Patent ID: 6683056
Filing Date: 2004-01-27
Classification: A61P,C07H,C40B

Abstract:
A compound having the structure whereinwhen Y is â€ƒor heteroaryl; R1, R2, R3, and R4 are the same or different and are independently selected from hydrogen, OH, OR7, lower alkyl, or halogen, or two of R1, R2, R3, and R4 together with the carbons to which they are attached can form an annelated five, six or seven membered carbocycle or heterocycle which may contain 1 to 4 heteroatoms in the ring which are N, O, S, SO, and/or SO2; R5 and R6 are the same or different and are independently selected from hydrogen, OH, OR7a, â€”OAryl, â€”OCH2Aryl, lower alkyl, cycloalkyl, Aryl, arylalkyl, CF3, arylalkenyl, â€”OCHF2, â€”OCF3, halogen, â€”CN, â€”CO2R7b, â€”CO2H, COR8f, CHOHR8g, CH(OH7h)R8h, â€”CONR8R8a, â€”NHCOR7c, â€”NHSO2R7d, â€”NHSO2Aryl, â€”SR7e, â€”SOR7f, â€”SO2R7g, â€”SO2Aryl, â€”OCH2CO2R7i, â€”OCH2CO2H, â€”OCH2CONR8bR8c, â€”OCH2CH2NR8dR8e, or a five, six or seven membered heterocycle which may contain 1 to 4 heteroatoms in the ring which are N, O, S, SO, and/or SO2, or R5 and R6 together with the carbons to which they are attached form an annelated five, six or seven membered carbocycle or heterocycle which may contain 1 to 4 heteroatoms in the ring which are N, O, S, SO, and/or SO2; R7, R7a, R7b, R7c, R7d, R7e, R7f, R7g, R7h and R7i are independently lower alkyl; R8, R8a, R8b, R8c, R8d, R8e, R8f, R8g and R8h are the same or different and are independently selected from hydrogen, alkyl,aryl, arylalkyl, cycloalkyl, or together with the nitrogen to which they are attached form an annelated five, six or seven membered heterocycle which may contain 1 to 4 heteroatoms in the ring which are N, O, S, SO, and/or SO2; A is O(CH2)m, S, NH(CH2)m, or (CH2)n where n is 0-3 and m is 0-2, and a pharmaceutically acceptable salt thereof, all stereoisomers thereof, and all prodrug esters thereof, with the following provisos that where A is (CH2)n and Y is â€ƒand 1) when R1 is OH and R3 is alkyl, at least one of R1, R4, R5 and R6 is not hydrogen; 2) when R2 and R3 are OH, at least one of R1, R4, R5 and R6 is not hydrogen; 3) when R2 is methyl, R5 is OH, and R6 is alkyl, at least one of R1, R3, and R4 is not hydrogen; 4) when R2 is chlorine, at least one of R1, R3, R4, R5 and R6 is not hydrogen; 5) when R2 is OH, R5 is OH and n is 2, R6 is not hydrogen or OH; and 6) when R1, R2, R3, R4, R5 and R6 are hydrogen, n is not 0; â€ƒand with the additional proviso that where A is O(CH2)m and Y is 7) when R2 is Cl and m is 0, at least one of R5 and R6 is not Cl.