Northern Illinois University and Stream Neuroscience Inc. have patented benzothiazole derivatives acting as phosphodiesterase‑4 (PDE4) inhibitors and reported to be useful for the treatment of cancer, cognitive, inflammatory and mood disorders.
Transpire Bio Inc. has signed an exclusive license agreement with Suzhou Intragrand Pharma Co. Ltd. for ITG-1052 (lenamilast), an investigational phosphodiesterase 4 (PDE4) inhibitor.
Phosphodiesterase 4 (PDE4) is an enzyme known to play a role in inflammatory responses, and it has been pinpointed as an interesting therapeutic target for diseases like atopic dermatitis (AD), but limited efficacy and side effects have prevented the approval of oral formulations.
Palisade Bio Inc. has submitted a clinical trial application (CTA) for PALI-2108 for the treatment of ulcerative colitis, following a pre-CTA consultation meeting with Health Canada. Pending clearance, the company anticipates initiating a phase I study by year-end.
Researchers from Southern Medical University have divulged the discovery and preclinical characterization of novel PDE4 inhibitors for the treatment of hepatic sepsis. Synthesis and optimization of a series of 7-alkoxybenzofurans led to the identification of compound [I] as the lead PDE4 inhibitor, with PDE4B and PDE4D IC50 values of 10.0 and 15.2 nM, respectively.
Reistone Biopharma Co. Ltd. has described phosphodiesterase PDE4B1 inhibitors reported to be useful for the treatment of asthma, chronic obstructive pulmonary disease, acute respiratory distress syndrome, atopic dermatitis, overactive bladder, psoriasis, ulcerative colitis and urticaria, among others.
Cerevel Therapeutics Inc. and Pfizer Inc. have jointly developed azaindole compounds acting as phosphodiesterase 4 (PDE4) inhibitors potentially useful for the treatment of psoriasis, atopic dermatitis, idiopathic pulmonary fibrosis, diabetes, sepsis, autoimmune disease, cystic fibrosis and inflammatory bowel disease, among others.
Sensorium Therapeutics Inc. has identified alkylated derivatives of mesembrine or mesembrenone acting as serotonin transporter (SERT) and/or phosphodiesterase PDE4 inhibitors reported to be useful for the treatment of anxiety, depression and stress disorders.
Palisade Bio Inc. has completed its analysis evaluating ex vivo bioactivation of PALI-2108, an orally administered, locally acting colon-specific phosphodiesterase-4 (PDE4) inhibitor prodrug in development for ulcerative colitis.
