Concert Pharmaceuticals, Inc.

Altus Biologics Inc.

Rose A Persichetti

Julie Fields Liu

Scott L Harbeson

Craig E Masse

Alexey L Margolin

Nancy L St Clair

Nazer K Khalaf

This invention relates to novel compounds which are derivatives of the phosphodiesterase inhibitor, cilostazol and pharmaceutically acceptable salts thereof. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administration of a phosphodiesterase inhibitor, such as cilostazol. The invention also relates to the use of the disclosed compounds and compositions as reagents in analytical studies involving cilostazol.

Analogues of cilostazol

This invention relates to novel compounds that are piperazine derivatives, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel piperazine compounds that are derivatives of the chemokine CCR5 receptor antagonist, vicriviroc. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administering chemokine CCR5 receptor antagonists, such as vicriviroc. The invention also relates to the use of one or more of the disclosed compounds as reagents in analytical studies involving vicriviroc.

Piperazine derivatives

This invention relates to novel compounds which are derivatives of the phosphodiesterase inhibitor, cilostazol and pharmaceutically acceptable salts thereof. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administration of an phosphodiesterase inhibitor, such as cilostazol. The invention also relates to the use of the disclosed compounds and compositions as reagents in analytical studies involving cilostazol.

This disclosure relates to novel substituted morpholinyl compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a 5HT4 serotonin receptor agonist.

Substituted morpholinyl compounds

Protein crystals crosslinked with a multifunctional crosslinking agent are produced that have the ability to change from an insoluble and stable form to a soluble and active form and to release protein activity at a controlled rate when a change in environment surrounding the crystals occurs. The change in environment may be a change in temperature, pH, chemical composition or shear force acting on the crystals, or a change from a concentrate to a dilute form, or a combination of the changes. The crosslinked protein crystals have a half-life activity under storage conditions greater than at least 2 times that of the soluble protein that is crystallized to form the crystals that are crosslinked, and under conditions of use have an activity similar to the soluble protein. Crosslinking is carried out by reacting a slurry of protein crystals with a multifunctional crosslinking agent such as glutaraldehyde, glyoxal, octanedialdehyde or succinaldehyde using a concentration of crosslinking agent and time for crosslinking that provides crosslinked protein crystals having the desired ability to change due to a change in environment. An epoxide multifunctional crosslinking agent may be used in combination with glutaraldehyde for crosslinking. The crosslinked protein crystals can be used for protein delivery, and may be used in cleaning agents such as detergents, pharmaceutical compositions, vaccines, personal care compositions, veterinary compositions, foods, feeds, diagnostics and decontamination formulations. Proteins used include enzymes and therapeutic or prophylactic proteins such as hormones and antibodies.

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Stow, MA, United States of America

Rose A Persichetti