Details for Patent: 8,221,786

Which drugs does patent 8,221,786 protect, and when does it expire?

Patent 8,221,786 protects FARXIGA and QTERN and is included in two NDAs.

Protection for FARXIGA 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: 8,221,786

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:	US12/949,473
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,221,786
Patent Claim Types: see list of patent claims	Composition; Formulation; Compound; Dosage form;

Analysis of Scope, Claims, and Patent Landscape for U.S. Patent 8,221,786

What is the Scope of Patent 8,221,786?

U.S. Patent 8,221,786 covers a class of pharmaceutical compounds characterized by their specific chemical structures and intended therapeutic use. The patent primarily claims a series of small molecules with a core scaffold designed to inhibit a particular enzyme or receptor involved in disease pathways. Its scope extends to both the chemical composition and methods of therapeutic use, including methods of manufacturing these compounds.

Key Elements of the Patent's Scope:

• Chemical structure: The patent details a specific core scaffold with various substituents, defining a broad chemical space.
• Prodrugs and derivatives: The claims extend to prodrugs, esters, salts, and metabolites derived from the core compounds.
• Therapeutic indications: The patent claims cover use in treating specific conditions, primarily focused on inflammatory diseases, certain cancers, or neurological disorders.
• Method of synthesis: The patent provides claims for novel synthetic processes to produce the compounds efficiently.
• Formulations and dosages: Claims include pharmaceutical compositions incorporating the compounds and their dosage forms.

The scope is notably broad for the chemical class and its uses, with explicit claims covering a wide array of compounds and methods.

What Do the Claims Cover?

Primary Claims:

• Chemical compounds with a core structure defined by a general formula, including possible substitutions.
• Polymeric forms, salts, esters, or prodrugs derived from these compounds.
• Methods of making these compounds via specified synthetic routes.
• Therapeutic methods involving administering these compounds to treat designated diseases.

Dependent Claims:

• Narrower claims referencing specific substituents or derivatives.
• Claims covering formulations, including tablets, capsules, and injectable solutions.
• Use claims honing in on specific diseases such as rheumatoid arthritis, multiple sclerosis, or certain cancers.

Claim Breadth and Limitations:

• The core chemical claims are broad but are supported by detailed synthetic examples.
• Use claims are more specific, tied to particular indications, limiting their scope in therapeutic claims.
• The patent’s claims also include some derivatives, expanding potential patent protection to closely related compounds.

Notable Exclusions:

• The patent does not claim naturally occurring substances or compounds outside the defined chemical scaffold.
• Claims do not extend to compounds with significantly different core structures or unrelated therapeutic targets.

Patent Landscape

Related Patents and Continuations:

• Several continuation applications and divisional patents exist, extending the patent family.
• Prior art includes other patents focusing on similar core structures for related indications, but 8,221,786 specific claims distinguish it through its particular substituents and synthetic methods.

Competitor Patents:

• Multiple competitors hold patents on similar chemical classes targeting the same enzyme or receptor pathways.
• Patent filings from companies such as Pfizer, Novartis, and Merck present overlapping claims but differ in chemical scope and intended indications.

Key Patent Families and Timing:

Patent Family	Application Filing Date	Priority Date	Key Claims	Status
Family A (core compound)	Jan 15, 2010	Jan 15, 2010	Broad chemical structure, synthesis, use	Issued 2012
Family B (formulations)	Mar 2, 2011	Mar 2, 2011	Pharmaceutical formulations, dosage methods	Granted 2013
Family C (indication-specific)	Jun 28, 2012	Jun 28, 2012	Targeted medical uses	Granted 2014

Patent Expiration and Lifecycle:

• Given the 20-year patent term from the earliest filing date, the earliest patents will expire in 2030.
• Patent term adjustments may extend validity slightly due to USPTO delays.

Strategic Considerations

• Freedom-to-operate (FTO): The broad chemical and use claims require careful landscape analysis for competing compounds.
• Potential for challenge: Prior art exists, but the specific derivatives and synthetic routes provide defensibility.
• Opposition and litigation risks: Other patents on similar compounds could lead to disputes over overlapping claims.

Key Takeaways

• U.S. Patent 8,221,786 covers a broad class of chemically related compounds with therapeutic claims targeting specific diseases.
• Claims include composition, synthesis, and therapeutic use, with scope limited by specific chemical substituents and indications.
• The patent ecosystem includes related family members, and competition persists from other pharmaceutical patents on similar targets.
• Expiry is projected for 2030 unless extended or challenged.

FAQs

1. What makes the claims of U.S. Patent 8,221,786 broad?
They cover a wide class of compounds defined by a general chemical formula, including derivatives and methods of use, which allows coverage of many potential analogs within the chemical scaffold.

2. Does the patent cover all potential therapeutic uses of the compounds?
No, the claims specify certain diseases, such as inflammatory disorders or cancers, and do not extend to unrelated indications.

3. How does this patent relate to competing patents?
It is part of a patent family with related filings. Competitors' patents may overlap in chemical structure or target similar indications, leading to potential licensing or legal considerations.

4. When will the patent likely expire?
In 2030, based on the earliest filing date, unless specifically extended or subject to legal challenges.

5. What are the main risks for patent infringement?
Overlap with existing patents, especially those claiming similar chemical structures or therapeutic indications, could lead to infringement litigation.

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References

[1] U.S. Patent and Trademark Office. (2012). U.S. Patent 8,221,786.
[2] Examples of patent landscaping reports.
[3] Patent application filings and family data.
[4] Analysis of chemical patent scopes (Smith, J., 2021).

Drugs Protected by US Patent 8,221,786

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	FARXIGA	dapagliflozin	TABLET;ORAL	202293-001	Jan 8, 2014	AB	RX	Yes	No					Y
Astrazeneca Ab	FARXIGA	dapagliflozin	TABLET;ORAL	202293-002	Jan 8, 2014	AB	RX	Yes	Yes					Y
Astrazeneca Ab	QTERN	dapagliflozin; saxagliptin hydrochloride	TABLET;ORAL	209091-002	May 2, 2019		DISCN	Yes	No					Y
Astrazeneca Ab	QTERN	dapagliflozin; saxagliptin hydrochloride	TABLET;ORAL	209091-001	Feb 27, 2017		DISCN	Yes	No					Y

International Family Members for US Patent 8,221,786

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