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-8734846-B2 优先权日:2008-06-16 标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles 发明人:ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS 权利人:BIND BIOSCIENCES INC 摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.
专利号:US-2013035307-A1 优先权日:2010-01-26 标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers 发明人:PRESTWICH GLENN D; KENNEDY THOMAS P 权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P 摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.
专利号:US-8193180-B2 优先权日:2007-01-24 标 题 :N-amino tetrahydrothiazine derivatives, method of manufacture and use 发明人:BRARD LAURENT; SINGH RAKESH KUMAR; KIM KYU KWANG; SAULNIER-SHOLLER GISELLE 权利人:BRARD LAURENT; SINGH RAKESH KUMAR; KIM KYU KWANG; SAULNIER-SHOLLER GISELLE; WOMEN & INFANTS HOSPITAL 摘要:This invention comprises the innovative synthesis of N-amino tetrahydrothiazine free bases and their salts. This invention further comprises the use of the derivatives and their therapeutic application as anticancer agents. Further this invention comprises their manufacture and use.
专利号:US-2008214827-A1 优先权日:2004-02-03 标 题:Synthesis of Cyanoimino-Benzoimidazoles 发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN 权利人:EURO CELTIQUE SA 摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.
1: Park MH, Kim SY, Moon C, Bae YC, Moon JI, Moon C. Differential cell death and Bcl-2 expression in the mouse retina after glutathione decrease by systemic D,L-buthionine sulphoximine administration. Mol Cells. 2013 Mar;35(3):235-42. doi: 10.1007/s10059-013-2276-y. Epub 2013 Feb 18. 2: Vukovic V, Nicklee T, Hedley DW. Differential effects of buthionine sulphoximine in hypoxic and non-hypoxic regions of human cervical carcinoma xenografts. Radiother Oncol. 2001 Jul;60(1):69-73. 13: Terradez P, Asensi M, Lasso de la Vega MC, Puertes IR, Viña J, Estrela JM. Depletion of tumour glutathione in vivo by buthionine sulphoximine: modulation by the rate of cellular proliferation and inhibition of cancer growth. Biochem J. 1993 Jun 1;292 ( Pt 2):477-83.
合成参考文献
参考文献:10.1007/s00232-011-9382-6 摘要:Nazıroğlu M, Özgül C, Çiğ B, Doğan S, Uğuz AC. Glutathione Modulates Ca2+ Influx and Oxidative Toxicity Through TRPM2 Channel in Rat Dorsal Root Ganglion Neurons. The Journal of Membrane Biology. 2011 Jul 12;242(3):109. doi: 10.1007/s00232-011-9382-6. 参考文献:10.1007/s10529-011-0684-7 摘要:Upadhyaya CP, Venkatesh J, Gururani MA, Asnin L, Sharma K, Ajappala H, Park SW. Transgenic potato overproducing L-ascorbic acid resisted an increase in methylglyoxal under salinity stress via maintaining higher reduced glutathione level and glyoxalase enzyme activity. Biotechnol Lett. 2011 Nov;33(11):2297–307. doi: 10.1007/s10529-011-0684-7.