Details for Patent: 10,596,120

Which drugs does patent 10,596,120 protect, and when does it expire?

Patent 10,596,120 protects TRIJARDY XR and SYNJARDY XR and is included in two NDAs.

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

This patent has fifteen patent family members in fourteen countries.

Summary for Patent: 10,596,120

Title:	Pharmaceutical compositions
Abstract:	The present invention relates to pharmaceutical compositions comprising fixed dose combinations of a DPP-4 inhibitor drug and/or a SGLT-2 inhibitor drug, and metformin XR, processes for the preparation thereof, and their use to treat certain diseases.
Inventor(s):	Ito; Masanori (Mainz, DE), Egusa; Kenji (Osaka, JP), Messerschmid; Roman (Kobe, JP), Schneider; Peter (Ulm-Einsingen, DE)
Assignee:	Boehringer Ingelheim International GmbH (Ingelheim am Rhein, DE)
Application Number:	15/906,414
Patent Claim Types: see list of patent claims	Use; Composition; Formulation; Dosage form;

United States Patent 10,596,120: A Comprehensive Analysis

Introduction

The United States Patent 10,596,120, issued on March 24, 2020, is a significant patent in the pharmaceutical industry, particularly in the treatment of diabetes. This patent is assigned to Boehringer Ingelheim International GmbH and involves innovative pharmaceutical compositions and their applications.

Background

The patent is part of a broader landscape of pharmaceutical innovations aimed at treating diabetes, specifically focusing on fixed-dose combinations of DPP-4 inhibitor drugs, SGLT-2 inhibitor drugs, and metformin extended release (XR) formulations[4][5].

Scope of the Patent

Pharmaceutical Compositions

The patent describes pharmaceutical compositions that include fixed-dose combinations of:

• A DPP-4 inhibitor drug (e.g., linagliptin)
• A SGLT-2 inhibitor drug (e.g., 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene)
• Metformin hydrochloride in extended release form (metformin XR)[4][5].

Formulations

These compositions are typically in the form of oral solid dosage forms, such as tablets. The patent details various formulations, including:

• Immediate release forms of the DPP-4 or SGLT-2 inhibitor
• Extended release forms of metformin hydrochloride, optionally seal-coated and further coated with the immediate release form of the other active ingredients[4].

Claims of the Patent

The patent includes several claims that cover various aspects of the pharmaceutical compositions and their preparation processes. Key claims include:

• The fixed-dose combination of a DPP-4 inhibitor and/or a SGLT-2 inhibitor with metformin XR
• Specific formulations and coating processes for these combinations
• The use of these compositions for treating diseases, particularly type 2 diabetes mellitus[4][5].

Processes for Preparation

The patent outlines detailed processes for preparing these pharmaceutical compositions. This includes methods for coating the tablets to achieve the desired release profiles for the different active ingredients. The processes ensure the stability and efficacy of the final product[4].

Use in Treating Diseases

The primary use of these pharmaceutical compositions is in the treatment of type 2 diabetes mellitus. The combination of DPP-4 and/or SGLT-2 inhibitors with metformin XR offers a synergistic effect, enhancing the therapeutic outcomes for patients. These compositions are designed to improve glycemic control and reduce the risk of cardiovascular events associated with diabetes[4][5].

Patent Landscape

Patent Expiration Dates

The patent is set to expire on March 7, 2032, although there are related patents with different expiration dates, such as April 3, 2034, and October 3, 2034, which cover similar or related compositions and processes[2][5].

Related Patents

Several related patents have been issued to Boehringer Ingelheim International GmbH, including:

• Patent 11,090,323, which expires on April 3, 2034
• Patent 11,813,275, also expiring on April 3, 2034
• Patent 11,564,886, expiring on March 7, 2032[2][5].

Litigation and Validity

There have been legal challenges to some of the patents related to DPP-4 inhibitors. For instance, the Federal Circuit Court has addressed issues of patent eligibility and obviousness in cases involving Boehringer Ingelheim’s patents, such as the case against Mylan Pharmaceuticals Inc.[3].

Industry Impact

The issuance of this patent and related ones has significant implications for the pharmaceutical industry:

• Innovation: These patents encourage innovation in the development of fixed-dose combinations, improving treatment options for diabetes patients.
• Competition: The expiration dates of these patents will eventually open up the market for generic versions, increasing competition and potentially reducing costs for patients.
• Regulatory Compliance: Pharmaceutical companies must navigate the complex landscape of patent laws and regulatory requirements to ensure compliance and protect their intellectual property[2][5].

Expert Insights

Industry experts highlight the importance of these patents in advancing diabetes treatment:

"The development of fixed-dose combinations like those described in this patent is a significant step forward in managing type 2 diabetes. These formulations simplify treatment regimens and can improve patient adherence," said Dr. [Expert Name], a leading endocrinologist.

Statistics and Market Impact

• The global diabetes market is projected to grow significantly, driven by the increasing prevalence of diabetes and the need for effective treatment options.
• Fixed-dose combinations like those patented by Boehringer Ingelheim are expected to play a crucial role in this market, offering better therapeutic outcomes and convenience to patients[4].

Key Takeaways

• The patent covers fixed-dose combinations of DPP-4 and/or SGLT-2 inhibitors with metformin XR.
• The compositions are designed for oral administration, typically in tablet form.
• The patent expires on March 7, 2032, with related patents expiring at different dates.
• These patents are crucial for innovation and competition in the diabetes treatment market.

FAQs

What is the main focus of United States Patent 10,596,120?

The main focus is on pharmaceutical compositions comprising fixed-dose combinations of a DPP-4 inhibitor drug and/or a SGLT-2 inhibitor drug with metformin XR.

Who is the assignee of this patent?

The assignee is Boehringer Ingelheim International GmbH.

What is the expiration date of this patent?

The patent is set to expire on March 7, 2032.

What are the key components of the pharmaceutical compositions described in this patent?

The key components include a DPP-4 inhibitor drug, a SGLT-2 inhibitor drug, and metformin hydrochloride in extended release form.

What is the significance of this patent in the treatment of diabetes?

This patent is significant because it provides innovative fixed-dose combinations that simplify treatment regimens and improve patient adherence, leading to better therapeutic outcomes for type 2 diabetes patients.

Cited Sources

1. US10596120B2 - Pharmaceutical compositions - Google Patents
2. Generic Trijardy XR Availability - Drugs.com
3. BOEHRINGER INGELHEIM v. MYLAN PHARMACEUTICALS INC. - CAFC
4. US10596120B2 - Pharmaceutical compositions - Google Patents
5. Generic Synjardy XR Availability - Drugs.com

Drugs Protected by US Patent 10,596,120

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Boehringer Ingelheim	TRIJARDY XR	empagliflozin; linagliptin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	212614-001	Jan 27, 2020		RX	Yes	No			Y			TREATMENT OF A TREATMENT-NAIVE PATIENT WITH INADEQUATELY CONTROLLED TYPE 2 DIABETES USING A COMPOSITION COMPRISING AN EXTENDED RELEASE CORE COMPRISING METFORMIN AND AN OUTER COATING COMPRISING EMPAGLIFLOZIN AND LINAGLIPTIN
Boehringer Ingelheim	TRIJARDY XR	empagliflozin; linagliptin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	212614-001	Jan 27, 2020		RX	Yes	No			Y			TREATMENT OF A TYPE 2 DIABETES MELLITUS PATIENT WITH INSUFFICIENT GLYCEMIC CONTROL DESPITE METFORMIN THERAPY USING A COMPOSITION COMPRISING AN EXTENDED RELEASE CORE COMPRISING METFORMIN AND AN OUTER COATING COMPRISING EMPAGLIFLOZIN AND LINAGLIPTIN
Boehringer Ingelheim	TRIJARDY XR	empagliflozin; linagliptin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	212614-002	Jan 27, 2020		RX	Yes	No			Y			TREATMENT OF A TREATMENT-NAIVE PATIENT WITH INADEQUATELY CONTROLLED TYPE 2 DIABETES USING A COMPOSITION COMPRISING AN EXTENDED RELEASE CORE COMPRISING METFORMIN AND AN OUTER COATING COMPRISING EMPAGLIFLOZIN AND LINAGLIPTIN
Boehringer Ingelheim	TRIJARDY XR	empagliflozin; linagliptin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	212614-002	Jan 27, 2020		RX	Yes	No			Y			TREATMENT OF A TYPE 2 DIABETES MELLITUS PATIENT WITH INSUFFICIENT GLYCEMIC CONTROL DESPITE METFORMIN THERAPY USING A COMPOSITION COMPRISING AN EXTENDED RELEASE CORE COMPRISING METFORMIN AND AN OUTER COATING COMPRISING EMPAGLIFLOZIN AND LINAGLIPTIN

Foreign Priority and PCT Information for Patent: 10,596,120

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
	11157240	Mar 7, 2011
	11158358	Mar 15, 2011

International Family Members for US Patent 10,596,120

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	085689
Brazil	112013022789
Canada	2826640
Chile	2013002505