Patent: 9,211,281

Summary for Patent: 9,211,281

Title:	Pesticidal compositions and processes related thereto
Abstract:	This document discloses molecules having the following formula (\"Formula One\"): ##STR00001## and processes associated therewith.
Inventor(s):	Lo; William C. (Fishers, IN), Hunter; James E. (Indianapolis, IN), Watson; Gerald B. (Zionsville, IN), Patny; Akshay (Waltham, MA), Iyer; Pravin S. (Secunderabad, IN), Boruwa; Joshodeep (Hyderabad, IN)
Assignee:	Dow AgroSciences LLC (Indianapolis, IN)
Application Number:	14/132,947
Patent Claims:	see list of patent claims

Patent 9,211,281: What the Claims Actually Cover and Where the US Landscape Likely Traps or Exempts Competitors

United States Patent 9,211,281 is drafted as a broad pesticidal composition claim set anchored on a highly substituted small molecule defined by a Formula One Markush-like structure (Claim 1), then expanded through extremely permissive add-on language (Claims 2-4, 12-14), and finally broadened again via form/derivative/capture formats (Claims 5-11, 17-18). The result is a patent that is not limited to one product profile, but instead reads on a class of analogs/formulations plus a wide range of co-formulated actives and delivery formats.

What does claim 1 cover, in enforceable terms?

Claim 1 structure: a Markush envelope around a specific scaffold

Claim 1 is a composition comprising a molecule according to Formula One, with variable definitions for R1-R13/X1-X3 and a specific substitution logic for the R11 region. Even without parsing the full 2D drawing, the control points are clear:

• Halogenation pattern
  • R2, R3, R4: each is F, Cl, Br, or I.
  • R10: F, Cl, Br, I, (C1-C8)alkyl, or halo(C1-C8)alkyl.
• Hydrogen locks
  • R1 = H
  • R5 = H
  • R7 = H
  • R8 = H
  • R9 = H
  • R11 depends on a specific amide/urea-like motif (see below)
  • R12 = H
  • R13 = H
• Haloalkyl handle
  • R6 = (C1-C8)haloalkyl
• R11 is tightly constrained but still broad
  • R11 has the pattern:
  • C(═X5)N(H)((C0-C8)alkyl)N(R11a)(C(═X5)(R11b))
  • X5 = O
  • R11a: H or (C1-C8)alkyl
  • each R11b: (C1-C8)alkyl, halo(C1-C8)alkyl, or cyclo(C3-C8)alkyl
• Bridge variables
  • X1 = CR12
  • X2 = CR13
  • X3 = CR9
    Since R12 = H, R13 = H, and R9 = H, these effectively lock the “X” positions to carbon-hydrogen at the relevant spots.

Enforceability impact. From a freedom-to-operate standpoint, Claim 1 is not “any halogenated pesticide.” It is anchored to a specific scaffold in Formula One. But the substitution breadth inside that scaffold is large (especially R2-R4, R6, and R10, plus R11b). That means competitors are not just looking at one compound. They are looking at a combinatorial analog space that stays inside the claim.

What claim 1 excludes (functionally)

Claim 1 includes many explicit locks (H’s and O at X5). It also requires:

• the R11 oxygen-containing carbonyl motif (X5 = O),
• the specific R11 substitution framework,
• and the specific mapping relationships X1/X2/X3 to CR12/CR13/CR9 (which are hydrogen in the claim).

If the actual marketed active uses a different carbonyl mapping (or replaces O with something else), or if the scaffold changes such that the “X positions” no longer match CR12/CR13/CR9, that is the main route out of Claim 1.

How do claims 2-4 expand the risk beyond the molecule?

Claim 2: co-formulation with almost any pesticidal class

Claim 2 adds a second layer: the composition of Claim 1 further comprising one or more compounds that are selected from broad functional categories.

The categories include:

• “caricidal, algicidal, avicidal, bactericidal, fungicidal, herbicidal, insecticidal, molluscicidal, nematicidal, rodenticidal, or virucidal”
• or antifeedants, bird repellents, chemosterilants, herbicide safeners, insect attractants, insect repellents, mammal repellents, mating disrupters, plant activators, plant growth regulators, or synergists
• or both

Key analytical point: Claim 2 does not force any co-active to be specific. The language is broad enough that virtually any multi-active agrochemical blend could satisfy Claim 2, as long as Claim 1’s molecule is present.

Claim 3: named co-actives (very large enumerated list)

Claim 3 further expands Claim 1 compositions with one or more compounds selected from a group that includes (3-ethoxypropyl)mercury bromide through essentially hundreds of pesticidal agents, including:

• common herbicides (e.g., 2,4-D, glyphosate),
• insecticides (e.g., imidacloprid, fipronil),
• fungicides (e.g., azoxystrobin),
• rodenticides (e.g., brodifacoum),
• and many more.

Even though the list is enormous and overlaps with mainstream agrochemical catalogs, its legal function is to provide explicit selection anchors: if a competitor uses any listed common active, Claim 3 becomes a straight read-on mechanism.

Claim 4: agricultural carrier

Claim 4 is standard but important for product packaging reality:

• the composition includes an agriculturally acceptable carrier.

This closes a common design-around tactic (selling “neat” active only) by covering carrier formulations.

Are there claim features that let you design around?

Claim 5-11: salt, derivative, isotopic, polymorph, hydrate, ester

Claims 5-11 cover numerous physical forms:

• acid addition salts (Claim 5)
• salt derivatives (Claim 6)
• hydrates (Claim 7)
• ester derivatives (Claim 8)
• crystal polymorphs (Claim 9)
• ^2H/^1H substitution (Claim 10)
• ^14C/^12C substitution (Claim 11)

Critical impact: these are classic “form coverage” clauses. If competitors try to escape infringement by using a different salt or polymorph, Claims 5-11 are designed to keep them inside the perimeter.

Claim 10 and 11: isotope variants are explicitly claimed

This blocks one high-leverage workaround in chemical patents: swapping to an isotope labeled or differently enriched version used for tracking, metabolism studies, or certain formulations.

Claims 17-18: encapsulation and particle size

Claims 17 and 18 extend coverage to encapsulated delivery:

• “encapsulated inside, or placed on the surface of, a capsule” (Claim 17)
• capsule diameter about 100-900 nanometers or 10-900 microns (Claim 18)

This is a serious formulation vector. It reads on:

• microcapsule agrochemical formulations,
• controlled-release coatings,
• and many nanoparticle delivery platforms that fall inside the size envelope.

Claim 12 and 13: co-formulated biopesticides and extra enumerated “mode of action” compounds

Claim 12: biopesticide add-on

Claim 12 says the Claim 1 composition further comprises a biopesticide. There is no restriction on which type. This further broadens the set of commercially plausible blends.

Claim 13: specific additional compounds

Claim 13 adds the further comprising feature for one or more compounds selected from a limited list of named chemical entities (a-j, with additional entries continuing).

Analytical significance is not the identity of every chemical in the list, but the claim construction effect:

• If a co-formulation includes any of those named members, Claim 13 becomes an additional infringement hook beyond Claim 2/3.

Claim 14: mode-of-action selection categories

Claim 14 covers adding compounds with specified pesticide modes of action:

• acetylcholinesterase inhibitor
• sodium channel modulator
• chitin biosynthesis inhibitor
• GABA and glutamate-gated chloride channel antagonists and agonists
• acetylcholine receptor agonist/antagonist
• MET I inhibitor
• Mg-stimulated ATPase inhibitor
• nicotinic acetylcholine receptor
• Midgut membrane disrupter
• oxidative phosphorylation disrupter
• ryanodine receptor (RyRs)

Critical landscape effect: even if the competitor does not use the exact co-actives in Claim 3, Claim 14 can still be satisfied if they formulate with actives in those MOA bins.

Claim 15-16: seeds (including genetically modified seeds)

Claim 15 extends to compositions further comprising a seed.

Claim 16 extends to a seed genetically modified to express specialized traits.

This matters in the US regulatory and commercial pipeline because:

• seed treatments and seed + chemistry packages can be operationally close to “composition comprising a seed” products.
• Genetically modified seed usage adds distribution complexity, but Claim 16 is drafted to catch it regardless.

What does the total claim set do to competitors?

1) Molecule perimeter is broad enough to cover many analogs

• R2-R4 are multiple halogens.
• R6 is any haloalkyl (C1-C8).
• R10 is halogen/alkyl/haloalkyl.
• R11a and R11b include H/alkyl and multiple alkyl/haloalkyl/cycloalkyl options.

This means competitors cannot safely assume “different halogen pattern” or “different short alkyl substitution” will avoid Claim 1.

2) Co-formulation language is “belt and suspenders”

• Claim 2 gives broad functional class coverage.
• Claim 3 provides an enormous named list that includes many widely-used actives.
• Claim 14 provides mode-of-action coverage as a second set of functional hooks.

A competitor blending the molecule from Claim 1 into any multi-active agrochemical mix is at elevated risk across multiple independent claim theories.

3) Form factors are already covered

Salt, hydrate, ester, polymorph, isotope variants, and microencapsulation are all claimed. This makes typical formulation-based design-around strategies less effective.

US patent landscape: how this claim set likely positions relative prior art

A precise “landscape” map requires bibliographic searching of US application families, citations, and claim construction history. That information is not present in the provided record. Under the constraints here, the analysis focuses on claim mechanics, which is where investors and R&D teams need a fast go/no-go framework.

Likely landscape implication

• The breadth of Claim 2/3/14 suggests the patentee is trying to capture downstream formulations and not only one active ingredient.
• The extensive salt/derivative/polymorph/isotope coverage suggests that infringement is meant to attach to practical commercial variants.
• The encapsulation size range suggests the molecule is also being targeted for controlled release platforms.

In practical terms, once a formulation team uses the molecule (or an accused analog meeting Formula One), there are many independent ways to satisfy “composition comprising” elements even if the rest of the product differs.

Critical claim vulnerabilities and litigation pressure points

Even broad claim language has friction points during validity and infringement analysis.

Potential vulnerabilities (based on drafting patterns)

1. Formula One scope depends on correct mapping of substituents
   • If an accused compound does not match one required variable constraint (e.g., R2/R3/R4 set, R6 haloalkyl constraint, R11 oxygen at X5, the H locks, or the X1/X2/X3 mappings), infringement can fail at the threshold.
2. “one or more compounds” for Claim 2/14 is permissive but must still be present
   • For infringement, the accused composition must still be “a composition according to claim 1” and include at least the selected classes. But the “selected classes” are broad enough that this is rarely a hard barrier for commercial blends.
3. Capsule size range is numeric and bounded
   • If a competitor uses capsule technology outside the claimed diameter envelope, Claim 18 may not apply. Claim 17 still applies to any capsule (no size limit), so design-around depends on avoiding capsule placement entirely or using a delivery format not meeting the claim’s capsule concept.

Key Takeaways

1. Claim 1 is a scaffold-level claim with wide substitution latitude (R2-R4, R6, R10, R11a/R11b) while locking several positions to H and locking X5 = O.
2. Claims 2-4 and 12-14 expand infringement to multi-active formulation space using both broad functional categories and an extremely large enumerated co-active list.
3. Claims 5-11 and 17-18 cover real-world commercial variants: salts, hydrates, esters, polymorphs, isotopes, and encapsulation across a broad particle size range.
4. Seed and genetically modified seed elements (Claims 15-16) widen product-form coverage into agricultural deployment formats.
5. The practical competitive risk is highest where teams plan to blend the molecule into carrier, seed treatment, or controlled-release microcapsule products, and where co-actives include commonly used mainstream pesticides.

FAQs

1. Is infringement likely if a competitor uses the molecule in a salt form?
   Yes. Claims 5-7 explicitly cover acid addition salts, salt derivatives, and hydrates; Claims 8-11 add ester derivatives, polymorphs, and isotope variants.

2. Do the co-active clauses require specific chemicals?
   Not always. Claim 2 uses broad functional class terms; Claim 14 uses mode-of-action bins. Claim 3 is specific but massive. Any accused “Claim 1 molecule + common co-actives” blend is at risk.

3. Can competitors avoid coverage by changing halogens or short alkyls on the scaffold?
   Not safely. Claim 1 allows substantial variation in R2-R4, R6, and R10, and provides broad options for R11a/R11b.

4. Does encapsulation add another infringement hook even for standard formulations?
   Yes. Claims 17-18 cover compositions where the molecule is inside or on a capsule, with a broad diameter envelope also specified.

5. What is the cleanest theoretical design-around?
   A compound that does not meet the Formula One constraints at the variable mapping level (especially the locked H positions and the R11 carbonyl motif with X5 = O) and avoids the capsule/seed/covered-form scenarios.

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References

[1] United States Patent 9,211,281 (claims 1-18 as provided in the prompt).

Details for Patent 9,211,281

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Hoffmann-la Roche Inc.	PEGASYS COPEGUS COMBINATION PACK	peginterferon alfa-2a and ribavirin		125083	June 04, 2004	9,211,281	2033-12-18
Schering Corporation A Subsidiary Of Merck & Co., Inc.	PEGINTRON/ REBETOL COMBO PACK	peginterferon alfa-2b and ribavirin		125196	June 13, 2008	9,211,281	2033-12-18