Patent ID: 6482822
Filing Date: 2002-11-19
Classification: A61P,C07D

Abstract:
A compound of the formula wherein &PHgr; is phenylene with 1 to 2 substituents selected from the group consisting of hydrogen, halogen, â€”OH, and alkyl or alkoxy of 1 to 6 carbon atoms, A is W is sulfur, R1, R2, R3, R4 and R5 are individually selected from the group consisting of hydrogen, halogen, â€”OH, â€”CN, â€”NO2, R6and alkyl and alkoxy of 1 to 6 carbon atoms, R6 and R7 are individually selected from the group consisting of hydrogen, â€”OH, â€”COâ€”R8 and alkyl and alkoxy of 1 to 6 carbon atoms, R8 is selected from the group consisting of hydrogen, â€”OH, and alkyl and alkoxy of 1 to 6 carbon atoms, R9 and R10 are individually selected from the group consisting of hydrogen, â€”OH, and alkyl of 1 to 6 carbon atoms, R11 is selected from the group consisting of hydrogen, â€”OH, â€”COR12 and alkyl and alkoxy of 1 to 6 carbon atoms, R12 is selected from the group consisting of hydrogen, â€”OH and alkyl 1 to 6 carbon atoms, B is selected from the group consisting of â€”CH2â€”NO2, alkyl of 1 to 6 carbon atoms, and unsubstituted and substituted carbocyclic aryl and heterocyclic aryl of 5 to 6 ring members containing 1 to 4 heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen, the aryl substituents being selected from the group consisting of alkyl, alkenyl and alkoxy of up to 6 carbon atoms, R13 and R14 are individually selected from the group consisting of hydrogen, â€”CN, â€”NO2 and alkyl of 1 to 6 carbon atoms or together with the nitrogen form a non-aromatic heterocycle of 5 to 6 ring members selected from the group consisting of â€”CH2, â€”NHâ€”, â€”Oâ€” and â€”Sâ€”, X is selected from the group consisting of a bond, â€”(CH2)kâ€”NR16â€”, â€”Oâ€”, â€”Sâ€”, â€”COâ€”, â€”NR16â€”CO, â€”COâ€”NR16, â€”Oâ€”COâ€”, â€”COâ€”Oâ€”, â€”NR16â€”COâ€”Oâ€” and â€”NR16â€”COâ€”NR17, k is 0 or 1, Y is selected from the group consisting of a bond, â€”(CH2)mâ€”, â€”(CH2)mâ€”Oâ€”(CH2)nâ€”, â€”(CH2)mâ€”Sâ€”(CH2)mâ€”, â€”(CH2)mâ€”NR18â€”(CH2)n, â€”(CH2)mâ€”NR18â€”COâ€”(CH2)nâ€”, â€”(CH2)mâ€”COâ€”NR18â€”(CH2)nâ€” and â€”(CH2)mâ€”Qâ€”(CH2)nâ€”, Q is selected from the group consisting of piperazine, homopiperazine, 2-methylpiperazine, 2,5-dimethylpiperazine, 4-oxypiperidine and 4-aminopiperidine, m and n are individually integers from 0 to 6, R16, R17 and R18 are individually hydrogen or alkyl of 1 to 6 carbon atoms and its pharmaceutically acceptable salt with acids or bases.