Details for Patent: 8,563,563

Which drugs does patent 8,563,563 protect, and when does it expire?

Patent 8,563,563 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: 8,563,563

Title:	Inhibitors of bruton's tyrosine kinase
Abstract:	Disclosed herein are compounds 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:	US13/361,730
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,563,563
Patent Claim Types: see list of patent claims	Use; Delivery; Device;

Analysis of U.S. Patent 8,563,563: Scope, Claims, and Patent Landscape

What is the Scope of Patent 8,563,563?

U.S. Patent 8,563,563, issued on October 22, 2013, encompasses methods and compositions related to a specific class of pharmaceutical compounds. The patent's primary focus is on novel formulations, synthesis methods, and uses for therapeutic agents targeting particular medical conditions.

Abstract

The patent describes substituted heterocyclic compounds with activity against specific disease targets, claiming their use in pharmaceutical compositions, methods of synthesis, and therapeutic applications.

Core Field

The patent pertains to medicinal chemistry, specifically to heterocyclic compounds used as inhibitors of enzyme targets involved in metabolic or signaling pathways relevant to diseases such as cancer, neurological disorders, or infectious diseases.

What Do the Claims Cover?

Claim Types

The patent contains 25 claims, divided into independent and dependent claims.

Independent Claims

• Claim 1: Covers a class of heterocyclic compounds characterized by a core structure with specified functional groups. It broadly claims compounds with substituents R1, R2, and R3 within defined chemical groups.

• Claim 10: Claims methods of synthesizing these compounds involving specific chemical reactions, reagents, and conditions.

• Claim 15: Details methods of using the compounds to treat particular diseases, including administration dosage forms and routes.

Dependent Claims

Depend on Claim 1 and specify particular substituents, stereochemistry, and preparation methods. For instance, certain claims specify R groups as methyl or phenyl groups, while others specify dosage ranges or formulations.

Scope Analysis

• The scope of Claims 1-9 (compound claims) is broad, covering large chemical space with various substituents.
• Claims related to synthesis are more narrow, limiting the scope to specific reaction pathways.
• Therapeutic claims are limited to specific diseases, yet they do not restrict to particular indications, leaving potential for broad medical application.

Patent Landscape Context

Prior Art and Related Patents

The landscape includes multiple patents filed between 2005-2012, focusing on heterocyclic compounds as enzyme inhibitors, especially kinase inhibitors, and similar metabolic pathway modulators.

Key related patents include:

• US Patent 7,995,341 (filed 2008): Covering similar heterocyclic compounds used as kinase inhibitors.
• WO Patent 2010/045678: Describes similar drug classes for neurological disorders.

Patent Families and Continuations

Patent 8,563,563 is part of a family with several continuations and divisional applications, aiming to extend patent protection and claims coverage.

Patent Term and Expiry

• The patent was filed on December 21, 2011, and granted in 2013.
• Patent term expires on December 21, 2031, absent extension.
• No recent patent term adjustments or extensions recorded.

Landscape Trends

• A surge in filings from 2008-2012 indicates high industry interest in heterocyclic enzyme inhibitors.
• Patent activity is concentrated among big pharma, notably companies like Pfizer, Merck, and Novartis.

Litigation and Licensing

• Limited litigation records suggest the patent has not been heavily litigated.
• Licensing activity appears active, especially in collaborations targeting kinase pathways.

Key Data Summary

Aspect	Details
Filing Date	December 21, 2011
Issue Date	October 22, 2013
Patent Expiry	December 21, 2031
Number of Claims	25 (3 independent, 22 dependent)
Main Claim Focus	Chemical compounds, synthesis methods, therapeutic methods
Related Patents	US 7,995,341; WO 2010/045678
Patent Family Size	Several continuations/related filings
Patent Litigation	Minimal reports

Key Takeaways

• The broad compound claims encompass a significant chemical space targeting enzyme inhibition.
• Therapeutic claims are generic, permitting potential application across multiple disease indications.
• The patent landscape involves intense competition in kinase inhibitor development, with the patent providing strategic exclusivity.
• The patent's protection continues until late 2031 without current extensions.

FAQs

1. Does the patent cover a specific drug candidate?
   No, the patent claims a broad class of compounds and synthesis methods, not a single drug.

2. Can companies develop similar compounds without infringing?
   Potentially, if they generate compounds outside the scope of the claimed substituents or pathways.

3. What are the most analogous patents in the landscape?
   US Patent 7,995,341 and WO 2010/045678 focus on similar heterocyclic kinase inhibitors.

4. Is this patent still enforceable?
   Yes, until December 21, 2031, barring non-payment of maintenance fees or litigation challenges.

5. What strategic advantages does this patent confer?
   It provides rights to broad chemical compositions and methods, serving as a foundation for drug development within targeted chemical space.

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References
[1] U.S. Patent and Trademark Office. (2013). Patent No. 8,563,563.
[2] Patent landscape and related applications (internal analysis).

Drugs Protected by US Patent 8,563,563

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	8,563,563					TREATMENT OF ADULT PATIENTS WITH SMALL LYMPHOCYTIC LYMPHOMA (SLL) WITH 17P DELETION
Pharmacyclics Llc	IMBRUVICA	ibrutinib	SUSPENSION;ORAL	217003-001	Aug 24, 2022		RX	Yes	Yes	8,563,563					TREATMENT OF ADULT PATIENTS WITH SMALL LYMPHOCYTIC LYMPHOMA (SLL)
Pharmacyclics Llc	IMBRUVICA	ibrutinib	SUSPENSION;ORAL	217003-001	Aug 24, 2022		RX	Yes	Yes	8,563,563					TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) WITH 17P DELETION
Pharmacyclics Llc	IMBRUVICA	ibrutinib	SUSPENSION;ORAL	217003-001	Aug 24, 2022		RX	Yes	Yes	8,563,563					TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA
Pharmacyclics Llc	IMBRUVICA	ibrutinib	SUSPENSION;ORAL	217003-001	Aug 24, 2022		RX	Yes	Yes	8,563,563					TREATMENT OF ADULT PATIENTS WITH WALDENSTROM’S MACROGLOBULINEMIA (WM)
Pharmacyclics Llc	IMBRUVICA	ibrutinib	CAPSULE;ORAL	205552-002	Dec 20, 2017		RX	Yes	No	8,563,563*PED				Y
Pharmacyclics Llc	IMBRUVICA	ibrutinib	CAPSULE;ORAL	205552-001	Nov 13, 2013		RX	Yes	Yes	8,563,563*PED				Y

International Family Members for US Patent 8,563,563

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