US 2011/0237791 A1 · 2-PYRIDONE COMPOUNDS

1:

A 2-pyridone compound represented by the formula [1]:
{wherein in the formula [1],
the ring represented by A represents a benzene ring or a pyridine ring,
R1 represents RA-ZA-;
wherein -ZA- represents a single bond or represents any of the following formulas [2]:
when -ZA- represents any of the formulas [2],
RA represents a lower alkyl group, a lower cycloalkyl group, a lower alkenyl group, a lower alkynyl group, an aryl group or a heterocyclyl group (wherein the lower alkyl group, lower cycloalkyl group, lower alkenyl group, lower alkynyl group, aryl group or heterocyclyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the following Substituent Group A1);
or
when -ZA- represents a single bond,
RA represents a lower alkyl group, a lower cycloalkyl group, a lower alkenyl group, a lower alkynyl group, an aryl group, a heterocyclyl group (wherein the lower alkyl group, lower cycloalkyl group, lower alkenyl group, lower alkynyl group, aryl group or heterocyclyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the following Substituent Group A1), a hydrogen atom, a cyano group, a halogen atom, a nitro group, a formyl group, a hydroxy group, an amino group, a carbamoyl group, a formylamino group, a sulfamoyl group or a ureido group;
X represents any of the structures represented by the formulas [3] shown below:
RX represents a hydrogen atom, a lower alkyl group, a lower cycloalkyl group, ORZ3, SRZ3 or NRZ3RZ4
RZ1, RZ2, RZ3 and RZ4 are the same or different and each represent a hydrogen atom or a lower alkyl group,
RY1 and RY2 are the same or different and each represent a hydrogen atom, a halogen atom, a lower alkyl group, a lower cycloalkyl group or a hydroxy group,
Y represents —O—, —S— or —NRZ5—,
RZ5 represents a hydrogen atom or a lower alkyl group,
R4 together with RY1 form a saturated or unsaturated 3- to 8-membered ring which is formed together with the carbon atom to which the substituents are bonded and which may contain one or more nitrogen, oxygen or sulfur atoms (wherein the ring is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the following Substituent Group A1),
or R4 together with RZ5 form a saturated or unsaturated 3- to 8-membered ring which is formed together with the nitrogen atom to which the substituents are bonded and which may contain one or more nitrogen, oxygen or sulfur atoms (wherein the ring is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the following Substituent Group A1),
or R4 represents RB-ZB-,
wherein -ZB- represents a single bond or represents any of the following formulas [4]:
when -ZB- represents any of the formulas [4],
RB represents a lower alkyl group, a lower cycloalkyl group, a lower alkenyl group, a lower alkynyl group, an aryl group or a heterocyclyl group (wherein the lower alkyl group, lower cycloalkyl group, lower alkenyl group, lower alkynyl group, aryl group or heterocyclyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the following Substituent Group A1);
or
when -ZB- represents a single bond,
RB represents a lower alkyl group, a lower cycloalkyl group, a lower alkenyl group, a lower alkynyl group, an aryl group, a heterocyclyl group (wherein the lower alkyl group, lower cycloalkyl group, lower alkenyl group, lower alkynyl group, aryl group or heterocyclyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the following Substituent Group A1), a hydrogen atom, a cyano group, a halogen atom, a nitro group, a formyl group, a hydroxy group, an amino group, a carbamoyl group, a formylamino group, a sulfamoyl group or a ureido group;
RZ6 and RZ7 are the same or different and each represent a hydrogen atom or a lower alkyl group,
RW represents ORC or NRCRZ8,
RC represents a lower alkyl group, a lower cycloalkyl group, a lower alkenyl group, a lower alkynyl group, an aryl group or a heterocyclyl group (wherein the lower alkyl group, lower cycloalkyl group, lower alkenyl group, lower alkynyl group, aryl group or heterocyclyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the following Substituent Group A1),
RZ8 represents a hydrogen atom or a lower alkyl group,
or RZ8 together with RC may form a saturated or unsaturated 3- to 8-membered ring which is formed together with the nitrogen atom to which the substituents are bonded and which may contain one or more nitrogen, oxygen or sulfur atoms (wherein the ring is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the following Substituent Group A1),
Substituent Group A1 represents a halogen atom, a nitro group, a cyano group, a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the group consisting of a halogen atom, a nitro group, a cyano group, a lower cycloalkyl group, an aryl group (wherein the aryl group is unsubstituted or substituted with 1 to 3 halogen atoms), a heterocyclyl group, a hydroxy group, a lower alkoxy group (wherein the lower alkoxy group is unsubstituted or substituted with 1 to 3 halogen atoms), a lower cycloalkoxy group, an aryloxy group, an aryl-lower alkoxy group, a heterocyclyloxy group, a heterocyclyl-lower alkoxy group, a lower alkylthio group, an amino group, a mono-lower alkylamino group, a mono-lower cycloalkylamino group, a di-lower alkylamino group, a lower alkanoyl group, a lower alkylsulfonyl group, a lower alkoxycarbonyl group, a lower alkanoylamino group and an oxo group), a lower cycloalkyl group, an aryl group, a heterocyclyl group (wherein the lower cycloalkyl group, aryl group or heterocyclyl group is unsubstituted or substituted with 1 to 2 groups which may be the same or different and selected from the following Substituent Group A2), a hydroxy group, a lower alkoxy group (wherein the lower alkoxy group is unsubstituted or substituted with 1 to 3 halogen atoms), a lower cycloalkoxy group, an aryloxy group, an aryl-lower alkoxy group, a heterocyclyloxy group, a heterocyclyl-lower alkoxy group, a lower alkylthio group, an amino group, a mono-lower alkylamino group, a mono-lower cycloalkylamino group, a di-lower alkylamino group, a lower alkanoyl group, a lower cycloalkylcarbonyl group, a heterocyclylcarbonyl group, a lower alkylsulfonyl group, a lower alkoxycarbonyl group, a lower alkanoylamino group or an oxo group,
Substituent Group A2 represents a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a mono-lower alkylamino group, a di-lower alkylamino group, a lower alkanoyl group, a lower alkylsulfonyl group, a lower alkoxycarbonyl group, a lower alkanoylamino group, a hydroxy group, a halogen atom, an oxo group or an amino group,
R2 and R3 are the same or different and each represent a hydrogen atom, a halogen atom, a cyano group, a carbamoyl group, a lower alkyl group, a lower alkylsulfonyl group, a lower cycloalkyl group, a lower alkoxy group, a lower cycloalkoxy group (wherein the lower alkyl group, lower alkylsulfonyl group, lower cycloalkyl group, lower alkoxy group or lower cycloalkoxy group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the group consisting of a halogen atom and a hydroxy group) or a hydroxy group,
or the adjacent R1 and R2 together form a C9-C12 fused bicyclic hydrocarbon ring or a C6-C11 fused bicyclic heteroring together with the benzene ring or pyridine ring to which the substituents are bonded (wherein the C9-C12 fused bicyclic hydrocarbon ring or C6-C11 fused bicyclic heteroring is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the following Substituent Group A4),
R5 and Substituent Group A4 are the same or different and each represent a halogen atom, a carbamoyl group, a lower alkanoyl group, an amino group, a di-lower alkylamino group, a lower alkyl group, a lower cycloalkyl group, a lower alkoxy group, a lower cycloalkoxy group, an aryl group, a heteroaryl group, an aryloxy group or a heterocyclyl group (wherein the lower alkyl group, lower cycloalkyl group, lower alkoxy group, lower cycloalkoxy group, aryl group, heteroaryl group, aryloxy group or heterocyclyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the following Substituent Group A3),
Substituent Group A3 represents a halogen atom, a nitro group, a cyano group, a hydroxy group, a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the group consisting of a halogen atom, a nitro group, a cyano group, a hydroxy group, a lower cycloalkyl group, an aryl group, a heterocyclyl group, a lower alkoxy group (wherein the lower alkoxy group is unsubstituted or substituted with 1 to 3 halogen atoms), a lower cycloalkoxy group, an aryloxy group, an aryl-lower alkoxy group, a heterocyclyloxy group, a heterocyclyl-lower alkoxy group, an amino group, a mono-lower alkylamino group, a mono-lower cycloalkylamino group and a di-lower alkylamino group), a lower cycloalkyl group, an aryl group, a heterocyclyl group, a lower alkoxy group (wherein the lower alkoxy group is unsubstituted or substituted with 1 to 3 halogen atoms), a lower cycloalkoxy group, an aryloxy group, an aryl-lower alkoxy group, a heterocyclyloxy group, a heterocyclyl-lower alkoxy group, an amino group, a mono-lower alkylamino group, a mono-lower cycloalkylamino group, a di-lower alkylamino group, a lower alkoxycarbonyl group or a carbamoyl group,
V represents a single bond or a lower alkylene group, and
W represents a single bond, an ether bond or a lower alkylene group (wherein the lower alkylene group may contain an ether bond)},
a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof.

36 more elements

2:

The 2-pyridone compound according to claim 1 represented by the formula [1]:
{wherein in the formula [1],
the ring represented by A represents a benzene ring or a pyridine ring,
R1 represents RA-ZA-,
wherein -ZA- represents a single bond or represents any of the following formulas [2]:
when -ZA- represents any of the formulas [2],
RA represents a lower alkyl group, a lower cycloalkyl group, a lower alkenyl group, a lower alkynyl group, an aryl group or a heterocyclyl group (wherein the lower alkyl group, lower cycloalkyl group, lower alkenyl group, lower alkynyl group, aryl group or heterocyclyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the following Substituent Group A1);
or
when -ZA- represents a single bond,
RA represents a lower alkyl group, a lower cycloalkyl group, a lower alkenyl group, a lower alkynyl group, an aryl group, a heterocyclyl group (wherein the lower alkyl group, lower cycloalkyl group, lower alkenyl group, lower alkynyl group, aryl group or heterocyclyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the following Substituent Group A1), a hydrogen atom, a cyano group, a halogen atom, a nitro group, a formyl group, a hydroxy group, an amino group, a carbamoyl group, a formylamino group, a sulfamoyl group or a ureido group;
X represents any of the structures represented by the formulas [3] shown below:
RX represents a hydrogen atom, a lower alkyl group, a lower cycloalkyl group, ORZ3, SRZ3 or NRZ3RZ4,
RZ1, RZ2, RZ3 and RZ4 are the same or different and each represent a hydrogen atom or a lower alkyl group,
RY1 and RY2 are the same or different and each represent a hydrogen atom, a halogen atom, a lower alkyl group, a lower cycloalkyl group or a hydroxy group,
Y represents —O—, —S— or —NRZ5—,
RZ5 represents a hydrogen atom or a lower alkyl group,
R4 together with RY1 form a saturated or unsaturated 3- to 8-membered ring which is formed together with the carbon atom to which the substituents are bonded and which may contain one or more nitrogen, oxygen or sulfur atoms (wherein the ring is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the following Substituent Group A1),
or R4 together with RZ5 form a saturated or unsaturated 3- to 8-membered ring which is formed together with the nitrogen atom to which the substituents are bonded and which may contain one or more nitrogen, oxygen or sulfur atoms (wherein the ring is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the following Substituent Group A1),
or R4 represents RB-ZB-,
wherein -ZB- represents a single bond or represents any of the following formulas [4]:
when -ZB- represents any of the formulas [4],
RB represents a lower alkyl group, a lower cycloalkyl group, a lower alkenyl group, a lower alkynyl group, an aryl group or a heterocyclyl group (wherein the lower alkyl group, lower cycloalkyl group, lower alkenyl group, lower alkynyl group, aryl group or heterocyclyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the following Substituent Group A1);
or
when -ZB- represents a single bond,
RB represents a lower alkyl group, a lower cycloalkyl group, a lower alkenyl group, a lower alkynyl group, an aryl group, a heterocyclyl group (wherein the lower alkyl group, lower cycloalkyl group, lower alkenyl group, lower alkynyl group, aryl group or heterocyclyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the following Substituent Group A1), a hydrogen atom, a cyano group, a halogen atom, a nitro group, a formyl group, a hydroxy group, an amino group, a carbamoyl group, a formylamino group, a sulfamoyl group or a ureido group;
RZ6 and RZ7 are the same or different and each represent a hydrogen atom or a lower alkyl group,
RW represents ORC or NRCRZ8,
RC represents a lower alkyl group, a lower cycloalkyl group, a lower alkenyl group, a lower alkynyl group, an aryl group or a heterocyclyl group (wherein the lower alkyl group, lower cycloalkyl group, lower alkenyl group, lower alkynyl group, aryl group or heterocyclyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the following Substituent Group A1),
RZ8 represents a hydrogen atom or a lower alkyl group,
or RZ8 together with RC may form a saturated or unsaturated 3- to 8-membered ring which is formed together with the nitrogen atom to which the substituents are bonded and which may contain one or more nitrogen, oxygen or sulfur atoms (wherein the ring is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the following Substituent Group A1),
Substituent Group A1 represents a halogen atom, a nitro group, a cyano group, a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the group consisting of a halogen atom, a nitro group, a cyano group, a lower cycloalkyl group, an aryl group, a heterocyclyl group, a hydroxy group, a lower alkoxy group (wherein the lower alkoxy group is unsubstituted or substituted with 1 to 3 halogen atoms), a lower cycloalkoxy group, an aryloxy group, an aryl-lower alkoxy group, a heterocyclyloxy group, a heterocyclyl-lower alkoxy group, a lower alkylthio group, an amino group, a mono-lower alkylamino group, a mono-lower cycloalkylamino group, a di-lower alkylamino group, a lower alkanoyl group, a lower alkylsulfonyl group, a lower alkoxycarbonyl group, a lower alkanoylamino group and an oxo group), a lower cycloalkyl group, an aryl group, a heterocyclyl group (wherein the lower cycloalkyl group, aryl group or heterocyclyl group is unsubstituted or substituted with 1 to 2 groups which may be the same or different and selected from the following Substituent Group A2), a hydroxy group, a lower alkoxy group (wherein the lower alkoxy group is unsubstituted or substituted with 1 to 3 halogen atoms), a lower cycloalkoxy group, an aryloxy group, an aryl-lower alkoxy group, a heterocyclyloxy group, a heterocyclyl-lower alkoxy group, a lower alkylthio group, an amino group, a mono-lower alkylamino group, a mono-lower cycloalkylamino group, a di-lower alkylamino group, a lower alkanoyl group, a lower alkylsulfonyl group, a lower alkoxycarbonyl group, a lower alkanoylamino group or an oxo group,
Substituent Group A2 represents a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a mono-lower alkylamino group, a di-lower alkylamino group, a lower alkanoyl group, a lower alkylsulfonyl group, a lower alkoxycarbonyl group, a lower alkanoylamino group, a hydroxy group, a halogen atom, an oxo group or an amino group,
R2 and R3 are the same or different and each represent a hydrogen atom, a halogen atom, a lower alkyl group, a lower cycloalkyl group, a lower alkoxy group or a lower cycloalkoxy group (wherein the lower alkyl group, lower cycloalkyl group, lower alkoxy group or lower cycloalkoxy group is unsubstituted or substituted with 1 to 3 halogen atoms),
or the adjacent R1 and R2 together form a C9-C12 fused bicyclic hydrocarbon ring or a C6-C11 fused bicyclic heteroring together with the benzene ring or pyridine ring to which the substituents are bonded (wherein the C9-C12 fused bicyclic hydrocarbon ring or C6-C11 fused bicyclic heteroring is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the following Substituent Group A4),
R5 and Substituent Group A4 are the same or different and each represent a halogen atom, a lower alkyl group, a lower cycloalkyl group, a lower alkoxy group, a lower cycloalkoxy group, an aryl group, a heteroaryl group or a heterocyclyl group (wherein the lower alkyl group, lower cycloalkyl group, lower alkoxy group, lower cycloalkoxy group, aryl group, heteroaryl group or heterocyclyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the following Substituent Group A3),
Substituent Group A3 represents a halogen atom, a nitro group, a cyano group, a hydroxy group, a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the group consisting of a halogen atom, a nitro group, a cyano group, a hydroxy group, a lower cycloalkyl group, an aryl group, a heterocyclyl group, a lower alkoxy group (wherein the lower alkoxy group is unsubstituted or substituted with 1 to 3 halogen atoms), a lower cycloalkoxy group, an aryloxy group, an aryl-lower alkoxy group, a heterocyclyloxy group, a heterocyclyl-lower alkoxy group, an amino group, a mono-lower alkylamino group, a mono-lower cycloalkylamino group and a di-lower alkylamino group), a lower cycloalkyl group, an aryl group, a heterocyclyl group, a lower alkoxy group (wherein the lower alkoxy group is unsubstituted or substituted with 1 to 3 halogen atoms), a lower cycloalkoxy group, an aryloxy group, an aryl-lower alkoxy group, a heterocyclyloxy group, a heterocyclyl-lower alkoxy group, an amino group, a mono-lower alkylamino group, a mono-lower cycloalkylamino group, a di-lower alkylamino group or a lower alkoxycarbonyl group,
V represents a single bond or a lower alkylene group, and
W represents a single bond, an ether bond or a lower alkylene group (wherein the lower alkylene group may contain an ether bond)},
a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof.

36 more elements

5:

The 2-pyridone compound according to claim 4 represented by the formula [7]:
{wherein in the formula [7],
R4 represents RB-ZB-,
wherein -ZB- represents a single bond or represents any of the following formulas [8]:
when -ZB- represents any of the formulas [8],
RB represents a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 2 groups which may be the same or different and selected from the following Substituent Group A1);
or
when -ZB- represents a single bond,
RB represents a lower alkyl group, a lower cycloalkyl group, an aryl group or a heterocyclyl group (wherein the lower alkyl group, lower cycloalkyl group, aryl group or heterocyclyl group is unsubstituted or substituted with 1 to 2 groups which may be the same or different and selected from the following Substituent Group A1);
Substituent Group A1 represents a halogen atom, a lower alkyl group, a lower cycloalkyl group, an aryl group, a heterocyclyl group (wherein the lower cycloalkyl group, aryl group or heterocyclyl group is unsubstituted or substituted with 1 to 2 groups which may be the same or different and selected from the following Substituent Group A2), a hydroxy group, a lower alkoxy group (wherein the lower alkoxy group is unsubstituted or substituted with 1 to 3 halogen atoms), a lower alkylthio group, an amino group, a mono-lower alkylamino group, a di-lower alkylamino group, a lower alkanoyl group, a lower alkylsulfonyl group, a lower alkoxycarbonyl group, a lower alkanoylamino group or an oxo group, and
Substituent Group A2 represents a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a mono-lower alkylamino group, a di-lower alkylamino group, a lower alkanoyl group, a lower alkylsulfonyl group, a lower alkoxycarbonyl group, a lower alkanoylamino group, a hydroxy group, a halogen atom, an oxo group or an amino group},
a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof.

9 more elements

6:

The 2-pyridone compound according to claim 5, wherein
R1 represents RA-ZA-,
wherein -ZA- represents a single bond or represents any of the following formulas [9]:
when -ZA- represents any of the formulas [9],
RA represents a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the group consisting of a halogen atom, a hydroxy group, a heterocyclyl group, a mono-lower alkylamino group and a di-lower alkylamino group), a lower cycloalkyl group or a heterocyclyl group (wherein the heterocyclyl group is unsubstituted or substituted with one lower alkyl group);
or
when -ZA- represents a single bond,
RA represents a hydrogen atom or a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the group consisting of a halogen atom, a hydroxy group, a heterocyclyl group, a lower alkoxy group and a di-lower alkylamino group);
R2 represents a hydrogen atom, a halogen atom, a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 3 halogen atoms) or a lower alkoxy group,
R4 represents RB-ZB-,
wherein -ZB- represents a single bond and
RB represents a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with one group selected from the group consisting of a lower cycloalkyl group, a heterocyclyl group, a hydroxy group and a lower alkanoylamino group), a lower cycloalkyl group (wherein the lower cycloalkyl group is unsubstituted or substituted with one group selected from the group consisting of a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with one hydroxy group), a hydroxy group and an oxo group) or a heterocyclyl group (wherein the heterocyclyl group is unsubstituted or substituted with 1 to 2 groups which may be the same or different and selected from the group consisting of a lower alkyl group, a hydroxy group, a lower alkanoyl group and an oxo group), and
R5 represents a halogen atom, a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the group consisting of a halogen atom and a hydroxy group), a lower cycloalkyl group or an aryl group,
a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof.

11 more elements

7:

The 2-pyridone compound according to claim 4 represented by the formula [10]:
{wherein in the formula [10],
R4 represents RB-ZB-,
wherein -ZB- represents a single bond or represents any of the following formulas [8]:
when -ZB- represents any of the formulas [8],
RB represents a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 2 groups which may be the same or different and selected from the following Substituent Group A1);
or
when -ZB- represents a single bond,
RB represents a lower alkyl group, a lower cycloalkyl group, an aryl group or a heterocyclyl group (wherein the lower alkyl group, lower cycloalkyl group, aryl group or heterocyclyl group is unsubstituted or substituted with 1 to 2 groups which may be the same or different and selected from the following Substituent Group A1);
Substituent Group A1 represents a halogen atom, a lower alkyl group, a lower cycloalkyl group, an aryl group, a heterocyclyl group (wherein the lower cycloalkyl group, aryl group or heterocyclyl group is unsubstituted or substituted with 1 to 2 groups which may be the same or different and selected from the following Substituent Group A2), a hydroxy group, a lower alkoxy group (wherein the lower alkoxy group is unsubstituted or substituted with 1 to 3 halogen atoms), a lower alkylthio group, an amino group, a mono-lower alkylamino group, a di-lower alkylamino group, a lower alkanoyl group, a lower alkylsulfonyl group, a lower alkoxycarbonyl group, a lower alkanoylamino group or an oxo group, and
Substituent Group A2 represents a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a mono-lower alkylamino group, a di-lower alkylamino group, a lower alkanoyl group, a lower alkylsulfonyl group, a lower alkoxycarbonyl group, a lower alkanoylamino group, a hydroxy group, a halogen atom, an oxo group or an amino group},
a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof.

9 more elements

8:

The 2-pyridone compound according to claim 7, wherein
R1 represents RA-ZA-,
wherein -ZA- represents a single bond or represents any of the following formulas [9]:
when -ZA- represents any of the formulas [9],
RA represents a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the group consisting of a halogen atom, a hydroxy group, a heterocyclyl group, a mono-lower alkylamino group and a di-lower alkylamino group), a lower cycloalkyl group or a heterocyclyl group (wherein the heterocyclyl group is unsubstituted or substituted with one lower alkyl group);
or
when -ZA- represents a single bond,
RA represents a hydrogen atom, a halogen atom, a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the group consisting of a halogen atom, a hydroxy group, a heterocyclyl group, a lower alkoxy group and a di-lower alkylamino group), a lower cycloalkyl group, an aryl group or a heterocyclyl group;
R2 represents a hydrogen atom, a halogen atom, a carbamoyl group, a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the group consisting of a halogen atom and a hydroxy group) or a lower alkoxy group (wherein the lower alkoxy group is unsubstituted or substituted with 1 to 3 halogen atoms),
R3 represents a hydrogen atom, a halogen atom, a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 3 halogen atoms), a lower alkoxy group or a hydroxy group,
R4 represents RB-ZB-,
wherein -ZB- represents a single bond and
RB represents a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with one group selected from the group consisting of a lower cycloalkyl group, an aryl group, a heterocyclyl group (wherein the heterocyclyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the group consisting of a lower alkyl group and an oxo group), a hydroxy group and a lower alkanoylamino group), a lower cycloalkyl group (wherein the lower cycloalkyl group is unsubstituted or substituted with one group selected from the group consisting of a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with one hydroxy group), a hydroxy group and an oxo group) or a heterocyclyl group (wherein the heterocyclyl group is unsubstituted or substituted with 1 to 2 groups which may be the same or different and selected from the group consisting of a lower alkyl group, a hydroxy group, a lower alkanoyl group, a lower cycloalkylcarbonyl group, a heterocyclylcarbonyl group, a lower alkylsulfonyl group and an oxo group), and
R5 represents a halogen atom, a carbamoyl group, a lower alkanoyl group, an amino group, a di-lower alkylamino group, a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the group consisting of a halogen atom and a hydroxy group), a lower cycloalkyl group (wherein the lower cycloalkyl group is unsubstituted or substituted with one hydroxy group), a lower alkoxy group (wherein the lower alkoxy group is unsubstituted or substituted with 1 to 3 halogen atoms), an aryl group, a heteroaryl group or an aryloxy group (wherein the aryloxy group is unsubstituted or substituted with one group selected from the group consisting of a halogen atom and a lower alkyl group),
a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof.

12 more elements

12:

Any of 2-pyridone compounds shown below:
6-{(E)-1-(3-chloro-4-ethoxyphenyl)-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}-3-cyclopropylpyridin-2(1H)-one,
6-{(E)-1-(4-chlorophenyl)-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}-3-cyclopropylpyridin-2(1H)-one,
6-{(E)-1-[3-chloro-4-(trifluoromethyl)phenyl]-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}-3-cyclopropylpyridin-2(1H)-one,
6-{(E)-1-(4-chloro-3-methylphenyl)-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}-3-cyclopropylpyridin-2(1H)-one,
6-{(E)-1-(4-chloro-3-fluorophenyl)-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}-3-cyclopropylpyridin-2(1H)-one,
3-cyclopropyl-6-{(E)-1-(4-fluoro-3-methylphenyl)-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}pyridin-2(1H)-one,
3-cyclopropyl-6-{(E)-1-[3-fluoro-4-(trifluoromethyl)phenyl]-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}pyridin-2(1H)-one,
3-cyclopropyl-6-{(E)-1-[4-fluoro-3-(trifluoromethyl)phenyl]-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}pyridin-2(1H)-one,
6-{(E)-1-(4-chloro-3-methoxyphenyl)-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}-3-cyclopropylpyridin-2(1H)-one,
3-cyclopropyl-6-{(E)-1-[4-(difluoromethyl)-3-fluorophenyl]-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}pyridin-2(1H)-one,
3-cyclopropyl-6-{(E)-1-[4-methoxy-3-(trifluoromethyl)phenyl]-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}pyridin-2(1H)-one,
3-cyclopropyl-6-{(E)-1-[3-methyl-4-(trifluoromethyl)phenyl]-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}pyridin-2(1H)-one,
6-{(E)-1-(4-chloro-2-fluorophenyl)-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}-3-cyclopropylpyridin-2(1H)-one,
3-cyclopropyl-6-{(E)-1-[2-fluoro-4-(trifluoromethyl)phenyl]-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}pyridin-2(1H)-one,
6-{(E)-1-[3-chloro-4-(cyclopropyloxy)phenyl]-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}-3-cyclopropylpyridin-2(1H)-one,
6-{(E)-1-[3-chloro-4-(2,2,2-trifluoroethoxy)phenyl]-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}-3-cyclopropylpyridin-2(1H)-one,
6-{(E)-1-(5-chloro-2-fluoro-4-methoxyphenyl)-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}-3-cyclopropylpyridin-2(1H)-one,
6-{(E)-1-[3-chloro-4-(difluoromethoxy)phenyl]-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}-3-cyclopropylpyridin-2(1H)-one,
3-cyclopropyl-6-{(E)-1-(4-ethoxy-2,3-difluorophenyl)-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}pyridin-2(1H)-one,
3-cyclopropyl-6-{(E)-1-[4-(cyclopropylsulfonyl)phenyl]-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}pyridin-2(1H)-one,
6-{(E)-1-(2-chloro-4-ethoxyphenyl)-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}-3-cyclopropylpyridin-2(1H)-one,
3-cyclopropyl-6-[(E)-2-[(2R)-5-oxopyrrolidin-2-yl]-1-{4-[(trifluoromethyl)sulfonyl]phenyl}ethenyl]pyridin-2(1H)-one,
3-chloro-6-{(E)-1-[4-(cyclopropylsulfonyl)phenyl]-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}pyridin-2(1H)-one,
3-chloro-6-{(E)-1-[3-chloro-4-(ethylsulfonyl)phenyl]-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}pyridin-2(1H)-one,
3-chloro-6-{(E)-1-[4-(cyclopentylsulfonyl)phenyl]-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}pyridin-2(1H)-one,
3-cyclopropyl-6-{(E)-1-[4-(methylsulfonyl)phenyl]-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}pyridin-2(1H)-one,
6-{(E)-1-[3-chloro-4-(cyclopropylsulfonyl)phenyl]-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}-3-cyclopropylpyridin-2(1H)-one,
3-cyclopropyl-6-{(E)-1-[4-(cyclopropylsulfonyl)-3-methylphenyl]-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}pyridin-2(1H)-one,
3-chloro-6-{(E)-1-[4-(cyclopropylsulfonyl)-3-methylphenyl]-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}pyridin-2(1H)-one and
3-chloro-6-{(E)-1-[3-chloro-4-(cyclopropylsulfonyl)phenyl]-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}pyridin-2(1H)-one,
a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof.

29 more elements

14:

The 2-pyridone compound according to claim 13 represented by the formula [14]:
{wherein in the formula [14],
R4 represents RB-ZB-,
wherein -ZB- represents a single bond or represents any of the following formulas [8]:
when -ZB- represents any of the formulas [8],
RB represents a lower alkyl group, a lower cycloalkyl group or a heterocyclyl group (wherein the lower alkyl group, lower cycloalkyl group or heterocyclyl group is unsubstituted or substituted with 1 to 2 groups which may be the same or different and selected from the following Substituent Group A1);
or
when -ZB- represents a single bond,
RB represents a lower alkyl group, a lower cycloalkyl group, an aryl group or a heterocyclyl group (wherein the lower alkyl group, lower cycloalkyl group, aryl group or heterocyclyl group is unsubstituted or substituted with 1 to 2 groups which may be the same or different and selected from the following Substituent Group A1);
Substituent Group A1 represents a halogen atom, a lower alkyl group, a lower cycloalkyl group, an aryl group, a heterocyclyl group (wherein the lower cycloalkyl group, aryl group or heterocyclyl group is unsubstituted or substituted with 1 to 2 groups which may be the same or different and selected from the following Substituent Group A2), a lower alkoxy group (wherein the lower alkoxy group is unsubstituted or substituted with 1 to 3 halogen atoms), a lower alkylthio group, an amino group, a mono-lower alkylamino group, a di-lower alkylamino group, a lower alkanoyl group, a lower alkylsulfonyl group, a lower alkoxycarbonyl group, a lower alkanoylamino group or an oxo group, and
Substituent Group A2 represents a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a mono-lower alkylamino group, a di-lower alkylamino group, a lower alkanoyl group, a lower alkylsulfonyl group, a lower alkoxycarbonyl group, a lower alkanoylamino group, a hydroxy group, a halogen atom, an oxo group or an amino group},
a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof.

9 more elements

15:

The 2-pyridone compound according to claim 14, wherein
R1 represents RA-ZA-,
wherein -ZA- represents a single bond or represents any of the following formulas [9]:
when -ZA- represents any of the formulas [9],
RA represents a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the group consisting of a halogen atom, a hydroxy group, a heterocyclyl group, a mono-lower alkylamino group and a di-lower alkylamino group), a lower cycloalkyl group or a heterocyclyl group (wherein the heterocyclyl group is unsubstituted or substituted with one lower alkyl group);
or
when -ZA- represents a single bond,
RA represents a hydrogen atom or a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the group consisting of a halogen atom, a hydroxy group, a heterocyclyl group, a lower alkoxy group and a di-lower alkylamino group);
R2 represents a hydrogen atom, a halogen atom, a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 3 halogen atoms) or a lower alkoxy group,
R4 represents RB-ZB-,
wherein -ZB- represents a single bond and
RB represents a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with one group selected from the group consisting of a lower cycloalkyl group, a heterocyclyl group, a hydroxy group and a lower alkanoylamino group), a lower cycloalkyl group (wherein the lower cycloalkyl group is unsubstituted or substituted with one group selected from the group consisting of a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with one hydroxy group), a hydroxy group and an oxo group) or a heterocyclyl group (wherein the heterocyclyl group is unsubstituted or substituted with 1 to 2 groups which may be the same or different and selected from the group consisting of a lower alkyl group, a hydroxy group, a lower alkanoyl group and an oxo group), and
R5 represents a halogen atom, a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the group consisting of a halogen atom and a hydroxy group), a lower cycloalkyl group or an aryl group,
a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof.

11 more elements

16:

The 2-pyridone compound according to claim 13 represented by the formula [15]:
{wherein in the formula [15],
R4 represents RB-ZB-,
wherein -ZB- represents a single bond or represents any of the following formulas [8]:
when -ZB- represents any of the formulas [8],
RB represents a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 2 groups which may be the same or different and selected from the following Substituent Group A1);
or
when -ZB- represents a single bond,
RB represents a lower alkyl group, a lower cycloalkyl group, an aryl group or a heterocyclyl group (wherein the lower alkyl group, lower cycloalkyl group, aryl group or heterocyclyl group is unsubstituted or substituted with 1 to 2 groups which may be the same or different and selected from the following Substituent Group A1);
Substituent Group A1 represents a halogen atom, a lower alkyl group, a lower cycloalkyl group, an aryl group, a heterocyclyl group (wherein the lower cycloalkyl group, aryl group or heterocyclyl group is unsubstituted or substituted with 1 to 2 groups which may be the same or different and selected from the following Substituent Group A2), a hydroxy group, a lower alkoxy group (wherein the lower alkoxy group is unsubstituted or substituted with 1 to 3 halogen atoms), a lower alkylthio group, an amino group, a mono-lower alkylamino group, a di-lower alkylamino group, a lower alkanoyl group, a lower alkylsulfonyl group, a lower alkoxycarbonyl group, a lower alkanoylamino group or an oxo group, and
Substituent Group A2 represents a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a mono-lower alkylamino group, a di-lower alkylamino group, a lower alkanoyl group, a lower alkylsulfonyl group, a lower alkoxycarbonyl group, a lower alkanoylamino group, a hydroxy group, a halogen atom, an oxo group or an amino group},
a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof.

9 more elements

17:

The 2-pyridone compound according to claim 16, wherein
R1 represents RA-ZA-,
wherein -ZA- represents a single bond or represents any of the following formulas [9]:
when -ZA- represents any of the formulas [9],
RA represents a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the group consisting of a halogen atom, a hydroxy group, a heterocyclyl group, a mono-lower alkylamino group and a di-lower alkylamino group), a lower cycloalkyl group or a heterocyclyl group (wherein the heterocyclyl group is unsubstituted or substituted with one lower alkyl group);
or
when -ZA- represents a single bond,
RA represents a hydrogen atom, a halogen atom, a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the group consisting of a halogen atom, a hydroxy group, a heterocyclyl group, a lower alkoxy group and a di-lower alkylamino group), a lower cycloalkyl group, an aryl group or a heterocyclyl group;
R2 represents a hydrogen atom, a halogen atom, a carbamoyl group, a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the group consisting of a halogen atom and a hydroxy group) or a lower alkoxy group (wherein the lower alkoxy group is unsubstituted or substituted with 1 to 3 halogen atoms),
R3 represents a hydrogen atom, a halogen atom, a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 3 halogen atoms), a lower alkoxy group or a hydroxy group,
R4 represents RB-ZB-,
wherein -ZB- represents a single bond and
RB represents a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with one group selected from the group consisting of a lower cycloalkyl group, an aryl group, a heterocyclyl group (wherein the heterocyclyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the group consisting of a lower alkyl group and an oxo group), a hydroxy group and a lower alkanoylamino group), a lower cycloalkyl group (wherein the lower cycloalkyl group is unsubstituted or substituted with one group selected from the group consisting of a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with one hydroxy group), a hydroxy group and an oxo group) or a heterocyclyl group (wherein the heterocyclyl group is unsubstituted or substituted with 1 to 2 groups which may be the same or different and selected from the group consisting of a lower alkyl group, a hydroxy group, a lower alkanoyl group, a lower cycloalkylcarbonyl group, a heterocyclylcarbonyl group, a lower alkylsulfonyl group and an oxo group), and
R5 represents a halogen atom, a carbamoyl group, a lower alkanoyl group, an amino group, a di-lower alkylamino group, a lower alkyl group (wherein the lower alkyl group is unsubstituted or substituted with 1 to 3 groups which may be the same or different and selected from the group consisting of a halogen atom and a hydroxy group), a lower cycloalkyl group (wherein the lower cycloalkyl group is unsubstituted or substituted with one hydroxy group), a lower alkoxy group (wherein the lower alkoxy group is unsubstituted or substituted with 1 to 3 halogen atoms), an aryl group, a heteroaryl group or an aryloxy group (wherein the aryloxy group is unsubstituted or substituted with one group selected from the group consisting of a halogen atom and a lower alkyl group),
a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof.

12 more elements

2-pyridone compounds

Life of this patent

2-pyridone compounds

Life of this patent

Abstract

Claims27