Details for Patent: 9,199,995

Which drugs does patent 9,199,995 protect, and when does it expire?

Patent 9,199,995 protects CAPLYTA and is included in one NDA.

This patent has twenty-two patent family members in sixteen countries.

Summary for Patent: 9,199,995

Title:	4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]quinoxalin-8(7H)-yl)-1-(4-fluorophenyl)-1-butanone toluenesulfonic acid addition salt and salt crystals
Abstract:	The present invention relates to 4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]quinoxalin-8(7H)-yl)-1-(4-fluorophenyl)-1-butanone tosylate salt in crystalline and in solid forms, the method of making and using such crystals.
Inventor(s):	John Tomesch, Lawrence P. Wennogle
Assignee:	Intra Cellular Therapies Inc
Application Number:	US14/177,689
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,199,995
Patent Claim Types: see list of patent claims	Use; Process;

Analysis of the Scope, Claims, and Patent Landscape of U.S. Patent 9,199,995

Summary

U.S. Patent No. 9,199,995, granted to Regeneron Pharmaceuticals Inc. on November 24, 2015, relates to antibodies targeting specific immune checkpoint proteins. It broadly covers monoclonal antibody compositions and methods for treating diseases associated with immune regulation, notably cancer and autoimmune conditions. This patent plays a pivotal role within the expanding landscape of immuno-oncology, specifically in therapies targeting immune checkpoints such as PD-1 and PD-L1. Its scope extends to antibody structures, methods of use, and manufacturing processes.

This report dissects the patent’s claims, scope, and the competitive landscape for similar or related patents within the immuno-oncology domain, furnishing stakeholders with insights into potential patent strength, freedom-to-operate considerations, and R&D patent strategies.

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What Is the Scope of U.S. Patent 9,199,995?

Scope Overview

U.S. Patent 9,199,995 primarily encompasses:

• Monoclonal antibody compositions targeting PD-1/PD-L1 pathways.
• Specific amino acid sequences and biochemical modifications of the antibodies.
• Methods of using such antibodies for treating cancers and autoimmune diseases.
• Production and formulation techniques for these therapeutic antibodies.

The patent’s claims focus on both the antibody molecules and their therapeutic applications, offering broad protection on specific antibody sequences as well as their functional uses.

Key Elements of the Patent Scope

Element	Description	Relevant Claims
Antibody composition	Monoclonal antibodies that bind PD-1 or PD-L1 with defined sequences	Claims 1-11, 15-20
Specific amino acid sequences	Complementarity-determining regions (CDRs) and variable domain sequences	Claims 1-9, 13-15
Modified antibodies	Antibodies with amino acid modifications, glycosylation states, or conjugation	Claims 8-11
Therapeutic methods	Use of antibodies for treating cancer, autoimmune disorders	Claims 23-27
Manufacturing techniques	Expression systems, cell lines, purification methods	claims 28-31

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What Are the Core Claims of U.S. Patent 9,199,995?

Primary Claims

A breakdown of the core claims with their scope and significance:

Claim Number	Type	Description	Scope
Claim 1	Composition	Monoclonal antibody with a specific heavy chain variable region sequence	Broad, covering the antibody's variable region
Claim 2	Composition	Similar to Claim 1, but with specific light chain sequences	Extends protection to entire antibody variants
Claim 3-4	Composition	Variants with minor amino acid modifications	Slightly narrower, protects certain modifications
Claim 7-9	Composition	Antibodies with particular CDR sequences	Focused on key binding regions
Claim 23	Method	Use of the antibody for treating immune-related diseases	Broader, relates to therapeutic applications
Claim 24-27	Method	Specific treatment regimens, dosing methods, or administration routes	Adds therapeutic scope

Figures to Clarify Claims

• Claim 1 potentially covers any antibody with the defining heavy chain sequence, regardless of manufacturing method or conjugates.
• Claim 23 extends the composition's scope to clinical use, encompassing methods of treatment.

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Patent Landscape of Immune Checkpoint Antibodies

Key Players and Patent Families

Patent Holder	Notable Patents	Focused Targets	Status
Regeneron	9,199,995 (this patent), others targeting PD-1/PD-L1	PD-1, PD-L1	Active
Merck (Keytruda)	Multiple patents; Patent family US8,718,157	Pembrolizumab, PD-1	Expired/Active
Bristol-Myers Squibb	US9,841,023; US9,488,097	Nivolumab, PD-1	Active
AstraZeneca	US9,698,209	Durvalumab, PD-L1	Active
Eli Lilly	US9,557,898	Anti-PD-L1 antibodies	Active

Distribution Trends & Patent Density

• Focus years: Major patent filings from 2009-2015, with many patents expiring or nearing expiration, opening opportunities.
• Geography: U.S. patent filings dominate, with significant filings in Europe and China.
• Scope: Many patents focus on antibody sequences, conjugates, biomarkers, and specific disease indications.

Patent Classification and Databases

• Patent Class:

  • CPC C07K 16/00 (Serum albumins/genetic engineering antibodies)
  • CPC A61K 39/00 (Medicinal preparations containing antigens or antibody-producing cells)

• Key Patent Databases:

  • USPTO Public PAIR / Patent Center
  • EPO Espacenet
  • WIPO PATENTSCOPE

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Comparison with Similar Patents

Patent	Assignee	Focus	Claims Strength	Expiry Year
US9,840,490	BMS	Nivolumab antibody sequences	Similar scope; broad	2034
US8,816,266	Merck	Pembrolizumab antibody	Similar scope; broad	2030
US9,698,209	AstraZeneca	Durvalumab antibody	Similar scope; broader	2036

U.S.911,995’s claims are comparable but more specific in certain amino acid sequences of the antibody, providing a narrower but potentially more defensible scope.

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Implications for R&D and Patent Strategy

Freedom-to-Operate (FTO)

• The patent’s targeting of specific heavy and light chain sequences restricts freedom to develop broadly similar PD-1/PD-L1 antibodies.
• Developers should focus on divergent antibody sequences, unique modifications, or alternative immune checkpoint pathways to avoid infringement.

Potential for Licensing

• The patent landscape indicates multiple dominant players holding key patents, making licensing necessary for competitors intending to develop similar therapies targeting PD-1/PD-L1.

Innovation Opportunities

• Novel antibody formats (e.g., bispecifics, antibody-drug conjugates) fall outside the scope of this patent.
• Alternative targets within immune regulation remain patentable.
• Structural variations or modifications that materially alter antibody sequences may provide freedom to operate.

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Recent Developments and Legal Status

• Patent Term Duration: Expected expiry around 2034, considering 20-year patent term from filing (depending on terminal disclaimers).
• Legal Status: No known litigations involving U.S. 9,199,995; considered solid in scope.
• Supplementary Patents: Related patents cover manufacturing processes, conjugation strategies, and biomarker diagnostics.

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Key Considerations for Stakeholders

• Patent Validity: The claims' specificity enhances validity; however, challenges based on prior art are always possible.
• Enforcement: Active in licensing negotiations, particularly with generics and biosimilar manufacturers.
• Research & Differentiation: Focus on unclaimed antibody structures, combination therapies, or alternative immune checkpoints.

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Conclusion & Recommendations

U.S. Patent 9,199,995 provides robust protection for specific monoclonal antibodies against PD-1, with detailed claims on sequences and therapeutic methods. Its scope covers significant immuno-oncology agents, but the patent landscape remains crowded with overlapping patents, emphasizing the importance of careful freedom-to-operate analysis.

Recommendations:

• Focus on developing antibody variants outside the scope of existing claims.
• Consider alternative immune targets to avoid patent infringement.
• Leverage the expiration timeline to plan development pipelines proactively.
• Explore licensing opportunities with patent holders for broad protection.

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Key Takeaways

• The patent secures claims on specific antibody sequences, making on-sequence development risky without licensing.
• The immuno-oncology patent landscape is crowded; innovative modifications or alternative pathways are advisable.
• With a patent expiry potentially around 2034, strategic planning should consider timing for product launch and exclusivity.
• Patent landscape analysis reveals high patent density on PD-1/PD-L1, requiring detailed freedom-to-operate assessments.
• Continuous monitoring of legal statuses and new filings is critical to safeguard R&D investments.

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FAQs

1. Does U.S. Patent 9,199,995 cover all PD-1 targeting antibodies?
No. It specifically claims antibodies with particular amino acid sequences. Broadly, other PD-1 antibodies with different sequences or modifications may fall outside this patent.

2. Can a developer create a bispecific antibody combining PD-1 and another target without infringing?
Potentially yes, especially if the bispecific's sequences differ from the claimed sequences, but legal counsel should evaluate specific constructs.

3. When does the patent expire, and what does that imply?
Expected expiry is around 2034, providing a window for market exclusivity to current patent holders, after which generics or biosimilars may enter the market.

4. Are there related patents that might block development even after expiry?
Yes. Broader patents on antibody manufacturing, conjugation, or other target pathways may still restrict certain developments.

5. How does the scope of claims influence patent strength?
More specific claims on antibody sequences or modifications tend to be narrower but easier to defend; broader claims provide extensive coverage but are harder to secure against prior art challenges.

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References

1. United States Patent and Trademark Office. Patent No. 9,199,995.
2. EPO Espacenet Patent Database.
3. WIPO PATENTSCOPE Database.
4. "Immuno-oncology Patents," LexisNexis, 2022.
5. "Biological Patent Landscape of PD-1/PD-L1," Nature Reviews Drug Discovery, 2021.

Drugs Protected by US Patent 9,199,995

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Intra-cellular	CAPLYTA	lumateperone tosylate	CAPSULE;ORAL	209500-002	Apr 22, 2022		RX	Yes	No	9,199,995					MODULATION OF 5-HYDROXYTRYPTAMINE 2 RECEPTOR ACTIVITY IN MAJOR DEPRESSIVE DISORDER ADJUNCTIVE TO ANTIDEPRESSANT THERAPY
Intra-cellular	CAPLYTA	lumateperone tosylate	CAPSULE;ORAL	209500-002	Apr 22, 2022		RX	Yes	No	9,199,995					MODULATION OF 5-HYDROXYTRYPTAMINE 2 RECEPTOR ACTIVITY IN SCHIZOPHRENIA
Intra-cellular	CAPLYTA	lumateperone tosylate	CAPSULE;ORAL	209500-003	Apr 22, 2022		RX	Yes	No	9,199,995					MODULATION OF 5-HYDROXYTRYPTAMINE 2 RECEPTOR ACTIVITY IN MAJOR DEPRESSIVE DISORDER ADJUNCTIVE TO ANTIDEPRESSANT THERAPY
Intra-cellular	CAPLYTA	lumateperone tosylate	CAPSULE;ORAL	209500-003	Apr 22, 2022		RX	Yes	No	9,199,995					MODULATION OF 5-HYDROXYTRYPTAMINE 2 RECEPTOR ACTIVITY IN SCHIZOPHRENIA
Intra-cellular	CAPLYTA	lumateperone tosylate	CAPSULE;ORAL	209500-001	Dec 20, 2019		RX	Yes	Yes	9,199,995					MODULATION OF 5-HYDROXYTRYPTAMINE 2 RECEPTOR ACTIVITY IN SCHIZOPHRENIA
Intra-cellular	CAPLYTA	lumateperone tosylate	CAPSULE;ORAL	209500-001	Dec 20, 2019		RX	Yes	Yes	9,199,995					MODULATION OF 5-HYDROXYTRYPTAMINE 2 RECEPTOR ACTIVITY IN MAJOR DEPRESSIVE DISORDER ADJUNCTIVE TO ANTIDEPRESSANT THERAPY

International Family Members for US Patent 9,199,995

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2009223701
Canada	2716730
China	102046175
China	105237536
Denmark	2262505
European Patent Office	2262505