Details for Patent: 10,414,751

Which drugs does patent 10,414,751 protect, and when does it expire?

Patent 10,414,751 protects VIVJOA and is included in one NDA.

This patent has twenty-two patent family members in nineteen countries.

Summary for Patent: 10,414,751

Title:	Antifungal compounds and processes for making
Abstract:	The present invention relates to polymorphic forms of compound 1 or 1a and processes for preparing compound 1 and 1a polymorphs, which are useful as antifungal agents. In particular, the invention seeks to provide a new methodology for preparing polymorphs of compound 1 and substituted derivatives thereof.
Inventor(s):	William J. Hoekstra, David Dale Wirth, Tracy Ehiwe, Thierry Bonnaud
Assignee:	Mycovia Pharmaceuticals Inc
Application Number:	US16/270,717
Patent Claim Types: see list of patent claims	Compound; Process;

Scope and Claims Analysis of US Patent 10,414,751 (Anhydrous Polymorph and Isolation Process) and the U.S. Patent Landscape

US Patent 10,414,751 is a crystalline form and manufacturing-process patent. Its enforceable scope is concentrated in (i) an anhydrous polymorph defined by a specific crystal structure (FIG. 9) and (ii) a solvent-suspension and isolation/drying route for converting a less-defined starting material (amorphous/solvate/hydrate) into that anhydrous solid. The claims are drafted to capture broad solvent combinations within defined classes (C3-C10 alcohols, selected hydrocarbons) and operational parameters (dried at ≥30°C).

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What claims are in US Patent 10,414,751 and how broad are they?

Short answer: Claim 1 protects the anhydrous polymorph of “compound of formula 1” defined by the crystal structure shown in FIG. 9; claims 2–12 protect a manufacturing process that isolates solids from a suspension of compound 1 in specified solvent systems, including conversion from amorphous/solvate/hydrate forms, with optional two-solvent combinations and drying at ≥30°C.

Claim 1: Product-by-polymorph defined by crystal structure (FIG. 9)

Claim 1

• “An anhydrous polymorph of a compound of formula 1”
• “polymorph has the crystal structure as shown in FIG. 9.”

Scope impact

• The claim is form-defining. Enforceability turns on whether an accused solid is (a) anhydrous and (b) has the same crystal structure as FIG. 9.
• The claim is not tied to a specific solvent history, particle size, or manufacturing conditions. If a competitor makes the same anhydrous polymorph through any route, it can still fall within Claim 1, assuming structural identity can be proven.

Potential boundary conditions in claim construction

• “Anhydrous” implies no included water. In practice, this often drives disputes over residual moisture content and whether a “thermodynamically anhydrous” solid is treated as anhydrous under the patent’s experimental characterization.
• “Crystal structure as shown in FIG. 9” is the key. If FIG. 9 is, for example, a powder XRD pattern, a CIF-derived structural model, or an indexing plot, claim scope will map to that dataset. If FIG. 9 is an XRD pattern, disputes usually include peak matching tolerances and method differences.

Claims 2–3: Process of isolating solid from suspension; starting material can be amorphous/solvate/hydrate

Claim 2

• “process to prepare an anhydrous polymorph of compound 1”
• “comprising suspending a compound of formula 1 in a solvent and isolating any solid material.”

Claim 3

• “compound suspended in the solvent is in one of an amorphous, solvate, or hydrate form.”

Scope impact

• Claim 2 is broad on what the starting form is only insofar as Claim 3 adds that limitation. With Claim 3 present as a dependent claim, you typically get layered protection:
  • Claim 2 covers the general suspension-isolation approach to generate the anhydrous polymorph, even if the starting form is not explicitly limited (depending on how “prepare an anhydrous polymorph” is construed).
  • Claim 3 strengthens coverage where the feedstock is known to be amorphous/solvate/hydrate.

“Suspending” and “isolating any solid material”

• “Suspending” is a functional step. It does not require true solution crystallization. It can include slurrying.
• “Isolating any solid material” is broad. It does not specify filtration vs centrifugation, or whether multiple solids are collected. That phrase supports capture of routes where solids are filtered and later dried.

Claims 4–6: Organic solvent limitation; C3–C10 alcohol; enumerated alcohols

Claim 4

• “solvent is an organic solvent.”

Claim 5

• “solvent is a C3–C10 alcohol.”

Claim 6

• specific list: n-propanol, i-propanol, n-butanol, i-butanol, s-butanol, t-butanol.

Scope impact

• This cluster is a strong protection zone because many pharmaceutical form-conversion processes use short-chain alcohols.
• If a competitor uses a different alcohol outside C3–C10 (eg C1–C2, C11+), they can avoid these dependent claims, but Claim 2 may still be asserted if the independent process limitation is satisfied.

Claims 7–12: Two-or-more solvents; alcohol + hydrocarbon; specific hydrocarbons; drying ≥30°C

Claim 7

• “two or more solvents.”

Claim 8

• “one solvent is a C3–C10 alcohol and one solvent is a hydrocarbon.”

Claim 9

• alcohol specified (same enumerated group).

Claim 10

• hydrocarbon specified: n-pentane, n-heptane or n-hexane, cyclohexane, or methylcyclohexane.

Claim 11

• example pair: “one solvent is i-propanol and one solvent is n-heptane.”

Claim 12

• “isolated solid material is dried at 30°C or higher.”

Scope impact

• Claim 8 is often where infringement risk concentrates because it covers a solvent-combination concept that is operationally common: alcohol as a reaction or conversion medium combined with a nonpolar hydrocarbon as an antisolvent or to control supersaturation and solid form outcome.
• Claim 10 enumerates specific hydrocarbon choices, which narrows the dependent coverage but also provides clear “design-around” points: using other hydrocarbons (eg heptane is included; what about isooctane, petroleum ether fractions, aromatic solvents) may or may not avoid literal infringement depending on whether the dependent claim is asserted and whether equivalents are pursued.

Drying at ≥30°C

• This is a process parameter that can be a practical infringement hook. If a competitor dries at <30°C to preserve a solvent molecule or to control anhydrousness, they may avoid Claim 12 while still infringing broader claims if they satisfy other limitations.

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How do FIG. 9 crystal structure and “anhydrous polymorph” drive infringement?

Short answer: The strongest product claim element is the crystal structure identity to FIG. 9, and the strongest process element is producing an anhydrous polymorph by suspension and isolation in the specified solvent systems. Those two facts define the proof burden.

What evidence typically matters for “crystal structure as shown in FIG. 9”

In U.S. patent litigation, the usual evidence set is:

• powder XRD patterns matched to the patent’s FIG. 9 dataset (with disclosure-driven peak assignment rules),
• solid-state characterization (often DSC, TGA) to support anhydrous status,
• moisture quantification (Karl Fischer or validated equivalent),
• and optionally solid-state NMR/IR if used to distinguish forms.

For validity and scope, the same dataset can also become the battleground if prior art documents disclose similar anhydrous forms or overlapping XRD patterns.

“Anhydrous” boundary: moisture, hydrate memory, and dynamic water

If an accused material has residual moisture or rehydrates on exposure, “anhydrous polymorph” can become contested. Claim scope is usually interpreted with the specification’s characterization methods.

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What does this patent likely claim protect beyond the form: conversion routes and process-driven exclusivity?

Short answer: The dependent claims are built to capture a typical form-conversion playbook: starting from non-crystalline or solvated/hydrated states, treating in specific solvent classes or combinations, isolating solids, and drying to achieve the targeted anhydrous polymorph.

Process concept map: limitation-by-limitation

1. Start with compound of formula 1 in amorphous/solvate/hydrate state (Claim 3).
2. Suspend in a solvent (Claim 2).
3. Use an organic solvent (Claim 4), and in narrower dependent claims:
   • use a C3–C10 alcohol (Claims 5–6), or
   • use two or more solvents (Claim 7) including:
     • one C3–C10 alcohol (Claims 8–9) and
     • one specified hydrocarbon (Claims 8, 10),
     • with an explicit example pairing (Claim 11).
4. Isolate solid material (Claim 2).
5. Dry at ≥30°C (Claim 12).

That structure supports both:

• product infringement (Claim 1) when the end state is made, and
• method infringement (Claims 2–12) even when the starting state is different.

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How does this patent fit into the U.S. patent landscape: Orange Book, FDA listing, and Paragraph IV risk?

Short answer: This analysis cannot produce a complete U.S. Orange Book status and generic/biosimilar risk picture from the claim text alone. No drug name, NDA/BLA number, or FDA-listed reference product is provided, so a precise “Orange Book status of the compound of formula 1” cannot be determined without that identifier.

What can still be stated from the claims alone

• The patent is drafted as a polymorph-form and process patent. That often appears in Orange Book listings when the reference product’s dosage form uses that specific form, or when the listed drug’s manufacturing uses the claimed form-conversion steps.
• The most likely enforcement targets, if this is listed, are:
  • Paragraph IV generic filers proposing the same or an equivalent anhydrous polymorph, and
  • filers whose process uses the same suspension-isolation approach with the claimed solvent systems.

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When does US 10,414,751 lose exclusivity in the U.S.? What is the likely expiration date?

Short answer: The claim text does not include filing date, priority date, patent term adjustment, or patent expiration data. Without those, an accurate expiration timeline cannot be stated.

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What patent landscape questions matter for this estate: other polymorph patents, method patents, and breadth overlap?

Short answer: Without the identity of “compound of formula 1,” this cannot be mapped to a complete family estate or competitor landscape. However, the claim drafting style indicates likely adjacency: other polymorphs (hydrates/solvates/amorphous), other conversion solvents, and other drying/isolating conditions.

Adjacent claim families commonly co-exist with this structure

• other polymorph patents:
  • hydrate, solvate, or different anhydrous polymorphs with different FIG. numbers.
• other process patents:
  • alternative solvent classes or antisolvents,
  • recrystallization conditions,
  • slurry pH, temperature, and mixing conditions (often not in the current claims but frequently in the specification).
• particle/process patents:
  • milling, comminution, spray drying or controlled crystallization to achieve a target form.

These are typically used to block design-arounds to avoid solvent enumeration or drying-temperature constraints.

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How strong is the patent estate for anhydrous polymorph exclusivity based on the claim structure?

Short answer: The estate strength is high on form-specific exclusivity (Claim 1) if FIG. 9 is tightly defined and experimentally reproducible. The process claims increase enforcement leverage because many manufacturing sites follow similar solvent antisolvent and drying steps.

Strength indicators visible in the claims

• Claim 1 is crystal-structure anchored, not merely “substantially the same XRD,” which usually increases enforceability if FIG. 9 is specific and disclosure-supported.
• Claims 8–11 show a narrow but actionable solvent-combination set that competitors often use. Even if they avoid one dependent claim by changing one solvent, Claim 2 and Claim 1 may remain available depending on product identity.

Primary fragility indicators (from claim design alone)

• If prior art discloses the same anhydrous polymorph, Claim 1 can be vulnerable regardless of solvent-processing novelty.
• If competitors can produce the same end-form via alternative routes not satisfying dependent solvent combinations, Claim 1 still captures them, but validity could hinge on prior art form disclosures rather than process novelty.

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What generic entry risks exist for products that use the same anhydrous polymorph?

Short answer: The key entry risk is whether the proposed generic produces the same anhydrous polymorph (Claim 1) or uses a suspension and isolation process in the claimed solvent classes and combinations (Claims 2–12).

Risk pathways

• Product route risk: generic manufactures an anhydrous polymorph matching FIG. 9.
• Process route risk: generic uses amorphous/solvate/hydrate feedstock, suspends in alcohol/hydrocarbon systems from the enumerated sets, isolates solids, and dries at ≥30°C.

Design-around touchpoints suggested by the claim text

• Use a solvent outside C3–C10 alcohols to avoid Claims 5–6 and 8–9 (but Claim 2 and Claim 1 may remain).
• Use a hydrocarbon outside the enumerated set to avoid Claims 8–10.
• Dry below 30°C to avoid Claim 12 (again, broader claims may still apply).
• Produce a different anhydrous polymorph whose structure does not match FIG. 9 to avoid Claim 1.

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How does this patent compare with typical polymorph patents in U.S. litigation?

Short answer: It follows a familiar two-layer strategy: a rigid product claim tied to a crystal structure (FIG. 9) plus a broad process claim coupled with narrower solvent embodiments and a drying threshold.

Practical litigation posture implied by the claim set

• Claim 1 often becomes the anchor because it covers any manufacturing method that yields the FIG.-9 anhydrous polymorph.
• Claims 2–12 provide additional hook claims to support a process narrative, especially if the accused manufacturer follows solvent-suspension and alcohol/hydrocarbon antisolvent workups.

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Key Takeaways

• Claim 1 is a form claim: an anhydrous polymorph of the “compound of formula 1” defined by crystal structure in FIG. 9. Infringement turns on whether an accused solid matches that structure and is anhydrous.
• Claims 2–3 are process claims: suspending compound 1 in a solvent and isolating solids; the feed can be amorphous, solvate, or hydrate.
• Claims 5–6 and Claims 8–10 broaden enforcement through commonly used C3–C10 alcohol systems and alcohol + specified hydrocarbon combinations.
• Claim 12 adds a concrete manufacturing parameter: drying at ≥30°C.
• Without the drug identity (and thus FDA listing details), this analysis cannot map the full U.S. Orange Book status, expiration timeline, or cross-family landscape for the specific reference product.

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FAQs

1) What does “crystal structure as shown in FIG. 9” control for infringement?
Whether the accused anhydrous polymorph is structurally identical to the FIG. 9 characterization, typically assessed by powder XRD and supporting solid-state tests.

2) Does the process claim require crystallization from solution?
No. “Suspending” and “isolating any solid material” supports slurry-style routes as long as the preparation yields the anhydrous polymorph.

3) Which solvents are explicitly covered by dependent claims?
C3–C10 alcohols (enumerated in Claim 6) and specific hydrocarbons (Claim 10), including combinations of an enumerated alcohol with an enumerated hydrocarbon.

4) Can a competitor avoid Claim 12 by drying at <30°C?
Claim 12 would be avoided, but infringement of Claim 1 and broader process claims may still be possible depending on the final polymorph and the other process steps.

5) If a generic makes the same FIG. 9 anhydrous polymorph using different solvents, is it still at risk?
Yes for Claim 1 if the final product matches the FIG. 9 anhydrous polymorph, because Claim 1 is not limited by the solvent system.

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References

No sources are provided because the request does not include bibliographic identifiers (assignee, filing/priority dates, specification text, FIG. 9 dataset description, or the underlying active ingredient and FDA reference product) needed to cite accurate external materials.

Drugs Protected by US Patent 10,414,751

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Mycovia Pharms	VIVJOA	oteseconazole	CAPSULE;ORAL	215888-001	Apr 26, 2022		RX	Yes	Yes			Y	Y

International Family Members for US Patent 10,414,751

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2016233113
Brazil	112017018823
Canada	2978339
China	107428724
Cyprus	1125554
Denmark	3271347