Stabilized thyroxine compounds
First Claim
1. A composition comprising a triiodothyronine protected at a phenolic hydroxyl with a protecting group said protecting group selected from the group consisting of dialkylphosphinate, diarylphosphinate, alkylarylphosphinate, dialkylphosphate, diarylphosphate, aklylarylphosphate, acetyl, trialkylsilyl, and benzyloxy carbonyl.
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Accused Products
Abstract
Throxinyldimethylphosphinate was invented as a prodrug to stabilize thyroxine, a drug widely used to treat hypothyroidism and depression. The presence of the dimethylphosphinate group at the phenolic hydroxyl of thyroxine is key to preventing thyroxine from decomposing through the proposed pathway. The prodrug will be hydrolyzed in the stomach or the gut into thyroxine and the biologically inert dimethylphosphinic acid. Related products may be stabilized with the same or similar protecting groups.
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Citations
40 Claims
- 1. A composition comprising a triiodothyronine protected at a phenolic hydroxyl with a protecting group said protecting group selected from the group consisting of dialkylphosphinate, diarylphosphinate, alkylarylphosphinate, dialkylphosphate, diarylphosphate, aklylarylphosphate, acetyl, trialkylsilyl, and benzyloxy carbonyl.
- 17. A composition comprising a reverse triiodothyronine protected at a phenolic hydroxyl with a protecting group, said protecting group selected from the group consisting of dialkylphosphinate, diarylphosphinate, alkylarylphosphinate, dialkylphosphate, diarylphosphate, acetyl, and benzyloxy carbonyl.
- 22. A composition comprising a 3,5 diiodothyronine protected at a phenolic hydroxyl with a protecting group, said protecting group selected from dialkylphosphinate, diarylphosphinate, alkylarylphosphinate, dialkylphosphate, diarylphosphate, acetyl, and benzyloxy carbonyl
- 28. A composition comprising a 3-monoiodothyronine protected at a phenolic hydroxyl with a protecting group selected dialkylphosphinate, diarylphosphinate, alkylarylphosphinate, dialkylphosphate, diarylphosphate, acetyl, and benzyloxy carbonyl.
- 33. A composition comprising a thyroxine protected at the phenolic hydroxyl with a protecting group selected from diarylphosphinate, alkylarylphosphinate, diarylphosphate, acetyl, and benzyloxy carbonyl.
Specification