Patent ID: 6414126
Filing Date: 2002-07-02
Classification: A61K,A61P,C07C,C07H

Abstract:
A compound having the structure whereinR1, 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 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; R3 and R4 are independently hydrogen, OH, OR5a, OAryl, OCH2Aryl, alkyl, cycloalkyl, CF3, â€”OCHF2, â€”OCF3, halogen, â€”CN, â€”CO2R5b, â€”CO2H, COR6b, â€”CH(OH)R6c, â€”CH (OR5h)R6d, â€”CONR6R6a, â€”NHCOR5c, â€”NHSO2R5d, â€”NHSO2Aryl, Aryl, â€”SR5e, â€”SOR5f, â€”SO2R5g, â€”SO2Aryl, 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 R3 and R4 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; 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 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, S, NH, or (CH2)n, where n is 0-3, or a pharmaceutically acceptable salt, stereoisomer, or prodrug ester thereof; with the proviso that where 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, â€”OCHF2, â€”OCF3, â€”CN, â€”CO2R5b, CH(OR5h)R6d, CH(OH)R6c, COR6b, â€”NHCOR5c, â€”NHSO2R5d, â€”NHSO2Aryl, Aryl, â€”SR5e, â€”SOR5f, â€”SO2R5g or â€”SO2Aryl.