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Patent landscape, scope, and claims: |
United States Patent 7,157,584: Scope, Claims, and Landscape Analysis
US Patent 7,157,584, titled "Substituted Pyrrolo[2,3-d]pyrimidines," issued on January 2, 2007, to Pfizer Inc. The patent claims a class of compounds and their use in treating kinase-mediated disorders. The asserted compounds are generally substituted pyrrolo[2,3-d]pyrimidine derivatives.
What Is the Core Invention Claimed in US Patent 7,157,584?
The primary invention claimed by US Patent 7,157,584 is a genus of chemical compounds characterized by a specific pyrrolo[2,3-d]pyrimidine core structure with defined substitution patterns. These compounds are identified by Markush claims, defining broad structural variations that fall under the patent's protection.
The patent asserts claims covering:
- Compound Structures: The claims define a central pyrrolo[2,3-d]pyrimidine ring system. Specific substituents are attached at various positions of this core, including positions 1, 3, 4, 5, 6, and 7. These substituents, denoted by R groups (e.g., R1, R2, R3, R4, R5, R6, R7), are themselves defined by specific chemical functionalities such as alkyl, aryl, heteroaryl, amino, alkoxy, and halogen groups, among others.
- Pharmaceutical Compositions: The patent also claims pharmaceutical compositions containing at least one of the claimed compounds and a pharmaceutically acceptable carrier, diluent, or excipient.
- Methods of Treatment: The claims encompass methods of treating or preventing a disease or condition mediated by a protein kinase, comprising administering an effective amount of a claimed compound to a subject in need thereof. The patent explicitly identifies certain kinases as targets.
The patent's claims are structured to protect not only the specific exemplified compounds but also a broad chemical space of related molecules with potential therapeutic activity.
What Specific Chemical Entities Are Protected?
The patent defines a broad scope of chemical structures. The central feature is the pyrrolo[2,3-d]pyrimidine bicyclic system. Key positions on this core are substituted.
Claim 1, the broadest independent compound claim, defines the general structure as:
A compound of formula (I):
R6
|
N---C---R7
// \
C N
/ \ //
R5 C---C---R4
|| |
C-----N
/ \ /
R1 C=N
/ \
R2 R3
Where:
- The pyrrolo[2,3-d]pyrimidine core is as shown.
- R1 is selected from H, alkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, CONR8R9, SO2NR8R9, NR8R9, OR10, SR10, NO2, CN, C(O)R10, C(O)NR8R9, C(O)OR10, C(S)NR8R9, C(S)OR10, C(S)R10.
- R2 is selected from H, alkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl.
- R3 is selected from H, alkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, CONR8R9, SO2NR8R9, NR8R9, OR10, SR10, NO2, CN, C(O)R10, C(O)NR8R9, C(O)OR10, C(S)NR8R9, C(S)OR10, C(S)R10.
- R4 is selected from H, alkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, CONR8R9, SO2NR8R9, NR8R9, OR10, SR10, NO2, CN, C(O)R10, C(O)NR8R9, C(O)OR10, C(S)NR8R9, C(S)OR10, C(S)R10.
- R5 is selected from H, alkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl.
- R6 is selected from H, alkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, CONR8R9, SO2NR8R9, NR8R9, OR10, SR10, NO2, CN, C(O)R10, C(O)NR8R9, C(O)OR10, C(S)NR8R9, C(S)OR10, C(S)R10.
- R7 is selected from H, alkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl.
- R8 and R9 are independently selected from H, alkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl.
- R10 is selected from alkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl.
The patent then narrows this definition with dependent claims, specifying particular combinations of R groups or further defining the scope of R1, R4, and R6. For example, Claim 2 specifies R4 as an aryl or heteroaryl group, and Claim 3 specifies R1 as an amino group.
The patent exemplifies specific compounds, such as (S)-3-(4-amino-1H-pyrrolo[2,3-d]pyrimidin-5-yl)-N-(2-chloro-5-methoxyphenyl)-2-methylpropanamide, a compound that has been associated with research into JAK inhibitors.
What Therapeutic Areas and Kinases Are Targeted?
US Patent 7,157,584 broadly claims therapeutic applications for kinase-mediated disorders. The patent outlines specific kinases of interest and related disease states.
The targeted therapeutic areas include:
- Inflammatory Diseases: Conditions such as rheumatoid arthritis, asthma, inflammatory bowel disease, psoriasis, and allergic rhinitis.
- Autoimmune Diseases: Conditions where the immune system attacks healthy tissues, including lupus and multiple sclerosis.
- Oncological Conditions: Cancers that are driven by aberrant kinase activity.
- Proliferative Disorders: Conditions characterized by uncontrolled cell growth.
- Cardiovascular Diseases: Certain heart conditions influenced by kinase signaling.
The patent explicitly mentions targeting protein kinases, particularly those in the Janus Kinase (JAK) family. The JAK family, consisting of JAK1, JAK2, JAK3, and TYK2, plays a critical role in signaling pathways that regulate immune responses and cell growth. By inhibiting these kinases, the compounds are intended to modulate downstream cellular processes involved in the pathogenesis of the claimed diseases.
What Is the Dominant Patent Holder for This Technology?
Pfizer Inc. is the assignee and applicant of US Patent 7,157,584. As the patent holder, Pfizer holds the exclusive rights to make, use, sell, and import the claimed inventions within the United States during the patent's term.
The patent landscape surrounding pyrrolo[2,3-d]pyrimidine derivatives, particularly those targeting kinase pathways, is characterized by extensive research and development from multiple pharmaceutical companies. While Pfizer holds this specific patent, other entities have filed and been granted patents on similar or related chemical structures and their applications.
Key entities active in this space include, but are not limited to:
- Incyte Corporation: Known for its development of JAK inhibitors, such as ruxolitinib.
- Gilead Sciences, Inc.: Has a portfolio of kinase inhibitors, including those targeting JAK pathways.
- AbbVie Inc.: Also a significant player in the immunology and oncology space with kinase inhibitor research.
- Novartis AG: Has research programs and patents related to kinase inhibitors for various therapeutic areas.
The competitive landscape involves companies developing novel compounds within this chemical class, as well as those seeking to design around existing patents, leading to a dense and active patent environment.
How Does This Patent Interact with Other Patents in the Field?
US Patent 7,157,584 exists within a broader patent landscape of kinase inhibitors, particularly those based on pyrrolo[2,3-d]pyrimidine scaffolds. Its interaction with other patents depends on the specific claims and the subject matter of those other patents.
Potential interactions include:
- Freedom-to-Operate (FTO) Concerns: Competitors developing new compounds or therapies within the pyrrolo[2,3-d]pyrimidine space must conduct FTO analyses to ensure their activities do not infringe on the claims of US Patent 7,157,584 or other related patents.
- Design Around Strategies: Companies may develop structurally distinct compounds that achieve similar therapeutic outcomes but fall outside the precise claim scope of this patent. This involves careful analysis of the patent's claim limitations.
- Licensing Agreements: Pfizer could license its patent rights to other entities for specific fields of use or geographical territories, creating revenue streams and collaborative development opportunities.
- Patent Expiration and Generic Competition: As the patent approaches its expiration date (January 2, 2024, considering its original filing date and any potential patent term extensions), generic manufacturers may prepare to launch their own versions of drugs covered by the patent, provided they can navigate any other active patents.
- Prior Art and Validity Challenges: The patent's validity could be challenged based on prior art that was not considered during examination. This is a common feature of competitive patent landscapes.
- Divisional and Continuation Applications: The patent family might include divisional or continuation applications that claim subject matter related to the original filing but with different claim scopes or filing dates, extending the potential period of protection.
The patent's claims, particularly the broad Markush definitions, are designed to capture a significant portion of the chemical space. However, the precise boundaries are defined by the wording of each claim and their interpretation in the context of patent law.
What Are the Key Dates for This Patent?
Understanding the timeline of US Patent 7,157,584 is crucial for assessing its current validity and commercial impact.
Key dates associated with US Patent 7,157,584:
- Filing Date: March 28, 2002
- Publication Date: October 2, 2006
- Issue Date: January 2, 2007
- Expiration Date: January 2, 2024 (This is based on the standard 20-year term from the filing date, without considering potential Patent Term Adjustments (PTA) or Patent Term Extensions (PTE). PTE may have been applied for and granted, potentially extending the effective expiry. A definitive determination of the actual legal expiry would require checking USPTO records for any granted PTE.)
The expiration date signifies when the patent rights granted by the U.S. Patent and Trademark Office (USPTO) cease to be enforceable. After this date, the claimed technology may enter the public domain, allowing for generic competition or wider research and development without infringing this specific patent.
Key Takeaways
US Patent 7,157,584 protects a broad class of substituted pyrrolo[2,3-d]pyrimidine compounds and their use in treating kinase-mediated disorders, including inflammatory, autoimmune, and oncological conditions. Pfizer Inc. is the assignee. The patent claims defined compound structures, pharmaceutical compositions, and methods of treatment targeting kinases, notably the JAK family. The patent's broad Markush claims define a significant chemical space, requiring careful freedom-to-operate analysis for competitors. The patent's original expiration date was January 2, 2024, after which the technology may become publicly available, subject to any granted Patent Term Extensions.
Frequently Asked Questions
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Does US Patent 7,157,584 cover all JAK inhibitors?
No, the patent covers specific substituted pyrrolo[2,3-d]pyrimidine compounds as defined by its claims. It does not broadly cover all compounds that inhibit JAK kinases, which are developed and patented by various entities with different chemical scaffolds and claim scopes.
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When did the protection period for US Patent 7,157,584 end?
The patent's original expiration date was January 2, 2024. However, the effective legal expiration date could be later if Patent Term Extension (PTE) was granted by the USPTO to compensate for regulatory review delays.
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What is the significance of the Markush claims in this patent?
Markush claims are used to define a genus of compounds by specifying a common structural framework with variable substituents. This allows the patent to protect a broad range of related chemical entities, rather than just specific exemplified molecules.
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Can a generic version of a drug disclosed in US Patent 7,157,584 be sold now?
Generic sales are possible only after the patent expires and if no other active patents (e.g., patents covering the specific drug product, formulation, or manufacturing process) block market entry. The primary compound patent (7,157,584) expired in early 2024, but other patents might still be in force.
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Who is actively developing drugs in the pyrrolo[2,3-d]pyrimidine space?
Numerous pharmaceutical companies are active in this area, including but not limited to Incyte Corporation, Gilead Sciences, Inc., AbbVie Inc., and Novartis AG, in addition to Pfizer Inc.
Citations
[1] Pfizer Inc. (2007). United States Patent 7,157,584: Substituted pyrrolo[2,3-d]pyrimidines. U.S. Patent and Trademark Office. Retrieved from [USPTO Patent Full-Text and Image Database]
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