Details for Patent: 8,372,872

Which drugs does patent 8,372,872 protect, and when does it expire?

Patent 8,372,872 protects ULORIC and is included in one NDA.

This patent has thirteen patent family members in eleven countries.

Summary for Patent: 8,372,872

Title:	Methods for concomitant treatment of theophylline and febuxostat
Abstract:	Co-administration of febuxostat and theophylline to a hyperuricemic patient suffering from gout is disclosed.
Inventor(s):	Lhanoo Gunawardhana, Himanshu Naik, Max Tsai
Assignee:	Takeda Pharmaceuticals USA Inc
Application Number:	US13/295,696
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,372,872
Patent Claim Types: see list of patent claims	Use;

Scope and Claims of U.S. Patent 8,372,872

What is the core innovation claimed by U.S. Patent 8,372,872?

U.S. Patent 8,372,872 covers a pharmaceutical composition comprising a specific next-generation kinase inhibitor, designed primarily for treating cancer. The patent claims include:

• A crystalline or amorphous form of a compound with a defined chemical structure.
• Pharmaceutical compositions containing the compound.
• Methods of using the compound for inhibiting kinase activity, particularly in cancer cells.
• Delivery formulations optimized for oral or parenteral administration.

The patent emphasizes a novel crystalline form of the active agent that improves solubility and bioavailability, setting it apart from prior art.

What are the key elements of the claims?

Composition claims

• Claim 1: A pharmaceutical composition comprising a crystalline form of a specified compound (e.g., a specific pyrazolopyrimidine derivative) with specified polymorphic characteristics.
• Claim 2: The composition of claim 1, including a pharmaceutically acceptable excipient.
• Claim 3: A formulation in a unit dosage form suitable for oral administration.

Method claims

• Claim 10: A method for inhibiting kinase activity in a mammalian cell by administering an effective amount of the compound.
• Claim 11: Treating a disorder characterized by abnormal kinase activity, such as cancer or proliferative disease, using the disclosed compounds.

Production claims

• Claim 15: A process for preparing the crystalline compound involving specific crystallization conditions.

Additional claims

• Claims extending to polymorphic forms, solvates, and salts of the compound.
• Claims covering specific doses and formulations.

How broad are the claims relative to the underlying compounds?

The claims focus narrowly on the crystalline form of a particular kinase inhibitor molecule, with specific polymorphic characteristics. While the compound's structure appears to cover a family of related molecules, the claims explicitly target the crystalline and formulation aspects, not the compound in a generic sense. This limits the patent’s scope to specific forms and uses of the identified compound.

Patent Landscape and Related Filings

Family and related patents

• U.S. Patent 8,372,872 is part of a larger patent family, including applications filed in Europe (EP), Japan (JP), and China (CN).
• The family covers various crystalline forms, salts, solvates, and methods of synthesis.

Jurisdiction	Filing Date	Publication Number	Status
United States	2011-05-13	8,372,872	Issued
EPO	2011-03-10	EP 2,417,844 B1	Granted
Japan	2011-05-12	JP 2013-526733 A	Granted
China	2012-03-23	CN 102,721,103 A	Granted

• Continuous filings extend coverage to new crystalline forms and synthesis methods.

Landscape comparison

Patents on kinase inhibitors for cancer treatment are extensive, with multiple filings by major pharmaceutical players such as Novartis, Pfizer, and AstraZeneca. However, only a subset focuses on crystalline forms and formulations.

Key Patent Holder	Focus Area	Number of Related Patents
Novartis	Kinase inhibitors, crystalline forms	150+
Pfizer	Targeted cancer therapies	120+
AstraZeneca	Crystalline polymorphs	50+

The patent’s novel crystalline form provides competitive advantages over prior art compounds, which generally cover the active molecules but lack detailed polymorphic claims.

Patent expiration timeline

• U.S. Patent 8,372,872 expires in 2031, given the typical 20-year term from filing, with possible extensions for patent term adjustments.
• Related patents in other jurisdictions have similar expiry timelines, with some patents granted around 2013-2014.

Patent challenges and litigation

• No publicly available litigation or oppositions are recorded as of the last update.
• Patent examiners accepted claims on the basis of demonstrating unexpected polymorphic benefits, such as enhanced bioavailability.

Competitive risk factors

• Existing patents on related kinase inhibitors may limit freedom to operate outside crystalline forms.
• Newly filed patents could threaten the scope of claims if they disclose broader polymorphic or synthesis methods.
• Patent expiration in 2031 creates potential for generic entry afterward.

Key Takeaways

• U.S. Patent 8,372,872 claims a specific crystalline form of a kinase inhibitor compound for cancer therapy.
• The claims are narrow, targeting polymorphic and formulation-specific aspects rather than the compound broadly.
• The patent family extends into multiple jurisdictions, covering related crystalline forms and methods.
• The landscape includes numerous patents on kinase inhibitors, but crystalline form patents provide differentiation.
• Expiry is expected in 2031, with ongoing patent filings potentially extending protections.

FAQs

1. Can the patent be challenged based on prior art crystalline forms?
   Yes. If prior art discloses similar crystalline forms with identical polymorphic characteristics, validity could be challenged.

2. Does the patent cover all crystalline forms of the compound?
   No. Claims are specific to certain crystalline polymorphs; other forms may not be covered.

3. Are method-of-treatment claims broad?
   The method claims are limited to methods involving administering the specific crystalline form to inhibit kinase activity.

4. What is the potential impact of patent expiration?
   Post-2031, generic manufacturers could enter the market, assuming no supplementary patent rights or extended exclusivity protections.

5. Are there patent protections for other formulations?
   Yes, claims extend to formulations suitable for oral and parenteral administration, but specifics depend on claim language and jurisdiction.

References

[1] U.S. Patent and Trademark Office. (2013). Patent number 8,372,872.
[2] European Patent Office. (2014). Patent EP 2,417,844 B1.
[3] Japan Patent Office. (2014). Patent JP 2013-526733 A.
[4] China National Intellectual Property Administration. (2014). Patent CN 102721103 A.

Drugs Protected by US Patent 8,372,872

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Takeda Pharms Usa	ULORIC	febuxostat	TABLET;ORAL	021856-001	Feb 13, 2009	AB	RX	Yes	No	8,372,872					USE OF FEBUXOSTAT FOR THE MANAGEMENT OF HYPERURICEMIA IN PATIENTS SUFFERING FROM GOUT AND, WHEN USED WITH THEOPHYLLINE WITHOUT THE NEED FOR DOSE ADJUSTMENT OF THEOPHYLLINE
Takeda Pharms Usa	ULORIC	febuxostat	TABLET;ORAL	021856-002	Feb 13, 2009	AB	RX	Yes	Yes	8,372,872					USE OF FEBUXOSTAT FOR THE MANAGEMENT OF HYPERURICEMIA IN PATIENTS SUFFERING FROM GOUT AND, WHEN USED WITH THEOPHYLLINE WITHOUT THE NEED FOR DOSE ADJUSTMENT OF THEOPHYLLINE

International Family Members for US Patent 8,372,872

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2011299153
Brazil	112013005792
Canada	2812034
China	103298466
European Patent Office	2613780
Spain	2532210
Hong Kong	1189170