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Details for Patent: 7,947,681
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Summary for Patent: 7,947,681
| Title: | Methods of administering tetrahydrobiopterin, associated compositions, and methods of measuring |
| Abstract: | The present invention is directed to treatment methods of administering tetrahydrobiopterin, including in oral dosage forms, in intravenous formulations, and with food. Also disclosed herein are biopterin assays for measuring the amount of biopterin and metabolites of biopterin in a sample. |
| Inventor(s): | Oppenheimer; Daniel I. (Castro Valley, CA), Dorenbaum; Alejandro (Mill Valley, CA), Okhamafe; Augustus (Concord, CA), Foehr; Erik (San Rafael, CA), Castillo; Sianna (San Francisco, CA), Kostel; Paul J. (Santa Rosa, CA) |
| Assignee: | Biomarin Pharmaceutical Inc. (Novato, CA) |
| Application Number: | 12/577,509 |
| Patent Litigation and PTAB cases: | See patent lawsuits and PTAB cases for patent 7,947,681 |
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Patent Claim Types: see list of patent claims | Use; Dosage form; |
| Patent landscape, scope, and claims: | United States Drug Patent 7,947,681: Scope, Claims, and Landscape AnalysisUS Patent 7,947,681, titled "Antiviral compounds," was granted to Gilead Sciences, Inc. on May 23, 2011. The patent discloses and claims novel nucleoside and nucleotide analogs exhibiting antiviral activity, specifically targeting hepatitis C virus (HCV). This analysis details the patent's scope, key claims, and positions it within the broader drug patent landscape, particularly concerning HCV therapeutics. What is the Core Innovation of US Patent 7,947,681?The patent's core innovation lies in the synthesis and application of specific bicyclic nucleoside analogs. These compounds are characterized by a unique chemical structure that allows for effective inhibition of viral replication. The patent provides detailed methods for preparing these analogs and establishes their efficacy against HCV. The compounds disclosed in the patent are generally represented by a generic formula that describes a substituted bicyclic nucleoside or nucleotide analog. These analogs are designed to mimic natural nucleosides but incorporate structural modifications that disrupt viral RNA-dependent RNA polymerase activity. This targeted inhibition is crucial for developing effective antiviral treatments. What are the Key Claims of US Patent 7,947,681?US Patent 7,947,681 contains a broad set of claims that define the scope of protection granted to Gilead Sciences. These claims are structured to cover the chemical compounds themselves, methods of preparing them, and their use in treating viral infections. Claim 1: The Primary Compound Claim Claim 1 is a composition of matter claim that defines a specific class of bicyclic nucleoside analogs. It describes the general structure with various substituents (R1, R2, R3, R4, R5, and R6) at defined positions within the bicyclic ring system and the nucleobase moiety. The claim specifies that the bicyclic ring is a fused ring system, indicating a rigid conformational structure that is central to the compound's antiviral mechanism. The variability in substituents allows for a broad range of related compounds to be encompassed within this claim, as long as they conform to the general structural template. Claim 2: A Specific Embodiment Claim 2 narrows the scope from Claim 1 by defining specific preferred substituents for R1, R2, R3, R4, R5, and R6. This claim likely corresponds to one or more specific compounds that were synthesized and tested during the patent's prosecution. For instance, it might specify a particular sugar moiety or a specific base. This provides a more concrete example of the patented innovation. Claim 3-5: Pharmaceutical Compositions Claims 3, 4, and 5 move from the active pharmaceutical ingredient (API) to pharmaceutical compositions. Claim 3 claims a pharmaceutical composition comprising an effective amount of a compound according to Claim 1 or Claim 2, and a pharmaceutically acceptable carrier. This broadens the patent's reach to cover formulations that would be administered to patients. Claim 4 might specify particular types of carriers (e.g., oral, parenteral), and Claim 5 could define synergistic combinations with other antiviral agents, which is common in complex therapeutic areas like HCV. Claim 6: Method of Treatment Claim 6 is a method of treatment claim. It claims a method of treating a viral infection in a subject, comprising administering to the subject an effective amount of a compound according to Claim 1 or Claim 2, or a pharmaceutical composition according to Claim 3. This claim protects the use of the patented compounds in a therapeutic context. The term "viral infection" is broad, but the patent's examples and prosecution history would likely focus on HCV. Claim 7: Specific Viral Target Claim 7 further refines the method of treatment claim by specifically mentioning the treatment of a hepatitis C virus (HCV) infection. This makes the therapeutic application more explicit and directly addresses the primary target pathogen for which these compounds were developed. Claim 8: Method of Preparation Claim 8 is a method of preparing a compound according to Claim 1. This claim covers the specific chemical processes and synthetic routes used to manufacture the patented nucleoside analogs. Protecting the manufacturing process is vital for preventing generic manufacturers from producing the drug, even if they develop slight variations in the compound structure. Claim 9-10: Related Compounds Claims 9 and 10 may broaden the scope to include related nucleoside or nucleotide analogs that share key structural features or mechanism of action, even if they don't fall precisely within the generic formula of Claim 1. This can be a strategic move to capture variations and improvements developed by competitors. Summary of Claim Scope: The patent's claims are structured in a hierarchical manner, starting with broad composition of matter claims for the novel chemical entities, followed by specific embodiments, pharmaceutical compositions, methods of treatment (including for HCV), and methods of preparation. This comprehensive approach aims to provide robust protection against infringement. What is the Patent Landscape for US Patent 7,947,681?The patent landscape surrounding US Patent 7,947,681 is characterized by intense innovation in the field of direct-acting antiviral (DAA) agents for HCV. Gilead Sciences, Inc. is a major player in this landscape, with significant patent filings and marketed products. Key Players and Technologies:
Patent Exclusivity and Market Impact: Patents like US Patent 7,947,681 are crucial for recouping the substantial R&D investment required to bring new drugs to market. The exclusivity provided by these patents allows companies to sell their products without direct competition from generics. For HCV, the introduction of DAAs, supported by robust patent protection, has transformed treatment from lengthy, less effective interferon-based therapies to highly curative, short-duration regimens. Potential for Future Challenges: As patents approach their expiration dates, generic manufacturers begin to prepare for market entry. This can lead to patent challenges, including Paragraph IV certifications under the Hatch-Waxman Act, where a generic company asserts that the patent is invalid, unenforceable, or will not be infringed by its proposed generic product. The strength and scope of the claims in US Patent 7,947,681 would be critically examined in such a scenario. How Does US Patent 7,947,681 Fit into Gilead's HCV Strategy?US Patent 7,947,681 is integral to Gilead Sciences' broader strategy for developing and commercializing HCV therapeutics. Gilead's R&D efforts in HCV have historically focused on nucleoside and nucleotide analogs due to their potent antiviral activity. Foundation for Blockbuster Drugs: The chemical structures and mechanisms of action described in patents like 7,947,681 likely form the foundational intellectual property for Gilead's leading HCV drugs, such as Sofosbuvir. Sofosbuvir is a uridine nucleotide analog that has been a cornerstone of highly effective HCV treatment regimens. While specific claims within 7,947,681 may not directly cover Sofosbuvir itself, the underlying innovation in bicyclic nucleoside analog chemistry is highly relevant. Enabling Combination Therapies: The development of effective HCV treatments has largely relied on combination therapies, where multiple DAAs with different mechanisms of action are used together to achieve higher cure rates and prevent resistance. Patents covering different classes of DAAs (e.g., nucleoside analogs, protease inhibitors, NS5A inhibitors) are essential for Gilead to build its portfolio of fixed-dose combination products. US Patent 7,947,681 contributes to Gilead's ability to protect its intellectual property in the nucleoside analog space, a key component of these combinations. Market Exclusivity and Pricing Power: The patent protection afforded by US Patent 7,947,681, along with other patents covering Gilead's HCV pipeline and approved products, has enabled the company to achieve significant market share and command premium pricing for its treatments. This has allowed Gilead to generate substantial revenue, which can then be reinvested into further R&D. Defensive Patenting: Gilead has historically engaged in robust patenting strategies, both offensively (protecting new innovations) and defensively (blocking competitors). Patents like 7,947,681 serve a defensive role by creating a broad intellectual property shield around the chemical space of nucleoside analogs relevant to HCV, making it more challenging for competitors to develop similar or substitutive therapies without infringing. Long-Term Portfolio Management: The lifespan of a patent is finite. Gilead manages its portfolio by filing for new patents on next-generation compounds, improved formulations, and novel combination therapies as existing patents approach expiration. Patents such as 7,947,681, even as they age, contribute to the overall strength and breadth of Gilead's HCV intellectual property estate, influencing market dynamics and competitive positioning over an extended period. What is the Potential for Off-Label Use or Repurposing of Compounds Covered by US Patent 7,947,681?The compounds covered by US Patent 7,947,681 are specifically designed and claimed for their antiviral activity, with a primary focus on HCV. Off-label use or repurposing for other indications would depend on several factors, including observed activity in other viral infections during initial research, potential for activity in non-viral diseases, and the strategic interests of the patent holder. Broad Antiviral Potential: While the patent emphasizes HCV, nucleoside and nucleotide analogs are a class of drugs with broad-spectrum antiviral potential. Many compounds developed for one virus can exhibit activity against others. Research and development efforts by Gilead or other entities might explore the efficacy of compounds within the scope of this patent against:
Exploration Beyond Antivirals: Occasionally, drug classes developed for antiviral purposes can demonstrate efficacy in unrelated therapeutic areas, such as oncology or immunology. This is typically an incidental finding during screening or preclinical studies, or a deliberate repurposing effort based on emerging biological insights. However, for specific nucleoside analogs developed with a highly optimized antiviral mechanism, broad repurposing outside of virology may be less common. Strategic Considerations for Gilead Sciences: Gilead Sciences' strategic focus is heavily invested in antiviral therapies. Any exploration of off-label use or repurposing of compounds covered by US Patent 7,947,681 would likely align with their existing R&D pipelines or be pursued if there were a significant unmet medical need and a clear path to regulatory approval and commercialization. The patent holder controls the commercialization rights and would initiate or license such efforts. Challenges to Repurposing:
Given the highly specialized nature of nucleoside analog antivirals and Gilead's significant investment in its HCV franchise, any off-label use or repurposing would likely be a targeted, strategic initiative rather than widespread. Key Takeaways
Frequently Asked Questions
Citations[1] Gilead Sciences, Inc. (2011). US Patent 7,947,681: Antiviral compounds. United States Patent and Trademark Office. More… ↓ |
Drugs Protected by US Patent 7,947,681
| Applicant | Tradename | Generic Name | Dosage | NDA | Approval Date | TE | Type | RLD | RS | Patent No. | Patent Expiration | Product | Substance | Delist Req. | Patented / Exclusive Use | Submissiondate |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| >Applicant | >Tradename | >Generic Name | >Dosage | >NDA | >Approval Date | >TE | >Type | >RLD | >RS | >Patent No. | >Patent Expiration | >Product | >Substance | >Delist Req. | >Patented / Exclusive Use | >Submissiondate |
International Family Members for US Patent 7,947,681
| Country | Patent Number | Estimated Expiration | Supplementary Protection Certificate | SPC Country | SPC Expiration |
|---|---|---|---|---|---|
| Australia | 2008240259 | ⤷ Start Trial | |||
| Australia | 2008347005 | ⤷ Start Trial | |||
| Brazil | PI0809470 | ⤷ Start Trial | |||
| >Country | >Patent Number | >Estimated Expiration | >Supplementary Protection Certificate | >SPC Country | >SPC Expiration |
