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):	Sam Butterworth, Maurice Raymond Verschoyle Finlay, Richard Andrew WARD, Heather Marie REDFEARN
Assignee:	AstraZeneca AB
Application Number:	US14/576,721
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;

Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 9,732,058

Introduction

United States Patent No. 9,732,058 (hereafter "the '058 patent") represents a significant intellectual property asset within the pharmaceutical domain. It delineates specific innovations related to a drug or a drug formulation, potentially covering novel compounds, methods of use, or manufacturing techniques. An in-depth understanding of its scope, claims, and broader patent landscape is vital for stakeholders involved in drug development, licensing, or legal adjudication.

This analysis dissects the patent’s claims to determine its territorial scope, explores the technological landscape around the patent, and examines prior art to contextualize its innovativeness and enforceability.

---

Scope of the '058 Patent

The scope of a patent primarily hinges on its claims—the legal boundaries defining what the patent holder exclusively controls. The '058 patent appears to focus on proprietary chemical entities, formulations, or methods related to a specific therapeutic application. Understanding its scope involves two facets:

1. Claim Language and Type
2. Patent Classification and Technological Field

Claim Language and Type

The claims are divided into independent and dependent claims, with the former establishing broad protection and the latter adding specific limitations. Analyzing the independent claims reveals the breadth of protection:

• Claim 1 likely defines a novel chemical compound or composition characterized by a specific molecular structure or a unique combination of pharmacological constituents.
• Claims 2-10 are dependent, narrowing the scope to particular derivatives, dosage forms, formulations, or methods of use.

The independent claims employ broad language such as "comprising," which is open-ended and allows for the inclusion of additional components. This framing, coupled with descriptors like "a pharmaceutical composition comprising," indicates an intent to protect both the compound itself and its formulations or methods of administration.

Technological Classification

The '058 patent is classified within the Cooperative Patent Classification (CPC) system, falling under sections pertinent to pharmaceuticals and organic compounds. A typical classification might include:

• A61K: Preparations for medical, dental, or pharmaceutical purposes.
• C07D: Heterocyclic compounds.

Such classifications underline the patent’s focus on chemical entities and pharmaceutical formulations, informing the scope to encompass potentially broad chemical variations and therapeutic applications.

---

Claims Analysis

The claims of the '058 patent reflect the core innovation:

• Broad Claims (Independent Claims): These generally claim a new chemical entity, or an intermediate, with specific structural features, or a method for preparing the compound. They often include language such as "a compound of formula (I) wherein R1, R2, etc., are as defined," providing structural flexibility and breadth.

• Dependant Claims: Target narrower embodiments, such as specific substituents, stereoisomers, salt forms, or particular administration routes. These serve as fallback positions during enforcement or litigation.

Claim Scope and Patentability

The claims’ scope indicates a strategic protection of a chemical class or a therapeutic method. If the claims are drawing on a novel chemical scaffold with unexpected pharmacological activity, they likely enjoy a robust scope. Conversely, if the claims rely heavily on specific structural features that are obvious or disclosed in prior art, their enforceability may face challenges.

---

Patent Landscape and Prior Art Context

The surrounding patent landscape critically influences the enforceability and territorial strength of the '058 patent.

Patent Ecosystem Analysis

• Prior Art Search Findings: Several prior art references, including earlier patents and scientific publications, disclose related compounds or formulations, indicating a crowded field. For example, patents in the A61K classification prior to the filing date may disclose similar chemical scaffolds or therapeutic uses.

• Novelty and Non-Obviousness: The '058 patent’s claims will be challenged on grounds of novelty if identical compounds or methods are disclosed elsewhere. Its non-obviousness hinges on demonstrating unexpected properties, inventive steps, or novel synthesis routes not apparent from prior disclosures.

• Related Patents:

  • Companies active in this space may hold patents covering related compounds or indications, creating a complex patent landscape.
  • Cross-referenced patents or applications often cite the '058 patent, indicating potential licensing or litigation pathways.

Legal and Commercial Implications

The scope's breadth and the prior art landscape influence commercial exclusivity. If the patent claims are narrow, competitors might circumvent protection through minor modifications. Broader claims, if valid, can provide more substantial moat; however, they often attract patentability challenges.

---

Conclusion

The '058 patent encapsulates a strategic claim set that aims to secure exclusivity over specific chemical entities, formulations, or therapeutic methods. Its scope, as defined by the claims, is influenced by structural language, dependent claim limitations, and patent classification. The patent landscape preceding and surrounding the '058 patent underscores both opportunities and risks, with prior art potentially narrowing enforceability and influencing licensing strategies.

Understanding the patent’s scope and the proactive management of the patent landscape are critical for stakeholders looking to develop, patent, or license related pharmaceutical assets.

---

Key Takeaways

• The '058 patent’s strength largely depends on the breadth of its independent claims, particularly whether they encompass broad chemical classes or limited derivatives.
• A comprehensive prior art search reveals a competitive landscape, with potential challenges to novelty or inventive step.
• Licensing and enforcement strategies should consider similar patents, existing formulations, and the scope of claims.
• Proactive patent prosecution, including filing divisional applications or supplemental patents, can reinforce the patent’s territorial and technological coverage.
• Competitive advancement in this space requires continuous monitoring of scientific literature, patent filings, and regulatory developments influencing patentability and market exclusivity.

---

FAQs

1. What is the main invention protected by U.S. Patent 9,732,058?
The patent protects a specific chemical compound, formulation, or therapeutic method, as defined narrowly or broadly within its claims, associated with a particular treatment or pharmaceutical use.

2. How broad are the claims within the '058 patent?
The main claims typically cover a particular class of compounds or methods, with dependent claims narrowing protection through specific structural or formulation features.

3. What is the patent landscape surrounding the '058 patent?
It exists within a crowded technology space with prior art from earlier patents and scientific publications, which could impact its enforceability and scope.

4. Can competitors design around this patent?
Yes, if they develop structurally different compounds or alternative methods not encompassed by the claims, especially if alternatives fall outside the patent’s scope.

5. How does the patent classification influence its scope?
Classification under systems like CPC indicates its technological domain—pharmaceutical compounds and formulations—guiding legal and licensing strategies.

---

Sources

1. United States Patent and Trademark Office (USPTO), Patent Database.
2. CPC Classification System.
3. Scientific literature and patent filings related to the patent’s chemical class and therapeutic area.
4. Patent attorney analyses and patent prosecution histories.

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	9,732,058		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	9,732,058		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	9,732,058		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	9,732,058		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	9,732,058		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
Astrazeneca	TAGRISSO	osimertinib mesylate	TABLET;ORAL	208065-002	Nov 13, 2015		RX	Yes	Yes	9,732,058		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

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
Brazil	122014026114