Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Recombinant or stably-transformed bacterium encoding one or...
Patent
1980-01-21
1984-10-30
Gerstl, Robert
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Recombinant or stably-transformed bacterium encoding one or...
536 46, 549 66, 549415, 549422, 549473, 549475, 556441, 560 56, 560100, 560102, 560107, 560116, 560119, 560227, 560228, 560256, 562498, 562501, 562466, 424317, C07C17700, C07C 5946, A01K 31557
Patent
active
044799667
ABSTRACT:
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.
Arai Yoshinobu
Hayashi Masaki
Konishi Yoshitaka
Gerstl Robert
Ono Pharmaceutical Company, Ltd.
Witherspoon John F.
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