Patent ID: 6380396
Filing Date: 2002-04-30
Classification: A61P,C07D

Abstract:
A compound selected from compounds according to any one of the formulae: whereinR is phenyl, C3-C7 cycloalkyl or heteroaryl, each of which being optionally benzo- or C3-C7 cycloalkyl-fused and optionally substituted, including in the benzo- or C3-C7 cycloalkyl-fused portion, by from 1 to 3 substituents each independently selected from C1-C4 alkyl, fluoro(C1-C4)alkyl, C1-C4 alkoxy, fluoro(C1-C4)alkoxy, phenoxy, C2-C4 alkanoyl, halo, C1-C4 alkoxycarbonyl, C3-C7 cycloalkyl, â€”S(O)m(C1-C4 alkyl), cyano, â€”NR2R3, â€”S(O)mNR2R3, â€”NR4(C1-C4 alkanoyl) and â€”CONR2R3, or R is 2,3-dihydrobenzo[b]furanyl or chromanyl; R1 is H or C1-C6 alkyl; R2 and R3 are either each independently selected from H and C1-C6 alkyl, or when taken together, represent C4-C6 alkylene; R4 is H or C1-C6 alkyl; m is 0, 1 or 2; W is a direct link, methylene or ethylene; X is unbranched C2-C4 alkylene; Ar is phenyl, naphthyl, benzyl, thienyl, benzo[b]thienyl or indolyl, each of which being optionally substituted by from 1 to 3 substituents each independently selected from C1-C4 alkyl, fluoro(C1-C4)alkyl, C1-C4 alkoxy, fluoro(C1-C4)alkoxy, halo and cyano, or Ar is 1,3-benzodioxolan-4 or 5-yl or 1,4-benzodioxan-5 or 6-yl; â€œheteroarylâ€ , used in the definition of R, means thienyl or a 5- or 6-membered ring heteroaryl group containing either from 1 to 4 nitrogen heteroatoms, or 1 or 2 nitrogen heteroatom(s) and 1 oxygen or sulphur heteroatom, with the proviso that when W is a direct link and R is optionally fused and optionally substituted heteroaryl, said heteroaryl is linked by a ring carbon atom to the carbonyl group; Z is a leaving group capable of forming a pharmaceutically acceptable anion (ZA), Z1 is a laving group and P is a protecting group; with the proviso that for a compound of the formula (XXIII), when R1 is H and â€œC1-C3 alkyleneâ€  is CH2, then Ar is not 2-chlorophenyl or 2,4-dichlorophenyl.