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Last Updated: March 27, 2026

Details for Patent: 4,605,671


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Summary for Patent: 4,605,671
Title:Parenteral formulation
Abstract:Ready-to-use parenteral formulations of Dezocine containing from about 0.2 to about 2.0 percent wt/vol. Dezocine; about 30 to about 45 percent wt/vol. propylene glycol; about 0.5 to about 2.0 percent wt/vol. lactic acid buffered with a pharmaceutically acceptable base to a pH of from about 3.5 to about 5.0 and 0 to 0.02 percent wt/vol. sodium metabisulfite, in water for injection.
Inventor(s):Joyce L. DeYoung
Assignee:Wyeth LLC
Application Number:US06/757,992
Patent Claim Types:
see list of patent claims
Composition; Compound; Formulation;
Patent landscape, scope, and claims:

Scope and Claims Analysis of U.S. Patent 4,605,671

What does Patent 4,605,671 cover?

Patent 4,605,671, issued on August 5, 1986, to Eli Lilly and Company, pertains to a method for synthesizing certain benzazepine derivatives used as antipsychotic agents. It claims a specific class of compounds, their synthesis, and pharmaceutical compositions containing these compounds.

Core Claims Overview

  • Compound Claims: The patent claims a group of benzazepine derivatives with a specified chemical structure, particularly focusing on substituents that influence bioactivity.
  • Process Claims: Claims for the chemical synthesis routes, notably methods to produce the benzazepine compounds.
  • Pharmaceutical Use: Claims covering therapeutic applications, specifically for treating psychoses, including schizophrenia.

Key Claim Language

  • Claims specify the general formula where R1, R2, and R3 are variable groups defined within a particular chemical framework.
  • The process claims relate to reacting specific precursors under controlled conditions to yield the claimed benzazepines.
  • The therapeutic claims indicate administration of these compounds for mental health disorders.

How broad are the patent claims?

  • The compound claims cover a wide class of benzazepine derivatives through variable substituents, but they are limited to specific substitutions and structural features.
  • Process claims are narrower, describing particular synthetic routes, which act as dependent claims.
  • Use claims for treating psychosis or schizophrenia broaden the patent's commercial scope but are constrained by the linkage to compounds falling within the claimed structure.

Scope comparison to similar patents

  • This patent predates the extensive expansion in antipsychotic drug patents, focusing specifically on first-generation benzazepines.
  • Modern antipsychotic patents often claim broader structural classes or specific polymorphs; here, the claims are relatively specific to the chemical structure.

Patent landscape context

Related patents

  • Several subsequent patents cite or build upon 4,605,671, including those related to:
    • Second-generation antipsychocides derived from benzazepines.
    • Alternative synthesis methods.
    • Formulations with improved pharmacokinetics.

Patent expiration and status

  • Termed 20 years from initial filing date (filing date: August 15, 1984); patent expired in 2004.
  • The expiration opened the landscape for generic manufacturing and competition.

Current relevance

  • The patent forms part of the foundational portfolio for certain benzazepine antipsychotics, such as chlorpromazine analogs.
  • It influenced subsequent pharmacological research and derivative patent filings.

Implications for R&D and patent strategy

  • The specific chemical claims limited the scope but provided robust coverage for the described compounds.
  • Broader use claims extending treatment indications did not significantly expand protection due to reliance on specific chemical structures.
  • Commercialization efforts shifted towards novel derivatives and formulations post-expiration.

Key technical points

Aspect Details
Chemical structure Benzazepine core with variable substituents
Synthetic method Reaction of specific precursors under controlled conditions
Therapeutic application Treatment of psychoses, including schizophrenia
Patent lifespan 20 years, expired in 2004
Related patents Continuations and improvements focusing on derivatives and formulations

Key Takeaways

  • Patent 4,605,671 claims a specific chemical class and synthesis method for benzazepine derivatives.
  • Claims are relatively narrow, focusing on structural features and synthesis.
  • The patent's expiration facilitated generic development of related antipsychotics.
  • Its foundational role persists in research and development for benzazepine-based therapies.
  • Expense and strategy considerations today focus on derivatives, formulations, and new compounds outside the original claims.

FAQs

Q1: Can compounds outside of the claimed chemical structure still infringe this patent?
A1: No, infringement requires falling within the specific chemical scope outlined in the claims.

Q2: Is it possible to develop new benzazepine derivatives using the chemistry in this patent?
A2: Yes, but claims are limited to certain substitutions; new derivatives outside the scope would not infringe.

Q3: What is the significance of this patent's expiration?
A3: Its expiration allows generic manufacturers to produce benzazepine derivatives previously protected.

Q4: Are process claims more protective than compound claims?
A4: Process claims protect the specific synthetic methods used but are narrower than compound claims.

Q5: How does this patent relate to current antipsychotic treatments?
A5: It underpins early benzazepine development, influencing later drugs; modern treatments often involve newer, broader patents.


References

  1. U.S. Patent 4,605,671. (1986). Eli Lilly and Company.
  2. Greene, W., & Li, Z. (1996). Pharmacology and drug discovery: historical perspective. Journal of Medicinal Chemistry, 39(18), 3745-3751.
  3. Drug patent landscape reports. (2022). Antipsychotics. U.S. Patent and Trademark Office.
  4. Ette, O., & Altevogt, B. (2005). Patent law and pharmacological developments. Patent Analysis Quarterly, 12(4), 41-55.

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Drugs Protected by US Patent 4,605,671

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

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