Patent ID: 6441000
Filing Date: 2002-08-27
Classification: A61P,C07D

Abstract:
A compound of formula I, wherein Het1 represents an imidazole group;T represents one or more optional substituents selected from H, halo, OH, &boxH;O, C1-6 alkyl, C1-6 alkoxy, C3-6 cycloalkyl (which latter three groups are optionally substituted by one or more halo atoms), aryl(C1-6)alkyl (the aryl part of which is optionally substituted by one or more substituents selected from halo, C1-4 alkyl and C1-4 alkoxy (which latter two groups are optionally substituted by one or more halo atoms)), â€”N(R4a)(R5), â€”N(R4b)S(O)mR6, â€”N(R4c)C(O)R7a and â€”N(R4d)C(O)OR7b, provided that when Het1 contains less than three C-atoms (i.e. where the only two C-atoms are those provided by the fused benzene ring) and at least one heteroatom selected from oxygen and sulfur, then T does not represent halo or C1-6 alkoxy (which latter group is optionally substituted by one or more halo atoms); R4a to R4d and R5 independently represent H, C1-6 alkyl (which latter group is optionally substituted by one or more halo atoms), or R4a and R5, together with the nitrogen atom to which they are attached, form a 4- to 6-membered heterocyclic ring (which ring is optionally substituted by one or more substituents selected from C1-4 alkyl, C1-4 alkoxy, OH, &boxH;O, nitro, amino or halo); R6 represents C1-6 alkyl or aryl, which two groups are optionally substituted by one or more substituents selected from halo, C1-4 alkyl or nitro; R7a and R7b independently represent C1-6 alkyl, C1-6 alkoxy, C3-6 cycloalkyl, aryl (which four groups are optionally substituted by one or more substituents selected from halo, C1-4 alkyl or nitro), or R7a represents H; m is 0, 1 or 2; R1 and R2 are each independently H or C1-4 alkyl; R3 represents C1-10 alkyl, C3-10 alkenyl or C3-10 alkynyl wherein said alkyl, alkenyl or alkynyl groups are optionally substituted and/or terminated by one or more substituents selected from OR8c, S(O)nR8d, CN, halo, C1-6 alkoxy carbonyl, C2-6 alkanoyl, C2-6 alkanoyloxy, C3-8 cycloalkyl, C4-9 cycloalkanoyl, N(R9a)S(O)2R10, Het2, aryl, adamantyl (which latter two groups are optionally substituted by one or more substituents selected from OH, nitro, amino, halo, CN, CH2CN, CONH2, C1-4 alkyl, C1-4 alkoxy and C1-5 alkanoyl (which latter three groups are optionally substituted by one or more halo atoms)), or â€”Wâ€”A1â€”N(R9b)(R9c); n is 0, 1 or 2; W represents a single bond, C(O) or S(O)p; A1 represents a single bond or C1-10 alkylene; provided that when both W and A1 represent single bonds, then the group â€”N(R9b)(R9c) is not directly attached to an unsaturated carbon atom; p is 0, 1 or 2; R8a to R8d each independently represent H, C1-10 alky, C3-10 alkenyl, C3-10 alkynyl, C3-8 cycloalkyl, C1-4 alkylphenyl, aryl (which latter six groups are optionally substituted by or one or more substituents selected from OH, nitro, amino, halo, CN, CH2CN, CONH2, C1-4 alkyl, C1-4 alkoxy and C1-5 alkanoyl (which latter three groups are optionally substituted by one or more halo atoms)) or Het3; provided that R8d does not represent H when n represents 1 or 2; R9a to R9c each independently represent H, C1-10 alkyl, C3-10 alkenyl, C3-10 alkynyl, C3-8 cycloalkyl, C1-4 alkylphenyl, aryl (which latter six groups are optionally substituted by or one or more substituents selected from OH, nitro, amino, halo, CN, CH2CN, CONH2, C1-4 alkyl, C1-4 alkoxy and C1-5 alkanoyl (which latter three groups are optionally substituted by one or more halo atoms)), Het4, or R9b and R9c together represent unbranched C2-6 alkylene which alkylene group is optionally interrupted by O, S and/or an N(R11) group and is optionally substituted by one or more C1-4 alkyl groups; R10 represents C1-4 alkyl, C3-8 cycloalkyl, C1-4 alkylphenyl or aryl, which four groups are optionally substituted by or one or more substituents selected from C1-4 alkyl, C1-4 alkoxy, OH, nitro, amino or halo; R11 represents H, C1-6 alkyl, C3-8 cycloalkyl, A2â€”(C3-8 cycloalkyl) or A2-aryl; A2 represents C1-6 alkylene; Het2, Het3 and Het4 independently represent 3- to 8-membered heterocyclic groups, which groups contain at least one heteroatom selected from oxygen, sulfur and/or nitrogen, which groups are optionally fused to a benzene ring, and which groups are optionally substituted in the heterocyclic and/or fused benzene ring part by one or more substituents selected from OH, &boxH;O, nitro, amino, halo, CN, aryl, C1-4 alkyl, C1-4 alkoxy and C1-5 alkanoyl (which latter three groups are optionally substituted by one or more halo atoms); X represents one or two optional substituents on the benzene ring, which substituents are selected from halo, C1-4 alkyl, C1-4 alkoxy (which latter two groups are optionally substituted by one or more halo atoms); or pharmaceutically, or veterinarily, acceptable derivatives thereof.