Gluetacs Therapeutics (Shanghai) Co. Ltd. has discovered new proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN)-binding moiety coupled to a SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2) and SMARCA4-targeting moiety. They are designed for use in the treatment of cancer, transplant rejection, infections, diabetes, autoimmune, neurological, inflammatory and cardiovascular disorders, among others.
Chengdu Diao Pharmaceutical Group Co. Ltd. has patented new 1,2,4-triazole compounds characterized as apelin receptor (APLNR) agonists. As such, they are described as useful for the treatment of obesity, hypertension, pulmonary hypertension, heart failure, diabetes, atherosclerosis, osteoporosis and sarcopenia.
Dovetree Medicines Unus Inc. has divulged new cellular tumor antigen p53 (TP53) (Y220C mutant) stabilizers potentially useful for the treatment of cancer.
The Scripps Research Institute has identified new baloxavir analogues and their prodrugs acting as new influenza cap-dependent endonuclease (CEN) inhibitors potentially useful for the treatment of influenza viral infections.
Solve Therapeutics Inc. has disclosed new antibody-drug conjugates (ADCs) comprising antibody or antigen binding fragments targeting trophoblast glycoprotein (TPBG; 5T4) linked to a cytotoxic drug and therefore potentially useful for the treatment of cancer.
Nyrada Pty Ltd. has synthesized new short transient receptor potential channel 6 (TRPC6) and 7 (TRPC7) antagonists potentially useful for the treatment of cancer.
Aurigene Oncology Ltd. and Olema Pharmaceuticals Inc. have disclosed new proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase CBL-B (CBLB)-binding moiety coupled to a histone acetyltransferase KAT6A (MOZ; MYST-3)-targeting moiety. They are described as potentially useful for the treatment of cancer.
Avelos Therapeutics Inc. has divulged new sulfur or selenium-containing compounds acting as DNA polymerase θ (POLθ; POLQ) inhibitors potentially useful for the treatment of cancer.
A Purdue Research Foundation patent details the discovery of 5/5-5/6 bisaryl compounds acting as mitogen-activated protein kinase kinase kinase 7 (MAP3K7; TAK1) inhibitors reported to be useful for the treatment of multiple myeloma and inflammatory disorders.
Beone Medicines I GmbH and Beone Pharmaceutical (Suzhou) Co. Ltd. have identified new macrocyclic GTPase KRAS inhibitors potentially useful for the treatment of cancer.