2-(2-Benzyloxy-Benzoyloxy)-Benzoic Acid置于acid体系中,化学反应生成 双水杨酸酯 参考文献:Iatrogenic Cost Factors Incorporating Mild And Moderate Adverse Events In The Economic Comparison Of Aceclofenac And Other Nsaids 标题:Iatrogenic Cost Factors Incorporating Mild And Moderate Adverse Events In The Economic Comparison Of Aceclofenac And Other Nsaids 摘要:目标:对乙酰氯芬酸与其他用于治疗包括骨关节炎,类风湿关节炎和强直性脊柱炎在内的常见关节病的非甾体抗炎药(nsaid)在功效和耐受性方面的经济性进行模型化分析.设计:构建了一个决策分析模型,以代表nsaid治疗的临床和经济后果.不依从性,缺乏疗效和不良事件发生率的数据来自比较随机双盲临床试验.使用当地单位治疗成本,并召集专家小组估计资源使用.同时使用经典的综合分析和自举方法来计算nsaid治疗成本的点估计值和95%置信区间.患者和干预措施:数据来自早期荟萃分析中包含的12项随机双盲临床试验.主要结局指标:包括nsaid治疗成本(药品获取成本和处方医生就诊费用)和医源性成本(未达到临床疗效患者的替代治疗成本以及与不良事件相关的医疗访问,治疗,诊断测试和住院费用)以及医源性成本因子(icf)作为主要结局指标.结果:平均值和95%置信区间显示,除吡罗昔康外,乙酰氯芬酸与其他nsaid在总成本上无统计学显著差异,尽管药品获取成本存在显著差异.乙酰氯芬酸的icf低于所有其他比较药物,乙酰氯芬酸200 Mg/天与双氯芬酸150 Mg/天,吲哚美辛100 Mg/天,萘普生1000 Mg/天,替诺昔康20 Mg/天或酮洛芬150 Mg/天之间的icf差异具有统计学意义.结论:这些结果表明,Nsaid的比较总体成本与药品获取成本关系不大,而icf是总体成本最重要的决定因素之一. DOI:10.2165/00019053-200119070-00006
专利号:US-8546532-B2 优先权日:2008-04-17 标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders 发明人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS 权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC 摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.
专利号:US-12264143-B2 优先权日:2020-12-17 标 题:Synthesis of cannabinoids and cannabinoid precursors, and related compounds, formulations, and methods of use 发明人:SAMMIS GLENN M; ROGGEN MARKUS 权利人:NALU BIO INC 摘要:Methods are provided for the synthesis of cannabinoids, including cannabidiol (CBD), cannabinol (CBN), cannabichromene (CBC), cannabidiolic acid (CBDA), cannabigerol (CBG), cannabigerolic acid (CBGA), cannabidivarin (CBDV), cannabidibutol (CBD-C4), dihydrocannabidiol (DCBD), tetrahydrocannabivarin (THCV), analogs thereof, and precursors to the foregoing. One method employs phloroglucinol or a phloroglucinol analog as a starting material. The syntheses are stereospecific, efficient, selective, and cost-effective, with little or no potential for generation of THC ((−)-trans-Δ9-tetrahydro-cannabinol) or any other psychoactive side product. Telescoped syntheses are also provided, as are new cannabinoids, pharmaceutical formulations, and methods of use.
专利号:WO-2017100796-A1 优先权日:2015-12-11 标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers 发明人:WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI 权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING 摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta- 4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for disgnostic and therapeutic uses.
专利号:US-2017283878-A1 优先权日:2015-12-11 标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers 发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING 权利人:ACADEMIA SINICA 摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.
专利号:US-8304409-B2 优先权日:2002-07-03 标 题:Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use 发明人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI 权利人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI; NICOX SA 摘要:The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, 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 therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and 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 and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders.
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.
1: Liang W, Verschuren L, Mulder P, van der Hoorn JW, Verheij J, van Dam AD, Boon MR, Princen HM, Havekes LM, Kleemann R, van den Hoek AM. Salsalate attenuates diet induced non-alcoholic steatohepatitis in mice by decreasing lipogenic and inflammatory processes. Br J Pharmacol. 2015 Nov;172(22):5293-305. doi: 10.1111/bph.13315. Epub 2015 Oct 22. doi: 10.1007/s12020-015-0535-8. Epub 2015 Feb 1. 3: Ariel D, Kim SH, Liu A, Abbasi F, Lamendola CA, Grove K, Tomasso V, Reaven GM. Salsalate-induced changes in lipid, lipoprotein, and apoprotein concentrations in overweight or obese, insulin-resistant, nondiabetic individuals. J Clin Lipidol. 2015 Sep-Oct;9(5):658-63. doi: 10.1016/j.jacl.2015.06.009. Epub 2015 Jun 18. 4: Penesova A, Koska J, Ortega E, Bunt JC, Bogardus C, de Courten B. Salsalate has no effect on insulin secretion but decreases insulin clearance: a randomized, placebo-controlled trial in subjects without diabetes. Diabetes Obes Metab. 2015 Jun;17(6):608-12. doi: 10.1111/dom.12450. Epub 2015 Mar 12. doi: 10.2337/db14-1125. Epub 2014 Dec 4. doi: 10.1002/oby.20991. Epub 2015 Feb 3.
合成参考文献
参考文献:10.18632/aging.100080 摘要:Donato AJ, Pierce GL, Lesniewski LA, Seals DR. Role of NFkappaB in age-related vascular endothelial dysfunction in humans. Aging (Albany NY). 2009 Aug 10;1(8):678–80. 参考文献:10.1016/j.mehy.2011.06.029 摘要:McCarty MF. Full-spectrum antioxidant therapy featuring astaxanthin coupled with lipoprivic strategies and salsalate for management of non-alcoholic fatty liver disease. Med Hypotheses. 2011 Oct;77(4):550–6. doi: 10.1016/j.mehy.2011.06.029.