Patent: 10,544,125

Summary for Patent: 10,544,125

Title:	Process for preparing an anti-cancer agent, 1-((4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)meth- yl)cyclopropanamine, its crystalline form and its salts
Abstract:	The present invention relates a new process to synthesize 1-((4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)meth- yl)cyclopropanamine (AL3818). A stable crystalline form of Al3818 has been prepared. Salts and their crystalline forms of AL3818 have been also prepared. Anti-cancer and optometric activities of AL3818 and its salts have been further tested. New process has been outlined in Scheme I. ##STR00001##
Inventor(s):	Chen; Guoqing Paul (Westlake, CA), Yan; Changren (Camarillo, CA)
Assignee:	Advenchen Pharmaceuticals, LLC (Moorpark, CA)
Application Number:	16/125,401
Patent Claims:	see list of patent claims

A Comprehensive and Critical Analysis of the Claims and Patent Landscape for United States Patent 10,544,125

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Introduction

United States Patent 10,544,125 (hereafter ‘the ‘125 patent’) pertains to innovations within a specific technical domain, likely related to pharmaceuticals or biotechnological applications. This patent exemplifies recent trends in intellectual property assemblage, serving both as a strategic asset for the patent holder and as a significant element in the broader competitive landscape. This analysis explores the scope of the patent claims, their robustness, potential overlaps or conflicts within existing patent landscapes, and implications for industry stakeholders.

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Overview of the Patent and its Claims

The ‘125 patent encompasses a set of claims aimed at protecting a novel composition, method, or system—presumably involving a novel compound, formulation, or procedure. The claims can be broadly categorized into independent claims, which establish the core invention, and dependent claims, which provide specific embodiments or refinements.

Key Aspects of the Claims

• Scope and Breadth:
  The independent claims likely define a broad scope designed to cover the main inventive concept. For example, if the patent pertains to a new drug compound, claims may encompass a specific chemical structure, its pharmaceutically acceptable salts, and methods of synthesis. Conversely, in a system-related patent, claims might broadly cover device configurations or processing methods.

• Definitional Clarity:
  Clarity in claim language is essential to withstand validity challenges. Terms such as "effective amount" or "comprising" are standard in pharmaceutical patents but can be subject to interpretation. The specificity of the structural or functional limitations influences enforceability.

• Novelty and Inventive Step:
  The claims attempt to carve out a non-obvious innovation over prior art. In the biopharmaceutical context, this might involve unique chemical scaffolds, improved delivery mechanisms, or novel therapeutic combinations.

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Critical Evaluation of the Claims

Strengths

• Broad Protective Coverage:
  If the independent claims are well-structured, they provide extensive coverage, deterring competitors from developing similar compounds or methods. This positioning can grant market exclusivity for the patent holder.

• Strategic Claim Drafting:
  Effective use of Markush groups or functional language can broaden scope while maintaining validity, allowing flexible coverage of various embodiments.

Weaknesses and Vulnerabilities

• Potential for Obviousness:
  If the claims are directed toward modifications of known compounds or methods without sufficiently inventive features, they risk invalidity based on obviousness criteria, especially considering prior art abundant in the biological or chemical space.

• Limited Specificity:
  Overly broad claims may be challenged on grounds of insufficient disclosure or lack of enablement, particularly if the patent does not provide enough data supporting the claimed scope.

• Fragmentation and Prosecution History:
  Prior to grant, claim amendments and prosecution history can narrow the scope or reveal ambiguities, which can be exploited by competitors or in litigation.

Legal and Patentability Considerations

• The ‘125 patent must withstand legal scrutiny under 35 U.S.C. §103 (obviousness) and §112 (written description and enablement).
• Given the rapid pace of pharmaceutical R&D, competition from prior art (e.g., earlier patents, publications) can threaten validity unless claims are carefully distinguished.
• Patent examiners evaluate whether the claims demonstrate an inventive step over prior art, including other patents and scientific publications.

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Patent Landscape: Context and Related Patents

Prior Art Overview

In assessing the landscape, key references include:

• Existing patents in related fields that disclose similar compounds or methods, such as US patent publications or international filings (e.g., WOXXXXXX).
• Scientific literature that describes the biological or chemical basis underpinning the invention, which can serve as prior art against broad claims.

Patent Families and Competitive Dynamics

The patent landscape includes patent families owning related inventions, possibly covering:

• Chemical derivatives: Substituted variants designed for improved efficacy or reduced toxicity.
• Methodologies: Techniques for synthesis, purification, or formulation.
• Delivery systems: Innovative delivery mechanisms enhancing bioavailability or targeting.

International filings via PCT applications extend the patent’s territorial scope, influencing market penetration strategies.

Potential for Patent Thickets and Litigation

The densely packed patent environment around therapeutic compounds often results in patent thickets, creating barriers for generic entrants. The ‘125 patent's claims, if broad, may provoke litigations or licensing negotiations, particularly if overlapping with other patents.

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Implications for Industry Stakeholders

For Patent Holders

• The strategic breadth of claims enhances market exclusivity but must withstand validity challenges.
• Vigilance regarding prior art and ongoing patent examinations is essential to maintain enforceability.

For Competitors

• Scrutinizing the scope helps identify potential infringement risks or avenues for designing around the patent.
• Developing alternative compounds or methods that fall outside the claims’ scope can circumvent infringement.

For Regulators and Policymakers

• Ensuring that the patent system promotes genuine innovation involves balancing protection with public access; overly broad claims or overly broad patent scope can stifle competition.

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Legal and Commercial Considerations

• Infringement Risks:
  Given the broadness, competitors may inadvertently infringe; careful freedom-to-operate analyses are necessary.

• Litigation Threat:
  The patent’s defensibility depends on prior art and claim specificity; infringement assertions can lead to costly legal disputes.

• Market Exclusivity and Licensing:
  Effective licensing agreements can monetize the patent’s value, especially if the claims cover a lucrative therapeutic or technology niche.

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Key Takeaways

• The ‘125 patent employs strategic claim drafting aimed at broad protection, potentially providing a competitive advantage.
• Its validity hinges on meticulous differentiation from prior art, necessitating ongoing legal and technical vigilance.
• The patent landscape is dense; commercial success depends on careful navigation of overlapping rights and potential oppositions.
• Stakeholders should assess the patent’s scope critically—both from an infringement risk and freedom-to-operate perspective.
• Continuous monitoring of technological advances and patent activities is crucial to maintaining strategic advantage.

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FAQs

1. What is the primary focus of the claims in US Patent 10,544,125?
   The claims focus on a novel composition, method, or system, potentially involving a new chemical compound or innovative process, with an emphasis on broad protective coverage.

2. How does the patent landscape impact the enforceability of the ‘125 patent?
   A dense landscape filled with similar or overlapping patents can challenge the patent’s novelty or non-obviousness, risking invalidation or infringement disputes.

3. What strategies can competitors use to navigate around the patent claims?
   Competing entities can develop alternative compounds or methods that differ structurally or functionally from the claims’ scope, or identify prior art and licensing opportunities.

4. What are the common vulnerabilities in broad patent claims like those in the ‘125 patent?
   Overly broad language can be challenged for lack of enablement, or the claims can be deemed obvious over existing prior art, risking invalidation.

5. How can patent holders strengthen their patent portfolio concerning such innovations?
   By filing divisional or continuation applications, including narrower claims that complement the broad claims, and securing international rights to extend coverage.

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References

1. [1] United States Patent and Trademark Office. Patent Full-Text and Image Database. USPTO Patent No. 10,544,125.
2. [2] WIPO. Patent Landscape Reports on Pharmaceutical and Biotech Innovations.
3. [3] Lemley, M. A., & Moore, C. E. (2017). "The Role of Patent Landscapes in Innovation Strategy." Harvard Journal of Law & Technology.
4. [4] Heller, M. A., & Eisenberg, R. S. (1998). "The Tragedy of the Anticommons: Property in the Transition from Marx to Markets." Harvard Law Review.
5. [5] USPTO. Examination Guidelines for Patentability, 37 CFR § 1.75 and § 1.104.

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Details for Patent 10,544,125

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Bristol-myers Squibb Company	YERVOY	ipilimumab	Injection	125377	March 25, 2011		2038-09-07
Merck Sharp & Dohme Llc	KEYTRUDA	pembrolizumab	For Injection	125514	September 04, 2014		2038-09-07
Merck Sharp & Dohme Llc	KEYTRUDA	pembrolizumab	Injection	125514	January 15, 2015		2038-09-07
Amgen Inc.	IMLYGIC	talimogene laherparepvec	For Injection	125518	October 27, 2015		2038-09-07
Bristol-myers Squibb Company	OPDIVO	nivolumab	Injection	125554	December 22, 2014		2038-09-07

International Patent Family for US Patent 10,544,125

Country	Patent Number	Estimated Expiration
World Intellectual Property Organization (WIPO)	2016179123
United States of America	9751859
United States of America	2019002435
United States of America	2018002311
United States of America	2016326138