Pharmaceutical P.I.N. Points - Patent Innovation News


Hemant N. Joshi, Ph.D., MBA - Tara Innovations, LLC - www.tarainovations.com and www.tara-marketing.com, [email protected]

The purpose of this column is to highlight and summarize recent key patents in the pharmaceutical arena issued by the US Patent O­ffice in August–September 2021.

Methods and Compositions Comprising Ursolic Acid and/or Resveratrol for Treating Diabetes, or Cancer

T. J. Slaga, J. Junco, H. Liang; S. Reyna; The Board of Regents of the University of Texas System; U.S. Patent # 11,090,311; August 17, 2021.

Ursolic acid (UA) is found in plants and fruits and it has been reported to have useful biochemical effects. Resveratrol is a stilbenoid - a type of natural phenol. It has been also studied for its potential therapeutic uses. This patent is a nutritional supplement comprising: ursolic acid and resveratrol in a ratio of ursolic acid to resveratrol of 3:1 to 1:3. RES and UA synergistically activate AMPK (AMP activated protein kinase) in a mouse model for skin cancer. RES sensitizes MT1/2 mouse papilloma cells and Ca3/7 mouse squamous carcinoma cells to UA. A higher concentration of RES increases the sensitivity of Ca3/7 cells to UA. UA and RES was also shown synergistically inhibit viability of human lung adenocarcinoma cell line A549.

Capsule for Detection of Gastrointestinal Motility and Method for Preparing the Same

Duan, H. Song, and S. Zhang; Ankon Medical Technologies, China; US Patent # 11,076,931; August 3, 2021.

Gastrointestinal motility is important for digestion and absorption of food. In the present invention, a capsule is used to detect the motility of GI tract. It comprises a capsule enclosure and one or more radiopaque markers filled in the capsule. Each radiopaque marker comprises a solid X-ray contrast agent, a medical grade plastic with a density less than 1.4 g/mL and an auxiliary agent. The X-ray contrast agent can be barium sulfate or bismuth sulfate or tungsten. The radiopaque markers are ring shaped markers, which come with four shapes of cross sections including O-ring, Double D, Cross and Tri-chamber. In one example, 25% Tungsten, 50% polypropylene and 25% auxiliary agent are mixed and injection molded or extruded in a ring-shaped mold to form the radiopaque marker. After cleaning and disinfecting, a preset quantity of radiopaque markers is filled into the capsule enclosure and packed and disinfected to form the detection capsule.

Diagnostic and Therapeutic Methods for the Treatment of Breast Cancer

A. Daemen and C. Metcalfe; Genentech, Inc., California, USA; US Patent # 11,081,236; August 3, 2021.

Estrogens and estrogen receptors (ER) are implicated in cancers, such as breast cancer. Estrogen receptor degradation is insufficient as a predictor of ER pathway activity or as a pharmacodynamics biomarker for endocrine therapy. There is an unmet need for biomarkers (e.g., transcriptional signatures), which comprehensively reflect ER pathway activity and can be useful in both diagnostic and therapeutic methods. The patent describes a method of identifying an ER pathway activity score. The patent also provides a method of selecting a therapy for an individual having breast cancer including an endocrine therapy. The ER pathway activity score is determined before and after endocrine therapy. 

Composition for Use as a Medicine or Dietetic Food in the Prevention and/or Treatment of Diabetes and Diabetes Associated Diseases

S. Banerjee; Berlin, DE; US Patent # 11,103,545; August 31, 2021.

The present invention relates to a composition of a maximum of six different plant extracts for use in the prevention and/ or treatment of diabetes Type 2 or Type 1. The plant extracts have antioxidative, anti-inflammatory, immune-modulating and neuronal hormone modulating properties. One of the combinations contained 160 mg Vitis vinifera (Grape seed), 180 mg of Phyllanthus emblica (Indian gooseberry), 160 mg Curcuma longa (turmeric) and 220 mg of Trigonella foenum-graecum (fenugreek) extracts. This is administered with at least one hypoglycemic agent such as metformin, sulfonyl urea, biguanide, glimepiride and their combinations. High oxidative stress prevails in diabetes. It is postulated that high oxidative stress in pancreatic islets leads to gradual apoptosis of beta cells, which in turn causes reduction in insulin production leading to uncontrolled diabetes.

Method of Treating Macular Degeneration Using Botulinum Toxin-Based Pharmaceuticals

G.E. Borodic; Canton, MA; U.S. Patent # 11,123,411; September 21, 2021.

Botulinum toxin is a neurotoxic protein produced by the bacterium Clostridium botulinum. It prevents the release of the neurotransmitter - acetylcholine from axon endings at the neuromuscular junction, thus causing flaccid paralysis. Macular degeneration is a major cause of human blindness, in a majority of cases, it could be irreversible. The botulinum neurotoxin is injected into or near the para-orbital region of the patient; along with an anti-VEGF agent such as bevacizumab. The botulinum neurotoxin increases potency or duration of action of the anti-VEGF agent. The botulinum neurotoxin is not injected in an intra-ocular region or a subconjunctival region.

Methods and Devices for Repair of Severed Peripheral Nerves with Erythropoietin

S.T. Li; STL Laboratories, Inc., USA; U.S. Patent # 11,116,876; September 14, 2021.

Erythropoietin is a glycoprotein cytokine secreted mainly by the kidney in response to cellular hypoxia. It stimulates red blood cell production in the bone marrow. A major clinical objective in the repair of severed peripheral nerves is to restore continuity between the proximal and distal nerve stumps, without which functional recovery is virtually impossible. The period of injury information transmittance, intracellular reorganization, and preparation for subsequent repair is referred to as the post-surgery latency period. After the latency period, axons from the proximal stump will sprout, extend in length, and attempt to reach its end target organ. Erythropoietin has been shown to shorten latency period, accelerate myelination of regenerated axons overall repair of peripheral ruptured nerve. This patent describes a drug-delivery device comprising a matrix formed of a biopolymer and an erythropoietin.

Nose-to-Brain Drug Delivery Device

S.K. Lee, K.H. Chung, I. Ullah, P. Kumar, and S. Lee; IUCF-HYU, Seoul, KR; U.S. Patent # 11,097,073; August 24, 2021.

Delivery of drugs directly to brain via the nose has many advantages. It has been termed a nose-to-brain drug delivery device. A nose-to-brain drug delivery device includes a chamber to store freeze-dried drug, another chamber to store a suitable solvent, a membrane for preventing the freeze-dried drug from being mixed with the solvent, and a compressor for providing a driving force. The membrane is opened by the driving force of the compressor to mix the freeze-dried drug with the solvent, thereby dissolving the freeze-dried drug, and the solution is sprayed by the driving force of the compressor. The drug solution is sprayed into a nose of a subject in a Mecca position state where the head of the subject faces a chest of the subject. There are four different head positions for nasal delivery of drugs - Mecca, Mygind, Ragan and Head back. Inventors chose the Mecca position for their drug delivery.

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