CAS: 3485-14-1; (2S,5R,6R)-6-(1-Aminocyclohexanecarboxamido)-3,3-Dimethyl-7-Oxo-4-Thia-1-Azabicyclo[3.2.0]Heptane-2-Carboxylic Acid

该化合物是一种源自6-氨基皮革酸的半合成二硝基苯丙胺抗生素. 它展示了抗克丁阳性和某些克丁阴性细菌的广谱性活动,与早期的青霉素相比,它更加稳定地防止乙酯. 它的化学结构以环己二烯基侧链为特征,有助于改善酸稳定性,从而改善口服生物利用率. 丙丙烯主要用于治疗易感染生物造成的呼吸道,尿道和软组织感染. 它的药理基因特征包括快速吸收和肾脏排泄,使之适合门诊管理. 化合物抗酶退化和可靠的组织渗透是临床应用的关键优势.

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      专利信息


      专利号:US-8017776-B2
      优先权日:2003-07-15
      标题 :Methods for synthesis of acyloxyalkyl compounds
      发明人:BHAT LAXMINARAYAN; GALLOP MARK A
      权利人:XENOPORT INC
      摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.

      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-8143437-B2
      优先权日:2002-02-19
      标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
      发明人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X
      权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC
      摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.

      专利号:EP-0024372-A1
      优先权日:1979-08-03
      标题:Derivatives of clavulanic acid, their preparation and pharmaceutical compositions containing them
      发明人:DENERLEY PAUL MILLINGTON; EGLINGTON ALFRED JOHN; HARBRIDGE JOHN BARRY
      权利人:BEECHAM GROUP PLC
      摘要:The compounds of the formula (II):n and salts and esters thereof wherein the hydroxyl group occupies position 2 or 4 R 1 and R 2 may be the same or different and represent hydrogen, halogen, hydroxy, lower alkyl, cyclopentyl, cyclohexyl, lower alkoxy or R, and R 2 when an adjacent carbon atoms may together represent a 1,4-buta-1,3-dienylene group or a polymethylene group containing from 3 to 5 carbon atoms; have been found to be β-lactam antibiotics and synergists with penicillins and cephalosporins. Their preparation and use is described. The synthesis of intermediates useful in their preparation is also described.

      专利号:WO-9925385-A1
      优先权日:1997-11-17
      标 题:A method of increasing nucleic acid synthesis with ultrasound
      发明人:UNGER EVAN C; MCCREERY THOMAS; SADEWASSER DAVID
      权利人:IMARX PHARMACEUTICAL CORP
      摘要:The present invention is directed to a method of increasing nucleic acid synthesis in a cell comprising administering to the cell a therapeutically effective amount of ultrasound for a therapeutically effective time such that said administration of said ultrasound results in said increased nucleic acid synthesis. The nucleic acid sequence may comprise an endogenous sequence or an exogenous sequence.

      专利号:US-2005010262-A1
      优先权日:2002-02-01
      标题 :Modulation of the pain circuitry to affect chronic pain
      发明人:REZAI ALI; SHARAN ASHWINI
      摘要:The present invention relates to methods of affecting chronic pain by electrically and/or chemically stimulating target sites of the pain circuitry associated with chronic pain. Such target sites include cerebral target sites, including limbic structures, associated with the emotional and suffering components of chronic pain, as well as deep brain target sites associated with the affective and sensory components of chronic pain. Also provided is a method of affecting chronic pain by stimulating a target site of the pain circuitry associated with chronic pain to stimulate the synthesis or release of endogenous opioids.

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      主要参考文献


      1: Scheld WM, Sydnor A Jr, Farr B, Gratz JC, Gwaltney JM Jr. Comparison of cyclacillin and amoxicillin for therapy for acute maxillary sinusitis. Antimicrob Agents Chemother. 1986 Sep;30(3):350-3.
      2: Hooton TM, Running K, Stamm WE. Single-dose therapy for cystitis in women. A comparison of trimethoprim-sulfamethoxazole, amoxicillin, and cyclacillin. JAMA. 1985 Jan 18;253(3):387-90.
      6: McLinn SE, Serlin S. Cyclacillin versus amoxicillin as treatment for acute otitis media. Pediatrics. 1983 Feb;71(2):196-9.

      合成参考文献


      摘要:Chemotherapy, 22(154), 1976 []
      摘要:Tested as SID 103770339 in AID 781325:
      参考文献:10.1007/s192-002-8352-0
      摘要:Ribeiro RM, Rossi P, Pacetta AM, Haddad JM, Pinotti JA. Therapy of uncomplicated urinary tract infections. Int Urogynecol J Pelvic Floor Dysfunct. 2002;13(3):190–4. doi: 10.1007/s192-002-8352-0.
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