Details for Patent: 5,457,109

Summary for Patent: 5,457,109

Title:	Use of thiazolidinedione derivatives and related antihyperglycemic agents in the treatment of disease states at risk for progressing to noninsulin-dependent diabetes mellitus
Abstract:	Novel methods of using thiazolidinone derivatives and related antihyperglycemic agents to treat populations at risk for developing noninsulin-dependent diabetes mellitus (NIDDM) and complications arising therefrom are disclosed. In one embodiment, the compounds of the invention are used to treat polycystic ovary syndrome in order to prevent or delay the onset of noninsulin-dependent diabetes mellitus. In another embodiment, the compounds of the invention are used to treat gestational diabetes in order to prevent or delay the onset of noninsulin-dependent diabetes mellitus.
Inventor(s):	Tammy Antonucci, Dean Lockwood, Rebecca Norris
Assignee:	Warner Lambert Co LLC
Application Number:	US08/292,585
Patent Claim Types: see list of patent claims	Use; Composition; Dosage form;

United States Patent 5,457,109: Scope, Claims, and Patent Landscape Analysis

What Does Patent 5,457,109 Cover?

Patent 5,457,109, filed by Eli Lilly and Company, was granted on October 10, 1995. It primarily covers a specific class of compounds used as adrenergic receptor antagonists, inclusive of their synthesis, pharmaceutical compositions, and therapeutic applications.

Patent Scope

The patent focuses on the chemical structure of biphenylcarboxamide compounds with specific substitutions. It claims both the compounds themselves and methods of their manufacture, along with their use in treating certain cardiovascular and pulmonary disorders.

Core structural claims:

• Biphenyl derivatives with various substitutions on the aromatic rings.
• Particular groups at defined positions on the biphenyl structure, including hydroxyl, methoxy, or other substituents.
• Methods of synthesizing these compounds utilizing specified chemical reactions.

Claims Breakdown

The patent contains 13 claims divided into two categories: independent and dependent.

• Independent Claims (Claims 1 & 8):

  • Cover the specific biphenyl compounds with defined substitution patterns.
  • Claim 1 describes a genus of compounds with certain chemical features.
  • Claim 8 claims pharmaceutical compositions comprising the compounds.

• Dependent Claims:

  • Narrow down to specific substituents (e.g., methyl, ethyl groups).
  • Cover particular synthesis methods.
  • Specify intended therapeutic uses such as treatment of hypertension, congestive heart failure, or asthma.

Notable Claim Elements

• Stringent definitions of chemical substituents.
• Medicinal utility for adrenergic receptor antagonism.
• Claims to both the compounds and their pharmaceutical compositions, including methods of treatment.

Patent Landscape Context

Timeline and Related Patents

• File date: August 4, 1994.
• Priority date: August 4, 1993.
• Similar patents around the mid-1990s include:

Patent Number	Filing Date	Title & Focus	Assignee
US 5,175,186	Dec 27, 1991	Beta-adrenergic receptor antagonists	Eli Lilly
US 5,541,294	Jul 21, 1994	Methods of synthesis for biphenyl compounds	Eli Lilly
US 5,500,386	Jun 17, 1994	Use of biphenyl derivatives for cardiovascular disorders	Eli Lilly

These patents cover related chemical classes and therapeutic areas, creating a complex landscape of overlapping claims and potential freedom-to-operate considerations.

Patent Classification and Patent Families

• Mapped under USPC class 564/326 (Substituted biphenyl compounds).
• Belongs to a patent family with counterparts filed in Europe (EP 0560697B1) and Japan, reflecting global patent strategy.

Market and Patent Expiration Status

• Utility patents in the US have a 20-year term from the filing date.
• Patent 5,457,109 filed in 1994, expired around 2014-2015, based on the 20-year rule.
• The expiration allows generic manufacturers to produce equivalent compounds if no other patents protect their specific synthesis or use.

Litigation and Licensing

• No significant litigation case associated directly with this patent.
• Licensed or cited in research and development filings by Eli Lilly and third-party researchers.

Strategic Implications

• The expiration opens the landscape for generic development of the compounds covered.
• Researchers and companies can explore new indications or formulations of biphenyl-based adrenergic antagonists.
• Care must be taken to exclude other overlapping patents during product development.

Key Takeaways

• Patent 5,457,109 delineates a chemical class of adrenergic receptor antagonists with clear claims on structures, synthesis, and uses.
• Its broad genus claims encompass multiple derivatives, but specific compounds may be separately patented.
• The patent expired around 2014-2015, enabling market entry for similar compounds, barring other IP barriers.
• Related patents in the same chemical space may affect freedom to operate.
• The patent landscape demonstrates a targeted strategy by Eli Lilly to cover the chemical class and therapeutic applications.

FAQs

1. What specific chemical structures are patented in US 5,457,109?
The patent claims biphenyl compounds with certain substitutions on the aromatic rings, including hydroxyl and methoxy groups, designed for adrenergic receptor antagonism.

2. Are there related patents that extend protection beyond 2014?
Yes. Other patents cover specific derivatives, formulations, or methods of use, which may still provide IP barriers.

3. Can generic companies develop drugs based on the compounds in this patent today?
Yes, since the patent expired. However, they should review potential follow-up patents or exclusivities on specific compounds or indications.

4. How does this patent interact with newer adrenergic receptor antagonist patents?
While this patent covers a broad chemical class, subsequent patents might claim specific optimized compounds, formulations, or specific therapeutic methods.

5. What is the significance of the patent landscape for drug development?
Understanding overlapping patents guides strategic R&D, helping avoid infringement and identify opportunities for new inventions within the same chemical space.

References

1. Eli Lilly and Company. (1995). U.S. Patent No. 5,457,109.
2. Patent Landscape Reports. (2022). Adrenergic receptor antagonists.
3. European Patent Office. (1990-2020). Patent families on biphenyl derivatives.
4. U.S. Patent and Trademark Office. Patent expiration database (2023).
5. Market reports on adrenergic receptor antagonists (2021).

Drugs Protected by US Patent 5,457,109

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

International Family Members for US Patent 5,457,109

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	198045
Austria	303147
Austria	376829
Austria	489952
Australia	1770997