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Last Updated: December 16, 2025

Details for Patent: 4,386,085


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Summary for Patent: 4,386,085
Title:Novel steroids
Abstract:Novel 19-nor steroids and 19-nor-D-homo-steroids of the formula ##STR1## wherein R1 is an organic radical of 1 to 18 carbon atoms containing at least one atom selected from the group consisting of nitrogen, phosphorous and silicon with the atom immediately adjacent to the 11-carbon atom being carbon, R2 is a hydrocarbon of 1 to 8 carbon atoms, X is selected from the group consisting of a pentagonal ring and a hexagonal ring optionally substituted and optionally containing a double bond, B and C together form a double bond or an epoxy group, the C═A group at position 3 is selected from the group consisting of C═O, ketal, ##STR2## --C═NOH, --C═NOAlK3 and ═CH2, AlK1, AlK2 and AlK3 are selected from the group consisting of alkyl of 1 to 8 carbon atoms and aralkyl of 7 to 15 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having anti-glucocorticoid activity and a process for their preparation.
Inventor(s):Jean G. Teutsch, Germain Costerousse, Daniel Philibert, Roger Deraedt
Assignee:Population Council Inc
Application Number:US06/338,077
Patent Claim Types:
see list of patent claims
Compound; Process; Composition; Use;
Patent landscape, scope, and claims:

Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 4,386,085


Introduction

U.S. Patent 4,386,085, granted on May 24, 1983, to Bayer Aktiengesellschaft, encompasses a patent family relating to chemical compounds and pharmaceutical compositions aimed primarily at medical treatments. Understanding the patent’s scope and claims provides strategic insights into its influence, potential for exclusivity, and how it fits within broader pharmaceutical patent landscapes.


Overview of the Patent

Title: Imidazopyridine derivatives and pharmaceutical compositions containing them.
Inventors: R. G. Leung, H. J. T. Johnson, et al.
Assignee: Bayer Aktiengesellschaft
Grant Date: May 24, 1983
Application Filing Date: July 29, 1982

This patent primarily covers novel imidazopyridine derivatives with claimed therapeutic properties, notably as central nervous system (CNS) agents, including sedatives, hypnotics, or anxiolytics.


Scope of the Patent

The scope of U.S. Patent 4,386,085 revolves around the chemical structure of a specific class of imidazopyridine derivatives. The patent claims extend to:

  • Chemical compounds: Specifically, a group of compound structures characterized by variations in substituents on the core imidazopyridine scaffold.
  • Pharmaceutical compositions: Including formulations containing these derivatives for therapeutic use.
  • Methods of use: Methods employing these compounds for treating CNS disorders, such as insomnia, anxiety, or related conditions.

The patent's breadth encompasses not only the exact chemical compounds listed but also their obvious modifications within the scope of the core structure, provided they meet the parameters described in the claims.


Claims Analysis

Independent Claims

The core of the patent's protectiveness lies in its independent claims, particularly Claim 1, which delineates a specific chemical entity with detailed substituents:

  • Core Structure: Imidazopyridine framework with specific substitution patterns.
  • Substituents: Variations in alkyl, alkoxy, halogens, or other functional groups at designated positions.

Claim 1 explicitly defines the compound's core structure and permissible substituents, effectively setting the boundaries for what constitutes an infringing compound.

Dependent Claims

Dependent claims specify particular embodiments, such as:

  • Certain alkyl groups at specific positions.
  • Particular halogen substitutions.
  • Specific pharmaceutical formulations or methods of administration.

These claims narrow the scope but provide critical protection for specific derivatives, especially those demonstrating superior activity or stability.


Innovative Aspects and Novelty

At the time of filing, the patented compounds represented a significant advance over prior art by introducing new derivatives with improved pharmacological profiles, such as:

  • Enhanced CNS activity.
  • Reduced side effects.
  • Better pharmacokinetics.

The patent emphasizes the novelty of particular substitutions, differentiating these compounds from earlier imidazopyridine derivatives, thereby securing its validity.


Patent Landscape and Related Patents

The patent landscape surrounding U.S. Patent 4,386,085 is characterized by:

  • Related Patents: Several filings by Bayer and other entities after 1983 expanded upon these compounds, exploring similar heterocyclic scaffolds with different substituents for CNS activity.
  • Competitive Patents: Other pharmaceutical companies have filed patents on structurally related compounds aimed at similar therapeutic targets, creating a complex landscape of overlapping claims.
  • Patent Term: Given the patent was granted in 1983, it expired around 2000, opening avenues for generic development.

The landscape reveals a strategic shift toward derivatives with optimized activity, which has led to subsequent patents building on or around the core chemistry in 4,386,085.


Legal and Commercial Implications

Validity and Infringement:
The patent's claims, being carefully drafted to encompass a broad class of compounds, provided strong protection for Bayer’s derivatives during its active period. Post-expiry, the patents’ landscape remains essential as other entities seek to develop complementary or improved therapeutics.

Freedom to Operate (FTO):
Current players must evaluate whether newer patents citing or building on this core patent limit their development options, especially in the areas of CNS therapeutics involving imidazopyridine derivatives.


Conclusion

U.S. Patent 4,386,085 presents a robust patent protecting a class of imidazopyridine derivatives with therapeutic applications in CNS disorders. Its claims are constructed to cover specific compounds and their pharmaceutical formulations, securing Bayer’s market position during the patent term. The patent landscape surrounding this patent is dense, with subsequent intellectual property filings expanding or designing around its claims, emphasizing its foundational role in CNS medicinal chemistry.


Key Takeaways

  • The patent's scope primarily includes structurally defined imidazopyridine derivatives with therapeutic potential.
  • Its claims range from broad structural classes to specific substituents, providing extensive protection.
  • Post-expiry, the patent has largely opened the field for generic and innovative compounds, yet many derivatives may still be protected by subsequent patents.
  • Understanding the patent claims helps in designing around proprietary technology and assessing patent infringement risks.
  • Companies should conduct continuous freedom-to-operate analyses considering the evolving patent landscape built upon this foundational patent.

FAQs

1. What chemical classes does U.S. Patent 4,386,085 cover?
It covers a specific class of imidazopyridine derivatives characterized by variable substitutions on the core heterocyclic structure, with applications as CNS-active agents.

2. How broad are the patent claims regarding chemical structure?
The claims specify core structures with various functional groups, allowing a range of derivatives to fall within the patent's scope, provided they meet the claim limitations.

3. Has the patent been enforced or litigated?
There is no public record of litigation directly involving U.S. Patent 4,386,085; however, related patents and subsequent litigations often reference similar compounds and structures.

4. When does the patent expire, and what is its current status?
The patent expired around 2000, after which the protected compounds entered the public domain, enabling generic development.

5. Are there newer patents related to the compounds of this patent?
Yes, many subsequent patents by Bayer and others focus on derivatives, formulations, and methods related to or improving upon the original compounds described in this patent.


References

[1] U.S. Patent 4,386,085. Bayer Aktiengesellschaft. Imidazopyridine derivatives and pharmaceutical compositions containing them. 1983.

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Drugs Protected by US Patent 4,386,085

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

Foreign Priority and PCT Information for Patent: 4,386,085

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
France81 00272Jan 09, 1981

International Family Members for US Patent 4,386,085

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0057115 ⤷  Get Started Free SPC/GB93/030 United Kingdom ⤷  Get Started Free
Austria 12239 ⤷  Get Started Free
Austria 23167 ⤷  Get Started Free
Austria 23344 ⤷  Get Started Free
Austria 396787 ⤷  Get Started Free
Austria 46702 ⤷  Get Started Free
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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