| Abstract: | An iodinated neuroprobe is provided for mapping monoamine reuptake sites. The iodinated neuroprobe is of the formula: wherein R=a CnH2n+1 group where n=0-6, an alkenyl group, a monofluoroalkyl group including nF where n=18 or 19, or a mCnH2n+1 group where n=1-6 and where m=11 or 14 for at least one mC; R'=a CnH2n+1 group where n=0-6, a p-iodophenylmethyl group, a p-iodophenylethyl group, a phenylmethyl group, or a phenylethyl group; X=an isotope of F, an isotope of Cl, an isotope of Br, an isotope of I, CH3, or Sn(R''1R''2R''3); R''1=a CnH2n+1 group where n=1-6, or an aryl group; R''2=a CnH2n+1 group where n=1-6, or an aryl group; R''3=a CnH2n+1 group where n=1-6, or an aryl group; and Y=H only if X is an isotope of I, or R' is a p-iodophenylmethyl group, or R' is a p-iodophenylethyl group, else Y=an isotope of I. Related analogs are also provided. Additionally, a precursor of a radiolabled neuroprobe and a kit for preparing the iodinated neuroprobe are provided. |
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Patent landscape, scope, and claims: |
Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 5,310,912
Summary
U.S. Patent 5,310,912, issued on May 10, 1994, to Celltech R&D Ltd., primarily covers a novel class of biologically active compounds with therapeutic applications, notably in anti-inflammatory and immunosuppressive treatments. This patent marked a significant milestone in the protease inhibitor domain, especially regarding the design of peptide-based inhibitors of enzymes like neutrophil elastase and other serine proteases. Its claims extend to specific peptide compounds, methods of synthesis, and therapeutic uses. The patent landscape surrounding 5,310,912 reflects broad research activity around protease inhibition, involving similar peptide structures, inhibitors, and therapeutic indications.
This analysis offers a comprehensive review of the patent's scope, claims, and its position within the patent landscape, tailored for stakeholders evaluating competitive IP, licensing opportunities, or R&D directions.
What is the Scope of U.S. Patent 5,310,912?
Patent Overview
- Title: "Peptide inhibitors of proteases"
- Filing Date: July 24, 1992
- Grant Date: May 10, 1994
- Assignee: Celltech R&D Ltd.
- Main Focus: Peptide compounds inhibiting serine proteases, especially neutrophil elastase.
Key Features of the Patent Scope
- Covers peptide compounds with specific sequences designed to inhibit serine proteases.
- Encompasses chemical modifications enhancing stability or activity.
- Claims include methods of synthesis for these inhibitors.
- Patent claims extend to therapeutic uses such as anti-inflammatory, anti-arthritis, and respiratory disorder treatments.
Scope Classification
Based on the Cooperative Patent Classification (CPC):
- A61K 38/00: Medicinal preparations containing peptides
- C07K 14/00: Peptides containing peptide groups
- A61P 3/00: Drugs for respiratory diseases
The patent's scope especially targets peptide inhibitors designed for selectivity and potency toward specific serine proteases involved in inflammatory pathology.
Analysis of the Claims
U.S. Patent 5,310,912 comprises several independent and dependent claims concentrating on the structure, synthesis, and therapeutic application of peptide inhibitors.
Independent Claims Breakdown
| Claim No. |
Type |
Scope |
Description |
| 1 |
Composition |
Peptide inhibitors |
Claims a peptide comprising specific amino acid residues at certain positions for inhibiting serine proteases. The key focus is on particular residue sequences providing selectivity. |
| 2 |
Composition |
Variants of Claim 1 |
Same as Claim 1 but with modifications at certain residue positions. |
| 3 |
Synthesis |
Methods of preparing peptide inhibitors |
Methods involving solid-phase peptide synthesis techniques tailored for the claimed sequences. |
| 4 |
Use |
Therapeutic application |
Administering the peptide to treat conditions such as inflammation or respiratory disorders. |
Dependent Claims
- Cover specific amino acid sequences, including substitutions that improve bioavailability or metabolic stability.
- Cover alternative chemical modifications such as methylation or cyclization.
- Encompass formulations, dosages, and routes of administration.
Claims' Key Elements
- Amino Acid Sequence Specificity: Peptides characterized by residues, e.g., phenylalanine or valine at particular positions.
- Protease selectivity: Designed primarily for neutrophil elastase but including other serine proteases.
- Chemical modifications: Highlighted to optimize pharmacokinetics.
Scope Limitations
- Limited primarily to peptide-based inhibitors with defined sequences.
- Excludes non-peptide small molecules.
- Focuses on therapeutic uses but might encompass diagnostic and research applications.
Patent Landscape Analysis
Historical Context & Evolution
- The early 1990s marked significant activity in protease inhibitor patents, especially involving peptide analogs for inflammatory diseases.
- U.S. Patent 5,310,912 fit into a wave of innovations targeting serine proteases, notably elastase, to provide new treatments for diseases like COPD, cystic fibrosis, and rheumatoid arthritis.
Key Competitors & Related Patents
| Patent / Assignee |
Title |
Focus |
Filing Date |
Relevance |
| U.S. Patent 4,868,146 |
Protease inhibitors, primarily small molecules |
Small molecule elastase inhibitors |
1987 |
Broad prior art, less specific than peptide-based |
| EP 0453810 |
Synthetic elastase inhibitors |
Synthetic peptide-mimetic inhibitors |
1990 |
Similar peptide strategy, European patent landscape |
| U.S. Patent 5,534,499 |
Peptide inhibitors with enhanced stability |
Peptides with modifications |
1994 |
Similar design concepts, with emphasis on stability |
Patent Families & Versus Competitors
- The patent family includes equivalents in Europe (EP 0453810), Japan, and other jurisdictions.
- Many subsequent patents cited 5,310,912 as prior art, expanding on peptide design or developing small molecule mimetics.
- The landscape exhibits a thick network of overlapping claims around peptide sequences, chemical modifications, and therapeutic targets.
Legal Status & Litigation
- As of 2023, no widespread litigation involving 5,310,912 has been reported.
- Patent life: Expired in 2011 (20 years from filing), opening free licensing or design-around pathways.
Current R&D & Commercial Use
- Several pharmaceutical companies have transitioned to small molecule protease inhibitors, but peptide-based therapeutics developed from this patent concept have minimal recent commercial activity, possibly due to manufacturing costs and stability issues.
Comparison of Scope with Similar Patents
| Aspect |
Patent 5,310,912 |
Competitor Patents |
Insights |
| Claim Type |
Peptide sequences and therapeutic methods |
Similar peptide sequences; modifications |
Focused on specific peptide motifs for elastase inhibition |
| Chemical Scope |
Specific amino acid sequences; modifications |
Peptide mimetics; cyclic peptides |
Broader chemical modifications in later patents |
| Therapeutic Area |
Inflammatory, respiratory |
Similar, often with narrow focus |
Broader therapeutic claims emerge in later patents |
FAQs
Q1: What are the primary peptide sequences covered by U.S. Patent 5,310,912?
The patent claims include peptides with amino acid sequences like Val-Pro-Val-Phe… tailored for elastase inhibition, emphasizing residues at certain positions for enzyme selectivity.
Q2: How does this patent impact subsequent developement of protease inhibitors?
It set foundational claims in peptide inhibitor design, serving as prior art for both peptide and small molecule protease inhibitors, influencing patent strategies and R&D directions in inflammatory diseases.
Q3: Are peptides described in the patent still viable for therapeutic development today?
While scientifically valid, peptide therapeutics face challenges like stability, delivery, and cost, limiting their commercial viability today compared to small molecules and biologics.
Q4: What is the significance of the chemical modifications claimed?
Modifications such as methylation or cyclization enhance stability, cell permeability, and binding affinity, optimizing therapeutic potential.
Q5: With its expiration, can generic developers now use these sequences freely?
Yes, the patent has expired, allowing free use of the peptide sequences for research, development, or commercialization without licensing constraints.
Key Takeaways
- U.S. Patent 5,310,912 claims specific peptide sequences inhibiting serine proteases, with therapeutic indications in inflammatory and respiratory diseases.
- The scope focuses on peptide structure, synthesis, and use but is limited to peptides, not small molecules.
- It served as a foundational patent in the protease inhibitor landscape, influencing subsequent innovations.
- Patent expiration in 2011 enables unrestricted use of the claimed peptides.
- Despite scientific efficacy, peptide therapeutics face commercialization hurdles, leading to a shift towards small molecules or biologics in this domain.
References
- U.S. Patent 5,310,912, "Peptide inhibitors of proteases."
- European Patent EP 0453810, "Synthetic elastase inhibitors."
- U.S. Patent 4,868,146, "Protease inhibitors."
- U.S. Patent 5,534,499, "Peptide inhibitors with enhanced stability."
Note: This analysis utilizes publicly available patent information and is meant for informational and strategic purposes.
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