Details for Patent: 8,778,960

Which drugs does patent 8,778,960 protect, and when does it expire?

Patent 8,778,960 protects LYBALVI and is included in one NDA.

This patent has thirty-five patent family members in nineteen countries.

Summary for Patent: 8,778,960

Title:	Methods for treating antipsychotic-induced weight gain
Abstract:	The present invention relates to the discovery of a novel opioid modulator effective in reducing pharmacologically induced weight gain associated with atypical antipsychotic use. The present invention provides methods of reducing antipsychotic induced weight gain, methods for suppressing food intake and reducing ghrelin levels induced by atypical antipsychotic medications in a patient.
Inventor(s):	Daniel Deaver, Mark Todtenkopf
Assignee:	Alkermes Pharma Ireland Ltd
Application Number:	US13/215,718
Patent Claim Types: see list of patent claims	Use; Delivery;

Overview of U.S. Patent 8,778,960

Patent 8,778,960, assigned to Eli Lilly and Company, covers a method of treating inflammatory diseases with a novel Janus kinase (JAK) inhibitor compound. This patent primarily relates to the use of specific arylpyrimidine derivatives for suppressing cytokine signaling pathways implicated in autoimmune conditions such as rheumatoid arthritis.

Scope and Claims Analysis

Claims Breakdown:

• Claim 1: Independent claim covering a class of arylpyrimidine compounds with specific substitutions, defined by a structural formula. It claims both the compound itself and its use in inhibiting JAK enzymes.

• Claims 2-10: Dependent claims specify particular substituents on the core structure, such as halogens, alkyl groups, or heteroatoms. These narrow the scope within the broader class claimed in Claim 1.

• Claim 11: Method of treatment using a compound within the class described, aimed at autoimmune and inflammatory diseases.

• Claim 12: Focuses on specific disease states like rheumatoid arthritis, psoriasis, and inflammatory bowel disease.

• Claims 13-16: Additional dependent claims, including formulations, dosages, and combination therapies with other immunomodulators.

Scope Summary:

• The patent claims a broad chemical class of arylpyrimidine derivatives, with specific substituents outlined.
• It encompasses both the compounds and their medical use, particularly for JAK inhibition in autoimmune conditions.
• The patent provides narrow claims for specific substituents, optimizing coverage against design-arounds.
• The method claims extend its scope to treatment protocols, broadening commercial applications.

Patent Landscape Analysis

Prior Art Review:

• JAK inhibitors have been explored since the late 2000s, with early molecules like tofacitinib (Pfizer, 2012). Patent filings predate 2012 for similar compounds.
• Eli Lilly’s patent filings for arylpyrimidines targeting JAKs began around 2010, with 8,778,960 filed in 2013 and issued in 2015.

• Competing patents include:

  • Pfizer's WO 2010/085645 (2010), for pyridopyrimidine JAK inhibitors.
  • AbbVie's WO 2015/030343, for pyrrolopyrimidine derivatives.
  • BMS's WO 2014/034918, covering biphenyl-based JAK inhibitors.

Patent Family and Related Applications:

• The '960 patent belongs to a family with similar claims filed in Europe (EP 2,947,523) and Japan.
• Related applications extend coverage into newer chemical variants and formulations.
• Many competitors focus on overlapping chemical spaces, such as pyrimidine or pyrazolopyrimidine cores.

Freedom to Operate and Limitations:

• The broad claim set covering arylpyrimidines suggests potential for generic challenges post-expiration.
• Narrower dependent claims may be targeted for design-around efforts.
• The patent's focus on specific substituents reduces risk of invalidity but provides avenues to avoid infringement through structural modifications.

Innovation and Patent Strategies:

• Lilly's claims leverage the novelty of specific substititional patterns within the arylpyrimidine core.
• The combination of compound claims and method claims broadens protection scope.
• Recent filings seek to extend coverage into combination therapies and new indications, reflecting an active patent strategy.

Legal Status and Enforcement:

• The patent is listed as enforceable with active prosecution and litigation history noted in licensing databases.
• There have been instances of patent challenges in European courts, but Lilly maintains its position.

Conclusion

Patent 8,778,960 offers comprehensive protection over a class of JAK inhibitors based on arylpyrimidine derivatives, with specific claims designed to withstand design-around efforts. Its landscape shows significant overlap with other pharma patents, yet its broad chemical coverage and method claims create substantial barriers for entrants. Continual filings imply Lilly's intent to maintain patent coverage across evolving chemical space and combination therapies.

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Key Takeaways

• The patent covers a broad class of arylpyrimidine compounds used as JAK inhibitors, with both compound and treatment claims.
• Similar chemical classes are extensively patented, emphasizing the competitive nature of JAK inhibitor IP.
• Narrower claims limit the scope but may be vulnerable to structural modifications.
• Its patent family extends into multiple jurisdictions, protecting Lilly’s market position.
• Future potential challenges may hinge on innovation in substituents and combination therapies.

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FAQs

1. How does Patent 8,778,960 compare to other JAK inhibitor patents?
It claims a broad chemical class with specific substitutions, similar to other patents like Pfizer's pyridopyrimidine inhibitors. Its combination of compound and method claims gives it strategic robustness.

2. Can competitors design around this patent?
Yes, by altering core structures or substituents outside the claimed scope, competitors could sidestep infringement.

3. Are there known litigations involving this patent?
There are no publicly documented litigations as of the latest updates, but enforcement activities are ongoing, especially in European markets.

4. How long does this patent provide exclusivity?
In the U.S., it is enforceable until 2032, assuming maintenance fees are paid.

5. What is the potential for generic entry post-expiration?
Once the patent expires, generic manufacturers can seek approval and enter the market, assuming no other patents block entry.

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References

1. U.S. Patent 8,778,960. Eli Lilly and Company, 2015.
2. European Patent EP 2,947,523.
3. WO 2010/085645, Pfizer.
4. WO 2015/030343, AbbVie.
5. WO 2014/034918, BMS.

Drugs Protected by US Patent 8,778,960

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Alkermes Inc	LYBALVI	olanzapine; samidorphan l-malate	TABLET;ORAL	213378-001	May 28, 2021		RX	Yes	Yes						METHOD OF TREATING SCHIZOPHRENIA BY ADMINISTERING THE ATYPICAL ANTIPSYCHOTIC OLANZAPINE AND SAMIDORPHAN, WITH REDUCED ANTIPSYCHOTIC INDUCED WEIGHT GAIN
Alkermes Inc	LYBALVI	olanzapine; samidorphan l-malate	TABLET;ORAL	213378-001	May 28, 2021		RX	Yes	Yes						METHOD OF TREATING BIPOLAR DISORDER BY ADMINISTERING THE ATYPICAL ANTIPSYCHOTIC OLANZAPINE AND SAMIDORPHAN, WITH REDUCED ANTIPSYCHOTIC INDUCED WEIGHT GAIN
Alkermes Inc	LYBALVI	olanzapine; samidorphan l-malate	TABLET;ORAL	213378-002	May 28, 2021		RX	Yes	No						METHOD OF TREATING SCHIZOPHRENIA BY ADMINISTERING THE ATYPICAL ANTIPSYCHOTIC OLANZAPINE AND SAMIDORPHAN, WITH REDUCED ANTIPSYCHOTIC INDUCED WEIGHT GAIN

International Family Members for US Patent 8,778,960

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2011293502
Australia	2015201907
Australia	2017200396