Organic compounds -- part of the class 532-570 series – Organic compounds – Carboxylic acid esters
Patent
1990-04-16
1991-10-01
Gerstl, Robert
Organic compounds -- part of the class 532-570 series
Organic compounds
Carboxylic acid esters
562501, C07L17700
Patent
active
050535269
ABSTRACT:
Disclosed is a pharmaceutical having circulation ameliorating effect and antiulcer effect containing a prostaglandin I.sub.2 analogue represented by the formula shown below or a non-toxic salt of its salt or a cyclodextrin inclusion compound thereof as the effective ingredient: ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group having 1 to 12 carbon atoms, a cycloalkyl group having 4 to 7 carbon atoms or a phenyl group; A represents a pentyl group, a cyclopentyl group, a cyclohexyl group, a 1-methyl-3-hexynyl group, a 2-methyl-3-hexynyl group, a 1-methylhexyl group, a 2-phenethyl group, a 1,1-dimethylpentyl group, a 2-methylpentyl group, a 1-cyclohexylethyl group, a 2-methylhexyl group, a 1-methyl-3-pentynyl group or 1 2,6-dimethyl-5-heptenyl group; the double bond between the carbon atoms at 4- and 5-positions is E or Z or a mixture thereof, the asymmetric center in the substituent represented by A is R-configuration or S-configuration or a mixture thereof.
The pharmaceuticals containing, as an active ingredient, prostaglandin I.sub.2 analogues of the present invention have potent platelet aggregation inhibiting effect, blood pressure depressing effect, vasodilative effect and antiulcer effect, and are also low in toxicity.
REFERENCES:
patent: 4699921 (1987-10-01), Shibasaki
patent: 4774341 (1988-09-01), Shibasuki
patent: 4777184 (1988-10-01), Kojima
Hayashi Yoshio
Horii Daijiro
Iseki Katsuhiko
Ishibashi Akira
Ishiyama Chiyoko
Gerstl Robert
Mitsubishi Kasei Corporation
Sagami Chemical Research Center
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