title: Benzisoxazole analogs as glycogen synthase activators, a patent evaluation (WO2011057956).
abstract: A small series of benzisoxazole analogs that effectively activate glycogen synthase (GS) was prepared in WO2011057956. These novel GS activators are claimed to be beneficial for the treatment or prophylaxis of metabolic disease and disorders. The 1,2-benzisoxazole-3-ol moiety is utilized in the present patent as a bioisoster of benzoic acid, which has often been employed in prior examples of the GS activators.
authors.affiliation: Daiichi Sankyo Co., Ltd., Lead Discovery & Optimization Research Laboratories I, 1-2-58, Hiromachi Shinagawa-ku, Tokyo 140-8710, Japan. uto.yoshikazu.pw@daiichisankyo.co.jp
authors.forename: Yoshikazu
authors.initials: Y
authors.lastname: Uto
mesh_terms: D000818:Animals; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy / Q000201:enzymology; D015195:Drug Design; D004789:Enzyme Activation; D020536:Enzyme Activators / Q000737:chemistry / Q000494:pharmacology*; D006006:Glycogen Synthase / Q000378:metabolism*; D006801:Humans; D007004:Hypoglycemic Agents / Q000737:chemistry / Q000494:pharmacology*; D007555:Isoxazoles / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D010330:Patents as Topic; D013329:Structure-Activity Relationship
chemical_list: C441200:1,2-benzisoxazole; D020536:Enzyme Activators; D007004:Hypoglycemic Agents; D007555:Isoxazoles; D006006:Glycogen Synthase