Patent ID: 6576628
Filing Date: 2003-06-10
Classification: A61P,C07C

Abstract:
A compound of formula (I) whereinR is selected from the group consisting of a straight-chained or branched, saturated or unsaturated residue containing 1 to 8 carbon atoms which is uninterrupted or interrupted by 1 or 2 heteroatoms selected from the group consisting of O, N and S, cyclopentyl, cyclohexyl, cycloheptyl, morpholinyl, thiamorpholinyl, piperidinyl, piperazinyl, tetrahydrofiuyl, tetrahydropyranyl, phenyl, naphthyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, imidazolyl, furanyl, oxazolyl, isothiazolyl, isooxazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, thiazolyl, indolyl, tetrahydronaphthyl, decalinyl, quinolyl, isoquinolyl, tetrahydroquinolyl, tetrahydroisoquinolyl, benzimidazolyl, indazolyl, oxindolyl, benzofuranyl, benzothienyl, benzthiazolyl, benzoxazolyl, purinyl, phenoxy, naphthoxy, pyridinyl-oxy, pyrimidinyl-oxy, pyridazinyl-oxy, pyrazinyl-oxy, imidazolyl-oxy, furanyl-oxy, oxazolyl-oxy, isothiazolyl-oxy, isooxazolyl-oxy, 1,2,3-triazolyl-oxy, 1,2,4-triazolyl-oxy, thiazolyl-oxy, indolyl-oxy, tetrahydronaphthoxy, decalinyl-oxy, quinolinyl-oxy, isoquinolinyl-oxy, tetrahydroquinolinyl-oxy, tetrahydroisoquinolinyl-oxy, benzimidazolyl-oxy, indazolyl-oxy, oxindolyl-oxy, benzofuranyl-oxy, benzothienyl-oxy, benzthiazolyl-oxy, benzoxazolyl-oxy, purinyl-oxy, phenyl-C1-C2 alkyl and naphthyl-C1-C2 alkyl, wherein the residues for R listed above are each independently unsubstituted or substituted with 1-3 substituents each independently selected from the group consisting of halogen, hydroxy, mercapto, C1-C3 alkyl, C3-C8 cycloalkyl, C4-C8 cycloalkenyl, hydroxy-C1-C3 alkyl, C1-C3 alkoxy, hydroxy-C1-C3 alkoxy, chloro-C1-C3 alkoxy, C1-C3 alkylmercapto, C1-C3 alkylsulfinyl, C1-C3 alkylsulfonyl, amino, C1-C3 alkylamino, di-C1-C3-alkylamino, nitro, carboxyl, carboxamido, C1-C3 alkoxycarbonyl, C1-C3 alkoxycarbonyl-C1-C3 alkyl, perfluoro-C1-C3 alkyl and aminocarbonyl, wherein the amino and aminocarbonyl substituents are each unsubstituted or substituted with 1-2 substituents each independently selected from the group consisting of C1-C6 alkyl, nitrile, oxo and alkanoyl of 1-3 carbons; R1 is selected from the group consisting of a straight-chained or branched, saturated or unsaturated residue containing 1 to 8 carbon atoms which is uninterrupted or interrupted by 1 or 2 heteroatoms selected from the group consisting of O, N and S, cyclopentyl, cyclohexyl, cycloheptyl, morpholinyl, thiamorpholinyl, piperidinyl, piperazinyl, tetrahydrofuryl, tetrahydropyranyl, phenyl, naphthyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, imidazolyl, furanyl, oxazolyl, isothiazolyl, isooxazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, thiazolyl, indolyl, tetrahydronaphthyl, decalinyl, quinolyl, isoquinolyl, tetrahydroquinolyl, tetrahydroisoquinolyl, benzimidazolyl, indazolyl, oxindolyl, benzofuranyl, benzothienyl, benzthiazolyl, benzoxazolyl, purinyl, phenyl-C1-C2 alkyl and naphthyl-C1-C3 alkyl, C1-C3 alkyl-pyridinyl, C1-C3 alkyl-pyrimidinyl, C1-C3 alkyl-pyridazinyl, C1-C3 alkyl-pyrazinyl, C1-C3 alkyl-imidazolyl, C1-C3 alkyl-furanyl, C1-C3 alkyl-oxazolyl, C1-C3 alkyl-isothiazolyl, C1-C3 alkyl-isooxazolyl, C1-C3 alkyl-1,2,3-triazolyl, C1-C3 alkyl-1,2,4-triazolyl, C1-C3 alkyl-thiazolyl, C1-C3 alkyl-mercaptophenyl and C1-C3 alkyl-indolyl, wherein the residues for R1 listed above are each independently unsubstituted or substituted with 1-3 substituents each independently selected from the group consisting of halogen, hydroxy, mercapto, alkylmercapto C1-C3 alkyl, C3-C8 cycloalkyl, C4-C8 cycloalkenyl, hydroxy-C1-C3 alkyl, C1-C3 alkoxy, hydroxy-C1-C3 alkoxy, chloro-C1-C3 alkoxy, C1-C3 alkylmercapto, C1-C3 alkylsulfinyl, C1-C3 alkylsulfonyl, amino, C1-C3 alkylamino, C1-C3 dialkylamino, nitro, carboxyl, carboxamido, C1â€”C3 alkoxycarbonyl, C1-C3 alkoxycarbonyl-C1-C3 alkyl, perfluoro-C1-C3 alkyl and aminocarbonyl, wherein the amino and aminocarbonyl substituents are each unsubstituted or substituted with 1-2 substituents each independently selected from the group consisting of C1-C6 alkyl, nitrile, oxo and alkanoyl of 1â€”3 carbons; R5 is hydrogen or a straight-chained or branched, saturated or unsaturated residue containing 1 to 8 carbon atoms which is uninterrupted or interrupted by 1 or 2 heteroatoms selected from the group consisting of O, N and S and R6 is selected from the group consisting of hydrogen, a straight-chained or branched, saturated or unsaturated residue containing 1 to 8 carbon atoms which is uninterrupted or interrupted by 1 or 2 heteroatoms selected from the group consisting of O, N and S, cyclopentyl, cyclohexyl, cycloheptyl, morpholinyl, thiamorpholinyl, piperidinyl, piperazinyl, tetrahydrofuryl, tetrahydropyranyl, phenyl, naphthyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, imidazolyl, furanyl, oxazolyl, isothiazolyl, isooxazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, thiazolyl, indolyl, tetrahydronaphthyl, decalinyl, quinolyl, isoquinolyl, tetrahydroquinolyl, tetrahydroisoquinolyl, benzimidazolyl, indazolyl, oxindolyl, benzofuranyl, benzothienyl, benzthiazolyl, benzoxazolyl, purinyl, phenyl-C1-C2 alkyl and naphthyl-C1-C2 alkyl, C1-C3 alkyl-pyridinyl, C1-C3 alkyl-pyrimidinyl, C1-C3 alkyl-pyridazinyl, C1-C3 alkyl-pyrazinyl, C1-C3 alkyl-imidazolyl, C1-C3 alkyl-furanyl, C1-C3 alkyl-oxazolyl, C1-C3 alkyl-isothiazolyl, C1-C3 alkyl-isooxazolyl, C1-C3 alkyl-1,2,3-triazolyl, C1-C3 alkyl-1,2,4-triazolyl, C1-C3 alkyl-thiazolyl, C1-C3 alkyl-mercaptophenyl and C1-C3 alkyl-indolyl, wherein the residues for R6 listed above are each independently unsubstituted or substituted with 1-3 substituents each independently selected from the group consisting of halogen, hydroxy, mercapto, alkylmercapto C1-C3 alkyl, C3-C8 cycloalkyl, C4-C8 cycloalkenyl, hydroxy-C1-C3 alkyl, C1-C3 alkoxy, hydroxy-C1-C3 alkoxy, chloro-C1-C3 alkoxy, C1-C3 alkylmercapto, C1-C3 alkylsulfinyl, C1-C3 alkylsulfonyl, amino, C1-C3 alkylamino, C1-C3 dialkylamino, nitro, carboxyl, carboxamido, C1-C3 alkoxycarbonyl, C1-C3 alkoxycarbonyl-C1-C3 alkyl, perfluoro-C1-C3 alkyl and aminocarbonyl, wherein the amino and aminocarbonyl substituents are each unsubstituted or substituted with 1-2 substituents each independently selected from the group consisting of C1-C6 alkyl, nitrile, oxo and alkanoyl of 1-3 carbons, or R5 and R6, together with the N atom to which they are bound, form a saturated or unsaturated 5-membered or 6-membered ring which contains 0 or 1 additional heteroatoms selected from the group consisting of oxygen, nitrogen and sulfur, the remainder of the atoms in the ring being carbon, or a pharmacologically acceptable salt, ester, optical isomer or prodrug thereof.