Patent ID: 6479516
Filing Date: 2002-11-12
Classification: A61P,C07D

Abstract:
A compound of formula I, whereinR1 and R2 are each independently H or C1-4 alkyl; R3 represents aryl (optionally substituted by one or more substituents selected from the group consisting of OH, nitro, halo, CN, CH2CN, CONH2, C1-4 alkyl, C1-4 alkoxy, C1-5 alkanoyl (which latter three groups are optionally substituted by one or more halo atoms) and â€”N(R4a)(R4b) or C1-10 alkyl, wherein said alkyl group is optionally substituted, and/or terminated by one or more substituents selected from the group consisting of OR4c, S(O)nR4d, CN, halo, C1-6 alkoxy carbonyl, C2-6 alkanoyl, C2-6 alkanoyloxy, C3-8 cycloalkyl, C4-9 cycloalkanoyl, N(R5a)S(O)2R6, Het1, aryl, adamantyl (which latter two groups are optionally substituted by one or more substituents selected from the group consisting of 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)), and Wâ€”A1â€”N(R5b)(R5c); 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(R5b)(R5c) is not directly attached to an unsaturated carbon atom; p is 0, 1, or 2; R4a to R4d 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 the group consisting of 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 Het2; provided that R4d does not represent H when n represents 1 or 2; R5a to R5c 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 the group consisting of 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; or R5b and R5c together represent unbranched C2-4 alkylene group which alkylene group is optionally interrupted by O, S or NR7 group and optionally substituted by one or more C1-4 alkyl groups; R6 represents C1-6 alkyl, C3-8 cycloalkyl, C1-4 alkylphenyl or aryl, which four groups are optionally substituted by or one or more substituents selected from the group consisting of C1-4 alkyl, C1-4 alkoxy, OH, nitro, amino and halo; R7 represents H, C1-6 alkyl, C3-8 cycloalkyl, A2 (C3-8 cycloalkyl) or A2-aryl; A2 represents C1-6 alkylene; Het1, Het2 and Het3 independently represent 3- to 8-membered heterocyclic groups, which groups contain at least one heteroatom selected from the group consisting of oxygen, sulfur and 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 the group consisting of 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); Y represents R11; R11 represents H; X represents one or more substituents on the benzene ring, which substituents are independently selected from the group consisting of halo, CN, nitro, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-7 cycloalkyl (which latter four groups are optionally substituted and/or terminated by one or more substituents selected from the group consisting of halo, CN, nitro, OH, C3-7 cycloalkyl, C1-6 alkoxy, C3-7 cycloalkoxy, C1-6 alkanoyl, C4-8 cycloalkanoyl, C2-6 alkoxycarbonyl, C2-6 alkanoyloxy, and N(R15a)(R15b)), C(O)R16a, C(O)OR16b, OC(O)R16c, S(O)rOR16d, S(O)tR17a, OR16e, N(R18a)(R18b), C(O)N(R18c)(R18d), OC(O)N(R18e)(R18f), N(R18g)C(O)R16f, N(R18b)C(O)OR19, N(R18i)C(O)N(R18j)(R18k), N(R18m)S(O)2R17b and B(OR15c)2; R15a to R15c independently represent H, C1-6 alkyl or C3-7 cycloalkyl (which latter two groups are optionally substituted by one or more halo atoms); R16a to R16f independently represent H, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-7 cycloalkyl (which latter four groups are optionally substituted by one or more substituents selected from the group consisting of halo, nitro, OH, C1-4 alkyl and C1-4 alkoxy) or Het8; R17a and R17b independently represent C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-7 cycloalkyl (which latter four groups are optionally substituted by one or more substituents selected from the group consisting of halo, nitro, OH, C1-4 alkyl and C1-4 alkoxy), Het9 or N(R20a)(R20b); provided that R17a does not represent N(R20a)(R20b) when t is 1; R18a to R18m independently represent H, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-7 cycloalkyl (which latter four groups are optionally substituted by one or more substituents selected from the group consisting of halo, nitro, OH, C1-4 alkyl and C1-4 alkoxy), or Het10, or R18j and R18k together represent unbranched C3-6 alkylene, which alkylene group is optionally interrupted by oxygen, sulfur or an NR20c group; R19 represents C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-7 cycloalkyl (which latter four groups are optionally substituted by one or more substituents selected from the group consisting of halo, nitro, OH, C1-4 alkyl and C1-4 alkoxy) or Het11; R20a to R20c independently represent H, C1-4 alkyl or C3-7 cycloalkyl (which latter two groups are optionally substituted by one or more halo atoms); r is 1 or 2; t is 0, 1 or 2; Het8 to Het11 represent 4- to 7- membered heterocyclic rings, which rings contain at least one heteroatom selected from the group consisting of oxygen, sulfur and nitrogen, and which rings are optionally substituted by one or more substituents selected from the group consisting of OH, &boxH;O, nitro, amino, halo, CN, aryl, C1-4 alkyl, C1-4 alkoxy, C1-6 cycloalkyl and C1-5 alkanoyl (which latter four groups are optionally substituted by one or more halo atoms); or pharmaceutically, or veterinarily, acceptable derivatives thereof.