专利号:US-7576211-B2 优先权日:2004-09-30 标题 :Synthesis of thienopyridinone compounds and related intermediates 发明人:DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; CHEN DONGLI; MARANTZ YAEL; SHACHAM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; BAR-HAIM SHAY; MOHANTY PRADYUMNA; LOBERA MERCEDES; WU LAURENCE 权利人:EPIX DELAWARE INC 摘要:The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.
专利号:US-4310535-A 优先权日:1976-11-30 标题:Combination of drugs and a method for the selective control of the immune reactions evoked in a host by the administration of antigens 发明人:PIERPAOLI WALTER 权利人:PIERPAOLI WALTER 摘要:The invention concerns a new composition or combination of drugs effective to selectively control the immune reactions which are evoked in a host by the administration of antigens. It comprises active components capable of simultaneously blocking the alpha -adrenergic receptors of the cells for catecholamine, blocking the dopaminergic receptors of the cells and increasing the synthesis of serotonin. Preferred drug combinations according to the invention contain in association phentolamine, haloperidol, L-5-hydroxy-tryptophane and possibly dopamine.
专利号:US-2008214827-A1 优先权日:2004-02-03 标 题:Synthesis of Cyanoimino-Benzoimidazoles 发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN 权利人:EURO CELTIQUE SA 摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.
专利号:US-11408016-B2 优先权日:2018-12-28 标 题:Amino acid dehydrogenase mutant and application in synthesis of L-glufosinate-ammonium thereof 发明人:XUE YAPING; CHENG FENG; LI HENG; ZHENG YUGUO; XU JIANMIAO 权利人:UNIV ZHEJIANG TECHNOLOGY 摘要:The present invention discloses an amino acid dehydrogenase mutant and application thereof in synthesizing L-glufosinate-ammonium, the amino acid dehydrogenase mutant is obtained by a single mutation or a multi-site mutation of the amino acid at position 95, 108, 172, 303 of the amino acid sequence shown in SEQ ID No. 2. The amino acid dehydrogenase mutant DyGDH-F95I-A108T-R172P-R303H prepared by the present invention has a specific enzyme activity that is 33 times higher than that of the original Aldo-keto reductase, and the concentration of the largest substrate, 2-carbonyl-4-(hydroxymethylphosphinyl)-butyric acid reaches 500 mM, the amino acid dehydrogenase mutant has more industrial application prospects. Using the amino acid dehydrogenase mutant to produce L-glufosinate-ammonium, the reaction time is significantly shortened, the general process takes 20 hours, and the reaction time of the present invention only requires 120 minutes, which shows that the amino acid dehydrogenase mutant has a good industrial application prospect.
专利号:US-2024287479-A1 优先权日:2021-08-23 标 题 :Glycosyltransferase mutant, and method for catalytic synthesis of rebaudioside m using glycosyltransferase mutant
专利号:US-2006084805-A1 优先权日:2004-09-30 标题:Synthesis of thienopyridinone compounds and related intermediates
1: Domínguez-Rodríguez LE, Stecina K, García-Ramírez DL, Mena-Avila E, Milla- Cruz JJ, Martínez-Silva L, Zhang M, Hultborn H, Quevedo JN. Candidate Interneurons Mediating the Resetting of the Locomotor Rhythm by Extensor Group I Afferents in the Cat. Neuroscience. 2020 Dec 1;450:96-112. doi: 10.1016/j.neuroscience.2020.09.017. Epub 2020 Sep 15. 57(2):937-948. doi: 10.1007/s12035-019-01788-2. Epub 2019 Oct 15. 3: Wang BS, Liu Z, Sun SL, Zhao Y. Identification of genes and candidate agents associated with pancreatic cancer. Tumour Biol. 2014 Jan;35(1):81-8. doi: 10.1007/s13277-013-1009-3. Epub 2013 Aug 10. 17(7):957-65. doi: 10.1177/1087057112444927. Epub 2012 Apr 24. 590(2):289-300. doi: 10.1113/jphysiol.2011.214643. Epub 2011 Nov 21. 6: Fuxe K, Dahlström AB, Jonsson G, Marcellino D, Guescini M, Dam M, Manger P, Agnati L. The discovery of central monoamine neurons gave volume transmission to the wired brain. Prog Neurobiol. 2010 Feb 9;90(2):82-100. doi: 10.1016/j.pneurobio.2009.10.012. Epub 2009 Oct 21. 877(3):285-90. doi: 10.1016/j.jchromb.2008.12.024. Epub 2008 Dec 24.