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:US-9693999-B2 优先权日:2011-01-26 标题:Small molecule RNase inhibitors and methods of use 发明人:DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE 权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education 摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.
专利号:US-8143437-B2 优先权日:2002-02-19 标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof 发明人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X 权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC 摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.
专利号:WO-0032619-A1 优先权日:1998-11-30 标题:Methods and compositions for identification of inhibitors of ribosome assembly 发明人:DAMMEL CAROL S; WATSON JULIE C 权利人:RIBOGENE INC 摘要:The invention provides a means for identifying novel antibiotics by screening for compounds that inhibit bacterial ribosome assembly and ribosomal protein synthesis, which comprises the screening of test compounds to identify those that inhibit the activity of a bacterial ribosomal protein. The in vitro and in vivo assays detect (a) increased translation of a reporter mRNA that is normally repressed in the presence of a ribosomal protein, (b) increased growth in cells that over-express ribosomal protein, and (c) decreased binding of the ribosomal protein to its target RNA. The invention encompasses the (a) methods of screening and testing compounds by the above methods, (b) compounds that are identified in the assay which inhibit ribosome assembly and protein synthesis and (c) methods for treatment using said compounds.
专利号:WO-2009056955-A1 优先权日:2007-10-30 标题 :Amine-bearing phospholipids (abps), their synthesis and use 发明人:ZUMBUEHL ANDREAS 权利人:UNIV BASEL; ZUMBUEHL ANDREAS 摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.
专利号:US-9868747-B2 优先权日:2014-02-18 标题:Marinopyrrole derivatives and methods of making and using same 发明人:LI RONGSHI; SEBTI SAID; LIU YAN; QIN YONG; SONG HAO; CHENG CHUNWEI 权利人:H LEE MOFFITT CANCER CT & RES; CHONGQING ZEIN PHARMACEUTICAL CO LTD 摘要:Marinopyrrole derivatives and methods for their synthesis and use are described herein. Novel cyclic and symmetric marinopyrroles with triazole substituents having antibacterial activity against resistant bacterial strains, such as MRSA are introduced. Also provided are methods of using the compounds for treating or preventing cancer and/or microbial infections.
1: Liu D, Geng T, Wang Y, Ding L. Pharmacokinetic profile of cefbuperazone in healthy Chinese volunteers after single and multiple drip intravenous infusion by HPLC-MS/MS. J Pharm Biomed Anal. 2016 Sep 10;129:28-33. doi: 10.1016/j.jpba.2016.06.029. Epub 2016 Jun 23. 4(6):415-23. 27(4):640-2. doi: 10.1128/aac.27.4.640. 4: Suzuki I, Senda H, Yokota T. In vivo activity of cefbuperazone (T-1982) against various experimental infections in mice. J Antibiot (Tokyo). 1985 Feb;38(2):249-58. doi: 10.7164/antibiotics.38.249. 11(9):577-84. 27(5):817-20. doi: 10.1128/aac.27.5.817. 7: Kager L, Brismar B, Malmborg AS, Nord CE. Impact of cefbuperazone on the colonic microflora in patients undergoing colorectal surgery. Drugs Exp Clin Res. 1986;12(12):983-6. 4(2):150-3. 26(4):585-90. doi: 10.1128/aac.26.4.585.
合成参考文献
参考文献:10.3412/jsb.42.757 摘要:Inada K, Kumagai K, Matui S, Suzuki M, Yoshida M. [Stimulation of human T lymphocyte colony formation by cefbuperazone and other beta-lactam antibiotics]. Nihon Saikingaku Zasshi. 1987 Sep;42(5):757–62. doi: 10.3412/jsb.42.757. 摘要:S6 | ITNANTIBIOTIC | Antibiotic List from the ITN MSCA ANSWER | DOI:10.5281/zenodo.2621956 摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2003).