专利号:US-2022064167-A1 优先权日:2018-05-17 标 题 :Imidazo-pyrazole carboxamide derivatives as anticancer agents and the synthesis thereof 发明人:DEMJÉN ANDRÃ?S; Puskás László; KANIZSAI IVAN; SZEBENI GÃ?BOR; ANGYAL ANIKÓ; GYURIS Márió; Hackler László 权利人:AVIDIN KFT 摘要:The present invention relates to novel imidazo[1,2-b]pyrazole carboxamide and carbothioamide derivatives of general formula (V), and the advantageous derivatives and pharmaceutically acceptable salts thereof, the synthesis thereof, and medicinal and/or pharmaceutical composition comprising these compounds thereof and synthesis thereof, and for use as a medicament, for use in the treatment of different diseases, advantageously of cancer. The subject compounds are advantageously for use in the treatment of solid malignancies, advantageously breast, lung, melanoma, gliomas, and myeloproliferative and myelodysplastic neoplasms, acute myelogenous/myeloid leukemias and colon cancer by the differentiation and subsequent apoptosis of pre-matured myeloid leukemic cells or myeloid-derived suppressor cells and/or by direct effect on solid tumors.
参考文献:10.1021/jm101212e 摘要:Reddy TRK, Li C, Guo X, Myrvang HK, Fischer PM, Dekker LV. Design, Synthesis, and Structure−Activity Relationship Exploration of 1-Substituted 4-Aroyl-3-hydroxy-5-phenyl-1H-pyrrol-2(5H)-one Analogues as Inhibitors of the Annexin A2−S100A10 Protein Interaction. J. Med. Chem. 2011 Mar 04;54(7):2080–94. doi: 10.1021/jm101212e.