📜2-(1-Phenylethyl)Pyridine置于potassium Tert-Butylate,二甲基亚砜,Sodium T-Butanolate体系中,用 甲苯 作为反应溶剂,化学反应 11.0H,反应生成 多西拉敏 参考文献:Transition-Metal Free Chemoselective Hydroxylation And Hydroxylation-deuteration Of Heterobenzylic Methylenes 标题:Transition-Metal Free Chemoselective Hydroxylation And Hydroxylation-deuteration Of Heterobenzylic Methylenes 摘要:We Developed An Approach For Direct Selective Hydroxylation Of Heterobenzylic Methylenes To Secondary Alcohols Avoiding Overoxidation To Ketones By Using A Kobu-T/dmso/air System. Most Reactions Could Reach Completion In Several Minutes To Give Hydroxylated Products In 41-76% Yields. Using Dmso-D6,This Protocol Resulted In Difunctionalization Of Heterobenzylic Methylenes To Afford α-Deuterated Secondary Alcohols (>93% Incorporation). By Employing This Method,Active Pharmaceutical Ingredients Carbinoxamine And Doxylamine Were Synthesized In Two Steps In Moderate Yields. DOI:10.1021/acs.Orglett.0C03108
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-7919505-B2 优先权日:2006-07-11 标题 :Xinafoate salt of a substituted 5-oxazol-2-yl-quinoline compound 发明人:TING PAULINE C; LEE JOE F; FENG KUNG-I; REEDER MICHAEL R; TRZASKA SCOTT T; ZHU MAN; MAO CHEN; FILIPOV DIMITAR L; ZARKADAS DIMITRIOS N 权利人:SCHERING CORP 摘要:The present invention relates to the compound of the formula n nTo methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to polymorphs and processes of synthesis of the polymorphic forms.
专利号:US-2011003780-A1 优先权日:2007-07-10 标题:Hydrogen chloride salt of a substituted 5-oxazol-2-yl-quinoline compound and a process for the production thereof 发明人:ZHU MAN 权利人:SCHERING CORP 摘要:The present invention relates to the compound of the Formula I: n n n n n n n n n n and to methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to a particular crystalline form and processes of synthesis of the crystalline form. n IM=105109
专利号:US-2015352230-A1 优先权日:2013-01-11 标 题:Synthesis and isolation of dendrimer based imaging systems 发明人:MULLEN DOUGLAS GURNETT; BAKER JR JAMES R; BANASZAK HOLL MARK M; HUANG BAOHUA; DOUGHERTY CASEY; BALL JACK 权利人:UNIV MICHIGAN 摘要:The present invention relates to novel methods of synthesis and isolation of antibodies conjugated with modular dendrimer nanoparticles. In particular, the present invention is directed to antibodies conjugated with novel modular dendrimer nanoparticles having precise numbers of imaging agents, methods of synthesizing the same, compositions comprising such antibodies conjugated with such modular dendrimer nanoparticles, as well as systems and methods utilizing the conjugates (e.g., in imaging settings) (e.g., in diagnostic and/or therapeutic settings) (e.g., for the delivery of therapeutics, imaging, and/or targeting agents).
专利号:US-2012232225-A1 优先权日:2009-08-26 标 题:Synthesis and isolation of dendrimer systems 发明人:BAKER JR JAMES R; BANASZAK HOLL MARK M; MULLEN DOUGLAS GURNETT; ORR BRADFORD G; DESAI ANKUR; SANDER LEONARD M; WADDELL JACK NEEL 权利人:BAKER JR JAMES R; BANASZAK HOLL MARK M; MULLEN DOUGLAS GURNETT; ORR BRADFORD G; DESAI ANKUR; SANDER LEONARD M; WADDELL JACK NEEL; UNIV MICHIGAN 摘要:The present invention relates to novel methods of synthesis and isolation of dendrimer systems. In particular, the present invention is directed to novel dendrimer conjugates with defined and limited numbers of ligand conjugates and high levels of structural uniformity, methods of synthesizing the same, compositions comprising the conjugates, as well 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) diagnosis and/or therapy, pain therapy, etc.)).
专利号:WO-2023075715-A1 优先权日:2021-10-26 标题 :A pharmaceutical formulation including leukotriene receptor antagonists and/or leukotriene synthesis inhibitors combined with non-steroidal anti-inflammatory drugs (nsaids) 发明人:OYTUN FARUK; CAN EFE 权利人:VSY BIYOTEKNOLOJI VE ILAC SANAYI ANONIM SIRKETI 摘要:This invention is related to a pharmaceutical formulation including Leukotriene receptor antagonists and/or Leukotriene synthesis inhibitors combined with non-steroidal anti-inflammatory drugs (NSAIDs) and antihistamines in ocular diseases and in inflammatory and allergic diseases for systemic and topical use. The objective of this invention is to create a novel formulation to be effective as much as steroids while having significantly less side effects for long-term use in treating ocular diseases, inflammatory and allergic diseases. In other words our aim is to achieve the inhibition of pro-inflammatory mediators (prostaglandins, thromboxane, histamine and leukotrienes) as much as steroids do with a safer combination.
1: Doxylamine/pyridoxine for nausea and vomiting in pregnancy. Drug Ther Bull. 2019 Mar;57(3):38-41. doi: 10.1136/dtb.2018.000053. Epub 2019 Jan 31. 2021 Jan–. 2012–. Doxylamine. 2017 Jan 16. 13(1):e0189978. doi: 10.1371/journal.pone.0189978. 5: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006–. Doxylamine. 2018 Dec 3. 118(4. Vyp. 2):67-72. Russian. doi: 10.17116/jnevro20181184267. 39(4):808-817. doi: 10.1007/s11096-017-0467-x. Epub 2017 May 2. 8: Abramowitz A, Miller ES, Wisner KL. Treatment options for hyperemesis gravidarum. Arch Womens Ment Health. 2017 Jun;20(3):363-372. doi: 10.1007/s00737-016-0707-4. Epub 2017 Jan 9.
合成参考文献
摘要:Toxicology Letters., 109(Suppl 摘要:USP Convention. USPDI - Drug Information for the Health Care Professional. 16th ed. Volume I. Rockville, MD: U.S. Pharmaceutical Convention, Inc. 1996 (Plus updates)., p. 327 摘要:Sunshine, Irving (ed.) Methodology for Analytical Toxicology. Cleveland: CRC Press, Inc., 1975., p. 441 摘要:Ashford, R.D. Ashford's Dictionary of Industrial Chemicals. London, England: Wavelength Publications Ltd., 1994., p. 376 摘要: