Pyrrolo[2,3-D]pyrimidine Derivatives: A Detailed Analysis of the Scope and Claims of United States Patent 9,035,074
Introduction
United States Patent 9,035,074, issued to Pfizer Inc., is a significant patent in the pharmaceutical industry, particularly in the realm of Janus Kinase (JAK) inhibitors. This patent, along with its associated claims and the broader patent landscape, is crucial for understanding the innovative contributions and the legal protections afforded to these compounds.
Background of the Invention
The patent describes pyrrolo[2,3-d]pyrimidine derivatives, which are pharmacologically active compounds designed to inhibit Janus Kinase (JAK) enzymes. JAK enzymes play a critical role in the signaling pathways of various cytokines and are implicated in several diseases, including autoimmune disorders, inflammatory conditions, and certain types of cancer[1][4].
Scope of the Patent
Chemical Structure and Synthesis
The patent outlines the chemical structure of the pyrrolo[2,3-d]pyrimidine derivatives, including various substituents and their configurations. These compounds are synthesized through specific methods, including chromatography on silica gel using a gradient of dichloromethane and methanol to purify the crude mixture of cis and trans isomers[1].
Pharmacological Use
The primary use of these derivatives is as JAK inhibitors, which makes them valuable for treating and preventing conditions mediated by JAK enzymes. These conditions include myositis, vasculitis, pemphigus, Crohn's disease, lupus, nephritis, psoriasis, multiple sclerosis, major depressive disorder, allergy, asthma, Sjogren's disease, dry eye syndrome, transplant rejection, cancer, inflammatory bowel disease, septic shock, cardiopulmonary dysfunction, acute respiratory disease, and cachexia[1].
Claims of the Patent
The patent includes several claims that define the scope of protection for the pyrrolo[2,3-d]pyrimidine derivatives:
Compound Claims
The patent claims specific chemical compounds with defined structures, including various substituents and configurations. These claims are detailed and specify the exact chemical formulae and structures of the compounds[1].
Pharmaceutical Compositions
The patent also claims pharmaceutical compositions that include these compounds along with a pharmaceutically acceptable carrier. This encompasses various formulations such as tablets, capsules, and solutions[1].
Methods of Treatment
Claims are made for methods of treating and preventing the aforementioned conditions by administering the pyrrolo[2,3-d]pyrimidine derivatives. These methods are tailored to the specific diseases and the dosages required for effective treatment[1].
Patent Landscape
Related Patents
Pfizer Inc. holds several related patents that also pertain to pyrrolo[2,3-d]pyrimidine derivatives as JAK inhibitors. These include U.S. Patents 9,545,405 and 9,549,929, all of which have the same expiration date of February 19, 2034. These patents collectively protect the intellectual property related to these compounds and their uses[5].
Patent Expiration and Exclusivity
The patent is set to expire on February 19, 2034. Additionally, the FDA has granted exclusivity periods for the drug product known as CIBINQO® (abrocitinib), which is based on these patents. The exclusivity periods include new patient population and new chemical entity exclusivities, which expire on February 9, 2026, and January 14, 2027, respectively[2][5].
Patent Term Extension
Pfizer Inc. has filed an application for a patent term extension under 35 U.S.C. 156, based on the FDA's approval of the NDA for CIBINQO®. This application is part of the process to extend the patent term due to the regulatory review period[2].
Metrics for Measuring Patent Scope
The scope of a patent can be measured using various metrics, such as independent claim length and independent claim count. These metrics are important in assessing the breadth and clarity of the patent claims. Narrower claims are often associated with a higher probability of grant and a shorter examination process, indicating better patent quality[3].
Impact on Innovation
The patent and its associated claims have significant implications for innovation in the pharmaceutical industry. By protecting the intellectual property related to these JAK inhibitors, Pfizer Inc. is incentivized to continue research and development in this area. However, overly broad or unclear claims can lead to increased licensing and litigation costs, potentially diminishing innovation[3].
Regulatory Review and Approval
The approval of CIBINQO® by the FDA is a critical aspect of the patent landscape. The regulatory review period and the subsequent approval process are factors in determining the eligibility for patent term extension. This ensures that the patent holder is compensated for the time spent in regulatory review[2].
Key Takeaways
- Chemical Structure and Synthesis: The patent describes specific pyrrolo[2,3-d]pyrimidine derivatives and their synthesis methods.
- Pharmacological Use: These compounds are used as JAK inhibitors for treating various autoimmune and inflammatory conditions.
- Claims: The patent includes claims for the compounds, pharmaceutical compositions, and methods of treatment.
- Patent Landscape: Related patents and exclusivity periods protect the intellectual property and market rights.
- Patent Expiration and Extension: The patent expires in 2034, with potential extensions based on regulatory review.
- Impact on Innovation: The patent's scope and clarity influence innovation and licensing costs in the pharmaceutical industry.
FAQs
What are the primary uses of the pyrrolo[2,3-d]pyrimidine derivatives described in U.S. Patent 9,035,074?
The primary uses are as Janus Kinase (JAK) inhibitors for treating conditions such as myositis, vasculitis, pemphigus, Crohn's disease, lupus, and others.
Who is the assignee of U.S. Patent 9,035,074?
The assignee is Pfizer Inc.
What is the expiration date of U.S. Patent 9,035,074?
The patent is set to expire on February 19, 2034.
Has a generic version of CIBINQO® been approved?
No, there is currently no therapeutically equivalent version of CIBINQO® available in the United States[5].
What metrics can be used to measure the scope of a patent?
Metrics such as independent claim length and independent claim count can be used to measure the scope and clarity of patent claims[3].
Sources
- United States Patent and Trademark Office. Pyrrolo[2,3-D]pyrimidine derivatives. US Patent 9,035,074 B2, issued May 19, 2015.
- Regulations.gov. Application for Patent Term Extension of U.S. Patent No. 9,035,074. Filed March 9, 2022.
- Hoover Institution. Patent Claims and Patent Scope. August 2016.
- Google Patents. Pyrrolo[2,3-D]pyrimidine derivatives. US Patent 9,035,074 B2.
- Drugs.com. Generic Cibinqo Availability. Updated November 6, 2024.
