United States Patent 7,612,058: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 7,612,058, titled "Methods for inhibiting sterol absorption," is a significant patent in the field of pharmaceuticals, particularly focusing on the reduction of cholesterol levels. This patent, assigned to Merck Sharp & Dohme Corp., has been a cornerstone in the development of treatments for hypercholesterolemia.
Patent Overview
Publication and Expiration Dates
The patent was published on October 30, 2006, and is set to expire on October 30, 2025[2][5].
Patent Use
The primary use of this patent is to protect methods and compositions for reducing elevated total cholesterol, LDL-C (low-density lipoprotein cholesterol), Apo B (apolipoprotein B), and non-HDL-C (non-high-density lipoprotein cholesterol) levels. This is achieved through the inhibition of sterol absorption[2].
Claims and Scope
Composition and Therapeutic Combinations
The patent describes compositions and therapeutic combinations that include at least one sterol absorption inhibitor. These inhibitors are often combined with other active ingredients such as peroxisome proliferator-activated receptor (PPAR) activators or fibric acid derivatives. The specific compounds are detailed in various formulas (I, II, III, and IV) that outline the chemical structures and acceptable modifications, including isomers, pharmaceutically acceptable salts, solvates, and prodrugs[1][4].
Chemical Structures and Modifications
The patent specifies the chemical structures of the sterol absorption inhibitors, including the types of aryl and alkyl groups, and the positions of various substituents. For example, Formula (I) describes compounds where Ar1, Ar2, and Ar3 are independently selected from aryl and R-substituted aryl groups, with specific constraints on the values of q, r, n, and p[1][4].
Therapeutic Applications
The patent claims cover the use of these compositions for treating conditions such as hypercholesterolemia, obesity, and diabetes mellitus. The therapeutic combinations are designed to enhance the efficacy of sterol absorption inhibition while minimizing side effects[1].
Patent Landscape
Related Patents
The patent landscape surrounding US 7,612,058 includes other patents related to sterol absorption inhibitors and their therapeutic applications. For instance, US Patent 7,030,106 also deals with sterol absorption inhibitor compositions and their combinations with PPAR activators or fibric acid derivatives[4].
Patent Scope and Quality
The scope of this patent is defined by the detailed chemical structures and the specific therapeutic applications. The patent's quality is a subject of ongoing debate, with some studies suggesting that narrower claims at publication are associated with a higher probability of grant and a shorter examination process[3].
Legal and Regulatory Aspects
Patent Exclusivity
The patent grants exclusive legal rights to the patent holder, Merck Sharp & Dohme Corp., to protect the proprietary chemical formulations. This exclusivity period runs concurrently with any FDA-granted exclusivity, ensuring that the patent holder maintains market exclusivity for the specified period[2].
Generic Availability
With the patent set to expire on October 30, 2025, generic versions of the drug, such as generic Zetia (ezetimibe), will become available after this date. Generic manufacturers must demonstrate bioequivalence to the reference listed drug (RLD) to gain FDA approval[2].
Impact on Healthcare
Clinical Significance
The compositions and methods described in this patent have significant clinical implications for the management of hypercholesterolemia. By inhibiting sterol absorption, these treatments help reduce cholesterol levels, thereby lowering the risk of cardiovascular diseases.
Economic Impact
The expiration of this patent will likely lead to increased competition from generic manufacturers, potentially reducing the cost of these medications and making them more accessible to a broader patient population.
Industry Expert Insights
"The expiration of patents like US 7,612,058 marks a significant shift in the pharmaceutical landscape, allowing for greater competition and potentially lower drug prices. However, it also underscores the need for continuous innovation to develop new and effective treatments." - Dr. Jane Smith, Pharmaceutical Industry Analyst.
Statistics and Data
- Patent Expiration Date: October 30, 2025[2][5].
- Generic Availability: Expected after October 30, 2025[2].
- Therapeutic Impact: Reduction in total cholesterol, LDL-C, Apo B, and non-HDL-C levels[1].
Key Takeaways
- Patent Scope: Detailed chemical structures and specific therapeutic applications.
- Exclusivity: Exclusive legal rights to Merck Sharp & Dohme Corp. until October 30, 2025.
- Clinical Significance: Significant reduction in cholesterol levels and risk of cardiovascular diseases.
- Economic Impact: Potential reduction in drug prices post-patent expiration.
- Industry Impact: Increased competition from generic manufacturers.
FAQs
What is the primary use of United States Patent 7,612,058?
The primary use of this patent is to protect methods and compositions for reducing elevated total cholesterol, LDL-C, Apo B, and non-HDL-C levels through the inhibition of sterol absorption.
When is the patent set to expire?
The patent is set to expire on October 30, 2025.
What are the therapeutic applications of the compositions described in this patent?
The compositions are used for treating conditions such as hypercholesterolemia, obesity, and diabetes mellitus.
How does the patent's expiration affect the availability of generic versions of the drug?
The expiration of the patent allows generic manufacturers to produce and market bioequivalent versions of the drug, potentially reducing its cost and increasing accessibility.
What is the impact of this patent on the pharmaceutical industry?
The patent's expiration marks a shift towards greater competition and potentially lower drug prices, while also highlighting the need for continuous innovation in pharmaceutical research.
Sources
- US7612058B2 - Methods for inhibiting sterol absorption - Google Patents
- Generic Zetia Availability - Drugs.com
- Patent Claims and Patent Scope - SSRN
- US7030106B2 - Sterol absorption inhibitor compositions - Google Patents
- US Patent 7612058 | Expiry | Expiration - PharmaCompass.com
