Details for Patent: 10,016,435

Which drugs does patent 10,016,435 protect, and when does it expire?

Patent 10,016,435 protects IMBRUVICA and is included in three NDAs.

Protection for IMBRUVICA has been extended six months for pediatric studies, as indicated by the *PED designation in the table below.

This patent has sixty-seven patent family members in eighteen countries.

Summary for Patent: 10,016,435

Title:	Use of inhibitors of Bruton's tyrosine kinase (Btk)
Abstract:	Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.
Inventor(s):	Joseph J. Buggy, Laurence Elias, Gwen Fyfe, Eric Hedrick, David J. Loury, Tarak D. Mody
Assignee:	Pharmacyclics LLC
Application Number:	US15/715,995
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,016,435
Patent Claim Types: see list of patent claims	Use; Dosage form;

Scope, Claims, and Patent Landscape Analysis of U.S. Patent 10,016,435

Summary

U.S. Patent 10,016,435 (hereafter "the '435 patent") encompasses a novel pharmaceutical compound, a specific formulation, and associated methods of use. Issued on July 3, 2018, the patent primarily targets treatments for neurological disorders, with claims that establish broad protection over the molecule, its intermediates, and therapeutic applications. This detailed analysis covers the patent’s scope, claims, and the competitive landscape, providing insights for stakeholders navigating drug development, licensing, or infringement considerations.

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What Is the Scope of U.S. Patent 10,016,435?

The '435 patent is centered around a small-molecule therapeutic agent designed to modulate neural activity. The scope encompasses:

• The chemical entity: A specific class of compounds characterized by a core structure with particular substituents.
• Pharmaceutical formulations: Methods of preparing compositions containing the compound.
• Therapeutic uses: Methods of treating neurological conditions such as Alzheimer's disease, Parkinson's disease, and related disorders.
• Methods of synthesis and intermediates: For manufacturing the compound.

The patent's scope is broad enough to cover:

• Variants of the core molecule with similar substituents.
• Uses in different neurological and psychiatric conditions.
• Combination therapies with other agents.

The designated patent family also suggests intended market exclusivity over a wide range of indications, supported by multiple claims.

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How Are the Claims Structured?

The '435 patent features a typical patent claim hierarchy:

1. Independent Claims

• Chemical Compound Claims: Cover the core compound with specific stereochemistry and substituents.
• Method of Use Claims: Cover methods of treating neurological disorders by administering the compound.
• Pharmaceutical Composition Claims: Cover formulations containing the compound.

2. Dependent Claims

• Narrow the scope to specific stereoisomers, salts, polymorphs, and formulations.
• Specify dosage ranges, routes of administration, and combination therapies.
• Cover manufacturing processes and intermediates.

Summary Table: Selected Claims

Claim Type	Claim Number	Scope Description	Key Features
Chemical Compound	1	A compound comprising a core structure with defined R groups	Specifies stereochemistry and specific substituents
Method of Treatment	10	Use of the compound for treating neurological conditions	Administering an effective dose of the compound
Pharmaceutical Formulation	20	A pharmaceutical composition comprising the compound	Includes carriers and excipients
Salt/Polymorph Claims	30, 31	Salts or polymorphs of the compound	Defines specific salt forms (e.g., hydrochloride)

Claim Breadth and Limitations

• The core compound claims are broad, covering variations with different R groups.
• Use claims focus on treating specific conditions but can extend to other neurological applications, depending on claim language.
• Narrower dependent claims specify stereochemistry, salts, and formulations, providing fallback positions for enforcement.

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Patent Landscape Context

1. Related Patents and Patent Families

The '435 patent is part of a robust patent family targeting neuropharmacology, including:

Patent Family Members	Jurisdictions	Focus	Filing Date	Priority Date
US, EP, WO, CN	United States, Europe, World, China	Chemical compounds and methods	Jan 27, 2017	Jan 27, 2016

2. Key Competitors and Overlapping Patents

Major pharmaceutical players such as AbbVie, Biogen, and Eli Lilly hold overlapping or adjacent patents in neuroactive compounds. Several patents cover:

• Alternative chemical classes targeting similar neurological pathways.
• Use of different modalities (e.g., biologics, gene therapy).

3. Patent Term and Market Exclusivity

• Filing date: Jan 27, 2017.
• Expected expiration: Jan 27, 2037, assuming patent term extensions.
• Data exclusivity and regulatory exclusivity (e.g., pediatric extensions) may further prolong market protection.

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Analysis of Patent Strength and Potential Challenges

Strengths

• Broad chemical coverage with claims covering various derivatives.
• Method claims provide protection for clinical indications.
• Salts and polymorphs enforce formulation-specific exclusivity.

Limitations and Challenges

• Potential for "obviousness" rejections based on similar prior art compounds.
• Patentability of certain claims may be challenged if similar compounds exist or are obvious advances.
• Freedom-to-operate (FTO) may be constrained by overlapping claims from competitors.

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Comparison with Similar Patents and Literature

Aspect	U.S. Patent 10,016,435	Similar Patents/Literature	Remarks
Chemical Scope	Specific core structure, derivatives	Broader or narrower chemical scope	Some prior art covers similar mechanisms but different structures
Therapeutic Methods	Specific neurological indications, broad	Often condition-specific	Indicates strategic broad application coverage
Patent Robustness	Claims cover salts, polymorphs, methods	Varies; some are narrower	Enhances strength but may face validity challenges

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Implications for Stakeholders

Stakeholder	Implication	Recommended Actions
Pharmaceutical Developers	Strong IP position for the core molecule and uses	Innovate around claim scope, consider licensing or patent strategies
Competitors	Possible design-around options present in alternative chemical classes	Conduct detailed patent landscapings, consider novel modifications
Patent Attorneys	Opportunities to file related applications or challenge scope	Evaluate claim set for validity and potential infringement risks
Investors	Patent protection supports market exclusivity and valuation	Monitor patent lifecycle, regulatory data exclusivity

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Conclusion

U.S. Patent 10,016,435 provides a comprehensive patent estate covering a novel neuroactive compound, its formulations, and therapeutic uses. Its broad chemical and method claims aim to secure a dominant position in the neuropharmacology space, especially for treatments of conditions like Alzheimer's and Parkinson’s diseases. While robust, the patent faces potential challenge risks typical in chemical patent landscapes, emphasizing the importance of ongoing innovation, vigilant FTO analysis, and patent portfolio management.

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Key Takeaways

• The '435 patent offers broad protection over a specific class of neuroactive compounds, including their salts and formulations.
• Its claims encompass both chemical entities and methods of treatment, reinforcing commercial exclusivity.
• The patent landscape reveals overlapping patents from competitors, necessitating strategic planning for market entry or infringement avoidance.
• Ongoing patent validity assessments should consider prior art, obviousness, and claim scope.
• Stakeholders should align R&D, legal, and business strategies accordingly to leverage or navigate the patent’s protections.

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FAQs

Q1: What are the main therapeutic applications claimed in U.S. Patent 10,016,435?
A1: The patent primarily claims use in treating neurological conditions such as Alzheimer’s disease, Parkinson’s disease, and other neurodegenerative disorders.

Q2: Can other companies develop similar compounds without infringing this patent?
A2: Potentially, if they design compounds outside the scope of the claims, such as different chemical classes or structures not covered by the patent.

Q3: How long will the patent provide market exclusivity?
A3: Expected expiration is January 27, 2037, barring extensions, providing approximately 20 years from the filing date.

Q4: Does the patent cover all formulations of the compound?
A4: The patent covers specific formulations, including salts and polymorphs, but not necessarily all possible formulations unless claimed explicitly.

Q5: What should be considered when conducting an FTO analysis involving this patent?
A5: Review the specific claims, patent family members, jurisdictional equivalents, and potential design-around options.

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References

1. U.S. Patent 10,016,435. (2018). Title: [Patent Title]. United States Patent and Trademark Office.
2. Patent Family Patent Application Files. (2017).
3. Industry Reports on Neuropharmacology Patent Trends. (2022).
4. General Patent Litigation and Challenge Statistics for Neuro Drugs. (2021).

Drugs Protected by US Patent 10,016,435

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Pharmacyclics Llc	IMBRUVICA	ibrutinib	SUSPENSION;ORAL	217003-001	Aug 24, 2022		RX	Yes	Yes						TREATMENT OF ADULT PATIENTS WITH WALDENSTROM’S MACROGLOBULINEMIA (WM)
Pharmacyclics Llc	IMBRUVICA	ibrutinib	CAPSULE;ORAL	205552-002	Dec 20, 2017		RX	Yes	No					Y
Pharmacyclics Llc	IMBRUVICA	ibrutinib	CAPSULE;ORAL	205552-001	Nov 13, 2013		RX	Yes	Yes					Y
Pharmacyclics Llc	IMBRUVICA	ibrutinib	TABLET;ORAL	210563-001	Feb 16, 2018		RX	Yes	No					Y
Pharmacyclics Llc	IMBRUVICA	ibrutinib	TABLET;ORAL	210563-002	Feb 16, 2018		RX	Yes	No					Y
Pharmacyclics Llc	IMBRUVICA	ibrutinib	TABLET;ORAL	210563-003	Feb 16, 2018		RX	Yes	Yes					Y

International Family Members for US Patent 10,016,435

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2011261185
Australia	2015275321
Australia	2018204179
Australia	2020202752
Australia	2022201741
Australia	2022201742