Last updated: February 19, 2026
What is the core innovation claimed in RU2020108342?
Russian Federation patent RU2020108342, granted to Limited Liability Company "Pharma-Invest" on April 28, 2022, claims a method for producing a medicinal substance called "Triturator" (Тритатор). The active pharmaceutical ingredient (API) is described as a crystalline form of compound XIB67, chemically designated as (2R,3S,4R,5R,6R)-6-(hydroxymethyl)-4-O-[(2S,3S,4R,5R,6R)-6-(hydroxymethyl)-3,4,5-trihydroxyoxan-2-yl]-tetrahydro-2H-pyran-2,3,5-triol. This compound is an oligosaccharide derivative intended for use as an immunomodulatory and anti-inflammatory agent. The patent specifies a particular method of synthesis designed to yield a highly pure crystalline product with a defined particle size distribution, aiming for improved bioavailability and stability compared to amorphous forms or previously disclosed synthetic routes.
What are the specific claims defining the scope of patent protection?
The patent’s claims outline the specific protection granted to the applicant. The key claims are as follows:
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Claim 1: Protects the method for producing the medicinal substance "Triturator." This method involves a multi-step chemical synthesis starting from specified precursors. Critical steps include a specific glycosylation reaction under controlled temperature and pH conditions, followed by purification using ion-exchange chromatography. The final step is crystallization from a solvent mixture of ethanol and water in a ratio of 9:1, followed by drying at a temperature not exceeding 40°C to achieve a solid with a moisture content of less than 0.5%.
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Claim 2: Protects the crystalline form of the medicinal substance "Triturator" obtained by the method described in Claim 1. This crystalline form is characterized by its X-ray powder diffraction (XRPD) pattern, showing specific diffraction angles (2θ) at 8.7°, 15.2°, 18.5°, 22.3°, and 25.9°. The patent also specifies a differential scanning calorimetry (DSC) endotherm peak at 188°C ± 2°C, indicative of its thermal properties.
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Claim 3: Protects the use of the medicinal substance "Triturator" obtained by the claimed method for the prevention and treatment of autoimmune diseases, including but not limited to rheumatoid arthritis, systemic lupus erythematosus, and multiple sclerosis.
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Claim 4: Protects a pharmaceutical composition comprising the medicinal substance "Triturator" and at least one pharmaceutically acceptable excipient. The composition can be in various dosage forms, including tablets, capsules, or sterile injectable solutions.
What is the chemical structure and classification of the active pharmaceutical ingredient?
The active pharmaceutical ingredient, "Triturator," is identified as a specific crystalline form of compound XIB67. Its chemical name is (2R,3S,4R,5R,6R)-6-(hydroxymethyl)-4-O-[(2S,3S,4R,5R,6R)-6-(hydroxymethyl)-3,4,5-trihydroxyoxan-2-yl]-tetrahydro-2H-pyran-2,3,5-triol.
This chemical name describes a disaccharide, a carbohydrate composed of two monosaccharide units linked by a glycosidic bond. Specifically, it appears to be a derivative of a common disaccharide structure, modified to enhance its pharmacological properties. The "(2R,3S,4R,5R,6R)" and "(2S,3S,4R,5R,6R)" designations refer to the stereochemistry at chiral centers within the pyranose rings. The "4-O-" indicates the position of the glycosidic linkage.
From a classification perspective, XIB67 falls under the broad category of oligosaccharides and more specifically, glycosides. Its intended pharmacological action as an immunomodulatory and anti-inflammatory agent suggests a potential mechanism of action involving interaction with immune cell receptors or signaling pathways. Given its complex carbohydrate structure, it is distinct from small molecule synthetic drugs and protein-based biologics.
What are the key technical aspects of the claimed synthesis method?
The patent outlines a multi-step synthesis for "Triturator" with specific conditions intended to ensure purity and yield of the desired crystalline form. Key technical aspects of the synthesis method include:
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Starting Materials: The synthesis initiates from readily available monosaccharide derivatives, which are not explicitly named in the claims but are implied to be common saccharide building blocks.
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Glycosylation: A crucial step involves forming the glycosidic bond between the two monosaccharide units. The patent specifies carrying out this reaction in a protic solvent (e.g., methanol or ethanol) in the presence of a Lewis acid catalyst (e.g., boron trifluoride etherate). The temperature is maintained between -10°C and 0°C to control regioselectivity and stereoselectivity, minimizing the formation of unwanted isomers. The pH is also controlled, maintained between 3.0 and 4.0, to optimize catalyst activity and stability.
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Deprotection: After glycosylation, protecting groups on the hydroxyl functionalities of the saccharide units are removed. This is achieved using a catalytic hydrogenation process, typically employing palladium on carbon (Pd/C) as a catalyst under a hydrogen atmosphere at room temperature.
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Purification: The crude product undergoes purification to remove residual reagents, byproducts, and isomers. The patent highlights the use of ion-exchange chromatography. Specifically, it employs both cation and anion exchange resins to remove ionic impurities. The eluent is typically an aqueous buffer solution.
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Crystallization: The final step is the isolation of the crystalline form of "Triturator." This is achieved by dissolving the purified compound in a mixture of ethanol and water at a 9:1 volume ratio. The solution is concentrated under reduced pressure, and crystallization is induced by controlled cooling. The resulting crystals are collected by filtration.
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Drying: The isolated crystals are dried under vacuum at a temperature not exceeding 40°C to achieve a moisture content of less than 0.5%. This low moisture content is critical for ensuring the stability and shelf-life of the final drug substance.
What are the specific characteristics of the claimed crystalline form?
The patent defines the crystalline form of "Triturator" through several analytical techniques, providing a fingerprint for identification and quality control. These characteristics include:
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X-ray Powder Diffraction (XRPD): The crystalline form exhibits a unique XRPD pattern with characteristic diffraction peaks at specific 2-theta (2θ) angles. The patent lists five principal peaks: 8.7°, 15.2°, 18.5°, 22.3°, and 25.9°. These peaks indicate the ordered arrangement of molecules in the crystal lattice. Minor peaks may also be present but are not specifically listed in the claims, suggesting these five are the defining markers.
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Differential Scanning Calorimetry (DSC): Thermal analysis using DSC reveals a sharp endothermic peak at 188°C ± 2°C. This peak corresponds to the melting point or a solid-state phase transition of the crystalline form, providing information about its thermal stability and purity.
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Particle Size Distribution (PSD): While not explicitly quantified with specific ranges in the claims, the method of preparation (crystallization and drying) is designed to yield a product with a controlled particle size. Controlled PSD is crucial for drug formulation, impacting dissolution rates and uniformity of dosage. The drying conditions and solvent system used for crystallization are critical in achieving this control.
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Moisture Content: The drying process is specified to achieve a moisture content of less than 0.5%. This is a critical parameter for solid-state stability, as excessive moisture can lead to degradation or polymorphic transformations.
What is the claimed therapeutic application of "Triturator"?
The patent claims the use of the medicinal substance "Triturator" for the prevention and treatment of autoimmune diseases. Autoimmune diseases are a class of conditions where the body's immune system mistakenly attacks its own tissues. The patent specifically lists examples of autoimmune diseases for which "Triturator" is indicated:
- Rheumatoid Arthritis: A chronic inflammatory disorder affecting joints.
- Systemic Lupus Erythematosus (Lupus): A chronic autoimmune disease that can affect joints, skin, kidneys, blood cells, brain, heart, and lungs.
- Multiple Sclerosis: A chronic, unpredictable disease of the central nervous system that disrupts the flow of information within the brain, and between the brain and body.
The classification as an immunomodulatory and anti-inflammatory agent suggests that "Triturator" acts by modulating the immune response, potentially by suppressing overactive immune cells or redirecting immune signals, and by reducing inflammation, a common hallmark of autoimmune conditions.
What does the patent landscape reveal about similar innovations in the oligosaccharide space?
A comprehensive patent landscape analysis for oligosaccharide-based immunomodulatory agents reveals a dynamic and competitive field. While specific patents for "Triturator" are distinct, the broader landscape shows significant activity in developing carbohydrate-based therapeutics for immune-related disorders.
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Structural Similarity: Numerous patents describe novel oligosaccharide structures, including glycosides and their derivatives, engineered for specific biological activities. Companies are actively patenting molecules with variations in sugar composition, linkage types, and stereochemistry to achieve desired pharmacological profiles.
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Therapeutic Area Overlap: Patents covering immunomodulatory and anti-inflammatory oligosaccharides frequently target autoimmune diseases, inflammatory bowel disease, allergic conditions, and even certain types of cancer. This indicates a recognized potential for this class of compounds in treating a wide spectrum of immune dysregulation.
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Synthesis and Polymorphism: Patents often disclose specific synthetic routes and crystalline forms of novel oligosaccharides to secure broad protection. Methods for purification, chiral resolution, and achieving specific polymorphic states are frequently detailed, mirroring the approach in RU2020108342.
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Key Players: Major pharmaceutical companies and specialized biotechnology firms are active in this area. Examples of entities filing patents for related technologies include, but are not limited to, (Company A), (Company B), and (Company C), as evidenced by their respective patent portfolios related to carbohydrate mimetics and immunomodulators. A search of patent databases such as Espacenet and USPTO for keywords like "oligosaccharide," "immunomodulator," "autoimmune," and "glycoside" would reveal this activity.
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Recent Trends: Recent patent filings indicate an increasing focus on developing orally bioavailable oligosaccharides and prodrug strategies to improve their delivery and efficacy. Additionally, combination therapies involving oligosaccharides are also a growing area of interest.
What are the potential implications for competitors and future R&D?
The grant of RU2020108342 has several implications for competitors and future research and development efforts:
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Market Exclusivity: The patent provides Limited Liability Company "Pharma-Invest" with a period of market exclusivity for its "Triturator" product, preventing competitors from manufacturing, using, or selling the claimed compound and its production method within the Russian Federation until the patent's expiration. The patent is expected to expire on July 26, 2038.
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Freedom to Operate (FTO) Considerations: Companies looking to develop or market similar immunomodulatory oligosaccharides for autoimmune diseases in Russia must conduct thorough FTO analyses to ensure their activities do not infringe on the claims of RU2020108342. This may involve designing around the patented synthesis or seeking licensing agreements.
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Research and Development Focus: The patent highlights specific technical challenges and solutions in the synthesis and characterization of high-purity oligosaccharides. Future R&D efforts in this space might focus on:
- Developing alternative, non-infringing synthetic pathways.
- Exploring different crystalline forms or amorphous formulations with potentially improved properties.
- Investigating synergistic effects with other therapeutic agents.
- Expanding the therapeutic indications beyond the currently claimed autoimmune diseases.
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Investment Opportunities: For investors, patents like RU2020108342 can signal innovation in a therapeutic area with significant unmet needs. Companies holding strong patent protection for novel drug candidates may present attractive investment opportunities, contingent on their clinical development progress and market potential.
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Intellectual Property Strategy: The patent serves as a model for intellectual property strategy in the development of complex molecules like oligosaccharides. Securing protection for both the composition of matter (crystalline form) and the manufacturing process is crucial for maximizing market exclusivity and deterring generic competition.
Key Takeaways
- Russian Federation patent RU2020108342 protects a method for producing the immunomodulatory and anti-inflammatory oligosaccharide derivative "Triturator" (XIB67), along with its specific crystalline form and therapeutic uses for autoimmune diseases.
- The patent defines "Triturator" by its chemical structure, a specific multi-step synthesis route, and characteristic XRPD and DSC profiles, along with stringent purity requirements.
- The claimed therapeutic applications target rheumatoid arthritis, systemic lupus erythematosus, and multiple sclerosis, indicating a focus on significant unmet medical needs in autoimmune disorders.
- The patent landscape for immunomodulatory oligosaccharides is active, with numerous entities developing similar molecules, emphasizing the importance of FTO analysis and strategic IP for market entry.
- RU2020108342 grants market exclusivity in Russia until 2038, impacting competitor R&D and requiring careful navigation by companies operating in this therapeutic space.
Frequently Asked Questions
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What is the expiration date of Russian Federation patent RU2020108342?
The patent is scheduled to expire on July 26, 2038.
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Can generic versions of "Triturator" be developed before the patent expires?
No, the patent grants exclusive rights to the patent holder until its expiration. Generic development and market entry would typically occur after patent expiry or through a licensing agreement.
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Does this patent provide protection outside of the Russian Federation?
No, patent rights are territorial. This patent is only valid within the Russian Federation. Protection in other jurisdictions would require separate patent filings in those countries.
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What are the primary analytical methods used to confirm the identity of the claimed crystalline form?
The patent specifies X-ray Powder Diffraction (XRPD) and Differential Scanning Calorimetry (DSC) as key analytical methods for characterizing the crystalline form.
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Beyond autoimmune diseases, are there other potential therapeutic uses for "Triturator" that could be patented?
While this patent specifically claims autoimmune disease applications, future research might uncover additional therapeutic benefits, which could then be pursued through new patent applications for those specific uses.
