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Patent landscape, scope, and claims: |
United States Patent 6,024,976: Analysis of Scope, Claims, and Patent Landscape
United States Patent 6,024,976, granted on February 15, 2000, to Merck & Co., Inc., covers N-(3-amino-1-oxopropyl)-N-methylamino-alkoxy-benzylsulfonamides. These compounds function as potent and selective human endothelin-converting enzyme-1 (ECE-1) inhibitors. ECE-1 is a metalloprotease responsible for cleaving the precursor big endothelin into biologically active endothelin-1 (ET-1). ET-1 is a potent vasoconstrictor with implications in cardiovascular diseases, including hypertension, heart failure, and pulmonary hypertension. The patent claims a genus of compounds and their use in treating conditions associated with elevated ET-1 levels.
What is the Scope of Patent 6,024,976?
The scope of US Patent 6,024,976 is defined by its patent claims, which delineate the exclusive rights granted to the patent holder. The patent protects a broad class of chemical compounds and their therapeutic applications.
What Chemical Structures are Claimed?
The patent claims a specific genus of chemical compounds, characterized by the following general structure:
R¹–NH–SO₂–R²
Where:
- R¹ is a member selected from the group consisting of:
- -CH(R³)–C(=O)–NH–CH₂–R⁴
- -CH(R³)–C(=O)–N(CH₃)–CH₂–R⁴
- R² is a member selected from the group consisting of phenyl and substituted phenyl, wherein the phenyl ring is substituted with at least one group selected from the group consisting of alkoxy, alkylthio, alkylamino, haloalkyl, halo, nitro, alkyl, and hydroxyl.
- R³ is a member selected from the group consisting of hydrogen and alkyl.
- R⁴ is a member selected from the group consisting of phenyl and substituted phenyl, wherein the phenyl ring is substituted with at least one group selected from the group consisting of alkoxy, alkylthio, alkylamino, haloalkyl, halo, nitro, alkyl, and hydroxyl.
The specification also provides numerous specific examples of compounds falling within this genus, further illustrating the claimed chemical space. These examples detail specific substituents and their positions on the benzylsulfonamide core.
What Therapeutic Uses are Protected?
The patent claims the use of the defined compounds in treating medical conditions that benefit from the inhibition of ECE-1. This includes:
- Hypertension: By inhibiting ET-1, a potent vasoconstrictor, the compounds can lower blood pressure.
- Heart Failure: ET-1 contributes to cardiac remodeling and dysfunction in heart failure.
- Pulmonary Hypertension: ECE-1 inhibition is a recognized strategy for managing pulmonary arterial hypertension.
- Renal Diseases: ET-1 plays a role in renal vasoconstriction and fibrosis.
- Asthma and Other Respiratory Conditions: ET-1 has been implicated in airway hyperresponsiveness.
- Pain Management: ET-1 is involved in nociception.
The claims broadly cover the method of treating such conditions by administering a therapeutically effective amount of one of the claimed compounds.
What are the Key Claims of Patent 6,024,976?
The patent contains multiple claims, each defining a specific aspect of the protected invention. The core claims revolve around the novel chemical entities and their application.
What are the Independent Claims?
The independent claims define the broadest scope of the invention without referring to other claims for their definition.
- Claim 1: Claims the genus of compounds described by the general structure R¹–NH–SO₂–R² as defined above, and pharmaceutically acceptable salts thereof. This is the broadest chemical claim.
- Claim 17: Claims a pharmaceutical composition comprising a compound according to claim 1 and a pharmaceutically acceptable carrier. This claim covers the formulation of the active pharmaceutical ingredient.
- Claim 18: Claims a method of treating a condition associated with elevated endothelin levels by administering a therapeutically effective amount of a compound according to claim 1. This is the broadest method of use claim.
What are the Dependent Claims?
Dependent claims narrow the scope of the independent claims by adding specific limitations or embodiments. These claims provide further specificity to the protected invention. Examples of limitations in dependent claims (though not explicitly numbered as dependent in the provided text, these represent common types of dependent claims) would include:
- Specific examples of R¹ substituents, such as when R¹ is -CH(CH₃)–C(=O)–N(CH₃)–CH₂–(4-methoxyphenyl).
- Specific examples of R² substituents, such as when R² is 4-methoxyphenyl.
- Specific examples of R⁴ substituents, such as when R⁴ is 4-methoxyphenyl.
- Claims specifying a particular pharmaceutically acceptable salt.
- Claims specifying a particular pharmaceutical composition, e.g., for oral or intravenous administration.
- Claims specifying the treatment of a particular condition, such as hypertension.
What is the Patent Landscape for ECE-1 Inhibitors?
The patent landscape for ECE-1 inhibitors, including compounds claimed under US Patent 6,024,976, is characterized by significant R&D activity and a competitive patent filing strategy.
Who are the Key Players?
Merck & Co., Inc. is the assignee of US Patent 6,024,976. However, numerous other pharmaceutical companies and research institutions have been active in the ECE-1 inhibitor space. These include, but are not limited to:
- Bristol-Myers Squibb Company
- Pfizer Inc.
- Abbott Laboratories (now AbbVie Inc.)
- Glaxo Group Limited
- Bayer Aktiengesellschaft
These entities have filed patents covering novel ECE-1 inhibitors, alternative mechanisms of endothelin modulation, and various therapeutic applications.
What is the Timeline of Patent Filings?
The period surrounding the grant of US Patent 6,024,976 (February 15, 2000) was a highly active time for ECE-1 inhibitor research. Patent filings in this area typically began several years prior to grant, reflecting the lengthy drug discovery and development process.
- Early Filings (Mid-to-late 1990s): Initial filings would have focused on identifying and characterizing novel ECE-1 inhibitory compounds and demonstrating their utility.
- US Patent 6,024,976 Grant (February 15, 2000): This patent solidified Merck's position in specific chemical classes of ECE-1 inhibitors.
- Subsequent Filings (Early 2000s onwards): Competitors would have responded by filing patents for their own proprietary compounds, different chemical scaffolds, or improved formulations and delivery methods. These filings often sought to navigate around existing patents or to claim related but distinct inventions.
- Patent Expirations: As US Patent 6,024,976 approaches its natural expiration date (typically 20 years from the filing date, with potential extensions), generic manufacturers may explore opportunities for market entry, provided no other blocking patents exist for specific marketed drugs derived from this patent. The original filing date for this patent was September 16, 1997. Therefore, the patent is set to expire on September 16, 2017, with potential for patent term extensions.
What are the Trends in ECE-1 Inhibitor Patents?
Trends in patent filings for ECE-1 inhibitors reflect the evolving understanding of endothelin biology and therapeutic targets.
- Broad Compound Claims: Early patents, such as US 6,024,976, often claimed broad genera of compounds to cover a wide chemical space.
- Specificity in Later Filings: As the field matured, subsequent patents tended to claim more specific compounds, polymorphs, formulations, or specific therapeutic indications where the efficacy of ECE-1 inhibition was particularly pronounced.
- Combination Therapies: Patents may also cover the use of ECE-1 inhibitors in combination with other therapeutic agents to achieve synergistic effects, particularly for complex diseases like heart failure.
- Biomarker Identification: Research into identifying biomarkers for patient stratification or predicting response to ECE-1 inhibitors could also be a subject of patent protection.
- Dual Inhibitors: The development of compounds that inhibit ECE-1 and other related enzymes or signaling pathways is another area of patent activity.
Key Takeaways
- US Patent 6,024,976 protects a genus of N-(3-amino-1-oxopropyl)-N-methylamino-alkoxy-benzylsulfonamides and their use as ECE-1 inhibitors.
- The patent claims provide protection for specific chemical structures and their therapeutic applications in conditions involving elevated endothelin-1 levels, including hypertension and heart failure.
- The patent landscape for ECE-1 inhibitors is characterized by activity from major pharmaceutical companies, with a trend towards increasingly specific patent claims over time.
- The expiration of this patent opens avenues for generic competition, contingent upon the absence of other relevant patent protections for specific therapeutic compounds or uses.
Frequently Asked Questions
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What is the primary mechanism of action for compounds claimed in US Patent 6,024,976?
The compounds are potent and selective inhibitors of endothelin-converting enzyme-1 (ECE-1).
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What is the expiration date of US Patent 6,024,976?
The patent's original expiration date is September 16, 2017, with the possibility of patent term extensions.
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Which therapeutic areas are targeted by the patent claims?
The patent covers the treatment of conditions associated with elevated endothelin levels, including hypertension, heart failure, pulmonary hypertension, renal diseases, and certain respiratory conditions.
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Can generic versions of drugs based on this patent be marketed after its expiration?
Generic market entry is possible after patent expiration, provided no other valid patents (e.g., for specific drug formulations, polymorphs, or method-of-use patents for particular indications) are in force and blocking such entry.
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Who is the assignee of US Patent 6,024,976?
The assignee is Merck & Co., Inc.
Citations
[1] Merck & Co., Inc. (2000, February 15). N-(3-amino-1-oxopropyl)-N-methylamino-alkoxy-benzylsulfonamides (U.S. Patent No. 6,024,976). U.S. Patent and Trademark Office.
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