158579-73-8Relevant articles and documents
Second generation 2-pyridyl biphenyl amide inhibitors of the hedgehog pathway
Castanedo, Georgette M.,Wang, Shumei,Robarge, Kirk D.,Blackwood, Elizabeth,Burdick, Daniel,Chang, Christine,Dijkgraaf, Gerrit J.P.,Gould, Stephen,Gunzner, Janet,Guichert, Oivin,Halladay, Jason,Khojasteh, Cyrus,Lee, Leslie,Marsters Jr., James C.,Murray, Lesley,Peterson, David,Plise, Emile,Salphati, Laurent,De Sauvage, Frederic J.,Wong, Susan,Sutherlin, Daniel P.
, p. 6748 - 6753 (2011/01/12)
Potent and efficacious inhibitors of the hedgehog pathway for the treatment of cancer have been prepared using the 2-pyridyl biphenyl amide scaffold common to the clinical lead GDC-0449. Analogs with polar groups in the para-position of the aryl amide ring optimized potency, had minimal CYP inhibition, and possessed good exposure in rats. Compounds 9d and 14f potently inhibited hedgehog signaling as measured by Gli1 mRNA and were found to be equivalent or more potent than GDC-0449, respectively, when studied in a Ptch+/- medulloblastoma allograft model, that is, highly dependent on hedgehog signaling.
IMIDAZO [1,2A] PYRIDINE DERIVATIVES, THEIR USE AS S1P1 AGONISTS AND METHODS FOR THEIR PRODUCTION
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Page/Page column 150-151, (2010/06/20)
The invention is directed to Compounds of Formula (I) as well as methods of making and using the compounds.
PYRIDYL INHIBITORS OF HEDGEHOG SIGNALLING
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Page/Page column 193, (2009/11/29)
The invention provides novel inhibitors of hedgehog signaling that are useful as s therapeutic agent for treating malignancies where the compounds have the general formula (I): where A, X, Y R1, R2, R3, R4, m and n are as described herein.
4-benzoyl isoxazoles derivatives and their use as herbicides
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, (2008/06/13)
4-Benzoylisoxazole derivatives of the formula wherein R is H or an ester; R1is alkyl, haloalkyl or optionally substituted cycloalkyl; R2is halogen, optionally halogenated alkyl, alkenyl or alkynyl; alkyl substituted with one or more —OR5; —NO2, —CN, —CO2R5, —S(O)pR6, —O(CH2)mOR5, —COR5, —NR5R6, —N(R8)SOqR7, —CONR9R10or —OR51; or optionally substituted phenyl; R3is —S(O)qR7; X is —N(R8)—; n is 0, 1, 2, 3, or 4; R5, R51and R6are independently H; optionally halogenated alkyl, alkenyl or alkynyl; optionally substituted phenyl; or cycloalkyl; R7is optionally halogenated alkyl, alkenyl or alkynyl; cycloalkyl; optionally substituted phenyl; or optionally substituted amino; R8is H; optionally halogenated alkyl, alkenyl or alkynyl; cycloalkyl; optionally substituted phenyl; or alkoxy; m is 1, 2 or 3; p is 0, 1 or 2; q is 0 or 2; and their use as herbicides are described.
Herbicidal 2-cyano-1,3-diones
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, (2008/06/13)
Herbicides derived from 2-cyano-1,3-diones have the formula: STR1 wherein R, R1, R2 R3, R4 and R5 are as defined in the description. The compounds are intended for use pre- and post-emergence as selective herbicides in maize and a large number of other monocotyledon crops.