553661-25-9Relevant articles and documents
CYCLOPROPANECARBOXAMIDO-SUBSTITUTE AROMATIC COMPOUNDS AS ANTI-TUMOR AGENTS
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Paragraph 0415; 0416, (2015/07/22)
Provided are cyclopropanecarboxamido-substituted aromatic compounds that inhibit protein kinases and their use in anti-tumor area. In particular, tyrosine-kinase inhibitors and Raf-kinase inhibitors as anti-tumor agents, their preparation, pharmaceutical composition, and their use in the treatment of cancer are also provided.
Pyridoimidazolones as novel potent inhibitors of v-Raf murine sarcoma viral oncogene homologue B1 (BRAF)
Niculescu-Duvaz, Dan,Gaulon, Catherine,Dijkstra, Harmen P.,Niculescu-Duvaz, Ion,Zambon, Alfonso,Menard, Delphine,Suijkerbuijk, Bart M. J. M.,Nourry, Arnaud,Davies, Lawrence,Manne, Helen,Friedlos, Frank,Ogilvie, Lesley,Hedley, Douglas,Whittaker, Steven,Kirk, Ruth,Gill, Adrian,Taylor, Richard D.,Raynaud, Florence I.,Moreno-Farre, Javier,Marais, Richard,Springer, Caroline J.
supporting information; experimental part, p. 2255 - 2264 (2010/01/15)
BRAF is a serine/threonine kinase that is mutated in a range of cancers, including 50-70% of melanomas, and has been validated as a therapeutic target. We have designed and synthesized mutant BRAF inhibitors containing pyridoimidazolone as a new hinge-binding scaffold. Compounds have been obtained which have low nanomolar potency for mutant BRAF (12 nM for compound 5i) and low micromolar cellular potency against a mutant BRAF melanoma cell line, WM266.4. The series benefits from very low metabolism, and pharmacokinetics (PK) that can be modulated by methylation of the NH groups of the imidazolone, resulting in compounds with fewer H-donors and a better PK profile. These compounds have great potential in the treatment of mutant BRAF melanomas.
Positive allosteric modulators of the nicotinic acetylcholine receptor
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Page 42, (2010/02/05)
The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals used to treat diseases or conditions in which α7 nAChR is known to be involved.
