Patent ID: 6451827
Filing Date: 2002-09-17
Classification: C07C,C07D,C07F

Abstract:
A compound of formula I having the structure wherein:B is aryl; D is halogen or aryl; R1 is hydrogen, alkyl of 1-6 carbon atoms, â€”SO2Ph(OH)(CO2H), â€”CH(R2)W, â€”CH2CH2Y, or â€”CH2CH2CH2Y; R2 is â€”CH2(1H-imidazol-4-yl), â€”CH2(3-1H-indolyl), â€”CH2CH2(1,3-dioxo-1,3-dihydro-isoindol-2-yl), â€”CH2CH2(1-oxo-1,3-dihydro-isoindol-2-yl), or â€”CH2(3-pyridyl); W is â€”CO2R3, â€”CONHOH, â€”CN, â€”CONHR3, aryl, heteroaryl, â€”CHO, â€”CH&boxH;NOR3, or â€”CH&boxH;NHNHR3; Y is â€”W, â€”OCH2CO2R3, aryl, heteroaryl, â€”C(&boxH;NOH)NH2, â€”OR3, â€”O(C&boxH;O)NR4R5, â€”NR3(C&boxH;O)OR3, â€”NR3(C&boxH;O)NR4R5, or â€”NR4R5; R3 is hydrogen or alkyl of 1-6 carbon atoms; R4 and R5 are each, independently, hydrogen, or alkyl of 1-6 carbon atoms or R4 and R5 are, together, â€”(CH2)nâ€”, or â€”CH2CH2XCH2CH2â€”; X is O, S, SO, SO2, NR3, or CH2; n is 2 to 5; C is â€”CONR6R7; R6 and R7 are each, independently, hydrogen, alkyl of 1-18 carbon atoms, aryl, heteroaryl, aralkyl of 6-20 carbon atoms, heteroaralkyl of 6-20 carbon atoms, cycloalkyl of 3-10 carbon atoms, â€”(CH2CH2O)nCH3, â€”(CH2)mA or R6 and R7 are, together, â€”(CH2)pâ€”, â€”(CH2)2N(CH3)(CH2)4â€”, â€”(CH2)2N(R8)(CH2)2â€”, or â€”(CH2)2CH(R8)-(CH2)2â€” with the proviso that at least one of R1, R6 or R7 is heteroaryl; R8 is hydrogen, alkyl of 1-18 carbon atoms, aryl, heteroaryl, aralkyl of 6-20 carbon atoms, heteroaralkyl of 6-20 carbon atoms, cycloalkyl of 3-10 carbon atoms, â€”(CH2CH2O)nCH3, â€”(CH2CH2CH2O)nCH3, or â€”(CH2)mA; A is aryl, heteroaryl, aryloxy, heteroaryloxy, arylthio, heteroarylthio, arylsulfoxy, heteroarylsulfoxy, arylsulfonyl, heteroarylsulfonyl, â€”CHF2, â€”CH2F, â€”CF3, â€”(CH2CH2O)nCH3, â€”(CH2CH2CH2O)nCH3, â€”CO2R3, â€”O(C&boxH;O)NR6R7, aralkyl or heteroaralkyloxy; m is 2 to 16; p is 2 to 12; or a pharmaceutically acceptable salt thereof.