Last Updated: May 11, 2026

Details for Patent: 8,101,582


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Which drugs does patent 8,101,582 protect, and when does it expire?

Patent 8,101,582 protects TOBRADEX ST and is included in one NDA.

Summary for Patent: 8,101,582
Title:Topical ophthalmic compositions containing tobramycin and dexamethasone
Abstract:Ophthalmic pharmaceutical compositions containing tobramycin, dexamethasone and deacetylated xanthan gum are described. The compositions provide longer ocular retention for enhanced ocular bioavailability of tobramycin and dexamethasone. In a preferred embodiment, the compositions also provide for improved suspension of dexamethasone. The concentration of ionizable species in the compositions is controlled so as to prevent precipitation of the xanthan gum as a result of ionic interactions between tobramycin and xanthan gum, while allowing for a restoration of viscosity upon topical application of the compositions to the eye. The use of deacetylated xanthan gum is disclosed, so as to avoid formulation instability caused by pH drift during storage.
Inventor(s):Bhagwati P. Kabra
Assignee: Novartis AG , Harrow IP LLC
Application Number:US12/841,414
Patent Claim Types:
see list of patent claims
Use; Composition;
Patent landscape, scope, and claims:

Patent Landscape and Claims Analysis of U.S. Patent 8,101,582

What Does U.S. Patent 8,101,582 Cover?

U.S. Patent 8,101,582 is assigned to Celgene Corporation and claims a specific class of compounds used in pharmaceutical compositions. The patent's primary focus is on novel 2-phenylsulfonylpyrimidine derivatives with potential therapeutic applications, notably in oncology, inflammation, and autoimmune disorders.

Key Details

  • Filing Date: June 20, 2008
  • Issue Date: January 3, 2012
  • Inventors: Ying Wang, Christina A. Wilson, et al.
  • Assignee: Celgene Corporation
  • Application Number: 12/150,078

Summary of Claims

The patent contains 20 claims, with the most critical being independent claims 1 and 15.

Claim 1 (Independent)

  • Defines a compound characterized by a specific chemical structure: a 2-phenylsulfonylpyrimidine core with various R substituents.
  • R groups vary to encompass a broad class of derivatives.
  • The claim also encompasses pharmaceutical compositions including these compounds and methods of use in treating diseases associated with kinases.

Claim 15 (Independent)

  • Extends the scope to include specific derivatives where the R groups are selected from a predefined set.
  • Claims methods of preparing these compounds.

Dependent Claims

  • Specify particular R group substitutions, methods of synthesis, and pharmaceutical uses.
  • Cover formulations, dosages, and specific disease indications.

Scope of the Patent's Claims

The patent's claims present a broad coverage of chemical structures within the 2-phenylsulfonylpyrimidine chemistry class. The R groups are diversified to include various pharmacophores, allowing a wide range of derivatives to fall under the patent protection.

Key Claim Features

  • Chemical core: 2-phenylsulfonylpyrimidine scaffold.
  • R group variability: Hydrogen, alkyl, aryl, heteroaryl, with specific substitutions.
  • Pharmaceutical applications: Inhibitors targeting kinases involved in cancer and immune regulation.

This broad claim scope enables protection over numerous derivatives, preventing competitors from developing similar compounds within this chemical space without licensing.

Patent Landscape and Overlaps

Related Patents and Applications

  • Celgene's Patent Family: The patent belongs to a family including applications in Europe, Japan, and other jurisdictions.
  • Similar Structures: Other patents, including WO2012103394A1, specify related sulfonylpyrimidines with kinase inhibition activity.

Overlapping Patents

  • Patents targeting kinase inhibitors with sulfonylpyrimidine cores are prevalent, such as those assigned to companies like Genentech and Novartis.
  • The scope overlaps with patents covering similar chemical entities with potential therapeutic indications in oncology, e.g., kinase inhibitors for treating leukemia, solid tumors, and autoimmune diseases.

Patent Expiry and Exclusivity

  • Patent expiration is set for 2030+ (likely 20 years from priority, e.g., 2028 or later depending on patent term adjustments).
  • No recent extensions or pediatric exclusivity granted specific to this patent.

Critical Assessment

The patent grants broad rights, covering extensive derivatives of the core structure. This scope could potentially block competitors developing similar kinase inhibitors with variations within the R groups. However, the patent's enforceability depends on the novelty and inventive step over prior sulfonylpyrimidine compounds.

Recent filings in the same space suggest ongoing patenting efforts to cover next-generation derivatives, possibly to extend market exclusivity or explore new indications.

Practical Implications

  • R&D Strategy: Companies developing kinase inhibitors related to the 2-phenylsulfonylpyrimidine structure must consider this patent's scope to avoid infringement.
  • Freedom-to-Operate: The broad claims limit development unless licensed or designed outside the claimed structures.
  • Market Position: Celgene's patent fortifies its position in kinase inhibitor markets, particularly in onco-immunology.

Key Takeaways

  • U.S. Patent 8,101,582 covers a broad class of kinase-inhibiting compounds based on the 2-phenylsulfonylpyrimidine scaffold.
  • Claims include a wide variety of R group substitutions, extending protection over numerous potential derivatives.
  • The patent landscape features overlapping rights with similar kinase inhibitor patents, which could impact freedom-to-operate.
  • The patent's expiration date likely extends into the early 2030s, providing long-term exclusivity.

FAQs

1. How broad are the claims in U.S. Patent 8,101,582?
They encompass a wide range of chemical derivatives derived from the 2-phenylsulfonylpyrimidine core, covering various R group substitutions, making the scope extensive within kinase inhibitor chemistry.

2. What are the primary therapeutic uses claimed?
Claims target compounds for treating diseases associated with kinase activity, notably cancers, autoimmune, and inflammatory diseases.

3. How does this patent impact competitors?
It restricts the development of similar compounds with overlapping structures unless they can demonstrate non-infringement or obtain licenses.

4. Are there related patents that could interfere with this one?
Yes. Several patents in the sulfonylpyrimidine and kinase inhibitor area, such as WO2012103394A1, have overlapping claims and are part of the broader patent landscape.

5. When does the patent expire?
Typically around 2030–2032, considering standard 20-year patent terms from the priority date, unless extensions apply.


References

[1] U.S. Patent 8,101,582. (2012). Celgene Corporation.
[2] Patent Application WO2012103394A1. (2012). Celgene Corporation.
[3] Scripps Research Institute. (2013). Kinase inhibitor patent landscape.
[4] U.S. Patent and Trademark Office. (2022). Patent expiration timelines.

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Drugs Protected by US Patent 8,101,582

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Harrow Eye TOBRADEX ST dexamethasone; tobramycin SUSPENSION/DROPS;OPHTHALMIC 050818-001 Feb 13, 2009 RX Yes Yes 8,101,582 ⤷  Start Trial Y USE OF A COMBINATION OF TOBRAMYCIN AND DEXAMETHASONE TO TREAT OCULAR INFLAMMATION WHERE AN INFECTION OR RISK OF INFECTION EXISTS ⤷  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

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