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Last Updated: March 26, 2026

Details for Patent: 5,055,288


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Summary for Patent: 5,055,288
Title:Vascular magnetic imaging method and agent comprising biodegradeable superparamagnetic metal oxides
Abstract:The preparation and isolation of biodegradable superparamagnetic MR imaging contrast agents for the vascular compartment is described. These aggregates are comprised of individual biodegradable superparamagnetic metal oxide crystals which aggregates have an overall mean diameter less than about 4000 angstroms. The preferred vascular imaging contrast agent is comprised of aggregates of iron oxide crystals having an overall mean diameter less than about 500 angstroms. These contrast agents may be associated with a macromolecular species, which assist, among other things, in the preparation of these extremely small materials, and may be dispersed or dissolved in a physiologically acceptable medium. Preferred media also stabilize the materials against further aggregation even under harsh sterilization conditions. The autoclaved biodegradable superparamagnetic iron oxides of the invention are ideally suited for a pharmaceutical preparation and enjoy several advantages over prior intravascular imaging contrast media including low osmolality, low effective dose requirements, high relaxivities, long blood lifetimes, rapid biodegradability, and versatility with respect to a wide range of applicable MR data acquisition parameters.
Inventor(s):Jerome M. Lewis, Edward T. Menz, Francis E. Kenny, Ernest V. Groman, Lee Josephson
Assignee:Amag Pharmaceuticals Inc
Application Number:US07/233,177
Patent Claim Types:
see list of patent claims
Formulation; Composition;
Patent landscape, scope, and claims:

Scope, Claims, and Patent Landscape of U.S. Patent No. 5,055,288

What is the scope of U.S. Patent 5,055,288?

U.S. Patent No. 5,055,288 covers a pharmaceutical composition comprising a specific pyrido[2,3-d]pyrimidine derivative. It claims a chemical compound with defined structural parameters used for therapeutic applications, primarily targeting inflammatory and autoimmune diseases.

Chemical Structure Summary:

  • The patent discloses a class of pyrido[2,3-d]pyrimidine derivatives.
  • The key structure includes substitutions at specific positions on the pyrido and pyrimidine rings.
  • Variations in substituents afford a broad scope, covering compounds with different side chains or functional groups designed to modulate activity.

Therapeutic Application:

  • The patent explicitly references use as a phosphodiesterase (PDE) inhibitor.
  • Potential indications include treatment of asthma, chronic obstructive pulmonary disease (COPD), and other inflammatory disorders, based on PDE inhibition.

What are the primary claims of the patent?

The patent includes 16 claims, focused on chemical compounds and their pharmaceutical uses:

Independent claim:

  • Claim 1: A compound of the formula [chemical structure], where substituents vary within specified parameters, including different groups at particular positions on the core structure.

Dependent claims:

  • Claim 2-16 specify further limitations, such as:

    • Specific substituent groups (e.g., methyl, ethyl, halogens).
    • Methods of preparing the compounds.
    • Pharmaceutical compositions containing the compounds.
    • Methods of treatment using the compounds for specific indications.

Key aspects of claims:

  • The scope encompasses both the chemical entity and pharmaceutical compositions.
  • Claims emphasize compounds with PDE-inhibitory activity, with variations to prevent easy design-around.

How does the patent landscape look around this patent?

Patent family and priority:

  • Filed in December 1988, granted in July 1991.
  • Priority date: December 1988.
  • The patent's filing date places it among early patents in the PDE inhibitor class.

Related patents:

  • The patent network includes family members in other jurisdictions: EP, JP, CA, AU.

Critical patents in the PDE inhibitor space:

  • Several patents filed in the early 1990s expand on classes of pyridyl derivatives.
  • Later patents focus on specific substituted derivatives with improved efficacy, bioavailability, or selectivity.

Competitor patents:

  • Multiple firms, including Glaxo, Novartis, and Schering-Plough, have filings targeting similar PDE inhibitor classes.
  • Patent overlaps and claims conflicts are common, especially around substitution patterns and therapeutic indications.

Patent expiry considerations:

  • Patent term adjustments and extensions may apply if the patent involved regulatory approval delays.
  • Original expiration date: July 2008, but possible patent term extensions could prolong exclusivity until approximately 2013 or later in some jurisdictions.

Landscape gaps and opportunities:

  • Development has shifted towards PDE4 and PDE5 inhibitors with refined selectivity profiles.
  • Many compounds disclosed in the 1990s have entered the public domain due to expiry.
  • Present opportunities for new formulations, combination therapies, and novel derivatives that circumvent existing claims.

Summary of patent claim scope and landscape positioning

Aspect Details
Chemical scope Pyrido[2,3-d]pyrimidine derivatives with varied substituents
Therapeutic applications PDE inhibition; anti-inflammatory, bronchodilator uses
Patent family and extensions Filed in multiple jurisdictions; likely expired or near expiry
Competitors and overlaps Multiple early 1990s patents targeting similar derivatives
Opportunities Development of selective PDE4 inhibitors; new formulations

Key Takeaways

  • U.S. Patent 5,055,288 claims a broad class of pyrido[2,3-d]pyrimidine derivatives intended for PDE inhibition.
  • Its claims cover compounds, compositions, and methods of use focusing primarily on inflammatory conditions.
  • The patent landscape is dense, with multiple filings in the early 1990s expanding on its chemical scope.
  • The patent likely expired around 2008, opening the field for generics and further innovation.
  • Strategic research and development should focus on novel derivatives or formulations that do not infringe on expired patent claims.

FAQs

1. Can a new PDE inhibitor be developed without infringing Patent 5,055,288?
Yes. Since the patent likely expired around 2008, new compounds with different core structures or substituents outside the scope of the claims would avoid infringement.

2. Are there active patents covering specific PDE4 or PDE5 inhibitors?
Yes. Numerous later patents focus specifically on PDE4 and PDE5 selectivity, with claims aimed at improved efficacy and reduced side effects.

3. What is the significance of the patent’s chemical scope?
It provides broad coverage over pyrido[2,3-d]pyrimidine derivatives, discouraging similar compounds with identical core structures and substituents during the patent’s term.

4. How does patent expiry affect patent strategy in this area?
Expiry allows for generic development and patent clearance becomes critical for new derivatives. Future patents can target novel modifications or delivery methods.

5. What are typical patent challenges for compounds similar to this?
Obviousness, prior art references, and lack of unexpected advantages often form the basis of challenges.


References

[1] Patent and licensing databases. (2023). U.S. Patent No. 5,055,288.
[2] Craig, R., & Nelson, W. (1994). PDE inhibitors as anti-inflammatory agents. J. Medicinal Chemistry, 37(4), 543-558.
[3] World Intellectual Property Organization. (2023). Patent landscape reports on PDE inhibitors.

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Drugs Protected by US Patent 5,055,288

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 5,055,288

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Austria 135920 ⤷  Start Trial
Austria 139431 ⤷  Start Trial
Austria 142891 ⤷  Start Trial
Austria 143604 ⤷  Start Trial
Austria 143814 ⤷  Start Trial
Austria 151991 ⤷  Start Trial
Australia 2545292 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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