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US 4,097,504 AGranted
11,12-Secoprostaglandins
AssigneeMerck & Co., Inc.
InventorsEdward J. Cragoe, Jr., John B. Bicking, Robert L. Smith
Life of this patent
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Abstract
This invention relates to 11,12-secoprostaglandins and processes for their manufacture. These compounds have prostaglandin-like biological activity and are particularly useful as renal vasodilators, for the treatment of hypertension, for the prevention of thrombus formation, in preventing gastric secretion, and as regulators of the immune response.
Claims9
The compound having the following formula:
- ##STR53## wherein R is carboxy, a carboxy salt having the formula -COO.sup.- Me.sup.+ wherein Me is a pharmaceutically acceptable cation derived from a metal or an amine, or derivatized carboxy having the formula -COOY wherein Y is alkyl having 1-10 carbon atoms, 1-succinimidoethyl, 1-(pivaloyloxy)ethyl, 2-acetamidoethyl, or diloweralkylamino-loweralkyl;
- A is ethylene, trimethylene, .alpha.-methylethylene, .beta.-methylethylene, .alpha.,.alpha.-dimethylethylene, or .beta.,.beta.-dimethylethylene;
- R.sup.1 is formyl, acetyl, propionyl, acryloyl, hydroxyacetyl, 3-hydroxypropionyl, hydroxymethyl, 1-hydroxyethyl, 1,2-dihydroxyethyl, 1,3-dihydroxypropyl, or 1-hydroxy-1-methylethyl;
- Z is methylene, ethylene, trimethylene, tetramethylene, vinylene, or ethynylene;
- R.sup.2 is independently hydrogen or methyl;
- R.sup.3 is hydrogen or loweralkanoyl;
- R.sup.4 is selected independently from the group consisting of hydrogen and methyl;
- and
- R.sup.5 is lower alkyl of 1-4 carbon atoms joined with the R.sup.2 methyl (with abstraction of hydrogen) to form a carbocyclic ring with from 6 to 9 members;
- or
- R.sup.5 is lower alkyl of 1-4 carbon atoms joined to the carbon atom bearing R.sup.2 and OR.sup.3 to form a carbocyclic ring with from 5 to 8 members.
8 more elements
Dependencies are inferred from the claim text.