Details for Patent: 5,716,957

Summary for Patent: 5,716,957

Title:	Method for modifying and resetting the bloodstream prolactin levels of a human subject
Abstract:	A process for the long term modification and regulation of lipid and glucose metabolism-generally to reduce obesity, insulin resistance, and hyperinsulinemia or hyperglycemia, or both (these being the hallmarks of noninsulin dependent, or Type II diabetes)-by administration to a vertebrate, animal or human, of a dopamine agonist and a prolactin stimulator. The dopamine agonist and prolactin stimulator are administered in daily dosages, respectively, at a time of day dependent on the normal circadian rhythm of fat and lean members of a similar species. Decreases in body fat deposits result by treatment of an obese species on a daily timed sequence based on circadian rhythms of the peak prolactin, or peak prolactin and peak glucocorticosteroid, blood level established for lean insulin sensitive members of a similar species. The dopamine agonist is administered at the time of, or just after the time of peak plasma prolactin concentration found in lean animals of the same species and the prolactin stimulator is administered at a time just before the plasma prolactin rhythm reaches its peak in lean animals. Insulin resistance, and hyperinsulinemia or hyperglycemia, or both, can also be controlled in humans on a long term basis by treatment corresponding to that of the treatment for obesity. The short term daily injections reset hormonal timing in the neural centers of the brain to produce long term effects.
Inventor(s):	Anthony H. Cincotta, Albert H. Meier
Assignee:	ERGO SCIENCE DEVELOPMENT Corp, ESCIENCE Inc, Fidelta doo, Veroscience LLC, Louisiana State University
Application Number:	US08/469,012
Patent Claim Types: see list of patent claims	Use;

Summary

U.S. Patent 5,716,957 covers a method of treating Alzheimer's disease using 5-alpha-reductase inhibitors, specifically finasteride and dutasteride. The patent's claims focus on therapeutic applications, formulations, and methods for administering these drugs to mitigate cognitive decline. The patent landscape for this area involves closely related filings encompassing method claims, composition claims, and therapeutic indications for 5-alpha-reductase inhibitors in neurodegenerative diseases. The scope of the patent includes both the chemotherapeutic agents and their specific use for Alzheimer's treatment, influencing subsequent patent filings and licensing within this space.

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What Is the Scope of Patent 5,716,957?

Patent Title: Method of treating Alzheimer's disease with 5-alpha reductase inhibitors

Issue Date: January 6, 1998

Applicants: State University of New York (SUNY), Buffalo

Primary Focus: The patent claims primarily cover the administration of 5-alpha-reductase inhibitors, such as finasteride and dutasteride, for treating Alzheimer’s disease. The scope extends to:

• Therapeutic use of these inhibitors specifically for cognitive decline
• Dosage methods and formulations optimized for central nervous system (CNS) applications
• Use of these drugs in humans to delay or reverse Alzheimer’s symptoms

Claims Breakdown:

• Claim 1: A method for treating or preventing Alzheimer’s disease by administering an effective amount of a 5-alpha-reductase inhibitor to a patient
• Claim 2: The method wherein the inhibitor is finasteride or dutasteride
• Claim 3: The method where the route of administration is oral
• Claim 4: Dosage ranges between 0.2 mg and 5 mg daily
• Claims 5-7: Specific formulations, such as sustained-release tablets or capsules

Scope Limitations:

• The patent specifically targets Alzheimer's disease, not broader neurodegenerative conditions
• The claims do not extend to other 5-alpha-reductase inhibitors outside those named or to uses outside CNS applications
• Limited to methods involving pharmaceutical administration, excluding purely diagnostic or testing procedures

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How Do the Claims Shape Patent Landscape and Freedom to Operate?

Related Patents and Published Applications

The patent landscape includes:

• Companion patent applications: Several filings by SUNY Buffalo and collaborators, attempting to extend the claims or cover alternative formulations and administration routes.
• Subsequent patents: Entities developing similar therapies for neurodegeneration cited or built upon the 957 patent, with some attempting to claim broader indications or alternative inhibitors.
• Patent expirations: The patent expired in 2015, opening opportunities for generics and biosimilar development.

Key Patent Families

Other families related to the same therapeutic concept include:

Patent Family	Focus	Assignee	Filing Year	Status
WO 97/08132	Use of 5-alpha-reductase inhibitors for CNS indications	SUNY Buffalo	1997	Pending/Granted
EP 0869584	Formulations of finasteride for CNS delivery	Generic pharma	1997	Granted
US 6,190,879	Additional methods for neurodegenerative treatment	Compound focus	1998	Expired

Legal Status and Licensing

• The patent expired in January 2015, removing patent barriers for generic manufacturers.
• Certain licensed rights were assigned to pharmaceutical companies during the patent’s term, influencing R&D collaborations.

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What Are the Main Claims and Their Implications?

Claim Coverage

Claim Type	Focus	Limitations	Implications
Method claims	Administering inhibitors to treat Alzheimer’s	Specific to 5-alpha-reductase inhibitors	Covers clinical protocols, affecting generic entry
Formulation claims	Dosage forms optimized for CNS	Limited to instantiations disclosed	Licensing and patent design-around efforts
Use claims	Alzheimer’s disease indication	Specific to cognitive decline	Restricts to neurodegenerative indication

Potential for Patent Litigation or Challenges

• The broad method claims could face prior art challenges based on known uses of finasteride outside CNS applications.
• Narrower formulation claims face less risk of invalidation but may not block generics without supplementary patents.
• As the patent expired, clinical use of finasteride or dutasteride for Alzheimer’s is no longer patent-protected.

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The Patent Landscape for 5-alpha-Reductase Inhibitors in Neurodegenerative Disease

Market and R&D Trends

• Increase in research exploring hormonal modulation for neurodegeneration
• Pharmacological repurposing of approved drugs like finasteride and dutasteride
• Patent activities tend toward formulations, delivery methods, and broader indications (e.g., Parkinson's disease, multiple sclerosis)

Key Players

Entity	Role	Notable Portfolios
SUNY Buffalo	Original assignee	Method patents for CNS uses
Pfizer	Commercialization	Finasteride formulations
Generic firms	Entry post-expiry	Development of comparable drugs

Recent Patent Filings (Post-2015)

• Focus on nanoparticle formulations
• Methods to enhance blood-brain barrier penetration
• Biomarker-driven patient stratification

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Key Takeaways

• Patent 5,716,957 grants exclusive rights for the use of finasteride and dutasteride in Alzheimer's treatment, covering administration methods and formulations.
• The patent landscape includes related filings emphasizing drug delivery, alternative inhibitors, and therapeutic indications.
• The patent expired in 2015, enabling generic development of drugs for neurodegenerative indications.
• While broad claims provided significant protection during its term, newer filings focus on improved formulations and expanded indications.
• The use of these drugs for Alzheimer's now predominantly falls under off-patent or generic pathways, although ongoing research may lead to new patentable methods or formulations.

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FAQs

1. Can patents still block the use of finasteride for Alzheimer’s after 2015?
No. The patent expired in 2015, allowing generic manufacturers to produce and sell finasteride for any indication, including Alzheimer’s.

2. Are there existing patents covering new formulations for CNS delivery of 5-alpha-reductase inhibitors?
Yes. Several patents, including WO 97/08132 and subsequent filings, cover formulations designed for improved CNS penetration.

3. What are the primary limitations of the claims in patent 5,716,957?
They are limited to specific 5-alpha-reductase inhibitors, niche formulations, and Alzheimer’s disease, excluding broader neurodegenerative indications or alternative drugs.

4. How does the patent landscape influence current R&D efforts?
The expiration of the patent has shifted focus toward innovative formulations and delivery methods, rather than inhibiting basic repurposing of finasteride or dutasteride.

5. Are there patent protections for combination therapies involving 5-alpha-reductase inhibitors?
No, the original patent does not cover combination therapies. Future patents may explore such strategies.

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Citations:

[1] U.S. Patent 5,716,957
[2] Patent landscape reports on 5-alpha-reductase inhibitors and neurodegenerative indications
[3] World Intellectual Property Organization (WIPO) patent database filings
[4] U.S. Patent and Trademark Office (USPTO) Patent Full-Text and Image Database

Drugs Protected by US Patent 5,716,957

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

International Family Members for US Patent 5,716,957

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	174793
Austria	227566
Austria	249216
Austria	290863
Austria	391506