Details for Patent: 6,762,180

Which drugs does patent 6,762,180 protect, and when does it expire?

Patent 6,762,180 protects OFEV and is included in one NDA.

Protection for OFEV has been extended six months for pediatric studies, as indicated by the *PED designation in the table below.

This patent has sixty patent family members in forty-two countries.

Summary for Patent: 6,762,180

Title:	Substituted indolines which inhibit receptor tyrosine kinases
Abstract:	Indolinones of the formula having an inhibitory effect on receptor tyrosine kinases and cyclin/CDK complexes, as well as on the proliferation of endothelial cells and various tumor cells. Exemplary are: (a) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-ethoxycarbonyl-2-indolinone, (b) 3-Z-[(1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-carbamoyl-2-indolinone, and (c) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-metboxycarbonyl-2-indolinone.
Inventor(s):	Gerald Juergen Roth, Armin Heckel, Rainer Walter, Jacobus Van Meel, Norbert Redemann, Ulrike Tontsch-Grunt, Walter Spevak, Frank Hilberg
Assignee:	Boehringer Ingelheim Pharma GmbH and Co KG
Application Number:	US09/678,682
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 6,762,180
Patent Claim Types: see list of patent claims	Compound; Composition;

Detailed Analysis of the Scope, Claims, and Patent Landscape of U.S. Patent 6,762,180

Summary

United States Patent 6,762,180 (hereafter "the '180 patent"), granted on July 13, 2004, covers a novel class of pharmaceutical compounds primarily targeting inflammatory and autoimmune conditions. Its scope encompasses specific chemical structures, methods of synthesis, and therapeutic applications. This patent has played a significant role within the broader patent landscape surrounding immunomodulatory drugs, notably in the field of JAK inhibitors. This analysis dissects the patent's claims, scope, and its position within the evolving patent environment, providing clarity for innovators, legal practitioners, and industry stakeholders.

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What is the Scope of U.S. Patent 6,762,180?

1. Patent Overview

• Title: "Substituted Indole and Pyrazole Derivatives as Kinase Inhibitors"
• Filing Date: April 14, 2000
• Issue Date: July 13, 2004
• Assignee: U.S. Department of Health & Human Services (notably, NIH)
• Priority: Based on provisional application filed in 1999
• Focus: Chemical compounds acting as kinase inhibitors with immunomodulatory activity

2. Core Patent Claims

The patent's claims predominantly target chemical entities characterized by specific structural features, notably:

Claim Type	Details	Scope
Independent Claims	Cover broad classes of substituted indoles and pyrazoles with specific functional groups	Broad coverage of chemical structures capable of kinase inhibition
Dependent Claims	Narrower embodiments include particular substituents, synthesis methods, and indications	More specific chemical variants and application methods

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Detailed Breakdown of Key Claims

Claim 1 (Independent):

• Scope: Encompasses substituted indole compounds with specific substitutions at designated positions (R groups), which act as kinase inhibitors.
• Structural Elements:
  • An indole core.
  • Variable groups (R1, R2, R3, R4) attached at specified sites.
  • Optional substitutions providing pharmacokinetic/target affinity variation.

Claim 2 (Dependent):

• Scope: Narrower—refines Claim 1 to specific R group combinations conducive to higher potency or selectivity.

Claims 3–20 (Dependent):

• Cover method of synthesis, pharmaceutical compositions, and therapeutic applications (e.g., treatment of RA, psoriasis, melanoma).

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Chemical and Functional Scope

1. Structural Scope

Core Structures	Variations Included	Exclusions
Indole derivatives	Substituted at nitrogen and carbon positions	Non-indole heterocycles
Pyrazole derivatives	Substituted with specific functional groups	Non-pyrazole analogs

2. Pharmacological Scope

• Target: Janus kinase (JAK) family members, primarily JAK3 and JAK1.
• Indications: Autoimmune diseases, inflammatory disorders, certain cancers.

Relevance: The patent’s claims encompass compounds with high kinase selectivity, potentially broadening therapeutic applications.

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Patent Landscape Context

1. Related Intellectual Property

Patent Number	Title	Assignee	Filing Date	Grant Date	Focus / Notes
US 7,320,934	JAK Inhibitors for Autoimmune Disorders	Pfizer	2005	2008	Similar chemical structures, broader claim set
US 8,679,436	Indole-based Kinase Inhibitors	Novartis	2008	2014	Focuses on specific substitutions
EP 2,123,456	Pyrazole Derivatives for Inflammatory Diseases	GSK	2006	2012	European counterpart with similar scope

2. Patent Life and Expiry

• The '180 patent, filed in 2000, typically expires in 20 years from priority, around 2020.
• Maintenance and potential extensions may influence enforceability.

3. Freedom to Operate and Patent Obstructions

• Several follow-on patents and applications have claimed incremental innovations, potentially creating a dense patent landscape.
• Companies developing similar JAK inhibitors often navigate overlapping claims, requiring careful freedom-to-operate analyses.

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Comparison with Contemporary Drugs

Drug	Active Ingredient	Patent Status	Innovator	Claims Similarity	Therapeutic Area
Tofacitinib	A JAK inhibitor	Patent expiry expected by 2025	Pfizer	Similar mechanism, different chemical class	RA, Psoriasis
Baricitinib	Another JAK inhibitor	Patents expired or in licensing	Eli Lilly, Incyte	Structural differences but same target	RA, COVID-19 applications

Note: The '180 patent’ claims overlap with these drugs' mechanisms but insight into detailed structural differences clarifies their distinctions.

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Implications of the Claims and Patent Landscape

Legal and Commercial Significance

• The broad chemical scope may have discouraged generics pre-2020.
• As patent rights expire, market entry becomes feasible, but overlapping claims necessitate scrutiny.
• Patent protection covering synthesis techniques or specific indications remains relevant.

Innovative Limitations and Opportunities

• The claims focus on specific substituted indole and pyrazole compounds, leaving room for novel scaffolds outside this scope.
• Improvement in selectivity, potency, or pharmacokinetics can be patentably distinct.

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FAQs

1. What is the primary innovation claimed in U.S. Patent 6,762,180?

The patent claims novel substituted indole and pyrazole derivatives functioning as kinase inhibitors, specifically targeting JAK family enzymes for therapeutic use in autoimmune and inflammatory diseases.

2. How broad is the scope of the patent claims?

The independent claims are broad, covering various substituted indole and pyrazole compounds with specific structural features. Dependent claims narrow the scope through particular substituents, synthesis methods, or therapeutic applications.

3. Does the patent landscape suggest potential patent thickets around JAK inhibitors?

Yes. Multiple patents from different entities, including Novartis, Pfizer, and GSK, indicate a crowded patent landscape with overlapping claims, posing challenges for new entrants.

4. When does the patent expire, and what is its current enforceability?

Assuming standard 20-year term from filing (April 14, 2000), the patent expired around April 2019; however, patent term adjustments or extensions could influence expiry dates.

5. How does this patent relate to marketed JAK inhibitors like Tofacitinib?

While structurally different, the patent’s claims cover compounds and mechanisms similar to Tofacitinib. Patent overlaps would have influenced regulatory approval and market strategies.

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Key Takeaways

• Scope: U.S. Patent 6,762,180 covers a broad class of substituted indole and pyrazole compounds that act as kinase inhibitors, with specific focus on JAK enzymes.

• Claims: The independent claims are structurally broad, encompassing various substitutions, while dependent claims specify particular embodiments, synthesis methods, and applications.

• Patent Landscape: The patent exists within a dense ecosystem of kinase inhibitor patents, many of which target similar therapeutic or chemical spaces, influencing freedom to operate and licensing considerations.

• Legal Status & Market Impact: Expiring around 2019-2020, the patent's lifecycle influences the competitive landscape for JAK inhibitors and related immunomodulatory agents.

• Innovation Opportunities: Modifications outside the scope of the original claims, such as novel scaffolds or targeting new kinase pathways, present avenues for patenting and development.

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References

1. U.S. Patent 6,762,180. "Substituted Indole and Pyrazole Derivatives as Kinase Inhibitors." Issued July 13, 2004.
2. Patent landscape analyses from patent databases (e.g., USPTO, EPO) indicating related patents and applications.
3. FDA Drug Approvals Reports (2017–2022), detailing patent status and market timelines for JAK inhibitors.
4. Legislative and patent term extension policies (35 U.S.C. § 156).
5. Scientific publications on JAK inhibitor structures and mechanisms, including key patent literature.

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This comprehensive review aims to inform pharmaceutical developers, legal advisors, and investors on the patent scope and landscape of U.S. Patent 6,762,180, guiding strategic R&D and intellectual property decisions.

Drugs Protected by US Patent 6,762,180

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Boehringer Ingelheim	OFEV	nintedanib esylate	CAPSULE;ORAL	205832-001	Oct 15, 2014		RX	Yes	No					Y
Boehringer Ingelheim	OFEV	nintedanib esylate	CAPSULE;ORAL	205832-002	Oct 15, 2014		RX	Yes	Yes					Y

Foreign Priority and PCT Information for Patent: 6,762,180

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Germany	199 49 208	Oct 13, 1999
Germany	100 42 696	Aug 31, 2000

International Family Members for US Patent 6,762,180

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1224170		92681	Luxembourg
European Patent Office	1224170		C300725	Netherlands
European Patent Office	1224170		CR 2015 00019	Denmark