Details for Patent: 8,859,510

Which drugs does patent 8,859,510 protect, and when does it expire?

Patent 8,859,510 protects DIFICID and is included in two NDAs.

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

This patent has one hundred and twenty-seven patent family members in twenty-nine countries.

Summary for Patent: 8,859,510

Title:	Macrocyclic polymorphs, compositions comprising such polymorphs, and methods of use and manufacture thereof
Abstract:	The invention relates to novel forms of compounds displaying broad spectrum antibiotic activity, especially crystalline polymorphic forms and amorphous forms of such compounds, compositions comprising such crystalline polymorphic forms and amorphous forms of such compounds, processes for manufacture and use thereof. The compounds and compositions of the invention are useful in the pharmaceutical industry, for example, in the treatment or prevention of diseases or disorders associated with the use of antibiotics, chemotherapies, or antiviral therapies, including, but not limited to, colitis, for example, pseudo-membranous colitis; antibiotic associated diarrhea; and infections due to Clostridium difficile ("C. difficile"), Clostridium perfringens ("C. perfringens"), Staphylococcus species, for example, methicillin-resistant Staphylococcus, or Enterococcus including Vancomycin-resistant enterococci.
Inventor(s):	Chiu; Yu-Hung (San Diego, CA), Che; Tessie Mary (San Diego, CA), Romero; Alex (Oakland, CA), Ichikawa; Yoshi (San Diego, CA), Shue; Youe-Kong (San Diego, CA)
Assignee:	Optimer Pharmaceuticals, Inc. (Lexington, MA)
Application Number:	12/523,790
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,859,510
Patent Claim Types: see list of patent claims	Use; Composition; Dosage form;

United States Patent 8,859,510: A Detailed Analysis of Scope, Claims, and Patent Landscape

Introduction

The United States Patent 8,859,510, titled "Macrocyclic polymorphs, compositions comprising such polymorphs, and methods of use and manufacture thereof," is a significant patent in the pharmaceutical sector, particularly in the area of antibiotic development. This patent, owned by Merck Sharp & Dohme Corp., covers novel forms of compounds with broad-spectrum antibiotic activity.

Background and Invention Overview

The patent relates to novel crystalline and amorphous forms of a compound, here referred to as "Compound of Formula I," which exhibits broad-spectrum antibiotic activity. These forms are particularly important in the development of pharmaceutical compositions, especially for the antibiotic fidaxomicin, marketed as DIFICID®[2][4].

Scope of Protection

Claim Coverage

The patent claims cover several key aspects:

• Novel Crystalline and Amorphous Forms: The invention encompasses various crystalline and amorphous forms of the Compound of Formula I. These forms are crucial for the stability, efficacy, and bioavailability of the antibiotic[4].
• Pharmaceutical Compositions: The patent includes claims for pharmaceutical compositions comprising the Compound of Formula I, either alone or in combination with other compounds like tiacumicins. These compositions can have varying concentrations of the Compound of Formula I, often exceeding 90% by weight[4].
• Methods of Use and Manufacture: The patent also covers methods for using and manufacturing these novel forms and compositions, which is essential for the production and application of the antibiotic[4].

Claim Drafting Strategies

The claims in this patent are drafted to ensure broad protection while maintaining specificity:

• Specific Formulations: Claims are specific about the percentage of the Compound of Formula I in the pharmaceutical compositions, ensuring that the patent covers a range of formulations that are practically useful[4].
• Combination Claims: The patent includes claims for combinations of the Compound of Formula I with other compounds, such as tiacumicins, which expands the scope of protection to various therapeutic applications[4].

Patent Landscape

Geographical and Organizational Context

The patent is part of Merck Sharp & Dohme Corp.'s extensive portfolio in the pharmaceutical sector. Merck, a global research-driven pharmaceutical company, is a leading player in the development and marketing of innovative health products[2].

Litigation and Enforcement

The patent has been involved in significant litigation. For instance, Merck and Cubist Pharmaceuticals have filed patent infringement suits against Actavis Labs. FL, following the submission of an Amended ANDA (Abbreviated New Drug Application) for a generic version of fidaxomicin. The litigation highlights the importance of this patent in protecting Merck's intellectual property rights[2][5].

Technological Milestones

The development of novel crystalline and amorphous forms of antibiotics like fidaxomicin represents a significant technological milestone:

• Stability and Efficacy: These novel forms enhance the stability and efficacy of the antibiotic, making it more effective in treating infections[4].
• Manufacturing Advancements: The methods of manufacture described in the patent reflect advancements in pharmaceutical manufacturing, ensuring consistent and high-quality production of the antibiotic[4].

Impact on Industry Standards

The patent influences industry standards in several ways:

• Quality and Consistency: By setting standards for the formulation and manufacture of antibiotics, the patent ensures that products meeting these standards are of high quality and consistent efficacy[4].
• Innovation: The protection afforded by this patent encourages further innovation in the field of antibiotic development, as companies invest in research and development to create new and improved formulations[3].

Applications Across Industries

While primarily focused on the pharmaceutical sector, the impact of this patent can be seen in various industries:

• Healthcare: The development of effective antibiotics is crucial for public health, and this patent contributes significantly to this effort[4].
• Research and Development: The patent's influence extends to academic and research institutions, where it serves as a benchmark for future research in antibiotic development[3].

Sufficiency of Disclosure and Patent Quality

The patent is scrutinized for its sufficiency of disclosure and overall quality:

• Detailed Descriptions: The patent provides detailed descriptions of the novel forms, compositions, and methods, ensuring that the disclosure is sufficient for a person of ordinary skill in the art to replicate the invention[4].
• Comparative Analysis: The patent's quality is assessed against standards in engineering journals, ensuring that it meets the necessary criteria for novelty, non-obviousness, and written description[3].

Key Takeaways

• The United States Patent 8,859,510 covers novel crystalline and amorphous forms of a broad-spectrum antibiotic compound.
• The patent includes specific claims for pharmaceutical compositions and methods of use and manufacture.
• It is part of Merck's extensive pharmaceutical portfolio and has been involved in significant litigation to protect intellectual property rights.
• The patent influences industry standards for quality and consistency in antibiotic development.
• It has broader implications across healthcare and research sectors.

FAQs

What is the main subject of the United States Patent 8,859,510?

The main subject is the novel crystalline and amorphous forms of a compound with broad-spectrum antibiotic activity, particularly fidaxomicin.

Who owns the United States Patent 8,859,510?

The patent is owned by Merck Sharp & Dohme Corp.

What are the key claims covered by the patent?

The patent covers novel forms of the antibiotic compound, pharmaceutical compositions comprising these forms, and methods for their use and manufacture.

How has the patent been involved in litigation?

The patent has been involved in litigation against Actavis Labs. FL following the submission of an Amended ANDA for a generic version of fidaxomicin.

What is the impact of this patent on industry standards?

The patent sets standards for the formulation and manufacture of antibiotics, ensuring high quality and consistent efficacy, and encourages further innovation in antibiotic development.

Cited Sources

1. United States Court of Appeals for the Federal Circuit - Decision - United States Court of Appeals for the Federal Circuit[1].
2. MERCK SHARP & DOHME CORP., CUBIST PHARMACEUTICAL - Plaintiffs' claim for patent infringement[2].
3. Quantum Leap: Decoding Quantum Computing Innovation - Historical Development & Current Trends of Quantum Computing Patents[3].
4. US8859510B2 - Macrocyclic polymorphs, compositions comprising such polymorphs, and methods of use and manufacture thereof - Google Patents[4].
5. ANDA 208443 ANDA APPROVAL Actavis Laboratories FL, Inc. - FDA Approval Letter[5].

Drugs Protected by US Patent 8,859,510

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Cubist Pharms Llc	DIFICID	fidaxomicin	FOR SUSPENSION;ORAL	213138-001	Jan 24, 2020		RX	Yes	Yes					Y
Cubist Pharms Llc	DIFICID	fidaxomicin	TABLET;ORAL	201699-001	May 27, 2011		RX	Yes	Yes					Y

Foreign Priority and PCT Information for Patent: 8,859,510

PCT Information
PCT Filed	January 22, 2008	PCT Application Number:	PCT/US2008/000735
PCT Publication Date:	July 31, 2008	PCT Publication Number:	WO2008/091554

International Family Members for US Patent 8,859,510

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1539977		C300727	Netherlands
European Patent Office	1539977		CA 2015 00020	Denmark
European Patent Office	1539977		92684	Luxembourg
European Patent Office	1539977		15C0028	France
European Patent Office	1539977		300727	Netherlands
European Patent Office	1539977		CR 2015 00020	Denmark
European Patent Office	1539977		16/2015	Austria