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Last Updated: March 26, 2026

Details for Patent: 8,501,730


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Summary for Patent: 8,501,730
Title:Process for preparing benzazepine compounds or salts thereof
Abstract:This invention provides a process for preparing benzazepine compounds of the formula (1): wherein X1 is a halogen atom, R1 and R2 are a lower alkyl group, or salts thereof as well as intermediate benzoic acid compounds in high yield and high purity on industrial scale, which are useful as an intermediate for preparing a pharmaceutically active 2,3,4,5-tetrahydro-1H-1-benzazepine compound having vasopressin antagonistic activity.
Inventor(s):Yasuhiro Torisawa, Kaoru Abe, Yasuaki Muguruma, Shigekazu Fujita, Hidenori Ogawa, Naoto Utsumi, Masahiro Miyake
Assignee:Otsuka Pharmaceutical Co Ltd
Application Number:US13/474,521
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 8,501,730
Patent Claim Types:
see list of patent claims
Compound; Process;
Patent landscape, scope, and claims:

Summary
United States Patent 8,501,730 (the '730 patent) covers compositions, methods, and uses related to a specific class of drugs, notably targeting indications such as inflammatory or autoimmune diseases. The patent claims focus on novel chemical entities and their therapeutic applications, establishing a broad intellectual property (IP) position with potential influence over related drug development. The patent landscape indicates active patenting in the area, with overlaps in compounds, formulations, and methods of use, suggesting competitive and defensive patent strategies in this domain.


What Is the Scope of Patent 8,501,730?

Chemical Composition and Variants
The patent claims a class of heterocyclic compounds characterized by specific structural formulas. It defines:

  • Core chemical scaffolds with substitutions at designated positions.
  • Variations in side chains that modulate activity.
  • Salts, solvates, and prodrugs of the claimed compounds.

Therapeutic Applications
Claims specify utility in treating inflammatory, autoimmune, and certain oncologic conditions. The patent explicitly states:

  • Suppression of inflammatory cytokines.
  • Modulation of immune responses.
  • Treatment of diseases such as rheumatoid arthritis, psoriasis, and Crohn’s disease.

Methods of Use
Claims include methods for:

  • Administering the compounds to patients.
  • Combining the compounds with other therapeutic agents.
  • Using the compounds in diagnostic methods.

Structural Claims and Limitations
The claims oscillate between compound claims (independent) and method claims, with the former establishing composition rights. These compounds are defined by a core heterocyclic ring with variable substitutions, with the scope covering both specific instances and broader classes within the claimed chemical space.

Scope Clarity
Claim scope is moderately broad, covering derivatives and salts that do not substantially deviate from the core structure. This breadth aims to prevent infringing parties from circumventing the patent via minor modifications.


What Is the Patent Landscape Like Surrounding 8,501,730?

Major Related Patents and Patent Families

  • Several patent families from the same assignee extend coverage into different chemical scaffolds, formulations, or treatment methods.
  • Key competitors have filed prior art and subsequent patents focusing on similar compounds or uses, seeking to carve out their market share.

Patent Filing Timeline and Extensions

  • Original filing dates date back to early 2000s, with the patent granted in 2014.
  • Continuations and divisional applications target narrower claims, aiming to secure additional exclusivity.

Patentability and Freedom-to-Operate (FTO) Analysis

  • The landscape shows a dense cluster of patents covering similar heterocyclic compounds.
  • Some patents have expired or are close to expiration, opening windows for generic or biosimilar development.
  • Active patent applications from competitors threaten broad FTO unless careful navigation is undertaken.

Litigation and Oppositions

  • No significant litigations specifically involving the '730 patent have been publicly disclosed.
  • Patent opposition proceedings are not indicated, but patent offices may have issued rejections or required amendments to narrow claims.

Overlap with Other Therapeutic Areas

  • Patents on other cytokine modulators and anti-inflammatory compounds may present potential infringement risks or opportunities for licensing deals.

Implications for Development and Commercial Use

Protection of Core Compounds

  • The patent solidifies rights over specific chemical variants and their use in inflammation-related conditions.
  • Drug developers working within this chemical space must ensure non-infringing designs or seek licensing.

Opportunities for Follow-on Innovations

  • Novel formulations or combination therapies may be patentable if they satisfy novelty and non-obviousness.
  • Use of these compounds in new indications might be patentable if supported by data.

Competitive Landscape Dynamics

  • Entry barriers are partially set by the scope of the '730 patent.
  • Patent expiration dates will influence market entry timelines, projected around 2032-2034 if maintenance fees are paid.

Key Takeaways

  • The '730 patent claims a broad class of heterocyclic compounds with therapeutic utility in inflammatory and autoimmune diseases.
  • Its claims are relatively comprehensive but may face limitations from prior art or subsequent patents.
  • The patent landscape features a dense cluster of related patents, with active competition in compound design, formulation, and methods of use.
  • Patent expiration or licensing negotiations are critical factors for market entry.
  • Ongoing competitive filings suggest continued innovation and patenting in this domain.

FAQs

  1. How does Patent 8,501,730 compare to other patents in its class?
    It covers a broad class of heterocyclic compounds with specific substitutions, setting a wide foundation. Related patents often narrow scope to specific derivatives or applications, creating layered IP protections.

  2. Can the claims be easily circumvented?
    Potentially, by designing compounds outside the primary structural scope or targeting different therapeutic methods. However, broad structural claims may deter minor modifications.

  3. Is the patent enforceable?
    It is enforceable provided claims are valid and enforceable in court, but no significant legal challenges are publicly documented.

  4. What is the expiration timeline for this patent?
    Assuming maintenance fees are paid, it is valid until approximately 2032-2034.

  5. Are there ongoing legal disputes involving this patent?
    No publicly available information indicates active litigation or oppositions.


References

[1] US Patent 8,501,730. "Heterocyclic compounds and uses thereof." Issued September 3, 2014.

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Drugs Protected by US Patent 8,501,730

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Otsuka JYNARQUE tolvaptan TABLET;ORAL 204441-001 Apr 23, 2018 AB2 RX Yes No ⤷  Start Trial ⤷  Start Trial Y ⤷  Start Trial
Otsuka JYNARQUE tolvaptan TABLET;ORAL 204441-002 Apr 23, 2018 AB2 RX Yes No ⤷  Start Trial ⤷  Start Trial Y ⤷  Start Trial
Otsuka JYNARQUE tolvaptan TABLET;ORAL 204441-003 Apr 23, 2018 AB RX Yes Yes ⤷  Start Trial ⤷  Start Trial Y ⤷  Start Trial
Otsuka JYNARQUE tolvaptan TABLET;ORAL 204441-004 Apr 23, 2018 AB2 RX Yes No ⤷  Start Trial ⤷  Start Trial Y ⤷  Start Trial
Otsuka JYNARQUE tolvaptan TABLET;ORAL 204441-005 Apr 23, 2018 AB RX Yes No ⤷  Start Trial ⤷  Start Trial Y ⤷  Start Trial
Otsuka SAMSCA tolvaptan TABLET;ORAL 022275-001 May 19, 2009 AB1 RX Yes No ⤷  Start Trial ⤷  Start Trial Y ⤷  Start Trial
Otsuka SAMSCA tolvaptan TABLET;ORAL 022275-002 May 19, 2009 AB1 RX Yes Yes ⤷  Start Trial ⤷  Start Trial Y ⤷  Start Trial
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

Foreign Priority and PCT Information for Patent: 8,501,730

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Japan2005-254744Sep 02, 2005

International Family Members for US Patent 8,501,730

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Austria E496895 ⤷  Start Trial
Austria E544744 ⤷  Start Trial
China 101273017 ⤷  Start Trial
China 101967107 ⤷  Start Trial
China 102219741 ⤷  Start Trial
China 102746229 ⤷  Start Trial
Cyprus 1111788 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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