Age-related diseases have been explained as due in part to the excessive generation and accumulation of waste products like the various insoluble protein aggregates observed in nondividing neurons of Alzheimer’s disease, Parkinson’s disease, amyotrophic lateral sclerosis and Huntington’s disease.
Aliad Biopharma Co. Ltd. has presented compounds acting as autophagy inducer, mTOR complex 1 (mTORC1) and mTORC2 inhibitors reported to be useful for the treatment of autism spectrum disorders, Alzheimer’s disease, epilepsy, fragile-X syndrome, macrocephaly and tuberous sclerosis.
Marvel Biotechnology Inc. has synthesized purine compounds acting as adenosine A2A receptor (ADORA2A) antagonists reported to be useful for the treatment of cancer, depression, multiple sclerosis, nonalcoholic steatohepatitis (NASH), scleroderma, attention deficit hyperactivity disorder (ADHD), and Parkinson's and Alzheimer's diseases.
China's National Medical Products Administration (NMPA) has cleared CSPC Pharmaceutical Group Limited to conduct clinical trials of TG-103 injection for the treatment of Alzheimer's disease and for the treatment of nonalcoholic steatohepatitis (NASH).
Autobahn Therapeutics Inc. has closed a US$32.7 million financing to support the company's continued work in the treatment of central nervous system (CNS) disorders and the advancement of ABX-002 through phase I and into phase II proof-of-concept studies for treatment-resistant depression (TRD).
Microsomal prostaglandin E2 synthase-1 (mPGES1) is a molecule belonging to the MAPEG superfamily and is involved in the conversion of PGH2 to excess PGE2 associated with pain and inflammation. Gesynta Pharma AB presented first data on the mPGES1 inhibitor GS-248 for the treatment of pain and inflammation. In their experiments, GS-248 demonstrated a human whole-blood assay (hWBA) IC50 of 0.4 nM, and hWBA activity about 1000-fold more potent than that of celecoxib. No cross reactivity was observed with COX1 or COX2. Moreover, the compound showed IC50 values for human, dog, rat/mouse and minipig mPGES1 of 2.5, 1.3, > 1000 and 23 nM, respectively.
Communication between adipose tissue and the brain increases the risk of cognitive impairment in patients with insulin resistance through extracellular vesicles (EVs) containing microRNAs (miRNAs). Neurons could be damaged when these nucleotides reach the hippocampus guided by membrane proteins in prediabetic overweight people.
Efforts at Abbvie Inc. to selectively target voltage-gated sodium channel subunit alpha Nav1.7 to treat pain led to the discovery of quinoline and quinolone agents and, through structure-activity relationship studies, the candidate product ABBV-318. While Nav1.7 potency could be achieved with earlier compounds, efforts were required to improve characteristics including hERG activity, pharmacokinetics and selectivity over Nav1.5, yielding compounds which blocked Nav1.7 as well as another target for treating pain, Nav1.8.
RSS
