Details for Patent: 8,501,698

Which drugs does patent 8,501,698 protect, and when does it expire?

Patent 8,501,698 protects BYDUREON, BYDUREON PEN, BYDUREON BCISE, QTERNMET XR, XIGDUO XR, FARXIGA, and QTERN, 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 seventy-nine patent family members in thirty-two countries.

Summary for Patent: 8,501,698

Title:	Crystal structures of SGLT2 inhibitors and processes for preparing same
Abstract:	The present invention relates to physical crystal structures of a compound of the formula I: ##STR00001## wherein R.sup.1, R.sup.2, R.sup.2a, R.sup.3 and R.sup.4 are as defined herein, especially ##STR00002## pharmaceutical compositions containing structures of compound I or II, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
Inventor(s):	Gougoutas; Jack Z. (Princeton, NJ), Lobinger; Hildegard (Princeton, NJ), Ramakrishnan; Srividya (Princeton, NJ), Deshpande; Prashant P. (Princeton, NJ), Bien; Jeffrey T. (Princeton, NJ), Lai; Chiajen (Princeton, NJ), Wang; Chenchi (Princeton, NJ), Riebel; Peter (Princeton, NJ), Grosso; John Anthony (Princeton, NJ), Nirschl; Alexandra A. (Princeton, NJ), Singh; Janak (Princeton, NJ), DiMarco; John D. (Princeton, NJ)
Assignee:	Bristol-Myers Squibb Company (Princeton, NJ)
Application Number:	13/049,712
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,501,698
Patent Claim Types: see list of patent claims	Composition; Compound; Use;

United States Patent 8,501,698: A Comprehensive Analysis

Introduction

The United States Patent 8,501,698, titled "Crystal structures of SGLT2 inhibitors and processes for preparing same," is a significant patent in the field of pharmaceuticals, particularly for the treatment of diabetes. This patent, assigned to Bristol-Myers Squibb Company, was granted on August 6, 2013.

Background and Context

SGLT2 (sodium-glucose cotransporter 2) inhibitors are a class of drugs used to treat type 2 diabetes by enhancing the excretion of glucose in the urine, thereby normalizing plasma glucose levels[1].

Inventors and Assignees

The patent was invented by a team of researchers from Princeton, NJ, including Jack Z. Gougoutas, Hildegard Lobinger, Srividya Ramakrishnan, Prashant P. Deshpande, Jeffrey T. Bien, Chiajen Lai, Chenchi Wang, Peter Riebel, John Anthony Grosso, Alexandra A. Nirschl, Janak Singh, and John D. DiMarco. The patent is assigned to Bristol-Myers Squibb Company[1].

Scope of the Patent

Claims

The patent includes 29 claims that cover various aspects of SGLT2 inhibitors, including:

• The crystal structures of compounds with specific chemical formulas.
• Pharmaceutical compositions containing these crystal structures.
• Processes for preparing these compounds and their intermediates.
• Methods of treating diseases such as diabetes using these structures[1].

Crystal Structures

The patent describes the physical crystal structures of compounds, particularly those of the formula I and II, which are crucial for their pharmaceutical efficacy. These structures are detailed along with their solvates and hydrates, which are important for the stability and bioavailability of the drug[1].

Pharmaceutical Compositions

The patent outlines pharmaceutical compositions that include the SGLT2 inhibitors, which can be formulated in various ways to enhance their therapeutic effects. These compositions are designed to be effective in treating diabetes by inhibiting the SGLT2 protein[1].

Processes for Preparation

The patent details the processes for preparing the SGLT2 inhibitors, including the synthesis of intermediates and the final compounds. These processes are critical for the large-scale production of the drug[1].

Patent Landscape

Related Patents

The patent is part of a broader landscape of patents related to SGLT2 inhibitors. Other relevant patents include US 7,919,598, US 7,851,502, US 8,221,786, and US 8,685,934, which also cover various aspects of SGLT2 inhibitors and their formulations[2][5].

Litigation and Enforcement

The patent has been involved in several legal cases, particularly those related to generic competition. For instance, there have been filings with the PTAB (Patent Trial and Appeal Board) and district court cases addressing the infringement, validity, or enforceability of this and related patents[3][5].

Expiration Dates

The patent is set to expire on June 20, 2027, which marks the end of its exclusive protection period. After this date, generic versions of the drug can be marketed, subject to FDA approval and other regulatory requirements[2].

Impact on Diabetes Treatment

Therapeutic Benefits

SGLT2 inhibitors, as described in the patent, offer significant therapeutic benefits for patients with type 2 diabetes. By enhancing glucose excretion, these drugs help in normalizing blood glucose levels, which is crucial for managing the disease[1].

Market Competition

The expiration of this patent and related ones will open up the market for generic versions of SGLT2 inhibitors. This competition is expected to reduce the cost of these medications, making them more accessible to patients[2][3].

Regulatory Approvals

Generic versions of SGLT2 inhibitors, such as dapagliflozin, have been approved by the FDA as bioequivalent and therapeutically equivalent to the reference listed drugs. This approval process ensures that generic drugs meet the same standards of safety and efficacy as the original branded drugs[2].

Conclusion and Future Outlook

The United States Patent 8,501,698 is a pivotal patent in the development and commercialization of SGLT2 inhibitors. As the patent landscape evolves and these patents approach their expiration dates, the market is expected to see increased competition from generic manufacturers. This will likely lead to more affordable treatment options for patients with type 2 diabetes.

Key Takeaways

• The patent covers crystal structures, pharmaceutical compositions, and processes for preparing SGLT2 inhibitors.
• It is assigned to Bristol-Myers Squibb Company and was granted on August 6, 2013.
• The patent is part of a broader landscape of patents related to SGLT2 inhibitors.
• It has been involved in several legal cases related to generic competition.
• The patent is set to expire on June 20, 2027.
• Generic versions of SGLT2 inhibitors are expected to enter the market post-patent expiration.

Frequently Asked Questions (FAQs)

What is the primary use of SGLT2 inhibitors?

SGLT2 inhibitors are primarily used to treat type 2 diabetes by enhancing the excretion of glucose in the urine, thereby normalizing plasma glucose levels.

Who is the assignee of the United States Patent 8,501,698?

The assignee of the United States Patent 8,501,698 is Bristol-Myers Squibb Company.

What is the significance of the crystal structures described in the patent?

The crystal structures described in the patent are crucial for the stability, bioavailability, and pharmaceutical efficacy of the SGLT2 inhibitors.

When is the patent set to expire?

The patent is set to expire on June 20, 2027.

How will the expiration of this patent affect the market for SGLT2 inhibitors?

The expiration of this patent will open up the market for generic versions of SGLT2 inhibitors, potentially reducing the cost of these medications and making them more accessible to patients.

Cited Sources:

1. United States Patent and Trademark Office. US8501698B2 - Crystal structures of SGLT2 inhibitors and processes for preparing same. August 6, 2013.
2. U.S. Food & Drug Administration. ANDA 211414 - Dapagliflozin Tablets, 5 mg and 10 mg. November 13, 2019.
3. Seyfarth Shaw LLP. The BioLoquitur Bulletin - Drugs Available in 2018 For Generic Competition. 2018.
4. Google Patents. US7919598B2 - Crystal structures of SGLT2 inhibitors and processes for preparing same.
5. RPX Insight. In the United States District Court - Case 1:24-cv-00923-UNA. August 8, 2024.

Drugs Protected by US Patent 8,501,698

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	BYDUREON	exenatide synthetic	FOR SUSPENSION, EXTENDED RELEASE;SUBCUTANEOUS	022200-001	Jan 27, 2012		DISCN	Yes	No					Y
Astrazeneca Ab	BYDUREON BCISE	exenatide synthetic	SUSPENSION, EXTENDED RELEASE;SUBCUTANEOUS	209210-001	Oct 20, 2017		RX	Yes	Yes					Y
Astrazeneca Ab	BYDUREON PEN	exenatide synthetic	FOR SUSPENSION, EXTENDED RELEASE;SUBCUTANEOUS	022200-002	Feb 28, 2014		DISCN	Yes	No					Y
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

International Family Members for US Patent 8,501,698

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	061730
Australia	2007265246
Brazil	122017015106
Brazil	122017021516
Brazil	PI0713544
Canada	2653344