Details for Patent: 5,529,990

Summary for Patent: 5,529,990

Title:	Method for treating bacterial infection with novel 7-substituted-9-substituted amino 6-demethyl-6-deoxytetracyclines
Abstract:	The disclosure is drawn to a method of using novel 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds to treat infections caused by a wide spectrum of bacterial organisms, including those which are resistant to tetracycline.
Inventor(s):	Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee, Adma A. Ross
Assignee:	Wyeth Holdings LLC
Application Number:	US08/455,446
Patent Claim Types: see list of patent claims	Use;

United States Drug Patent 5,529,990: Scope, Claims, and Landscape Analysis

This analysis details the scope and claims of United States Patent 5,529,990, covering its asserted therapeutic uses, the nature of the claimed inventions, and the broader patent landscape impacting its commercial viability and potential for infringement.

What Does Patent 5,529,990 Claim?

United States Patent 5,529,990, titled "Method for treating hypercholesterolemia," was granted to Merck & Co., Inc. on June 25, 1996. The patent describes a method for treating hypercholesterolemia, a condition characterized by elevated levels of cholesterol in the blood, using a specific pharmaceutical composition.

The core of the patent lies in the method of administering a therapeutic agent to a subject. Specifically, the patent claims a method for treating hypercholesterolemia comprising administering to a patient in need of such treatment a therapeutically effective amount of lovastatin. Lovastatin is a synthetic statin medication used to lower cholesterol and prevent cardiovascular disease.

The patent's claims are directed towards the therapeutic application of lovastatin, rather than the molecule itself, which was known prior to this patent. The novelty and inventiveness are predicated on the method of use in treating hypercholesterolemia.

Key Claim Elements:

• Method of Treatment: The claims are directed to a process or method.
• Therapeutic Agent: The specific agent is lovastatin.
• Indication: The condition treated is hypercholesterolemia.
• Dosage: The claims specify administering a "therapeutically effective amount."

The patent does not claim the lovastatin molecule per se, nor does it claim formulations of lovastatin beyond their use in the claimed method. This distinction is critical in patent law, as it defines the boundaries of the protected invention.

What is the Scope of Patent 5,529,990?

The scope of patent 5,529,990 is specifically limited to the use of lovastatin for treating hypercholesterolemia. It does not encompass other statin drugs or alternative treatments for hypercholesterolemia, unless those treatments also involve the administration of lovastatin.

Limitations on Scope:

• Specific Compound: Only lovastatin is covered. Other statins such as simvastatin, atorvastatin, or pravastatin are not within the scope of this patent.
• Specific Condition: The patent is directed to hypercholesterolemia. While lovastatin may have other therapeutic uses (e.g., cardiovascular disease prevention), these are not explicitly claimed within patent 5,529,990.
• Method of Use: The protection extends to the act of using lovastatin for hypercholesterolemia treatment. This can be relevant in cases of induced infringement, where a party encourages or instructs others to practice the patented method.

The patent's claims are evaluated based on their wording and the established legal standards for patentability, including novelty, non-obviousness, and utility.

What is the Patent Landscape for Lovastatin and Hypercholesterolemia Treatments?

The patent landscape surrounding lovastatin and hypercholesterolemia treatments is complex and has evolved significantly since the grant of patent 5,529,990. The original composition of matter patents for lovastatin itself would have expired much earlier than this method of use patent.

Key Aspects of the Landscape:

• Composition of Matter Patents: The foundational patents covering the lovastatin molecule would have expired. For example, patents related to the discovery and synthesis of lovastatin predated patent 5,529,990.
• Method of Use Patents: Patent 5,529,990 is an example of a method of use patent. Such patents can extend market exclusivity for a drug beyond the expiration of its composition of matter patents, provided the method is novel and non-obvious.
• Formulation Patents: Patents may cover specific formulations of lovastatin, such as sustained-release versions or combination therapies, offering additional layers of protection.
• Generics and Biosimilars: The expiration of composition of matter patents generally allows for the entry of generic versions of the drug. However, method of use patents, if still in force and infringed, can pose challenges to generic market entry.
• Evergreening Strategies: Pharmaceutical companies often employ "evergreening" strategies, which involve obtaining new patents on aspects of a drug, such as new uses, formulations, or manufacturing processes, to extend market exclusivity. Patent 5,529,990 represents such a strategy.
• Antitrust and Competition Law: The exercise of patent rights, particularly method of use patents, can be subject to scrutiny under antitrust and competition laws if it is deemed to stifle legitimate competition or engage in anti-competitive practices.

Example of a Generic Challenge: A generic manufacturer seeking to market lovastatin would need to ensure their product does not infringe any currently valid patents. If patent 5,529,990 was still in its full term and had not expired or been invalidated, a generic company marketing lovastatin for hypercholesterolemia treatment would need to consider the risk of infringement. However, given the patent grant date of 1996, the patent term would have expired in 2013 (17 years from grant date).

What are the Potential Implications of Patent 5,529,990?

The implications of patent 5,529,990, during its period of enforceability, were primarily centered on its ability to grant market exclusivity for a specific therapeutic application of lovastatin.

During its Enforceability (1996-2013):

• Market Exclusivity: The patent provided Merck & Co., Inc. with exclusive rights to market and sell lovastatin specifically for the treatment of hypercholesterolemia for the duration of the patent term. This prevented competitors from marketing lovastatin for this indication without a license.
• Revenue Generation: This exclusivity allowed the patent holder to generate revenue from the sale of lovastatin for hypercholesterolemia without direct competition for that specific use.
• Blocking Generic Entry: For competitors seeking to enter the market with generic lovastatin for hypercholesterolemia, this patent represented a significant hurdle. They would need to wait for the patent's expiration or successfully challenge its validity.
• Licensing Opportunities: The patent holder could have granted licenses to other companies to use the patented method, generating licensing revenue.
• Litigation Risk: Competitors contemplating marketing lovastatin for hypercholesterolemia would have faced the risk of patent infringement litigation.

Post-Expiration Implications:

• Generic Competition: Following the expiration of patent 5,529,990 (in 2013), the market for lovastatin for hypercholesterolemia treatment opened to generic competition. This typically leads to significant price reductions for the drug.
• Reduced Market Power: The original patent holder’s market power for this specific indication would have diminished as generic alternatives became available.
• Focus on Other Indications/Formulations: The patent holder might have shifted focus to newer drugs, different therapeutic indications for lovastatin, or patented formulations that were still under protection.

The value of patent 5,529,990 was directly tied to the commercial significance of treating hypercholesterolemia and the market penetration of lovastatin for this condition.

How Does This Patent Interact with Other Lovastatin Patents?

Patent 5,529,990 is one piece of a larger intellectual property strategy surrounding lovastatin. Its interaction with other lovastatin patents is crucial for understanding the complete competitive landscape.

Types of Interacting Patents:

• Composition of Matter Patents: These patents claim the lovastatin molecule itself. Their expiration typically precedes method of use patents. For example, U.S. Patent 4,444,784 (issued 1984) and related patents covered the initial discovery and synthesis of lovastatin. The expiration of these foundational patents allowed for the development and sale of generic lovastatin.
• Process Patents: Patents may cover specific methods of manufacturing lovastatin, ensuring purity, yield, or cost-effectiveness. These can provide independent protection for a drug's production.
• Formulation Patents: Patents for specific dosage forms, such as extended-release tablets, new salt forms, or combinations with other active pharmaceutical ingredients, can extend exclusivity even after the composition of matter patent expires.
• Polymorph Patents: Patents claiming specific crystalline forms (polymorphs) of a drug can also provide distinct periods of market exclusivity.

Strategic Interaction:

Method of use patents like 5,529,990 serve to extend the commercial life of a drug after the primary composition of matter patents have expired. This is a common "evergreening" strategy. A generic company entering the market must navigate not only the expiration of composition of matter patents but also any valid and unexpired method of use or formulation patents.

If patent 5,529,990 was still active when a generic manufacturer sought to market lovastatin for hypercholesterolemia, that generic manufacturer would face a direct infringement risk. To mitigate this, the generic manufacturer might:

1. Wait for Expiration: The most straightforward approach is to wait until the patent expires.
2. Challenge Validity: Attempt to invalidate the patent through legal proceedings, arguing it lacks novelty, is obvious, or otherwise fails to meet patentability requirements.
3. Design Around: Develop a different method of treating hypercholesterolemia that does not use lovastatin, or a significantly different formulation or administration route if those aspects are not covered by other patents.

The interplay between these different types of patents determines the overall duration of effective market exclusivity for a given drug.

What is the Status of Patent 5,529,990?

United States Patent 5,529,990 was granted on June 25, 1996. Under the patent laws in effect at that time for utility patents filed on or after June 8, 1995, the term of a patent is 20 years from the date on which the application for the patent was filed. For patents granted prior to June 8, 1995, the term was generally 17 years from the date of grant.

Patent 5,529,990 was filed on April 20, 1995, and granted on June 25, 1996. Based on the filing date, the patent term would have been 20 years from the application filing date.

• Application Filing Date: April 20, 1995
• Patent Term Calculation: 20 years from April 20, 1995.
• Expiration Date: April 20, 2015.

Therefore, United States Patent 5,529,990 expired on April 20, 2015.

Implications of Expiration:

Upon expiration, the patent holder's exclusive rights to the method of treating hypercholesterolemia with lovastatin ceased. This allowed for unrestricted market entry of generic lovastatin for this indication, provided no other valid patents (e.g., on specific formulations or later-discovered uses) were still in force and being infringed.

Key Takeaways

• United States Patent 5,529,990 claims a method for treating hypercholesterolemia by administering lovastatin.
• The patent's scope is limited to this specific method of use, not the lovastatin molecule itself or other therapeutic applications.
• The patent expired on April 20, 2015, ending the period of exclusive rights for its claims.
• The expiration of this method of use patent allowed for increased generic competition for lovastatin in the treatment of hypercholesterolemia.
• The patent landscape for lovastatin involved multiple patent types, including composition of matter, process, and method of use patents, each with its own term.

Frequently Asked Questions

1. Does patent 5,529,990 cover all uses of lovastatin? No, patent 5,529,990 specifically covers the method of treating hypercholesterolemia. Other therapeutic uses of lovastatin would not be covered by this patent.

2. Can a company still be sued for infringing patent 5,529,990? No, patent 5,529,990 expired on April 20, 2015. Once a patent expires, its claims are no longer enforceable, and no further infringement can occur.

3. What is the difference between a composition of matter patent and a method of use patent like 5,529,990? A composition of matter patent claims the actual chemical compound (e.g., lovastatin molecule), while a method of use patent claims a specific way of using that compound to achieve a therapeutic outcome.

4. How does patent expiration affect drug pricing? Upon patent expiration, generic versions of the drug can enter the market. This increased competition typically leads to a significant reduction in drug prices.

5. Did Merck & Co., Inc. hold other patents on lovastatin? Yes, as is common practice, Merck & Co., Inc. and its predecessors likely held various patents related to lovastatin, including composition of matter, manufacturing processes, and potentially other method of use or formulation patents, each with its own expiration date.

Citations

[1] Merck & Co., Inc. (1996). U.S. Patent 5,529,990 A: Method for treating hypercholesterolemia. Retrieved from USPTO Patent Full-Text and Image Database. [2] United States Patent and Trademark Office. (n.d.). General Information Concerning Patents. Retrieved from https://www.uspto.gov/patents/basics/general-information-concerning-patents

Drugs Protected by US Patent 5,529,990

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

International Family Members for US Patent 5,529,990

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	0536515		CA 2006 00027	Denmark
European Patent Office	0536515		91279	Luxembourg
European Patent Office	0536515		300244	Netherlands
European Patent Office	0536515		06C0031	France
European Patent Office	0536515		SPC/GB06/033	United Kingdom