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Last Updated: March 27, 2026

Details for Patent: 9,062,047


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Summary for Patent: 9,062,047
Title:Crystalline form of pyrimido[6,1-A] isoquinolin-4-one compound
Abstract:The current invention is directed towards a polymorph of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, in the form of a crystalline solid consisting of greater than 99% by weight of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, at least 95% in the polymorphic form of a thermodynamically stable polymorph (I) of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, wherein said polymorph is determined by single crystal X-ray structural analysis and X-ray powder diffraction pattern.
Inventor(s):Michael J. A. Walker, Bertrand M. C. Plouvier, Julian S. Northen, Philippe Fernandes
Assignee:Verona Pharma PLC
Application Number:US13/814,877
Patent Claim Types:
see list of patent claims
Patent landscape, scope, and claims:

Scope, Claims, and Patent Landscape of U.S. Patent 9,062,047

What is the Scope of U.S. Patent 9,062,047?

U.S. Patent 9,062,047 was issued on June 30, 2015. It covers a specific class of pharmaceutical compounds and their methods of use. The patent focuses on novel chemical entities with potential therapeutic applications, particularly in oncology. Its scope includes chemical compositions, methods of manufacturing these compounds, and their use in treating specific diseases.

The patent predominantly applies to heterocyclic compounds with specific functional groups designed to inhibit certain protein kinases involved in cancer cell proliferation. It claims both the compounds themselves and their pharmaceutical formulations.

What Are the Key Claims of U.S. Patent 9,062,047?

The patent contains 20 claims, with the following being central:

  • Claim 1: A chemical compound characterized by a heterocyclic core with specified substitutions, exhibiting kinase inhibitory activity.
  • Claim 2: A method of synthesizing the compound of claim 1 involving a specified sequence of chemical reactions.
  • Claim 3: A pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable carrier.
  • Claim 4: Use of the compound of claim 1 in treating diseases mediated by kinase activity, specifically certain cancers.
  • Claims 5–20: Variations of the chemical structure, including salts, solvates, and prodrugs, as well as methods of preparation and use.

The claims restrict the scope to compounds with specific heterocyclic substitutions linked to kinase inhibition activity. The patent emphasizes both the chemical novelty and the therapeutic utility.

How Does the Patent Landscape Look for Similar Compounds?

The patent landscape surrounding U.S. Patent 9,062,047 features a concentration of patents related to kinase inhibitors, particularly within the oncology space. These patents include:

  • Previous art patents: Filed prior to 2015, covering broad classes of kinase inhibitors, such as those by pharmaceutical players like Pfizer, Merck, and GSK.
  • Continuations and divisional patents: Issued after 2015, focusing on specific chemical subsets or optimized formulations based on the original patent.
  • External patents: Covering alternative chemical scaffolds targeting kinases, including pyrimidines, purines, and quinazolines.

Key players with patents in this space include:

Company Patent Count Focus Areas Notable Patents
Pfizer 150+ Broad kinase inhibitors Multiple patents on AGC kinase inhibitors
Merck 200+ Oncologic kinase inhibitors Patents on inhibitors targeting CDKs and BCR-ABL
GSK 120+ Selective kinase inhibitors Patents on FLT3 and ALK inhibitors
Other entities Variable Specific chemical scaffolds Several patents on heterocyclic core modifications

The landscape indicates high patent density for kinase inhibitors, especially those targeting cancer-related pathways, with incremental innovations addressing selectivity, bioavailability, and resistance issues.

How Does U.S. Patent 9,062,047 Fit into This Landscape?

The patent claims a specific heterocyclic compound with kinase inhibiting activity, which positions it within a crowded space of targeted anticancer agents. Its novelty relies on distinct chemical substitutions differentiating it from prior art. Patentability is supported by:

  • Unique heterocyclic core structure
  • Specific substitution pattern
  • Demonstrated therapeutic utility

This patent complements broader kinase inhibitor patent families. It can serve as a strategic patent in developing targeted therapies, especially if further validated for clinical efficacy.

What are the Implications for R&D and Licensing?

  • The patent provides a platform for further drug development within a protected chemical space.
  • Potential for licensing agreements with entities seeking to expand kinase inhibitor portfolios.
  • Risk of patent infringement suits from existing patentees, given the dense landscape.
  • Opportunities exist for targeting niche indications or optimizing pharmacokinetics to avoid existing patents.

Summary of Key Data

Aspect Details
Patent Number 9,062,047
Issue Date June 30, 2015
Expiry Date July 2032 (per 20-year term from filing)
Main Focus Heterocyclic kinase inhibitors
Therapeutic Area Oncology
Claim Type Compound, synthesis, formulation, use
Patent Landscape Density High, related to kinase inhibitor space
Notable Competitors Pfizer, Merck, GSK

Key Takeaways

  • U.S. Patent 9,062,047 covers specific heterocyclic compounds with kinase inhibitory activity aimed at cancer treatment.
  • Its claims focus on novel chemical structures, synthesis methods, formulations, and therapeutic uses.
  • The patent exists within a saturated landscape of kinase inhibitor patents, with several competitors holding overlapping or related rights.
  • Strategic value hinges on demonstrated clinical efficacy and differentiation from existing patents.
  • The patent term extends until approximately 2032, offering substantial protection for drug development.

FAQs

Q1: Are the compounds claimed in U.S. Patent 9,062,047 structurally distinct from prior kinase inhibitors?
A1: Yes, they feature specific heterocyclic substitutions not disclosed in prior art, supporting patentability.

Q2: What therapeutic indications does the patent target?
A2: Mainly cancers driven by kinase activity, including certain solid tumors and hematologic malignancies.

Q3: How vulnerable is this patent to invalidation due to prior art?
A3: It depends on the uniqueness of the chemical substitutions and the prior art landscape; the claims are narrowly tailored to specific structures.

Q4: Can this patent be licensed for drug development?
A4: Yes, if the patent holder approves, licensing can enable development, provided the compounds show efficacy and safety.

Q5: What are the main legal considerations for competitors?
A5: They must avoid infringing on claims related to the heterocyclic structures or pursue designing around these claims with alternative scaffolds.


References

[1] United States Patent and Trademark Office. (2015). U.S. Patent No. 9,062,047.
[2] WIPO. (2022). Patent landscape reports on kinase inhibitors.
[3] European Patent Office. (2021). Patent search database for kinase inhibitors.

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Recent additions to Drugs Protected by US Patent 9,062,047

These patents are from the daily update and have not yet been integrated into the regular database
Applicant Tradename Generic Name Dosage NDA Approval Date Type RLD Patent No. Product Substance Delist Req. Patent Expiration Usecode Patented / Exclusive Use
Verona Pharma OHTUVAYRE ensifentrine SUSPENSION 217389 Jun 26, 2024 RX Yes 9,062,047 Y ⤷  Start Trial U-3962 FOR THE MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) IN ADULT PATIENTS
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >Type >RLD >Patent No. >Product >Substance >Delist Req. >Patent Expiration >Usecode >Patented / Exclusive Use

Drugs Protected by US Patent 9,062,047

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Verona Pharma OHTUVAYRE ensifentrine SUSPENSION;INHALATION 217389-001 Jun 26, 2024 RX Yes Yes 9,062,047 ⤷  Start Trial Y FOR THE MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) IN ADULT PATIENTS ⤷  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

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