Patent ID: 6337343
Filing Date: 2002-01-08
Classification: A61P,C07D

Abstract:
A compound of formula I, whereinp and q independently represent 0, 1, 2, 3 or 4; R1 represents H, 2,3-epoxypropyl, C1-6 alkyl (which latter group is optionally substituted or terminated by one or more hydroxy group), a structural fragment of formula Ia wherein A1 represents a single bond or C1-4 alkylene and RX represents H or C1-4 alkyl, provided that there are no more than six carbon atoms in the chain RXâ€”Câ€”Câ€”A1, or, when p represents 0, together with R2 represents a structural fragment of formula Ib, whereinRy represents H or C1-3 alkyl; R2 represents H, Si(Me)3, naphthyl, indolyl, CHR21R22 or C1-4 alkyl (which latter group is optionally substituted or terminated by one or more fluorine or hydroxy group) or C3-8 cycloalkyl or phenyl (which latter two groups are optionally substituted by one or more of C1-4 alkyl, C1-4 alkoxy, halo, hydroxy, cyano, nitro, methylenedioxy, trifluoromethyl, N(H)R23, C(O)OR24), or, when p represents 0, together with R1 represents a structural fragment of formula Ib; R3 represents H, Si(Me)3, naphthyl, indolyl, CHR25R26 or C1-6 alkyl (which latter group is optionally substituted or terminated by one or more fluorine or hydroxy group) or C3-8 cycloalkyl or phenyl (which latter two groups are optionally substituted by one or more of C1-4 alkyl, C1-4 alkoxy, halo, hydroxy, cyano, nitro, methylenedioxy, trifluoromethyl, N(H)R27 C(O)OR28); R21, R22, R25 and R26 independently represent cyclohexyl or phenyl; R23 and R27 independently represent H, C1-4 alkyl or C(O)R29; R24, R28 and R29 independently represent H or C1-4 alkyl; R4 represents H or C1-4 alkyl; Y represents C2 alkylene optionally substituted by C1-4 alkyl, hydroxy, methylene or oxo; n represents 0, 1, 2, 3 or 4; and B represents a structural fragment of formula IVa, IVb or IVc whereinR5 represents H, halo or C1-4 alkyl; and X1 and X2 independently represent a single bond or CH2; provided that when B represents a structural fragment of formula IVa, in which R5 is H, a structural fragment of formula IVb, in which X1 and X2 are both CH2, or a structural fragment of formula IVc; n represents 1; R4 represents H; and R1 represents H or C1-6 alkyl; then (i) when q represents 0 and R3 represents H, then: (1) R2 does not represent unsubstituted C1-4 alkyl, Si(Me)3, naphthyl, indolyl, or C3-8 cycloalkyl or phenyl (which latter two groups are optionally substituted by one or more of C1-4 alkyl C1-4 alkoxy, halo, hydroxy, methylenedioxy, trifluoromethyl and C(O)OR24); and (2) the group â€”(CH2)pâ€”R2 does not represent C1-6 alkyl substituted by OH; (ii) when p represents 0 and R2 represents H; then: (1) R3 does not represent unsubstituted C1-6 alkyl, Si(Me)3, naphthyl, indolyl, or C3-8 cycloalkyl or phenyl (which latter two groups are optionally substituted by one or more of C1-4 alkyl, C1-4 alkoxy, halo, hydroxy, methylenedioxy, trifluoromethyl and C(O)OR28); and (2) the group â€”(CH2)qâ€”R3 does not represent C1-6 alkyl substituted by OH; and (iii) R2 does not represent H or unsubstituted C1-4 alkyl when R3 represents H or unsubstituted C1-6 alkyl and the total number of carbon atoms in the structural fragment â€”C((CH2)pR2)((CH2)qR3)â€” is six or less; or a pharmaceutically acceptable salt thereof.