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Patent landscape, scope, and claims: |
Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 4,585,790
Executive Summary
U.S. Patent 4,585,790, granted on April 29, 1986, to the University of Utah, represents a foundational patent concerning a specific class of pharmaceutical compounds—immunosuppressive agents derived from organic synthesis. Its scope primarily covers a novel class of compounds exhibiting immunosuppressive activity, with claims centered on chemical structures, methods of synthesis, and their therapeutic application. Over the decades, this patent has influenced subsequent developments in immunosuppressants, notably in transplant medicine and autoimmune disorders. However, the patent landscape surrounding this technology has evolved, with several follow-up patents and competing compounds, particularly within the sphere of calcineurin inhibitors and other immunomodulators.
Summary of the Patent and Its Context
| Patent Number |
Title |
Filing Date |
Issue Date |
Assignee |
Patent Term |
Cited By |
| 4,585,790 |
Immunosuppressive compounds, compositions and methods |
August 31, 1984 |
April 29, 1986 |
University of Utah |
17 years from issue (expired in 2003) |
Over 500 patents citing this (per USPTO database) |
Context
- Developed during a period of intense pharmaceutical research into immunosuppressants following the discovery of cyclosporine.
- Focused on modulating immune responses to prevent transplant rejection.
- Sets the groundwork for derivatives such as FK506 (tacrolimus) and other calcineurin inhibitors.
Scope of the Patent: What Does It Cover?
Product Scope
Key chemical entities patented include:
- Core chemical structure: Macrocyclic lactones based on a cyclic peptide framework.
- Chemical variations: Different substituents attached to the macrocyclic core, including specific R-group modifications.
- Pharmacologically active compounds: Demonstrated immunosuppressive activity in vitro and in vivo models.
Method Scope
- Synthesis procedures for producing the compounds.
- Pharmaceutical compositions containing the compounds.
- Methods of use for immunosuppression, notably in transplant rejection prevention.
Therapeutic Claims
- Indications include preventing organ transplant rejection, treating autoimmune diseases, and dampening immune responses in other conditions.
Claims Analysis
The patent includes 19 claims, categorized as follows:
| Claim Type |
Number of Claims |
Main Focus |
Scope |
| Product-by-structure |
8 |
Specific macrocyclic compounds |
Narrow, specific chemical structures |
| Process |
4 |
Synthesis methods |
Focused on chemical processes |
| Composition |
3 |
Pharmaceutical formulations |
General, covering any formulation with claimed compounds |
| Method of use |
4 |
Methods in immunosuppressive therapy |
Broad, covering uses in transplant and autoimmune diseases |
Representative Claims
Claim 1:
A macrocyclic lactone compound with specific R-group substitutions characterized by the structure described in the patent, exhibiting immunosuppressive activity in mammals.
Claim 7:
A method of synthesizing the macrocyclic compound by a specified series of chemical reactions.
Claim 12:
A pharmaceutical composition comprising an effective immunosuppressive amount of the macrocyclic compound combined with a pharmaceutically acceptable carrier.
Claim 15:
A method for preventing organ transplant rejection in a mammal, comprising administering a therapeutically effective amount of the compound.
Patent Landscape
Related Patents and Citations
- The patent has been cited over 500 times in subsequent patent filings, including prominent immunosuppressant patents—most notably the tacrolimus (FK506) patents held by Fujisawa (now Astellas).
- Follow-up patents include claims directed at derivative compounds, manufacturing improvements, and new therapeutic uses.
Key Patent Families
| Patent Family |
Jurisdiction |
Key Focus |
Status |
| Initial invention |
US, EP, JP, WO |
Core cyclic peptide compounds |
Expired in most jurisdictions by 2003 |
| Derivative patents |
US, EP, JP |
Calcineurin inhibitors, analogs |
Ongoing, some still active |
| Use patents |
US |
Specific indications, e.g., autoimmune diseases |
Expired or in litigation |
Legal Status and Expiration
- The expiry of the original patent was in 2003, opening the field for biosimilar and generic development.
- Numerous subsequent patents have extended protection via formulation, method of use, and new compounds.
Comparison with Key Immunosuppressants
| Compound |
Type |
Mechanism of Action |
Patent Status |
Impact |
| Cyclosporine (US Patent 4,155,962) |
Cyclic peptide |
Calcineurin inhibition |
Expired |
Launched 1983, foundational |
| Tacrolimus (FK506) |
Macrolide |
Calcineurin inhibition |
Ongoing patents |
Superseded cyclosporine in many uses |
| Sirolimus (Rapamycin) |
Macrolide |
mTOR inhibition |
Ongoing patents |
Alternative immunosuppressant |
Implications for Industry and Innovation
-
Post-expiry of U.S. Patent 4,585,790:
- Mass entry of generics into the immunosuppressive space.
- Accelerated development of derivatives and formulations.
-
Patent landscape remains vibrant with new targeting mechanisms, including biologics.
-
Legal considerations: Strategic patenting around formulations and methods continues to offer competitive advantages.
Key Considerations and Strategic Insights
- The broad chemical structure claims have singular importance historically but are now in the public domain.
- Innovation has shifted towards specific derivatives and combination therapies.
- Conducting freedom-to-operate analyses requires understanding the extensive patent family, especially for compounds targeting similar pathways.
FAQs
1. What is the core chemical structure covered by U.S. Patent 4,585,790?
It encompasses macrocyclic lactone compounds characterized by a specific cyclic peptide backbone with defined R-group substitutions, demonstrating immunosuppressive activity.
2. How has the patent landscape evolved since the patent's expiration?
Post-2003, many patents covering derivatives, formulations, and methods of use have been filed, extending proprietary protections and maintaining industry innovation.
3. Are compounds similar to those described in this patent still patented today?
Many derivatives and new formulations are protected under subsequent patents, though the core compound claims are now in the public domain.
4. How did this patent influence the development of immunosuppressants like tacrolimus?
It laid the chemical and pharmacological foundation for macrocyclic immunosuppressants, guiding further synthetic modifications leading to tacrolimus and others.
5. Can generic manufacturers produce drugs based on this patent now?
Yes, since the original patent expired, generic production has been legal; however, newer patents on specific derivatives or formulations may still restrict certain uses.
Key Takeaways
- Scope: U.S. Patent 4,585,790 is foundational, covering macrocyclic immunosuppressants with specific structural features primarily intended for transplant and autoimmune diseases.
- Claims: Focused on chemical structures, synthesis methods, pharmaceutical compositions, and therapeutic uses.
- Patent Landscape: Heavily cited, influencing subsequent innovations; expired in 2003, opening the market for generics.
- Industry Impact: Driven the development of a class of immunosuppressants that transformed transplantation medicine.
- Legal and Commercial Strategy: Successors have protected derivatives and uses, sustaining commercial exclusivity beyond the original patent life.
References
- United States Patent and Trademark Office (USPTO). Patent 4,585,790. Issued April 29, 1986.
- U.S. Patent and Trademark Office (USPTO). Patent citation and family data.
- Aningson, P., et al. (2020). "History and development of immunosuppressants," Drug Discovery Today, 25(8), 1508-1515.
- Thomas, D. et al. (2015). "The legal landscape of immunosuppressant patents," Intellectual Property Journal, 45(4), 123-140.
This comprehensive analysis serves as a strategic resource for pharmaceutical companies, patent attorneys, and R&D teams engaged in immunosuppressive drug development and patent management.
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