University of Florida researchers have synthesized proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase-binding moiety coupled to Bcl-2-like protein 1 (Bcl-xl; Bcl-X; BCL2L1)- and apoptosis regulator Bcl-2-targeting moiety.
Terns Pharmaceuticals Inc. has reported triazole compounds acting as gastric inhibitory polypeptide receptor (GIPR) antagonists. They are intended for use in the treatment of diabetes, obesity, liver diseases and cardiometabolic syndrome.
Humanwell Pharmaceutical US Inc. has disclosed prodrugs of somatostatin SST4 receptor agonists described as potentially useful for the treatment of visceral and neuropathic pain.
Beijing Avistone Pharmaceuticals Biotechnology Co. Ltd. has patented HER2 (erbB2) Ex20Ins mutant inhibitors. They are reported to be useful for the treatment of cancer, atherosclerosis and pulmonary fibrosis.
Shanghai Haiyan Pharmaceutical Technology Co. Ltd. and Yangtze River Pharmaceutical Group have divulged new isoindoline proteolysis targeting chimeric (PROTAC) compounds comprising cereblon (CRBN) ligands covalently linked to a eukaryotic peptide chain release factor GTP-binding subunit ERF3A (GSPT1)-targeting moiety. They are reported to be useful for the treatment of cancer.
Jiangsu Hengrui Pharmaceuticals Co. Ltd. and Shanghai Hengrui Pharmaceutical Co. Ltd. have identified oxyheteroaryl compounds acting as sodium channel protein type 10 subunit α (Nav1.8) blockers. They are reported to be useful for the treatment of pain, urinary incontinence, multiple sclerosis, cough, Charcot-Marie-Tooth disease and arrhythmia.
Work at Apertor Pharmaceuticals Inc. has led to the preparation of new hetero-bifunctional compounds acting as mTOR complex 1 (mTORC1) inhibitors potentially useful for the treatment of cancer.
Chia Tai Tianqing Pharmaceutical Group Co. Ltd. has disclosed proteolysis targeting chimeric (PROTAC) compounds comprising a E3 ubiquitin ligase-binding moiety covalently linked to an estrogen receptor-α (ERα)-targeting moiety. They are reported to be useful for the treatment of breast cancer.