The Upjohn Co.

Udo F Axen

John C Sih

The present invention relates to novel 2-decarboxy-2-tetrazolyl-6-keto-PG compounds, which are useful for inducing a variety of prostacyclin-like pharmacological effects. Accordingly, these compounds are useful pharmacological agents for the same purposes for which prostacyclin is employed.

2-Decarboxy-2-tetrazolyl-6-keto-PG compounds

Prostaglandin E (PGE)-type derivatives and analogs having a 6-keto feature are disclosed, including processes for preparing them and the appropriate intermediates, said derivatives having pharmacological activity.

2-Decarboxy-2-tetrazolyl-6-keto-PGE.sub.1 compounds

The present invention provides 2,5-inter-o-phenylene-3,4-dinor-5,9.alpha.-epoxy-PGF.sub.1 amides. These compounds are useful for a wide variety of pharmacological and therapeutical purposes, e.g., as antithrombotic agents.

2,5-Inter-o-phenylene-3,4-dinor-5,9.alpha.-epoxy PGF.sub.1 amides

The present invention provides 2,5-inter-o-phenylene-3,4-dinor-6,9.alpha.-epoxy-6.beta.-6-iodo-PGF.sub.1 compounds. These compounds are intermediates for preparing 2,5-inter-o-phenylene-3,4-dinor-prostacyclin analogs, which are useful for pharmacological purposes, e.g., as antithrombotic agents.

2,5-Inter-o-phenylene-3,4-dinor-5,9.alpha.-epoxy-6-iodo-PGF.sub.1

The present invention provides 2,5-inter-o-phenylene-3,4-dinor-5,9.alpha.-epoxy-6-iodo-PGF.sub.1 amides. These compounds are intermediates for preparing 2,5-inter-o-phenylene-3,4-dinor-prostacyclin analogs, which are useful for pharmacological purposes, e.g., as antithrombotic agents.

2,5-Inter-o-phenylene-3,4-dinor-5,9.alpha.-epoxy-6-iodo-PGF.sub.1 amides

The present invention provides 2,5-inter-o-phenylene-3,4-dinor-6,9.alpha.-epoxy-6.beta.-PGF.sub.1 amides. These compounds are useful for a wide variety of pharmacological and therapeutical purposes, e.g., as antithrombotic agents.

2,5-Inter-o-phenylene-3,4-dinor-6,9.alpha.-epoxy-6.beta.-PGF.sub.1 amides

The present invention provides 2,5-inter-o-phenylene-3,4-dinor-6,9.alpha.-epoxy-6.beta.-5-iodo-PGF.sub.1 amides. These compounds are intermediates for preparing 2,5-inter-o-phenylene-3,4-dinor-prostacyclin analogs, which are useful for pharmacological purposes, e.g., as antithrombotic agents.

2,5-Inter-o-phenylene-3,4

The present invention provides 2,5-inter-o-phenylene-3,4-dinor-6,9.alpha.-epoxy-6.beta.-PGF.sub.1 compounds. These compounds are useful for a wide variety of pharmacological and therapeutical purposes, e.g., as antithrombotic agents.

2,5-Inter-o-phenylene-3,4-dinor-6,9.alpha.-epoxy-6.beta.-PGF.sub.1

This invention relates to certain structural and pharmacological analogs of prostacyclin (PGI.sub.2) and 5,6-dehydroprostacyclin (PGI.sub.1) and 5,9.alpha.-epoxy-9-deoxy-PGF.sub.1, wherein between the position beta to the carboxy (C-2) and C-5 there is substituted an inter-o-phenylene for the ethylene chain. These novel 2,5-inter-o-phenylene-3,4-dinor-prostaglandin or prostacyclin-type compounds are useful for certain of the same pharmacological purposes as prostacyclin, particularly being smooth muscle stimulators, blood pressure depressors and platelet aggregation inhibitors. Also provided are novel intermediates therefor, namely corresponding interphenylene-containing PGF.sub.2.alpha. and 5-halo-PGI.sub.1 and 6-halo-5,9.alpha.-epoxy-9-deoxy-PGF.sub.1 compounds.

2,5-Inter-o-phenylene-3,4-dinor-5,9.alpha.-epoxy-9-deoxy-PGF.sub.1

The present invention provides 2,5-inter-o-phenylene-3,4-dinor-PGF.sub.2 amides. These compounds are intermediates for preparing 2,5-inter-o-phenylene-3,4-dinor-prostacyclin analogs, which are useful for pharmacological purposes, e.g., as antithrombotic agents.

2,5-Inter-o-phenylene-3,4-dinor-PGF.sub.2 amides

The present invention provides 2,5-inter-o-phenylene-3,4-dinor-PGF.sub.2 compounds. These compounds are intermediates for preparing 2,5-inter-o-phenylene-3,4-dinor-prostacyclin analogs, which are useful for pharmacological purposes, e.g., as antithrombotic agents.

2,5-Inter-O-phenylene-3,4-dinor-PGF.sub.2 compounds

The present invention provides 2,5-inter-o-phenylene-3,4-dinor-6,9.alpha.-epoxy-6.beta.-5-iodo-PGF.sub.1 compounds. These compounds are intermediates for preparing 2,5-inter-o-phenylene-3,4-dinor-prostacyclin analogs, which are useful for pharmacological purposes, e.g., as antithrombotic agents.

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Plainwell, MI, United States of America

Udo F Axen