CAS: 144143-96-4; (E)-4-((2-Butyl-5-(2-Carboxy-3-(Thiophen-2-yl)Prop-1-En-1-yl)-1H-Imidazol-1-yl)Methyl)Benzoic Acid Methanesulfonic Acid Salt

依普罗沙坦 反应生成甲磺酸依普罗沙坦
参考文献: Process For The Preparation Of Eprosartan[fr] Procédé De Préparation D'éprosartan
标题: Process For The Preparation Of Eprosartan[fr] Procédé De Préparation D'éprosartan
摘要:本文披露了一种改进的新型合成过程,用于制备厄普罗沙坦.该过程包括在存在阴离子交换树脂或dbu的碱的条件下,将式(II)的2-N-丁基-4-甲酰基咪唑与从以下组中选择的n保护基进行处理:甲基丙烯酸酯的c1-C4烷基衍生物;巴豆烯酸酯的c1-C4烷基衍生物;或丙烯酸酯的c1-C4烷基衍生物,可选地在溶剂的存在下,获得n保护化合物(III),这是第一阶段.第二阶段包括将第一阶段获得的n保护化合物(III)与2-(2-噻吩甲基)丙二酸单乙酯反应,得到化合物(v).第三阶段包括将从第二阶段得到的化合物(v)与甲基-4-(溴甲基)苯甲酸酯反应,得到化合物(vii).进一步地,使用苛性钠溶液同时水解酯基和去除n保护基,以得到式(i)的厄普罗沙坦,这是第四阶段.最后,在第五阶段制备厄普罗沙坦的药用可接受盐.

专利信息

专利号:US-2008287407-A1
优先权日:2003-12-10
标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
发明人：GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
权利人:NITROMED INC
摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate 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 pyruvate 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 pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

专利号:CN-117778448-A
优先权日:2023-12-14
标题 :Application of VvMYC2 gene in promoting the synthesis of monoterpene components in Sunshine Rose

专利号:CN-115927122-B
优先权日:2023-01-17
标题:Post-metagen prepared from Lactobacillus paracasei and having effects of promoting synthesis of host HA and enhancing application of HA

专利号:US-2023053729-A1
优先权日:2019-12-24
标 题 :A recombinant filamentous fungus for producing ethanol and its construction and application
发明人：TIAN CHAOGUANG; ZHANG YONGLI; LI JINGEN; SUN TAO; LIU QIAN; SUN WENLIANG
权利人:TIANJIN INST IND BIOTECHNOLOGY CAS
摘要:The invention discloses a construction method of genetic engineering fungi of filamentous fungi. Through the genetic engineering method, the filamentous fungi overexpress the positive regulation genes of ethanol synthesis, and/or down regulate the negative regulation genes of endogenous ethanol synthesis to obtain genetic engineering strains. Or overexpression of acetaldehyde dehydrogenase and ethanol dehydrogenase containing mitochondrial localization signal sequence, or overexpression of pyruvate decarboxylase and ethanol dehydrogenase containing mitochondrial localization signal sequence, or overexpression of acetaldehyde dehydrogenase, ethanol dehydrogenase and pyruvate decarboxylase containing mitochondrial localization signal sequence in filamentous fungal cells. Compared with the original strain, the ethanol synthesis ability of the obtained genetically engineered strains are improved.

专利号:US-11285169-B2
优先权日:2013-03-13
标题 :Methods for modulating chemotherapeutic cytotoxicity
发明人：ROBERTS DAVID D; SOTO PANTOJA DAVID R
权利人:US HEALTH
摘要:Methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent, such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are provided. Example disclosed methods reduce cardiotoxicity. In one example, the methods include administering to a subject with cancer an effective amount of a CD47 antisense morpholino oligonucleotide and an anthracycline such as doxorubicin. Methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are also provided. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the DNA damaging agent.

专利号:US-2019275058-A1
优先权日:2016-03-04
标题:Compositions and methods for treating addiction or substance use disorders
发明人：DETKE MICHAEL; GLOFF CAROL; STRAUB JULIE
权利人:EMBERA NEUROTHERAPEUTICS INC
摘要:The present invention is directed to compositions and methods for treating addiction and/or substance use disorders, including nicotine addiction associated with smoking tobacco. In particular, this invention is directed to combinations of low doses of a cortisol synthesis inhibitor, such as metyrapone, in combination with low doses of a benzodiazepine, such as oxazepam. The compositions and methods of the present invention include pharmaceutical compositions and methods that are safe and efficacious for treating animals and humans.