CAS: 113359-04-9; Cefozopran

2-(5-氨基-1,2,4-噻二唑-3-基)-2(Z)-甲氧基亚胺基乙酸 S－巯基苯并噻唑酯,1-[[(6R,7R)-7-氨基-2-羧基-8-氧代-5-硫杂-1-氮杂二环[4.2.0]辛-2-烯-3-基]甲基]咪唑并[1,2-B]哒嗪碘化物置于三正丁胺体系中,用 四氢呋喃,水 用作溶剂,化学反应 15.0H,以95%的收率获得头孢唑兰
参考文献:头孢菌素类抗生素头孢唑仑游离碱的制备和分离工艺改进
标题:头孢菌素类抗生素头孢唑仑游离碱的制备和分离工艺改进
摘要:描述了头孢菌素抗生素头孢唑仑的有效合成.本方法不涉及用于分离的色谱纯化,并且是成本有效的并且适合大规模合成.
Doi:10.1021/op900128Z

专利信息

专利号:WO-2012095438-A1
优先权日:2011-01-12
标 题 :Particles and suspensions of cephalosporin antibiotics
发明人：NIEDERMANN HANS PETER; BOTHE HEIKO
权利人:INTERVET INT BV; NIEDERMANN HANS PETER; BOTHE HEIKO
摘要:Disclosed is a method of making particles of a cephalosporin antibiotic, particularly cefquinome, wherein use is made of diafiltration. The diafiltration can be with anti- solvent, in which case a precipitate is obtained of particles as such. The diafiltration can also be with a pharmaceutically acceptable suspension medium. In that case several process steps of isolating, drying, transporting of particles can be avoided, because the suspension resulting from the synthesis of the particles is directly turned into a final drug product formulation.

专利号:US-9066864-B2
优先权日:2011-01-12
标 题:Use of liquid medium exchange by cross flow filtration in the preparation of drug suspensions
发明人：NIEDERMANN HANS PETER; BOTHE HEIKO
权利人:NIEDERMANN HANS PETER; BOTHE HEIKO; INTERVET INC
摘要:Disclosed is a method of making particles of a drug wherein use is made of diafiltration. The diafiltration can be with anti-solvent, in which case a precipitate is obtained of particles as such. The diafiltration can also be with a pharmaceutically acceptable suspension medium. In that case several process steps of isolating, drying, transporting of particles can be avoided, because the suspension resulting from the synthesis of the particles is directly turned into a final drug product formulation.

专利号:US-2009111737-A1
优先权日:1999-05-24
标题:Novel antibacterial agents
发明人：CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES
权利人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES
摘要:This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands hasn a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.

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-11135200-B2
优先权日:2014-12-20
标题:Antimicrobial drug synthesis and therapeutic compositions
发明人：GREGG JOHN MALCOLM HALL
权利人:GREGG JOHN MALCOLM HALL
摘要:This invention relates to the medical use of an antimicrobial agent, racemic Ornidazole, its (R) and (S) enantiomers, or pharmaceutically acceptable salts or esters thereof, and to methods of treatment which involve treating a subject with Ornidazole. The racemic (rac)-ornidazole, its enantiomers, or pharmaceutically acceptable salts or esters thereof, may be used in combination with other actives. The invention also relates to pharmaceutical formulations and compositions comprising (rac)-ornidazole, (R)-ornidazole, (S)-ornidazole, or pharmaceutically acceptable salts or esters thereof, and/or other actives as well as methods to stereoselectively manufacture the enantiomers.

专利号:RU-2007407-C1
优先权日:1987-12-04
标 题:METHOD OF SYNTHESIS OF 7 - β - [(Z) - 2 - (5 - AMINO - 1,2,4 - THIADIAZOLE - 3 - YL) - 2 - METHOXYIMINOACETAMIDO1 - 3 - [1 - IMIDAZO - (1,2 - B) - PYRIDEZINE]METHYL - 3 - CEPHEME - 4 - CARBOXYLATE HYDROCHLORIDE HYDRATE CRYSTALS OR ITS SOLVATES