专利号:WO-2023091726-A1 优先权日:2021-11-18 标题:Inhibitors of cyclin‑dependent kinase 12 (cdk12) 发明人:BENOIT GUILLAUME; CARULLI JOHN; CHEN FEI; CHUAQUI CLAUDIO; CIBLAT STEPHANE; COOPER ELLIOT; DAGENAIS ROBIN; HU SHANHU; KABRO ANZHELIKA; LAPLACA DEREK; MARINEAU JASON; MOEBIUS DAVID; MOON DIANE; SOLODININ ANDREI; WHITMORE KENNETH 权利人:SYROS PHARMACEUTICALS INC 摘要:The present invention provides chemical compounds that inhibit one or more families of kinases (e.g., serine/threonine kinases, including one or more of the families of CDK proteins, and in particular, CDK12). More specifically, the present invention provides CDK12 inhibitors, of formula (I), pharmaceutically acceptable salts and isotopically labeled derivatives thereof, pharmaceutical compositions containing the compounds/inhibitors, and methods of their synthesis and use in treating proliferative diseases (e.g., a bladder cancer, a breast cancer, Ewing's sarcoma, a gastric cancer, a gastrointestinal cancer, a hematologic cancer, a lung cancer (e.g., small cell lung cancer (SCLC)), an ovarian cancer (e.g., a high grade serous ovarian cancer), a pancreatic cancer (e.g., pancreatic ductal adenocarcinoma (PDAC)), a brain cancer (e.g., glioblastoma), or a prostate cancer), alone or in combination with a second therapeutic agent. The proliferative disease can be a cancer, benign neoplasm, or pathologic angiogenesis, and any of the therapeutic methods or uses described herein can include a step of diagnosing the patient's disease. In other embodiments of the invention, the compositions described herein (e.g., the compounds, pharmaceutical compositions, and kits containing them) are used for the treatment of myotonic dystrophy (type 1 or type 2).
专利号:US-7612064-B2 优先权日:2003-05-26 标题:Sulfopyrroles 发明人:EBERLE MARTIN; ERMERT PHILIPP; OBRECHT DANIEL; LACH FRANK; LUTHER ANATOL; BACHMANN FELIX; STREBEL ALLESSANDRO 权利人:TAKEDA PHARMACEUTICAL 摘要:The invention relates to compounds of formula (I) wherein R 1 represents aryl, aralkyl or heteroaryl, R 2 is aryl or heteroaryl and R 3 is aryl, heteroaryl or optionally substituted aminomethyl, to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to the use of a compounds of formula (I) for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using compounds of formula (I) or of pharmaceutical compositions containing same.
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合成参考文献
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