DCT

1:20-cv-01153

Boehringer Ingelheim Pharma Inc v. Sun Pharmaceutical Industries Ltd

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I. Executive Summary and Procedural Information

  • Parties & Counsel:
  • Case Identification: 1:20-cv-01153, D. Del., 08/28/2020
  • Venue Allegations: Venue is alleged to be proper in the District of Delaware because each Defendant is incorporated in Delaware and therefore "resides" in the district.
  • Core Dispute: Plaintiffs allege that Defendants’ submission of an Abbreviated New Drug Application (ANDA) to the FDA for a generic version of Plaintiffs' TRIJARDY XR® tablets constitutes an act of patent infringement under the Hatch-Waxman Act.
  • Technical Context: The technology concerns fixed-dose combination pharmaceutical tablets for treating type 2 diabetes, a significant and widespread metabolic disorder requiring long-term glycemic control.
  • Key Procedural History: The lawsuit was triggered by Defendants’ submission of ANDA No. 214843 and Plaintiffs’ receipt of letters on or about July 20, 2020, containing Paragraph IV certifications, which assert that the patents-in-suit are invalid or will not be infringed by the proposed generic product.

Case Timeline

Date Event
2008-04-03 Earliest Priority Date for ’705, ’016, ’379 Patents
2013-04-05 Earliest Priority Date for ’998, ’637, ’172 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
2017-09-19 Earliest Priority Date for ’120 Patent
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
2020-03-24 U.S. Patent No. 10,596,120 Issues
2020-07-20 Plaintiffs receive Defendants' Paragraph IV Certification letters (approximate date)
2020-08-28 Complaint Filed

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

Due to the number of patents-in-suit, full analysis is provided for two representative patents for which documents were supplied, U.S. Patent Nos. 10,022,379 and 10,258,637, followed by capsule summaries for the remaining patents based on information in the complaint.

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"

The Invention Explained

  • Problem Addressed: The patent addresses chemical incompatibility and degradation problems that arise when formulating fixed-dose combination tablets containing DPP-4 inhibitors that have a primary or secondary amino group, particularly when combined with other drugs or common pharmaceutical excipients like metformin (’379 Patent, col. 5:6-24). These incompatibilities can lead to poor stability and an "assay decrease" of the active ingredient, especially in low-dosage DPP-4 inhibitor formulations (’379 Patent, col. 5:39-47).
  • The Patented Solution: The invention claims to solve this stability problem by incorporating a "nucleophilic and/or basic agent," such as the amino acid L-arginine, into the pharmaceutical composition (’379 Patent, col. 5:48-61). This agent acts as a stabilizer or buffering agent, protecting the DPP-4 inhibitor from chemical degradation caused by reactions with the partner drug or excipients (’379 Patent, col. 6:1-10, 20-25).
  • Technical Importance: This approach enables the creation of stable, reliable fixed-dose combination tablets, which are crucial for improving patient compliance in chronic diseases like type 2 diabetes that often require multiple medications.

Key Claims at a Glance

  • The complaint alleges infringement of at least one claim without specifying which claims are asserted (Compl. ¶102). Independent claim 1 is representative of the invention's composition.
  • Essential elements of Independent Claim 1:
    • A solid pharmaceutical composition comprising 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine (linagliptin).
    • Metformin hydrochloride.
    • One or more pharmaceutical excipients.
    • L-arginine as a basic amino acid.
    • Wherein the composition is a mono-layer tablet and comprises specific weight percentages of the components.
  • The complaint does not explicitly reserve the right to assert dependent claims but makes a general allegation of infringement.

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

The Invention Explained

  • Problem Addressed: The patent background describes the significant challenge of treating type 2 diabetes in patients who also suffer from renal impairment or chronic kidney disease (CKD) (’637 Patent, col. 1:21-41). Many common anti-diabetic medications are either contraindicated or require dose adjustments in this patient population due to risks associated with renal excretion, such as lactic acidosis with metformin or hypoglycemia with certain insulin secretagogues (’637 Patent, col. 1:35-41).
  • The Patented Solution: The invention provides a method for treating type 2 diabetes in patients with specific levels of renal impairment by administering an SGLT-2 inhibitor, particularly empagliflozin (’637 Patent, col. 2:42-49). The claims are directed to methods of improving glycemic control in patients within defined ranges of moderate renal impairment, a population with limited treatment options.
  • Technical Importance: This invention provides a targeted therapeutic method for a vulnerable and difficult-to-treat patient sub-population, addressing an unmet medical need for safe and effective glycemic control in patients with CKD.

Key Claims at a Glance

  • The complaint alleges infringement of at least one claim without specifying which claims are asserted (Compl. ¶116). Independent claim 1 is representative of the patented method.
  • Essential elements of Independent Claim 1:
    • A method for improving glycemic control in a patient with type 2 diabetes mellitus.
    • The method comprises administering empagliflozin to the patient.
    • The patient is characterized as having moderate A renal impairment, defined as having an estimated glomerular filtration rate (eGFR) of ≥45 ml/min/1.73 m² and <60 ml/min/1.73 m².
  • The complaint does not explicitly reserve the right to assert dependent claims but makes a general allegation of infringement.

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

  • Technology Synopsis: Based on its title and context within the suit, this patent appears to relate to pharmaceutical compositions containing empagliflozin (a glucopyranosyl-substituted benzene derivative), one of the active ingredients in TRIJARDY XR®. The patent likely addresses formulation challenges to ensure stability and proper delivery of this SGLT-2 inhibitor.
  • Asserted Claims: At least one claim is asserted (Compl. ¶44).
  • Accused Features: The Sun ANDA Product, an extended-release tablet containing empagliflozin, is alleged to be a pharmaceutical composition that infringes (Compl. ¶1, 11, 39, 44).

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"

  • Technology Synopsis: This patent, based on its title, appears to cover pharmaceutical tablets that are fixed-dose combinations of a DPP-IV inhibitor (linagliptin) with another antidiabetic agent (such as metformin or empagliflozin). The invention likely relates to the specific formulation required to create a stable and effective combination tablet.
  • Asserted Claims: At least one claim is asserted (Compl. ¶59).
  • Accused Features: The Sun ANDA Product, a three-drug combination tablet including the DPP-IV inhibitor linagliptin, is the infringing instrumentality (Compl. ¶1, 11, 39, 59).

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"

  • Technology Synopsis: Similar to the ’705 Patent, the title suggests this patent covers fixed-dose combination tablets containing a DPP-IV inhibitor (linagliptin) and another antidiabetic agent. It likely claims a specific formulation, manufacturing process, or method of using such tablets.
  • Asserted Claims: At least one claim is asserted (Compl. ¶73).
  • Accused Features: The Sun ANDA Product is a tablet that combines a DPP-IV inhibitor with other antidiabetic agents, which is the subject matter of the patent (Compl. ¶1, 11, 39, 73).

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

  • Technology Synopsis: The title suggests this patent relates to pharmaceutical compositions and their use in methods of treatment. Given its association with TRIJARDY XR®, it likely covers compositions containing empagliflozin and/or linagliptin and methods of using them to treat conditions like type 2 diabetes.
  • Asserted Claims: At least one claim is asserted (Compl. ¶87).
  • Accused Features: The Sun ANDA Product is alleged to be a pharmaceutical composition whose use infringes the patent's claims (Compl. ¶1, 11, 39, 87).

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

  • Technology Synopsis: The title is identical to that of the ’998 Patent, suggesting it is part of the same patent family and covers related subject matter, such as specific compositions containing empagliflozin and/or linagliptin or methods of using such compositions for treatment.
  • Asserted Claims: At least one claim is asserted (Compl. ¶131).
  • Accused Features: The Sun ANDA Product and its intended use are alleged to infringe the claims of the patent (Compl. ¶1, 11, 39, 131).

U.S. Patent No. 10,596,120 - "Pharmaceutical Compositions"

  • Technology Synopsis: This patent's general title suggests it claims specific pharmaceutical formulations. In the context of the lawsuit, it likely covers the particular combination of active ingredients and/or excipients found in TRIJARDY XR® and, allegedly, in the Sun ANDA Product.
  • Asserted Claims: At least one claim is asserted (Compl. ¶146).
  • Accused Features: The Sun ANDA Product is alleged to be a pharmaceutical composition that infringes the patent's claims (Compl. ¶1, 11, 39, 146).

III. The Accused Instrumentality

Product Identification

  • The accused instrumentality is Defendants' proposed generic empagliflozin/linagliptin/metformin hydrochloride extended-release tablets, for which Defendants submitted ANDA No. 214843 to the FDA (Compl. ¶11).

Functionality and Market Context

  • The Sun ANDA Product is a fixed-dose combination drug intended for the treatment of type 2 diabetes (Compl. ¶1). It combines three active ingredients with different mechanisms of action: empagliflozin (an SGLT-2 inhibitor), linagliptin (a DPP-IV inhibitor), and metformin hydrochloride (a biguanide). The product is formulated as an extended-release tablet and is presented in multiple dosage strengths (Compl. ¶11). The complaint alleges that the Sun ANDA Product refers to and relies upon Plaintiffs' TRIJARDY XR® New Drug Application and that data has been submitted to demonstrate its bioequivalence to TRIJARDY XR® (Compl. ¶42, 57).

No probative visual evidence provided in complaint.

IV. Analysis of Infringement Allegations

The complaint does not provide sufficient detail for a claim-by-claim analysis or the creation of claim charts. The infringement allegations are premised on 35 U.S.C. § 271(e)(2)(A), which defines the submission of an ANDA seeking approval to market a drug claimed in a patent before its expiration as a statutory act of infringement (Compl. ¶44, 59, 73, 87, 102, 116, 131, 146). The central theory is that the commercial manufacture, use, or sale of the Sun ANDA Product upon FDA approval would infringe claims of the patents-in-suit directed to compositions, formulations, and methods of use.

  • ’379 Patent (Composition Claim) Allegations: The complaint alleges that by filing the ANDA for a product containing linagliptin and metformin, Defendants have infringed the ’379 Patent (Compl. ¶102). The infringement would be literal, as the Sun ANDA Product is alleged to be a pharmaceutical composition containing the same active ingredients as the patented invention.
    • Identified Points of Contention: A primary question will be one of compositional identity. Sun's Paragraph IV certification suggests non-infringement is a defense (Compl. ¶101). The dispute may turn on whether Sun’s formulation contains every element of the asserted claims, including not just the active ingredients but also specific excipients like the L-arginine stabilizer, in the claimed ratios or forms. Another key point of contention will be the validity of the patent claims.
  • ’637 Patent (Method of Use Claim) Allegations: The complaint alleges that the eventual use of the Sun ANDA Product as directed would infringe the method claims of the ’637 Patent (Compl. ¶119-120). Infringement would be induced by Defendants' proposed product labeling, which would instruct physicians and patients to administer the drug to the patient population claimed in the patent.
    • Identified Points of Contention: The central legal question will be induced infringement. The analysis will focus on whether the proposed label for the Sun ANDA Product encourages, recommends, or promotes its administration to patients with "moderate A renal impairment" as defined by the specific eGFR ranges in the claims. A technical question is whether the product's use in the real world would necessarily meet the method steps recited in the claims.

V. Key Claim Terms for Construction

  • For the ’379 Patent

    • The Term: "a suitable buffering agent" / "L-arginine"
    • Context and Importance: The use of L-arginine as a stabilizing/buffering agent appears to be a core technical feature of the invention claimed in the ’379 Patent to solve the problem of DPP-4 inhibitor degradation. The construction of this term and its functional requirements will be critical to determining the scope of the composition claims and whether Defendants’ formulation, which may or may not use L-arginine in the same way, infringes.
    • Intrinsic Evidence for Interpretation:
      • Evidence for a Broader Interpretation: The specification describes the stabilizing agent as a "nucleophilic and/or basic agent" and a "suitable buffering agent", listing L-arginine as a preferred example (’379 Patent, col. 6:1-10, 20-25). This could support an interpretation where other basic amino acids or buffering agents are considered equivalent.
      • Evidence for a Narrower Interpretation: The claims and detailed examples focus specifically on L-arginine and its particular stabilizing effect on the DPP-4 inhibitor (’379 Patent, col. 6:20-25; Claim 1). This may support an interpretation limiting the claim to compositions that specifically use L-arginine to perform the recited stabilizing function.

  • For the ’637 Patent

    • The Term: "a patient... having moderate A renal impairment"
    • Context and Importance: This term defines the specific patient population to which the patented method of treatment applies. The infringement analysis for this method patent will depend entirely on whether the instructions for use on the Sun ANDA Product's label will direct or lead physicians to prescribe the drug to patients falling within this definition.
    • Intrinsic Evidence for Interpretation:
      • Evidence for a Broader Interpretation: The specification provides a general classification of chronic kidney disease stages (CKD 1-5) based on GFR (’637 Patent, col. 1:25-35). This context could be used to argue that the term should be understood in its broader clinical sense, not just the specific numbers in the claim.
      • Evidence for a Narrower Interpretation: Independent claim 1 explicitly defines the term by a specific numerical range: "an estimated glomerular filtration rate (eGFR) of ≥45 ml/min/1.73 m² and <60 ml/min/1.73 m²" (’637 Patent, col. 28:56-62). This explicit definition provides strong evidence that the claim scope is precisely limited to patients who fall within that measured range, and no broader.

VI. Other Allegations

  • Indirect Infringement: The complaint alleges both induced and contributory infringement for all patents-in-suit. The allegations are based on Defendants’ knowledge of the patents and the assertion that Defendants’ promotional materials and package inserts for the Sun ANDA Product will instruct and encourage medical professionals and patients to use the product in an infringing manner (Compl. ¶50-51, 65-66, 79-80, 93-94, 108-109, 122-123, 137-138, 152-153).
  • Willful Infringement: The complaint does not contain an explicit allegation of willful infringement. However, for each patent, it alleges that the case is "exceptional" under 35 U.S.C. § 285, which is the statutory basis for an award of attorney's fees, and requests such a finding in the prayer for relief (Compl. ¶54, 68, 82, 97, 111, 126, 141, 156; Prayer for Relief ¶b).

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

  • A central issue will be one of compositional scope: For the formulation patents (e.g., ’379, ’705, ’016), the case will likely turn on whether the precise formulation of Sun's proposed generic product, including its specific combination of active ingredients and excipients, falls within the boundaries of the asserted patent claims, or whether Sun has successfully "designed around" the patented technology.
  • A key question will be one of induced infringement: For the method-of-use patents (e.g., ’637, ’998, ’172), the dispute will focus on whether the final, FDA-approved product label for Sun’s generic will either explicitly or implicitly instruct physicians to prescribe the drug to the specific patient populations defined in the claims, such as those with moderate renal impairment.
  • A foundational issue for all asserted patents will be validity: Stemming from Defendants' Paragraph IV certifications, a primary focus of the litigation will be whether Defendants can prove by clear and convincing evidence that Plaintiffs' patent claims are invalid as obvious, anticipated, or otherwise failing to meet statutory requirements in light of the prior art.