DCT

1:21-cv-00530

Boehringer Ingelheim Pharma Inc v. Lupin Ltd

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I. Executive Summary and Procedural Information

  • Parties & Counsel:
  • Case Identification: 1:21-cv-00530, D. Del., 04/13/2021
  • Venue Allegations: Venue is alleged to be proper in the District of Delaware because Defendant Lupin Pharmaceuticals, Inc. is incorporated in Delaware, and Defendant Lupin Ltd. is a foreign corporation that may be sued in any judicial district.
  • Core Dispute: Plaintiff alleges that Defendants' submission of an Abbreviated New Drug Application (ANDA) to the FDA, seeking to market generic versions of Plaintiff's TRIJARDY® XR diabetes medication, constitutes an act of infringement of seven U.S. patents.
  • Technical Context: The dispute centers on pharmaceutical compositions for treating type 2 diabetes mellitus, specifically fixed-dose combination tablets containing a DPP-4 inhibitor (linagliptin), an SGLT2 inhibitor (empagliflozin), and metformin.
  • Key Procedural History: The action was triggered by Plaintiff's receipt on or about March 4, 2021, of Paragraph IV certification letters from Defendants, which stated that claims of the patents-in-suit are either invalid or will not be infringed by the commercial manufacture, use, or sale of the proposed generic product.

Case Timeline

Date Event
2008-04-03 Priority Date for ’705, ’016, and ’379 Patents
2008-08-07 Priority Date for ’172 Patent
2013-04-05 Priority Date for ’998 and ’637 Patents
2013-10-08 U.S. Patent No. 8,551,957 Issues
2015-10-13 U.S. Patent No. 9,155,705 Issues
2016-08-16 U.S. Patent No. 9,415,016 Issues
2018-04-24 U.S. Patent No. 9,949,998 Issues
2018-07-17 U.S. Patent No. 10,022,379 Issues
2019-04-16 U.S. Patent No. 10,258,637 Issues
2019-09-10 U.S. Patent No. 10,406,172 Issues
2021-03-04 Plaintiff receives Paragraph IV certification letters from Lupin
2021-04-13 Complaint Filed

II. Technology and Patent(s)-in-Suit Analysis

U.S. Patent No. 8,551,957 - "Pharmaceutical Composition Comprising a Glucopyranosyl-Substituted Benzene Derivate"

  • Issued: October 8, 2013

The Invention Explained

  • Problem Addressed: The patent addresses the general need for effective pharmaceutical compositions for treating metabolic disorders like type 2 diabetes using SGLT-2 inhibitors (’957 Patent, col. 1:15-26).
  • The Patented Solution: The invention is a specific oral pharmaceutical formulation containing the SGLT-2 inhibitor empagliflozin combined with a set of standard pharmaceutical excipients: one or more fillers, binders, disintegrants, and lubricants (’957 Patent, Abstract; col. 3:1-12). This combination creates a stable and effective solid dosage form for administration to patients.
  • Technical Importance: The invention provides a concrete formulation for orally administering a member of the then-emerging SGLT-2 inhibitor class of drugs, facilitating its use as a practical therapy for type 2 diabetes.

Key Claims at a Glance

  • The complaint asserts at least one unspecified claim (Compl. ¶37). Independent claim 1 is representative.
  • Claim 1 of the ’957 Patent includes the following essential elements:
    • A pharmaceutical composition comprising:
    • The compound 1-chloro-4-(β-D-glucopyranos-1-yl)-2-(4-((S)-tetrahydrofuran-3-yloxy)-benzyl)-benzene (empagliflozin);
    • one or more fillers;
    • one or more binders;
    • one or more disintegrants; and
    • one or more lubricants.
  • The complaint does not explicitly reserve the right to assert dependent claims.

U.S. Patent No. 9,155,705 - "DPP-IV Inhibitor Combined with a Further Antidiabetic Agent, Tablets Comprising Such Formulations, Their Use and Process for Their Preparation"

  • Issued: October 13, 2015

The Invention Explained

  • Problem Addressed: The patent notes that DPP-4 inhibitors with a primary or secondary amino group can exhibit incompatibilities and degradation problems when formulated with other drugs or common excipients, particularly in fixed-dose combination tablets (’705 Patent, col. 5:6-25).
  • The Patented Solution: The invention claims to solve this stability problem through a pharmaceutical composition that combines a DPP-4 inhibitor (linagliptin) and a partner drug (metformin) with a stabilizing agent, identified in the specification as a nucleophilic and/or basic agent like L-arginine, to prevent chemical degradation (’705 Patent, col. 6:3-10; col. 6:36-50).
  • Technical Importance: This technology enables the creation of stable, fixed-dose combination tablets containing chemically sensitive DPP-4 inhibitors, simplifying treatment regimens for diabetic patients who require multiple medications.

Key Claims at a Glance

  • The complaint asserts at least one unspecified claim (Compl. ¶52). Independent claim 1 is representative.
  • Claim 1 of the ’705 Patent includes the following essential elements:
    • A pharmaceutical composition comprising a DPP-4 inhibitor and metformin hydrochloride;
    • wherein the DPP-4 inhibitor is 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine (linagliptin); and
    • wherein the composition further comprises one or more pharmaceutical excipients.
  • The complaint does not explicitly reserve the right to assert dependent claims.

U.S. Patent No. 9,415,016 - "DPP-IV inhibitor combined with a further antidiabetic agent, tablets comprising such formulations, their use and process for their preparation"

  • Issued: August 16, 2016
  • Technology Synopsis: This patent is related to the ’705 Patent and addresses the same technical problem of creating stable fixed-dose combination tablets containing a DPP-4 inhibitor like linagliptin and a partner drug like metformin (’016 Patent, Abstract; col. 5:6-25). The solution involves specific formulations that overcome chemical incompatibilities.
  • Asserted Claims: The complaint asserts at least one unspecified claim (Compl. ¶66).
  • Accused Features: The accused features are Lupin's proposed generic tablets containing linagliptin and metformin hydrochloride (Compl. ¶10).

U.S. Patent No. 9,949,998 - "Pharmaceutical Composition, Methods for Treating and Uses Thereof"

  • Issued: April 24, 2018
  • Technology Synopsis: This patent relates to pharmaceutical compositions containing the SGLT-2 inhibitor empagliflozin for treating or preventing metabolic disorders in patients with renal impairment or chronic kidney disease (’998 Patent, Abstract). The invention covers methods of using empagliflozin to improve glycemic control in this specific patient population.
  • Asserted Claims: The complaint asserts at least one unspecified claim (Compl. ¶80).
  • Accused Features: The accused features are Lupin's proposed generic tablets containing empagliflozin, which will be marketed with a label instructing use for treating type 2 diabetes (Compl. ¶¶ 10, 86).

U.S. Patent No. 10,022,379 - "DPP-IV inhibitor combined with a further antidiabetic agent, tablets comprising such formulations, their use and process for their preparation"

  • Issued: July 17, 2018
  • Technology Synopsis: As part of the same family as the ’705 and ’016 patents, this patent also addresses the technical challenge of creating stable fixed-dose combination tablets of a DPP-4 inhibitor and a partner drug (’379 Patent, Abstract). The patented solution involves specific formulations that include a stabilizing agent, such as L-arginine, to prevent degradation.
  • Asserted Claims: The complaint asserts at least one unspecified claim (Compl. ¶95).
  • Accused Features: The accused features are Lupin's proposed generic tablets containing linagliptin and metformin hydrochloride (Compl. ¶10).

U.S. Patent No. 10,258,637 - "Pharmaceutical Composition, Method for Treating and Uses Thereof"

  • Issued: April 16, 2019
  • Technology Synopsis: This patent is part of the same family as the ’998 Patent and is directed to methods of using the SGLT-2 inhibitor empagliflozin to treat type 2 diabetes in patients with renal impairment or chronic kidney disease (’637 Patent, Abstract). It specifically claims methods of improving glycemic control in patients with defined levels of renal function.
  • Asserted Claims: The complaint asserts at least one unspecified claim (Compl. ¶109).
  • Accused Features: The accused features are Lupin's proposed generic tablets containing empagliflozin and the associated product labeling that will direct its use in treating type 2 diabetes (Compl. ¶¶ 10, 115).

U.S. Patent No. 10,406,172 - "Pharmaceutical Composition, Method for Treating and Uses Thereof"

  • Issued: September 10, 2019
  • Technology Synopsis: This patent relates to pharmaceutical compositions that combine an SGLT2 inhibitor (empagliflozin) and a DPP-4 inhibitor (linagliptin) for treating metabolic disorders (’172 Patent, Abstract). It covers the fixed-dose combination of these two active ingredients.
  • Asserted Claims: The complaint asserts at least one unspecified claim (Compl. ¶124).
  • Accused Features: The accused features are Lupin's proposed generic tablets containing the combination of empagliflozin and linagliptin (Compl. ¶10).

III. The Accused Instrumentality

Product Identification

  • The accused products are Lupin's proposed generic empagliflozin/linagliptin/metformin hydrochloride extended-release tablets in 5 mg/2.5 mg/1000 mg; 10 mg/5 mg/1000 mg; 12.5 mg/2.5 mg/1000 mg; and 25 mg/5 mg/1000 mg dosages, for which Lupin submitted ANDA No. 215072 (the "Lupin ANDA Product") (Compl. ¶10).

Functionality and Market Context

  • The Lupin ANDA Product is a fixed-dose combination drug intended for the treatment of type 2 diabetes. The complaint alleges that Lupin has represented its product as being bioequivalent to Plaintiff's branded drug, TRIJARDY® XR (Compl. ¶35). Upon FDA approval, the product would compete with TRIJARDY® XR as a lower-cost generic alternative.

IV. Analysis of Infringement Allegations

The complaint makes general allegations of infringement under 35 U.S.C. § 271(e)(2) based on the filing of the ANDA, without providing a detailed claim chart or mapping specific product features to claim elements. The analysis below is based on representative independent claims and the general description of the accused product.

’957 Patent Infringement Allegations

Claim Element (from Independent Claim 1) Alleged Infringing Functionality Complaint Citation Patent Citation
A pharmaceutical composition comprising: 1-chloro-4-(β-D-glucopyranos-1-yl)-2-(4-((S)-tetrahydrofuran-3-yloxy)-benzyl)-benzene The Lupin ANDA Product is an empagliflozin tablet containing this active ingredient. ¶10 col. 1:6-12
one or more fillers, one or more binders, one or more disintegrants, and one or more lubricants As a tablet for oral use, the Lupin ANDA Product is a formulation that necessarily contains pharmaceutical excipients, including those recited in the claim. ¶10 col. 3:5-12

’705 Patent Infringement Allegations

Claim Element (from Independent Claim 1) Alleged Infringing Functionality Complaint Citation Patent Citation
A pharmaceutical composition comprising a DPP-4 inhibitor...wherein the DPP-4 inhibitor is 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine The Lupin ANDA Product is a linagliptin tablet containing this active ingredient. ¶10 col. 22:9-15
and metformin hydrochloride The Lupin ANDA Product contains metformin hydrochloride as a second active ingredient. ¶10 col. 19:50-54
wherein the composition further comprises one or more pharmaceutical excipients As an oral tablet, the Lupin ANDA Product is a formulation that necessarily contains pharmaceutical excipients. ¶10 col. 5:56-65
  • Identified Points of Contention:
    • Scope Questions: For the ’705 Patent family, a central issue may be whether the term "pharmaceutical composition" should be construed to require a stabilizing agent, such as L-arginine. The specification heavily emphasizes the problem of chemical instability and presents the use of a stabilizer as the solution (’705 Patent, col. 5:6-25, col. 6:3-10), yet the independent claim does not explicitly recite this element. This raises the question of whether a composition without such a stabilizing feature falls within the claim's scope.
    • Technical Questions: A key technical question, typical for ANDA litigation, is whether the specific formulation disclosed in Lupin's confidential ANDA—including the selection of excipients, their quantities, and the manufacturing process—is identical to or equivalent to the formulations covered by the asserted claims. The complaint does not provide sufficient detail for analysis of this point.

No probative visual evidence provided in complaint.

V. Key Claim Terms for Construction

The complaint does not provide sufficient detail to identify specific claim terms that are in dispute. However, based on the patent specifications, the construction of the following terms may be central to the case.

  • The Term: "pharmaceutical composition" (from ’705 Patent, Claim 1)
  • Context and Importance: The definition of this term is critical because the ’705 Patent specification describes the invention as solving a specific problem of chemical instability between the active ingredients and excipients. Practitioners may focus on this term because Lupin could argue that to be a "composition" under the patent, the formulation must be stable in the manner described, implicitly requiring a stabilizing element that is absent from its own product.
  • Intrinsic Evidence for Interpretation:
    • Evidence for a Broader Interpretation: The plain language of Claim 1 only requires the two active ingredients and "one or more pharmaceutical excipients," which could support a broad reading that covers any formulation containing these components, regardless of its stability profile or the presence of a specific stabilizer.
    • Evidence for a Narrower Interpretation: The patent's background explicitly states that DPP-4 inhibitors with amino groups "show incompatibilities, degradation problems, or extraction problems with a number of customary excipients" (’705 Patent, col. 5:8-12). The solution is described as using a "nucleophilic and/or basic agent" to achieve a "chemically stable FDC formulation" (’705 Patent, col. 6:3-10, col. 6:53-56). This language may support a narrower construction where the term "pharmaceutical composition" is limited to formulations that incorporate the inventive stabilizing concept.

VI. Other Allegations

  • Indirect Infringement: The complaint alleges that Lupin will induce and contribute to infringement of all asserted patents. This is based on allegations that Lupin knows its ANDA Product is especially adapted for an infringing use and that its promotional materials and package inserts will instruct medical professionals and patients to use the product in a manner that directly infringes the patent claims (e.g., Compl. ¶¶ 41-44, 56-59).
  • Willful Infringement: The complaint does not allege "willful infringement" but asserts for each patent that the case is "exceptional" under 35 U.S.C. § 285, warranting attorneys' fees (e.g., Compl. ¶¶ 47, 61). This allegation is based on Lupin's filing of the ANDA with knowledge of the patents, as evidenced by its Paragraph IV certifications.

VII. Analyst’s Conclusion: Key Questions for the Case

  • A core issue will be one of claim scope versus the specification: For the patents related to combination formulations (e.g., the ’705, ’016, and ’379 patents), a key question will be whether the claims can be interpreted broadly to cover any combination of the recited active ingredients, or if they will be narrowed by the specification's extensive discussion of solving a specific chemical stability problem, potentially requiring a stabilizing feature that may be absent in the accused product.
  • A second central question is one of infringement by equivalence: Because this is an ANDA case, the dispute will turn on the specific, confidential details of Lupin's formulation. A key evidentiary question will be whether the excipients and composition of the Lupin ANDA Product are literally covered by the asserted claims or, if not, whether they are equivalent under the doctrine of equivalents.
  • Finally, the case will involve a fundamental question of validity: Lupin's Paragraph IV certifications assert that the patents-in-suit are invalid. The ultimate outcome will likely depend on whether Lupin can prove by clear and convincing evidence that the asserted claims are invalid as anticipated or rendered obvious by prior art predating the patents' priority dates.