6,9-Methano-PGI2 analogues
AssigneeOno Pharmaceutical Co., Ltd.
InventorsMasaki Hayashi, Yoshitaka Konishi, Yoshinobu Arai
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AssigneeOno Pharmaceutical Co., Ltd.
InventorsMasaki Hayashi, Yoshitaka Konishi, Yoshinobu Arai
Estimating the term…
Prostaglandin I.sub.2 analogues of the formula: ##STR1## [wherein the symbol between the carbon atoms in positions 5 and 6 represents a single or double bond, Y represents ethylene or trans-vinylene, R.sup.1 represents hydrogen, alkyl of 1 to 12 carbon atoms, aralkyl of 7 to 12 carbon atoms, cycloalkyl of 4 to 7 carbon atoms optionally substituted by alkyl of 1 to 4 carbon atoms, phenyl optionally substituted by chlorine, trifluoromethyl, alkyl of 1 to 4 carbon atoms or phenyl, a --C.sub.m H.sub.2m COOR.sup.7 group (wherein m represents an integer of from 1 to 12 and R.sup.7 represents alkyl of 1 to 4 carbon atoms), a --C.sub.n H.sub.2n OR.sup.8 group (wherein n represents an integer of from 2 to 12 and R.sup.8 represents hydrogen or alkyl of 1 to 4 carbon atoms) or a ##STR2## group (wherein R.sup.9 and R.sup.10 each represent alkyl of 1 to 4 carbon atoms and n is as hereinbefore defined), R.sup.2 represents hydrogen or a hydroxy-protecting group, R.sup.3 represents hydrogen or a hydroxy-protecting group which is eliminated under acidic conditions, R.sup.4 represents hydrogen, methyl or ethyl, R.sup.5 represents a single bond or alkylene of 1 to 4 carbon atoms optionally substituted by a chlorine atom (provided that, when R.sup.5 is alkylene substituted by chlorine, R.sup.6 represents hydrogen or alkyl) R.sup.6 represents hydrogen, alkyl or 1 to 8 carbon atoms, cycloalkyl of 4 to 7 carbon atoms optionally substituted by alkyl of 1 to 8 carbon atoms, or phenyl or phenoxy optionally substituted by cholrine, trifluoromethyl or alkyl of 1 to 4 carbon atoms, and when represents a double bond that bond is E, Z or a mixture thereof and when, represents a single bond, the absolute configuration of C.sub.6 is R, S or a mixture thereof] and, when R.sup.2 and R.sup.3 represent hydrogen, cyclodextrin clathrates of such acids and esters and, when R.sup.1, R.sup.2 and R.sup.3 represent hydrogen, non-toxic salts thereof and, when R.sup.1 represents ##STR3## in which n, R.sup.9 and R.sup.10 are as hereinbefore defined, non-toxic acid addition salts thereof, are new compounds, possessing prostaglandin-like activity.
A prostaglandin I.sub.2 analogue of the formula:
Dependencies are inferred from the claim text.