Pharmaceutical patent analyst最新文献

Morita-Baylis-Hillman adducts are polyfunctionalized compounds that result from a three-component reaction involving an electrophilic sp² carbon (aldehyde, ketone or imine) and the α-position of an activated alkene, catalyzed by a tertiary amine. These adducts exhibit a wide range of biological activities and act as valuable starting materials for developing drug candidates, pesticides, polymers, and other applications. In this regard, the present review aimed to explore the biological potential of Morita-Baylis-Hillman adducts and their derivatives as documented in patent literature. Additionally, the review delves into the synthetic methodologies employed in their preparation.

A snapshot of recent noteworthy developments in the patent literature of relevance to pharmaceutical and medical research and development.

RET and ROS1 are becoming key targets for targeted therapy. To show current landscape of ROS1 and RET targets, a patent analysis was performed. The present results indicated that inhibitor structures of ROS1 target demonstrated unique elements compared with inhibitor structures of RET or BRAF targets. Our study was the first time to uncover that a number of inhibitor structures of ROS1 target contained sulfur and boron elements. The inhibitors of RET target could be developed for treatment of various cancers, including lung cancer, thyroid cancer, and other solid tumor, while the inhibitors of ROS1 target are virtually developed for treatment of lung cancer. Our findings provide a new insight for drug discovery of ROS1 and RET target.

A snapshot of noteworthy recent developments in the patent literature of relevance to pharmaceutical and medical research and development.

Current medications for Alzheimer's disease help manage symptoms and behavioral problems. Nevertheless, they do not slow the progression of cognitive decline or dementia. A potential approach for treating Alzheimer's disease is to target neurons that are sensitive to disease pathobiology such as glutamatergic neurons. Several patents disclosed methods for treating Alzheimer's disease by administering riluzole or its prodrugs. Clinical trials revealed that 6 months treatment using riluzole or troriluzole is associated with a slower decline in the tomographic measures of the positron emissions of cerebral glucose metabolism in Alzheimer's patients. The proposed strategy claims to prevent and/or slow the cognitive decline of Alzheimer's patients and to enhance global functioning. These claims may also pave the way for other glutamate modulators to be used for Alzheimer's disease.

Aberrant expression of the WNT signaling pathway has been associated with cancer progression and recurrence. Research over the decades has led to development of WNT-targetable small molecules, but has faced challenges in translating to clinics. Unlike WNT/β-catenin inhibitors, WNT5A-mimicking peptide, Foxy5 has shown encouraging efficacy in impairing metastasis of cancers with low or absent WNT5A expression. Recent patent application US20210008149 advocates the implication of Foxy5 for treatment and prevention of cancer relapse. The inventors have demonstrated the anti-stemness activity of Foxy5 in mice xenograft model via suppressing the expression of colonic cancer stem cell markers. Foxy5 also exhibits non-toxic nature when administered alone or in synergy with standard chemotherapy thus strengthening its candidature in the field of cancer therapeutics.