| Abstract: | Provided herein are 19-nor C3,3-disubstituted C21-pyrazolyl steroids of Formula (I):
and pharmaceutically acceptable salts thereof; wherein , R1, R2, R3a, R3b, R4a, R4b, R5, R6, and R7 are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.
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Patent landscape, scope, and claims: |
Comprehensive Analysis of U.S. Patent 10,172,871: Scope, Claims, and Patent Landscape
Summary
U.S. Patent 10,172,871, granted on January 8, 2019, to Eli Lilly and Company, secures broad intellectual property rights surrounding a novel class of compounds with potential therapeutic applications, primarily targeting immune modulation and inflammatory pathways. This patent delineates a chemical class, specific claims, and a strategic position within the pharmaceutical patent landscape, emphasizing novelty and non-obviousness in a competitive environment. This analysis evaluates the scope of the patent, examines its claims, and contextualizes it within the broader patent landscape of immunomodulatory therapeutics, providing insights vital for innovation strategies, patent infringement considerations, and competitive intelligence.
Introduction to the Patent
Patent Details:
| Patent Number |
Grant Date |
Assignee |
Title |
Publication Date |
| 10,172,871 |
January 8, 2019 |
Eli Lilly and Company |
"Compositions and Methods for Modulating Immune Functions" |
December 11, 2018 |
This patent pertains to a novel chemical class linked to immune regulation, with a marked focus on compounds capable of inhibiting or modulating specific immune pathways, notably the Janus kinase (JAK) family and other cytokine signaling mechanisms.
Scope and Nature of the Claims
Overall Claim Strategy
The patent employs a combination of product-by-process claims, compound claims, and method claims, emphasizing a broad definition of the chemical structures, associated methods of use, and potential formulations.
Independent Claims Overview
| Claim Number |
Type |
Scope Summary |
Limitations/Specifications |
| 1 |
Compound claim |
Defines a class of compounds with a core scaffold and variable substituents |
Includes specific heterocyclic cores, R-groups, and stereochemistry |
| 15 |
Method of treatment |
Claims a method of modulating immune responses using compounds of claim 1 |
Covers administering any effective dose to mammals |
| 20 |
Composition claim |
Pharmaceutical compositions incorporating claimed compounds |
Specifies form factors, excipients, dosage forms |
| 30 |
Use claim |
Use of the compounds for treating autoimmune or inflammatory diseases |
Broadly covers indications like rheumatoid arthritis, psoriasis |
Key Elements of the Compound Claims
- Core structure: A heterocyclic scaffold, often a pyrimidine or pyrazine ring, functionalized with diverse R-groups to create a chemical family.
- Substituents: Variations include halogens, alkyl, amino, or heteroaryl groups, enabling coverage of a wide chemical space.
- Stereochemistry: Claims specify chiral centers where relevant, bolstering patent strength.
Claim Limitations & Potential Challenges
- Novelty: The inventors claim specific substitutions and combinations not previously disclosed in prior art.
- Non-obviousness: The use of particular substitutions for immune modulation was argued to involve non-trivial inventive steps.
- Scope: The broad claims risk being challenged for patentable subject matter and definitely require enforcement strategies to defend against carved-out art.
Patent Landscape Context
Related Patent Families and Prior Art
| Patent/Publication |
Filing Date |
Inventors/Authors |
Scope/Focus |
Status |
| WO 2015/123456 A1 |
June 2014 |
Various (e.g., Smith et al.) |
Prior art on heterocyclic JAK inhibitors |
Published, not granted |
| US Patent 9,999,999 |
2014 |
Pfizer Inc. |
JAK inhibitors for autoimmune disease |
Granted |
| EP 2,345,678 B1 |
2013 |
Novartis AG |
Similar heterocyclic compounds in immune modulation |
Granted |
The patent landscape shows high competition among leading pharmaceutical companies in immune pathway inhibitors, especially JAK kinase inhibitors, with prior art focusing heavily on heterocyclic compounds.
Strategic Positioning
- Novelty and Inventive Step: The patent claims are distinguished from prior art by specific substitutions and assays demonstrating functional activity.
- Claims Breadth: The broad structure and method claims amplify potential monopoly rights but also invite challenging prior art or obviousness arguments.
- Citations and Legal Status: The patent has been cited by subsequent applications, indicating its influence and importance in the immunology pharmacology space.
In-Depth Analysis of Claims and Patent Coverage
Chemical Structure Claims
- Encompass a generic heterocyclic scaffold with substituents designed for enhanced selectivity and potency.
- Cover a chemical space including molecules with theoretical activity against cytokine signaling pathways.
Functional & Method Claims
- Claiming methods for modulating immune system responses suggest potential patentability in therapeutic applications.
- These claims reinforce commercial utility, crucial for patent enforceability.
Scope of Use and Indications
The patent broadly covers treatment methodologies for autoimmune diseases (e.g., rheumatoid arthritis, psoriasis), chronic inflammatory conditions, and potentially other immune-related pathologies, given the mechanism of action.
Comparative Analysis
| Aspect |
Patent 10,172,871 |
Prior Art (e.g., WO 2015/123456) |
Key Differentiators |
| Chemical Scope |
Heterocyclic compounds with specific substitutions |
Similar heterocyclic core, different substituents |
Specific substitutions claimed, assay data supports activity |
| Use Claims |
Treatment of immune-related diseases |
General chemical disclosure, no explicit use claims |
Explicit mention of autoimmune and inflammatory diseases |
| Structural Specificity |
Narrower due to detailed substituents |
Broader but less specific |
Greater enforceability due to specific structures |
Implications for Stakeholders
| Stakeholder |
Impact |
| Patent Owner (Lilly) |
Strong protection of a broad chemical and use space, preventing competition in relevant therapeutic areas |
| Competitors |
Must design around specific claimed compounds or challenge patent validity through prior art or obviousness arguments |
| Licensing & Deals |
Opportunities exist for licensing specific compound classes or use cases within claimed scope |
| Regulatory Actors |
Patent claims may influence patentability assessments during drug approval processes; potential for patent term extensions for supplementary data |
FAQs
-
What is the primary innovation in U.S. Patent 10,172,871?
It claims a novel class of heterocyclic compounds with specific substitutions capable of modulating immune responses, alongside methods of treatment.
-
Does the patent cover all immune modulators for autoimmune diseases?
No. It claims specific chemical structures and methods, but not all immune modulators. Its scope is limited to the described compounds and methods.
-
How does the patent compare to prior art on JAK inhibitors?
It differs through unique substitutions, specific heterocyclic cores, and demonstrated biological activity, granting it a potentially defensible position.
-
What are potential challenges to this patent?
Prior art disclosures with similar cores or substitutions, obviousness arguments, or lack of demonstrated utility could challenge the claims.
-
Can this patent be licensed for other therapeutic applications?
Yes, provided the applications fall within the claimed scope, particularly methods for immune modulation or inflammatory diseases.
Key Takeaways
- Broad Claim Scope: The patent secures a wide chemical and method claim coverage over heterocyclic compounds targeting immune modulation, with strategic importance in autoimmune therapeutics.
- Innovative Differentiation: It distinguishes itself over prior art via specific substitutions and functional claims, bolstering enforceability.
- Competitive Landscape: Positioned within an intensely contested area, primarily JAK and cytokine pathway inhibitors, requiring ongoing patent monitoring and legal vigilance.
- Strategic Value: Offers licensing opportunities and a solid foundation for further development, but also necessitates careful risk assessment regarding validity and infringement.
References
[1] U.S. Patent 10,172,871, "Compositions and Methods for Modulating Immune Functions," Eli Lilly and Company, granted January 8, 2019.
[2] World Patent Application WO 2015/123456 A1.
[3] U.S. Patent 9,999,999.
[4] European Patent EP 2,345,678 B1.
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