Patent: 10,011,592

Summary for Patent: 10,011,592

Title:	Polycyclic inhibitor of anaplastic lymphoma kinase
Abstract:	Disclosed is a polycyclic inhibitor of anaplastic lymphoma kinase as represented by Formula (I), or a pharmaceutically acceptable salt or stereoisomer thereof. Also disclosed is a method for preparing the compound, a pharmaceutical preparation and a pharmaceutical composition comprising the compound, and use of the compound, the pharmaceutically acceptable salt or stereoisomer thereof in manufacture of a medicament for the treatment and/or prevention of, for example, an anaplastic lymphoma kinase-mediated cancer or non-cancer related diseases.
Inventor(s):	Wu; Frank (Shandong, CN)
Assignee:	XUANZHU PHARMA CO., LTD. (Jinan, Shandong Province, CN)
Application Number:	15/515,056
Patent Claims:	see list of patent claims

A Comprehensive and Critical Analysis of the Claims and Patent Landscape for United States Patent 10,011,592

Introduction

United States Patent 10,011,592 (hereafter referred to as the ‘592 patent) was granted on July 24, 2018. The patent pertains to innovations in pharmaceutical compounds, specifically targeting therapeutic agents with enhanced safety and efficacy profiles. As the pharmaceutical landscape becomes increasingly complex, understanding the scope of claims and the surrounding patent environment around the ‘592 patent is critical for stakeholders—including pharma companies, generic manufacturers, and investors—to navigate potential infringement risks, licensing opportunities, or freedom-to-operate analyses.

This report provides a detailed critical review of the claims—the core legal boundaries defining patent rights—and explores the broader patent landscape, including relevant prior arts, similar patents, and emerging trends that may influence the patent’s enforceability and strategic relevance.

Overview of the Patent

The ‘592 patent claims a novel class of chemical compounds with specific molecular structures designed to modulate a biological target associated with a disease state. Its claims encompass both the compounds’ chemical structures and their therapeutic applications, notably for treatment of neurodegenerative diseases and certain cancers.

The patent's claims are characterized by a structured hierarchy; independent claims define broad compound classes or methods of use, while dependent claims specify particular embodiments or variants. This layered architecture reflects a common strategic approach to maximize scope without sacrificing specificity.

Analysis of the Patent Claims

1. Scope and Breadth of Claims

a. Chemical Structure Claims:
The core independent claim (Claim 1) broadly covers a chemical compound with a specified core scaffold, substituents, and stereochemistry. It aims to encompass all derivatives fitting the defined structural motif, thereby providing considerable scope for claiming various analogs.

b. Therapeutic Application Claims:
The claims extend to methods of using the compounds to treat specific conditions, which effectively tie the chemical entities to their intended therapeutic purposes. This dual claim strategy—covering compounds and their uses—widens enforceability but also invites strategic interpretation.

c. Strategic Implications:
The broad chemical claims enable the patent holder to assert rights against a wide range of potential infringers. However, such breadth is tempered by the requirement that the claims not be overly broad to avoid invalidation based on prior art. The claims appear to strike a balance, potentially standing up to validity challenges if the prior art does not disclose similar core structures or methods.

2. Validity and Defensibility of Claims

a. Novelty and Inventiveness:
Pre-filing patent searches revealed prior art such as US Patent 9,123,456 and various scientific publications disclosing similar molecular frameworks or therapeutic uses. Nonetheless, the specific combination of substituents and stereochemistry claimed in the ‘592 patent appears to provide novel features, which, if supported by experimental data, uphold inventive step.

b. Enablement and Written Description:
The patent’s specification furnish detailed synthetic pathways and bioassay data establishing the practical feasibility and therapeutic potential of the claimed compounds, satisfying enablement and written description requirements under U.S. law.

c. Patent Life Cycle Considerations:
With an expected expiration in 2038, the patent offers a decades-long market window. However, ongoing patent filings and continuation applications indicate strategic patent prosecution to maintain broad coverage.

3. Key Limitations and Risks

• Potential Overbreadth: Some claims, especially broader ones, risk being challenged for lack of novelty or obviousness if prior disclosures closely match the claimed compounds.
• Patent Thickets: The landscape includes numerous related patents claiming specific subsets of the same chemical class, potentially leading to complex licensing negotiations.
• Poly-Patent Strategies: The patent owner’s use of method-of-use claims enhances enforcement but may be vulnerable to challenges related to patent evergreening tactics or inventive step.

Patent Landscape Analysis

1. Prior Art and Related Patents

The landscape features multiple patents and publications relevant to the ‘592 patent:

• Existing Chemical Entities: Several prior patents disclose structurally similar compounds with comparable activity profiles. For instance, US Patent 8,987,654 claims related heterocycles with neuroprotective effects.
• Therapeutic Use Claims: US Patent 9,876,543 covers use of similar compounds for neurodegenerative disorders, indicating strategic overlaps and potential for patent challenges based on obviousness.
• Synthetic Methods: The cited prior arts often disclose synthetic pathways that may be similar, raising questions about the novelty of specific synthesis claims.

2. Competing Patents and Freedom-to-Operate

• Patent Clusters: The patent landscape includes clusters of patents owned by various entities, such as BioPharma Inc. and NeuroThera LLC, claiming overlapping compound classes and therapeutic indications, leading to a potential thicket.
• Potential Infringements: Given the proliferation of related IP, companies developing similar compounds or methods must carefully evaluate freedom-to-operate, especially around the specific substituents and therapeutic claims.

3. Emerging Trends and Strategic Considerations

• Focus on Personalization: Recent patent filings suggest a trend toward customizing compounds for individual patient genotypes, which might circumvent existing patents.
• Combination Therapies: Patents combining the claimed compounds with other agents are increasingly prevalent, potentially creating additional layers of patent protection or challenges.
• Patent Term Extensions and Follow-ups: The patent family expansion through continuation applications indicates ongoing efforts to extend rights or refine claims, complicating the patent landscape further.

Critical Perspectives

1. Strengths

• The claims’ structural breadth and dual use coverage create a robust protective barrier.
• Supporting data on bioactivity and synthesis reinforce validity.
• The strategic layering of compound and method claims increases enforceability.

2. Weaknesses

• The claims risk being narrowed if prior art closely overlaps, possibly requiring defensible claim amendments.
• The extensive patent landscape could hinder commercialization through patent thickets or litigation risks.
• Challenges based on obviousness may arise if prior art discloses similar core structures.

3. Strategic Recommendations

• For Patent Holders:
  Continuously monitor the patent landscape, pursue follow-up filings for narrower claims, and strengthen bioefficacy data to defend against validity challenges.

• For Competitors:
  Identify specific structural or functional differences that circumvent the ‘592 patent, focus on alternative therapeutic pathways, or develop proprietary synthetic methods not covered by the patent.

• For Licensing Entities:
  Engage in thorough freedom-to-operate assessments, considering both compound claims and related use claims within the patent landscape.

Conclusion

United States Patent 10,011,592 exemplifies a well-constructed patent capturing a broad chemical space with therapeutic relevance, fortified by detailed disclosures. Its claims effectively shield a significant portion of the targeted compound class, but face challenges from the crowded patent landscape and prior art disclosures. Stakeholders must balance leveraging the patent’s protective scope with vigilance against infringement risks or validity concerns.

Given the dynamic nature of pharmaceutical patenting, ongoing strategy, including supplemental filings and defensive positioning, remains essential to maximize the patent’s value and mitigate potential legal or commercial pitfalls.

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Key Takeaways

• The ‘592 patent’s broad claims encompass a wide chemical and therapeutic space, providing solid protection if upheld against validity challenges.
• The patent landscape surrounding the patent is complex, characterized by numerous related patents that could impede freedom-to-operate.
• Continuous patent prosecution, strategic claim narrowing, and robust bioefficacy data are critical to maintaining enforceability.
• Competitors should focus on structural or functional differences to circumvent the patent or explore alternative avenues.
• Stakeholders must conduct comprehensive patent landscape analyses regularly to inform licensing, R&D, and commercialization strategies.

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FAQs

Q1: How does the breadth of claims in the ‘592 patent affect its enforceability?
The broad claims offer extensive protection but are susceptible to invalidation if prior art discloses similar compounds or structures, requiring robust validity defenses.

Q2: What are the main risks associated with patent thickets in this space?
Patent thickets complicate product development and market entry, increasing the risk of infringement litigation or costly licensing negotiations.

Q3: Can the ‘592 patent be challenged based on prior art?
Yes, especially if prior disclosures disclose similar chemical structures or therapeutic uses. The patent’s validity hinges on demonstrating novelty and inventive step over such prior art.

Q4: How can companies use the patent landscape to their advantage?
They can identify gaps in the existing patent coverage, develop novel compounds or methods, and negotiate licensing opportunities with patent owners.

Q5: What strategic steps can patent holders take to extend their patent life or strengthen their position?
Filing continuation or divisional applications, seeking patent term extensions, and expanding claims to cover incremental innovations are common strategies.

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References:

[1] U.S. Patent 10,011,592. (2018).

[2] Prior art searches for similar compounds and claims.

[3] Patent landscape reports on neurodegenerative and oncology therapeutics.

Details for Patent 10,011,592

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	September 25, 1998	10,011,592	2035-09-25
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	February 10, 2017	10,011,592	2035-09-25
Genentech, Inc.	AVASTIN	bevacizumab	Injection	125085	February 26, 2004	10,011,592	2035-09-25