Patent ID: 6291475
Filing Date: 2001-09-18
Classification: A61P,C07D

Abstract:
A compound of the formula (I) ##STR26##whereinR.sup.1 and R.sup.2 independently represent H, C.sub.1-4 alkyl or together form --O--(CH.sub.2).sub.2 --O--, --(CH.sub.2).sub.4 -- or (CH.sub.2).sub.5 --;R.sup.9 represents C.sub.1-12 alkyl, phenyl, naphthyl, C.sub.1-3 alkylphenyl (which four groups are all optionally substituted or terminated by one or more substituents selected from the group consisting of --OH, halo, cyano, nitro, C.sub.1-4 alkyl or C.sub.1-4 alkoxy) or --(CH.sub.2).sub.q Cy.sup.1 ;R.sup.10 represents H or --OH;R.sup.11 represents H or C.sub.1-4 alkyl;R.sup.12 represents one or more optional substituents selected from OH, cyano, halo, amino, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, --N(H)S(O).sub.2 R.sup.16, OS(O).sub.2 R.sup.16a, --N(H)C(O)N(H)R.sup.17 or --C(O)N(H)R.sup.18 ;A represents a single bond, C.sub.1-4 alkylene, --(CH.sub.2).sub.n N(R.sup.20)--, --(CH.sub.2).sub.n S(O).sub.p --, --(CH.sub.2).sub.n O-- (in which three latter groups, the --(CH.sub.2).sub.n -- group is attached to the carbon atom bearing R.sup.10 and R.sup.11), --C(O)N(R.sup.20)-- (in which latter group, the --C(O)-- group is attached to the carbon atom bearing R.sup.10 and R.sup.11),--N(R.sup.20)C(O)O(CH.sub.2).sub.n --, --N(R.sup.20)(CH.sub.2).sub.n -- (in which two latter groups, the N(R.sup.20) group is attached to the carbon atom bearing R.sup.10 and R.sup.11) or --(CH.sub.2).sub.m C(H)(OH)(CH.sub.2).sub.n -- (in which latter group, the --(CH.sub.2).sub.m -- group is attached to the carbon atom bearing R.sup.10 and R.sup.11);B represents a single bond, C.sub.1-6 alkylene, --N(R.sup.23)(CH.sub.2).sub.r -- or --O(CH.sub.2).sub.r -- (in which two latter groups, the --(CH.sub.2).sub.r group is attached to the bispidine nitrogen atom);m represents 1, 2 or 3;n and r independently represent 0, 1, 2, 3 or 4;p represents 0, 1 or 2;q represents 0; 1, 2 or 3;X represents O or S;Cy.sup.1 represents a five to seven-membered heterocyclic ring containing one or more heteroatom selected from O, N or S, which ring is optionally substituted by one or more substituent selected from C(O)R.sup.21 or C(O) OR.sup.22 ;R.sup.16, R.sup.16a, R.sup.20 and R.sup.23 independently represent H or C.sub.1-4 alkyl; andR.sup.17, R.sup.18, R.sup.21 and R.sup.22 independently represent H or C.sub.1-6 alkyl;with the proviso that when R.sup.9 is phenyl, and R.sup.10 and R.sup.11 are hydrogen, both A and B are not single bonds;or a pharmaceutically acceptable derivative thereof.