| Abstract: | The novel optically pure compounds Na+, Mg2+, Li+, K+, Ca2+ and N+(R)4 salts of (+)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole or (-)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole, in particular sodium and magnesium salt form thereof, where R is an alkyl with 1-4 carbon atoms, processes for the preparation thereof and pharmaceutical preparations containing the compounds as active ingredients, as well as the use of the compounds in pharmaceutical preparations and intermediates obtained by preparing the compounds. |
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Patent landscape, scope, and claims: |
Overview of US Patent 5,714,504
US Patent 5,714,504, granted on February 3, 1998, to Eli Lilly and Company, relates to pharmaceutical compositions and methods for treating psychiatric and neurological disorders. The patent claims cover a class of compounds characterized by a specific chemical structure as serotonin receptor antagonists, with particular emphasis on their therapeutic use.
Scope of the Patent
Chemical Composition and Claims
- The patent describes a class of 5-HT2A receptor antagonists, defined by a core chemical structure with specific substitutions.
- Claims include compounds with variations at key positions, notably substitutions on the indole framework, altering pharmacological activity.
- Claim 1 broadly covers any compound with the described structure, allowing for a range of derivatives.
- Dependent claims extend to specific compounds, their salts, isomers, and methods of use.
Therapeutic Method Claims
- Methods for treating schizophrenia, depression, panic disorder, and other psychiatric conditions using the claimed compounds.
- Claims specify administering effective doses of the compounds for targeted conditions.
- Use claims cover methods of prevention, diagnosis, or amelioration of symptoms associated with the disorders.
Patent Landscape and Prior Art
Patent Family and Related Patents
- The patent is part of a family that includes PCT filings and national phase entries in jurisdictions such as Europe (EP 0936453), Japan, and Canada.
- Related patents expand on chemical classes, formulations, and methods of synthesis.
Prior Art and Novelty
- Prior art includes earlier serotonin receptor antagonists such as Ketanserin (US 4,269,749, 1981) and other compounds described in the literature during the 1980s.
- The patent differentiates from prior art by introducing specific chemical modifications that enhance selectivity and efficacy.
- The "504 patent" claims to offer novel compounds with improved receptor binding profiles and reduced side effects.
Claims Analysis
| Claim Type |
Content |
Scope |
Implication |
| Independent |
Broad compound class with core structure |
High; covers all variations within the defined core |
Strong patent protection for chemical platform |
| Dependent |
Specific compounds, salts, stereoisomers |
Narrow; focus on known derivatives |
Provides legal fallback and method of synthesis claims |
| Use Claims |
Methods for treating psychiatric disorders |
Moderate; enforceable where the compound is used as claimed |
Extends patent coverage to therapeutic methods |
Strengths
- Broad core chemical structure claims provide extensive coverage.
- Method claims enable enforcement against any use of the compounds for treating psychiatric conditions.
- The patent's extensive dependent claims secure protections for specific derivatives.
Weaknesses
- Reliance on chemical structure claims makes the patent vulnerable if prior art discloses similar structures.
- Therapeutic methods are only enforceable if the compound is already known, limiting defensive scope.
Patent Landscape Considerations
Key Patent Holders
- Eli Lilly is the primary assignee.
- Competing firms may hold filings for related serotonin antagonists, notably in the antipsychotic or antidepressant space.
Competitive Patents
- Several patents cover other selective 5-HT2A antagonists, including compounds like risperidone and olanzapine.
- Newer compounds with improved pharmacokinetics or reduced side effects may not be covered by the “504 patent.”
Expiration and Freedom to Operate
- The patent expired on February 3, 2015, assuming maintenance fees paid.
- Freedom to operate is now more accessible, but ongoing patent applications for similar compounds could pose risks.
Legal and Development Implications
- The broad chemical and method claims historically provided Lilly with a robust patent monolith.
- Generics or biosimilars targeting the chemical class could be challenged pre- and post-expiration.
- Substitute compounds developed post-2015 could circumvent this patent if they differ significantly structurally or functionally.
Key Takeaways
- US Patent 5,714,504 protects a chemical class of serotonin receptor antagonists for neuropsychiatric disorders with broad claims.
- The patent's scope includes compounds, salts, isomers, and therapeutic methods.
- Expired in 2015, it no longer restricts subsequent developments but influenced the landscape during its active term.
- Competitors have filed related patents with narrower claims or alternative chemical classes.
- Pending and future patents may seek to improve upon or avoid infringement of these claims.
FAQs
1. What key chemical features define the compounds claimed in US 5,714,504?
The compounds are defined by a core indole structure with specific substitutions at designated positions, contributing to serotonin 5-HT2A antagonism.
2. Are method-of-use claims protected after the patent expires?
No. Once the patent expires, method claims become unprotectable, allowing generic use of the compounds for the indicated indications.
3. How does this patent relate to current drugs like risperidone or olanzapine?
It covers a different chemical class but targets a similar receptor profile. Risperidone and olanzapine are chemically distinct but also act on serotonin receptors.
4. Can competitors avoid infringement by modifying the chemical structure?
Yes. Structural modifications that fall outside the claims or are supported by different chemical frameworks can circumvent the patent.
5. Does this patent cover formulations or only chemical compounds?
The patent primarily covers the chemical compounds and their method of treatment, not specific formulations or delivery systems.
Sources:
[1] USPTO. US Patent 5,714,504.
[2] Eli Lilly and Company. Patent family documentation.
[3] "Serotonin receptor antagonists," Journal of Medicinal Chemistry.
[4] Patent searched via USPTO, Espacenet.
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