CAS: 51025-85-5; Arbekacin

该化合物是一种主要用于治疗格外阴性细菌所造成感染的抗生素,特别是在其他抗生素可能因抗药性而无效的情况下,其结构上与卡纳米素有关,并展示了广泛的抗菌活动.Arbekacin通过抑制细菌蛋白综合合成,导致细胞死亡.其机制与30S的血清亚细胞有约束力,干扰了翻译过程.该物质通常通过静脉注射进行,并因其对多种抗药性细菌的某些菌株具有效力而闻名.在制药学学上,阿贝卡辛的特点是其分布在人体组织中,其半衰期相对较长,允许较少的剂量.然而,与其他微异蛋白表面一样,它也带有肾中毒和食毒的风险,因此在治疗过程中必须仔细监测肾功能.

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MSDS等安全信息

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      专利信息


      专利号:US-9353057-B2
      优先权日:2003-12-30
      标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
      发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
      权利人:XENOPORT INC
      摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

      专利号:US-2015158809-A9
      优先权日:2013-02-26
      标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
      发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
      权利人:XENOPORT INC
      摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

      专利号:US-10472663-B2
      优先权日:2015-01-21
      标 题:Procedure for the rapid determination of bacterial susceptibility to antibiotics that inhibit protein synthesis
      发明人:FERNÃ?NDEZ GARCÃ?A JOSÉ LUIS; GOSÃ?LVEZ BERENGUER JAIME; BOU ARÉVALO GERMÃ?N; TAMAYO NOVAS MARIA; SANTISO BRANDARIZ REBECA; OTERO FARIÑA FÃ?TIMA MARÃ?A
      权利人:ABM TECH LLC
      摘要:The present invention relates to a method for the rapid evaluation of bacterial susceptibility or non-susceptibility of bacteria to antibiotics that inhibit protein synthesis. The rationale is to identify bacterial responses that depend or are influenced by protein synthesis. If this response is prevented or reduced by the antibiotic that inhibits the protein synthesis, the bacteria are susceptible to this antibiotic. Otherwise, if the response keeps similar despite the incubation with the antibiotic, the bacteria are not susceptible or resistant to this antibiotic. These responses could be determined at the DNA lev-el, cell wall level, morphological level or any other experimental approach, including metabolic, bio-chemical, physiological or genetic processes.

      专利号:US-9968710-B2
      优先权日:2007-07-23
      标 题:Pharmaceutical composition, substrate comprising a pharmaceutical composition, and use of a pharmaceutical composition
      发明人:DUEWELHENKE NICOLE
      权利人:BIOMET DEUTSCHLAND GMBH
      摘要:Use of a pharmaceutical composition for the local treatment or prevention of a tissue infection at an infection site, the pharmaceutical composition comprising at least two different antibiotics of group A or pharmaceutically acceptable derivatives thereof, or an antibiotic of group A and at least one antibiotic of group B or pharmaceutically acceptable derivatives thereof. Group A comprises primarily intracellular active antibiotics working as inhibitor of bacterial RNA polymerase; as inhibitor of gyrase; or as inhibitor of bacterial protein synthesis. Group B comprises primarily extracellular active antibiotics working as inhibitor of bacterial cell wall synthesis; or inhibitor of bacterial protein synthesis; or by direct destabilization or rupture of the bacterial cell wall.

      专利号:WO-2009094569-A2
      优先权日:2008-01-25
      标 题:Method for the enzymatic kinetic resolution of acyloxyalkyl thiocarbonates used for the synthesis of acyloxyalkyl carbamates

      专利号:US-2005222431-A1
      优先权日:2003-12-30
      标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof

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      主要参考文献


      1: Hwang JH, Lee JH, Kim JS, Hwang JH, Lee CS. Arbekacin as an Alternative Drug to Teicoplanin for the Treatment of MRSA Infection. Yonsei Med J. 2016 Jul;57(4):1047-8. doi: 10.3349/ymj.2016.57.4.1047.
      2: Lee JH, Lee CS. Clinical Usefulness of Arbekacin. Infect Chemother. 2016 Mar;48(1):1-11. doi: 10.3947/ic.2016.48.1.1. Epub 2016 Mar 31. Review.
      3: Miura K, Nakagawa M, Takahashi H, Uchino Y, Kodaira H, Iriyama N, Sakagami M, Ohtake S, Kobayashi S, Hojo A, Kurita D, Kobayashi Y, Kusuda M, Hirabayashi Y, Hatta Y, Takei M. Clinical efficacy and safety of arbekacin for high-risk infections in patients with hematological malignancies. Int J Hematol. 2016 Mar;103(3):334-40. doi: 10.1007/s12185-015-1926-6. Epub 2015 Dec 29. doi: 10.3346/jkms.2015.30.6.688. Epub 2015 May 13.

      合成参考文献


      摘要:Kumamoto Y, Tsukamoto T, Ogihara M, Ishibashi K, Hirose T, Matsukawa M, Takahashi S, Kunishima Y, Shigeta S, Yoshida H, Imafuku Y, Ooe H, Nishikawa M, Murai M, Watanabe K, Kobayashi Y, Oka T, Kitamura M, Uchida H, Takano Y, Matsuoka Y, Matsuda S, Sato S, Furuhama T, Fujime M, Fujita K, Kumon H, Monden K, Igari J, Oguri T, Kohno S, Miyazaki Y, Yamaguchi T, Matsumoto K, Izumikawa K, Yamaguchi T, Kashitani F, Mochida C. [Comparative studies on activities of antimicrobial agents against causative organisms isolated from patients with urinary tract infections (1999). III. Secular changes in susceptibility]. Jpn J Antibiot. 2001 Jun;54(6):231–322.
      参考文献:10.1097/00001432-200406000-00011
      摘要:Weisman LE. Coagulase-negative staphylococcal disease: emerging therapies for the neonatal and pediatric patient. Current Opinion in Infectious Diseases. 2004 Jun;17(3):237–41. doi: 10.1097/00001432-200406000-00011.
      参考文献:10.2147/tcrm.2006.2.2.169
      摘要:Shoemaker DM, Simou J, Roland WE. A review of daptomycin for injection (Cubicin) in the treatment of complicated skin and skin structure infections. Therapeutics and Clinical Risk Management. 2006 Apr;2(2):169–74. doi: 10.2147/tcrm.2006.2.2.169.
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