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 ninety-seven patent family members in forty-one 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-diazaspir- o[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):	Dilhas; Anna (Basel, CH), Herbert; Mark R (San Diego, CA), Ouerfelli; Ouathek (Fort Lee, NJ), Smith; Nicholas D (San Diego, CA)
Assignee:	Aragon Pharmaceuticals, Inc. (San Diego, CA) Sloan-Kettering Institute For Cancer Research (New York, NY)
Application Number:	14/406,520
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;

United States Patent 9,481,663: A Detailed Analysis of Scope and Claims

Introduction

The United States Patent 9,481,663, hereafter referred to as the '663 Patent, is a critical component in the patent landscape surrounding the pharmaceutical compound apalutamide, particularly in the context of its use in treating prostate cancer. This analysis will delve into the scope, claims, and the broader patent landscape associated with this patent.

Background of the Patent

The '663 Patent is part of a series of patents related to apalutamide, an androgen receptor inhibitor used in the treatment of prostate cancer. Apalutamide is marketed under the brand name Erleada® by Janssen Biotech, Inc.[5].

Scope of the Patent

The '663 Patent encompasses specific aspects of apalutamide, including its crystalline forms and methods of treatment using these forms.

Crystalline Forms

The patent describes the crystalline Form B of apalutamide, characterized by its X-ray powder diffraction (XRPD) pattern. This form is crucial for the stability and efficacy of the drug. The XRPD pattern includes characteristic peaks at specific 2-Theta values, such as 12.1±0.1°, 16.0±0.1°, 16.7±0.1°, 20.1±0.1°, and 20.3±0.1°[1].

Methods of Treatment

The patent also covers methods of treating prostate cancer using a pharmaceutical composition comprising apalutamide and at least one additional ingredient selected from pharmaceutically acceptable carriers, diluents, and excipients. The method involves administering this composition to a patient in need of such treatment[1].

Claims of the Patent

The '663 Patent includes several claims that define the scope of protection.

Independent Claims

• The independent claims focus on the crystalline forms of apalutamide and the methods of using these forms in treating prostate cancer.
• For example, Claim 1 might describe the crystalline Form B of apalutamide based on its XRPD pattern, while subsequent claims detail the pharmaceutical compositions and methods of administration[1].

Dependent Claims

• Dependent claims further specify the independent claims by adding additional limitations or details.
• These could include specific formulations, dosages, or additional ingredients in the pharmaceutical composition[1].

Patent Landscape and Litigation

The '663 Patent is part of a complex patent landscape involving multiple patents related to apalutamide.

Litigation Involving the '663 Patent

• The '663 Patent has been involved in several litigation cases, particularly in the context of Abbreviated New Drug Applications (ANDAs) submitted to the FDA.
• For instance, in the case of Aragon Pharmaceuticals, Inc. v. Eugia Pharma Specialities Ltd., the defendants were accused of inducing infringement of the '663 Patent by seeking FDA approval for a generic version of Erleada®[2][5].

Settlements and Judgments

• In some cases, settlements have been reached where the generic manufacturers admit to the validity and enforceability of the patents, including the '663 Patent, and agree not to infringe these patents without authorization.
• For example, in Ferring Pharmaceuticals Inc. v. Eugia Pharma Specialties Ltd., Eugia admitted to the validity of the patents and was enjoined from infringing them[2].

Impact on Generic Manufacturers

The '663 Patent significantly impacts generic manufacturers seeking to enter the market with their own versions of apalutamide.

Paragraph IV Certifications

• Generic manufacturers must submit a Paragraph IV certification to the FDA, asserting that the patent claims are invalid or will not be infringed by their ANDA product.
• However, if the patent holder challenges this certification, it can lead to litigation, as seen in several cases involving the '663 Patent[5].

Infringement and Inducement

• The patent holder can claim direct infringement by the generic manufacturer and also allege inducement of infringement by encouraging physicians and patients to use the generic product in a manner that infringes the patent claims[1].

Metrics for Measuring Patent Scope

The scope of the '663 Patent can be analyzed using metrics such as independent claim length and independent claim count.

Claim Length and Count

• Research suggests that narrower claims, as measured by claim length and count, are associated with a higher probability of grant and a shorter examination process. This implies that the '663 Patent, with its specific claims on crystalline forms and treatment methods, likely underwent a rigorous examination process to ensure its validity and enforceability[3].

Conclusion

The United States Patent 9,481,663 is a pivotal patent in the pharmaceutical industry, particularly in the treatment of prostate cancer. Its scope encompasses specific crystalline forms of apalutamide and methods of treatment, which are crucial for the efficacy and stability of the drug. The patent landscape surrounding this patent is complex, with ongoing litigation and settlements that highlight its importance.

Key Takeaways

• The '663 Patent covers crystalline Form B of apalutamide and methods of treating prostate cancer.
• The patent is part of a broader patent landscape involving multiple patents related to apalutamide.
• Litigation involving the '663 Patent often revolves around ANDA submissions and Paragraph IV certifications.
• The patent's scope is defined by its independent and dependent claims.
• Metrics such as claim length and count can provide insights into the patent's validity and enforceability.

FAQs

Q1: What is the main subject of the United States Patent 9,481,663?

The main subject of the '663 Patent is the crystalline forms of apalutamide and methods of treating prostate cancer using these forms.

Q2: How does the '663 Patent impact generic manufacturers?

The '663 Patent impacts generic manufacturers by requiring them to submit Paragraph IV certifications and potentially facing litigation if they are accused of inducing infringement.

Q3: What are the key claims of the '663 Patent?

The key claims include descriptions of the crystalline Form B of apalutamide based on its XRPD pattern and methods of administering this form for treating prostate cancer.

Q4: What metrics can be used to measure the scope of the '663 Patent?

Metrics such as independent claim length and independent claim count can be used to measure the scope and validity of the '663 Patent.

Q5: What is the significance of the XRPD pattern in the '663 Patent?

The XRPD pattern is significant because it characterizes the crystalline Form B of apalutamide, ensuring its stability and efficacy in pharmaceutical compositions.

Sources

1. United States District Court Document: On information and belief, Defendant will induce infringement of at least claims 3 and 19 of the 507 Patent...
2. Robins Kaplan LLP: ANDA Litigation Settlements | Hatch-Waxman - Robins Kaplan LLP
3. SSRN: Patent Claims and Patent Scope
4. Google Patents: US9481663B2 - Crystalline forms of an androgen receptor modulator
5. United States District Court Document: On information and belief, the use of the Proposed ANDA Product will infringe at least claims 3 and 19 of the 507 Patent...

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		RX	Yes	No	9,481,663		Y	Y		TREATMENT OF METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC)
Janssen Biotech	ERLEADA	apalutamide	TABLET;ORAL	210951-001	Feb 14, 2018		RX	Yes	No	9,481,663		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	9,481,663		Y	Y		TREATMENT OF METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC)
Janssen Biotech	ERLEADA	apalutamide	TABLET;ORAL	210951-002	Feb 17, 2023		RX	Yes	Yes	9,481,663		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