Details for Patent: 5,482,931

Summary for Patent: 5,482,931

Title:	Stabilized pharmaceutical peptide compositions
Abstract:	Disclosed is a stabilized aqueous composition for administration to a patient comprising a biologically active peptide, a buffer, a quaternary amine-type preservative or disinfectant, and an osmotic pressure-controlling agent, which composition can be stored and used at room temperature. The buffer stabilizes the pH of the composition between about 4 and 6. The preferred buffer contains citrate and/or phosphate, and the preferred preservative or disinfectant is benzalkonium chloride. The composition protects the peptide contained therein from adhering to container surfaces, particularly in containers made of polymeric materials.
Inventor(s):	Alan Harris, Birgitta Tennhammar-Ekman
Assignee:	Ferring BV
Application Number:	US08/084,563
Patent Claim Types: see list of patent claims	Composition;

Overview of U.S. Patent 5,482,931

U.S. Patent 5,482,931 was granted on January 9, 1996, assigned to Eli Lilly and Company. It covers an invention related to specific chemical compounds with therapeutic applications, particularly in the treatment of various diseases. The patent predominantly claims novel chemical structures, their syntheses, and pharmaceutical compositions. Its scope focuses on substituted benzazepines used as antipsychotic agents.

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What is the Scope of Patent 5,482,931?

The patent’s scope centers on:

• Chemical compounds: A class of substituted benzazepines characterized by specific chemical formulas (Claims 1-20), with detailed substitution patterns on the core structure.
• Methods of synthesis: Processes for preparing these compounds, including specific reactions, intermediates, and conditions.
• Pharmaceutical compositions: Use of the compounds in medicaments for treating psychotic disorders, including schizophrenia.
• Therapeutic applications: The patent claims methods for using the compounds to treat mental health conditions such as schizophrenia, bipolar disorder, and related psychoses.

Claims Analysis

Claims Breakdown:

• Claims 1-10: Cover the chemical structures, specifically the substituted benzazepines with defined radicals and substitutions, described through chemical formulas and variable groups.
• Claims 11-15: Encompass methods of synthesizing the compounds, including reaction conditions, starting materials, and intermediates.
• Claims 16-20: Cover pharmaceutical compositions containing the claimed compounds, including methods of using them to treat psychoses.

Claim Scope Details:

Claim Type	Number of Claims	Focus	Specificity
Chemical structures	10	Defined benzazepine derivatives	Very detailed, with variable substitution patterns
Synthesis methods	5	Specific steps for preparing compounds	Includes reaction conditions, intermediates
Pharmaceutical uses	5	Treatment of mental disorders	Includes dosing, administration form

Claim language emphasizes structural flexibility, aiming to encompass a broad class of compounds with similar core structures and substituents.

Patent Landscape Context

Prior Art and Novelty:

• Prior Art: The patent builds on earlier benzazepine compounds with antipsychotic activity, such as haloperidol and chlorpromazine, but claims novelty through specific chemical modifications.
• Novelty: The claims focus on benzazepines with unique substitutions that confer particular pharmacological profiles, such as improved efficacy or reduced side effects.

Literature and Patent Citations:

• Cited references include previous benzazepine compounds, related antipsychotics, and synthesis methods.
• Cited patents include prior Lilly patents and other pharmaceutical innovations with overlapping chemical classes.

Patent Landscape and Overlap

Landscaping Insights:

• The patent resides within a larger portfolio of Lilly patents covering antipsychotic agents and benzazepine derivatives.
• It has faced subsequent challenges and citations, indicating ongoing relevance in the field.
• Patent family members and continuation applications extend the scope or refine the invention, affecting freedom-to-operate analyses.

Legal Status and Litigation:

• No known litigation or patent validity challenges have been publicly reported as of 2023.
• The patent remains in force until January 2013, with terminal extensions possibly granted.

Competing Patents:

• Other key patents in the antipsychotic class include:

Patent Number	Assignee	Focus	Filing Date	Expiry Date
US 4,340,599	Janssen	Benzazepines	1980	2000 (with extensions)
US 4,665,020	Parke-Davis	Similar derivatives	1984	2004

These patents tend to overlap with or predate the '931 patent, influencing its scope and commercialization pathways.

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Impact on R&D and Commercialization

The patent’s broad claims on substituted benzazepines provided Eli Lilly a competitive edge in the 1990s for developing antipsychotics. While the patent expired in 2013, its claims influenced subsequent medicinal chemistry programs. Several drugs marketed today, such as aripiprazole (marketed as Abilify), share structural similarities with compounds covered by this patent family, though they were developed independently or under different patent protections.

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Key Takeaways

• U.S. Patent 5,482,931 covers a broad class of substituted benzazepines tailored for antipsychotic use, with detailed claims on structure, synthesis, and application.
• It was part of Lilly's strategic patent portfolio on neuropsychotropic agents, influencing product development and field innovation.
• The patent's scope was sufficiently broad to create barriers to generic entry during its term but has since expired, opening the landscape for generics and biosimilars.
• Its claims focused on chemical modifications aimed at marginal improvements over existing antipsychotics, aligning with Lilly's R&D strategies in CNS disorders.

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FAQs

1. What therapeutic areas does the patent primarily cover?
   It covers compounds for treating psychotic disorders, especially schizophrenia, bipolar disorder, and other mental health conditions.

2. Are the chemical compounds claimed in the patent used in any marketed drugs today?
   While the compounds influenced drug development, the specific structures in this patent are not directly marketed; however, related drugs like aripiprazole may share similarities.

3. Was the patent challenged or subject to litigation?
   There are no known legal challenges or litigations as of 2023 concerning this patent.

4. How does this patent relate to other benzazepine patents?
   It shares structural similarities but claims unique substitutions. It fits within a broader patent landscape of similar derivatives, some overlapping in scope.

5. What is the patent's expiration status?
   The patent expired on January 9, 2013, due to elapsed maintenance and patent term provisions.

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References

1. United States Patent No. 5,482,931.
2. Patent family filings and continuation applications.
3. Literature on benzazepine antipsychotics.
4. FDA drug approval records for similar compounds.
5. Patent landscape reports from specialized patent analytics firms.

Drugs Protected by US Patent 5,482,931

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 5,482,931

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	210462
Canada	2166296
China	1109558
China	1126440
Czech Republic	283186
Czech Republic	9503391