COMPOUNDS DIRECTED AGAINST PILUS BIOGENESIS AND ACTIVITY IN PATHOGENIC BACTERIA; METHODS AND COMPOSITIONS FOR SYNTHESIS THEREOF

WIPO Patent Application WO2001020995

A9

Many Gram-negative pathogens assemble adhesive structures on their surfaces that allow them to colonize host tissues and cause disease. Novel compositions which inhibit or prevent the formation of a pilus chaperone-subunit complex are disclosed. Interfering with the function of the pili chaperone negatively affects the chaperone/usher pathway which is one molecular mechanism by which Gram-negative bacteria assemble adhesive pili structures and thus prevent or inhibit pilus assembly. Also provided are methods for the treatment or prevention of diseases caused by tissue-adhering pilus-forming bacteria by inhibiting the function of pilus chaperones. Also provided are pharmaceutical preparations capable of inhibiting or preventing the formation of a pilus chaperone-subunit complex. Also provided are methods of synthesizing the N-substituted amino acid compounds and compounds useful for the synthesis thereof. In particular, novel fluorinated linker compounds and methods of synthesis are provided. Methods for using the fluorinated linker compounds in methods of solid-phase synthesis of the N-substituted amino acid compounds are also disclosed.

KIHLBERG JAN (SE)
LARSSON ANDREAS (SE)
SVENSSON ANETTE (SE)
FEX TOMAS (SE)
HULTGREN SCOTT J (US)
PINKNER JERRY (US)

PCT/US2000/026177

November 14, 2002

September 22, 2000

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UNIV WASHINGTON (US)
KIHLBERG JAN (SE)
LARSSON ANDREAS (SE)
SVENSSON ANETTE (SE)
FEX TOMAS (SE)
HULTGREN SCOTT J (US)
PINKNER JERRY (US)

A01N37/44; A01N37/46; C07D209/14; C07D311/12; C07D405/12; (IPC1-7): A01N57/00; C07D305/00; C07D309/00; C07D311/00; C07D311/02; C07D311/04; C07D321/00

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