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Heterocyclic compounds

  • US 6,069,159 A
  • Filed: 05/10/1999
  • Issued: 05/30/2000
  • Est. Priority Date: 05/10/1996
  • Status: Expired due to Fees
First Claim
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1. A compound of formula I:

  • ##STR17## W is S or O;

    R8 is selected from the group consisting of hydrogen and C1 -C4 alkyl;

    R10'"'"' is C2 -C5 alkynyl;

    R11'"'"' is aryl or 5 to 6 member heterocyclic ring each of which is optionally substituted with one or more independently selected from the group consisting of halogen, --CN, C1-4 -alkyl, C1-4 -alkoxy, --OCF3, --CF3, --CONH2, --CSNH2 ;

    --OH, --COR6'"'"', CH2 --OH, and --NH2 ;

    G is selected from one of the following azacyclic or azabicyclic ring systems;

    ##STR18## or G is optionally substituted C3 -C8 cycloalkyl wherein the cycloalkyl substituents are selected from R1 and R2 ;

    or optionally substituted C1-6 -alkyl wherein the substitution is --NR6 R7 ;

    R6 and R7 independently are selected from the group consisting of hydrogen and C1-6 -alkyl;

    or R6 and R7 together with the nitrogen atom optionally form a 4- to 6-member ring;

    R1 and R2 independently are selected from the group consisting of hydrogen, C1-15 -alkyl, C2-5 -alkenyl, C2-5 -alkynyl, C1-10 -alkoxy, and C1-5 -alkyl substituted with one or more independently selected from the group consisting of --OH, --COR6'"'"', CH2 --OH, halogen, --NH2, carboxy, ##STR19## and phenyl;

    R9 and R9 '"'"' are each independently selected from the group consisting of hydrogen, halogen, C1-4 -alkoxy, C1-4 -alkyl, --CN, --OCF3, --CONH2 and --CSNH2 ;

    R6'"'"' is hydrogen, C1-6 -alkyl;

    R3 is selected from the group consisting of hydrogen, C1-5 -alkyl, C2-5 -alkenyl and C2-5 -alkynyl;

    n is 0, 1 or 2;

    m is 0, 1 or 2;

    p is 0, 1 or 2;

    q is 1 or 2;

    r is 0, 1 or 2;

    . . is a single or double bond; and

    pharmaceutically acceptable salts and solvates thereof.

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