CAS: 144457-28-3; (S)-2-(2-Chlorophenyl)-2-(6,7-Dihydrothieno[3,2-C]Pyridin-5(4H)-yl)Acetic Acid

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CAS号1007128-30-4 (1S)-quinolin-4... | CAS号113665-84-2 氯吡格雷 | CAS号50-00-0 甲醛 | CAS号141315-50-6 (+)-2-氯-L-苯基甘氨酸 | CAS号120202-66-6 硫酸氯吡格雷 | CAS号113665-84-2 氯吡格雷 | CAS号144750-42-5 (S)-(O-氯苯基)-6,7...

📜氯吡格雷置于potassium Dihydrogenphosphate,Sodium Citrate,三羟甲基氨基甲烷,Magnesium Chloride体系中,化学反应 0.25H,反应生成氯吡格雷酸
参考文献:最佳 Ph 8.5 至 9 用于水解人肝微粒体中 Vixotrigin 和羧酸酯酶 1 的其他碱性底物
标题:最佳 Ph 8.5 至 9 用于水解人肝微粒体中 Vixotrigin 和羧酸酯酶 1 的其他碱性底物
摘要:摘要 Vixotrigine 是一种电压和使用依赖性钠通道阻滞剂,正在研究用于治疗神经性疼痛.维索三嗪在人体中的主要体内代谢途径之一是甲酰胺水解形成羧酸代谢物 M14. 羧酸酯酶 (Ces) 抑制剂磷酸双 (4-硝基苯) 以浓度依赖性方式抑制人肝细胞中 M14 的体外形成.水解反应被鉴定为由重组人 Ces1B 催化. 最初观测到在 Ph 7.4 时人肝微粒体中仅微量形成 M14 使我们怀疑 Ces1 的参与,Ces1 是一种定位于内质网的酶和人肝脏中的主要羧酸酯酶.进一步研究表明,在人肝微粒体中,Vixotrigin 和 Ces1 的其他两种碱性底物哌醋甲酯和奥司他韦水解的最佳 Ph 值为 8.5-9,高于它们各自的 Pk A(碱基),表明中性形式的碱性底物可能是肝微粒体中 Ces1 催化的首选.
Doi:10.1080/00498254.2021.2018629

专利信息

专利号:US-10005720-B2
优先权日:2013-04-05
标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
发明人：SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

专利号:US-11807883-B2
优先权日:2020-11-03
标 题:Polypeptide tag, highly soluble recombinant nitrilase and application thereof in synthesis of pharmaceutical chemicals
发明人：XUE YAPING; XIE DONG; XIONG NENG; ZHENG YUGUO
权利人:UNIV ZHEJIANG TECHNOLOGY
摘要:The present invention provides a polypeptide tag and its application in the synthesis of pharmaceutical chemicals, the recombinant nitrilase was obtained by connecting a polypeptide tag to the N-terminus of the amino acid sequence of the nitrilase; wherein amino acids at both ends of the polypeptide tag are uncharged glycine G, and the rest are a random combination of any one or more of glycine G, histidine H, glutamic acid E, aspartic acid D, lysine K and arginine R; The activity of the recombinant nitrilase in the preparation of 1-cyanocyclohexyl acetic acid is up to 3034.7 U/g dcw, the polypeptide tag significantly improves the soluble expression of nitrilase, and the whole cell catalyst hydrolyzes 1M substrate with the same concentration 30 minutes faster than the mother enzyme. The method provided by the present invention can also be used for the biocatalytic reaction of other pharmaceutical intermediates as the substrate catalyzed by the nitrilase, improving the activity of the whole cell catalyst in reaction, and also improving the solubility of other types of nitrilases and the activity of the corresponding whole cell catalysts.

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: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-2002183366-A1
优先权日:2001-03-23
标题:Cyclooxygenase-2 inhibitors, compositions and methods of use
发明人：GARVEY DAVID S; SCHROEDER JOSEPH D
摘要:This invention describes novel compounds that are cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, 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, optionally, at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal toxicity or other toxicities; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.

专利号:US-2024343691-A1
优先权日:2006-12-28
标题:Compositions for modulating a kinase cascade and methods of use thereof
发明人：HANGAUER JR DAVID G; PATRA DEBASIS; CODY JEREMY A; PALMER GRANT J; ISBESTER PAUL K; SALSBURY JONATHON
权利人:ATNX SPV LLC
摘要:The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl) pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.