Details for Patent: 8,946,235

Which drugs does patent 8,946,235 protect, and when does it expire?

Patent 8,946,235 protects TAGRISSO and is included in one NDA.

This patent has one hundred and thirty-four patent family members in forty-one countries.

Summary for Patent: 8,946,235

Title:	2-(2,4,5-substituted-anilino) pyrimidine compounds
Abstract:	The present invention relates to certain 2-(2,4,5-substituted-anilino)pyrimidine compounds and pharmaceutically acceptable salts thereof which may be useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (for example the L858R activating mutant, the Exon19 deletion activating mutant and the T790M resistance mutant). Such compounds and salts thereof may be useful in the treatment or prevention of a number of different cancers. The invention also relates to pharmaceutical compositions comprising said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of said compounds and to methods of treatment of diseases mediated by various different forms of EGFR using such compounds and salts thereof.
Inventor(s):	Butterworth; Sam (Cheshire, GB), Finlay; Maurice Raymond Verschoyle (Cheshire, GB), Ward; Richard Andrew (Cheshire, GB), Redfearn; Heather Marie (Cheshire, GB)
Assignee:	AstraZeneca AB (Sodertalje, SE)
Application Number:	13/557,871
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,946,235
Patent Claim Types: see list of patent claims	Compound; Composition; Use;

Understanding the Scope and Claims of United States Patent 8,946,235

Introduction to Patent 8,946,235

United States Patent 8,946,235, titled "2-(2,4,5-substituted-anilino)pyrimidine compounds," is a significant patent in the pharmaceutical industry, particularly in the development and treatment of certain types of cancer. Here, we will delve into the details of this patent, including its scope, claims, and the broader patent landscape it operates within.

Background and Inventors

This patent was issued on February 3, 2015, and is assigned to AstraZeneca AB. The inventors listed include Sam Butterworth, Maurice Raymond Verschoyle Finlay, Richard Andrew Ward, Heather Marie Redfearn, and others who contributed to the development of these compounds[4].

Scope of the Patent

The scope of Patent 8,946,235 is defined by its claims, which are the legally binding descriptions of the invention. The patent covers a class of compounds known as 2-(2,4,5-substituted-anilino)pyrimidine compounds. These compounds are of particular interest due to their potential therapeutic applications, especially in the treatment of cancer.

Claims of the Patent

The claims of this patent are detailed and specific, outlining the structural requirements for the compounds. Here are some key aspects:

• Chemical Structure: The patent describes compounds with a specific pyrimidine core substituted with anilino groups at the 2, 4, and 5 positions. These substitutions can include various functional groups such as methyl, amino, and methoxy[4].
• Pharmaceutical Uses: The compounds are claimed for their use in treating various diseases, including cancer. Specifically, they are targeted at treating non-small cell lung cancer (NSCLC) and other cancers that are resistant to existing treatments like gefitinib and erlotinib[2].

Pharmaceutical Applications

One of the most notable applications of these compounds is in the treatment of NSCLC, particularly in cases with the T790M EGFR mutation. This mutation makes the cancer resistant to first-generation EGFR inhibitors like gefitinib and erlotinib. The compounds covered by this patent, such as osimertinib (marketed as Tagrisso®), are irreversible EGFR inhibitors that covalently bind to the cysteine 773 residue in the EGFR T790M mutant, thereby inhibiting the growth of cancer cells[2].

Patent Landscape

The patent landscape surrounding US 8,946,235 is complex and involves multiple related patents. Here are some key points:

• Related Patents: Other patents, such as US 9,732,058 and US 10,596,162, also cover aspects of these compounds and their use in treating cancer. These patents often reference the same prior art, including the PCT application WO 2006/084058[2].
• Litigation: The patents related to Tagrisso® have been involved in litigation, with AstraZeneca and its licensees enforcing their rights against potential infringers. This highlights the importance of these patents in protecting the intellectual property related to these life-saving drugs[2].

Patent Expiration and Generic Availability

The patent expiration dates for the compounds covered by US 8,946,235 are crucial for understanding when generic versions might become available. The primary patent for Tagrisso® is set to expire on January 2, 2035, although other related patents may have different expiration dates[5].

Strategic Importance of Broad Claims

In the pharmaceutical industry, the scope of patent claims is often a subject of strategic consideration. Patentees typically aim for broader claims to prevent competitors from easily designing around the patented invention. This approach ensures that minor modifications to the original compound do not allow competitors to avoid infringement[3].

Impact on Cancer Treatment

The compounds covered by this patent have significantly impacted the treatment of NSCLC, especially in cases with the T790M EGFR mutation. These irreversible EGFR inhibitors have provided new treatment options for patients who were previously resistant to other therapies.

Industry Expert Insights

Industry experts emphasize the importance of robust patent protection in the pharmaceutical sector. As noted by legal experts, "A patent is a legal tool, providing its owners the right to prevent others from using, producing, offering to sell, selling and importing the inventive product in the country where it was registered, for 20 years"[3].

Conclusion

United States Patent 8,946,235 is a pivotal patent in the field of cancer treatment, particularly for NSCLC with the T790M EGFR mutation. Its scope and claims are carefully crafted to protect the innovative compounds developed by AstraZeneca and its collaborators. Understanding this patent and its place within the broader patent landscape is essential for both pharmaceutical companies and healthcare professionals.

Key Takeaways

• Compound Structure: The patent covers 2-(2,4,5-substituted-anilino)pyrimidine compounds with specific substitutions.
• Therapeutic Use: These compounds are used in treating NSCLC, especially cases with the T790M EGFR mutation.
• Patent Expiration: The primary patent for Tagrisso® expires on January 2, 2035.
• Litigation: The patents have been involved in litigation to protect intellectual property rights.
• Strategic Importance: Broad claims are crucial to prevent competitors from designing around the patented invention.

FAQs

Q: What is the main therapeutic application of the compounds covered by US 8,946,235?

A: The main therapeutic application is in the treatment of non-small cell lung cancer (NSCLC), particularly in cases with the T790M EGFR mutation.

Q: Who are the inventors listed on US 8,946,235?

A: The inventors include Sam Butterworth, Maurice Raymond Verschoyle Finlay, Richard Andrew Ward, Heather Marie Redfearn, and others.

Q: What is the significance of the T790M EGFR mutation in NSCLC?

A: The T790M EGFR mutation makes NSCLC resistant to first-generation EGFR inhibitors like gefitinib and erlotinib, necessitating the use of irreversible EGFR inhibitors like osimertinib.

Q: When does the primary patent for Tagrisso® expire?

A: The primary patent for Tagrisso® is set to expire on January 2, 2035.

Q: Why are broad patent claims important in the pharmaceutical industry?

A: Broad patent claims prevent competitors from easily designing around the patented invention, thereby protecting the intellectual property rights of the patentee.

Sources

1. US8946235B2 - 2-(2,4,5-substituted-anilino) pyrimidine compounds - Google Patents.
2. in the united states district court - Insight.RPXCorp.
3. Patent claims' scope – is bigger always better? Trends in the pharmaceuticals industry - Pearl Cohen.
4. US8946235B2 - 2-(2,4,5-substituted-anilino) pyrimidine compounds - Google Patents.
5. Generic Tagrisso Availability - Drugs.com.

Drugs Protected by US Patent 8,946,235

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Astrazeneca	TAGRISSO	osimertinib mesylate	TABLET;ORAL	208065-001	Nov 13, 2015		RX	Yes	No			Y	Y		TREATMENT OF PATIENTS WITH METASTATIC EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) T790M MUTATION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC), WHO HAVE PROGRESSED ON OR AFTER EGFR TKI THERAPY
Astrazeneca	TAGRISSO	osimertinib mesylate	TABLET;ORAL	208065-001	Nov 13, 2015		RX	Yes	No			Y	Y		TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21L858R MUTATIONS
Astrazeneca	TAGRISSO	osimertinib mesylate	TABLET;ORAL	208065-001	Nov 13, 2015		RX	Yes	No			Y	Y		ADJUVANT THERAPY AFTER TUMOR RESECTION IN PATIENTS WITH NON-SMALL CELL LUNG CANCER(NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19DELETIONS OR EXON 21 L858R MUTATIONS
Astrazeneca	TAGRISSO	osimertinib mesylate	TABLET;ORAL	208065-001	Nov 13, 2015		RX	Yes	No			Y	Y		TREATMENT OF PATIENTS WITH LOCALLY ADVANCED, UNRESECTABLE (STAGE III) NSCLC WHOSE DISEASE HAS NOT PROGRESSED DURING OR FOLLOWING PLATINUM-BASED CHEMORADIATION THERAPY AND WHOSE TUMORS HAVE EGFR EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS

International Family Members for US Patent 8,946,235

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	087336
Argentina	115019
Australia	2012288626
Brazil	112014001768