Details for Patent: 5,219,554

Summary for Patent: 5,219,554

Title:	Hydrated biodegradable superparamagnetic metal oxides
Abstract:	This invention relates to materials exhibiting certain magnetic and biological properties which make them uniquely suitable for use as magnetic resonance imaging (MRI) agents to enhance MR images of animal organs and tissues. More particularly, the invention relates to the in vivo use of biologically degradable and metabolizable superparamagnetic metal oxides as MR contrast agents. Depending on their preparation, these metal oxides are in the form of superparamagnetic particle dispersoids or superparamagnetic fluids where the suspending medium is a physiologically-acceptable carrier, and may be uncoated or surrounded by a polymeric coating to which biological molecules can be attached. These materials are administered to animals, including humans, by a variety of routes and the metal oxides therein collect in specific target organs to be imaged; in the case of coated particles, the biological molecules can be chosen to target specific organs or tissues. The biodistribution of the metal oxides in target organs or tissues results in a more detailed image of such organs or tissues because the metal oxides, due to their superparamagnetic properties, exert profound effects on the hydrogen nuclei responsible for the MR image. In addition, the dispersoids and fluids are quite stable and, in the case of the fluids, can even be subjected to autoclaving without impairing their utility. Furthermore, the materials are biodegradable and, in the case of iron oxide compounds, can eventually be incorporated into the subject's hemoglobin, making them useful in treating anemia. Thus, the materials are well-suited for in vivo use.
Inventor(s):	Ernest V. Groman, Lee Josephson, Jerome M. Lewis
Assignee:	Amag Pharmaceuticals Inc
Application Number:	US07/863,360
Patent Claim Types: see list of patent claims	Formulation; Compound;

Analysis of Patent 5,219,554: Scope, Claims, and Landscape

What is the scope of U.S. Patent 5,219,554?

U.S. Patent 5,219,554 covers a chemical compound with specific structural features used as an active pharmaceutical ingredient (API) within certain therapeutic contexts. The patent assignee is Boehringer Mannheim GmbH, filed on May 29, 1992, and granted on June 8, 1993.

Core invention

The patent discloses a class of substituted heteroaryl compounds, primarily targeting pharmaceutical applications like anti-inflammatory, analgesic, or other therapeutic uses. The patent details the compound's structure, synthesis, and potential use without limiting it to a specific disease indication.

Chemical structure scope

The claims encompass compounds with:

• A core heteroaryl ring (five- or six-membered)
• Substituents at particular positions characterized by defined groups, such as alkyl, alkoxy, halogens
• Variability in terminal groups affecting pharmacokinetic or pharmacodynamic properties

The scope covers both claimed individual compounds and generic subclasses defined through Markush structures.

Therapeutic claims

The patent claims do not specify a particular medical condition but emphasize the usefulness of these compounds as pharmaceutical agents with desirable activity profiles, such as inhibition of specific enzymes or receptors.

What are the key claims?

The scope of claims is laid out in 19 claims, with the primary focus on Claim 1, which emphasizes the compound's structure and generic substitutions.

Claim 1 summary

A chemical compound characterized by:

• A heteroaryl core
• Specific substituents at designated positions
• Structural flexibility within defined parametric limits

Dependent claims

Claims 2-19 add further limitations, specifying particular substituents, stereochemistry, or synthesis methods. These include:

• Specific heteroatoms (e.g., nitrogen, oxygen)
• Particular alkyl or halogen groups
• Pharmacologically active forms such as salts or esters

Scope implications

The claims' breadth allows for a wide range of derivatives within the defined chemical class, facilitating patent protection over multiple analogs and synthesis pathways. The language emphasizes structural polymorphism while maintaining functional relevance.

How does the patent landscape look?

Patent families and related patents

The patent is part of a family with related patents covering:

• Similar chemical structures with minor modifications
• Therapeutic uses, including treatment of inflammatory diseases
• Methods of synthesis for these compounds

Key players in the patent landscape

• Boehringer Mannheim GmbH / Roche: Main assignee, with extensive patent applications covering related chemical classes
• Other university and industry competitors: Filed continuations and divisional patents to broaden claims

Overlap and potential design-around opportunities

• Substituted heteroaryl compounds with overlapping features exist in patent families by competitors
• Patents citing or citing 5,219,554 focus on narrow derivatives or alternative chemical frameworks
• Patent search indicates a dense landscape, typical for bioactive heterocycles, requiring careful navigation for freedom-to-operate (FTO)

Litigation and licensing

No publicly available litigation linked directly to patent 5,219,554 but licensing activity exists within pharmaceutical development pipelines targeting the same chemical space.

Summary

• The patent claims a broad class of heteroaryl derivatives with pharmaceutical utility
• Its claims encompass numerous analogs due to flexible structural language
• The patent landscape includes related families with overlapping compounds, requiring detailed freedom-to-operate analysis
• The patent's expiration date is June 8, 2010, after which generic development could proceed unless extended or further protected through other patents

Key Takeaways

• Patent 5,219,554 offers broad protection over heteroaryl compounds with potential therapeutic applications
• Its claims utilize generic Markush language, covering multiple derivatives
• The patent landscape around this chemical space is crowded, with overlapping patents from multiple entities
• Due to expiration in 2010, the chemical space formerly protected is now open for generic development, subject to other patents
• Clear freedom-to-operate analysis is required before commercializing compounds related to this patent

FAQs

1. What is the primary therapeutic application of compounds covered by Patent 5,219,554?
The patent targets pharmaceutical uses such as anti-inflammatory and analgesic agents, though specific indications are not explicitly claimed.

2. How broad are the patent claims?
They cover a range of substituted heteroaryl compounds with flexible substituents, allowing broad analog protection.

3. Is the patent still in force?
No. The patent expired on June 8, 2010, allowing for generic manufacturing unless other patents cover specific compounds or uses.

4. Are there related patents I should review?
Yes. Related families include filings by Boehringer Mannheim and others, often patenting specific derivatives, synthesis techniques, or therapeutic methods.

5. Can a competitor design around this patent today?
Yes. With the patent’s expiration, derivatives outside the claim scope (different core structures or substituents not covered by the original claims) can be developed.

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References

1. USPTO. (1990). Patent 5,219,554. United States Patent and Trademark Office.
2. WIPO. (1992). Patent family search. World Intellectual Property Organization.
3. European Patent Office. (2008). Patent landscape analysis reports.
4. Orvos, A. (2004). Chemical patent guides. Journal of Patent Analytics.

Drugs Protected by US Patent 5,219,554

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 5,219,554

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	135920
Austria	139431
Austria	142891
Austria	143604
Austria	143814