Researchers at Schrodinger Inc. and Takeda Pharmaceutical Co. Ltd. have described 3C-like proteinase (3CLpro; Mpro; nsp5) inhibitors reported to be useful for the treatment of coronavirus acute respiratory syndrome.
Scientists at H. Lundbeck A/S and Vernalis (R&D) Ltd. have divulged leucine-rich repeat kinase 2 (LRRK2; Dardarin) and LRRK2 G2019S mutant inhibitors reported to be useful for the treatment of Parkinson’s disease, Lewy body dementia and multiple system atrophy.
Scientists at East China Normal University, East China University of Science & Technology, Jinfeng Laboratory and Zhengzhou University have identified ribosomal protein S6 kinase α-6 (RPS6KA6; RSK-4) inhibitors reported to be useful for the treatment of cancer.
Jnana Therapeutics Inc. has synthesized sodium-dependent neutral amino acid transporter B(0)AT1 (SLC6A19) inhibitors reported to be useful for the treatment of amino acid metabolism disorders, amino acid transport disorders and metabolic and nutritional genetic disorders, among others.
Cullgen (Shanghai) Inc. has disclosed proteolysis targeting chimera (PROTAC) compounds comprising a DDB1- and CUL4-associated factor 1 (DCAF1) binding moiety covalently linked to target protein moiety (such as bromodomain-containing protein 4 [BRD4; HUNK1], cyclin-dependent kinase 4 [CDK4] and estrogen receptor α [ER-α; ESR1]) through a linker reported to be useful for the treatment of cancer.
Having failed in their efforts to get the U.S. NIH to march in on Xtandi’s patents under the Bayh-Dole Act because of price, Knowledge Ecology International and two other advocacy groups are now asking the Centers for Medicare & Medicaid Services (CMS) to do what the NIH refused to do. But rather than pressing for a march-in, which can be a lengthy process, the groups are pushing for CMS to use other statutory tools to clear the way for Xtandi (enzalutamide) generics to launch in the U.S. before Astellas Pharma Inc.’s three remaining patents for the prostate cancer drug expire in 2026 and 2027.
Eli Lilly and Co. continues its development of an oral drug delivery device that can successfully deliver a drug that would otherwise be ineffective when taken orally.
Cerevel Therapeutics LLC has described muscarinic M4 receptor agonists reported to be useful for the treatment of pain, sleep disorder, schizophrenia, substance abuse and dependence, drug-induced dyskinesia, Alzheimer’s disease and Parkinson’s disease.
Simcere Zaiming Pharmaceutical Co. Ltd. has divulged proteolysis targeting chimera (PROTAC) compounds comprising a cereblon E3 ubiquitin ligase binding moiety coupled to a probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α) and/or bromodomain-containing protein 4 (BRD4; HUNK1) targeting moiety through a linker reported to be useful for the treatment of cancer.
Scientists at Ez Bioxcel Solutions Pvt Ltd., Invea Therapeutics Inc. and Inveniai LLC have identified apoptosis-associated speck-like protein containing a CARD (PYCARD; ASC) inhibitors reported to be useful for the treatment of primary sclerosing cholangitis, arthritis and inflammatory disorders.