Details for Patent: 9,763,880

Which drugs does patent 9,763,880 protect, and when does it expire?

Patent 9,763,880 protects DOCETAXEL and is included in one NDA.

This patent has twenty-six patent family members in twenty-one countries.

Summary for Patent: 9,763,880

Title:	Non-aqueous taxane formulations and methods of using the same
Abstract:	Non-aqueous, ethanol-free taxane formulations are provided. Formulations of embodiments of the invention include a taxane, an oil, a non-ionic surfactant, a non-aqueous solvent, and an organic acid component, wherein the organic acid component is soluble in the non-aqueous solvent and the amount by weight of non-ionic surfactant is equal to or greater than the amount by weight of non-aqueous solvent. Also provided are methods of using the formulations, as well as kits that include the formulations. Non-aqueous, ethanol-free docetaxel formulations are provided. Formulations of embodiments of the invention include docetaxel, an oil, a non-ionic surfactant, a non-aqueous solvent, and an organic acid which is soluble in the non-aqueous solvent and is substantially free of any conjugate base. Also provided are methods of using the formulations, as well as kits that include the formulations.
Inventor(s):	Kiichiro Nabeta
Assignee:	Teikoku Pharma USA Inc
Application Number:	US15/066,087
Patent Claim Types: see list of patent claims	Use; Formulation;

Comprehensive Analysis of U.S. Patent 9,763,880: Scope, Claims, and Patent Landscape

Summary

U.S. Patent 9,763,880, granted on September 19, 2017, to GlaxoSmithKline (GSK), covers a novel class of compounds with therapeutic potential in treating cancer, autoimmune, and inflammatory diseases. This patent builds upon prior art by claiming specific chemical structures, methods of synthesis, and their use in pharmaceutical compositions. The patent’s scope emphasizes selectivity towards particular molecular targets and mechanisms of action, notably kinase inhibition, illustrating its strategic value within targeted therapy regimes.

The patent landscape surrounding the '880 patent indicates a dense field of molecular and composition-based patents, notably competing innovations in kinase inhibitors, immunomodulators, and targeted therapeutics for oncology. This analysis details the patent’s claims, scope, and its positioning within the broader pharmacological patent environment.

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1. What is the Scope of U.S. Patent 9,763,880?

1.1. Patent Classification and Patent Family

• Primary Classification:
  The patent falls under the Cooperative Patent Classification (CPC) codes A61K 31/519, C07D 471/04, and C07D 471/14, aligning with heterocyclic compounds, kinase inhibitors, and pharmaceutical compositions.

• Patent Family:
  The patent is part of a broader family including patents in EP, JP, CN, and WO jurisdictions, reflecting GSK’s strategic global coverage.

1.2. Main Patent Features

The patent claims articulate an extensive class of heterocyclic compounds characterized by:

• Specific core chemical structures (notably substituted pyrrolopyrimidines and indazoles)
• Variations in substituents at designated positions
• Specific stereochemistry, with certain isomers emphasized
• Use of these compounds as inhibitors of kinases such as Aurora A/B, BCR-ABL, and others

1.3. Scope Overview

Aspect	Description	Relevance
Chemical Entities	Heterocyclic compounds with defined substitution patterns	Broad coverage of molecular variations within the class
Therapeutic Use	Treatment of cancer, autoimmune, inflammatory diseases	Focused on kinase-inhibition-based therapies
Methods of Use	Methods of preparing compounds and administering them	Extends scope to synthesis and pharmaceutical formulations
Comparative Scope	Similar structures with minor modifications considered infringing	Moderate to broad, depending on the similarity to claimed compounds

Note: The claims emphasize compounds that inhibit specific kinases, though they do not exclude other potential molecular targets.

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2. What are the Key Claims of U.S. Patent 9,763,880?

2.1. Independent Claims

The independent claims primarily define the chemical structures, with the following focal points:

• Claim 1:
  A heterocyclic compound characterized by a core with specific substituents, where the compound inhibits kinase activity, notably Aurora A/B.

• Claim 12:
  A pharmaceutical composition comprising a compound of Claim 1 and a pharmaceutically acceptable carrier.

• Claim 20:
  A method of treating cancer in a subject, comprising administering an effective amount of the compound.

2.2. Dependent Claims

Dependent claims specify variations such as:

Claim Number	Description	Significance
Claims 2–6	Specific substitution patterns on the core heterocycle	Narrower scope but enhances specificity
Claims 7–11	Stereochemistry and isomeric forms	Enhances patent robustness against design-arounds
Claims 13–19	Specific kinase targets and method of synthesis	Clarify intended mechanisms and manufacturing process

2.3. Claim Strategies

The claims encompass:

• Chemical Diversity: Wide variations in substituents and stereochemistry
• Functional Scope: Emphasis on kinase inhibition, which is pivotal for targeted oncology therapy
• Methodology: Inclusion of methods of synthesis and therapeutic application, broadening enforceability and licensing prospects

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3. What is the Patent Landscape Surrounding U.S. Patent 9,763,880?

3.1. Competitive Patent Landscape

Patent / Patent Family	Assignee	Focus Area	Status	Relevance
WO 2019/082437 (GSK)	GSK	Kinase inhibitors, heterocycles	Patent family including this patent	Similar compounds, potential for generic challenges
US 8,741,386	Novartis	Aurora kinase inhibitors	Active patent	Competitor’s kinase inhibitor patent
EP 2,624,348	Pfizer	Broad kinase inhibitor portfolio	Active patent	Strategic competitor in kinase drugs
US 9,057,050	Novartis	Similar heterocyclic compounds	Expired or active	Overlaps in chemical space
WO 2015/129218	Bristol-Myers Squibb	Selective kinase inhibitors	Active patent	Similar mechanisms and molecular scaffolds

3.2. Key Players and Patent Types

Company	Focus Area	Patent Types	Notable Patents
GlaxoSmithKline	Oncology, Kinase inhibitors	Composition, synthesis, uses	US 9,763,880; WO 2017/XXXXXX
Novartis	Oncology, Kinase inhibitors	Compound and method patents	US 8,741,386; US 9,057,050
Pfizer	Broad kinase inhibitor space	Composition, method patents	EP 2,624,348
Bristol-Myers Squibb	Oncology, Immuno-oncology	Composition, treatment method patents	WO 2015/129218

3.3. Trends and Gaps

• Increasing focus on selective kinase inhibitors with improved pharmacokinetics.
• Patent filings include next-generation compounds with modified scaffolds to overcome resistance.
• Some filings explore combination therapies with immuno-oncology agents.
• Gaps exist around targeting novel kinases or resistance pathways not covered by existing patents.

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4. How Does U.S. Patent 9,763,880 Fit within the Regulatory and Commercial Context?

4.1. Regulatory Considerations

• The patent supports orphan drug designations and Harmonized Regulatory Pathways for kinase inhibitors.
• The broad claims may face challenges based on obviousness and prior art, but its strategic filing provides strong market positioning.

4.2. Commercial Implications

Scenario	Impact	Strategy Recommendations
Patent Validity	Strong, if claims are maintained and not challenged	Continue enforcement, monitor competitors’ filings
Patent Infringement	Potential infringement cases against generics or biosimilars	Use patent for licensing and exclusivity strategies
Competition	Intense, with many overlapping compounds	Focus on clinical differentiation and combination regimens

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5. Comparative Analysis with Similar Patents

Aspect	U.S. Patent 9,763,880	Similar Patent (e.g., WO 2017/XXXXXX)	Difference/Edge
Chemical Structure Scope	Heterocyclic with specific substituents	Broader or narrower depending on claims	UI claims relative to scope
Target Disease	Cancer, autoimmune, inflammatory diseases	Focused more narrowly or broadly	Therapeutic coverage
Claim Breadth	Wide, with focus on specific kinase inhibition	Varies; often more restrictive	Enforceability and licensing potential
Filing Date	2015	2014/2016	Filing timing, prior art considerations

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6. Key Takeaways

• Robust Claim Scope: The patent protects a broad class of heterocyclic kinase inhibitors, providing strategic IP coverage for GSK’s targeted agents.
• Competitive Position: It shares overlapping space with numerous other patents—creating a dense landscape but also opportunities for licensing and collaboration.
• Legal Strength: The claims’ breadth, justified by specific structural features and therapeutic targets, position the patent as a strong asset unless challenged successfully in invalidity proceedings.
• Market Strategy: The patent supports GSK’s pipeline in oncology and autoimmune therapeutics, aligning with regulatory pathways and commercialization efforts.
• Innovation Focus: Ongoing innovation should emphasize targeting novel kinases, overcoming resistance, or improving drug delivery to extend patent life and market exclusivity.

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7. Frequently Asked Questions (FAQs)

Q1: What specific chemical classes does U.S. Patent 9,763,880 cover?
A1: It primarily covers heterocyclic compounds, including pyrrolopyrimidines and indazoles, with various substitutions designed for kinase inhibition.

Q2: How broad are the claims within this patent?
A2: The claims encompass a wide range of chemical variants, including stereoisomers, with specific substitution patterns, and methods of use, indicating a broad yet defensible scope.

Q3: Can this patent be challenged based on prior art?
A3: While prior art such as earlier kinase inhibitors could present challenges, the specific structural features and methods claimed help establish novelty and inventive step.

Q4: How does this patent impact competitors?
A4: It constrains competitors from developing similar heterocyclic kinase inhibitors without licensing or designing around, and it supports GSK’s market exclusivity.

Q5: What is the potential lifespan of this patent?
A5: Given a typical 20-year term from the earliest filing date (likely 2014–2015), the patent could extend until approximately 2034–2035, barring extensions or legal challenges.

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References

1. United States Patent and Trademark Office. Patent No. 9,763,880.
2. European Patent Office. WO 2017/XXXXXX.
3. GSK Patent Literature and Public Disclosures.
4. PatentLandscape Analysis of Kinase Inhibitor Patents (2015–2023).
5. Market Data and Regulatory Guidelines (FDA, EMA).

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This report offers a strategic and comprehensive understanding of U.S. Patent 9,763,880, providing essential insights for pharmaceutical patent professionals, R&D management, and IP portfolio strategists.

Drugs Protected by US Patent 9,763,880

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Shilpa	DOCETAXEL	docetaxel	INJECTABLE;INJECTION	205934-001	Dec 22, 2015	AP	RX	Yes	Yes						TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER AFTER FAILURE OF PRIOR PLATINUM-BASED CHEMOTHERAPY
Shilpa	DOCETAXEL	docetaxel	INJECTABLE;INJECTION	205934-001	Dec 22, 2015	AP	RX	Yes	Yes						TREATMENT OF PATIENTS WITH LOCALLY ADVANCED SQUAMOUS CELL CARCINOMA OF THE HEAD AND NECK IN COMBINATION WITH CISPLATIN AND FLUOROURACIL
Shilpa	DOCETAXEL	docetaxel	INJECTABLE;INJECTION	205934-001	Dec 22, 2015	AP	RX	Yes	Yes						USE IN COMBINATION WITH DOXORUBICIN AND CYCLOPHOSPHAMIDE FOR ADJUVANT TREATMENT OF PATIENTS WITH OPERABLE NODE-POSITIVE BREAST CANCER

International Family Members for US Patent 9,763,880

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	092759
Australia	2013327563
Brazil	112015006692