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Title:
LINKED PURINE PTERIN HPPK INHIBITORS USEFUL AS ANTIBACTERIAL AGENTS
Document Type and Number:
WIPO Patent Application WO/2011/159471
Kind Code:
A3
Abstract:
The disclosure provides linked purine pterin compounds and analogues thereof that are novel HPPK inhibitors. The HPPK inhibitors described herein are compounds and the pharmaceutically acceptable salts thereof of general Formula I: (I). The variables, e.g. A1 to A3, R1 to R4, L1, L2, B1, and B2 are described herein. Compounds and salts of Formula I bind to HPPK with high affinity and specificity. Pharmaceutical compositions containing an HPPK inhibitor of Formula I and methods of treating a bacterial infection in a patient by providing one or more HPPK inhibitors of Formula I to the patient are also provided. Processes and intermediates useful for preparing compounds of Formula I are also provided. Methods of using the disclosed compounds to guide the development of additional novel anti-bacterial agents are also provided.

Inventors:
SHI GENBIN (US)
SHAW GARY X (US)
JI XINHUA (US)
Application Number:
PCT/US2011/038744
Publication Date:
April 12, 2012
Filing Date:
June 01, 2011
Export Citation:
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Assignee:
US HEALTH (US)
SHI GENBIN (US)
SHAW GARY X (US)
JI XINHUA (US)
International Classes:
C07H19/16; A61K31/7076; A61P31/00; C07D405/14; C07D475/04; C07H19/167; C07H21/02; G16B15/30
Foreign References:
EP0884317B12005-05-18
JPH0656669A1994-03-01
Other References:
HENNIG, M. ET AL.: "The Structure and Function of the 6-Hydroxymethyl-7,8-dihydropterin Pyrophos phokinase from Haemophilus influenzae", JOURNAL OF MOLECULAR BIOLOGY, vol. 287, 1999, pages 211 - 219
BLASZCZYK, J. ET AL.: "Catalytic Center Assembly of HPPK as Revealed by the Crystal Structure of a Ternary Complex at 1.25A Resolution", STRUCTURE, vol. 8, October 2000 (2000-10-01), pages 1049 - 1058, XP055085117, DOI: doi:10.1016/S0969-2126(00)00502-5
Attorney, Agent or Firm:
MAXWELL, Leslie-Anne (20 Church Street 22nd Floo, Hartford Connecticut, US)
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