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Pharmaceutically active compounds

  • US 6,503,908 B1
  • Filed: 10/06/2000
  • Issued: 01/07/2003
  • Est. Priority Date: 10/11/1999
  • Status: Expired due to Fees
First Claim
Patent Images

1. A compound of formula I, embedded imagewhereinR1 and R2 independently represent phenyl (optionally substituted by one or more substituents selected from halo, —

  • CN, —

    CF3, —

    OCF3, C1-4 alkoxy or C1-4 alkyl (which latter two groups are optionally substituted by C1-4 haloalkyl or C1-4 haloalkoxy)) or C1-6 alkyl optionally interrupted by —

    O—

    , —

    S— and

    /or —

    N(R4)— and

    /or optionally substituted and/or terminated by Het2, a N-linked heterocyclic group (selected from piperidinyl and morpholinyl) or phenyl (which latter group is optionally substituted by one or more substituents selected from halo, —

    CN, —

    CF3, —

    OCF3, C1-4 alkoxy or C1-4 alkyl (which latter two groups are optionally substituted by C1-4 haloalkyl or C1-4 haloalkoxy));

    R4 represents H or C1-4 alkyl;

    R3 represents OR5 or N(R6)R7;

    R5 represents C3-6 cycloalkyl, —

    (C1-4 alkylene)-1-piperidinyl, tetrahydrofuranyl, tetrahydropyranyl or C1-6 alkyl, which latter group is optionally substituted and/or terminated by one or two substituents selected from C3-5 cycloalkyl, —

    OR8, —

    N(R6)R7, phenyl, furanyl and pyridinyl, and which C1-6 alkyl group is optionally terminated by a C1-4 haloalkyl group;

    R6 and R7 independently represent, at each occurrence, H, C1-4 alkyl (optionally substituted by C3-5 cycloalkyl or C1-4 alkoxy), or R6 and R7, together with the nitrogen atom to which they are attached, form an azetidinyl, pyrrolidinyl, piperidinyl or morpholinyl group;

    R8 represents H, C1-4 alkyl (which C1-4 alkyl group is optionally terminated by a C1-4 haloalkyl group) or benzyl;

    Het1 represents a 4-R9-1-piperazinyl group optionally substituted with one or two C1-4 alkyl groups and optionally in the form of its 4-N-oxide;

    R9 represents H, pyridinyl, pyrimidinyl, C3-6 alkenyl or C1-4 alkyl optionally substituted by one or two substituents selected from —

    OH, —

    N(R6)R7, —

    C(O)N(R6)R7, benzodioxolyl, benzodioxanyl or phenyl (which latter group is optionally substituted by C1-4 alkoxy);

    Het2 represents a C-linked 6-membered heterocyclic group containing one or two nitrogen atoms, optionally in the form of its mono-N-oxide, or a C-linked 5-membered heterocyclic group containing two or three nitrogen atoms, wherein either of said heterocyclic groups is optionally substituted with C1-4 alkyl, C1-4 alkoxy or N(H)R10; and

    R10 represents H, C1-4 alkyl or C1-4 alkanoyl;

    or a pharmaceutically, or a veterinarily, acceptable derivative thereof.

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