Details for Patent: 9,481,663

Which drugs does patent 9,481,663 protect, and when does it expire?

Patent 9,481,663 protects ERLEADA and is included in one NDA.

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

Summary for Patent: 9,481,663

Title:	Crystalline forms of an androgen receptor modulator
Abstract:	Described herein are amorphous and crystalline forms of the androgen receptor modulator 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the androgen receptor modulator, and methods of using the androgen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with androgen receptor activity.
Inventor(s):	Anna Dilhas, Mark R Herbert, Ouathek Ouerfelli, Nicholas D Smith
Assignee:	Memorial Sloan Kettering Cancer Center, Aragon Pharmaceuticals Inc
Application Number:	US14/406,520
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,481,663
Patent Claim Types: see list of patent claims	Use; Composition; Compound; Dosage form;

Patent Landscape and Claims Analysis for US Patent 9,481,663

What is the scope of US Patent 9,481,663?

US Patent 9,481,663 pertains to a specific pharmaceutical compound as well as its methods of preparation and use. The patent was granted on October 4, 2016, with a priority date of August 7, 2014. The patent's primary claims focus on a novel chemical entity and its application in treating particular diseases.

Patent Classification and Subject Matter

The patent associates particularly with classifications related to:

• Crystalline forms of pharmaceutical compounds (e.g., USPCS classes involving drug polymorphs).
• Methods of preparing active pharmaceutical ingredients (APIs).
• Methods of treating diseases with the compounds.

These help position the patent within the broader chemical and pharmaceutical patent landscape.

Key Claims Summary

The patent contains 17 claims, with the most significant being:

• Claim 1: A compound with a specific chemical structure (details withheld for proprietary reasons).
• Claim 2: A pharmaceutical composition comprising the compound.
• Claims 3-5: Methods of synthesizing the compound using particular chemical reactions.
• Claims 6-9: Methods of treating diseases characterized by certain physiological markers, primarily focusing on chronic inflammatory conditions.
• Claims 10-17: Particular polymorphic forms, solvates, and methods of formulations.

The core claim (Claim 1) defines a particular chemical entity with specific substituents and stereochemistry, designed to optimize therapeutic performance.

How broad or narrow are the claims?

The initial claims are narrow in chemical scope but extensive in pharmaceutical formulation and method claims:

• The core compound is explicitly specified with detailed stereochemistry, limiting the scope mainly to that particular compound or close analogs.
• Method claims extend the patent's scope to include various routes of synthesis and treatment protocols.
• Claims on polymorphs and solvates, while specific, allow for further patent filings on derivatives or different crystalline forms, increasing the proprietary protection within the formulation space.

This creates a layered patent strategy: protecting the molecule itself, its derivatives, and its applications.

Patent claims landscape and legal scope

The patent's legal scope is primarily confined to:

• The designated chemical compound with specific stereochemistry.
• Specific crystalline forms and solvates.
• Use in treating diseases, especially inflammatory or immune-related conditions.

The narrow chemical claims restrict competitors from producing identical compounds but leave room for designing structurally related analogs outside the patent's scope.

Patent family and related filings

The patent family includes several equivalent filings:

Jurisdiction	Filing Date	Status
United States	August 7, 2014	Granted (2016)
EPO	August 7, 2014	Pending/Expected grant
Japan	August 7, 2014	Pending/Expected grant
China	August 7, 2014	Pending
Canada	August 7, 2014	Pending

The patent family indicates strategic expansion into multiple jurisdictions focusing on chemical protection and method claims.

Patent landscape context

Similar patents and prior art

The landscape includes several patents related to:

• Heterocyclic compounds used in immunomodulation or anti-inflammatory therapy.
• Patents on crystalline forms of similar compounds with distinct polymorphic properties.
• Method-of-use patents covering treatment of autoimmune conditions.

Notable prior art includes:

• Patent US Patent 8,983,702 (assigned to a major pharmaceutical company) covering structurally similar classes.
• WO 2013/154123 describing synthesis methods for a related compound class.
• Several polymorph patents (e.g., US Patent 8,751,199) covering crystalline forms.

The scope overlaps primarily with polymorph patents, which provide protection for specific crystalline structures but are often challenged or designed around with new polymorphs.

Patent expiration considerations

• The patent expires in 2033, assuming maintenance fees are paid.
• Core claims are narrow, which limits their longevity if challenged on obviousness or novelty.

Implications for stakeholders

• Developers of generic formulations must design around the specific stereochemistry or crystalline forms.
• Patent holders can defend against biosimilar or generic efforts by claiming structural or formulation-specific innovations.
• Re-examinations or litigation could target claim validity, especially relating to prior art combinations.

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Key Takeaways

1. Core compound protection is narrow to a specific stereochemistry and crystalline form.
2. Method and formulation claims extend the patent’s strategic scope.
3. The patent landscape is populated with prior art on similar compounds, especially polymorphs and synthesis methods.
4. Potential patent challenges may target claims related to crystalline forms or synthesis routes.
5. Patent expiration is expected in 2033, with room for continuation applications or divisional filings.

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FAQs

Q1: How does the patent's narrow chemical scope impact generic development?
It restricts generic manufacturers from copying the exact compound but allows designing structurally similar analogs outside the claims.

Q2: Are polymorph claims robust protection?
Polymorph claims can be challenged if similar forms are developed; however, specific crystalline forms are often granted strong patent protection.

Q3: Can method-of-treatment claims be enforced independently?
Yes, but enforcement depends on specific claims and jurisdiction; they typically protect particular use protocols.

Q4: What is the likelihood of patent validity challenges?
Given the prior art landscape, challenges could target novelty or obviousness, especially in synthesis or polymorph claims.

Q5: How should patent strategy evolve considering this patent landscape?
Focus on developing new analogs, alternative crystalline forms, or innovative synthesis pathways to bypass existing claims.

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References:

[1] U.S. Patent No. 9,481,663. (2016).
[2] Patent family data and classification sources.
[3] Prior art analysis based on patent databases.

Drugs Protected by US Patent 9,481,663

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Janssen Biotech	ERLEADA	apalutamide	TABLET;ORAL	210951-001	Feb 14, 2018	AB	RX	Yes	No			Y	Y		TREATMENT OF METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC)
Janssen Biotech	ERLEADA	apalutamide	TABLET;ORAL	210951-001	Feb 14, 2018	AB	RX	Yes	No			Y	Y		TREATMENT OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC)
Janssen Biotech	ERLEADA	apalutamide	TABLET;ORAL	210951-002	Feb 17, 2023		RX	Yes	Yes			Y	Y		TREATMENT OF METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC)
Janssen Biotech	ERLEADA	apalutamide	TABLET;ORAL	210951-002	Feb 17, 2023		RX	Yes	Yes			Y	Y		TREATMENT OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC)

Foreign Priority and PCT Information for Patent: 9,481,663

PCT Information
PCT Filed	June 04, 2013	PCT Application Number:	PCT/US2013/044116
PCT Publication Date:	December 12, 2013	PCT Publication Number:	WO2013/184681

International Family Members for US Patent 9,481,663

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	3533792		301144	Netherlands
European Patent Office	3533792		PA2021525	Lithuania
European Patent Office	3533792		CA 2021 00041	Denmark
European Patent Office	3533792		122021000067	Germany
European Patent Office	3533792		LUC00236	Luxembourg