Patent ID: 6555524
Filing Date: 2003-04-29
Classification: A61P,C07H

Abstract:
A compound of the formula or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein:X1 is O, â€”CR4R5â€” or â€”NR4â€”; R1 is H or C1-C10 alkyl, wherein 1 to 3 carbons of said alkyl are optionally replaced by a heteroatom selected from a group consisting of O, S and â€”N(R4)â€”, and said alkyl is optionally substituted by 1 to 3 substituents independently selected from the group consisting of â€”C(O)O(C1-C10 alkyl), C1-C10 alkoxy, C1-C10 alkanoyl, halo, nitro, cyano, 4 to 10 membered heterocyclyl, C1-C10 alkyl, â€”NR4R55, C6-C10 aryl, â€”S(O)n(C1-C10 alkyl) wherein n is an integer ranging from 0 to 2, and â€”SO2NR4R5; R2 is â€”(CR4R5)n(4 to 10 membered heterocyclic) or â€”(CR4R5)n(C6-C10aryl), wherein n is an integer from 0 to 6, and wherein from 1 to 3 R4 or R5 groups of the â€”(CR4R5)nâ€” moiety of the foregoing R2 groups are optionally replaced with a halo substituent, and the heterocyclic and aryl moieties of the foregoing R2 groups are optionally substituted with 1 to 4 R3 groups; each R3 is independently selected from halo, cyano, nitro, trifluoromethoxy, trifluoromethyl, azido, hydroxy, C1-C6 alkoxy, C1-C10 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, â€”C(O)R6, â€”C(O)OR6, â€”OC(O)R6, â€”NR6C(O)R7, â€”NR6C(O)NR1R7, â€”NR6C(O)OR7, â€”C(O)NR6R7, â€”NR6R7, â€”NR6OR7, â€”SO2NR6R7, â€”S(O)j(C1-C6 alkyl) wherein j is an integer from 0 to 2, â€”(CR1R2)t(C6-C10 aryl), â€”(CR4R5)t(4 to 10 membered heterocyclic), â€”(CR4R5)qC(O) (CR4R5)t(C6-C10 aryl), â€”(CR4R5)qC(O) (CR4R5)t(4 to 10 membered heterocyclic), â€”(CR4R5)tO(CR4R5)q(C6-C10 aryl), â€”(CR4R5)tO(CR4R5)q(4 to 10 membered heterocyclic), â€”(CR4R5)qSO2(CR4R5)t(C6-C10 aryl), and â€”(CR4R5)qSO2(CR4R5)t(4 to 10 membered heterocyclic), wherein q and t are each independently an integer from 0 to 5, 1 or 2 ring carbon atoms of the heterocyclic moieties of the foregoing R3 groups are optionally substituted by an oxo (&boxH;O) moiety, and the alkyl, alkenyl, alkynyl, aryl and heterocyclic moieties of the foregoing R3 groups are optionally substituted by 1 to 3 substituents independently selected from the group consisting of halo, cyano, nitro, trifluoromethyl, trifluoromethoxy, azido, â€”OR6, â€”C(O)R6, â€”C(O)OR6, â€”OC(O)R6, â€”NR6C(O)R7, â€”C(O)NR6R7, â€”NR6R7, â€”NR6OR7, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, â€”(CR4R5)t(C6-C10 aryl), and â€”(CR4R5) (4 to 10 membered heterocyclic), wherein t is an integer from 0 to 5; each R4 and R5 is independently selected from the group consisting of H and C1-C6 alkyl; each R6 and R7 is independently selected the group consisting of from H, C1-C6 alkyl, â€”(CR4R5)t(C6-C10 aryl), and â€”(CR4R5)t(4 to 10 membered heterocyclic), wherein t is an integer from 0 to 5, 1 or 2 ring carbon atoms of the heterocyclic group are optionally substituted by an oxo (&boxH;O) moiety, and the alkyl, aryl and heterocyclic moieties of the foregoing R6 and R7 groups are optionally substituted by 1 to 3 substituents independently selected the group consisting of from halo, cyano, nitro, â€”NR4R5, trifluoromethyl, trifluoromethoxy, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, hydroxy, and C1-C6 alkoxy; R8 is H, â€”C(O) (C1-C6 alkyl), benzyl, benzyloxycarbonyl or (C1-C6 alkyl)3 silyl; R9 is H, C1-C10 alkyl; C2-C4 alkenyl; or C2-C4 alkynyl; and R10 is selected from the group consisting of from chloro, bromo, iodo, fluoro, and cyano.