Patent ID: 6218393
Filing Date: 2001-04-17
Classification: A61P,C07D

Abstract:
A compound which is an anthranilic acid of formula (I): ##STR330##whereineach of R, R.sup.1 and R.sup.2, which are the same or different, is H, C.sub.1 -C.sub.6 alkyl, OH, C.sub.1 -C.sub.6 alkoxy, halogen, nitro, or N(R.sup.10 R.sup.11) wherein each of R.sup.10 and R.sup.11, which are the same or different, is H or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2, being attached to adjacent positions of ring b, together form a methylenedioxy or ethylenedioxy group;R.sup.3 is H or C.sub.1 -C.sub.6 alkyl;R.sup.4 is C.sub.1 -C.sub.6 alkyl or R.sup.4 represents --CH.sub.2 -- or --CH.sub.2 CH.sub.2 -- which is attached either (i) to position 2 of ring b to complete a saturated 5- or 6-membered nitrogen-containing ring fused to ring b, or (ii) to the position in ring a adjacent to that to which X, being a single bond, is linked, thereby completing a saturated 5- or 6-membered nitrogen-containing ring fused to ring a;R.sup.5 is H, OH or C.sub.1 -C.sub.6 alkyl;X is a direct bond, O, S, --S--(CH.sub.2).sub.p -- or --O--(CH.sub.2).sub.p -- wherein p is an integer of 1 to 6;R.sub.6 is H, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy;q is 0 or 1;Ar is an unsaturated carbocyclic or heterocyclic group;each of R.sup.7 and R.sup.8, which are the same or different, is H, C.sub.1 -C.sub.6 alkyl which is unsubstituted or substituted, C.sub.1 -C.sub.6 alkoxy, hydroxy, halogen, phenyl, --NHOH, nitro, a group N(R.sup.10 R.sup.11) as defined above or a group SR.sup.12 wherein R.sup.12 is H or C.sub.1 -C.sub.6 alkyl; or R.sup.7 and R.sup.8, when situated on adjacent carbon atoms, form together with the carbon atoms to which they are attached a benzene ring or a methylenedioxy substituent;R.sup.9 is phenyl or an unsaturated heterocyclic group, each of which is unsubstituted or substituted by C.sub.1 -C.sub.6 alkyl, OH, C.sub.1 -C.sub.6 alkoxy, halogen, C.sub.3 -C.sub.6 cycloalkyl, phenyl, benzyl, trifluoromethyl, nitro, acetyl, benzoyl or N(R.sup.10 R.sup.11) as defined above, or two substituents on adjacent ring positions of the said phenyl or heterocyclic group together complete a saturated or unsaturated 6-membered ring or form a methylenedioxy group;n is 0 or 1; andm is 0 or an integer of 1 to 6;or a pharmaceutically acceptable salt thereof.