合成目标产物 Clotrimazole 主要起始原料 Imidazole And Phosphorous Acid, Diphenyl Ester And Clotrimazole Imp. A (Pharmeuropa): (2-Chlorophenyl)Diphenylmethanol And 4-Methyl-2-Pentanone
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:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
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-5798236-A 优先权日:1992-09-30 标 题 :Synthesis of quinic acid from glucose 发明人:FROST JOHN W; DRATHS KAREN M; WARD TIMOTHY L 权利人:GENENCOR INT 摘要:There are described methods for the synthesis of quinoid organic compounds from a renewable energy source such as glucose. The method comprises enhancing the amount of glucose equivalents introduced into the pathway, blocking the common pathway so as to accumulate dehydroquinate and converting the dehydroquinate to quinic acid.
专利号:US-11311505-B2 优先权日:2017-02-24 标 题:Synergistic compositions to stimulate the synthesis of human lung and sinus surfactants to decrease coughing, increase FEV-1/FVC ratios, decrease lung fibrosis, by increasing apoptosis of myofibroblasts 发明人:MARTIN ALAIN 权利人:MARTIN ALAIN; CELLULAR SCIENCES INC 摘要:Methods for the treatment of patients with both Chronic Obstructive Pulmonary Disease (COPD) and pulmonary fibrosis, and of patients with idiopathic pulmonary fibrosis without COPD, by stimulating the synthesis of human and animal patient lung and sinus surfactants to increase lung functions, inhibiting fibrosis and reducing coughing and nasal erythema, include the following steps: A) analyzing and diagnosing a patient with a lung ailment selected from the group consisting of i) both COPD and pulmonary fibrosis; and ii) idiopathic pulmonary fibrosis without COPD; and, B) treating the patient to raise the patient's lung functions including FEV1/FVC ratio by contacting mammalian cells with a [therapeutically effective amount of a treatment] composition that includes: a) a pyruvate salt; b) a phosphate; c) a salt of calcium; and d) a salt of magnesium, in an aqueous carrier, containing no more than 2.2 grams of said pyruvate salt per liter.
1: El-Asmar J, Gonzalez R, Bookout R, Mishra A, Kharfan-Dabaja MA. Clotrimazole troches induce supratherapeutic blood levels of sirolimus and tacrolimus in an allogeneic hematopoietic cell-transplant recipient resulting in acute kidney injury. Hematol Oncol Stem Cell Ther. 2015 Nov 27. pii: S1658-3876(15)00103-X. doi: 10.1016/j.hemonc.2015.11.001. [Epub ahead of print] doi: 10.1155/2015/261397. Epub 2015 Oct 13. 4: Pais P, Costa C, Pires C, Shimizu K, Chibana H, Teixeira MC. Membrane proteome-wide response to the antifungal drug clotrimazole in Candida glabrata: role of the transcription factor CgPdr1 and the Drug:H+ Antiporters CgTpo1_1 and CgTpo1_2. Mol Cell Proteomics. 2015 Oct 28. pii: mcp.M114.045344. [Epub ahead of print] doi: 10.1016/j.colsurfb.2015.10.003. [Epub ahead of print] doi: 10.1016/j.chroma.2015.09.063. Epub 2015 Sep 25. doi: 10.1016/j.bmcl.2015.09.007. Epub 2015 Sep 5. doi: 10.1371/journal.pntd.0004098. eCollection 2015 Sep. 10: Nezhad ZK, Nagai N, Yamamoto K, Kaji H, Nishizawa M, Saya H, Nakazawa T, Abe T. Application of clotrimazole via a novel controlled release device provides potent retinal protection. J Mater Sci Mater Med. 2015 Sep;26(9):230. doi: 10.1007/s10856-015-5561-9. Epub 2015 Sep 3.
合成参考文献
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