Patent ID: 6051568
Filing Date: 2000-04-18
Classification: A61P,C07D

Abstract:
A compound of formula I, ##STR15## wherein p and q independently represent 0, 1, 2, 3 or 4;R.sup.1 represents H, 2,3-epoxypropyl, C.sub.1-6 alkyl (which latter group is optionally substituted or terminated by one or more hydroxy group), a structural fragment of formula Ia ##STR16## wherein A.sup.1 represents a single bond or C.sub.1-4 alkylene and R.sup.X represents H or C.sub.1-4 alkyl, provided that there are no more than six carbon atoms in the chain R.sup.X -C-C-A.sup.1, or, when p represents 0, together with R.sup.2 represents a structural fragment of formula Ib, ##STR17## wherein R.sup.y represents H or C.sub.1-3 alkyl; R.sup.2 represents H, Si(Me).sub.3, naphthyl, indolyl, CHR.sup.21 R.sup.22 or C.sub.1-4 alkyl (which latter group is optionally substituted or terminated by one or more fluorine or hydroxy group) or C.sub.3-8 cycloalkyl or phenyl (which latter two groups are optionally substituted by one or more of C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halo, hydroxy, cyano, nitro, methylenedioxy, trifluoromethyl, N(H)R.sup.23, C(O)OR.sup.24), or, when p represents 0, together with R.sup.1 represents a structural fragment of formula Ib;R.sup.3 represents H, Si(Me).sub.3, naphthyl, indolyl, CHR.sup.25 R.sup.26 or C.sub.1-6 alkyl (which latter group is optionally substituted or terminated by one or more fluorine or hydroxy group) or C.sub.3-8 cycloalkyl or phenyl (which latter two groups are optionally substituted by one or more of C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halo, hydroxy, cyano, nitro, methylenedioxy, trifluoromethyl, N(H)R.sup.27 C(O)OR.sup.28);R.sup.21, R.sup.22, R.sup.25 and R.sup.26 independently represent cyclohexyl or phenyl;R.sup.23 and R.sup.27 independently represent H, C.sub.1-4 alkyl or C(O)R.sup.29 ;R.sup.24, R.sup.28 and R.sup.29 independently represent H or C.sub.1-4 alkyl;R.sup.4 represents H or C.sub.1-4 alkyl;Y represents CH.sub.2 ;n represents 0, 1, 2, 3 or 4; andB represents a structural fragment of formula IVa, IVb or IVc ##STR18## wherein R.sup.5 represents H, halo or C.sub.1-4 alkyl; andX.sup.1 and X.sup.2 independently represent a single bond or CH.sub.2 ;provided that(a) when B represents a structural fragment of formula IVa, in which R.sup.5 is H. a structural fragment of formula IVb, in which X.sup.1 and X.sup.2 are both CH.sub.2, or a structural fragment of formula IVc;n represents 1;R.sup.4 represents H; andR.sup.1 represents H or C.sub.1-6 alkyl; then(i) when q represents 0 and R.sup.3 represents H, then:--(1) R.sup.2 does not represent unsubstituted C.sub.1-4 alkyl, Si(Me).sub.3, naphthyl, indolyl, or C.sub.3-8 cycloalkyl or phenyl (which latter two groups are optionally substituted by one or more of C.sub.1-4 alky, C.sub.1-4 alkoxy, halo, hydroxy, methylenedioxy, trifluoromethyl and C(O)OR.sup.24); and(2) p does not represent 0, 1 or 2 when R.sup.2 represents C.sub.1-4 alkyl terminated by OH; or(ii) when p represents 0 and R.sup.2 represents H; then:--(1) R.sup.3 does not represent C.sub.1-6 alkyl, Si(Me).sub.3, naphthyl, indolyl, or C.sub.3-8 cycloalkyl or phenyl (which latter two groups are optionally substituted by one or more of C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halo, hydroxy, methylenedioxy, trifluoromethyl and C(O)OR.sup.28); and(2) q does not represent 0 when R.sup.3 represents C.sub.1-4 alkyl terminated by OH; or(iii) R.sup.2 does not represent H or unsubstituted C.sub.1-4 alkyl when R.sup.3 represents H or unsubstituted C.sub.1-6 alkyl and the total number of carbon atoms in the structural fragment -C((CH.sub.2).sub.p R.sup.2)((CH.sub.2).sub.q R.sup.3)- is less than six;or a pharmaceutically acceptable salt thereof.