Mars, Incorporated

Thetis Pharmaceuticals LLC

Gunnar Erik Jagdmann, Jr

Michael C Van Zandt

Frank C Sciavolino

Gary Mathias

Jessica J Dworak

The present invention relates to compounds of Formulas I-IV, which are salts of special lipid mediators of inflammation, compositions containing same, and methods of using same in the treatment of various diseases and disorders characterized by chronic or excessive inflammation, or both.

Compositions and methods relating to salts of specialized pro-resolving mediators

Compounds according to Formula I are potent inhibitors of Arginase I and II activity: where R, R, R, R, D, W, X, Y, and Z are defined in the specification. The invention also provides pharmaceutical compositions of the compounds and methods of their use in treating or preventing a disease or a condition associated with arginase activity.

Arginase inhibitors as therapeutics

The present invention relates to compounds of Formulas I-IV, which are salts of special lipid mediators of inflammation, compositions containing same, and methods of using same in the treatment of various diseases and disorders characterized by chronic or excessive inflammation, or both. Provided are pharmaceutical compositions adapted to deliver the compounds the lower gastrointestinal tract and methods of using same as monotherapy in the treatment of inflammatory diseases or disorders of the lower gastrointestinal tract, and in combination therapy with 5-aminosalicylate.

The present invention relates to compounds of Formulas I-IV and compositions comprising same, including pharmaceutical compositions. The compounds of Formulas I-IV represent new salt forms of specialized pro-resolving mediators ('SPMs') which include lipoxins, resolvins, protectins, and their aspirin-triggered counterparts. The SPM salts described here contain at least one or two SPM molecules ionically bound to at least one basic function that is provided by a scaffold as described in Formulas I-IV. Also provided are methods for pharmaceutical and non-pharmaceutical uses of such compounds and compositions describing same.

The present invention relates to compounds of Formula IV, compositions comprising same, and their use in therapy wherein A and B are each independently a specialized pro-resolving mediator ('SPM') molecule selected from an E series resolvin, a D series resolvin, and their aspirin-triggered counterparts, and M, R, R, Xand Xare as defined herein.

The present invention relates to compounds which are salts of specialized pro-resolving mediators (referred to herein as 'SPMs') which include lipoxins, resolvins, protectins, and their aspirin-triggered counterparts. The SPM salts described here contain at least one or two SPM molecules ionically bound to at least one basic function that is provided by a scaffold moiety as described herein, compositions containing same, and methods of using same in the treatment of various diseases and disorders characterized by chronic or excessive inflammation, or both.

The inventive boronic acid analogs are potent inhibitors of Arginase I and II activity. These compounds are candidate therapeutics for treating a disease or disorder associated with an imbalance in the activity or concentration of cellular arginase I and arginase II enzymes. The invention also provides pharmaceutical compositions of the inventive compounds and methods for using the compositions for therapy.

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Branford, CT, United States of America

Gunnar Erik Jagdmann, Jr