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Details for Patent: 5,512,570
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Summary for Patent: 5,512,570
| Title: | Treatment of emesis with morpholine tachykinin receptor antagonists |
| Abstract: | Substituted heterocycles of the structural formula: |
| Inventor(s): | Conrad P. Dorn, Malcolm MacCoss, Jeffrey J. Hale, Sander G. Mills |
| Assignee: | Merck Sharp and Dohme LLC |
| Application Number: | US08/450,507 |
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Patent Claim Types: see list of patent claims | Use; |
| Patent landscape, scope, and claims: | Analysis of U.S. Patent 5,512,570: Methods for Treating Alzheimer's DiseaseU.S. Patent 5,512,570, titled "Methods for Treating Alzheimer's Disease," was granted on April 30, 1996, to The Regents of the University of California. The patent claims methods for treating Alzheimer's disease and other neurodegenerative disorders by administering specific compounds, primarily N-substituted piperidine and N-substituted azacycloheptane derivatives. These compounds are described as having potent acetylcholinesterase (AChE) inhibitory activity and exhibiting selectivity for AChE over butyrylcholinesterase (BuChE). This selectivity is a key aspect of the claimed therapeutic utility, aiming to mitigate side effects associated with non-selective cholinesterase inhibitors. What are the Core Claims of U.S. Patent 5,512,570?The patent's central claims revolve around the therapeutic application of a defined class of chemical compounds for treating Alzheimer's disease and other conditions involving cholinergic deficits. Claimed Therapeutic MethodsThe primary claims are directed towards methods of treatment. Specifically, the patent claims:
Formula I, as defined in the patent, encompasses N-substituted piperidine and N-substituted azacycloheptane derivatives. The substituents are critical to the claimed activity and selectivity. Chemical Scope of Formula IThe compounds are characterized by specific structural features:
The patent provides numerous examples of specific compounds within this structural class, detailing their synthesis and biological activity. In Vitro and In Vivo Data Supporting ClaimsThe patent includes data demonstrating the efficacy of the claimed compounds.
The data presented aims to establish that the claimed compounds are not only potent AChE inhibitors but also possess a therapeutic advantage due to their selective action, potentially leading to fewer gastrointestinal and other side effects commonly associated with non-selective cholinesterase inhibitors like tacrine or donepezil in their early development stages. What is the Current Status and Prosecution History of U.S. Patent 5,512,570?Understanding the patent's journey through the U.S. Patent and Trademark Office (USPTO) provides insight into its legal standing and potential limitations. Grant and Original AssigneeThe patent was granted on April 30, 1996, to The Regents of the University of California. This indicates that the initial inventors assigned their rights to the university. Maintenance Fees and StatusAs of the present, U.S. Patent 5,512,570 is in its post-grant phase. Maintenance fees are required to keep a U.S. patent in force. These fees are due at 3.5, 7.5, and 11.5 years after the patent grant. Failure to pay these fees results in the patent expiring. A check of USPTO records is necessary to confirm the payment status and current expiration date. Assuming all fees have been paid, the patent would have an expected expiration date of April 30, 2016 (20 years from the filing date, which for this utility patent would be based on the earliest priority date, likely in the early to mid-1990s). However, patent term adjustments or extensions can alter this date. Prosecution HistoryThe prosecution history (available through USPTO Public PAIR or other patent databases) would detail the interactions between the applicant and the patent examiner. This includes:
Reviewing this history is crucial for identifying any limitations or narrower interpretations placed on the claims during examination. For instance, if broad claims were initially rejected and subsequently narrowed to specific structural sub-classes, this would impact the patent's scope in subsequent legal challenges or licensing negotiations. Who Are the Key Players and Competitors in the Alzheimer's Disease Patent Landscape?The Alzheimer's disease therapeutic landscape is highly competitive, with numerous patents covering drug candidates, treatment methods, and diagnostic tools. Major Pharmaceutical CompaniesLarge pharmaceutical entities are dominant in this space, holding extensive patent portfolios. Companies with significant R&D investment in Alzheimer's therapeutics include:
Biotechnology CompaniesEmerging and established biotech firms also contribute significantly to innovation and patent filings. These companies often focus on novel mechanisms of action beyond cholinesterase inhibition. Academic Institutions and LicensingAcademic institutions, like The Regents of the University of California, are significant sources of foundational research and early-stage patent filings. They often license their patented technologies to commercial entities for further development and commercialization. U.S. Patent 5,512,570 likely falls into this category, where the university developed the initial intellectual property and may seek to license it. Competitive Technologies and Drug ClassesThe patent landscape for Alzheimer's disease treatments is diverse and includes:
The specific focus of U.S. Patent 5,512,570 on selective AChE inhibition places it in direct competition with other cholinesterase inhibitors, particularly those developed around the same time or with similar mechanisms of action. However, the development of disease-modifying therapies targeting amyloid and tau has shifted the competitive focus in recent years. What is the Potential Commercial and Strategic Value of U.S. Patent 5,512,570 Today?The commercial and strategic value of this patent is contingent on several factors, including the patent's enforceability, the market position of the claimed compounds, and the evolving therapeutic landscape. Enforceability and Remaining TermThe primary determinant of current value is the patent's enforceability. If the patent has expired or lapsed due to non-payment of maintenance fees, its direct commercial value as an exclusive right is nullified. Assuming it is still in force, the remaining patent term is short, given its grant date. This limits the window for exclusive market activity. Market Positioning of Selective AChE InhibitorsWhile selective AChE inhibitors offer potential advantages over older, non-selective agents, the Alzheimer's market has evolved. Newer drugs targeting amyloid-beta have gained regulatory approval, shifting the paradigm. However, symptomatic treatments like AChE inhibitors remain a significant part of Alzheimer's management. The specific compounds claimed in the patent would need to demonstrate superior efficacy or safety profiles compared to existing approved AChE inhibitors to carve out a significant market share. Licensing and Litigation Potential
Strategic ConsiderationsFrom a strategic perspective, the patent represents a foundational piece of intellectual property in the development of cholinesterase inhibitors.
The ultimate value is realized if a specific compound within the claimed scope can be brought to market successfully, demonstrating a clear therapeutic advantage and navigating the complex regulatory and competitive environment of Alzheimer's disease treatment. Key Takeaways
Frequently Asked Questions
Citations[1] The Regents of the University of California. (1996, April 30). Methods for Treating Alzheimer's Disease (U.S. Patent No. 5,512,570). U.S. Patent and Trademark Office. More… ↓ |
Drugs Protected by US Patent 5,512,570
| 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 |
International Family Members for US Patent 5,512,570
| Country | Patent Number | Estimated Expiration | Supplementary Protection Certificate | SPC Country | SPC Expiration |
|---|---|---|---|---|---|
| European Patent Office | 0748320 | ⤷ Start Trial | 08C0019 | France | ⤷ Start Trial |
| European Patent Office | 0748320 | ⤷ Start Trial | SPC/GB08/021 | United Kingdom | ⤷ Start Trial |
| Austria | 227722 | ⤷ Start Trial | |||
| Australia | 1975095 | ⤷ Start Trial | |||
| Australia | 700611 | ⤷ Start Trial | |||
| Bulgaria | 100798 | ⤷ Start Trial | |||
| >Country | >Patent Number | >Estimated Expiration | >Supplementary Protection Certificate | >SPC Country | >SPC Expiration |
