Novel Ru(II) Complexes as Type-I/-II Photosensitizers for Multimodal Hypoxia-Tolerant Chemo-Photodynamic/Immune Therapy.

SCOHIA PHARMA, Inc. September 10, 2020 Publication regarding medicinal chemistry research on a GPR40 full agonist (SCO-267) The research group of SCOHIA PHARMA, Inc. has published research results on the medicinal chemistry leading up to the discovery of SCO-267, a GPR40 full agonist. The results have been published online in the Journal of Medicinal Chemistry and in the EFMC-ISMC & EFMC-YMCS Virtual Poster Session on September 9, 2020. Article title: Design and Identification of a GPR40 Full Agonist (SCO-267) Possessing a 2-Carbamoylphenyl Piperidine Moiety https://pubs.acs.org/doi/10.1021/acs.jmedchem.0c00843 Poster presentation title: Design and Identification of a GPR40 Full Agonist (SCO-267) Possessing a 2-Carbamoylphenyl Piperidine Moiety for the Treatment of Type 2 Diabetes Mellitus View Poster SCO-267 is a first-in-class full agonist of GPR40, a G protein-coupled receptor expressed in the pancreatic islets and gastrointestinal tract. SCO-267-mediated full agonism of GPR40 promotes secretions of islet and gastrointestinal hormones, including GLP-1, and is therefore expected to exert a powerful therapeutic effect in diabetes. Additionally, our research group recently reported that SCO-267 has potential as a treatment for obesity and non-alcoholic fatty liver disease (NAFLD). In this publication, the medicinal chemistry research that led to the discovery of SCO-267 is reported. By optimization of the structure of a lead compound for strong receptor activation and improvement of its physicochemical properties—conversion of the highly planar mother skeleton to a saturated ring and introduction of a polar group into the appropriate position—we have discovered SCO-267, which has strong full agonistic activity against human GPR40 and a good profile as a drug candidate. The presentation also included potent anti-diabetic, anti-obesity, and anti-NAFLD effects of SCO-267 in the respective animal disease models. Contact for inquiries: info@scohia.com