1-(6-溴吡啶-3-基甲基)-4-乙基哌嗪置于tris-(Dibenzylideneacetone)Dipalladium(0),氨,Caesium Carbonate,4,5-双二苯基膦-9,9-二甲基氧杂蒽体系中,用 1,4-二氧六环,甲醇 用作溶剂,化学反应 2.0H,反应生成玻玛西尼 参考文献: Combination Therapy For Cancer[fr] Polythérapie Contre Le Cancer 标题: Combination Therapy For Cancer[fr] Polythérapie Contre Le Cancer 摘要:本发明提供了用于治疗和治疗非小细胞肺癌的药物制剂的制备以及治疗方法,包括:[5-(4-乙基哌嗪-1-基甲基)-吡啶-2-基]-[5-氟-4-(7-氟-3-异丙基-2-甲基-3H-苯并咪唑-5-基)-嘧啶-2-基]-胺,或其药学上可接受的盐,与抗vegfr2抗体结合,最好是拉姆西单抗.
专利号:US-11873305-B2 优先权日:2020-06-30 标题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds 发明人:ZHANG HAIMING; XU JIE; WUITSCHIK GEORG; ANGELAUD REMY; HEROLD SEBASTIAN; STUTZ ALFRED; BRUETSCH TOBIAS; BURKHARD JOHANNES 权利人:GENENTECH INC; HOFFMANN LA ROCHE 摘要:Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.
专利号:US-12383499-B2 优先权日:2018-01-01 标题:Scale up synthesis of silicasome nanocarriers 发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG 权利人:UNIV CALIFORNIA 摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).
专利号:WO-2024199465-A1 优先权日:2023-03-30 标 题:Unnatural amino acid in cellulo synthesis for site-specific protein modification 发明人:CHAN MICHAEL KENNETH; LEE MARIANNE; CHENG JIAHUI 权利人:UNIV HONG KONG CHINESE 摘要:Provided are genetically modified host cells containing engineered enzymes that support the synthesis of unnatural amino acids, such as D-Cys-ε-Lys, and the incorporation of such unnatural amino acids into a newly synthesized protein. These cells are therefore capable of in vivo or in cellulo synthesis of a protein containing one or more unnatural amino acids strategically placed at pre-determined locations for site-specific modification of the protein. Also provided are the corresponding methods for in vivo synthesis of modified proteins as well as the modified proteins produced by the method.
专利号:US-12043612-B2 优先权日:2020-05-09 标 题 :Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same 发明人:ALLAN LAURA E N; CHEN CHUNGPIN HERMAN; DONG HANQING; GROSSO JOHN A; HASKELL III ROYAL J; LLOYD RHYS; REECE HAYLEY 权利人:ARVINAS OPERATIONS INC 摘要:The present disclosure relates to ultra-pure forms, polymorphs, amorphous forms, and formulations of N-[(1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-({4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]piperazin-1-yl}methyl)piperidin-1-yl]pyridazine-3-carboxamide, referred to herein as Compound A:The present disclosure also relates methods of manufacturing and purifying the same, as well as intermediates useful in the synthesis of Compound A. The ultra-pure forms, polymorphs, amorphous forms, and formulations of Compound A can be used as therapeutic agents for the treatment of various diseases and conditions such as cancer.
专利号:US-2023037284-A9 优先权日:2018-11-30 标题:Combination therapy of peptidomimetic macrocycles 发明人:GUERLAVAIS VINCENT; ANNIS DAVID ALLEN 权利人:AILERON THERAPEUTICS INC 摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.
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.
1: Naz S, Sowers AL, Choudhuri R, Wissler MF, Gamson J, Mathias A, Cook JA, Mitchell JB. Abemaciclib, a Selective CDK4/6 Inhibitor Enhances the Radiosensitivity of Non-Small Cell Lung Cancer in vitro and in vivo. Clin Cancer Res. 2018 May 1. pii: clincanres.3575.2017. doi: 10.1158/1078-0432.CCR-17-3575. [Epub ahead of print] doi: 10.1016/j.celrep.2018.02.053. doi: 10.1080/14656566.2018.1448787. Epub 2018 Mar 9. doi: 10.2147/DDDT.S137783. eCollection 2018. Review. 5: O'Brien N, Conklin D, Beckmann R, Luo T, Chau K, Thomas J, Mc Nulty A, Marchal C, Kalous O, von Euw E, Hurvitz S, Mockbee C, Slamon DJ. Preclinical Activity of Abemaciclib Alone or in Combination with Antimitotic and Targeted Therapies in Breast Cancer. Mol Cancer Ther. 2018 May;17(5):897-907. doi: 10.1158/1535-7163.MCT-17-0290. Epub 2018 Feb 26. doi: 10.18632/oncotarget.22244. eCollection 2017 Nov 21. 7: Gong X, Litchfield LM, Webster Y, Chio LC, Wong SS, Stewart TR, Dowless M, Dempsey J, Zeng Y, Torres R, Boehnke K, Mur C, Marugán C, Baquero C, Yu C, Bray SM, Wulur IH, Bi C, Chu S, Qian HR, Iversen PW, Merzoug FF, Ye XS, Reinhard C, De Dios A, Du J, Caldwell CW, Lallena MJ, Beckmann RP, Buchanan SG. Genomic Aberrations that Activate D-type Cyclins Are Associated with Enhanced Sensitivity to the CDK4 and CDK6 Inhibitor Abemaciclib. Cancer Cell. 2017 Dec 11;32(6):761-776.e6. doi: 10.1016/j.ccell.2017.11.006. doi: 10.18632/oncotarget.19618. eCollection 2017 Nov 10.
合成参考文献
参考文献:10.1093/annonc/mdw612 摘要:Crockford A, Zalmas LP, Grönroos E, Dewhurst SM, McGranahan N, Cuomo ME, Encheva V, Snijders AP, Begum J, Purewal S, Cerveira J, Patel H, Renshaw MJ, Swanton C. Cyclin D mediates tolerance of genome-doubling in cancers with functional p53. Ann Oncol. 2017 Jan 01;28(1):149–56. 参考文献:10.1158/1078-0432.ccr-17-3575 摘要:Naz S, Sowers A, Choudhuri R, Wissler M, Gamson J, Mathias A, Cook JA, Mitchell JB. Abemaciclib, a Selective CDK4/6 Inhibitor, Enhances the Radiosensitivity of Non-Small Cell Lung Cancer In Vitro and In Vivo. Clin Cancer Res. 2018 Aug 15;24(16):3994–4005. 参考文献:10.1007/s10549-018-4783-1 摘要:Abraham J, Coleman R, Elias A, Holmes FA, Kalinsky K, Kittaneh M, Lower E, Mahtani R, Terry Mamounas E, Pegram M, Vogel C, The Breast Cancer Therapy Expert Group (BCTEG). Use of cyclin-dependent kinase (CDK) 4/6 inhibitors for hormone receptor-positive, human epidermal growth factor receptor 2-negative, metastatic breast cancer: a roundtable discussion by The Breast Cancer Therapy Expert Group (BCTEG). Breast Cancer Research and Treatment. 2018 May 04;171(1):11–20. doi: 10.1007/s10549-018-4783-1.