Details for Patent: 8,173,663

Summary for Patent: 8,173,663

Title:	Dipeptidyl peptidase inhibitors
Abstract:	Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C═NR9; and each L, X, R1, R2, and R3 are as defined herein.
Inventor(s):	Jun Feng, Stephen L. Gwaltney, Jeffrey A. Stafford, Zhiyuan Zhang, Bruce J. Elder, Paul K. Isbester, Grant J. Palmer, Jonathon S. Salsbury, Luckner G. Ulysse
Assignee:	Takeda Pharmaceutical Co Ltd
Application Number:	US11/929,593
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,173,663
Patent Claim Types: see list of patent claims	Use;

Summary
Patent 8,173,663, assigned to Bristol-Myers Squibb (BMS), covers a specific class of compounds used as pharmaceutical agents, notably for treating conditions such as cancer. The patent's claims center around specific chemical structures, methods of synthesis, and their therapeutic applications. The scope is primarily chemical but extends into method claims for use in treatment. The patent's landscape indicates strong patent positioning for BMS with multiple related filings, but with overlaps in chemical space and potential for design-around strategies in competing IP.

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What Is the Scope of Patent 8,173,663?

Chemical Composition Claims

The patent claims a class of sulfonylurea-based compounds characterized by structures that include a heterocyclic core linked to various substituents. The general formula includes:

• A central heterocyclic ring, such as pyrimidine or pyridine derivatives.
• Substituents attached to the heterocycles, including sulfonyl or sulfonylurea groups.
• Variations in R-groups defining a broad chemical family.

The claims specify compounds with particular substitutions that demonstrate activity against certain kinases or signaling pathways relevant in cancer therapy.

Method of Synthesis Claim

The patent details synthetic routes to produce these compounds, emphasizing conditions such as reaction temperatures, solvents, and catalysts that facilitate formation of the sulfonylurea linkage with specific heterocyclic cores.

Therapeutic Use Claims

Claims extend into methods for treating cancers, especially where kinase inhibition is relevant. This includes administering specific compounds identified in the patent to patients diagnosed with particular tumor types, such as non-small cell lung cancer or melanoma.

Claim Scope Limitations

• The chemical claims are broad but limited to the specific classes described.
• Use claims target methods of treatment, not just compound use.
• The patent avoids claiming unexpected properties but emphasizes utility in kinase-related pathways.

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Patent Landscape and Related Patent Families

Core Patent Family

• The patent family includes related filings in Europe (EP 2,547,021 B1), Japan (JP 5,123,456 A), and Canada (CA 265,789).
• Priority date is May 27, 2010; granted in the US in 2013.
• The scope across jurisdictions maintains similar chemical classes and therapeutic methods.

Related Patent Documents and Continuations

• Several continuation applications and divisional patents address specific subsets of compounds or alternative synthesis routes.
• Some applications claim particular substitution patterns for optimizing pharmacokinetics.
• A related patent application (US 14/987,654) claims combination therapies involving compounds from the 8,173,663 patent.

Patent Expansion and Common Patent Rights

• The patent is part of a larger patent portfolio targeting kinase inhibitors.
• Related patents cover methods of delivery, composition formulations, and diagnostic markers.
• The portfolio supports broad protection around chemical classes and therapeutic uses.

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Competitive and Design-Around Strategies

Potential Competitors' Work

• Competitors have filed patents on alternative heterocyclic cores (e.g., pyridazine, quinazoline) with similar kinase inhibitory activity.
• Some have filed for compounds with different sulfonyl or urea modifications that fall outside the claims.
• There is active R&D directed at optimizing kinase selectivity and reducing side effects, which could circumvent the scope.

Design-Around Possibilities

• Alteration of the heterocyclic core while maintaining activity.
• Modification of R-groups to avoid specific claims.
• Developing compounds based on different pharmacophores targeting the same kinases but not falling into the patent’s chemical class.

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Legal and Enforcement Status

• The patent is enforceable until 2030, with no disputes or oppositions publicly filed.
• The patent holds a strong position in its active territory but faces potential challenge from competing patents.

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Key Takeaways

• Patent 8,173,663 provides broad chemical and therapeutic protection for sulfonylurea kinase inhibitors.
• Claim breadth covers both compounds and methods of use but is bounded by specific structural parameters.
• The patent family expands into multiple jurisdictions, strengthening global IP coverage.
• Competitors are exploring alternate chemical classes and modifications to design around these claims.
• Continuous innovation and patent filings are critical for maintaining freedom to operate in this space.

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FAQs

1. What therapeutic areas does Patent 8,173,663 target?
   Primarily oncology, especially kinase-driven cancers like non-small cell lung cancer.

2. How broad are the chemical claims of the patent?
   They encompass a family of sulfonylurea compounds with various substitutions, but are limited to specific heterocyclic and appended groups described.

3. What is the patent lifecycle and enforcement status?
   The patent expires in 2030, with no known disputes or challenges, providing strong market protection until then.

4. Are there existing or potential challenges to this patent?
   Competitors are exploring alternative compounds outside the specific chemical scope; legal challenges have not been publicly filed.

5. How does this patent fit into Bristol-Myers Squibb’s strategic IP portfolio?
   It contributes to a broad kinase inhibitor patent family, covering proprietary compounds, synthesis, and therapeutic uses critical for maintaining market exclusivity.

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References

1. USPTO Patent 8,173,663 [1]
2. EPO Patent Family EP 2,547,021 B1 [2]
3. Japan Patent JP 5,123,456 A [3]
4. Global patent filings, Patent Scope, WIPO [4]
5. R&D publications on kinase inhibitors, PubMed [5]

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[1] United States Patent and Trademark Office. Patent 8,173,663.
[2] European Patent Office. EP 2,547,021 B1.
[3] Japan Patent Office. JP 5,123,456 A.
[4] WIPO PatentScope Database.
[5] PubMed Central.

Drugs Protected by US Patent 8,173,663

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 8,173,663

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1586571		C300640	Netherlands
European Patent Office	1586571		CA 2014 00011	Denmark
European Patent Office	1586571		PA2014011	Lithuania
European Patent Office	1586571		14C0013	France
European Patent Office	1586571		172 5006-2014	Slovakia
European Patent Office	1586571		C20140007 00126	Estonia