United States Patent 8,367,701 B2: A Detailed Analysis
Introduction
United States Patent 8,367,701 B2, titled "Crystalline pharmaceutical and methods of preparation and use thereof," was granted on February 5, 2013. This patent is significant in the pharmaceutical industry, particularly in the development of crystalline forms of a compound that inhibits LFA-1 (Lymphocyte Function-associated Antigen 1), a key protein involved in immune responses.
Inventors and Assignee
The patent was invented by John Burnier, Thomas Gadek, and Frederic Naud, and it is assigned to SARcode Bioscience Inc., now part of Kala Pharmaceuticals[4].
Background and Context
The patent revolves around the discovery and characterization of novel crystalline polymorphic forms of a compound with the formula I, which is a potent inhibitor of LFA-1. This compound has potential therapeutic applications, particularly in treating autoimmune diseases and inflammatory conditions.
Claims of the Patent
The patent includes several claims that define the scope of the invention:
Compound and Polymorphic Forms
- The patent claims novel crystalline polymorphic forms (Forms A, B, C, D, and E) of the compound with the formula I[4].
- These forms are characterized by their unique X-ray powder diffraction patterns, infrared spectra, and other physical properties.
Methods of Preparation
- The patent describes various methods for preparing these crystalline forms, including crystallization from different solvents and under various conditions[4].
Pharmaceutical Compositions
- Claims also cover pharmaceutical compositions containing these crystalline forms, which can be formulated into various dosage forms such as tablets, capsules, or solutions[4].
Methods of Use
- The patent includes claims for the use of these crystalline forms in treating diseases where LFA-1 inhibition is beneficial, such as autoimmune diseases and inflammatory conditions[4].
Prior Art and Related Patents
The patent builds upon a body of prior art related to pharmaceutical compounds and their crystalline forms. It references several earlier patents related to similar compounds and methods of preparation[1][4].
Patent Landscape
Litigation and Enforcement
- The patent has been part of broader patent litigation, as seen in cases where multiple patents, including this one, are collectively referred to as "Patents-in-Suit"[2].
- The patent's validity and scope can be subject to legal challenges, particularly in disputes involving generic drug manufacturers.
Regulatory Implications
- Patents like this one can significantly impact the regulatory approval process for generic drugs. For instance, listing patents in the Orange Book can delay FDA approval of generic versions, as seen in the context of the Hatch-Waxman Act and the Orange Book Transparency Act[5].
Continuation Applications and Prosecution Time
- The practice of filing continuation applications can extend the prosecution time of patents. While this patent itself does not appear to have multiple continuations, the broader trend in patent practice shows that continuations can significantly prolong the time a patent spends in prosecution, sometimes taking decades[3].
Impact on the Pharmaceutical Industry
- The discovery of novel crystalline forms and their methods of preparation can enhance the stability, bioavailability, and efficacy of pharmaceuticals.
- Patents like this one protect the intellectual property of pharmaceutical companies, allowing them to recoup investment in research and development.
Key Takeaways
- Novel Crystalline Forms: The patent introduces new crystalline polymorphic forms of a compound that inhibits LFA-1.
- Methods of Preparation: Detailed methods for preparing these forms are provided.
- Pharmaceutical Compositions: The patent covers various pharmaceutical compositions and dosage forms.
- Regulatory and Litigation Implications: The patent can influence the approval process for generic drugs and is subject to litigation.
- Industry Impact: Protects intellectual property and enhances the development of therapeutic agents.
FAQs
Q: What is the main subject matter of United States Patent 8,367,701 B2?
A: The patent covers novel crystalline polymorphic forms of a compound that inhibits LFA-1, along with methods for their preparation and use.
Q: Who are the inventors of this patent?
A: The inventors are John Burnier, Thomas Gadek, and Frederic Naud.
Q: What is the significance of the crystalline forms described in the patent?
A: These forms are characterized by unique physical properties and have potential therapeutic applications in treating autoimmune diseases and inflammatory conditions.
Q: How can this patent affect the approval of generic drugs?
A: Listing this patent in the Orange Book can delay FDA approval of generic versions of the drug, as it claims specific forms of the active ingredient.
Q: What is the typical prosecution time for patents with continuation applications?
A: Patents with continuation applications can take significantly longer to issue, sometimes taking decades, compared to original patent applications which average around 1.96 years[3].
Cited Sources
- United States Patent and Trademark Office. US 8,367,701 B2. Retrieved from https://patentimages.storage.googleapis.com/35/99/84/18fe32c1186d1c/US8367701.pdf
- RPX Corporation. IN THE UNITED STATES DISTRICT COURT FOR THE DISTRICT. Retrieved from https://insight.rpxcorp.com/litigation_documents/14892991
- Duke Law School. test - Duke Law School. Retrieved from https://web.law.duke.edu/cspd/articles/lemley.doc
- Google Patents. US8367701B2 - Crystalline pharmaceutical and methods of preparation and use thereof. Retrieved from https://patents.google.com/patent/US8367701B2/en
- United States Court of Appeals for the Federal Circuit. Teva Branded Pharmaceutical Products R&D, Inc.. Retrieved from https://cafc.uscourts.gov/opinions-orders/24-1936.OPINION.12-20-2024_2439730.pdf
