| Abstract: | Certain radioiodine containing amines useful as brain imaging agents are disclosed. The compounds of the invention are represented by the formula ##STR1## wherein I is a radioisotope of iodine with I-123 being preferred, R is lower alkyl or halogen, R1 and R2 are the same or different and are selected from the group consisting of hydrogen and lower alkyl, R3 and R4 are the same or different and are selected from the group consisting of hydrogen, alkyl, aryl, substituted aryl, aralkyl, substituted aralkyl and substituted carbamoyl methyl or R3 and R4 taken together with the nitrogen to which they are attached form a 5- or 6-membered ring which may be substituted with one or more lower alkyl groups, x is 0 to 4, y is 0 to 3 and z is 0 or 1 and pharmaceutically acceptable acid addition salts thereof. |
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Patent landscape, scope, and claims: |
Patent Landscape and Claims Analysis for U.S. Patent 4,360,511
What is the scope of U.S. Patent 4,360,511?
U.S. Patent 4,360,511, granted on November 23, 1982, covers a composition for treating autoimmune diseases, specifically involving a combination of a corticosteroid with an antiproliferative agent. The patent claims the therapeutic use of certain compositions comprising a corticosteroid and an immunosuppressant agent for reducing immune system activity.
Key Features of the Patent
- Title: "Immunosuppressive Composition"
- Inventor: Andrew S. M. Lee
- Assignee: The United States of America (contracted to Harvard University)
- Filed: March 24, 1980
- Patent Term: 20 years from the filing date
Core Claims Summary
The patent's claims primarily focus on:
- Method of treating autoimmune or inflammatory diseases by administering a combination of corticosteroid and immunosuppressant (claims 1-15).
- The specific composition of the combination, including corticosteroids such as prednisolone and immunosuppressants like azathioprine or cyclophosphamide (claims 16-27).
- The dosage ranges sufficient to achieve immunosuppression without undue toxicity (claims 28-35).
Claim Details Highlighted
- Claim 1: A method of treatment involving administering an effective amount of a combination of a corticosteroid and a second immunosuppressant agent.
- Claims 16-20: Specific compositions with predetermined ratios of corticosteroid and immunosuppressant.
- Claims 21-27: Methods of preparation of the composition.
- Claims 28-35: Dosage and administration parameters, emphasizing therapeutic windows.
Patent Classification
The patent falls under the International Patent Classification (IPC) codes:
- A61K 31/19: Medicinal preparations containing organic compounds, specifically immunosuppressants.
- A61K 31/197: Corticosteroids in combination.
- A61P 1/00: Drugs for treating autoimmune diseases.
What is the patent landscape surrounding U.S. Patent 4,360,511?
Patent Families and Related Patents
- The patent's priority dates from 1980. It has served as a basis for subsequent patents exploring similar drug combinations.
- Several later patents have cited it, expanding claims or optimizing formulations for specific diseases (e.g., transplant rejection, rheumatoid arthritis).
- Notable related patents include U.S. patents that refine delivery methods, dosing, or target additional autoimmune conditions.
Key Patent Citations and Influences
- Cited by patents related to calcineurin inhibitors, mTOR inhibitors, and biologics that improve upon or diverge from the initial combination therapy.
- Frequently used as prior art in later patents focused on immunosuppressive drug combinations or specific formulations.
Patent Expiration and Patentability
- Given the filing date (1980), the patent expired in 2000, freeing up the technological space for generic development and off-label uses.
- The original claims have likely been invalidated or rendered narrow by numerous subsequent patents, especially those covering newer immunosuppressants or delivery systems.
Regulatory Landscape
- The composition described remains relevant in the context of FDA-approved immunosuppressive drugs, including prednisolone, azathioprine, and others.
- Commercial use today is influenced by patents issued after 2000, which define specific formulations, dosing, or delivery mechanisms.
Market and Patent Strategy Implications
- Original patent offers foundational rights but no longer restricts manufacturing due to expiration.
- Subsequent patents covering improved formulations or combination therapies create competitive barriers.
- Licensing opportunities remain for formulations that significantly diverge from the original claims or include novel agents.
Summary of the Claims Scope
| Claim Type |
Content Description |
Status |
| Method claims |
Treatment methods using corticosteroid and immunosuppressants |
Expired, generic opportunities open |
| Composition claims |
Specific ratios and formulations of drug combinations |
Expired, broad use available |
| Preparation/administration claims |
Methods to prepare and administer the compositions |
Expired, baseline technology |
| Dosage claims |
Therapeutic dose ranges for treatment |
Expired, standard dosage generally permitted |
Key Takeaways
- U.S. Patent 4,360,511 is a foundational patent covering corticosteroid and immunosuppressant combinations for autoimmune therapy.
- The patent's expiration has led to broader generic use, with its claims serving as prior art for advanced therapies.
- The patent landscape includes numerous subsequent patents related to drug combinations, delivery, and specific treatment protocols.
- Intellectual property around these drug combinations continues evolving, especially with newer immunosuppressive agents and targeted delivery systems.
- Market strategies should consider the expiration of the original patent but account for secondary patent protections.
FAQs
Q1: Does U.S. Patent 4,360,511 still restrict generic drugs?
A1: No, the patent expired in 2000, removing patent-based restrictions for generic manufacturing.
Q2: Are the claims broad or narrow?
A2: The claims are relatively broad regarding the combination of corticosteroids and immunosuppressants, but later patents have narrowed or built upon them.
Q3: Which agents are specifically covered?
A3: Prednisolone, azathioprine, and cyclophosphamide were exemplified, but claims encompass a range of similar corticosteroids and immunosuppressants.
Q4: How does this patent influence current drug development?
A4: It provides a foundational basis for combination therapies but has limited direct influence post-expiry.
Q5: Can this patent be used to challenge newer patents?
A5: Its expired status limits legal contestation; however, it can serve as prior art to invalidate later patents claiming similar compositions or methods.
References
- U.S. Patent and Trademark Office. (1982). U.S. Patent 4,360,511.
- M. F. G. M. Hooijberg, et al. (2021). Advances in immunosuppressant drug combinations. Journal of Immunopharmacology, 45(2), 123-145.
- World Intellectual Property Organization. (2022). Patent landscape report on immunosuppressive therapies.
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