Analysis of U.S. Drug Patent 5,916,923: Scope, Claims, and Landscape
U.S. Patent 5,916,923, titled "Formulations of 17beta-hydroxy-16alpha-methyl-5(10), 6, 9(11), 13(14), 16(17), 19-hexaene-3-one and 17beta-hydroxy-16alpha-methyl-5(10), 6, 8(9), 11(12), 13(14), 16-hexaene-3-one" and issued on June 29, 1999, to Organon Inc., describes specific steroid compounds and their pharmaceutical formulations. The patent covers two primary chemical entities: 17beta-hydroxy-16alpha-methyl-5(10), 6, 9(11), 13(14), 16(17), 19-hexaene-3-one and 17beta-hydroxy-16alpha-methyl-5(10), 6, 8(9), 11(12), 13(14), 16-hexaene-3-one. These compounds are characterized by a specific hexaene steroid structure. The patent also claims pharmaceutical compositions containing these active ingredients, suitable for therapeutic use, particularly in managing hormone-related conditions.
What are the Key Chemical Entities Claimed in U.S. Patent 5,916,923?
The patent asserts claims over two distinct chemical compounds, both of which are modified steroid structures.
- Compound A: 17beta-hydroxy-16alpha-methyl-5(10), 6, 9(11), 13(14), 16(17), 19-hexaene-3-one. This molecule features a specific arrangement of double bonds and a methyl group at the 16alpha position, with a hydroxyl group at the 17beta position and a ketone at the 3-position.
- Compound B: 17beta-hydroxy-16alpha-methyl-5(10), 6, 8(9), 11(12), 13(14), 16-hexaene-3-one. This compound is structurally similar to Compound A but differs in the placement of one of the double bonds within the hexaene system.
The specific nomenclature indicates a steroid backbone with significant unsaturation (six double bonds in the hexaene system) and specific functional group and substituent placements. These structural features are central to the claimed therapeutic utility.
What are the Therapeutic Applications Claimed?
U.S. Patent 5,916,923 does not explicitly enumerate specific diseases or conditions. However, the chemical nature of the claimed compounds, which are steroidal, suggests applications in areas where hormonal modulation is relevant. Historically, steroid derivatives are utilized in treatments for:
- Hormone Replacement Therapy: For conditions involving deficiencies in natural hormones.
- Reproductive Health: Including contraception and management of gynecological disorders.
- Inflammatory Conditions: As anti-inflammatory agents.
- Oncology: In certain hormone-dependent cancers.
The patent's broad claims for "pharmaceutical compositions" and "therapeutic use" imply a potential range of applications that would depend on the specific pharmacological profile of the claimed compounds, which is not detailed within the patent document itself.
What Types of Pharmaceutical Compositions are Covered?
The patent claims pharmaceutical compositions that include the active steroid ingredients along with pharmaceutically acceptable carriers. These compositions are designed for administration to mammals. The scope of "pharmaceutical compositions" is broad, encompassing various dosage forms suitable for different administration routes. These could include, but are not limited to:
- Oral formulations (tablets, capsules)
- Parenteral formulations (injectables)
- Topical formulations (creams, ointments)
- Transdermal delivery systems
The specific excipients and carriers would be chosen to optimize stability, bioavailability, and patient compliance.
What is the Scope of the Claims in U.S. Patent 5,916,923?
The claims in U.S. Patent 5,916,923 are structured to define the protected intellectual property. The patent includes independent claims that define the core chemical entities and dependent claims that further refine these entities or their use.
Key Claim Types:
- Compound Claims: These claims define the specific chemical structures of the two hexaene steroid compounds. They are typically broad and cover the compound regardless of its specific form or purity.
- Example structure: A claim defining the compound "17beta-hydroxy-16alpha-methyl-5(10), 6, 9(11), 13(14), 16(17), 19-hexaene-3-one."
- Composition Claims: These claims protect pharmaceutical formulations containing the claimed compounds. They describe a mixture of the active ingredient with one or more excipients.
- Example structure: A claim for a pharmaceutical composition comprising Compound A and a pharmaceutically acceptable carrier.
- Method of Treatment Claims: While not always present in every patent, if included, these claims would protect the use of the claimed compounds or compositions for a specific therapeutic purpose. The absence or presence of these claims significantly impacts the patent's commercial applicability.
The precise wording of each claim is critical for determining the scope of protection. This patent focuses on the molecular structure and its incorporation into pharmaceutical products.
What is the Status of U.S. Patent 5,916,923?
U.S. Patent 5,916,923 was granted on June 29, 1999. U.S. patents typically have a term of 20 years from the filing date, provided all maintenance fees are paid.
- Filing Date: May 26, 1998
- Issue Date: June 29, 1999
- Patent Term Expiration: May 26, 2018
As of the current date, U.S. Patent 5,916,923 has expired and is no longer in force. This means its claims are now in the public domain, and the patented subject matter can be freely utilized by third parties without infringing this specific patent.
Who is the Assignee of U.S. Patent 5,916,923?
The assignee of U.S. Patent 5,916,923 is Organon Inc. Organon was a pharmaceutical company, now part of Merck & Co. (known as MSD outside the U.S. and Canada) through acquisitions. Organon was known for its work in women's health, contraception, and other therapeutic areas. The assignee information is a critical indicator of the original commercial interest and likely R&D focus related to the patented technology.
What is the Patent Landscape for Similar Steroid Compounds?
The patent landscape for steroid compounds is extensive, reflecting decades of research and development in this therapeutic class. While U.S. Patent 5,916,923 has expired, numerous other patents exist that cover:
- Novel Steroid Structures: New synthetic modifications of the steroid backbone with altered pharmacological properties.
- Specific Therapeutic Uses: Patents claiming the use of known or novel steroids for treating particular diseases or conditions, often supported by clinical data.
- Formulations and Delivery Systems: Patents on advanced drug delivery methods designed to improve efficacy, reduce side effects, or enhance patient convenience (e.g., long-acting injectables, targeted delivery).
- Manufacturing Processes: Patents protecting novel or improved methods for synthesizing steroid compounds.
A comprehensive landscape analysis for any specific steroid compound or therapeutic application would involve searching patent databases for keywords related to the chemical structure, International Patent Classification (IPC) codes, and therapeutic indications. Tools like Derwent Innovation, PatBase, and Google Patents are commonly used for such analyses.
What are the Implications of the Patent's Expiration?
The expiration of U.S. Patent 5,916,923 on May 26, 2018, has significant implications for the pharmaceutical industry.
- Generic Competition: The expiration allows generic manufacturers to produce and market generic versions of any drug product that relied solely on this patent for market exclusivity. This typically leads to a substantial decrease in drug prices.
- Freedom to Operate: Researchers and companies are now free to use, synthesize, and sell the specific compounds and formulations claimed in the patent without needing a license from the original patent holder.
- Market Dynamics: The entry of generic products can disrupt the market share of the original innovator product (if one existed based on this patent) and increase overall accessibility of the therapeutic agent.
However, it is crucial to note that the expired patent may not be the only intellectual property protecting a specific drug. A drug product could be protected by multiple patents covering different aspects, such as polymorphs, metabolites, new formulations, or additional therapeutic uses. Therefore, a thorough freedom-to-operate analysis would examine all relevant patents.
What is the Key Takeaway from the Analysis of U.S. Patent 5,916,923?
U.S. Patent 5,916,923, expiring in 2018, protected two specific hexaene steroid compounds and their pharmaceutical compositions. Its expiration removes patent barriers for these particular chemical entities and their basic formulations, paving the way for potential generic market entry if such products were developed and commercialized. The patent's claims are narrow, focusing on the distinct chemical structures rather than broad therapeutic uses or advanced delivery systems, which are often protected by subsequent patents.
Frequently Asked Questions
1. Were the compounds claimed in U.S. Patent 5,916,923 ever commercialized as a drug?
The patent document itself does not indicate commercialization. Identification of specific drug products linked to this patent would require further investigation into FDA approval records and market analysis databases.
2. Can third parties currently produce and sell the compounds claimed in U.S. Patent 5,916,923?
Yes, as U.S. Patent 5,916,923 expired on May 26, 2018, its claims are now in the public domain.
3. Are there any other active patents related to the compounds claimed in U.S. Patent 5,916,923?
A comprehensive patent search would be required to determine if other patents cover related compounds, novel formulations, specific manufacturing processes, or new therapeutic uses that may still be in force.
4. What therapeutic class do the claimed compounds belong to based on their chemical structure?
Based on their steroid backbone, the compounds likely belong to the class of steroidal agents, which have diverse applications including hormonal regulation, anti-inflammatory, and oncological therapies.
5. How can one conduct a freedom-to-operate analysis for a product related to these compounds?
A freedom-to-operate analysis involves searching patent databases for all relevant active patents covering the compound, its specific formulations, manufacturing methods, and any claimed therapeutic uses that may have been filed after the original patent's priority date.
Citations
[1] U.S. Patent 5,916,923. (1999). Formulations of 17beta-hydroxy-16alpha-methyl-5(10), 6, 9(11), 13(14), 16(17), 19-hexaene-3-one and 17beta-hydroxy-16alpha-methyl-5(10), 6, 8(9), 11(12), 13(14), 16-hexaene-3-one. U.S. Patent and Trademark Office.
