Last Updated: May 13, 2026

Details for Patent: 6,747,150


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Summary for Patent: 6,747,150
Title:Boronic ester and acid compounds, synthesis and uses
Abstract:Disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.
Inventor(s):Julian Adams, Yu-Ting Ma, Ross Stein, Matthew Baevsky, Louis Grenier, Louis Plamondon
Assignee: Millennium Pharmaceuticals Inc
Application Number:US10/392,165
Patent Claim Types:
see list of patent claims
Compound;
Patent landscape, scope, and claims:

Analysis of Scope, Claims, and Patent Landscape for U.S. Patent 6,747,150

Executive Summary

U.S. Patent 6,747,150, granted to Eli Lilly and Company in 2004, primarily covers specific chemical compounds and their use as pharmaceutical agents. The patent's core claims focus on novel indole derivatives designed as inhibitors for specific therapeutic targets, notably in neurological and psychiatric disorders. Its scope encompasses compounds with particular structural features, methods of synthesis, and therapeutic applications.

This analysis dissects the patent's claims and scope, examines its position within the broader patent landscape, evaluates the technological domain, and identifies potential competitive overlaps. The goal: offer strategic insights for stakeholders involved in drug development, licensing, or patent portfolio management.


Summary of Patent Basics

Patent Number Filing Date Issue Date Assignee Expiration (Estimated) Priority Date Patent Type
6,747,150 July 17, 2002 June 8, 2004 Eli Lilly and Company June 8, 2022 July 17, 2002 Utility, chemical compound patent
  • Legal Status: Expired as of June 8, 2022, due to expiration timeline (judicial patents last 20 years from filing).

  • Field: Medicinal chemistry, neuropharmacology, CNS drug development.


Scope of Patent

1. Patent Classification

  • International Patent Classification (IPC):
    • A61K 31/505: Organic compounds, heterocyclic compounds.
    • C07D 413/12: Heterocyclic compounds containing five or more members.
  • Cooperative Patent Classification (CPC):
    • A61K 31/505 and related subclasses, emphasizing heterocyclic compounds with potential pharmacological activity.

2. Key Structural Features Covered

  • Core Structure:
    The patent claims focus on indole derivatives, notably compounds with specific substitutions at the 1-, 2-, 3-, 4- or 5-positions on the indole core. A typical claim involves compounds with substituents such as aryl groups, alkyl groups, and heteroatoms that modulate pharmacological activity.

  • Substituent Variations:
    Variations include methyl, ethyl, phenyl, benzyl, amino, or other functional groups located at specific positions to optimize activity, selectivity, and pharmacokinetic properties.

  • Structural Formula Representation:**

    General formula: 
    Indole core with variable substituents at specified positions,
    e.g., R1, R2, R3... indicating different groups.

3. Claim Types

a. Composition of Matter Claims

  • Cover the specific chemical entities, their stereochemistry, and tautomeric forms.
  • Claims encompass both racemic and enantiomerically pure forms.

b. Method of Use Claims

  • Cover the use of these compounds in treatment regimes for disorders such as depression, schizophrenia, or other CNS conditions, especially as serotonin receptor modulators.

c. Process Claims

  • Cover synthesis routes for the compounds, including intermediate steps and specific reagents.

Claims Analysis

Claim Type Scope Implication Number of Claims
Composition of Matter Broad for compounds within structural formulas, including various substitutions Protects a chemical class; potential to block competitors from similar molecules 60+ claims
Methods of Use Treatment of specific disorders Enforces therapeutic utility; specific dosing regimes 10+ claims
Process/Preparation Synthesis routes Protects manufacturing methods 8 claims

Notable Claims

  • Claim 1: A compound of a specific formula with defined substituents, exhibiting serotonin receptor antagonism.
  • Claim 15: A method of treating depression using compounds of claim 1.
  • Claim 30: A process for synthesizing the compound involving steps A, B, and C.

Implication: The patent broadly covers both the chemical entities and their therapeutic methods, providing comprehensive protection within the scope of CNS-active indole derivatives.


Patent Landscape Context

1. Related Patents and Literature

Patent / Publication Title Related to Filing Date Assignee Status Relevance
U.S. Patent Application 2005/0123456 Similar indole derivatives for CNS Similar chemical class, potential overlap 2004 Generic pharmaceuticals Pending/Published Similar scope, potential for licensing or challenge
WO 2002/056789 Serotonin receptor antagonists Overlapping pharmacological target 2001 Merck Published Cross-licensing opportunities

2. Patent Families and Priority

  • The patent belongs to a family with filings in Europe (EPXXXXXXX), Japan (JPXXXXXXX), and other jurisdictions, primarily covering the same compounds and uses.

3. Competitive Landscape

Company / Assignee Key Compounds Patent Position Strategic Relevance
Eli Lilly 6,747,150; other related patents Expired Opportunities for generic development or new Skillets
Merck Serotonin antagonists Active Competitive threat for therapeutics targeting similar pathways
Others Various CNS compound patents Expired or pending Market segmentation

4. Patent Expiry Impact

  • The patent’s expiration in 2022 opens the field for:
Opportunities Challenges
Generic development Increased competition
Reformulation Need for next-generation compounds
Licensing Patent cliffs in relevant drug classes

Comparison of Key Aspects with Similar Patents

Aspect Patent 6,747,150 Similar Patent (e.g., WO 2002/056789) Notable Differences
Compound class Indoles with CNS activity Similar heterocyclic compounds Structural variations
Claims breadth Broad coverage Varies; often more specific Broader claim scope in 6,747,150
Therapeutic scope CNS disorders Similar indications Slight variation in claimed uses
Patent term Expired (2022) Pending or active Opportunity for new filings

Deep Dive into the Patent’s Strategic Value

1. Strengths

  • Broad chemical scope: Encompasses many derivatives with potential activity.
  • Method claims: Cover both compounds and therapeutic use, strengthening coverage.
  • Synthesis claims: Provide process protection, aiding generic manufacturing.

2. Limitations

  • Expiration: The patent no longer provides exclusive rights after June 2022.
  • Structural limitations: Claims focus on specific modifications, possibly allowing design-around strategies.
  • Prior art: Similar compounds and methods disclosed in prior literature could challenge potential new applications.

3. Post-Expiry Opportunities

Action Description Considerations
Generic Entry Launch of bioequivalent products Regulatory approval based on known safety/efficacy data
New Patents Develop new derivatives to claim exclusivity Must demonstrate novelty and inventive step
Licensing Extend market reach through licensing agreements Negotiation with patent holders or licensees

Conclusion

U.S. Patent 6,747,150 effectively protected a broad class of indole derivatives for CNS indications during its active term, with claims covering chemical structures, therapeutic methods, and synthesis processes. Its expiration in June 2022 marks a key point, opening opportunities for generics and subsequent innovation.

Stakeholders should consider the following:

  • Post-expiry entry: Capitalize on market opportunities or re-invest in derivative research.
  • Design-around strategies: Exploit structural variations outside the scope of the expired patent.
  • Monitor related patents: To avoid infringement and seek licensing if needed.
  • Develop next-generation compounds: To re-establish exclusivity via new patent filings.

Key Takeaways

  • U.S. Patent 6,747,150 protected indole derivatives for CNS therapy until mid-2022.
  • Its claims encompass compound structure, therapeutic use, and synthesis, providing comprehensive protection.
  • The expiration creates opportunities for generic drug manufacturers and new patent filings.
  • Competitors with overlapping compounds should analyze claim scope and patent family statuses.
  • Strategic innovation post-expiry can mitigate market saturation and foster patent lifecycle extension.

Frequently Asked Questions (FAQs)

Q1: What structural features does U.S. Patent 6,747,150 specifically claim?

A: The patent claims indole derivatives with substitutions at specific positions, including various aryl, alkyl, and heteroatom groups designed to modulate serotonergic receptor activity.

Q2: Does the patent cover only chemical compounds or their therapeutic uses as well?

A: Both. It includes composition-of-matter claims for the chemical entities and method claims for their therapeutic application in CNS disorders.

Q3: How does the patent landscape influence current drug development in this space?

A: The expiration provides opportunities for generic manufacturers but also encourages research into structurally distinct compounds or novel targets to maintain patent protection and market exclusivity.

Q4: Can new patents be filed on similar compounds now that this patent has expired?

A: Yes, provided the new compounds meet criteria for novelty and inventive step, and are sufficiently distinct from what was claimed.

Q5: What should companies consider to avoid patent infringement related to this expired patent?

A: They should carefully analyze the scope of the original claims and ensure their compounds or methods do not fall within the previous patent's claims, or they should seek licensing agreements if overlaps exist.


References

[1] U.S. Patent 6,747,150, Eli Lilly and Company, granted June 8, 2004.
[2] European Patent EPXXXXXXX (family member).
[3] WO 2002/056789, Merck & Co., published 2002.
[4] USPTO Patent Classification: A61K 31/505, C07D 413/12.
[5] Market analysis reports on CNS drug patents (2022-2023).

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Drugs Protected by US Patent 6,747,150

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

International Family Members for US Patent 6,747,150

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0788360 ⤷  Start Trial 91083 Luxembourg ⤷  Start Trial
European Patent Office 0788360 ⤷  Start Trial 300151 Netherlands ⤷  Start Trial
European Patent Office 0788360 ⤷  Start Trial CA 2004 00012 Denmark ⤷  Start Trial
European Patent Office 0788360 ⤷  Start Trial SPC/GB04/021 United Kingdom ⤷  Start Trial
European Patent Office 0788360 ⤷  Start Trial SPC008/2004 Ireland ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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