鲁索替尼置于磷酸体系中,用 异丙醇 用作溶剂,以171.7 Mg的收率获得磷酸鲁索替尼 参考文献: Jak P13K/mtor Combination Therapy[fr] Polythérapie Par Jak P13K/mtor 标题: Jak P13K/mtor Combination Therapy[fr] Polythérapie Par Jak P13K/mtor 摘要:本文提供了一种组合疗法,包括jak激酶抑制剂和双重pbk/mtor抑制剂,以及利用这种组合疗法治疗各种癌症的方法.
专利号:US-2022118094-A1 优先权日:2019-02-21 标题:Synthesis of biomimetic cell wall structure 发明人:WANG YONG; SHI PENG 权利人:PENN STATE RES FOUND 摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.
专利号:US-9732097-B2 优先权日:2015-05-11 标 题:Process for the synthesis of a phosphoinositide 3-kinase inhibitor 发明人:ZHOU JIACHENG; QIAO LEI; WENG LINGKAI 权利人:INCYTE CORP 摘要:The present application is directed to processes and intermediates for making (S)-7-(1-((9H-purin-6-yl)amino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one, which is an inhibitor of phosphoinositide 3-kinases (PI3Ks), useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
专利号:US-2023322787-A1 优先权日:2020-08-12 标 题 :Process for preparing enantiomerically enriched jak inhibitors 发明人:WIEDEMANN SEAN; COWDEN CAMERON J; BAZINET PATRICK; KAVOURIS KATHRYN E; WU KUO-MING; LEWIS ROBERT S 权利人:CONCERT PHARMACEUTICALS INC 摘要:Certain aspects of the present invention are directed to improved processes for preparing enantiomerically enriched intermediates for the synthesis of ruxolitinib and deuterated forms of ruxolitinib. Certain aspects are also directed to deuterated intermediates useful in the synthesis of deuterated forms of ruxolitinib. Certain aspects are also directed to reaction mixtures for preparing enantiomerically enriched intermediates useful in the synthesis of ruxolitinib and deuterated forms of ruxolitinib.
专利号:US-2018140724-A1 优先权日:2015-05-27 标 题:Tumor Deliverable Iron and Protein Synthesis Inhibitors as a New Class of Drugs for the Diagnosis and Treatment of Cancer 发明人:DENG CHANGCHUN; LIPSTEIN MARK; O'CONNOR OWEN A 权利人:DENG CHANGCHUN; LIPSTEIN MARK; OCONNOR OWEN A; UNIV COLUMBIA 摘要:Tumor deliverable iron (TDI) drugs and pharmaceutical compositions and kits comprising them are provided and methods for delivering iron to tumors specifically, either intracellularly or extracellularly. As a result, TDI drugs are useful as a sensitizer for radiation therapy, radio-diagnosis, and chemotherapy, and are of interest. In other embodiments, tumor deliverable protein synthesis inhibitors (TDPSI) are provided and can be delivered to tumors, but not normal cells. These TDPSI drugs and pharmaceutical compositions and kits comprising them are useful for their treatment of cancer, either alone or in combination with other active anti-cancer drugs.
专利号:US-10562904-B2 优先权日:2015-12-31 标 题:Synthesis process of ruxolitinib 发明人:ZHANG XIQUAN; ZHANG AIMING; ZHOU ZHOU; YANG LEILEI; YAO HUADONG; ZHU XUEYAN; WANG HUBO 权利人:CHIA TAI TIANQING PHARMACEUTICAL GROUP CO LTD 摘要:The present application falls within the field of drug synthesis, and in particular, the present application relates to a method for preparing ruxolitinib, and a method for preparing the intermediate and relevant intermediates used. The method comprises reacting a compound of formula II with a compound of formula IV or a salt thereof to obtain a compound of formula III, and then subjecting the compound of formula III to an acyl halogenation reaction, an amidation reaction, and a reaction dehydrating an amide to form a cyano group or removing the protecting group to prepare ruxolitinib. The method has the characteristics of brief steps, a high stereoselectivity, a high utilization ratio of atoms, mild reaction conditions and convenient post treatment. The method avoids using expensive asymmetric reaction catalysts, and is suitable for industrial production.
专利号:US-12180228-B2 优先权日:2019-06-05 标题:Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof 发明人:MOVASSAGHI MOHAMMAD; OLSSON CHASE ROBERT; SCOTT TONY Z; CHEAH JAIME; PAYETTE JOSHUA NATHANIEL 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The present disclosure provides, e.g., compounds, compositions, kits, methods of synthesis, and methods of use, involving epipolythiodiketopiperazines and polythiodiketopiperazines.
: Boldrini V, Vannucchi AM, Guglielmelli P. A safety evaluation of ruxolitinib for the treatment of polycythemia vera. Expert Opin Drug Saf. 2023 Dec 29:1-7. doi: 10.1080/14740338.2023.2299391. Epub ahead of print. 2006–. Ruxolitinib. 2023 Dec 15. 15(11):1188-1195. doi: 10.4254/wjh.v15.i11.1188. 4: Yunianto I, Currie M, Chitcholtan K, Sykes P. Potential drug repurposing of ruxolitinib to inhibit the JAK/STAT pathway for the treatment of patients with epithelial ovarian cancer. J Obstet Gynaecol Res. 2023 Nov;49(11):2563-2574. doi: 10.1111/jog.15761. Epub 2023 Aug 10. 37(11):2222-2230. doi: 10.1111/jdv.19162. Epub 2023 May 15. 25(5):577-584. doi: 10.1007/s40272-023-00577-8. Epub 2023 Jun 7. 5(4):1-4. doi: 10.46989/001c.87501. 8: Hwang JR, Driscoll MS. Review of Ruxolitinib for Treatment of Non-Segmental Vitiligo. Ann Pharmacother. 2023 Aug;57(8):948-955. doi: 10.1177/10600280221143748. Epub 2022 Dec 23. 16(1):82. doi: 10.1186/s13045-023-01471-z.