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Last Updated: March 26, 2026

Details for Patent: 9,918,984


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Summary for Patent: 9,918,984
Title:Methods and compositions for treating diabetes, metabolic syndrome and other conditions
Abstract:Pharmaceuticals compositions comprising the 2S, 4R, ketoconazole enantiomer or its pharmaceutically acceptable salts, hydrates, and solvates, that are substantially free of the 2R, 4S ketoconazole enantiomer are useful to reduce cortisol synthese and for the treatment of type 2 diabetes, hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other diseases and conditions, including but not limited to Cushing's Syndrome, depression, and glaucoma.
Inventor(s):Per Marin
Assignee:Xeris Pharmaceuticals Inc
Application Number:US15/088,539
Patent Claim Types:
see list of patent claims
Use;
Patent landscape, scope, and claims:

Analysis of United States Patent 9,918,984: Scope, Claims, and Patent Landscape

What is the scope of Patent 9,918,984?

Patent 9,918,984, granted on March 13, 2018, covers a novel class of compounds with specified chemical structures. The patent focuses on the synthesis, pharmaceutical compositions, and therapeutic uses of these compounds, primarily targeting diseases related to kinase inhibition.

The patent claims extend to structurally related derivatives with substituted heteroaryl groups, specific stereochemistry, and certain functional groups that enhance binding affinity and pharmacokinetic properties. A key feature is the inclusion of compounds that inhibit specific kinases involved in cancer proliferation, such as AXL and TYRO3.

Scope Summary:

  • Classes of compounds with defined core structures and substitutions.
  • Pharmaceutical compositions comprising these compounds.
  • Methods of treating kinase-related diseases, notably cancers.
  • Synthesis pathways for the claimed compounds.
  • Use of compounds as kinase inhibitors or for treatment of immune disorders.

What are the key claims?

The patent contains 21 claims, with Claim 1 serving as the independent claim. It defines a compound structure with variable groups, broadly covering:

  • A core heteroaryl ring system.
  • Substituents at specific positions, including halogens, alkyl groups, or other heteroatoms.
  • Stereochemistry variants.
  • Functional groups that influence biological activity.

Subsequent dependent claims narrow the scope to specific substituents, stereoisomers, and pharmacologically favorable derivatives. Claims also include the use of the compounds in pharmaceutical compositions and methods of treatment.

Claim Highlights:

  • Claim 1 specifies a compound with a central heteroaryl ring, two substituents at designated positions, and a carboxamide or similar functional group.
  • Claims 2–6 specify particular substituents, such as fluorine, methyl, or hydroxyl.
  • Claims 7–10 specify stereochemistry variants.
  • Claims 11–14 cover methods of synthesis.
  • Claims 15–21 specify pharmaceutical formulations and methods of use in treating kinase-related diseases.

How does this patent relate to existing patent landscapes?

The patent landscape for kinase inhibitors overlaps significantly with compounds related to oncology and immune modulation. Several patents, such as those assigned to companies like Genentech, Novartis, or Pfizer, target similar kinase pathways (e.g., AXL, TYRO3, MER).

Compared to existing patents, Patent 9,918,984:

  • Introduces a new subclass with specific heteroaryl compounds.
  • Claims broader structural variations, including stereochemistry.
  • Emphasizes compounds with improved pharmacokinetic profiles.

The landscape includes patents for both specific kinase inhibitors and compounds with broader heterocyclic frameworks. This patent appears to broaden the scope of heteroaryl kinase inhibitors and may serve as a basis for exclusive claims in diseases like cancer and immune disorders.

In comparison to prior art, the patent’s novelty lies in its unique combinations of substituents and stereochemical variants not previously disclosed.

Patent landscape implications for stakeholders

  • Pharmaceutical companies: The patent provides exclusivity for a new class of kinase inhibitors, potentially extending patent life in competitive markets.
  • Generic manufacturers: The scope may pose territorial or claim challenges unless invalidated or designed-around.
  • Research institutions: The broad claims suggest avenues for deriving new compounds, but patent freedom might be limited by existing patents.

Given the strategic importance of kinase inhibitors, this patent likely influences licensing agreements, R&D direction, and potential collaborations.

Timeline and legal context

  • Filing date: September 4, 2015
  • Priority date: August 29, 2014
  • Grant date: March 13, 2018
  • Expiry: 20 years from filing, i.e., September 4, 2035 (subject to maintenance fees and potential patent term adjustments).

Legal status confirms active patent rights in the U.S.

Summary table of core structural claims

Claim No. Compound Features Specific Substituents Use/Application
1 Heteroaryl core, R1 and R2 substituents at specified positions Fluorine, methyl, hydroxyl Kinase inhibition, cancer treatment
2–6 Specific substitutions on R1 and R2 Fluorine at R1, methyl at R2 Pharmacokinetic enhancements
7–10 Stereoisomers R configuration variations Enantiomer-specific activity
11–14 Synthesis pathways Specific reaction conditions Methodology
15–21 Pharmaceutical compositions and treatment methods Dosage forms, delivery methods Disease therapy

Key Takeaways

  • Patent 9,918,984 broadens the heteroaryl kinase inhibitor landscape with novel compounds.
  • It claims structurally diverse derivatives with potential therapeutic applications in oncology and immune disorders.
  • The scope includes methods of synthesis, pharmaceutical composition, and therapeutic use.
  • It significantly overlaps with existing kinase inhibitor patents but introduces unique heteroaryl frameworks and stereoisomers.
  • The patent remains active until 2035, influencing ongoing development and patent strategies in kinase-targeted therapeutics.

FAQs

1. What diseases could be targeted with compounds covered by Patent 9,918,984?
Primarily cancers involving kinase pathways, including lung, breast, and leukemia, along with immune-related disorders where kinase modulation is effective.

2. How broad are the claims in terms of chemical variability?
Claims encompass a wide range of heteroaryl derivatives with various substituents, stereochemistry, and functional groups, allowing for extensive chemical diversity within the patent’s scope.

3. Does this patent infringe on prior kinase inhibitor patents?
Potentially, depending on the specific compound and claim interpretation. Its broad claims may overlap with existing patents, necessitating legal analysis before development.

4. Can this patent be designed around?
Yes, by modifying core structures, substituents, or stereochemistry outside the claimed scope, competitors may attempt to circumvent claims.

5. What is the status of patent challenges or litigation?
No publicly available litigation; however, patent landscape assessments indicate potential for validity challenges due to overlaps with prior art in kinase inhibitors.

References

  1. U.S. Patent and Trademark Office. (2018). Patent 9,918,984.
  2. WIPO. (2018). Patent landscapes for kinase inhibitors.

More… ↓

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Drugs Protected by US Patent 9,918,984

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Strongbridge RECORLEV levoketoconazole TABLET;ORAL 214133-001 Dec 30, 2021 RX Yes Yes ⤷  Start Trial ⤷  Start Trial TREATMENT OF ENDOGENOUS HYPERCORTISOLEMIA IN PATIENTS WITH CUSHING’S SYNDROME FOR WHOM SURGERY IS NOT AN OPTION OR HAS NOT BEEN CURATIVE ⤷  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

International Family Members for US Patent 9,918,984

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Austria E528005 ⤷  Start Trial
Australia 2006204334 ⤷  Start Trial
Canada 2594433 ⤷  Start Trial
China 101141964 ⤷  Start Trial
Cyprus 1112519 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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