United States Patent 8,987,323: A Detailed Analysis
Introduction
United States Patent 8,987,323, titled "Crystalline form of benzylbenzene SGLT2 inhibitor," is a significant patent in the pharmaceutical industry, particularly in the treatment of hyperglycemia. This patent, granted on March 24, 2015, is assigned to Theracos, Inc. and involves the development of a stable crystalline form of a compound that inhibits the sodium-dependent glucose cotransporter 2 (SGLT2).
Background of the Invention
The invention addresses the need for a stable and well-defined crystalline form of an SGLT2 inhibitor. SGLT2 inhibitors are crucial in treating hyperglycemia by increasing the excretion of glucose in the urine. The availability of a well-defined crystalline form allows for the purification of the drug substance through recrystallization, which is essential for improving the physical and chemical stability of the pharmaceutical composition[2].
Summary of the Invention
The patent describes the preparation and characterization of a crystalline form of the compound (2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-(2-cyclopropoxyethoxy)benzyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol. This compound is synthesized using methods outlined in previous patent applications and publications, such as U.S. Publication No. 2009/0118201 and PCT/US2009/054585[2].
Claims of the Patent
The patent includes several claims that define the scope of the invention:
- Claim 1: This claim describes the crystalline form of the SGLT2 inhibitor compound, specifying its structural and chemical characteristics.
- Claim 2-5: These claims detail various aspects of the crystalline form, including its X-ray powder diffraction (XRPD) pattern, Raman spectroscopy peaks, and other physical properties.
- Claim 6-10: These claims cover methods for preparing the crystalline form, including recrystallization processes.
- Claim 11-15: These claims pertain to pharmaceutical compositions containing the crystalline form of the SGLT2 inhibitor and methods for treating hyperglycemia using these compositions[1][2].
Patent Landscape
Related Patents and Applications
The patent is part of a series of related applications and patents. It is a continuation of U.S. application Ser. No. 13/158,724, filed on June 13, 2011, which also claims foreign priority under 35 U.S.C. § 119 to PCT/CN2010/073865, filed on June 12, 2010. This indicates a complex and interconnected patent landscape where multiple applications and patents are linked to protect various aspects of the invention[2].
Polymorph Patents
The patent landscape for pharmaceuticals often includes polymorph patents, which cover different crystalline forms of the same compound. For the SGLT2 inhibitor in question, the crystalline form described in this patent is crucial for ensuring stability and efficacy. Polymorph patents can extend the patent life of a drug by providing additional protection beyond the compound patent, as seen in the analysis of 30 small molecule new drugs approved by the FDA in 2023, where many polymorph patents expire later than the corresponding compound patents[4].
Expiration Dates and Time Gaps
The expiration dates of compound patents and polymorph patents can vary significantly. For example, the polymorph patent for a drug like Brenzavvy (US8987323B2) expires in 2032, while the compound patent expires in 2029, creating a time gap that can extend market exclusivity[4].
Significance and Impact
Stability and Purification
The crystalline form described in this patent is significant because it allows for the purification of the drug substance through recrystallization, enhancing the physical and chemical stability of the pharmaceutical composition. This stability is crucial for ensuring the efficacy and safety of the drug[2].
Market Protection
The patent provides Theracos, Inc. with market protection for their SGLT2 inhibitor, preventing other companies from manufacturing or selling the same crystalline form of the compound. This protection is vital for recouping investment in research and development and maintaining a competitive edge in the market.
Therapeutic Implications
The SGLT2 inhibitor is used to treat hyperglycemia by increasing glucose excretion in the urine. The stable crystalline form of this compound ensures consistent therapeutic effects, which is critical for managing diabetes and other related conditions.
Industry Context
Patent Portfolios
The strategy behind this patent aligns with the concept of patent portfolios, where companies seek to obtain a large quantity of related patents to protect their innovations comprehensively. This approach is more about securing a broad range of marketplace protections rather than evaluating the individual worth of each patent[3].
Patent Intensity
The increasing patent intensity in the pharmaceutical industry, where more patents are filed per research and development dollar, reflects the competitive nature of the field. Companies like Theracos, Inc. must navigate this landscape to protect their innovations and maintain market position[3].
Key Takeaways
- Stable Crystalline Form: The patent describes a stable crystalline form of an SGLT2 inhibitor, crucial for purification and stability.
- Market Protection: The patent provides market protection, extending the exclusivity period for the drug.
- Therapeutic Significance: The stable form ensures consistent therapeutic effects in treating hyperglycemia.
- Patent Landscape: The patent is part of a complex landscape involving related applications and polymorph patents.
- Industry Strategy: The patent aligns with the strategy of building comprehensive patent portfolios.
Frequently Asked Questions (FAQs)
Q: What is the main subject of United States Patent 8,987,323?
A: The main subject is the crystalline form of a benzylbenzene SGLT2 inhibitor used in treating hyperglycemia.
Q: Why is the crystalline form important?
A: The crystalline form is important for the purification and stability of the drug substance, ensuring its efficacy and safety.
Q: How does this patent fit into the broader patent landscape?
A: It is part of a series of related applications and patents, including polymorph patents that extend market exclusivity.
Q: What is the therapeutic significance of this patent?
A: The stable crystalline form ensures consistent therapeutic effects in treating hyperglycemia, which is critical for managing diabetes.
Q: How does this patent align with industry strategies?
A: It aligns with the strategy of building comprehensive patent portfolios to protect innovations and maintain market position.
Sources Cited
- United States Patent and Trademark Office. US00898.7323B2: Crystalline form of benzylbenzene SGLT2 inhibitor. March 24, 2015.
- Justia Patents. Crystalline form of benzylbenzene SGLT2 inhibitor. July 30, 2020.
- Penn Carey Law: Legal Scholarship Repository. Patent Portfolios. University of Pennsylvania Law Review, Vol. 154: 1.
- Crystal Pharmatech. Review of Polymorph Patent Application of 30 Small Molecule New Drugs Approved by the FDA in 2023. Crystal Pharmatech.
