Pharmaceutically active compounds

Details Pharmaceutically active compounds Pharmaceutically active compounds

C - Chemistry, Metallurgy

07

D

260/271, 260/299

C07D 471/08 (2006.01) C07D 223/04 (2006.01) C07D 487/08 (2006.01)

Patent

CA 1223873

ABSTRACT A compound of formula (I), or a pharmaceutically acceptable salt, or N-oxide thereof, or a solvate of any of the foregoing: Image (I) wherein p is 0 to 2; q is 0 to 3; j is 0 to 4; one of R5 and R6 is hydrogen, C1-6 alkyl, phenyl or phenyl-C1-3 alkyl, which phenyl moietes may be substituted by C1-6 alkyl, C1-6 alkoxy, CF3 or halogen; and the other of R5 and R6 is hydrogen or C1-6 alkyl; and - 2 - A is of formula (II): Image (II) wherein R2, R3 and R4 are each independently selected from hydrogen, halogen, CF3, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-7 acyl, C1-7 carboxylic acylamino, C1-6 alkylsulphonylamino, N-(C1-6 alkylsulphonyl)-N- C1-4 alkylamino, C1-6 alkylsulphonyl, C1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C1-4 alkylamino optionally N-substituted by one or two groups selected from C1-6 alkyl, C3-8 cycloalkyl, C3-8 cycloalkyl C1-4 alkyl, phenyl or phenyl C1-4 alkyl groups or optionally N-disubstituted by C4-5 polymethylene; or any two together are C1-2 alkylenedioxy; j is 0 to 4; and i) R1 is independently any one of the values for R2, R3 or R4 except hydrogen or together with R2 is C1-2 alkylenedioxy, C1-2 oxyalkylenethio, C2-3 alkyleneoxy or N-(C1-2 oxyalkylene)-N-C1-6 alkylamino; and one of X is CO and the other is NH; or ii) X is CO and Y is NR16 where R1 and R16 together are C1-2 alkylene; or - 3 - ii) A is of formula (III): Image (III) wherein: R2, R3 and R4 are as defined in formula (II); G is -N= or -NR13 where R13 is hydrogen or C1-4 alkyl; L is >C<; E, J and X are each independently -CHR14, -CR14=, -N= or -NR15 where R14 is hydrogen, C1-4 alkyl or C1-4 alkylthio, and R15 is hydrogen or C1-4 alkyl, or one of E, J and Z is C:B where B is O or S and the other two are each independently -CR14=, -N= or -NR15 where R14 and R15 are as defined; or E is a bond, one of J and Z is -CHR14=, -N= or -NH15 as defined and the other is -CHR14=, -N=, O or S; or iii) A is of formula (IV): Image (IV) - 4 - wherein: R1, R3 and R4 are as defined in formula (II), except that none is combined with any other variable to form a divalent group; and the nitrogen atom depicted in formula (I) is separated from the nearest nitrogen atom in the moiety A by at least 2 carbon atoms; a process therefor and compositions thereof.

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