Patent ID: 6166011
Filing Date: 2000-12-26
Classification: A61K,A61P,C07D

Abstract:
A compound of the formula (I): ##STR99## or a pharmaceutically acceptable salt, or solvate thereof, wherein: X is O or S;R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are each independently H, OH, OCO(C.sub.1-6 alkyl), CO.sub.2 (C.sub.1-6 alkyl), CONH.sub.2, CONH(C.sub.1-6 alkyl), CON(C.sub.1-6 alkyl).sub.2, halo, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyloxy, C.sub.2-6 alkenyl, aryl.sup.1, C.sub.1-6 alkyl optionally substituted by one or more substituents selected from halo and C.sub.3-7 cycloalkyl, and C.sub.1-6 alkoxy optionally substituted by one or more substituents selected from fluoro and C.sub.3-7 cycloalkyl;A is unbranched alkylene of four carbons optionally substituted by up to three C.sub.1-6 alkyl groups;D is O or S;E is NH or N(C.sub.1-6 alkyl);G is C.sub.1-14 alkyl or C.sub.2-14 alkenyl, each of which is optionally substituted by one or more substituents independently selected from halo, aryl, C.sub.1-4 alkoxy, cycloalk, het and NR.sup.5 R.sup.6 ;R.sup.5 and R.sup.6 are either each independently H or C.sub.1-4 alkyl, or are taken together to form, with the nitrogen atom to which they are attached, a 4 to 7-membered heterocyclic ring optionally containing another hetero-moiety selected from NR.sup.7, O and S(O).sub.p, and which 4 to 7-membered heterocyclic ring is optionally substituted by up to 3 substituents independently selected from C.sub.1-6 alkyl and C.sub.1-6 alkoxy;R.sup.7 is H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, COR.sup.8, SO.sub.2 R.sup.8, CONR.sup.9 R.sup.10, CO.sub.2 R.sup.8 or SO.sub.2 NR.sup.9 R.sup.10 ;R.sup.8 is C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl, aryl.sup.1, or C.sub.1-6 alkyl optionally substituted by C.sub.3-7 cycloalkyl or aryl.sup.1 ;R.sup.9 and R.sup.10 are each independently H, C.sub.2-6 alkenyl, C.sub.3-7 cycloalkyl, or C.sub.1-6 alkyl optionally substituted by C.sub.3-7 cycloalkyl or aryl;p is 0, 1, or 2;wherein ""aryl"" means phenyl or naphthyl, each of which is optionally substituted by up to 3 substituents independently selected from C.sub.1-6 alkyl optionally substituted by one or more halo or C.sub.3-7 cycloalkyl groups, C.sub.2-6 alkenyl, C.sub.1-6 alkoxy, C.sub.2-6 alkenyloxy, OH, halo, NO.sub.2, phenyloxy, benzyloxy, phenyl and NII.sub.2 ;""aryl.sup.1 "" means phenyl, naphthyl or benzyl, each of which is optionally substituted by 1 or 2 substituents independently selected from C.sub.1-6 alkyl optionally substituted by one or more halo or C.sub.3-7 cycloalkyl groups, C.sub.1-6 alkoxy and halo;""cycloalk"" is C.sub.3-8 cycloalkyl optionally substituted by up to 3 substituents independently selected from C.sub.2-6 alkenyl, C.sub.1-6 alkoxy, C.sub.2-6 alkenyloxy, OH, halo, and C.sub.1-6 alkyl optionally substituted by one or more halo;and ""het"" means a 5- or 6-membered monocyclic, or 8-, 9- or 10-membered bicyclic heterocycle containing 1 to 3 heteroatoms independently selected from O, N and S, which is optionally substituted by up to 3 substituents independently selected from C.sub.1-6 alkyl optionally substituted by one or more halo or C.sub.3-7 cycloalkyl groups, C.sub.2-6 alkenyl, C.sub.1-6 alkoxy, C.sub.2-6 alkenyloxy, OH, halo, NO.sub.2, phenyloxy, benzyloxy and NH.sub.2.