专利号:US-2018222848-A1 优先权日:2015-08-04 标 题:Salt of Dihydrophenylglycine Methyl Ester 发明人:VAN DER DOES THOMAS; MOODY HAROLD MONRO; LI WEIDONG 权利人:DSM SINOCHEM PHARM NL BV 摘要:The present invention relates to the hemi sulfuric acid salt of methyl (R)-2-amino-2-(cyclohexa-1,4-dien-1-yl)acetate, also trivially referred to as the hemi sulfuric acid salt of D-dihydrophenylglycine methyl ester, to a method for the preparation of said salt and to the use of said salt in the enzymatic synthesis of antibiotics.
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:EP-0024372-A1 优先权日:1979-08-03 标题:Derivatives of clavulanic acid, their preparation and pharmaceutical compositions containing them 发明人:DENERLEY PAUL MILLINGTON; EGLINGTON ALFRED JOHN; HARBRIDGE JOHN BARRY 权利人:BEECHAM GROUP PLC 摘要:The compounds of the formula (II):n and salts and esters thereof wherein the hydroxyl group occupies position 2 or 4 R 1 and R 2 may be the same or different and represent hydrogen, halogen, hydroxy, lower alkyl, cyclopentyl, cyclohexyl, lower alkoxy or R, and R 2 when an adjacent carbon atoms may together represent a 1,4-buta-1,3-dienylene group or a polymethylene group containing from 3 to 5 carbon atoms; have been found to be β-lactam antibiotics and synergists with penicillins and cephalosporins. Their preparation and use is described. The synthesis of intermediates useful in their preparation is also described.
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.
1: el Zawahry M, Aziz AA, Soliman M, Shoeib S, Tadros SS. Clinical and bacteriological evaluation of a twice daily regimen of epicillin capsules for the treatment of skin infections. Br J Dermatol. 1976 Aug;95(2):177-80. 3: Limson BM, Siasoco RE, Dial FP. The effect of combined sodium epicillin injection and orally administered epicillin in the treatment of acute infective illness. Med J Aust. 1972 Dec 9;2(24):1348-51. 6: Basker MJ, Gwynn MN, White AR. Comparative activities of ampicillin, epicillin and amoxycillin in vitro and in vivo. Chemotherapy. 1979;25(3):170-80. Review.
合成参考文献
摘要:S6 | ITNANTIBIOTIC | Antibiotic List from the ITN MSCA ANSWER | DOI:10.5281/zenodo.2621956 参考文献:10.1007/bf01642027 摘要:Hamilton-Miller JM, Brumfitt W. Newer beta-lactam antibiotics. Infection. 1974;2(2):82–94. doi: 10.1007/bf01642027. 摘要:Medicamentos de Actualidad., 9(100), 1973 摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2003).