- Design and synthesis of orally available MEK inhibitors with potent in vivo antitumor efficacy
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The structure-based design, synthesis, and biological evaluation of two novel series of potent and selective MEK kinase inhibitors are described herein. The elaboration of a lead pyrrole derivative to a bicyclic dihydroindolone core provided compounds wit
- Adams, Mark E.,Wallace, Michael B.,Kanouni, Toufike,Scorah, Nicholas,O'Connell, Shawn M.,Miyake, Hiroshi,Shi, Lihong,Halkowycz, Petro,Zhang, Lilly,Dong, Qing
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scheme or table
p. 2411 - 2414
(2012/05/05)
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- POLYMORPHS OF A MEK INHIBITOR
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The present invention relates to polymorphic forms of 7-(4-Bromo-2-fluoro-phenylamino)-6-methyl-5-oxo-1,3,5-tetrahydro-indolizine-8-carboxylic acid (2-hydroxy-ethoxy)-amide and a hydrate thereof which are useful in the treatment of a disease, disorder or syndrome associated with MEK inhibition, such as cancer, in mammals. The invention also relates to compositions thereof and to methods of using such compositions in the treatment of cancer in mammals, especially humans.
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Page/Page column 17
(2011/06/25)
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- MEK INHIBITOR SALTS AND SOLVATES THEREOF
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The present invention relates to sodium salt forms of 7-(4-Bromo-2-fluoro- phenylamino)-6-methyl-5-oxo-1,3,5-tetrahydro-indolizine-8-carboxylic acid (2- hydroxyethoxy)-amide and 7-(4-Bromo-2-fluoro-phenylamino)-5-oxo- 1,2,3,5-tetrahydro- indolizine-8-carboxylic acid cyclopropylmethoxy-amide and their corresponding solvates and polymorphs, which are useful in the treatment of a disease, disorder or syndrome associated with MEK inhibition, such as cancer, in mammals.
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Page/Page column 14; 21
(2011/06/25)
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- MAPK/ERK KINASE INHIBITORS
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Compounds of the following formula are provided for use with MEK: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
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Page/Page column 37; 38
(2009/05/28)
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- Heterocyclic Compounds as MEK Inhibitors
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The present invention relates to compounds of formula I and pharmaceutically acceptable salts. These compounds can act as potential MEK inhibitors in the treatment of hyperproliferative diseases, like cancer and inflammation. The present invention also reveals methods of preparation thereof.
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Page/Page column 22; 80
(2009/12/02)
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