专利号:US-12123041-B2 优先权日:2018-09-21 标 题:Method for the production of amino sugar-containing products 发明人:MAERTENS JO; BAUWENS DAVID; VAN BELLEGEM WOUTER; COUSSEMENT PIETER; DUCHI DRIES; DE MEY MARJAN 权利人:UNIV GENT 摘要:A method or producing amino sugar (containing) products using metabolically engineered microorganisms is disclosed, wherein the conversion of UDP-N-acetylglucosamine to cell envelope precursors and molecules is reduced by altering the activity of enzymes involved in the synthesis of cell envelope precursors and molecules.
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-4340672-A 优先权日:1979-09-19 标 题:Enzymatic synthesis of β-lactam antibacterials 发明人:KONDO EIJI; MITSUGI TAKASHI; FUJIWARA TAMIO; MUNEYUKI RYONOSUKE 权利人:SHIONOGI & CO 摘要:Penicillins and cephalosporins can be synthesized by the action of an acylase on a penicillin or cephalosporin nucleus amine as substrate and an ester (I) of the following formula as the acyl source: (I) (wherein RCO is an acyl group in penicillin or cephalosporin side chains; X is a hydrogen atom, lower alkyl group or hydroxy-lower alkyl group; Y is a hydrogen atom or a lower alkyl group; and n is a positive integer). The novel acyl source (I) is also disclosed.
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:US-2025228841-A1 优先权日:2024-01-12 标题 :Compositions affecting pigment production and methods for treatment of bacterial diseases 发明人:Lee Wai Yip Thomas; LO KAI YIP GEORGE 权利人:APTORUM THERAPEUTICS LTD 摘要:Provided herein are compounds, derivatives thereof, composition comprising one or more of said compounds and derivatives, and methods for prevention and/or treatment of microbial infections and/or related diseases or conditions. The present compounds and/or derivatives thereof can be represented by Formula (II):The present methods include administering to a subject an effective amount of one or more compounds of Formula (II). In one embodiment, said microbial infections are bacterial infections. More specifically, the bacterial infections are staphylococcal infections. Compositions are provided that include compounds of formula II in combination with one or more antibiotics or one or more staphyloxanthin-synthesis-inhibiting compounds.
专利号:US-2025002508-A1 优先权日:2020-05-05 标题 :Boronic acid derivatives and synthesis, polymorphic forms, and therapeutic uses thereof 发明人:HECKER SCOTT J; BOYER SERGE HENRI; BIO MATTHEW M; FANG YUANQING; GONZALES DE CASTRO ANGELA; LEFORT LAURENT; ZHU ZUOLIN; LINDER THOMAS 权利人:QPEX BIOPHARMA INC 摘要:Disclosed herein are antimicrobial compounds, polymorphic forms, compositions, pharmaceutical compositions, the method of use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents, for example, β-lactamase inhibitors (BLIs).
1: He R, Yu ZH, Zhang RY, Wu L, Gunawan AM, Zhang ZY. Cefsulodin Inspired Potent and Selective Inhibitors of mPTPB, a Virulent Phosphatase from Mycobacterium tuberculosis. ACS Med Chem Lett. 2015 Nov 3;6(12):1231-5. doi: 10.1021/acsmedchemlett.5b00373. 2: Tan LK, Ooi PT, Carniel E, Thong KL. Evaluation of a modified Cefsulodin- Irgasan-Novobiocin agar for isolation of Yersinia spp. PLoS One. 2014 Aug 29;9(8):e106329. doi: 10.1371/journal.pone.0106329. 3: Sarkar SK, Dutta M, Kumar A, Mallik D, Ghosh AS. Sub-inhibitory cefsulodin sensitization of E. coli to β-lactams is mediated by PBP1b inhibition. PLoS One. 2012;7(11):e48598. doi: 10.1371/journal.pone.0048598. Epub 2012 Nov 6.
合成参考文献
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