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RGT-068A is a potent, selective, and orally bioavailable small molecule inhibitor of mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1). Developed by Regor Therapeutics (also referred to as Ruagen), RGT-068A is designed as a preclinical candidate for the potential treatment of autoimmune diseases and MALT1-dependent cancers, such as diffuse large B-cell lymphoma (DLBCL). The compound features a pyrazoloaminopyrimidine core, and its synthesis involves a highly efficient Heck reaction and N-directed asymmetric hydrogenation to construct its chiral ether unit.
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