CAS: 53-86-1; 2-(1-(4-Chlorobenzoyl)-5-Methoxy-2-Methyl-1H-Indol-3-yl)Acetic Acid

上下游产品

1-(4-Chlorbenzoyl)-5-methoxy-2-methyl-1H-indolyl-3-essigsaeure-2-oxo-propylester 2-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetoxy]-2'-hydroxy-diethyloxide 5-Methoxy-2-methylindole-3-acetic acid 4-chloro-benzoyl chloride[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]acetic acid 2,5-dioxopyrrolidin-1-yl ester 1H-indole-3-acetic acid, 1-(4-chlorobenzoyl)-5-methoxy-2-methyl 2-(4-benzyl-1-piperazinyl)ethyl ester Indopred 1-(4-Chlorbenzoyl)-5-methoxy-2-methyl-indol-3-essigsaeure-(11β,17-dihydroxy-3,20-dioxo-4-pregnen-21-yl)ester

吲哚美辛ep杂质i置于sodium Hydroxide体系中,用 甲醇,水 作为反应溶剂,化学反应 1.0H,以99%的收率获得产物吲哚美辛
参考文献:肌红蛋白催化未受保护吲哚的 C−h 官能化
标题:肌红蛋白催化未受保护吲哚的 C−h 官能化
摘要:功能化吲哚是生物活性天然产物和药物中反复出现的基序.虽然过渡金属催化的卡宾转移提供了一条有吸引力的途径来获得 C3 功能化吲哚,但由于来自更容易的 Nh 插入反应的竞争,这些方案仅在 N 保护吲哚存在的情况下才可行.在此,报道了一种能够使未受保护的吲哚直接 C−h 官能化的生物催化策略.肌红蛋白的工程变体为该反应提供了有效的生物催化剂,这在生物界中是没有先例的,能够在α-重氮乙酸乙酯存在下转化多种吲哚,以高转化率产生相应的c3功能化衍生物,并且优异的化学选择性.可以利用这种策略来开发一种简洁的化学酶途径来提供非甾体类抗炎药吲哚美辛.
DOI:10.1002/anie.201804779

专利信息

专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人：BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:US-8420850-B2
优先权日:2010-05-14
标 题:Compounds for the synthesis of biostable polyurethane, polyurea or polyurea urethane polymers
发明人：DUOCASTELLA CODINA LLUIS; MOLINA MARIA; ARAD OFIR; BORRELL BILBAO JOSE IGNACIO; GARCIA DAVID SANCHEZ; PETTERSON SALOM SOFIA HENRIETTE
权利人:DUOCASTELLA CODINA LLUIS; MOLINA MARIA; ARAD OFIR; BORRELL BILBAO JOSE IGNACIO; GARCIA DAVID SANCHEZ; PETTERSON SALOM SOFIA HENRIETTE; IBERHOSPITEX SA
摘要:The invention comprises compounds which are derived from a drug or a substance with therapeutic properties, and useful as reagents for the synthesis of biostable polymers including said drug in their backbone, namely polyurethanes, polyureas or polyurea urethanes that are biocompatible and biostable. The invention also comprises the processes for preparing the compounds and the polymers, and to the use of these polymers for the manufacture of medical devices.

专利号:US-5043328-A
优先权日:1986-05-09
标 题 :Formulations containing unsaturated fatty acids for the synthesis of prostaglandins and hydroxy-fatty acids in biological systems
发明人：WEITHMANN KLAUS U
权利人:HOECHST AG
摘要:The present invention relates to formulations containing unsaturated fatty acids for the synthesis of prostaglandins and hydroxy-fatty acids in biological systems and to the use of such formulations for the preparation of medicaments which are suitable for curing prostaglandin deficiencies in humans or animal, for example healing or preventing diseases of the gastro-intestinal tract.

专利号:WO-9614060-A1
优先权日:1994-11-04
标题 :Use of receptor agonists to stimulate superoxide dismutase activity
发明人：MARKLUND STEFAN L; STRAALIN PONTUS
权利人:MARKLUND STEFAN L; STRAALIN PONTUS
摘要:The present invention relates to the use of a substance for the manufacture of a composition for stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells. In particular, the invention relates to the use of a substance for the manufacture of a composition for prophylaxis or treatment of a disease or disorder connected with the presence or formation of superoxide radicals and other toxic intermediates derived from the superoxide radical. Further, the invention relates to a method for determining the effect of a substance with respect to stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells and to substances which have been selected by said method. Within the scope of the invention is a method of preventing, diminishing, controlling or inhibiting a disease or disorder connected with the presence or formation of superoxide radicals and other toxic intermediates derived from the superoxide radical in a patient who has been established to have a high risk of developing a such disease or disorder, or who has developed a such disease or disorder, the method comprising administering an effective amount of a substance which is capable of stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells.

专利号:US-7211590-B2
优先权日:2002-08-01
标 题:Nitrosated proton pump inhibitors, compositions and methods of use
发明人：FANG XINQIN; GARVEY DAVID S; LETTS L GORDON
权利人:NITROMED INC
摘要:The invention describes novel nitrosated proton pump inhibitor compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated proton pump inhibitor compound, 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 proton pump inhibitor compound, 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 proton pump inhibitor compound, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating gastrointestinal disorders; facilitating ulcer healing; decreasing the recurrence of ulcers; improving gastroprotective properties, anti-Helicobacter pylori properties or antacid properties of proton pump inhibitors; decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds; treating bacterial infections and/or viral infections.

专利号:US-6512137-B1
优先权日:1999-01-26
标题 :Synthesis method of nitroxymethylphenyl esters of aspirin derivatives
发明人：DEL SOLDATO PIERO; GARUFI MICHELE
权利人:NICOX SA
摘要:The invention describes a method for the synthesis of nitroxymethylphenyl esters of aspirin derivatives.