Patent ID: 6329338
Filing Date: 2001-12-11
Classification: A61P,C07D,Y02P

Abstract:
A cyclodepsipeptide compound derived from PF1022 substance, which is represented by the following general formula(I) ##STR9##wherein (i) R.sup.1 stands for a hydrogen atom and R.sup.2 stand for a cyano-(C.sub.1 -C.sub.6)alkoxy group, a thiocarbamoyl-(C.sub.1 -C.sub.6)alkoxy group, an amino-(C.sub.1 -C.sub.6)alkoxy group, an amino-(C.sub.1 -C.sub.6)alkoxy group having t-butyloxycarbonyl group as an amino-protecting group, an N-mono-(C.sub.1 -C.sub.6)alkylamino-(C.sub.1 -C.sub.6)alkoxy group, an N,N-di-(C.sub.1 -C.sub.6) alkylamino-(C.sub.1 -C.sub.6)alkoxy group, an N,N-di-((C.sub.1 -C.sub.6)alkoxy-(C.sub.1 -C.sub.6)alkyl)amino-(C.sub.1 -C.sub.6)alkoxy group, or a cyclic amino-(C.sub.1 -C.sub.6)alkoxy group of which the cyclic amino group is morpholino group, pyrrolidino group or piperidino group; or R.sup.2 is a (C.sub.1 -C.sub.6)alkoxy group having, as a substituent thereon, a saturated or unsaturated 5- or 6-membered heterocyclic ring which is chosen from pyrrolidine, imidazole, thiazole, furan, tetrahydrofuran, a 5-(C.sub.1 -C.sub.6)alkyl-1,2,4-oxadiazole, a 5-(halo-substituted or unsubstituted)phenyl-1,2,4-oxadiazole, a 5-(C.sub.3 -C.sub.6)cycloalkyl-1,2,4-oxadiazole, a halo-substituted or unsubstituted pyridine, and an N-alkyl-substituted or unsubstituted tetrahydropyrimidine and which heterocyclic ring may further optionally have as a substituent a phenyl group or a phenyl group substituted by a halo group selected from the group consisting of chlorine, bromine and fluorine; or R.sup.2 is a (C.sub.2 -C.sub.6)alkanoyl group optionally having a substituent which is selected from the group consisting of a halogen atom and a hydroxyl group, or R.sup.2 is a carbamoyl group, an N-mono-(C.sub.1 -C.sub.6)alkylcarbamoyl group, or an N,N-di-(C.sub.1 -C.sub.6)alkylcarbamoyl group, or a cyclic amino-carbonyl group of which the cyclic amino group is morpholino group, pyrrolidino group or piperidino group; or R.sup.2 is an N-mono-(C.sub.1 -C.sub.6)alkylamino-alkoxycarbonyl group, or an N,N-di-(C.sub.1 -C.sub.6)alkylamino-(C.sub.1 -C.sub.6)alkoxycarbonyl group, or a cyclic amino-(C.sub.1 -C.sub.6)alkoxycarbonyl group of which the cyclic amino group is morpholino group, pyrrolidino group or piperidino group; or R.sup.2 is a formyloxy-(C.sub.1 -C.sub.6)alkylcarbonyl group; or R.sup.2 is a carboxyl group or 2-aminothiazolyl group; or alternatively (ii) R.sup.1 and R.sup.2 are identical to each other and each stand for a cyano-(C.sub.1 -C.sub.6)alkoxy group, a thiocarbamoyl-(C.sub.1 -C.sub.6)alkoxy group, an amino-(C.sub.1 -C.sub.6)alkoxy group, an amino-(C.sub.1 -C.sub.6)alkoxy group having t-butyloxycarbonyl group as an amino-protecting group, an N-mono-(C.sub.1 -C.sub.6)alkylamino-(C.sub.1 -C.sub.6)alkoxy group, an N,N-di-(C.sub.1 -C.sub.6)alkylamino-(C.sub.1 -C.sub.6)alkoxy group, an N,N-di-((C.sub.1 -C.sub.6)alkoxy-(C.sub.1 -C.sub.6)alkyl)amino-(C.sub.1 -C.sub.6)alkoxy group, or a cyclic amino-(C.sub.1 -C.sub.6)alkoxy group of which the cyclic amino group is morpholino group, pyrrolidino group or piperidino group; or R.sup.1 and R.sup.2 each stand for a (C.sub.1 -C.sub.6)alkoxy group having, as a substituent thereon, a saturated or unsaturated 5- or 6-membered heterocyclic ring which is chosen from pyrrolidine, imidazole, thiazole, furan, tetrahydrofuran, a 5-(C.sub.1 -C.sub.6)alkyl-1,2,4-oxadiazole, a 5-(halo-substituted or unsubstituted) phenyl-1,2,4-oxadiazole, a 5-(C.sub.3 -C.sub.6)cycloalkyl-1,2,4-oxadiazole, a halo-substituted or unsubstituted pyridine, and an N-alkyl-substituted or unsubstituted tetrahydropyrimidine, and which heterocyclic ring may further optionally have as a substituent a phenyl group or a phenyl group substituted by a halo group selected from the group consisting of chlorine, bromine or fluorines or R.sup.1 and R.sup.2 each stand for a (C.sub.2 -C.sub.6)alkanoyl group optionally having a substituent which is selected from the group consisting of a halogen atom and hydroxyl group; or R.sup.1 and R.sup.2 each stand for a carbamoyl group, an N-mono-(C.sub.1 -C.sub.6)alkylcarbamoyl group, or an N,N-di-(C.sub.1 -C.sub.6)alkylcarbamoyl group, or a cyclic amino-carbonyl group of which the cyclic amino group is morpholino group, pyrrolidino group or piperidino group; or R.sup.1 and R.sup.2 each stand for an N-mono-(C.sub.1 -C.sub.6)alkylamino-(C.sub.1 -C.sub.6)alkoxycarbonyl group, or an N,N-di-(C.sub.1 -C.sub.6)alkylamino-(C.sub.1 -C.sub.6)alkoxycarbonyl group, or a cyclic amino-(C.sub.1 -C.sub.6)alkoxycarbonyl group of which the cyclic amino group is morpholino group, pyrrolidino group or piperidino group; or R.sup.1 and R.sup.2 each stand for a formyloxy-(C.sub.1 -C.sub.6)alkylcarbonyl group, or a carboxyl group or 2-aminothiazolyl group, and Me stands for methyl group.