N-methoxylamine hydr°Chlorideerythromycin A(E)-2'-O-4''-O-diformyl-9-deoxo-9-methoxyiminoerythromycin A(E)-11-O-(2-dimethylaminoethoxy)methyl-9-deoxo-9-methoxyiminoerythromycin A
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: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.
专利号:US-9907753-B2 优先权日:2010-03-19 标 题 :Lipid vesicle compositions and methods of use 发明人:IRVINE DARRELL J; MOON JAEHYUN 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The invention provides delivery systems comprised of stabilized multilamellar vesicles, as well as compositions, methods of synthesis, and methods of use thereof. The stabilized multilamellar vesicles may comprise prophylactic, therapeutic and/or diagnostic agents.
专利号:US-7179794-B2 优先权日:1998-06-08 标题 :Multivalent macrolide antibiotics 发明人:GRIFFIN JOHN H; PACE JOHN L 权利人:THERAVANCE INC 摘要:Disclosed are multibinding compounds which include macrolide antibiotics, aminoglycosides, lincosamides, oxazolidinones, streptoramins, tetracycline and/or other compounds which bind to bacterial ribosomal RNA and/or to one or more proteins involved in ribosomal protein synthesis in the bacterium, which are useful in treating bacterial infections. The compounds adversely affect protein expression and have an antibacterial effect. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is macrolide antibiotic, aminoglycoside, lincosamide, oxazolidinone, streptogramin, tetracycline or other compound which binds to bacterial ribosomal RNA and/or one or more proteins involved in ribosomal protein synthesis in the bacterium.
专利号:US-2014315720-A1 优先权日:2012-10-24 标 题 :Polysaccharide ester microspheres and methods and articles relating thereto 发明人:FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY 权利人:CELANESE ACETATE LLC 摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.
1: Shafuddin E, Mills GD, Holmes MD, Poole PJ, Mullins PR, Black PN. A double-blind, randomised, placebo-controlled study of roxithromycin and doxycycline combination, roxithromycin alone, or matching placebo for 12 weeks in adults with frequent exacerbations of chronic obstructive pulmonary disease. J Negat Results Biomed. 2015 Sep 7;14:15. doi: 10.1186/s12952-015-0034-8. 2: Choi Y, Koh SJ, Lee HS, Kim JW, Gwan Kim B, Lee KL, Kim JS. Roxithromycin inhibits nuclear factor kappaB signaling and endoplasmic reticulum stress in intestinal epithelial cells and ameliorates experimental colitis in mice. Exp Biol Med (Maywood). 2015 Dec;240(12):1664-71. doi: 10.1177/1535370215591829. Epub 2015 Jun 18. 3: Dai YR, Wu HY, Wu LQ, Xu H, Yin J, Yan SS, Zeng WX. Roxithromycin reduces the viability of cultured airway smooth muscle cells from a rat model of asthma. Eur Rev Med Pharmacol Sci. 2014;18(23):3564-72. doi: 10.1016/j.jiac.2013.07.010. Epub 2013 Dec 11. doi: 10.1097/FTD.0000000000000203. doi: 10.1016/j.ejps.2014.12.019. Epub 2015 Jan 2. doi: 10.1136/bmj.g4930.
合成参考文献
参考文献:10.1021/jm101593u 摘要:Lee Y, Choi JY, Fu H, Harvey C, Ravindran S, Roush WR, Boothroyd JC, Khosla C. Chemistry and biology of macrolide antiparasitic agents. J Med Chem. 2011 Apr 28;54(8):2792–804.