12-08-2021 дата публикации
Номер: US20210246100A1
Provided herein are anti-fibrotic compounds, in particular those of Formula (I), that inhibit the TGF-beta signaling pathway. Also provided are pharmaceutical compositions comprising the anti-fibrotic compounds, and methods of treating diseases or conditions associated with fibrosis, inflammation, and benign or malignant neoplastic diseases in a subject by administering a compound or composition described herein. 5. The compound of or , or a pharmaceutically acceptable salt thereof , whereinX is O or a bond;Y is O or a bond;Z is O or a bond;{'sup': 1', '2', '1', '2', '8, 'Rand Rare independently hydrogen, alkyl, alkynyl, cycloalkylalkyl, heteroarylalkyl, heterocyclyl, or heterocyclylalkyl, wherein Rand Rare each optionally substituted with 1 or 2 independent substituents R;'}{'sup': 1', '2, 'or Rand Rtogether with the atoms to which they are attached form a heterocyclyl ring;'}{'sup': 3', '3', '8, 'Ris hydrogen, alkyl, alkynyl, heteroarylalkyl, heterocyclyl, or heterocyclylalkyl, wherein Ris optionally substituted with 1 or 2 independent substituents R;'}{'sup': 6', 'c, 'sub': '2', 'each occurrence of Ris, independently, halogen, cyano, alkyl, heteroaryl, heterocyclyl, or —S(O)R;'}m is 1 or 2;{'sup': 8', 'a', 'b, 'each occurrence of Ris, independently, alkyl or NRR; and'}{'sup': a', 'b', 'c, 'each occurrence of R, R, and Ris, independently, hydrogen, alkyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, and heterocyclyl.'}8. The compound of or , or a pharmaceutically acceptable salt thereof , whereinX is O or a bond;Y is O or a bond; provided that at least one of X and Y is O;{'sup': 1', '2, 'Rand Rare independently, alkyl, alkynyl, heteroarylalkyl, heterocyclyl, or heterocyclylalkyl, wherein said heteroarylalkyl, heterocyclyl, and heterocyclylalkyl are optionally substituted with 1 or 2 independent alkyl groups;'}{'sup': 6', 'c, 'sub': '2', 'each occurrence of Ris, independently, halogen, cyano, alkyl, heteroaryl, heterocyclyl, or —S(O)R;'}m is 1 or 2 ...
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