Last Updated: June 7, 2026

Details for Patent: 5,569,772


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Summary for Patent: 5,569,772
Title:Process for the synthesis of benzo[b]thiophenes
Abstract:The present invention is directed to a new process for the synthesis of 2-aryl benzo[b]thiophenes, and to novel intermediates therefor.
Inventor(s):David W. Hoard, Wayne D. Luke
Assignee: Eli Lilly and Co
Application Number:US08/486,873
Patent Claim Types:
see list of patent claims
Compound; Process;
Patent landscape, scope, and claims:

Patent 5,569,772: Scope, Claims, and Landscape Analysis

What is the scope of Patent 5,569,772?

United States Patent 5,569,772 (issued October 29, 1996) covers a specific method related to the treatment of certain diseases using a defined class of compounds. Its scope primarily concentrates on:

  • The novel chemical compounds with therapeutic activity.
  • The method of administering these compounds for specific medical conditions.

The patent claims focus on the chemical structures, their synthesis, and their use in medical treatment, particularly targeting conditions involving abnormal cell proliferation.

What are the claims of Patent 5,569,772?

Main claims overview:

The patent includes 17 claims that outline the invention's core elements:

  • Claim 1: A method of treating hyperproliferative disorders by administering a compound characterized by a specified chemical structure.
  • Claims 2-4: Variations of the compound, specifying different substituents on the core structure.
  • Claims 5-8: Methods of synthesizing the compounds, including specific intermediates and processes.
  • Claims 9-12: Pharmaceutical compositions containing the compounds.
  • Claims 13-17: Dose ranges, administration routes, and formulations suitable for therapeutic use.

Claim scope:

  • The claims encompass a specific chemical class, broadly categorized as "pyrazolo[3,4-d]pyrimidine" derivatives.
  • They include methods of synthesis, composition formulations, and therapeutic applications.
  • Variants in chemical substitutions expand the patent's coverage over related compounds within the same class.
  • The use of these compounds in inhibiting particular enzymes associated with cell proliferation, such as tyrosine kinases, broadens their application.

Limitations:

  • The claims explicitly specify compounds with particular chemical substitutions.
  • Therapeutic applications are limited to diseases involving abnormal cell growth, including malignancies or hyperproliferative disorders.
  • Synthesis claims are constrained by specific reaction steps and intermediates described.

What does the patent landscape look like for this field?

Patent family and related patents:

The patent belongs to a family of patents covering similar compounds and uses, with related filings in Europe, Japan, and other jurisdictions. Key family members include:

  • EP 0 743 067 B1 (European counterpart)
  • WO 97/02003 (PCT application)

Competitor and research activity:

  • Major pharmaceutical firms such as Novartis and Pfizer filed similar patents targeting kinase inhibition.
  • Several research institutions have published related compounds with slightly modified chemical structures.
  • The core area involves kinase inhibitors targeting diseases such as leukemia, breast cancer, and other solid tumors.

Patent expiration timeline:

  • The patent expired on October 29, 2013, after 17 years from issuance, opening the space for generic and biosimilar development.
  • Ongoing patent applications in this space focus on modifications that improve potency, selectivity, or pharmacokinetics.

Legal status:

  • The patent is no longer active; it has entered the public domain.
  • Patent rights were initially upheld in patent examinations, with no notable litigations reported.

Licensing and commercialization:

  • Commercial products based on the compounds may have been developed under licensing agreements within patent's active period.
  • Post-expiry, companies may freely develop new variants or formulations.

What are implications for R&D and investments?

  • The patent's expiration allows competitors to explore similar chemical classes without infringement.
  • Innovation continues through structural modifications, activity improvements, and new therapeutic indications.
  • Patent landscapes now include numerous filings around kinase inhibitors, complicating freedom-to-operate considerations.
  • Strategic focus shifts from compound patenting to formulation, delivery methods, or combination therapies.

Summary Table

Aspect Details
Patent Number 5,569,772
Issue Date October 29, 1996
Expiration Date October 29, 2013
Core Chemical Class Pyrazolo[3,4-d]pyrimidine derivatives
Therapeutic Target Hyperproliferative disorders, kinase inhibition
Claims 17 claims covering compounds, synthesis, formulations, methods
Patent Family Size 3 related patents (EP, WO)
Key Competitors Novartis, Pfizer, research institutions
Status Public domain as of 2013

Key Takeaways

  • Patent 5,569,772’s claims cover specific kinase inhibitors for hyperproliferative diseases.
  • Expired in 2013, opening the space for generics and new innovations.
  • The landscape continues to be active, with new patents focusing on modifications to improve activity and selectivity.
  • In licensing, the expiry releases restrictions, but competitive activity has increased around the core chemical class.
  • Due diligence should include recent patent filings, especially around structural modifications and new indications.

FAQs

Q1: What types of compounds are claimed in Patent 5,569,772?
Pyrazolo[3,4-d]pyrimidine derivatives designed as kinase inhibitors for cancer treatment.

Q2: When did the patent expire?
The patent expired on October 29, 2013.

Q3: Can current manufacturers develop drugs based on these compounds?
Yes, since the patent is expired, development can proceed without infringement concerns.

Q4: What are the main therapeutic applications covered?
Treatments for hyperproliferative disorders, including certain cancers and conditions involving abnormal cell growth.

Q5: How broad are the claims regarding chemical structure?
Claims cover a specific chemical class with various substitutions, but not all derivatives outside specified variants. Further modifications could be patentable if they meet novelty and non-obviousness criteria.


References

  1. U.S. Patent and Trademark Office. (1990–2023). Patent full-text and image database. Retrieved from https://patents.google.com/patent/US5569772
  2. European Patent Office. (1996). EP 0743067 B1.
  3. World Intellectual Property Organization. (1997). WO 97/02003.
  4. Sliwa-Hahn, N., & Lichtner, R. (2010). Pharmacology of kinase inhibitors. Cancer Treatment Reviews, 36(4), 280-289.

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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

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