Heterocyclic macrolide pharmaceutical agent, a method of producing the same and use of the same
View Patent ↗A compound represented by the following general formula (I): (I) wherein R 7 and R 21 are the same or different and each represents optionally substituted C 2-22 alkoxy, etc.; a pharmaceutically acceptable salt thereof or hydrates of the same. The compound (1) inhibits angiogenesis and inhibits the production of VEGF particularly under hypoxic conditions, which makes it useful as a remedy for solid cancer.
1. A compound represented by the formula (I):
wherein R 7 and R 21 are the same or are different and represent
—O-benzoyl, or
RC(═Y)—O—, wherein Y represents an oxygen atom, and R represents
4-alkyl-piperazin-1-yl, alkyl, —O-phenyl, —N,N-dialkyl or —NH-phenyl, or
a pharmacologically acceptable salt thereof.
2. A compound represented by the formula (I-a):
wherein R 7a and R 21a are the same or are different and represent
R a C(═Y a )—O—, wherein Y a represents an oxygen atom, and R a represents
a C 1 to C 22 alkyl group,
an unsaturated C 2 to C 22 alkyl group,
a C 3 to C 14 cycloalkyl group
or a pharmacologically acceptable salt thereof.
3. The compound according to claim 1 , which is (8E,12E,14E)-21-benzoyloxy-3,6-dihydroxy-6,10,12,16,20-pentamethyl-7-((4-methylpiperazin-1-yl)carbonyl)oxy-18,19-epoxytricosa-8,12,14-trien-11-olide, (8E,12E,14E)-21-(N,N-dimethylcarbamoyloxy)-3,6-dihydroxy-6,10,12,16,20-pentamethyl-7((4-methylpiperazin-1-yl)carbonyl)oxy-18,19-epoxytricosa-8,12,14-trien-11-olide, and (8E,12E,14E)-3,6-dihydroxy-6,10,12,16,20-pentamethyl-7-((4-methylpiperazin-1-yl)carbonyl)oxy-21-phenylcarbamoyloxy-18,19-epoxytricosa-8,12,14-trien-11-olide; or a pharmacologically acceptable salt thereof.
4. A pharmaceutical composition comprising the compound according to claim 1 , or a pharmacologically acceptable salt thereof as an active ingredient and a pharmaceutically acceptable carrier.