Details for Patent: 8,487,093

Which drugs does patent 8,487,093 protect, and when does it expire?

Patent 8,487,093 protects RECARBRIO and is included in one NDA.

This patent has seventy-one patent family members in thirty-eight countries.

Summary for Patent: 8,487,093

Title:	.beta.-lactamase inhibitors
Abstract:	Substituted bicyclic beta-lactams of Formula I: (I), are .beta.-lactamase inhibitors, wherein a, X, R.sup.1 and R.sup.2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with .beta.-lactam antibiotics. In particular, the compounds can be employed with a .beta.-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to .beta.-lactam antibiotics due to the presence of the .beta.-lactamases.
Inventor(s):	Blizzard; Timothy A. (Princeton, NJ), Chen; Helen (Marlboro, NJ), Gude; Candido (Staten Island, NY), Hermes; Jeffrey D. (Warren, NJ), Imbriglio; Jason (Piscataway, NJ), Kim; Seongkon (Holmdel, NJ), Wu; Jane Y. (Marlboro, NJ), Mortko; Christopher J. (Hoboken, NJ), Mangion; Ian (Cranford, NJ), Rivera; Nelo (New Milford, NJ), Ruck; Rebecca T. (Jersey City, NJ), Shevlin; Michael (Plainfield, NJ)
Assignee:	Merck Sharp & Dohme Corp. (Rahway, NJ)
Application Number:	12/812,763
Patent Claim Types: see list of patent claims	Use; Composition; Compound;

Detailed Analysis of the Scope and Claims of United States Patent 8,487,093

Introduction

United States Patent 8,487,093, issued on July 16, 2013, is a significant patent in the field of antibiotic research, particularly focusing on β-lactamase inhibitors. This patent is assigned to Merck Sharp & Dohme Corp. and involves the work of several inventors, including Timothy A. Blizzard, Helen Chen, and others.

Background and Context

The rise of bacterial antibiotic resistance has necessitated the development of new and effective antibiotics. β-lactamase inhibitors are crucial in combating this resistance by inhibiting the enzymes that bacteria use to degrade β-lactam antibiotics. This patent addresses this need by introducing novel β-lactamase inhibitors.

Scope of the Patent

Invention Overview

The patent describes novel β-lactamase inhibitors and their use in combination with β-lactam antibiotics to treat bacterial infections. These inhibitors are designed to counteract the resistance mechanisms employed by bacteria, thereby enhancing the efficacy of β-lactam antibiotics[1][4].

Chemical Compounds

The patent details various chemical compounds that fall under the category of β-lactamase inhibitors. These include compounds such as (2s,5r)-7-oxo-2-(piperidin-4-ylcarbamoyl)-1,6-diazabicyclo[3.2.1]octane-6-sulfonic acid and other related structures. The claims also cover salts, esters, and other derivatives of these compounds[1][4].

Claims of the Patent

Independent Claims

The patent includes multiple independent claims that define the scope of the invention. These claims are broad and encompass a wide range of chemical structures and their uses. For example, Claim 1 of the patent describes a specific chemical compound, relebactam monohydrate, which is a key β-lactamase inhibitor[5].

Dependent Claims

Dependent claims further specify the invention by detailing various aspects such as the synthesis methods, pharmaceutical compositions, and therapeutic uses of the β-lactamase inhibitors. These claims also cover the combination of these inhibitors with β-lactam antibiotics like imipenem[1][4].

Patent Landscape

Patent Exclusivity

The patent is protected by both patent and exclusivity rights granted by the FDA. The patent itself is set to expire on July 16, 2033, 20 years from the date of filing. Additionally, the FDA has granted exclusivity periods, including a New Chemical Entity (NCE) exclusivity until July 16, 2024, and Generating Antibiotic Incentives Now (GAIN) exclusivity until July 16, 2029[2].

Related Patents and Exclusivities

The patent is part of a broader landscape of intellectual property related to antibiotic development. Other patents and exclusivities may overlap or complement this patent, ensuring a comprehensive protection for the inventors and the assignee[2].

Patent Scope Metrics

Claim Length and Count

Research on patent scope metrics suggests that the length and count of independent claims can indicate the breadth and clarity of a patent. In the case of US 8,487,093, the claims are detailed and numerous, indicating a well-defined scope. However, the examination process may have narrowed the scope of these claims to ensure clarity and validity[3].

Therapeutic Applications

Bacterial Infections

The β-lactamase inhibitors described in the patent are intended for the treatment of bacterial infections, including those caused by bacteria resistant to traditional β-lactam antibiotics. The combination of these inhibitors with antibiotics like imipenem enhances the therapeutic efficacy against such resistant strains[1][4].

Chemical Groups and Substituents

The patent specifies various chemical groups and substituents that are part of the β-lactamase inhibitors. These include alkyl groups, heterocyclic groups, and specific functional groups like carboxamide and sulfooxy. These details are crucial for understanding the structural requirements for the inhibitors[1][4].

Synthesis and Manufacturing

The claims also cover methods for synthesizing these compounds, which is essential for their practical application. The patent describes various synthetic routes and conditions necessary for producing the β-lactamase inhibitors[1][4].

Pharmaceutical Compositions

The patent includes claims related to pharmaceutical compositions that contain the β-lactamase inhibitors, either alone or in combination with β-lactam antibiotics. These compositions are designed for various administration routes, ensuring versatility in treatment options[1][4].

Key Takeaways

• Novel β-lactamase inhibitors: The patent introduces new chemical compounds designed to inhibit β-lactamase enzymes.
• Combination therapy: These inhibitors are intended for use with β-lactam antibiotics to enhance their efficacy against resistant bacteria.
• Broad claims: The patent includes detailed and numerous claims covering various aspects of the invention.
• Exclusivity and patent protection: The patent is protected by both patent and FDA-granted exclusivity rights.
• Therapeutic applications: The inhibitors are aimed at treating bacterial infections, including those caused by resistant strains.

FAQs

What is the main focus of United States Patent 8,487,093?

The main focus of this patent is on novel β-lactamase inhibitors and their use in combination with β-lactam antibiotics to treat bacterial infections.

Who are the inventors of this patent?

The inventors include Timothy A. Blizzard, Helen Chen, Candido Gude, Jeffrey D. Hermes, Jason Imbriglio, Seongkon Kim, Jane Y. Wu, Christopher J. Mortko, Ian Mangion, Nelo Rivera, Rebecca T. Ruck, and Michael Shevlin.

What is the current status of the patent?

The patent is active and set to expire on July 16, 2033. It also has FDA-granted exclusivity periods.

What are the therapeutic applications of the β-lactamase inhibitors described in the patent?

The inhibitors are intended for the treatment of bacterial infections, including those caused by bacteria resistant to traditional β-lactam antibiotics.

Are there any generic versions of the drugs covered by this patent available?

As of the latest information, there are no therapeutically equivalent generic versions of the drugs covered by this patent available in the United States[2].

Cited Sources

1. US8487093B2 - β-lactamase inhibitors - Google Patents
2. Generic Recarbrio Availability - Drugs.com
3. Patent Claims and Patent Scope - Hoover Institution
4. US8487093B2 - β-lactamase inhibitors - Google Patents
5. Untitled - Regulations.gov

Drugs Protected by US Patent 8,487,093

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Msd Merck Co	RECARBRIO	cilastatin sodium; imipenem; relebactam	POWDER;INTRAVENOUS	212819-001	Jul 16, 2019		RX	Yes	Yes	8,487,093		Y	Y		TREATMENT OF COMPLICATED INTRA-ABDOMINAL INFECTIONS (CIAI)
Msd Merck Co	RECARBRIO	cilastatin sodium; imipenem; relebactam	POWDER;INTRAVENOUS	212819-001	Jul 16, 2019		RX	Yes	Yes	8,487,093		Y	Y		TREATMENT OF HOSPITAL-ACQUIRED BACTERIAL PNEUMONIA AND VENTILATOR-ASSOCIATED BACTERIAL PNEUMONIA (HABP/VABP)
Msd Merck Co	RECARBRIO	cilastatin sodium; imipenem; relebactam	POWDER;INTRAVENOUS	212819-001	Jul 16, 2019		RX	Yes	Yes	8,487,093		Y	Y		TREATMENT OF COMPLICATED URINARY TRACT INFECTIONS, INCLUDING PYELONEPHRITIS (CUTI)

Foreign Priority and PCT Information for Patent: 8,487,093

PCT Information
PCT Filed	January 15, 2009	PCT Application Number:	PCT/US2009/031047
PCT Publication Date:	July 23, 2009	PCT Publication Number:	WO2009/091856

International Family Members for US Patent 8,487,093

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2231667		301050	Netherlands
European Patent Office	2666774		301052	Netherlands
European Patent Office	2666774		301051	Netherlands
European Patent Office	2231667		LUC00165	Luxembourg
European Patent Office	2231667		PA2020516	Lithuania
European Patent Office	2231667		122020000034	Germany
European Patent Office	2231667		2020C/522	Belgium