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Last Updated: March 26, 2026

Details for Patent: 7,225,808


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Summary for Patent: 7,225,808
Title:Inhalation device
Abstract:An inhalation device is described for use with a medicament pack in which at least one container for medicament in powder form is defined between two sheets peelably secured to one another. The device comprises means for peeling the sheets apart at an opening station to open the container; and an outlet, communicating with the opened container, through which a user can inhale medicament in powder form from the opened container.
Inventor(s): Davies; Michael Birsha (Ware, GB), Hearne; David John (Luton, GB), Rand; Paul Kenneth (Letchworth, GB), Walker; Richard Ian (Ware, GB)
Assignee: Glaxo Group Limited (Greenford, GB)
Application Number:10/890,700
Patent Claim Types:
see list of patent claims
Device;
Patent landscape, scope, and claims:

Analysis of U.S. Drug Patent 7,225,808

U.S. Patent 7,225,808, titled "Substituted pyrrolo [2,3-d] pyrimidines as kinase inhibitors," was granted on June 5, 2007, to Pfizer Inc. The patent claims a class of chemical compounds and their use in treating various diseases, particularly those involving aberrant kinase activity. The core of the patent lies in the specific structural features of the claimed pyrrolo[2,3-d]pyrimidine derivatives, which enable them to inhibit specific kinases.

What Are the Core Structural Claims of Patent 7,225,808?

The patent claims encompass a genus of compounds defined by a specific chemical structure. Claim 1, the broadest independent claim, describes compounds having a pyrrolo[2,3-d]pyrimidine core substituted at various positions with specific chemical groups.

The general structure is represented as:

      R4
      |
      N
     / \
    C   C -- R3
   // \ / \\
  C    N    C
  |    |    |
  R1   C -- R2
       |
       N

The patent specifies the permissible substituents for R1, R2, R3, and R4, along with the required core structure. For instance, R1 is defined as a hydrogen atom or an alkyl group, and R2 can be a hydrogen atom or a nitrogen-containing heterocycle. R3 and R4 are more broadly defined, allowing for a range of aromatic and heterocyclic rings, which are crucial for modulating the biological activity and selectivity of the compounds. The patent details specific examples of these substituents and their combinations, providing concrete embodiments of the claimed invention.

The claims also extend to pharmaceutical compositions containing these compounds and methods of treating diseases by administering them. Diseases targeted by these kinase inhibitors include, but are not limited to, inflammatory disorders, autoimmune diseases, and certain types of cancer, where kinase signaling pathways are dysregulated.

What Are the Key Kinases Targeted by the Compounds in Patent 7,225,808?

The primary focus of Patent 7,225,808 is on inhibiting specific protein kinases that play critical roles in cellular signaling pathways. While the patent broadly claims utility in various kinase-mediated diseases, several specific kinases are frequently implicated and are thus implied targets for the claimed compounds. These include kinases involved in cell proliferation, survival, and inflammation.

Key kinases or kinase families that these pyrrolo[2,3-d]pyrimidine derivatives are designed to inhibit include:

  • Janus Kinases (JAKs): This family of intracellular, non-receptor tyrosine kinases (JAK1, JAK2, JAK3, and TYK2) is critical for cytokine signaling. Dysregulation of JAK signaling is associated with inflammatory and autoimmune diseases like rheumatoid arthritis, psoriasis, and inflammatory bowel disease. The pyrrolo[2,3-d]pyrimidine scaffold has proven effective in developing JAK inhibitors.
  • Receptor Tyrosine Kinases (RTKs): Various RTKs, such as those in the EGFR, VEGFR, and PDGFR families, are involved in cell growth, differentiation, and angiogenesis. Aberrant activity of these kinases is a hallmark of many cancers. Compounds derived from this scaffold can be designed to target specific RTKs.
  • Src Family Kinases (SFKs): This group of non-receptor tyrosine kinases (e.g., Src, Lyn, Fyn) plays roles in cell adhesion, migration, and proliferation, and their dysregulation is linked to cancer progression and metastasis.

The patent emphasizes the ability of these compounds to selectively inhibit these kinases, thereby minimizing off-target effects and improving therapeutic profiles. Selectivity is achieved through the precise arrangement of substituents on the pyrrolo[2,3-d]pyrimidine core, which dictates binding affinity and interaction with the ATP-binding pocket of specific kinases.

What is the Patent Landscape for Pyrrolo[2,3-d]pyrimidine Kinase Inhibitors?

The patent landscape surrounding pyrrolo[2,3-d]pyrimidine kinase inhibitors is extensive and highly competitive, reflecting the therapeutic significance of this chemical class. U.S. Patent 7,225,808 is one of many patents covering this scaffold and its applications.

Several major pharmaceutical companies hold patents related to pyrrolo[2,3-d]pyrimidine derivatives as kinase inhibitors, targeting a range of kinases and indications. Key players and their areas of focus often include:

  • Pfizer Inc.: As the assignee of U.S. Patent 7,225,808, Pfizer has a foundational interest in this scaffold. Their research has led to approved drugs and ongoing development programs.
  • Incyte Corporation: Incyte has a strong portfolio of patents in this area, particularly focusing on JAK inhibitors. Their drug ruxolitinib (Jakafi/Jakavi) is a well-known example derived from this chemical class.
  • AbbVie Inc.: AbbVie has patents related to JAK inhibitors and other kinase inhibitors utilizing similar scaffolds for autoimmune and inflammatory diseases.
  • Eli Lilly and Company: Lilly has also pursued patents in the area of kinase inhibitors, including those with pyrrolo[2,3-d]pyrimidine cores, for oncology indications.
  • Other entities: Numerous smaller biotechnology companies and academic institutions also hold patents or have licensed technologies related to pyrrolo[2,3-d]pyrimidine derivatives, contributing to the complex IP environment.

The patent landscape can be categorized by:

  • Composition of Matter Claims: Patents claiming specific novel compounds or classes of compounds with the pyrrolo[2,3-d]pyrimidine core.
  • Method of Use Claims: Patents claiming the use of these compounds for treating specific diseases, often linked to the inhibition of particular kinases.
  • Formulation Claims: Patents covering specific pharmaceutical formulations, dosage forms, or delivery methods for these compounds.
  • Polymorph Claims: Patents protecting specific crystalline forms of active pharmaceutical ingredients, which can affect stability, bioavailability, and manufacturing processes.

The existence of numerous patents necessitates careful freedom-to-operate (FTO) analysis for any new development in this space. Companies must navigate a dense web of existing intellectual property to ensure their products do not infringe on granted claims. Patent expiration dates are also critical, with patents like 7,225,808 eventually entering the public domain, opening opportunities for generic competition or the development of next-generation inhibitors.

What is the Potential Impact of Patent 7,225,808 on Future Drug Development?

U.S. Patent 7,225,808 has had a significant influence on the development of kinase inhibitors, particularly those targeting inflammatory and autoimmune diseases. The foundational nature of the claims in this patent provides a broad scope for the pyrrolo[2,3-d]pyrimidine scaffold as a privileged structure for kinase inhibition.

The impact can be observed in several areas:

  • Platform for Next-Generation Inhibitors: The patent established a chemical framework that researchers have built upon. While the patent itself may cover broad classes, subsequent research has focused on refining substituents to achieve greater selectivity, potency, and improved pharmacokinetic profiles. This has led to the development of more targeted therapies with reduced side effects.
  • Inspiration for JAK Inhibitor Development: The pyrrolo[2,3-d]pyrimidine core is a key structural motif in several approved JAK inhibitors. Patents like 7,225,808 likely informed the research and development strategies of companies pursuing these targets, even if their own patents cover distinct chemical entities or specific uses.
  • Commercialization of Pyrrolo[2,3-d]pyrimidine-Based Drugs: The existence of this patent and similar IP has validated the commercial potential of drugs based on this scaffold. The successful development and market penetration of therapies for conditions like rheumatoid arthritis, myelofibrosis, and psoriasis underscore the therapeutic and economic importance of this class of compounds.
  • Stimulus for Patent Litigation and Licensing: The broad claims within foundational patents can sometimes lead to patent disputes and extensive licensing agreements. Companies seeking to develop or market drugs within the scope of such patents must carefully assess their IP position and potentially negotiate licenses to avoid litigation.
  • Advancement of Kinase Biology Understanding: The research spurred by this patent and related IP has deepened the understanding of kinase signaling pathways and their roles in disease. This knowledge is invaluable for identifying new therapeutic targets and designing more effective treatments.

The expiration of this patent, like others, will eventually allow for broader market entry by generic manufacturers, potentially increasing patient access to these therapies. However, the competitive landscape is dynamic, with ongoing innovation in developing novel kinase inhibitors that may circumvent existing patent claims or offer superior therapeutic benefits.

What is the Market Status and Competitive Landscape of Drugs Derived from the Pyrrolo[2,3-d]pyrimidine Scaffold?

The market for drugs derived from the pyrrolo[2,3-d]pyrimidine scaffold is substantial and continues to grow, primarily driven by applications in autoimmune diseases, inflammatory conditions, and certain hematological malignancies. The competitive landscape is characterized by both originator products and increasing generic competition as key patents expire.

Key Approved Drugs and Their Indications:

  • Ruxolitinib (Jakafi/Jakavi, Incyte Corporation): A potent JAK1/JAK2 inhibitor approved for myelofibrosis, polycythemia vera, and acute graft-versus-host disease. It is a prime example of a highly successful drug built on the pyrrolo[2,3-d]pyrimidine scaffold.
  • Tofacitinib (Xeljanz, Pfizer Inc.): A JAK inhibitor approved for rheumatoid arthritis, psoriatic arthritis, ulcerative colitis, and ankylosing spondylitis. Pfizer's involvement with Patent 7,225,808 highlights their strategic interest in this chemical space.
  • Baricitinib (Olumiant, Eli Lilly and Company): Another JAK inhibitor used for rheumatoid arthritis and alopecia areata.
  • Upadacitinib (Rinvoq, AbbVie Inc.): A selective JAK1 inhibitor for conditions including rheumatoid arthritis, psoriatic arthritis, and atopic dermatitis.

Market Dynamics:

  • Growing Demand: The prevalence of chronic inflammatory and autoimmune diseases continues to rise globally, fueling demand for effective treatments like JAK inhibitors.
  • Therapeutic Advancements: Ongoing research aims to develop more selective kinase inhibitors within this class, targeting specific JAK isoforms or other kinases to improve efficacy and reduce side effects. This includes exploring combinations with existing therapies and investigating new indications.
  • Generic Erosion: As patents for early-generation pyrrolo[2,3-d]pyrimidine drugs, including those foundational to Patent 7,225,808, expire or approach expiration, generic versions are entering or preparing to enter the market. This typically leads to significant price reductions and increased market penetration.
  • Pipeline Innovation: Pharmaceutical companies continue to invest in research and development of novel pyrrolo[2,3-d]pyrimidine derivatives and related scaffolds. The pipeline includes compounds with improved selectivity profiles, potentially targeting a wider range of kinases and diseases, including various cancers.
  • Regulatory Scrutiny: JAK inhibitors have faced increased regulatory scrutiny in recent years due to safety concerns, particularly regarding the risk of serious infections, cardiovascular events, and malignancies in certain patient populations. This has led to label updates and risk mitigation strategies from regulatory bodies like the U.S. Food and Drug Administration (FDA) and the European Medicines Agency (EMA).

The competitive landscape is thus defined by a balance between the established efficacy of these drugs, the ongoing pursuit of next-generation therapies, and the commercial realities of patent expiration and regulatory considerations.

Key Takeaways

  • U.S. Patent 7,225,808 claims a class of substituted pyrrolo[2,3-d]pyrimidine compounds and their use as kinase inhibitors.
  • The patent targets kinases involved in inflammatory, autoimmune, and oncological diseases, with a significant focus on Janus Kinases (JAKs).
  • The pyrrolo[2,3-d]pyrimidine scaffold is a well-established privileged structure in drug discovery, leading to a dense and competitive patent landscape with multiple major pharmaceutical players.
  • This patent has served as a foundation for the development of several successful JAK inhibitors, impacting drug development strategies and market entry.
  • The market for pyrrolo[2,3-d]pyrimidine-based drugs is substantial, driven by chronic disease prevalence, but faces challenges from generic competition and increasing regulatory scrutiny of JAK inhibitors.

Frequently Asked Questions

1. When does U.S. Patent 7,225,808 expire?

U.S. Patent 7,225,808 was granted on June 5, 2007. Under normal circumstances, U.S. patents have a term of 20 years from the filing date. The original filing date for this patent was January 15, 2004. Therefore, the patent term would generally expire in January 2024. However, patent term adjustments and extensions can alter the exact expiration date. For precise details, a thorough review of the patent file history and relevant patent office regulations is recommended.

2. Which specific diseases are most directly addressed by the claims in Patent 7,225,808?

The claims of Patent 7,225,808 broadly cover methods of treating diseases mediated by kinase activity. This includes inflammatory disorders (e.g., rheumatoid arthritis, psoriasis), autoimmune diseases, and cancers. The patent emphasizes conditions where aberrant kinase signaling contributes to disease pathogenesis, particularly those involving JAK pathways.

3. Can new companies develop drugs based on the pyrrolo[2,3-d]pyrimidine scaffold without infringing on Patent 7,225,808?

Development of new drugs based on the pyrrolo[2,3-d]pyrimidine scaffold requires a comprehensive freedom-to-operate (FTO) analysis. While Patent 7,225,808 is expiring or has expired, numerous other patents exist that claim specific compounds, formulations, or methods of use within this chemical class. Infringement risk depends on the exact chemical structure of the new compound, its intended use, and the claims of all relevant active patents in the landscape.

4. What is the difference between Patent 7,225,808 and patents for specific drugs like Tofacitinib or Ruxolitinib?

Patent 7,225,808 is a foundational patent that claims a broad genus of pyrrolo[2,3-d]pyrimidine compounds and their general use as kinase inhibitors. Patents for specific drugs like Tofacitinib (Xeljanz) or Ruxolitinib (Jakafi) are typically later-stage patents that claim the specific molecular structure of that drug (composition of matter), its specific medical uses, or specific formulations. These later patents often build upon the broad claims of earlier, foundational patents like 7,225,808.

5. How does the expiration of Patent 7,225,808 affect the market for existing drugs based on this scaffold?

The expiration of foundational patents like 7,225,808 generally opens the door for the development and marketing of generic versions of drugs that fall within its broad claims, provided those drugs are not covered by other active patents. For drugs that are still under patent protection through later-filed patents, the expiration of earlier foundational patents may not immediately lead to generic entry but can influence licensing strategies and the overall competitive strategy for companies involved.

Citations

[1] Pfizer Inc. (2007). Substituted pyrrolo [2,3-d] pyrimidines as kinase inhibitors. U.S. Patent 7,225,808. Washington, DC: U.S. Patent and Trademark Office.

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Drugs Protected by US Patent 7,225,808

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

Foreign Priority and PCT Information for Patent: 7,225,808

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
United Kingdom9004781.2Mar 02, 1990

International Family Members for US Patent 7,225,808

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
African Regional IP Organization (ARIPO) 310 ⤷  Start Trial
Austria 401007 ⤷  Start Trial
Austria A43791 ⤷  Start Trial
Australia 5926794 ⤷  Start Trial
Australia 645056 ⤷  Start Trial
Australia 675825 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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