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US 4,057,572 AGranted
4,4,5,5-Tetradehydro-.omega.-aryl-11-deoxy-PGE.sub.1 , analogs
AssigneeThe Upjohn Company
InventorChiu-Hong Lin
Life of this patent
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Abstract
This invention comprises certain analogs of the prostaglandins in which there is a triple bond between C-5 and C-6 or C-4 and C-5. Also provided in this invention, are novel chemical processes useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.
Claims32
A prostaglandin analog of the formula ##STR1## WHEREIN G IS ONE, 2, OR 3;
- WHEREIN Y is trans-CH.dbd.CH--;
- wherein M.sub.1 is ##STR2## wherein R.sub.5 is hydrogen or methyl;
- WHEREIN Z.sub.3 is oxa or methylene, with the proviso that Z.sub.3 is oxa only when R.sub.3 and R.sub.4 are hydrogen or methyl;
- Wherein T is chloro, fluoro, trifluoromethyl, alkyl of one to 3 carbon atoms, inclusive, or alkoxy of one to 3 carbon atoms, inclusive, and s is zero, one, 2, or 3, the various T's being the same or different, with the proviso that not more than two T's are other than alkyl;
- Wherein L.sub.1 is ##STR3## wherein R.sub.3 and R.sub.4 are hydrogen, methyl, or fluoro, being the same or different, with the proviso that one of R.sub.3 and R.sub.4 is fluoro only when the other is hydrogen or fluoro;
- and
- Wherein R.sub.1 is hydrogen, alkyl of one to 12 carbon atoms, inclusive, cycloalkyl of 3 to 10 carbon atoms, inclusive, aralkyl of 7 to 12 carbon atoms, inclusive, phenyl, phenyl substituted with one, two, or three chloro or alkyl of one to 3 carbon atoms, inclusive, or a pharmacologically acceptable cation.
4 more elements
Dependencies are inferred from the claim text.