| abstract |
A compound of the formula: or one of its pharmaceutically acceptable salts or radiolabeled forms, where: month 0; one of R1 and R2 is hydrogen, acyl, acyloxy, alkenyl, alkoxy, alkoxyalkoxy, alkoxyalkyl, alkoxycarbonyl, alkoxyimino, alkoxysulfonyl, alkyl, alkylcarbonyl, alkylsulfonyl, alkynyl, amido, carboxy, cyano, cycloalkyl, fluoroalkoxy, haloalkoxy, haloalkoxy, haloalkoxy , hydroxyalkyl, mercapto, nitro, alkylthio, -NRARB, (NRARB) carbonyl, -SO2N (R14a) (R14b), -N (R14a) SO2 (R14b), a group of formula -L2-R6, or a group of formula -L3a-R6a-L3b-Rab; the other of R1 and R2 is selected from the group consisting of hydrogen, cyano, halogen, alkyl, cycloalkyl, fluoroalkyl, alkoxy, alkoxyalkyl, fluoroalkoxy, alkylthio, -SO2N (R14a) (R14b), and -N (R14a) SO2 (R14b ); R3a and R3b are each independently selected from the group consisting of hydrogen, cyano, halogen; alkyl, cycloalkyl, fluoroalkyl, alkoxy, alkoxyalkyl, fluoroalkoxy, alkylthio, -SO2N (R14a) (R14b), and -N (R14a) SO2 (R14b); R4 and R5 are each independently selected from the group consisting of alkyl, fluoroalkyl, hydroxyalkyl, alkoxyalkyl, and cycloalkyl; or R4 and R5 taken together with the nitrogen atom to which they are attached form an aromatic ring; R6 is aryl, heterocycle or heterocycloalkyl; R6a is aryl or heterocycle; R6b is aryl or heterocycle; L is a bond or alkylene; L2 is a bond, -O-, alkylene, -C (= O) -, -S-, -SO2N (R14a) -, -N (R14a) SO2-, -C (O) N (R14a) -, - N (R14a) C (O) -, or -N (R15) -; L3a and L3b are each independently selected from the group consisting of a bond, -O-, alkylene, -C (= O) -, -S- , -SO2N (R14a) -, -N (R14a) SO2--, -C (O) N (R14a) -, -N (R14a) C (O) -, and -N (R15) -; R10 is selected from the group consisting of hydrogen, cyano, fluoro, hydroxy, and alkyl; R14a and R14b are each independently selected at each occurrence of the group consisting of hydrogen, alkyl, and cycloalkyl; R is selected from the group consisting of hydrogen, alkyl, acyl, alkoxycarbonyl, and (R14a) (R14b) NC (O) -; and RA and RB are independently selected from hydrogen, alkyl, acyl, haloalkyl, alkoxycarbonyl, cycloalkyl, and formyl. |