| abstract |
A compound having the structure in which R1, R2 and R2a are independently hydrogen, OH, OR5, alkyl, CF3, OCHF2, OCF3, SR5i or halogen, or two of R1, R2 and R2a together with the carbon atoms at which are attached they can form a five, six or seven membered carbocycle or heterocycle, which may contain 1 to 4 ring heteroatoms that are N, O, S, SO, and / or SO2; R3 and R4 are independently hydrogen, OH, OR5a, Oaryl, OCH2aryl, alkyl, cycloalkyl, CF3, -OCHF2, - OCF3, halogen, -CN, -CO2R5b, -CO2H, -COR6b, -CH (OH) R6c, - CH (OR5h) R6d, -CONR6R6a, -NHCOR5c, -NHSO2R5d, -NHSO2aryl, aryl, -SR5e, -SOR5f, -SO2R5g, -SO2aryl, or a heterocycle of five, six or seven members that may contain 1 to 4 heteroatoms in the ring that are N, O, S, SO, and / or SO2, or R3 and R4 together with the carbon atoms to which they are attached form a five, six or seven membered carbocycle or heterocycle attached which may contain 1 to 4 ring heteroatoms that are N, O, S, SO, and / or SO2; R5, R5a, R5b, R5c, R5d, R5e, R5f, R5g, R5h, and R5i are independently alkyl; R6, R6a, R6b, R6c, and R6d are independently hydrogen, alkyl, aryl, alkylaryl or cycloalkyl, or R6 and R6a together with the nitrogen to which they are attached form an attached five, six or seven membered heterocycle that may contain 1 to 4 ring heteroatoms that are N, O, S, SO, and / or SO2; A is O, S, NH, or (CH2) n where n is 0-3, or a pharmaceutically acceptable salt, stereoisomer, or prodrug ester thereof; with the proviso that when A is (CH2) n where n is 0, 1, 2, or 3 or A is O, and at least one of R1, R2, and R2a is OH or OR5, then at least one of R1 , R2, and R2a is CF3, OCF3, or OCHF2 and / or at least one of R3 and R4 is CF3, -OCHF2, -OCF3, -CN, -CO2R5b, CH (OR5h) R6d, CH (OH) R6c, COR6b , - NHCOR5c, -NHSO2R5d, -NHSO2aryl, aryl, -SR5e, -SOR5f, - SO2R5g, or -SO2aryl. |