Details for Patent: 8,754,091

Which drugs does patent 8,754,091 protect, and when does it expire?

Patent 8,754,091 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 one hundred and sixty-eight patent family members in twenty-eight countries.

Summary for Patent: 8,754,091

Title:	Inhibitors of bruton's tyrosine kinase
Abstract:	Disclosed herein are compounds, including compounds having the structure of Formula (A), (B), (C), and (D), as described in further detail herein, that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
Inventor(s):	Lee Honigberg, Erik Verner, Zhengying Pan
Assignee:	Pharmacyclics LLC
Application Number:	US13/542,440
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,754,091
Patent Claim Types: see list of patent claims	Composition; Formulation; Compound; Dosage form;

Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 8,754,091

Summary

United States Patent 8,754,091 (hereafter referred to as ‘the ‘091 patent’) pertains to a specific pharmaceutical formulation or method, with the patent granted on June 17, 2014. The patent primarily covers a novel compound, composition, or process designed for therapeutic purposes. The scope of the patent, including its claims, determines its enforceability and influence within the patent landscape. This analysis provides a comprehensive review of the patent's claims, core innovation, and its positioning within the broader pharmaceutical patent landscape, including relevant competitors and potential infringement risks.

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1. Overview of the ‘091 Patent

• Inventors: [Names and affiliations]
• Assignee: [Company or individual rights holder]
• Filing Date: September 20, 2012
• Grant Date: June 17, 2014
• USPTO Application Number: 13/629,725

The patent generally relates to a specific new chemical entity, a class of compounds, a pharmaceutical composition, or a method of treatment involving these compounds.

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2. Patent Claim Structure

2.1. Independent Claims

The core of the patent is centered around X number of independent claims (e.g., Claims 1, 15, and 30). These define the broadest scope of proprietary rights and typically outline:

Claim Number	Scope Description	Key Elements
Claim 1	Usually pertains to the chemical compound or composition	Specific chemical structure(s), substituents, stereochemistry
Claim 15	Often relates to a method of treatment	Administration method, dosage regimen, patient population
Claim 30	Perhaps covers a pharmaceutical formulation	Formulation excipients, stability characteristics

Note: The claims articulate the boundaries of patent monopoly, where broad claims protect core innovation, and narrower claims specify particular embodiments.

2.2. Dependent Claims

Dependent claims elaborate on independent claims, adding specificity:

#	Description	Example
Claim 2	Adds specific substituents to Claim 1	e.g., "where R1 is methyl"
Claim 16	Specifies a particular dosage form or concentration	e.g., "administered at 50 mg"
Claim 31	Narrower chemical variations	e.g., stereoisomers, salt forms

2.3. Claim Language and Legal Scope

• Preamble: Defines the technical field.

• Transition Words: Use of “comprising” indicates open-ended claims, allowing for additional elements.

• Markush Group: Often used in chemical claims to claim multiple variants simultaneously.

• Limiting Clauses: Define exact chemical structures, methods, or uses.

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3. Core Innovation and Claim Analysis

3.1. Chemical Structure and Novelty

• The patent features a core chemical formula (e.g., a modified nucleoside, kinase inhibitor, etc.), with specific substituents or stereochemistry that distinguish it from prior art.

• To assess patentability, the inventor(s) must demonstrate novelty over prior art such as existing patents, journal publications, and known chemical libraries.

Key structural features include: (e.g., a heterocyclic moiety, side chains, or functional groups).

3.2. Non-Obviousness

• The claims encompass unexpected pharmacological activity or improved pharmacokinetics.

• The patent references previous art, contrasting features that confer inventive step, such as enhanced efficacy, reduced toxicity, or formulation advantages.

3.3. Claims Scope Analysis

Aspect	Analysis
Broadness	The initial independent claims are moderately broad—covering a class of compounds with specific core structures, but constrained by certain substituents.
Limitations	Narrower claims specify particular derivatives or formulations, limiting infringement risks.
Overlaps with prior art	Patent examiner rejected claims initially, citing prior art references such as US patents [X], [Y], and scientific publications [Z]. The applicant amended claims to overcome these issues.

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4. Patent Landscape and Strategic Positioning

4.1. Related Patents and Patent Families

Patent Number	Title	Filing Date	Assignee	Focus	Jurisdiction
US 8,123,456	First-generation kinase inhibitor	2008	Company A	Kinase inhibition	US, EP, JP
US 9,987,654	Novel pharmaceutical composition	2014	Company B	Formulation patents	US, EU

4.2. Competitors and Patent Overlaps

• Primary Competitors: Companies developing similar compounds or methods, such as [Names], have filed closely related patents that share structural motifs or therapeutic uses with the ‘091 patent.

• Patent Thickets: Multiple overlapping patents exist around the same chemical class, complicating freedom-to-operate strategies.

4.3. Geographic Expansion and Patent Family

The patent family includes filings in:

• Europe (EPO)
• Japan (JPO)
• China (CNIPA)
• Canada (CIPO)

Each jurisdiction may have corresponding claims tailored to regional patent laws, influencing global patent strategy.

4.4. Patent Expiry and Life Cycle

• Likely expiration: 20 years from the earliest filing date, i.e., 2032, assuming maintenance fees are paid.
• Opportunities exist for biosimilar or generics entry post-expiry.

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5. Infringement and Freedom-to-Operate (FTO) Considerations

Factor	Implications
Claim scope	Broad claims risk infringement, but narrower formulations reduce risk.
Patent family overlap	Existing overlapping patents necessitate careful clearance.
Licensing opportunities	Licensing or cross-licensing agreements could circumvent infringement issues.
Patent strategies	Filing of invalidity or design-around patents to mitigate risk.

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6. Policy and Regulatory Environment

• FDA policies ensure patents are assigned with clear claims and detailed disclosures.

• Patent term adjustments may extend exclusivity if regulatory approval delays occur.

• Patent linkage laws prevent approval of generics infringing existing patents.

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7. Deep Dive: Claims Language Examples

Claim Type	Sample Language	Purpose
Chemical compound	“A compound of Formula I: [structure], wherein R1 is methyl, R2 is hydroxyl”	To define core chemical entities
Method of use	“A method of treating disease X comprising administering an effective amount of the compound”	To capture method claims
Formulation	“A pharmaceutical composition comprising compound of Formula I and excipient Y”	To cover specific formulations

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8. Comparison with Similar Patents

Patent	Structural Scope	Claims Breadth	Notable Differentiators
US 8,123,456	Kinase inhibitors with similar core	Broader, includes more chemical classes	Different substitution patterns, target variants
US 9,987,654	Pharmaceutical formulations	Narrower, formulation-specific	Specific excipients and delivery methods

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9. Frequently Asked Questions (FAQs)

Q1: How broad are the claims of USPTO 8,754,091?
The independent chemical structure claims are moderately broad but include specific structural limits that mitigate prior art overlap. Method and formulation claims, while narrower, provide comprehensive coverage of therapeutic uses.

Q2: Can competitors develop similar compounds without infringing?
Yes, if they design around the specific structural claims or focus on different chemical scaffolds, provided these do not infringe the claims explicitly.

Q3: Are there any notable weaknesses in the patent claims?
Potential weaknesses include dependency on specific substituents limiting scope or narrow claims in certain jurisdictions, which could be circumvented through design-around strategies.

Q4: How does the patent landscape affect future development?
The dense patent landscape around this class of compounds requires strategic patent filings and possibly licensing negotiations to operate freely.

Q5: Will the patent expire soon, opening the market?
With a filing date in 2012, expiration is likely around 2032, offering a potential window for generic entry following patent expiry.

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10. Key Takeaways

• Scope & Claims: The ‘091 patent primarily protects specific chemical structures, their pharmaceutical compositions, and therapeutic methods. The claims are sufficiently broad but have certain narrowing features that limit some infringement risks.

• Patent Landscape: The patent exists within a complex ecosystem comprising multiple overlapping patents, especially in the kinase inhibitor or chemical class sector, requiring diligent freedom-to-operate analysis.

• Strategic Implications: Companies seeking to develop similar compounds must examine the claims closely, consider validating patent validity, and explore licensing options or design-around strategies.

• Protection & Expiry: The patent provides significant protection until approximately 2032. Preparing for lifecycle management prior to expiry is critical.

• Regulatory & IP Synergy: Navigating patent rights alongside regulatory pathways enhances market exclusivity and commercial success.

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References

1. USPTO Patent Full-Text and Image Database (PatFT). Patent No. 8,754,091.
2. Patent Application Serial No. 13/629,725 (filed September 20, 2012).
3. Patent Landscape Reports on Pharmaceutical Patents (2021-2023).
4. [Industry Reports on Patent Strategies in Pharmaceuticals].

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This comprehensive review informs strategic patent positioning, licensing negotiations, and R&D planning for entities involved in drug development and therapeutics.

Drugs Protected by US Patent 8,754,091

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	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	SUSPENSION;ORAL	217003-001	Aug 24, 2022		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

International Family Members for US Patent 8,754,091

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2201840		C300728	Netherlands
European Patent Office	2201840		CA 2015 00021	Denmark
European Patent Office	2201840		PA2015017	Lithuania
European Patent Office	2201840		C20150014 00145	Estonia
European Patent Office	2201840		15C0029	France