专利号:US-12391691-B2 优先权日:2018-11-16 标题:Synthesis of key intermediate of KRAS G12C inhibitor compound 发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY 权利人:AMGEN INC 摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as
专利号:US-2025206736-A1 优先权日:2019-11-14 标题 :Synthesis of kras g12c inhibitor compound 发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN 权利人:AMGEN INC 摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.
专利号:US-12295961-B2 优先权日:2009-12-31 标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols 发明人:DHINGRA OM 权利人:MARIUS PHARMACEUTICALS INC 摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.
专利号:WO-2025031833-A1 优先权日:2023-08-04 标 题:Recombinant strain and use thereof in production of scoulerine 发明人:CHEN YUN; JIAO XIANG 权利人:CHRYSEA LTD; CHEN YUN 摘要:Disclosed are recombinant yeast strains and a use thereof in the production of a benzylisoquinoline alkaloid. The recombinant yeast strains comprise berberine bridge enzyme. De novo synthesis of scoulerine and a benzylisoquinoline alkaloid is achieved through multiple strategies, and the yield thereof is significantly increased. The recombinant yeast strains provided by the present invention can produce scoulerine and other benzylisoquinoline alkaloids at high efficiency, and has important value in applications.
专利号:US-12416029-B2 优先权日:2016-06-27 标 题 :Compositions and methods for making benzylisoquinoline alkaloids, morphinan alkaloids, thebaine, and derivatives thereof 发明人:FACCHINI PETER JAMES; CHEN XUE; COLBECK JEFFREY C; TUCKER JOSEPH E 权利人:ANTHEIA INC 摘要:Disclosed herein are methods that may be used for the synthesis of benzylisoquinoline alkaloids (“BIAsâ€?) such as alkaloid morphinan. The methods disclosed can be used to produce thebaine, oripavine, codeine, morphine, oxycodone, hydrocodone, oxymorphone, hydromorphone, naltrexone, naloxone, hydroxycodeinone, neopinone, and/or buprenorphine. Compositions and organisms useful for the synthesis of BIAs, including thebaine synthesis polypeptides, purine permeases, and polynucleotides encoding the same, are provided.
专利号:US-10793885-B2 优先权日:2013-08-16 标 题 :Compositions and methods for making noscapine and synthesis intermediates thereof 发明人:FACCHINI PETER JAMES; CHEN XUE; DANG THI THU THUY 权利人:WILLOW BIOSCIENCES INC 摘要:Methods for the manufacture of the therapeutic chemical compound noscapine and noscapine synthesis intermediates comprising contacting a noscapine pathway precursor selected from a first canadine derivative, a first papaveroxine derivative and narcotine hemiacetal with at least one of the enzymes selected from the group CYP82Y1, CYP82X1, AT1, CYP82X2, OMT, CXE1 and NOS.
1: Park MR, Chen X, Lang DE, Ng KKS, Facchini PJ. Heterodimeric O-methyltransferases involved in the biosynthesis of noscapine in opium poppy. Plant J. 2018 May 3. doi: 10.1111/tpj.13947. [Epub ahead of print] doi: 10.1073/pnas.1721469115. Epub 2018 Apr 2. 3: Abedini D, Monfared SR, Abbasi A. The effects of promoter variations of the N-Methylcanadine 1-Hydroxylase (CYP82Y1) gene on the noscapine production in opium poppy. Sci Rep. 2018 Mar 21;8(1):4973. doi: 10.1038/s41598-018-23351-0. 4: Rabzia A, Khazaei M, Rashidi Z, Khazaei MR. Synergistic Anticancer Effect of Paclitaxel and Noscapine on Human Prostate Cancer Cell Lines. Iran J Pharm Res. 2017 Fall;16(4):1432-1442.
合成参考文献
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