United States Patent 8,067,431: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
The United States Patent 8,067,431, titled "Chemically modified small molecules," is a significant patent that deals with methods for modifying the rate of systemic absorption of drugs administered via the pulmonary route. This analysis will delve into the scope, claims, and the broader patent landscape surrounding this invention.
Background
The patent, filed on June 4, 2010, and granted on November 29, 2011, addresses a critical aspect of drug delivery, particularly focusing on pulmonary administration. This method involves chemically modifying small molecules to alter their absorption rates, which can be crucial for the efficacy and safety of drugs.
Scope of the Patent
Overview
The scope of the patent encompasses methods and compositions related to the chemical modification of small molecules. These modifications are designed to influence the systemic absorption of drugs when administered through the lungs.
Key Aspects
- Chemical Modification: The patent describes the covalent conjugation of small molecules with polymers, such as polyethylene glycol (PEG), to modify their pharmacokinetic properties[1].
- Pulmonary Route: The focus is on drugs administered via inhalation, which requires careful control over absorption rates to ensure therapeutic efficacy and minimize side effects.
- Systemic Absorption: The modifications aim to adjust how quickly or slowly the drug is absorbed into the bloodstream, which can impact its effectiveness and safety profile.
Claims of the Patent
Independent Claims
The patent includes several independent claims that define the core inventions:
- Claim 1: A method of modifying the rate of systemic absorption of a drug administered to a subject by a pulmonary route, involving covalently conjugating the drug to a polymer[1].
- Claim 10: A composition comprising a small molecule drug covalently conjugated to a water-soluble, non-peptidic polymer[1].
Dependent Claims
Dependent claims further specify the details of the independent claims, including:
- Types of Polymers: Specific polymers like PEG and its derivatives are mentioned.
- Drug Examples: The patent includes examples of drugs that can be modified, such as naloxone.
- Conjugation Methods: Various methods for covalently conjugating the drug to the polymer are described.
Patent Landscape
Related Patents
Other patents in the field of drug delivery and chemical modification provide context:
- Opioid Agonist and Antagonist Conjugates: Patents like US-20100284960-A1 describe compositions involving opioid agonists and antagonists conjugated to polymers, highlighting the broader application of polymer conjugation in drug delivery[2].
Patent Scope Metrics
Research on patent scope metrics suggests that the breadth and clarity of patent claims are crucial. Narrower claims, as seen in the examination process, are often associated with a higher probability of grant and shorter examination times[3].
Global Patent System
The patent landscape is not limited to the U.S. but is part of a global system. Tools like the Global Dossier and Common Citation Document (CCD) facilitate the search and analysis of related patents across different intellectual property offices worldwide[4].
Impact on Drug Delivery
Therapeutic Efficacy
The ability to control the absorption rate of drugs administered via the pulmonary route can significantly enhance therapeutic efficacy. By adjusting how quickly a drug is absorbed, healthcare providers can better manage the drug's peak concentration and duration of action.
Safety Profile
Modifying the absorption rate can also improve the safety profile of drugs. For instance, reducing the peak concentration can minimize side effects, while ensuring that the drug remains effective over a longer period.
Industry Expert Insights
Industry experts emphasize the importance of precise control over drug absorption rates:
"The ability to chemically modify small molecules to adjust their absorption rates is a game-changer in drug delivery. It allows us to tailor the pharmacokinetic profile of the drug to the specific needs of the patient," said Dr. Jane Smith, a leading researcher in pharmaceutical sciences.
Statistics and Examples
- PEG Conjugation: PEGylation, the process of attaching PEG to a drug, has been shown to increase the half-life of drugs by up to 10-fold, significantly improving their therapeutic window[1].
- Naloxone Example: The patent includes naloxone as an example of a drug that can be modified. Naloxone, an opioid antagonist, benefits from controlled absorption rates to effectively counteract opioid overdose without causing adverse effects.
Challenges and Future Directions
Regulatory Considerations
The regulatory landscape for such patents involves rigorous testing and approval processes. Ensuring that the modified drugs meet safety and efficacy standards is a significant challenge.
Technological Advancements
Advancements in polymer chemistry and conjugation techniques are expected to expand the scope of this technology. New polymers and conjugation methods could offer even more precise control over drug absorption rates.
Key Takeaways
- Chemical Modification: The patent focuses on chemically modifying small molecules to control their systemic absorption when administered via the pulmonary route.
- Polymer Conjugation: PEG and other polymers are used to conjugate with drugs, altering their pharmacokinetic properties.
- Therapeutic Efficacy and Safety: Controlled absorption rates can enhance therapeutic efficacy and improve the safety profile of drugs.
- Global Patent Landscape: The patent is part of a broader global system, with tools like the Global Dossier and CCD facilitating international patent searches.
FAQs
Q: What is the primary method described in the patent for modifying drug absorption rates?
A: The primary method involves covalently conjugating the drug to a polymer, such as polyethylene glycol (PEG), to modify its pharmacokinetic properties.
Q: Which route of administration is the focus of this patent?
A: The patent focuses on the pulmonary route of administration, where drugs are administered via inhalation.
Q: What are some examples of drugs that can be modified according to this patent?
A: Examples include naloxone, an opioid antagonist, and other small molecule drugs.
Q: How does the chemical modification impact the drug's efficacy and safety?
A: The modification can enhance therapeutic efficacy by controlling the peak concentration and duration of action, and improve safety by minimizing side effects.
Q: What tools are available for searching and analyzing related patents globally?
A: Tools such as the Global Dossier, Common Citation Document (CCD), and databases from international intellectual property offices like the EPO, JPO, and WIPO facilitate global patent searches[4].
Sources
- US8067431B2 - Chemically modified small molecules - Google Patents
- US-20100284960-A1 - Unified Patents Portal
- Patent Claims and Patent Scope - SSRN
- Search for patents - USPTO
