TREA

Thiazolyl-benzimidazoles

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Information

  • Patent Application
  • 20070203210
  • Publication Number
    20070203210
  • Date Filed
    February 07, 2007
    18 years ago
  • Date Published
    August 30, 2007
    17 years ago
Information
Abstract
The invention is directed to compounds of formula (1)
Description
Claims
  • 1. A compound of formula (1)
  • 2. The compound of claim 1 wherein R2 is optionally substituted aryl.
  • 3. The compound of claim 2 wherein R1 is —C(O)R5.
  • 4. The compound of claim 3 wherein R5 is —OH.
  • 5. The compound of claim 1 wherein R2 is optionally substituted heteroaryl.
  • 6. The compound of claim 5 wherein R1 is C(O)R5 and R5 is —OH.
  • 7. The compound of claim 4 wherein R2 is optionally substituted phenyl.
  • 8. The compound of claim 7 wherein R2 is phenyl substituted with at least one member selected from the group consisting of hydroxyl and halogen.
  • 9. The compound of claim 8 wherein R2 is phenyl substituted with halogen.
  • 10. The compound of claim 9 wherein R2 is phenyl substituted in the 3-position with halogen.
  • 11. The compound of claim 3 wherein R5 is —NR6R7.
  • 12. The compound of claim 11 wherein R6 and R7 are independently selected from the group consisting of hydrogen, lower alkyl, and optionally substituted aryl.
  • 13. The compound of claim 1 wherein n is 1 or 2 and Q2 is independently selected from the group consisting of halogen, lower alkoxy, lower alkoxy-loweralkyleneoxy, and lower alkyl.
  • 14. The compound of claim 2 wherein R1 is heterocyclyl.
  • 15. The compound of claim 14, wherein said heterocyclyl group comprises a nitrogen atom.
  • 16. A compound of claim 4 selected from the group consisting of:
  • 17. A compound of claim 11 selected from the group consisting of:
  • 18. A compound of claim 12 which is 5,6-Dimethoxy-1-[4-phenyl-5-(1H-tetrazol-5-yl)-thiazol-2-yl]-1H-benzoimidazole.
  • 19. A composition comprising a compound of claim 1 and one or more members selected from the group consisting of pharmaceutically acceptable carriers and adjuvants.
  • 20. A method for treating a subject afflicted with a disease or condition that responds to modulation of PLK1 activity, comprising administering to said subject an amount of a compound of claim 1 effective to modulate the activity of PLK1 activity in said subject, wherein said modulation ameliorates said disease or condition.
  • 21. A method for treating a subject afflicted with a disease or condition that responds to modulation of PLK1 activity, comprising administering to said subject an amount of a composition of claim 15 effective to modulate the activity of PLK1 activity in said subject, wherein said modulation ameliorates said disease or condition.
  • 22. A method for preparing a compound according to claim 1 comprising the steps of: reacting a compound of formula (II)
  • 23. The method of claim 18, wherein X is a member selected from the group consisting of Cl, Br, I, and O-triflate.
Provisional Applications (1)
Number Date Country
60776964 Feb 2006 US