专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-2005186197-A1 优先权日:2002-08-29 标 题:Peptide inhibitors of beta lactamases 发明人:PALZKILL TIMOTHY; HUANG WANZHI 摘要:Peptide inhibitors of β-lactamases have been identified by the synthesis of peptide arrays using synthesis SPOT technology. These peptide inhibitors of β-lactamase have activity against a broad spectrum of β-lactamases and are useful in a variety of applications.
专利号:US-2006178357-A1 优先权日:2005-02-10 标题 :Chphalosporin-derived mercaptans as inhibitors of serine and metallo-beta-lactamases 发明人:BUYNAK JOHN D; CHEN HANSONG 权利人:BUYNAK JOHN D; CHEN HANSONG 摘要:Compounds of formula I: See Formula I in Figures Section n nwherein R 1 , R 2 , R 3 , R 4 and n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting simultaneously serine and metallo-β-lactamase enzymes, for enhancing the activity of β-lactam antibiotics, and for treating β-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and novel intermediates useful for the synthesis of compounds of formula I.
专利号:US-8017776-B2 优先权日:2003-07-15 标题 :Methods for synthesis of acyloxyalkyl compounds 发明人:BHAT LAXMINARAYAN; GALLOP MARK A 权利人:XENOPORT INC 摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.
专利号:EP-0942745-B1 优先权日:1996-08-26 标题:Use of hyaluronidase 发明人:TUFVESON GUNNAR; HAELLGREN ROGER; JOHNSSON CECILIA; WAHLBERG JAN 权利人:TUFVESON GUNNAR; HAELLGREN ROGER; JOHNSSON CECILIA; WAHLBERG JAN 摘要:The use of hyaluronidase in the manufacturing of a drug for the treatment of conditions of interstitial edema in connection with organ grafting associated with an increased local content of hyaluronan in the connective tissue of a mammal. The drug comprises hyaluronidase in an amount giving a daily dosage of from 1 to 100,000 IU/kg body weight when given locally or systemically to a mammal. A method of treating conditions of interstitial edema in connection with organ grafting associated with an increased local synthesis of hyaluronan by systemic or local treatment with a pharmaceutical comprising hyaluronidase.
专利号:US-10443047-B2 优先权日:2014-05-01 标题 :Increasing cellular lipid production by increasing the activity of diacylglycerol acyltransferase and decreasing the activity of triacylglycerol lipase 发明人:TSAKRAKLIDES VASILIKI; BREVNOVA ELENA E 权利人:NOVOGY INC 摘要:Disclosed are methods and compositions for increasing the triacylglycerol content of a cell by up-regulating diacylglycerol acyltransferase and down-regulating triacylglycerol lipase. In some embodiments, a DGA1 protein is expressed and a native TGL3 gene is knocked out, thereby increasing the synthesis of triacylglycerol and decreasing its consumption, respectively.
1: Steere AC, Strle F, Wormser GP, Hu LT, Branda JA, Hovius JW, Li X, Mead PS. Lyme borreliosis. Nat Rev Dis Primers. 2016 Dec 15;2:16090. doi: 10.1038/nrdp.2016.90. Review. Erratum in: Nat Rev Dis Primers. 2017 Aug 03;3:17062. 2: Dalal N, Buckner IS, Wildfong PLD. Experimental Determination and Theoretical Calculation of the Eutectic Composition of Cefuroxime Axetil Diastereomers. AAPS PharmSciTech. 2017 Oct;18(7):2570-2578. doi: 10.1208/s12249-017-0739-8. Epub 2017 Feb 22. Review. doi: 10.3109/10717544.2013.871603. Epub 2014 Jan 13. 7: Marx MA, Fant WK. Cefuroxime axetil. Drug Intell Clin Pharm. 1988 Sep;22(9):651-8. Review. doi: 10.1155/2015/921049. Epub 2015 Jan 11.
合成参考文献
参考文献:10.1159/000089019 摘要:Krasagakis K, Samonis G, Maniatakis P, Georgala S, Tosca A. Bullous erysipelas: clinical presentation, staphylococcal involvement and methicillin resistance. Dermatology. 2006;212(1):31–5. doi: 10.1159/000089019. 参考文献:10.1007/s10549-005-9058-y 摘要:Ruvalcaba-Limón E, Robles-Vidal C, Poitevin-Chacón A, Chávez-Macgregor M, Gamboa-Vignolle C, Vilar-Compte D. Complications after breast cancer surgery in patients treated with concomitant preoperative chemoradiation: A case-control analysis. Breast Cancer Res Treat. 2006 Jan;95(2):147–52. doi: 10.1007/s10549-005-9058-y. 参考文献:10.1007/s00404-011-1967-x 摘要:Bowkalow S, Brauer M, Groß W, Schleußner E. Severe H1N1-infection during pregnancy. Archives of Gynecology and Obstetrics. 2011 Jul 12;284(5):1133. doi: 10.1007/s00404-011-1967-x. 参考文献:10.1007/s10096-011-1322-y 摘要:Smithson A, Chico C, Ramos J, Netto C, Sanchez M, Ruiz J, Porron R, Bastida MT. Prevalence and risk factors for quinolone resistance among Escherichia coli strains isolated from males with community febrile urinary tract infection. European Journal of Clinical Microbiology & Infectious Diseases. 2011 Jul 15;31(4):423–30. doi: 10.1007/s10096-011-1322-y. 参考文献:10.1016/j.ophtha.2011.04.021 摘要:Shalchi Z, Gurbaxani A, Baker M, Nash J. Antibiotic resistance in microbial keratitis: ten-year experience of corneal scrapes in the United Kingdom. Ophthalmology. 2011 Nov;118(11):2161–5. doi: 10.1016/j.ophtha.2011.04.021.