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2-PYRIDINE DERIVATIVES AS INHIBITORS OF NEUTROPHILE ELASTASE

  • US 20090131483A1
  • Filed: 03/14/2006
  • Published: 05/21/2009
  • Est. Priority Date: 03/16/2005
  • Status: Abandoned Application
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1. A compound of formula wherein R1 represents hydrogen or C1-C6 alkyl;

  • R2 represents halogen, cyano, carboxyl, hydroxyl, nitro, —

    C(O)H, —

    C(O)NR10R11, —

    NR12R13 or a group selected from C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylcarbonyl, C1-C6 alkoxycarbonyl, C2-C6 alkenyl, C2-C6 alkynyl and a saturated or unsaturated 3- to 10-membered ring system optionally comprising at least one ring heteroatom selected from nitrogen, oxygen and sulphur, each group being optionally substituted by one or more substituents independently selected from halogen, cyano, carboxyl, hydroxyl, oxygen, nitro, —

    S(O)pR15, —

    NR16S(O)qR17, —

    C(O)NR18R19, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylcarbonyl, C1-C6 alkoxycarbonyl and a saturated or unsaturated 5- to 6-membered monocyclic ring system optionally comprising at least one ring heteroatom selected from nitrogen, oxygen and sulphur;

    R3 represents a phenyl group substituted with at least one substituent selected from halogen, cyano, nitro, trifluoromethyl or methylcarbonyl;

    R4 represents hydrogen or C1-C6 alkyl optionally substituted with at least one substituent selected from hydroxyl and C1-C6 alkoxy;

    X represents a bond or a group —

    C1-C6 alkylene-Y—

    , wherein Y represents a single bond, oxygen atom, NR24 or S(O)w;

    R5 represents a monocyclic ring system selected fromi) phenoxy,ii) phenyl,iii) a 5- or 6-membered heteroaromatic ring comprising at least one ring heteroatom selected from nitrogen, oxygen and sulphur,iv) a saturated or partially unsaturated C3-C6 hydrocarbyl ring, orv) a saturated or partially unsaturated 4- to 7-membered heterocyclic ring comprising at least one ring heteroatom selected from oxygen, S(O)r and NR20, wherein at least one of the ring carbon atoms may be optionally replaced by a carbonyl group;

    R5 being substituted by at least one substituent selected from oxygen, C3-C8 cycloalkyl, —

    S(O)vR21, and C1-C6 alkyl substituted with at least one substituent selected from cyano, hydroxyl, C1-C6 alkoxy, C1-C6 alkylthio and —

    C(O)NR22R23;

    R10, R11, R12 and R13 each independently represent hydrogen or C1-C6 alkyl;

    p is 0, 1 or 2;

    q is 0, 1 or 2;

    r is 0, 1 or 2;

    w is 0, 1 or 2;

    R15, R16, R17, R18 and R19 each independently represent hydrogen or C1-C6 alkyl;

    R20 represents hydrogen, C1-C6 alkyl, C1-C6 alkylcarbonyl or C1-C6 alkoxycarbonyl;

    v is 0, 1 or 2;

    R21 represents hydrogen, C1-C6 alkyl or C3-C8 cycloalkyl;

    R22 and R23 each independently represent hydrogen or C1-C6 alkyl;

    R24 represents hydrogen or C1-C6 alkyl;

    with the proviso that when R5 is substituted with a C3-C8 cycloalkyl or an —

    S(O)vR21 substituent group, then R2 represents either(a) a substituted C1-C6 alkyl group in which at least one substituent group is cyano, carboxyl, —

    S(O)pR15, —

    NR16S(O)qR17, —

    C(O)NR18R19 or C1-C6 alkoxycarbonyl(b) a substituted C2-C6 alkynyl group in which at least one substituent group is hydroxyl, or(c) a substituted C1-C6 alkoxy group in which at least one substituent group is a 5- to 6-membered saturated or unsaturated monocyclic ring system optionally comprising at least one ring heteroatom selected from nitrogen, oxygen and sulphur;

    or a pharmaceutically acceptable salt thereof.

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