CAS: 4922-68-3; 3-Bromo[1,2,4]Triazolo[4,3-A]Pyridine

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1557624-66-4 1783979-27-0 1443252-68-3

上下游产品

1,2,4-噻唑并[4,3-A]吡啶 [1,2,4]Triazolo[4,3-A]Pyridine 274-80-6

1,2,4-噻唑并[4,3-A]吡啶 以60的收率获得产物3-溴-[1,2,4]噻唑并[4,3-A]吡啶
参考文献:Protein Kinase Inhibitors (Variants),Use Thereof In Treating Oncological Diseases And A Pharmaceutical Composition Based Thereon
标题:Protein Kinase Inhibitors (Variants),Use Thereof In Treating Oncological Diseases And A Pharmaceutical Composition Based Thereon
摘要:本发明涉及使用新的化学化合物家族辅助治疗肿瘤,慢性炎症和类似疾病,这些化合物家族在抑制abl激酶及其突变形式以及其他具有治疗意义的激酶方面具有提高的效率.本发明描述了蛋白激酶抑制剂,其形式为通式(I)和通式(II)的化合物,或其互变异构体,单个异构体,异构体混合物,药学上可接受的盐,溶剂或其水合物.

专利信息

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).