| abstract |
A compound of Formula I, (See formula) in which R is H or C1-C6 alkyl; R1 is H, COOR, C3-C8 cycloalkyl, or C1-C6 alkyl, C2-C6 alkenyl, or C1-C6 alkoxy each of which may be unsubstituted or substituted with fluoro, methylenedioxyphenyl, or phenyl which may be unsubstituted or substituted with R6; R2 is H, halo, or C1-C6 alkyl which may be unsubstituted or substituted with C1-C6 alkoxy, oxo, fluoro, or R2 is phenyl, furyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl , triazolyl, oxadiazolyl, thiadiazolyl, tetrazolyl, pyridyl, pyrrolidinyl, piperidinyl, tetrahydropyranyl, tetrahydrothiopyranyl, piperazinyl, or morpholinyl, each of which may be unsubstituted or substituted with R6; R3 is H, C1-C6 alkyl, or phenyl which may be unsubstituted or substituted with R6; X is O or S; R4 is C1-C6 alkyl or C3-C8 cycloalkyl, any of which may be unsubstituted or substituted with fluoro, oxo, or C1-C6 alkoxy which may be unsubstituted or substituted with C1-C6 alkoxy, or phenyl optionally substituted with R6, or any of which may be substituted with phenyl, naphthyl, furyl, thienyl, pyrrolyl, tetrahydrofuryl, pyrrolidinyl, pyrrolinyl, tetrahydrothienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, triazolyl, oxadiazolyl, tetrazolyl, tetrazolyl, tetrazolyl , piperidinyl, tetrahydropyranyl, tetrahydrothiopyranyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperazinyl, morpholinyl, benzofuryl, dihydrobenzofuryl, benzothienyl, dihydrobenzothienyl, indolyl, indolinyl, indazolyl, benzoxazolyl, benzothiazolyl, benzimidazolyl, benzisoxazolyl, benzisothiazolyl, benzodioxolyl, quinolyl, isoquinolyl, quinazolinyl, quinoxazolinyl , dihydrobenzopyranyl, dihydrobenzothiopyranyl, or 1,4-benzodioxanyl, each or of which it may be unsubstituted or substituted with R6, or C1-C6 alkyl may also be substituted with C3-C8 cycloalkyl or with phenoxy which may be unsubstituted or substituted with R6 or with phenyl, naphthyl, furyl, thienyl, pyrrolyl , tetrahydrofuryl, pyrrolidinyl, pyrrolinyl, tetrahydrothienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, triazolyl, oxadiazolyl, thiadiazolyl, tetrazolyl, pyridyl, piperidinyl, tetrahydropyranyl, tetrahydrothiopyranyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperazinyl, morpholinyl, benzofuryl, dihydrobenzofuryl , benzothienyl, dihydrobenzothienyl, indolyl, indolinyl, indazolyl, benzoxazolyl, benxothiazolyl, benzimidazolyl, bencisoxazolyl, bencisothiazolyl, benzodioxolyl, quinolyl, isoquinolyl, quinazolinyl, quinoxazolinyl, dihydrobenzyl, dihydrobenzylbenzyl, dihydrobenzylbenzyl, dihydrobenzylbenzyl, dihydrobenzylbenzyl, dihydrobenzylbenzyl, dihydrobenzylbenzyl, dihydrobenzylbenzyl, dihydrobenzylbenzyl, dihydrobenzylbenzyl, dihydrobenzylthio, benzyl dihydrobenzyl, benzyl dihydrobenzyl, and dihydrobenzylbenzene substituted or substituted with R6, or R4 is phenyl, naphthyl, furi so, thienyl, pyrrolyl, tetrahydrofuryl, pyrrolidinyl, pyrrolinyl, tetrahydrothienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, triazolyl, oxadiazolyl, thiadiazolyl, tetrazolyl, pyridyl, piperidinyl, tetrahydropyranyl, tetrahydrothiopyranyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperazinyl, morpholinyl, benzofuryl, dihydrobenzofuryl, benzothienyl, dihydrobenzothienyl, indolyl, indolinyl, indazolyl, benzoxazolyl, benxotiazolilo, benzimidazolyl, benzisoxazolyl, benzisothiazolyl, benzodioxolyl, quinolyl, isoquinolyl, quinazolinyl, quinoxazolinyl, dihydrobenzopyranyl, dihydrobenzothiopyranyl, or 1,4-benzodioxanyl, each of which may be unsubstituted or substituted with R 6, or with phenyl, furyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, Isothiazolyl, triazolyl, oxadiazolyl, thiadiazolyl, tetrazolyl, pyridyl, pyrrolidinyl, piperidinyl, tetrahydropyranyl, tetrahydrothiranyl , pi perazinyl, morpholinyl, benzodioxolyl, dihydrobenzofuranyl, indolyl, pyrimidinyl or phenoxy, each of which may be unsubstituted or substituted with R6; R5 is H, halo or C1-C6 alkyl optionally substituted with oxo; R6 is halo, CF3, C1-C6 alkyl optionally substituted with oxo or hydroxy, or C1-C6 alkoxy optionally substituted with fluoro; and pharmaceutically acceptable salts and esters. |