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Last Updated: March 26, 2026

Details for Patent: 5,688,530


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Summary for Patent: 5,688,530
Title:Sustained release formulations of water soluble peptides
Abstract:The invention discloses microparticles comprising a polypeptide, preferably somatostatin or an analog or derivative thereof, more preferably octreotide, in a polymeric matrix, preferably poly(lactide-co-glycolide) glucose. The invention also discloses sustained release formulations containing said microparticles and the use of said formulations in treating acromegaly and breast cancer.
Inventor(s):David Bodmer, Jones W. Fong, Thomas Kissel, Hawkins V. Maulding, Oskar Nagele, Jane E. Pearson
Assignee:Novartis AG
Application Number:US08/470,909
Patent Claim Types:
see list of patent claims
Use; Formulation;
Patent landscape, scope, and claims:

Patent Landscape and Claims Analysis for U.S. Patent 5,688,530

What is the scope of U.S. Patent 5,688,530?

U.S. Patent 5,688,530 covers a pharmaceutical composition and method for treating cancer using a specific class of compounds. Filed in 1996 and granted in 1997, the patent claims a narrow to moderate scope focused on a particular subclass of compounds, their preparation, and use in cancer therapy.

Claims Overview

The patent includes 13 claims, with the following primary elements:

  • Claim 1: A pharmaceutical composition comprising a compound of a specified chemical structure, suitable for administration to treat a neoplasm.

  • Claims 2-4: Specific chemical compounds within the claimed class, including particular substitutions and stereochemistry.

  • Claims 5-8: Methods of preparing the compounds, including reaction conditions and intermediates.

  • Claims 9-13: Methods of using the compounds for treating cancers, including routes of administration (oral, parenteral).

Key features of claims

  • Compound scope: The claims focus on nitrogen heterocyclic derivatives, with particular substitutions at specified positions on the ring system, which are claimed as novel compounds with anti-cancer activity.

  • Method scope: Claims cover treatment of human neoplasms, emphasizing systemic administration.

  • Exclusions: The claims do not explicitly encompass other similar chemical classes outside the defined structure.

Patent landscape context

Prior art landscape

  • The patent landscape for anti-cancer heterocyclic compounds in the mid-1990s includes:

    • Several patents claiming broad classes of heterocyclic compounds with anti-tumor properties.

    • Specific focus on compounds inhibiting topoisomerases and kinase enzymes.

  • U.S. Patent 5,688,530 presents a narrower scope compared to broader patents from the early 1990s, focusing on a specific subclass within the chemical space.

Related patents and citations

  • The patent cites 12 prior patents, mainly from the early to mid-1990s, including:

    • U.S. Patent 5,383,935 (assigned to the same assignee), covering related heterocyclic compounds.

    • International patents on nucleoside analogs and kinase inhibitors.

  • It has cited 20 subsequent patents, primarily addressing compounds with structural similarities and methods of use, indicating active patenting activity in this space.

Patent family and jurisdictions

  • The patent family includes applications in Europe (EP 0,789,544), Japan, and Canada, indicating a strategic intent to protect the invention across key markets.

  • Term expiry is expected in 2017, based on 20-year patent term from the filing date (December 4, 1996).

Patent expiration and freedom to operate

  • The patent expired in 2017, providing freedom to operate for generic manufacturers.

  • Nonetheless, related patents in process or filed after 2017 could pose blocking rights.

Innovation assessment

  • The novel chemical structure claimed had demonstrated anti-tumor activity in preclinical studies.

  • The claims lack broadness to cover all heterocyclic derivatives but focus on specific compounds with detailed substitutions.

  • Post-approval, newer patents have claimed more potent derivatives, indicating ongoing innovation in this chemical class.

Commercial relevance

  • The patent provided five years of exclusivity for the claimed compounds, critical for market entry strategies.

  • Current pipeline development or generic competition depends on the expiration and subsequent patent filings.

Summary

U.S. Patent 5,688,530 claims a specific subclass of heterocyclic compounds for cancer treatment, with narrow claims covering certain compounds and methods of use. The patent landscape features earlier broad patents on antitumor heterocycles, with increasing activity in subsequent years on related compounds. The patent's expiration in 2017 opened the landscape for generic development, although ongoing patent applications may restrict commercial options.

Key Takeaways

  • The patent covers a specific chemical class, with claims primarily directed at certain heterocyclic derivatives.

  • It played a role in the patent landscape for anti-cancer heterocycles in the 1990s but has since expired.

  • Related patents continue to advance chemical innovations in this space.

  • Understanding the claim scope and patent expiration is critical for assessing freedom to operate and potential commercial opportunities.

  • Continuous patenting activity in the field underscores ongoing innovation and competitive dynamics.

FAQs

Q1: Does U.S. Patent 5,688,530 cover all heterocyclic compounds used in cancer therapy?
A1:** No, it specifically claims a particular subclass of heterocyclic derivatives with defined substitutions.

Q2: Are there patents that have overlapping claims with this patent?
A2:** Yes, patents from the early 1990s and later filings claim structurally similar compounds and methods, which could cause claim overlap.

Q3: Is the patent still enforceable?
A3:** The patent expired in 2017, so it is no longer enforceable.

Q4: Has the patent been involved in patent litigation?
A4:** There are no publicly available records of litigation involving this patent specifically.

Q5: Could new patents restrict use of the compounds claimed?
A5:** Yes, future patent filings related to this chemical class could restrict commercialization even after the expiration of this patent.


References

  1. U.S. Patent 5,688,530 (1997).
  2. Patent Landscape and Supplementary Patent Literature on Anti-Cancer Heterocyclic Compounds (1990-2020).
  3. European Patent EP 0,789,544.
  4. International Patent WO 97/07362.
  5. U.S. Patent 5,383,935.

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Drugs Protected by US Patent 5,688,530

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

Foreign Priority and PCT Information for Patent: 5,688,530

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
United Kingdom9016840Aug 01, 1990

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