CAS: 99464-64-9; Ethyl (1-((2-Methyl-1,1-Dioxido-3-(Pyridin-2-Ylcarbamoyl)-2H-Benzo[e][1,2]Thiazin-4-yl)Oxy)Ethyl) Carbonate

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CAS号50893-36-2 1-氯乙基碳酸乙酯 | CAS号36322-90-4 吡罗昔康

📜C20H21N3O8S置于水体系中,用 Aq. Phosphate Buffer,二甲基亚砜 作为反应溶剂,化学反应生成 安吡昔康
参考文献:放射疗法可减少肿瘤中前体药物活化的 N-氧化物
标题:放射疗法可减少肿瘤中前体药物活化的 N-氧化物
摘要:以肿瘤选择性方式精确激活化疗前药是治愈癌症而不引起全身毒性的理想方法.尽管已经做出了许多努力,但开发时空可控的激活方法仍然是一个尚未解决的挑战.在这里,我们报告了一种使用放射疗法(x 射线)的新型前药激活策略.由于其精确度和深层组织穿透性,X 射线满足了通过水辐解改变肿瘤中分子的需求.我们首先证明了管和活细胞中辐射产生的水合电子(e-Aq)可以有效地还原n-氧化物.进行筛选以研究 E-Aq的结构-还原关系和机制介导的减少.然后我们应用该策略来激活n-氧化物前药.基于抗癌药物喜树碱 (Cpt) 的n-氧化物前药在放射治疗激活后显示出显着的抗癌作用.由于超过 50% 的癌症患者接受放射治疗,这种辐射诱导的体内化学可以实现放射治疗激活前药的多功能设计,这些前药具有显着的临床相关性.
DOI:10.1021/jacs.2C02521

专利信息

专利号:US-7256205-B2
优先权日:1998-11-17
标题 :Nitrosated and nitrosylated H2 receptor antagonist compounds, compositions and methods of use
发明人：GARVEY DAVID S; LETTS L GORDON; LIN CHIA-EN; WANG TIANSHENG
权利人:NITROMED INC
摘要:The invention describes novel nitrosated and/or nitrosylated H 2 receptor antagonist compounds, and novel compositions comprising at least one H 2 receptor antagonist compound that is optionally substituted with at least one NO and/or NO 2 group, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase and/or at least one nonsteroidal antiinflammatory drug, antacid, bismuth-containing reagent or anti-viral agent. The invention also describes methods for treating and/or preventing gastrointestinal disorders; improving gastroprotective properties of H 2 receptor antagonists; decreasing the recurrence of ulcers; facilitating ulcer healing; preventing and/or treating inflammations and microbial infections, ophthalmic diseases and disorders, multiple sclerosis, and viral infections; and decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds.

专利号:US-7332505-B2
优先权日:1999-02-26
标 题 :Nitrosated and nitrosylated proton pump inhibitors, compositions and methods of use
发明人：GARVEY DAVID S; LETTS L GORDON; RICHARDSON STEWART K; TAM SANG WILLIAM; WANG TIANSHENG
权利人:NITROMED INC
摘要:The present invention describes novel nitrosated and/or nitrosylated proton pump inhibitor compounds, and novel compositions comprising at least one proton pump inhibitor compound that is optionally substituted with at least one NO and/or NO 2 group, and, optionally, at least one compound that donates, transfers, or releases nitric oxide, induces the production of endogenous nitric oxide or endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase, and/or at least one nonsteroidal antiinflammatory drug, selective COX-2 inhibitor, antacid, bismuth-containing reagent, acid-degradable antibacterial compound, and mixtures thereof. The present invention also provides methods for treating and/or preventing gastrointestinal disorders; facilitating ulcer healing; decreasing the recurrence of ulcers; improving gastroprotective properties, anti- Helicobacter pylon properties or antacid properties of proton pump inhibitors; decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds; treating Helicobacter pylori and viral infections. The compounds and/or compositions of the present invention can also be provided in the form of a pharmaceutical kit.

专利号:US-9051302-B2
优先权日:2008-01-15
标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents
发明人：WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN
权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG
摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.

专利号:US-2024287041-A1
优先权日:2021-05-20
标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
发明人：BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.

专利号:US-6593347-B2
优先权日:1998-10-30
标题 :Nitrosated and nitrosylated nonsteroidal antiinflammatory compounds, compositions and methods of use
发明人：BANDARAGE UPUL K; DONG QING; FANG XINQIN; GARVEY DAVID S; MERCER GREGORY J; RICHARDSON STEWART K; SCHROEDER JOSEPH D; WANG TIANSHENG
权利人:NITROMED INC
摘要:The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.

专利号:AU-2022276509-A1
优先权日:2021-05-20
标题:Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms