Compounds and methods for delivery of prostacyclin analogs
AssigneeUnited Therapeutics Corporation
InventorsKen Phares, David Mottola
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Abstract
This invention pertains generally to prostacyclin analogs and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis. Generally, the compounds and methods of the present invention increase the oral bioavailability and circulating concentrations of treprostinil when administered orally. Compounds of the present invention have the following formula:
Claims26
A method of treating pulmonary hypertension comprising orally administering a pharmaceutically effective amount of a compound of structure II to a subject in need thereof:
- wherein,
- R1 is independently selected from the group consisting of H, substituted and unsubstituted alkyl groups, arylalkyl groups and groups wherein OR1 form a substituted or unsubstituted glycolamide ester;
- R2 and R3 may be the same or different and are independently selected from the group consisting of H, phosphate and groups wherein OR2 and OR3 form esters of amino acids or proteins, with the proviso that all of R1, R2 and R3 are not H;
- enantiomers thereof;
- and
- a pharmaceutically acceptable salt of the compound.
A method of treating pulmonary hypertension comprising orally administering to a subject in need thereof an effective amount of a compound of the following structure:
A method of treating peripheral vascular disease, promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation, providing cytoprotection, preventing atherogenesis, or inducing angiogenesis comprising orally administering a pharmaceutically effective amount of a compound of structure II to a subject in need thereof:
- wherein,
- R1 is independently selected from the group consisting of H, substituted and unsubstituted alkyl groups, arylalkyl groups and groups wherein OR1 form a substituted or unsubstituted glycolamide ester;
- R2 and R3 may be the same or different and are independently selected from the group consisting of H, phosphate and groups wherein OR2 and OR3 form esters of amino acids or proteins, with the proviso that all of R1, R2 and R3 are not H;
- enantiomers thereof;
- and
- a pharmaceutically acceptable salt of the compound.
Dependencies are inferred from the claim text.