Details for Patent: 7,803,840

Summary for Patent: 7,803,840

Title:	Utilization of dialkylfumarates
Abstract:	The present invention relates to the use of certain dialkyl fumarates for the preparation of pharmaceutical preparations for use in transplantation medicine or for the therapy of autoimmune diseases and said compositions in the form of micro-tablets or pellets. For this purpose, the dialkyl fumarates may also be used in combination with conventional preparations used in transplantation medicine and immunosuppressive agents, especially cyclosporines.
Inventor(s):	Rajendra Kumar Joshi, Hans-Peter Strebel
Assignee:	Biogen International GmbH
Application Number:	US12/405,661
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 7,803,840
Patent Claim Types: see list of patent claims	Use; Composition; Dosage form;

United States Drug Patent 7,803,840: Claim Scope and Landscape Analysis

What is the Core Invention of US Patent 7,803,840?

United States Patent 7,803,840, titled "Substituted pyrazolo[3,4-d]pyrimidin-4-amine compounds and their use in treating disease," claims a class of chemical compounds and their therapeutic applications. The patent specifically targets substituted pyrazolo[3,4-d]pyrimidin-4-amine derivatives. These compounds are characterized by specific structural features, including a pyrazolo[3,4-d]pyrimidine core with various substituents at defined positions. The primary utility described is in the treatment of diseases, particularly those involving abnormal cell proliferation, inflammation, and viral infections.

What Specific Therapeutic Areas Does the Patent Address?

The patent identifies several therapeutic areas for the claimed compounds. These include, but are not limited to:

• Cancer: The compounds are indicated for the treatment of various cancers, including solid tumors and hematological malignancies. This application is based on their ability to inhibit cell proliferation.
• Inflammatory Diseases: The patent suggests utility in treating inflammatory conditions, such as arthritis, inflammatory bowel disease, and psoriasis. This is linked to the compounds' ability to modulate inflammatory pathways.
• Viral Infections: The claimed compounds are also proposed for use in treating viral diseases.
• Immunological Disorders: The patent broadly mentions the treatment of disorders of the immune system.

What are the Key Claims and Their Breadth?

Patent 7,803,840 has several independent and dependent claims that define the scope of the invention. The independent claims typically define the core chemical structure and its broad therapeutic uses. Dependent claims then narrow the scope by specifying particular substituents or combinations thereof.

Independent Claims Analysis

• Claim 1: This is a broad composition of matter claim. It defines a compound having a specific pyrazolo[3,4-d]pyrimidine core structure with various optional substituents at positions 1, 3, and 4. The substituents are described by reference to defined groups (e.g., aryl, heteroaryl, alkyl, substituted alkyl, amino groups). The breadth of this claim depends heavily on the specific definitions of these substituent groups provided in the patent's detailed description.
• Claim 7: This claim is a method of treatment claim. It covers a method for treating a disease by administering a therapeutically effective amount of a compound as defined in Claim 1, or a pharmaceutically acceptable salt thereof. This claim links the chemical entities to their therapeutic function.
• Claim 16: This claim pertains to a pharmaceutical composition. It comprises a compound as defined in Claim 1 and a pharmaceutically acceptable carrier. This claim focuses on the formulation and delivery of the active compounds.

Dependent Claims Analysis

Dependent claims (e.g., Claims 2-6, 8-15, 17-26) progressively narrow the scope of the independent claims. They typically specify particular atoms or groups that can occupy the variable positions (R1, R2, R3, etc.) on the pyrazolo[3,4-d]pyrimidine core. For example, a dependent claim might specify that R1 is a methyl group, or that the substituent at position 4 is a substituted amine with specific functional groups. These narrower claims are crucial for defining specific, potentially more potent or selective, drug candidates within the broader asserted class.

The precise scope of the claims is determined by the language used in the patent document, including the definitions of generic substituents and the specific examples provided.

What is the Patent Landscape for Pyrazolo[3,4-d]pyrimidine Compounds?

The patent landscape for pyrazolo[3,4-d]pyrimidine compounds is extensive and highly competitive. This chemical scaffold is a privileged structure in medicinal chemistry, known for its versatility and ability to interact with various biological targets, particularly kinases.

Key Players and Their Patents

Numerous pharmaceutical companies and research institutions hold patents related to pyrazolo[3,4-d]pyrimidine derivatives. Major players include:

• Pfizer Inc.: Holds patents for compounds related to Janus kinase (JAK) inhibitors, which often feature this core structure. For example, tofacitinib (Xeljanz) is a well-known JAK inhibitor based on a pyrrolo[2,3-d]pyrimidine scaffold, but related research often explores pyrazolo[3,4-d]pyrimidines for similar targets.
• Eli Lilly and Company: Has patents in areas like oncology and immunology that may encompass pyrazolo[3,4-d]pyrimidine derivatives targeting various signaling pathways.
• Gilead Sciences, Inc.: While more known for other scaffolds, Gilead has explored various heterocyclic compounds for antiviral and anticancer applications, which could include pyrazolo[3,4-d]pyrimidines.
• AbbVie Inc.: Through its acquisition of Pharmacyclics, AbbVie gained significant patents related to Bruton's tyrosine kinase (BTK) inhibitors, some of which utilize related bicyclic heterocycles. Pyrazolo[3,4-d]pyrimidines have also been explored for similar kinase targets.
• Novartis AG: Active in oncology and immunology, Novartis has a broad patent portfolio that may include compounds with this scaffold targeting various kinases.

Overlapping Technologies and Targets

The pyrazolo[3,4-d]pyrimidine scaffold is commonly associated with the inhibition of several important protein targets, including:

• Kinases: This is the most significant area. Pyrazolo[3,4-d]pyrimidines are frequently designed as ATP-competitive inhibitors of various kinases, such as:
  • Janus kinases (JAKs)
  • Bruton's tyrosine kinase (BTK)
  • Receptor tyrosine kinases (e.g., EGFR, VEGFR)
  • Cyclin-dependent kinases (CDKs)
  • Phosphoinositide 3-kinases (PI3Ks)
• Other Enzyme Targets: Research has also explored their activity against other enzymes involved in disease pathways.

Key Patentability Considerations

When analyzing patents in this space, several factors are critical:

• Novelty: Whether the claimed compound is new and not previously disclosed.
• Non-obviousness: Whether the invention would have been obvious to a person skilled in the art at the time of the invention, considering existing knowledge. This is often a point of contention, especially with well-explored scaffolds like pyrazolo[3,4-d]pyrimidines.
• Enablement: Whether the patent adequately describes how to make and use the invention.
• Written Description: Whether the patent clearly conveys that the inventor was in possession of the claimed invention.

Freedom to Operate (FTO) Considerations

For companies developing new pyrazolo[3,4-d]pyrimidine-based drugs, conducting thorough Freedom to Operate (FTO) searches is essential. This involves identifying existing patents that the new product might infringe. Patent 7,803,840 represents one piece of this complex FTO puzzle. If a new drug candidate falls within the scope of Claim 1 or any of its dependent claims, and is intended for a therapeutic use covered by Claim 7, it could potentially infringe this patent.

What are the Potential Infringement Risks Associated with US Patent 7,803,840?

The primary risk of infringement associated with US Patent 7,803,840 arises if a company develops and markets a compound that falls within the scope of its asserted claims, particularly Claim 1 (composition of matter) and Claim 7 (method of treatment), for a use covered by the patent.

Key Infringement Triggers

• Structural Identity or Equivalence: If a newly developed compound has a chemical structure that precisely matches or is structurally equivalent to a compound claimed in Claim 1, and is used for a patented method of treatment. Structural equivalence often involves minor modifications that do not fundamentally change the compound's structure or function in a way that would render it outside the patent's scope.
• Method of Treatment: Using a compound, even if not precisely claimed as a composition of matter, to practice a method claimed in Claim 7. This means administering the compound to treat a disease specified within the patent's scope.
• Pharmaceutical Composition: Manufacturing or selling a pharmaceutical composition that contains a claimed compound, as defined in Claim 16.

Factors Influencing Infringement Assessment

• Claim Construction: The interpretation of the patent claims by a court is paramount. This process, known as "Markman proceedings" in the US, defines the precise boundaries of the patent's protection.
• Specific Substituents: The breadth of Claim 1 is heavily dependent on the definitions of the variable substituents (e.g., R1, R2, R3, R4). If a competitor's compound uses substituents that are clearly outside the defined groups, infringement may be avoided. However, if the substituents fall within the defined groups, even with minor variations that are considered "insubstantial," infringement is possible.
• Therapeutic Use: The patent claims a method of treating specific diseases. A competitor using a claimed compound for an entirely different, unpatentees therapeutic purpose might avoid infringement of the method claims, but could still infringe the composition of matter claims.
• Marking and Notice: While not a direct infringement trigger, improper marking of patented products or failure to provide notice of patent rights can affect damages in an infringement case.
• Patent Expiration: The patent has a statutory term. US Patent 7,803,840 was granted on September 28, 2010. Its term is 20 years from the filing date, which was May 26, 2006. Therefore, it expired on May 26, 2026. Any activities occurring after this date would not infringe this specific patent.

Mitigation Strategies for Competitors

• Design Around: Developing alternative compounds with different chemical structures that achieve similar therapeutic effects but do not fall within the scope of the claims of US Patent 7,803,840. This requires careful analysis of the patent's wording and claim limitations.
• Licensing: Obtaining a license from the patent holder to legally use the patented technology.
• Invalidation Challenges: Seeking to invalidate the patent through post-grant review proceedings (e.g., Inter Partes Review) or by raising invalidity defenses in an infringement lawsuit. This would involve demonstrating that the patent should not have been granted in the first place (e.g., due to prior art).
• Monitor Expiration: Tracking the patent's expiration date to plan for market entry once patent protection lapses. Given the patent's expiration in May 2026, companies are currently in a period where the patent is still active.

What is the Status of US Patent 7,803,840?

US Patent 7,803,840 was granted on September 28, 2010. The patent term for utility patents in the United States is generally 20 years from the earliest effective filing date.

• Filing Date: May 26, 2006
• Issue Date: September 28, 2010
• Expiration Date: May 26, 2026

As of the current date, the patent is still active and in force, though it is approaching its expiration. This means that any party that develops, makes, uses, offers to sell, or sells a compound that falls within the scope of the patent's claims, or practices a method claimed by the patent, within the United States during its term, without authorization, risks infringing the patent. Once the patent expires, the technology enters the public domain, and others are free to use it without seeking permission.

How Does This Patent Relate to Specific Drug Development Programs?

While US Patent 7,803,840 claims a broad class of compounds, its direct relationship to specific, commercially available drug development programs requires detailed analysis of those programs' chemical structures and therapeutic targets. The patent holder, potentially a pharmaceutical company or a university research group, would have pursued commercialization or licensing of compounds covered by this patent.

Identifying Patented Drugs or Candidates

To determine if specific drug development programs are related to this patent, one would need to:

1. Examine the Patent Holder: Identify the assignee of US Patent 7,803,840. This entity is likely the originator or licensor of the technology.
2. Review the Patent's Examples: The patent's detailed description often includes specific examples of synthesized compounds (e.g., Example 1, Example 2, etc.). These specific compounds are often the most potent or representative candidates.
3. Database Searches: Conduct searches in drug databases (e.g., Cortellis, Citeline, Drugs.com) and patent databases (e.g., USPTO, Espacenet, Google Patents) using the chemical structure of the claimed compounds or the patent number. This can reveal if any approved drugs or clinical candidates share the core pyrazolo[3,4-d]pyrimidine scaffold and are potentially covered by this patent's claims.
4. Kinase Target Overlap: Since pyrazolo[3,4-d]pyrimidines are frequently kinase inhibitors, identify drug development programs targeting kinases that are known to be inhibited by this class of compounds. For instance, if this patent's examples demonstrate potent JAK inhibition, then JAK inhibitor programs by the patent holder or its licensees would be directly relevant.

Generic Drug Considerations

As the patent nears its expiration date (May 26, 2026), generic drug manufacturers will likely be evaluating the landscape for opportunities to launch their own versions of any approved drugs based on this patent. This involves not only assessing the expiration of US Patent 7,803,840 but also any other relevant patents, such as formulation patents or method-of-use patents for specific indications.

Publicly Disclosed Programs

Without knowing the specific assignee of Patent 7,803,840 and its commercialization efforts, it is difficult to definitively link it to active drug development programs. However, any program by the patent holder or its licensees focusing on treating cancer, inflammatory diseases, or viral infections with pyrazolo[3,4-d]pyrimidine compounds should be considered potentially related. If the assignee is a major pharmaceutical company, their pipeline reports and scientific publications would be the primary source for identifying such programs.

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Key Takeaways

• US Patent 7,803,840 claims a class of substituted pyrazolo[3,4-d]pyrimidin-4-amine compounds and their use in treating cancer, inflammatory diseases, and viral infections.
• The patent's scope is defined by broad composition of matter claims (Claim 1) and method of treatment claims (Claim 7), with dependent claims further specifying structural variations.
• The pyrazolo[3,4-d]pyrimidine scaffold is a competitive area, frequently targeted for kinase inhibition by numerous pharmaceutical entities.
• Infringement risks arise from developing or marketing compounds or treatments that fall within the patent's claims before its expiration on May 26, 2026.
• Companies seeking to develop compounds in this chemical space must conduct thorough Freedom to Operate analyses and consider design-around strategies, licensing, or invalidation challenges.

Frequently Asked Questions

• What specific chemical structures are protected by US Patent 7,803,840? The patent protects compounds based on a pyrazolo[3,4-d]pyrimidine core with variable substituents at defined positions. The precise structures are detailed in the independent claim 1 and its dependent claims, which specify particular aryl, heteroaryl, alkyl, and amino groups.
• When does US Patent 7,803,840 expire? US Patent 7,803,840, filed on May 26, 2006, expires on May 26, 2026.
• Can I use a compound from US Patent 7,803,840 for research purposes without infringing? Generally, non-commercial research use, particularly academic research not for profit, may fall under experimental use exceptions, but this is highly fact-specific and subject to legal interpretation. Commercial research or development that leads to a commercial product would likely require a license.
• If a compound is structurally similar but not identical to those claimed, can it still infringe? Yes, infringement can occur through the doctrine of equivalents if the asserted compound is substantially the same and performs the same function in substantially the same way to achieve the same result as a claimed invention, even if not identical.
• What are the primary therapeutic targets for compounds described in this patent? The patent primarily targets diseases involving abnormal cell proliferation (cancer), inflammation, and viral infections, often through the inhibition of protein kinases, though other targets are possible.

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Citations

[1] United States Patent 7,803,840. (2010). Substituted pyrazolo[3,4-d]pyrimidin-4-amine compounds and their use in treating disease. Retrieved from USPTO Patent Full-Text and Image Database.

Drugs Protected by US Patent 7,803,840

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: 7,803,840

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Germany	198 53 487	Nov 19, 1998

International Family Members for US Patent 7,803,840

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1131065		C300675	Netherlands
European Patent Office	1131065		CA 2014 00036	Denmark
European Patent Office	1131065		PA2014023	Lithuania
European Patent Office	1131065		92488	Luxembourg
European Patent Office	1131065		39/2014	Austria
European Patent Office	1131065		1490039-3	Sweden