Details for Patent: 8,148,399

Which drugs does patent 8,148,399 protect, and when does it expire?

Patent 8,148,399 protects OLYSIO and is included in one NDA.

This patent has sixty-three patent family members in forty-one countries.

Summary for Patent: 8,148,399

Title:	Macrocyclic inhibitors of hepatitis C virus
Abstract:	Inhibitors of HCV replication of formula (I) ##STR00001## and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R.sup.1 is --OR.sup.7, --NH--SO.sub.2R.sup.8; R.sup.2 is hydrogen, and where X is C or CH, R.sup.2 may also be C.sub.1-6alkyl; R.sup.3 is hydrogen, C.sub.1-6alkyl, C.sub.3-7cycloalkyl; R.sup.4 is aryl or Het; n is 3, 4, 5, or 6; R.sup.5 is halo, C.sub.1-6alkyl, hydroxy, C.sub.1-6alkoxy, phenyl, or Het; R.sup.6 is C.sub.1-6alkoxy, or dimethylamino; R.sup.7 is hydrogen; aryl; Het; C.sub.3-7cycloalkyl optionally substituted with C.sub.1-6alkyl; or C.sub.1-6alkyl optionally substituted with C.sub.3-7cycloalkyl, aryl or with Het; R.sup.8 is aryl; Het; C.sub.3-7cycloalkyl optionally substituted with C.sub.1-6alkyl; or C.sub.1-6alkyl optionally substituted with C.sub.3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur, and being optionally substituted with one, two or three substituents; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.
Inventor(s):	Simmen; Kenneth Alan (Tervuren, BE), De Kock; Herman Augustinus (Arendonk, BE), Raboisson; Pierre Jean-Marie Bernard (Sterrebeek, BE), Nilsson; Karl Magnus (Huddinge, SE), Samuelsson; Bengt Bertil (Huddinge, SE), Rosenquist; .ANG.sa Annica Kristina (Huddinge, SE)
Assignee:	Tibotec Pharmaceuticals Ltd. (Eastgate, County Cork, IE) Medivar AB (Huddinge, SE)
Application Number:	11/632,102
Patent Claim Types: see list of patent claims	Compound; Composition; Use; Process;

United States Patent 8,148,399: A Detailed Analysis of Scope and Claims

Introduction

United States Patent 8,148,399, granted to Janssen Pharmaceuticals, is a significant patent in the field of pharmaceuticals, particularly for the treatment of Hepatitis C. This patent is one of the primary patents related to simeprevir, a protease inhibitor used in the treatment of Hepatitis C virus (HCV) infection.

Overview of Simeprevir

Simeprevir is a macrocyclic compound that inhibits the NS3/4A protease of the HCV, a crucial enzyme for the replication of the virus. This inhibition is key to the therapeutic effect of simeprevir in treating HCV infections[1][4].

Patent Details

Patent Number and Title

• Patent Number: US8148399B2
• Title: Macrocyclic compounds and methods for treating hepatitis C virus infection

Filing and Grant Dates

• Filing Date: The exact filing date is not specified in the sources, but it is part of a series of patents filed by Janssen Pharmaceuticals.
• Grant Date: The patent was granted on April 3, 2012.

Assignee

• Assignee: Janssen Pharmaceuticals, Inc.

Scope of the Patent

Claims

The patent US8148399B2 primarily relates to the base compound of simeprevir. Here are some key aspects of the claims:

• Product Claims: The patent claims the chemical molecule of simeprevir, which is the active pharmaceutical ingredient. This is considered a primary patent and is among the strongest types of patents, as it prevents others from making, selling, or importing the chemical product[4].
• Composition Claims: The patent also includes claims related to compositions containing simeprevir. These compositions are crucial for the formulation of the drug.
• Method of Use Claims: While the primary focus is on the compound itself, there are also claims related to methods of using simeprevir for treating HCV infections.

Dependency and Divisional Patents

• Divisional Patents: This patent has two divisional patents, US8153800B2 and US8349869B2. US8153800B2 relates to macrocyclic compounds and processes for preparing these compounds and compositions. US8349869B2 claims a macrocyclic compound, its N-oxide, pharmaceutically acceptable salt, or stereoisomer, and combinations with interferon-α, pegylated interferon-α, and/or ribavirin[1][4].

Patent Landscape

Primary vs. Secondary Patents

• Primary Patents: US8148399B2 is considered a primary patent as it claims the base compound of simeprevir. Primary patents are typically the strongest and most critical for protecting the core invention[4].
• Secondary Patents: The divisional patents (US8153800B2 and US8349869B2) are classified as secondary patents. These patents cover specific pharmaceutical formulations, methods of use, product derivatives, and processes. Secondary patents are generally easier to circumvent or "invent around" compared to primary patents[4].

Global Patent Coverage

• International Filings: The patent family related to simeprevir includes filings in various countries and regions, including but not limited to the United States, India, and several other jurisdictions. This global coverage is crucial for protecting the intellectual property rights of Janssen Pharmaceuticals across different markets[4].

Impact on Generic Entry

• Barrier to Generic Entry: The primary patent (US8148399B2) significantly constrains the launch of generic products where it is granted and enforceable. Secondary patents, while easier to circumvent, can still delay generic entry by requiring competitors to formulate the drug differently or use alternative processes[4].

Patent Scope Metrics

Independent Claim Length and Count

• Metrics for Patent Scope: Research suggests that metrics such as independent claim length and independent claim count can be used to measure patent scope. These metrics can indicate the breadth and complexity of the patent claims. For US8148399B2, the detailed claims structure would reflect its scope and the level of protection it offers[3].

Expiration and Enforcement

Patent Expiration

• Expected Expiration: The expected expiration date for US8148399B2 would typically be 20 years from the filing date, assuming no extensions or adjustments. However, the exact expiration date is not specified in the sources provided[4].

Enforcement

• Enforcement Responsibility: It is the responsibility of Janssen Pharmaceuticals to enforce its patent rights if the USPTO grants the patent. This includes monitoring for infringement and taking legal action when necessary[5].

Conclusion

United States Patent 8,148,399 is a pivotal patent in the pharmaceutical industry, particularly for the treatment of HCV. It protects the base compound of simeprevir, a crucial drug in the fight against HCV, and has significant implications for both the innovator company and potential generic competitors.

Key Takeaways

• Primary Patent Protection: US8148399B2 provides strong protection for the base compound of simeprevir.
• Divisional Patents: The patent has divisional patents covering various aspects such as compositions, processes, and combinations with other treatments.
• Global Coverage: The patent family includes filings in multiple jurisdictions to ensure broad protection.
• Impact on Generic Entry: The primary patent significantly delays generic entry, while secondary patents can also pose barriers.
• Patent Scope Metrics: Metrics like independent claim length and count can help measure the scope and complexity of the patent.

FAQs

What is the main subject of US Patent 8,148,399?

The main subject of US Patent 8,148,399 is the macrocyclic compound simeprevir, used in the treatment of Hepatitis C virus (HCV) infection.

What types of claims are included in US Patent 8,148,399?

The patent includes product claims for the chemical molecule of simeprevir, composition claims, and method of use claims.

What are the divisional patents of US8148399B2?

The divisional patents are US8153800B2 and US8349869B2, which cover macrocyclic compounds, processes, and combinations with other treatments.

How does this patent impact generic entry?

The primary patent significantly delays generic entry by preventing others from making, selling, or importing the chemical product. Secondary patents can also pose barriers by requiring competitors to formulate the drug differently.

What metrics can be used to measure the scope of a patent like US8148399B2?

Metrics such as independent claim length and independent claim count can be used to measure the scope and complexity of the patent claims.

Sources

1. Hcv Ns3/4a 3 Protease Inhibitors: Simeprevir, Process Patents And Evaluation - Auctores Online
2. Patent Claims Research Dataset - USPTO
3. Patent Claims and Patent Scope - Hoover Institution
4. SIMEPREVIR - World Health Organization (WHO)
5. Nonprovisional (Utility) Patent Application Filing Guide - USPTO

Drugs Protected by US Patent 8,148,399

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Janssen Prods	OLYSIO	simeprevir sodium	CAPSULE;ORAL	205123-001	Nov 22, 2013		DISCN	Yes	No			Y	Y		METHOD OF TREATING HEPATITIS C

Foreign Priority and PCT Information for Patent: 8,148,399

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
	05107074	Jul 29, 2005
	05107417	Aug 11, 2005
	06101280	Feb 3, 2006

PCT Information
PCT Filed	July 28, 2006	PCT Application Number:	PCT/EP2006/064820
PCT Publication Date:	February 08, 2007	PCT Publication Number:	WO2007/014926

International Family Members for US Patent 8,148,399

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1912999		CA 2014 00053	Denmark
European Patent Office	1912999		C300697	Netherlands
European Patent Office	1912999		PA2014036	Lithuania
European Patent Office	1912999		1490062-5	Sweden
European Patent Office	1912999		14C0076	France