Patent ID: 6458830
Filing Date: 2002-10-01
Classification: A61P,C07D

Abstract:
A compound of the formula (I): whereinR1 is hydrogen, halogen, C1-6alkyl, C1-6alkoxy, fluoroC1-6alkyl, fluoroC1-6alkoxy, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, NO2, CN, SRa, SORa, SO2Ra, CO2Ra, CONRaRb, C2-6alkenyl, C2-6alkynyl or C1-4alkyl substituted by C1-4alkoxy, wherein Ra and Rb each independently represent hydrogen or C1-4alkyl; R2 is hydrogen, halogen, C1-6alkyl, fluoroC1-6alkyl or C1-6alkoxy substituted by C1-4alkoxy; R3 is hydrogen, halogen or fluoroC1-6alkyl; R4 is hydrogen, halogen, C1-6alkyl, C1-6alkoxy, fluoroC1-6alkyl, fluoroC1-6alkoxy, hydroxy, NO2, CN, SRa, SORa, SO2Ra, CO2Ra, CONRaRb, C2-6alkenyl, C2-6alkynyl or C1-4alkyl substituted by C1-4alkoxy, wherein Ra and Rb are as previously defined; R5 is hydrogen, halogen, C1-6alkyl, fluoroC1-6alkyl or C1-6alkoxy substituted by C1-4alkoxy; R6 represents hydrogen or a C1-4alkyl group optionally substituted by a hydroxy group; R7 represents halogen, hydroxy, C2-4alkenyl, C2-4alkynyl, N3, â€”NR11R12, â€”NRaCORb, â€”OSO2Ra, â€”(CH2)pNRa(CH2)qCOORb, CORa, COORa, â€”N&boxH;C&boxH;O, or a five membered or six membered nitrogen-containing heteroaromatic ring optionally containing 1, 2 or 3 additional heteroatoms selected from N, O and S which heteroaromatic ring is optionally substituted at any substitutable position by a substituent selected from &boxH;O, &boxH;S, halogen, hydroxy, â€”SH, CORa, CO2Ra, â€”ZNR11R12, C1-4alkyl, hydroxyC1-4alkyl, fluoroC1-4alkyl, chloroC1-4alkyl, C1-4alkoxy, fluoroC1-4alkoxy or C1-4alkoxy substituted by a C1-4alkoxy or hydroxyl group, and wherein said C2-4alkenyl and C2-4alkynyl groups are optionally substituted by a substituent selected from halogen, hydroxy, N3, â€”NR11R12, â€”NRaCORb, â€”OSO2Ra, â€”(CH2)pNRa(CH2)qCOORb, CORa or COORa; R8 represents hydrogen, C1-6alkyl, fluoroC1-6alkyl, hydroxy, C1-6alkoxy or hydroxyC1-6alkyl; R9 and R10 each independently represent hydrogen, halogen, C1-6alkyl, CH2ORc, oxo, CO2Ra or CONRaRb where Ra and Rb are as previously defined and Rc represents hydrogen, C1-6alkyl or phenyl; R11 is hydrogen, C1-4alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, C2-4alkyl substituted by a C1-4alkoxy or hydroxyl group, or R11 is a five membered or six membered nitrogen-containing heteroaromatic ring as previously defined; R12 is hydrogen or C1-4alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or C2-4alkyl substituted by a C1-4alkoxy or hydroxyl group; or R11, R12 and the nitrogen atom to which they are attached form a heteroaliphatic ring of 4 to 7 ring atoms, optionally substituted by one or two groups selected from hydroxy, CORe, CO2Re, C1-4alkyl optionally substituted by a C1-4alkoxy or hydroxyl group, or C1-4alkoxy optionally substituted by a C1-4alkoxy or hydroxyl group, or a five membered or six membered nitrogen-containing heteroaromatic ring as previously defined, or said heteroaliphatic ring is substituted by a spiro-fused lactone ring, and said heteroaliphatic ring optionally containing a double bond, which heteroaliphatic ring may optionally contain an oxygen or sulphur ring atom, a group S(O) or S(O)2 or a second nitrogen atom which will be part of a NH or NRd moiety, where Rd is C1-4alkyl optionally substituted by hydroxy or C1-4alkoxy, and where Re is hydrogen, C1-4alkyl or benzyl; or R11, R12 and the nitrogen atom to which they are attached form a non-aromatic azabicyclic ring system of 6 to 12 ring atoms; or R11, R12 and the nitrogen atom to which they are attached form a heteroaliphatic ring of 4 to 7 ring atoms to which is fused a benzene ring or a five membered or six membered nitrogen-containing heteroaromatic ring optionally containing 1, 2 or 3 additional heteroatoms selected from N, O and S; Z represents a bond, C1-6alkylene or C3-6cycloalkylene; n is zero, 1 or 2; p is 1 or 2; and q is 1 or 2; or a pharmaceutically acceptable salt thereof.