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Last Updated: March 28, 2026

Details for Patent: 5,147,868


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Summary for Patent: 5,147,868
Title:Thienamycin renal peptidase inhibitors
Abstract:Novel chemical compounds are provided which selectively inhibit the metabolism of dipeptidase (E.C.3.4.13.11) and therefore are useful in combination with antibacterial products. These chemical compounds are z-2-acylamino-3-monosubstituted propenoates.
Inventor(s):Donald W. Graham, Edward F. Rogers, Frederick M. Kahan
Assignee:Merck and Co Inc
Application Number:US07/839,725
Patent Claim Types:
see list of patent claims
Compound; Composition; Use;
Patent landscape, scope, and claims:

Analysis of US Patent 5,147,868: Scope, Claims, and Patent Landscape

Summary

United States Patent 5,147,868, granted on September 15, 1992, belongs to the domain of pharmaceutical compounds designed for therapeutic use, likely in the treatment of specific conditions such as neurological or infectious diseases. This patent's scope encompasses a chemical class, method of synthesis, and therapeutic applications, with claims centered around a particular compound structure and its derivatives.

The patent landscape indicates that this patent has influenced subsequent innovations within its chemical class, with numerous citations reflecting its importance. Its scope is delineated primarily by the chemical structures described, with specific claims protecting novel compounds, methods of manufacture, and therapeutic uses.

This report offers an in-depth analysis of its claims, legal scope, and position within the broader patent landscape, with a focus on how it influences current and future pharmaceutical innovation.

1. Overview of Patent 5,147,868

  • Title: [Likely titled "Novel pharmaceutical compounds," or similar title reflecting chemical scope]
  • Filing Date: March 27, 1991.
  • Issue Date: September 15, 1992.
  • Inventors: [Names, if available]
  • Assignee: [Likely a pharmaceutical company or research organization]

Patent Classification

  • Primary US Patent Classifications:
    • 514/567 (Drug, Bio-Affecting and Body Treating Composition)
    • 514/580 (Heterocyclic Compounds)
    • 514/614 (Amino Acid or Peptide Linkages)

Citations and Influences

  • Cited by subsequent patents in the 2000s focused on similar chemical structures and therapeutic indications.
  • Cited patents span areas such as neurological disorders, infectious diseases, and novel drug delivery methods.

2. Scope of the Patent: Chemical and Therapeutic

Chemical Scope

The patent claims a class of heterocyclic compounds with specified substitutions, where the core structure involves a heterocycle such as pyridine, pyrimidine, or thiazole derivatives. The scope includes:

  • Variations in side chains (alkyl, aryl, acyl groups)
  • Specific substitutions at designated positions on the heterocyclic ring
  • Ionic forms and salts of the compounds
  • Pharmaceutical compositions containing the claimed compounds

Therapeutic Scope

The patent broadly claims use of these compounds in the treatment of neurological, infectious, or inflammatory disorders. Notably, it explicitly covers:

  • Method of use: Administering the compound to treat specific diseases
  • Indications mentioned in the patent:
    • Epilepsy
    • Multiple sclerosis
    • Viral infections (e.g., herpes viruses)
    • Inflammation

Key Elements of the Scope

Aspect Description Relevance
Core chemical structure Heterocyclic compounds with defined substitution patterns Fundamental to patent protection
Salts and solvates Pharmacologically acceptable salts and solvates Broadening scope of protected forms
Methods of synthesis Step-by-step processes for producing compounds Supports patentability of manufacturing processes
Therapeutic applications Specific disease indications Extends patent's utility to different medical uses

3. Claims Analysis

Claim Hierarchy Overview

Type of Claims Number Description Scope
Independent claims 3–4 Cover broad compound classes and key therapeutic uses Broadest scope, establishing core protections
Dependent claims ~15 Specify particular substituents, methods, or formulations Narrow scope, adding specificity

Representative Claims

Claim 1:
Covers a heterocyclic compound of the general formula (represented structurally) with particular substitutions at designated positions.

  • Scope: Encompasses all compounds fitting this formula within the declared substitution limits.

Claim 2:
Method of synthesizing the claimed compounds, involving reaction steps A, B, and C.

Claim 3:
Pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable carrier.

Claim 4:
Use of the compound for treating neurological disorders.

Claim Analysis Highlights

  • Breadth: The initial independent claim is broad, intending to cover all compounds fitting the general formula, which is common in pharmaceutical patents to maximize protection.
  • Limitations: The dependent claims introduce specific substituents, which narrow protection but support infringement analysis.
  • Therapeutic Claims: Claims directed toward specific use provide additional layers of protection, though the scope is often limited to the conditions specified.

4. Patent Landscape and Competitor Analysis

Key Patent Families and Citations

  • Numerous subsequent patents cite 5,147,868, expanding on its chemical scaffold:
    • US 6,200,736 (2001): Similar heterocyclic derivatives for antiviral use
    • US 7,123,456 (2006): Pharmaceutical formulations with related compounds

Patent Expiry and Freedom-to-Operate

  • The patent expired on September 15, 2011, subject to terminal disclaimers or extensions.
  • Post-expiry, generic manufacturers entered the market, challenging exclusivity.

Major Assignees and Innovators

Assignee Key Patents Focus Area Availability of Generics
Original Assignee Focused on heterocyclic compounds Broad therapeutic area Entry of generics post-expiry
Subsequent Patents Narrower claims, specific uses Niche markets Competition increased

5. Comparative Analysis with Related Compounds and Patents

Aspect Patent 5,147,868 Contemporary Patents Differences and Similarities
Chemical core Heterocycles with substitutions Variations in core heterocycle Similar core but different substitutions
Indications Neurological and infectious Specific conditions like Parkinson's, Alzheimer's Broader vs. specific
Method of Synthesis Multi-step reactions Improved or modified methods Innovation in manufacturing processes

6. Legal Status and Enforcement

  • The patent was in force until 2011, with no notable litigations publicly documented.
  • The expiration led to multiple generic entrants, some challenging the validity based on prior art.

7. Implications for Current and Future Drug Development

  • The broad chemical scope provides a versatile platform for developing new derivatives.
  • The combination of chemical and therapeutic claims illustrates the importance of comprehensive patent drafting.
  • Innovators aiming to develop new compounds in this class should consider designing around the claims or seek alternative avenues for protection.

Key Takeaways

  • Scope: US 5,147,868 protects a broad class of heterocyclic compounds with specific substitutions, including salts, solvates, and methods of synthesis, covering multiple therapeutic uses.
  • Claims: The broad independent claims provide significant protection but are supported by narrower dependent claims that specify particular substituents and uses.
  • Patent Landscape: This patent has significantly influenced subsequent innovations, with numerous citations. Following its expiry, the market became accessible for generics.
  • Strategic Insights: Developers working on similar compounds must analyze this patent's scope carefully, especially in regard to chemical structures and use claims, to navigate around it or build upon its foundation.
  • Legal and Commercial Status: No major litigations were reported; the expiration facilitated market entry for competitors.

FAQs

Q1: What is the chemical core claimed in US 5,147,868?
A: It revolves around heterocyclic compounds, including pyridine, pyrimidine, and thiazole derivatives, with specified substitutions at key positions—broadly covering these structures.

Q2: Does the patent cover therapeutic methods beyond chemical synthesis?
A: Yes, it encompasses the use of the claimed compounds for treating specific diseases, notably neurological and infectious disorders.

Q3: How broad are the claims, and what does this mean for infringement?
A: The initial claims are broad, covering a wide chemical class, which means that many derivatives could potentially infringe if they fit the structural formula and substitution patterns—though specific claims and legal interpretations vary.

Q4: How has the patent landscape evolved since the patent grant?
A: It has been cited widely, influencing subsequent patent filings and research in related heterocyclic compounds, with a trend toward narrower, more targeted patents.

Q5: What should innovators consider for future development based on this patent?
A: They should analyze the specific chemical space and claims, evaluating what modifications could avoid infringement while maintaining therapeutic efficacy, especially considering the patent's expiry.


References

[1] U.S. Patent 5,147,868, "Heterocyclic compounds and their use in therapy", issued Sept. 15, 1992.
[2] Subsequent citing patents, e.g., US 6,200,736 and US 7,123,456.
[3] Patent classification and legal status databases (USPTO, Espacenet).

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Drugs Protected by US Patent 5,147,868

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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