Details for Patent: 8,436,180

Which drugs does patent 8,436,180 protect, and when does it expire?

Patent 8,436,180 protects KERENDIA and is included in one NDA.

This patent has fifty-nine patent family members in forty-five countries.

Summary for Patent: 8,436,180

Title:	Substituted-4-aryl-1,4-dihydro-1,6-naphthyridinamides and use thereof
Abstract:	The present application relates to novel substituted 4-aryl-1,4-dihydro-1,6-naphthyridine-3-carboxamides, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders.
Inventor(s):	Barfacker; Lars (Oberhausen, DE), Kolkhof; Peter (Wuppertal, DE), Schlemmer; Karl-Heinz (Wuppertal, DE), Grosser; Rolf (Leverkusen, DE), Nitsche; Adam (Pulheim, DE), Klein; Martina (Heiligenhaus, DE), Munter; Klaus (Wulfrath, DE), Albrecht-Kupper; Barbara (Wulfrath, DE), Hartmann; Elke (Wuppertal, DE)
Assignee:	Bayer Intellectual Property GmbH (Monheim, DE)
Application Number:	12/526,951
Patent Claim Types: see list of patent claims	Use; Composition; Compound; Process;

United States Patent 8,436,180: A Detailed Analysis of Scope, Claims, and Patent Landscape

Introduction

United States Patent 8,436,180, titled "Substituted-4-aryl-1,4-dihydro-1,6-naphthyridinamides and use thereof," was issued on May 7, 2013. This patent is assigned to Bayer Intellectual Property GmbH and covers novel compounds, their preparation, and their use in treating various diseases, particularly cardiovascular disorders.

Inventors and Assignee

The patent was invented by a team of researchers including Lars Bärfacker, Peter Kolkhof, Karl-Heinz Schlemmer, Rolf Grosser, Adam Nitsche, Martina Klein, Klaus Münter, Barbara Albrecht-Küpper, and Elke Hartmann. The assignee is Bayer Intellectual Property GmbH, based in Monheim, Germany[2][4].

Patent Scope

Compounds and Structure

The patent describes novel substituted 4-aryl-1,4-dihydro-1,6-naphthyridine-3-carboxamides. These compounds are characterized by specific structural elements, including various aryl and alkyl groups, and other functional groups such as cyano, nitro, and trifluoromethoxy groups. The detailed chemical structures and synthesis methods are outlined in the patent[1][4].

Therapeutic Uses

The compounds are intended for the treatment and/or prophylaxis of various diseases, particularly those related to cardiovascular disorders. Specific conditions mentioned include hypertension, hyperaldosteronism, and fibrosis. The compounds are believed to have therapeutic benefits due to their ability to modulate mineralocorticoid receptor activity, which is crucial in managing conditions like heart failure and hypertension[1][4].

Claims

Independent and Dependent Claims

The patent includes a series of independent and dependent claims that define the scope of the invention. Independent claims broadly describe the novel compounds, their preparation methods, and their therapeutic uses. Dependent claims further specify the structural features of the compounds, such as the types of aryl and alkyl groups, and the specific diseases they are intended to treat[1][4].

Claim Interpretation

The interpretation of patent claims is crucial for understanding the exclusive rights granted to the patent holder. Claims in this patent are designed to define the extent of the exclusive rights, specifying what is considered the invention and what is not. However, as discussed in scholarly literature, the interpretation of claims can be subject to uncertainty due to policy debates over the proper scope of patent exclusion[3].

Patent Landscape

Patent Expiration Dates

The patent is set to expire on April 12, 2029. This expiration date is significant as it marks the end of the exclusive rights granted to Bayer Intellectual Property GmbH, after which the compounds and their uses will enter the public domain[2].

Exclusivity Periods

In addition to the patent, the drug associated with this patent, Kerendia, has been granted exclusivity periods by the FDA. These exclusivity periods, which can run concurrently with the patent, provide additional protection against generic competition. The exclusivity periods for Kerendia are set to expire on September 1, 2025, and July 9, 2026[2].

Related Patents and Publications

The patent is part of a broader landscape of related patents and publications. Other patents and applications filed by Bayer and other entities cover similar compounds and therapeutic uses, indicating a competitive and evolving field in cardiovascular disease treatment[1][4].

Manufacturing and Use

Synthesis Methods

The patent details the synthesis methods for the novel compounds, including the necessary reagents, reaction conditions, and purification steps. This information is crucial for manufacturers to replicate the compounds[1][4].

Therapeutic Applications

The use of these compounds in treating cardiovascular disorders is a key aspect of the patent. The therapeutic applications are supported by research indicating the compounds' efficacy in modulating mineralocorticoid receptor activity, which is vital for managing conditions like hypertension and heart failure[1][4].

Regulatory and Legal Aspects

FDA Approval and Exclusivity

The drug associated with this patent, Kerendia, has received FDA approval, which includes exclusivity periods that protect the drug from generic competition. As of the current date, there is no generic version of Kerendia available in the United States[2].

Patent Litigation and Uncertainty

The patent system is subject to litigation and uncertainty, particularly regarding the interpretation of claims. This uncertainty can arise from policy debates over the scope of patent exclusion and the fundamental meaning of claims, which can impact the smooth operation of the patent system[3].

Key Takeaways

• Novel Compounds: The patent covers novel substituted 4-aryl-1,4-dihydro-1,6-naphthyridine-3-carboxamides.
• Therapeutic Uses: These compounds are intended for treating cardiovascular disorders, including hypertension and hyperaldosteronism.
• Patent Expiration: The patent expires on April 12, 2029.
• Exclusivity Periods: Additional FDA-granted exclusivity periods expire on September 1, 2025, and July 9, 2026.
• Regulatory Protection: The drug associated with this patent, Kerendia, has no generic version available as of the current date.

FAQs

What is the main subject of United States Patent 8,436,180?

The main subject of this patent is novel substituted 4-aryl-1,4-dihydro-1,6-naphthyridine-3-carboxamides, their preparation, and their use in treating various diseases, particularly cardiovascular disorders.

Who are the inventors of this patent?

The inventors include Lars Bärfacker, Peter Kolkhof, Karl-Heinz Schlemmer, Rolf Grosser, Adam Nitsche, Martina Klein, Klaus Münter, Barbara Albrecht-Küpper, and Elke Hartmann.

What is the therapeutic use of the compounds described in this patent?

The compounds are intended for the treatment and/or prophylaxis of diseases such as hypertension, hyperaldosteronism, and fibrosis, primarily through their action on mineralocorticoid receptors.

When does the patent expire?

The patent is set to expire on April 12, 2029.

Is there a generic version of the drug associated with this patent available?

As of the current date, there is no generic version of Kerendia, the drug associated with this patent, available in the United States.

Cited Sources

1. United States Patent and Trademark Office. US8436180B2 - Substituted-4-aryl-1,4-dihydro-1,6-naphthyridinamides and use thereof. May 7, 2013.
2. Drugs.com. Generic Kerendia Availability. November 6, 2024.
3. Cornell Law Faculty Publications. The Unresolved Interpretive Ambiguity of Patent Claims. 2013.
4. Google Patents. US8436180B2 - Substituted-4-aryl-1,4-dihydro-1,6-naphthyridinamides and use thereof. May 7, 2013.

Drugs Protected by US Patent 8,436,180

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Bayer Hlthcare	KERENDIA	finerenone	TABLET;ORAL	215341-001	Jul 9, 2021		RX	Yes	No			Y	Y
Bayer Hlthcare	KERENDIA	finerenone	TABLET;ORAL	215341-002	Jul 9, 2021		RX	Yes	Yes			Y	Y

Foreign Priority and PCT Information for Patent: 8,436,180

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Germany	10 2007 009 494	Feb 27, 2007

PCT Information
PCT Filed	February 19, 2008	PCT Application Number:	PCT/EP2008/001257
PCT Publication Date:	September 04, 2008	PCT Publication Number:	WO2008/104306

International Family Members for US Patent 8,436,180

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2132206		C02132206/01	Switzerland
European Patent Office	2132206		LUC00260	Luxembourg
European Patent Office	2132206		PA2022512	Lithuania