Fudan University and Shanghaitech University have developed proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase binding agent coupled to Bcl-2-like protein 1 (Bcl-xl; Bcl-X; BCL2L1) targeting moiety via linker. They are reported to be useful for the treatment of cancer, autoimmune disease, myelofibrosis, neurodegeneration, kidney fibrosis, transplant rejection, diabetes and cardiovascular disorders, among others.
Pyrrole fused-ring pyrazole compounds have been prepared by Hangzhou Zhongmei Huadong Pharmaceutical Co. Ltd. and characterized as mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1; HPK1; MEKKK1) inhibitors reported to be useful for the treatment of cancer.
Research at Merck KGaA has led to the development of substituted heterocycles acting as kinesin-like protein KIFC1 (HSET) inhibitors reported to be useful for the treatment of cancer.
Innovo Therapeutics Inc. has prepared and tested new isoindolinone derivative compounds characterized as caspase-1 (IL-1β-converting enzyme), interleukin-1β (IL1B; IL-1β) and apoptosis inhibitors reported to be useful for the treatment of osteoarthritis and pain.
Biohaven Therapeutics Ltd. has patented new pyrazolo[1,5-a]pyridin-2,3-yl amides acting as potassium voltage-gated channel subfamily KQT member 2/3 (KCNQ2/3) activators.
Lawrence Livermore National Laboratory, Leidos Biomedical Research Inc. and Theras Inc. have jointly patented GTPase KRAS (G12C mutant) inhibitors reported to be useful for the treatment of cancer.
A Design Therapeutics Inc. patent details conjugates consisting of DNA-binding moiety capable of noncovalently binding to a nucleotide repeat sequence linked to protein binding moiety through oligomeric backbone linker.
Research at Blossomhill Therapeutics Inc. has led to the discovery of new macrocyclic compounds acting as tyrosine kinase inhibitors and reported to be useful for the treatment of autoimmune disease.
Beijing Scitech-MQ Pharmaceuticals Ltd. described receptor-interacting serine/threonine-protein kinase 1 (RIPK1) inhibitors reported to be useful for the treatment of cancer.