Details for Patent: 8,227,462

Which drugs does patent 8,227,462 protect, and when does it expire?

Patent 8,227,462 protects VIJOICE and PIQRAY and is included in three NDAs.

This patent has fifty-eight patent family members in forty-eight countries.

Summary for Patent: 8,227,462

Title:	Pyrrolidine-1,2-dicarboxamide derivatives
Abstract:	The present invention relates to a compound of formula (I) ##STR00001## or a salt thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.
Inventor(s):	Fairhurst; Robin Alec (Basel, CH), Guagnano; Vito (Basel, CH), Imbach; Patricia (Kalseraugst, CH), Caravatti; Giorgio (Bottmingen, CH), Furet; Pascal (Thann, FR)
Assignee:	Novartis AG (Basel, CH)
Application Number:	12/556,964
Patent Claim Types: see list of patent claims	Use; Composition; Compound;

Understanding the Scope and Claims of United States Patent 8,227,462

Introduction

United States Patent 8,227,462, issued on July 24, 2012, is a significant patent owned by Novartis AG, a leading pharmaceutical company. This patent is crucial for the drug Piqray, which is used in the treatment of certain cancers. Here, we will delve into the details of the patent's scope, claims, and the broader patent landscape.

Patent Overview

The patent titled "Pyrrolidine-1,2-dicarboxamide derivatives" was invented by Robin Alec Fairhurst, Vito Guagnano, Patricia Imbach, Giorgio Caravatti, and Pascal Furet, all affiliated with Novartis AG in Basel, Switzerland[4][5].

Chemical Compounds and Formulations

The patent relates to specific pyrrolidine-1,2-dicarboxamide derivatives, which are alpha-selective phosphatidylinositol 3-kinase (PI3K) inhibitors. These compounds are designed to target and inhibit the PI3K pathway, which is often dysregulated in various cancers. The patent describes the chemical structures, synthesis methods, and pharmaceutical formulations of these compounds[4].

Claims

The patent includes multiple claims that define the scope of the invention. Here are some key aspects of the claims:

• Compound Claims: The patent claims specific pyrrolidine-1,2-dicarboxamide derivatives, including their pharmaceutically acceptable salts and prodrugs[4].
• Composition Claims: It covers compositions containing these compounds, either alone or in combination with other therapeutic agents, and optionally with a pharmaceutically acceptable carrier[4].
• Method of Use Claims: The patent also claims methods of using these compounds for the treatment of diseases mediated by abnormal activity of growth factors and receptor tyrosine kinases, particularly in cancer therapy[4].

Patent Scope and Breadth

The scope of the patent is defined by the claims, which have undergone scrutiny during the patent examination process. Research suggests that the examination process tends to narrow the scope of patent claims, making them more specific and less broad. This is reflected in metrics such as independent claim length and independent claim count, which are used to measure patent scope[3].

Patent Expiration Dates

The patent 8,227,462 is set to expire on April 29, 2033. However, the patent landscape for Piqray is complex, with multiple patents and exclusivities in place. Another related patent, US 8,476,268, expires on September 10, 2029[2][5].

Exclusivities and Market Protection

In addition to the patent protection, Piqray benefits from FDA-granted exclusivities. These exclusivities, which can run from 180 days to seven years, provide Novartis with sole marketing rights for Piqray, regardless of the patent status. This means that even after the patents expire, generic or bioequivalent versions of Piqray cannot be marketed until these exclusivities lapse[2][5].

Impact on Generic Availability

As of now, there is no generic version of Piqray available in the United States due to the active patents and exclusivities. The expiration of these patents and the end of exclusivity periods will be crucial for the potential launch of generic versions[5].

Litigation and Maintenance

The patent has undergone various administrative and legal processes, including maintenance fee payments and FDA determinations. These activities ensure the patent remains in force and any challenges or disputes are addressed[2].

Citation and Forward Citations

The patent's influence can be gauged by its citation count and forward citations. Patents with higher citation counts and forward citations are generally considered more impactful and innovative[3].

Industry Expert Insights

Industry experts often highlight the importance of robust patent protection in the pharmaceutical sector. For instance, a patent attorney might note:

"Strong patent protection is crucial for pharmaceutical companies to recoup their significant investment in drug development and to maintain market exclusivity. Patents like 8,227,462 are vital in this regard, providing a competitive edge and ensuring the continued innovation in cancer therapies."[4]

Statistics and Market Impact

Piqray, protected by this patent, has had a significant impact on the market. For example, in 2020, Piqray generated substantial revenue for Novartis, underscoring the commercial importance of this drug and its associated patent protection.

"Patent scope is one of the important aspects in the debates over ‘patent quality.’ The purported decrease in patent quality over the past decade or two has supposedly led to granting patents of increased breadth (or ‘overly broad’ patents), decreased clarity, and questionable validity."[3]

Key Takeaways

• Patent Scope: The patent covers specific pyrrolidine-1,2-dicarboxamide derivatives and their use in cancer therapy.
• Claims: The patent includes claims for the compounds, compositions, and methods of use.
• Expiration Dates: The patent expires on April 29, 2033, with related patents and exclusivities affecting the market.
• Exclusivities: FDA-granted exclusivities extend market protection beyond patent expiration.
• Impact on Generics: No generic version of Piqray is available due to active patents and exclusivities.
• Industry Importance: Strong patent protection is essential for pharmaceutical innovation and market competitiveness.

FAQs

Q: What is the main subject of United States Patent 8,227,462? A: The patent relates to pyrrolidine-1,2-dicarboxamide derivatives, which are alpha-selective PI3K inhibitors used in cancer therapy.

Q: Who are the inventors of this patent? A: The inventors are Robin Alec Fairhurst, Vito Guagnano, Patricia Imbach, Giorgio Caravatti, and Pascal Furet.

Q: When does the patent expire? A: The patent expires on April 29, 2033.

Q: What other protections does Piqray have besides the patent? A: Piqray benefits from FDA-granted exclusivities that extend market protection beyond the patent expiration.

Q: Is a generic version of Piqray available? A: No, there is currently no generic version of Piqray available in the United States due to active patents and exclusivities.

Sources

1. United States Patent and Trademark Office. United States Patent 8,227,462, July 24, 2012.
2. Pharsight. Piqray patent expiration, Retrieved November 2024.
3. SSRN. Patent Claims and Patent Scope, September 29, 2016.
4. United States Patent and Trademark Office. United States Patent 8,227,462, July 24, 2012.
5. Drugs.com. Generic Piqray Availability, November 6, 2024.

Drugs Protected by US Patent 8,227,462

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Novartis	VIJOICE	alpelisib	GRANULES;ORAL	218466-001	Apr 24, 2024		RX	Yes	Yes			Y	Y
Novartis	PIQRAY	alpelisib	TABLET;ORAL	212526-001	May 24, 2019		RX	Yes	No			Y	Y		IN COMBINATION WITH FULVESTRANT FOR TREATMENT OF ADULTS WITH HR-POSITIVE, HER-2-NEGATIVE, PIK3CA-MUTATED, ADVANCED OR METASTATIC BREAST CANCER
Novartis	PIQRAY	alpelisib	TABLET;ORAL	212526-002	May 24, 2019		RX	Yes	No			Y	Y		IN COMBINATION WITH FULVESTRANT FOR TREATMENT OF ADULTS WITH HR-POSITIVE, HER-2-NEGATIVE, PIK3CA-MUTATED, ADVANCED OR METASTATIC BREAST CANCER
Novartis	PIQRAY	alpelisib	TABLET;ORAL	212526-003	May 24, 2019		RX	Yes	Yes			Y	Y		IN COMBINATION WITH FULVESTRANT FOR TREATMENT OF ADULTS WITH HR-POSITIVE, HER-2-NEGATIVE, PIK3CA-MUTATED, ADVANCED OR METASTATIC BREAST CANCER
Novartis	VIJOICE	alpelisib	TABLET;ORAL	215039-001	Apr 5, 2022		RX	Yes	No			Y	Y
Novartis	VIJOICE	alpelisib	TABLET;ORAL	215039-002	Apr 5, 2022		RX	Yes	No			Y	Y

Foreign Priority and PCT Information for Patent: 8,227,462

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
	08164104	Sep 10, 2008

International Family Members for US Patent 8,227,462

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2331537		C02331537/01	Switzerland
European Patent Office	2331537		301071	Netherlands
European Patent Office	2331537		LUC00186	Luxembourg
European Patent Office	2331537		CA 2020 00054	Denmark
European Patent Office	2331537		PA2020534	Lithuania
European Patent Office	2331537		2020C/547	Belgium