Patent ID: 6221898
Filing Date: 2001-04-24
Classification: A61P,C07C,C07D,C07F

Abstract:
A compound of formula I, ##STR15##whereinone of R.sup.1 and R.sup.2 represents a structural fragment of formula Ia ##STR16##and the other represents R.sup.4 ;Z represents O or N(R.sup.5);R.sup.3 represents one or more optional substituents selected from OH, halo, cyano, nitro, C(O)OR.sup.6, C.sub.1-6 alkoxy or C.sub.1-6 alkyl (which two latter groups are optionally substituted and/or terminated by one or more halo or hydroxy group) or N(R.sup.7)R.sup.8 ;R.sup.4 represents H, OH, halo, cyano, nitro, C(O)OR.sup.6, C.sub.1-6 alkoxy or C.sub.1-6 alkyl (which two latter groups are optionally substituted and/or terminated by one or more halo or hydroxy group) or N(R.sup.7)R.sup.8 ;Ar.sup.1 represents phenyl, C.sub.1-3 alkylphenyl, C.sub.1-3 alkyldiphenyl, C.sub.3-7 cycloalkyl, C.sub.1-3 -alkyl-C.sub.3-7 -cycloalkyl, C.sub.1-3 -alkyl-di-C.sub.3-7 -cycloalkyl, naphthyl, C.sub.1-3 alkylnaphthyl, thienyl, imidazolyl or isoxazolyl, all of which may be substituted by one or more substituent selected from OH, halo, cyano, nitro, C(O)OR.sup.6, C.sub.1-6 alkoxy or C.sub.1-6 alkyl (which two latter groups are optionally substituted and/or terminated by one or more halo or hydroxy group) or N(R.sup.7)R.sup.8 ;R.sup.5 represents H, C.sub.1-6 alkyl, phenyl or C.sub.1-3 alkylphenyl (which three latter groups are optionally substituted and/or terminated by one or more substituent selected from OH, halo, cyano, nitro, C(O)OR.sup.9, C(O)N(R.sup.10)R.sup.11, P(O)(R.sup.12)R.sup.13, P(O)(OR.sup.14)OR.sup.15, S(O).sub.2 (R.sup.16)R.sup.17, S(O).sub.2 N(R.sup.18)R.sup.19, C.sub.1-6 alkoxy or C.sub.1-6 alkyl (which two latter groups are optionally substituted and/or terminated by one or more halo or hydroxy group) or N(R.sup.20)R.sup.21);Y represents O, S, S(O), S(O).sub.2 or N(R.sup.22);R.sup.10 and R.sup.11 independently represent H, OR.sup.23, C(O)R.sup.24, OC(O)R.sup.25, C(O)OR.sup.26, C.sub.1-4 alkyl, (which latter group is optionally substituted and/or terminated by one or more substituent selected from C.sub.1-4 alkyl, OR.sup.27, N(R.sup.28)R.sup.29, C(O)OR.sup.30 C(O)N(R.sup.31)R.sup.32, P(O)(R.sup.33)R.sup.34, P(O)(OR.sup.35)OR.sup.36 and S(O).sub.2 N(R.sup.37)R.sup.38), --(CH.sub.2 CH.sub.2 O--).sub.p R.sup.39 or, together with the nitrogen atom to which they are attached, form a C.sub.4-7 nitrogen-containing, aromatic or non-aromatic, ring which ring may contain a further heteroatom or group (as appropriate) selected from O, S and N(R.sup.40) and may further be substituted by one or more substituent selected from C(O)R.sup.41, C(O)OR.sup.42 or C(O)N(R.sup.43)R.sup.44 ;R.sup.28, R.sup.29, R.sup.30, R.sup.31, R.sup.32 and R.sup.40 independently represent H or C.sub.1-6 alkyl, which latter group is optionally substituted and/or terminated by one or more substituent selected from C(O)R.sup.45, C(O)OR.sup.46 or C(O)N(R.sup.47)R.sup.48 ;at each occurance, R.sup.6, R.sup.7 and R.sup.8 independently represent H or C.sub.1-4 alkyl; R.sup.9 R.sup.12 R.sup.13, R.sup.14, R.sup.15, R.sup.16, R.sup.17, R.sup.18, R.sup.19, R.sup.20, R.sup.21, R.sup.22, R.sup.23, R.sup.24, R.sup.25, R.sup.26, R.sup.27, R.sup.33, R.sup.34, R.sup.35, R.sup.36, R.sup.37, R.sup.38, R.sup.39, R.sup.41, R.sup.42, R.sup.43, R.sup.44, R.sup.45, R.sup.46, R.sup.47 and R.sup.48 independently represent H or C.sub.1-4 alkyl;n represents 0, 1, 2, 3 or 4;p represents 1, 2, 3, 4, 5 or 6; andB represents a structural fragment of formula Ib, Ic, Id or Ie ##STR17##whereinX.sup.1 and X.sup.2 independently represent a single bond or CH.sub.2 ;or a pharmaceutically acceptable salt thereof, provided that when:(i) B represents a structural fragment of formula Ic;(ii) n represents 0 to 4;(iii) either of R.sup.1 or R.sup.2 represents a structural fragment of formula Ia, and the other represents R.sup.4 in which:(a) Z represents O or N(Rs) (in which R.sup.5 represents H, C.sub.1-6 alkyl, phenyl or C.sub.1 alkylphenyl); and(b) Ar.sup.1 represents phenyl, optionally substituted by one or more substituents selected from OH, halo, cyano, nitro, C(O)OR.sup.6 (in which R.sup.6 is H or methyl), C.sub.1-6 alkoxy, C.sub.1-2 alkoxy substituted by F, C.sub.1-6 alkyl optionally substituted by hydroxy or N(R.sup.7)R.sup.8 (in which R.sup.7 and R.sup.8 both represent H or C.sub.1-4 alkyl or one of R.sup.7 represents H and the other represents C.sub.1-4 alkyl); and(iv) R.sup.3 and/or R.sup.4 represents H, OH, halo, cyano, nitro, C(O)OR.sup.6 (in which R.sup.6 is H or C.sub.1-4 alkyl), C.sub.1-4 alkyl, C.sub.1 alkyl substituted by fluoro, C.sub.1-6 alkyl substituted by OH or C.sub.1-4 alkoxy; then Y does not represent O, S or N(R.sup.22) (in which R.sup.22 represents H or C.sub.1-4 alkyl).