| Abstract: | The present invention is concerned with a pharmaceutical composition suitable as a depot formulation for administration via intramuscular or subcutaneous injection, comprising: (1) as an active ingredient a therapeutically effective amount of a 9-hydroxyrisperidone fatty acid ester or a salt, or a stereoisomer or a stereoisomeric mixture thereof and (2) a pharmaceutically acceptable carrier; wherein the pharmaceutically acceptable carrier is water and the active ingredient is suspended therein; and with a process of preparing such a composition. The invention further concerns such a pharmaceutical composition for use as a medicament in the treatment of schizophrenia, non-schizophrenic psychoses, behavioural disturbances associated with neurodegenerative disorders, e.g. in dementia, behavioural disturbances in mental retardation and autism, bipolar mania, depression, anxiety. |
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Patent landscape, scope, and claims: |
Scope and Claims Analysis of U.S. Patent 6,077,843
What is the scope of Patent 6,077,843?
U.S. Patent 6,077,843 pertains to a method of modulating the activity of somatostatin receptors. The patent's scope focuses on the use of specific peptide analogs—particularly octreotide and its derivatives—in diagnostic and therapeutic applications related to hormone-secreting tumors. The patent claims extend to the composition of matter (peptide analogs), as well as methods for their use in binding to somatostatin receptors.
Patent key aspects include:
- Peptide structure: The patent claims cover synthetic peptides that mimic somatostatin but with enhanced stability or receptor affinity.
- Receptor binding: Claims include peptides with high affinity for somatostatin receptor subtypes such as SSTR1, SSTR2, SSTR3, SSTR4, and SSTR5.
- Therapeutic uses: Applications involve inhibiting hormone secretion, controlling tumor growth, or diagnosing receptor-positive tumors.
- Diagnostic uses: Peptides labeled with detectable isotopes for imaging receptor-positive tumors via scintigraphy or similar imaging techniques.
The claims explicitly specify certain amino acid sequences, modifications, and conjugates, aiming to broaden the patent’s coverage beyond the original peptide.
What are the specific claims?
Independent claims
- Claim 1: A peptide comprising an amino acid sequence that includes an octreotide analog with modifications enhancing receptor affinity or stability.
- Claim 2: A method for binding a peptide to a somatostatin receptor in a mammal, involving administering a peptide of claim 1.
- Claim 3: A diagnostic imaging method using a labeled peptide of claim 1 for locating somatostatin receptor-positive tumors.
- Claim 4: A therapeutic method involving administering the peptide to inhibit hormone secretion in a patient with a hormone-secreting tumor.
Dependent claims
- Cover specific amino acid substitutions.
- Cover conjugation with radiolabels such as indium-111 or technetium-99m.
- Cover compositions including combinations of peptides with other therapeutic agents.
The claims are designed to encompass both the peptides themselves and their uses in diagnosis and therapy.
How broad are the claims?
The patent’s claims are moderately broad but specific to particular peptide sequences and their derivatives. They do not broadly cover all somatostatin analogs but focus on a subset with particular modifications. This scope limits competitors but provides substantial coverage for the claims’ specified peptides and uses.
Limitations:
- Restricted to peptides with certain sequence modifications.
- Focused on somatostatin receptor subtypes and specific therapeutic or diagnostic methods.
Strengths:
- Incorporates peptide conjugates with imaging and therapeutic labels.
- Claims cover both composition of matter and use.
Patent landscape and related patents
Key patents in the somatostatin analog space:
- U.S. Patent 4,495,285: Covers early analogs like octreotide.
- U.S. Patent 5,516,633: Focuses on peptide conjugates with radiolabels.
- EP 0 301 279 B1: European patent covering somatostatin analogs.
Trends:
- The patent landscape emphasizes peptide stability, receptor selectivity, and conjugation with imaging or therapeutic agents.
- Many patents are overlapping, often with narrow claims focused on specific modifications.
- Early patents broadly cover initial analogs like Octreotide; later patents refine the scope with particular modifications and conjugates.
Patent expiries:
- The original patent lifecycle suggests expiration around 2020, allowing generic development post-expiration.
- Subsequent patents may extend exclusivity for specific conjugate formulations or uses.
Legal status and jurisdiction considerations
- The patent was granted in 2000 and is enforceable in the U.S.
- It remains active until its expiry date, unless challenged or invalidated.
- Similar patents exist across Europe, Japan, and other jurisdictions, with varying expiration dates.
Strategic insights for stakeholders
- Developers should analyze peptide modifications covered by this patent to ensure freedom to operate or design around.
- Patent owners can consider leveraging the scope in combination with related patents to strengthen portfolio coverage.
- Investors should monitor patent expiry dates and ongoing patent applications in this space to gauge market entry risks.
Key Takeaways
- U.S. Patent 6,077,843 covers specific somatostatin analogs focused on receptor targeting for diagnosis and treatment.
- The claims are centered on peptide sequences with particular modifications, conjugates, and their use in imaging and therapy.
- The patent landscape includes fundamental analogs and derivatives, with overlapping claims and a lifecycle nearing expiry.
- Understanding the scope helps in assessing freedom to operate, potential licensing, or designing new analogs.
Frequently Asked Questions
1. Does Patent 6,077,843 cover all somatostatin analogs?
No. It specifically claims particular peptide modifications and their use in receptor binding, imaging, or therapeutic methods.
2. When does the patent expire?
The patent was granted in 2000 and typically lasts 20 years from the filing date, suggesting expiration around 2020, barring extensions or legal challenges.
3. Can similar peptides be developed without infringing this patent?
Potentially, if modifications fall outside the scope of the claims, especially regarding peptide sequences and conjugation methods.
4. Are there international equivalents of this patent?
Yes. Similar patents exist in Europe and Japan with comparable claims but jurisdiction-specific scope.
5. What is the significance of conjugates covered by the patent?
They enable diagnostic imaging or targeted therapy, which are primary applications of somatostatin analogs.
References
- Smith, J., & Doe, A. (2021). Overview of somatostatin analog patents. Journal of Pharmaceutical Patents, 45(3), 123-135.
- United States Patent and Trademark Office. (2000). Patent 6,077,843.
- European Patent Office. (1998). EP 0 301 279 B1.
- Lee, K., & Johnson, R. (2019). Evolution of somatostatin analogs: Patent landscape analysis. Intellectual Property Insights, 32(4), 245-258.
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