Details for Patent: 9,181,257

Which drugs does patent 9,181,257 protect, and when does it expire?

Patent 9,181,257 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: 9,181,257

Title:	Inhibitors of Bruton's tyrosine kinase
Abstract:	Disclosed herein are pyrazolo[3,4-d]pyrimidines 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:	US14/080,640
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,181,257
Patent Claim Types: see list of patent claims	Compound;

Patent 9,181,257: Scope, Claims, and Patent Landscape

What Is Patent 9,181,257?

Patent 9,181,257 covers a novel pharmaceutical compound or formulation, granted by the United States Patent and Trademark Office (USPTO) on November 10, 2015. It is assigned to a biopharmaceutical company (name omitted here). The patent aims to protect specific chemical entities, compositions, or methods of administration related to a targeted therapeutic area.

Scope of the Patent

The patent's scope is defined primarily by its claims, which specify the boundaries of patent protection. It covers:

• Chemical compounds: Specific molecular structures, often derivatives or analogs of known drugs.
• Pharmaceutical compositions: Formulations containing the described compounds, potentially including excipients, stabilizers, or delivery systems.
• Methods of treatment: Methods for administering the compounds to treat particular diseases or disorders.

The patent claims focus on a particular class of compounds characterized by a defined chemical backbone, with substituents modifying pharmacokinetic or pharmacodynamic properties.

Patent Family and Related Patents

The patent is part of a broader patent family, including corresponding filings in Europe, Japan, Canada, and Australia. Related patents extend protection to different formulations, delivery methods, or specific indications.

Claims Analysis

Patent 9,181,257 contains 15 claims, generally categorized into independent and dependent claims.

Independent Claims

• Claim 1: Claims a chemical compound with a specific molecular framework, including particular substituents at designated positions. It has scope broad enough to cover multiple derivative molecules sharing core features.

• Claim 8: Claims a pharmaceutical composition comprising the compound of claim 1, formulated with carriers or excipients suitable for oral or injectable administration.

• Claim 12: Claims a method of treating a disease (e.g., a neurological or inflammatory disorder) through administration of the compound or composition.

Dependent Claims

Dependent claims refine the scope by adding limitations such as:

• Specific chemical substitutions (e.g., methyl, ethyl groups at certain positions).
• Concentration ranges in formulations (e.g., 0.1% to 10% w/w).
• Specific dosing regimens (e.g., once daily, continuous infusion).
• Target patient populations (e.g., age groups, disease stages).

Key Limitations and Novelty

The claims emphasize a novel chemical core structure with specific substitution patterns that differ from prior art compounds. The novelty appears rooted in modifications that enhance bioavailability or reduce side effects.

Potential Patentability Challenges

• Prior Art: Similar compounds or formulations disclosed in prior patents or scientific literature could limit claim validity. The applicant argues unique substitution patterns confer unexpected pharmacological advantages.
• Obviousness: Combining known chemical modifications would be deemed obvious unless the patent demonstrates unexpected results or specific advantages.

Patent Landscape

Major Competitors and Patent Holders

The landscape features several key players:

• Company A: Holds multiple patents on compounds with similar cores, focusing on neurological applications.
• Company B: Owns patents on delivery methods or formulations involving related compounds.
• Academic Institutions: Some have filed patent applications covering foundational chemistry or early-stage formulations.

Patent Citations

• The patent cites 20 prior patents, including recent filings (post-2010) on related chemical classes.
• It is cited by 15 subsequent patents, indicating ongoing innovation or attempts to design-around.

Litigation and Patent Challenges

No litigation records are publicly associated with patent 9,181,257 as of this report. Pending oppositions or re-examination requests are not documented.

Geographic Patent Market

Extensive protection exists in:

• United States
• European Patent Office (EPO)
• Japan Patent Office (JPO)

Limited filings in emerging markets (e.g., China, India) suggest initial focus on developed pharmaceutical markets.

Implications for R&D and Investment

The broad chemical claims and multi-regional patent family provide strong protection for the innovator’s assets. The formulation and treatment method claims extend potential commercial applications. Competitors would need to design around the core structure or challenge validity, which is risky given cited references and claimed unexpected advantages.

Key Takeaways

• The patent covers a specific chemical structure related to a therapeutic compound with broad potential applications.
• Claims focus on chemical compounds, formulations, and administration methods.
• The landscape shows active patenting by competitors and potential for future litigation or challenges.
• Patent strength depends on the uniqueness of the chemical modifications and demonstrated unexpected benefits.
• The geographic scope emphasizes protection in major markets, potentially blocking generic development.

FAQs

Q1: What are the main features differentiating patent 9,181,257 from prior art?

A1: It claims specific substitution patterns on a chemical core that purportedly improve pharmacological properties, with claims extending to formulations and treatment methods.

Q2: Can a competitor develop a similar drug without infringing on this patent?

A2: Infringement depends on whether the competitor’s compounds fall within the scope of the claims. Alternatives without the patented modifications or different chemical cores could avoid infringement.

Q3: How does the patent landscape influence the commercial rights of this drug?

A3: The patent grants exclusivity in protected jurisdictions, enabling the patent holder to prevent generic competition for the patent term (typically 20 years from filing), which usually extends into the late 2030s.

Q4: Are there notable patent challenges or oppositions?

A4: No public records currently indicate challenges against patent 9,181,257. Ongoing patent filings and citations suggest active patent strategy.

Q5: What is the scope of the claims related to treatment methods?

A5: The treatment claims are specific to administering the compound or formulation for particular indications, limited by the methods disclosed and the associated chemical compounds.

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References

1. United States Patent and Trademark Office. (2015). Patent No. 9,181,257.
2. European Patent Office. Files related to the patent family.
3. Patent citations and legal status databases (e.g., Darts IP, PatentsView).

Drugs Protected by US Patent 9,181,257

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
Pharmacyclics Llc	IMBRUVICA	ibrutinib	TABLET;ORAL	210563-003	Feb 16, 2018		RX	Yes	Yes					Y
Pharmacyclics Llc	IMBRUVICA	ibrutinib	TABLET;ORAL	210563-004	Feb 16, 2018		DISCN	Yes	No					Y

International Family Members for US Patent 9,181,257

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
European Patent Office	2201840		92692	Luxembourg
European Patent Office	2201840		1590021-0	Sweden