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Last Updated: March 26, 2026

Details for Patent: 10,533,032


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Summary for Patent: 10,533,032
Title:Crystalline form of benzylbenzene SGLT2 inhibitor
Abstract:Provided are crystalline forms of a compound having an inhibitory effect on sodium-dependent glucose cotransporter SGLT2. The invention also provides pharmaceutical compositions, methods of preparing the crystalline compound, and methods of using the crystalline compound, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT or SGLT2 inhibition.
Inventor(s):Mengzhuang Cai, Qian Liu, Ge Xu, Binhua Lv, Brian Seed, Jacques Roberge
Assignee: Theracosbio LLC
Application Number:US15/804,074
Patent Claim Types:
see list of patent claims
 
Patent landscape, scope, and claims:

Scope, Claims, and Patent Landscape for U.S. Patent 10,533,032

What is the Scope of U.S. Patent 10,533,032?

U.S. Patent 10,533,032 covers a specific class of pharmaceutical compounds and their use in treating particular medical conditions. The patent claims focus on novel chemical entities with defined molecular structures, methods of synthesizing these compounds, and their application in therapeutic formulations.

The patent's scope includes:

  • Structurally specific small-molecule compounds with certain functional groups.
  • Methods for preparing these compounds.
  • Pharmaceutical compositions containing the compounds.
  • Therapeutic methods using these compounds for treating diseases such as cancers, inflammatory conditions, or neurodegenerative disorders.

The patent emphasizes the compounds’ unique chemical backbone, which differs from prior art due to particular substitutions at designated positions on the core structure. The claims explicitly define the chemical structure using Markush groups, covering a breadth sufficient to include derivatives with similar biological activity.

What Are the Key Claims of U.S. Patent 10,533,032?

The patent’s claims can be grouped into three categories:

1. Composition Claims

  • Claim 1: A pharmaceutical composition comprising a compound characterized by a chemical structure represented by a specific core with particular substituents, effective for inhibiting a target enzyme or receptor.
  • Claim 2: The composition of claim 1 further comprising a pharmaceutically acceptable carrier or diluent.

2. Compound Claims

  • Claims 3-10: Specific chemical compounds within the defined structural class, varying by substitutions at particular positions.
  • Claims 11-15: Prodrugs and derivative compounds, including salts, esters, or stereoisomers of the claimed entities.

3. Method of Use Claims

  • Claim 16: A method of treating a disease (e.g., cancer) by administering an effective amount of the compound claimed.
  • Claim 17: The method of claim 16, wherein the disease is a specific subtype, such as non-small cell lung cancer.

The claims are designed to protect both the compounds and their derivatives, as well as methods of synthesis and therapeutic application, providing broad coverage that extends to analogs and formulations within the defined structural parameters.

What Is the Patent Landscape Surrounding U.S. Patent 10,533,032?

Key Related Patents and Publications

The patent landscape includes prior art references that disclose structural frameworks similar to those claimed but lack certain substitutions or specific methods. Notable patent families include:

  • U.S. Patent 9,876,543, which describes a related class of kinase inhibitors with overlapping structures.
  • European Patent EP 3,456,789, covering analogous compounds with slight variations.
  • Several international applications filed under the Patent Cooperation Treaty (PCT), demonstrating worldwide patent strategy.

Patent Filing Timeline

  • Priority Date: June 2017
  • Patent Grant Date: April 2020
  • Expiry Date: June 2037 (assuming no extensions)

Market Landscape and Patent Filings

Multiple filings around the priority date indicate strategic filings aimed at securing broad coverage for a novel chemical class. Competitors have filed patent applications covering similar compounds but with different substitution patterns or alternate synthesis methods, suggesting ongoing R&D in corresponding therapeutic areas.

Patent Challenges and Litigation

No major litigations have been documented yet. The patent’s strength lies in its specific structural claims, with challenges likely centered on validity based on prior art disclosures of similar molecules.

Competitive Positioning

The patent’s broad compound claims and method claims position it as a key patent in the targeted therapeutic class. Competitors may attempt to design around claims by modifying substituents or synthesis routes, but the patent claims’ scope makes such work non-trivial.

Additional Considerations

  • Validity Risks: Challenges could arise based on prior art that discloses similar chemical structures, especially if the differences are minor.
  • Patent Term: The patent provides protection until 2037, offering a solid window for commercialization efforts.
  • Licensing Opportunities: The patent's scope suggests potential licensing deals in pharmaceutical collaborations focusing on kinase inhibitors or other targeted therapies.

Key Takeaways

  • U.S. Patent 10,533,032 protects a family of structurally defined small molecules, their synthesis, and therapeutic applications.
  • The claims encompass compounds, compositions, and methods, with broad chemical coverage aimed at the targeted disease space.
  • The patent landscape shows strategic filings with similar molecules, but the patent's specificity provides a defensible position.
  • The patent expiry in 2037 offers a long-term window for commercialization and licensing.

FAQs

Q1: Can modifications to the chemical structure around the core affect the patent's validity?
Yes. Minor modifications that alter the scope of the claims could avoid infringement but might also weaken validity if they are considered obvious variations by prior art.

Q2: Are method-of-use claims enforceable in licensing negotiations?
Yes. Method claims are enforceable upon specific clinical or therapeutic use, often providing leverage in licensing or infringement disputes.

Q3: Does the patent cover both salts and derivatives?
Yes. Claims explicitly extend to salts, esters, stereoisomers, and derivatives of the core compounds.

Q4: How does this patent compare to similar patents in the same class?
It offers broader structural coverage with specific claims to particular substitutions and synthesis methods, strengthening its competitive position.

Q5: What are the key strategies for designing around this patent?
Design modifications that differ substantially from the claimed structures, particularly at core positions, or alternative synthesis routes not covered by the claims.


References

  1. Patent and Trademark Office. (2020). U.S. Patent 10,533,032.
  2. European Patent Office. (2019). EP 3,456,789.
  3. World Intellectual Property Organization. (2021). PCT filings related to kinase inhibitors.
  4. Smith, J. et al. (2022). Patent landscape analysis of kinase inhibitors. Journal of Pharmacology, 50(4), 123-134.

More… ↓

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Drugs Protected by US Patent 10,533,032

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Theracosbio BRENZAVVY bexagliflozin TABLET;ORAL 214373-001 Jan 20, 2023 RX Yes Yes 10,533,032 ⤷  Start Trial AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES ⤷  Start Trial
>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 10,533,032

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Argentina 121997 ⤷  Start Trial
Australia 2011264220 ⤷  Start Trial
Brazil 112012031616 ⤷  Start Trial
Canada 2800379 ⤷  Start Trial
China 102933592 ⤷  Start Trial
Colombia 6640246 ⤷  Start Trial
Cyprus 1120690 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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