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Sunday, 12 June 2016

TD 1607

STR1
STR1

TD-1607

Phase I
A glycopeptide-cephalosporin heterodimer potentially for the treatment of gram-positive bacterial infection.
CAS No. 827040-07-3
C95 H109 Cl3 N18 O31 S2, 
Molecular Weight, 2169.47
Vancomycin, 29-​[[[2-​[[6-​[[[1-​[[(6R,​7R)​-​7-​[[(2Z)​-​2-​(2-​amino-​5-​chloro-​4-​thiazolyl)​-​2-​(methoxyimino)​acetyl]​amino]​-​2-​carboxy-​8-​oxo-​5-​thia-​1-​azabicyclo[4.2.0]​oct-​2-​en-​3-​yl]​methyl]​pyridinium-​4-​yl]​methyl]​amino]​-​1,​6-​dioxohexyl]​amino]​ethyl]​amino]​methyl]​-​, inner salt
Vancomycin, 29-[[[2-[[6-[[[1-[[(6R,7R)-7-[[(2Z)-(2-amino-5-chloro-4-thiazolyl)(methoxyimino)acetyl]amino]-2-carboxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methyl]pyridinium-4-yl]methyl]amino]-1,6-dioxohexyl]amino]ethyl]amino]methyl]-, inner salt
  • Originator Theravance
  • Developer Theravance Biopharma
  • Class Antibacterials; Cephalosporins; Glycopeptides
  • Mechanism of Action Cell wall inhibitors
    • Phase I Gram-positive infections

    Most Recent Events

    • 21 Apr 2016 Phase I development is ongoing in USA
    • 01 Jul 2014 Theravance completes a phase I trial in Healthy volunteers in in USA (NCT01949103)
    • 02 Jun 2014 Theravance Biopharma is formed as a spin-off of Theravance
    • CompanyTheravance Biopharma Inc.
      DescriptionGlycopeptide cephalosporin heterodimer antibiotic
      Molecular Target 
      Mechanism of Action 
      Therapeutic ModalitySmall molecule: Combination
      Latest Stage of DevelopmentPhase I
      Standard IndicationGram-negative bacterial infection
      Indication DetailsTreat Gram-positive bacterial infections
PATENT
WO 2005005436
https://www.google.com/patents/WO2005005436A2?cl=en29
The present invention provides novel cross-linked glycopeptide - cephalosporin compounds that are useful as antibiotics. The compounds of this invention have a unique chemical structure in which a glycopeptide group is covalently linked to a pyridinium moiety of a cephalosporin group. Among other properties, compounds of this invention have been found to possess surprising and unexpected potency against Gram-positive bacteria including methicillin-resistant Staphylococci aureus (MRSA). Accordingly, in one aspect, the invention provides a compound of formula I:
Figure imgf000004_0001
 
////////Theravance Biopharma, TD 1607, phase 1, glycopeptide-cephalosporin heterodimer ,  gram-positive bacterial infection
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