CAS: 252260-02-9; Posizolid

该化合物是一种合成的氧化氮素抗生素,因其在治疗包括多抗药菌在内的抗药性细菌引起的感染方面的潜在用途而受到调查调查,它展示了类似于直肠菌,抑制细菌蛋白合成,与50S核子细胞结合的抗菌素的机制,Posizolid的特征是其针对各种病原体的广泛频谱活动,包括抗血压球和肺炎;其化学结构包括一种双环氧氮素核心,有助于其抗菌特性;Posolid在临床前期和临床研究中表现出希望,展示了优美的药性皮肤学和较弱的培养抗药力的倾向,此外,还对其安全特征进行了评估,研究显示一种可耐性的侧效果简介;然而,就最新数据而言,必须指出,必须进行进一步研究和临床试验,以充分确立其广泛临床使用的效率和安全性.

结构式图片

欧盟法规

ECHA物质C&L通报

合成工艺路线路线简述

    海关参考信息

    专利信息


    专利号:US-10443047-B2
    优先权日:2014-05-01
    标题 :Increasing cellular lipid production by increasing the activity of diacylglycerol acyltransferase and decreasing the activity of triacylglycerol lipase
    发明人:TSAKRAKLIDES VASILIKI; BREVNOVA ELENA E
    权利人:NOVOGY INC
    摘要:Disclosed are methods and compositions for increasing the triacylglycerol content of a cell by up-regulating diacylglycerol acyltransferase and down-regulating triacylglycerol lipase. In some embodiments, a DGA1 protein is expressed and a native TGL3 gene is knocked out, thereby increasing the synthesis of triacylglycerol and decreasing its consumption, respectively.

    专利号:US-2023364251-A1
    优先权日:2020-08-06
    标 题:Methods for the synthesis of protein-drug conjugates
    发明人:BORCHARDT ALLEN; HUGHES ROBERT MICHAEL
    权利人:CIDARA THERAPEUTICS INC
    摘要:The present invention relates to intermediates and methods for synthesizing protein-drug conjugates that can be used for the treatment of diseases and related conditions.

    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-2024207302-A1
    优先权日:2021-04-01
    标 题 :Antiviral compounds, methods for the manufacturing of compounds, antiviral pharmaceutical composition, use of the compounds and method for the oral treatment of coronavirus infection and related diseases thereof
    发明人:CALIXTO JOãO BATISTA; RABI NALLAR JAIME ALBERTO; LOPES E SOUZA THIAGO MORENO
    权利人:CALIXTO JOAO BATISTA; RABI NALLAR JAIME ALBERTO; LOPES E SOUZA THIAGO MORENO
    摘要:The present invention relates to antiviral compounds selected from cytokinins, their nucleosides and nucleotide analogs, and their prodrugs as inhibitors of viral RNA synthesis, or their salts, solvates, derivatives, or even combinations of aforementioned compounds, for prophylactic treatment, curative (therapeutic) or mitigative coronavirus infection, represented by human and veterinary coronavirus, SARS-COV-2 and MHIV, and for the treatment of individuals potentially exposed to COVID-19. The present invention also comprises the methods for the manufacturing of such compounds, the antiviral pharmaceutical composition containing the compounds of the invention, as well as the use of the compounds, combinations of compounds, and method for the prophylactic, curative (therapeutic) or mitigative treatment of coronavirus infection, represented by coronavirus, in especial SARS-COV-2 and of patients with COVID-19, individual infected with SARS-COV-2 or potentially exposed to this virus. The antiviral activity of the compounds of this invention against SARS-COV-2 was greatly enhanced by inhibiting the 3′-5′-exonuclease. Synergistic results of the compounds according to the present invention were obtained from the combination with repurposed drugs.

    专利号:TW-202220698-A
    优先权日:2020-08-06
    标题:Methods for the synthesis of protein-drug conjugates

    专利号:EP-4192512-A1
    优先权日:2020-08-06
    标题 :Methods for the synthesis of protein-drug conjugates
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    主要参考文献


    1: Jadhavar PS, Vaja MD, Dhameliya TM, Chakraborti AK. Oxazolidinones as Anti-tubercular Agents: Discovery, Development and Future Perspectives. Curr Med Chem. 2015;22(38):4379-97. doi: 10.4155/fmc.15.128. Epub 2015 Oct 27. doi: 10.1128/AAC.01691-15. doi: 10.1126/scitranslmed.3009500. doi: 10.1183/09031936.00162314. Epub 2014 Nov 27. Review. doi: 10.1128/AAC.00137-14. Epub 2014 May 12.
    7: Werngren J, Wijkander M, Perskvist N, Balasubramanian V, Sambandamurthy VK, Rodrigues C, Hoffner S. In vitro activity of AZD5847 against geographically diverse clinical isolates of Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2014 Jul;58(7):4222-3. doi: 10.1128/AAC.02718-14. Epub 2014 Apr 28.
    8: Zhang M, Sala C, Dhar N, Vocat A, Sambandamurthy VK, Sharma S, Marriner G, Balasubramanian V, Cole ST. In vitro and in vivo activities of three oxazolidinones against nonreplicating Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2014 Jun;58(6):3217-23. doi: 10.1128/AAC.02410-14. Epub 2014 Mar 24.

    合成参考文献


    参考文献:10.1007/s10156-004-0307-5
    摘要:Gemmell CG. Glycopeptide resistance in Staphylococcus aureus: is it a real threat J Infect Chemother. 2004 Apr;10(2):69–75. doi: 10.1007/s10156-004-0307-5.
    参考文献:10.1128/aac.46.8.2662-2664.2002
    摘要:Anderegg TR, Biedenbach DJ, Jones RN. In Vitro Evaluation of AZD2563, a Novel Oxazolidinone, against 603 Recent Staphylococcal Isolates. Antimicrob Agents Chemother. 2002 Aug;46(8):2662–4. doi: 10.1128/aac.46.8.2662-2664.2002.
    摘要:Johnson AP. AZD-2563 AstraZeneca. Curr Opin Investig Drugs. 2002 Jun;3(6):848–52.
    参考文献:10.1016/j.ijantimicag.2003.05.007
    摘要:Anderegg TR, Jones RN. Preliminary susceptibility testing guidelines for AZD2563, a long-acting oxazolidinone. Int J Antimicrob Agents. 2004 Jan;23(1):6–10. doi: 10.1016/j.ijantimicag.2003.05.007.
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