Bicyclic Isoxazoline Herbicides for Low-Rate Weed Control

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Solution Overview

Problem

Existing herbicides suffer from insufficient herbicidal activity, particularly at low application rates, and unsatisfactory selectivity, leading to low compatibility with crop plants and potential toxicity to humans and animals.

Innovation Solution

Development of bicyclic heterocycle compounds, including their agriculturally acceptable salts, amides, esters, or thioesters, with specific substituents that provide strong herbicidal activity, low toxicity, and high compatibility with crop plants, offering a broad spectrum of activity against unwanted vegetation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If conventional herbicides are used, then unwanted vegetation can be controlled, but herbicidal activity is insufficient at low application rates

Engineering Contradiction:

Improveapplication rateVSAvoidherbicidal activity

Core Design Contradiction:

Quantity of substanceVSReliability

Solution Approach 1:

The patent modifies the chemical structure of herbicide molecules by introducing specific substituent patterns at defined positions (R1-R6 groups) to optimize biological activity. This structural parameter change enables the compounds to achieve high herbicidal efficacy at low application rates while maintaining selectivity and crop safety

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The invention creates composite molecular structures combining bicyclic heterocycle cores with various functional groups (carboxamides, esters, thioesters) and diverse substituents. This molecular composite approach allows tuning of herbicidal activity, selectivity, and environmental safety properties simultaneously

Inventive Principle:

Principle #40Composite materials

2Reliability

If conventional herbicides are used, then herbicidal activity can be increased, but selectivity and compatibility with crop plants decrease

Engineering Contradiction:

Improveherbicidal activityVSAvoidtoxicity to humans and animals

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces specific substituent groups at defined positions (R1-R6) on the molecular structure to create localized functional regions. These local structural modifications enhance herbicidal activity at the target site while reducing non-specific toxicity to humans, animals, and crop plants through improved selectivity

Inventive Principle:

Principle #3Local quality

3Reliability

If herbicidal activity is increased, then unwanted vegetation control improves, but compatibility with crop plants deteriorates

Engineering Contradiction:

Improveherbicidal activityVSAvoidcompatibility with crop plants

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent optimizes molecular parameters including substituent types, positions, and configurations to achieve high herbicidal activity while maintaining crop safety. The bicyclic heterocycle framework with specific R1-R6 substituents provides enhanced selectivity between target weeds and crop plants

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS12617803B2Condensed isoxazoline derivatives and their use as herbicides

Publication Date: 2026.05.05 BASF SE

AI summary

The invention relates to compounds of formula (I), and their use as herbicides. In said formula, R1 to R6 represent groups such as hydrogen, halo-gen or organic groups such as alkyl, alkenyl, alkynyl, or alkoxy; W is a bicyclic heterocycle; X is a bond or a divalent unit; Y is hydrogen, cyano, hydroxyl or a linear or cyclic organic group. The invention further refers to a composition comprising such compound and to the use thereof for controlling unwanted vegetation.