The invention is directed to 6-(4-pyι?midinyl)-1 H-indazole derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein R1 - R4 are defined herein. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of immune and metabolic diseases and disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
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Page/Page column 204-205
(2010/07/10)
SUBSTITUTED BENZOTHIOPHENE COMPOUNDS AND USES THEREOF
Disclosed are compounds of the formula (I), wherein R1, R2, R3 and R4 are described herein, which are active as anti-inflammatory agents. Also disclosed are methods of using and making such compounds.
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Page/Page column 54-55
(2010/02/10)
The Synthesis and Transition Temperatures of Some Fluoro-Substituted 4-Cyanophenyl and 4-Cyanobiphenyl-4'-yl 4-Pentyl- and 4-Butoxy-Benzoates
A series of 4-cyanophenyl 4-X-benzoates and a series of 4-cyanobiphenyl-4'-yl 4-X-benzoates (X= pentyl, butoxy) have been prepared without fluoro-substitution and with mono-fluoro to tetra-fluoro-substitution; all possible combinations of substitution patterns at the positions ortho- to the cyano group and ortho- to the carboxylate group have been obtained in an attempt to determine the structural features which are responsible for some members of these series showing very large positive values of dielectric anisotropy.The synthesis of novel precursors required for the preparation of these esters is described and the melting points and transition temperatures of the esters are discussed and an explanation is provided for the variation of Tn-1 values with position and extent of fluoro-substitution. - Keywords: Fluoro-substitution, phenyl and biphenyl benzoates, terminal cyano namatogens.
Gray, G. W.,Hird, M.,Lacey, D.,Toyne, K. J.
p. 165 - 190
(2007/10/02)
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