Cephalosporin antibiotics
    4.
    发明授权
    Cephalosporin antibiotics 失效
    头孢菌素类抗生素

    公开(公告)号:US6087355A

    公开(公告)日:2000-07-11

    申请号:US730042

    申请日:1996-10-11

    CPC分类号: C07D501/00

    摘要: The present invention includes novel compounds of formula ##STR1## where A, B, D, and E are selected from the group consisting of carbon, nitrogen and sulfur, R.sup.99 is selected from the group consisting of sulfur, SO, SO.sub.2, NH, N-alkyl, oxygen, C.dbd.C (cis or trans), and C.tbd.C, and R.sup.12 is NR.sup.13 R.sup.14, ##STR2## The invention also includes the pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to .beta.-lactam antibiotics and are useful as antibacterial agents. The invention also relates to novel intermediates useful for making the novel compounds of the present invention and to novel methods for producing the novel compounds and intermediate compounds.

    摘要翻译: 本发明包括新的式A化合物,其中A,B,D和E选自碳,氮和硫,R99选自硫,SO,SO 2,NH,N-烷基, 氧,C = C(顺式或反式)和C 3BOND C,R 12为NR 13 R 14。本发明还包括对广谱生物体表现出抗生素活性的药理学上可接受的盐,包括对β-内酰胺抗生素具有抗性的生物体, 作为抗菌剂是有用的。 本发明还涉及可用于制备本发明的新化合物的新型中间体和用于生产新化合物和中间体化合物的新方法。

    Water-soluble prodrugs of chloramphenicol, thiamphenicol, and analogs thereof
    6.
    发明授权
    Water-soluble prodrugs of chloramphenicol, thiamphenicol, and analogs thereof 失效
    氯霉素,甲砜霉素及其类似物的水溶性前药

    公开(公告)号:US08044230B2

    公开(公告)日:2011-10-25

    申请号:US11953972

    申请日:2007-12-11

    申请人: Tomasz W. Glinka

    发明人: Tomasz W. Glinka

    CPC分类号: C07C317/32 C07D233/60

    摘要: The present invention discloses certain novel prodrugs of chloramphenicol or thiamphenicol, or of an analog of either, including prodrugs of pharmaceutically acceptable salts of chloramphenicol or thiamphenicol or of their analogs, including nitrogen-containing esters of both alcohol groups of such compounds. In certain embodiments these novel prodrugs are sufficiently water-soluble to serve the functions needed of a prodrug of chloramphenicol or thiamphenicol or of an analog of either. In one embodiment, a certain subclass of the compounds also possesses the hydrolytic stability needed to maintain the prodrug in solution in the subject's system until appropriate conditions exist when the prodrug can hydrolyze, releasing the active compound in question.

    摘要翻译: 本发明公开了氯霉素或甲砜霉素或其类似物的某些新型前药,包括氯霉素或硫代霉酚或其类似物的药学上可接受的盐的前药,包括这些化合物的两个醇基的含氮酯。 在某些实施方案中,这些新型前药具有足够的水溶性,以满足氯霉素或甲砜霉素或其类似物的前药所需的功能。 在一个实施方案中,化合物的某些亚类还具有将前药保持在受试者系统的溶液中所需的水解稳定性,直到前药可以水解,释放所讨论的活性化合物时才存在适当的条件。

    Cephalosporin antibiotics
    9.
    发明授权
    Cephalosporin antibiotics 失效
    头孢菌素类抗生素

    公开(公告)号:US6030965A

    公开(公告)日:2000-02-29

    申请号:US940508

    申请日:1997-09-30

    CPC分类号: C07D501/00

    摘要: The present invention includes novel compounds of formula where A, B, D, and E are selected from the group consisting of carbon, nitrogen and sulfur, R.sup.99 is selected from the group consisting of sulfur, SO, S0.sub.2, NH, N-alkyl, oxygen, C.dbd.C (cis or trans), and C.tbd.C, and R.sup.12 is NR.sup.13 R.sup.14, ##STR1## The invention also includes the pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to .beta.-lactam antibiotics and are useful as antibacterial agents. The invention also relates to novel intermediates useful for making the novel compounds of the present invention and to novel methods for producing the novel compounds and intermediate compounds.

    摘要翻译: 本发明包括新的式A化合物,其中A,B,D和E选自碳,氮和硫,R99选自硫,SO,SO 2,NH,N-烷基, 氧,C = C(顺式或反式)和C 3BOND C,R 12为NR 13 R 14。本发明还包括对广谱生物体表现出抗生素活性的药理学上可接受的盐,包括对β-内酰胺抗生素具有抗性的生物体, 作为抗菌剂是有用的。 本发明还涉及可用于制备本发明的新化合物的新型中间体和用于生产新化合物和中间体化合物的新方法。

    Aminoglycoside derivatives
    10.
    发明授权
    Aminoglycoside derivatives 有权
    氨基糖苷衍生物

    公开(公告)号:US08906868B2

    公开(公告)日:2014-12-09

    申请号:US13697302

    申请日:2011-05-12

    CPC分类号: C07H15/236

    摘要: The present invention relates to antimicrobial agents. Some embodiments include compounds, compositions, methods of preparation, and methods of treatment using new aminoglycosides and aminoglycoside derivatives.

    摘要翻译: 本发明涉及抗微生物剂。 一些实施方案包括化合物,组合物,制备方法和使用新的氨基糖苷类和氨基糖苷衍生物的治疗方法。