Details for Patent: 8,399,469

Which drugs does patent 8,399,469 protect, and when does it expire?

Patent 8,399,469 protects ABILIFY MAINTENA KIT and ABILIFY ASIMTUFII and is included in two NDAs.

This patent has one hundred and seventy patent family members in thirty-three countries.

Summary for Patent: 8,399,469

Title:	Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
Abstract:	The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous aripiprazole crystals is stored for an extended period.
Inventor(s):	Bando; Takuji (Tokushima, JP), Aoki; Satoshi (Naruto, JP), Kawasaki; Junichi (Tokushima, JP), Ishigami; Makoto (Tokushima, JP), Taniguchi; Youichi (Tokushima, JP), Yabuuchi; Tsuyoshi (Tokushima, JP), Fujimoto; Kiyoshi (Naruto, JP), Nishioka; Yoshihiro (Tokushima, JP), Kobayashi; Noriyuki (Tokushima, JP), Fujimura; Tsutomu (Naruto, JP), Takahashi; Masanori (Tokushima, JP), Abe; Kaoru (Tokushima, JP), Nakagawa; Tomonori (Tokushima, JP), Shinhama; Koichi (Tokushima, JP), Utsumi; Naoto (Naruto, JP), Tominaga; Michiaki (Tokushima, JP), Ooi; Yoshihiro (Tokushima, JP), Yamada; Shohei (Tokushima, JP), Tomikawa; Kenji (Tokushima, JP)
Assignee:	Otsuka Pharmaceutical Co., Ltd. (Chiyoda-ku, Tokyo, JP)
Application Number:	11/790,604
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,399,469
Patent Claim Types: see list of patent claims	Process; Formulation;

United States Patent 8,399,469: A Detailed Analysis of Scope, Claims, and Patent Landscape

Introduction

The United States Patent 8,399,469, titled "Low hygroscopic aripiprazole drug substance and processes for the preparation thereof," is a significant patent in the pharmaceutical industry, particularly in the field of psychiatric medications. This patent, held by Otsuka Pharmaceutical Co., Ltd. and H. Lundbeck A/S, pertains to the formulation and preparation of aripiprazole, a drug commonly used to treat schizophrenia, bipolar disorder, and major depressive disorder.

Background of Aripiprazole

Aripiprazole is an atypical antipsychotic medication that has been widely used since its approval by the FDA in 2002. However, one of the challenges associated with aripiprazole is its hygroscopic nature, which can lead to the formation of hydrates and affect the drug's stability and efficacy.

Patent Overview

Invention Description

The patent 8,399,469 describes low hygroscopic forms of aripiprazole and the processes for their preparation. These forms are designed to prevent the conversion to hydrates and maintain the drug's stability under various environmental conditions[1][4].

Claims

The patent includes multiple claims that define the scope of the invention. These claims cover:

• Composition Claims: Specific formulations of aripiprazole that are low in hygroscopicity.
• Process Claims: Methods for preparing these low hygroscopic forms of aripiprazole.
• Use Claims: The use of these formulations in pharmaceutical products.

Scope of the Patent

Independent Claim Length and Count

The scope of the patent can be analyzed using metrics such as independent claim length and independent claim count. These metrics help in understanding the breadth and clarity of the patent claims. For instance, narrower claims with shorter lengths and fewer independent claims are generally associated with higher grant rates and shorter examination processes[3].

Claim Construction

The claim construction process is crucial in determining the meaning and scope of the patent claims. This process involves interpreting the language of the claims to establish what is covered by the patent and what is not. In the context of patent 8,399,469, the claim construction would focus on the specific formulations and processes described to ensure that any potential infringers are clearly identified[5].

Patent Landscape

Related Patents

The patent 8,399,469 is part of a larger portfolio of patents related to aripiprazole. Other patents, such as U.S. Patent Nos. 7,807,680, 8,030,313, and 8,722,679, also cover various aspects of aripiprazole formulations and processes. These patents collectively form a robust intellectual property protection strategy for Otsuka and Lundbeck[2].

Litigation and Enforcement

The patent has been involved in several litigation cases, particularly against generic drug manufacturers. For example, Otsuka and Lundbeck have filed complaints against Mylan Laboratories Limited, Viatris Inc., and Mylan Pharmaceuticals Inc. for alleged patent infringement related to their Abbreviated New Drug Application (ANDA) filings. These lawsuits highlight the importance of this patent in protecting the intellectual property rights of the original drug developers[2].

Impact on the Pharmaceutical Industry

Innovation and Competition

The patent 8,399,469 has significant implications for innovation and competition in the pharmaceutical industry. By protecting the specific formulations and processes of low hygroscopic aripiprazole, it ensures that the original developers can recoup their investment in research and development. However, it also limits the entry of generic competitors, which can affect the availability and affordability of the drug[3].

Regulatory Compliance

Compliance with this patent is crucial for any company seeking to manufacture or market aripiprazole. The FDA approval process for generic versions of the drug must ensure that the formulations do not infringe on the claims of this patent, adding a layer of complexity to the regulatory landscape[2].

Challenges and Criticisms

Patent Quality and Scope

There have been debates about the quality and scope of pharmaceutical patents, including those related to aripiprazole. Critics argue that overly broad or unclear claims can stifle innovation and lead to unnecessary litigation costs. However, the metrics used to measure patent scope, such as independent claim length and count, suggest that the claims in patent 8,399,469 are relatively specific and well-defined[3].

Hygroscopicity and Drug Stability

The primary challenge addressed by this patent is the hygroscopic nature of aripiprazole. The low hygroscopic forms described in the patent are crucial for maintaining the drug's stability and efficacy. This innovation is a significant advancement in pharmaceutical formulation technology[1][4].

Conclusion

The United States Patent 8,399,469 is a critical component of the intellectual property portfolio for aripiprazole, ensuring the stability and efficacy of this important psychiatric medication. The patent's scope, claims, and the surrounding patent landscape highlight its significance in protecting innovation and regulating competition in the pharmaceutical industry.

Key Takeaways

• Low Hygroscopic Forms: The patent describes specific formulations of aripiprazole that are low in hygroscopicity, ensuring the drug's stability.
• Process and Composition Claims: The patent covers both the processes for preparing these forms and the compositions themselves.
• Litigation and Enforcement: The patent has been involved in several litigation cases to protect against generic infringement.
• Impact on Industry: The patent affects innovation, competition, and regulatory compliance in the pharmaceutical industry.
• Challenges and Criticisms: The patent faces scrutiny regarding patent quality and scope, but its specific claims are well-defined.

FAQs

Q: What is the main focus of the United States Patent 8,399,469?

A: The main focus is on low hygroscopic forms of aripiprazole and the processes for their preparation.

Q: Why is the hygroscopic nature of aripiprazole a concern?

A: The hygroscopic nature can lead to the formation of hydrates, affecting the drug's stability and efficacy.

Q: What metrics are used to analyze the scope of the patent?

A: Metrics such as independent claim length and independent claim count are used to analyze the scope.

Q: Has the patent been involved in any litigation?

A: Yes, it has been involved in several litigation cases against generic drug manufacturers.

Q: How does the patent impact the pharmaceutical industry?

A: It affects innovation, competition, and regulatory compliance by protecting the intellectual property rights of the original developers.

Drugs Protected by US Patent 8,399,469

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 Pharm Co Ltd	ABILIFY MAINTENA KIT	aripiprazole	FOR SUSPENSION, EXTENDED RELEASE;INTRAMUSCULAR	202971-001	Feb 28, 2013		RX	Yes	No				Y
Otsuka Pharm Co Ltd	ABILIFY MAINTENA KIT	aripiprazole	FOR SUSPENSION, EXTENDED RELEASE;INTRAMUSCULAR	202971-003	Sep 29, 2014		RX	Yes	No				Y
Otsuka Pharm Co Ltd	ABILIFY MAINTENA KIT	aripiprazole	FOR SUSPENSION, EXTENDED RELEASE;INTRAMUSCULAR	202971-002	Feb 28, 2013		RX	Yes	Yes				Y
Otsuka Pharm Co Ltd	ABILIFY MAINTENA KIT	aripiprazole	FOR SUSPENSION, EXTENDED RELEASE;INTRAMUSCULAR	202971-004	Sep 29, 2014		RX	Yes	No				Y

Foreign Priority and PCT Information for Patent: 8,399,469

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Japan	2001-290645	Sep 25, 2001
Japan	2001-348276	Nov 14, 2001
Canada	2379005	Mar 27, 2002

International Family Members for US Patent 8,399,469

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	033485
Argentina	056503
Argentina	073111
Argentina	077635