.omega.-Halo-PGI.sub.2 analogues

Drug – bio-affecting and body treating compositions – Conjugate or complex of monoclonal or polyclonal antibody,... – Conjugated via claimed linking group – bond – chelating agent,...

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424285, 536 46, 536103, 542426, 542429, 26034622, 26034673, A61K 3170, A61K 3158, C07D307935

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042320097

ABSTRACT:
Prostaglandin I.sub.2 analogues of the formula: ##STR1## [wherein 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 at least one alkyl group containing from 1 to 4 carbon atoms, phenyl unsubstituted or substituted by at least one chlorine atom, trifluoromethyl group, alkyl group containing from 1 to 4 carbon atoms or phenyl group, a --C.sub.m H.sub.2m COOR.sup.4 group (wherein m is an integer from 1 to 12 and R.sup.4 represents alkyl of 1 to 4 carbon atoms), a C.sub.n H.sub.2n OR.sup.5 group (wherein n is an integer from 2 to 12 and R.sup.5 represents hydrogen or alkyl of 1 to 4 carbon atoms), or a ##STR2## (wherein n is as hereinbefore defined and R.sup.6 and R.sup.7 each represent alkyl of 1 to 4 carbon atoms), R.sup.2 represents hydrogen, methyl or ethyl, X represents a --C.sub.p H.sub.2p --group (wherein p is an integer from 2 to 8) or a ##STR3## (wherein R.sup.8 represents a single bond, or alkylene of 1 to 4 carbon atoms, R.sup.9 represents a single bond or alkylene of 1 to 8 carbon atoms, and q is an integer from 3 to 6), R.sup.3 represents chlorine or fluorine, the wavy line attached to the carbon atoms in positions 11 and 15 represents .alpha.- or .beta.-configuration or mixtures thereof, and the double bond between C.sub.5 -C.sub.6 is Z] and cyclodextrin clathrates thereof and, when appropriate non-toxic salts, including acid addition salts, thereof, are new compounds possessing prostaglandin-like activity.

REFERENCES:
Chem. and Engineering News, Dec. 1976, p. 17.

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