Patent ID: 6342497
Filing Date: 2002-01-29
Classification: A61P,C07H,Y02P

Abstract:
A compound of the formula or a pharmaceutically acceptable salt, prodrug, or hydrate thereof wherein:R1 is H and R2 is â€”NR3R4, â€”NR4C(O)R3, â€”OC(O)NR3R4 or â€”OR3; or R1 and R2 are taken together to form &boxH;O, &boxH;Nâ€”OR3, &boxH;CR4R3, &boxH;CR4C(O)R3, &boxH;CR4C(O)OR3, or &boxH;CR4C(O)NR3R4; each R3 is independently selected from H, C1-C10 alkyl, C2-C10 alkenyl, â€”(CH2)t(C3-C10 cycloalkyl), â€”(CH2)t(C6-C10 aryl), and â€”(CH2)t(4-10 membered heterocyclic), wherein t is an integer ranging from 0 to 5, said alkyl group optionally has 1 or 2 hetero moieties selected from O, â€”S(O)jâ€” wherein j is an integer ranging from 0 to 2, and â€”N(R7)â€” with the proviso that two O atoms, two S atoms, or an O and S atom are not attached directly to each other; said cycloalkyl, aryl and heterocyclic R3 groups are optionally fused to a benzene ring, a C5-C8 saturated cyclic group, or a 4-10 membered heterocyclic group; the â€”(CH2)tâ€” moieties of the foregoing R3 groups optionally have a carbon-carbon double or triple bond where t is an integer between 2 and 5; and the foregoing R3 groups, except H but having any optional fused rings referred to above, are optionally substituted by 1 to 5 R5 groups; each R4 is independently H or C1-C10 alkyl; each R5 is independently selected from C1-C10 alkyl, C3-C10 cycloalkyl, halo, cyano, nitro, trifluoromethyl, trifluoromethoxy, azido, â€”OR6, â€”C(O)R6, â€”C(O)OR6, â€”NR7C(O)OR9, â€”OC(O)R6, â€”NR7SO2R9, â€”SO2NR6R7, â€”NR7C(O)R6, â€”C(O)NR6R7, â€”NR6R7, â€”S(O)j(CH2)m(C6-C10 aryl), â€”S(O)j(C1-C6 alkyl), wherein j is an integer ranging from 0 to 2, â€”(CH2)m(C6C10 aryl), â€”O(CH2)m(C6-C10 aryl), â€”NR7(CH2)m(C6-C10 aryl), and â€”(CH2)m(4-10 membered heterocyclic), wherein m is an integer ranging from 0 to 4; said alkyl group optionally has 1 or 2 hetero moieties selected from O, â€”S(O)jâ€” wherein j is an integer ranging from 0 to 2, and â€”N(R7)â€” with the proviso that two O atoms, two S atoms, or an O and S atom are not attached directly to each other; said cycloalkyl, aryl and heterocyclic R5 groups are optionally fused to a C6-C10 aryl group, a C5-C8 saturated cyclic group, or a 4-10 membered heterocyclic group; and said alkyl, cycloalkyl, aryl and heterocyclic R5 groups are optionally substituted by 1 to 5 substituents independently selected from halo, cyano, nitro, trifluoromethyl, difluoromethoxy, trifluoromethoxy, azido, â€”NR7SO2R9, â€”SO2NR6R7, â€”C(O)R6, â€”C(O)OR6, â€”OC(O)R6, â€”NR7C(O)OR9, â€”NR7C(O)R6, â€”C(O)NR6R7, â€”NR6R7, â€”OR6, C1-C10 alkyl, â€”(CH2)m(C6-C10 aryl), and â€”(CH2)m(4-10 membered heterocyclic), wherein m is an integer ranging from 0 to 4; each R6 is independently selected from H, C1-C10 alkyl, C3-C10 cycloalkyl, â€”(CH2)m(C6-C10 aryl), and â€”(CH2)m(4-10 membered heterocyclic), wherein m is an integer ranging from 0 to 4; said alkyl group optionally has 1 or 2 hetero moieties selected from O, â€”S(O)jâ€” wherein j is an integer ranging from 0 to 2, and â€”N(R7)â€” with the proviso that two O atoms, two S atoms, or an O and S atom are not attached directly to each other; said cycloalkyl, aryl and heterocyclic R6 groups are optionally fused to a C6-C10 aryl group, a C5-C8 saturated cyclic group, or a 4-10 membered heterocyclic group; and the foregoing R6 substituents, except H, are optionally substituted by 1 to 5 substituents independently selected from halo, cyano, nitro, trifluoromethyl, difluoromethoxy, trifluoromethoxy, azido, â€”C(O)R7, â€”C(O)OR7, â€”OC(O)R7, â€”NR7C(O)R8, â€”C(O)NR7R8, â€”NR7R8, hydroxy, C1-C6 alkyl, and C1-C6 alkoxy; each R7 and R8 is independently H or C1-C6 alkyl; and, R9 is selected from the substituents provided in the definition of R6 except H.