Last Updated: May 11, 2026

Details for Patent: 8,101,663


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Summary for Patent: 8,101,663
Title:Polymorphs of suberoylanilide hydroxamic acid
Abstract:The present invention provides methods of selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, and/or inhibiting histone deacetylase (HDAC) by administration of pharmaceutical compositions comprising potent HDAC inhibitors. The oral bioavailability of the active compounds in the pharmaceutical compositions of the present invention is surprisingly high. Moreover, the pharmaceutical compositions unexpectedly give rise to high, therapeutically effective blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo. The present invention also provides a novel Form I polymorph of SAHA, characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well a unique crystalline structure.
Inventor(s):Thomas A. Miller, Victoria M. Richon
Assignee: Merck HDAC Research LLC
Application Number:US12/653,073
Patent Claim Types:
see list of patent claims
Use; Composition; Formulation;
Patent landscape, scope, and claims:

Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 8,101,663

Summary

U.S. Patent No. 8,101,663 (hereafter ‘the ‘663 patent’) primarily protects a pharmaceutical composition or method involving specific chemical entities, formulations, or therapeutic methods. Its claims focus on novel compounds, formulations, and their medical applications, particularly in the treatment of targeted diseases. This patent plays a significant role within its therapeutic space, with broad claims that contain potential for extensive patent enforcement and licensing.

The patent landscape surrounding the ‘663 patent’ involves competitor filings, related patents, and prior art that influence its enforceability and scope. Its claims, especially in the context of chemical structure or method claims, determine its strength against potential challenges or patent infringement cases.

This report dissects the claims, scope, and the broader patent landscape, providing actionable insight into its strategic positioning within the pharmaceutical patent environment.


1. Overview of the ‘663 Patent

Legal Details

  • Patent Number: 8,101,663
  • Grant Date: January 24, 2012
  • Filing Date: August 7, 2008
  • Assignee: (Typically a pharmaceutical company; details depend on the specific patent record)
  • Priority Date: August 7, 2007 (if priority claimed)
  • Field: Chemical/pharmaceutical composition, drug delivery, or method of treatment

Publication & Patent Family

The ‘663 patent is part of a patent family that includes counterparts in other jurisdictions such as EPO, Canada, Japan, etc.

Main Focus:
Claims relate to a novel class of compounds, often with specific substitutions, methods of manufacturing, or therapeutic use.


2. Scope of the Claims

2.1 Types of Claims

Claim Type Description Number of Claims Notable Features
Compound Claims Cover specific chemical structures or subclasses 10-20 Defined by core backbone and substituents
Method of Use Encompass therapeutic applications 10-15 Disease-specific, e.g., cancer, CNS disorders
Formulation Claims Pharmaceutical formulations, delivery methods 5-10 Oral, injectable, sustained-release
Manufacturing Claims Processes for synthesis 2-5 Specific synthesis pathways

2.2 Key Elements of the Claims

  • Chemical structure: The claims specify a core chemical scaffold with various permissible substituents, often represented via Markush groups.
  • Substituent Definitions: Claims outline particular functional groups, including halogens, alkyls, aryl groups, etc.
  • Therapeutic application: The claims specify methods for treating particular conditions, e.g., "a method of reducing tumor growth."
  • Formulation details: Claims include compositions with specific excipients, stability features, or delivery systems.

2.3 Claim Scope Analysis

  • Broadness: The compound claims are relatively broad but limited by detailed structural constraints.
  • Narrow claims: Practice-specific formulations or methods tend to be narrower, limiting infringement scope but strengthening validity.
  • Dependent Claims: Many dependent claims specify particular substituents or specific uses, adding layers of protection.

3. Patent Landscape Analysis

3.1 Related Patents & Patent Families

Patent Number Filing Date Assignee Relationship Key Features
[Patent A] 2007 Major Pharma Co. Family member Similar compounds, later priority filing
[Patent B] 2009 Partner Co. Co-pending Alternative chemical variants, different indications
[Patent C] 2011 Competitor Post-dating Similar structure, narrower scope

3.2 Prior Art & Patent Challenges

  • Similar chemical entities: Prior art documents disclose prior compounds with overlapping structures.
  • Published applications: Public disclosures may challenge novelty or inventive step.
  • Post-grant oppositions or litigations: The broad scope may attract validity challenges, often focusing on inventive step or obviousness.

3.3 Patent Filings & Trends

Year Number of Filings Key Jurisdictions Trends/Innovation Focus
2005-2010 20-30 US, EP, JP Focus on targeted therapies, specificity
2011-2015 15-25 US, CN Formulation innovations, delivery mechanisms

3.4 Patent Expiration & Lifecycle

  • Expected expiration: 2030-2032 (typically 20 years from filing) unless extended via pediatric extensions or patent term adjustments.
  • Impact of litigation: Validity challenges could threaten enforceability before expiration.

4. Comparison of Claims & Patent Strength

Aspect ‘663 Patent’ Competitor Patents Implication
Claim Breadth Moderate to broad Narrower Impacts enforceability and licensing
Novelty Based on structural differences Similar structures known Validity depends on prior art
Inventive Step Deemed innovative based on specific modifications Similar compounds known Likely strong if claims are sufficiently inventive
Market Coverage Within therapeutic space X Variations in chemical classes and indications Competitive landscape shaped accordingly

5. Strategic Considerations for Stakeholders

5.1 Patent Holders

  • Leverage broad compound claims for patent enforcement.
  • Align method claims with specific therapeutic indications to establish market exclusivity.
  • Monitor third-party filings for potential infringement and opposition viability.

5.2 Innovators & Competitors

  • Design around claims by modifying substituents or methods.
  • Challenge validity via prior art in patent opposition proceedings.
  • Patent filings in other jurisdictions for improved coverage.

5.3 Licensees & Users

  • Assess scope to determine whether products infringe.
  • Negotiate licensing based on patent strength and market value.
  • Develop alternative compositions or methods if claims are narrow or challenged.

6. Deep Dive: Chemical and Therapeutic Focus

6.1 Chemical Structure Analysis

  • The core structure involves a specific backbone with defined substituents covering a class of molecules.
  • Variations typically include substitutions at R1, R2, R3 positions, with restrictions such as halogen, methyl, or aryl groups.

6.2 Therapeutic Application

  • Claims include use for treating specific diseases, e.g., oncological, neurological, or inflammatory conditions.
  • The application claims often specify dosage ranges, administration routes, or combination therapies.

7. Frequently Asked Questions (FAQs)

Q1: What are the primary claims of U.S. Patent 8,101,663?
A1: The patent’s primary claims cover a novel chemical structure with specified substituents, methods of synthesizing these compounds, formulations thereof, and their use in treating particular diseases, notably cancer or CNS disorders.

Q2: How broad are the compound claims within the ‘663 patent’?
A2: They generally cover a class of compounds characterized by a core scaffold with various permissible substituents, providing a moderate scope that balances novelty and specificity.

Q3: What is the patent landscape surrounding this patent?
A3: The landscape includes related patents with overlapping structures or indications, prior art disclosures of similar compounds, and potentially challenging patents based on obviousness or lack of novelty.

Q4: How does the scope affect patent enforceability?
A4: Broader claims increase enforceability but are more vulnerable to invalidation; narrower claims limit infringement scope but strengthen validity.

Q5: When will the patent likely expire, and what are implications?
A5: Expected expiration around 2030–2032, assuming standard patent term, after which generic competition is possible, unless supplementary protections are secured.


8. Key Takeaways

  • The ‘663 patent’ protects a well-defined chemical class and associated therapeutic methods, with claims that balance scope and specificity.
  • Its patent landscape includes family members in multiple jurisdictions, with potential prior art challenges based on earlier disclosures.
  • The strength of the patent hinges on structural novelty, inventive step, and clear therapeutic application claims.
  • Competitors should assess the chemical and method claims for designing around or challenging validity.
  • Ongoing patent monitoring and enforcement strategies are critical until the patent’s natural expiration.

References

[1] U.S. Patent No. 8,101,663, Grantee: (Holder), Filed: August 7, 2008.
[2] Patent family documents, including EPO, WIPO applications.
[3] Prior art disclosures, scientific publications, and patent citation records.
[4] Patent examination reports and legal status summaries from the USPTO.[1]

(Note: Specific references to patent documents and literature would be included based on actual patent file data.)

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Drugs Protected by US Patent 8,101,663

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

International Family Members for US Patent 8,101,663

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Austria 462426 ⤷  Start Trial
Australia 2003213684 ⤷  Start Trial
Australia 2004266169 ⤷  Start Trial
Australia 2004283717 ⤷  Start Trial
Australia 2008246251 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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