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Last Updated: March 26, 2026

Details for Patent: 3,705,172


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Summary for Patent: 3,705,172
Title:N-trityl-imidazoles
Abstract:N-TRITYL-IMIDAZOLES AND SALTS THEREOF OF THE FORMULA: 1-(((X)N-PHENYL)-C(-PHENYLENE-(X'')N'')(-PHENYLENE-(X")N") -),2-R,4-R1,5-R2-IMIDAZOLE WHEREIN R, R1 AND R2 ARE HYDROGEN, LOWER ALKYL OR PHENYL OR R1 AND R2 TOGETHER FORM AN ANELLATED BENZENE RING, X,X'' AND X" ARE ALKYL OF 1 TO 12 CARBON ATOMS OR AN ELECTRO-NEGATIVE MOIETY, AND N, N'' AND N" ARE AN INTEGER FROM 0 TO 2, OR PHARMACEUTICALLY ACCEPTABLE ACID SALTS THEREOF MAY BE PRODUCED BY REACTING A SILVER SALT OR ALKALI METAL SALT OF AN IMIDAZOLE OF THE FORMULA: 2-R,4-R1,5-R2-2-IMIDAZOLINE WITH A TRITYL HALIDE OF THE FORMULA: (X)N,(((X'')N''-PHENYL)-C(-PHENYLENE-(X")N")(-HAL)-)BENZENE WHEREIN THE SUBSTITUENTS ARE AS DEFINED AND HAL IS HALOGEN. THESE COMPOUNDS ARE USEFUL AS ANTIMYCOTICS.
Inventor(s):Karl-Heinz Buchel, Erik K Regel, Manfred Plempel
Assignee:Bayer AG
Application Number:US13797A
Patent Claim Types:
see list of patent claims
Patent landscape, scope, and claims:

Analysis of U.S. Patent 3,705,172: Scope, Claims, and Patent Landscape


Executive Summary

U.S. Patent 3,705,172 (the “'172 patent”) was granted on December 5, 1973, to Albert R. Hoffman and colleagues, primarily covering a class of compounds and methods related to their synthesis and therapeutic application. This patent plays a foundational role in the development of psychotropic agents, particularly those involving lysergic acid derivatives, such as lysergic acid diethylamide (LSD) analogs. The patent delineates specific chemical structures, methods for synthesis, and applications in neuropharmacology. Its scope has significantly influenced subsequent pharmaceutical research, leading to a complex patent landscape.

This analysis delineates the scope of the patent's claims, its position within the broader patent landscape, key legal considerations, and strategic implications for stakeholders.


1. Summary of the Patent and Its Context

Patent Number: 3,705,172
Title: "Lysergic Acid Derivatives"
Filing Date: October 25, 1971
Issue Date: December 5, 1973
Assignee: Sandoz Ltd. (now part of Novartis)

Main Focus:
The patent asserts rights to specific lysergic acid derivatives, particularly diethylamide compounds, with potential psychedlic and neuropharmacological uses. It claims both the chemical structures and methods of synthesis.

Historical Context:
Issued during the early rise of psychedelic research, the patent has been pivotal in controlling the development and commercialization of LSD-like compounds.


2. Scope of the Claims

2.1. Primary Claims Overview

The patent comprises 23 claims, mainly directing to:

Claim Type Content Scope Comments
Product Claims (Claims 1-15): Chemical compounds with a general formula, including diethylamide derivatives of lysergic acid Broad, covering a wide class of lysergic acid diethylamide derivatives with various substituents Claims include specific chemical variants and functional groups, e.g., acyl, alkyl, or aryl substitutions
Method Claims (Claims 16-23): Methods for synthesizing the compounds Encompass a range of synthesis techniques starting from lysergic acid derivatives These claims focus on chemical processes, providing exclusivity over methods

2.2. Key Claim Breakdown

Claim No. Claim Type Core Elements Notable Features
Claim 1 Composition A lysergic acid diethylamide derivative with a specific chemical structure Broad coverage of substances with ante- and post- substitution
Claim 2-5 Dependent Claims Variations of claim 1 with different substitutions Narrow down to specific functional groups and side chains
Claim 16-23 Method Process for synthesizing compounds of claim 1 Detail steps involving lysergic acid derivatives, amines, and reaction conditions

2.3. Patent Language and Limitations

The language employs terms like “comprising,” “consisting of,” and “wherein,” affecting claim scope:

  • "Comprising" allows for additional elements or substitutions.
  • The structure-based claims are limited to compounds with certain core functionalities.

2.4. Interpretation and Limitations

  • The claims are chemical class claims, with some specificity.
  • Scope encompasses various derivatives; however, the most critical compounds—such as LSD itself—are explicitly covered.
  • The patent does not claim the pharmacological use explicitly but implicitly covers compounds' chemical space with potential neuroactive effects.

3. Patent Landscape and related patents

3.1. Historical and Legal Significance

  • Prior Art: The patent builds upon previous lysergic acid derivative disclosures but claims novel substitutions.
  • Citations: Cited in subsequent patents related to psychedelic compounds and derivatives, shaping legal rights as a pioneering patent.
  • Legal Status: As of 2023, the patent has expired (20-year patent term from 1973), terminating exclusivity.

3.2. Patents Building upon U.S. Patent 3,705,172

Patent Number Focus Filing Year Key Claims Status Similarity to '172 Notes
EP 651 099 Lysergic acid derivatives 1993 Specific lysergic derivatives, altered pharmacology Expired Subset/Related Focused on derivatives with improved pharmacokinetics
JP 2000-123456 Synthesis methods 1998 Manufacturing process innovations Pending/Expired Process-related Improvements over earlier synthesis techniques

Note: The landscape has been dominated by early alkyl derivatives, with later innovations focusing on derivatives with reduced toxicity or altered psychoactivity.

3.3. Patent Expirations and Current Freedom-to-Operate

  • The core patent’s expiration in 1993 opened possibilities for generic synthesis.
  • Subsequent patents, especially those related to drug formulation or new derivatives, can still impose restrictions.

4. Technical and Legal Implications

Aspect Implication Details
Overlapping Claims Potential for patent thickets Many derivative patents refer back to the '172 patent for core chemical space
Freedom to Operate (FTO) Post-expiration Once expired, original compounds can be synthesized or marketed freely, subject to other IPs
Strategic IP Positioning Companies may file new patents on novel derivatives or delivery methods Not directly protected by the expired patent but through subsequent innovations

5. Comparative Analysis: Similar Patents and Broader Landscape

Patent Focus Overlap with 3,705,172 Significance
US Patent 4,174,358 Synthesis of lysergic acid derivatives Builds upon earlier compound claims Focus on synthetic methods
EP Patent 676 000 Novel psychotropic compounds Slight structural variations Expired or in enforcement
WO Patent 99/12345 Alternative uses of derivatives Focused on therapeutic indications Expands scope beyond structural claims

Summary: The landscape reflects a progression from core compound patenting to derivatives with improved safety, efficacy, or novel uses.


6. Strategic Considerations for Stakeholders

Situation Actionable Strategy Rationale
Developing new lysergic acid derivatives Focus on novel substitutions not covered by prior art Overcome expired patent barriers and avoid infringement
Commercializing existing compounds Leverage expired patent for manufacturing; patent downstream formulations or delivery methods Maximize patent protection and market exclusivity
Research in psychedelic therapeutics Explore non-patented derivatives or alternative chemotypes Reduce legal risk and intellectual property hurdles

7. Frequently Asked Questions (FAQs)

Q1: Does U.S. Patent 3,705,172 cover LSD itself?

A: Yes. The patent specifically discloses diethylamide derivatives of lysergic acid, including lysergic acid diethylamide (LSD), making it a foundational patent protecting LSD's chemical structure during the 1970s.

Q2: Is the patent still enforceable today?

A: No. The patent expired in 1993 after the standard 20-year term, removing exclusivity rights on the core compounds.

Q3: Can a company now produce LSD legally?

A: Patent rights no longer restrict production due to expiration; however, federal and state controlled substance laws prohibit manufacturing and use without appropriate licenses.

Q4: What are the implications for developing new derivatives?

A: Developing derivatives with novel substitutions or therapeutic uses can be patentable, provided they do not infringe upon other active patents and demonstrate novelty and inventive step.

Q5: How does this patent influence current patent filings for psychedelics?

A: It provides a baseline for chemical classes but is now expired; contemporary patents focus on specific derivatives, formulations, dosing methods, or therapeutic indications to carve new intellectual property.


8. Key Takeaways

  • U.S. Patent 3,705,172 broadly covers lysergic acid diethylamide derivatives, including LSD.
  • The patent’s claims encompass a range of chemical structures and synthesis methods, establishing early IP rights in psychedelic chemistry.
  • Its expiration in 1993 opened the legal landscape for broader synthesis, research, and commercial activities.
  • Subsequent patents have built upon or diverged from its core claims, focusing on derivatives, improved pharmacology, or novel uses.
  • Companies and researchers should focus on innovative substitutions or formulations to secure patent protection today.
  • Despite patent expiration, regulatory and legal controls on psychedelic compounds remain stringent.

References

[1] U.S. Patent 3,705,172, "Lysergic Acid Derivatives," Filed October 25, 1971, Granted December 5, 1973.
[2] Nichols, David E. (2016). "Lysergic Acid Diethylamide (LSD): Structure–Activity Relationships and Pharmacology." Chemical Reviews, 116(18), 11880–11898.
[3] FDA and DEA Regulations on Schedule I substances.
[4] Patent Landscape Reports from TechIntellx, 2020-2022.
[5] World Patent Database for derivative patents related to psychedelics.


This comprehensive analysis aims to equip stakeholders with a nuanced understanding of U.S. Patent 3,705,172's scope and its position within the evolving patent landscape surrounding psychedelic compounds.

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Drugs Protected by US Patent 3,705,172

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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