Details for Patent: 6,515,117

Which drugs does patent 6,515,117 protect, and when does it expire?

Patent 6,515,117 protects QTERNMET XR, QTERN, BYDUREON, BYDUREON PEN, BYDUREON BCISE, XIGDUO XR, and FARXIGA, and is included in six NDAs.

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

This patent has one hundred and fourteen patent family members in forty-one countries.

Summary for Patent: 6,515,117

Title:	C-aryl glucoside SGLT2 inhibitors and method
Abstract:	An SGLT2 inhibiting compound is provided having the formula ##STR1## A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above compound alone or in combination with another antidiabetic agent or other therapeutic agent.
Inventor(s):	Ellsworth; Bruce (Princeton, NJ), Washburn; William N. (Titusville, NJ), Sher; Philip M. (Plainsboro, NJ), Wu; Gang (Princeton, NJ), Meng; Wei (Pennington, NJ)
Assignee:	Bristol-Myers Squibb Company (Princeton, NJ)
Application Number:	10/151,436
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 6,515,117
Patent Claim Types: see list of patent claims	Compound; Composition; Use;

United States Patent 6,515,117: A Detailed Analysis of Scope, Claims, and Patent Landscape

Introduction

The United States Patent 6,515,117, titled "C-aryl glucoside SGLT2 inhibitors and method," is a significant patent in the field of diabetes treatment. This patent, granted on February 4, 2003, covers compounds and methods for treating diabetes and related diseases using SGLT2 inhibitors. Here is a comprehensive analysis of its scope, claims, and the surrounding patent landscape.

Inventors and Assignees

The patent was invented by a team of researchers including Bruce Ellsworth, Wei Meng, Philip M. Sher, William N. Washburn, and Gang Wu, all affiliated with various locations in New Jersey[1].

Scope of the Patent

SGLT2 Inhibitors

The patent focuses on C-aryl glucoside SGLT2 inhibitors, which are a class of drugs designed to inhibit the sodium-glucose cotransporter 2 (SGLT2). These inhibitors work by enhancing the excretion of glucose in the urine, thereby reducing plasma glucose levels in diabetic patients[4].

Chemical Structure

The patent describes specific chemical structures of these inhibitors, providing detailed formulas and methods for their synthesis. This includes compounds with specific C-aryl glucoside moieties that are crucial for their inhibitory activity[1][5].

Therapeutic Use

The primary therapeutic use of these compounds is in the treatment of diabetes and related diseases. By inhibiting SGLT2, these drugs help in managing blood glucose levels, which is essential for the management of type 2 diabetes[1][4].

Claims of the Patent

Compound Claims

The patent includes claims for the specific chemical compounds that act as SGLT2 inhibitors. These claims are detailed and cover various aspects of the compounds, including their structural formulas and stereochemistry[1][5].

Method Claims

In addition to the compound claims, the patent also includes method claims. These cover the use of these compounds in treating diabetes and related diseases, as well as methods for their synthesis and administration[1][5].

Patent Landscape

Related Patents

The patent landscape surrounding US 6,515,117 includes several related patents that also deal with SGLT2 inhibitors. For example, US 8,501,698 B2, granted to Bristol-Myers Squibb Company, covers crystal structures of SGLT2 inhibitors and processes for preparing them. This patent builds upon the foundational work described in US 6,515,117[4].

Litigation and Enforcement

The patent has been involved in litigation, particularly in cases related to generic competition. For instance, AstraZeneca AB has filed a complaint against Sun Pharmaceutical Industries Limited and Sun Pharmaceutical Industries, Inc., alleging patent infringement related to the submission of an Abbreviated New Drug Application (ANDA) for a generic version of a product that uses SGLT2 inhibitors[2].

Patent Citations and References

The patent is cited in several other patents and publications, indicating its influence in the field of diabetes treatment. It is referenced in patents such as US 8,501,698 B2, which further develops the concept of SGLT2 inhibitors[4].

Impact on Diabetes Treatment

Clinical Significance

The compounds and methods described in this patent have significant clinical implications. SGLT2 inhibitors have become a crucial class of drugs in the management of type 2 diabetes, offering a new mechanism of action that complements traditional therapies like metformin and insulin[4].

Market Presence

Drugs based on this patent, such as dapagliflozin (marketed as XIGDUO XR® by AstraZeneca), have gained substantial market presence. These drugs are widely prescribed and have been shown to improve glycemic control and reduce the risk of cardiovascular events in diabetic patients[2].

Patent Expiration and Generic Competition

Expiration Date

The patent's expiration date is critical for understanding the timeline for generic competition. Once the patent expires, generic versions of the drug can be approved and marketed, potentially changing the market dynamics[2].

Generic Challenges

Companies like Sun Pharmaceutical Industries have already begun the process of seeking approval for generic versions of SGLT2 inhibitors, which could lead to increased competition and reduced prices for these medications[2].

Conclusion

The United States Patent 6,515,117 is a pivotal patent in the field of diabetes treatment, particularly in the development and use of SGLT2 inhibitors. Its scope and claims cover specific compounds and methods that have been widely adopted in clinical practice. The patent landscape surrounding this invention includes related patents, litigation, and a significant impact on the treatment of diabetes.

Key Takeaways

• SGLT2 Inhibitors: The patent covers C-aryl glucoside SGLT2 inhibitors, which enhance glucose excretion in the urine.
• Therapeutic Use: These compounds are used primarily for treating diabetes and related diseases.
• Litigation: The patent has been involved in litigation related to generic competition.
• Clinical Impact: SGLT2 inhibitors have become a crucial class of drugs in diabetes management.
• Market Presence: Drugs based on this patent are widely prescribed and have a significant market presence.

FAQs

What is the primary mechanism of action of SGLT2 inhibitors?

SGLT2 inhibitors work by enhancing the excretion of glucose in the urine, thereby reducing plasma glucose levels in diabetic patients.

Who are the inventors of US Patent 6,515,117?

The inventors include Bruce Ellsworth, Wei Meng, Philip M. Sher, William N. Washburn, and Gang Wu.

What is the significance of this patent in diabetes treatment?

This patent covers compounds and methods that have led to the development of a new class of drugs (SGLT2 inhibitors) crucial for managing type 2 diabetes.

What is the current status of generic competition for SGLT2 inhibitors?

Companies like Sun Pharmaceutical Industries are seeking approval for generic versions, which could lead to increased competition and reduced prices.

How does the expiration of this patent affect the market?

Once the patent expires, generic versions of the drug can be approved and marketed, potentially changing market dynamics and reducing prices.

Sources

1. Patent Buddy: C-aryl glucoside SGLT2 inhibitors and method - Patent Buddy
2. Insight.rpxcorp.com: AstraZeneca AB, Plaintiff, v. SUN PHARMACEUTICAL INDUSTRIES LIMITED, and SUN PHARMACEUTICAL INDUSTRIES, INC., Defendants.
3. Seyfarth Shaw LLP: The BioLoquitur Bulletin - Seyfarth Shaw LLP
4. Google APIs: (12) United States Patent - googleapis.com
5. Unified Patents: US-6515117-B2 - C-aryl Glucoside Sglt2 Inhibitors and Method

Drugs Protected by US Patent 6,515,117

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	6,515,117		Y	Y		TREATMENT OF TYPE 2 DIABETES MELLITUS
Astrazeneca Ab	QTERNMET XR	dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	210874-002	May 2, 2019		DISCN	Yes	No	6,515,117		Y	Y		TREATMENT OF TYPE 2 DIABETES MELLITUS
Astrazeneca Ab	QTERNMET XR	dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	210874-003	May 2, 2019		DISCN	Yes	No	6,515,117		Y	Y		TREATMENT OF TYPE 2 DIABETES MELLITUS
Astrazeneca Ab	QTERNMET XR	dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	210874-004	May 2, 2019		DISCN	Yes	No	6,515,117		Y	Y		TREATMENT OF TYPE 2 DIABETES MELLITUS
Astrazeneca Ab	QTERN	dapagliflozin; saxagliptin hydrochloride	TABLET;ORAL	209091-002	May 2, 2019		RX	Yes	No	6,515,117		Y	Y		TREATMENT OF TYPE 2 DIABETES MELLITUS

International Family Members for US Patent 6,515,117

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1506211		C300585	Netherlands
European Patent Office	1506211		PA2013008	Lithuania
European Patent Office	1506211		122013000033	Germany
European Patent Office	1506211		C20130006 00074	Estonia
European Patent Office	1506211		92182	Luxembourg