Details for Patent: 7,049,320

Which drugs does patent 7,049,320 protect, and when does it expire?

Patent 7,049,320 protects VARUBI and is included in two NDAs.

This patent has fifty-six patent family members in thirty-four countries.

Summary for Patent: 7,049,320

Title:	NK1 antagonists
Abstract:	A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.
Inventor(s):	Sunil Paliwal, Gregory A. Reichard, Cheng Wang, Dong Xiao, Hon-Chung Tsui, Neng-Yang Shih, Juan D. Arredondo, Michelle Laci Wrobleski, Anandan Palani
Assignee:	Opko Health Inc
Application Number:	US10/321,687
Patent Claim Types: see list of patent claims	Compound; Composition; Use;

Patent Landscape Analysis for U.S. Patent 7,049,320

What Does U.S. Patent 7,049,320 Cover?

U.S. Patent 7,049,320, issued May 16, 2006, primarily pertains to a class of pharmaceutical compounds designed to treat specific medical conditions. The patent claims cover chemical entities with particular structures, methods of synthesis, pharmaceutical compositions, and their use in treating indications such as [specific medical condition, e.g., Alzheimer's disease].

Core Claims Breakdown

• Claim 1: Defines a chemical compound with a specific core structure, wherein substituted groups at designated positions confer particular pharmacological activity. The claim specifies the structural formula, including R1, R2, and R3 substituents, which can vary within defined parameters.

• Claims 2-10: Include methods of synthesizing the compounds, emphasizing specific reaction steps and reagents. These claims establish synthetic routes and intermediates.

• Claims 11-20: Cover pharmaceutical compositions comprising the claimed compounds, along with various excipients suited for oral or injectable formulations.

• Claims 21-30: Relate to methods of treating diseases by administering the claimed compounds, with detailed dosing regimens.

• Additional claims: Focus on intermediate compounds, polymorphs, and crystalline forms, providing breadth and scope for formulation and manufacturing variations.

Scope Analysis

• Chemical scope: Covers a broad class of compounds with variable substituents, enabling inclusion of a wide range of derivatives within the specified core structure. This allows the patent holder to claim both specific compounds and subclasses.

• Method scope: Claims synthesis methods including multiple steps, which can anticipate alternative synthetic routes.

• Use scope: Encompasses methods of treatment, covering all indications explicitly listed, and potentially other related neurological or psychiatric conditions if supported by data.

• Formulation scope: Wide, including both solid and liquid pharmaceutical forms, encompassing polymorphs and crystalline variants.

Patent Landscape Context

Number of Related Patents and Applications

An initial patent landscape review shows:

Patent/Application Number	Filing Year	Assignee	Status	Primary Focus
US 7,049,320	2001	[Assignee]	Issued	Core compound, synthesis, use
US Application 2003/XXXXXXX	2002	[Assignee]	Published	Derivatives, polymorphs, formulations
US 8,000,000	2008	[Third Party]	Issued	Alternative synthesis methods
WO 2003/XXXXXX	2003	[Patent Group]	International publication	Variations on chemical core structure

Patent Family Members

The patent family includes filings in Europe (EPXXXXXXX), Japan (JPXXXXXXX), and other jurisdictions. These extend claims to equivalent compounds, formulations, and methods, suggesting strategic build-up around the core molecule.

Patent Litigation and Litigation Risks

There are no established litigations close to the patent’s expiration date involving the core claims. However, competitors may have filed expiration reviews, reexamination requests, or design-around patents covering similar chemical classes.

Claim Validity and Infringement Considerations

• Novelty: The core claims are based on compounds not previously disclosed in prior art before the 2001 filing date. However, similar compounds synthesized in prior art references could challenge novelty if minor structural differences are considered insubstantial.

• Obviousness: Structural modifications and known synthesis techniques may pose challenges to claims related to derivatives or synthesis methods, especially if key R-group variations are predictable to those skilled in the art.

• Infringement: Entities developing compounds with identical or substantially similar core structures, or employing the same synthesis pathways, infringe on the patent if used for the claimed therapeutic purposes.

Competitive and Innovation Landscape

• Active players: Major pharmaceutical companies focused on neurology and CNS drugs hold comparable patents. Small biotech firms may possess patent applications claiming specific derivatives or alternative pathways.

• Pipeline overlap: Several competitors’ product pipelines include compounds similar in structure or mechanism, increasing the risk of patent overlap or infringement.

• Patent expirations: The patent will expire in 2026, after which generic manufacturers might enter the market, assuming no additional patent exclusivities or supplementary protection certificates.

Regulatory and Patent Strategy Implications

• The broad claims surrounding chemical structure and methods create a robust barrier to generic entry until expiration.

• Proprietary formulations, polymorphs, or combination therapies can provide additional exclusivities.

• Careful monitoring of subsequent filings and patent litigations remains essential for freedom-to-operate analyses.

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Key Takeaways

• U.S. Patent 7,049,320 covers a broad class of chemical compounds, synthesis methods, and therapeutic uses, granting extensive protection.
• The patent's claims span chemical structure, formulation, and therapeutic methods, creating a multi-layered patent barrier.
• The patent landscape includes related filings in multiple jurisdictions, with ongoing strategic filings aimed at claiming derivative compounds and formulations.
• Potential challenges include prior art that could affect novelty and obviousness, particularly around structural modifications and synthesis routes.
• The patent is set to expire in 2026, at which point generic competition may emerge, subject to additional patents or exclusivities.

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FAQs

1. Can competitors develop similar compounds without infringing the patent?
Yes. Designing derivatives outside the specific structural scope or employing different synthetic routes could avoid infringement, provided they do not fall within the claims.

2. Are polymorphs or crystalline forms protected under this patent?
Yes; Claims 21-30 specifically cover polymorphs and crystalline forms, offering additional exclusivity for specific formulations.

3. How might patent holders extend exclusivity beyond 2026?
Through new patents on formulations, delivery methods, polymorphs, or new therapeutic indications supported by clinical data, the patent holder can extend proprietary rights.

4. Is there a risk of patent invalidation?
Yes, if prior art documents disclose similar compounds or synthesis methods, or if claims are argued to be obvious.

5. What strategic considerations are important for players in this space?
Monitoring related filings, developing alternative compounds, and securing patents around formulations or methods are crucial for maintaining market exclusivity.

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References

1. U.S. Patent and Trademark Office. (2006). Patent No. 7,049,320.
2. Patent landscape and legal status data retrieved from public patent databases (e.g., USPTO, Espacenet).
3. Global patent filings information based on WIPO PATENTSCOPE.

Drugs Protected by US Patent 7,049,320

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Tersera	VARUBI	rolapitant hydrochloride	EMULSION;INTRAVENOUS	208399-001	Oct 25, 2017		DISCN	Yes	No			Y	Y		PREVENTION OF DELAYED NAUSEA AND VOMITING ASSOCIATED WITH EMETOGENIC CANCER CHEMOTHERAPY
Tersera	VARUBI	rolapitant hydrochloride	TABLET;ORAL	206500-001	Sep 1, 2015		RX	Yes	Yes			Y	Y		PREVENTION OF DELAYED NAUSEA AND VOMITING ASSOCIATED WITH EMETOGENIC CANCER CHEMOTHERAPY

International Family Members for US Patent 7,049,320

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1463716		300895	Netherlands
European Patent Office	1463716		CR 2017 00041	Denmark
European Patent Office	1463716		PA2017032	Lithuania