6,8-二氟-1,4-二氢-1-(甲基氨基)-7-(4-甲基-1-哌嗪基)-4-氧代-3-喹啉羧酸置于四甲基氢氧化铵,氨,Sodium Hydroxide体系中,用 乙醇,二氯甲烷,水 用作溶剂,化学反应 5.0H,反应生成马波沙星 参考文献: A Process For A Preparation Of Marbofloxacin And Intermediate Thereof[fr] Procédé D'élaboration De Marbofloxacine,Et Intermédiaire à Cet Effet 标题: A Process For A Preparation Of Marbofloxacin And Intermediate Thereof[fr] Procédé D'élaboration De Marbofloxacine,Et Intermédiaire à Cet Effet 摘要:该发明描述了一种新颖的马伯氟沙星及其中间体的制备方法,包括将化学式(III)的氢氧化铵(nr1R2R3R4,其中r1,R2,R3和r4独立地选自h,烷基,烷基芳基,芳基和/或杂环烷基)与化学式(II)的化合物反应,其中r选自h,烷基,芳基烷基,碱金属阳离子,Nh4阳离子,Nr1R2R3R4阳离子;X为卤素,如氯,溴,氟,哌嗪基,可能被取代或未取代,R'选自h,甲酰基或coo烷基.
专利号:US-2024082118-A1 优先权日:2021-05-19 标 题:Topical compositions and methods of preparing the same 发明人:ABRAMOVICH SAGI; AVIDOR GAL; LANDA BENZION 权利人:LANDA LABS 2012 LTD 摘要:There is disclosed a composition comprising a water-insoluble thermoplastic compound capable of stimulating collagen synthesis (CSSC), the CSSC having a molecular weight of more than 0.6 kDa and being dispersed in a polar carrier as nano-elements having an average diameter of 200 nm or less and a viscosity of 107 mPa·s or less. The nano-elements of CSSC can be capable of stimulating the synthesis of skin proteins and/or enabling the delivery of active agents upon their application to a surface to be treated therewith. Methods for preparing the compositions and uses thereof are also provided.
专利号:US-11332444-B2 优先权日:2018-04-25 标题:Method for the hydrolysis of quinolonecarboxylic esters 发明人:FEY PETER; BERWE MATHIAS; WIRTHS Joerg; WISCHNAT RALF; LONGERICH MARKUS; DIETZEL ANTJE 权利人:BAYER ANIMAL HEALTH GMBH 摘要:Quinolonecarboxylic esters of the general formula (II) are hydrolyzed to quinolonecarboxylic acids of the general formula (I):The method comprises the step A):A) reacting compounds of the formula (II) with a mixture comprising acetic acid, sulfuric acid and waterIn step A), ≥30 to ≤40 mol of acetic acid, ≥0.3 to ≤1 mol of sulfuric acid and ≥0.9 to ≤2.5 mol of water are used per mole of compounds of the formula (II). The method is particularly suitable for the synthesis of the intermediate (I) in the synthesis of pradofloxacin.
专利号:US-8093381-B2 优先权日:2007-05-24 标题:Method of synthesis of fluoroquinolones 发明人:BERTHON-CEDILLE LAURENCE; LEGUERN MARIE-EMMANUELLE; RENAUD GILLES; TOMBRET FRANCIS 权利人:BERTHON-CEDILLE LAURENCE; LEGUERN MARIE-EMMANUELLE; RENAUD GILLES; TOMBRET FRANCIS; BIOCODEX 摘要:The invention relates to a method of preparation of fluoroquinolones of formula (I) from compounds of formula (II): n nin which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and X are as defined in Claim 1.
专利号:US-2025144039-A1 优先权日:2022-07-13 标题:Compositions comprising surface modified globular nano-particles 发明人:ABRAMOVICH SAGI; AVIDOR GAL; LANDA BENZION 权利人:LANDA LABS 2012 LTD 摘要:There are disclosed compositions comprising core-shell nano-elements composed in their core of a water-insoluble thermoplastic compound having a molecular weight of more than 0.6 kDa and in their shell of at least one fatty amine, or a part thereof, the core-shell nano-elements having a viscosity of 107 mPa·s or less and being dispersed in a polar carrier as nano-elements having an average diameter of 200 nm or less. The water-insoluble thermoplastic compound can be capable of stimulating the synthesis of skin proteins and/or enabling the delivery of active agents upon application of the core-shell nano-elements to a surface to be treated therewith. Methods for preparing the composition and uses thereof are also provided.
专利号:US-2009054643-A1 优先权日:2007-05-24 标 题:Novel method of synthesis of fluoroquinolones
专利号:WO-2024013694-A1 优先权日:2022-07-13 标题 :Compositions comprising surface modified globular nano-particles 发明人:ABRAMOVICH SAGI; AVIDOR GAL; LANDA BENZION 权利人:LANDA LABS 2012 LTD 摘要:There are disclosed compositions comprising core-shell nano-elements composed in their core of a water-insoluble thermoplastic compound having a molecular weight of more than 0.6 kDa and in their shell of at least one fatty amine, or a part thereof, the core-shell nano-elements having a viscosity of 107 mPa·s or less and being dispersed in a polar carrier as nano-elements having an average diameter of 200 nm or less. The water-insoluble thermoplastic compound can be capable of stimulating the synthesis of skin proteins and/or enabling the delivery of active agents upon application of the core-shell nano-elements to a surface to be treated therewith. Methods for preparing the composition and uses thereof are also provided.
1: Jerzsele Á, Pásztiné-Gere E. Evaluating synergy between marbofloxacin and gentamicin in Pseudomonas aeruginosa strains isolated from dogs with otitis externa. Acta Microbiol Immunol Hung. 2015 Mar;62(1):45-55. doi: 10.1556/AMicr.62.2015.1.4. doi: 10.1080/00071668.2014.998989. Epub 2015 Jan 29. doi: 10.1186/s12917-015-0604-5. 4: Qu Y, Qiu Z, Cao C, Lu Y, Sun M, Liang C, Zeng Z. Pharmacokinetics/pharmacodynamics of marbofloxacin in a Pasteurella multocida serious murine lung infection model. BMC Vet Res. 2015 Dec 2;11:294. doi: 10.1186/s12917-015-0608-1. 5: Yang F, Yang YR, Wang L, Huang XH, Qiao G, Zeng ZL. Estimating marbofloxacin withdrawal time in broiler chickens using a population physiologically based pharmacokinetics model. J Vet Pharmacol Ther. 2014 Dec;37(6):579-88. doi: 10.1111/jvp.12137.. Epub 2014 Jun 6. doi: 10.1111/jvp.12214. Epub 2015 Feb 18. doi: 10.3389/fmicb.2015.00759. eCollection 2015.