Details for Patent: 9,732,058

Which drugs does patent 9,732,058 protect, and when does it expire?

Patent 9,732,058 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: 9,732,058

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 such compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of such 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 (Macclesfield, GB), Finlay; Maurice Raymond Verschoyle (Macclesfield, GB), Ward; Richard Andrew (Macclesfield, GB), Redfearn; Heather Marie (Macclesfield, GB)
Assignee:	ASTRAZENECA AB (SE)
Application Number:	14/576,721
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,732,058
Patent Claim Types: see list of patent claims	Use; Composition; Compound;

Understanding the Scope and Claims of United States Patent 9,732,058: A Detailed Analysis

Introduction

United States Patent 9,732,058, issued to AstraZeneca AB, is a crucial patent protecting the drug Tagrisso (osimertinib), a significant treatment for non-small cell lung cancer (NSCLC). This patent is part of a broader patent landscape that safeguards the intellectual property of Tagrisso, ensuring AstraZeneca's exclusive rights to manufacture and market the drug.

Patent Overview

Patent Number and Title

The patent in question is US9732058B2, titled "2-(2,4,5-substituted-anilino)pyrimidine compounds"[2][4].

Issuance and Inventors

This patent was issued on August 15, 2017, to inventors Sam Butterworth, Maurice Raymond Verschoyle Finlay, Richard Andrew Ward, and Heather Marie Redfearn, all affiliated with AstraZeneca AB[2][4].

Patent Claims

Active Ingredient Protection

The patent protects specific 2-(2,4,5-substituted-anilino)pyrimidine compounds and their pharmaceutically acceptable salts. These compounds are the active ingredients in Tagrisso, which is an irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. The claims are narrowly defined to cover the exact chemical structures and their therapeutic uses, particularly in treating NSCLC[4].

Scope of Protection

The scope of this patent is limited to the specific chemical compounds and their use in treating certain types of cancer. This narrow scope is a result of the patent examination process, which tends to narrow the claims to ensure clarity and validity. Research indicates that narrower claims are associated with a higher probability of grant and a shorter examination process[3].

Patent Expiry Date

Current Status

The patent is set to expire on August 8, 2032. This date is critical as it marks the end of AstraZeneca's exclusive rights to the protected compounds, potentially allowing generic versions of Tagrisso to enter the market[1][2].

Exclusivities and Their Impact

FDA-Granted Exclusivities

In addition to patent protection, Tagrisso benefits from several FDA-granted exclusivities, including New Chemical Entity (NCE) exclusivity, New Indication exclusivity, and Orphan Drug Exclusivity. These exclusivities, which extend beyond the patent expiry dates, prevent other companies from marketing generic or bioequivalent versions of Tagrisso until they expire. For example, the Orphan Drug Exclusivity for Tagrisso extends until November 13, 2022, and another until April 18, 2025[1].

Legal Activities and Patent Landscape

Ongoing Legal Events

The patent landscape for Tagrisso is dynamic, with ongoing legal activities that can affect the patent's expiry date. Recent activities include patent issue dates, recordation of patent grants, and issue fee payments. These activities are crucial for tracking any changes that might impact the generic launch date of Tagrisso[1].

International Patent Protection

Tagrisso is protected by patents in multiple countries, not just the United States. Understanding the global patent landscape is essential for strategizing market entry, as it helps identify markets with weaker patent protection that could be ideal for generic entry[1].

Litigation and Patent Infringement

Patent Infringement Cases

There have been legal disputes involving Tagrisso, such as the case filed by Puma Biotechnology, Inc. and Wyeth LLC against AstraZeneca, alleging patent infringement related to the treatment of NSCLC. These cases highlight the complexity and competitive nature of the pharmaceutical patent landscape[5].

Impact on Generic Launch

Generic Availability

The expiry of the patent and the exclusivities will be pivotal in determining when generic versions of Tagrisso can be launched. Until these protections expire, AstraZeneca retains exclusive rights to the market, delaying the entry of generic competitors[1][2].

Conclusion

United States Patent 9,732,058 is a key component of the intellectual property protection for Tagrisso, safeguarding AstraZeneca's rights to this critical cancer treatment. The patent's narrow scope, combined with FDA-granted exclusivities and ongoing legal activities, ensures AstraZeneca's market dominance until the expiry dates.

Key Takeaways

• Patent Protection: US9732058B2 protects specific 2-(2,4,5-substituted-anilino)pyrimidine compounds used in Tagrisso.
• Expiry Date: The patent is set to expire on August 8, 2032.
• Exclusivities: FDA-granted exclusivities extend beyond patent expiry dates, delaying generic entry.
• Legal Activities: Ongoing legal events can impact the patent's expiry date and generic launch.
• Global Landscape: Tagrisso is protected by patents in multiple countries, affecting global market entry strategies.

FAQs

1. What is the main compound protected by US9732058B2? The main compound protected is 2-(2,4,5-substituted-anilino)pyrimidine, which is the active ingredient in Tagrisso.

2. When is the patent set to expire? The patent is set to expire on August 8, 2032.

3. What other protections besides patents safeguard Tagrisso? Tagrisso is also protected by FDA-granted exclusivities, including New Chemical Entity, New Indication, and Orphan Drug Exclusivities.

4. How do ongoing legal activities affect the patent? Ongoing legal activities, such as patent issue dates and oppositions, can change the patent's expiry date and impact the generic launch.

5. Why is understanding the global patent landscape important? Understanding the global patent landscape helps identify markets with weaker patent protection, which could be ideal for generic entry.

Sources

1. Pharsight: Tagrisso patent expiration - Pharsight
2. Drugs.com: Generic Tagrisso Availability - Drugs.com
3. SSRN: Patent Claims and Patent Scope - Search eLibrary :: SSRN
4. Google Patents: US9732058B2 - 2-(2,4,5-substituted-anilino)pyrimidine compounds
5. Insight.rpxcorp.com: in the united states district court

Drugs Protected by US Patent 9,732,058

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
Astrazeneca	TAGRISSO	osimertinib mesylate	TABLET;ORAL	208065-001	Nov 13, 2015		RX	Yes	No			Y	Y		TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS IN COMBINATION WITH PEMETREXED AND PLATINUM-BASED CHEMOTHERAPY

International Family Members for US Patent 9,732,058

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	087336
Argentina	115019
Australia	2012288626
Brazil	112014001768
Brazil	122014026094