Detailed Analysis of the Scope and Claims of United States Patent 10,550,081
Overview of the Patent
United States Patent 10,550,081, titled "Crystalline freebase forms of a biphenyl compound," is a significant patent in the pharmaceutical industry, particularly in the treatment of pulmonary disorders. Here is a detailed analysis of its scope, claims, and the broader patent landscape.
Patent Background
The patent was issued on February 4, 2020, to Theravance Biopharma R&D IP, LLC, with Grahame Woollam listed as the inventor. This patent is part of a series of patents related to the drug revefenacin, marketed under the brand name YUPELRI, which is used for the maintenance treatment of chronic obstructive pulmonary disease (COPD)[1][5].
Scope of the Patent
Crystalline Freebase Forms
The patent primarily focuses on two crystalline freebase forms of the biphenyl compound biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester. These forms, designated as Form III and Form IV, are anhydrous freebase crystal polymorphs. The crystalline freebases are characterized by their melting points, with Form III having a melting point of about 125°C and Form IV having a melting point of about 119°C[4][5].
Pharmaceutical Compositions
The patent describes various pharmaceutical compositions that include these crystalline freebases. These compositions can be formulated in different ways, such as in an aqueous isotonic saline solution buffered with citrate to a pH of about 5, or as part of a dry powder inhaler. The compositions are designed to be therapeutically effective for treating pulmonary disorders, including COPD and asthma[4].
Methods of Treatment
The patent outlines methods for treating pulmonary disorders by administering the crystalline freebase forms. This includes methods for producing bronchodilation and for antagonizing muscarinic receptors, which are key in managing symptoms of COPD and asthma[4].
Claims of the Patent
Independent Claims
The patent includes several independent claims that define the scope of the invention. These claims cover:
- Crystalline Freebase Forms: The specific crystalline freebase forms of the biphenyl compound, including their structural and physical properties.
- Pharmaceutical Compositions: The formulations that include the crystalline freebases, such as aqueous solutions and dry powder inhalers.
- Methods of Treatment: The methods for administering the crystalline freebases to treat pulmonary disorders[4].
Dependent Claims
Dependent claims further specify the details of the independent claims, including the preparation processes for the crystalline freebases, the intermediates involved, and the specific therapeutic uses of the compositions.
Patent Landscape
Related Patents
The patent 10,550,081 is part of a larger portfolio of patents related to revefenacin. Other relevant patents include:
- US8541451: Covers methods for treating COPD and is listed in the Orange Book as covering YUPELRI[2].
- US9765028: Relates to crystalline freebase forms of the biphenyl compound and is also listed in the Orange Book[2].
- US11008289: Another patent covering crystalline freebase forms and methods of treatment, issued to Theravance Biopharma R&D IP, LLC[5].
Patent Expiration Dates
The patent 10,550,081 is set to expire on July 14, 2030. Other related patents have expiration dates ranging from March 10, 2025, to October 31, 2028, and July 14, 2030[5].
Litigation and Enforcement
The patents related to revefenacin, including 10,550,081, are subject to litigation. For example, Theravance Biopharma and its partners have filed a complaint against Qilu Pharmaceutical Co., Ltd. and Qilu Pharma Inc. for patent infringement related to the filing of an Abbreviated New Drug Application (ANDA) for a generic version of YUPELRI[2].
Impact on the Pharmaceutical Industry
Innovation and Competition
The patent landscape around revefenacin highlights the complex interplay between innovation and competition in the pharmaceutical industry. The multiple patents covering different aspects of the drug ensure a period of exclusivity for the innovator companies, which can impact the timing and feasibility of generic entries into the market[3].
Patient Access
The expiration of these patents will eventually allow for the entry of generic versions of revefenacin, potentially increasing patient access to this critical medication for COPD. However, the ongoing litigation and the robust patent portfolio may delay this process[2][5].
Key Takeaways
- Crystalline Freebase Forms: The patent 10,550,081 specifically covers two crystalline freebase forms of a biphenyl compound used in treating COPD and asthma.
- Pharmaceutical Compositions: The patent describes various formulations and methods of administration for these crystalline freebases.
- Patent Landscape: The patent is part of a larger portfolio related to revefenacin, with multiple patents covering different aspects of the drug.
- Expiration Dates: The patent is set to expire on July 14, 2030, with other related patents expiring at various dates between 2025 and 2030.
- Litigation: Ongoing litigation related to these patents can impact the timing of generic entries into the market.
FAQs
What is the primary use of the drug covered by patent 10,550,081?
The primary use of the drug covered by patent 10,550,081 is the maintenance treatment of chronic obstructive pulmonary disease (COPD).
Who are the assignees of the patent 10,550,081?
The assignee of the patent 10,550,081 is Theravance Biopharma R&D IP, LLC.
What are the crystalline freebase forms described in the patent?
The patent describes two crystalline freebase forms, Form III and Form IV, which are anhydrous freebase crystal polymorphs of the biphenyl compound.
When is the patent 10,550,081 set to expire?
The patent 10,550,081 is set to expire on July 14, 2030.
What is the significance of the patent landscape around revefenacin?
The patent landscape around revefenacin ensures a period of exclusivity for the innovator companies, impacting the timing and feasibility of generic entries into the market.
Sources
- DrugBank: Revefenacin: Uses, Interactions, Mechanism of Action.
- Insight.RPXCorp: Case 2:24-cv-02689 Document 1 Filed 06/18/24.
- SSRN: Patent Claims and Patent Scope.
- Google Patents: US10550081B2 - Crystalline freebase forms of a biphenyl compound.
- Drugs.com: Generic Yupelri Availability.
