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).
专利号:US-4684724-A 优先权日:1981-12-25 标题:4-Cyano-2-azetidinones and production thereof 发明人:OCHIAI MICHIHIKO; KISHIMOTO SHOJI; MATSUO TAISUKE 权利人:TAKEDA CHEMICAL INDUSTRIES LTD 摘要:4-Cyano-2-azetidinone derivatives represented by the formula ##STR1## wherein R 1 is an amino group which may be acylated or protected, X is a hydrogen atom or a methoxy group and W is a hydrogen atom or a sulfo group, and methods of producing the same, for example, as represented by ##STR2## wherein R 2 is an acylated or protected amino group, Y is a halogen atom or a group having the formula --OCOR 3 , --SCOR 3 or --S(O) n --R 3 (R 3 being a hydrocarbyl group and n an integer 1 or 2), R 4 is an amino group which may be acylated or protected and X is as defined above. Compounds [I] are useful as advantageous intermediates for the synthesis of optically active 4-substituted-2-azetidinone derivatives, and, when W=SO 3 H, [I] are also useful as antimicrobial agents and as beta-lactamase inhibitors.
专利号:US-9839642-B2 优先权日:2014-05-09 标 题:Beta-tetrazolyl-propionic acids as metallo-beta-lactamase inhibitors 发明人:TANG HAIFENG; YANG SHU-WEI; MANDAL MIHIR; SU JING; LI GUOQING; PAN WEIDONG; TANG HAIQUN; DEJESUS REYNALDA; PAN JIANPING; HAGMANN WILLIAM; DING FA-XIANG; XIAO LI; PASTERNAK ALEXANDER; HUANG YUHUA; DONG SHUZHI; YANG DEXI 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula I that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
专利号:US-9708336-B2 优先权日:2014-01-22 标题 :Metallo-beta-lactamase inhibitors 发明人:MANDAL MIHIR; TANG HAIFENG; XIAO LI; SU JING; LI GUOQING; YANG SHU-WEI; PAN WEIDONG; TANG HAIQUN; DEJESUS REYNALDA; HICKS JACQUELINE; LOMBARDO MATTHEW; CHU HONG; HAGMANN WILLIAM; PASTERNAK ALEX; GU XIN; JIANG JINLONG; DONG SHUZHI; DING FA-XIANG; LONDON CLARE; BISWAS DIPSHIKHA; YOUNG KATHERINE; HUNTER DAVID N; ZHAO ZHIQIANG; YANG DEXI 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
专利号:CN-108421514-A 优先权日:2017-06-29 标题:A reaction kettle for one-pot synthesis of sulbenicillin sodium and preferential crystallization
专利号:US-2005053642-A1 优先权日:2000-08-23 标题:Biocompatible materials 发明人:ULBRICHT MATHIAS; THOM VOLKMAR; JANKOVA KATJA; ALTANKOV GEORGE; JONSSON GUNNAR 摘要:The present invention teaches a novel approach of creating biocmpatible surfaces, said surfaces being capable of functionally interact with biological material. SAid biocompatible surfaces comrise at least two comonents, such as a hydrophobic substratum and a macromolecule of hydrophilic nature, which, in a cooperativity, form together the novel biocoompatible surfaces. The novel approach is ased on contacting said hydrophobic substratum with a laterally patterned monomolecular layer of said hydrophilic and flexible macromolecules, exhibiting a pronounced excluded volume. The htus formed two component surface is, in respect to polarity and morphology, a molecularly heterogeneous surface. Structural features of said macromolecular monolayer (as e.g. the layer thickness or its lateral density) are determined by: i) the structural features of the layer forming macromolecules (as e.g. their MW or their molecular architecture) and ii) the method of creating said monomolecular layer (as e.g. by physi- or chemisorbing, or by chemically binding said macromolecules). The structural features of the layer forming macromolecules(s) is in turn determined by synthesis. AMount and conformation and thus also biological activity of biological material (as e.g. polypeptides) which contact the novel biocompatible surface, is determined and maintained by the cooperative action of the underlying hydrophobic substratum and the macromolecular layer. In this way it becomes possible to maintain and control biological interactions between said contacted polypeptides and other biological compounds as e.g. cells, antibodies and the like. Consequently, the present invention aims to reduce and/or eliminate the deactivation and/or denaturation associated with the contacting of polypeptides and/or other biological material to a hydrophobic substratum surface.
1: Ripa S, Mignini F, Patrizi I, Ferrante L, Prenna M, Falcioni E. Sulbenicillin: pharmacokinetics and penetration into bronchial secretion in elderly patients. Chemioterapia. 1987 Aug;6(4):277-81. doi: 10.1002/chem.201405058. Epub 2014 Nov 3. 6: Hakamata M, Hozawa J, Saito H, Fukuoka K, Yamagami M, Usami S. [Evaluation of clinical efficacy of sulbenicillin following surgery of malignant maxillary tumors. Transport of sulbenicillin to the exudates from the surgical wound of the maxilla and its therapeutic effects]. Jpn J Antibiot. 1982 May;35(5):1254-60. Japanese. Japanese. 9: Macchioni PL, Del Din G, Filippi G, Baricchi R, Bertani A, Portioli I. Clinical assessment of sulbenicillin in acute respiratory tract infection. Drugs Exp Clin Res. 1985;11(12):879-83. Review. Italian.
合成参考文献
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