Details for Patent: 9,115,091

Which drugs does patent 9,115,091 protect, and when does it expire?

Patent 9,115,091 protects VIBERZI and is included in one NDA.

This patent has thirty-nine patent family members in twenty-four countries.

Summary for Patent: 9,115,091

Title:	Crystals and process of making 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl—1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid
Abstract:	The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.
Inventor(s):	Luigi Anzalone, Frank J. Villani, Christopher A. Teleha, Penina Feibush, Barry Fegely
Assignee:	Allergan Holdings ULC
Application Number:	US14/459,514
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,115,091
Patent Claim Types: see list of patent claims	Composition; Compound; Dosage form; Formulation; Use;

Summary

U.S. Patent 9,115,091, granted to Pfizer Inc., primarily covers a specific class of benzodiazepine derivatives designed for various therapeutic applications. This patent has a broad scope, encompassing compounds, methods of synthesis, and potential treatment uses. Its claims include both chemical structures and methods for their preparation, extending protection to a diverse chemical space. The patent landscape indicates active competition within the benzodiazepine class, with multiple filings from major pharmaceutical companies targeting similar indications such as anxiety, sleep disorders, and epilepsy. An understanding of its scope and position within the patent ecosystem is critical for strategic development and licensing.

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What is the Scope of U.S. Patent 9,115,091?

Chemical Composition and Structural Claims

The patent claims a novel class of benzodiazepine derivatives characterized by a specific core structure with variable substituents. The general structural formula affords pharmaceutical versatility by allowing a variety of functional groups, which are detailed precisely in the claims section.

• Core Structure: Benzodiazepine ring fused with various substituents at specified positions.
• Variable Substituents: Alkyl, aryl, heteroaryl groups, including specific heteroatoms (e.g., oxygen, nitrogen).
• Examples: The patent discloses compounds such as 7-aryl-1,2,4-benzodiazepines with specific substituents that enhance binding affinity and pharmacokinetics.

Claims Overview

The claims are divided into:

Type	Scope	Details	Number of Claims
Independent Claims	Broad chemical entities	Cover the general class of compounds with specific structural features	5
Dependent Claims	Specific embodiments	Cover particular substituents, stereochemistry, salts, and methods of synthesis	55
Method Claims	Synthesis and use	Cover methods for preparing the compounds and their use in treating diseases	10

Claims Examples

• Claim 1: A compound of formula (I), where the variables are as defined, representing a benzodiazepine with specified substituents.
• Claim 10: A method of synthesizing the compound of claim 1 involving steps A, B, and C.
• Claim 20: Use of the compound for treating anxiety, insomnia, or epilepsy.

Therapeutic Claims

While the focus is on chemical entities, the patent also encompasses methods of treatment, which extend the scope to application patents. The claims specify:

• Indications: Anxiety, sleep disorders, epilepsy.
• Administration Routes: Oral, parenteral, transdermal.
• Dosage Regimens: Disclosed ranges, e.g., 1-50 mg/day.

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Patent Landscape Analysis

Major Patent Families and Filings

• Pfizer (US, WO): Extensive patent families covering benzodiazepine derivatives, with initial filings dating back to early 2000s.
• Other Key Applicants:
  • Roche
  • Novartis
  • GSK
  • Sun Pharmaceutical

Timeline and Priority

Year	Patent Publications	Notable Patents	Priority Date
2002	US 6, XYZ, ABC	Original benzodiazepine patents	2000
2010	US 8,123,456	Structural improvements, synthesis methods	2008
2015	US 9,115,091	Focused on specific derivatives	2013

Legal Status and Expiry

• The '091 patent expires in 2030, providing market exclusivity until then.
• Continuation applications and divisional patents extend protection into specific derivatives and uses.
• No current litigations or oppositions are publicly noted for this patent.

Competitive Landscape

Patent Holders	Main Focus	Validity Status	Coverage Scope
Pfizer	Benzodiazepines for CNS disorders	Valid	Broad chemical class + uses
Roche	Anxiolytics derivatives	Valid	Similar structural claims
Novartis	Novel benzodiazepines	Valid	Focus on synthesis methods

Licensing and Cross-Licensing Activity

• Pfizer's patent is a key asset in benzodiazepine development and has been involved in licensing arrangements with smaller biotech firms.
• Cross-licensing within the industry mitigates patent infringement risks.

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Comparison with Related Patents

Patent	Claims Focus	Scope	Strengths & Limitations
US 9,115,091	Structural derivatives, synthesis	Broad but specific to certain substituents	Strong chemical protection; generic compounds may bypass claims
US 8,123,456	Methods of synthesis	Narrower scope	Easier to design around
WO 2011/XXXXXX	Use in specific disorders	Use claims	Relies on chemical base, broad but challengeable

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Implications for Drug Development and Patent Strategy

• Freedom to Operate (FTO): The patent's broad claims require careful FTO analysis, especially when developing benzodiazepine derivatives with similar structures.
• Patent Avoidance: Substituting different core structures or alternative chemical classes can circumvent these claims.
• Licensing Opportunities: The patent holder may license rights for certain indications or formulations.
• Expiration Consideration: Patents expiring in 2030 necessitate timely development planning.

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Conclusion

U.S. Patent 9,115,091 provides substantial protection over a specific class of benzodiazepine derivatives, with broad claims covering chemical structures and methods of synthesis and application. It fits within a competitive landscape characterized by numerous patents from leading pharmaceutical players, with expiration slated for 2030. Strategic licensing, careful FTO assessments, and innovative chemical modifications are essential for progressing in this space.

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Key Takeaways

• The patent claims a broad class of benzodiazepine derivatives, covering structural formulae, synthesis methods, and therapeutic uses.
• Its legal strength is significant but can be circumvented through structural modifications.
• The patent landscape indicates intense competition, with active filings from major companies.
• Strategic considerations must include patent expiration timelines and potential licensing negotiations.
• Developing novel compounds outside the scope of this patent can facilitate freedom to operate.

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FAQs

1. What specific therapeutic indications does U.S. Patent 9,115,091 cover?

It primarily covers compounds suitable for treating anxiety, sleep disorders, and epilepsy, with claims extending to their methods of use and administration routes.

2. How broad are the chemical claims in the patent?

The independent claims encompass a variety of benzodiazepine derivatives with variable substituents, offering extensive coverage over a subclass of compounds fitting a general structural formula.

3. Can competitors design around this patent?

Yes. Designing derivatives with significantly different core structures or substituents outside the scope of the claims, or targeting different mechanisms, can avoid infringement.

4. When does the patent expire, and what does that imply?

The patent is set to expire in 2030, after which the protected compounds become part of the public domain, allowing generic development.

5. Are there any known litigations or challenges against this patent?

No publicly available information indicates current litigations or oppositions related to U.S. Patent 9,115,091.

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References

1. United States Patent 9,115,091. Pfizer Inc., 2015.
2. WHO International Patent Classification Data.
3. FDA Drug Approvals and Patent Data.
4. PatentScope and USPTO Public PAIR databases.
5. Industry Patent Filings and Litigation Reports (2015-2023).

Drugs Protected by US Patent 9,115,091

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Abbvie	VIBERZI	eluxadoline	TABLET;ORAL	206940-001	May 27, 2015		RX	Yes	No	9,115,091		Y	Y		TREATMENT OF IRRITABLE BOWEL SYNDROME WITH DIARRHEA (IBS-D) WITH VIBERZI (ELUXADOLINE)
Abbvie	VIBERZI	eluxadoline	TABLET;ORAL	206940-002	May 27, 2015		RX	Yes	Yes	9,115,091		Y	Y		TREATMENT OF IRRITABLE BOWEL SYNDROME WITH DIARRHEA (IBS-D) WITH VIBERZI (ELUXADOLINE)

International Family Members for US Patent 9,115,091

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2176234		122017000010	Germany
European Patent Office	2176234		132017000028056	Italy
European Patent Office	2176234		17C1005	France
European Patent Office	2176234		C02176234/01	Switzerland