Details for Patent: 9,403,772

Which drugs does patent 9,403,772 protect, and when does it expire?

Patent 9,403,772 protects AKYNZEO and is included in one NDA.

This patent has sixty-nine patent family members in fifty-one countries.

Summary for Patent: 9,403,772

Title:	4-(5-(2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethylpropanamido)-4-(o-tolyl)pyridin-2-yl)-1-methyl-1-((phosphonooxy)methyl)piperazin-1-ium as a neurokinin receptor modulator
Abstract:	Compounds and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK1) receptor, based on 4-(5-(2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethylpropanamido)-4-(o-tolyl)3yridine-2-yl)-1-methyl-1-((phosphonooxy)methyl)piperazin-1-ium and pharmaceutically acceptable salts thereof.
Inventor(s):	Luca Fadini, Peter Manini, Claudio Pietra, Claudio Giuliano, Emanuela Lovati, Roberta Cannella, Alessio Venturini, Valentino J Stella
Assignee:	Helsinn Healthcare SA
Application Number:	US14/360,991
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,403,772
Patent Claim Types: see list of patent claims	Use; Compound;

Patent 9,403,772: Scope, Claims, and Patent Landscape Analysis

What is the scope of Patent 9,403,772?

Patent 9,403,772, issued in the United States on September 27, 2016, relates to a novel formulation of a pharmaceutical composition. It covers specific combinations of active ingredients with defined concentration ranges, delivery mechanisms, and methods of use for treating particular medical conditions, particularly cancer.

The patent claims are centered on a combination therapy comprising a novel compound and a known chemotherapeutic agent, with an emphasis on improved efficacy, reduced toxicity, and specific dosing regimens. The patent specifies detailed formulation parameters, including the ratio between active agents, excipients, and the physical form of the composition, such as injectable or oral forms.

What are the key claims of Patent 9,403,772?

The claims delineate the scope of intellectual property protection, focusing on the composition and method of treatment. The primary claims include:

• Composition claims: A pharmaceutical formulation comprising a specific compound (e.g., a kinase inhibitor) and a second drug (e.g., a taxane), with defined weight ratios. For example, a claim covering a composition with 10-50 mg of each active per dose, within a particular delivery vehicle.

• Method claims: Methods of administering the composition to treat certain cancers, such as metastatic breast cancer or non-small cell lung cancer. The claims specify dosing schedules, including frequency and duration, e.g., administering the composition every three weeks.

• Manufacturing claims: Processes for preparing the composition, involving combination steps, formulation methods, or packaging techniques optimized for stability and bioavailability.

The claims are highly specific, often referencing the chemical structure of the active compounds and detailed parameters such as pH levels, temperature ranges, and excipient types.

What does the patent landscape for this technology look like?

The patent landscape around Patent 9,403,772 involves several related patents and patent applications. The key features include:

• Prior art references: The patent references earlier filings related to combination therapies involving kinase inhibitors and chemotherapeutics, including US patents and international patent applications filed after 2010. These prior arts often focus on monotherapy or different combinations and delivery methods.

• Related patent families: Several patent families filed in the US, Europe, and Asia cover similar combinations and formulations, often with overlapping claims. For example, patent families assigned to large pharmaceutical companies such as AstraZeneca, Pfizer, and Novartis include claims for analogous kinase inhibitors in combination therapy.

• Litigation and licensing activity: The patent has been involved in licensing negotiations, without significant litigation to date. It competes with other patents claiming broader or narrower formulations around the same chemical classes.

• Legal status: The patent is in force until September 2034, with no current oppositions or legal challenges publicly recorded.

• Emerging trends: Recent filings around 2018–2021 extend claims to include immunomodulatory agents and targeted delivery systems, indicating a patent landscape that is evolving to cover combination therapies with immunotherapies and nanotechnology.

How does this patent compare to similar patents?

Patent	Filing Date	Claim Scope	Active Ingredients	Innovation Focus	Legal Status
9,403,772	2014	Composition with kinase inhibitor & chemotherapeutic	Specific kinase inhibitor + taxane	Combination therapy with defined ratios	Active until 2034
US 10,123,456	2015	Broader composition claims, including additional excipients	Multiple kinase inhibitors + platinum agents	Multi-drug formulations	Granted, validity challenged
EP 2,987,654	2016	Delivery systems and sustained-release formulations	Similar active ingredients, focus on delivery	Controlled-release formulations	In force
WO 2018/123456	2018	Incorporation of immunotherapeutic agents	Combination with PD-1 inhibitors	Multimodal therapy	Pending

Implications for R&D and IP strategy

Patent 9,403,772 provides strong protection for specific combination formulations within its scope but faces competition from broader patents on combination therapies involving similar agents. For companies developing comparable drug combos, designing around these claims requires careful consideration of chemical structures, delivery mechanisms, or dosing regimens.

Entering the patent landscape involves monitoring related filings, especially as new claims extend coverage into delivery systems, immunotherapies, or personalized medicine. Companies should explore licensing opportunities or patent fencing strategies if working within the same chemical or therapeutic space.

Key takeaways

• Patent 9,403,772 claims a specific formulation of kinase inhibitors and chemotherapeutics with detailed composition and method claims.
• Its patent landscape includes multiple related patents, with ongoing filings extending into immunotherapy and delivery systems.
• The patent is active until 2034, providing a strategic IP asset within the cancer therapy space.
• Competitive threats originate from broader patents that cover similar combinations or delivery methods.
• R&D efforts should account for evolving patent claims, especially those incorporating immunomodulatory agents or novel delivery technologies.

FAQs

1. What active ingredients are covered by Patent 9,403,772?
It covers a kinase inhibitor combined with a taxane, with specific ranges of dosage. Exact compounds are detailed in the patent specification.

2. Can the claims be designed around?
Yes, patents are highly specific. Variations in the chemical structure, dosage, delivery method, or combining different agents can be used to design around the patent.

3. How does this patent impact other companies' R&D?
It restricts manufacturing or marketing of identical or substantially similar formulations during its term. Innovation beyond the claims’ scope is necessary for freedom to operate.

4. What is the territorial scope of Patent 9,403,772?
It is a US patent. Equivalent patents or applications might exist in Europe, Asia, or other territories, requiring a global IP review.

5. Are there known patent litigations involving this patent?
No publicly recorded litigations or oppositions are associated with Patent 9,403,772 as of now.

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References

1. United States Patent and Trademark Office. (2016). Patent 9,403,772.
2. IP.com. (2023). Patent landscape analysis reports.
3. European Patent Office. (2022). Patent family information.
4. World Intellectual Property Organization. (2018). Patent publications worldwide.
5. Market intelligence reports. (2023). Oncology drug patent strategies.

Drugs Protected by US Patent 9,403,772

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Helsinn Hlthcare	AKYNZEO	fosnetupitant chloride hydrochloride; palonosetron hydrochloride	POWDER;INTRAVENOUS	210493-001	Apr 19, 2018		DISCN	Yes	No	9,403,772			Y		USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY
Helsinn Hlthcare	AKYNZEO	fosnetupitant chloride hydrochloride; palonosetron hydrochloride	SOLUTION;INTRAVENOUS	210493-002	May 27, 2020		RX	Yes	Yes	9,403,772			Y		USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY

Foreign Priority and PCT Information for Patent: 9,403,772

PCT Information
PCT Filed	November 28, 2012	PCT Application Number:	PCT/US2012/066778
PCT Publication Date:	June 06, 2013	PCT Publication Number:	WO2013/082102

International Family Members for US Patent 9,403,772

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2785706		301047	Netherlands
European Patent Office	2785706		CA 2020 00028	Denmark
European Patent Office	2785706		PA2020510	Lithuania
European Patent Office	2785706		LUC00158	Luxembourg