193977-34-3Relevant articles and documents
Synthetic studies connected with the preparation of 4-cyclopropyl-7-fluoro-6-(4-methylpiperazin-1-yl)-1,2,4,9-tetrahydrothiazolo[5, 4-b]quinoline-2,9-dione
Radl, Stanislav
, p. 791 - 799 (1997)
Target 4-cyclopropyl-7-fluoro-6-(4-methylpiperazin-1-yl)-1,2,4,9-tetrahydrothiazolo[5, 4-b]quinoline-2,9-dione (5a) was obtained from 3-amino-1-cyclopropyl-6-fluoro-7-(4-methylpiperazin-1-yl)-2-mercaptoquinolin- 4(1H)-one (9b). This intermediate was obtained from 3-amino-1-cyclopropyl-6,7-difluoro-2-(methylsulfinyl)quinolin-4(1H)-one (9f) via 3-amino-1-cyclopropyl-6-fluoro-7-(4-methylpiperazin-1-yl)-2-(methylsulfinyl) quinolin-4(1H)-one (9c). Compound 9f was prepared from 2,4,5-trifluoroacetophenone (6a) in several steps. 4-Cyclopropyl-6,7-difluoro-2,3,4,9-tetrahydrothiazolo[5,4-b]quinoline-3,4-dione (5b) was prepared similarly as the target compound. Treatment of 5b with N-methylpiperazine did not afford 5a but 1-cyclopropyl-6,7-difluoro-2-mercapto-3-[(4-methylpiperazin-1-yl)carbonylamino] quinolin-4(1H)-one (11). Several unsuccessful attempts to prepare compound 5a and/or some useful intermediates of its synthesis are also described.
TGF-Beta Inhibitors
-
Paragraph 0726, (2016/09/26)
Disclosed are imidazole and thiazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, A, Z, R1 and R′ are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-β, and can be used to treat disease by blocking TGF-β signaling.
