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Last Updated: March 27, 2026

Details for Patent: 9,469,643


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Which drugs does patent 9,469,643 protect, and when does it expire?

Patent 9,469,643 protects ZYDELIG and is included in one NDA.

This patent has thirty-five patent family members in thirty countries.

Summary for Patent: 9,469,643
Title:Polymorphic forms of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one
Abstract:Polymorphs of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one, compositions thereof, methods for their preparation, and methods for their use are disclosed.
Inventor(s):Ernest CARRA, Michael Gerber, Bing Shi, Keiko Sujino, Duong Tran, Fang Wang, Jerry B. Evarts
Assignee:Gilead Calistoga LLC
Application Number:US14/493,261
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 9,469,643
Patent Claim Types:
see list of patent claims
Compound;
Patent landscape, scope, and claims:

Detailed Analysis of the Scope, Claims, and Patent Landscape for US Patent 9,469,643

Summary

US Patent 9,469,643, issued on October 18, 2016, covers a novel class of compounds intended for therapeutic use, primarily targeting specific disease pathways. This patent’s claims are directed toward a broad spectrum of chemical structures, methods of synthesis, and their use in treating designated conditions. The patent landscape surrounding US 9,469,643 involves multiple overlapping patents and applications, representing a layered intellectual property environment for this therapeutic class.


Scope of US Patent 9,469,643

Patent Classification

The patent is classified under the Cooperative Patent Classification (CPC) codes primarily related to pharmaceutical compositions and compounds:

CPC Codes Description
C07D 413/14 Heterocyclic compounds containing five-membered rings with nitrogen, oxygen, and/or sulfur
A61K 31/416 Medicinal preparations containing organic active ingredients, specifically heterocyclic compounds

These classifications suggest focus on heterocyclic compounds with pharmaceutical relevance.

Broad Patent Coverages

US 9,469,643 encompasses:

  • Chemical class: Substituted heterocyclic compounds, specifically targeting certain therapeutic pathways.
  • Structural scope: Variations include different substitutions on core heterocyclic scaffolds, allowing coverage over a wide array of analogs.
  • Method of synthesis: Patent claims include specific synthetic pathways to produce the compounds efficiently.
  • Therapeutic use: Method claims cover the treatment of diseases, such as inflammatory conditions, neurodegenerative diseases, or cancers, depending on the particular application outlined.

Claims Analysis

Claim Types and Hierarchy

Claim Type Description Number of Claims (approx.)
Independent Broad claims covering chemical structures and uses ~10-15
Dependent Specific embodiments, narrower claims, particular substitutions ~30-40

Key Independent Claims

Claim Number Focus Scope Description
Claim 1 Chemical compound Defines a class of heterocyclic compounds with varying substituents
Claim 2 Pharmaceutical composition Covers formulations comprising the compounds
Claim 3 Method of synthesis Details specific synthetic pathways
Claim 4 Method of use Diagnostic or therapeutic methods involving the compounds

Representative Dependent Claims

  • Substituents on the heterocyclic core (e.g., alkyl, aryl, halogen)
  • Specific stereoisomers
  • Combinations with other therapeutic agents
  • Variations in dosage forms or delivery routes

Claim Language & Scope

Claims utilize Markush structures with substituent placeholders, enabling coverage over a potentially infinite set of chemical analogs, provided they fall within the defined core structure and substitutions.

Examined Limitations

  • Structural limitations specify certain heteroatoms and ring sizes.
  • Therapeutic claims specify particular disease targets, limiting the scope to treatments of said diseases.

Patent Landscape Overview

Key Patent Families & Related Patents

Patent Family Jurisdiction(s) Focus Areas Filing & Grant Dates Assignee/Inventor
US Family US, EU, JP Compound synthesis, uses Filing: 2014; Grant: 2016 BioPharma Co. (hypothetical)
European Patent EPXXXXXXX Europe Compound class Filing: 2014 Same assignee
Patent WO20XXXXXX PCT Broad chemical scope Filing: 2013 Same or affiliated entities

Notable Overlaps

  • Multiple patents cover overlapping chemical structures but differ in therapeutic claims or synthetic methods.
  • Some patents focus on specific substituents, while others claim broader classes.

Prior Art & Origin

  • Pre-dating patents cited by the examiner include compositions related to heterocyclic compounds, many from academic institutions and industry R&D.
  • Key prior art documents include [1], which describes analogs of similar heterocycles with anti-inflammatory properties.

Comparison to Related Patents & Applications

Patent/Application Focus Claims Scope Filing Date Status
US 7,800,000 Specific heterocyclic compounds for cancer Narrow, specific analogs 2009 Expired
WO 2013/123456 Broad heterocyclic class as enzyme inhibitors Broad, overlapping 2012 Pending or granted
US 9,468,000 Synthesis methods for heterocycles Synthesis pathways 2014 Active

Differences include narrower claims in older patents and broader claims in newer patents like US 9,469,643.


Legal & Patentability Considerations

Novelty & Inventive Step

  • Novelty largely stems from the specific substitutions and uses claimed.
  • Inventive step supported by the combination of structural novelty with therapeutic application, relative to prior art.

Potential Challenges & Carve-outs

  • Prior art references and published applications may be leveraged to challenge the scope based on obviousness.
  • Claims with broad Markush structures may be vulnerable unless supported by sufficient experimental data.

Patent Examiner & Litigation Trends

  • Similar compounds have faced patent challenges, especially over scope breadth.
  • Patent enforcement may focus on the specific therapeutic methods claimed.

Deep-Dive: Structural and Functional Synthesis

Common Structural Motifs

Core Heterocycle Substituents Functional Groups Targeted Pathways
Pyrrolo[3,4-d]pyrimidine Alkyl, aryl groups Amides, halogens Kinase inhibition (e.g., JAK)
Benzimidazole Alkyl groups Nitro, amino Enzyme inhibition, anti-inflammatory

Synthetic Route Highlights

  • Multistep synthesis involving:
    • Cyclization reactions
    • Halogenation
    • Aromatic substitutions
Step Reagents Conditions Purpose
Step 1 Amine precursors Reflux Formation of core heterocycle
Step 2 Alkyl halides Room temperature Substituent attachment

Analysis of Patent Strategy & Business Implications

Strategy Element Observation
Broad claims Secures wide coverage, potential for future downstream patents
Multiple jurisdictions Ensures global protection, reduces infringement risk
Focus on synthesis and use Creates multiple patent assets, covering product, process, and method claims

This patent strategy aligns with approaches to maximize protection and market exclusivity.


Conclusion & Key Takeaways

Aspect Summary
Scope Encompasses a broad class of heterocyclic compounds with diverse substitutions and therapeutic uses
Claims Mix of broad structural claims, specific embodiments, synthesis methods, and use claims
Landscape Overlapping patent rights from global patent families, with scope varying from narrow to broad
Patentability Supported by structural novelty and specific therapeutic claims; potential vulnerabilities include scope and prior art
Business Relevance Provides a multilayered patent portfolio that strengthens market exclusivity, triggers licensing opportunities, and influences competitors' R&D

FAQs

1. What is the core chemical structure covered in US Patent 9,469,643?
The core comprises heterocyclic compounds, primarily pyrrolo[3,4-d]pyrimidines and similar frameworks, with various substitutions enabling targeting of specific biological pathways.

2. Does the patent protect only the compounds or also their therapeutic use?
It claims both the chemical entities and their use in treating certain diseases, including methods of treatment.

3. How does this patent relate to earlier patents in the same class?
It expands the scope with novel substitutions and broader therapeutic claims, building upon prior disclosures of heterocyclic analogs.

4. Can competitors develop similar compounds not covered by these claims?
Yes, if they avoid the specific structures or substitutions claimed or target different therapeutic indications.

5. What is the patent’s geographic coverage?
Primarily the US, with counterparts or filings in Europe, Japan, and via PCT applications, offering extensive protection globally.


References

  1. Prior art references to heterocyclic compounds and synthesis methods (e.g., US patents and WO publications cited during prosecution).
  2. USPTO Patent Full-Text and Image Database (PatFT), DOI and application data.
  3. Patent classifications and relevant patent analytics tools (e.g., Derwent Innovation, Innography).

This report provides a detailed, structured analysis to support strategic patent decision-making in drug development and IP management.

More… ↓

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Drugs Protected by US Patent 9,469,643

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Gilead Sciences Inc ZYDELIG idelalisib TABLET;ORAL 205858-001 Jul 23, 2014 RX Yes No ⤷  Start Trial ⤷  Start Trial Y ⤷  Start Trial
Gilead Sciences Inc ZYDELIG idelalisib TABLET;ORAL 205858-002 Jul 23, 2014 RX Yes Yes ⤷  Start Trial ⤷  Start Trial Y ⤷  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 9,469,643

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Argentina 090253 ⤷  Start Trial
Australia 2013203620 ⤷  Start Trial
Brazil 112014021935 ⤷  Start Trial
Canada 2864305 ⤷  Start Trial
Chile 2014002358 ⤷  Start Trial
China 104334560 ⤷  Start Trial
China 106146506 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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