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6-(aryl-amido or aryl-amidomethyl)-naphthalen-2-yloxy-acidic derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)

  • US 6,589,970 B2
  • Filed: 06/13/2002
  • Issued: 07/08/2003
  • Est. Priority Date: 06/20/2001
  • Status: Expired due to Fees
First Claim
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1. A compound of the formula:

  • embedded imageWherein;

    Ar is phenyl, naphthyl, furanyl, benzofuranyl, indolyl, pyrazolyl, oxazolyl, fluorenyl, phenylcycloalkane where the cycloalkane can be cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl and Ar can be optionally substituted by from 1 to 3 groups selected from C1-C6 alkyl, C1-C6 alkoxy, hydroxy, phenyl-(CH2)0-6

    , phenyl-(CH2)0-6O—

    , C3-C6 cycloalkyl, —

    (CH2)—

    C3-C6 cycloalkyl, halogen, C1-C3 perflouroalkyl and C1-C3 perfluoroalkoxy where phenyl can be substituted with from 1 to 3 groups selected from C1-C6 alkyl, C1-C6 alkoxy, phenyl, halogen, trifluoromethyl or trifluoromethoxy;

    R1 is hydrogen, C1-C6 alkyl or phenyl-(CH2)1-6

    where phenyl can be substituted with C1-C6 alkyl, C1-C6 alkoxy, halogen, trifluoromethyl or trifluoromethoxy;

    R2 and R3 are independently hydrogen, C1-C6 alkyl, phenyl-(CH2)0-3

    , halogen and C1-C3 perfluoroalkyl where phenyl can be substitute with C1-C6 alkyl, C1-C6 alkoxy, halogen, trifluoromethyl or trifluoromethoxy. R4 is —

    CHR5CO2H or —

    CH2-tetrazole where R5 is hydrogen or benzyl; and

    n=0 or 1;

    or a pharmaceutically acceptable salt or ester form thereof.

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