Researchers from Binzhou Medical University and affiliated organizations have detailed the synthesis and optimization of a new series of 1,4,5,6-tetrahydrobenzo [2,3]oxepino[4,5-d]pyrimidin-2-amine derivatives, which resulted in the identification of compound [I] as the lead candidate with potent anti-neuroinflammatory activity in vitro.

The preBötzinger complex (preBötC) appears to play a relevant role in opiate-induced respiratory depression, as suggested by studies in animal models. However, limited research concerning preBötC physiology in humans has been conducted, and no human in vitro models of the preBötC exist.

The FDA has cleared an IND application for ADEL-Y01, being jointly developed by Oscotec Inc. and Adel Inc., for the treatment of Alzheimer’s disease. A phase Ia/b study will include healthy volunteers, and participants with mild cognitive impairment due to Alzheimer’s disease or mild Alzheimer’s disease.

Ephrin type-A receptor 2 (EphA2) is a type I transmembrane glycoprotein highly expressed in a wide range of tumors such as bladder, pancreatic, esophageal, colorectal, or non-small-cell lung cancer, among others. Furthermore, in most normal tissues, EphA2 is found at low levels and plays a relevant role in carcinogenesis control and tumor progression modulation.

Phoenix Pharmalabs Inc. has reported findings from in vivo studies that demonstrated that the company’s lead compound, PPL-138, reduced symptoms of post-traumatic stress disorder (PTSD) and decreased alcohol consumption in a rat model of PTSD/alcohol use disorder (AUD). The studies were conducted at the University of Oklahoma Health Sciences Center and Florida Atlantic University under a grant from the U.S. Department of Defense.

Novel effective antivirals against SARS-CoV-2 are needed because of the emergence of novel variants and the potential risk of SARS-CoV-2/MERS-CoV recombination. The SARS-CoV-2 main protease (Mpro) is a promising antiviral target. Mpro presents a His41-Cys145 catalytic dyad in the central part of its active site, which confers a natural advantage for developing covalent drugs.