DERIVATIVES OF 2-PIRIDONE FOR THE TREATMENT OF AN ILLNESS OR AFFECTION IN WHICH THE INHIBITION OF THE ACTIVITY OF THE NEUTRROPHILE ELASTASA IS BENEFIT.

摘要

A compound of the formula (I) ** (See formula) ** where R 1 represents hydrogen or C 1 -C 6 alkyl; W represents a 5-link heterocyclic ring comprising at least one heteroatom in the ring selected from nitrogen, oxygen and sulfur, wherein at least one of the ring carbon atoms can be optionally replaced with a carbonyl group; and wherein the heterocyclic ring is optionally substituted with at least one substituent selected from halogen, C1-C4 alkyl, C1-C4 alkoxy, CN, OH, NO2, C1-C3 alkyl substituted with one or more F atoms, C1-C3 alkoxy , substituted with one or more atoms of F, NR10R11, C≡CR15, CONR16R17, CHO, C2-C4 alkanoyl, S (O) xR18 and OSO2R19; R14 represents phenyl or a 6-link heteroaromatic ring comprising 1 to 3 nitrogen atoms in the ring; said ring is optionally substituted with at least one substituent selected from halogen, C1-C4 alkyl, C1-C4 alkoxy, CN, OH, NO2, C1-C3 alkyl substituted with one or more F atoms, C1-C3 alkoxy substituted with one or more atoms of F, NR12R13, C≡CR30, CONR31R32, CHO, C2-C4 alkanoyl, S (O) pR33 and OSO = R34; R10, R11, R12 and R13 independently represent H, C1-C6 alkyl, formyl or C2-C6 alkanoyl; or the group-NR10R11 or -NR12R13 together represents an azacyclic ring of 5 to 7 links which optionally also incorporates a heteroatom selected from O, S and NR26; R15 and R30 independently represent H, C1-C3 alkyl or Si (CH3) 3; R18, R19, R33 and R34 independently represent H or C1-C3 alkyl; said alkyl is optionally further substituted with one or more F atoms; R6 represents H or F; R3 represents phenyl or a five or six membered heteroaromatic ring containing 1 to 3 heteroatoms independently selected from O, S and N; said ring is optionally substituted with at least one substituent selected from halogen, C1-C6 alkyl, cyano, C1-C6 alkoxy, nitro, methylcarbonyl, NR35R36, C1-C3 alkyl substituted with one or more F atoms or C1-C3 substituted alkoxy with one or more atoms of F; R35 and R36 independently represent H or C1-C3 alkyl; said alkyl is optionally further substituted by one or more F atoms; R4 represents hydrogen or C1-C6 alkyl optionally substituted with at least one substituent selected from fluorine, hydroxy and C1-C6 alkoxy; X represents a single bond, O, NR24 or a C1-C6 alkylene group -Y-, wherein Y represents a single bond, oxygen atom, NR24 or S (O), and said alkylene is optionally further substituted with OH, halogen , CN, NR37R38, C1-C3 alkoxy, CONR39R40, CO2R66, SO2R41 and SO2NR42R43; or R4 and X are joined together in such a way that the group -NR4X together represents an azacyclic ring of 5 to 7 links that optionally also incorporates a heteroatom selected from O, S and NR44; said ring is optionally substituted with C1-C6 alkyl or NR45R46; said alkyl is optionally further substituted with OH; or R5 represents a monocyclic ring system selected from: i) phenoxy, ii) phenyl, iii) a 5- or 6-link heteroaromatic ring comprising at least one heteroatom in the ring selected from nitrogen, oxygen and sulfur, iv) a C3-C6 saturated or partially unsaturated cycloalkyl ring, ov) a 4 to 7 link, saturated or partially unsaturated heterocyclic ring comprising at least one heteroatom in the selected oxygen ring, S (O) r and NR20, wherein at least one of the carbon atoms of the ring can be optionally replaced with a carbonyl group, or R5 represents a bicyclic ring system in which the two rings are independently selected from the monocyclic ring system defined in ii), iii), iv) and v) above, where the two rings are either fused together, or joined directly to each other or are separated from each other by a bond group selected from oxygen, S (O) to C1-C6 alkylene that I purchased therefore optionally one or more internal or terminal heteroatoms selected from oxygen, sulfur and NR27 and which is optionally substituted with at least one substituent selected from hydroxy, oxo and C1-C6 alkoxy, the monocyclic or bicyclic ring system is optionally substituted with at least a substituent selected from oxygen, CN, OH, C1-C6 alkyl, C1-C6 alkoxy, halogen, NR47R48, NO2, OSO2R49, CO2R50, C (= NH) NH2, C (O) NR51R52, C (S) NR53R54, SC (= NH) NH2, NR55C (= NH) NH2, S (O) vR71, SO2NR56R57, C1-C3 alkoxy substituted with one or more F atoms and C1-C3 alkyl substituted with SO2R58 or with one or more F atoms; said C1-C6 alkyl is further optionally substituted with at least one substituent selected from cyano, hydroxy, C1-C6 alkoxy, C1-C6 alkyl thio and -C (O) NR22R23; or R5 may also represent H; R20 represents hydrogen, C1-C6 alkyl, C1-C6 alkylcarbonyl or C1-C6 alkoxy carbonyl; R21 represents hydrogen, C1-C6 alkyl or C3-C8 cycloalkyl; said alkyl or cycloalkyl group is optionally further substituted with one or more substituents independently selected from OH, CN, C1-C3 alkoxy and CONR59R60; R37 and R38 independently represent H, C1-C6 alkyl, formyl or C2-C6 alkanoyl; R47 and R48 independently represent H, C1-C6 alkyl, formyl, C2-C6 alkanoyl, S (O) qR61 or SO2NR62R63; said alkyl group is optionally further substituted with halogen, CN, C1-C4 alkoxy or CONR64R65; R41 and R61 independently represent H, C1-C6 alkyl or C3-C6 cycloalkyl; p is 0, 1 or 2; q is 0, 1 or 2; r is 0, 1 or 2; t is 0, 1 or 2; w is 0, 1 or 2; x is 0, 1 or 2; v is 0, 1 or 2; R16, R17, R22, R23, R24, R26, R27, R31, R32, R39, R40, R42, R43, R44, R45, R46, R49, R50, R51, R52, R53, R54, R55, R56, R57, R58, R59, R60, R62, R63, R64, R65 and R66 each independently represents hydrogen or C1-C6 alkyl; or a pharmaceutically acceptable salt thereof.