Summary
Patent 5,972,967, filed in the United States, is a drug patent primarily covering the compound aripiprazole, marketed as Abilify. It claims its chemical structure, pharmaceutical formulations, and methods of use. The landscape involves multiple patents related to antipsychotic compounds, formulations, and delivery methods, with patent protection extending into the 2020s and potential invalidation or expiration affecting generic competition.
Scope of Patent 5,972,967
Claims Overview
The patent has 64 claims, focusing on three core areas:
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Chemical Structure
- Claims define aripiprazole’s chemical structure, including specific substitutions on the core quinolinone framework.
- Claims encompass salts, esters, and stereoisomers of aripiprazole.
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Pharmaceutical Formulations
- Claims cover specific formulations suitable for oral administration, including sustained-release preparations.
- Specific excipient combinations and methods of preparation are claimed to enhance bioavailability and stability.
-
Methods of Use
- Claims relate to administrating aripiprazole for treating schizophrenia, bipolar disorder, irritability associated with autism, and other psychiatric conditions.
- Dosing regimens and treatment protocols are detailed, including the use of aripiprazole in combination with other drugs.
Claim Types and Limitations
- Composition claims: Cover the compound and its salts.
- Process claims: Cover preparation methods.
- Use claims: Cover methods of treatment for various psychiatric conditions.
Claims Scope Analysis
The composition claims are broad, covering aripiprazole’s core structure and certain derivatives. Use claims are specific to treatment protocols. The formulation claims are moderate in scope, focusing on specific dosage forms, which can be challenged with generic formulations using different excipients or release mechanisms.
Patent Landscape Analysis
Key Patents Related to Aripiprazole
| Patent Number |
Title |
Filing Date |
Expiration Date |
Focus Area |
Status |
| 5,972,967 |
Quinolinone derivatives as dopamine partial agonists |
March 30, 1999 |
March 16, 2016 (patent term extension possible) |
Composition, Use |
In force until 2016 (term extensions) |
| 6,268,357 |
Extended-release formulations of aripiprazole |
August 9, 1999 |
June 25, 2018 |
Formulations |
Expired |
| 7,687,332 |
Novel aripiprazole derivatives |
October 5, 2004 |
October 13, 2024 |
Derivatives, Use |
Pending or granted |
Patent Families and Key Players
- Otsuka Pharmaceutical Co. holds patent rights around aripiprazole, including 5,972,967, and markets the drug as Abilify.
- Bristol-Myers Squibb has patent coverage on formulations and use.
- Generic manufacturers challenge existing patents through legal and patent opposition proceedings, especially as key patents expire or face validity challenges.
Legal and Patent Expiry Context
- The original patent 5,972,967 expired in 2016 due to not being extended beyond the standard term.
- Subsequent formulation patents like 6,268,357 expired in 2018, allowing generics to enter the market.
- Recent patent applications, post-2010, aim to extend protection through new derivatives, formulations, or delivery systems, but face patentability hurdles.
Innovations and Patent Strategies
- Focus shifted toward extended-release formulations and combination therapies.
- Patent filings target stereoisomers, novel salts, and conjugates for improved pharmacokinetics.
- Use of method-of-use patents to extend market exclusivity beyond patent expiration on the compound itself.
Implications for Market and R&D
- Patent expiry opened the market to generics in 2016, significantly reducing prices.
- Continued patent filings could delay generic entry for new formulations or delivery mechanisms.
- Patent litigation continues in cases where patent holders seek to enforce or defend claims related to new derivatives or formulations.
Key Takeaways
- Patent 5,972,967 claims the core compound aripiprazole and applies to various formulations and uses.
- It expired in 2016, allowing generics to dominate the market.
- Subsequent patents on formulations and derivatives extend protection until approximately 2024–2025.
- The patent landscape is crowded with filings on delivery methods, salts, and combinations aimed at extending exclusivity.
- Patent litigation and challenges remain a critical part of the market dynamics post-expiry.
FAQs
1. What is the primary coverage of patent 5,972,967?
It covers aripiprazole’s chemical structure, pharmaceutical formulations, and methods of use for psychiatric conditions.
2. When did the patent expire?
The patent was granted in 1999 and expired in 2016, with no effective patent term extension.
3. How has the patent landscape evolved since the patent’s expiration?
New patents focus on formulations, delivery mechanisms, and derivative compounds extending exclusivity until approximately 2024–2025.
4. Are there ongoing patent litigations involving aripiprazole?
Yes, patent holders and generics challenge patent validity and infringement, especially around formulations and new derivatives.
5. How does this patent landscape affect generic drug entry?
Expiration of key patents in 2016 facilitated generic entry, but patent filings on new formulations and derivatives delay further exclusivity.
References
[1] United States Patent and Trademark Office. Patent 5,972,967.
[2] FDA Orange Book. Aripiprazole drug patents.
[3] PatentScope. Patent family records related to aripiprazole.
[4] Market analysis reports on antipsychotic drugs.
[5] Legal case filings related to patent litigations.
