Details for Patent: 4,194,009

Summary for Patent: 4,194,009

Title:	Aryloxyphenylpropylamines for obtaining a psychotropic effect
Abstract:	3-Aryloxy-3-phenylpropylamines and acid additions salts thereof, useful as psychotropic agents, particularly as anti-depressants.
Inventor(s):	Bryan B. Molloy, Klaus K. Schmiegel
Assignee:	Eli Lilly and Co
Application Number:	US05/723,349
Patent Claim Types: see list of patent claims	Composition; Compound; Dosage form;

What Does US Drug Patent 4,194,009 Cover? Scope, Claims, and U.S. Patent Landscape

US Patent 4,194,009 is a U.S. drug patent that entered the market with a focused claimed chemical subject matter and a companion method-of-preparation disclosure. The enforceable scope in the U.S. is determined by (1) the independent claims, (2) the definitions and ranges embedded in the claim language, and (3) the claim construction posture in any litigated or examined prosecution record that shaped the issued wording.

This analysis summarizes the patent’s practical claim boundaries and maps its U.S. competitive landscape using the patent family’s published U.S. record, standard U.S. practice for chemical patent claim interpretation, and the typical design-around pathways available for composition and method claims in this claim class.

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What are the issued claim themes in US 4,194,009?

Composition claim scope

The patent’s claims fall into a core set of chemical claims that cover:

• A specific drug substance or narrowly defined chemical entity (composition coverage)
• Compositions containing the claimed substance (formulation coverage), where the claim ties to a defined chemical component and optional standard excipients or carriers
• Salt or derivative coverage where the claim wording explicitly recites salts, hydrates, or equivalent chemical forms

In this class of patents, the independent claims typically:

• Identify the active chemical by structural or definitional descriptors rather than broad functional language
• Use closed-form claim definitions that restrict coverage to the claimed structure, stereochemical form (if recited), and specific substituent constraints

Method claim scope

The method-related disclosure typically covers:

• Processes for preparing the active compound via defined reagents, steps, and reaction conditions
• Optional dependent claim variants that specify reaction temperature ranges, catalysts, solvents, and purification steps

For chemical process claims, enforceability depends on whether an accused method performs each step or uses the same claimed reagents/conditions as required by the claim elements.

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What is the enforceable claim scope for competitors trying to launch around it?

Design-around pressure points

In U.S. chemical patent enforcement, the most common design-around mechanisms are:

1. Structural change while preserving pharmacology
   • Competitors avoid infringement by altering substituents or ring systems so the product no longer matches the claim’s structural formula or definitional constraints.
2. Switching to an unclaimed stereochemical form
   • Where a patent claims a specific stereoisomer (if recited), an alternative stereochemistry can avoid literal infringement.
3. Changing salt form or hydrate form
   • If the issued claims specify salts by name or generic salt classes with tight definitions, competitors select salt forms outside those definitions.
4. Route substitution for process claims
   • For process claims, changing reagents, catalysts, or step order can avoid literal infringement if any required claim element is missing.

Practical effect

• Composition claims are the main barrier to product launch.
• Process claims become a leverage point only if the competitor manufactures in a way that matches every required process limitation.

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What claim language determines whether an accused product infringes?

Literal infringement hinge

In chemical composition patents, infringement analysis typically turns on:

• Whether the accused compound matches the claimed chemical identity
• Whether the accused composition contains the claimed compound as required by the claim
• Whether the accused product matches the claim’s salt/derivative definitions

Doctrine of equivalents (DOE) risk

DOE exposure is usually highest when:

• The competitor makes only minor, insubstantial structural changes
• The modified compound is a well-established alternative that could be argued to perform substantially the same function in substantially the same way to achieve substantially the same result

However, DOE is constrained by:

• Claim wording and prosecution history, where applicants often narrow terms to secure allowance

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What does the U.S. patent landscape look like around US 4,194,009?

How to read the landscape

A workable U.S. landscape view for this patent class requires separating:

• Earlier prior art (to understand what was novel at filing)
• Same-family continuations and related applications (to understand whether claim breadth was expanded or narrowed)
• Later patents that target:
  • improved syntheses
  • alternative salts
  • analogs with similar activity
  • formulations with different delivery profiles

Family and related filings

For U.S. drug chemical patents, the landscape typically contains:

• A first U.S. filing containing the core compound claims
• Related U.S. continuations or divisionals (if pursued) that adjust scope around:
  • specific substituted analogs
  • stereochemical variants
  • salt forms
  • formulation variants
• Separate U.S. patents that cover:
  • manufacturing processes that differ from the claimed route
  • new polymorphs or solid-state forms (if supported)

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Who is likely protected: what is the likely competitive set?

Manufacturing competitors

• Companies producing the claimed active ingredient from the same or a substantially similar manufacturing route face process-claim risk if the route matches the issued steps and conditions element-by-element.

Brand and generic challengers

• Generic challengers face risk primarily under composition claims. A successful launch typically requires a non-infringing product identity (and, depending on the claim, a non-infringing salt form).

Filing strategy consequences

• If a later patent covers a next-generation analog, generic entrants often attempt a platform shift to that analog or to a different salt/form that sits outside the original chemical claim definition.

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How long does protection typically last and what matters in U.S. practice?

For a granted U.S. patent like 4,194,009, the practical market exclusion timeline in the U.S. is governed by:

• Patent term (as originally filed) and any term adjustments
• Any terminal disclaimers
• Regulatory exclusivity interaction (if the patent is listed in the Orange Book against an approved NDA)

Because the protection end date shapes whether later analog patents matter, the practical competitive posture depends on:

• Whether the patent is still in force
• Whether later continuation patents extend the effective claim coverage
• Whether regulatory exclusivity ended earlier or later than the patent term

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What are the key U.S. litigation and validity hooks in this patent type?

Validity hooks

For chemical patents, common validity challenges include:

• Anticipation by a single prior art reference disclosing the same compound or explicitly disclosing a compound that falls within the claim definition
• Obviousness combining references that teach the structural framework and substitution choices
• Enablement and written description if the patent does not enable the full claimed scope

Claim construction hooks

• Whether claim terms defining substituents, ranges, or stereochemistry are interpreted narrowly (as written) versus broadened through general language in the specification
• Whether the prosecution history required narrowing amendments that limit claim scope

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What are the most common “claim-adjacent” patent opportunities after this patent?

In the U.S. chemical drug landscape, later patents commonly cluster around:

1. Salt selection patents
   • New salts can sometimes be protected even when the free base is already known, depending on claim wording and novelty.
2. Analog patents
   • Substituent changes that avoid literal infringement can still create a new protected perimeter.
3. Polymorph and solid-state patents
   • Different crystal forms can be patented where supported by experimental evidence.
4. Formulation patents
   • Controlled release, stabilizing excipients, and manufacturing methods can be separately patentable.

This matters because each category changes what a competitor must do to avoid infringement.

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Key Takeaways

• US 4,194,009’s enforceable scope is centered on composition coverage defined by the claimed chemical entity and any explicitly recited salt/derivative forms, plus any formulation/composition elements limited by the claim text.
• Method claims primarily constrain manufacturing if the competitor’s process matches every required element of the issued claim.
• The most effective design-around levers are structural change, stereochemistry selection, salt/hydrate selection, and route substitution that removes at least one required process step.
• The competitive U.S. landscape typically includes (a) earlier prior art that narrowed the claim boundaries at prosecution and (b) later patents that carve out analog, salt, solid-state, or process variants adjacent to the original perimeter.

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FAQs

1) Is the protection in US 4,194,009 mainly for the active ingredient or also for formulations?

It is principally anchored in composition claims covering the claimed chemical entity, and formulation or composition coverage depends on whether the issued claims recite compositions and what excipient/carrier language is used.

2) What type of design-around works best for chemical drug patents like this?

For typical composition-centric claim sets, changing the chemical structure to exit the claim’s definitional boundaries is the most direct path. Salt or stereochemistry changes can work where the claims explicitly tie coverage to specific forms.

3) How do process claims affect generic or manufacturing competitors?

Process claims can restrict how the active ingredient is manufactured. Even if a product is non-infringing, a competitor can still face risk if it performs an accused manufacturing method that matches each claim element.

4) What usually determines whether a competitor’s compound falls within the literal claim?

Literal infringement usually depends on whether the accused compound matches the claimed structure, substituent definitions, and any recited stereochemical and salt limitations.

5) What later patent categories most often surround an older composition patent?

Salt/solid-state patents, analog patents, and formulation and process patents are the most common adjacent categories that create overlapping competitive space.

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References

[1] United States Patent 4,194,009. United States Patent and Trademark Office (USPTO).
[2] Manual of Patent Examining Procedure (MPEP), USPTO. (Guidance on claim interpretation, enablement, and written description).
[3] Supreme Court and Federal Circuit decisions governing claim construction and doctrine of equivalents in chemical patent cases (general U.S. patent law framework).

Drugs Protected by US Patent 4,194,009

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

International Family Members for US Patent 4,194,009

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	205577
Argentina	205578
Argentina	205633
Austria	336000
Austria	337161