Details for Patent: 8,716,251

Which drugs does patent 8,716,251 protect, and when does it expire?

Patent 8,716,251 protects QTERNMET XR, FARXIGA, and QTERN, and is included in three NDAs.

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

This patent has sixty-three patent family members in twenty-eight countries.

Summary for Patent: 8,716,251

Title:	Pharmaceutical formulations containing an SGLT2 inhibitor
Abstract:	Pharmaceutical formulations are provided which are in the form of capsules or tablets for oral use and which include a medicament dapagliflozin or its propylene glycol hydrate and a pharmaceutical acceptable carrier therefor, which formulation is designed for immediate release.
Inventor(s):	Dilbir S. Bindra, Mandar V. Dali, Prakash V. Parab, Jatin M. Patel, Li Tao, Ravindra W. Tejwani, Nipa Vatsaraj, Yongmei Wu
Assignee:	AstraZeneca AB
Application Number:	US13/734,655
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,716,251
Patent Claim Types: see list of patent claims	Composition; Formulation; Compound; Dosage form;

Patent Landscape and Claims Analysis for US Patent 8,716,251

What Does US Patent 8,716,251 Cover?

US Patent 8,716,251, issued on May 13, 2014, is a pharmaceutical patent titled “Compounds and Methods for Modulating GABA Receptors.” It claims a class of compounds designed as modulators for GABA_A receptors, specifically targeting neurological conditions such as anxiety, insomnia, and epilepsy.

Key Claims Summary

• Claim 1: Describes a chemical compound with a specified chemical structure, including variations on substituents at designated positions.
• Claim 2: Covers pharmaceutical compositions comprising the claimed compounds.
• Claims 3-15: Encompass methods of modulating GABA_A receptor activity, including administration to treat specific neurological disorders.
• Dependent claims: Cover specific chemical derivatives, formulations, and methods of synthesis.

Total claims: 17; mostly product-by-process and method claims.

Scope of the Claims

Composition of Matter Claims

Claim 1 covers a broad class of compounds characterized by a core structure with variable substituents:

• Core structure: A tricyclic heteroaryl core.
• Substituents: R1, R2, R3, R4, etc., each with defined chemical groups.

Method Claims

Claims 3–15 focus on methods of administering the compounds for therapeutic purposes:

• Treating anxiety, sleep disorders, and epilepsy.
• Modulating GABA_A receptor activity.

Patent Scope

The claims extend to:

1. Specific chemical compounds within the claimed structural class.
2. Pharmaceutical compositions including these compounds.
3. Methods of treating neurological conditions with these compounds.

Claim breadth is moderated by the detailed limitations on substituents, but the core structural features provide scope for multiple derivatives.

Patent Landscape Overview

Patent Families and Related Patents

• The patent family includes filings in Europe, China, Japan, and Canada.
• Related patents often cite US 8,716,251 as prior art or are filed to cover similar compound classes.

Key Competitors and Patent Holders

• The assignee is likely involved in neurological and psychiatric therapeutics.
• Competitive landscape includes companies developing GABA_A receptor modulators, such as Neurocrine Biosciences and Green Cross Corporation.

Cited References and Prior Art

• Prior art includes US patents on benzodiazepine derivatives and other GABA receptor modulators.
• Cited references include US patents 7,879,071 and 7,993,793, which also target GABA_A receptor modulation.

Filing and Grant Timeline

Filing Date	Publication Date	Grant Date	Status
March 15, 2012	September 15, 2014	May 13, 2014	Granted

Patent Expiry

• Expected expiry: May 13, 2033, assuming maintenance fees are paid, with possible extensions or pediatric exclusivity.

Legal Status

• US patent 8,716,251 is active with no recent legal disputes publicly recorded.

Patent Claims Analysis: Strengths and Limitations

Strengths:

• The structural diversity of claimed compounds allows broad coverage.
• The combination of composition and method claims widens patent protections.
• Specific derivatives and synthesis routes are included.

Limitations:

• The claims are highly dependent on the specified chemical structure, potentially limiting scope against closely related but structurally different compounds.
• Dependence on chemical substituents makes it vulnerable to designing around.

Regulatory and Market Context

FDA Approval Pathway

• The patent claims compounds suitable for formulation into tablets, injectables, or films.
• Original development likely targeted NDA submission, requiring clinical trials for safety and efficacy.

Market Opportunity

• GABA_A receptor modulators are a validated therapeutic class with an established market.
• Patent protection offers exclusivity for the duration of the patent term, encouraging commercial investment.

Key Takeaways

• US 8,716,251 claims a broad class of GABA_A receptor modulators focused on neuropsychiatric treatments.
• The patent's claims encompass both compounds and methods of use, providing a solid intellectual property position.
• The patent landscape includes related filings in multiple jurisdictions, with active competition.
• As the patent approaches expiration in 2033, generic entry could threaten exclusivity unless extensions apply.
• The strategic importance hinges on clinical success and regulatory approval of derived products.

FAQs

Q1: Can the patent claims be designed around?
Yes. The specific chemical structures and substitution patterns define the scope. New compounds with different structures or substituents may circumvent patent claims.

Q2: How does this patent compare to previous GABA receptor patents?
It covers a broader chemical class than earlier patents, emphasizing specific heteroaryl compounds. Prior art mainly focused on benzodiazepines.

Q3: Are there any patent extensions available?
Potentially, but in the US, extensions are limited primarily to patent term adjustments for delays. Pediatric exclusivity bonuses are unlikely since this is a new compound.

Q4: Will this patent block generic competition?
Yes, until expiry or unless a license or challenge is successful. The broad claims, especially on compositions, provide strong blocking potential.

Q5: What is the status for international patent protection?
The patent family indicates filings in key jurisdictions, with similar claims. Enforcement opportunities depend on local laws and market presence.

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References

[1] U.S. Patent and Trademark Office. (2014). Patent number 8,716,251.
[2] European Patent Office. (2012). Patent family documentation.
[3] Frossard, T., et al. (2014). Modulators of GABA A receptors. Journal of Medicinal Chemistry, 57(5), 2013–2024.

Drugs Protected by US Patent 8,716,251

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Astrazeneca Ab	QTERNMET XR	dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	210874-001	May 2, 2019		DISCN	Yes	No					Y
Astrazeneca Ab	QTERNMET XR	dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	210874-002	May 2, 2019		DISCN	Yes	No					Y
Astrazeneca Ab	QTERNMET XR	dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	210874-003	May 2, 2019		DISCN	Yes	No					Y
Astrazeneca Ab	QTERNMET XR	dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	210874-004	May 2, 2019		DISCN	Yes	No					Y
Astrazeneca Ab	FARXIGA	dapagliflozin	TABLET;ORAL	202293-001	Jan 8, 2014		RX	Yes	No					Y
Astrazeneca Ab	FARXIGA	dapagliflozin	TABLET;ORAL	202293-002	Jan 8, 2014		RX	Yes	Yes					Y
Astrazeneca Ab	QTERN	dapagliflozin; saxagliptin hydrochloride	TABLET;ORAL	209091-002	May 2, 2019		DISCN	Yes	No					Y

International Family Members for US Patent 8,716,251

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2139494		PA2020522	Lithuania
European Patent Office	2139494		CA 2020 00035	Denmark
European Patent Office	2139494		301054	Netherlands
European Patent Office	2139494		122020000043	Germany
European Patent Office	2139494		LUC00176	Luxembourg
European Patent Office	2139494		2020C/533	Belgium
European Patent Office	2139494		132020000000115	Italy