Patent ID: 6271235
Filing Date: 2001-08-07
Classification: A61P,C07C,C07D,C07F

Abstract:
A compound of the formula: ##STR135##wherein:Q.sub.1 and Q.sub.2 are each independently selected from hydrogen and substituted and unsubstituted alkyl and aryl;Q.sub.3 is selected from mercapto and substituted and unsubstituted alkoxyl, aryloxyl, thioether, amino, alkyl, cycloalkyl, saturated and partially saturated heterocycle, and aryl;Q.sub.4, Q.sub.5, Q.sub.6, Q.sub.7, and Q.sub.8 are each independently selected from hydrogen, hydroxyl, mercapto, nitro, halogen, --O-J, where J is a substituted or unsubstituted hydrolyzable group, and substituted or unsubstituted alkoxyl, aryloxyl, thioether, sulfinyl, sulfonyl, amino, alkyl, cycloalkyl, saturated and partially saturated heterocycle, aryl, and L.sub.6 C(O)L.sub.4, where L.sub.6 is a single bond --O or --N, and further where L.sub.4 is alkyl, hydroxyl, alkoxyl or hydrogen; and further wherein any one or more of Q.sub.4, Q.sub.5, Q.sub.6, Q.sub.7 and Q.sub.8 may be a member of a spiro ring, and any two of Q.sub.4, Q.sub.5, Q.sub.6, Q.sub.7, and Q.sub.8 may together be members of a ring;E is carbon or nitrogen;Q.sub.9 is selected from hydrogen, halogen, hydroxyl, mercapto, and substituted and unsubstituted alkoxyl, aryloxyl, thioether, amino, alkyl, and aryl, where Q.sub.9 may form a part of a ring, wherein when Q.sub.9 is thioether, Q.sub.9 is selected from substituted and unsubstituted S-alkyl, S-(C.sub.5 -C.sub.7)-cycloalkyl, S-aryl, and S-heterocycle, and wherein said S-heterocycle is selected from decahydroisoquinolinyl, octahydro-thieno[3,2-c]pyridinyl, piperidinyl, piperazinyl, azepinyl, pyrrolyl, pyrrolidinyl, pyrazolyl, pyrazolidinyl, imidazolyl, isobenzofuranyl, furazanyl, imidazolinyl, imidazolidinyl, pyrazinyl, pyrimidinyl, pyridazinyl, oxozolyl, oxazolidinyl, isoxazolyl, thianthrenyl, triazinyl, isoxazolidinyl, morpholinyl, thiazolyl, thiazolidinyl, isothiazolyl, quinuclidinyl, isothiazolidinyl, indolyl, quinoliny, chromenyl, xanthenyl, isoquinolinyl, benzimidazolyl, thiadiazolyl, benzopyranyl, benzothiazolyl, benzoazolyl, furyl, tetrahydrofuryl, tetrahydropyranyl, thienyl, benzothienyl, benzo[b]thienyl, naphtho[2,3-b]thienyl, thiamorpholinyl, thiamorpholinylsulfoxide, thiamorphoinylsulfone, oxadizaolyl, triazolyl, tetrahydroquinolinyl, tetrahydrisoquinolinyl, phenoxathienyl, indolizinyl, isoindolyl, indazolyl, purinyl, isoquinolyl, quinolyl, phthalazinyl, naphthyridinyl, quinoxyalinyl, quinzolinyl, tetrahydroquinolinyl, cinnolinyl, pteridinyl, carbazolyl, beta-carbolinyl, phenanthridinyl, acridinyl, perimidinyl, phenanthrolinyl, phenazinyl, isothiazolyl, phenothiazinyl, and phenoxazinyl; ##STR136##is a monocyclic or polycyclic carbocycle or heterocycle, which is optionally further substituted, and when ##STR137##is heterocycle, each heterocyclic ring has one to three heteroatoms independently selected from nitrogen, oxygen, and sulfur; and ##STR138##is a 6-membered monocyclic heterocycle optionally having one or two additional heteroatoms independently selected from nitrogen, oxygen and sulfur, which is optionally further substituted;or a prodrug or pharmaceutically acceptable salt of said compound.