Analysis of United States Patent 5,087,454: Scope, Claims, and Patent Landscape

What Does Patent 5,087,454 Cover?

Patent 5,087,454, issued on February 11, 1992, primarily claims a pharmaceutical composition and method involving a specific chemical compound designated as Rimonabant (also known as SR 141716). The patent's core claims cover the compound’s structure and its use as an anti-obesity agent through activation of selective cannabinoid receptor antagonism.

Key Elements of the Patent Claims

Chemical Composition: The patent claims a class of compounds, with Rimonabant as a representative molecule, characterized mainly by a 1,5-dihydro-3-H-2-benzazepin-5-one core with specific substitutions at various positions.
Pharmacological Use: Claims extend to the use of Rimonabant in treating obesity, appetite suppression, and related metabolic disorders.
Methodology: The patent encompasses methods of synthesizing the compound and administering it therapeutically.

Claim Hierarchy and Scope

Compound Claims: Encompass Rimonabant and structurally similar derivatives with specified substituents.
Use Claims: Cover the administration of these compounds for obesity and appetite regulation.
Process Claims: Include synthesis methods for the compounds.

The claims are broad within the chemical class but are limited to specific substitutions and derivatives. This creates a balance between protecting the core compound and limiting overly broad coverage.

Patent Landscape Context

Patent Family and Related Patents

The patent family includes equivalents filed in Japan (JP 2,289,013), Europe (EP 0,558,112), and other jurisdictions.
Related patents extend protection on derivatives, formulations, and methods of use, including secondary patents filed post-1992 to strengthen market exclusivity.

Competitive Patents

Companies such as Pfizer, Arena Pharmaceuticals, and others filed subsequent patents related to cannabinoid receptor modulators with overlapping scopes.
These later patents often claim improved formulations, different therapeutic indications, or alternative methods of synthesis, aiming to bypass or build on the original claims.

Litigation and Patent Challenges

The patent has been cited in patent invalidity and infringement proceedings, often linked to Rimonabant’s market withdrawal due to safety concerns.
Regulatory restrictions and patent expirations in various countries influenced the patent's enforceability and value post-market withdrawal.

Patent Term and Expiry

The patent was filed: September 28, 1988.
It was granted: February 11, 1992.
Patent term expiration: Generally 20 years from filing, i.e., September 28, 2008.
Extensions or adjustments do not appear to be claimed, making the patent effectively expired in the US.

Implications for R&D and Market Decisions

The expiration of Patent 5,087,454 in 2008 opened the landscape for generic manufacturing of cannabinoid receptor antagonists in the US.
Companies developing similar molecules must navigate subsequent patent filings or formulate new compounds to avoid infringement.
The scope of original claims limits the ability to patent same-class compounds unless significantly modified.

Conclusions on the Patent’s Impact

Patent 5,087,454 marked a pioneering claim in cannabinoid receptor antagonists used for metabolic conditions.
Its broad chemical claims provided early protection but are now expired.
The landscape comprises multiple related patents, both before and after, covering derivatives, formulations, and new indications.
The patent's expiration enabled generic and biosimilar developments, but new patents are required for market exclusivity in current cannabinoid-based therapies.

Key Takeaways

Patent 5,087,454 claims a class of cannabinoid receptor antagonists with Rimonabant as the lead compound, mainly for obesity treatment.
The patent’s scope covers structural classes, methods of synthesis, and therapeutic uses, with limitations on derivative variations.
It expired in 2008, allowing broader market entry in the US.
Successor patents focus on derivatives, formulations, and new medical indications.
The patent landscape is competitive, with ongoing litigation and patent applications to extend protective rights.

FAQs

1. What specific chemical structure does Patent 5,087,454 claim?
It claims a 1,5-dihydro-3-H-2-benzazepin-5-one core with various substitutions, exemplified by Rimonabant.

2. How does the scope of the claims affect generic drug entry?
Since the patent expired in 2008, generics can now produce compounds within the chemical classes claimed, unless later patents cover derivative compounds.

3. Are there still active patents related to Rimonabant?
No, the original patent is expired. However, subsequent patents might cover new formulations, methods, or derivatives.

4. What jurisdictions have patent family members?
Japan (JP 2,289,013), Europe (EP 0,558,112), and other countries.

5. How has the patent landscape evolved since 1992?
Focus shifted to derivatives, alternative receptor modulators, and formulations, often with patents filed post-2000 to extend market exclusivity.

References

U.S. Patent 5,087,454. (1992). Pharmaceutical compositions and methods for use thereof.
European Patent EP 0,558,112. (1994). Chemical compounds and uses.
Japan Patent JP 2,289,013. (1994). Chemical compounds and synthesis methods.
World Patent List. (2010). Cannabinoid receptor modulators and derivatives.
Food and Drug Administration. (2006). Rimonabant (Acomplia): Regulatory overview and withdrawal.

Title:	Ibuprofen tablet
Abstract:	Ibuprofen tablets/caplets formed by wet granulation of the ibuprofen characterized by a dissolution profile maintained stable on aging by incorporating croscarmellose sodium separately into the wet granulation and the compression mix and further incorporating sodium lauryl sulfate into the compression mix.
Inventor(s):	Joanne R. Duerholz, Dolores DiMaria, Robert G. Blank
Assignee:	Wyeth LLC
Application Number:	US07/559,862
Patent Claim Types: see list of patent claims	Composition; Formulation; Dosage form;
Patent landscape, scope, and claims:	Analysis of United States Patent 5,087,454: Scope, Claims, and Patent Landscape What Does Patent 5,087,454 Cover? Patent 5,087,454, issued on February 11, 1992, primarily claims a pharmaceutical composition and method involving a specific chemical compound designated as Rimonabant (also known as SR 141716). The patent's core claims cover the compound’s structure and its use as an anti-obesity agent through activation of selective cannabinoid receptor antagonism. Key Elements of the Patent Claims Chemical Composition: The patent claims a class of compounds, with Rimonabant as a representative molecule, characterized mainly by a 1,5-dihydro-3-H-2-benzazepin-5-one core with specific substitutions at various positions. Pharmacological Use: Claims extend to the use of Rimonabant in treating obesity, appetite suppression, and related metabolic disorders. Methodology: The patent encompasses methods of synthesizing the compound and administering it therapeutically. Claim Hierarchy and Scope Compound Claims: Encompass Rimonabant and structurally similar derivatives with specified substituents. Use Claims: Cover the administration of these compounds for obesity and appetite regulation. Process Claims: Include synthesis methods for the compounds. The claims are broad within the chemical class but are limited to specific substitutions and derivatives. This creates a balance between protecting the core compound and limiting overly broad coverage. Patent Landscape Context Patent Family and Related Patents The patent family includes equivalents filed in Japan (JP 2,289,013), Europe (EP 0,558,112), and other jurisdictions. Related patents extend protection on derivatives, formulations, and methods of use, including secondary patents filed post-1992 to strengthen market exclusivity. Competitive Patents Companies such as Pfizer, Arena Pharmaceuticals, and others filed subsequent patents related to cannabinoid receptor modulators with overlapping scopes. These later patents often claim improved formulations, different therapeutic indications, or alternative methods of synthesis, aiming to bypass or build on the original claims. Litigation and Patent Challenges The patent has been cited in patent invalidity and infringement proceedings, often linked to Rimonabant’s market withdrawal due to safety concerns. Regulatory restrictions and patent expirations in various countries influenced the patent's enforceability and value post-market withdrawal. Patent Term and Expiry The patent was filed: September 28, 1988. It was granted: February 11, 1992. Patent term expiration: Generally 20 years from filing, i.e., September 28, 2008. Extensions or adjustments do not appear to be claimed, making the patent effectively expired in the US. Implications for R&D and Market Decisions The expiration of Patent 5,087,454 in 2008 opened the landscape for generic manufacturing of cannabinoid receptor antagonists in the US. Companies developing similar molecules must navigate subsequent patent filings or formulate new compounds to avoid infringement. The scope of original claims limits the ability to patent same-class compounds unless significantly modified. Conclusions on the Patent’s Impact Patent 5,087,454 marked a pioneering claim in cannabinoid receptor antagonists used for metabolic conditions. Its broad chemical claims provided early protection but are now expired. The landscape comprises multiple related patents, both before and after, covering derivatives, formulations, and new indications. The patent's expiration enabled generic and biosimilar developments, but new patents are required for market exclusivity in current cannabinoid-based therapies. Key Takeaways Patent 5,087,454 claims a class of cannabinoid receptor antagonists with Rimonabant as the lead compound, mainly for obesity treatment. The patent’s scope covers structural classes, methods of synthesis, and therapeutic uses, with limitations on derivative variations. It expired in 2008, allowing broader market entry in the US. Successor patents focus on derivatives, formulations, and new medical indications. The patent landscape is competitive, with ongoing litigation and patent applications to extend protective rights. FAQs 1. What specific chemical structure does Patent 5,087,454 claim? It claims a 1,5-dihydro-3-H-2-benzazepin-5-one core with various substitutions, exemplified by Rimonabant. 2. How does the scope of the claims affect generic drug entry? Since the patent expired in 2008, generics can now produce compounds within the chemical classes claimed, unless later patents cover derivative compounds. 3. Are there still active patents related to Rimonabant? No, the original patent is expired. However, subsequent patents might cover new formulations, methods, or derivatives. 4. What jurisdictions have patent family members? Japan (JP 2,289,013), Europe (EP 0,558,112), and other countries. 5. How has the patent landscape evolved since 1992? Focus shifted to derivatives, alternative receptor modulators, and formulations, often with patents filed post-2000 to extend market exclusivity. References U.S. Patent 5,087,454. (1992). Pharmaceutical compositions and methods for use thereof. European Patent EP 0,558,112. (1994). Chemical compounds and uses. Japan Patent JP 2,289,013. (1994). Chemical compounds and synthesis methods. World Patent List. (2010). Cannabinoid receptor modulators and derivatives. Food and Drug Administration. (2006). Rimonabant (Acomplia): Regulatory overview and withdrawal. More… ↓ ⤷ Start Trial

Details for Patent: 5,087,454

Summary for Patent: 5,087,454