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Inhibitors of farnesyl-protein transferase

  • US 5,780,488 A
  • Filed: 03/26/1997
  • Issued: 07/14/1998
  • Est. Priority Date: 04/03/1996
  • Status: Expired due to Fees
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Assignment
First Claim
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1. A compound represented by formula I:

  • ##STR8## or a pharmaceutically acceptable salt thereof, wherein;

    R1a, R1b and R2 are independently selected from the group consisting of;

    hydrogen, aryl, heterocyclyl, C3 -C10 cycloalkyl, C2 -C6 alkenyl, C2 -C6 alkynyl, R8 O--, R9 S(O)m --, (R8)2 NC(O)--, R8 C(O)NR8 --, CN, NO2, (R8)2 NC(NR8)--, R8 C(O)--, R8 OC(O)--, N3, --N(R8)2, R9 OC(O)NR8 -- and C1 -C6 alkyl, unsubstituted or substituted by 1-3 groups selected from the group consisting of;

    halo, aryl, heterocyclyl, C3 -C10 cycloalkyl, C2 -C6 alkenyl, C2 -C6 alkynyl, R8 O--, R9 S(O)m --, R8 C(O)NR8 --, CN, (R8)2 NC(NR8)--, R8 C(O)--, R8 OC(O)--, N3, --N(R8)2 and R9 OC(O)NR8 --;

    R3 and R4 are independently selected from the group consisting of;

    H, F, Cl, Br, --NR82, CF3, NO2, R8 O--, R9 S(O)m --, (R8)2 NC(O)--, R8 C(O)NH--, H2 NC(NH)--, R8 C(O)--, R8 OC(O)--, N3, CN, R9 OC(O)NR8 --, C1 -C20 alkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl;

    A3 is selected from;

    --NR5 S(O)m -- or --S(O)m NR5 --, with m equal to 0, 1 or 2, and R5 selected from the group consisting of;

    hydrogen, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl, unsubstituted or substituted C3 -C10 cycloalkyl, and C1 -C6 alkyl, unsubstituted or substituted with 1-3 members selected from the group consisting of;

    unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl, unsubstituted or substituted C3 -C10 cycloalkyl, --N(R8)2, --CF3, --NO2, (R8)O--, (R9)S(O)m --, (R8)C(O)NH--, H2 NC(NH)--, (R8)C(O)--, (R8)OC(O)--, N3, CN and (R9)OC(O)NR8 --;

    R6 and R7 are independently selected from the group consisting of;

    hydrogen, aryl, heterocyclyl, C3 -C10 cycloalkyl, C2 -C6 alkenyl, C2 -C6 alkynyl, C1-6 perfluoroalkyl, F, Cl, Br, R8 O--, R9 S(O)m --, R8 C(O)NR8 --, CN, NO2, (R8)2 NC(NR8)--, R8 C(O)--, R8 OC(O)--, N3, --N(R8)2, R9 OC(O)NR8 -- and C1 -C6 alkyl unsubstituted or substituted by 1-3 groups selected from;

    aryl, heterocyclyl, C3 -C10 cycloalkyl, C2 -C6 alkenyl, C2 -C6 alkynyl, perfluoroalkyl, F, Cl, Br, R8 O--, R9 S(O)m --, R8 C(O)NR8 --, CN, (R8)2 NC(NR8)--, R8 C(O)--, R8 OC(O)--, N3, --N(R8)2 and R9 OC(O)NR8 --;

    each R8 is independently selected from hydrogen, C1 -C6 alkyl, aryl and aralkyl;

    each R9 is independently selected from C1 -C6 alkyl and aryl;

    A1 and A2 are independently selected from the group consisting of;

    a bond, --CH═

    CH--, --C.tbd.C--, --C(O)--, --C(O)NR8 --, --NR8 C(O)--, --O--, --N(R8)--, --S(O)2 N(R8)--, --N(R8)S(O)2 --, and S(O)m ;

    X represents aryl or heteroaryl;

    V is selected from the group consisting of;

    hydrogen, heterocyclyl, aryl, C1 -C20 alkyl wherein from 0 to 4 carbon atoms are replaced with a heteroatom selected from O, S, and N, and C2 -C20 alkenyl, provided that V is not hydrogen if A1 is S(O)m and V is not hydrogen if A1 is a bond, n is 0 and A2 is S(O)m ;

    W represents heterocyclyl;

    each n and p independently represents 0, 1, 2, 3 or 4;

    r is 0 to 5, provided that r is 0 when V is hydrogen, andt is 1.

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