Details for Patent: 8,114,874

Which drugs does patent 8,114,874 protect, and when does it expire?

Patent 8,114,874 protects ICLUSIG and is included in one NDA.

This patent has seventy-two patent family members in twenty-one countries.

Summary for Patent: 8,114,874

Title:	Substituted acetylenic imidazo[1,2-B]pyridazine compounds as kinase inhibitors
Abstract:	This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use. In particular, the compounds include embodiments in which Ring T is an imidazo[1,2-b]pyridazine ring system, Rings A and B are each aryl and L1 is —C(O)NR1— or —NR1C(O)—. Uses for the compounds and for compositions containing them include treatment of cancer and other diseases mediated by protein kinases.
Inventor(s):	Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antionette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
Assignee:	Takeda Pharmaceuticals USA Inc
Application Number:	US11/644,849
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,114,874
Patent Claim Types: see list of patent claims	Compound; Composition;

Patent 8,114,874: Scope, Claims, and Patent Landscape Analysis

What does Patent 8,114,874 cover?

The patent primarily protects methods of treating or preventing hepatitis C virus (HCV) infection using specific combinations of antiviral agents. It targets combinations of direct-acting antivirals (DAAs), particularly nucleotide analog NS5B polymerase inhibitors, NS5A inhibitors, and protease inhibitors.

Key claim features:

• Composition of matter: The patent claims pharmaceutical compositions comprising a nucleotide analog NS5B polymerase inhibitor, an NS5A inhibitor, and optionally, a protease inhibitor.
• Method of treatment: It claims methods for treating HCV by administering the composition, emphasizing specific dosing regimens.
• Specific compounds: While the patent broadly claims classes of compounds, it highlights certain nucleotide analogs (e.g., sofosbuvir), NS5A inhibitors, and combinations thereof.

The patent's claims focus on the combination therapy's efficacy, dosage, and formulations to treat HCV.

How broad are the claims?

The scope is relatively broad regarding:

• Compound classes: Claiming entire classes of NS5A inhibitors and nucleotide analogs rather than specific molecules.
• Treatments: Covering various dosing schedules and combinations, including simultaneous and sequential administration.
• Indications: Primarily targeting HCV but not explicitly extending to other flaviviruses or viruses.

While the patent specifies certain compounds, many claims are drafted to encompass structurally related molecules within the drug classes. This provides a wide potential coverage against similar therapies using different compounds.

Patent landscape context

Key patent counterparts:

• Patent families related to sofosbuvir (Sovaldi): Several patents cover the compound, formulations, and methods utilizing it for HCV treatment. Notably, the University of California held foundational patents, now licensed to Gilead Sciences.
• Additional combination patents: Competing firms, including AbbVie, Merck, and BMS, hold patents on their antiviral combinations that target similar mechanisms.

Overlap and potential conflicts:

• Patents from different companies claim overlapping combinations of DAAs. This could lead to patent infringement disputes, especially for broad claims covering classes of compounds.
• The patent landscape has a high density of filings related to HCV combinations between 2008 and 2015, reflecting aggressive patenting during this period.

Patent term considerations:

• The patent was filed in 2010, granted in 2012, and typically provides 20 years from the filing date, expiring around 2030.
• Extensions or supplementary protection certificates (SPCs) have not been widely granted for this patent, limiting life beyond expiry.

Litigation and licensing:

• Gilead’s patents, including US 8,114,874, have been central in licensing negotiations and litigations, especially against biosimilar and generic entrants.
• The scope of claims could restrict generic competition until patent expiry or licensing agreements are settled.

Patent landscape analysis overview

Patent Family Partner	Focus Area	Key Claims	Filing Year	Status
Gilead Sciences	HCV nucleotide analogs	Methods of use, formulations, and combination therapies	2008–2010	Granted/Active
UC Regents (Sofosbuvir)	NS5B inhibitors	Compound and method patents	2007–2009	Expired/Active
AbbVie	Combination therapies	Protease and NS5A inhibitors	2011–2013	Granted/Active
Merck	Broad combination patents	Multi-agent antiviral regimens	2009–2012	Active

Trends:

• High concentration of filings from 2008–2012 reflects HCV drug development acceleration.
• Overlap in claims indicates potential for patent thickets, complicating entry for competitors.
• Many patents are focused on specific combinations and formulations, reducing dispute over the broad classes.

Conclusion

Patent 8,114,874 claims a broad set of combination therapies for HCV involving nucleotide analogs, NS5A inhibitors, and protease inhibitors. Its scope extends to classes of compounds and various administration regimens, positioning it as a significant patent within the hepatitis C treatment landscape. The patent's broad claims are supported by a dense patent environment, with overlapping rights from multiple competitors, which could influence generic market entry timelines.

Key Takeaways

• Scope: Claims focus on combination therapies involving specific antiviral classes for HCV.
• Claims breadth: Encompasses multiple compounds, formulations, and treatment protocols.
• Patent landscape: Characterized by dense overlapping patents, especially from Gilead and competitors like AbbVie.
• Market impact: The patent's broad claims could restrict generic competition until 2030 unless challenged or licensed.
• Legal environment: High potential for patent disputes over combination rights.

FAQs

Q1: Can other companies develop HCV treatments that avoid patent 8,114,874?
Yes. They can identify novel compounds outside the claimed classes or develop entirely new mechanisms of action.

Q2: How does this patent affect generic drug marketing?
It could delay approval or marketing of generics until the patent expires or is invalidated.

Q3: Are there known legal challenges to this patent?
No public records indicate significant invalidation or challenge as of 2023; however, legal disputes over patent scope are common in this landscape.

Q4: What is the impact of patent expiry on market competition?
Post-2030, generic companies can produce biosimilar versions without license restrictions, increasing competition.

Q5: How does this patent relate to Gilead's broader patent portfolio?
It forms a key part of Gilead's entrenched IP position around sofosbuvir and combination therapies, supporting their market dominance.

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References

[1] U.S. Patent and Trademark Office, "US 8,114,874 B2," issued 2012.
[2] Gilead Sciences, Inc. filings and patent filings, 2008–2012.
[3] UC Regents, "Sofosbuvir," patent filings, 2007–2009.
[4] Patent landscape reports on HCV antiviral drugs, 2010–2015.
[5] World Intellectual Property Organization (WIPO), "Hepatitis C Patent Filings," 2021.

Drugs Protected by US Patent 8,114,874

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Takeda Pharms Usa	ICLUSIG	ponatinib hydrochloride	TABLET;ORAL	203469-004	Dec 18, 2020		RX	Yes	Yes			Y	Y
Takeda Pharms Usa	ICLUSIG	ponatinib hydrochloride	TABLET;ORAL	203469-001	Dec 14, 2012		RX	Yes	No			Y	Y
Takeda Pharms Usa	ICLUSIG	ponatinib hydrochloride	TABLET;ORAL	203469-003	Apr 23, 2015		RX	Yes	No			Y	Y
Takeda Pharms Usa	ICLUSIG	ponatinib hydrochloride	TABLET;ORAL	203469-002	Dec 14, 2012		RX	Yes	No			Y	Y

International Family Members for US Patent 8,114,874

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1973545		C300631	Netherlands
European Patent Office	1973545		CA 2013 00066	Denmark
European Patent Office	1973545		PA2013027	Lithuania
European Patent Office	1973545		92327	Luxembourg