| Abstract: | The present invention provides iRNA agents comprising at least one subunit of the formula (I): ##STR00001## wherein: A and B are each independently for each occurrence O, N(R.sup.N) or S; X and Y are each independently for each occurrence H, OH, a hydroxyl protecting group, a phosphate group, a phosphodiester group, an activated phosphate group, an activated phosphite group, a phosphoramidite, a solid support, --P(Z')(Z'')O-nucleoside, --P(Z')(Z'')O-oligonucleotide, a lipid, a PEG, a steroid, a lipophile, a polymer, --P(Z')(Z'')O-Linker-OP(Z''')(Z'''')O-oligonucleotide, a nucleotide, an oligonucleotide, --P(Z')(Z'')-formula (I), --P(Z')(Z'')-- or -Linker-R; R is L.sup.G, -Linker-L.sup.G, or has the structure shown below: ##STR00002## L.sup.G is independently for each occurrence a carbohydrate, e.g., monosaccharide, disaccharide, trisaccharide, tetrasaccharide, oligosaccharide, polysaccharide; R.sup.N is independently for each occurrence H, methyl, ethyl, propyl, isopropyl, butyl, or benzyl; and Z', Z'', Z''' and Z'''' are each independently for each occurrence O or S. |
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Patent landscape, scope, and claims: |
Understanding the Scope and Claims of United States Patent 8,106,022
Introduction
United States Patent 8,106,022, titled "Carbohydrate conjugates as delivery agents for oligonucleotides," is a significant patent in the field of therapeutic agent delivery, particularly focusing on the use of carbohydrate conjugates for the in vivo delivery of oligonucleotides. Here, we will delve into the details of the patent's scope, claims, and the broader patent landscape surrounding this invention.
Background
The patent, issued on January 3, 2012, is part of a series of continuations and continuations-in-part, tracing back to initial filings in 2007 and 2008. This patent is assigned to Alnylam Pharmaceuticals, Inc., a company renowned for its work in RNA interference (RNAi) therapeutics[1].
Field of Invention
The patent pertains to the field of therapeutic agent delivery, specifically using carbohydrate conjugates to enhance the delivery of oligonucleotides, such as small interfering RNA (siRNA) and microRNA (miRNA). These conjugates are designed to improve the stability, targeting, and cellular uptake of oligonucleotides, which are crucial for their therapeutic efficacy[1].
Claims
The patent includes several key claims that define its scope:
Independent Claims
- The patent claims novel carbohydrate conjugates and iRNA agents comprising these conjugates. These claims are broad and cover various aspects of the conjugates, including their structure, composition, and methods of preparation[1].
Dependent Claims
- Dependent claims further specify the types of carbohydrates, the linkers used, and the methods for introducing these iRNA agents into cells. These claims provide detailed descriptions of how the conjugates are made and how they function[1].
Method Claims
- The patent also includes method claims that describe the processes for making these compositions and introducing the iRNA agents into cells. These methods are critical for the therapeutic application of the oligonucleotides[1].
Scope of the Patent
The scope of the patent is extensive and covers several key areas:
Carbohydrate Conjugates
- The patent describes various carbohydrate conjugates that can be used to deliver oligonucleotides. These conjugates are designed to target specific tissues or cells, enhancing the therapeutic efficacy of the oligonucleotides[1].
iRNA Agents
- The iRNA agents, including siRNA and miRNA, are central to the patent. These agents are used to silence specific genes, and the carbohydrate conjugates play a crucial role in their delivery and stability[1].
Therapeutic Applications
- The patent outlines various therapeutic applications for these iRNA agents, including the treatment of disease conditions such as genetic disorders, viral infections, and cancer[1].
Patent Landscape
Continuation and Continuation-in-Part Patents
- The patent is part of a series of continuation and continuation-in-part applications, indicating a continuous effort to refine and expand the original invention. This strategy helps in maintaining a robust patent portfolio and extending the protection period[1].
Related Patents
- Other patents, such as US 8,828,956, US 8,450,467, and US 9,397,975, are related to this patent and provide additional protection for various aspects of the carbohydrate conjugates and iRNA agents. These patents collectively form a comprehensive patent strategy for Alnylam Pharmaceuticals[4].
Expiration Dates
- The patent expires 20 years from the date of the earliest non-provisional application, which in this case would be around 2028, considering the initial filing dates. However, the exact expiration date can be influenced by various factors, including patent term adjustments and extensions[5].
Practical Implications
Drug Development
- This patent has significant implications for drug development, particularly in the field of RNAi therapeutics. The carbohydrate conjugates described in the patent have been used in drugs like Amvuttra (patent US 8,106,022 is one of the foundational patents for Amvuttra's delivery agents)[4].
Patent Strategy
- Alnylam's patent strategy, as evident from this and related patents, involves a thorough and continuous approach to protecting their intellectual property. This includes filing multiple patents to cover different aspects of the invention and ensuring comprehensive protection in various jurisdictions[4].
Industry Impact
Innovation and Competition
- The patent has contributed to the advancement of RNAi therapeutics by providing innovative solutions for oligonucleotide delivery. However, it also sets a high bar for competitors, who must navigate around these patents or seek licenses to use similar technologies[3].
Licensing and Litigation
- The broad scope of the patent claims can lead to licensing and litigation issues. Companies may need to negotiate licenses or face potential litigation if they develop similar technologies without proper authorization[3].
Key Takeaways
- Carbohydrate Conjugates: The patent introduces novel carbohydrate conjugates for delivering oligonucleotides, enhancing their stability and cellular uptake.
- iRNA Agents: The patent covers iRNA agents, including siRNA and miRNA, and their therapeutic applications.
- Comprehensive Protection: The patent is part of a robust patent portfolio that includes multiple related patents to ensure comprehensive protection.
- Expiration Dates: The patent expires around 2028, but this date can be influenced by various factors.
- Industry Impact: The patent has significant implications for drug development and sets a high bar for competitors in the field of RNAi therapeutics.
FAQs
Q: What is the main focus of United States Patent 8,106,022?
A: The main focus is on carbohydrate conjugates as delivery agents for oligonucleotides, such as siRNA and miRNA.
Q: Who is the assignee of this patent?
A: The assignee is Alnylam Pharmaceuticals, Inc.
Q: What are the therapeutic applications of the iRNA agents described in the patent?
A: The therapeutic applications include the treatment of genetic disorders, viral infections, and cancer.
Q: How does this patent fit into Alnylam's broader patent strategy?
A: It is part of a comprehensive patent strategy that includes multiple related patents to ensure broad protection for their RNAi therapeutics.
Q: What is the expected expiration date of this patent?
A: The patent is expected to expire around 2028, considering the initial filing dates and standard patent term.
Sources
- Justia Patents: Carbohydrate conjugates as delivery agents for oligonucleotides.
- Drugs.com: Generic Oxlumo Availability.
- SSRN: Patent Claims and Patent Scope.
- Patsnap: siRNA Drug Amvuttra Patent Research and Practical Operation Guide.
- Drugs.com: Generic Amvuttra Availability.
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