An F. Hoffmann-la Roche Ltd. and Hoffmann-la Roche Inc. patent describes prodrugs of serine/threonine-protein salt-inducible kinases (SIK) inhibitors. They are reported to be useful for the treatment of atherosclerosis, type 2 diabetes, giant cell arteritis, glomerulonephritis, inflammatory bowel disease, metabolic dysfunction-associated steatohepatitis (MASH; NASH), primary sclerosing cholangitis and rheumatoid arthritis.
Researchers at F. Hoffmann-La Roche Ltd. and Hoffmann-La Roche Inc. have discovered GTPase KRAS mutant inhibitors, particularly G12V, G12D and G12C mutant inhibitors. They are reported to be useful for the treatment of cancer.
F. Hoffmann-La Roche Ltd. and Hoffmann-La Roche Inc. have synthesized pyridone carboxamide-derived compounds acting as soluble epoxide hydrolase inhibitors. They are reported to be useful for the treatment of diabetic retinopathy, neuropathic pain and neurodegenerative diseases.
F. Hoffmann-La Roche Ltd. and Hoffmann-La Roche Inc. have synthesized NLRP3 inflammasome inhibitors reported to be useful for the treatment of asthma, chronic obstructive pulmonary disease, cardiometabolic syndrome, cardiovascular disorders, Parkinson’s disease and Alzheimer’s disease.
F. Hoffmann-La Roche Ltd. and Hoffmann-La Roche Inc. have divulged kinesin-like protein KIF18A inhibitors reported to be useful for the treatment of cancer.
F. Hoffmann-La Roche Ltd. and Hoffmann-La Roche Inc. have divulged monoglyceride lipase (MGLL; MAGL) inhibitors reported to be useful for the treatment of cancer, amyotrophic lateral sclerosis, multiple sclerosis, pain, neuroinflammation, neurodegeneration, Alzheimer’s disease and inflammatory bowel disease, among other disorders.
F. Hoffmann-La Roche Ltd. and Hoffmann-La Roche Inc. have discovered new heteroarylphenyl ether derivatives acting as cyclin-dependent kinase CDK8/cyclin C inhibitors. As such, they are reported to be useful for the treatment of graft-vs.-host disease, transplant rejection, multiple sclerosis, rheumatoid arthritis, atopic dermatitis, psoriasis, amyotrophic lateral sclerosis and stroke, among others.
F. Hoffmann-La Roche Ltd. and Hoffmann-La Roche Inc. have divulged bifunctional epoxide hydrolase 2 (EPHX2; sEH) inhibitors reported to be useful for the treatment of pain, diabetic retinopathy and neurodegeneration. An exemplified compound (Ex 23 pg 78, claim 18) inhibited human sEH activity (IC50=0.5 nM) using Rapidfire mass spectrometry (RFMS) assays (WO 2025125135).
F. Hoffmann-La Roche Ltd. and Hoffmann-La Roche Inc. have identified new macrocyclic compounds acting as GTPase KRAS (G12C mutant) inhibitors reported to be useful for the treatment of cancer.
