4415-84-3Relevant articles and documents
QUINOLINE DERIVATIVES AS INHIBITORS OF AXL/MER RTK AND CSF1R
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Page/Page column 81, (2019/12/25)
The present invention relates to quinoline derivatives which are inhibitors for Axl/Mer RTK (receptor tyrosine kinase) and CSF1R (colony stimulating factor 1 receptor). These compounds are suitable for the treatment of disorders associated with, accompanied by, caused by or induced by Axl/Mer RTK and CSF1R, in particular a hyperfunction thereof. The compounds are suitable for the treatment of hyperproliferative disorders, such as cancer, particularly immune-suppressive cancer (such as those cancers with an immunosuppression of innate immunity in a tumor microenvironment (TME), refractory cancer and cancer metastases. They are also useful in the treatment of inflammatory diseases and/or neurodegenerative diseases.
Practical synthesis of a peptide deformylase (PDF) inhibitor
Liu, Yugang,Prashad, Mahavir,Ciszewski, Lech,Vargas, Kevin,Repic, Oljan,Blacklock, Thomas J.
, p. 183 - 191 (2013/01/03)
A practical chromatography-free synthesis of an N-formylated hydroxylamine peptide deformylase inhibitor LCD320 is described. A diastereoselective Michael reaction of (4S)-3-[2-(cyclobutylmethyl)-l-oxo-2-propenyl]-4-(phenylmethyl)-2- oxazolidinone with 0-benzyl hydroxylamine was used to establish the key stereogenic center. We found that traces of residual Li+ from a previous step had a great impact on the diastereoselectivity of this reaction. A very efficient amidalion coupling reaction of proline derivative (2S,4R)-4-fluoro-1,2-m-pyrrolidinedicarboxylic acid 1,1-dimethylethyl ester with weakly nucleophilic 3-pyridazinamine using methanesulfonyl chloride in the presence of l-methylimidazole in DMF was also developed that proceeded without racemization.
Structure activity relations in acids related to cyclobutanecarboxylic acid
Vergnon,Girard,Legheand,et al.
, p. 65 - 71 (2007/10/13)
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