Patent ID: 6495549
Filing Date: 2002-12-17
Classification: A61K,A61P,C07D

Abstract:
A method of treating neuronal degeneration comprising administering an effective amount of a compound of the formula (I): or a pharmaceutically acceptable salt, or solvate thereof, wherein:X is O or S; R1, R2, R3, and R4 are each independently H, OH, OCO(C1-6 alkyl), CO2(C1-6 alkyl), CONH2, CONH(C1-6 alyl), CON(C1-6 alkyl)2, halo, C3-7 cycloalkyl, C3-7 cycloalkyloxy, C2-6 alkenyl, aryl1, C1-6 alkyl optionally substituted by one or more substituents selected from halo and C3-7 cycloalkyl, and C1-6 alkoxy optionally substituted by one or more substituents selected from fluoro and C3-7 cycloalkyl; A is unbranched alkylene of four carbons optionally substituted by up to three C1-6 alkyl groups; D is O or S; E is NH or N(C1-6 alkyl); G is C1-14 alkyl or C2-14 alkenyl, each of which is optionally substituted by one or more substituents independently selected from halo, aryl, C1-4 alkoxy, cycloalk, bet and NR5R6; R5 and R6 are either each independently H or C1-4 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 NR7, O and S(O)p, and which 4 to 7-membered heterocyclic ring is optionally substituted by up to 3 substituents independently selected from C1-6 alkyl and C1-6 alkoxy; R7is H, C1-6 alkyl, C2-6 alkenyl, COR8, SO2R8, CO NR9R10, CO2R8 or SO2NR9R10; R8 is C3-7 cycloalkyl, C2-6 alkenyl, aryl1, or C1-6 alkyl optionally substituted by C3-7 cycloalkly or aryl1; R9 and R10 are each independently H, C2-6 alkenyl, C3-7 cycloalkyl, or C1-6 alkyl optionally substituted by C3-7 cycloalkyl or aryl; p is 0, 1, or 2; wherein â€œarylâ€  means phenyl or naphthyl, each of which is optionally substituted by up to 3 substituents independently selected from C1-6 alkyl optionally substituted by one or more halo or C3-7 cycloalkyl groups, C2-4 alkenyl, C1-6 alkoxy, C2-6 alkenyloxy, OH, halo, NO2, phenyloxy, benzyloxy, phenyl and NH2; â€œarylâ€  means phenyl, naphthyl or benzyl, each of which is optionally substituted by 1 or 2 substituents independently selected from C1-6 alkyl optionally substituted by one or more halo or C3-7 cycloalkyl groups, C1-6 alkoxy and halo; â€œcycloalkâ€  is C3-8 cycloalkyl optionally substituted by up to 3 substituents independently selected from C2-6 aLkenyl, C1-6 alkoxy, C2-6 alkenyloxy, OH, halo, and C1-6 alkyl optionally substituted by one or more halo; and â€œhetâ€  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 C1-6 alkyl optionally substituted by one or more halo or C3-7 cycloalkyl groups, C2-6 alkenyl, C1-6 alkoxy, C2-6 alkenyloxy, OH, halo, NO2, phenyloxy, benzyloxy and NH2.