环丙沙星置于盐酸体系中,用 1,4-二氧六环,二氯甲烷 作为反应溶剂,化学反应 1.0H,以95%的收率获得产物环丙沙星盐酸盐 参考文献: Antibiotic Resistance Breakers[fr] Agents De Rupture De Résistance Aux Antibiotiques 标题: Antibiotic Resistance Breakers[fr] Agents De Rupture De Résistance Aux Antibiotiques 摘要:该发明涉及公式(a1)的抗生素化合物及其药学上可接受的盐,溶剂化合物,互变异构体和它们的组合,其中x和l是可选的连接物,Ra或r1中的一个包括ar1,其中ar1是一种抗生素耐药性破坏基团,包括可选择取代的c6-10芳基,C7-13芳基烷基,C5-10杂芳基,C6-13杂芳基烷基,C5-10杂环烷基,C6-13杂环烷基,C3-10碳环烷基,C4-13碳环烷基,-C(=nr')-Nr'R''或-ch2-Ch=ch2基团;在将该化合物用于细菌感染后,该基团减少或预防外流.该发明还公开了包括公式(a1)化合物的药物组合物以及将这些化合物用作药物的用途,特别是用于治疗细菌感染,如耐药性细菌感染.
专利号:US-8557979-B2 优先权日:2004-06-10 标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation 发明人:CHOI WOO-BAEG; KOWALIK EWA 权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC 摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.
专利号:US-10933051-B2 优先权日:2017-06-09 标 题 :Carbapenem compounds and compositions for the treatment of bacterial infections 发明人:CHOI WOO-BAEG; TOMIOKA TAKASHI; JOO HYUNG-YEUL; TRUONG PHONG; MIN BRIAN 权利人:FOB SYNTHESIS INC 摘要:The present invention provides carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections, including drug resistant or multiple-drug resistant bacterial infections, and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.
专利号:WO-2012127505-A3 优先权日:2011-03-21 标题 :Improved process for the preparation of ciprofloxacin and its acid addition salts 发明人:DAVULURI RAMAMOHAN RAO; PONNAIAH RAVI; BAWANE SUNIL; PATHY ASHOK KUMAR; MALI SUNIL 权利人:DAVULURI RAMAMOHAN RAO 摘要:An improved process for the synthesis of 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinoline carboxylic acid (Ciprofloxacin) or and its acid addition salts preferablyhydrochloride salt with high yield and high purity, the process comprising of reacting 6-fluoro-7-chloro-1-cyclopropyl-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid with piperazine in presence of a catalyst in an organic solvent.
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-11993606-B2 优先权日:2015-10-16 标题:Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof 发明人:MOHAMED MOHAMED-ESLAM F; OTHMAN AHMED A; PANGAN AILEEN L; SONG IN-HO; KLÜNDER BEN; VOSS JEFFREY W; PADLEY ROBERT J; CAMP HEIDI S 权利人:ABBVIE INC 摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and various spondyloarthritic conditions, including types of axial spondyloarthritis (axSpA)), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating active non-radiographic axSpA (nr-axSpA) and methods for treating active ankylosing spondylitis (AS).
专利号:US-11976077-B2 优先权日:2015-10-16 标 题 :Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-α]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms therof 发明人:PANGAN AILEEN L; TEIXEIRA HENRIQUE D; MOHAMED MOHAMED-ESLAM F; OTHMAN AHMED A; KLÜNDER BEN; VOSS JEFFREY W; PADLEY ROBERT J; CAMP HEIDI S 权利人:ABBVIE INC 摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and atopic dermatitis), kits, methods of synthesis, and products-by-process.
摘要:Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental Animals, Research Reports., 11(411), 1985 摘要:Iyakuhin Kenkyu. Study of Medical Supplies., 19(735), 1988 参考文献:10.1007/s00423-008-0345-z 摘要:Banasiewicz T, Meissner W, Pyda P, Wierzbicki T, Głyda M, Musiał M, Smoliński S, Iwanik K, Drews M. Partial thyroidectomy under local anaesthesia-the analysis of 49 subsequent cases. Langenbecks Arch Surg. 2008 Sep;393(5):715–9. doi: 10.1007/s00423-008-0345-z.