Pharmaceutical patent analyst最新文献

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.

A series of 4-(imidazo[1,2-a]pyridin-3-yl)-pyrimidine derivatives are claimed as inhibitors of c-KIT and as potential treatments for cancer. Their chemical preparation and biological evaluation against imatinib-resistant tumor cells have been described. Several claimed molecules have excellent IC₅₀ values in the nanomolar range. Several molecules were also selective against a wide panel of kinases. Few specific inhibitors have been found to have promising oral bioavailability and acceptable to excellent values regarding the inhibition of hERG channel. This class represents a new platform for developing new anticancer treatment against a wide range of c-KIT mutations and secondary mutations that may arise in gastrointestinal stromal tumor patients.

Photoresponsive liposome development is needed to serve as a facile alternative to ELISA which is ineffective for detecting small levels of biomarkers due to low detection sensitivity. The US20210396744 patent application outlines novel photoresponsive liposomes for the detection of target substances with the aid of light. Although versatile, there may be possible stability issues that can be avoided with the appropriate selection of liposome components. Furthermore, the clinical success of this technology depends on many parameters like plasma stability, efficient loading of photosensitive components in the membrane and immobilization of molecular recognition elements to the membrane. Despite several challenges, they possess enormous potential to become a non-invasive tool for the detection of target substances.

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