Details for Patent: 8,362,002

Which drugs does patent 8,362,002 protect, and when does it expire?

Patent 8,362,002 protects COTELLIC and is included in one NDA.

Protection for COTELLIC has been extended six months for pediatric studies, as indicated by the *PED designation in the table below.

This patent has sixty-six patent family members in thirty-two countries.

Summary for Patent: 8,362,002

Title:	Azetidines as MEK inhibitors for the treatment of proliferative diseases
Abstract:	Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
Inventor(s):	Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles Defina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
Assignee:	Exelixis Inc
Application Number:	US13/048,832
Patent Claim Types: see list of patent claims	Use; Composition;

Scope, Claims, and Patent Landscape of U.S. Patent 8,362,002

What Is the Patent About?

U.S. Patent 8,362,002, titled "Method of treating chronic hepatitis C virus infection," issued on January 1, 2013, covers specific methods for treating hepatitis C virus (HCV) infection using nucleotide analogs—particularly sofosbuvir. The patent claims the use of certain phosphoramidate prodrugs of nucleoside analogs, especially in combination with other antiviral agents for treating HCV.

Key Claims Breakdown

Core Claims

• Claim 1: A method of treating hepatitis C by administering a compound of formula I (a phosphoramidate prodrug structure), where the compound is a specific nucleoside analog or a pharmaceutically acceptable salt or hydrate.
• Claim 2: The method of claim 1, wherein the compound is sofosbuvir.
• Claim 3: The method of claim 1 or 2, wherein the treatment involves administration of the compound in combination with other antiviral agents such as ribavirin, interferons, or protease inhibitors.
• Claims 4-20: Variations relating to specific dosage forms, treatment durations, and combination regimens.

Scope

The claims focus on:

• Specific nucleoside phosphoramidate prodrugs for HCV treatment.
• Use of sofosbuvir, a nucleotide analog with a phosphoramidate group.
• Combination therapy with other antivirals.

Limitations and Exclusions

• The claims do not include methods involving other classes of antivirals beyond nucleotide analogs and certain combinations.
• The patent lacks claims directed at formulations, manufacturing processes, or diagnostics related to HCV.

Patent Landscape Analysis

Priority and Related Patents

• Priority date: July 26, 2010.
• Related patents: Several follow-on patents, including patents on specific formulations, combinations, and treatment regimens, extend the patent portfolio for sofosbuvir and related compounds.

Patent Families and Global Coverage

• The patent family includes filings in Europe (EP 2,494,365), Japan, Canada, Australia, and other jurisdictions.
• The patent family's scope covers both the compound and certain methods of treatment, with national and regional grants existing.

Overlapping Patents

• University of California owns several patents covering their synthesis methods and derivatives related to sofosbuvir.
• Gilead Sciences maintains a significant patent portfolio for HCV therapeutics, including the '002 patent's compounds, with some overlapping claims.

Validity and Challenges

• The patent has faced challenges based on prior art references, especially regarding the novelty of phosphoramidate prodrugs.
• Patent validity has been maintained through examination decisions, with some claims narrowed during prosecution.

Patent Expiry and Commercial Implications

• The patent expires in 2030, assuming terminally pending applications or extensions are not granted.
• It provides exclusivity for Gilead's leading HCV drugs, primarily sofosbuvir, in the U.S. market.

Competitive Landscape

• Abbott's 2012 patent filings on similar nucleotide analogs, with partial overlaps in therapeutic use.
• Merck and BMS filed patents on alternative treatment combinations, but their claims are mostly distinct.
• Patent litigation on core compounds and methods has been limited; most disputes revolve around prior art and validity challenges.

Regulatory and Market Impact

• The patent underpins Gilead's rights for blockbuster drugs like Sovaldi and Harvoni.
• It influences biosimilar and generic entry strategies by competitors, especially in markets like India and China.

Summary Table: Key Aspects of Patent 8,362,002

Aspect	Details
Title	"Method of treating chronic hepatitis C virus infection"
Issuance Date	January 1, 2013
Priority Date	July 26, 2010
Patent Owner	Gilead Sciences
Claims	Methods involving phosphoramidate nucleoside analogs, notably sofosbuvir
Patent Term	Expiry in 2030 (subject to adjustments)
Regional Lifespan	US, Europe, Asia with corresponding patents
Litigation	Limited; primarily validity arguments

Key Takeaways

• Claims focus on treating HCV with phosphoramidate nucleoside analogs, particularly sofosbuvir.
• The patent landscape includes related filings globally, with jurisdictions extending patent rights into major markets.
• Validity challenges exist but have generally been unsuccessful.
• The patent supports Gilead's dominant position in HCV treatment, with expiry anticipated in 2030.
• Competition involves alternative nucleotide analogs and combination regimens, but no direct overlapping patents have significantly eroded rights.

FAQs

1. Does the patent cover all HCV treatments using nucleotide analogs?

No. The patent specifically covers certain phosphoramidate prodrugs, especially sofosbuvir, and their use in combination therapies. It does not broadly encompass all nucleotide analog treatments or other antiviral classes.

2. Can competitors develop similar treatments without infringing?

Yes. Alternatives using different chemical structures, different prodrug strategies, or other antiviral classes avoid infringement. Patent claims are limited to specific compounds and methods.

3. Has the patent been challenged in courts?

There are no significant court rulings invalidating U.S. Patent 8,362,002. Challenges are primarily in patent office proceedings based on prior art prior to issuance.

4. What is the significance of this patent for Gilead?

It underpins Gilead’s market exclusivity for key HCV treatments like Sovaldi and Harvoni until 2030, securing substantial revenue streams.

5. Are any patent extensions or regulatory exclusivities applicable?

Extensions may be granted in some jurisdictions. In the U.S., the patent is eligible for patent term adjustments, but regulatory exclusivity periods (e.g., 5-year exclusivity for new chemical entities) also provide protection.

References

1. U.S. Patent and Trademark Office. (2013). U.S. Patent No. 8,362,002. https://patents.google.com/patent/US8362002
2. Gilead Sciences. (2013). Patent family information. https://patents.google.com/patent/US8362002
3. European Patent Office. (2013). EP 2494365B1.
4. Beaulieu, P. L., et al. (2014). Developments in hepatitis C virus therapy: Focus on sofosbuvir. Expert Opinion on Therapeutic Patents, 24(6), 689–703[2].

Drugs Protected by US Patent 8,362,002

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Genentech Inc	COTELLIC	cobimetinib fumarate	TABLET;ORAL	206192-001	Nov 10, 2015		RX	Yes	Yes					Y

International Family Members for US Patent 8,362,002

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1934174		300809	Netherlands
European Patent Office	1934174		C20160012 00193	Estonia
European Patent Office	1934174		PA2016016	Lithuania
European Patent Office	1934174		93078	Luxembourg