This disclosure provides compounds and pharmaceutically acceptable salts thereof of Formula I (Formula I) The variables, e.g. R1-R4, and Z are defined herein. Y is Y is (II). Certain compounds of Formula I are highly potent against resistant tumor cell lines driven by BRAFV600E monomer melanoma cells (A375 or SK-MEL-239), p61-BRAFV600E dimer splice variant melanoma cells (SK-MEL-239-C4) and colorectal (RKO) and lung cancer (A549) cells, and at the same time display a highly desirable pharmacological profile in a mice tumor model.
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Paragraph 0143
(2022/02/28)
COMT INHIBITING METHODS AND COMPOSITIONS
Compounds that inhibit COMT enzyme and pharmaceutical compositions comprising the same are provided herein. Methods of treating various psychiatric and neurological disorders with the compounds and pharmaceutical compositions described herein are also provided.
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(2017/07/14)
An efficient coupling of N-tosylhydrazones with 2-halopyridines: Synthesis of 2-α-styrylpyridines endowed with antitumor activity
The synthesis of 2-α-styrylpyridines has been carried out by using the coupling of polyoxygenated N-tosylhydrazones with various 2-halopyridines. We demonstrated that the use of a catalytic amount of PdCl2(MeCN) 2 in combination with a bidentate ferrocene DPPF or a monodentate alkyl phosphine tBu2MeP-HBF4 constitutes an efficient protocol for this coupling, providing 2-α-styrylpyridines 2 in satisfactory to good yields. Among several polyoxygenated derivatives 2 evaluated, compound 2aa was found to exhibit excellent antiproliferative and antimitotic activities comparable to that of the reference compound isoCA-4. The Royal Society of Chemistry 2013.
This invention provides a compound the formula (I), wherein R1 represents an aryl group having from 6 to 10 ring carbon atoms etc.; R2 represents a hydrogen atom etc., n epresents 0, 1 or 2; said heteroaryl group is unsubstituted or
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Page/Page column 43
(2010/02/11)
1-‘2-(4-HYDROXYPHENYL)-2-HYDROXYETHYL!-PIPERIDIN-4-OL COMPOUNDS AS NMDA RECEPTOR ANTAGONISTS
This invention provides a compound of the formula (I), wherein R1 and R2 independently represents a hydrogen atom or the like; R3 represents an aryl group having from 6 to 10 ring carbon or the like; said aryl groups havin
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Page/Page column 74-75
(2010/02/11)
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