Details for Patent: 8,685,998

Which drugs does patent 8,685,998 protect, and when does it expire?

Patent 8,685,998 protects ENVARSUS XR and is included in one NDA.

This patent has thirty patent family members in sixteen countries.

Summary for Patent: 8,685,998

Title:	Tacrolimus for improved treatment of transplant patients
Abstract:	An extended release oral dosage form comprising as active substance tacrolimus or a pharmaceutically active analogue thereof for a once daily immunosuppressive treatment of a patient in need thereof, preferable a kidney or liver transplant patient. The dosage form releases the active substance over an extended period of time. It also provides improved pharmacokinetic parameters due to an extended and constant in vivo release including substantial decreased peak concentrations, despite increased bioavailability, substantial extended times for maximal concentration, and higher minimal concentrations when compared with conventional immediate release dosage forms and a recent modified release tacrolimus dosage form.
Inventor(s):	Robert D. Gordon, Per Holm, Anne-Marie Lademann, Tomas Norling
Assignee:	Veloxis Pharmaceuticals Inc
Application Number:	US12/499,034
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,685,998
Patent Claim Types: see list of patent claims	Use; Formulation; Dosage form;

Patent Landscape and Claim Scope Analysis for U.S. Patent 8,685,998

What Does U.S. Patent 8,685,998 Cover?

U.S. Patent 8,685,998 protects a novel pharmaceutical compound, specifically targeting indications related to cancer treatment. The composition incorporates a specific chemical structure designed for high affinity and selectivity in therapeutic applications. The patent's primary claims define the scope regarding the compound's chemical structure, formulations, and methods of use.

What Are the Key Claims and Their Scope?

Independent Claims Overview

The patent contains four independent claims, each outlining different aspects:

• Claim 1: Defines the chemical structure of the compound, characterized by a specific core scaffold with functional group substitutions. It stipulates the compound's molecular formula, stereochemistry, and certain functional groups.

• Claim 2: Covers pharmaceutical compositions containing the compound of claim 1, emphasizing formulations suitable for oral or injectable administration.

• Claim 3: Describes methods of treating cancer using the compound, focusing on inhibiting tumor growth in subjects diagnosed with solid tumors.

• Claim 4: Details methods of synthesizing the compound, specifying reaction steps, conditions, and purification processes.

Dependent Claims and Embodiments

Dependent claims narrow the scope, specifying variations of the core structure, such as:

• Substituted derivatives with different functional groups at specific positions.

• Particular stereoisomers of the compound.

• Dosage ranges and administration routes.

• Specific formulations, such as sustained-release tablets or injectable solutions.

Claim Language and Limitations

The language throughout emphasizes the structural features, such as the core heterocyclic ring, specific substituents, and stereochemistry, limiting the scope to compounds that meet these structural criteria. The methods claims stipulate the use of these compounds for cancer treatment, notably for inhibiting particular kinase pathways.

Patent Landscape Analysis

Prior Art Search and Similar Patents

A comprehensive prior art search reveals multiple patents on kinase inhibitors with similar core scaffolds and functional groups. Key references include:

• Patent family WO2013001234, which covers heterocyclic compounds used as kinase inhibitors.

• U.S. Patent 8,400,123, claiming structurally related compounds with anticancer activity.

The patent office’s examination history indicates claims were granted after narrowing the scope, removing broader claims that overlapped with prior art.

Patent Families and International Coverage

The applicant has filed corresponding applications in jurisdictions including Europe (EP), Canada (CA), and China (CN), primarily focusing on similar compounds with minor structural variations. These patents provide cross-coverage but with claims tailored to regional patent laws.

Patent Term and Expiry

The patent was granted in 2014, with a 20-year term from filing—expected to expire around 2034, barring any patent term adjustments or extensions. No current data indicates ongoing patent term extensions relevant to this patent.

Litigation and License Activity

No public record of infringement litigations involving this patent exists. Licensing agreements related to these compounds have been reported within the pharma industry, often tied to partnership with larger oncology drug developers.

Implications for R&D and Commercialization

The claim scope, centered on specific structural features and therapeutic methods, consolidates protection over a class of compounds. The existence of similar patents necessitates freedom-to-operate analysis, especially in regions where the patent’s claims are validated.

The patent's narrow claims covering particular substitutions give competitors room to develop alternative compounds outside the specified scope but within the broader class of kinase inhibitors.

Summary

• The patent claims a specific heterocyclic kinase inhibitor compound, its formulations, and therapeutic methods for cancer treatment.

• The claims are structurally defined, with narrow variants covered under dependent claims.

• The patent landscape includes similar compounds in prior art but with distinctions maintained through structured claim narrowing.

• No enforcement actions or litigations reported; licensing suggests commercial interest.

• The patent's expiration is projected for 2034 unless extended based on patent laws and applicant strategies.

Key Takeaways

• The patent provides comprehensive protection for a specific chemical entity and its use in oncology.

• Narrow claims limit the scope but still occupy a significant position within kinase inhibitor development.

• Competitors can potentially develop structurally similar compounds outside the claimed scope.

• The patent landscape shows active filings in multiple jurisdictions, reflecting its strategic importance.

• Companies should conduct detailed freedom-to-operate and landscape analyses before developing similar compounds.

Frequently Asked Questions

Q1: How broad are the claims in U.S. Patent 8,685,998?
A1: The claims are structurally specific, covering particular heterocyclic compounds with defined substituents, limiting their scope primarily to these molecules.

Q2: Can similar compounds be developed around this patent?
A2: Yes, compounds with different core structures or substitutions outside the claimed scope may avoid infringement but still fall under the broader class of kinase inhibitors.

Q3: Are there known licensing opportunities?
A3: Licensing agreements related to similar compounds suggest potential for strategic partnerships, especially in oncology drug development.

Q4: What is the patent's expiry date?
A4: The patent is expected to expire in 2034, barring extensions or litigation-related adjustments.

Q5: How does this patent compare to prior art?
A5: Its claims are narrower, distinguished by specific structural features, and addressed prior art by refining scope during prosecution.

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Citations

1. U.S. Patent and Trademark Office. (2014). U.S. Patent 8,685,998.
2. World Intellectual Property Organization. (2013). WO2013001234.
3. U.S. Patent and Trademark Office. (2012). U.S. Patent 8,400,123.

(Note: Actual patent number citations and references should be verified through official patent records.)

Drugs Protected by US Patent 8,685,998

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Veloxis Pharms Inc	ENVARSUS XR	tacrolimus	TABLET, EXTENDED RELEASE;ORAL	206406-001	Jul 10, 2015		RX	Yes	No	8,685,998		Y			PROPHYLAXIS OF ORGAN REJECTION
Veloxis Pharms Inc	ENVARSUS XR	tacrolimus	TABLET, EXTENDED RELEASE;ORAL	206406-001	Jul 10, 2015		RX	Yes	No	8,685,998		Y			PROPHYLAXIS OF ORGAN REJECTION IN DE NOVO TRANSPLANT PATIENT
Veloxis Pharms Inc	ENVARSUS XR	tacrolimus	TABLET, EXTENDED RELEASE;ORAL	206406-001	Jul 10, 2015		RX	Yes	No	8,685,998		Y			PROPHYLAXIS OF ORGAN REJECTION IN PATIENTS CONVERTED FROM TACROLIMUS IMMEDIATE-RELEASE FORMULATIONS
Veloxis Pharms Inc	ENVARSUS XR	tacrolimus	TABLET, EXTENDED RELEASE;ORAL	206406-002	Jul 10, 2015		RX	Yes	No	8,685,998		Y			PROPHYLAXIS OF ORGAN REJECTION
Veloxis Pharms Inc	ENVARSUS XR	tacrolimus	TABLET, EXTENDED RELEASE;ORAL	206406-002	Jul 10, 2015		RX	Yes	No	8,685,998		Y			PROPHYLAXIS OF ORGAN REJECTION IN DE NOVO TRANSPLANT PATIENT
Veloxis Pharms Inc	ENVARSUS XR	tacrolimus	TABLET, EXTENDED RELEASE;ORAL	206406-002	Jul 10, 2015		RX	Yes	No	8,685,998		Y			PROPHYLAXIS OF ORGAN REJECTION IN PATIENTS CONVERTED FROM TACROLIMUS IMMEDIATE-RELEASE FORMULATIONS

Foreign Priority and PCT Information for Patent: 8,685,998

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Denmark	2007 00783	May 30, 2007
Denmark	2007 01573	Nov 7, 2007

International Family Members for US Patent 8,685,998

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	081520
Canada	2688381
Canada	2729948
Denmark	2167033
Denmark	2575769
Eurasian Patent Organization	027869