Fungicidal compositions containing derivatives of 2, 4-dioxo-1, 4-dihydrothieno[2, 3-d]pyrimidine

A composition and fungicidal technology, applied in the direction of chemicals, fungicides, biocides for biological control, etc., can solve problems such as reducing the efficacy of chemical fungicides

Active Publication Date: 2018-07-31
GILEAD APOLLO INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] For example, the rapid emergence of resistance to chemical fungicides often reduces the efficacy of some chemical fungicides

Method used

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  • Fungicidal compositions containing derivatives of 2, 4-dioxo-1, 4-dihydrothieno[2, 3-d]pyrimidine
  • Fungicidal compositions containing derivatives of 2, 4-dioxo-1, 4-dihydrothieno[2, 3-d]pyrimidine
  • Fungicidal compositions containing derivatives of 2, 4-dioxo-1, 4-dihydrothieno[2, 3-d]pyrimidine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0437] Example 1: In Vitro Pathogen Growth Inhibition Assay

[0438] Growth inhibition assays were performed to determine the ability of compounds to control the growth of fungal pathogens such as Botrtyis cinerea (Bc), Collectotrichum graminicola (Cg), Diplodia maydis, Dm), Fusarium moniliforme (Fm), North American soybean sudden death syndrome (Fusarium virguliforme, Fv), Phytophthora capsicum (Phytophthoracapsici, Pc), Rhizoctonia solani (Rs) and wheat Septoria tritici (St).

[0439] Compounds listed in Table 1 were each dissolved in DMSO at 2.5 mg / ml to generate compound stock solutions ("stock solutions"). Stock solutions were diluted with DMSO by 5-fold serial dilution in 96-well stock plates and two sets of final concentrations were obtained in vitro, 50, 10 and 2 ppm or 2, 0.4 and 0.08 ppm.

[0440] A set of positive controls was also prepared in which various concentrations of Soraphen (2, 0.4 and 0.08 ppm), metalaxyl (1.1, 0.22 and 0.04 ppm) and metconazole (2, 0.4...

Embodiment 2

[0458] Embodiment 2: Leaf protection test of control of barley powdery mildew

[0459] Plants (Hordeum vulgare cv. Perry) were grown for 6 days in 2 inch square pots containing fertilizer modified Metromix 200 medium. For propagation, plants were maintained in a growth chamber at 20-21° C., 16 hour photocycle, 400 uM light, 70% humidity, and subirrigated as needed. After inoculation with the pathogen of Blumeria graminis f. sp. hordei, the plants were kept at 20-22° C., 70% relative humidity and 200 uM light to promote infection and disease development.

[0460] 6 days after sowing (first true leaf fully expanded), test compounds were dissolved in a solution of 5% acetone and 0.005% Tween 80 surfactant. Apply the solution to both sides of the leaves using an atomizer until fully wetted. The amount of compound applied to the foliage is typically 200, 100, 50, 10 or 2 ppm, but this can vary.

[0461] Twenty-four hours after treatment, the plants were moved to a cooler room an...

Embodiment 3

[0466] Example 3: Leaf Protection for Cucumber Powdery Mildew Control

[0467]Plants (Cucumis sativus cv. Straight Eight) were grown for 10 days in 2.5 inch square pots containing fertilizer modified Metromix 200 medium. For propagation, plants were kept in a growth chamber at 23-27°C, 16-hour light cycle, ambient humidity, and subirrigated as needed. After inoculation with the pathogen of cucumber powdery mildew ( Sphaerotheca fuliginea ), plants were maintained at 23-27° C., 16 hour photocycle, 60% relative humidity, and subirrigated as needed to promote infection and disease development.

[0468] 10 days after sowing (75% of the first true leaf unfolded and no second leaf appeared), the test compounds were dissolved in a solution of 5% acetone and 0.05% Tween 20 surfactant. Apply the solution to both sides of the leaves using an atomizer until fully wetted. The amount of compound applied to the foliage is typically 200, 100, 50 or 10 ppm, but this can vary.

[0469] Twen...

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Abstract

The present invention provides compounds that exhibit activity as fungicides and are useful, for example, in methods for the control of fungal pathogens in plants and can be applied to said plants ina variety of ways.

Description

[0001] Related Application Cross Reference [0002] This application claims priority under 35 U.S.C. § 119(e) to U.S. Provisional Application No. 62 / 259,935, filed November 25, 2015, which is hereby incorporated by reference in its entirety. technical field [0003] Provided herein are compounds that exhibit pesticidal activity and are useful, for example, in methods of controlling fungal pathogens and diseases caused by fungal pathogens in plants. Background of the invention [0004] Acetyl-CoA carboxylase ("ACCase") is an essential catalyst for the rate-limiting step of fatty acid biosynthesis in eukaryotes and prokaryotes. Phytopathogenic fungi can infect crops in the field or after harvest, causing considerable economic losses to farmers and producers worldwide. In addition to agricultural effects, a number of debilitating illnesses or deaths occur when food and feed contaminated with fungi or the toxins they produce are ingested by humans or livestock. About 10,000 sp...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A01N43/90A01P3/00A01N43/88A01N43/56A01N43/653A01N37/46A01N47/24A01N37/50A01N63/02A01N51/00A01N43/82A01N25/00
CPCA01N43/90C07D495/04A01N25/00A01N37/46A01N37/50A01N43/56A01N43/653A01N43/82A01N43/88A01N47/24A01N51/00A01N63/22A01N2300/00A01C1/06A01G7/06A01N25/30
Inventor J.L.班尼特K.C.菲茨西蒙斯S.高希J.R.格林伍德小威廉.P.哈肯森G.C.哈里曼S.M.莱特德莫拉代B.J.肖特U.J.斯洛姆齐恩斯卡J.M.斯坦
Owner GILEAD APOLLO INC
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