Additional early-stage research and drug discovery news in brief, from: Karolinska Development, Tonix Pharmaceuticals, Transcode Therapeutics, Umecrine Cognition, Vycellix.
Novartis AG has identified diaminocyclopentylpyridine derivatives acting as proprotein convertase subtilisin/kexin-type 9 (PCSK9) inhibitors and thus reported to be useful for the treatment of hypercholesterolemia, hyperlipidemia, hypertriglyceridemia, sitosterolemia, vascular inflammation, atherosclerosis, peripheral vascular and coronary heart disease, among others.
Alchemedicine Inc. has prepared and tested new angiotensin AT1 receptor (AGTR1) antagonists reported to be useful for the treatment of cancer, hypertension, glaucoma and renal disorders.
Research at Seoul National University has led to the identification of thiourea compounds acting as nuclear receptor RORα (RORA) agonists reported to be useful for the treatment of inflammation and metabolic diseases.
An Agios Pharmaceuticals Inc. patent describes branched-chain-amino-acid aminotransferase, mitochondrial (BCAT2) inhibitors reported to be useful for the treatment of isovaleric acidemia, maple syrup urine disease, methylmalonic acidemia and propionic acidemia.
Case Western Reserve University has patented conjugates consisting of a PSMA-targeting moiety covalently linked to a chelating agent comprising metals.
Diffuse intrinsic pontine glioma (DIPG) is an almost universally fatal brain pediatric tumor and the only tumor indication where palliative radiotherapy is the current standard of care. Although chimeric antigen receptor (CAR) T-cell therapy may hold promise for treating DIPG, the elevated tumor heterogeneity and the prospect of antigen escape make the identification of additional targets crucial. Therefore, multiple targets need to be validated to facilitate a multipronged approach.
Bronchiectasis is an irreversible chronic respiratory condition arising from secondary infections that presents as chronic cough with daily purulent sputum due to a permanent abnormal widening of bronchi.
Dtx Pharma Inc.’s Dtx-1252, an investigational small interfering RNA (siRNA) therapeutic, has been awarded U.S. orphan drug designation for the treatment of Charcot-Marie-Tooth disease type 1A (CMT1A).
Researchers from Structure Therapeutics Inc. recently presented details on the discovery and preclinical evaluation of two new apelin receptor (APJ, APLNR) agonists – ANPA-0073 and ANPA-0137 – being developed for the treatment of pulmonary diseases.
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