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-10022366-B2 优先权日:2013-04-23 标 题:Extending and maintaining micropore viability of microneedle treated skin with lipid biosynthesis inhibitors for sustained drug delivery 发明人:STINCHCOMB AUDRA L; GHOSH PRIYANKA 权利人:STINCHCOMB AUDRA L; GHOSH PRIYANKA; UNIV MARYLAND; UNIV KENTUCKY RES FOUND 摘要:Microneedles and their use as a physical skin permeation enhancement technique facilitate drug delivery across the skin in therapeutically relevant concentrations. Micropores created in the skin by MNs reseal because of normal healing processes of the skin, thus limiting the duration of the drug delivery window. Pore lifetime enhancement strategies can increase effectiveness of MNs as a drug delivery mechanism by prolonging the delivery window. Fluvastatin (FLU) was used to enhance pore lifetime by inhibiting the synthesis of cholesterol, a major component of the stratum corneum lipids. The skin recovered within a 30-45-min time period following the removal of occlusion, and there was no significant irritation observed due to the treatment compared to the control sites. Thus, it can be concluded that localized skin treatment with FLU can be used to extend micropore lifetime and deliver drugs for up to 7 days across MN-treated skin.
专利号:US-8367819-B2 优先权日:2004-06-10 标 题:Synthesis of caprolactam from lysine 发明人:FROST JOHN W 权利人:UNIV MICHIGAN STATE; FROST JOHN W 摘要:In various embodiments, the present invention can involve a method of synthesizing α-amino-ε-caprolactam. The method can comprise heating a salt of L-lysine in a solvent comprising an alcohol. In other embodiments, the present invention can involve methods for synthesizing ε-caprolactam. The methods can comprise heating a salt of L-lysine in a solvent comprising an alcohol and deaminating the reaction product. In various embodiments, the invention can include methods of converting biomass into nylon 6. The methods can comprise heating L-lysine in a solvent comprising an alcohol to produce α-amino-εcaprolactam, deaminating to produce ε-caprolactam and polymerizing into nylon 6, wherein the L-lysine is derived from the biomass. In other embodiments, the present invention can include methods of making nylon 6. The methods can comprise synthesizing ε-caprolactam and then polymerizing, wherein the ε-caprolactam is derived from L-lysine.
专利号:US-11273138-B2 优先权日:2017-11-02 标 题 :Use of amino acid supplementation for improved muscle protein synthesis 发明人:WOLFE ROBERT R; FERRANDO ARNY 权利人:BIOVENTURES LLC 摘要:The present invention encompasses an amino acid composition for stimulating muscle protein synthesis. Further, the present disclosure relates generally to the use of an anabolic amino acid composition for the stimulation of muscle protein synthesis. In particular, disclosed are compositions and methods of using the same for the prevention and/or treatment of a loss of any one of muscle mass, muscle strength, muscle function, and physical function, or any combination thereof, in a mammal, especially an adult mammal. Also provided are kits comprising a composition for the stimulation of muscle protein synthesis and, in certain embodiments, instructions for administration.
专利号:US-2023192682-A1 优先权日:2019-11-14 标题:Improved synthesis of kras g12c inhibitor compound
摘要:Gekkan Yakuji. Pharmaceuticals Monthly., 23(1253), 1981 参考文献:10.1007/s002800050962 摘要:Vasandani VM, Burris JA, Sung C. Reversible nephrotoxicity of onconase and effect of lysine pH on renal onconase uptake. Cancer Chemotherapy and Pharmacology. 1999 Jun 17;44(2):164–9. doi: 10.1007/s002800050962.