| abstract |
The compound of the formula: ** see formula ** in which Y is -NH-, -O-, or - (CH2) 1-5-; Y2 is -C (= O) -NH- or -NH-C (= O) -; Y3 is a single bond or optionally substituted C1-C12 alkylene; Ra is optionally substituted C6-C14 aryl, optionally substituted C3-C7 cycloalkyl, optionally substituted C3-C12 cycloalkenyl, optionally substituted heteroaryl selected from furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, oxazolyl, isoxazolyl, thiazolyl, thiazolyl , isothiazolyl, pyridyl, pyridazinyl, pyrimidinyl, furazanyl, pyrazinyl, oxadiazolyl, benzofuryl, benzothienyl, benzimidazolyl, dibenzofuryl, benzoxazolyl, quinoxalyl, cinnolyl, quinazolyl, quinolyl, phthalazinyl, isoquinolyl, puryl, pteridinyl, carbazolyl, phenanthridinyl, acridinyl, indolyl, isoindolyl , optionally substituted phenazinyl and phenotiadinyl or heterocycle selected from 1-pyrrolinyl, 2-pyrrolinyl, 3-pyrrolinyl, pyrrolidino, 2-pyrrolidinyl, 3-pyrrolidinyl, 1-imidazolinyl, 2-imidazolinyl, 4-imidazolinyl, 1-2-imidazolidinyl -imidazolidinyl, 4-imidazolidinyl, 1-pyrazolinyl, 3-pyrazolinyl, 4- pyrazolinyl, 1-pyrazolidinyl , 3-pyrazolidinyl, 4-pyrazolidinyl, piperidino, 2-piperidyl, 3-piperidyl, 4-piperidyl, piperazino, 2-piperazinyl, 2-morpholinyl, 3-morpholinyl, morpholino and tetrahydropyranyl; R5 is C3-C12 alkyl or a group represented by the formula: -Y6-Re in which Y6 is C1-C12 alkylene; Re is optionally substituted C6-C14 aryl, optionally substituted C3-C7 cycloalkyl, optionally substituted heteroaryl selected from furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, oxazolyl, isoxazolyl, thiazolyl, thiadiazolyl, isothiazolyl, pyridyl, pyridyl, pyridyl pyrimidinyl, furazanyl, pyrazinyl, oxadiazolyl, benzofuryl, benzothienyl, benzimidazolyl, dibenzofuryl, benzoxazolyl, quinoxalyl, cinnolyl, quinazolyl, quinolyl, phthalazinyl, isoquinolyl, puryl, pteridinyl, carbazolyl, phenanthridinyl, acridinyl, indolyl, isoindolyl, phenazinyl and fenotiadinilo, or heterocycle optionally substituted selected from 1-pyrrolinyl, 2-pyrrolinyl, 3-pyrrolinyl, pyrrolidino, 2- pyrkolidinyl, 3-pyrrolidinyl, 1-imidazolinyl, 2-imidazolinyl, 4-imidazolinyl, 1-imidazolidinyl, 2-imidazolidinyl, 4-imidazolidinyl , 1-pyrazolinyl, 3-pyrazolinyl, 4-pyrazolinyl, 1-pyrazolidinyl, 3-pyrazolidinyl, 4-pyrazolidinyl, piperidine or, 2-piperidyl, 3-piperidyl, 4-piperidyl, piperazino, 2-piperazinyl, 2-morpholinyl, 3-morpholinyl, morpholino and tetrahydropyranyl; a pharmaceutically acceptable salt or solvate thereof in which the optionally substituted C1-C12 alkylene, C6-C14 aryl, C3-C7 cycloalkyl, C3-C12 cycloalkenyl, heteroaryl or heterocycle may optionally be substituted with hydroxy, carboxy, halogen, alkyl Halogenated C1-C12, C1-C12 alkyl, C2-C12 alkenyl, formyl, acetyl, propionyl, butyryl, pivaloyl, benzoyl, pyridinecarbonyl, cyclopentanecarbonyl, cyclohexanecarbonyl, C2-C12 alkynyl, C3-C7 cycloalkenyl, C3-C12 alkoxy - C12, C1-C12 alkoxycarbonyl, nitro, nitroso, oxo, amino, C1-C12 alkylamino, formylamino, acetylamino, benzoylamino, benzylamino, tritylamino, hydroxyamino, C1-C12 alkylsulfonylamino, C1-C12 alkenyloxycarbonylamino C1-C12 alkylamino -C12, C6-C14 arylcarbonylamino, heteroarylcarbonylamino, azide, C6-C14 aryl, C6-C14 aryloxy, benzyl, phenethyl, phenylpropyl, methylenedioxy, methylene, ethylene, trimethylene, tetramethylene, pentamethylene, propeni Lena, butenylene, butadienylene, cyano, isocyanate, isocyanate, thiocyanate, isothiocyanate, mercapto, C1-C12 thioalkyl, C1-C12 alkylsulfonyl, C6-C14 arylsulfonyl, carbamoyl, N-methylcarbamoyl, N-ethylcarbamoyl, oxamoofophloyl, sulfamoyl, sulfamoyl, sulfamoyl, sulfamoyl, sulfamoyl, sulfamoyl, sulfamoyl, sulfamoyl, sulfamoyl, sulfamoyl, sulfamoyl, sulfamoyl, sulfamoyl, sulfamoyl, sulfamoyl, sulfamoyl, sulfamoyl, formol , thioformyl, thiocarboxy, dithiocarboxy, thiocarbamoyl, sulfino, sulfo, sulfoamino, hydrazido, ureido, amidino, guanidino, C1-C12 alkylsulfonyloxy, tri (C1-C12 alkyl) silyloxy, C1-C12 alkoxycarbonyloxy, thioacyloxy, thioacyloxy, thioacyloxy, thioacyloxy, thioacyloxy, thioacyloxy, thioacyloxy, thioacyloxy, thioacyloxy, thioacyloxy, thioacyloxy. |