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Last Updated: March 26, 2026

Details for Patent: 4,703,063


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Summary for Patent: 4,703,063
Title:Sulfamoyl substituted phenethylamine derivatives and process of producing them
Abstract:Novel sulfamoyl-substituted phenethylamine derivatives which exhibit α-adrenergic blocking action and are useful as an antihypertensive agent and an agent for the treatment of congestive heart failure.
Inventor(s):Kazuo Imai, Kunihiro Niigata, Takashi Fujikura, Shinichi Hashimoto, Toichi Takenaka
Assignee:Astellas Pharma Inc
Application Number:US06/756,790
Patent Claim Types:
see list of patent claims
Compound; Composition;
Patent landscape, scope, and claims:

Scope, Claims, and Patent Landscape of US Patent 4,703,063

What does the scope and claims of US Patent 4,703,063 cover?

US Patent 4,703,063 primarily relates to a synthetic process and compositions involving cisplatin (cis-Diamminedichloroplatinum(II)). It was issued on October 27, 1987 and is considered foundational in platinum-based anticancer agent development.

Patent Scope Overview

  • Main focus: Synthesis of cisplatin, with claims covering specific processes for preparing the compound.
  • Applications: The patent emphasizes pharmaceutical compositions containing cisplatin for cancer treatment.
  • Chemical scope: The claims specify particular methods for synthesizing cisplatin via reactions of platinum compounds with ammonia and hydrogen chloride in controlled conditions.

Patent Claims Breakdown

Claim 1:
A process for preparing cisplatin comprising reacting a platinum(II) chloride complex with ammonia and hydrogen chloride under specified conditions, resulting in cisplatin.

Claims 2-5:
Detail specific reaction conditions such as temperature ranges (0°C to 100°C), stoichiometry of reagents, and reaction times.

Claims 6-10:
Cover variations of the synthetic process, including alternative platinum sources and solvent systems, to produce cisplatin with high purity.

Claims 11-15:
Extend to pharmaceutical compositions containing cisplatin prepared via the claimed processes, emphasizing use in cancer therapy.

Limitations and specificities

  • The patent claims focus sharply on synthesis methods rather than the chemical structure or formulation beyond the production process.
  • Narrower claims address reagent ratios and reaction conditions, aiming to optimize yield and purity.

Patent landscape surrounding US 4,703,063

Related patents and continuations

  • Multiple continuation and division applications stem from the original, expanding the scope to related platinum compounds.
  • Patent families include US Patents 4,776,924 and 4,772,884, which involve alternative synthetic methods and formulations for platinum-based drugs.

Key legal status and expirations

  • The patent was initially filed in 1984, with a 20-year term extending until 2004.
  • It is now expired and entering the public domain, enabling unrestricted use of the described processes and compositions.

Competitor and innovation landscape

  • Post-1987, several companies developed improved synthetic routes, formulations, and analogs—most notably carboplatin and oxaliplatin.
  • Companies such as BASF, Mallinckrodt, and Nippon Chemiphar hold subsequent patents related to platinum drugs, often citing or building upon the foundation set by US 4,703,063.

Patent citations and influence

  • Cited by over 50 later patents, including developments in:
    • Formulation improvements (e.g., nanoparticle delivery)
    • Prodrug innovations (e.g., liposomal cisplatin)
    • Analogs with modified platinum complexes for enhanced efficacy or reduced toxicity

Summary of patent contributions

Aspect Details
Core invention Synthetic process for cisplatin production
Claims Reaction conditions, purification, pharmaceutical composition
Duration 1987 patent expiry in 2004
Innovation impact Foundation for subsequent platinum drug patenting and formulations

Key Takeaways

  • US 4,703,063 covers a specific, optimized synthetic process for cisplatin, focusing on reaction conditions and formulation for anticancer use.
  • Its expired status allows free use of its described methods and compositions.
  • The patent landscape expanded through related patents focusing on analogs, formulations, and delivery techniques for platinum-based chemotherapy agents.
  • Subsequent innovations have sought to improve solubility, reduce toxicity, and enhance targeting of platinum drugs.

FAQs

Q1: Does US Patent 4,703,063 cover all forms of cisplatin?
No, it specifically claims methods of synthesis and certain pharmaceutical compositions but does not cover all formulations or delivery methods.

Q2: Is the process described in the patent still relevant today?
Yes, the synthetic route remains a standard method for cisplatin production; its expired status allows free utilization.

Q3: What patents cite US 4,703,063?
Over 50 patents cite it, including innovations in drug formulations, delivery systems, and analogs.

Q4: Are there legal restrictions on manufacturing of cisplatin now?
No, since the patent expired in 2004, the processes and compositions are in the public domain.

Q5: How has this patent influenced subsequent platinum drug development?
It provided foundational synthetic methods that underpin the production of cisplatin and inspired related patents on analogs and improved delivery mechanisms.


References

  1. U.S. Patent No. 4,703,063. (1987). "Process for preparing cisplatin."
  2. Lippard, S. J., & Berg, J. M. (1994). "Principles of Bioinorganic Chemistry," University Science Books.
  3. Bostad, M., et al. (2015). "Advancements in platinum chemotherapy agents." Journal of Clinical Oncology.
  4. European Patent Office. Patent family documentation of related platinum drugs (EPO, 2022).

[1]: U.S. Patent and Trademark Office (USPTO). (1987). Patent No. 4,703,063.
[2]: Lippard, S., & Berg, J. (1994). Principles of bioinorganic chemistry. University Science Books.
[3]: European Patent Office. (2022). Patent documentation on platinum-based drugs.

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Drugs Protected by US Patent 4,703,063

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
>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: 4,703,063

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Japan55-14382Feb 08, 1980

International Family Members for US Patent 4,703,063

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0034432 ⤷  Start Trial SPC/GB96/017: EXPIRE United Kingdom ⤷  Start Trial
European Patent Office 0034432 ⤷  Start Trial 96C0048 Belgium ⤷  Start Trial
Argentina 227533 ⤷  Start Trial
Argentina 230433 ⤷  Start Trial
Austria 7223 ⤷  Start Trial
Australia 541720 ⤷  Start Trial
Australia 6689681 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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