Patent ID: 6828319
Filing Date: 2004-12-07
Classification: A61K,A61P,C07D,Y02A

Abstract:
A compound of the formula or a pharmaceutically acceptable hydrate or salt thereof,wherein:R5 is NH; R6 is â€”H or C1-C4 alkyl; X is â€”C(O)â€”, â€”CH2â€”, â€”CH(halo)-, â€”CH(OH)(CH2)nâ€”, â€”CH(OH)-arylene-, â€”Oâ€”, â€”NHâ€”, â€”Sâ€” or â€”CH(NR11R12)â€”, wherein n is an integer ranging from 0-5; R11 and R12 are independently -hydrogen or â€”C1-C9 alkyl, or N, R11 and R12 are taken together to form a 5-10 membered aromatic or non-aromatic carbocycle in which 1-4 ring carbon atoms are independently replaced with a N, O or S atom, at least one of which is a nitrogen atom; R1, R2, R3, R4, R7, R8, R9 and R10 are independently -hydrogen, -halo, -hydroxy, â€”Oâ€”(C1-C5 alkyl), â€”C1-C10 alkyl, -alkylhalo, â€”C2-C10 alkenyl, â€”C3-C8 carbocycle, -aryl, â€”NH2, -alkylamino, â€”C(O)OH, â€”C(O)O(C1-C5 alkyl), â€”OC(O)(C1-C5 alkyl), NO2 or -A-B; wherein A is â€”SO2â€”, â€”SO2NHâ€”, â€”NHCOâ€”, â€”NHCONHâ€”, â€”Oâ€”, â€”COâ€”, â€”OC(O)â€”, â€”C(O)Oâ€”, â€”CONHâ€”, â€”CON(C1-C4 alkyl)-, â€”NHâ€”, â€”CH2â€”, â€”Sâ€” or â€”C(S)â€”; B is â€”C1-C10 alkyl, â€”C2-C10 alkenyl, -heterocycle, â€”C3-C8 carbocycle, -aryl, â€”NZ1Z2, -alkylamino, -aminodialkyl, -arylamido, â€”C(O)OH, â€”C(O)Oâ€”(C1-C5 alkyl), â€”C(O)O-phenyl, a 5-10 membered aromatic or non-aromatic carbocycle in which 1-4 of the ring carbon atoms are independently replaced with a N, O or S atom, or B is a C1-C5 alkyl group in which one of the C1-C5 alkyl group's hydrogen atoms is replaced with a 5-10 membered aromatic or non-aromatic carbocycle in which 1-4 of the carbocycle's ring carbon atoms are independently replaced with a N, O or S atom, any of the foregoing B groups being unsubstituted or substituted with one or more of â€”Oâ€”(C1-C5 alkyl), -halo, -alkyihalo, -alkanol, -alkylamino, -hydroxy, â€”NO2, â€”NH2, -aminoalkyl, -aminodialkyl, â€”C1-C10 alkyl, â€”C2-C10 alkenyl, â€”C2-C10 alkynyl, -aryl, -benzyl, -alkylamido, -alkylcarboxy, â€”C1-C5 alkylene-C(O)Oâ€”C1-C5 alkyl, C1-C5 alkylene-OC(O)-C1-C5 alkyl or a 5-10 membered aromatic or non-aromatic carbocycle in which 1-4 ring carbon atoms are independently replaced with a N, O or S atom, at least one of which is a nitrogen atom; and Z1 and Z2 are independently â€”H or â€”C1-C10 alkyl, which is unsubstituted or substituted with one or more of -halo, â€”OH or â€”N(Z3)(Z4), where Z3 and Z4 are independently, â€”H or â€”C1-C5 alkyl, which is unsubstituted or substituted with one or more of -halo, -hydroxy or â€”NH2; or N, Z3 and Z4 are taken together to form an unsubstituted or substituted 5-10 membered aromatic or non-aromatic carbocycle in which 1-4 ring carbon atoms are independently replaced with a N, O or S atom, at least one of which is a nitrogen atom; or N, Z1 and Z2 are taken together to form a 5-10 membered aromatic or non-aromatic carbocycle in which 1-4 ring carbon atoms are independently replaced with a N, O or S atom, at least one of which is a nitrogen atom.