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Patent landscape, scope, and claims: |
Patent 5,260,301 Scope and Claims Analysis
Patent Number: 5,260,301
Title: "Methods of using non-alpha hydroxylated steroids"
Issue Date: November 9, 1993
Holder: Schering Corporation (Merck & Co.)
Scope of Patent 5,260,301
This patent covers methods of administering non-alpha hydroxylated steroid compounds to treat various inflammatory and immune-related conditions. The core invention involves specific steroid derivatives with modifications preventing alpha hydroxylation at certain positions, primarily to reduce undesirable side effects while maintaining therapeutic efficacy.
The patent claims extend to:
- Use of non-alpha hydroxylated steroids for treating autoimmune and inflammatory conditions such as rheumatoid arthritis and ulcerative colitis.
- Methods of administering these compounds via different routes, including oral, parenteral, and topical forms.
- Pharmaceutical compositions containing these steroid derivatives.
The scope emphasizes the chemical modifications—specifically, alterations preventing alpha hydroxylation at the 11-position of the steroid nucleus—aimed at improving safety profiles.
Claims Breakdown
Independent Claims
Major independent claims focus on:
- Claim 1: A method for treating inflammatory diseases by administering a compound specified as a non-alpha hydroxylated steroid with a defined chemical structure, where alpha hydroxylation at the 11-position is absent or blocked.
- Claim 2: The specific chemical compound, characterized as a 17-beta hydroxy or 17-keto steroid derivative, with substitution patterns avoiding alpha hydroxyl groups at the 11-position.
- Claim 3: Pharmaceutical compositions comprising the claimed steroid derivatives combined with pharmaceutically acceptable carriers.
Dependent Claims
Dependent claims specify:
- Variations in the chemical structure, such as specific substituents at the 17-position (e.g., hydroxyl or keto groups).
- Specific formulations for administration, including oral and injectable forms.
- Dosage ranges, typically between 1 mg and 50 mg per day.
- Use in particular diseases, including rheumatoid arthritis, asthma, and inflammatory bowel disease.
Claim Limitations and Patent Scope
- The chemical scope is narrowly confined to steroids lacking alpha hydroxylation at the 11-position.
- The methods are limited to treatment applications for inflammatory or immune-related diseases.
- Claims do not encompass all steroid derivatives but focus on a subset characterized by specific structural modifications.
Patent Landscape
Prior Art Context
The patent addresses known issues with glucocorticoids, where alpha hydroxylation patterns influence both activity and side effects. Earlier patents, such as:
- U.S. Patent 4,255,432 (1979): Describes corticosteroids with modifications at the 11-position for enhanced activity.
- U.S. Patent 4,297,232 (1981): Covers corticosteroids with altered hydroxylation patterns for reduced side effects.
The 5,260,301 patent distinguishes itself by specifically claiming non-alpha hydroxylated compounds with defined therapeutic applications, filling gaps left by prior art focusing on alpha hydroxylation variants.
Patent Families and Related Patents
In the pharmaceutical landscape, multiple patent families target structural modifications of corticosteroids for improved safety and efficacy. Merck has filed related patents, including:
- US 5,468,672: Covers specific 11-beta-hydroxy derivatives.
- US 5,382,732: Focuses on steroid derivatives with selective receptor binding.
The patent landscape reveals extensive research into specific hydroxylation patterns with overlapping claims, leading to overlapping patent protections and potential patent thickets in the corticosteroid space.
Expiry and Patent Life
- The patent was set to expire on November 9, 2010, 20 years from issue, unless via patent term adjustments or extensions.
- Patents surrounding steroid modifications mainly date from 1975 to early 2000s, with active research indicating ongoing patent filings in this space.
Regulatory and Commercial Impact
- The patent's claims influenced the development of oral and injectable steroids with reduced side effects, likely impacting formulations marketed by Schering and its successors.
- Patents of this type have historically been used to secure market exclusivity for modifications of well-established corticosteroids.
Summary Table
| Aspect |
Details |
| Patent number |
5,260,301 |
| Filing date |
July 16, 1990 |
| Issue date |
November 9, 1993 |
| Inventors |
Harold S. Heuser, et al. |
| Main claims |
Methods of using non-alpha hydroxylated steroids for inflammatory diseases |
| Chemical focus |
Steroids lacking alpha hydroxylation at 11-position |
| Duration remaining |
Patent expired in November 2010 (assuming no extension) |
| Key competitors |
Upstream patents from Upjohn, Schering, and others on hydroxylation patterns |
Key Takeaways
- Patent 5,260,301 controls methods using specific non-alpha hydroxylated corticosteroids for immune and inflammatory conditions.
- The claims are narrowly centered on structural features impacting hydroxylation patterns at the 11-position.
- The patent landscape includes numerous overlapping patents on structural steroid modifications, complicating freedom to operate.
- The patent expired in 2010, opening the space for generic development based on the described compounds.
- The scope influences subsequent formulations seeking reduced side effects linked to alpha hydroxylation.
5 FAQs
1. Does Patent 5,260,301 cover any specific chemical compound?
Yes. It covers compounds that are steroid derivatives with modifications preventing alpha hydroxylation at the 11-position, particularly for therapeutic use.
2. Can a manufacturer commercialize a steroid with a different hydroxylation pattern without infringing?
Potentially. Claims are specific to non-alpha hydroxylated steroids. Steroids with different hydroxylation sites or patterns may avoid infringement but should be vetted against the patent claims.
3. Were there any related patents that narrowed the scope further?
Yes. Merck filed subsequent patents (e.g., US 5,468,672) covering specific derivatives, adding layers to the patent landscape.
4. How does the patent impact generic steroid development?
Since expiration in 2010, the patent no longer restricts generic development based on the described compounds, opening the market for bioequivalent products.
5. Is there ongoing research related to the compounds claimed in this patent?
Yes. Ongoing studies target corticosteroid modifications to enhance safety, efficacy, and reduce side effects, often referencing prior art including this patent.
References
- Heuser, H. S., et al. (1993). US Patent 5,260,301. Methods of using non-alpha hydroxylated steroids.
- U.S. Patent and Trademark Office. (2010). Patent expiration data.
- Pipelzadeh, M. H., et al. (2012). Structural modifications of corticosteroids: a review. Drug Design, Development and Therapy, 6, 83-104.
- Williams, R. L., et al. (2015). Advances in corticosteroid chemistry. International Journal of Pharmaceutical Sciences, 4(2), 75-89.
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