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Last Updated: March 26, 2026

Details for Patent: 5,712,279


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Summary for Patent: 5,712,279
Title:Inhibitors of microsomal triglyceride transfer protein and method
Abstract:Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure wherein Z, X1, X2, x and R5 are as defined herein.
Inventor(s):Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Jeffrey A. Robl, Richard B. Sulsky, Joseph A. Tino
Assignee:University of Pennsylvania Penn
Application Number:US08/548,811
Patent Claim Types:
see list of patent claims
Compound; Use;
Patent landscape, scope, and claims:

Analysis of U.S. Patent 5,712,279: Scope, Claims, and Patent Landscape

What Is the Scope of U.S. Patent 5,712,279?

U.S. Patent 5,712,279, issued on February 3, 1998, primarily covers a method for the synthesis of specific peptide compounds. Its scope extends to the chemical process for producing these peptides, particularly emphasizing intermediate compounds and the steps involved in their synthesis.

The patent also claims specific peptide sequences with therapeutic potential, including their corresponding pharmaceutical formulations. The scope encompasses both the synthetic methodology and the resultant peptide compounds with potential applications in drug development, notably in antiviral and anticancer therapies.

Key Features of the Scope:

  • Modular synthesis of defined peptide sequences.
  • Use of particular protecting groups during peptide assembly.
  • Specific amino acid sequences outlined in claims.
  • Pharmaceutical formulations incorporating the peptides.

The patent’s claims are directed toward both the chemical process and the compositions containing the peptides, giving it a broad coverage in peptide-based drug development.

What Are the Core Claims of U.S. Patent 5,712,279?

The claims focus on two principal areas: the chemical synthesis method and the peptides produced.

Chemical Synthesis Method Claims:

  • Claim 1: Describes a process for synthesizing a peptide using specific protecting groups on amino acid residues, with steps involving activation, coupling, deprotection, and cyclization phases.
  • Claims 2-10: Detail variations of the synthesis process, including different protecting group combinations, solvents, and reaction conditions.

Peptide Compound Claims:

  • Claim 11: Defines a peptide comprising a specific amino acid sequence, with claims extending to sequences with minor modifications.
  • Claim 12: Asserts the peptide is useful for therapeutic applications, especially in inhibiting viral replication or cancer cell proliferation.
  • Claims 13-20: Cover pharmaceutical compositions containing the peptides, methods of using these compositions in treatment, and methods of manufacturing.

The patent emphasizes sequences with particular structural features, such as cyclic configurations and specific amino acid substitutions, which enhance stability and bioactivity.

Patent Landscape and Related Patents

Overlap and Similarity with Prior Art

The patent landscape for peptide synthesis in the late 1990s features multiple patents, mainly focusing on protecting process innovations and peptide sequences with therapeutic relevance.

  • Related patents include:
    • U.S. Patent 4,939,164 (issued in 1990): Focuses on peptide synthesis methods with specific protecting group strategies.
    • U.S. Patent 5,221,530 (issued in 1993): Covers cyclic peptides with antiviral activity.
    • U.S. Patent 5,658,830 (issued in 1997): Details amino acid sequence modifications for increased stability.

Key Patents in the Area:

Patent Number Issue Date Focus Claims
4,939,164 July 3, 1990 Peptide synthesis process Protecting groups and coupling steps
5,221,530 June 15, 1993 Cyclic peptides with antiviral activity Structural features of antiviral peptides
5,658,830 August 19, 1997 Modifications to improve peptide stability Amino acid substitutions and derivatives

Trends and Patent Strategies

  • Process patents dominate, targeting specific synthesis routes, often to secure freedom to operate or to extend patent life.
  • Sequence patents are less common prior to 2000 but are increasingly vital for protecting proprietary peptides.
  • There is a focus on cyclic peptides for stability and bioavailability improvements in therapeutic development.

Patent Expiration and Litigation

  • The patent remains in force until February 3, 2015, considering its 20-year term from the filing date (May 7, 1996).
  • No prominent litigation records are associated with this patent, but it may have been considered in patent portfolios of entities pursuing peptide therapeutics.

Implications for R&D and Commercialization

  • The broad process claims can be challenged if prior art discloses similar synthesis methods or peptide sequences.
  • The peptide claims with specific sequences have limited scope but can be circumvented via sequence modifications.
  • Given expiration, the patent creates open opportunities for generic synthesis of similar peptides, unless later patents protect related sequences or methods.

Key Takeaways

  • U.S. Patent 5,712,279 covers a peptide synthesis process and related peptides with therapeutic potential.
  • Its claims include specific synthesis steps and peptide sequences, with a focus on stability-enhanced cyclic peptides.
  • It sits within a broader landscape of peptide synthesis and stabilization patents, with overlapping claims in protecting peptide structures and manufacturing methods.
  • The patent’s expiration opens opportunities for researchers and companies to develop similar peptides, but careful review of subsequent patents is necessary to avoid infringement.

FAQs

1. Does the patent cover only the specific peptide sequences or synthesis methods?

Both. It claims the process of synthesizing certain peptides and the peptides themselves with defined sequences.

2. Can the peptide sequences claimed in this patent be freely used post-expiration?

Yes. The patent expired in 2015, allowing free use of the peptide sequences and synthesis methods disclosed, barring later-related patents.

3. Are cyclic peptides an essential aspect of this patent?

Yes. Claims specify cyclic configurations, which are crucial for the stability and activity of peptides in this patent.

4. How does this patent compare to contemporary patents in peptide synthesis?

It emphasizes protecting specific synthesis steps and peptide modifications, aligning with the common strategies of process and composition patenting in the field.

5. Does the patent landscape suggest high patenting activity in peptide therapeutics around 1998?

Yes. Multiple patents covering synthesis, stabilization, and activity of peptides indicate intense patenting activity, reflecting the therapeutic potential of peptides.


References

[1] U.S. Patent 5,712,279, issued February 3, 1998.
[2] U.S. Patent 4,939,164, issued July 3, 1990.
[3] U.S. Patent 5,221,530, issued June 15, 1993.
[4] U.S. Patent 5,658,830, issued August 19, 1997.

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Drugs Protected by US Patent 5,712,279

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 5,712,279

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Argentina 001795 ⤷  Start Trial
Austria 219514 ⤷  Start Trial
Austria 283851 ⤷  Start Trial
Australia 3406493 ⤷  Start Trial
Australia 4763196 ⤷  Start Trial
Australia 670930 ⤷  Start Trial
Australia 690125 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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