Details for Patent: 8,349,840

Which drugs does patent 8,349,840 protect, and when does it expire?

Patent 8,349,840 protects REXULTI and is included in one NDA.

Protection for REXULTI has been extended six months for pediatric studies, as indicated by the *PED designation in the table below.

This patent has thirty-six patent family members in twenty-nine countries.

Summary for Patent: 8,349,840

Title:	Piperazine-substituted benzothiophenes for treatment of mental disorders
Abstract:	The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety. ##STR00001##
Inventor(s):	Yamashita; Hiroshi (Tokushima, JP), Ito; Nobuaki (Tokushima, JP), Miyamura; Shin (Tokushima, JP), Oshima; Kunio (Tokushima, JP), Matsubara; Jun (Tokushima, JP), Kuroda; Hideaki (Tokushima, JP), Takahashi; Haruka (Tokushima, JP), Shimizu; Satoshi (Tokushima, JP), Tanaka; Tatsuyoshi (Tokushima, JP)
Assignee:	Otsuka Pharmaceutical Co., Ltd. (Tokyo, JP)
Application Number:	12/970,690
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,349,840
Patent Claim Types: see list of patent claims	Composition; Compound; Use;

United States Patent 8,349,840: A Detailed Analysis of Scope, Claims, and Patent Landscape

Introduction

The United States Patent 8,349,840, titled "Piperazine-substituted benzothiophenes for treatment of mental disorders," is a significant patent in the pharmaceutical industry, particularly in the realm of antipsychotic medications. This patent, held by Otsuka Pharmaceutical Co., Ltd., covers a class of compounds with potential therapeutic benefits for mental health disorders.

Background and Purpose

The patent aims to provide antipsychotic drugs with a wider treatment spectrum, fewer side effects, and excellent tolerability. This is achieved through the development of piperazine-substituted benzothiophenes, which are designed to interact with various neurotransmitter systems in the brain, thereby alleviating symptoms of mental disorders such as schizophrenia and bipolar disorder[4].

Chemical Structure and Composition

The patent describes a specific class of chemical compounds, notably the piperazine-substituted benzothiophenes. These compounds are characterized by their unique molecular structure, which includes a benzothiophene core substituted with a piperazine group. The chemical compound 7-[3-[4-(1-benzothiophen-4-yl)piperazin-1-yl]propoxy]-3,4-dihydro-2H-isoquinolin-1-one is a prime example of these compounds[4].

Claims of the Patent

The patent includes several claims that define the scope of the invention. These claims are divided into independent and dependent claims.

• Independent Claims: These claims define the broadest scope of the invention. They typically describe the general structure of the piperazine-substituted benzothiophenes and their use in treating mental disorders.
• Dependent Claims: These claims narrow down the scope by specifying particular aspects of the compounds, such as specific substituents, dosages, and methods of administration[4].

Patent Scope and Breadth

The scope of the patent is critical in determining its impact on the pharmaceutical industry. The patent scope is measured by metrics such as independent claim length and independent claim count. Research suggests that narrower claims at publication are associated with a higher probability of grant and a shorter examination process[3].

In the case of US 8,349,840, the claims are carefully crafted to ensure a balance between breadth and specificity. The patent covers a range of compounds and their therapeutic applications, providing a robust foundation for Otsuka's intellectual property in this area.

Patent Landscape and Litigation

The patent landscape surrounding US 8,349,840 is complex and involves several legal battles. Otsuka has been involved in various patent infringement cases, particularly against generic drug manufacturers seeking to produce versions of the patented compounds.

• ANDA Litigation: One notable case is Otsuka Pharmaceutical Co., Ltd. v. MSN Labs. Pvt. Ltd., where Otsuka asserted that MSN's Abbreviated New Drug Application (ANDA) would infringe on the patents, including US 8,349,840. The settlement terms included the dismissal of affirmative defenses and counterclaims without prejudice, with each party bearing its own costs[5].

Validity and Enforceability

The validity and enforceability of the patent have been upheld in several legal proceedings. The asserted claims of the patents-in-suit, including US 8,349,840, have been found not to be invalid or unenforceable. This reinforces the patent's strength and Otsuka's ability to protect its intellectual property[5].

Impact on the Pharmaceutical Industry

The patent has significant implications for the pharmaceutical industry, particularly in the development of antipsychotic medications. By protecting the intellectual property related to these compounds, Otsuka ensures that it can continue to invest in research and development without immediate generic competition.

Future Implications

As the patent approaches its expiration date, generic manufacturers will likely increase their efforts to challenge the patent or develop non-infringing alternatives. This could lead to a more competitive market for antipsychotic medications, potentially benefiting patients through lower prices and increased treatment options.

Conclusion

The United States Patent 8,349,840 is a crucial piece of intellectual property in the pharmaceutical sector, particularly for the treatment of mental disorders. Its scope, claims, and the surrounding patent landscape highlight the complex interplay between innovation, legal protection, and market competition.

Key Takeaways

• Chemical Structure: The patent covers piperazine-substituted benzothiophenes with specific molecular structures.
• Therapeutic Use: These compounds are designed to treat mental disorders such as schizophrenia and bipolar disorder.
• Claims: The patent includes both independent and dependent claims that define the scope of the invention.
• Patent Scope: The patent's scope is balanced between breadth and specificity, ensuring robust intellectual property protection.
• Litigation: Otsuka has successfully defended the patent against generic manufacturers in several legal cases.
• Validity and Enforceability: The patent has been found valid and enforceable in various legal proceedings.

FAQs

Q: What is the main purpose of the United States Patent 8,349,840? A: The main purpose is to provide antipsychotic drugs with a wider treatment spectrum, fewer side effects, and excellent tolerability.

Q: What class of compounds does the patent cover? A: The patent covers piperazine-substituted benzothiophenes.

Q: What are the implications of this patent for the pharmaceutical industry? A: The patent protects Otsuka's intellectual property, allowing continued investment in research and development, and impacts the competitive landscape for antipsychotic medications.

Q: Has the patent been involved in any significant litigation? A: Yes, Otsuka has been involved in several patent infringement cases, including against generic drug manufacturers.

Q: What is the current legal status of the patent? A: The patent has been found valid and enforceable in various legal proceedings.

Sources

1. US8349840B2 - Piperazine-substituted benzothiophenes for treatment of mental disorders - Google Patents
2. Case 1:19-cv-01955-UNA Document 1 Filed 10/15/19 - RPX Insight
3. Patent Claims and Patent Scope - Hoover Institution
4. US8349840B2 - Piperazine-substituted benzothiophenes for treatment of mental disorders - Google Patents
5. ANDA Litigation Settlements | Hatch-Waxman - Robins Kaplan LLP

Drugs Protected by US Patent 8,349,840

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Otsuka	REXULTI	brexpiprazole	TABLET;ORAL	205422-001	Jul 10, 2015	AB	RX	Yes	No					Y
Otsuka	REXULTI	brexpiprazole	TABLET;ORAL	205422-002	Jul 10, 2015	AB	RX	Yes	No					Y
Otsuka	REXULTI	brexpiprazole	TABLET;ORAL	205422-003	Jul 10, 2015	AB	RX	Yes	No					Y
Otsuka	REXULTI	brexpiprazole	TABLET;ORAL	205422-004	Jul 10, 2015	AB	RX	Yes	Yes					Y
Otsuka	REXULTI	brexpiprazole	TABLET;ORAL	205422-005	Jul 10, 2015	AB	RX	Yes	No					Y
Otsuka	REXULTI	brexpiprazole	TABLET;ORAL	205422-006	Jul 10, 2015	AB	RX	Yes	No					Y

Foreign Priority and PCT Information for Patent: 8,349,840

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Japan	2005-116698	Apr 14, 2005

International Family Members for US Patent 8,349,840

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1869025		300946	Netherlands
European Patent Office	1869025		122018000088	Germany
European Patent Office	1869025		PA2018509	Lithuania
European Patent Office	1869025		CA 2018 00028	Denmark
European Patent Office	1869025		LUC00086	Luxembourg
European Patent Office	1869025		32/2018	Austria
European Patent Office	1869025		2018C/037	Belgium