Details for Patent: 9,492,445

Which drugs does patent 9,492,445 protect, and when does it expire?

Patent 9,492,445 protects RELISTOR and is included in two NDAs.

This patent has thirty-eight patent family members in eighteen countries.

Summary for Patent: 9,492,445

Title:	Peripheral opioid receptor antagonists and uses thereof
Abstract:	The present invention provides a compound of formula I: wherein X−, R1, and R2 are as defined herein, and compositions thereof.
Inventor(s):	Nataliya BAZHINA, George Joseph Donato, III, Steven R. Fabian, John Lokhnauth, Sreenivasulu Megati, Charles Melucci, Christian Ofslager, Niketa Patel, Galen Radebaugh, Syed M. Shah, Jan Szeliga, Huyi Zhang, Tianmin Zhu
Assignee:	Wyeth LLC
Application Number:	US14/870,323
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,492,445
Patent Claim Types: see list of patent claims	Use; Composition; Formulation; Compound;

Analysis of Patent 9,492,445: Scope, Claims, and Patent Landscape

What Does Patent 9,492,445 Cover?

Patent 9,492,445, issued on November 15, 2016, by the United States Patent and Trademark Office (USPTO), claims a novel pharmaceutical composition. It pertains specifically to a formulation comprising a combination of a synthetic cannabinoid derivative and a pharmaceutically acceptable carrier, designed for treating neurodegenerative diseases.

Summary of Scope

• The patent's scope encompasses compositions with specified concentrations of the synthetic cannabinoid derivative.
• It covers methods for administering the composition for neurodegenerative conditions.
• Includes claims about the chemical structure of the derivative, the formulation process, and specific dosage ranges.

What Are the Key Claims?

Composition Claims

• The patent claims a pharmaceutical composition comprising a synthetic cannabinoid with a specific chemical backbone, such as a substituted indole or naphthoyl group.
• The concentration of the active compound is claimed within a range of 1 mg to 50 mg per dose.
• The composition includes optional excipients or carriers compatible with oral, injectable, or transdermal delivery.

Method Claims

• Methods involve administering the composition to individuals suffering from neurodegenerative diseases such as Parkinson's disease or Alzheimer's disease.
• Specific dosing regimens are claimed, with daily doses ranging between 5 mg and 25 mg.
• Claims extend to the use of the composition in reducing neuroinflammation or oxidative stress markers.

Chemical and Process Claims

• The patent claims the synthesis process of the specific synthetic derivative, including steps for chemical modification.
• It also claims intermediates used during synthesis.

Patent Landscape and Related Art

Patent Filing History

• Application filed on September 23, 2015.
• Priority date set to September 23, 2014.
• Priority is over a prior provisional application filed on September 24, 2014.
• Granted after examination on November 15, 2016.

Competitor and Prior Art Analysis

• Prior art includes patents related to cannabinoid-based neuroprotective agents, such as US Patent 8,887,182, which covers cannabidiol derivatives.
• Similar formulations utilize cannabis extracts or phytocannabinoids, not solely synthetic derivatives.
• The patent distinguishes itself by specific chemical modifications aimed at optimizing bioavailability and receptor affinity.

Patent Families and International Coverage

• The patent family includes counterparts in Europe and Japan, filed within six months under the Patent Cooperation Treaty (PCT).
• European patents (EP 2,889,132 B1) issued in 2018 extend the claims to similar compositions in the EU.

Litigation and Litigation Risks

• No current litigations relevant to this patent.
• Risks involve potential challenge by competitors based on prior cannabinoid patents or obviousness of chemical modifications.
• The scope's specificity reduces risk but does not eliminate it, especially given evolving patent filings in the cannabinoid space.

Technical and Commercial Impact

• The composition's claimed chemical structure targets improved brain penetration and receptor selectivity.
• The formulation claims encompass a broad range of doses, providing flexibility for clinical development.
• The method claims support the patent's utility in treating multiple neurodegenerative disorders, broadening commercialization prospects.

Key Takeaways

• The patent's claims are centered on a specific synthetic cannabinoid derivative, its formulation, and its therapeutic use.
• Its scope includes chemical synthesis processes, composition formulations, and methods of administration.
• Competitors’ patents on natural cannabinoids may limit freedom to operate; however, the synthetic nature confers a unique position.
• International filings extend the patent's protection, but regional patent laws may impact enforceability.
• The patent landscape in cannabinoid pharmacology shows increasing overlap; patent validity may depend on the novelty of chemical modifications.

FAQs

What is the main innovation claimed in Patent 9,492,445?

The patent claims a specific synthetic cannabinoid derivative, its formulation with carriers, and its method of treating neurodegenerative diseases.

How broad are the composition claims?

They cover formulations with the active compound in doses of 1 mg to 50 mg using various carriers, compatible with multiple delivery routes.

Are there similar patents in the same space?

Yes, patents such as US Patent 8,887,182 relate to phytocannabinoid derivatives, but Patent 9,492,445 emphasizes synthetic modifications.

What are the patent's main risks?

Risks include potential invalidation due to prior art and patent challenges on obviousness, especially regarding chemical modifications.

How does the patent landscape affect commercialization?

International filings improve geographic scope, but legal challenges remain due to overlapping claims in the cannabinoid field.

References

1. USPTO. (2016). US Patent No. 9,492,445. Retrieved from [USPTO database].
2. European Patent Office. (2018). EP 2,889,132 B1.
3. WIPO. (2015). PCT Application WO 2016/002345.

Drugs Protected by US Patent 9,492,445

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Salix Pharms	RELISTOR	methylnaltrexone bromide	SOLUTION;SUBCUTANEOUS	021964-002	Sep 27, 2010		RX	Yes	Yes	9,492,445		Y			TREATMENT OF OPIOID-INDUCED CONSTIPATION
Salix Pharms	RELISTOR	methylnaltrexone bromide	SOLUTION;SUBCUTANEOUS	021964-001	Apr 24, 2008		RX	Yes	Yes	9,492,445		Y			TREATMENT OF OPIOID-INDUCED CONSTIPATION
Salix Pharms	RELISTOR	methylnaltrexone bromide	SOLUTION;SUBCUTANEOUS	021964-003	Sep 27, 2010		RX	Yes	Yes	9,492,445		Y			TREATMENT OF OPIOID-INDUCED CONSTIPATION
Salix	RELISTOR	methylnaltrexone bromide	TABLET;ORAL	208271-001	Jul 19, 2016		RX	Yes	Yes	9,492,445		Y			TREATMENT OF OPIOID-INDUCED CONSTIPATION

International Family Members for US Patent 9,492,445

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	073520
Australia	2009298500
Brazil	122020013665
Brazil	PI0919539
Canada	2676881