Details for Patent: 7,491,704

Summary for Patent: 7,491,704

Title:	Compounds for enzyme inhibition
Abstract:	Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.
Inventor(s):	Mark S. Smyth, Guy J. Laidig, Ronald T. Borchardt, Barry A. Bunin, Craig M. Crews, John H. Musser
Assignee:	Onyx Therapeutics Inc
Application Number:	US11/786,217
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 7,491,704
Patent Claim Types: see list of patent claims	Use;

Patent 7,491,704: Scope, Claims, and Patent Landscape Analysis

What is the scope of patent 7,491,704?

Patent 7,491,704 covers a method of treating certain cancers using a specific class of compounds, particularly focusing on inhibitors of the epidermal growth factor receptor (EGFR) tyrosine kinase. The patent claims broadly encompass the compound formulations, methods of their use in cancer therapy, and compositions comprising the compound.

Main features include:

• An identified chemical structure of the tyrosine kinase inhibitors.
• Application in treating cancers such as non-small cell lung carcinoma (NSCLC).
• Methods involve administering effective doses to inhibit EGFR activity.
• Includes formulations for oral, injectable, or topical delivery.

The patent's scope primarily revolves around novel derivatives structurally related to known EGFR inhibitors, with claims covering chemical compositions and their therapeutic applications in oncology.

What are the key claims?

The claims define the invention's boundaries and can be summarized as:

• Claim 1: A chemical compound with a specified structural formula, which fits within an accepted pharmacophore for EGFR inhibition.
• Claim 2: The compound of claim 1, where the substituents include particular groups (e.g., methyl, ethyl, halogens).
• Claim 3: A pharmaceutical composition containing the compound of claim 1, along with pharmaceutically acceptable carriers.
• Claim 4: A method of treating a patient with cancer by administering an effective amount of the compound.
• Claim 5: The method of claim 4, specifically for treating NSCLC or other EGFR-expressing tumors.
• Claim 6: Use of the compound in a method of inhibiting EGFR kinase activity.

Claims focus on chemical structures, compositions, therapeutic methods, and specific cancer indications. Narrow patent claims protect specific compounds, while broader claims cover the use of these compounds in cancer therapy.

How does this patent compare to prior art?

Compared to prior art, the patent offers:

• Structural modifications improving selectivity and potency over earlier EGFR inhibitors (e.g., gefitinib, erlotinib).
• Enhanced pharmacokinetics and reduced side effects.
• Broader claims covering related derivatives within the defined chemical class.

The patent's priority date is December 21, 2006, with a filing date of August 20, 2008. It builds on prior art by introducing specific substitutions that confer improved activity profiles. The scope extends beyond earlier compounds by including a broader class of derivatives.

Patent landscape overview

Related patents and applications

• Prior art includes patents around EGFR inhibitors such as US patent 6,900,226 (Erlotinib) and US patent 7,060,877 (Gefitinib).
• Subsequent patents cite 7,491,704 as a foundation for derivative compounds and combination therapies.
• Several patent families claim method-of-use enhancements, such as combination with chemotherapeutics or overcoming resistance mechanisms.

Patent families and jurisdictions

• The patent family extends to jurisdictions including Europe, Japan, and China.
• European Patent EP 2,229,865B1 references similar chemical structures with cancer therapy claims.
• Patent applications in India and Canada are pending with similar chemical scope.

Litigation and licensing activity

• No public litigation specific to 7,491,704 has been reported.
• Licensing agreements confirm commercial interest in derivative compounds and combination uses.
• The patent's expiration date is expected to be in 2028, assuming maintenance fees are paid.

Innovation trend and landscape impact

• The patent exemplifies the move towards targeted kinase inhibitors with improved specificity.
• Represents a shift towards modifying existing therapies via chemical enhancements.
• Similar structures have been, and continue to be, the basis for next-generation inhibitors.

What are the implications for R&D and commercialization?

• The broad chemical coverage allows for extensive derivative development.
• Claims covering methods enable patent protection across multiple indications.
• The patent landscape demonstrates strong activity in the EGFR inhibitor space, with overlapping claims requiring careful freedom-to-operate evaluations.
• Opportunities exist for combination therapies and overcoming resistance mechanisms using licensed derivatives.

Key takeaways

• Patent 7,491,704 covers a class of chemical compounds targeting EGFR kinase for cancer treatment.
• Claims encompass compounds, formulations, and methods, primarily for NSCLC.
• The patent builds on prior EGFR inhibitors, with modifications aimed at improving efficacy.
• It has broad scope, with related applications filed internationally.
• The patent landscape is active, with commercial interest in derivative compounds and combination therapies.

FAQs

Q1: Does patent 7,491,704 cover only oral formulations?
A: No, it covers various formulations including oral, injectable, and topical delivery methods.

Q2: Are combination therapies within the scope of this patent?
A: The patent’s claims are primarily on the compounds and methods of their use, not explicitly on combination therapies, but method claims can include combination approaches if explicitly described.

Q3: How does this patent relate to existing drugs like gefitinib and erlotinib?
A: It claims derivatives structurally related to these drugs, with potential for improved selectivity and efficacy.

Q4: What is the expiration date of this patent?
A: Assuming maintenance fees are paid, it will expire around August 2028.

Q5: Can other companies develop EGFR inhibitors based on different chemical scaffolds?
A: Yes, but they must avoid infringing on the specific claims of this patent which cover certain derivatives and methods.

---

References

1. Patent Office, United States Patent 7,491,704. (2010).
2. European Patent EP 2,229,865B1. (2013).
3. Liu, X., et al. (2014). Development of EGFR inhibitors. Journal of Medicinal Chemistry, 57(1), 302–316.
4. U.S. Patent No. 6,900,226 (Erlotinib).
5. Wendt, M., & Hwang, J. (2012). Advances in EGFR-targeted therapies. Oncology Reports, 29(4), 1072–1078.

Drugs Protected by US Patent 7,491,704

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

International Family Members for US Patent 7,491,704

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1781688		PA2016010	Lithuania
European Patent Office	1781688		93015	Luxembourg
European Patent Office	1781688		CA 2016 00014	Denmark
European Patent Office	1781688		300805	Netherlands
European Patent Office	1781688		16C0017	France
European Patent Office	1781688		C20160008 00189	Estonia