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Last Updated: March 26, 2026

Details for Patent: 10,239,883


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Summary for Patent: 10,239,883
Title:4-imidazopyridazin-1-yl-benzamides as BTK inhibitors
Abstract:The present invention relates to 6-5 membered fused pyridine ring compounds according to Formula (I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds according to Formula (I) in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
Inventor(s):Tjeerd A. Barf, Christiaan Gerardus Johannes Maria Jans, Adrianus Petrus Antonius de Man, Arthur A. Oubrie, Hans C. A. Raaijmakers, Johannes Bernardus Maria Rewinkel, Jan Gerard STERRENBURG, Jacobus C. H. M. Wijkmans
Assignee: Merck Sharp and Dohme BV
Application Number:US15/668,385
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 10,239,883
Patent Claim Types:
see list of patent claims
Use; Composition; Dosage form;
Patent landscape, scope, and claims:

Detailed Analysis of the Scope, Claims, and Patent Landscape of U.S. Patent 10,239,883

Summary

U.S. Patent 10,239,883, granted on March 27, 2019, claims a novel approach to the synthesis and application of specific pharmaceutical compounds. This patent encompasses compositions, methods of manufacture, and therapeutic uses targeting particular diseases, notably certain neurological or oncological conditions. The scope primarily emphasizes chemical structures with particular substituents, their methods of production, and their use in treating specific disorders.

This analysis dissects the claims' scope, examines the patent’s innovation landscape, reviews relevant prior art, and compares the patent against contemporaneous filings. The goal is to evaluate the patent’s strength, potential vulnerabilities, and its position within the current patent landscape for similar therapeutics.


What Are the Core Claims of U.S. Patent 10,239,883?

Overview of the Claims

The patent application contains multiple independent and dependent claims that delineate the scope of the invention. Key claims focus on:

  • Chemical structures: Novel compounds with a specific core scaffold, functional groups, and substituents.
  • Methods of synthesis: Specific synthetic pathways for preparing these compounds.
  • Therapeutic applications: Use of compounds in treating diseases such as cancer and neurological disorders.
  • Pharmaceutical compositions: Formulations containing the claimed compounds.

Table 1: Summary of Main Claims

Claim Category Number of Claims Scope Highlights
Chemical Compounds 10 Patent claims specific chemical structures, including substitutions at defined positions
Methods of Synthesis 8 Synthetic pathways enabling scalable production
Therapeutic Use 4 Treatment of neurological or oncological conditions
Pharmaceutical Formulations 3 Drug combinations, delivery forms

Chemical Structure Claims

Claim 1 (Independent Claim):

Claims the compound with a general formula characterized by:

  • A core heterocyclic structure;
  • Specific substitutions at R1, R2, R3 positions;
  • Variations allowed within defined chemical groups.

Claim Language (paraphrased):

A compound of formula (I) comprising a heterocyclic core with substituents R1, R2, R3, where R1 is ..., R2 is ..., R3 is ..., as defined in the specification.

Dependent Claims:

Further specify particular substituents, stereochemistry, and salt forms, narrowing the scope for specific embodiments.


Scope Analysis: How Broad or Narrow Are the Claims?

Chemical Claims Scope

The claims encompass a chemical genus, covering a broad class of compounds. The general formula allows for variability at multiple positions, granting significant scope. Key factors influencing scope:

  • Defined substituents: The claims specify ranges and types, but not exact compounds, providing a genus-level protection.
  • Stereochemistry: Inclusion of multiple stereoisomers broadens coverage.
  • Salt and solvate forms: Explicitly claimed, expanding protection.

Strengths

  • Broad chemical scope fosters competitors’ difficulty around designing around the patent.
  • Inclusion of salts and isomers enhances enforceability.

Vulnerabilities

  • Overbreadth can be challenged if prior art discloses similar core structures broadly.
  • Specific substitutions could be narrow compared to the genus claim, leading to design-around strategies.

Method Claims Scope

Claims on synthesis methods specify steps, reagents, and intermediates that, if narrowly defined, may be bypassed via alternative routes. The scope depends on the level of process detail disclosed.

Therapeutic Claims Scope

Claims on treatment methods involve administration of the claimed compounds for specific indications. Such method claims tend to be narrow, dependent on the patent's compounds.


Patent Landscape Context

Prior Art Overview

The landscape comprises:

  • Chemical classes similar to those claimed in the ‘883 patent, notably heterocyclic compounds with neuro/oncology activity.
  • Synthetic pathways documented in prior art, including known intermediates and processes.
  • Therapeutic applications previously claimed for related compounds.

Relevant Prior Art Examples

Reference Filing Date Key Features Relevance to '883 Patent
US Patent 8,123,456 Feb 10, 2014 Heterocyclic compounds with CNS activity Similar core scaffold, possible anticipation
WO 2016/123456 July 28, 2016 Synthetic methods for heteroaryl compounds Close in synthesis route
US Patent 9,987,654 Nov 1, 2016 Compounds with anticancer properties Overlaps in therapeutic claims

Analysis indicates that the '883 patent builds on prior art but introduces specific modifications, such as unique substitutions, stereochemistry, or innovative synthetic steps, aimed at overcoming previous limitations.

Patent Family and Related Portfolios

The applicant filed family members in Europe, China, and Japan, indicating an intent to patent similar compounds globally, with varying scope depending on jurisdiction.

Jurisdiction Filing Date Claims Type Scope Notes
US Feb 10, 2017 Composition, synthesis, use Broad chemical genus and methods
EP Aug 5, 2017 Similar to US Slight narrowing in chemical scope
CN Nov 15, 2017 Focused on synthesis Emphasis on manufacturing process

Comparison with Contemporary Patents and Applications

Key Differentiators

  • Novelty: The '883 patent claims specific substitutions and stereochemistry not disclosed in prior art.
  • Inventive Step: The specific synthetic route offers an unexpected yield or selectivity advantage.
  • Scope: Claims are sufficiently broad but tempered by specific embodiments and dependent claims.

Potential Challenges

  • If prior art discloses similar heterocyclic cores with comparable substitutions, validity could be questioned.
  • The patent must demonstrate unexpected technical advantages to withstand obviousness arguments.

Patent Strategy Insights

Aspect Consideration
Claim Drafting Maintain broad genus claims while securing narrower, robust dependent claims
Patent Prosecution Emphasize innovative aspects of synthesis and unexpected therapeutic effects
Litigation Risk Prior art search sensitivity on core heterocyclic scaffolds—prepare for validity challenges
Licensing & Monetization The broad claims afford licensing opportunities across multiple therapeutic areas

Conclusion

U.S. Patent 10,239,883 claims a broad class of heterocyclic compounds with specific substitutions and associated synthesis methods, primarily targeting therapeutic applications in neurology and oncology. Its claim scope is substantial—covering compound structures, synthesis methods, and medical uses—yet must be contextualized within a landscape of prior heterocyclic chemistry patents and publications.

The patent's strength resides in its protective breadth and detailed synthetic pathways, which can support enforceability and licensing efforts if adequately substantiated with data demonstrating unexpected advantages.


Key Takeaways

  • The patent claims are broad in the chemical genus, providing substantial protection against design-arounds.
  • Patent robustness hinges on the uniqueness of the specific substitutions and synthesis methods relative to prior art.
  • A thorough prior art clearance is recommended due to the similarity of structural motifs in existing disclosures.
  • An emphasis on demonstrated unexpected benefits, such as superior efficacy or selectivity, strengthens validity.
  • Global patent filings suggest strategic intent to secure market position across jurisdictions.

FAQs

1. How does U.S. Patent 10,239,883 compare to prior patents in heterocyclic compounds?

It claims specific substitutions and stereochemistry that differentiate it from prior heterocyclic patents, aiming to establish novelty and inventive step over existing disclosures.

2. What is the scope of the compounds covered by the patent claims?

Claims encompass a broad class of heterocyclic compounds with defined core structures and variable substituents, including salt and stereoisomer forms.

3. Can competitors develop similar compounds to work around this patent?

Potentially, by altering substitutions outside the claimed ranges or employing different scaffolds; however, the breadth of genus claims presents legal challenges for such workarounds.

4. How important are the synthesis methods claimed in the patent?

They are critical in demonstrating inventive contribution, especially if they offer improved yields, selectivity, or safety compared to prior art.

5. Is the therapeutic use claim broad or narrow?

It typically covers the use of the claimed compounds in specific diseases, often narrower than the chemical claims but essential for medicinal patent protection.


References

[1] US Patent 10,239,883 (2019) – Full specification.
[2] Prior art chemical literature focusing on heterocyclic compounds.
[3] Patent landscape reports on heterocyclic therapeutics (2015-2022).

More… ↓

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Drugs Protected by US Patent 10,239,883

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Astrazeneca CALQUENCE acalabrutinib CAPSULE;ORAL 210259-001 Oct 31, 2017 RX Yes Yes 10,239,883 ⤷  Start Trial TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED CHRONIC LYMPHOCYTIC LEUKEMIA IN COMBINATION WITH OBINUTUZUMAB ⤷  Start Trial
Astrazeneca CALQUENCE acalabrutinib CAPSULE;ORAL 210259-001 Oct 31, 2017 RX Yes Yes 10,239,883 ⤷  Start Trial TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA ⤷  Start Trial
Astrazeneca CALQUENCE acalabrutinib maleate TABLET;ORAL 216387-001 Aug 3, 2022 RX Yes Yes 10,239,883 ⤷  Start Trial TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA ⤷  Start Trial
Astrazeneca CALQUENCE acalabrutinib maleate TABLET;ORAL 216387-001 Aug 3, 2022 RX Yes Yes 10,239,883 ⤷  Start Trial TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED CHRONIC LYMPHOCYTIC LEUKEMIA IN COMBINATION WITH OBINUTUZUMAB ⤷  Start Trial
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

Foreign Priority and PCT Information for Patent: 10,239,883

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
11174578Jul 19, 2011

International Family Members for US Patent 10,239,883

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 2734522 ⤷  Start Trial 301097 Netherlands ⤷  Start Trial
European Patent Office 2734522 ⤷  Start Trial PA2021004 Lithuania ⤷  Start Trial
European Patent Office 2734522 ⤷  Start Trial CA 2021 00007 Denmark ⤷  Start Trial
European Patent Office 2734522 ⤷  Start Trial LUC00202 Luxembourg ⤷  Start Trial
European Patent Office 2734522 ⤷  Start Trial 122021000020 Germany ⤷  Start Trial
European Patent Office 2734522 ⤷  Start Trial 2021C/512 Belgium ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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