Monomethyl fumarate-carrier conjugates and methods of their use

• Main Authors: BRIGGS, Timothy, GUNASEKERA, Dinara Shashanka, NUDEL, Kathleen, PECK, Spencer Cory, YASUDA, Koji, ALEXANDER, Jessica Elizabeth, CASEY Jr., John, LIANG, Anna, KIM, Mi-Jeong, BUCKBINDER, Leonard, KAMALI SARVESTANI, Afrand, LANTER, Bernard, TAYLOR, Steven John, BERRY, David Arthur, ROSS, Cheri
• Format: Patent
• Language: English
• Published: 10.06.2021
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Disclosed are conjugates of monomethyl fumarate and a carrier group or aminocarrier group, or a pharmaceutically acceptable salt thereof. In the conjugates, monomethyl fumarate acyl is covalently bonded to the carrier group or aminocarrier group through a carbon-oxygen bond that is cleavable in vivo. The carrier group may include a core, e.g., a monosaccharide, a sugar acid (e.g., acid monosaccharide), a sugar alcohol, or a catechin polyphenol. The aminocarrier group may include a core, e.g., an aminomonosaccharide. The carrier group or aminocarrier group may include, e.g., at least one short chain fatty acid acyl, at least one tryptophan analogue, at least one ketone body, or at least one preketone body. Also disclosed are pharmaceutical compositions containing the conjugates and methods of their use.