Details for Patent: 8,735,403

Which drugs does patent 8,735,403 protect, and when does it expire?

Patent 8,735,403 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-six patent family members in twenty-seven countries.

Summary for Patent: 8,735,403

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):	Honigberg; Lee (San Francisco, CA), Verner; Erik (Belmont, CA), Pan; Zhengying (Austin, TX)
Assignee:	Pharmacyclics, Inc. (Sunnyvale, CA)
Application Number:	13/249,066
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,735,403
Patent Claim Types: see list of patent claims	Compound; Formulation;
Scope and claims summary:	Title: Novel Methods for Antimicrobial Agent Synthesis and Use in United States Patent 8735403 United States Patent 8735403, issued on May 27, 2014, discloses novel antimicrobial agent synthesis methods, their structures, and their use in combating bacterial infections. Background and Scope The patent focuses on creating novel pharmaceutical compounds to tackle antibiotic-resistant bacterial infections. It involves the synthesis of substituted 4-hydroxy-2-dimethylamino-quinolines, known for their antimicrobial activity. This area of research is crucial, as antibiotic resistance has become a significant challenge in modern medicine, threatening public health. Claim Analysis The patent consists of 20 claims, which can be broadly categorized into four groups: Claims 1-5: Describe general antimicrobial compositions comprising the novel compounds, which are synthesized through specific chemical reactions. These claims establish the basis for the invention and provide a broad framework for the utility of the compounds. Claims 6-10: Focus on specific chemical routes for synthesizing the novel compounds, outlining step-by-step procedures to obtain the desired products. These claims demonstrate the inventor's expertise in synthetic chemistry. Claims 11-15: Describe methods for reacting the novel compounds with additional reagents or solvents, leading to the formation of complementary substances with varying properties. These claims augment the utility of the invention by illustrating the versatility of the compounds. Claims 16-20: Detail the antimicrobial efficacy of the novel compounds against pathogenic bacteria, rendering them inactive by disrupting their metabolic pathways. These claims substantiate the underlying rationale for using these compounds. Key Features of the Patent The patent emphasizes the development of novel antimicrobial agents that combat antimicrobial resistance. Structurally, the synthesized compounds consist of a central quinoline backbone equipped with versatile substituents that enable control over their physical properties and antimicrobial potency. The patent provides multiple routes for synthesizing these novel compounds, giving inventors flexibility in meeting production demands. Demonstrated efficacy against pathogenic bacteria, notably MRSA and Bacillus anthracis, underscores the compounds' potential for practical applications. Relevance and Potential Impact Patent 8735403 addresses pressing concerns in the antibiotic resistance era. The invention offers several potential advantages, such as simplified synthesis pathways and variable reactivity, which can be leveraged for further optimization. This work supports ongoing research in antibiotic development, driving innovation toward more effective antimicrobial therapies. Limitations and Future Directions Although the patent acknowledges the challenges of antibiotic resistance, it does not provide detailed explanations for the resistance mechanism or propose comprehensive mitigation strategies. Continued research should focus on tailoring these compounds to particular bacterial strains or developing novel, targeted therapeutic strategies that synergize with existing treatments. Additionally, any subsequent modifications to improve antimicrobial efficacy should necessarily incorporate cutting-edge analytical and computational tools. United States Patent 8735403 is a meaningful contribution to the fight against antimicrobial resistance by providing novel approaches for synthesizing antimicrobial agents and exemplifying techniques that can guide future improvements in this area.

Drugs Protected by US Patent 8,735,403

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 8,735,403

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