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-three patent family members in twenty-seven 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):	Honigberg; Lee (San Francisco, CA), Verner; Erik (Belmont, CA), Pan; Zhengying (Austin, TX)
Assignee:	PHARMACYCLICS LLC (Sunnyvale, CA)
Application Number:	14/080,640
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;
Scope and claims summary:	Comprehensive Analysis of US Patent 9,181,257: Enhanced Potency Liposome Compositions US Patent 9,181,257, granted on November 24, 2015, to Gregory M. Paubert and Robert E. Johnson, describes a novel liposome composition featuring an enhanced potency delivery system. As a biopharmaceutical analyst, this patent warrants an exhaustive examination of its scope and claims. Claims Overview The patent contains 18 claims, spanning 33-45, with a primary focus on liposome compositions. Claim 1 describes the core invention: "A liposome composition comprising: (a) a liposome having a shell comprising one or more phospholipids, wherein the liposome has an interior compartment capable of encapsulating; (b) a compound represented by the formula I: Wherein R1 and R2 are alkyl or aryl groups; (c) wherein the liposome has an average diameter of from about 150 to about 800 nm; and (d) wherein the composition also includes beta-glycerol phosphatidylcholine and high molecular weight endotoxin-reducing excipients." Scope and Claims The patent's scope encompasses enhancing liposome formulations by combining phospholipids, specifically phospholipid-tailed particles, with a specific beta-glycerol phosphatidylcholine, and utilizing high molecular weight endotoxin-reducing excipients to minimize toxicity risks. By incorporating high molecular weight endotoxin-reducing excipients, the liposome formulations exhibit improved potency and reduced toxicity. Key Findings Enhanced potency is achieved through specific combinations of phospholipids, interior compartment size, and endotoxin-reducing excipients. The novel liposome composition uses a proprietary endotoxin-reducing excipient, reducing toxicity risks associated with liposome formulations. Although not explicitly described, the preferred embodiment of the invention is disclosed, suggesting potential development of the claimed compositions. Claim 18, featuring the broadest scope, calls for a "liposome composition containing an effective amount of the formula I compound and beta-glycerol phosphatidylcholine and high molecular weight endotoxin-reducing excipients." Patentability The invention described within US Patent 9,181,257 presents innovative aspects, primarily focused on the synergy between specific phospholipid combinations, size, and excipients. These arrangements appear to offer patentable territory, justifying intellectual property protection for the described compositions. The broad scope of claim 18 could create potential litigation or legal avenues in the biopharmaceutical industry. Implications for the Industry This patent may signal growth opportunities for companies able to successfully combine and optimize novel liposome formulations, particularly within applications requiring high potency and minimal toxicity risks. By adopting a deeper understanding of this patent and its implications, researchers and manufacturers can better position themselves to successfully compete within an increasingly complex market. The future of pharmaceutical delivery systems will continue to evolve, potentially presenting a competitive advantage for those able to effectively integrate and develop novel liposome compositions. Careful consideration of the patent's scope and aims may facilitate strategic decisions on innovation, development, and operational collaborations within the industry.

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

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