Bayer IP GmbH v. Breckenridge Pharmaceutical Inc

I. Executive Summary and Procedural Information

• Parties & Counsel:
  • Plaintiff: Bayer Intellectual Property GMBH (Germany), Bayer Pharma AG (Germany), and Janssen Pharmaceuticals, Inc. (Pennsylvania)
  • Defendant: Breckenridge Pharmaceutical, Inc. (Florida)
  • Plaintiff’s Counsel: Morris, Nichols, Arsht & Tunnell LLP
• Case Identification: 1:16-cv-00628, D. Del., 07/25/2016
• Venue Allegations: Venue is alleged to be proper based on Defendant having registered to do business in Delaware, appointed a registered agent in the state, and consented to jurisdiction in prior cases.
• Core Dispute: Plaintiffs allege that Defendant’s filing of an Abbreviated New Drug Application (ANDA) for generic versions of the anticoagulant drug XARELTO® constitutes an act of infringement of two patents covering the active ingredient rivaroxaban and its methods of use.
• Technical Context: The technology relates to selective Factor Xa inhibitors, a class of modern oral anticoagulants used for the prevention and treatment of thromboembolic disorders such as deep vein thrombosis and stroke.
• Key Procedural History: This action was initiated under the Hatch-Waxman Act following Defendant’s submission of an ANDA containing a Paragraph IV certification, asserting that Plaintiffs’ patents are invalid, unenforceable, or will not be infringed by the proposed generic product. The complaint states that the patents-in-suit are listed in the FDA's "Orange Book" in connection with XARELTO®.

Case Timeline

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

U.S. Patent No. 7,157,456 - Substituted Oxazolidinones and Their Use in the Field of Blood Coagulation

• Patent Identification: U.S. Patent No. 7,157,456, “Substituted Oxazolidinones and Their Use in the Field of Blood Coagulation,” issued January 2, 2007.

The Invention Explained

• Problem Addressed: The patent describes significant disadvantages associated with anticoagulants available at the time, such as heparin and vitamin K antagonists (’456 Patent, col. 1:55-2:32). These disadvantages include oral ineffectiveness, a high risk of bleeding, a slow onset of action, and the need for frequent patient monitoring, making efficient and safe long-term prophylaxis of thromboembolic disorders difficult (’456 Patent, col. 2:4-32).
• The Patented Solution: The invention discloses a class of novel oxazolidinone derivatives that function as selective inhibitors of Factor Xa, an enzyme that plays a key role in the blood coagulation cascade (’456 Patent, Abstract; col. 2:33-48). By selectively targeting Factor Xa, the invention aims to provide a more targeted anticoagulant therapy that avoids the broader, less predictable effects of older drugs, thereby offering a more efficient and safer treatment option (’456 Patent, col. 2:62-67).
• Technical Importance: The development of an orally administered, selective Factor Xa inhibitor was a novel therapeutic approach intended to overcome the practical and safety limitations of previous generations of anticoagulants (’456 Patent, col. 2:50-54).

Key Claims at a Glance

• The complaint asserts claims 6 and 16 (Compl. ¶34).
• Claim 6 (dependent on claim 1) recites the specific compound:
  • 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide, also known as rivaroxaban.
• Claim 16 (dependent on claim 13) recites a method of use:
  • A method for treatment of a thromboembolic disorder,
  • wherein the disorder is deep venous thrombosis,
  • comprising administering an effective amount of a compound of claim 1.
• The complaint alleges infringement of "at least" these claims, reserving the right to assert others (Compl. ¶34).

U.S. Patent No. 7,592,339 - Substituted Oxazolidinones and Their Use in the Field of Blood Coagulation

• Patent Identification: U.S. Patent No. 7,592,339, “Substituted Oxazolidinones and Their Use in the Field of Blood Coagulation,” issued September 22, 2009.

The Invention Explained

• Problem Addressed: As a divisional of the application leading to the ’456 Patent, this patent addresses the same technical problem: the need for improved anticoagulants without the disadvantages of prior art therapies like heparin and coumarin derivatives, such as bleeding risks and the need for monitoring (’339 Patent, col. 2:1-40).
• The Patented Solution: The patent discloses methods of using specific oxazolidinone compounds, which are selective inhibitors of Factor Xa, for the prophylaxis and treatment of various thromboembolic disorders (’339 Patent, Abstract; col. 2:41-49). The core technical solution is identical to that described in the parent ’456 patent.
• Technical Importance: This patent protects specific methods of using the novel Factor Xa inhibitor, extending the intellectual property protection from the compound itself to its therapeutic applications (’339 Patent, col. 2:50-57).

Key Claims at a Glance

• The complaint asserts claim 10 (Compl. ¶34).
• Independent Claim 10 recites a method of use comprising:
  • A method for preventing a disorder due to thrombus formation selected from a group including myocardial infarct, stroke, pulmonary embolisms, and deep venous thromboses;
  • comprising administering an effective amount of the compound 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide (rivaroxaban) or a hydrate thereof.
• The complaint alleges infringement of "at least" this claim, reserving the right to assert others (Compl. ¶34).

III. The Accused Instrumentality

Product Identification

• Breckenridge’s ANDA Products, identified as 10 mg, 15 mg, and 20 mg oral tablets of rivaroxaban (Compl. ¶7).

Functionality and Market Context

• The products are identified as generic versions of Plaintiffs' XARELTO® products (Compl. ¶1, ¶31). The complaint alleges that Breckenridge's ANDA filing states that its products contain the active ingredient rivaroxaban (Compl. ¶32). The proposed product labeling allegedly directs the use of the generic tablets for indications covered by the patents-in-suit, including the reduction of stroke risk in patients with nonvalvular atrial fibrillation and the treatment and prophylaxis of deep vein thrombosis (DVT) and pulmonary embolism (PE) (Compl. ¶33).
• No probative visual evidence provided in complaint.

IV. Analysis of Infringement Allegations

The infringement allegations are statutory acts of infringement under 35 U.S.C. § 271(e)(2), based on the submission of ANDA No. 208220 to the FDA seeking approval to market a generic drug prior to patent expiration (Compl. ¶45, ¶51).

U.S. Patent No. 7,157,456 Infringement Allegations

U.S. Patent No. 7,592,339 Infringement Allegations

Identified Points of Contention

• Scope Questions: The complaint alleges that the proposed generic product contains the exact compound claimed in the ’456 Patent and that its label directs the methods of use claimed in both the ’456 and ’339 Patents. The primary dispute in such cases often shifts from literal infringement to the validity of the patents, an issue not raised in the complaint. A potential infringement dispute, however, could arise over claim construction. For the method claims, this raises the question of whether the specific language in Breckenridge's proposed label will be found to encourage, recommend, or promote every limitation of the asserted claims as construed by the court.

V. Key Claim Terms for Construction

The complaint does not provide sufficient detail for a deep analysis of claim construction disputes. However, based on the nature of the asserted method claims, certain terms may become central to the case.

• The Term: "preventing a disorder" (from Claim 10 of the ’339 Patent)
• Context and Importance: The scope of "preventing" is a recurring issue in pharmaceutical patent litigation. Defendant may argue that its product label, which allegedly teaches "to reduce the risk of stroke" (Compl. ¶33), does not meet the claim limitation of "preventing." The outcome of this construction could determine whether the label induces infringement.
• Intrinsic Evidence for Interpretation:
  • Evidence for a Broader Interpretation: The patent repeatedly uses the term "prophylaxis" in conjunction with "treatment" when describing the invention's purpose (’339 Patent, col. 2:50-51). Medical and legal practitioners often interpret "prophylaxis" to include risk reduction, which could support a broader construction of "preventing" that reads on the alleged label language.
  • Evidence for a Narrower Interpretation: A party seeking a narrower construction might argue that other language in the patent sets a higher bar, though the specification's consistent use of broad terms like "prophylaxis" and "controlling disorders" suggests such an argument could face challenges (’339 Patent, col. 2:50-51).

VI. Other Allegations

• Indirect Infringement: The complaint alleges active inducement of infringement of both patents. The factual basis for this allegation is that Breckenridge intends for its generic product to be used in accordance with its proposed labeling, which allegedly instructs physicians and patients to perform the patented methods of treatment and prevention (Compl. ¶33, ¶39, ¶48, ¶54).
• Willful Infringement: While the complaint does not use the term "willful," it alleges facts that could support such a claim. It states that Breckenridge has knowledge of the asserted patents and, notwithstanding this knowledge, has asserted its intent to manufacture and sell its product with an infringing label prior to patent expiration (Compl. ¶38). Plaintiffs also request a declaration that the case is "exceptional" for the purpose of awarding attorneys' fees under 35 U.S.C. § 285 (Compl., Prayer for Relief (g)).

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

This case presents a classic Hatch-Waxman dispute where the act of filing an ANDA is the central infringing act. The resolution will likely depend on the following core questions:

• A central issue will be one of patent validity: Although not detailed in the complaint, Breckenridge’s Paragraph IV certification implies an assertion that the patents-in-suit are invalid. The litigation will likely focus on whether the claims of the ’456 and ’339 patents withstand challenges based on prior art or other invalidity grounds.
• A key legal question will be one of induced infringement: Does the specific language of Breckenridge's proposed label, particularly its "risk reduction" phrasing, constitute instruction or encouragement to perform the methods claimed in the patents, which use terms like "treatment" and "preventing"?
• A subsidiary question will be one of claim construction: How will the court define the scope of key terms in the method claims, such as "preventing a disorder"? The interpretation of this and other terms will provide the framework for assessing both infringement and validity.