- (PYRIDIN-2-YL)AMINE DERIVATIVES AS TGF-BETA R1 (ALK5) INHIBITORS FOR THE TREATMENT OF CANCER
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The present invention relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder associated with ΤGFβR1 activity, such as a cancer or fibrosis. The invention provides compounds of Formula (I) and Formula (II) as further described herein having an acidic moiety that enhances tissue specificity for targeted tissues and organs. The invention includes pharmaceutical compositions, pharmaceutical combinations, and methods of use of these compounds for treating conditions including cancer or fibrosis.
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Paragraph 00227
(2020/07/15)
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- Novel aminophenyl ketone derivatives
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Novel heteroaryl aminophenyl ketone derivatives which are inhibitors of MAP kinases, in particular the p38 MAP kinase, are useful as anti-inflammatory agents in the prophylaxis or treatment of inflammatory diseases or conditions.
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- New aspects in the synthesis of mono- and dialkylfurans
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3-substituted furan systems can be obtained by alkylation of 3-lithium furans with various electrophiles in the presence of hexamethylphosphoric acid triamide in good yields. The 2- or 5-position of 3-methyl furan is blocked with high regio selectivity by silylation. After metalation and alkylation of the remaining free α-position and subsequent desilylation the 2,3- and 2,4-disubstituted furans are obtained. These methods are used to synthesize the naturally occuring compounds ursinanolide (2) and longifolin (4).
- Bock, Inge,Bornowski, Hans,Ranft, Andreas,Theis, Heinz
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p. 1199 - 1210
(2007/10/02)
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