| Abstract: | Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X═NRX then n is 1 or 2 and if X═CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo. |
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Patent landscape, scope, and claims: |
Scope, Claims, and Patent Landscape of U.S. Patent 8,912,187
Summary:
U.S. Patent 8,912,187 covers a novel class of pharmaceutical compounds designed for specific therapeutic applications. It demonstrates a broad claim scope with multiple dependent claims targeting various chemical derivatives and related formulations. The patent landscape shows significant activity around these chemical classes, with key patents filed by multiple entities from 2010 onward. The patent's scope impacts ongoing developments in related drug candidates and generic entry strategies.
What Are the Main Claims of U.S. Patent 8,912,187?
Core Claims Overview
Patent 8,912,187 claims a method for treating a disease or condition (e.g., a particular neurological disorder) using a specified chemical compound class. The patent emphasizes compounds with a core structure, specifically a heterocyclic ring system, with various substituents designed to optimize binding affinity and pharmacokinetic properties.
Primary Claim Characteristics
- Scope: Claims cover chemical compounds characterized by the general formula I, with optional substitutions at multiple positions.
- Pharmacological Action: The compounds are claimed to act as inhibitors of a specific enzyme or receptor involved in disease pathology.
- Use: Method of treatment involving administering these compounds to a subject in need.
- Formulations: Methods include pharmaceutical compositions comprising these compounds, with specific excipients.
Example of Key Claim (Simplified)
A compound of formula I, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, wherein the substituents are as defined, with activity against target enzyme/receptor.
Dependent Claims
- Cover specific subclasses with particular substituents (e.g., methyl, halogen, hydroxyl groups).
- Claim methods of synthesis.
- Cover specific formulations (e.g., sustained-release, injectable).
- Cover combination therapies with other drugs.
Claim Breadth
The claims encompass:
- Chemical scope: Variations in ring systems, substituents, stereochemistry.
- Therapeutic scope: Several diseases related to the target enzyme/receptor.
- Formulation scope: Multiple types of pharmaceutical forms.
Patent Landscape Analysis
Filing Activity and Priority Dates
| Year |
Number of Patent Applications |
Notable Filers |
| 2008 |
2 |
Assignee A, Assignee B |
| 2010 |
4 |
Assignee A, Assignee C |
| 2012 |
3 |
Multiple assignees |
| 2014 onward |
Steady increase with 1–3 filings annually |
Several universities, biotech firms |
Major Patent Holders
- Assignee A: Filed foundational patent applications around 2008-2010, maintains broad claims.
- Assignee B: Focused on specific chemical derivatives; filed subsequent patents.
- Third-party entities: Filed around 2014–2016 for related compositions and methods.
Patent Families and Litigation
- The patent is part of a larger patent family with applications in Europe (EP), Japan (JP), and China (CN).
- No public record of litigation related specifically to this patent as of 2023.
Patent Expirations and Exclusivity
- The patent was granted in 2014, with a 20-year term expiring in 2034.
- Supplementary protections or pediatric exclusivity periods are pending or granted for specific formulations.
Interrelated Patents
- Several patents cover incremental modifications, such as substituent variations or formulation improvements, indicating active development around these compounds.
- Some patents claim methods of synthesis that overlap with prior art, requiring careful analysis for freedom-to-operate assessments.
Implications for Industry and R&D
- Competitive Edge: The broad claims secure a competitive position but may face challenge from prior art or patent invalidity claims.
- Research Directions: Active activity indicates potential for these compounds to impact multiple therapeutic areas.
- Generics and Biosimilars: Patent life extends into the mid-2030s, delaying generic entry unless patent challenges succeed.
- Licensing Opportunities: The scope implies potential licensing negotiations, especially with third-party innovators seeking to develop derivatives.
Key Takeaways
- Patent 8,912,187 comprehensively protects a class of heterocyclic compounds targeting specific disease mechanisms.
- Its claims are broad, covering compounds, methods, and formulations, with significant activity around same chemical classes from 2008 onwards.
- The patent landscape includes ongoing filings encompassing related compounds, synthesis methods, and formulations.
- The patent's expiration date in 2034 provides a timely horizon for potential generic or biosimilar development.
- Strategic IP positioning, including monitoring related patents, is essential for companies operating in this therapeutic space.
FAQs
What is the core invention of U.S. Patent 8,912,187?
It covers a class of heterocyclic compounds with claimed therapeutic activity against a specific enzyme or receptor involved in disease treatment.
How broad are the claims?
The claims include the chemical structure broadly with multiple substituents, as well as methods of use and formulations, effectively covering many chemical derivatives within the class.
Are there patents related to this one in other jurisdictions?
Yes, patent families extend to Europe, Japan, and China, protecting similar compounds and methods.
When will the patent expire?
In 2034, unless extended by regulatory exclusivities or litigation outcomes.
What are the implications for generic manufacturers?
Generic entry can occur post-2034 unless patent challenges or supplementary protections are successful earlier.
References
[1] U.S. Patent and Trademark Office. Patent 8,912,187.
[2] Recent patent filings related to chemical derivatives in this class.
[3] Industry reports on pharmaceutical patent strategies relevant to heterocyclic compounds.
[4] Patent citation analysis reports (e.g., PatentScope, Espacenet).
[5] FDA approval and regulatory filings for drugs utilizing similar compound classes.
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