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.

Quinoline inhibitors are appealing medicinal products for a range of illnesses and problems. It is bicyclic heterocyclic scaffold has been intensively employed in pharmacological research and is well known for its wide range of biological purposes. Biological activities exhibited by quinoline derivatives, such as anti-inflammatory properties, antioxidant, antimicrobial, anti-tubercular, antidiabetic, anti-malarial and others are covered in detail in this review. The IC₅₀ of patented inhibitors might range from nm to μM range, based on the experiments used. It presents an outline of patents file between 2002 and 2023 concerning to biological activities by quinoline derivatives. As a result, it is critical to develop additional chemical quinoline core alterations for novel chemical compounds and enhanced pharmacological impacts.

Aim: the activity of patent claims by Mexican pharmaceutical companies is unknown. Objective: analyse the trend in patents of Mexican pharmaceutical companies. Method: a search for patents was carried out in the patent database of the Mexican Institute of Industrial Property, using the list of Mexican pharmaceutical companies belonging to the Mexican Association of Pharmaceutical Research Industries, and the codes A61K, A61P and C07 of the International Patent Classification. Results: the leading companies in patent applications were Liomont, Senosiain and RIMSA; however, Mexican pharmaceutical companies claim very few patents, only 266 patent applications in the period 2000-2020, with a technological factor with a value of zero, and a commercial factor of little value. Conclusion: Mexican pharmaceutical companies lack a robust patent system, without growth, and with a low percentage of patents with high commercial value.

Pancreatic adenocarcinoma, a devastating disease, has the worst cancer prognosis in humans. It often develops resistance to common chemotherapy medications, such as gemcitabine, taxol and 5-fluorouracil. The dense stroma limits therapeutic efficacy in treating this disease. Low or limited drug loading capacity is another problem with current chemotherapeutic agents. There is a need to develop novel approaches to overcome these issues. Hence, an innovative approach has been proposed to co-deliver both hydrophilic (Gemcitabine) and hydrophobic (Paclitaxel) drugs in a single carrier using lipid bilayer-mesoporous silica nanoparticles (LB-MSNP). MSNPs offer effective drug delivery due to their superior bioavailability and physicochemical properties. Further, in order to achieve clinical translation and regulatory approval, toxicity and biodegradability of MSNPs must be resolved.

Post-surgery cancer recurrence is one of the reasons for increased cancer cases. The effective usage of the enhanced permeability and retention effect of a nanocarrier infused with the bioresponsive release mechanism of checkpoint inhibitors (aPD1 and aCTLA4) can become a boon to mankind. DNA nanococoons (DNCs) comprising cytosine-phosphorothioate-guanine oligodeoxynucleotides (CpG-ODNs) with potent immunostimulatory effects can significantly enhance anti-cancer activity. Triglycerylmonostearate (TGMS) with enzymatic cleavage potential at the wound sites of tumor resection, upon caging with restriction enzyme (HhaI) followed by attaching to DNCs, makes the immunotherapy bioresponsive. Hhal-TGMS-DNCs-aPD1 triggered by the inflammation at the wound site undergoes enzymatic cleavage, releases the restriction enzyme, converts DNCs to CpG ODNs sequentially and with sustained aPD1 release exerts an appreciable anti-cancer effect.

Aging and proteotoxicity go hand in hand. Inhibiting proteotoxicity has been proposed to extend lifespan. This invention describes a new strategy to limit proteotoxicity and to extend the lifespan. Loss of function of sul-2, the Caenorhabditis elegans steroid sulfatase, elevates the pool of sulfated steroid hormones, increases longevity and ameliorates protein aggregation diseases. The present invention provides a group of molecules for use in the prevention of aging-associated proteotoxicity caused by protein aggregation diseases and/or to increase the lifespan of a eukaryotic organism. These molecules are either steroid sulfatase inhibitors or sulfated C19 steroids, both of which reproduce the phenotype of sul-2 mutants. One particular representative example is STX-64. Potential applications of the claims have been demonstrated in animal models of Parkinson's disease, Huntington's disease and Alzheimer's disease.

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

Leishmaniasis, a neglected tropical disease, is caused by protozoal parasites of the genus Leishmania. Clinical manifestations vary from asymptomatic to lethal grade depending on the type of the disease. The currently available antileishmanial drugs suffer from considerable limitations. There is a dire need for better and safer drugs and/or vaccines to eradicate this disease. There are enormous developments ongoing in this field. Newer combinations of existing drugs and newer drugs targeting these intracellular parasites as well as their vectors are being tried to control the disease. Attempts to develop vaccines to enhance the immunity of the patient have shown some promise. This article is a peep into the recent patent developments in this field.

Repurposing of approved drugs allows strong savings in time and investment. Rimantadine is an FDA-approved drug for prevention and treatment of influenza A infection. Patent US2021330605 describes the use of rimantadine, an adamantane derivative, for the treatment of melanoma, breast cancer and head and neck squamous cell carcinoma. Rimantadine inhibited proliferation of cell lines of melanoma, breast cancer, and head and neck squamous cell carcinoma, increased the survival of mice injected with cancer cell lines and restores the expression of MHC class I. Rimantadine has the potential to be used successfully in the treatment of head and neck squamous cell carcinoma.