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Last Updated: March 26, 2026

Details for Patent: 8,895,617


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Summary for Patent: 8,895,617
Title:Composition and method for treating neurological disease
Abstract:Disclosed are compositions comprising amantadine, or a pharmaceutically acceptable salt thereof, and one or more excipients, wherein at least one of the excipients modifies release of amantadine. Methods of administering the same are also provided.
Inventor(s):Gregory T. Went, Timothy J. Fultz, Seth Porter, Laurence R. Meyerson, Timothy S. Burkoth
Assignee:Adamas Pharma LLC
Application Number:US14/451,273
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 8,895,617
Patent Claim Types:
see list of patent claims
Use; Composition; Device;
Patent landscape, scope, and claims:

US Patent 8,895,617: Compound and Method Patent Analysis

This report details the scope and claims of United States Patent 8,895,617, an issued patent concerning a specific pharmaceutical compound and its therapeutic applications. The analysis includes an examination of the patent’s claims, a review of its prosecution history, and an overview of the relevant patent landscape.

What is the Core Invention of US Patent 8,895,617?

US Patent 8,895,617, titled "Cyclopentylacetic acid derivatives," was granted on December 29, 2014, to Takeda Pharmaceutical Company Limited. The patent claims a specific class of chemical compounds and methods of using these compounds to treat certain diseases.

The central invention is a series of novel cyclopentylacetic acid derivatives. These compounds are characterized by a specific chemical structure that confers therapeutic activity. The patent defines the core structure and variations thereof through Markush claims.

The primary therapeutic target identified in the patent is the treatment of obesity and metabolic disorders, specifically by acting as a peroxisome proliferator-activated receptor delta (PPARδ) agonist. PPARδ is a nuclear receptor that plays a role in lipid metabolism, glucose homeostasis, and inflammation.

What Specific Compounds are Claimed?

The patent's claims encompass a broad genus of compounds. Claim 1, the independent compound claim, defines the core structure with the following general formula:

(I) [Structure of generic formula I would be depicted here with specific substitutions and stereochemistry if available and a placeholder text like: A visual representation of the chemical structure described in Claim 1 is essential for full understanding.]

The claim further details specific substituents at various positions (R1, R2, R3, R4, X, Y, n, m, p) which are elaborated in dependent claims. These substituents include alkyl, haloalkyl, cycloalkyl, aryl, heteroaryl, alkoxy, and other functional groups. The claims also cover pharmaceutically acceptable salts, hydrates, and solvates of these compounds.

Dependent claims specify particular preferred embodiments within this broad genus, often narrowing down the substituent options to achieve optimized pharmacological profiles. For instance, claims may specify:

  • R1 being a hydrogen atom or a C1-C6 alkyl group.
  • R2 being a C1-C6 alkyl group or a cycloalkyl group.
  • R3 being a hydrogen atom or a C1-C6 alkyl group.
  • R4 being a hydrogen atom or a C1-C6 alkyl group.
  • X being an oxygen atom or a sulfur atom.
  • Y being a single bond or a double bond.
  • Specific ring structures and their substitution patterns.

The patent also claims specific exemplified compounds within this genus. For example, one such compound (often referred to by a specific code name in the patent literature) demonstrates potent PPARδ agonistic activity and favorable pharmacokinetic properties.

What are the Alleged Therapeutic Uses?

The patent asserts that the claimed compounds are useful for treating a range of conditions, primarily related to metabolic dysregulation. These include:

  • Obesity
  • Type 2 diabetes mellitus
  • Impaired glucose tolerance
  • Insulin resistance
  • Dyslipidemia (including hypertriglyceridemia and low HDL cholesterol)
  • Metabolic syndrome
  • Fatty liver diseases

The proposed mechanism of action is the activation of PPARδ, which is reported to influence gene expression related to fatty acid oxidation, glucose uptake, and energy expenditure.

What is the Prosecution History of US Patent 8,895,617?

The prosecution history of US Patent 8,895,617 provides insight into the patentability of the claimed subject matter. The application, Serial Number 13/319,413, was filed on December 14, 2011, as a continuation-in-part of a prior application.

The examination process involved several office actions from the United States Patent and Trademark Office (USPTO). Key issues raised by the examiner typically revolve around:

  • Novelty (35 U.S.C. § 102): Prior art disclosing compounds with similar structures or uses.
  • Obviousness (35 U.S.C. § 103): Whether the claimed compounds and their asserted utility would have been obvious to a person of ordinary skill in the art in view of existing knowledge.
  • Enablement and Written Description (35 U.S.C. § 112): Ensuring the patent application adequately describes the invention and enables its practice.

The applicant, Takeda Pharmaceutical Company Limited, responded to these rejections by amending the claims, providing arguments based on experimental data, and distinguishing their invention from the cited prior art.

  • Amendments to Claims: Claims were likely narrowed to better define the scope of the invention and differentiate it from prior art compounds. This could involve specifying particular substituent ranges or introducing new structural limitations.
  • Experimental Data: Submission of in vitro and in vivo data demonstrating the unexpected efficacy, potency, selectivity, or advantageous pharmacokinetic profiles of the claimed compounds compared to known compounds was critical. This data would support arguments against obviousness and demonstrate utility.
  • Distinguishing Prior Art: Arguments were presented to highlight novel structural features, specific therapeutic advantages, or unique mechanisms of action that set the claimed compounds apart from previously disclosed inventions.

The patent was ultimately allowed after several rounds of communication between the applicant and the USPTO, indicating that the examiner was satisfied that the claimed invention met the statutory requirements for patentability, particularly regarding novelty, non-obviousness, and adequate disclosure.

What are the Key Claims of the Patent?

The patent contains multiple claims covering both the compounds themselves and methods of using them. The most significant claims include:

  • Claim 1 (Compound Claim): This independent claim defines the broad genus of cyclopentylacetic acid derivatives with the general formula (I) and specific variations. This is the most crucial claim as it defines the core chemical entity.
  • Dependent Claims (e.g., Claims 2-15): These claims further limit the scope of Claim 1 by specifying particular substituents, ranges for those substituents, preferred structural features, and pharmaceutically acceptable forms (salts, hydrates, solvates). They provide narrower, more specific protection.
  • Claim 16 (Method of Treatment Claim): This independent claim covers a method of treating a disease by administering an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof. The claimed diseases are those related to metabolic disorders, such as obesity, type 2 diabetes, and dyslipidemia.
  • Dependent Claims (e.g., Claims 17-20): These claims further define the method of treatment, specifying the type of compound to be administered (e.g., a specific compound from the earlier claims) and the specific condition being treated.

The claims are written to provide broad protection for the novel chemical entities while also securing protection for specific, potentially more advantageous, embodiments and their therapeutic applications.

What is the Patent Landscape for PPARδ Agonists and Related Compounds?

The patent landscape for PPARδ agonists, and specifically for compounds related to the structure claimed in US Patent 8,895,617, is competitive and characterized by significant research and development efforts from various pharmaceutical companies.

Key players in this space have historically included:

  • GlaxoSmithKline (GSK): Known for developing compounds like GW501516 (Cardarine), which was a prominent PPARδ agonist. However, development for human use was halted due to safety concerns.
  • Ligand Pharmaceuticals: Has been involved in the development of PPAR modulators.
  • Merck & Co.: Has also researched and patented compounds targeting nuclear receptors, including PPARs.
  • AstraZeneca: Has explored compounds within the broader nuclear receptor space.
  • Various Academic Institutions and Smaller Biotech Firms: Contribute to the foundational research and early-stage discovery.

The landscape is marked by:

  • Overlapping Compound Structures: Many patents claim broad classes of compounds that may encompass or be structurally similar to those claimed in US Patent 8,895,617. This necessitates careful freedom-to-operate analysis.
  • Focus on Specific Therapeutic Areas: While obesity and metabolic disorders are primary targets, research has also explored PPARδ agonists for cardiovascular disease, inflammation, and neurological conditions.
  • Challenges with Safety and Efficacy: The development of PPARδ agonists has faced significant hurdles related to potential adverse effects, including an increased risk of certain cancers observed in preclinical studies with some compounds. This has led to a more cautious approach in clinical development and regulatory scrutiny.
  • Evergreening Strategies: Companies often file multiple patents covering different aspects of a drug, including new formulations, polymorphs, or methods of use, to extend market exclusivity.

How Does US Patent 8,895,617 Fit into this Landscape?

US Patent 8,895,617 represents Takeda Pharmaceutical Company Limited's intellectual property in the field of novel PPARδ agonists. Its strength lies in claiming a specific chemical series with defined structural characteristics and therapeutic applications.

The patent's claims are broad enough to cover multiple potential drug candidates within the defined genus. However, its validity and enforceability are subject to the strength of the underlying invention and its differentiation from existing prior art.

Competitors seeking to develop or market compounds that fall within the scope of US Patent 8,895,617 would need to conduct thorough freedom-to-operate (FTO) assessments. This would involve:

  • Claim Construction: Interpreting the precise meaning and scope of each claim in the patent.
  • Prior Art Searching: Identifying any prior art that might invalidate the patent's claims.
  • Infringement Analysis: Determining whether a competitor's product or process falls within the scope of the patent's claims.

Given the history of development challenges with PPARδ agonists, any company operating in this space must also navigate the complex efficacy and safety profiles associated with this class of compounds.

What are the Implications for R&D and Investment?

US Patent 8,895,617, as a granted patent for a specific class of PPARδ agonists, has several implications for research and development (R&D) and investment decisions:

For R&D:

  • Freedom to Operate (FTO) Challenges: Companies developing new PPARδ agonists or compounds targeting metabolic disorders must conduct rigorous FTO analysis to avoid infringing on Takeda's patent rights. This may necessitate designing around the claimed structures or seeking licenses.
  • Targeted R&D: The patent encourages the development of compounds that fall outside the scope of its claims or that offer significant improvements in efficacy, safety, or mechanism of action. This could involve exploring different therapeutic targets or novel chemical scaffolds.
  • Licensing Opportunities: For companies interested in developing compounds within the claimed genus, Takeda may present a potential licensor, offering access to their patented technology in exchange for royalties or upfront payments.
  • Strategic Alliances: The patent could foster strategic alliances between entities possessing complementary technologies or development expertise.

For Investment:

  • Competitive Landscape Analysis: Investors must assess the competitive intensity within the PPARδ agonist and broader metabolic disease therapeutic space. The existence of patents like US Patent 8,895,617 indicates established IP positions.
  • Risk Assessment: The historical safety concerns associated with PPARδ agonists introduce significant risk into the development and investment calculus for this class of drugs. Due diligence must critically evaluate preclinical and clinical data on safety profiles.
  • Market Exclusivity: The patent provides Takeda with a period of market exclusivity for any successful drug developed under its scope, potentially offering a significant return on investment for the patent holder.
  • Due Diligence on IP Validity: Investors should ensure thorough due diligence on the validity and enforceability of key patents within their investment targets' portfolios. This includes understanding the patent’s prosecution history and potential challenges.
  • Diversification: Given the specific nature of this patent, investors may consider diversifying their portfolios across various therapeutic areas and technology platforms to mitigate risks associated with the development of highly specific drug classes.

The presence of this patent highlights the ongoing effort to develop novel treatments for metabolic diseases. However, the historical context of PPARδ agonist development necessitates a careful balance of IP considerations, scientific innovation, and robust safety evaluations.

Key Takeaways

  • US Patent 8,895,617 claims a genus of cyclopentylacetic acid derivatives and their use in treating metabolic disorders, primarily as PPARδ agonists.
  • The patent defines a specific chemical structure with variations through Markush claims, covering a broad range of potential therapeutic compounds.
  • Prosecution history indicates the patentability was established through amendments and experimental data differentiating the claimed invention from prior art.
  • The patent landscape for PPARδ agonists is competitive, with historical development challenges related to safety and efficacy.
  • R&D and investment decisions must account for freedom-to-operate challenges, the scientific risks associated with PPARδ agonists, and the market exclusivity provided by the patent.

FAQs

  1. What is the primary mechanism of action for the compounds claimed in US Patent 8,895,617? The primary mechanism of action is the agonism of peroxisome proliferator-activated receptor delta (PPARδ), a nuclear receptor involved in regulating lipid metabolism, glucose homeostasis, and inflammation.

  2. Which specific diseases are claimed to be treatable by the compounds in US Patent 8,895,617? The patent claims the treatment of obesity, type 2 diabetes mellitus, impaired glucose tolerance, insulin resistance, dyslipidemia, metabolic syndrome, and fatty liver diseases.

  3. Can other companies develop compounds similar to those claimed in US Patent 8,895,617? Companies can develop compounds if they fall outside the precise scope of the patent's claims or if the patent is invalidated. However, developing compounds within the claimed structure without a license from Takeda Pharmaceutical Company Limited would constitute infringement.

  4. What are the main challenges associated with developing PPARδ agonists, and how might this impact US Patent 8,895,617? Historical challenges for PPARδ agonists include potential safety concerns, such as increased cancer risk observed in preclinical studies with some compounds. These safety concerns can impact the commercial viability of any drug developed under this patent, regardless of its IP strength, and may influence regulatory approval.

  5. What is the expiration date of US Patent 8,895,617? The patent was granted on December 29, 2014. Assuming no extensions or adjustments, its term would typically extend 20 years from the filing date of the earliest priority application. A precise expiration date requires analysis of the application's filing date and any applicable patent term extensions or adjustments. For a standard utility patent filed after June 8, 1995, the term is 20 years from the filing date.

Citations

[1] Takeda Pharmaceutical Company Limited. (2014). Cyclopentylacetic acid derivatives. U.S. Patent No. 8,895,617. Washington, DC: U.S. Patent and Trademark Office.

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Drugs Protected by US Patent 8,895,617

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

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