Patent ID: 6352982
Filing Date: 2002-03-05
Classification: A61P,C07D

Abstract:
A compound of the formula: wherein ring A is C6-14 aromatic hydrocarbon ring, which may have 1 to 4 substituents selected from halogen, C1-6 alkyl, halogeno-C1-6 alkyl, phenyl, benzyl, C1-6 alkoxy, halogeno-C1-6 alkoxy, phenoxy, C7-14 aralkyloxy, formyloxy, C1-6 alkyl-carbonyloxy, C1-6 alkylthio, halogeno-C1-6 alkylthio, hydroxy, mercapto, cyano, nitro, carboxy, formyl, C1-6 alkyl-carbonyl, benzoyl, C1-6 alkoxy-carbonyl, phenoxycarbonyl, amino, mono- or di-C1-6 alkylamino, formylamino, C1-6 alkyl-carbonylamino, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, sulfo, C1-6 alkylsulfonyl, benzoyl-C1-6 alkoxy, hydroxy-C1-6 alkoxy, C1-6 alkoxy-carbonyl-C1-6 alkoxy, C3-14 cycloalkyl-C1-6 alkoxy, imidazol-1-yl-C1-6 alkoxy, C7-14 aralkyloxy-carbonyl-C1-6 alkoxy, hydroxyphenyl-C1-6 alkoxy and C7-14 aralkyloxy-carbonyl,ring B is 1) C6-14 aromatic hydrocarbon ring, 2) 5- or 6-membered monocyclic aromatic heterocyclic ring having 1 to 4 hetero atoms selected from nitrogen, oxygen and sulfur in addition to carbon atoms or 3) bi- or tricyclic aromatic condensed heterocyclic ring which is formed by the condensation of benzene ring and the said 5- or 6-membered monocyclic aromatic heterocyclic ring, which may have 1 to 4 substituents selected from halogen, C1-6 alkyl, halogeno-C1-6 alkyl, phenyl, benzyl, C1-6 alkoxy, halogeno-C1-6 alkoxy, phenoxy, C7-14 aralkyloxy, formyloxy, C1-6 alkyl-carbonyloxy, C1-6 alkylthio, halogeno-C1-6 alkylthio, hydroxy, mercapto, cyano, nitro, carboxy, formyl, C1-6 alkyl-carbonyl, benzoyl, C1-6 alkoxy-carbonyl, phenoxycarbonyl, amino, mono- or di-C1-6 alkylamino, formylamino, C1-6 alkyl-carbonylamino, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, sulfo, C1-6 alkylsulfonyl, benzoyl-C1-6 alkoxy, hydroxy-C1-6 alkoxy, C1-6 alkoxy-carbonyl-C1-6 alkoxy, C3-14 cycloalkyl-C1-6 alkoxy, imidazol-1-yl-C1-6 alkoxy, C7-14 aralkyloxy-carbonyl-C1-6 alkoxy, hydroxyphenyl-C1-6 alkoxy and C7-14 aralkyloxy-carbonyl, mono- or di-C1-6 alkylamino-C1-6 alkoxy and mono- or di-C1-6 alklamino-carbonyloxy, ring B may form, by combining with R2, bi-cyclic non-aromatic condensed nitrogen-containing heterocyclic ring which is formed by the condensation of benzene ring and the 5- or 6-membered monocyclic non-aromatic heterocyclic ring having 1 to 3 hetero atoms selected from nitrogen, oxygen and sulfur, which may have 1 to 4 substituents selected from halogen, C1-6 alkyl, halogeno-C1-6 alkyl, phenyl, benzyl, C1-6 alkoxy, halogeno-C1-6 alkoxy, phenoxy, C7-14 aralkyloxy, formyloxy, C1-6 alkyl-carbonyloxy, C1-6 alkylthio, halogeno-C1-6 alkylthio, hydroxy, mercapto, cyano, nitro, carboxy, formyl, C1-6 alkyl-carbonyl, benzoyl, C1-6 alkoxy-carbonyl, phenoxycarbonyl, amino, mono- or di-C1-6 alkylamino, formylamino, C1-6 alkyl-carbonylamino, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, sulfo, C1-6 alkylsulfonyl, benzoyl-C1-6 alkoxy, hydroxy-C1-6 alkoxy, C1-6 alkoxy-carbonyl-C1-6 alkoxy, C3-14cycloalkyl-C1-6 alkoxy, imidazol-1-yl-C1-6 alkoxy, C7-14 aralkyloxy-carbonyl-C1-6 alkoxy, hydroxyphenyl-C1-6 alkoxy and C7-14 aralkyloxy-carbonyl, Z is 1) a C3-14 cycloalkyl group, a C3-14 cycloalkenyl group, a C3-14 cycloalkadienyl group, an indanyl group or a C6-14 aryl group, a 5- or 6-membered monocyclic aromatic or non-aromatic heterocyclic ring having 1 to 4 hetero atoms selected from nitrogen, oxygen and sulfur in addition to carbon atoms, or a bi- or tri-cyclic aromatic condensed heterocyclic ring which is formed by the condensation of benzene ring and the said 5- or 6-membered monocyclic aromatic heterocyclic ring or these partial reduction, which may have 1 to 5 substituents selected from halogen, C1-6 alkyl, halogeno-C1-6 alkyl, phenyl, benzyl, C1-6 alkoxy, halogeno-C1-6 alkoxy, phenoxy, C7-14 aralkyloxy, formyloxy, C1-6 alkyl-carbonyloxy, C1-6 alkylthio, halogeno-C1-6 alkylthio, hydroxy, mercapto, cyano, nitro, carboxy, formyl, C1-6 alkyl-carbonyl, benzoyl, C1-6 alkoxy-carbonyl, phenoxycarbonyl, amino, mono- or di-C1-6 alkylamino, formylamino, C1-6 alkyl-carbonylamino, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, sulfo, C1-6 alkylsulfonyl, benzoyl-C1-6 alkoxy, hydroxy-C1-6 alkoxy, C1-6 alkoxy-carbonyl-C1-6 alkoxy, C3-14 cycloalkyl-C1-6 alkoxy, imidazol-1-yl-C1-6 alkoxy, C7-14 aralkyloxy-carbonyl-C1-6 alkoxy, hydroxyphenyl-C1-6 alkoxy, C7-14 aralkyloxy-carbonyl, oxo and thioxo, or 2) a C1-10 alkyl group, a C2-10 alkenyl group or a C2-10 alkynyl group, which may have 1 to 5 substituents selected from (1)halogen, (2)nitro, (3)cyano, (4)imino, (5)(i)amino which may have 1 to 2 substituents selected from C1-6 alkyl which may be substituted with 1 to 5 halogen, phenyl, benzyl, formyl, C1-6 alkyl-carbonyl, benzoyl, C16 alkoxy-carbonyl, C7-14 aralkyloxy-carbonyl, sulfo, C1-6 alkylsulfonyl and C1-6 alkylamino-carbonyl, (ii)pyrrolidinyl, (iii)piperidyl, (iv)morpholinyl, (v)thio-morpholinyl, (vi) 4-methylpiperidyl, (vii) 4-phenylpiperidyl, (viii)4-benzyloxycarbonylpiperidyl, (6)hydroxy which may have substituents selected from (i)C1-6 alkyl which may have 1 to 3 substituents selected from halogen, hydroxy, C16 alkoxy, formyl, C1-6 alkyl-carbonyl, carboxy, C1-6 alkoxy-carbonyl, amino, mono- or di-C1-6 alkylamino, pyrrolidinyl, piperidyl, morpholinyl, thio-morpholinyl, 4-methylpiperidyl, 4-phenylpiperidyl, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, phenoxy, mono- or di-C1-6 alkyl-carbamoyloxy, formylamino, C1-6 alkyl-carbonylamino, formyloxy and C1-6 alkyl-carbonyloxy, (ii)C6-10 aryl which may be have 1 to 5 substituents selected from halogen, hydroxy, C1-6 alkoxy, formyl, C1-6 alkyl-carbonyl, carboxy, C1-6 alkoxy-carbonyl, amino, mono- or di-C1-6 alkylamino, pyrrolidinyl, piperidyl, morpholinyl, thio-morpholinyl, 4-methylpiperidyl, 4-phenylpiperidyl, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, phenoxy, mono- or di-C1-6 alkyl-carbamoyloxy, formylamino, C1-6 alkyl-carbonylamino, formyloxy, C1-6 alkyl-carbonyloxy, C1-6 alkyl and halogeno-C1-6 alkyl, (iii)C714 aralkyl which may have 1 to 5 substituents selected from halogen, hydroxy, C1-6 alkoxy, formyl, C1-6 alkyl-carbonyl, carboxy, C1-6 alkoxy-carbonyl, amino, mono- or di-C1-6 alkylamino, pyrrolidinyl, piperidyl, morpholinyl, thio-morpholinyl, 4-methylpiperidyl, 4-phenylpiperidyl, carbamoyl, mono- or di-C1-6 alkylcarbamoyl, phenoxy, mono- or di-C1-6 alkyl-carbamoyloxy, formylamino, C1-6 alkyl-carbonylamino, formyloxy, C1-6 alkyl-carbonyloxy, C1-6 alkyl and halogeno-C1-6 alkyl and (iv)formyl, C1-6 alkyl-carbonyl, benzoyl, C1-6 alkoxy-carbonyl, benzyloxycarbonyl, C1-6 alkylsulfonyl, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, which may have 1 to 3 substitutents selected from halogen, hydroxy, C1-6 alkoxy, formyl, C1-6 alkyl-carbonyl, carboxy, C1-6 alkoxy-carbonyl, amino, mono- or di-C1-6 alkylamino, pyrrolidinyl, piperidyl, morpholinyl, thio-morpholinyl, 4-methylpiperidyl, 4-phenylpiperidyl, carbamoyl, mono- or di-C1-6 alkylcarbamoyl, phenoxy, mono- or di-C1-6 alkyl-carbamoyloxy, formylamino, C1-6 alkyl-carbonylamino, formyloxy and C1-6 alkyl-carbonyloxy, (7)carboxy which may be substituted with C1-6 alkyl, benzyl or mono- or di-C1-6 alkylamino, (8)C3-6 cycloalkyl, (9)C3-6 cycloalkenyl, (10)5- or 6-membered monocyclic aromatic heterocyclic ring having 1 to 4 hetero atoms selected from nitrogen, oxygen and sulfur in addition to carbon atoms or bi- or tri-cyclic aromatic condensed heterocyclic ring which is formed by the condensation of benzene ring and the said S- or 6-membered monocyclic aromatic heterocyclic ring, which may have 1 to 4 substituents selected from halogen, C1-6 alkyl, halogeno-C1-6 alkyl, phenyl, benzyl, C1-6 alkoxy, halogeno-C1-6 alkoxy, phenoxy, C7-14 aralkyloxy, formyloxy, C1-6 alkyl-carbonyloxy, C1-6 alkylthio, halogeno-C1-6 alkylthio, hydroxy, mercapto, cyano, nitro, carboxy, formyl, C1-6 alkyl-carbonyl, benzoyl, C1-6 alkoxy-carbonyl, phenoxycarbonyl, amino, mono- or di-C1-6 alkylamino, formylamino, C1-6 alkyl-carbonylamino, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, sulfo, C1-6 alkylsulfonyl, benzoyl-C1-6 alkoxy, hydroxy-C1-6 alkoxy, C1-6 alkoxy-carbonyl-C1-6 alkoxy, C3-14 cycloalkyl-C1-6 alkoxy, imidazol-1-yl-C1-6 alkoxy, C7-14 aralkyloxy-carbonyl-C1-6 alkoxy, hydroxyphenyl-C1-6 alkoxy and C7-14 aralkyloxy-carbonyl, (11)oxo and (12)pyrrolidinyl, R1 is 1) a hydrogen atom, 2) a C1-10 alkyl group, a C2-10 alkenyl group, a C2-10 alkynyl group, a C3-10 cycloalkyl group, a C3-10 cycloalkenyl group, a C5-10 cycloalkadienyl group, a C6-14 aryl group or a C7-14aralkyl group, which may have 1 to 5 substituents selected from (1)halogen, (2)nitro, (3)cyano, (4)imino, (5)(i)amino which may have 1 to 2 substituents selected from C1-6 alkyl which may have 1 to 5 substituents selected from halogen, phenyl, benzyl, formyl, C1-6 alkyl-carbonyl, benzoyl, C1-6 alkoxy-carbonyl, C7-14 aralkyloxy-carbonyl, sulfo, C1-6 alkylsulfonyl and C1-6 alkylamino-carbonyl, (ii)pyrrolidinyl, (iii)piperidyl, (iv)morpholinyl, (v)thio-morpholinyl, (vi)4-methylpiperidyl, (vii)4-phenylcarbonylpiperidyl, (viii)4-benzyloxycarbonylpiperidyl,(6)hydroxy which may have substituents selected from (i)C1-6 alkyl which may have 1 to 3 substituents selected from halogen, hydroxy, C1-6 alkoxy, formyl, C1-6 alkyl-carbonyl, carboxy, C1-6 alkoxy-carbonyl, amino, mono- or di-C1-6 alkylamino, pyrrolidinyl, piperidyl, morpholinyl, thio-morpholinyl, 4-methylpiperidyl, 4-phenylpiperidyl, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, phenoxy, mono- or di-C1-6 alkyl-carbamoyloxy, formylamino, C1-6 alkyl-carbonylamino, formyloxy and C1-6 alkyl-carbonyloxy, (ii)C6-10 aryl which may have 1 to 5 substituents selected from halogen, hydroxy, C1-6 alkoxy, formyl, C1-6 alkyl-carbonyl, carboxy, C1-6 alkoxy-carbonyl, amino, mono- or di-C1-6 alkylamino, pyrrolidinyl, piperidyl, morpholinyl, thio-morpholinyl, 4-methylpiperidyl, 4-phenylpiperidyl, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, phenoxy, mono- or di-C1-6 alkyl-carbamoyloxy, formylamino, C1-6 alkyl-carbonylamino, formyloxy, C1-6 alkyl-carbonyloxy, C1-6 alkyl and halogeno-C1-6 alkyl, (iii)C7-14 aralkyl which may have 1 to 5 substituents selected from halogen, hydroxy, C1-6 alkoxy, formyl, C1-6 alkyl-carbonyl, carboxy, C1-6 alkoxy-carbonyl, amino, mono- or di-C1-6 alkylamino, pyrrolidinyl, piperidyl, morpholinyl, thio-morpholinyl, 4-methylpiperidyl, 4-phenylpiperidyl, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, phenoxy, mono- or di-C1-6 alkyl-carbamoyloxy, formylamino, C1-6 alkyl-carbonylamino, formyloxy, C1-6 alkyl-carbonyloxy, C1-6 alkyl and halogeno-C1-6 alkyl and (iv)formyl, C1-6 alkyl-carbonyl, benzoyl, C1-6 alkoxy-carbonyl, benzyloxycarbonyl, C1-6 alkylsulfonyl, carbamoyl or mono- or di-C1-6 alkyl-carbamoyl, which may have 1 to 3 substitutents selected from halogen, hydroxy, C1-6 alkoxy, formyl, C1-6 alkyl-carbonyl, carboxy, C1-6 alkoxy-carbonyl, amino, mono- or di-C1-6 alkylamino, pyrrolidinyl, piperidyl, morpholinyl, thio-morpholinyl, 4-methylpiperidyl, 4-phenylpiperidyl, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, phenoxy, mono- or di-C1-6 alkyl-carbamoyloxy, formylamino, C1-6 alkyl-carbonylamino, formyloxy and C1-6 alkyl-carbonyloxy, (7)carboxy which may be substituted with C1-6 alkyl, benzyl or mono- or di-C1-6 alkylamino, (8)C3-6 cycloalkyl, (9)C3-6 cycloalkenyl, (10)5- or 6-membered monocyclic aromatic heterocyclic ring having 1 to 4 hetero atoms selected from nitrogen, oxygen and sulfur in addition to carbon atoms or bi- or tri-cyclic aromatic condensed heterocyclic ring which is formed by the condensation of benzene ring and the said 5- or 6-membered monocyclic aromatic heterocyclic ring, which may have 1 to 4 substituents selected from halogen, C1-6 alkyl, halogeno-C1-6 alkyl, phenyl, benzyl, C1-6 alkoxy, halogeno-C1-6 alkoxy, phenoxy, C7-4 aralkyloxy, formyloxy, C1-6 alkyl-carbonyloxy, C1-5 alkylthio, halogeno-C1-6 alkylthio, hydroxy, mercapto, cyano, nitro, carboxy, formyl, C1-6 alkyl-carbonyl, benzoyl, C1-6 alkoxy-carbonyl, phenoxycarbonyl, amino, mono- or di-C1-6 alkylamino, formylamino, C1-6 alkyl-carbonylamino, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, sulfo, C1-6 alkylsulfonyl, benzoyl-C1-6 alkoxy, hydroxy-C1-6 alkoxy, C1-6 alkoxy-carbonyl-C1-6 alkoxy, C3-14 cycloalkyl-C1-6 alkoxy, imidazol-1-yl-C1-6 alkoxy, C7-14 aralkyloxy-carbonyl-C1-6 alkoxy, hydroxyphenyl-C1-6 alkoxy and C7-14 aralkyloxy-carbonyl, and in addition to these substituents, a C6-14 aryl group or a C7-14 aralkyl group which may have 1 to 5 substituents selected from C1-6 alkyl, halogeno-C1-6 alkyl and C6-14 aryl which may have 1 to 5 substituents selected from halogen, C1-6 alkyl, halogeno-C1-6 alkyl, C1-6 alkoxy, C7-14 aralkyloxy, hydroxy, amino, mono- or di-C1-6 alkylmino, carboxy, C1-6 alkyl-carbonyl, C1-6 alkoxy-carbonyl, nitro and cyano, or 3) 5- or 6-membered monocyclic aromatic heterocyclic ring having 1 to 4 hetero atoms selected from nitrogen, oxygen and sulfur in addition to carbon atoms or bi- or tri-cyclic aromatic condensed heterocyclic ring which is formed by the condensation of benzene ring and the said 5- or 6-membered monocyclic aromatic heterocyclic ring, which may have 1 to 4 substituents selected from halogen, C16 alkyl, halogeno-C1-6 alkyl, phenyl, benzyl, C1-6 alkoxy, halogeno-C1-6 alkoxy, phenoxy, C7-14 aralkyloxy, formyloxy, C1-6 alkyl-carbonyloxy, C1-6 alkylthio, halogeno-C1-6 alkylthio, hydroxy, mercapto, cyano, nitro, carboxy, formyl, C1-6 alkyl-carbonyl, benzoyl, C1-6 alkoxy-carbonyl, phenoxycarbonyl, amino, mono- or di-C1-6 alkylamino, formylamino, C1-6 alkyl-carbonylamino, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, sulfo, C1-6 alkylsulfonyl, benzoyl-C1-6 alkoxy, hydroxy-C1-6 alkoxy, C1-6 alkoxy-carbonyl-C1-6 alkoxy, C3-4 cycloalkyl-C1-6 alkoxy, imidazol-1-yl-C1-6 alkoxy, C7-14 aralkyloxy-carbonyl-C1-6 alkoxy, hydroxyphenyl-C1-6 alkoxy and C7-14 aralkyloxy-carbonyl, R2 is (A) an unsubstituted amino group, (B) an amino group which have 1 to 2 substitutents selected from 1) a C1-10 alkyl group, a C2-10alkenyl group, a C2-10-alkynyl group, a C3-10 cycloalkyl group, a C3-10 cycloalkenyl group, a C5-10 cycloalkadienyl group, a C6-14 aryl group or a C7-14aralkyl group, which may have 1 to 5 substituents selected from (1)halogen, (2)nitro, (3)cyano, (4)imino, (5)(i)amino which may have 1 to 2 substituents selected from C1-6 alkyl which may be substituted with 1 to 5 halogen, phenyl, benzyl, formyl, C1-6 alkyl-carbonyl, benzoyl, C1-6 alkoxy-carbonyl, C7-14 aralkyloxy-carbonyl, sulfo, C1-6 alkylsulfonyl and C1-6 alkylamino-carbonyl, (ii)pyrrolidinyl, (iii)piperidyl, (iv)morpholinyl, (v) thio-morpholinyl, (vi) 4-methylpiperidyl, (vii)4-phenylpiperidyl, (viii)4-benzyloxycarbonylpiperidyl, (6)hydroxy which may have substituents selected from (i)C1-6 alkyl which may have 1 to 3 substituents selected from halogen, hydroxy, C1-6 alkoxy, formyl, C1-6 alkyl-carbonyl, carboxy, C1-6 alkoxy-carbonyl, amino, mono- or di-C1-6 alkylamino, pyrrolidinyl, piperidyl, morpholinyl, thio-morpholinyl, 4-methylpiperidyl, 4-phenylpiperidyl, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, phenoxy, mono- or di-C1-6 alkyl-carbamoyloxy, formylamino, C1-6 alkyl-carbonylamino, formyloxy and C1-6 alkyl-carbonyloxy, (ii)C6-10 aryl which may have 1 to 5 substituents selected from halogen, hydroxy, C1-6 alkoxy, formyl, C1-6 alkyl-carbonyl, carboxy, C1-6 alkoxy-carbonyl, amino, mono- or di-C1-6 alkylamino, pyrrolidinyl, piperidyl, morpholinyl, thio-morpholinyl, 4-methylpiperidyl, 4-phenylpiperidyl, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, phenoxy, mono- or di-C1-6 alkyl-carbamoyloxy, formylamino, C1-6 alkyl-carbonylamino, formyloxy, C1-6 alkyl-carbonyloxy, C1-6 alkyl and halogeno-C1-6 alkyl, (iii)C7-14 aralkyl which may have 1 to 5 substituents selected from halogen, hydroxy, C1-6 alkoxy, formyl, C1-6 alkyl-carbonyl, carboxy, C1-6 alkoxy-carbonyl, amino, mono- or di-C1-6 alkylamino, pyrrolidinyl, piperidyl, morpholinyl, thio-morpholinyl, 4-methylpiperidyl, 4-phenylpiperidyl, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, phenoxy, mono- or di-C1-6 alkyl-carbamoyloxy, formylamino, C1-6 alkyl-carbonylamino, formyloxy, C1-6 alkyl-carbonyloxy, C1-6 alkyl and halogeno-C1-6 alkyl and (iv)formyl, C1-6 alkyl-carbonyl, benzoyl, C1-6 alkoxy-carbonyl, benzyloxycarbonyl, C1-6 alkylsulfonyl, carbamoyl or mono- or di-C1-6 alkyl-carbamoyl, which may have 1 to 3 substitutents selected from halogen, hydroxy, C1-6 alkoxy, formyl, C1-6 alkyl-carbonyl, carboxy, C1-6 alkoxy-carbonyl, amino, mono- or di-C1-6 alkylamino, pyrrolidinyl, piperidyl, morpholinyl, thio-morpholinyl, 4-methylpiperidyl, 4-phenylpiperidyl, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, phenoxy, mono- or di-C1-6 alkyl-carbamoyloxy, formylamino, C1-6 alkyl-carbonylamino, formyloxy and C1-6 alkyl-carbonyloxy, (7)carboxy which may be substituted with C1-6 alkyl, benzyl or mono- or di-C1-6 alkylamino, (8)C3-6 cycloalkyl, (9)C3-6 cycloalkenyl, (10)5- or 6-membered monocyclic aromatic heterocyclic ring having 1 to 4 hetero atoms selected from nitrogen, oxygen and sulfur in addition to carbon atoms or bi- or tri-cyclic aromatic condensed heterocyclic ring which is formed by the condensation of benzene ring and the said 5- or 6-membered monocyclic aromatic heterocyclic ring, which may have 1 to 4 substituents selected from halogen, C1-6 alkyl, halogeno-C1-6 alkyl, phenyl, benzyl, C1-6 alkoxy, halogeno-C1-6 alkoxy, phenoxy, C7-14 aralkyloxy, formyloxy, C1-6 alkyl-carbonyloxy, C1-6 alkylthio, halogeno-C1-6 alkylthio, hydroxy, mercapto, cyano, nitro, carboxy, formyl, C1-6 alkyl-carbonyl, benzoyl, C1-6 alkoxy-carbonyl, phenoxycarbonyl, amino, mono- or di-C1-6 alkylamino, formylamino, C1-6 alkyl-carbonylamino, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, sulfo, C1-6 alkylsulfonyl, benzoyl-C1-6 alkoxy, hydroxy-C1-6 alkoxy, C1-6 alkoxy-carbonyl-C1-6 alkoxy, C3-14 cycloalkyl-C1-6 alkoxy, imidazol-1-yl-C1-6 alkoxy, C7-14 aralkyloxy-carbonyl-C1-6 alkoxy, hydroxyphenyl-C1-6 alkoxy and C7-14 aralkyloxy-carbonyl, and in addition to these substituents, a C6-14 aryl group or a C7-14 aralkyl group which may have 1 to 5 substituents selected from C1-6 alkyl, halogeno-C1-6 alkyl and C1-4 aryl which may have 1 to 5 substituents selected from halogen, C1-6 alkyl, halogeno-C1-6 alkyl, C1-6 alkoxy, C7-14 aralkyloxy, hydroxy, amino, mono- or di-C1-6 alkylmino, carboxy, C1-6 alkyl-carbonyl, C1-6 alkoxy-carbonyl, nitro and cyano, 2) 5- or 6-membered monocyclic heterocyclic ring having 1 to 4 hetero atoms selected from nitrogen, oxygen and sulfur in addition to carbon atoms or bi- or tri-cyclic condensed heterocyclic ring which is formed by the condensation of benzene ring and the said 5- or 6-membered monocyclic heterocyclic ring, which may have 1 to 4 substituents selected from halogen, C1-6 alkyl, halogeno-C1-6 alkyl, phenyl, benzyl, C1-6 alkoxy, halogeno-C1-6 alkoxy, phenoxy, C7-14 aralkyloxy, formyloxy, C1-6 alkyl-carbonyloxy, C1-6 alkylthio, halogeno-C1-6 alkylthio, hydroxy, mercapto, cyano, nitro, carboxy, formyl, C1-6 alkyl-carbonyl, benzoyl, C1-6 alkoxy-carbonyl, phenoxycarbonyl, amino, mono- or di-C1-6 alkylamino, formylamino, C1-6 alkyl-carbonylamino, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, sulfo, C1-6 alkylsulfonyl, benzoyl-C1-6 alkoxy, hydroxy-C1-6 alkoxy, C1-6 alkoxy-carbonyl-C1-6 alkoxy, C3-14cycloalkyl-C1-6 alkoxy, imidazol-1-yl-C1-6 alkoxy, C7-14 aralkyloxy-carbonyl-C1-6 alkoxy, hydroxyphenyl-C1-6 alkoxy and C7-14 aralkyloxy-carbonyl and 3) formyl, C1-6 alkyl-carbonyl, benzoyl, C1-6 alkoxy-carbonyl, C7-14 aralkyloxy-carbonyl, piperidin-4-ylcarbonyl, C1-6 alkylsulfonyl, carbamoyl or mono- or di-C1-6 alkyl-carbamoyl, which may have 1 to 3 substitutents selected from halogen, hydroxy, C1-6 alkoxy, formyl, C1-6 alkyl-carbonyl, carboxy, C1-6 alkoxy-carbonyl, amino, mono- or di-C1-6 alkylamino, pyrrolidinyl, piperidyl, morpholinyl, thio-morpholinyl, 4-methylpiperidyl, 4-phenylpiperidyl, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, phenoxy, mono- or di-C1-6 alkyl-carbamoyloxy, formylamino, C1-6 alkyl-carbonylamino, formyloxy and C1-6 alkyl-carbonyloxy, or (C) 5 to 7-membered nitrogen-containing heterocyclic group having 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur or condensed nitrogen-containing heterocyclic group which is formed by the condensation of the said 5 to 7-membered nitrogen-containing heterocyclic ring and benzene or pyridine, which may have 1 to 4 substituents selected from halogen, C1-6 alkyl, halogeno-C1-6 alkyl, phenyl, benzyl, C1-6 alkoxy, halogeno-C1-6 alkoxy, phenoxy, C7-14 aralkyloxy, formyloxy, C1-6 alkyl-carbonyloxy, C1-6 alkylthio, halogeno-C1-6 alkylthio, hydroxy, mercapto, cyano, nitro, carboxy, formyl, C1-6 alkyl-carbonyl, benzoyl, C1-6 alkoxy-carbonyl, phenoxycarbonyl, amino, mono- or di-C1-6 alkylamino, formylamino, C1-6 alkyl-carbonylamino, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, sulfo, C1-6 alkylsulfonyl, benzoyl-C1-6 alkoxy, hydroxy-C1-6 alkoxy, C1-6 alkoxy-carbonyl-C1-6 alkoxy, C3-14 cycloalkyl-C1-6 alkoxy, imidazol-1-yl-C1-6 alkoxy, C7-14 aralkyloxy-carbonyl-C1-6 alkoxy, hydroxyphenyl-C1-6 alkoxy and C7-14 aralkyloxy-carbonyl, D is a bond, or a C1-10 alkylene group which may have C3-6 cycloalkylene or phenylene and may have 1 to 3 substituents selected from C1-6 alkyl, halogeno-C1-6 alkyl, phenyl and benzyl, E is a bond, â€”CON(Ra), â€”N(Ra)COâ€”, â€”N(Rb)CON(Rc)â€”, â€”N(Rd)COOâ€”, â€”N(Re)SO2â€”, â€”COOâ€”, â€”N(Rf)â€”, â€”Oâ€”, â€”Sâ€” â€”SOâ€”, â€”SO2â€”, in which Ra, Rb, Rc, Rd, Re and Rf are respectively a hydrogen atom or a C1-10 alkyl group, a C2-10 alkenyl group, a C2-10 alkynyl group, a C3-10 cycloalkyl group, a C3-10 cycloalkenyl group, a C5-10 cycloalkadienyl group, a C6-14 aryl group or a C7-14 aralkyl group, which may have 1 to 5 substituents selected from (1)halogen, (2)nitro, (3)cyano, (4)imino, (5)(i)amino which may have 1 to 2 substituents selected from C1-6 alkyl which may have 1 to 5 substituents selected from halogen, phenyl, benzyl, formyl, C1-6 alkyl-carbonyl, benzoyl, C1-6 alkoxy-carbonyl, C7-14 aralkyloxy-carbonyl, sulfo, C1-6 alkylsulfonyl and C1-6 alkylamino-carbonyl, (ii)pyrrolidinyl, (iii)piperidyl, (iv)morpholinyl, (v)thio-morpholinyl, (vi) 4-methylpiperidyl, (vii) 4-phenylpiperidyl, (viii)4-benzyloxycarbonylpiperidyl, (6)hydroxy which may have substituents selected from (i)C1-6 alkyl which may have 1 to 3 substituents selected from halogen, hydroxy, C1-6 alkoxy, formyl, C1-6 alkyl-carbonyl, carboxy, C1-6 alkoxy-carbonyl, amino, mono- or di-C1-6 alkylamino, pyrrolidinyl, piperidyl, morpholinyl, thio-morpholinyl, 4-methylpiperidyl, 4-phenylpiperidyl, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, phenoxy, mono- or di-C1-6 alkyl-carbamoyloxy, formylamino, C1-6 alkyl-carbonylamino, formyloxy and C1-6 alkyl-carbonyloxy, (ii)C6-10 aryl which may have 1 to 5 substituents selected from halogen, hydroxy, C1-6 alkoxy, formyl, C1-6 alkyl-carbonyl, carboxy, C1-6 alkoxy-carbonyl, amino, mono- or di-C1-6 alkylamino, pyrrolidinyl, piperidyl, morpholinyl, thio-morpholinyl, 4-methylpiperidyl, 4-phenylpiperidyl, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, phenoxy, mono- or di-C1-6 alkyl-carbamoyloxy, formylamino, C1-6 alkyl-carbonylamino, formyloxy, C1-6 alkyl-carbonyloxy, C1-6 alkyl and halogeno-C1-6 alkyl, (iii)C7-14 aralkyl which may have 1 to 5 substituents selected from halogen, hydroxy, C1-6 alkoxy, formyl, C1-6 alkyl-carbonyl, carboxy, C1-6 alkoxy-carbonyl, amino, mono- or di-C1-6 alkylamino, pyrrolidinyl, piperidyl, morpholinyl, thio-morpholinyl, 4-methylpiperidyl, 4-phenylpiperidyl, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, phenoxy, mono- or di-C1-6 alkyl-carbamoyloxy, formylamino, C1-6 alkyl-carbonylamino, formyloxy, C1-6 alkyl-carbonyloxy, C1-6 alkyl and halogeno-C1-6 alkyl and (iv)formyl, C1-6 alkyl-carbonyl, benzoyl, C1-6 alkoxy-carbonyl, benzyloxycarbonyl, C1-6 alkylsulfonyl, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, which may have 1 to 3 substitutents selected from halogen, hydroxy, C1-6 alkoxy, formyl, C1-6 alkyl-carbonyl, carboxy, C1-6 alkoxy-carbonyl, amino, mono- or di-C1-6 alkylamino, pyrrolidinyl, piperidyl, morpholinyl, thio-morpholinyl, 4-methylpiperidyl, 4-phenylpiperidyl, carbamoyl, mono- or di-C1-6 alkylcarbamoyl, phenoxy, mono- or di-C1-6 alkyl-carbamoyloxy, formylamino, C1-6 alkyl-carbonylamino, formyloxy and C1-6 alkyl-carbonyloxy, (7)carboxy which may be substituted with C1-6 alkyl, benzyl or mono- or di-C1-6 alkylamino, (8)C3-6 cycloalkyl, (9)C3-6 cycloalkenyl, (10)5- or 6-membered monocyclic aromatic heterocyclic ring having 1 to 4 hetero atoms selected from nitrogen, oxygen and sulfur in addition to carbon atoms or bi- or tri-cyclic aromatic condensed heterocyclic ring which is formed by the condensation of benzene ring and the said 5- or 6-membered monocyclic aromatic heterocyclic ring, which may have 1 to 4 substituents selected from halogen, C1-6 alkyl, halogeno-C1-6 alkyl, phenyl, benzyl, C1-6 alkoxy, halogeno-C1-6 alkoxy, phenoxy, C7-14 aralkyloxy, formyloxy, C1-6 alkyl-carbonyloxy, C1-6 alkylthio, halogeno-C1-6 alkylthio, hydroxy, mercapto, cyano, nitro, carboxy, formyl, C1-6 alkyl-carbonyl, benzoyl, C1-6 alkoxy-carbonyl, phenoxycarbonyl, amino, mono- or di-C1-6 alkylamino, formylamino, C1-6 alkyl-carbonylamino, carbamoyl, mono- or di-C1-6 alkyl-carbamoyl, sulfo, C1-6 alkylsulfonyl, benzoyl-C1-6 alkoxy, hydroxy-C1-6 alkoxy, C1-6 alkoxy-carbonyl-C1-6 alkoxy, C3-14 cycloalkyl-C1-6 alkoxy, imidazol-1-yl-C1-6 alkoxy, C7-14 aralkyloxy-carbonyl-C1-6 alkoxy, hydroxyphenyl-C1-6 alkoxy and C7-14 aralkyloxy-carbonyl, and in addition to these substituents, a C6-14 aryl group or a C7-14 aralkyl group which may have 1 to 5 substituents selected from C1-6 alkyl, halogeno-C1-6 alkyl and C6-14 aryl which may have 1 to 5 substituents selected from halogen, C1-6 alkyl, halogeno-C1-6 alkyl, C1-6 alkoxy, C7-14 aralkyloxy, hydroxy, amino, mono- or di-C1-6 alkylmino, carboxy, C1-6 alkyl-carbonyl, C1-6 alkoxy-carbonyl, nitro and cyano,G is a bond, or a C1-10 alkylene group which may have C3-6 cycloalkylene or phenylene and may have 1 to 3 substituents selected from C1-6 alkyl, halogeno-C1-6 alkyl, phenyl and benzyl, L is a C1-10 alkylene group which may be mediated by â€”Oâ€” or â€”Sâ€”, may have C3-6 cycloalkylene or phenylene and may have 1 to 3 substituents selected from C1-6 alkyl, halogeno-C1-6 alkyl, phenyl and benzyl, X is two hydrogen atoms, an oxygen atom or a sulfur atom,  is a single bond, and Y is an oxygen atom, or a salt thereof.