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Inhibitors of microsomal triglyceride transfer protein and method

  • US 5,885,983 A
  • Filed: 04/23/1997
  • Issued: 03/23/1999
  • Est. Priority Date: 05/10/1996
  • Status: Expired due to Term
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Assignment
First Claim
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1. A compound which has the structure ##STR296## where Q is ##STR297## R1 is a fluorenyl-type group of the structure ##STR298## R1 is an indenyl-type group of the structure ##STR299## Z1 and Z2 are the same or different and are independently a bond, O, S, ##STR300## with the proviso that with respect to B, at least one of Z1 and Z2 will be other than a bond;

  • R11 is alkylene, alkenylene or alkynylene of up to 10 carbon atoms;

    arylene or mixed arylene-alkylene;

    R12 is hydrogen, alkyl, alkenyl, aryl, haloalkyl, trihaloalkyl, trihaloalkylalkyl, heteroaryl, heteroarylalkyl, arylalkyl, arylalkenyl, cyclo-alkyl, aryloxy, alkoxy, arylalkoxy or cycloalkyl-alkyl, with the provisos that(1) when R12 is H, aryloxy, alkoxy or arylalkoxy, then Z2 is ##STR301## or a bond and (2) when Z2 is a bond, R12 cannot be heteroaryl or heteroarylalkyl;

    Z is bond, O, S, N-alkyl, N-aryl, or alkylene or alkenylene from 2 to 5 carbon atoms;

    R13, R14, R15, and R16 are independently hydrogen, alkyl, halo, haloalkyl, aryl, cycloalkyl, cyclo-heteroalkyl, alkenyl, alkynyl, hydroxy, alkoxy, nitro, amino, thio, alkylsulfonyl, arylsulfonyl, alkylthio, arylthio, aminocarbonyl, alkylcarbonyloxy, arylcarbonylamino, alkylcarbonylamino, arylalkyl, heteroaryl, heteroarylalkyl or aryloxy;

    R15a and R16a are independently hydrogen, alkyl, halo, haloalkyl, aryl, cycloalkyl, cycloheteroalkyl, alkenyl, alkynyl, alkoxy, alkylsulfonyl, arylsulfonyl, alkylthio, arylthio, aminocarbonyl, alkylcarbonyloxy, arylcarbonylamino, alkylcarbonylamino, arylalkyl, heteroaryl, heteroarylalkyl, or aryloxy;

    R5 is independently alkyl, alkenyl, alkynyl, aryl, alkoxy, aryloxy, arylalkoxy, heteroaryl, arylalkyl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, polycycloalkyl, polycycloalkylalkyl, cycloalkenyl, cycloheteroalkyl, heteroaryloxy, cycloalkenylalkyl, polycycloalkenyl, polycycloalkenylalkyl, heteroarylcarbonyl, amino, alkylamino, arylamino, heteroarylamino, cycloalkyloxy, cycloalkylamino, all optionally substituted through available carbon atoms with 1, 2, 3 or 4 groups selected from hydrogen, halo, alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl, aryl, heteroaryl, arylalkyl, arylcycloalkyl, arylalkenyl, arylalkynyl, aryloxy, aryloxyalkyl, arylalkoxy, arylazo, heteroaryloxo, heteroarylalkyl, heteroarylalkenyl, heteroaryloxy, hydroxy, nitro, cyano, amino, substituted amino, thiol, alkylthio, arylthio, heteroarylthio, arylthioalkyl, alkylcarbonyl, arylcarbonyl, arylaminocarbonyl, alkoxycarbonyl, aminocarbonyl, alkynylaminocarbonyl, alkylaminocarbonyl, alkenylaminocarbonyl, alkylcarbonyloxy, arylcarbonyloxy, alkylcarbonylamino, arylcarbonylamino, arylsulfinyl, arylsulfinylalkyl, arylsulfonyl, alkylsulfonyl, arylsulfonylamino, heteroarylcarbonylamino, heteroarylsulfinyl, heteroarylthio, heteroarylsulfonyl, alkylsulfinyl;

    R6 is hydrogen or C1 -C4 alkyl or C1 -C4 alkenyl;

    all optionally substituted with 1, 2, 3 or 4 groups which may independently be any of the substituents listed in the definition of R5 set out above;

    ##STR302## are the same or different and are independently selected from heteroaryl containing 5- or 6-ring members;

    oran N-oxide ##STR303## thereof;

    a stereoisomer thereof;

    or a pharmaceutically acceptable salt thereof.

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