Patent TW-200406208-A (TW)
Title: New compounds
Inventor: EBDEN MARK RICHARD
IPC: A61K31/505
Filed: 2003-07-25
Abstract: A compound of formula (1), pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof: wherein R1 is a group selected from C3-7carbocyclyl, C1-8alkyl, C2-6alkenyl and C2-6alkynyl; wherein the group is optionally substituted by 1,2 or 3 substituents independently selected from fluoro, nitrile, -OR4, -NR5R6, -CONR5R6, -COOR7, -NR8COR9, -SR10, -SO2R10, -SO2NR5R6, -NR8SO2R9, phenyl or heteroaryl; wherein phenyl and heteroaryl are optionally substituted by 1, 2 or 3 substituents independently selected from halo, cyano, nitro, -OR4, -NR5R6, -CONR5R6, -COOR7, -NR8COR9, -SR10, -SO2R10, -SO2NR5R6, -NR8SO2R9, C1-6alkyl and trifluoromethyl; wherein R2 is C3-7carbocyclyl, optionally substituted by 1, 2 or 3 substituents independently selected from: (a) fluoro, -OR4, -NR5R6 -CONR5R6, -COOR7, -NR8COR9, -SR10, -SO2R10, -SO2NR5R6, -NR8SO2R9; (b) a 3-8 membered ring optionally containing 1, 2 or 3 atoms selected from O, S, -NR8 and whereby the ring is optionally substituted by C1-3alkyl or fluoro; or (c) phenyl or heteroaryl, each of which is optionally substituted by 1, 2 or 3 substituents independently selected from halo, cyano, nitro, -OR4, -NR5R6, -CONR5R6, -NR8COR9, - SO2NR5R6, -NR8SO2R9, C1-6alkyl and trifluoromethyl; or R2 is a group selected from C1-8alkyl, C2-6alkenyl or C2-6alkynyl wherein the group is substituted by 1,2 or 3 substituents independently selected from hydroxy, amino, C1-6alkoxy, C1-6alkylamino, di(C1-6alkyl)amino, N-(C1-6alkyl)-N-(phenyl)amino, N-C1-6alkylcarbamoyl, N,N-di(C1-6alkyl)carbamoyl, N-(C1-6alkyl)-N-(phenyl)carbamoyl, carboxy, phenoxycarbonyl, -NR8COR9, -SO2R10, -SO2NR5R6 and -NR8SO2R9; wherein R3 is hydrogen or independently R2; R4 is hydrogen or a group selected from C1-6alkyl and phenyl, wherein the group is optionally substituted by 1 or 2 substituents independently selected from halo, phenyl, -OR11 and -NR12R13; R5 and R6 are independently hydrogen or a group selected from C1-6alkyl and phenyl wherein the group is optionally substituted by 1, 2 or 3 substituents independently selected from halo, phenyl, -OR14, -NR15R16, -COOR14, -CONR15R16, -NR15COR16, -SO2R10, -SONR15R16 and NR15SO2R16 or R5 and R6 together with the nitrogen atom to which they are attached form a 4- to 7-membered saturated heterocyclic ring system optionally containing a further heteroatom selected from oxygen and nitrogen atoms, which ring is optionally substituted by 1, 2 or 3 substituents independently selected from phenyl, -OR14, -COOR14, -NR15R16, -CONR15R16, -NR15COR16, -SO2R10, -SONR15R16, NR15SO2R16 or C1-6alkyl (optionally substituted by 1 or 2 substituents independently selected from halo, -NR15R16 and -OR17 groups); R10 is hydrogen or a group selected from C1-6alkyl or phenyl, wherein the group is optionally substituted by 1, 2 or 3 substituents independently selected from halo, phenyl, -OR17 and - NR15R16; and each of R7, R8, R9, R11, R12, R13, R14, R15, R16, R17 is independently hydrogen, C1-6alkyl or phenyl; X is hydrogen, halo, cyano, nitro, hydroxy, C1-6alkoxy (optionally substituted by 1 or 2 substituents selected from halo, -OR11 and -NR12R13), -NR5R6, -COOR7, -NR8COR9, thio, C1-6alkylthio (optionally substituted by 1 or 2 substituents selected from halo, -OR17, -NR15R16), -SO2R10 or a group selected from C3-7carbocyclyl, C1-8alkyl, C2-6alkenyl or C2-6alkynyl, wherein the group is optionally substituted by 1,2 or 3 substituents independently selected from halo, -OR4, -NR5R6, -CONR5R6, -COOR7, -NR8COR9, -SR10, -SO2R10, -SO2NR5R6 and -NR8SO2R9; Rx is trifluoromethyl, -NR5R6, phenyl, napthyl, monocyclic or bicyclic heteroaryl wherein a heteroring may be partially or fully saturated and one or more ring carbon atoms may form a carbonyl group, and wherein each phenyl or heteroaryl group is optionally substituted by 1, 2 or 3 substituents independently selected from halo, cyano, nitro, -OR4, -NR5R6, -CONR5R6, -COR7, -COOR7, -NR8COR9, -SR10, -SO2R10, -SO2NR5R6, -NR8SO2R9, C1-6alkyl or trifluoromethyl; or Rx is a group selected from C3-7carbocyclyl, C1-8alkyl, C2-6alkenyl and C2-6alkynyl whereby the group is optionally substituted by 1, 2 or 3 substituents independently selected from halo, -OR4, -NR5R6, -CONR5R6, -COR7, -COOR7, -NR8COR9, -SR10, -SO2R10, -SO2NR5R6, -NR8SO2R9, phenyl or heteroaryl; and wherein each phenyl or heteroaryl group is optionally substituted by 1,2 or 3 substituents independently selected from halo, cyano, nitro, -OR4, -NR5R6, -CONR5R6, -COR7, -COOR7, -NR8COR9, -SR10, -SO2R10, -SO2NR5R6, -NR8SO2R9, C1-6alkyl or trifluoromethyl; or Rx and X together form a 4 to 8-membered sulfonamide ring optionally substituted by 1, 2 or 3 substituents independently selected from halo, -OR4, -NR5R6, -CONR5R6, -COOR7, - NR8COR9, -SR10, -SO2R10, -SO2NR5R6, -NR8SO2R9, phenyl or heteroaryl; wherein phenyl and heteroaryl are optionally substituted by 1, 2 or 3 substituents independently selected from halo, cyano, nitro, -OR4, -NR5R6, -CONR5R6, -COOR7, -NR8COR9, -SR10, -SO2R10, -SO2NR5R6, -NR8SO2R9, C1-6alkyl and trifluoromethyl.