专利号:US-2025163076-A1 优先权日:2022-02-18 标 题 :Synthesis of bruton's tyrosine kinase inhibitors 发明人:TRAN NGOC DUC; XIOURAS CHRISTOS; CLEATOR EDWARD; MATON WILLIAM MARC; RAMMELOO THOMAS JOACHIM LANDEWALD; FERNANDES PHILIPPE; BONGARTZ JEAN-PIERRE A; CAO DUY CHI TRUNG; HORWITZ MATTHEW ALLAN; JUSSEAU XAVIER JEAN-MARIE; LEMAIRE SÉBASTIEN FRANCOIS-EMMANUEL; SCHWEITZER-CHAPUT BERTRAND 权利人:JANSSEN PHARMACEUTICA NV 摘要:The present disclosure is directed to methods of synthesizing a compound of Formula (I), where the R groups are defined herein, and to methods of synthesizing a compound of Formula (II). Some aspects of the present disclosure is directed to converting the compound of Formula (II) into its P form.
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:WO-2023156599-A1 优先权日:2022-02-18 标 题 :Synthesis of bruton's tyrosine kinase inhibitors
专利号:EP-4479405-A1 优先权日:2022-02-18 标 题:Synthesis of bruton's tyrosine kinase inhibitors
专利号:CN-118715228-A 优先权日:2022-02-18 标题 :Synthesis of bruton's tyrosine kinase inhibitor
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合成参考文献
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