Pfizer Focuses Recent Patent Activity on Antibacterial Agents

By Steve Brachmann
September 12, 2014

Pfizer, Inc., is a major American developer of pharmaceutical medications and vaccines for a wide spectrum of medical disciplines. The majority of Pfizer’s business is operated in the northeastern United States, where the company has its corporate headquarters in New York City and its research headquarters in Groton, CT. A Pfizer vaccine that helps to protect against clostridium difficile, a potentially life-threatening bowel infection, received a fast-track designation from the U.S. Food and Drug Administration in late August of this year. The company also recently announced that it has struck a partnership with fellow American pharmaceutical giant Merck & Co. to conduct and evaluate a study on a treatment for lung cancer. Although Pfizer’s efforts to acquire British drug manufacturer AstraZeneca were squashed in May, speculation regarding stock movement in recent weeks has led some to believe that Pfizer may try to revisit the negotiations soon.

The Companies We Follow series  is visiting this major manufacturer of medications as we continue our survey of recent innovations in pharmaceutical fields. Patent applications recently published by the U.S. Patent and Trademark Office show that Pfizer’s recent development goals have focused on a broad spectrum of diseases and disorders. We discuss a trio of patent applications related to treatments involving the nervous system, including a couple of medications treating Alzheimer’s disease along with a host of other ailments. A couple of patent applications are also related to novel treatments for cancer, especially in the area of preventing cancerous growth.

Treatments for a number of bacterial infections which can develop in hospital settings was another field of innovation reflected both in Pfizer’s patent applications as well as the patents recently assigned to the company. A couple of recently issued patents protect treatments against gram-negative bacteria by inhibiting a catalyst enzyme necessary for bacterial reproduction. Medications for inflammatory diseases and allergic conditions were protected by a couple of patents also issued within these past few weeks. We also explore two patents assigned to Pfizer which disclose and protect useful treatments for Type II diabetes.

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Pfizer Patent Applications: Cancer Treatments, Neurological Health and Preventing Bacterial Infections

Pfizer is a developer of some of the most major pharmaceutical innovations over the past few decades, including the cholesterol reducing Lipitor; Lyrica, a treatment for fibromyalgia and neuropathic pain; Celebrex, an anti-inflammatory medication; and Viagra, a drug for men’s reproductive systems. As we noted in our introductory section, Pfizer is trying to make its presence felt in the field of cancer research along with partner corporation Merck. With this in mind, we noted a couple of patent applications filed by this corporation to protect novel cancer treatments. Compounds for use in antibody-drug-conjugates (ADCs) designed to fight against cancerous growths are described within U.S. Patent Application No. 20140134193, which is titled Spliceostatin Analogs and Methods for Their Preparation. The invention focuses on novel analogs and derivatives of cytotoxic spliceostatin, which can be used as part of a treatment to kill or inhibit the proliferation of tumors and cancer cells, or treat other pathological conditions. Another compound developed to prevent against cancerous tumor growth is disclosed in U.S. Patent Application No. 20140179667, filed under the title Aryl and Heteroaryl Fused Lactams. The compound that would be protected by this patent application inhibits the activity of wild or mutant enhancer of zeste homolog 2 (EZH2), a catalyst that plays a key role in regulating gene expression. EZH2 is often overexpressed in cancer cells and has been linked to chemoresistance and metastasis.

Diseases and health conditions affecting a patient’s nervous system are also addressed by a couple of other medicinal innovations developed in recent months by Pfizer. In our recent coverage of other pharmaceutical manufacturers, like Eli Lilly, we caught a couple of inventions related to the treatment of Alzheimer’s disease, a condition causing neurological degeneration in older patients which is likely to grow in prevalence over the coming years. U.S. Patent Application No. 20140243312, which is titled Pyrrolo[2,3-D]Pyramidine Derivatives, would protect preparations of a pharmaceutical compound useful in the inhibition of Janus Kinase (JAK), which plays a role in cytokine signaling which leads to gene expression. Improper kinase activity has been connected to Alzheimer’s disease and many other health conditions, like cancer, autoimmune disease, cardiovascular disease and more. Another method for treating Alzheimer’s could be protected for this company through the filing of U.S. Patent Application No. 20140155627, entitled Process for Forming Amorphous Atorvastatin. The process of forming atorvastatin that would be protected here provides for the large-scale production of amorphous atorvastatin without excessive toxicity or environmental concerns. The amorphous atorvastatin created in this process can be used to treat Alzheimer’s disease as well as osteoporosis and hypercholesterolemia. Methods for treating neuropathic pain, caused by damage to the nervous system, that have been created by Pfizer are discussed within U.S. Patent Application No. 20140206670, filed under the title Combinations Comprising Alpha-2-Delta Ligands. This treatment combines alpha-2-delta ligands with a dual serotonin-noradrenaline re-uptake inhibitor (DSNRI), which have a synergistic effect allowing them to treat neuropathic pain within a patient. This synergistic effect also allows patients to be treated for pain with lower pharmaceutical doses, reducing the risk of side effects when administering the medication.

When a patient’s health condition reaches the point of hospitalization, it is ideal to give those people the optimal protections possible against bacterial infections that can be contracted in hospital settings and exacerbate already poor health issues. Pfizer is hoping to patent a compound designed to prevent bacterial infections with U.S. Patent Application No. 20140206651, filed under the title Hydroxamic Acid Derivatives Useful as Antibacterial Agents. This patent application would protect a pharmaceutical compound that provides an antibiotic agent to act against gram-negative bacteria, which is found in hospital settings. Gram-negative bacteria causes infection and is increasingly resistant to prior antibiotics and other drugs.

Cardiovascular disease is another major health problem among populations in developed countries, and millions of Americans are at risk of developing heart disease and suffering cardiac events. An antibody used to treat those suffering disorders involving improper cholesterol levels may become part of Pfizer’s patent portfolio through the filing of U.S. Patent Application No. 20140161821, titled Treatment with Anti-PCSK9 Antibodies. The proprotein convertase subtilisin kexin type 9 (PCSK9) agonist antibody disclosed here can treat disorders characterized by elevated levels of low-density lipoprotein (LDL) cholesterol, which may include atherosclerosis, acute coronary syndrome and other cardiovascular disease.

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Issued Patents of Note: Allergy Suppressants, Diabetes Treatments and More Bacterial Protections

For many decades, since the middle of the 20th Century, Pfizer has operated mainly as a research-oriented pharmaceutical developer. This has resulted in a very strong patent portfolio for the corporation, with new patents being added to these holdings every week representing a wide scope of medicinal innovation. Bacterial infections caused by pathogens like Psuedomonas aeruginosa, which are targeted by the technology described in the ‘651 patent application in the previous section, are also the focus of two pharmaceutical compounds protected through patents recently issued by the USPTO. U.S. Patent No. 8809333, which is titled Imidazole, Pyrazole, and Triazole Derivatives Useful as Antibacterial Agents, protects novel hydroxamic derivatives used to treat bacterial infections by inhibiting LpxC, a catalyst enzyme necessary for lipid biosynthesis. Suppressing the biosynthesis of certain lipids catalyzed by LpxC can be fatal to the bacterial infection. Another innovation regarding a new class of LpxC inhibitors is protected for Pfizer through the recently issued U.S. Patent No. 8779148, entitled Fluoro-Pyridinone Derivatives Useful as Antibacterial Agents. Although the chemical makeup of this compound differs from the pharmaceutical compound protected by the ‘333 patent above, it also works to inhibit cellular LpxC activity within the body of a patient suffering from a gram-negative bacterial infection. Interestingly, both of these pharmaceutical innovations can be used in doses for either human or animal consumption, in case there is a need to treat for bacterial infection in livestock or companion animals.

Allergies of various kinds are endemic to populations in developed countries, and it’s estimated that between 20 percent and 30 percent of the population in Western countries are affected by these health conditions. We noticed that allergy medicines were one area of development for which Pfizer just received a couple of new U.S. patent grants. A composition that can help in the suppression of allergic reactions is protected and disclosed by U.S. Patent No. 8722053, which is titled IgE CH3 Peptide Vaccine. This patent protects an immunogen, an antigen producing an immune system response, which is comprised of an antigenic immunoglobin E (IgE) peptide. This allergy treatment is capable of producing anti-IgE antibodies to reduce levels of circulating free IgE in lower doses, reducing toxicity issues as well as cost. Anti-inflammatory drugs for the treatment of a wide spectrum of allergic conditions have also been protected by Pfizer through U.S. Patent No. 8822439, issued under the title Glucocorticoid Receptor Agonists. The compound protected by this patent can be topically applied for the treatment of inflammatory and allergic conditions, including asthma and psoriasis. This innovation offers more metabolic stability than previous treatments, which increases the in vivo half-life of the treatment and can reduce the dosage required to treat a patient.

Finally, we’re closing up our look at Pfizer’s recently patented pharmaceutical inventions with a look at a couple of patents issued by the USPTO to protect novel treatments for diabetes and related conditions. U.S. Patent No. 8735396, which is titled Benzofuranyl Derivatives, protects a novel treatment method for non-insulin dependent diabetes mellitus (NIDDM), or Type II diabetes. The pharmaceutical treatment method protected by this patent works to induce cellular glucokinase activity, thereby inducing glycogen synthesis and preventing the release of glucose into a patient’s blood. This glucokinase activator can also provide therapeutic benefits for diabetes symptoms, including obesity and hypertension. Patients suffering from Type II diabetes or obesity-related diseases will have a new treatment option available through Pfizer thanks to U.S. Patent No. 8802688, entitled Substituted Acetyl-CoA Carboxylase Inhibitors. This patent protects yet another pharmaceutical compound developed by this company; this particular compound is designed to inhibit the activity of acetyl-CoA carboxylase (ACC). Inhibition of ACC can increase fatty acid utilization while decreasing fatty acid synthesis, leading to the selective loss of body fat.

The Author

Steve Brachmann

Steve Brachmann is a freelance journalist located in Buffalo, New York. He has worked professionally as a freelancer for more than a decade. He writes about technology and innovation. His work has been published by The Buffalo News, The Hamburg Sun, USAToday.com, Chron.com, Motley Fool and OpenLettersMonthly.com. Steve also provides website copy and documents for various business clients and is available for research projects and freelance work.

Warning & Disclaimer: The pages, articles and comments on IPWatchdog.com do not constitute legal advice, nor do they create any attorney-client relationship. The articles published express the personal opinion and views of the author and should not be attributed to the author’s employer, clients or the sponsors of IPWatchdog.com. Read more.

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