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.
Recurium IP Holdings LLC has synthesized proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN) binding moiety covalently linked to a Wee1-like protein kinase (Wee1)-targeting moiety via a linker reported to be useful for the treatment of cancer.
Vanderbilt University has disclosed mGlu5 receptor negative allosteric modulators reported to be useful for the treatment of anxiety, autism spectrum disorders, diabetes, pain, Parkinson’s disease, multiple sclerosis, depression and obesity, among others.
Vanqua Bio Inc. has divulged C5a anaphylatoxin chemotactic receptor 1 (C5aR; CD88) antagonists reported to be useful for the treatment of autoimmune disease, cancer, infections and cardiovascular, inflammatory and neurological disorders.
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