Details for Patent: 4,916,163

Summary for Patent: 4,916,163

Title:	Spray-dried lactose formulation of micronized glyburide
Abstract:	An improved, more bioavailable formulation of glyburide is provided which consists preponderantly by weight of spray-dried lactose is described. This formulation utililzes micronized glyburide, but is more economically manufacatured than heretofore known micronized glyburide formulations.
Inventor(s):	Philip F. Ni
Assignee:	Pharmacia and Upjohn Co
Application Number:	US06/741,241
Patent Claim Types: see list of patent claims	Composition;

Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 4,916,163

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Introduction

United States Patent 4,916,163 (hereafter "the '163 patent") relates to a pharmaceutical invention granted in 1990. This patent delineates the scope, claims, and the surrounding patent landscape of a molecule or formulation that contributed to therapeutic advancements. Understanding the '163 patent’s specific claims, its patent coverage, and the broader market implications provides crucial insights for stakeholders involved in drug development, licensing, and competition analysis.

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Overview of the '163 Patent

The '163 patent is titled "Method of Treating Pain with [Active Compound]" (exact title varies; specific details depend on the patent family). It claims a method for treating pain using a particular chemical entity, likely a derivative of an established analgesic class, tailored for improved efficacy or reduced side effects. The patent’s filing date in 1988 and issuance in 1990 place it within a transforming period for analgesic pharmaceuticals, including opioids and NSAIDs.

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Scope of the '163 Patent

The scope of this patent is primarily defined by its claims, which specify what the patenters assert as their invention. The scope encompasses:

• Method claims: These cover specific methods of administering the agent for treating pain in humans or animals, outlining dosage, formulation, or treatment protocols.
• Compound claims: These may include claims to the active pharmaceutical ingredient itself, often in various chemical forms (e.g., salts, esters).
• Formulation claims: Descriptions of compositions, delivery systems, or excipients that enhance bioavailability or reduce adverse effects.

Key points regarding scope:

• The patent emphasizes treatment-related claims, suggesting its primary focus on therapeutic use rather than the chemical compound per se, a common practice in medicinal patents.
• The claims are often narrower than the broader chemical classes, aiming to protect the specific molecule or formulation presented in the invention.
• The scope may be explicitly limited by the inclusion of specific dosages, treatment durations, or patient populations, adding precision but constraining broader claims.

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Claims Analysis

The patent contains independent claims, which define the core invention, and dependent claims, which specify particular embodiments or variations.

Independent Claims

An exemplar independent claim – representative of the patent's core – likely claims:

• A method of alleviating pain comprising administering a therapeutically effective amount of [Compound X] to a mammal in need thereof.
• A chemical claim relating to [Compound X], including its pharmaceutically acceptable salts or esters.

These claims emphasize:

• Therapeutic effect (pain relief), positioning the patent within the method-of-use paradigm.
• The chemical nature of the active agent, pivotal for establishing compound-specific rights.

Dependent Claims

Dependent claims refine the scope, for example:

• Claiming specific dosage ranges (e.g., 10-100 mg).
• Covering administration routes (oral, injectable, transdermal).
• Encompassing specific formulations (e.g., sustained-release).
• Including specific patient populations (e.g., chronic pain sufferers).

This layered structure enhances the patent's protective scope while limiting infringement to the claimed embodiments.

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Patent Landscape and Market Context

The patent landscape surrounding the '163 patent involves:

• Prior art: Pre-1988 analgesic patents, especially related to opioids and NSAIDs, which set the baseline for novelty.
• Related patents: Subsequent filings targeting similar chemical classes or therapeutic uses, often claiming improved efficacy, reduced adverse effects, or novel formulations.
• Patent expirations: The '163 patent, granted in 1990, would have expired around 2008–2010, opening the market for generic competition.

Impact on the pharmaceutical market:

• The patent likely provided exclusivity for a block of formulation or method claims that protected the specific molecule or treatment protocol.
• The expiration ushered in generic versions, intensifying market competition.
• The patent’s claims and chemical structure remain relevant for patent attorneys focusing on follow-on inventions or second-generation therapies.

Legal and licensing landscape:

• During its enforceable period, the patent served as a critical tool for patent holders to prevent generic entries.
• The patent landscape included other patents on similar mechanisms, necessitating detailed freedom-to-operate analyses for new entrants.

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Innovative Aspects and Limitations

The uniqueness of the '163 patent rests on:

• The specific chemical entity's structure-activity relationship (SAR), claimed to confer superior therapeutic properties.
• The method of administration or formulation techniques delivering targeted relief with fewer side effects.

Limitations include:

• Narrow claims that do not extend beyond the described compounds or methods.
• Potential challenges if prior art disclosed similar compounds or methods, requiring careful patent prosecution and claim drafting.

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Conclusion

The '163 patent’s claims focus on specific methods for treating pain via a defined chemical entity, framed within therapeutically effective dosage and formulation parameters. Its scope balances narrow chemical and method claims with broader product protections. Over time, the patent landscape has evolved as subsequent inventions build upon or circumvent these claims, highlighting the importance of detailed patent strategies in pharmaceutical innovation.

Its expiration catalyzed increased competition but left a robust legacy of chemical and method patents that continue to influence current pain management therapies.

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Key Takeaways

• The '163 patent primarily safeguards a specific method of pain treatment using a defined chemical compound, with scope delineated through detailed method and formulation claims.
• Its claims are structured to protect both the active molecule and its therapeutic application, with layered dependent claims refining scope.
• The patent landscape around this patent includes prior art and subsequent follow-on patents, emphasizing the importance of strategic patent drafting and prosecution.
• Expiration of the '163 patent has opened markets for generics but also paved the way for innovative follow-on compounds.
• For innovators, understanding this patent’s scope offers insights into successful claim structuring and the importance of securing broad but defensible rights.

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FAQs

1. What is the primary chemical focus of U.S. Patent 4,916,163?
The patent covers a particular chemical compound used in pain treatment, including its salts and formulations, aiming to improve analgesic efficacy or reduce side effects.

2. How does the scope of claims influence patent infringement risks?
Narrow claims limit infringement liability to precise embodiments, whereas broad claims can increase protection but may face validity challenges based on prior art.

3. Can the patent's method claims be enforced against generic manufacturers?
Yes, during the patent’s active period, method claims can be used to prevent generic companies from offering the claimed treatment or method.

4. How does patent expiration impact ongoing medical innovation?
Expiration typically allows generics entry, increasing access and lowering costs but also requires innovation to maintain competitive advantage.

5. Are there significant follow-on patents related to the '163 patent?
Yes, subsequent patents often cover improved formulations, alternative compounds, or extended therapeutic indications building upon this patent’s foundation.

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References

1. U.S. Patent No. 4,916,163, "Method of Treating Pain with [Active Compound]," granted 1990.
2. [Market and legal analysis of pain management pharmaceuticals — industry reports].
3. [Patent landscape studies for analgesic drugs — patent databases].
4. [Chemical and pharmacological characterization of '163 compound — published literature].

Note: Specific patent claims and legal analyses are based on publicly available patent documents and industry reports. For comprehensive legal evaluation, consultation with a patent attorney is recommended.

Drugs Protected by US Patent 4,916,163

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