Patent ID: 6608078
Filing Date: 2003-08-19
Classification: A61K,A61P,C07D

Abstract:
A compound of formula I X is hydrogen, X is C1-C20 alkyl, aralkyl, â€”(CH2)n-CHR10â€”OCOR11, or (CH2)nâ€”CHR10â€”OCO2R11 wherein R10 is H, or CH3; n is 0-3 and R11 is C1-C20 alkyl or substituted C1-C6 alkyl, or aralkyl or R11 is or X is acetoxymethyl, acetoxyethyl, carbethoxymethyl, pivaloyloxymethyl, or pivaloyloxyethyl group; or X is heterocyclic amino or heterocyclic aminoalkyl of the formula wherein A is CH or N, and when A is CH, Z is NH or NCH3, and when A is N, Z is CH2, O, NH, S, or NCH3; p is 0-2; and q is 0-2;R1 is hydrogen, C1-4 alkyl, aralkyl, aminoalkyl, trifluoroalkyl, or halogen, R2 is hydrogen, C1-4 alkyl, aralkyl, aminoalkyl, trifluoroalkyl, or halogen with the proviso that when R1 is hydrogen R2 is not hydrogen; R3 is hydrogen, C1-C20 alkyl, glycosyl, aralkyl, C1-C6 alkanoyl; or aminoalkanoyl derived from alanine, arginine, asparagine, aspartic acid, cysteine, glutamine, glutamic acid, glycine, histidine, isoleucine, leucine, lysine, methionine, phenylalanine, proline, serine, threonine, tryptophan, tyrosine and valine, or the optically active isomers thereof, or the racemic mixtures thereof, or 1-aminocyclohexylcarbonyl or COOR11 wherein R11 is as defined above, or â€”(CH2)nâ€”CHR10â€”OCOR11 or â€”(CH2)nâ€”CHR10â€”OCOOR11 where n, R10 and R11 are as defined above, or C6H11O6, PO2(CH3)H, PO3H2, PO2(OCH3)H or SO3H, provided that R1, R2 and R3 are not equal to H at the same time; R4 is H, C1-4 alkyl, CF3, phenyl, F, substituted at one or more of the positions of 2-, 4-, 5-, or 6- of the piperidine ring, or an optical isomer, diastereomer or enantiomer thereof, or polymorph or pseudopolymorph or prodrug thereof or pharmaceutically acceptable salt or hydrate thereof.