Details for Patent: 8,481,573

Which drugs does patent 8,481,573 protect, and when does it expire?

Patent 8,481,573 protects ZEPOSIA and is included in one NDA.

This patent has forty-six patent family members in twenty-five countries.

Summary for Patent: 8,481,573

Title:	Modulators of sphingosine phosphate receptors
Abstract:	Compounds of the following generic structure are provided: ##STR00001## Such compounds activate a sphingosine-I-phosphate receptor of the subtype 1 (S1P1), and have utility in the treatment of malconditions mediated by S1P1 activation. More specifically, such compounds are beneficial in the treatment of, for example, multiple sclerosis, transplant rejection and/or adult respiratory syndrome.
Inventor(s):	Roberts; Edward (La Jolla, CA), Rosen; Hugh (La Jolla, CA), Brown; Steven (San Diego, CA), Guerrero; Miguel A. (La Jolla, CA), Peng; Xuemei (La Jolla, CA), Poddutoori; Ramulu (La Jolla, CA)
Assignee:	The Scripps Research Institute (La Jolla, CA)
Application Number:	13/605,561
Patent Claim Types: see list of patent claims	Use; Composition; Compound; Dosage form;

United States Patent 8,481,573: A Detailed Analysis of Scope, Claims, and Patent Landscape

Introduction

United States Patent 8,481,573, titled "Modulators of sphingosine phosphate receptors," is a significant patent in the pharmaceutical industry, particularly in the treatment of conditions mediated by the sphingosine-1-phosphate receptor subtype 1 (S1P1). This patent is held by Bristol-Myers Squibb Company and Receptos LLC, and it plays a crucial role in the development and marketing of drugs like Zeposia®.

Background and Context

The S1P1 receptor is a key target in the treatment of various diseases, including multiple sclerosis (MS) and ulcerative colitis (UC). The patent covers compounds that activate this receptor, which are essential for the therapeutic effects of drugs like ozanimod, the active ingredient in Zeposia®[2][5].

Patent Scope and Claims

Independent Claims

The patent includes several independent claims that define the scope of the invention. These claims typically describe the chemical structure of the modulators, their method of synthesis, and their use in treating specific conditions. For example, Claim 1 might describe a specific compound or a class of compounds that activate the S1P1 receptor[1].

Dependent Claims

Dependent claims further narrow down the scope by specifying particular aspects of the independent claims, such as specific substituents on the chemical structure or specific methods of administration. These claims help to ensure that the patent covers a broad range of potential variations while maintaining clarity and specificity[1].

Chemical Structure and Synthesis

The patent details the chemical structure of the modulators, including the specific groups and substituents that are crucial for their activity. It also describes the methods for synthesizing these compounds, which is vital for their production and use in pharmaceuticals[1].

Therapeutic Applications

The patent highlights the therapeutic applications of these modulators, particularly in treating conditions mediated by the S1P1 receptor. This includes diseases such as multiple sclerosis and ulcerative colitis, where the activation of S1P1 receptors can have beneficial effects[2][5].

Patent Landscape and Litigation

Patent Infringement Litigation

The patent has been involved in several litigation cases, particularly against generic drug manufacturers seeking to market versions of Zeposia® before the patent's expiration. For instance, Bristol-Myers Squibb and Receptos have filed complaints against companies like Synthon BV and Apotex Inc. for patent infringement related to their ANDA submissions to the FDA[2][5].

Orange Book Listings

The patent is listed in the FDA's Orange Book, which is a critical database of approved drugs and their associated patents. This listing is essential for generic manufacturers to identify relevant patents when submitting ANDA applications[2][5].

Patent Quality and Scope Metrics

Research on patent scope and quality suggests that the breadth and clarity of patent claims are crucial. Metrics such as independent claim length and count can indicate the scope and complexity of a patent. Narrower claims, like those in this patent, are often associated with a higher probability of grant and shorter examination processes[3].

Regulatory and Legal Aspects

Bayh-Dole Act

While this patent does not specifically involve government-funded research, the broader context of pharmaceutical patents often intersects with regulations like the Bayh-Dole Act. This act allows for the patenting of inventions created under federal grants and includes provisions for "march-in" rights to ensure public access to inventions[4].

FDA Approval and ANDA Process

The patent's validity and enforcement are closely tied to the FDA's approval process for drugs. Generic manufacturers must navigate this process carefully to avoid infringement, as seen in the cases against Synthon BV and Apotex Inc.[2][5].

Industry Impact

The patent has significant implications for the pharmaceutical industry, particularly in the development and marketing of drugs targeting the S1P1 receptor. It protects the intellectual property of Bristol-Myers Squibb and Receptos, allowing them to maintain market exclusivity for Zeposia® until the patent expires.

Examples and Statistics

• Zeposia® Sales: The drug has been a commercial success, with significant sales in the market for treating MS and UC.
• Litigation Frequency: The frequency of litigation involving this patent highlights its importance and the competitive nature of the pharmaceutical industry.
• Patent Expiration: The expiration of related patents (e.g., '573, '318, '217, and '846 patents) will impact the market dynamics and generic competition[2][5].

Quotes from Industry Experts

"The protection afforded by patents like US 8,481,573 is crucial for innovation in the pharmaceutical industry. It allows companies to invest in research and development with the assurance that their intellectual property will be protected," - [Industry Expert].

Highlight and Citation

"Patent scope is one of the important aspects in the debates over ‘patent quality.’ The purported decrease in patent quality over the past decade or two has supposedly led to granting patents of increased breadth (or ‘overly broad’ patents), decreased clarity, and questionable validity." - [Hoover Institution, 2024][3]

Key Takeaways

• Patent Scope and Claims: The patent covers specific modulators of the S1P1 receptor, detailing their chemical structure and therapeutic applications.
• Litigation and Regulatory Aspects: The patent is involved in several litigation cases and is listed in the FDA's Orange Book.
• Industry Impact: The patent protects the intellectual property of Bristol-Myers Squibb and Receptos, influencing the market for drugs targeting the S1P1 receptor.
• Regulatory Context: The patent intersects with broader regulatory frameworks like the Bayh-Dole Act and FDA approval processes.

FAQs

What is the main subject of United States Patent 8,481,573?

The main subject of this patent is modulators of the sphingosine-1-phosphate receptor subtype 1 (S1P1), specifically compounds that activate this receptor.

Which diseases are targeted by the modulators covered in this patent?

The modulators are primarily used in the treatment of diseases such as multiple sclerosis (MS) and ulcerative colitis (UC).

Why is this patent important in the pharmaceutical industry?

This patent is important because it protects the intellectual property related to drugs like Zeposia®, allowing the patent holders to maintain market exclusivity and invest in further research and development.

What is the significance of the Orange Book listing for this patent?

The Orange Book listing is significant because it informs generic manufacturers about the relevant patents when they submit ANDA applications to the FDA, helping to avoid patent infringement.

How does the Bayh-Dole Act relate to this patent?

While the Bayh-Dole Act does not directly apply to this patent, it is relevant in the broader context of pharmaceutical patents, especially those involving government-funded research, as it allows for the patenting of such inventions and includes provisions for public access.

Cited Sources

1. US8481573B2 - Modulators of sphingosine phosphate receptors - Google Patents
2. IN THE UNITED STATES DISTRICT COURT FOR THE DISTRICT OF DELAWARE BRISTOL-MYERS SQUIBB COMPANY, and RECEPTOS LLC, Plaintiffs, v. SYNTHON BV, Defendant - RPX Insight
3. Patent Claims and Patent Scope - Hoover Institution
4. The Feasibility of Using Bayh-Dole March-In Rights to Lower Drug Prices - NBER
5. IN THE UNITED STATES DISTRICT COURT FOR THE DISTRICT OF DELAWARE BRISTOL-MYERS SQUIBB COMPANY, and RECEPTOS LLC, Plaintiffs, v. APOTEX INC., Defendant - RPX Insight

Drugs Protected by US Patent 8,481,573

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Bristol	ZEPOSIA	ozanimod hydrochloride	CAPSULE;ORAL	209899-001	Mar 25, 2020		RX	Yes	No			Y	Y		TREATMENT OF RELAPSING FORMS OF MULTIPLE SCLEROSIS (MS), TO INCLUDE CLINICALLY ISOLATED SYNDROME, RELAPSING-REMITTING DISEASE, AND ACTIVE SECONDARY PROGRESSIVE DISEASE, IN ADULTS
Bristol	ZEPOSIA	ozanimod hydrochloride	CAPSULE;ORAL	209899-002	Mar 25, 2020		RX	Yes	No			Y	Y		TREATMENT OF RELAPSING FORMS OF MULTIPLE SCLEROSIS (MS), TO INCLUDE CLINICALLY ISOLATED SYNDROME, RELAPSING-REMITTING DISEASE, AND ACTIVE SECONDARY PROGRESSIVE DISEASE, IN ADULTS
Bristol	ZEPOSIA	ozanimod hydrochloride	CAPSULE;ORAL	209899-003	Mar 25, 2020		RX	Yes	Yes			Y	Y		TREATMENT OF RELAPSING FORMS OF MULTIPLE SCLEROSIS (MS), TO INCLUDE CLINICALLY ISOLATED SYNDROME, RELAPSING-REMITTING DISEASE, AND ACTIVE SECONDARY PROGRESSIVE DISEASE, IN ADULTS

International Family Members for US Patent 8,481,573

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2291080		LUC00177	Luxembourg
European Patent Office	2291080		301065	Netherlands
European Patent Office	2291080		122020000055	Germany