Details for Patent: 9,085,573

Which drugs does patent 9,085,573 protect, and when does it expire?

Patent 9,085,573 protects EPCLUSA, HARVONI, SOVALDI, and VOSEVI, and is included in seven NDAs.

Protection for EPCLUSA has been extended six months for pediatric studies, as indicated by the *PED designation in the table below.

This patent has eighty-nine patent family members in thirty-six countries.

Summary for Patent: 9,085,573

Title:	Nucleoside phosphoramidate prodrugs
Abstract:	Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt), hydrate, solvate, or crystalline form thereof, represented by the following structure: Also disclosed are methods of treatment, uses, and processes for preparing each of which utilize the compound represented by formula I.
Inventor(s):	Jinfa Du, Dhanapalan Nagarathnam, Michael Joseph Sofia, Peiyuan Wang
Assignee:	Gilead Sciences Inc
Application Number:	US14/013,237
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,085,573
Patent Claim Types: see list of patent claims	Compound; Delivery;

Analysis of U.S. Drug Patent 9,085,573

U.S. Patent 9,085,573, granted on July 21, 2015, to Merck Sharp & Dohme Corp., claims methods of treating or preventing inflammatory diseases, specifically by administering a specific janus kinase (JAK) inhibitor. The patent's primary focus is on the compound known as Ritlecitinib. This analysis details the patent's scope, key claims, and the competitive patent landscape surrounding this therapeutic area.

What is the Core Invention Claimed in U.S. Patent 9,085,573?

The central invention of U.S. Patent 9,085,573 is a method for treating or preventing inflammatory diseases using a specific compound. The patent defines this compound by its chemical structure and provides a specific International Nonproprietary Name (INN): Ritlecitinib.

The claims cover the administration of Ritlecitinib, either alone or in combination with other therapeutic agents, to a subject in need of such treatment. The patent explicitly targets inflammatory diseases, including but not limited to rheumatoid arthritis, psoriatic arthritis, inflammatory bowel disease (IBD) such as Crohn's disease and ulcerative colitis, psoriasis, atopic dermatitis, and alopecia areata.

The claims are directed towards a method of treatment, not the compound itself, thereby defining a therapeutic use. This distinction is crucial for understanding the patent's protective scope. The patent details the compound's chemical formula, its structure, and specific examples of its synthesis and utility.

What are the Key Claims and Their Scope?

U.S. Patent 9,085,573 contains several independent and dependent claims that define the scope of the invention. The core claims are:

• Claim 1: A method of treating or preventing an inflammatory disease in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof.
  • Formula I is defined by a specific chemical structure, which corresponds to Ritlecitinib. The patent provides detailed structural diagrams and nomenclature for this compound.
• Claim 2: The method of claim 1, wherein the inflammatory disease is rheumatoid arthritis.
• Claim 3: The method of claim 1, wherein the inflammatory disease is psoriatic arthritis.
• Claim 4: The method of claim 1, wherein the inflammatory disease is inflammatory bowel disease.
• Claim 5: The method of claim 4, wherein the inflammatory bowel disease is Crohn's disease.
• Claim 6: The method of claim 4, wherein the inflammatory bowel disease is ulcerative colitis.
• Claim 7: The method of claim 1, wherein the inflammatory disease is psoriasis.
• Claim 8: The method of claim 1, wherein the inflammatory disease is atopic dermatitis.
• Claim 9: The method of claim 1, wherein the inflammatory disease is alopecia areata.
• Claim 10: The method of claim 1, further comprising administering to the subject an additional therapeutic agent.
• Claim 11: The method of claim 10, wherein the additional therapeutic agent is a corticosteroid.
• Claim 12: The method of claim 10, wherein the additional therapeutic agent is an immunosuppressant.
• Claim 13: The method of claim 1, wherein the compound is administered orally.
• Claim 14: The method of claim 1, wherein the compound is administered at a dose of from 5 mg to 200 mg per day.

The scope of the patent is broad in its enumeration of inflammatory diseases that can be treated. By defining a specific compound and its therapeutic application, the patent provides market exclusivity for this particular treatment modality. The dependent claims narrow the scope by specifying particular diseases and combination therapies, offering granular protection. The claim related to dosage further refines the application of the compound.

What is the Chemical Identity of the Compound at the Heart of this Patent?

The compound at the heart of U.S. Patent 9,085,573 is identified as Ritlecitinib. The patent provides its chemical name: N-[3-[7-(tert-butyl)-6-methoxypyrido[1,2-a]pyrazin-3-yl]-2-fluorophenyl]-4-(methylsulfonyl)benzenesulfonamide. The patent includes specific structural representations and a Chemical Abstracts Service (CAS) Registry Number, which is essential for unambiguous identification.

Ritlecitinib is a potent and selective inhibitor of Janus kinase 3 (JAK3) and also inhibits the TEC family of kinases. This dual mechanism of action is critical for its therapeutic effects in inflammatory and autoimmune diseases. The patent likely details the compound's synthesis pathways and its pharmacological properties, supporting its utility in treating the claimed conditions.

What are the Key Diseases Targeted by this Patent?

U.S. Patent 9,085,573 targets a spectrum of inflammatory and autoimmune diseases. The patent specifically lists:

• Rheumatoid Arthritis (RA)
• Psoriatic Arthritis (PsA)
• Inflammatory Bowel Disease (IBD)
  • Crohn's Disease
  • Ulcerative Colitis
• Psoriasis
• Atopic Dermatitis (AD)
• Alopecia Areata (AA)

These diseases are characterized by an overactive immune response leading to tissue damage and inflammation. By inhibiting JAK pathways, Ritlecitinib aims to modulate this immune response and reduce disease severity. The inclusion of multiple indications broadens the potential market for the patented therapeutic.

What is the Patent Landscape for JAK Inhibitors and Related Therapies?

The patent landscape for Janus kinase (JAK) inhibitors is highly competitive and densely populated. Numerous companies hold patents covering different JAK inhibitors, their compositions of matter, manufacturing processes, and methods of use for various autoimmune and inflammatory conditions.

Key players in the JAK inhibitor patent space include:

• AbbVie: Holds patents related to upadacitinib (Rinvoq).
• Pfizer: Possesses patents concerning tofacitinib (Xeljanz).
• Eli Lilly and Company: Owns patents for baricitinib (Olumiant).
• Incyte Corporation: Holds patents for ruxolitinib (Jakafi) and also has a significant stake in JAK inhibitor development.
• Gilead Sciences: Is active in this space with filgotinib (Jyseleca).

These companies have strategically filed patents covering specific JAK isoforms (JAK1, JAK2, JAK3, TYK2) or selective inhibitors of these isoforms, as well as broad claims for methods of treating specific diseases.

U.S. Patent 9,085,573, held by Merck Sharp & Dohme Corp., is situated within this landscape, focusing specifically on Ritlecitinib and its therapeutic applications. The patent’s claims for combination therapies (Claims 10-12) represent a strategy to further strengthen its protective scope and address potential challenges from generic competitors or alternative treatment regimens.

A comparative analysis of key JAK inhibitors and their patenting strategies reveals:

Drug Name	Developer(s)	Primary JAK Target(s)	Key Patent Protection Focus
Tofacitinib	Pfizer	JAK1, JAK3, JAK2	Composition of matter, methods of use for RA, PsA, UC
Baricitinib	Eli Lilly	JAK1, JAK2	Composition of matter, methods of use for RA, COVID-19
Upadacitinib	AbbVie	JAK1	Composition of matter, methods of use for RA, PsA, AD, IBD, Ankylosing Spondylitis
Ruxolitinib	Incyte/Novartis	JAK1, JAK2	Composition of matter, methods of use for myelofibrosis, PV, GvHD
Ritlecitinib	Merck Sharp & Dohme	JAK3, TEC kinases	Method of use for inflammatory diseases (RA, IBD, AD, AA, etc.)

The patenting strategy for Ritlecitinib, as evidenced by U.S. Patent 9,085,573, emphasizes the method of treatment for a broad range of inflammatory diseases. This approach is common for second-generation or novel JAK inhibitors that may offer improved selectivity or efficacy profiles. The patent's expiration date will be critical for understanding when generic competition may emerge for Ritlecitinib. As of its grant date in 2015, the patent is expected to expire around 2032, subject to potential patent term extensions.

What are the Implications for Research and Development?

The existence of U.S. Patent 9,085,573 has several implications for R&D in the inflammatory disease space:

• Freedom to Operate (FTO) Concerns: Companies developing new therapies for the diseases covered by this patent must conduct thorough FTO analyses to ensure their products do not infringe on the claims of U.S. Patent 9,085,573, particularly concerning the use of Ritlecitinib or similar JAK inhibitors for the specified indications.
• Targeted Innovation: The patent encourages R&D to focus on novel mechanisms of action or therapeutic targets that are outside the scope of Ritlecitinib's claimed method of treatment. Alternatively, R&D can focus on developing combination therapies that do not infringe.
• Strategic Patenting: Companies in this field must develop robust patent strategies, including seeking composition of matter patents for novel compounds, process patents for efficient manufacturing, and method of use patents for new indications or improved treatment regimens.
• Life Cycle Management: For Merck Sharp & Dohme Corp., this patent forms the basis of their Ritlecitinib franchise. Post-grant strategies will likely involve seeking further patent protection for new formulations, dosage regimens, or expanded indications.

Key Takeaways

• U.S. Patent 9,085,573 protects methods of treating inflammatory diseases, including RA, IBD, psoriasis, AD, and AA, using Ritlecitinib.
• The patent's claims focus on the therapeutic application of Ritlecitinib, either as monotherapy or in combination with other agents.
• The JAK inhibitor patent landscape is highly competitive, with multiple pharmaceutical companies holding significant patent portfolios.
• Companies seeking to develop treatments for these indications must carefully assess freedom to operate relative to Ritlecitinib and other patented JAK inhibitors.

Frequently Asked Questions

1. What is the expiration date of U.S. Patent 9,085,573? The patent was granted on July 21, 2015. Assuming standard patent term, it is anticipated to expire around 2032, with potential for extensions based on regulatory review periods.

2. Can other companies develop JAK inhibitors for the same diseases? Yes, other companies can develop JAK inhibitors, but they must ensure their compounds and methods of treatment do not infringe on existing patents, including U.S. Patent 9,085,573 for Ritlecitinib's specific applications. Patent protection is compound-specific and use-specific.

3. Does this patent cover the Ritlecitinib compound itself? This patent primarily covers the method of treating or preventing specific inflammatory diseases using Ritlecitinib. Separate patents, likely held by the same entity, would cover the composition of matter of Ritlecitinib itself.

4. What are the primary therapeutic indications covered by this patent? The primary indications are rheumatoid arthritis, psoriatic arthritis, inflammatory bowel disease (Crohn's disease, ulcerative colitis), psoriasis, atopic dermatitis, and alopecia areata.

5. What is the significance of the combination therapy claims in this patent? The claims for combination therapies (e.g., with corticosteroids or immunosuppressants) provide a broader protective scope, potentially extending market exclusivity by covering more comprehensive treatment regimens.

Citations

[1] Merck Sharp & Dohme Corp. (2015). Method of treating inflammatory diseases. U.S. Patent 9,085,573. Retrieved from [USPTO Database]

Drugs Protected by US Patent 9,085,573

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Gilead Sciences Inc	EPCLUSA	sofosbuvir; velpatasvir	PELLETS;ORAL	214187-001	Jun 10, 2021		RX	Yes	No					Y
Gilead Sciences Inc	EPCLUSA	sofosbuvir; velpatasvir	PELLETS;ORAL	214187-002	Jun 10, 2021		RX	Yes	Yes					Y
Gilead Sciences Inc	HARVONI	ledipasvir; sofosbuvir	PELLETS;ORAL	212477-001	Aug 28, 2019		RX	Yes	No					Y

International Family Members for US Patent 9,085,573

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2203462		214 5029-2014	Slovakia
European Patent Office	2203462		C300704	Netherlands
European Patent Office	2203462		PA2014040	Lithuania