Last Updated: May 10, 2026

Details for Patent: 4,284,786


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Summary for Patent: 4,284,786
Title:5-Methylisoxazole-4-carboxylic-(4-trifluoromethyl)-anilide
Abstract:5-Methylisoxazole-4-carboxylic acid-(4-trifluoromethyl)-anilide and a process for its preparation is described. The compound has an antirheumatic, antiphlogistic, antipyretic and analgesic action, and can be used for the treatment of multiple sclerosis.
Inventor(s):Friedrich-Johannes Kammerer, Rudolf Schleyerbach
Assignee: Sanofi Aventis Deutschland GmbH
Application Number:US06/103,551
Patent Claim Types:
see list of patent claims
Compound;
Patent landscape, scope, and claims:

What does US Patent 4,284,786 claim, and how does it shape the US landscape?

US Patent 4,284,786 (the “’786 patent”) contains a single provided independent claim directed to a specific small-molecule anilide defined as 5-Methylisoxazole-4-carboxylic acid-4-(trifluoromethyl)anilide (claim 1). The claim scope is narrow in identity (one defined chemical entity) and narrow in structure (one defined substitution pattern on the isoxazole and one defined anilide linkage with a 4-trifluoromethyl group).

What is the core claim scope (claim 1)?

The claim language provided is:

  • Claim 1: “5-Methylisoxazole-4-carboxylic acid-4-trifluoromethyl-anilide of the formula ##STR6##”

Practical scope implications from the claim as stated

  • Single-structure coverage. The claim is directed to one compound with a specific heterocycle substitution pattern and one specific anilide substitution.
  • Structural “lock-in.” “5-Methylisoxazole-4-carboxylic acid” fixes:
    • The ring identity (isoxazole)
    • The substitution position “5-methyl”
    • The carboxylic acid position “4-carboxylic acid” prior to conversion to the anilide
  • Anilide linkage fixed. “-anilide” indicates the carboxylic acid is amidated with an aniline derivative (not an ester, not an acid, not a different amide identity).
  • Para substitution fixed. “4-trifluoromethyl-anilide” fixes the aryl substitution at the 4-position as CF3. No other aryl substitution patterns are included in the literal text you supplied.
  • No functional breadth. The claim does not recite activity, use, polymorphs, salts, hydrates, or a genus of analogs. With only one specific entity, infringement focus typically tracks exact structural match (and any dependent-claim design around is not visible from the single claim text provided).

What is the claim “moving parts” test for infringement?

From the literal identity constraints in claim 1, a product either meets the claimed formula/structure or does not. The key “must-have” elements are:

  1. Isoxazole core with methyl at position 5.
  2. Carboxamide formation at the isoxazole-4-carboxylic acid position (anilide, not carboxylic acid).
  3. Anilide aryl ring with CF3 at the 4-position.
  4. Overall molecule matches the formula (STR6) as printed in the patent.

This is a “closed-form” claim posture: it is not written as “a compound selected from,” and the claim does not include variables (substituent ranges, alternative groups, or tautomer/polymorph/open-chain analogs) in the text you provided.


How to read the “formula-of-STR6” constraint (what it typically does to scope)

Even without the graphic in the prompt, claim 1 is structured around “of the formula ##STR6##,” which in US pharmaceutical chemistry patents typically means:

  • The compound is defined by explicit atom connectivity and substitution positions.
  • Literal infringement analysis centers on whether an accused compound has the same skeleton and substituents as STR6.

Business consequence: For a portfolio or competitive landscape view, this kind of claim usually maps to:

  • A smaller chemical library risk surface than genus claims.
  • A higher precision “hit” rate when candidates are true structural analogs.

What does this mean for the US patent landscape?

Where does this patent sit (composition vs. use vs. method)?

Based on your provided claim, US 4,284,786 is a composition claim for a defined chemical entity (a specific anilide). It is not a method-of-treatment or dosing regimen claim in what you supplied.

Landscape consequence

  • The strongest freedom-to-operate (FTO) pressure comes from products that manufacture/sell/import that exact compound (or in some jurisdictions, certain equivalents depending on claim interpretation and doctrine of equivalents).
  • If competitors pursue different analogs (different CF3 position, different aryl substituent, different amide, or different isoxazole substitution), they may avoid literal scope while still potentially raising doctrine-of-equivalents risk. Your prompt does not provide enough claim detail to quantify that risk, so the analysis stays at the structural-coverage level visible in claim 1.

How narrow identity claims tend to interact with later filings

For later US filings, the typical landscape patterns around a narrow entity claim are:

  • Around-the-core analog strategy: Future patent applications often claim “similar” scaffolds by changing one structural element (for example, aryl substitution pattern, amide nitrogen substituent identity, or heterocycle substitution). Narrow entity claims reduce overlap with these analogs unless the later filings happen to recapture the exact STR6 structure.
  • Salt/polymorph strategy: If the compound is an active ingredient, later filings frequently pursue specific salt forms or solid-state forms. Your prompt includes only claim 1 and does not provide further claim set details, so no direct conclusion can be drawn about whether 4,284,786 covers salts or polymorphs in its claim language as provided.

What is the exploitable competitive intelligence from the claim wording?

Key differentiators in competitors’ chemotypes

The two “high-information” structural handles in claim 1 are:

  • Isoxazole 5-methyl / 4-carboxamide pattern
  • Anilide with 4-CF3 substitution

Competitive programs that keep the isoxazole pattern but change the aniline ring, or keep the aniline CF3 but change the isoxazole substitution, are less likely to fall within literal claim coverage for STR6. Programs that preserve both handles (exact identity) face the clearest claim mapping.


Key Takeaways

  • US Patent 4,284,786 claim 1 is a single-entity composition claim directed to 5-Methylisoxazole-4-carboxylic acid-4-trifluoromethyl-anilide as defined by formula STR6.
  • The scope is structurally narrow: it fixes ring identity, key substitution positions, and the anilide linkage with para-CF3.
  • For landscape purposes, the main competitive risk zone is true structural identity matches to STR6; analogs that alter the isoxazole substitution pattern, the amide form, or the aryl substitution pattern are outside the literal wording as provided.

FAQs

1) Is claim 1 a genus or a single compound claim?

It is a single compound claim: it names one defined chemical entity and references one formula (STR6).

2) Does claim 1 cover salts or polymorphs?

The provided claim text is limited to the named anilide compound “of the formula STR6.” No salt/polymorph coverage is visible in the claim language you provided.

3) What structural elements are essential to meet the claim literally?

The molecule must have the 5-methylisoxazole-4-carboxamide scaffold and an anilide aryl ring with a 4-trifluoromethyl substituent, matching the connectivity of STR6.

4) Do functional claims (like “for treating disease”) appear in claim 1?

Not in the provided claim 1 text. It is a composition identity claim.

5) What is the practical competitive implication for analog programs?

Analog programs that change either the isoxazole substitution pattern or the anilide aryl substitution pattern are less likely to fall within the literal scope of claim 1, which is anchored to one defined structure.


References

[1] United States Patent and Trademark Office (USPTO). US Patent 4,284,786. (Claim 1 text as provided in the prompt: “5-Methylisoxazole-4-carboxylic acid-4-trifluoromethyl-anilide of the formula ##STR6##.”)

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Drugs Protected by US Patent 4,284,786

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: 4,284,786

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Germany2854439Dec 16, 1978

International Family Members for US Patent 4,284,786

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Argentina 222680 ⤷  Start Trial
Argentina 226894 ⤷  Start Trial
Austria 1067 ⤷  Start Trial
Australia 529341 ⤷  Start Trial
Australia 5385379 ⤷  Start Trial
Bulgaria 60764 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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