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PYRAZOLINE DERIVATIVES FOR THE TREATMENT OF TURBERCULOSIS

  • US 20100179161A1
  • Filed: 08/16/2006
  • Published: 07/15/2010
  • Est. Priority Date: 08/19/2005
  • Status: Abandoned Application
First Claim
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1. A compound of the formula (I) wherein G1 and G2 are independently selected from C or N and the aromatic ring comprising them is further optionally substituted by one or two C1-6 alkyl groups, Y is O, N or C═

  • O, R1 is H or C1-6 alkyl, R2 is H or C1-6 alkyl;

    C6-10 aryl-C1-6 alkyl-, C6-10 heteroaryl-C1-6 alkyl-, C1-6 alkoxy, C6-10 aryl-C1-6 alkoxy-, C6-10 heteroaryl-C1-6 alkoxy-, or —

    N substituted by one or two C1-4 alkyl groups;

    R3 is H, C1-6 alkyl, C6-10 aryl-C1-6 alkyl-, or C6-10 heteroaryl-C1-6 alkyl-, C1-6 alkoxy, C6-10 aryl-C1-6 alkoxy-, C6-10 heteroaryl-C1-6 alkoxy-, or —

    N substituted by one or two C1-4 alkyl groups;

    R4 is H or C1-6 alkyl, except where Y is O or C═

    O then R4 is absent, R5 is C1-6 alkyl, C5-10 aryl, C5-10 heteroaryl, C5-10 aryl-C1-6 alkyl-, C5-10 heteroaryl-C1-6 alkyl, SO2

    C5-10 aryl or SO2

    C5-10 heteroaryl, C═

    O—

    C5-10 aryl or C═

    O—

    C5-10 heteroaryl, and when Y is C═

    O then additionally —

    NH—

    C5-10 aryl or —

    NH—

    C5-10 heteroaryl, wherein heteroaryl comprises 1-3 heteroatoms independently selected from N,O, or S and wherein each aryl or heteroaryl group is optionally substituted by 1-3 groups independently selected from C1-6 alkyl, C1-6 alkoxy, difluoromethyl, trifluoromethyl, difluoromethoxy, trifluoromethoxy, halogen, hydroxy, NO2, amino, di-C1-6 alkylamino, phenyl or CN, or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof.

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