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Inhibitors of IMPDH enzyme

  • US 5,807,876 A
  • Filed: 04/23/1996
  • Issued: 09/15/1998
  • Est. Priority Date: 04/23/1996
  • Status: Expired due to Term
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3
Assignments
First Claim
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1. A compound of the formula:

  • ##STR50## wherein;

    E is oxygen;

    G and G'"'"' are independently selected from the group consisting of R6 and (CH2)n --Y;

    D is selected from the group consisting of C(O), C(S) and S(O)2 ;

    B is phenylene;

    B'"'"' is phenyl;

    wherein each of B and B'"'"' optionally comprises up to 3 substituents, wherein;

    the first of said substituents, if present, is selected from R1, R2, R4 or R5,the second of said substituents, if present, is selected from R1 or R4, andthe third of said substituents, if present, is R1 ;

    wherein;

    each R1 is independently selected from 1,2-methylenedioxy, 1,2-ethylenedioxy, R6 or (CH2)n --Y;

    wherein n is 0, 1 or 2; and

    Y is selected from halogen, CN, NO2, CF3, OCF3, OH, SR6, S(O) R6, SO2 R6, NH2, NHR6, N(R6)2, NR6 R8, COOH, COOR6 or OR6 ;

    each R2 is independently selected from (C1 -C4)-straight or branched alkyl, or (C2 -C4)-straight or branched alkenyl or alkynyl; and

    each R2 optionally comprises up to 2 substituents, wherein;

    the first of said substituents, if present, is selected from R1, R4 and R5, andthe second of said substituents, if present, is R1 ;

    each R4 is independently selected from OR5, OC(O)R6, OC(O)R5, OC(O)OR6, OC(O)OR5, OC(O)N(R6)2, OP(O)(OR6)2, SR6, SR5, S(O)R6, S(O)R5, SO2 R6, SO2 R5, SO2 N(R6)2, SO2 NR5 R6, SO3 R6, C(O)R5, C(O)OR5, C(O)R6, C(O)OR6, NC(O)C(O)R6, NC(O)C(O)R5, NC(O)C(O)OR6, NC(O)C(O)N(R6)2, C(O)N(R6)2, C(O)N(OR6)R6, C(O)N(OR6)R5, C(NOR6)R6, C(NOR6)R5, N(R6)2, NR6 C(O)R1, NR6 C(O)R6, NR6 C(O)R5, NR6 C(O)OR6, NR6 C(O)OR5, NR6 C(O)N(R6)2, NR6 C(O)NR5 R6, NR6 SO2 R6, NR6 SO2 R5, NR6 SO2 N (R6)2, NR6 SO2 NR5 R6, N(OR6)R6, N(OR6)R5, P(O)(OR6)N(R6)2, and P(O)(OR6)2 ;

    each R5 is a monocyclic or a bicyclic ring system consisting of 5 to 6 members per ring, wherein said ring system optionally comprises up to 4 heteroatoms selected from N, O, or S, and wherein a CH2 adjacent to said N, O or S maybe substituted with C(O); and

    each R5 optionally comprises up to 3 substituents, each of which, if present, is R1 ;

    each R6 is independently selected from H, (C1-C4)-straight or branched alkyl, or (C2-C4)-straight or branched alkenyl; and

    each R6 optionally substituted with R7;

    R7 is a monocyclic or a bicyclic ring system consisting of 5 to 6 members per ring, wherein said ring system optionally comprises up to 4 heteroatoms selected from N, O, or S, and wherein a CH2 adjacent to said N, O or S maybe substituted with C(O); and

    each R7 optionally comprises up to 2 substituents independently chosen from H, (C1 -C4)-straight or branched alkyl, or (C2 -C4) straight or branched alkenyl, 1,2-methylenedioxy, 1,2-ethylenedioxy, or (CH2)n --Z;

    wherein n is 0, 1 or 2; and

    wherein if B is unsubstituted phenyl and all of said substituents present are on B'"'"' are R1, then at least one of said R1 substituents is not chloro, bromo or iodo; and

    wherein B and B'"'"' are not simultaneously unsubstituted phenyl.

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