Deuterium enriched analogues of tadalafil as PDE5 inhibitors

Details Deuterium enriched analogues of tadalafil as PDE5 inhibitors Deuterium enriched analogues of tadalafil as PDE5 inhibitors

2011-01-04

2011-01-04

Wilson, James O (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C544S343000

Reexamination Certificate

active

07863274

ABSTRACT:
The present invention relates to derivatives of tadalafil represented by the formula:or a salt thereof, wherein:X1and X2are simultaneously fluoro; or X1is deuterium and X2is selected from hydrogen or deuterium;each Y is independently selected from deuterium or hydrogen;the hydrogen attached to the indole nitrogen is optionally replaced by deuterium; andeach carbon is independently optionally replaced by13C. These compounds are selective PDE5 inhibitors and possess advantageous biopharmaceutical and pharmacokinetic properties. The invention further provides compositions comprising these compounds and methods of treating diseases and conditions that are responsive to PDE5 inhibition, alone and in combination with additional agents.

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