NOVEL COMPOUNDS AS HIF-1ALPHAINHIBITORS AND MANUFACTURING PROCESS THEREOF

摘要

The present invention relates to novel compounds as HIF-1α inhibitors, manufacturing process thereof, and a pharmaceutical compositions. The compounds according to the present invention having inhibition activity against HIF-1α, can be used as a therapeutic prevention and/or treatment for various solid cancers such as colon cancer, liver cancer, stomach cancer and breast cancer. Also, the compounds according to the present invention are useful in the treatment of diabetic retinopathy and rheumatoid arthritis, which are aggravated by HIF-1α-mediated VEGFA expression.

主权项

1. A compound represented by Formula I, pharmaceutically acceptable salt, hydrate or solvate thereof.wherein,
R1 represents hydrogen, methyl, fluoro or chloro; R2 represents hydrogen or methyl; R3 represents, wherein, Ra represents dimethyl, cyclopropyl, N,N-dimethylaminoethyl or 2-furanylmethyl; Rb represents hydrogen, (S)-methyl or (R)-methyl; Re represents hydrogen, methyl, isopropyl, tert-butoxycarbonyl(Boc), 4-trifluoromethylbenzyl, hydroxyethyl or propynyl; and Rd represents Re represents hydrogen or hydroxyl; and n represents 1, 2 or 3.