30
(2008/06/13)
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- Novel imidazole derivatives, production method thereof and use thereof
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The present invention provides a compound having a steroid C17,20-lyase-inhibitory activity and useful for the therapy and prophylaxis of tumor such as prostatism, breast cancer and the like, and a method for efficiently separating an optically active compound of this compound from a mixture of optical isomers thereof, a compound of the formula: wherein each symbol is as defined in the specification, a salt thereof or a prodrug thereof, and a method for obtaining an optically active compound by optically resolving a mixture of optical isomers by the use of a resolving agent such as tartranilic acid and the like.
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- PROCESS FOR PRODUCING FUSED IMIDAZOLE COMPOUND, REFORMATSKY REAGENT IN STABLE FORM, AND PROCESS FOR PRODUCING THE SAME
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The present invention provides an industrially advantageous process for producing a steroid C17,20 lyase inhibitor represented by the general formula (I): and a Reformatsky reagent in a stable form suitable for the process.In the present invention, a compound represented by the general formula (I) is produced by reducing a specific β-hydroxy ester compound derivative or a salt thereof obtained from a specific carbonyl compound in a Reformatsky reaction in the presence of a metal hydride complex and a metal halide, and then subjecting it to a ring-closing reaction. In the above Reformatsky reaction, it is useful to use a stable solution of a compound represented by the general formula BrZnCH2COOC2H5 or a crystal of the compound which is represented by the formula (BrZnCH2COOC2H5·THF)2.
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