Insmed Incorporated

Franziska Leifer

Vladimir Malinin

Adam Plaunt

Walter Perkins

Donna M Konicek

Zhili Li

Jimin Zhang

Kuan-Ju Chen

Keith Dipetrillo

Prostacyclin compounds and compositions comprising the same are provided herein. Specifically, prostacyclin compounds comprising treprostinil covalently linked to a linear C-Calkyl, branched C-Calkyl, linear C-Calkenyl, branched C-Calkenyl, aryl, aryl-C-Calkyl or an amino acid or a peptide (e.g., dipeptide, tripeptide, tetrapeptide) are described. The linkage, in one embodiment, is via a carbamate, amide or ester bond. Prostacyclin compounds provided herein can also include at least one hydrogen atom substituted with at least one deuterium atom. Methods for treating pulmonary hypertension (e.g., pulmonary arterial hypertension) and portopulmonary hypertension are also provided.

Prostacyclin compounds, compositions and methods of use thereof

Methods for making prodrugs of treprostinil and treprostinil derivatives are provided. Specifically, methods are provided herein for producing prostacyclin compounds comprising treprostinil covalently linked to a linear C-Calkyl, branched C-Calkyl, linear C-Calkenyl, branched C-Calkenyl, aryl, aryl-C-Calkyl or an amino acid or a peptide (e.g., dipeptide, tripeptide, tetrapeptide). The linkage, in one embodiment, is via an amide or ester bond. Prostacyclin compounds provided herein can also include at least one hydrogen atom substituted with at least one deuterium atom. The compounds provided herein can be used to treat pulmonary hypertension (e.g., pulmonary arterial hypertension) and portopulmonary hypertension.

Methods of manufacturing treprostinil and treprostinil derivative prodrugs

Methods for making prodrugs of trepreostinil and treprostinil derivatives are provided. Specifically, methods are provided herein for producing prostacyclin compounds comprising treprostinil covalently linked to a linear C-Calkyl, branched C-Calkyl, linear C-Calkenyl, branched C-Calkenyl, aryl, aryl-C-Calkyl or an amino acid or a peptide (e.g., dipeptide, tripeptide, tetrapeptide). The linkage, in one embodiment, is via an amide or ester bond. Prostacyclin compounds provided herein can also include at least one hydrogen atom substituted with at least one deuterium atom. The compounds provided herein can be used to treat pulmonary hypertension (e.g., pulmonary arterial hypertension) and portopulmonary hypertension.

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Princeton, NJ, United States of America

Franziska Leifer