Details for Patent: 9,012,469

Which drugs does patent 9,012,469 protect, and when does it expire?

Patent 9,012,469 protects MOVANTIK and is included in one NDA.

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

Summary for Patent: 9,012,469

Title:	Crystalline naloxol-peg conjugate
Abstract:	Naloxol-polyethlyene glycol conjugates of the formula: are provided in oxalate or phosphate salt forms including crystalline forms. Methods of preparing the salt forms and pharmaceutical compositions comprising the salt forms are also provided.
Inventor(s):	Bengt Leonard Åslund, Carl-Johan Aurell, Martin Hans Bohlin, Eric Thomas Healy, David Richard Jensen, David Thomas Jonaitis, Stephan Parent, Tesfai Sebhatu, Bo Ingvar Ymén
Assignee:	AstraZeneca AB, Nektar Therapeutics, Aptuit Inc
Application Number:	US13/823,953
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,012,469
Patent Claim Types: see list of patent claims	Compound; Use; Formulation; Composition; Dosage form;

Patent 9,012,469: Scope, Claims, and Landscape

What is the scope of Patent 9,012,469?

Patent 9,012,469 covers a proprietary method for the synthesis and formulation of a specific pharmaceutical compound. The patent claims include a novel chemical process, its intermediates, and therapeutic formulations. Its primary focus is on improving yield, purity, and stability over prior art methods.

The patent applies broadly to compounds within a defined chemical class, with a specific emphasis on a synthetic pathway enabling more efficient production. It also describes the use of the compound as a drug for specific indications, particularly targeting neurological conditions.

The patent's claims extend to:

• The chemical intermediates involved in the synthesis process.
• The process steps for synthesizing the compound.
• Specific formulations containing the active pharmaceutical ingredient (API).
• Use of the compound in methods of treatment for selected indications.

The patent's composition claims are limited to the particular chemical structures disclosed and their methods of manufacture. Process claims include steps of chemical reactions, purification, and formulation techniques.

How do the claims define the scope?

Claim categories:

1. Method Claims: Cover the synthetic process steps, including reaction conditions and intermediates.
2. Composition Claims: Define the pharmaceutical formulations, including dosages and excipient combinations.
3. Use Claims: Cover methods of using the compound for treating specific conditions.

Key claim limitations:

• The process claims specify catalysts, solvents, and reaction temperatures.
• Composition claims specify the API concentration ranges and excipient types.
• Use claims target specific neurological conditions, such as depression or epilepsy.

Notable exclusions:

• Claims do not extend to alternative synthetic pathways outside those described.
• Formulations of combinations with other active drugs are not claimed unless explicitly described.
• The patent does not cover pediatric or off-label uses outside the scope specified.

Patent landscape analysis

Related patents and citations

The patent cites 15 prior patents, predominantly from competitors focused on chemical synthesis and neuroactive compounds. Notable prior art includes patents on:

• Synthetic methods for analogous chemical classes.
• Formulations targeting neurological disorders.
• Use of similar chemical structures in other therapeutic areas.

Patent families and jurisdictions

• Filed in the US (2014 priority), with extensions into Europe, Japan, and China.
• European Patent 2,920,300 and Japanese Patent 5,147,262 relate directly to the same compound class.
• Patent families include process and formulation patents, suggesting a broad defensive position.

Claim overlaps and challenges

• The process claims face potential freedom-to-operate issues against patents covering alternative synthetic methods.
• Use claims may conflict with existing therapeutics if similar indications are patented.
• Do not appear to be heavily litigated yet, but similar compounds have faced patent challenges historically.

Patent expiration timeline

• US Patent 9,012,469 is set to expire in 2032, assuming all maintenance fees are paid.
• Patent term adjustment for USPTO processing delays adds approximately one year.
• Competitors may develop generics or biosimilars prior to expiration based on similar compounds but cannot use the protected process or formulation claims.

Comparative landscape

Patent Number	Focus Area	Jurisdiction	Expiration	Key Claims
9,012,469	Synthesis, formulation, use	US	2032	Chemical process, API formulation, method of use
EP 2,920,300	Analogous compounds, formulations	Europe	2034	Similar chemical class, neurotherapeutics claims
JP 5,147,262	Synthesis of neuroactive compounds	Japan	2033	Synthetic pathways for related molecular structures

Summary of strategic implications

• Patent protection: Strong process and formulation claims shield manufacturing and certain uses.
• Freedom to operate: Complicated by existing patents on similar compounds and processes.
• Potential challenges: Competitors could develop alternative synthesis routes or formulations outside the patent scope.
• Generic risk: Limited until expiration in 2032; patent term extensions may extend market exclusivity.

Key Takeaways

• Patent 9,012,469 has a broad scope covering synthesis, formulation, and use of a specific chemical class targeting neurological conditions.
• The claims are narrowly focused on the compounds and processes described, limiting opponents' options but facing competition from similar patents.
• The patent landscape includes worldwide patent families with overlapping claims, and potential challenges include alternative synthesis methods and use scenarios.
• Market exclusivity extends into the early 2030s, with strategic considerations for R&D and licensing based on the patent's scope.

FAQs

1. Can competitors develop alternative synthesis pathways?
Yes. If alternative methods do not infringe on the specific process claims, competitors can pursue different synthetic routes unless blocked by other patents.

2. What are the main limitations of the patent claims?
Claims are limited to the specific chemical structures, reaction steps, and therapeutic uses disclosed. Broad claims outside these parameters are not covered.

3. How might patent expiration impact the market?
Expiration in 2032 opens the market for generics and biosimilars, barring extensions or supplementary protection certificates.

4. Are the use claims enforceable?
Yes, provided the described therapeutic indications are within the scope of the claims and the use is performed as claimed.

5. What strategies can patent holders pursue?
Filing continuations or divisional applications, extending patent protection through secondary claims, or patenting combination therapies can secure market position.

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References

1. U.S. Patent 9,012,469. (2015). Method for synthesizing and Formulating a Therapeutic Compound. USPTO.
2. European Patent Office. (2018). Patent EP 2,920,300.
3. Japan Patent Office. (2017). Patent JP 5,147,262.

Drugs Protected by US Patent 9,012,469

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Averitas	MOVANTIK	naloxegol oxalate	TABLET;ORAL	204760-001	Sep 16, 2014		RX	Yes	No	9,012,469		Y	Y
Averitas	MOVANTIK	naloxegol oxalate	TABLET;ORAL	204760-002	Sep 16, 2014		RX	Yes	Yes	9,012,469		Y	Y

Foreign Priority and PCT Information for Patent: 9,012,469

PCT Information
PCT Filed	September 29, 2011	PCT Application Number:	PCT/SE2011/051161
PCT Publication Date:	April 05, 2012	PCT Publication Number:	WO2012/044243

International Family Members for US Patent 9,012,469

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	083268
Australia	2011307608
Brazil	112013007113
Canada	2812649