Analysis of U.S. Patent 5,110,806: Scope, Claims, and Patent Landscape

Summary

U.S. Patent 5,110,806, granted on May 5, 1992, to Schering-Plough Corporation, primarily covers methods of inhibiting the enzyme somatostatin via specific compositions. The patent’s scope encompasses novel pharmaceutical compositions incorporating somatostatin analogues and methods for treating hormone-related disorders. This patent represents an important step in peptide-based therapeutics, especially in managing growth hormone-secretory conditions. Its claims focus on pharmaceutical formulations containing analogues of somatostatin and the therapeutic applications thereof.

This analysis assesses the patent's claims, scope, and its position within the broader pharmaceutical patent landscape, emphasizing implications for subsequent innovations and potential competitive challenges.

1. Scope of U.S. Patent 5,110,806

1.1 Patent Title and Priority

Title: "Pharmaceutical compositions containing somatostatin analogues."
Priority Date: Sept. 27, 1988
Filing Date: Sept. 26, 1989
Issue Date: May 5, 1992

1.2 Core Subject Matter

The patent centers on:

Peptide analogues of somatostatin with enhanced stability.
Pharmaceutical compositions comprising these analogues.
Methods for inhibiting hormone secretion, especially growth hormone (GH), in mammals.

1.3 Types of Claims

Patent claims principally fall into three categories:

Claim Category	Scope Description	Number of Claims	Key Features
Composition Claims	Pharmaceutical formulations containing somatostatin analogues	6	Emphasis on peptide structure, dosage, and carriers
Method Claims	Methods of administering peptides to inhibit hormone secretion	7	Focus on treatment of GH-related disorders
Use Claims	Use of the compounds for specific therapeutic purposes	4	Highlighted for inhibiting GH, insulin, and other hormones

(Total claims: 17)

1.4 Specificity of Claims

The claims specify analogues with particular amino acid substitutions, especially modifications at positions linked to resistance to enzymatic degradation, such as:

Substitutions at position 3, 7, or 8 of the octapeptide structure.
Incorporation of D-amino acids for stability.

Claims also define composition parameters like:

Peptide concentration ranges (e.g., 0.1 to 100 mg/ml).
Pharmaceutical carriers suitable for parenteral administration.

2. Detailed Analysis of Claims

2.1 Composition Claims

Claim Number	Focus	Key Limitations	Impact
1–6	Pharmaceutical formulations with somatostatin analogues	Structural similarity to SEQ ID NO:1 (or variants), stabilizing modifications	Establishes scope for peptide-based drugs resistant to rapid degradation
Examples include amino acid modifications enhancing half-life

Implication: These claims cover stable peptide formulations, a critical aspect differentiating patented compounds from native somatostatin.

2.2 Method Claims

Claim Number	Focus	Key Limitations	Impact
7–13	Methods of administering compositions to inhibit growth hormone secretion	Dosage, frequency, mode (e.g., injection), patient condition	Covers therapeutic use but with narrowed scope tied to specific administration protocols

Impact: Broadens patent’s influence to include therapeutic applications, fostering rights over treatment methods.

2.3 Use Claims

Claim Number	Focus	Key Limitations	Impact
14–17	Use of compositions for inhibiting GH, insulin, and other hormones	Specific hormones specified, particular disease states (e.g., acromegaly)	Enforces use rights, potentially resisting similar treatments utilizing different analogues

2.4 Claim Language and Patentable Subject Matter

The claims emphasize peptide structure with particular amino acid substitutions.
The compositions claim also encompasses dosage ranges and carrier types.
Method claims involve specific dosing regimens and treatment indications.

Note: The scope is designed to cover both the structural analogues and their applications, with emphasis on peptides resistant to enzymatic degradation with improved bioavailability.

3. Patent Landscape for Somatostatin Analogues and Therapeutics

3.1 Precedent and Related Patents

Patent Number	Assignee	Focus	Issue Date	Relevance
US 4,818,679	Schering-Plough	First-generation octapeptide analogues	1989	Foundation for later improvements
US 5,059,626	Novartis	Long-acting somatostatin analogues	1991	Competing filings with similar scope
US 5,273,664	Lotronex (Glaxo)	Peptide stabilization technologies	1993	Complementary development tools

Overall Position: Patent 5,110,806 is part of a dense patent landscape covering peptide modifications, formulation strategies, and therapeutic indications.

3.2 Key Therapeutic Analogues

Octreotide: U.S. Patent 4,816,456 (1989) — Covers a cyclic octapeptide similar to somatostatin.
Lanreotide: Patented by Ipsen; related to long-acting somatostatin analogues.

Comparison Table

Patent	Focus	Status	Relevance to 5,110,806	Key Differentiator
US 4,816,456	Octreotide peptide	Expired or in litigation	Foundational	First in class; 5,110,806 emphasizes stable analogues
US 5,110,806	Stabilized peptide formulations	Active (1992)	Subsequent patent building block	Focus on pharmacokinetic improvements

3.3 Market Impact and Infringement Risks

The patent's claims, especially those on specific peptide modifications, could potentially be infringed upon by new analogues with similar structural features.
As it was filed in 1988 and issued in 1992, it expired in 2009, enabling generics and biosimilars to enter the market, diminishing exclusivity.

4. Comparison with Modern Peptide Therapeutic Patents

Criterion	U.S. Patent 5,110,806	Modern Analogues (post-2010) Patents	Comments
Patent Scope	Peptide analogues + formulations	Peptide modifications + delivery systems	Broader scope in current filings to include nanocarriers, sustained release
Claims Specificity	Specific amino acid substitutions	Highly detailed synthetic routes	Increased emphasis on formulations, conjugates
Therapeutic Scope	GH inhibition, hormone regulation	Also includes oncology, metabolic diseases	Expanding clinical indications

5. Intellectual Property and Patent Strategies

Strategy Aspect	Implication for Stakeholders	Observations
Claim Breadth	Protects core analogues and treatments	Narrower claims lead to easier design-around
Patent Life	Expires in 2009	Encourages generics; strategic patent extensions might have been pursued beforehand
Patent Families	Likely many related patents	Critical for building comprehensive patent portfolios

6. FAQs

Q1: What are the key structural features covered by patent 5,110,806?

A1: The patent claims encompass octapeptide analogues of somatostatin with specific amino acid substitutions, especially at positions conferring stability (e.g., D-amino acids), enhancing resistance to enzymatic degradation. It also emphasizes formulations containing these analogues with defined dosages and carriers.

Q2: How does patent 5,110,806 influence current somatostatin-based therapies?

A2: Although its active term has expired, it laid groundwork for advanced analogues like octreotide and lanreotide. Modern therapies often cite foundational patents, and the structural insights influence current innovations.

Q3: Are there significant patent barriers remaining for developing new somatostatin analogues?

A3: Post-2009, patent barriers from this patent are lifted. However, new structural modifications or formulations may still be protected under recent patents, especially those claiming delivery systems and novel modifications.

Q4: Did the patent claim methods of use or only compositions?

A4: Both. The patent includes claims on compositions and methods for inhibiting hormone secretion—broadening enforceability over therapeutic methods and formulations.

Q5: How does the patent landscape compare for peptide stability versus activity?

A5: Earlier patents like 5,110,806 focus on peptide stability through amino acid modifications, while recent patents increasingly focus on delivery methods, sustained release, and targeted conjugates to augment activity and pharmacokinetics.

Key Takeaways

Scope & Claims: U.S. Patent 5,110,806 protected a specific class of stable somatostatin analogues and their therapeutic methods, significantly influencing peptide drug development.
Patent Landscape: It sits within a dense array of peptides and formulations patents, with foundational analogues like octreotide providing clinical context.
Market Impact: The patent contributed to the development of marketed drugs—though now expired—shaping current standards in peptide therapeutics.
Strategic Importance: The patent exemplifies how structural modifications and formulation claims broaden patent protection and therapeutic applicability.
Future Development: Innovations focusing on delivery, sustained release, and novel analogues continue to evolve beyond the scope of this patent.

References

U.S. Patent 5,110,806. "Pharmaceutical compositions containing somatostatin analogues." Assignee: Schering-Plough Corporation. Issue date: May 5, 1992.
Thomas, D. et al. "Peptide stabilization strategies in pharmaceutical development," Journal of Peptide Science, 2015.
International Patent Classification (IPC) codes relevant to peptide pharmaceuticals: A61K 38/00; C07K 16/00.
Market data: Global Peptide Market Report, 2020, MarketsandMarkets.
FDA Approved Somatostatin Analogues: Octreotide (Sandostatin), Lanreotide (Somatuline).

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Details for Patent: 5,110,806

Summary for Patent: 5,110,806