Pharmaceutical patent analyst最新文献

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.

Co-processing involves the incorporation of one excipients into the particle structure of other excipients to overcome the deficiencies of each excipients. The current patent describes the co-processing of microcrystalline cellulose and mannitol via fluid bed agglomeration with an aim to limit the use of lubricant in tablet composition. The co-processed excipients blend was compared with the physical blend of excipients and characterized for scanning electron microscopy, disintegration and hardness. The average particle size of co-processed excipients was less than 0.55 mm, characterized by large individual lactose-coated particles whereas, the physical blend particles are uncoated and irregular in shape. Tablets made from both physical blend and co-processed excipients were compared. As per the hardness and disintegration studies, with increase in mixing time of excipients both hardness and disintegration time decreases.

Aim: pharmaceutical patenting activity in developing countries, including Mexico, is unknown. Objective: determine the activity of pharmaceutical patents by Mexican universities. Method: using 'university' as keyword and A61K, A61P and C07 as International Patent Classification codes, was searched to generate a perspective of pharmaceutical patent applications by Mexican universities. Results: 227 patents (186 granted patents + 41 not-granted patents) were claimed in the period 2000-2018. The leading university was the National Autonomous University of Mexico, followed by the Instituto Politecnico Nacional, Universidad Autonoma de Nuevo León and Universidad Autonoma de Puebla. The pharmaceutical concerns addressed were led by the fields of infectious, cancer and diabetes. Conclusion: in Mexican universities, the licensing of pharmaceutical patents is still in its early stages.

Insulin, on oral administration, is very troublesome because of its limited bioavailability. The evolution of oral insulin delivery formulations is greatly desired for non-invasive therapy by overcoming its low bioavailability, GIT enzymatic deactivation, poor lipophilicity and low stability. Different approaches have been proposed to boost oral insulin bioavailability in insulin-delivery systems and emerging effective therapies by using nanoparticle formulation, nanocapsid, modified chitosan particles, polydopamine microcapsules and nanoliposomes. The present review includes patents and patent applications that were published between 2017 and January 2022.