- QUINOLINE DERIVATIVES AS INHIBITORS OF AXL/MER RTK AND CSF1R
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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.
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- PYRIDAZINONE GLUCOKINASE ACTIVATORS
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
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Page/Page column 46
(2009/10/30)
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- Practical synthesis of a peptide deformylase (PDF) inhibitor
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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.
- Liu, Yugang,Prashad, Mahavir,Ciszewski, Lech,Vargas, Kevin,Repic, Oljan,Blacklock, Thomas J.
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p. 183 - 191
(2013/01/03)
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- LONG-ACTING CONTRACEPTIVE AGENTS: CYCLOPROPYL AND CYCLOBUTYL ESTERS OF NORETHISTERONE
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Several esters of norethisterone (17α-ethynyl-17β-hydroxyestr-4-en-3-one) with carboxylic acids containing a cyclopropyl or cyclobutyl ring have been synthesized and the stereochemistries of the side-chains determined.
- Shafiee, A.,Vossoghi, M.,Savabi, F.,Vlahov, R.,Tarpanov, V.,et al.
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p. 291 - 308
(2007/10/02)
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