2,2-Difluoro-16-phenoxy-13,14-dihydro-PGF.sub.1, analogs
AssigneeThe Upjohn Company
InventorUdo F. Axen
Life of this patent
Estimating the term…
Abstract
2,2-Difluoro prostaglandin E, F.sub..alpha., F.sub..beta., A, and B analogs are disclosed with intermediates and with processes for making them. These compounds differ from the prostaglandins in that they have two fluoro atoms at the C-2 position in place of the two hydrogen atoms at C-2 in the prostaglandins. These compounds are useful for a variety of pharmacological purposes, including antiulcer, inhibition of platelet aggregation, increase in nasal patency, labor induction at term, and wound healing.
Claims58
A compound of the formula ##STR1## OR A MIXTURE COMPRISING THAT COMPOUND AND THE ENANTIOMER THEREOF, WHEREIN G IS 2 TO 4, INCLUSIVE;
- Wherein M.sub.1 is ##STR2## or ##STR3## wherein R.sub.7 and R.sub.8 are hydrogen or methyl, with the proviso that one of R.sub.7 or R.sub.8 is methyl only when the other is hydrogen;
- Wherein T is alkyl of one to 3 carbon atoms, inclusive, fluoro, chloro, trifluoromethyl, or --OR.sub.4 wherein R.sub.4 is alkyl of one to 3 carbon atoms, inclusive, and wherein s is zero, one, 2, or 3, with the proviso that not more than two T's are other than alkyl;
- 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 1, 2, or 3 chloro, alkyl of 1 to 4 carbon atoms, inclusive, or a pharmacologically acceptable cation, ##STR4## WHEREIN R.sub.5 is hydrogen or methyl, with the proviso that R.sub.5 is methyl only when R.sub.7 and R.sub.8 are both hydrogen.
Dependencies are inferred from the claim text.