Merck, Pfizer and Eli Lilly patenting to stay ahead of patent cliff

Two men try to reach across the divideThe early months of 2015 have been interesting ones for the pharmaceutical industry, an incredibly valuable industry sector that comes under our focus from time to time here at IPWatchdog. The first quarter of this calendar year has seen a number of mergers and acquisitions which are showing us that the patent market for pharmaceuticals is quite active right now. We recently profiled some of the IP portfolio held by Auspex Pharmaceuticals, purchased for $3.5 billion in March by Teva Pharmaceuticals and that’s only one of a handful of multi-billion deals that have occurred within the past few weeks.

Of much concern over the past few months is the patent cliff being faced by some pharmaceutical companies because of the loss of certain patent protections for high-profile, blockbuster drugs. In February 2015, Moody’s Investor Service published a “Global Pharmaceuticals Snapshot”, which identified the stability of certain companies based on their patent pipelines and exposure to patent expirations. According to Moody’s, the five companies that have higher patent exposure than they did in 2013 are Novo Nordisk, Amgen, Merck, Pfizer and Eli Lilly. Of the these companies, Merck, Pfizer and Eli Lilly, are companies that we have covered in the past as part of our Companies We Follow series. With that in mind, today we wanted to take some time to look at the patents recently issued to this trio of pharmaceutical firms to see how these companies are trying to rebuild their interests in the face of patent expirations.



Merck Patents Treatments for Schizophrenia, Chronic Pain and Hepatitis C


“Merck UG Office” by Montgomery County Planning Commission is licensed under CC BY-SA 2.0.

It’s been a tough couple of months for Merck, Sharp & Dohme Corp. of Rahway, NJ, where patents are concerned. In December, the $8.4 billion purchase of Cubist Pharmaceuticals turned sour for Merck after a federal judge invalidated four of the five patents protecting Cubicin, an antibiotic that accounts for about 80 percent of Cubist’s sales. The company has also had to divert resources in order to respond to generic variations of Nasonex and other medications that competitors have been trying to unload on the market in the face of certain Merck patent holdings. Still, in April, Merck spent $434 million to develop a business partnership with Arvinas, which develops protein-targeting therapeutics for ridding unwanted proteins from a patient’s body.

We were intrigued to find a couple of patents issued to Merck in recent weeks to protect treatments for neurological disorders, especially schizophrenia. U.S. Patent No. 8993779, which is titled Positive Allosteric Modulators of MGLUR2, protects a pharmaceutical compound composed of a benzimidazolone derivative which works to modulate the mGluR2 receptor to treat disorders associated with glutamate dysfunction, including schizophrenia. Glutamate is an important amino acid involved with a range of central nervous functions, including motor control and cardiovascular regulation. Pharmaceutical treatments for schizophrenia are also discussed within U.S. Patent No. 8969364, titled Inhibitors of Catechol O-Methyl Transferase and Their Use in the Treatment of Psychotic Disorders. The patent claims a compound that acts as an inhibitor of catechol O-methyltransferase (COMT), an enzyme which is important for the breaking down of dopamine in the prefrontal cortex of the human brain. The invention is designed to selectively enhance dopamine neurotransmission to treat the cognitive symptoms of both schizophrenia and bipolar disorder, which cause overlapping symptoms and are both linked to genetic COMT activity.

Merck has also been busy developing antiviral medications for the treatment of some major pathogens, such as the hepatitis C virus. U.S. Patent No. 8980920, which is titled Antiviral Compounds of Three Linked Aryl Moieties to Treat Diseases Such as Hepatitis C, protects a pharmaceutical compound that contains linked tricyclic aryl compounds for the treatment or prevention of hepatitis C in a patient. The innovative treatment addresses a need for small-molecule compounds with desirable physicochemical properties for inhibiting viruses and reducing viral load. We also took a closer look at a treatment developed for those suffering from chronic pain after a traumatic injury, which is explained within U.S. Patent No. 8952001, issued under the title Amino-Heteroaryl Derivatives as HCN Blockers. The patent discloses the use of amino heteroaryl derivatives as a pharmaceutical treatment for chronic neuropathic pain by blocking hyperpolarization-activated, cyclic nucleotide-gated (HCN) channels, thereby inhibiting certain currents that can induce spontaneous nerve activity leading to chronic pain after an injury, disease or surgery.


Eli Lilly Obtaining Fewer Patents, Focusing on Cancer and Alzheimer’s


By Eli Lilly and Company, converted to PNG by Huwmanbeing.Huwmanbeing at en.wikipedia [Public domain], from Wikimedia Commons

2014 was also a rough year for pharmaceutical developer Eli Lilly and Company of Indianapolis, IN. Expirations of patents protecting Cymbalta, a treatment for depression, and the osteoporosis medication Evista have caused sales of both to drop by more than half, 74 percent in the case of Evista. Near the end of March, this company announced a partnership with Chinese-based Innovent Biologics which will involve a $56 million investment by Eli Lilly to jointly develop three experimental cancer drugs. As we’ve pointed out in recent posts here on IPWatchdog, Chinese joint venture rules which compel foreign firms to transfer intellectual property rights to Chinese domestic firms should give executives at Eli Lilly at least some pause while pursuing this partnership. The corporation has shown the willingness to protect their IP rights through legal arbitration with foreign governments, such as the NAFTA arbitration proceedings initiated by Eli Lilly in September 2013 in response to the Canadian government’s invalidation of patents protecting Strattera, an adult ADHD medication, and Zyprexa, a treatment for psychotic mental disorders.

Even though the Moody’s report on pharmaceutical firms identified Eli Lilly as having a strong new drug pipeline, our research using Innography’s patent portfolio analysis tools is showing us that the company has received relatively few patents in recent months. Over the past year, Eli Lilly earned 45 patents from the U.S. Patent and Trademark Office; by comparison, Merck was issued 461 U.S. patents over the same period of time.

Cancer and Alzheimer’s disease are two pathological heavyweights that continue to baffle modern medicine but recent patents indicate that Eli Lilly is focused on contributing to this area of concern. U.S. Patent No. 9000023, entitled Disubstituted Phthalazine Hedgehog Pathway Antagonists, claims a method of treating cancer in a mammal by administering an effective amount of a pharmaceutical compound containing novel 1,4-disubstituted phthalazine hedgehog pathway antagonists, which play an important role in both embryonic pattern formation and adult tissue maintenance. This innovation serves as a treatment option for any of the many cancers which are driven by inappropriate hedgehog signaling. The diagnosis of Alzheimer’s disease or a predisposition towards that neurological disorder is the focus of U.S. Patent No. 8932557, which is titled Imaging Agents for Detecting Neurological Dysfunction. It protects a method of administering a radiolabeled compound to a patient, allowing the compound to distribute into brain tissue and imaging the brain tissue so that a high amount of compound binding to brain tissue is seen as an indicator of Alzheimer’s disease. This innovation employs conventional imaging techniques, such as positron emission tomography (PET) or single photon emission computed tomography (SPECT).

Anemias of chronic diseases like cancer or kidney disease are targeted by the Eli Lilly innovation protected by U.S. Patent No. 8980582, titled BMP-6 Antibodies and DNA Encoding the Same. It claims a DNA molecule with a specific polynucleotide sequence that causes the expression of an antibody to bind with human BMP-6, a bone morphogenetic protein linked to the expression of hepcidin, itself a key hormone involved in iron homeostasis. This treatment selectively binds with BMP-6 while minimally bonding with either BMP-5 or BMP-7, closely related proteins which are not associated with anemias of chronic disease.

Eli Lilly’s research and development goals extend into parasite control not only for humans but animals and plants as well. U.S. Patent No. 8889710, which is titled Parasiticidal Dihydroisoxazole Compounds, claims a dihydroisoxazole compound useful for controlling parasite infestations in both animals and agriculture; this treatment targets ectoparasites such as fleas, lice, ticks and mosquitos. This innovative compound was developed to provide effective long-term and safe control of parasites for companion animals like dogs and cats, as well as any plant part for agricultural uses.



Pfizer Focuses on Neurological Disorders, Also Invents Anti-Nicotine Vaccine


“Lyrica” by Acdx – Own work. Licensed under CC BY-SA 3.0 via Wikimedia Commons

Pfizer is the top drugmaker in the United States, but it too has been suffering from patent expirations which are expected to cost the company $3.5 billion during 2015. Along with patents that have already expired for Celebrex, Viagra and Lipitor, the company will also be faced with patent expirations related to Enbrel and Zyvox in the coming years. Pfizer has been active in regards to fighting generic painkillers that are being prescribed in Britain which infringe on the company’s intellectual properties in that area which are active until 2017. Interestingly, Pfizer is one company that has already determined that Chinese economic waters are too dangerous to navigate currently and the company announced at the beginning of April that it would cease commercial vaccine operations in China this year. According to Innography, Pfizer’s U.S. patent grants last year were double that of Eli Lilly’s at 90 patents.

Neurological disorders and neurodegenerative conditions were a big focus over at Pfizer to judge by a couple of patents that we spotted during our most recent survey. A compound useful for treating either Alzheimer’s disease or Down’s syndrome is featured by U.S. Patent No. 8916564, titled Substituted Pyrido[1,2-a]pyrazines for the Treatment of Neurodegenerative and Neurological Disorders. The bicyclic pyridinone that can modulate the production of peptides that can lead to the formation of neurological deposits of amyloid protein, a contributing factor of dementia. The treatment of human cognitive deficits is also the subject of U.S. Patent No. 8933095, issued under the title KAT II Inhibitors. This patent protects a compound that provides a bicyclic inhibitor of the KAT II enzyme, a brain enzyme important for the production of kynurenic acid. The reduction of kynurenic acid has shown the beneficial ability to improve cognitive processes impacted by neurological disorders.

A vaccine that can be strategically applied to prevent against cancers has been protected for Pfizer through the issue of U.S. Patent No. 8895017, entitled HER-2 Peptides and Vaccines. The patent claims an isolated immunogenic HER-2 peptide comprised of an extracellular domain-derived peptide with a specific amino acid sequence. The treatment targets tumors, especially those of the breast and ovaries, that over-express human epidermal growth factor receptor-2 (HER-2) by eliciting an immune response to the isolated immunogenic HER-2 peptide of the invention. Finally, we were also intrigued by the novel vaccine developed for the treatment of nicotine addiction which is outlined within U.S. Patent No. 8980276, titled Conjugates for the Prevention or Treatment of Nicotine Addiction. The patent protects a hapten-carrier conjugate derived from nicotine that serves as an antigenic component of an anti-nicotine vaccine. The invention enhances quit rates and smoking cessation rates in individuals who want to quit by reducing the amount of nicotine that can enter the brain; the invention can also prevent nicotine addiction from developing in non-smokers.


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