United States Patent 8,436,185: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 8,436,185, issued on May 7, 2013, is a significant patent in the pharmaceutical sector, particularly in the field of cancer treatment. This patent, assigned to Merck Sharp & Dohme Corp., pertains to pharmaceutically acceptable salts of a specific compound known as 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide, which is an inhibitor of the enzyme poly(ADP-ribose)polymerase (PARP).
Inventors and Assignees
The patent was invented by Jennifer R. Foley and Robert Darrin Wilson, and it is assigned to Merck Sharp & Dohme Corp., a major pharmaceutical company[1][5].
Background of the Invention
The compound in question, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide, is known for its role in inhibiting PARP, an enzyme involved in DNA repair. PARP inhibitors are particularly useful in treating cancers that are deficient in homologous recombination (HR) dependent DNA double-strand break repair, such as certain types of breast and ovarian cancers[1][2].
Scope of the Patent
Pharmaceutically Acceptable Salts
The patent covers various pharmaceutically acceptable salts of the compound, including but not limited to tosylate, hydrochloride, sulfate, benzenesulfonate, fumarate, and succinate salts. These salts are crucial for enhancing the solubility, stability, and bioavailability of the drug[1][5].
Therapeutic Uses
The compounds and their salts are useful as mono-therapies or in combination with other treatments for various conditions, including cancer. Specifically, they are effective in treating cancers that are deficient in HR-dependent DNA repair pathways. Additionally, these compounds have potential uses in reducing cell necrosis in conditions such as stroke and myocardial infarction[1].
Claims of the Patent
Independent Claims
The patent includes several independent claims that define the scope of the invention. These claims specify the chemical structure of the compound, its pharmaceutically acceptable salts, and the methods of preparing these salts. For instance, Claim 1 describes the compound 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide and its salts, while subsequent claims detail specific salt forms and their preparation methods[1][5].
Dependent Claims
Dependent claims further narrow down the scope by specifying particular aspects of the invention, such as the synthesis of specific salt forms, their crystalline structures, and their pharmaceutical formulations. These claims provide a detailed description of how the invention can be practiced and what constitutes an infringement[1].
Patent Landscape
Related Patents
Several other patents are related to this invention, either by covering different aspects of the same compound or by addressing similar therapeutic areas. For example:
- Patent 11,091,459: This patent, issued in 2021, covers specific solid forms of niraparib, another PARP inhibitor, and is set to expire on March 27, 2038[2].
- Patent 8,143,241: Issued in 2012, this patent relates to the use of PARP inhibitors in treating cancers deficient in HR-dependent DNA repair and is set to expire on August 12, 2027[2].
Expiration Dates
The patent 8,436,185 itself is set to expire 20 years from the date of its filing, which would be around January 8, 2029, assuming no extensions or adjustments under U.S.C. 154(b)[1][2].
Global Patent Filings
The invention has been protected through various international patent filings, including PCT applications and national phase entries in multiple countries. This global protection ensures that the patent holder has exclusive rights to the invention across different jurisdictions[1].
Impact on Innovation and Litigation
Patent Scope and Quality
The scope of this patent, like many others in the pharmaceutical sector, is subject to scrutiny regarding its breadth and clarity. Metrics such as independent claim length and independent claim count are used to assess patent scope and quality. Narrower claims, as seen in this patent, are generally associated with a higher probability of grant and a shorter examination process[3].
Litigation and Licensing
The patent's scope can influence litigation and licensing costs. Broader claims may lead to increased litigation costs due to disputes over infringement, while narrower claims can provide clearer boundaries, reducing the likelihood of legal challenges[3].
Processes for Preparation
The patent also describes methods for preparing the compound and its salts. These processes are detailed in other related patents, such as U.S. Pat. No. 8,071,623 and U.S. Pat. No. 9,580,407, which provide novel procedures and intermediates for the synthesis of niraparib[4].
Conclusion
United States Patent 8,436,185 is a critical piece of intellectual property in the field of cancer treatment, particularly for PARP inhibitors. The patent's scope, covering various pharmaceutically acceptable salts of the compound, ensures broad protection for the invention. Understanding the claims, related patents, and the broader patent landscape is essential for navigating the complex world of pharmaceutical innovation and litigation.
Key Takeaways
- The patent covers pharmaceutically acceptable salts of a PARP inhibitor.
- It includes specific claims for the compound and its salts.
- The patent is part of a larger landscape of related patents on PARP inhibitors.
- The expiration date is around January 8, 2029.
- The patent's scope and quality are crucial for innovation and litigation.
FAQs
What is the main compound covered by United States Patent 8,436,185?
The main compound is 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide, an inhibitor of the enzyme poly(ADP-ribose)polymerase (PARP).
Who are the inventors of this patent?
The inventors are Jennifer R. Foley and Robert Darrin Wilson.
What are the therapeutic uses of the compounds covered by this patent?
The compounds are useful in treating cancers deficient in HR-dependent DNA repair pathways and have potential uses in reducing cell necrosis in conditions such as stroke and myocardial infarction.
When is the patent set to expire?
The patent is set to expire around January 8, 2029, assuming no extensions or adjustments.
How does the patent landscape affect innovation and litigation in this field?
The patent landscape, including the scope and clarity of claims, influences innovation by defining what constitutes an infringement and affects litigation by determining the boundaries of legal disputes.
Sources
- United States Patent and Trademark Office, "Pharmaceutically acceptable salts of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide," US8436185B2, May 7, 2013.
- Drugs.com, "Generic Akeega Availability," November 6, 2024.
- Hoover Institution, "Patent Claims and Patent Scope," August 18, 2024.
- Justia Patents, "Processes for the preparation of Niraparib and intermediates thereof," February 23, 2021.
- Google Patents, "Pharmaceutically acceptable salts of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide," US8436185B2.
