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Pyrazole derivative

  • US 20010011090A1
  • Filed: 02/02/2001
  • Published: 08/02/2001
  • Est. Priority Date: 10/13/1997
  • Status: Active Grant
First Claim
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1. A pyrazole derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof (in the formula, each symbol has the following meaning;

  • D;

    pyrazolyl which may have 1 to 3 substituents selected from the group consisting of —

    Alk, —

    lower alkenyl, —

    lower alkynyl, —

    halogeno—

    lower alkyl, —

    Alk—

    cycloalkyl, —

    Alk—

    O—

    Alk, —

    cycloalkyl, —

    O—

    Alk, —

    COOH, —

    COO—

    Alk and —

    Hal, n;

    0 or 1, B;

    phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X;



    NR—

    CR2R3

    , —

    CR2R3

    NR1

    , —

    NR1

    SO2

    , —

    SO2

    N1

    or —

    CR4

    CR5

    , R1;



    H, —

    OH, —

    Alk, —

    O—

    Alk or —

    CO—

    Alk, R2 and R3;

    the same or different from each other and each represents —

    H or —

    Alk, or R2 and R3 together form ═

    O or ═

    S, R4 and R5;

    the same or different from each other and each represents —

    H, —

    Hal, —

    halogeno—

    lower alkyl or —

    Alk, and A;

    benzene ring which may have one or more substituents;

    mono-, di- or tricyclic fused heteroaryl which may have one or more substituents;

    cycloalkyl which may have one or more substituents;

    a nitrogen-containing, saturated ring group which may have one or more substituents;

    lower alkenyl which may have one or more substituents;

    lower alkynyl which may have one or more substituents;

    or Alk which may have one or more substituents, or A and X may together form a group represented by a formula (wherein A2 is a nitrogen-containing hetero ring selected from the group consisting of 1-pyrrolidinyl, pyrazolidinyl, piperidino, piperazinyl, morpholino, 3,4-dihydro-2H-1, 4-benzoxazin-4-yl and indolinyl, wherein said hetero ring may have one or more substituents), with the proviso that (1) when D is 3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl, n is 0, B is 1,4-phenylene and X is NHCO, A is a group other than 4-methyl-1,2, 3-thiadiazol-5-yl, (2) when D is 1-methyl-5-trifluoromethyl-1H-pyrazol-3-yl, n is 0, B is thiophene-2,5-diyl and X is CONH, A is a group other than 4-chlorophenyl, (3) when D is 1-methyl-3-trifluoromethyl-1H-pyrazol-5-yl, n is 0, B is thiophene-2,5-diyl and X is CONH, A is a group other than benzyl, (4) when D is 4-ethoxycarbonyl-5-trifluoromethyl-1H-pyrazol-1-yl, n is 0, B is 1,4-phenylene and Y is NHCO, A is a group other than trichlorovinyl, (5) when D is 1H-pyrazol-1-yl, n is 0, B is 1,4-phenylene and Y is NHCO, A is a group other than 2-ethoxyvinyl, and (6) when n is 1, D is 1H-pyrazol-5-yl substituted with at least one trifluoromethyl group or 1H-pyrazol-1-yl substituted with at least one trifluoromethyl group).

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