Insect neuropeptide analogs

Abstract

The present invention relates to analogues of insect neuropeptides that are active against insects, such as Diptera, Hemiptera, Blattodea and / or Lepidoptera, and to the use of these as insect control agents (e.g., insecticides) and plant protection agents.

Description

[Technical Field]

[0001] The present invention relates to analogues of insect neuropeptides that are active against insects, such as those of the orders Diptera, Hemiptera, Blattodea, and / or Lepidoptera, and to the use of these as insect control agents (e.g., insecticides) and plant protection agents. [Background technology]

[0002] The global reliance on broad-spectrum insecticides with well-established damaging effects is increasing the need for the development of more environmentally friendly and selective insecticides. The development and use of neuropeptide synthesis analogs offer a promising avenue for advancing these more environmentally friendly and selective insecticides.

[0003] In insects, neuropeptides are regulatory peptides that play functional roles in growth and development, behavior and reproduction, metabolism and homeostasis, and muscle movement.

[0004] Due to their high specificity, neuropeptides and their related receptors (typically G protein-coupled receptors, GPCRs) can be developed for insecticides that selectively reduce the fitness of target pests while minimizing harmful environmental impacts and harming other non-target species, such as pollinators, whose populations have been found to be dangerously reduced due to the use of pest control agents / insecticides.

[0005] The insect neuropeptide family includes insect kinins and cardiac-promoting peptides (CAPA, CAP2b) neuropeptides.

[0006] The present invention provides kinin peptides and analogues. [Prior art documents] [Patent Documents]

[0007]

Patent Document 1

Patent document 2

Patent Document 3

Patent document 4

Patent document 5

Patent document 6

Patent document 7

Patent document 8

Non-licensed literature

[0008] [Non-licensed document 1] Systema Naturae, Brands,SJ (Editor)1989-2005.{j}Systema Naturae 2000.Amsterdam, The Netherlands, [http: / / sn2000.taxonomy.nl / ] [Non-licensed document 2] Developing the Arsenal Against Pest and Vector Dipterans: Inputs of Transgenic and Paratransgenic Biotechnologies, Ogaugwu and Durvasula, IntechOpen, 2017:{j}DOI:10.5772 / 66440 [Non-licensed document 3] Mozafari, MR "Nanoliposomes: preparation and analysis." Liposomes: Methods and Protocols, Volume 1: Pharmaceutical Nanocarriers (2010): 29-50

Non-licensed Document 4

Summary of the Invention

Problems to be Solved by the Invention

[0009] The inventors have discovered a novel analog of kinin peptide that has insecticidal activity against insects encoding kinin peptide such as those of Diptera, Hemiptera, Blattodea and / or Lepidoptera, and thus may potentially be found for use as a pest control agent or insecticide, but has little or no effect on important pollen-mediated species such as honeybees. The inventors have also discovered a novel kinin peptide.

Means for Solving the Problems

[0010] In a first aspect, the present invention provides an insecticidal compound having the following formula (XX), R 1 -L 1 -Y 1 -Y-Z-Y 2 -R 2 (XX) In the formula, R 1 is hydrogen (which may be represented as "H-" or "Hy-"), C 1~4 alkyl (e.g., methyl, ethyl, propyl, butyl), formyl, -N(R 1a )-C(=N + (R 1b )(R 1c ))NR 1d R 1e 、-C(=N + (R 1b )(R 1c ))NR 1d R 1e 、acyl, fatty acyl, benzyl, benzoyl, heteroaryl or trifluoroacetyl, -NHC 1~18Alkyl, -NHC 6~16 aryl, -NH-C 1~6 Alkyl-C 6~10 It is an aryl, biotin, sugar moiety, (poly)alkylene glycol, heterocyclyl, phosphate, or sulfate; R 1a , R 1b , R 1c , R 1d and R 1e Each of them is either hydrogen or C 1~4 Independently selected from alkyl groups (e.g., methyl, ethyl, propyl, butyl); Any alkyl, formyl, acyl, fatty acyl, benzyl, benzoyl, heteroaryl, or trifluoroacetyl, -NHC 1~18 Alkyl, -NHC 6~16 aryl, -NH-C 1~6 Alkyl-C 6~10 Aryl or (poly)alkylene glycols contain halogens, C 1~6 Alkyl, C 1~6 It may be substituted with one or more groups selected from haloalkyl groups, sugar moieties, phosphates, or sulfates; L 1 It does not exist, or * -(C=O)C 1~16 Alkylene-NH-(in the formula, * Y 1 , represents a connection point to Y or Z); (C 1~20 ) Alkilen, (C 2~20 ) Alkenylene, (Poly)alkylene glycol; L 1 This may be substituted with one or more groups selected from oxo (=O), halogen, =N, and =S; Y 1 It is either absent or a peptide containing one or two amino acids; Y is either absent or a peptide containing 1 to 16 amino acids; Y may contain a (poly)alkylene glycol linker in its peptide sequence; Y 2 It is either absent or a peptide containing one or two amino acids; Z is expressed by the formula: F # -X 2 -X 3 -W # -X 5 It is a peptide, During the ceremony, X 2 is, S # , Y # , K # , N # , or H # Selected from; X 3 is, S # , A # , P # , V # , or T # Selected from; X 5 G # , A # Selected from; During the ceremony, `` # " indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs; R 2 NH2, NR 2a H, NR 2a R 2b , OH or OR 2a And; in the formula, R 2a and R 2b Each of them, if present, independently, C 1~6 Alkyl (e.g., methyl, ethyl, propyl, butyl, pentyl, or hexyl), C 3~6 Alkenil, C 6~16 Ariel, C 6~16 Aryl-C 1~6 Alkyl, C 1~6 Alkylene-C 6~16 Aryl, or C 1~6 These are haloalkyls, and each of them is a halogen, C 1~6 Alkyl, or C 1~6 It may be substituted with one or more groups selected from haloalkyl groups.

[0011] In certain embodiments, Y 1 and Y 2 are both absent.

[0012] In another aspect, the present invention provides an insecticidal compound having the following formula (I), R 1 -L 1 -Y-Z-R 2 (I) wherein, R 1 is hydrogen (which may be represented as "H-" or "Hy-"), C 1~4 alkyl (e.g., methyl, ethyl, propyl, butyl), formyl, -N(R 1a )-C(=N + (R 1b )(R 1c ))NR 1d R 1e 、-C(=N + (R 1b )(R 1c ))NR 1d R 1e 、acyl, fatty acyl, benzyl, benzoyl, heteroaryl or trifluoroacetyl, -NHC 1~18 alkyl, -NHC 6~16 aryl, -NH-C 1~6 alkyl-C 6~10 aryl, biotin, a sugar moiety or (poly)alkylene glycol, phosphate or sulfate; R 1a 、R 1b 、R 1c 、R 1d and R 1e each is independently selected from hydrogen or C 1~4 alkyl (e.g., methyl, ethyl, propyl, butyl); Any alkyl, formyl, acyl, fatty acyl, benzyl, benzoyl, heteroaryl or trifluoroacetyl, -NHC 1~18 alkyl, -NHC 6~16 aryl, -NH-C 1~6 alkyl-C 6~10Aryl or (poly)alkylene glycols contain halogens, C 1~6 Alkyl, C 1~6 It may be substituted with one or more groups selected from haloalkyl groups, sugar moieties, phosphates, or sulfates; L 1 It does not exist, or * -(C=O)C 1~16 Alkylene-NH-(in the formula, * (This represents a connection point to Y or Z). (C 1~20 ) Alkilen, (C 2~20 ) Alkenylene, (Poly)alkylene glycol; L 1 This may be substituted with one or more groups selected from oxo (=O), halogen, =N, and =S; Y is either absent or a peptide containing 1 to 16 amino acids; Y may contain a (poly)alkylene glycol linker in its peptide sequence; Z is expressed by the formula: F # -X 2 -X 3 -W # -X 5 It is a peptide, During the ceremony, X 2 is, S # , Y # , K # , N # , or H # Selected from; X 3 is, S # , A # , P # , V # , or T # Selected from; X 5 G # , A # Selected from; During the ceremony, `` #" indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs; R 2 NH2, NR 2a H, NR 2a R 2b , OH or OR 2a And; in the formula, R 2a and R 2b Each of them, if present, independently, C 1~6 Alkyl (e.g., methyl, ethyl, propyl, butyl, pentyl, or hexyl), C 3~6 Alkenil, C 6~16 Ariel, C 6~16 Aryl-C 1~6 Alkyl, C 1~6 Alkylene-C 6~16 Aryl, or C 1~6 These are haloalkyls, and each of them is a halogen, C 1~6 Alkyl, or C 1~6 It may be substituted with one or more groups selected from haloalkyl groups.

[0013] Preferably, R 1 C is hydrogen (which can be represented as "H-" or "Hy-"), C 1~4 Alkyl (e.g., methyl, ethyl, propyl, butyl), formyl, -N(R 1a )-C(=N + (R 1b )(R 1c ))NR 1d R 1e , -C(=N + (R 1b )(R 1c ))NR 1d R 1e Acyl, fatty acyl, benzyl, benzoyl, heteroaryl or trifluoroacetyl, -NHC 1~18 Alkyl, -NHC 6~16 aryl, -NH-C 1~6 Alkyl-C 6~10 It is an aryl, biotin, sugar moiety, or (poly)alkylene glycol; R 1a , R 1b , R1c , R 1d and R 1e Each of them is either hydrogen or C 1~4 Independently selected from alkyl groups (e.g., methyl, ethyl, propyl, butyl); Any alkyl, formyl, acyl, fatty acyl, benzyl, benzoyl, heteroaryl, or trifluoroacetyl, -NHC 1~18 Alkyl, -NHC 6~16 aryl, -NH-C 1~6 Alkyl-C 6~10 Aryl or (poly)alkylene glycols contain halogens, C 1~6 Alkyl, C 1~6 It may be substituted with one or more groups selected from the haloalkyl or sugar moieties.

[0014] Preferably, X 2 is, S # , Y # , N # or H # Selected from.

[0015] Preferably, R 2 NH2, NR 2a H, NR 2a R 2b OR 2a And; in the formula, R 2a and R 2b Each of them, if present, independently, C 1~6 Alkyl (e.g., methyl, ethyl, propyl, butyl, pentyl, or hexyl), C 3~6 Alkenil, C 6~16 Ariel, C 6~16 Aryl-C 1~6 Alkyl, C 1~6 Alkylene-C 6~16 Aryl, or C 1~6 These are haloalkyls, and each of them is a halogen, C 1~6 Alkyl, or C 1~6 It may be substituted with one or more groups selected from haloalkyl groups.

[0016] In another embodiment, the present invention provides an insecticidal compound having the following formula (I): R 1 -L 1 -YZR 2 (I) During the ceremony, R 1 C is hydrogen (which can be represented as "H-" or "Hy-"), C 1~4 Alkyl (e.g., methyl, ethyl, propyl, butyl), formyl, -N(R 1a )-C(=N + (R 1b )(R 1c ))NR 1d R 1e , -C(=N + (R 1b )(R 1c ))NR 1d R 1e Acyl, fatty acyl, benzyl, benzoyl, heteroaryl or trifluoroacetyl, -NHC 1~18 Alkyl, -NHC 6~16 aryl, -NH-C 1~6 Alkyl-C 6~10 It is an aryl, biotin, sugar moiety, or (poly)alkylene glycol; R 1a , R 1b , R 1c , R 1d and R 1e Each of them is either hydrogen or C 1~4 Independently selected from alkyl groups (e.g., methyl, ethyl, propyl, butyl); Any alkyl, formyl, acyl, fatty acyl, benzyl, benzoyl, heteroaryl, or trifluoroacetyl, -NHC 1~18 Alkyl, -NHC 6~16 aryl, -NH-C 1~6 Alkyl-C 6~10 Aryl or (poly)alkylene glycols contain halogens, C 1~6 Alkyl, C 1~6 It may be substituted with one or more groups selected from the haloalkyl or sugar moieties; L 1 It does not exist, or * -(C=O)C 1~16 Alkylene-NH-(in the formula, * (This represents a connection point to Y or Z). (C 1~20 ) Alkilen, (C 2~20 ) Alkenylene, (Poly)alkylene glycol; L 1 This may be substituted with one or more groups selected from oxo (=O), halogen, =N, and =S; Y is either absent or a peptide containing 1 to 16 amino acids; Y may contain a (poly)alkylene glycol linker in its peptide sequence; Z is expressed by the formula: F # -X 2 -X 3 -W # -X 5 It is a peptide, During the ceremony, X 2 is, S # , Y # , N # or H # Selected from; X 3 is, S # , A # , P # , V # , or T # Selected from; X 5 G # , A # Selected from; During the ceremony, `` # " indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs; R 2 NH2, NR 2a H, NR 2a R 2b , or OR 2a And; in the formula, R 2a and R 2b Each of them, if present, independently, C1~6 Alkyl (e.g., methyl, ethyl, propyl, butyl, pentyl, or hexyl), C 3~6 Alkenil, C 6~16 Ariel, C 6~16 Aryl-C 1~6 Alkyl, C 1~6 Alkylene-C 6~16 Aryl, or C 1~6 These are haloalkyls, and each of them is a halogen, C 1~6 Alkyl, or C 1~6 It may be substituted with one or more groups selected from haloalkyl groups.

[0017] Preferably, Z is, Formula Z a It is a peptide produced by Z a The formula is: -F # -H # -S # -W # -G # (Sequence ID 1) It is a peptide of; During the ceremony, `` # The symbol " indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs.

[0018] Preferably, Z is given by formula Z b It is a peptide produced by Z b The formula is: -F # -X 2b -X 3b -W # -X 5b It is a peptide, During the ceremony, X 2b is the amino acid residue S # , Y # , K # , N # or H # Selected from; X 3b is the amino acid residue S # , A # , P # , V # or T# Selected from; X 5b is amino acid residue A # Or G # Selected from; During the ceremony, `` # The symbol " indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs.

[0019] Preferably, Z is given by formula Z b If it is a peptide by X 3b is the amino acid residue S # Or A # Selected from, in the formula, # The symbol " indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs.

[0020] Preferably, Z is given by formula Z c It is a peptide produced by Z c The formula is: -F # -S # -X 3c -W # -G # (Sequence 2) It is a peptide, In the formula, X 3c is amino acid residue A # , P # , V # or T # Selected from; During the ceremony, `` # The symbol " indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs.

[0021] Preferably, Y is absent or a peptide containing 1 to 14 amino acids. Preferably, Y is absent or a peptide containing 1 to 12 amino acids.

[0022] Preferably, compounds of formula (I) (e.g., formulas (Ia), (Ib), and (Ic)) have been found to have specific uses as insecticides against Diptera, Hemiptera, Blattodea, and / or Lepidoptera insects.

[0023] Preferably, compounds of formula (I) (e.g., formulas (Ia), (Ib), and (Ic)) have been found to have specific uses as insecticides against Diptera, Hemiptera, or Lepidoptera insects.

[0024] Preferably, compounds of formula (I) (e.g., formulas (Ia), (Ib), and (Ic)) have been found to have specific uses as insecticides against Diptera insects (e.g., Drosophila species).

[0025] Preferably, compounds of formula (I) (e.g., formulas (Ia), (Ib), and (Ic)) have been found to have specific uses as insecticides against Drosophila species.

[0026] Preferably, compounds of formula (I) (e.g., formulas (Ia), (Ib), and (Ic)) have been found to have specific uses as insecticides against hemipteran insects (e.g., Halyomorpha halys or Myzus persicae).

[0027] Preferably, compounds of formula (I) (e.g., formulas (Ia), (Ib), and (Ic)) have been found to have specific use as insecticides against the species Hariomorpa haris.

[0028] Preferably, compounds of formula (I) (e.g., formulas (Ia), (Ib), and (Ic)) have been found to have specific use as insecticides against the species *Mizus persicae*.

[0029] Preferably, compounds of formula (I) (e.g., formulas (Ia), (Ib), and (Ic)) have been found to have specific uses as insecticides against insects of the order Lepidoptera (e.g., Plutella xylostella or Spodeptera frugiperda).

[0030] Preferably, compounds of formula (I) (e.g., formulas (Ia), (Ib), and (Ic)) have been found to have specific use as insecticides against Plutella xirostera species.

[0031] Preferably, compounds of formula (I) (e.g., formulas (Ia), (Ib), and (Ic)) have been found to have specific use as insecticides against the species Spodoptera fulgiperda.

[0032] Preferably, compounds of formula (I) (e.g., formulas (Ia), (Ib), and (Ic)) have been found to have specific use as insecticides against insects of the order Blattodea (e.g., the German cockroach (Blattella germanica)).

[0033] Preferably, compounds of formula (I) (e.g., formulas (Ia), (Ib), and (Ic)) have been found to have specific use as insecticides against the German cockroach species.

[0034] Preferably, the compound of formula (XX) is found to have a specific use for any of the species considered above.

[0035] Therefore, compounds of formula (I) (e.g., formulas (Ia), (Ib), and (Ic)) can be applied to any of the methods or uses described herein.

[0036] Therefore, compounds of formulas (XX) and (I) (e.g., formulas (Ia), (Ib), and (Ic)) can be applied to any of the methods or uses described herein.

[0037] Preferably, compounds of formulas (XX) and (I) (e.g., formulas (Ia), (Ib), and (Ic)) are, for example, Y 1 , Y 2 and / or the Z group comprises at least one modified amino acid or non-natural amino acid analog. The at least one modified amino acid or non-natural amino acid analog may be as defined elsewhere in this specification.

[0038] " # The label indicates that the residue in question may be a modified version of the amino acid, or that the residue may be replaced by a non-natural amino acid analog. For example, S # This indicates that the residue may be serine, modified serine (e.g., D-serine, beta-serine), or a non-natural amino acid (e.g., [Aib]).

[0039] In another embodiment, a composition is provided comprising a compound as defined herein or a salt thereof, mixed with one or more solvents, carriers, diluents, adjuvants, preservatives, dispersants, emulsifiers, or synergists. Preferably, the composition is an agricultural composition, and the composition is an insect control composition or a plant protection composition.

[0040] In another embodiment, the use of the compounds defined herein, or salts or solvates thereof, or compositions defined herein, as insect control agents is provided. The use may be as an insecticide against insects encoding kinin peptides. The use may be as an insecticide against Hemiptera, Diptera, Blattodea and / or Lepidoptera insects, preferably Hemiptera, Diptera and / or Lepidoptera insects.

[0041] In another embodiment, a method for killing insects is provided, comprising the step of contacting an insect population with a compound or salt thereof as defined herein or a composition as defined herein. Preferably, the insects are insects encoding kinin peptides, such as Hemiptera, Diptera, Blattodea and / or Lepidoptera, and more preferably Hemiptera, Diptera and / or Lepidoptera.

[0042] In another embodiment, a method is provided for increasing the mortality rate of hemipteran, dipteran and / or lepidopteran insects, comprising the step of contacting hemipteran, dipteran and / or lepidopteran insects or populations of hemipteran, dipteran and / or lepidopteran insects with a compound or salt thereof as defined herein, or a composition as defined herein.

[0043] In another embodiment, a method is provided for increasing the mortality rate of cockroach insects, comprising the step of contacting a cockroach insect or a population of cockroach insects with a compound or salt thereof as defined herein, or a composition as defined herein.

[0044] In another embodiment, the use of a compound or salt thereof as defined herein, or a composition as defined herein, is provided as a plant protectant for protecting plants from insects encoding kinin peptides.

[0045] In another embodiment, the use of compounds or salts thereof, or compositions as defined herein, as plant protectants, for protecting plants from hemipteran, diptera, and / or lepidopteran insects is provided.

[0046] In another embodiment, the use of compounds or salts thereof as defined herein, or compositions as defined herein, as plant protectants, for protecting plants from cockroach insects is provided.

[0047] In another embodiment, a method is provided for inhibiting plant parasitism by insects encoding kinin peptides, comprising the step of contacting the plant with a compound or salt thereof as defined herein, or a composition as defined herein. Preferably, the compound or composition is applied to the plant while the plant is free from or substantially free from insects encoding kinin peptides.

[0048] In another embodiment, a method is provided for inhibiting plant parasitism by hemipteran, dipteran, and / or lepidopteran insects, comprising the step of contacting the plant with a compound or salt thereof as defined herein, or a composition as defined herein. Preferably, the compound or composition is applied to the plant while the plant is free from, or substantially free from, hemipteran, dipteran, and / or lepidopteran insects.

[0049] In another embodiment, a method is provided for inhibiting plant parasitism by cockroach insects, comprising the step of contacting the plant with a compound or salt thereof as defined herein, or a composition as defined herein. Preferably, the compound or composition is applied to the plant while the plant is free or substantially free of cockroach insects.

[0050] In another embodiment, a method is provided for reducing plant parasitism by insects encoding kinin peptides or for reducing the load of insects encoding kinin peptides on plants, the method comprising the step of contacting the plants with a compound or salt thereof as defined herein, or a composition as defined herein.

[0051] In another embodiment, a method is provided for reducing parasitism of plants by hemipteran, dipteran and / or lepidopteran insects, or for reducing the load of hemipteran, dipteran and / or lepidopteran insects on plants, the method comprising the step of contacting the plants with a compound or salt thereof as defined herein, or a composition as defined herein.

[0052] In another embodiment, a method is provided for reducing or decreasing the infestation of cockroach insects on plants, comprising the step of contacting the plants with a compound or salt thereof as defined herein, or a composition as defined herein.

[0053] Suitable insects that encode kinin peptides include insects of the orders Hemiptera, Diptera, and / or Lepidoptera. Other insects that can encode kinin peptides are those of the order Blattodea.

[0054] In another embodiment, the use of the compounds or compositions defined herein as insecticides or as plant protectants for protecting plants or parts thereof from insects is provided.

[0055] In another embodiment, a) Diptera insects, preferably selected from Drosophila melanogaster or Drosophila suzukii; b) Hemiptera insects, for example aphids, preferably selected from Aphis fabae, Acyrthosiphon pisum, Amrasca biguttula, Rhopalosiphum padi or Rhopalosiphum padi; and / or c) Lepidopteran insects, preferably selected from Plutella xirostera or Spodoptera fulgiperda; and / or d) Cockroach insects (e.g., German cockroach) The use of the compounds or compositions defined herein for this purpose is provided.

[0056] In another embodiment, a method for increasing insect mortality is provided, comprising the step of contacting an insect or a population of insects with a compound or composition as defined herein.

[0057] In another embodiment, a method is provided for inhibiting or preventing insect infestation of plants, comprising the step of bringing a plant or a part thereof, or a site where a plant is growing or intended to grow, into contact with a compound or composition as defined herein. Preferably, the compound or composition is brought into contact with the plant or a part thereof, or a site where a plant is growing or intended to grow, in a state where the plant or a part thereof is free of insects, or substantially free of insects.

[0058] In another embodiment, a method is provided for reducing or treating insect infestation on plants or reducing the insect load on plants, comprising the step of bringing a plant or a part thereof, or the land on which the plant is growing, into contact with a compound or composition as defined herein.

[0059] Preferably, the land where plants are growing or are intended to grow may include agricultural land suitable for growing plants, and preferably, such land includes fields.

[0060] Preferably, insects are a) Diptera insects, preferably selected from Drosophila melanogaster or Drosophila japonica; b) Hemiptera insects, for example aphids, preferably selected from Aphis fabae, Acyrthsiphon pisum, Misus persicae, or pea aphids; c) Lepidopteran insects, preferably selected from Plutella xirostera or Spodoptera fulgiperda; and / or d) A cockroach insect, preferably a German cockroach.

[0061] Preferably, contacting insects or insect colonies, plants or parts thereof, or land includes watering, feeding, spraying, atomizing, foaming, fogging, culturing in hydroculture, culturing in hydroponics, coating, immersion, injection and / or covering insects or insect colonies, plants or parts thereof, or land with the compositions defined herein. Contacting may include injecting plants (e.g., trees) or parts thereof with the compositions defined herein using systems and methods such as those described in WO2020 / 021041, WO2023 / 161802, WO2022 / 264053, WO2022 / 189386, WO2022 / 165248, WO2021 / 152093, WO2020 / 212612 and WO2020 / 021041, the entire contents of which are incorporated by reference.

[0062] Preferably, insects or insect colonies, plants or parts thereof, or land are treated with an effective concentration, preferably 10 -3 ~10 -9 Contact with the compound defined herein at concentration M.

[0063] In another embodiment, a method for producing an insecticidal compound according to the first embodiment, (a) A step of chemically synthesizing an insecticidal compound of formula (I) or (XX), or a precursor thereof. A method including this is provided.

[0064] In one embodiment, the chemical synthesis includes the method described in the example.

[0065] Further features of aspects and embodiments of the present invention are defined under the following headings. Any feature in any section can be combined with any aspect of the embodiments in any viable combination. [Modes for carrying out the invention]

[0066] definition Throughout this specification and the claims, the conventional three-letter and one-letter codes for naturally occurring amino acids, namely A (Ala), G (Gly), L (Leu), I (Ile), V (Val), F (Phe), W (Trp), S (Ser), T (Thr), Y (Tyr), N (Asn), Q (Gln), D (Asp), E (Glu), K (Lys), R (Arg), H (His), M (Met), C (Cys), and P (Pro), are used.

[0067] In general, in this specification, when a single-letter code is accompanied by the symbol "#", it indicates that it may be in its naturally occurring form, a modified form, or can be replaced by a non-proteinogenic amino acid. For example, "A # " indicates that it includes unmodified alanine, modified alanine (e.g., N-methylalanine), or that the alanine residue may be substituted with another unnatural amino acid analog (e.g., α-aminoisobutyric acid (Aib)). Preferably, F # -H # -S # -W # -G # In the motif (SEQ ID NO: 1), the residues may be in their naturally occurring form or in a modified form.

[0068] Preferably, F # -H # -S # -W # -G # In the (SEQ ID NO: 1) motif, a single residue may be substituted with a non-proteinogenic amino acid, such as FH[Aib]WG (SEQ ID NO: 3), in which serine is substituted with α-aminoisobutyric acid (Aib).

[0069] Preferably, F # -H # -S # -W # -G #In the motif (SEQ ID NO: 1), a single residue may be substituted with a D-amino acid or an N-methylated amino acid, for example, FHsWG (SEQ ID NO: 4) in which serine is substituted with D-serine, or FH[n-me-S]WG (SEQ ID NO: 5) in which serine is substituted with N-methylserine.

[0070] As used herein, “amino acids” may refer to naturally occurring amino acids, or any other amino acids, including synthetic amino acids and non-proteinogenic amino acids. In this context, “naturally occurring” means the 20 amino acids encoded by the standard genetic code, which are sometimes called proteinogenic amino acids.

[0071] The term amino acid is an abbreviation for α-amino[alpha-amino]carboxylic acid. Each molecule contains a central carbon (C) atom called the α-carbon, to which both an amino group and a carboxyl group are bonded. The remaining two bonds of the α-carbon atom are generally to a hydrogen (H) atom and the following R: [ka] It is filled with side chains, which are shown as follows.

[0072] In the present invention, the modified amino acid has an α hydrogen atom that is C 1~6 The α-alkylated amino acid may be an α-methylated amino acid, for example, an α-methyl-L-serine ([α-Me)S]. Preferably, the α-alkylated amino acid is an α-methylated amino acid, for example, given the notation α-methyl-L-serine ([α-Me)S): [ka] That is the case.

[0073] Commonly accepted three-letter codes and other abbreviations for other amino acids, such as hydroxyproline (Hyp: L-hydroxyproline or (2S,4R)-4-hydroxyproline), octahydroindole-2-carboxylic acid (Oic), sarcosine (Sar), norleucine (Nle), alpha-aminoisobutyric acid (Aib), and thiazolidinedione-4-carboxylic acid (Thz), may also be used.

[0074] The term "Thz" refers to an amino acid residue that is a thiazolidined-4-carboxylic acid residue, for example, (R)-thiazolidined-4-carboxylic acid: [ka] This indicates that it has been replaced with [something].

[0075] The notation "Ahx" indicates 6-aminohexanoic acid (also known as 6-aminocaproic acid or ε-aminocaproic acid). "Ado" indicates 12-aminododecanoic acid.

[0076] The notation "Ava" refers to the 5-aminovaleric acid portion, that is, [ka] This indicates.

[0077] The notation "n-me" preceding an amino acid code is used to indicate an N-methylated amino acid residue. Therefore, for example, "[n-me-V]" indicates N-methylvaline, "[n-me-A]" indicates N-methylalanine, and "[n-me-L]" indicates N-methylleucine.

[0078] Other such amino acids may be indicated in square brackets "[ ]" (e.g., "[Aib]") when used in a general formula or sequence herein, especially when the remainder of the formula or sequence is indicated using a single-letter code.

[0079] Unless otherwise specified, the amino acid residues in the peptides of this invention are in the L-configuration. However, D-configured amino acids can be incorporated as modifications. In this context, lowercase amino acid codes can be used to represent the D-configuration of the amino acid; for example, [a] represents the D-configuration of alanine.

[0080] Beta-amino acid residues can also be used in the compounds of the present invention. Such residues can be indicated by the symbol "β" followed by the conventional code for the corresponding alpha-amino acid. Thus, [βhL] (or [B3L]) represents a residue of beta-homoleucine (3-amino-5-methylcaproic acid), [βA] represents a residue of beta-alanine (3-aminopropanoic acid), [βhA] (or [B3A]) represents a residue of beta-homolananine, [βhV] represents a residue of beta-homovaline, sometimes called beta-leucine (3-amino-4-methylpentanoic acid), [βhF] (or [B3F]) represents a residue of beta-homophenylalanine, and [βhP] (or [B3P]) represents a residue of beta-homoproline.

[0081] An amino acid "peptoid analog" is an analog in which the side chain is bonded to a nitrogen in the peptide backbone instead of the α-carbon found in proteinogenic peptides. Such residues can be indicated by the notation "peptoid" followed by the conventional code for the corresponding α-amino acid. An example of a peptoid is the peptoid of phenylalanine: [ka] These are some examples. The above residue may also have the notation [peptoid-F], indicating the peptoid of phenylalanine.

[0082] "Biotin-modified" amino acid analogs are amino acid residues that incorporate a biotin moiety as part of their side chain. For example, the notation "[biotin-K]" indicates that the biotin moiety is: [ka] This shows lysine residues modified by side chains to include [specific component].

[0083] Alternatively, or furthermore, the biotin portion may be located at the terminal position. Therefore, R 1 It may be biotin. The notation [biotin]- represents the terminal biotin portion; for example, the subsequence [biotin]-S is given by formula: [ka] It has.

[0084] The modified amino acid precursors used to prepare the peptides disclosed herein can be commercially available or synthesized by methods known in the art.

[0085] C x~xx This notation refers to the number of carbon atoms in a functional group. The number in the "x" position represents the minimum number of carbon atoms, and the number in the "xx" position represents the maximum number of carbon atoms. For example, C 1~6 Alkyl refers to an alkyl group as defined herein, having 1 to 6 carbon atoms.

[0086] The notations i, n, or t are used herein in the usual manner for various alkyl groups. Specifically, the suffixes refer to the arrangement of atoms and represent linear ("n") or branched ("i" or "t") alkyl groups.

[0087] As used herein, the term "alkyl" refers to a saturated linear or branched monovalent hydrocarbon group, and alkyl groups may be substituted. The number of carbon atoms in an alkyl group can be specified using the notation above, for example, if there are 1 to 8 carbon atoms, then "C 1~8The term "-alkyl" can be used. Examples of alkyl groups include methyl (Me, -CH3), ethyl (Et, -CH2CH3), 1-propyl (n-Pr, n-propyl, -CH2CH2CH3), 2-propyl (i-Pr, i-propyl, -CH(CH3)2), and 1-butyl (n-Bu, n-butyl, -CH2CH2CH2CH3).

[0088] An alkylene, alkenylene, or alkynylene group is an alkyl, alkenyl, or alkynyl group that is located between two other chemical groups and functions to link them together. 1~6 "Alkylene" refers to a straight-chain saturated divalent hydrocarbon group with 1 to 6 carbon atoms or a branched-chain saturated divalent hydrocarbon group with 3 to 6 carbon atoms. Examples of alkylene groups include methylene (-CH2-), 1,1-ethylene (-CH(CH3)-), 1,2-ethylene (-CH2CH2-), 1,1-propylene (-CH(CH2CH3)-), and 2,2-propylene (-C(CH3)2-).

[0089] As used herein, the term “alkenyl” refers to a monovalent hydrocarbon group, either linear or branched, having at least one unsaturated site, i.e., a carbon-carbon double bond. Alkenyl groups may be substituted and include groups having “cis” and “trans” orientations, or “E” and “Z” orientations. The number of carbon atoms in an alkenyl group can be specified using the above notation; for example, if there are 2 to 8 carbon atoms, “C 2~8 The term "alkenyl" can be used. Examples of alkenyl groups include, but are not limited to, ethenyl (-CH=CH2) and propa-1-enyl (-CH=CHCH3).

[0090] In the chemical structure described herein, [ka] or [ka] This represents a bonding point or group, for example, a group described in relation to various functional groups.

[0091] The term "aryl" refers to a cyclic or polycyclic aromatic ring having 5 to 12 carbon atoms. The term aryl includes both monovalent and divalent species. Aryls include groups with monocyclic rings and groups with more than one ring, such as fused rings or spiro rings. In the case of groups with more than one ring, at least one of the rings is aromatic. The number of carbon atoms in an aryl group can be specified using the notation above; for example, if there are 6 to 16 carbon atoms, it is written as "C 6~16 The term "aryl" can be used. The aryl group may be substituted. Examples of aryl groups include phenyl, naphthyl, biphenyl, phenantrenyl, naphthacenyl, 1,2,3,4-tetrahydronaphthalenyl, 1H-indenyl, 2,3-dihydro-1H-indenyl, and fluorenyl. The preferred aryl group is fluorenyl.

[0092] The terms “heteroaryl” or “heteroaromatic” refer to aromatic monocyclic, bicyclic, or polycyclic rings that incorporate one or more heteroatoms (e.g., 1 to 4, particularly 1, 2, or 3) selected from nitrogen, oxygen, or sulfur. The term heteroaryl includes both monovalent and divalent species. Examples of heteroaryl groups are monocyclic and bicyclic groups containing 5 to 12 ring members, more commonly 5 to 10 ring members. Heteroaryl groups may be, for example, 5- or 6-membered monocyclic rings or 9- or 10-membered bicyclic rings, for example, bicyclic structures formed from fused 5- and 6-membered rings or two fused 6-membered rings. Each ring can typically contain up to about 4 heteroatoms selected from nitrogen, sulfur, and oxygen. Typically, heteroaryl rings contain up to 3 heteroatoms, more commonly up to 2, for example, 1 heteroatom. In one embodiment, the heteroaryl ring contains at least one ring nitrogen atom. The nitrogen atoms in the heteroaryl ring may be basic, as in the case of imidazole or pyridine, or they may be essentially non-basic, as in the case of indole or pyrrole nitrogen. Generally, the number of basic nitrogen atoms present in a heteroaryl group containing any amino group substituent of the ring is less than five.

[0093] Examples of heteroaryls include furyl, pyrrolyl, thienyl, oxazolyl, isoxazolyl, imidazolyl, pyrazolyl, thiazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, triazolyl, tetrazolyl, pyridyl, pyridadinyl, pyrimidinyl, pyrazinyl, 1,3,5-triazeninyl, benzofuranyl, indolyl, isoindolyl, benzothienyl, benzoxazolyl, benzimidazolyl, benzothiazolyl, benzothiazolyl, indazolyl, prinyl, benzoflazanil, quinolyl, isoxyl Examples include noryl, quinazolinil, quinoxalinil, synnorinil, pteridinil, naphthilidinil, carbazolyl, phenadinil, benzisoquinolinil, pyridopyradinil, thieno[2,3-b]furanil, 2H-flo[3,2-b]-pyranil, 5H-pyrido[2,3-d]-o-oxazinil, 1H-pyrazo[4,3-d]-oxazolyl, 4H-imidazo[4,5-d]thiazolyl, pyrazino[2,3-d]pyridazinil, imidazo[2,1-b]thiazolyl, and imidazo[1,2-b][1,2,4]triazinil. "Heteroaryl" also includes partially aromatic bicyclic or polycyclic ring systems in which at least one ring is an aromatic ring and one or more of the other rings are non-aromatic saturated or partially saturated rings, but at least one ring contains one or more heteroatoms selected from nitrogen, oxygen, or sulfur. Examples of partially aromatic heteroaryl groups include, for example, tetrahydroisoquinolinyl, tetrahydroquinolinyl, 2-oxo-1,2,3,4-tetrahydroquinolinyl, dihydrobenzthienyl, dihydrobenzofuranyl, 2,3-dihydro-benzo[1,4]dioxynyl, benzo[1,3]dioxolyl, 2,2-dioxo-1,3-dihydro-2-benzothienyl, 4,5,6,7-tetrahydrobenzofuranyl, indlinyl, 1,2,3,4-tetrahydro-1,8-naphthilidinyl, 1,2,3,4-tetrahydropyrido[2,3-b]pyradinyl, and 3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazinyl. Particularly preferred heteroaryls are indolyl, which may be denoted as "[Ind]".

[0094] Examples of five-membered heteroaryl groups include, but are not limited to, pyrrolyl, furanyl, thienyl, imidazolyl, furazanyl, oxazolyl, oxadiazolyl, oxatriazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, triazolyl, and tetrazolyl groups.

[0095] Examples of six-membered heteroaryl groups include, but are not limited to, pyridyl, pyrazinyl, pyridadinyl, pyrimidinyl, and triazinyl.

[0096] Bicyclic heteroaryl groups are, for example, A benzene ring fused to a five-membered or six-membered ring containing one, two, or three ring heteroatoms; A pyridine ring condensed into a five-membered or six-membered ring containing one, two, or three ring heteroatoms; A pyrimidine ring condensed into a five-membered or six-membered ring containing one or two ring heteroatoms; A pyrrole ring fused to a five-membered or six-membered ring containing one, two, or three ring heteroatoms; A pyrazole ring fused to a five-membered or six-membered ring containing one or two ring heteroatoms; A pyrazine ring fused to a five-membered or six-membered ring containing one or two ring heteroatoms; An imidazole ring fused to a five-membered or six-membered ring containing one or two ring heteroatoms; An oxazole ring fused to a five-membered or six-membered ring containing one or two ring heteroatoms; An isoxazole ring fused to a five-membered or six-membered ring containing one or two ring heteroatoms; A thiazole ring fused to a five-membered or six-membered ring containing one or two ring heteroatoms; An isothiazole ring fused to a five-membered or six-membered ring containing one or two ring heteroatoms; A thiophene ring fused to a five-membered or six-membered ring containing one, two, or three ring heteroatoms; A furan ring fused to a five-membered or six-membered ring containing one, two, or three ring heteroatoms; A cyclohexyl ring fused to a 5-membered or 6-membered aromatic heterocycle containing 1, 2, or 3 ring heteroatoms; and The group may be selected from a cyclopentyl ring fused to a 5-membered or 6-membered heteroaromatic ring containing 1, 2, or 3 ring heteroatoms.

[0097] Specific examples of bicyclic heteroaryl groups containing a six-membered ring fused to a five-membered ring include, but are not limited to, benzofuranyl, benzothiophenyl, benzimidazolyl, benzoxazolyl, benzoisoxazolyl, benzothiazolyl, benzoisothiazolyl, isobenzofuranyl, indolyl, isoindolyl, indollidinyl, indolinyl, isoindolinyl, prinyl (e.g., adeninyl, guaninyl), indazolyl, benzodioxolyl, and pyrazolopyridinyl groups. A preferred bicyclic heteroaryl group is indolyl.

[0098] Specific examples of bicyclic heteroaryl groups containing two fused six-membered rings include, but are not limited to, quinolinyl, isoquinolinyl, chromanyl, thiochromanyl, clomenyl, isochromanyl, chromanyl, isochromanyl, benzodioxanyl, quinolidinyl, benzooxazinyl, benzodiadinyl, pyridopyridinyl, quinoxalinyl, quinazolinyl, cinnolinyl, phthalazinyl, naphthilidinyl, and pteridinyl groups.

[0099] As used herein, the term halogen refers to one or more of fluorine (F), chlorine (Cl), bromine (Br), or iodine (I). The terms "halo" or "halogeno" refer to fluoro, chloro, bromo, and iodine.

[0100] A "haloalkyl" refers to an alkyl group having one or more halogen substituents. The number of carbon atoms in a haloalkyl group can be specified using the notation described above; for example, if there are 1 to 8 carbon atoms, the term "C1-8-haloalkyl" can be used. An example of a haloalkyl group is trifluoromethyl (-CF3).

[0101] The term “including” is used in this description and claims and does not exclude any other elements or processes. When an indefinite or definite article, e.g., “a” or “an” or “the,” is used to refer to a singular noun, it includes the plural form of that noun unless something else is specifically stated.

[0102] As used herein, the term "about" refers to a measurable value such as a parameter, quantity, or time period, and means to include variations of and from a specified value of + / -10%, preferably + / -5%, more preferably + / -1%, and even more preferably + / -0.1%, insofar as such variations are appropriate for carrying out the disclosed invention. It should be understood that the value referred to by the modifier "about" is also preferably disclosed specifically.

[0103] As used herein, “plant” means the whole plant or a part thereof, including fresh fruits, vegetables, and seeds. A plant or plant part may be a living plant or a part thereof. Furthermore, as used herein, the term “plant” encompasses the whole plant, the ancestors and descendants of a plant, and plant parts including seeds, sprouts, stems, leaves, roots (including tubers), flowers, and tissues and organs, each of which contains the gene / nucleic acid of interest. The term “plant” also encompasses plant cells, suspension cultures, callus tissue, embryos, meristematic regions, gametophytes, sporophytes, pollen, and microspores, each of which contains the gene / nucleic acid of interest.

[0104] As used herein, “crops” means plant species or varieties grown to be harvested for food, animal feed, fuel, or any other economic purpose. In non-limiting examples, such crops include: corn, grains, e.g., wheat, rye, barley, and oats; sorghum, rice, sugar beets, and fodder beets; fruits, e.g., pears (e.g., apples and pears); citrus fruits (e.g., oranges, lemons, limes, grapefruit, or mandarins); drupes (e.g., peaches, nectarines, or plums); nuts (e.g., almonds or walnuts); soft fruits (e.g., cherries, strawberries, blackberries, or raspberries); plantage or grapes; legumes, e.g., beans, lentils, peas, and soybeans; oil crops, e.g., sunflowers, safflower, rapeseed, and canola. , castor or olive, melon, for example cucumber, melon or pumpkin, fiber plants, for example cotton, flax or hemp, fuel crops, for example sugarcane, pampas grass or switchgrass, vegetables, for example potato, tomato, pepper, lettuce, spinach, onion, carrot, eggplant, asparagus or cabbage, ornamental plants, for example flowers (for example petunias, pelargoniums, roses, tulips, lilies or chrysanthemums), shrubs, broad-leaved trees (for example poplar or willow) and evergreen trees (for example conifers), grasses, for example lawns, turf or pasture, or other useful plants, for example coffee, tea, tobacco, hops, pepper, rubber or latex plants.

[0105] As used herein, “pest” refers to an organism that is harmful to plants, animals, humans or matters of human interest, and includes, but is not limited to, crop pests such as insects (as defined later), household pests or insects such as cockroaches and ants, and pathogens such as malaria mosquitoes.

[0106] As used herein, "pest infection" or "pest disease" refers to any inflammatory condition, disease, or disorder in living organisms such as plants, animals, or humans that is caused by pests.

[0107] As used interchangeably herein, “active substance,” “active ingredient,” or “active ingredient” means any biological, biochemical, or chemical element, including microorganisms, and its derivatives, fragments, or compounds thereof, that have a general or specific effect on harmful organisms, including, if these ingredients arise naturally or by manufacture, any impurities that inevitably arise from the manufacturing process, in relation to a subject, in particular, plants, parts of plants, or pests of plant products.

[0108] As used herein, the terms “effective amount” and “effective dose” refer to the amount required to achieve the desired result.

[0109] As used herein, "insect" is used in a broad, general sense and includes all species of the Panarthropoda superphylum, including the phyla Arthropoda, Tardigrada, and Onychophora (Classification Systema Naturae, Brands, SJ (ed.) 1989-2005. Systema Naturae 2000. Amsterdam, The Netherlands [http: / / sn2000.taxonomy.nl / ]); and includes all different stages of the life cycle, such as eggs, larvae, nymphs, pupae, and adults, but not limited to these. Appropriate pests are defined elsewhere in this specification.

[0110] As used herein, “insecticide compound” refers to a compound that has biological activity against insects (as defined above), including but not limited to compounds capable of killing insects, larval anthelmintics, insect growth regulators, behavioral modifiers, attractants, repellents, pheromones, kairomones, allomones, and entomopathogenic fungi, viruses, and proteins. Insecticides preferably exert their biological activity through contact with insects, without the need for ingestion by insects. Insecticides include not only readily available compounds or compound formulations, but also inactive precursor forms that can be activated by external factors. In some cases, insecticides may be combined with other materials such as synergistic or mitigating agents, flavorings, or odor compositions. Preferably, the compound is contained within a carrier as defined above. “Contained within a carrier” as used herein means, but is not limited to, being bound or contained by means such as embedding, encapsulation, and adsorption.

[0111] Throughout this specification, including the following claims, unless otherwise required by context, the words “comprise” and “include,” as well as variations such as “comprises,” “comprising,” and “including,” mean to include the integer or process or group of integers or processes described, but not to exclude any other integer or process or group of integers or processes.

[0112] Where used herein and in the appended claims, the singular forms “a,” “an,” and “the” refer to multiple subjects unless the context clearly indicates otherwise. Ranges may be expressed herein as “about” one particular value to and / or “about” another particular value. Where such ranges are expressed, another embodiment includes one particular value to and / or another particular value. Similarly, where a value is expressed as an approximation by the use of the antecedent “about,” it is understood that a particular value forms another embodiment. The term “about” in relation to a number is arbitrary and means, for example, + / - 10%.

[0113] Further definition of the compound of the present invention The specific compounds of the present invention include, for example, compounds of formula (I) or (XX), and unless otherwise stated, R 1 , L 1 , Y, Y 1 , Y 2 , Z, R 2 Each of the and any associated substituents has either the meaning previously defined herein or the meaning defined in any of paragraphs (1) to (28) herein. (1)R 1 teeth, hydrogen -C(=N + Me2)NMe2, Asil, Fat acyl, benzyl, Benzoyl, Heteroaryl, Trifluoroacetyl, -NHC 1~18 Alkyl, -NHC 6~16 Ariel, -NH-C 1~6 Alkyl-C 6~10 Ariel; sugar part; Biotin; Selected from (poly)alkylene glycols (e.g., polyethylene glycols such as PEG-1 to PEG-16); R 1a , R 1b , R 1c , R 1d and R 1e Each of them is either hydrogen or C 1~4 Independently selected from alkyl groups (e.g., methyl, ethyl, propyl, butyl); Any alkyl, formyl, acyl, fatty acyl, benzyl, benzoyl, heteroaryl, or trifluoroacetyl, -NHC 1~18 Alkyl, -NHC 6~16 aryl, -NH-C 1~6 Alkyl-C 6~10 Aryl or (poly)alkylene glycols contain halogens, C 1~6 Alkyl, C 1~6 It may be substituted with one or more groups selected from the haloalkyl or sugar moieties; (2)R 1 teeth, hydrogen; Acyls that may be substituted with sugar moieties; Fat acyl; heteroaryl; -NHC 6~16 Ariel; sugar part; Biotin; or formula * -(OCH2CH2) n -R p (Poly)ethylene glycol (in the formula, * L 1 , Y 1 , represents a connection point to Y or Z, n is an integer from 1 to 16, and Rp is selected from -NH2OH or -OMe. (3)R 1 teeth, hydrogen; An acyl which may be substituted with a sugar moiety, wherein the acyl group is selected from formyl, acetyl (Ac), propanoyl, and butanoyl; Fatty acyls selected from palmitoyl, butyryl, cerotoyl, decanoyl, docosenoyl, dodecanoyl, eleostearoyl, heptanol, hexanoyl, eicosanoyl, eicosenoyl, lignoceroyl, linoleoyl, lipoyl, myristreoyl, nonanoyl, octadecanoyl, octanoyl, palmitoyl, stearoyl, undecanoyl, and valeryl; A heteroaryl selected from indolyl ([Ind]); -NHC 6~16 Ariel; Monosaccharide or disaccharide portion; Biotin; formula * -(OCH2CH2) n -R p (Poly)ethylene glycol (in the formula, * L 1 , Y 1 , represents a connection point to Y or Z, n is an integer from 4 to 12, and Rp is selected from -NH2OH or -OMe. (4)R 1 teeth, hydrogen; Acetyl that may be substituted with a monosaccharide or disaccharide moiety; Palmitoil; Indrill, formula * -(OCH2CH2) n -R p (Poly)ethylene glycol (in the formula, * is L 1 , Y 1 , represents a connection point to Y or Z, n is an integer from 6 to 10, and Rp is selected from -NH2 or -OH. (5)R 1 teeth, hydrogen; Acetyl; formula * -(OCH2CH2)8-NH2(PEG8) (poly)ethylene glycol (wherein the formula, * L 1 , Y 1 Selected from (representing a connection point to Y or Z). (6)R1 It is either hydrogen or acetyl. (7)L 1 It does not exist, or * -(C=O)C 1~10 -alkylene-NH-(in the formula, * This represents a connection point to Z. C 1~10 It is alkylene L 1 It may be substituted with one or more oxo (=O) groups. (8)L 1 It does not exist, or -(C=O)C 4~12 -alkylene-NH-(in the formula, * L 1 , Y 1 , represents a connection point to Y or Z); -(C=O)-C 1~4 It is an alkylene-(C=O)-. (9)L 1 It does not exist, or [ka] (In the formula, * L 1 , Y 1 , representing a connection point to Y or Z); or [ka] That is the case. (10)L 1 It does not exist, or [ka] That is the case. (11) In partial YZ and its subformulas, one or more modifications or non-natural amino acids, if present, independently iN-methylated amino acids; ii. Non-proteinogenic amino acids, such as hydroxyproline (Hyp:L-hydroxyproline or (2S,4R)-4-hydroxyproline), octahydroindole-2-carboxylic acid (Oic), sarcosine (Sar), norleucine (Nle), α-aminoisobutyric acid (Aib), or thiazolidinedione-4-carboxylic acid (Thz); iii. D-amino acids; iv. α-alkylated (e.g., α-methylated) amino acids; v. Beta-amino acids; vi. Peptoid amino acid analogs; vii. Sugar-modified amino acids; or viii. Selected from biotin-modified amino acids. (12) In partial YZ and its subformulas, one or more modifications or non-natural amino acids, if present, independently iN-methylated amino acids; ii. Non-proteinogenic amino acids, such as hydroxyproline (Hyp:L-hydroxyproline or (2S,4R)-4-hydroxyproline), octahydroindole-2-carboxylic acid (Oic), sarcosine (Sar), norleucine (Nle), α-aminoisobutyric acid (Aib), or thiazolidinedione-4-carboxylic acid (Thz); iii. α-methylated amino acids; iv. D-amino acids; or v. Selected from beta-amino acids. (13) In partial YZ and its subformulas, one or more modifications or non-natural amino acids, if present, independently iN-methylated amino acids; ii. Non-proteinogenic amino acids, such as hydroxyproline (Hyp:L-hydroxyproline or (2S,4R)-4-hydroxyproline), octahydroindole-2-carboxylic acid (Oic), sarcosine (Sar), norleucine (Nle), α-aminoisobutyric acid (Aib), or thiazolidinedione-4-carboxylic acid (Thz); iii. α-methylated amino acids; iv. Selected from D-amino acids. (14) In partial YZ and its subformulas, one or more modifications or non-natural amino acids, if present, independently iN-methylated amino acids; ii. α-aminoisobutyric acid (Aib); iii. Thiazolidine-4-carboxylic acid (Thz); iv. α-methylated amino acids; Selected from vD-amino acids. (15) In partial YZ and its subformulas, one or more modifications or non-natural amino acids, if present, independently iN-methylated amino acids; iii. Selected from D-amino acids. (16) Y is either absent or a peptide containing 1 to 16 amino acids. (17) Y is either absent or a peptide containing 1 to 12 (e.g., 3 to 10) amino acids. (18) Y is either absent or a peptide containing 1 to 8 amino acids. (19) Z is defined anywhere in this specification as Z a , Z b or Z c It is the basis. (20) Z is defined anywhere in this specification as Z a It is the basis. (21) Z is defined anywhere in this specification as Z b It is the basis. (22) Z is defined as Z as defined anywhere in this specification. c It is the basis. (23)R 2 NH2, NR 2a H or NR 2a R 2b And R 2a and R 2b Each of them, if present, independently, C 1~6 It is an alkyl group (for example, methyl, ethyl, propyl, butyl, pentyl, or hexyl). (24)R 2 It is NH2; (25)Y1 This refers to a peptide that is either absent or contains one or two amino acid residues. (26)Y 1 It does not exist. (27)Y 2 This refers to a peptide that is either absent or contains one or two amino acid residues. (28)Y 2 It does not exist.

[0114] Preferably, R 1 This is defined in any one of the above paragraphs (1) to (6). Most preferably, R 1 This is defined in any one of the paragraphs (4) to (6) above.

[0115] Preferably, L 1 This is defined in any one of paragraphs (7) to (10) above. Most preferably, L 1 This is as defined in paragraph (10) above.

[0116] Preferably, Y is as defined in any one of paragraphs (16) to (18), or as defined herein. a , Y b Or Y c It is the basis.

[0117] Preferably, Z is as defined in any one of paragraphs (19) to (22).

[0118] Preferably, at least one modified amino acid or non-natural amino acid analog in peptide Y and / or Z is as defined in any one of paragraphs (11) to (15) above. Most preferably, at least one modified amino acid or non-natural amino acid analog in peptide Y and / or Z is as defined in any one of paragraphs (13) to (15) above. Most preferably, at least one modified amino acid or non-natural amino acid analog in peptide Y and / or Z is as defined in paragraph (14) or (15).

[0119] Preferably, R 2 This is as defined in paragraph (23) or (24) above. Most preferably, R 2 This is as defined in paragraph (24) above.

[0120] Preferably, Y 1 This is defined in either paragraph (25) or (26) above. Most preferably, Y 1 This is defined in paragraph (26) above.

[0121] Preferably, Y 2 This is defined in either paragraph (27) or (28) above. Most preferably, Y 2 This is as defined in paragraph (28) above.

[0122] The specific peptide of the present invention Compound of formula (Ia) The present invention also relates to a compound of formula (Ia) (a subformula of formula (I)) that finds specific uses for Diptera insects.

[0123] In certain embodiments of the present invention, the present invention provides an insecticidal compound having the following formula (Ia): R 1 -L 1 -Y a -Z a -R 2 (Ia) During the ceremony, R 1 , L 1 , and R 2 This is as defined herein; Y a is a Y group as defined herein, and optionally, Y a It is either absent or a peptide containing 1 to 12 amino acids; Z a The formula is: -F # -H #-S # -W # -G # (Sequence ID 1) It is a peptide, During the ceremony, `` # The symbol "F", "H", "S", "W", and "G" independently indicate that the residues are an unmodified amino acid, a modified amino acid, or a non-natural amino acid analog.

[0124] Preferably, motif Y a -Z a At least one of the residues in the molecule is a modified amino acid or a non-natural amino acid analog.

[0125] Preferably, motif Y a -Z a At least one of the residues in the molecule is a modified amino acid or a non-natural amino acid analog, provided that S # If the residue is an α-aminoisobutyric acid group ([Aib]), then motif Y a -Z a It further contains at least one D-amino acid.

[0126] Preferably, motif Y a -Z a One or more modified amino acids or non-natural amino acid analogs are independently defined as defined in any part of this specification. One or more modified amino acids or non-natural amino acid analogs are independently defined as defined in any one of paragraphs (11) to (15) of this specification. More preferably, one or more modified amino acids or non-natural amino acid analogs are independently defined as defined in any one of paragraphs (13), (14), or (15).

[0127] In one embodiment of the compound of formula (Ia), one or more modified amino acids or unnatural amino acid analogs are independently selected from N-methylated amino acids, aminoisobutyric acid (Aib), or D-amino acids.

[0128] Preferably, Z a The part is the peptide of formula ZaI: FH# -S # -WG(Z a l) (Sequence ID 6) In the formula, at least one of the "H" and "S" residues is a modified amino acid or a non-natural amino acid analog as defined herein.

[0129] Preferably, Z a The part is the peptide of formula ZaI-I: FHS # -WG(ZaI-I)(Sequence ID 7) In the formula, the "S" residue is a modified amino acid or a non-natural amino acid analog as defined herein.

[0130] Preferably, Z a The part is the peptide of formula ZaI-I: FHS # -WG (Sequence ID 8) During the ceremony, “S # The residue is selected from α-aminoisobutyric acid, N-methylserine, or D-serine.

[0131] Preferably, Z a The part is the peptide of formula ZaI-I: FHS # -WG (Sequence ID 9) During the ceremony, “S # The residue is selected from N-methylserine or D-serine.

[0132] Preferably, Z a The part is formula: FHSWG (Sequence ID 10) FH[Aib]WG (Sequence ID 3) FHsWG(sequence number 4); or This is the peptide FH[n-me-S]WG (SEQ ID NO: 5).

[0133] Preferably, Z a The part is formula: FHsWG(sequence number 4); or This is the peptide FH[n-me-S]WG (SEQ ID NO: 5).

[0134] Preferably, Y a This is a peptide that either does not contain amino acids, or contains 1 to 12 amino acids, which may include a PEG linker. More preferably, Y a It is a peptide containing 1 to 12 amino acids, for example, 3 to 10 amino acids.

[0135] Preferably, Y a It does not exist, or the expression: Y a1 ---K # -Q # -R # It is a peptide, In the formula, Y a1 It is either absent or a peptide containing 1 to 9 amino acids; During the ceremony, `` # " indicates that the residue is one of the naturally occurring amino acids, modified amino acids, or unnatural amino acid analogs as defined herein.

[0136] Preferably, Y a It does not exist, or the expression: Y a1 ---KQR # It is a peptide, In the formula, Y a1 It is either absent or a peptide containing 1 to 9 amino acids; During the ceremony, “R # The residue is a modified amino acid or a non-natural amino acid analog as defined herein.

[0137] Preferably, Y a It does not exist, or the expression: Y a1 ---KQR # It is a peptide, In the formula, Y a1 It is either absent or a peptide containing 1 to 9 amino acids; During the ceremony, “R #The residue is selected from N-methylarginine or d-arginine.

[0138] Preferably, Y a The part does not exist, or it is an expression: KQr; NSVVLGKKQr(sequence number 11); or NSVVLGKKQ[n-me-R](Sequence ID 12) It has.

[0139] Preferably, Y a -Z a The part is formula: Y a1 ---K # -Q # -R # ---FH # -S # -WG(sequence number 13); or FH # -S # -WG (Sequence ID 138) It is a peptide, In the formula, Y a1 It is either absent or a peptide containing 1 to 9 amino acids; During the ceremony, `` # The notation " indicates that the residues "K", "Q", "R", "H", and "S" are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs; In the formula, at least one of the residues "K", "Q", "R", "H", and "S" is a modified amino acid or a non-natural amino acid analog as defined herein.

[0140] Preferably, Y a -Z a The part is formula: Y a1 ---KQR # ---FH # -S # -WG(sequence number 14); or FH # -S # -WG (Sequence ID 6) It is a peptide, In the formula, Ya1 It is either absent or a peptide containing 1 to 9 amino acids; During the ceremony, `` # The notation " indicates that the residues "R", "H", and "S" are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs; However, at least one of the residues "R", "H", and "S" is a modified amino acid or a non-natural amino acid analog as defined herein.

[0141] Preferably, Y a -Z a The part is formula: Y a1 ---KQR # ---FHS # -WG(sequence number 15); or FHS # -WG (Sequence ID 7) It is a peptide, In the formula, Y a1 It is either absent or a peptide containing 1 to 9 amino acids; During the ceremony, `` # This indicates that residues "R" and "S" are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs; However, at least one of the residues "R" (if present) and "S" is a modified amino acid or a non-natural amino acid analog as defined herein.

[0142] Preferably, Y a -Z a The part is formula: Y a1 ---KQR # ---FHS # -WG(sequence number 16); or FHS # -WG (Sequence ID 7) It is a peptide, In the formula, Y a1 It is either absent or a peptide containing 1 to 9 amino acids; During the ceremony, `` #This indicates that the residues "R" (if present) and "S" are independently selected from modified amino acids or non-natural amino acid analogs as defined herein.

[0143] Preferably, Y a -Z a The part is formula: Y a1 ---KQR # ---FHS # -WG(sequence number 17); or FHS # -WG (Sequence ID 9) It is a peptide, In the formula, Y a1 It is either absent or a peptide containing 1 to 9 amino acids; During the ceremony, `` # This indicates that residues "R" and "S" are independently selected from d-amino acids or N-methylated amino acids. In other words, "R # The residue is selected from N-methylarginine or d-arginine; "S # The residue is selected from N-methylserine or D-serine.

[0144] Specific compounds of formula (Ia) include the compounds or salts thereof listed in the table below. [Table 1]

[0145] Specific applications of the compound of formula (Ia) Preferably, compounds of formula (Ia) have been found to have specific use as insecticides against dipteran insects (e.g., insects of the genus Drosophila). Therefore, such compounds can be applied in appropriate manner as defined herein.

[0146] The use of the compound according to formula (Ia) as defined herein as an insecticide is also provided. Preferably, such use is as an insecticide against Diptera insects (e.g., insects of the genus Drosophila).

[0147] A method for increasing the mortality rate of dipteran insects is also provided, comprising the step of contacting a dipteran insect or a population of dipteran insects with a compound according to formula (Ia) as defined herein, or a composition comprising a compound according to formula (Ia) as defined herein.

[0148] Also provided are compounds according to formula (Ia) as defined herein, or compositions comprising compounds according to formula (Ia) as defined herein, for use as plant protectants to protect plants from dipteran insects.

[0149] A method for inhibiting plant parasitism by dipteran insects is also provided, comprising the step of contacting the plant with a compound according to formula (Ia) as defined herein, or a composition comprising a compound according to formula (Ia) as defined herein. Preferably, the compound is applied to the plant while the plant is free from or substantially free from dipteran insects.

[0150] In a particular embodiment, the compound of formula (Ia) is Z a The part is formula Z a If it is a peptide of l, specific use as an insecticide against dipteran insects (e.g., Drosophila melanogaster) has been found. FH # -S # -WG(Z a l) (Sequence ID 6) In the formula, at least one of the "H" and "S" residues is a modified amino acid or a non-natural amino acid analog as defined herein.

[0151] In a particular embodiment, the compound of formula (Ia) is Z a If the portion is a peptide of formula ZaI-I, specific use as an insecticide against dipteran insects (e.g., Drosophila melanogaster) has been found. FHS# -WG(ZaI-I)(Sequence ID 7) In the formula, the "S" residue is a modified amino acid or a non-natural amino acid analog as defined herein. Preferably, "S # The residue is selected from α-aminoisobutyric acid, N-methylserine, or D-serine.

[0152] Compounds of formula (Ia) and its subformulas are particularly used for Diptera insects, but these compounds can also be applied to any of the insect orders or species described herein in the methods and uses described herein, for example, Lepidoptera or Hemiptera.

[0153] Preferably, the compound of formula (Ia) can be used in combination with one or more additional insecticides described herein.

[0154] In one embodiment, the compound of formula (Ia) can be used in combination with one or more additional insecticides described herein as an insect control agent for diptera insects.

[0155] Compound of formula (Ib) The present invention also relates to a compound of formula (Ia) (a subformula of formula (I)) that finds specific uses for hemipteran insects (e.g., *Hymenomorpha harris* and *Camponotus persicae*).

[0156] In another embodiment, the present invention provides an insecticidal compound having the following formula (Ib): R 1 -L 1 -Y b -Z b -R 2 (Ib) During the ceremony, R 1 , L 1 , and R 2 This is as defined herein, Y b is a Y group as defined herein, and optionally, Y bIt is either absent or a peptide containing 1 to 14 amino acids; Z b The formula is: -F # -X 2b -X 3b -W # -X 5b It is a peptide, During the ceremony, X 2b is the amino acid residue S # , Y # , K # , N # or H # Selected from; X 3b is the amino acid residue S # , A # , P # , V # or T # Selected from; X 5b is amino acid residue A # Or G # Selected from; During the ceremony, `` # The symbol " indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs.

[0157] Preferably, Z b The formula is: -F # -X 2b -X 3b -W # -X 5b It is a peptide, During the ceremony, X 2b is the amino acid residue S # , Y # , N # or H # Selected from; X 3b is the amino acid residue S # , A # , P # , V # or T # Selected from; X5b is amino acid residue A # Or G # Selected from; During the ceremony, `` # The symbol " indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs.

[0158] Preferably, Z b The formula is: -F # -X 2b -X 3b -W # -X 5b It is a peptide, During the ceremony, X 2b is the amino acid residue S # , Y # , N # or H # Selected from; X 3b is the amino acid residue S # Or A # , P # , V # or T # Selected from; X 5b is amino acid residue A # Or G # Selected from; During the ceremony, `` # The symbol " indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs.

[0159] More preferably, Z b The formula is: -F # -X 2b -X 3b -W # -X 5b It is a peptide, During the ceremony, X 2b is the amino acid residue S # , Y # or N # Selected from; X 3bis the amino acid residue S # Or A # Selected from; X 5b is amino acid residue A # Or G # Selected from; During the ceremony, `` # The symbol " indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs.

[0160] Preferably, Z b The formula is: F # -X 1b -X 2b -WX 4b It is a peptide, During the ceremony, X 2b is selected from amino acid residues S, Y, or N; X 3b is the amino acid residue S # Or A # Selected from; X 5b This is selected from amino acid residues A or G.

[0161] Preferably, Z b The formula is: F-X1b-X 2b -WX 4b It is a peptide, During the ceremony, X 2b is selected from amino acid residues S, Y, or N; X 3b is the amino acid residue S # Or A # Selected from; X 5b This is selected from amino acid residues A or G.

[0162] Preferably, Z b is (ZbI)~(ZbVIII)(Z b Sub-expression of): F # -S # -S# -W # -G # (Sequence code 24)(ZbI); F # -S # -S # -W # -A # (Sequence code 25)(ZbII); F # -N # -S # -W # -A # (Sequence number 26)(ZbIII); F # -Y # -S # -W # -G # (Sequence code 27)(ZbIV); F # -N # -A # -W # -A # (Sequence code 28)(ZbV); F # -S # -A # -W # -G # (Sequence code 29)(ZbVI); F # -N # -S # -W # -G # (Sequence code 30)(ZbVII); or F # -K # -S # -W # -G # (Sequence ID 31)(ZbVIII) A peptide having a formula selected from one of the following, During the ceremony, `` # Any residue marked with '' is independently one of the listed unmodified amino acids, modified amino acids, or unnatural amino acid analogs.

[0163] Preferably, Z b is (ZbI-I)~(ZbVI-III-I)(Z bSub-expression of): F # -SS # -WG (Sequence ID 32) (ZbI-I); F # -SS # -WA(sequence number 33) (ZbII-I); F # -NS # -WA (Sequence ID 34) (ZbIII-I); F # -YS # -WG (Sequence ID 35) (ZbIV-I); F # -NA # -WA (Sequence ID 36) (ZbV-I); F # -SA # -WG (Sequence ID 37) (ZbVI-I); F # -NS # -WG(sequence number 38) (ZbVII-I); or F # -KS # -WG (Sequence ID 39) (ZbVIII-I) A peptide having a formula selected from one of the following, During the ceremony, `` # Any residue marked with '' is independently one of the listed unmodified amino acids, modified amino acids, or unnatural amino acid analogs.

[0164] Preferably, in formulas (ZbI-I) to (ZbVIII-I), the modifications or non-natural amino acid analogs may be as defined in any part of this specification.

[0165] In certain embodiments, in formulas (ZbI-I) to (ZbVIII-I), the modified or unnatural amino acid analog is selected from N-methylated amino acids, α-methylated amino acids, aminoisobutyric acid (Aib), D-amino acids, or beta-amino acids.

[0166] In a particular embodiment, in the compound of formula (Ib), Z b is a peptide of the formula (ZbI)~(ZbVIII) or (ZbI-I)~(ZbVIII-I), F # The residues indicated as such are selected from unmodified amino acid F (phenylalanine) or N-methylated phenylalanine.

[0167] In a particular embodiment, in the compound of formula (Ib), Z b is a peptide of the formula (ZbI)~(ZbIV) or (ZbI-I)~(ZbIV-I), S # The residues indicated are selected from unmodified amino acids S (serine), n-methylated serine, beta-serine, alpha-methylserine, or D-serine.

[0168] Preferably, Z b is (ZbI)~(ZbVI)(Z b Sub-expression of): F # -S # -S # -W # -G # (Sequence code 24)(ZbI); F # -S # -S # -W # -A # (Sequence code 25)(ZbII); F # -N # -S # -W # -A # (Sequence number 26)(ZbIII); F # -Y # -S # -W # -G # (Sequence code 27)(ZbIV); F # -N # -A # -W # -A # (Sequence code 28)(ZbV); or F# -S # -A # -W # -G # (Sequence ID 29)(ZbVI) A peptide having a formula selected from one of the following, During the ceremony, `` # Any residue marked with '' is independently one of the listed unmodified amino acids, modified amino acids, or unnatural amino acid analogs.

[0169] Preferably, Z b is (ZbI)~(ZbVI-I)(Z b Sub-expression of): F # -SS # -WG (Sequence ID 32)(ZbI-I); F # -SS # -WA (Sequence ID 33)(ZbII-I); F # -NS # -WA (Sequence ID 34)(ZbIII-I); F # -YS # -WG (Sequence ID 35)(ZbIV-I); F # -NA # -WA (sequence number 36)(ZbV-I); or F # -SA # -WG (Sequence ID 37)(ZbVI-I) A peptide having a formula selected from one of the following, During the ceremony, `` # Any residue marked with '' is independently one of the listed unmodified amino acids, modified amino acids, or unnatural amino acid analogs.

[0170] Preferably, in formulas (ZbI-I) to (ZbVI-I), the modifications or non-natural amino acid analogs may be as defined in any part of this specification.

[0171] In certain embodiments, in formulas (ZbI-I) to (ZbVI-I), the modified or unnatural amino acid analog is selected from N-methylated amino acids, α-methylated amino acids, aminoisobutyric acid (Aib), D-amino acids, or beta-amino acids.

[0172] In a particular embodiment, in the compound of formula (Ib), Z b is a peptide of the formula (ZbI)~(ZbVI) or (ZbI-I)~(ZbVI-I), F # The residues indicated as such are selected from unmodified amino acid F (phenylalanine) or N-methylated phenylalanine.

[0173] In a particular embodiment, in the compound of formula (Ib), Z b is a peptide of the formula (ZbI)~(ZbIV) or (ZbI-I)~(ZbIV-I), S # The residues indicated are selected from unmodified amino acids S (serine), n-methylated serine, beta-serine, alpha-methylserine, or D-serine.

[0174] In another specific embodiment, in a compound of formula (Ib), Z b is a peptide of formula (ZbI) or (ZbI-I), F # The residues indicated are either unmodified amino acid F (phenylalanine) or N-methylated phenylalanine. S # These are unmodified amino acids S (serine), n-methylated serine, beta-serine, alpha-methylserine, or D-serine.

[0175] Preferably, Z b teeth, FSSWG (Sequence ID 40) FSSWA (Sequence ID 41) FNSWA (Sequence ID 42) FYAWG (Sequence ID 43) FN[Aib]WA (Sequence ID 44) FN-βA-WA (SEQ ID NO: 45) (n-me-F)-SsWG(Sequence ID 46) (n-me-F)-S-βA-WG (Sequence ID 47) (n-me-F)-S-(α-Me)S-WG(Sequence ID 48); FNSWG(sequence number 49); or FKSWG (Sequence ID 50) Selected from.

[0176] Preferably, Z b teeth, FSSWG (Sequence ID 40) FSSWA (Sequence ID 41) FNSWA (Sequence ID 42) FYAWG (Sequence ID 43) FN[Aib]WA (Sequence ID 44) FN-βA-WA (SEQ ID NO: 45) (n-me-F)-SsWG(Sequence ID 46) (n-me-F)-S-βA-WG (Sequence ID 47) (n-me-F)-S-(α-Me)S-WG (Sequence ID 48) Selected from.

[0177] In one embodiment, motif Y b ~Z b At least one of the residues in the molecule is a modified amino acid or a non-natural amino acid analog.

[0178] Appropriately, motif Y b ~Z bOne or more modified amino acids or non-natural amino acid analogs are independently defined as defined in any part of this specification. One or more modified amino acids or non-natural amino acid analogs are independently defined as defined in any one of paragraphs (11) to (15) of this specification. More preferably, one or more modified amino acids or non-natural amino acid analogs are independently defined as defined in any one of paragraphs (13), (14), or (15).

[0179] In one embodiment of the compound of formula (Ib), one or more modified amino acids or unnatural amino acid analogs, if present, are independently selected from N-methylated amino acids, aminoisobutyric acid (Aib), D-amino acids, or beta-amino acids.

[0180] Preferably, Y b It is either absent or a peptide containing 1 to 14 amino acids. More preferably, Y b It is a peptide containing 1 to 12 amino acids.

[0181] Preferably, Y b It may contain one or more modified amino acids or unnatural amino acid analogs. Preferably, Y b The one or more modified amino acids or unnatural amino acid analogs present are d-amino acids.

[0182] Preferably, Y b teeth, DPKYK(sequence number 51); AK; AR; SK; VP; PI; GPD; Sk; RQKTV(sequence number 52); PA; ASDKHGRPKQT(sequence number 53); Y; GPA; AAA; NAA; PA; VPA; TNTA(SEQ ID NO: 54); PR; GAD; DPA; SSA; RAFTSTGSSRSPA(Sequence ID 55); PAS; DAG; SSG; DPV; DAA; GSG; DDDSDVSESGSK(sequence number 56); S; G; LDRSEGRVSKAL(Sequence ID 57); WGQSSVGAV(sequence number 58); or GAE Selected from.

[0183] Preferably, Y b teeth, DPKYK(sequence number 51); AK; AR; SK; VP; PI; GPD; Sk; RQKTV(sequence number 52); PA; or ASDKHGRPKQT(Sequence ID 53) Selected from.

[0184] Specific compounds of formula (Ib) include the compounds listed in the table below, or their salts or solvates. [Table 2]

[0185] Specific compounds of formula (Ib) include the compounds or salts thereof listed in the table below. [Table 3]

[0186] Specific applications of the compound of formula (Ib) Preferably, compounds of formula (Ib) have been found to have specific use as insecticides against hemipteran insects (e.g., *Hymenomorpha harris* and *Thuidium persicae*). Thus, such compounds can be applied in appropriate ways as defined herein.

[0187] The compound of formula (Ib) can be found to have specific use as an insecticide against the species Hariomorpa haris.

[0188] Compounds of formula (Ib) can be found to have specific uses as insecticides against aphid species.

[0189] Compound (Ib) can be found to have specific use as an insecticide against the species *Mizus persicae*.

[0190] In a particular embodiment, the compound of formula (Ib) is Z b The part is (ZbI)~(ZbVIII)(Z b If the peptide is one of the subformulas of the formula (subformula of ), then specific use as an insecticide against hemipteran insects (e.g., *Hariomorpa haris*) has been found: F # -S # -S # -W # -G # (Sequence code 24)(ZbI); F # -S # -S # -W # -A # (Sequence code 25)(ZbII); F # -N # -S # -W # -A # (Sequence number 26)(ZbIII); F # -Y # -S # -W# -G # (Sequence code 27)(ZbIV); F # -N # -A # -W # -A # (Sequence code 28)(ZbV); F # -S # -A # -W # -G # (Sequence code 29)(ZbVI); F # -N # -S # -W # -G # (Sequence code 30)(ZbVII); or F # -K # -S # -W # -G # (Sequence ID 31)(ZbVIII) A peptide having a formula selected from one of the following, During the ceremony, `` # Any residue marked with '' is independently one of the listed unmodified amino acids, modified amino acids, or unnatural amino acid analogs.

[0191] In a particular embodiment, the compound of formula (Ib) is Z b The part is (ZbI)~(ZbVI)(Z b If the peptide is one of the subformulas of the formula (subformula of ), then specific use as an insecticide against hemipteran insects (e.g., *Hariomorpa haris*) has been found: F # -S # -S # -W # -G # (Sequence code 24)(ZbI); F # -S # -S # -W # -A # (Sequence code 25)(ZbII); F # -N# -S # -W # -A # (SEQ ID NO: 26)(ZbIII); F # -Y # -S # -W # -G # (SEQ ID NO: 27)(ZbIV); F # -N # -A # -W # -A # (SEQ ID NO: 28)(ZbV); or F # -S # -A # -W # -G # (SEQ ID NO: 29)(ZbVI); wherein any residue marked with " # " is independently any of the listed unmodified amino acids, modified amino acids or unnatural amino acid analogs.

[0192] In certain embodiments, when the compound of formula (Ib) is a peptide having a formula in which Z b is selected from any one of (ZbI-I) to (ZbV-I) (sub-formulas of Z b ), a particular use as an insecticide against Hemiptera insects (e.g., the species Helicoverpa armigera) is found: F # -S-S # -W-G (SEQ ID NO: 32)(ZbI-I); F # -S-S # -W-A (SEQ ID NO: 33)(ZbII-I); F # -N-S # -W-A (SEQ ID NO: 34)(ZbIII-I); F # -Y-S # -W-G (SEQ ID NO: 35)(ZbIV-I); or F # -N-A # -W-A (SEQ ID NO: 36)(ZbV-I); wherein, "# Any residue marked with '' is independently one of the listed unmodified amino acids, modified amino acids, or unnatural amino acid analogs.

[0193] In a particular embodiment, the compound of formula (Ib) is Z b (ZbI) or (ZbI-I)(Z b If the peptide has a formula selected from the subformulas of , specific use as an insecticide against hemipteran insects (e.g., *Hymenomorpha harris* or *Tricholoma persicae* insects) has been found: F # -S # -S # -W # -G # (Sequence code 24)(ZbI); or F # -SS # -WG (Sequence ID 32)(ZbI-I); During the ceremony, `` # Any residue marked with '' is independently one of the listed unmodified amino acids, modified amino acids, or unnatural amino acid analogs.

[0194] The use of the compound according to formula (Ib) as defined herein as an insecticide is also provided. Preferably, such use is as an insecticide against hemipteran insects (e.g., *Hymenomorpha harris* or *Campyris persicae*).

[0195] A method for increasing the mortality rate of hemipteran insects is also provided, comprising the step of contacting a population of hemipteran insects (e.g., *Hyriomorpa harris* or *Camponotus persicae*) or hemipteran insects (e.g., *Hyriomorpa harris* or *Camponotus persicae*) with a compound according to formula (Ib) as defined herein, or a composition comprising a compound according to formula (Ib) as defined herein.

[0196] Also provided are compounds according to formula (Ib) as defined herein, or compositions comprising compounds according to formula (Ib) as defined herein, for use as plant protectants to protect plants from hemipteran insects (e.g., *Hymenomorpha harris* or *Campylocentrotus persicae*).

[0197] A method for inhibiting plant parasitism by hemipteran insects (e.g., *Hymenomorpha harris* or *Tricholoma persicae*) is also provided, comprising the step of contacting the plant with a compound according to formula (Ib) as defined herein, or a composition comprising a compound according to formula (Ib) as defined herein. Preferably, the compound is applied to the plant while it is free from or substantially free from hemipteran insects (e.g., *Hymenomorpha harris* or *Tricholoma persicae*).

[0198] Compounds of formula (Ib) and its subformulas are particularly used against hemipteran insects (e.g., *Hymenomorpha harris* or *Campylocentrotus persicae*), but these compounds may also be applied to any of the insect orders or species described herein in the methods and uses described herein, for example, to diptera or lepidoptera insects.

[0199] Preferably, the compound of formula (Ib) can be used in combination with one or more additional insecticides described herein.

[0200] In one embodiment, the compound of formula (Ib) can be used in combination with one or more additional insecticides described herein as an insect control agent against M. persicae.

[0201] In one embodiment, the compound of formula (Ib) can be used in combination with one or more additional insecticides described herein as an insect control agent for hemipteran insects.

[0202] Additional insecticides can be selected from CAPA peptides, such as SDSKNT[n-me-A]LWFGPRL-[NH2](SEQ ID NO: 134)(SB-P-015), ASG[b3L]VAFPRV-[NH2](SEQ ID NO: 135)(2315), or Palm-LVAFPRV-[NH2](SEQ ID NO: 136)(AH59).

[0203] In certain embodiments, compounds of formula (Ib) are found to have specific use as insecticides against cockroach insects (e.g., German cockroaches). Preferably, in such embodiments, Z b is (ZbI-I), (ZbIII-I), or (ZbIV-I)(Z b Sub-expression of): F # -SS # -WG (Sequence ID 32)(ZbI-I); F # -NS # -WA (Sequence ID 34)(ZbIII-I); or F # -YS # -WG (Sequence ID 35)(ZbIV-I) A peptide having a formula selected from one of the following, During the ceremony, `` # Any residue marked with '' is independently one of the listed unmodified amino acids, modified amino acids, or unnatural amino acid analogs.

[0204] Compound of formula (Ic) The present invention also relates to a compound of formula (Ic) (a subformula of formula (I)) for which specific uses are found for insects of the order Lepidoptera (e.g., Plutella xirostera or Spodoptera fulgiperda).

[0205] In certain embodiments of the present invention, the present invention provides an insecticidal compound having the following formula (Ic): R 1 -L 1 -Y c -Z c -R 2 (I C) During the ceremony, R 1 , L 1 , and R 2 This is as defined herein; Y c is a Y group as defined herein, and optionally, Y b It is either absent or a peptide containing 1 to 12 amino acids; Z c The formula is: -F # -S # -X 3c -W # -G # (Sequence 2) It is a peptide, In the formula, X 3c is amino acid residue A # , P # , V # or T # Selected from; During the ceremony, `` # The symbol " indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs.

[0206] Preferably, Z c The formula is: -FSX 3c -WG(Sequence ID 118)(ZcI) It is a peptide, X 3c is amino acid residue A # , P # , V # or T # Selected from; In the formula, any residue marked with "#" is independently one of the listed unmodified amino acids, modified amino acids, or unnatural amino acid analogs.

[0207] Preferably, X 3c P # or V # That is the case.

[0208] Preferably, Z cis ZcI-I to ZcI-IV: -F-S-A # -W-G (SEQ ID NO: 119)(ZcI-I) -F-S-P # -W-G (SEQ ID NO: 120)(ZcI-II) -F-S-V # -W-G (SEQ ID NO: 121)(ZcI-III) -F-S-T # -W-G (SEQ ID NO: 122)(ZcI-IV) a peptide of the formula selected from: In the formula, any residue marked with "#" is independently any of the listed unmodified amino acids, modified amino acids or unnatural amino acid analogs.

[0209] Preferably, at least one of the residues in motif Y c -Z c is a modified amino acid or an unnatural amino acid analog.

[0210] Preferably, one or more of the modified amino acids or unnatural amino acid analogs in motif Y c -Z c are independently as defined anywhere in this specification. One or more modified amino acids or unnatural amino acid analogs are independently as defined in any one of paragraphs (11)-(15) of this specification. More preferably, one or more modified amino acids or unnatural amino acid analogs are independently as defined in any one of paragraphs (13), (14), or (15).

[0211] In one embodiment of the compound of formula (Ic), one or more modified amino acids or unnatural amino acid analogs are independently selected from N-methylated amino acids, amino isobutyric acid (Aib), thiazolidine-4-carboxylic acid (Thz), beta amino acids or D-amino acids.

[0212] Preferably, Z c is FSPWG(SEQ ID NO: 101) FSAWG (Sequence ID 102) FSVWG (Sequence ID 103) FSTWG (Sequence ID 104) FS-βA-WG (SEQ ID NO: 105) FS-Thz-WG (Sequence ID 106) It is a peptide of the formula selected from the following.

[0213] Preferably, Y c It is either absent or a peptide of 1 to 12 amino acids. More preferably, Y c It is either absent or a peptide of 1 to 8 amino acids. More preferably, Y b It is a peptide containing 1 to 4 amino acids.

[0214] Preferably, Y c It does not exist, or VR; N; KVK; SFS; or Y Selected from.

[0215] Specific compounds of formula (Ic) include the compounds listed in the table below, or their salts or solvates. [Table 4]

[0216] Specific applications of compounds of formula (Ic) Preferably, compounds of formula (Ic) have been found to have specific use as insecticides against lepidopteran insects (e.g., Plutella xirostera or Spodoptera fulgiperda). Thus, such compounds can be applied in appropriate ways as defined herein.

[0217] The use of the compound according to formula (Ic) as defined herein as an insecticide is also provided. Preferably, such use is as an insecticide against lepidopteran insects (e.g., Plutella xirostera or Spodoptera fulgiperda).

[0218] A method for increasing the mortality rate of lepidopteran insects is also provided, comprising the step of contacting a lepidopteran insect (e.g., Plutella xirostella or Spodoptera fulgiperda) or a population of lepidopteran insects (e.g., a population of Plutella xirostella) with a compound according to formula (Ic) as defined herein, or a composition comprising a compound according to formula (Ic) as defined herein.

[0219] Also provided are compounds according to formula (Ic) as defined herein, or compositions comprising compounds according to formula (Ic) as defined herein, for use as plant protectants to protect plants from lepidopteran insects (e.g., Plutella xirostella or Spodoptera fulgiperda).

[0220] A method for inhibiting plant parasitism by lepidopteran insects (e.g., Plutella xirostella or Spodoptera fulgiperda) is also provided, comprising the step of contacting the plant with a compound according to formula (Ic) as defined herein, or a composition comprising a compound according to formula (Ic) as defined herein. Preferably, the compound is applied to the plant while the plant is free from or substantially free from lepidopteran insects (e.g., Plutella xirostella or Spodoptera fulgiperda).

[0221] Compound (Ic) can be found to have specific use as an insecticide against Plutella xylostella species.

[0222] The compound of formula (Ic) can be found to have specific use as an insecticide against the species Spodoptera fulgiperda.

[0223] In a particular embodiment, the compound of formula (Ic) is Z c If the part is a peptide of a formula selected from any one of ZcI-I to ZcI-IV, specific use as an insecticide against lepidopteran insects (e.g., Plutella xirostera or Spodoptera fulgiperda) has been found: -FSA #-WG (Sequence ID 119)(ZcI-I) -FSP # -WG (Sequence ID 120)(ZcI-II) -FSV # -WG (Sequence ID 121)(ZcI-III) -FST # -WG (Sequence ID 122)(ZcI-IV) The peptide is selected from the following formulas: In the formula, any residue marked with "#" is independently one of the listed unmodified amino acids, modified amino acids, or unnatural amino acid analogs.

[0224] In a particular embodiment, the compound of formula (Ic) is Z c If the portion is a peptide of a formula selected from one of ZcI-I, ZcI-II, or ZcI-IV, specific uses as an insecticide against lepidopteran insects (e.g., Plutella xirostera or Spodoptera fulgiperda) have been found: -FSA # -WG (Sequence ID 119)(ZcI-I) -FSP # -WG (Sequence ID 120)(ZcI-II) -FST # -WG (Sequence ID 122)(ZcI-IV) The peptide is selected from the following formulas: In the formula, any residue marked with "#" is independently one of the listed unmodified amino acids, modified amino acids, or unnatural amino acid analogs.

[0225] Compounds of formula (Ic) and its subformulas are particularly used against lepidopteran insects (e.g., Plutella xirostera or Spodoptera fulgiperda), but these compounds may also be applied to any of the insect orders or species described herein in the methods and uses described herein, for example, diptera or hemipteran insects.

[0226] Preferably, the compound of formula (Ic) can be used in combination with one or more additional insecticides described herein.

[0227] In one embodiment, the compound of formula (Ic) can be used in combination with one or more additional insecticides described herein as an insect control agent for lepidopteran insects.

[0228] In one embodiment, the compound of the present invention may be any of the kinin analogs listed herein. Examples of kinin analog peptides include the compounds disclosed herein and their salts or solvates, particularly those listed in the table below. [Table 5]

[0229] Further examples of kinin analog peptides include the compounds disclosed herein, and their salts or solvates, in particular those listed in the table below. [Table 6A] [Table 6B]

[0230] Further description of the compound of the present invention In some embodiments, the compounds of the present invention may be in the form of salts or solvates.

[0231] The compounds of the present invention can be provided in combination with one or more additional active insecticides, such as those described herein.

[0232] R 1 , L 1 and R 2 The terminal groups located at the N-terminus and C-terminus of the peptide skeleton are R 1 and R 2 This is shown. Therefore, R1 This is the nitrogen atom of the N-terminal amino group of Y (L, if necessary). 1 or Y 1 (via) bonded, R 2 is Z or Y 2 It bonds to the C-terminal carbonyl carbon atom.

[0233] In addition to containing at least one modified or non-natural amino acid residue, the compounds of the present invention may preferably contain further functional groups at the N or C terminus. Preferably, the compounds may be functionalized to increase cuticle permeability or to increase stability. Preferably, the compounds may be functionalized with aromatic, aliphatic or lipophilic groups. Therefore, preferably, R 1 This may be an aromatic, heteroaromatic, aliphatic, or lipophilic group.

[0234] In certain embodiments, the compound can be functionalized with lipophilic groups such as fatty acyl groups. Examples of fatty acyl groups include, but are not limited to, palmitoyl, butyryl, cerotoyl, decanoyl, docosenoyl, dodecanoyl, eleostearoyl, heptanol, hexanoyl, eicosanoyl, eicosenoyl, lignoceroyl, linoleoyl, lipoyl, myristreoyl, nonanoyl, octadecanoyl, octanoyl, palmitoyl, stearoyl, undecanoyl, and valeryl. Therefore, preferably, R 1 The base may be palmitoyl ([Palm]).

[0235] In one embodiment, the compound can be functionalized with an aromatic group such as a benzyl or benzoyl group, which may be a benzoic acid derivative or a benzophenone derivative. Therefore, preferably, R 1 The group may be an aromatic group such as 4-benzoylbenzoic acid, or a derivative such as 4-benzoylbenzoyl.

[0236] In one embodiment, the compound can be functionalized with an acyl group. The "acyl" group is represented by formula R 3a -C(O)- group, and in the formula, R 3a C1~6 Alkyl, for example, formyl, acetyl (Ac), propanoyl, butanoyl, or R 3a is benzoyl. Preferably, R 3a The group is R such as acetyl (Ac). 1b -C(O)- may also be acceptable.

[0237] In some embodiments, R 1 The base may be a biotin moiety. Therefore, the biotin moiety can be incorporated into an amino acid residue (e.g., a modified lysine side chain) or terminal.

[0238] In a particular embodiment, R 1 The group can be substituted with a sugar moiety. The amino acid residue can also be modified with a sugar moiety; that is, the amino acid residue may be a "sugar-modified analogue." The sugar moiety may be a monosaccharide or a disaccharide. Examples of monosaccharides include glucose, 6-deoxyglucose, mannose, galactose, glucosamine, galactosamine, N-acetylglucosamine, N-acetylgalactosamine, glucuronic acid, allose, altrose, growth, idose, fucose, talose, ribose, deoxyribose, arabinose, xylose, lyxose, ribulose, xylulose, fructose, psicose, sorbose, or tagatose. Examples of disaccharides include sucrose, lactose, lactulose, allolactose, maltose, isomaltose, isomaltulose, trehalose, cellobiose, kordibiose, nigerose, sophorose, laminaribiose, genthiobiose, thiomaltose, mannobiose, or their N-, C-, or S-glycoside derivatives. Most preferably, the sugar portion is selected from glucosamine or galactosamine.

[0239] The sugar may be modified at the N-terminus or as part of a Ser side-chain modification. As part of the N-terminus, a spacer is usually added (e.g., succinic acid, Suc). R with such modifications 1 -L 1An example of a -Z sequence is sugar-Suc-SDSKNTAL. The notation "sugar" may refer to any of the sugars described herein, such as glucosamine or galactosamine.

[0240] Preferably, the compound can also be modified with a (poly)alkylene glycol polymer. This modification is R 1 , L 1 Alternatively, it may be present in the Z portion. Preferably, R 1 The base may be (poly)alkylene glycol. The presence of a polymer facilitates the formulation of the compound. A preferred (poly)alkylene glycol is polyethylene glycol (PEG). Therefore, the compound is preferably R 1 At the position, or linker L 1 The molecule can be PEGylated via covalent bonding of polyethylene glycol to amino acid residues in Z. The PEG group can have any suitable terminal group such as NH2OH or Ome.

[0241] The PEG group present as a linker portion or as part of a modified peptide chain has the formula [-(OCH2CH2)n-], where n is preferably an integer from 1 to 16.

[0242] R 1 C is hydrogen (which may be indicated as "H-" or "Hy-", or may not be indicated in a particular peptide sequence), C 1~4 Alkyl (e.g., methyl, ethyl, propyl, butyl), -N(R 1a )-C(=N + (R 1b )(R 1c ))NR 1d R 1e , or -C(=N + (R 1b )(R 1c ))NR 1d R 1e Selected from, R 1a , R 1b , R 1c , R 1d and R 1eEach of them independently contains hydrogen or C 1~4 Alkyl (e.g., methyl, ethyl, propyl, butyl), preferably selected from hydrogen or methyl.

[0243] In some embodiments, R 1 -C(=N + (R 1b )(R 1c ))NR 1d R 1e If R 1a , R 1b , R 1c , R 1d and R 1e Each of them is methyl, that is, R 1 is -C(=N + It is Me2)NMe2.

[0244] R 1 If = "H" (or "Hy"), then R 1 Typically, it shows a free primary amino group at the N-terminus. The other hydrogen atoms of the N-terminal amino group are R 1 Regardless of its properties, it is typically invariant. Exceptionally, if the N-terminal residue is N-methylated, even if the N-terminal residue has a secondary amine group, R 1 It can still be represented as H. Therefore, the N-methylated leucine residue at the N-terminus is R 1 -[n-me-L]-(wherein, R 1 It can be shown that (is H). However, it can also be simply shown that R 1 -L-(wherein, R 1 It can be represented as (where is methyl, and other hydrogen atoms are not shown).

[0245] In a particular embodiment, L 1 Y 1 It may contain a carbonyl group C=O adjacent to the N-terminus of the Y or Z group. For example, L 1 teeth, * -(C=O)C 1~12 Alkylene-NH-,-(C=O)C 1~10 Alkylene (C=O)-, * -(C=O)C1~10 It may be an alkylene (for example, -(C=O)-, i.e., a C1 alkylene which may be substituted with an oxo), and any L in the formula 1 The group may be substituted with one or more oxo (=O) groups, in the formula, * Y 1 This represents a connection point to Y or Z.

[0246] In some embodiments, R 1 If L is hydrogen, 1 It does not exist, or * -(C=O)C 1~16 It is alkylene-NH-, and in the formula, * Y 1 , represents a connection point to Y or Z, for example, R 1 is hydrogen, L 1 teeth, * -(C=O)C 1~6 Alkylene-NH-, for example. [ka] That is the case.

[0247] In a particular embodiment, L 1 If it exists, * -(C=O)C 1~10 It is alkylene-NH-, and in the formula, * Y 1 , represents a connection point to Y or Z. For example, L 1 teeth, * -(C=O)C 1~6 Alkylene-NH-, for example. [ka] And, This can be considered a residue of 6-aminohexanoic acid (Ahx).

[0248] In some embodiments, R 1 If it is hydrogen, L 1 It does not exist, or * -(C=O)C 1~16It is alkylene-NH-, and in the formula, * Y 1 , represents a connection point to Y or Z, for example, R 1 is hydrogen, L 1 teeth, * -(C=O)C11 alkylene-NH2, in the formula, * Y 1 , represents a connection point to Y or Z, that is, [ka] That is the case.

[0249] In a particular embodiment, L 1 If it exists, * -(C=O)C 1~12 It is alkylene-NH-, and in the formula, * Y 1 , represents a connection point to Y or Z. For example, L 1 teeth, * -(C=O)C 6~12 -alkylene-NH-, for example * -(C=O)C 11 It may also be alkylene-NH2, in the formula, * Y 1 , represents a connection point to Y or Z, that is, [ka] And, This can be considered a residue of 12-aminododecanoic acid (Ado).

[0250] L 1 If R 1 R is typically hydrogen (H). For example, 1 is hydrogen, L 1 teeth * -(C=O)C 1~6 Alkylene-NH-, for example. [ka] That is the case.

[0251] In some embodiments, R 1 -C(=N + (R 1b )(R 1c ))NR 1d R 1e If L 1 It does not exist, for example, R 1 is -C(=N + It is Me2)NMe2 and L 1 It does not exist. In such embodiments, R 1 The group, along with the N-terminal nitrogen, forms the following guanidine-based structure: [ka] It forms (represented as "NR" in the following structure).

[0252] Typically, L 1 -(C=O)C 1~10 -If it is alkylene-NH-, R 1 H is H.

[0253] Typically, R 1 -C(=N + (R 1b )(R 1c ))NR 1d R 1e If L 1 It does not exist. R 1 -C(=N + (R 1b )(R 1c ))NR 1d R 1e - and L 1 If R does not exist, 1 The group, together with the N-terminal nitrogen of the peptide sequence Z, forms a guanidine-based group (as discussed above). Preferably, "-C(=N + (R 1b )(R 1c ))NR 1d R 1e " is -C(=N + It is Me2)NMe2.

[0254] R 2 NH2, NR2a H, NR 2a R 2b , or OR 2a And in the formula, R 2a and R 2b Each of these is as defined herein. Preferably, R 2 This is NH2 (represented as [NH2] in the sequence).

[0255] "Guanidil" is R 1 -C(=N + This refers to the case where it is Me2)NMe2, and the terminal structure formed by "guanidyl-L-" is as follows. [ka]

[0256] Y 1 and Y 2 The compounds defined herein have terminal R1s at the N-terminus and C-terminus, respectively. 1 Base and R 2 It may contain one or two further peptide groups located between the group and the other. Preferably, these groups are Y 1 and Y 2 These are groups. If present, these groups are located on either side of the Z peptide group.

[0257] In one embodiment, Y 1 and Y 2 The basis does not exist.

[0258] In one embodiment, compound Y 1 It contains only the group Y. 2 Includes only the base.

[0259] In one embodiment, compound Y 1 and Y 2 Includes the base.

[0260] Preferably, Y 1 and Y 2The group, if present, independently contains one or two amino acids. Preferably, Y 1 and Y 2 The group preferably independently comprises any amino acid selected from M, R, G, and K.

[0261] In one embodiment, Y 1 and Y 2 The base is independently selected from GR, RG, KR, RK, K, R, M, and G. In one embodiment, Y 1 and Y 2 The base is independently selected from RG, KR, and K.

[0262] In one embodiment, compound Y 2 Includes only the base, Y 2 The base is selected from RG, KR, and K.

[0263] Modified amino acids and unnatural amino acid analogs In certain embodiments, at least one residue in peptides Y and Z (including their sub-formulas) is a modified or unnatural amino acid analog. The modified or unnatural amino acid analog may be any analog known to those skilled in the art. Examples of modified or unnatural amino acid analogs include: iN-methylated amino acids; ii. Peptoid analogs; iii. Sugar-modified analogs; iv. Biotin modification analogs v. Beta amino acids, vi. D-stereoconfiguration amino acids vii. Non-proteinogenic amino acids, such as hydroxyproline (Hyp:L-hydroxyproline or (2S,4R)-4-hydroxyproline), octahydroindole-2-carboxylic acid (Oic), sarcosine (Sar), norleucine (Nle), α-aminoisobutyric acid (Aib), thienylalanine (Thi), thiazolidine-4-carboxylic acid (Thz), phenylglycine (Phg), or gamma-aminobutyric acid (gaba), etc. viiiα-alkylated amino acids These include, Alternatively, the side chains of two amino acid residues can join together to form a cyclic structure (for example, intramolecular amide formation by a condensation reaction between the side chain of arginine or lysine and the side chain of aspartic acid or glutamic acid).

[0264] The compounds of the present invention may contain one or more modified amino acids or unnatural amino acid analogs in the Y peptide, Z peptide, or both the Y peptide and the Z peptide.

[0265] In certain embodiments, at least one residue in the Y portion is a modified or unnatural amino acid analog.

[0266] The compounds of the present invention may contain multiple modified amino acids or unnatural amino acid analogs in the peptide sequence YZ.

[0267] In one embodiment, the peptide portion YZ (including its sub-formula) contains five unmodified amino acid residues.

[0268] In one embodiment, the peptide portion YZ (including its sub-formula) comprises four unmodified amino acid residues and one modified amino acid or unnatural amino acid analog.

[0269] In one embodiment, the peptide portion YZ (including its sub-formula) comprises three unmodified amino acid residues and two modified amino acids or unnatural amino acid analogs.

[0270] In one embodiment, the peptide portion YZ (including its sub-formula) comprises two unmodified amino acid residues and four modified amino acids or unnatural amino acid analogs.

[0271] Preferably, at least two residues in the peptide portion YZ (including its sub-formula) are unmodified amino acids. More preferably, at least three residues in the peptide portion YZ are unmodified amino acids.

[0272] In certain embodiments, peptide YZ (including its sub-formula) comprises one, two, three, or four modified amino acids or non-natural amino acid analogs. In certain embodiments, peptide YZ comprises one, two, or three modified amino acids or non-natural amino acid analogs. In certain embodiments, peptide YZ comprises one or two modified amino acids or non-natural amino acid analogs. In certain embodiments, peptide YZ comprises a single modified amino acid or non-natural amino acid analog.

[0273] In certain embodiments, 1 to 5 residues in the peptide portion YZ (including its sub-formula) are modified amino acids or unnatural amino acid analogs. In certain embodiments, 1 to 4 residues in the peptide portion YZ are modified amino acids or unnatural amino acid analogs. In certain embodiments, 1 to 3 residues in the peptide portion YZ are modified amino acids or unnatural amino acid analogs.

[0274] In certain embodiments, peptide YZ (including its sub-formula) contains five or fewer modified amino acids or unnatural amino acid analogs. In certain embodiments, peptide YZ contains four or fewer modified amino acids or unnatural amino acid analogs. In certain embodiments, peptide YZ contains three or fewer modified amino acids or unnatural amino acid analogs.

[0275] In other embodiments, peptide YZ (including its sub-formulas) does not contain modified amino acids or unnatural amino acid analogs. Therefore, peptide YZ (including its sub-formulas) may contain only unmodified amino acids, i.e., each residue is an enumerated protein constituent amino acid residue.

[0276] Detailed consideration of the invention Activation Preferably, the compound is active against hemipteran insects and / or diptera insects. Preferably, the compound is active against hemipteran insects. Therefore, the compounds of the present invention are particularly useful against hemipteran insects.

[0277] Preferably, the compound has activity against cockroach and / or lepidopteran insects.

[0278] The compounds typically increase insect mortality, for example, when applied topically to a suitable insect or ingested by a suitable insect. Therefore, the described compounds (and compositions containing them) can be considered insecticides and can be called "insect control agents."

[0279] While we do not wish to be bound by theory, some or all of the described effects may be mediated by agonist activity at kinin receptors in target insects. Examples of kinin receptors thought to be present in target insects include GPCR kinins. Preferably, the compounds of the present invention bind to one or more kinin receptors of the target insect. Preferably, the compounds of the present invention have agonist activity when bound to kinin receptors of target insects. Preferably, the compounds of the present invention bind to kinin receptors. Preferably, the compounds of the present invention are agonists of kinin receptors.

[0280] In particular, the peptide analogs described herein are thought to retain agonist activity while exhibiting superior stability, especially with respect to proteases, compared to wild-type kinin peptides. Therefore, they are considered to have excellent applicability as insecticides. Insect control agents

[0281] The term "insect control agent" refers to a substance used to increase the mortality rate of insects (i.e., as an insecticide). Any compound or composition thereof of the present invention can be considered an insect control agent and can be used as such. Preferably, the present invention provides the use of the compounds or compositions of the present invention as insect control agents for, for example, dipteran insects, hemipteran insects, cockroach insects and / or lepidopteran insects. Thus, insect control agents can be administered to increase the mortality rate of a given insect or insect population.

[0282] As used herein, an increase in mortality is intended to refer to an increase in the percentage of dead insects compared to the percentage of dead insects in an insect population that is identical except for not being exposed to the insect control agent of the present invention.

[0283] Preferably, insect mortality can be calculated as the number of dead insects per treated area / total number of insects. Preferably, the treated area may be a well on a plate, one or more leaves, or an entire plant. Preferably, insect mortality can be measured by performing the leaf immersion assay described herein in the examples.

[0284] Insecticides can be used to reduce the size of an insect population, inhibit its growth, or inhibit its feeding (for example, compared to an insect population that is identical except for not being exposed to the agent).

[0285] The insect control composition is a composition containing the described insect control agent.

[0286] Plant protection agent The term "plant protectant" refers to a substance used to protect a plant or plant part from insects, for example, from parasitism or colonization, or to serve as a food source for such insects (for example, by sap discharge). Any compound or composition thereof of the present invention can be considered a plant protectant and can be used as such. Preferably, the present invention provides the use of the compounds or compositions thereof as plant protectants for protecting plants from, for example, dipteran insects, hemipteran insects, cockroach insects and / or lepidopteran insects.

[0287] Parasitism or colonization may be carried out by larvae (or nymphs), adults, or by the use of the plant as a host or storage site for eggs. However, the terms “parasitism” and “colony formation” should not be interpreted as requiring the presence of insects that are harmful to the plant.

[0288] Plant protectants can be applied, in particular, to reduce the insect load on a plant or part of a plant, to inhibit or reduce insect infestation of plants, to inhibit an increase in the insect load on a plant or part of a plant (e.g., to reduce its rate), or to maintain a plant free of insects, compared to a plant that is identical except for having an insect population that has not been exposed to the agent. Accordingly, plant protectants can be applied to plants or parts of plants that already have hemipteran, dipteran, and / or lepidopteran insects, or to plants or parts of plants that do not have, or are substantially free of, hemipteran, dipteran, dipteran, bladderwrack, and / or lepidopteran insects.

[0289] The plant protection composition is a composition comprising a plant protection agent, i.e., the compound of the present invention described herein.

[0290] plant As used herein, “plant or part of plant” or “plant or part thereof” means any part of a plant, including but not limited to leaves, stems, roots, flowers, buds, bulbs, and seeds.

[0291] Suitable plants or parts thereof that can be protected by the compounds or compositions thereof of the present invention, or by the agents thereof, include agricultural, horticultural, or economically important crops and plants. Suitable plants include the following: Manila hemp (Musa textilis), alfalfa (Medicago sativa), Prunus dulcis, anise (Pimpinella anisum), Malus sylvestris, apricot (Prunus armeniaca), betel nut (Areca catechu), celery (Arracacia xanthorhiza), arrowroot (Maranta arundinacea), artichoke (Cynara scolymus), Jerusalem artichoke (Helianthus tuberosus), asparagus (Asparagus officinalis), avocado (Persea americona), pearl millet (Pennisetum americanum), Bambara bean (Vigna subterranean), banana (Musa paradisiaca), barley (Hordeum vulgare), kidney bean (Phaseolus) (vulgaris), kidney bean species (Phaseolus), cowpea species (vigna spp.), sugar beet (Beta vulgaris), citrus bergamia (Citrus bergamia), raspberry species (Rubus spp.), pepper (Piper nigrum), acacia mearnsii, vine species (Vaccinium spp.), Brazil nut (Bertholletia excelsa), breadfruit (Artocarpus altilis), broad bean (Vicia faba), cauliflower (Brassica oleracea botrytis), sorghum (Sorghum bicolor), Brussels sprouts (Brassica oleracea gemmifera), buckwheat (Fagopyrum esculentum), cabbage (Brassica oleracea capitate), turnip (Brassica Brassica spp. (rapa), Brassica species.), cacao (Theobroma cacao), melon (Cucumis melo), caraway (Carum carvi), cardamom (Elettaria cardamomum), cardoon (Cynara cardunculus), grasshopper (Ceratonia siliqua), carrot (Daucus carota), cashew tree (Anacardium occidentale), cassava (Manihot esculenta), castor bean (Ricinus communis), cauliflower (Brassica oleracea botrytis), celery (Apium graveolens), chayote (Sechium edule), cherry species (Prunus spp.), European chestnut (Castanea sativa), chickpea (Cicer arietinum), chicory (Cichorium intybus), chicory (Cichorium Intybus), Capsicum species, Cinnamomum verum, Cymbopogon nardus, Citron (Citrus medica), Citrus veticulata, Trifolium species, Syzygium aromaticum, Cocos nucifera, Colocasia species, Xanthosoma species, Coffee species, Cola species, Brassica napus, Zea mays, Valerianella locusta, Gossypium species, Vigna (unguiculate), Vaccinium spp., Lepidium sativum, Cucumis sativus, Ribes spp.), Annona reticulata, taro (Colocasia esculenta), date palm (Phoenix dactylifera), moringa (Moringa oleifera), kidney bean species (Phaseolus spp.), garlic (Allium sativum), onion (Allium cepa), pea (Pisum sativum), macaroni wheat (Triticum durum), xanthosoma species (Xanthosoma spp.), taro species (Colocasia spp.), eggplant (Solanum melongena), endive (Cichorium endivia), Lygeum spartum, fennel (Foeniculum vulgare), fenugreek (Trigonella foenumgraecum), fig (Ficus Carica, European hazelnut (Corylus avellane), Furcraea macrophylla, flax (Linum usitatissimum), New Zealand hemp (Phormium tenax), Pelargonium spp., Geranium spp., ginger (Zingiber officinalis), Langenaria spp., Cucurbita spp.), chickpea (Cicer arietinum), grapefruit (Citrus paradise), grape (Vitis vinifera), Lygeum spartum, timothy grass (Dactylis glomerata), peanut (Arachis hypogaea), guava (Psidium guajava), hazelnut, hemp (Cannabis sativa), Crotalaria juncea, Agave fourcroydes, Lawsonia inermis, hops (Humulus lupulus), horseradish (Armoracia rusticana), Indigofera tinctorial, Jasminum spp., Corchorus spp.), kale (Brassica oleracea acephala), kapok (Ceiba pentandra), kenaf (Hibiscus cannabinus), kohlrabi (Brassica oleracea gongylodes), Lavandula species (Lavandula spp.), leek (Allium ampeloprasum), lemon (Citrus limon), lemongrass (Cymbopogon citratus), lentil (Lens culinaris), bush clover species (Lespendeza spp.), lettuce (Lactuca sativa), licorice (Glycyrrhiza glabra), lime (Citrus aurantifolia), citrus limetta (Citrus limetta), flax (Linum usitatissimum), lychee (Litchi chinensis), loquat (Eriobotrya) Lupinus japonica, Lupinus spp., Macadamia spp.), Nutwood (Myristica fragrans), Agave atrovirens, Ponkan (Citrus reticulata), Mango (Mangifera indica), Cassava (Manihot esculenta), Rye (Secale cereal), European quince (Mespilus germanica), Melon (Cucumis melo), Millet (Penicum miliaceum), Finger millet (Eleusine coracana), Proso millet (Setaria italica), Barnyard millet (Echinochloa crusgalli), Finger millet (Eleusine coracana), Mentha spp., Morus spp., Morus alba, Agaricus spp., Pleurotus genus (spp.), Volvariella, Brassica nigra, Sinapis alba, Prunus persica, New Zealand hemp, Guizotia abyssinica, Myristica fragrans, Avena spp., Elaeis guineensis, Abelmoschus esculentus, Olea europea, Papaver somniferum, Citrus sinensis, Citrus aurantium, Dactylis glomerate, Metroxylon spp.), fan palm (Borassus flabellifer), papaya (Carica papaya), parsnip (Pastinaca sativa), European pear (Pyrus communis), pea (Pisum sativum), pecan (Carya illinoensis), chili pepper (Capsicum annuum), persimmon (Diospyros kaki), American persimmon (Diospyros virginiana), pigeon pea (Cajanus cajan), pineapple (Ananas comosus), Pistacia spp., plum (Prunus domestica), pomegranate (Punica granatum), pomegranate (Citrus grandis), potato (Solamum tuberosum), sweet potato (Ipomoea batatas), pumpkin species, white-flowered chrysanthemum (Chrysanthemum) cineraraiefolium), Aspidosperma spp., quince (Cydonia oblonga), cinchona spp., quinoa (Chenopodium quinoa), radish (Raphanus sativus (including wasabi radish (Cochlearia armoracia))), ramie (Boehmeria nivea), Agrostis spp., ramie (Boehmeria nivea), Rheum spp., rice (Oryza sativa), African rice (Oryza glaberrima), rose spp., rubber tree (Hevea brasiliensis), rye (Secale cereal), Lolium spp., safflower (Carthamus tinctorius), Sago palm species (Metroxylon spp.), Onobrychis viciifolia, Valerianella locusta, Tragopogon porrifolius, Achras sapota, Ponkan orange, Cabbage (Brassica ileracea capitate), Scorzonera hispanica, Sesamum indicum, Butyrospermum paradoxum, Agave sislana, Lime (Citrus aurantifolia), Soybean (Glycine max), Spelt wheat (Triticum spelta), Spinach (Spinacia oleracea), Rye (Secale cereal), Pumpkin species, Fragaria species, Sudan grass (Sorghum) Bicolor Sudanense), sugarcane (Saccharum officinarum), sunflower (Helianthus annuus), Crotalaria juncea, Citrus limetta, sweet potato (Iopmoea batatas), ponkan orange, Xanthosoma sagittifolium, cassava (Manihot esculenta), taro (Colocasia esculenta), tea plant (Camellia sinensis), teff (Eragrostis abyssinica), orchard grass (Phleum pratense), tobacco (Nicotiana tabacum), tomato (Lycopersicum esculentum), Lotus spp., Aleurites (spp.), turnip (Brassica rapa), Urena lobate, vanilla (Vanilla planifolia), vetch (Vicia sativa), walnut species (Juglans spp.)This may include any or part of the following: watermelon (Citrullus lanatus), acacia mearnsii, species of wheat (Triticum spp.), species of barley (Hordeum spp.), species of yam (Dioscorea spp.), and mate tea (Ilex paraguariensis).

[0292] Preferably, the plants or parts thereof that can be protected by the agent of the present invention are selected from plants that are parasitized by hemipteran, diptera and / or lepidoptera insects, or plants that attract hemipteran, diptera and / or lepidoptera insects. Preferably, the plants or parts thereof that are parasitized by hemipteran, diptera and / or lepidoptera insects, or that attract hemipteran, diptera and / or lepidoptera insects, are any of those listed above.

[0293] Preferably, the plant or part thereof that is parasitized by or attracts hemipteran insects is one of those listed above.

[0294] Preferably, the plant or part thereof that is parasitized by or attracts cockroach insects is one of those listed above.

[0295] Preferably, the plant or part thereof that is parasitized by or attracts dipteran insects is one of those listed above.

[0296] Preferably, the plant or part thereof that is parasitized by or attracts lepidopteran insects is one of those listed above.

[0297] In one embodiment, plants or parts thereof are parasitized by or attract hemipteran insects, such as cereal crops like wheat (genus *Tetramorium*), wild oats (genus *Oat*), rye (genus *Secale*), barley (genus *Barley*), rice (genus *Oryza*), and maize (genus *Zea*); apples (genus *Malus*), pears (genus *Pyrus*); strawberries (genus *Rubus*), blueberries (genus *Vaccinum*), blackberries (genus *Rubus*), raspberries (genus *Rubus*), citrus fruits (genus *Citrus*), and olives (genus *Olea*). spp.)), durian (Locusta spp.), longan fruit (Dimocarpus spp.), lychee (L. chinensis), persimmon (Diospyros spp.), beans and peas (including, but not limited to, species of the genera *Phragmites*, *Vigna*, *Pisum*, *Lens*, *Glycine*, *Cicer*, *Cajanus*, and *Arachis*), sugar beet (Beta vulgaris), sugarcane (Saccharum genus) The selection is made from or a portion thereof of fruit and vegetable crops, including spp., lettuce (Lactuca spp.), rapeseed (Brassica genus), leeks (Allium spp.), tomatoes (Solanum spp.), pepper (Capsicum spp.), asparagus (A. officinalis), melon, squash, pumpkin (Cucumis spp.), and tubers (potato) (Solanum genus).

[0298] In one embodiment, a plant or part thereof is selected from plants that are parasitized by aphids, preferably by M. persicae, or that attract them, such as Solanaceae, Cruciferae, and Leguminosae; wheat (winter wheat (Triticum aestivum) Examples include cereal crops such as wheat species (including L); peaches (Prunus species), strawberries (Ipomoea species), blueberries (Vaccinium species), blackberries (Rubus species), raspberries (Rubus species), Brassica species such as Brassica napus, lettuce (Lettuce species), tomatoes (Solanum species), peppers (Pepper species), beans and peas (including, but not limited to, cowpea and pea species), melons, squash, pumpkins (Cucumber species), citrus fruits (Citrus species), and tubers (potatoes) (Solanum species), or parts thereof. In one embodiment, the plant is a vegetable crop, preferably a Brassica species.

[0299] In one embodiment, a plant or part thereof is a plant that is parasitized by or attracts dipteran insects, such as cereals (wheat species); wild oats (oat species); rye (rye species); barley (barley species), rice (rice species) and maize (maize species); beans and peas (including, but not limited to, species of kidney beans, cowpeas, peas, lentils, soybeans, chickpeas, pigeon peas, and peanuts); apples (Malus spp.), pears (Pyrus spp.); strawberries (Fragaria spp.), blueberries (Vaccinum spp.), and blackberries (Rubus species). spp.), raspberry (Rubus spp.), cherry, plum, apricot, peach, nectarine (Prunus genus), blackcurrant, redcurrant, whitecurrant, gooseberry (Ribes spp.), kiwifruit (Actinidia spp.), papaya (Carica spp.), avocado (Persea spp.), mango (Mangifera indica L), longan fruit (Dimocarpus spp.), lychee (L. chinensis), grape (Vitis spp.), fig (Ficus genus) Fruit crops including passion fruit (Passiflora spp.), Asian pear (Pyrus species), citrus fruits (Citrus species), and olive (Olea spp.); vegetable crops including leeks (Allium species), eggplant, tomato (Solanum species), pepper (Piper species), lettuce (Lettuce species), rapeseed (Brassica species), and zucchini, melon, squash, pumpkin (Cucumber species); root vegetables of the Apiaceae family, including carrots (Daucus spp.) and American angelica (Pastinaca species), or a selection thereof.

[0300] In one embodiment, plants or parts thereof are parasitized by or attract lepidopteran insects, such as cereal crops like wheat (genus *Tetramorium*), wild oats (genus *Oat*), rye (genus *Rye*), barley (genus *Barley*), rice (genus *Rice*), and maize (genus *Maize*); apples (genus *Malus*), pears (genus *Pyrus*); nuts (e.g., almonds (*P. amygdalus*), pistachios (*Pistacia vera*), walnuts (*Juglandaceae*), hazelnuts (*Corylus*)); and avocados (*Persea*). Avocado (including Americana (Lauraceaea)), blueberry (Vaccinium genus), citrus fruits (Citrus genus), olive (Olea genus), durian (Durio spp.), longan (Longan genus), lychee (L. chinensis), persimmon (Diospyros genus); beans and peas (including, but not limited to, species of the genera *Vicia cracca*, *Vigna*, *Vicia oleracea*, *Soybean*, *Papaver rhynchophylla*, *Pea japonica*, and *Peanuta*); sugar beet (Beta The selection is made from or a portion thereof of fruit and vegetable crops, including vulgaris, sugarcane (sugarcane), lettuce (lettuce), rapeseed (rapeseed), leeks (allium), tomatoes (solanum), pepper (pepper), asparagus (asparagus (A. officinalis)), melon, squash, pumpkin (cucumber), and tubers (potato) (Solanum spp.).

[0301] insect The compounds, compositions, combinations, and agents of the present invention appropriately have activity against the insects described above. Preferably, the compounds, compositions, combinations, and agents of the present invention preferably have activity against Hemiptera, Diptera, Blattodea, or Lepidoptera insects, more preferably against Hemiptera, Diptera, or Lepidoptera insects. However, the compounds may also have activity against other insects described herein.

[0302] The compounds, compositions, and agents of the present invention may be effective against any insect. For example, from the phylum Arthropoda, particularly the class of arachnids, such as species of the genera Acarus, Aceria shedolni, Aculops, Acuulus, Amblyomma, Amphitetranychus viennensis, Argas, Boophilus, Brevipalpus, Bryobia praetiosa, Centruroides, Chorioptes, and Dermanyssus. Dermatophagoides pteronyssius, Dermatophagoides farinae, Dermacentor spp., Eotetranychus spp., Epitrimerus pyri, Eutetranychus spp., Eriophyes spp., Halotydeus destructor, Hemitarsonemus spp., Hyalomma spp., Ixodes spp., Latrodectus spp., Loxosceles spp.), Metatetranychus spp., Nupersa spp., Oligonychus spp., Ornithodorus spp., Ornithonyssus spp., Panonychus spp.These include *Phyllocoptruta oleivora*, *Polyphagotarsonemus latus*, species of the genera *Psoroptes*, *Rhipicephalus*, *Rhizoglyphus*, *Sarcoptes*, *Scorpio maurus*, *Stenotarsonemus*, *Tarsonemus*, *Tetranychus*, *Vaejovis*, and *Vasates lycopersici*.

[0303] Further examples come from the order Anoplura (Phothritaptera), such as species of the genera Damalinia, Haematopinus, Linognathus, Pediculus, Ptirus pubis, and Trichodectes.

[0304] Further examples come from the order Chilopoda, such as species of the genera Geophilus and Scutigera.

[0305] Another example comes from the order Collembola, such as Onychiurus armatus.

[0306] Further examples come from the class Diplopoda, such as Blaniulus guttulatus.

[0307] Further examples are from the Diptera order, such as species of Aedes, Agromyza, Anastrepha, Anopheles, Asphondylia, Bactrocera, Bibio hortulanus, Calliphora erythrocephala, Mediterranean fruit fly (Ceratitis capitata), Chironomida, Chrysomyia, Chrysops, and Cochliomyia. spp.), Contarinia spp., Cordylobia anthropophaga, Culex spp., Culicoides spp., Culiceta spp., Cuterebra spp., Dacus oleae, Dasyneura spp., Delia spp., Dermatobia hominis, Drosophila spp., Echinocnemus spp., Fannia spp., Gasterophilus spp.), tsetse fly species (Glossina spp.), horsefly species (Haematopota spp.), Hydrellia species (Hydrellia spp.), Hillemia species (Hylemyia spp.), Hyppobosca species (Hyppobosca spp.), cow flies (Hypoderma spp.), Liriomyza species (Liriomyza spp.), blowflies (Lucilia spp.), Lutzomia species (Lutzomia spp.), Mansonia species (Mansonia spp.), houseflies (Musca spp.), Nezara species (Nezara spp.)), Oestrus spp., Oscinella frit, Pegomyia spp., Phlebotomus spp., Phorbia spp., Phormia spp., Prodiplosis spp., Psila rosae, Rhagoletis spp., Sarcophaga spp., Simulium spp., Stomoxys spp., Tabanus spp., Tannia spp., Tetanops It is a species of the genus Tipula (spp.). Further examples come from the Heteroptera suborder, such as Anasa tristis, species of the genera Antestiopsis, Boisea, Blissus, Calocoris, Campylomma livida, Cavelerius, Cimex, Collaria, Creontiades dilutus, Dasynus piperis, Dichelops furcatus, and Diconocoris heweti. hewetti), species of the genera Dysdercus, Euschistus, Eurygaster, Heliopeltis, Horcias nobilellus, Leptocorisa, Leptoglossus phyllopus, Lygus), Macropes excavatus, Miridae family, Monalonion atratum, Nezara genus species (NeZ. aThese include species of the genus Oebalus (ra spp.), the family Pentatomidae, Piesma quadrata, Piezodorus spp., Psallus spp., Pseudacysta persea, Rhodnius spp., Sahlbergella singularis, Scaptocoris castanea, Scotinophora spp., Stephanitis nashi, Tibraca spp., and Triatoma spp. Further examples come from the suborder Homoptera, such as species of the genera Acyrthosipon, Acrogonia, Aeneolamia, Aganoscena, Aleurodes, Aleurolobus barodensis, Aleurothrixus, Amrasca, Anuraphis cardui, Aonidiella, Aphanostigma pin, and Aphis. spp.), Arboridia apicalis, Aspidiella spp., Aspidiotus spp., Atanus spp., Aulacorthum solani, Bemisia spp., Brachycaudus helichrysii, Brachycolus spp.), Brevicoryne brassicae, Calligypona marginata, Carneocephala fulgida, Ceratovacuna lanigera, Cercopidae, Ceroplastes spp., Chaetosiphon fragaefolii, Chionaspis tegalensis, Chlorita onukii, Chromaphis juglandicola, Chrysomphalus ficus, Cicadulina Coccomytilus halli, Coccus spp., Cryptomyzus ribis, Dalbulus spp., Dialeurodes spp., Diaphorina spp., Diaspis spp., Drosicha spp., Dysaphis spp., Dysmicoccus spp., Empoasca spp., Eriosoma spp., Erythroneura spp. spp.), Euscelis bilobatus, Ferrisia spp., Geococus coffeae, Hieroglyphus spp., Homalodisca coagulata, Hyalopterus arundinis, Icerya spp., Idiocerus spp., Idioscopus spp.), Laodelphax striatellus, Lecanium spp., Lepidosaphes spp., Lipaphis erysimi, Macrosiphum spp., Mahanarva spp., Melanaphis sacchari, Metcalfiella spp., Metopolophium dirhodum, Monellia costalis, Monelliopsis pecanis, Myzus spp., Nasonovia livisnigri ribisnigri), Nephotettix spp., Nilaparvata lugens, Oncometopia spp., Orthezia praelonga, Parabemisia myricae, Paratrioza spp., Parlatoria spp., Pemphigus spp., Peregrinus maidis, Phenacoccus spp., Phloeomyzus passerinii, Phorodon humuli, Phylloxera genus spp.), Pinnaspis aspidistrae, Planococcus species, Protopulvinaria pyriformis, Pseudaulacaspis pentagona, Pseudococcus species, Psylla species, Pteromalus species), species of the genera Pyrilla, Quadraspidiotus, Quesada gigas, species of Rastrococcus, species of Rhopalosiphum, species of Saissetia, Scaphoides titanus, Schizaphis graminum, Selenaspidus articulatus, species of Sogata, Sogatella furcifera, species of Sogatodes, Stictocephala These include *festina*, *Tenalaphara malayensis*, *Tinocallis caryaefoliae*, species of the genera *Tomaspis*, *Toxoptera*, *Trialeurodes*, *Trioza*, *Typhlocyba*, *Unaspis*, *Viteus vitifolii*, and species of the genera *Zygina*.

[0308] Further examples come from the Hymenoptera order, such as species of the genera Acromyrmex, Athalia, Atta, Diprion, Hoplocampa, Lasius, Monomorium pharaonis, Solenopsis invicta, Tapinoma, and Vespa.

[0309] Further examples come from the order Isopoda, such as the pill bug (Armadillidium vulgare), the woodlouse (Oniscus asellus), and the sowbug (Porcellio scaber).

[0310] Further examples come from the order Blattodea, such as the German cockroach (B. germanica), the Eastern cockroach (Blatta orientalis), the American cockroach (Periplaneta America), species of the genus Periplaneta, the brown-banded cockroach (Supella longipalpa), and the brown-banded cockroach (Supella longipalpa); as well as from the family Termitidae.

[0311] Further examples come from the order Isoptera, such as species of the genera Coptotermes, Cornitermes cumulans, Cryptotermes, Incisitermes, Microtermes obesi, Odontotermes, and Reticulitermes.

[0312] Further examples are from the order Lepidoptera, such as Acronicta major, Adoxophyes spp., Aedia leucomelas, Agrotis spp., Alabama spp., Amyelois transitella, Anarsia spp., Anticarsia spp., Argyroploce spp., Barathra brassicae, Borbo cinnara, Bucculatrix thurberiella, and Bupalus pinialius. *Pinia piniarius*, *Busseola* spp., *Cacoecia* spp., *Caloptilia theivora*, *Capua reticulana*, *Carpocapsa pomonella*, *Carposina niponensis*, *Chematobia brumata*, *Chilo* spp., *Choristoneura* spp., *Clysia ambiguella*, *Cnaphalocerus* spp., *Cnephasia* spp., *Conopomorpha* spp. spp.), Conotrachelus spp., Copitarsia spp., Cydia spp., Dalaca noctuides, Diaphania spp., Diatraea saccharalis, Earias spp.), Ecdytolopha aurantium, Elasmopalpus lignosellus, Eldana saccharina, Ephestia spp., Epinotia spp., Epiphyas postvittana, Etiella spp., Eulia spp., Eupoecilia ambiguella, Euproctis spp., Euxoa spp., Feltia spp., Galleria * Mellonella*, Gracilaria spp., Grapholitha spp., Hedylepta spp., Helicoverpa spp., Heliothis spp., Hofmannophila pseudospretella, Homoeosoma spp., Homona spp., Hyponomeuta padella, Kakivoria flavofasciata, Laphygma spp., Laspeyresia molesta, Leucinodes orbonalis * orbonalis*, *Leucoptera* spp., *Lithocolletis* spp., *Lithophane antennata*, *Lobesia* spp., *Loxagrotis albicosta*, *Lymantria* spp., *Lyonetia* spp.), Malacosoma neustria, Maruca testulalis, cutworm (Mamestra brassicae), species of the genus Mocis (Mods spp.), Mythimna separata, species of the genus Nymphula (Nymphula spp.), species of Oiketicus (Oiketicus spp.), species of Oria (Oria spp.), species of Orthaga (Orthaga spp.), species of Ostrinia (Ostrinia spp.), Oulema Oryzae, Panolis flammea, species of Parna (Parnara spp.), species of Pectinophora (Pectinophora spp.), Perileucoptera spp., Putrimaea spp., Phyllocnistis citrella, Phyllonorycter spp., Pieris spp., Platynota stultana, Plodia interpunctella, Plusia spp., Plutella xirostella, Prays spp., Prodenia spp., Protoparce spp., Pseudaletia spp., Pseudoplusia includens (includens), Pyrausta nubilalis, Rachiplusia nu, Schoenobius spp., Scirpophaga spp., Scotia segetum, Sesamia spp., Sparganothis spp., Spodoptera fulgiperda, Spodoptera spp., Stathmopoda spp.These include *Stomopteryx subsecivella*, species of *Synanthedon*, *Tecia solanivora*, *Thermesia gemmatalis*, *Tinea pellionella*, *Tineola bisselliella*, species of *Tortrix*, *Trichophaga tapetzella*, species of *Trichoplusia*, *Tuta absoluta*, and species of *Virachola*.

[0313] Further examples come from the order Orthoptera, such as Acheta domesticus, species of the genera Dichroplus, species of Grillotalpa, Leucophaea maderae, species of the genera Locusta, species of Melanoplus, the human flea (Pulex irritans), and Schistocerca gregaria.

[0314] Further examples come from the order Orthoptera, such as species of the genera Ceratophyllus, Ctenocephalides, Tunga penetrans, and Xenopsylla cheopis.

[0315] Further examples come from the Symphyla class, such as the Scutigerella spp.

[0316] Further examples come from the order Thysanoptera, such as Anaphothrips obscurus, Baliothrips biformis, Drepanothris reuteri, Enneothrips flavens, Frankliniella spp., Heliothrips spp., Hercinotorips femoralis, Rhipiphorothrips cruentatus, Scirtothrips spp., Taeniothrips cardamoni, and thrips. (spp.). Further examples come from the order Zygentoma (=Thysanura), such as Lepisma saccharina and Thermobia domestica.

[0317] hemiptera insects The compounds and compositions of the present invention preferably have activity against Hemiptera insects, including aphids, planthoppers, leafhoppers, stink bugs, shield bugs, and cicadas. Preferably, the compounds, compositions, and agents of the present invention preferably have activity against aphids.

[0318] Hemiptera are defined by a distinctive mouthpart with a "rostrum" morphology, which includes modified mandibles and mandibles that form a "caudal projection," covered within a modified labrum.

[0319] Many insects within these groups possess endogenous neuropeptides that have sequence homology to the peptides described herein, suggesting that their analogues may be active against these insects.

[0320] Insects may belong to the suborder Sternorryncha, for example, the superfamilies Aphidoidea (aphids), Aleyrodoidea (whiteflies), Coccoidea (scale insects), Phylloxeroidea (including the families Phylloxeridae or "phylloxerans" and Adelgidae or woolly conifer aphids), or Psylloidea (psyllids, etc.).

[0321] Therefore, the insect may be an aphid, that is, a member of the superfamily Aphidoidea. Aphids (order Hemiptera: superfamily Aphidoidea) are agricultural pests. 38 It is one of the most important groups of plant viruses, and all plant viruses transmitted by insects. 39Aphids are vectors in approximately 50% of infections. Within that superfamily, aphids belong to the subfamilies Aiceoninae, Anoeciinae, Aphidinae, Baltichaitophorinae, Calaphidinae, Chaitophorinae, Drepanosiphinae, Eriosomatinae, Greenideinae, Hormaphidinae, Israelaphidinae, Lachninae, and Li It may also be a part of the Aphididae family, including the subfamilies zeriinae, Macropodaphidinae, Mindarinae, Neophyllaphidinae, Phloeomyzinae, Phyllaphidinae, Pterastheniinae, Saltusaphidinae, Spicaphidinae, Taiwanaphidinae, Tamaliinae, and Thelaxinae.

[0322] Aphids include, for example, genera Acyrthosiphon (e.g., pea aphid), Aphis (e.g., cotton aphid (Aphis gossypii), Aphis glycines), Diuraphis (e.g., Diuraphis noxia), Macrosiphum (e.g., Macrosiphum rosae, Macrosiphum euphorbiae) It may also be a genus of euphorbiae, Myzus (e.g., Myzus persicae), Rhopalosiphum (e.g., the wheat aphid), or Sitobion (e.g., Sitobion avenae).

[0323] The peach aphid (Mizusu persicae) is the most economically important aphid crop pest worldwide, with a global distribution and host range spanning over 400 species within 40 different plant families. For example, it is a major pest of agricultural crops including fruits and potatoes, and acts as a viral vector.

[0324] Macrosihum rosae (rose aphid) is a major horticultural pest, particularly of cultivated roses, and is a vector for the transmission of 12 plant viruses, including the strawberry mild yellow edge virus.

[0325] Cotton aphids (also known as cotton or melon aphids) are pests of the Cucurbitaceae family and cotton plants.

[0326] Other insects besides aphids may include, for example, those belonging to the family Adelgiidae, such as the genus Adelges (e.g., Adelges tsugae).

[0327] The insect may belong to the family Aleyrodidae, for example, the genus Bemisia (e.g., Bemisia tabaci) or the genus Trialeurodes (e.g., Trialeurodes vaporariorum).

[0328] The insect may belong to the superfamily Psyllidoidea, for example, the genus Pachypsylla (e.g., Pachypsylla venusta).

[0329] As an example of a hemipteran insect other than the suborder Stomachrophora, the insect may belong to the family Cimicidae, for example, the genus Cimex, for example, Cimex lectularius.

[0330] The insects may belong to the family Cicadellidae, for example, the genera Cuerna (e.g., Cuerna arida), Graminella (e.g., Graminella nigrifrons), and Homalodisca (e.g., Homalodisca vitripennis). The family Cicadellidae also includes the two-spotted green leafhopper.

[0331] The insect may be a part of the family Delphacidae, for example, the genus Nilaparvata (e.g., the brown planthopper) or the genus Sogatella (e.g., the white-backed planthopper). For example, the brown planthopper (Nilaparvata lugens) is a pest of rice crops, particularly in Asia.

[0332] The insect may belong to the family Liviidae, for example, the genus Diaphorina (e.g., the citrus psyllid (Diaphorina citri)).

[0333] The insects may be from the family Miridae, for example, the genera Pseudatomoscelis (e.g., Pseudatomoscelis seriatus), Lygus (e.g., Lygus hesperus), or Tupiocoris (e.g., Tupiocoris notatus). For example, Pseudatomoscelis seriatus (the cotton flea beetle) is a pest of cotton.

[0334] The insects belong to the family Pentatomidae, for example, the genera Acrosternum (e.g., Acrosternum hilare), Banasa (e.g., Banasa dimidiata), Euschistus (e.g., Euschistus servus, Euschistus heros), Halyomorpha (e.g., Halyomorpha halis), Murgantia (e.g., Murgantia histrionica), Nezara (e.g., Nezara viridula), and Plautia (e.g., Plautia stari). It may also be a species of the genus Podisus (e.g., Podisus maculiventris). For example, Acrosternum hilare (green stink bug) is a major pest of cotton. Euscistus cerus (brown stink bug) is a pest of many crops, including seeds, grains, nuts and fruits, especially in the southern United States. Southern green stink bug is a pest of cereal and soybean crops, especially in Brazil.

[0335] The insect may belong to the family Pyrrhocoridae, for example, the genus Pyrrhocoris (e.g., Pyrrhocoris apterus).

[0336] The insect may belong to the family Reduviidae, for example, the genus Rhodnius (e.g., Rhodnius prolixus), or the genus Triatoma (e.g., the Brazilian assassin bug Triatoma infestans). Rhodnius prolixus is a vector for human disease (Chagas disease).

[0337] The insect may belong to the family Triozida, for example, the genus Acanthocasuarina (e.g., Acanthocasuarina muellerianae).

[0338] In one embodiment, the insect can be selected from the following species: H. harris, E. heros, A. hilare, cotton aphid, E. celus, M. persicae, southern green stink bug, brown planthopper, P. ceriatus, and R. prolyxus.

[0339] In one embodiment, the insect is a brown planthopper. In one embodiment, the compounds, compositions, and agents of the present invention may have activity against brown planthoppers.

[0340] In one embodiment, the insect is of the M. persicae species. In one embodiment, the compounds, compositions, and agents of the present invention may have activity against M. persicae.

[0341] Diptera insects The compounds and compositions of the present invention may be active against Diptera insects.

[0342] In particular, it may be active against fruit flies, including those of the Drosophilidae family and the Drosophila genus such as Drosophila melanogaster. It may also be active against insects of the Tephritidae family, including those of the genera Anastrepha, Bactrocera, Ceratitis, Dacus, Rhagoltis, and Tephritis.

[0343] The families Drosophilidae and Tephritidae are collectively known as fruit flies.

[0344] This compound is found in flies of the family Chloropteridae (chloropter flies) and the following genera: Phytomyza genus (e.g., Phytomyza angelicastri); The genus Melani (e.g., Melani agromyza); The genus Antherigona (for example, species of the genus Antherigona (Antherigona spp)); The genus Delia (for example, Delia radicum); The genus Contarinia (e.g., Contarinia sorghicola); It may also possess activity against other important dipteran pests such as flies.

[0345] For further details on these and other examples, see Developing the Arsenal Against Pest and Vector Dipterans: Inputs of Transgenic and Paratransgenic Biotechnologies, Ogaugwu and Durvasula, IntechOpen, 2017: DOI:10.5772 / 66440.

[0346] Cockroach insects The compounds, compositions, and agents of the present invention may be active against cockroach insects of the order Blattodea, such as German cockroaches, Eastern cockroaches, American cockroaches, and brown-banded cockroaches.

[0347] In particular, it may have activity against insects of the genus Blatella. Preferably, the compounds, compositions, and agents of the present invention may have activity against the German cockroach.

[0348] In one embodiment, the compounds, compositions, and agents of the present invention may have activity against German cockroaches.

[0349] Lepidopteran insects The compounds, compositions, and agents of the present invention may be active against lepidopteran insects.

[0350] In particular, the compounds, compositions, and agents of the present invention may be active against insects of the genera Heliothis, Plutella, Spodoptera, and Cydia. Preferably, the compounds, compositions, and agents of the present invention may be active against the following species: Heliothis peltigera, H. virescens, Spodoptera species, Spodoptera fulgiperda, and Cydia pomonella (codling moth), larvae of Heliothis species including peltigera and virescens, Spodoptera littoralis (these represent a very diverse group of Heliothinae and Spodoptera moth species, which are agricultural pests worldwide), and Plutella xirostella (diamondback moth, the most important global pest of the Brassica genus).

[0351] In one embodiment, the compounds, compositions, and agents of the present invention may have activity against Plutella xirostella.

[0352] In one embodiment, the compounds, compositions, and agents of the present invention may have activity against Spodoptera flugiperda.

[0353] household pests The compounds, compositions, and agents of the present invention may also be active against household pests such as cockroaches and termites (termites of the Termitidae family, etc.). Among more than 3,000 species, these may include German cockroaches, Eastern cockroaches (Blatta orientalis), American cockroaches (Periplaneta americana), and brown-banded cockroaches (Supella longipalpa). Cockroaches are common household pests worldwide and can transmit various diseases. Control of these and other household pests (e.g., ants) is envisioned by treating surfaces where insects crawl, particularly with bait containing the compounds, compositions, and agents of the present invention, and by direct spray application of the compounds, compositions, and agents of the present invention.

[0354] Therefore, further embodiments of the present invention may include bait comprising the compound or composition of the present invention, preferably which may be bait for household pests. Further embodiments of the present invention may include methods for controlling household pests, reducing the population of household pests, suppressing the population of household pests, or increasing the mortality rate of household pests, the methods comprising the steps of treating a surface that household pests come into contact with (e.g., wood) with the compound or composition of the present invention, or bringing household pests into contact with the compound or composition of the present invention. Further details of such methods are described below. Optionally, the treatment or contact may include preferred application means such as spraying, as described elsewhere in this specification. Therefore, preferably, sprayable formulations comprising the compound or composition of the present invention are also envisioned. Preferred formulations are described elsewhere in this specification.

[0355] Method and Use of the Invention How to increase insect mortality The present invention provides a method for increasing insect mortality, comprising the step of contacting an insect or insect population with a compound, composition, or combination described herein. The insect or insect population may be a Hemiptera, Diptera, and / or Lepidoptera insect. The insect or insect population may also be a Blattodea insect.

[0356] In one embodiment, a method is provided for increasing the mortality rate of diptera insects, comprising the step of contacting diptera insects or a population of diptera insects with a compound, composition, or combination of the present invention.

[0357] In one particular embodiment, a method is provided for increasing the mortality rate of Drosophila suzukii insects or insect populations, comprising the step of contacting the Drosophila suzukii insects or insect populations with the compound, composition or combination of the present invention.

[0358] In one embodiment, a method is provided for increasing the mortality rate of hemipteran insects, comprising the step of contacting a hemipteran insect or a population of hemipteran insects with a compound or composition defined herein.

[0359] In one particular embodiment, a method is provided for increasing the mortality rate of aphids, comprising the step of contacting aphid insects or insect populations with a compound, composition or combination as defined herein.

[0360] In one particular embodiment, a method is provided for increasing the mortality rate of the bean aphid (Aphis fabae), pea aphid (Aphis fabae), peach aphid (Myzus persicae), two-spotted green leafhopper (Myzus persicae), or wheat aphid (Myzus persicae), comprising the step of contacting the insect or insect population with a compound, composition, or combination defined herein.

[0361] In one particular embodiment, a method is provided for increasing the mortality rate of *Thuidium persicae* insects or insect populations, comprising the step of contacting *Thuidium persicae* insects or insect populations with a compound or composition defined herein.

[0362] In one particular embodiment, a method is provided for increasing the mortality rate of wheat aphids, comprising the step of contacting wheat aphid insects or insect populations with a compound, composition or combination defined herein.

[0363] In one embodiment, a method is provided for inhibiting plant parasitism by brown planthoppers, comprising the step of contacting a plant with a compound or composition defined herein.

[0364] In one particular embodiment, a method is provided for increasing the mortality rate of brown planthoppers, comprising the step of contacting a brown planthopper insect or a population of insects with a compound, composition, or combination as defined herein.

[0365] In one particular embodiment, a method is provided for increasing the mortality rate of the two-spotted green leafhopper insect or insect population, comprising the step of contacting the two-spotted green leafhopper insect or insect population with a compound, composition or combination as defined herein.

[0366] In one embodiment, a method is provided for increasing the mortality rate of lepidopteran insects, comprising the step of contacting a lepidopteran insect or a population of lepidopteran insects with a compound or composition of the present invention.

[0367] In one particular embodiment, a method is provided for increasing the mortality rate of Plutella xirostera insects or insect populations, comprising the step of contacting the insects with a compound, composition, or combination defined herein.

[0368] In one particular embodiment, a method is provided for increasing the mortality rate of Spodoptera fulgiperda insects or insect populations, comprising the step of contacting the insects or insect populations with a compound, composition or combination defined herein.

[0369] In one embodiment, a method is provided for increasing the mortality rate of cockroach insects, comprising the step of contacting a population of cockroach insects or lepidopteran insects with a compound, composition, or combination defined herein.

[0370] In one particular embodiment, a method is provided for increasing the mortality rate of German cockroaches, comprising the step of contacting a German cockroach insect or a population of insects with a compound, composition or combination as defined herein.

[0371] Methods for inhibiting or reducing parasitic growth of plants or land. In one embodiment, a method is provided for inhibiting parasitism of plants by dipteran insects, comprising the step of contacting a plant with a compound or composition of the present invention.

[0372] In one embodiment, a method is provided for inhibiting parasitism of plants by hemipteran insects, comprising the step of contacting a plant with a compound or composition defined in the present invention.

[0373] In one particular embodiment, a method is provided for increasing the mortality rate of *Thuidium persicae* insects or insect populations, comprising the step of contacting *Thuidium persicae* insects or insect populations with a compound or composition defined herein.

[0374] In one embodiment, a method is provided for inhibiting plant parasitism by Mizusu persicae, comprising the step of contacting a plant with a compound or composition defined in the present invention.

[0375] In one particular embodiment, a method is provided for inhibiting plant parasitism by Mizusu persicae, comprising the step of contacting a plant with a compound or composition defined in the present invention.

[0376] In one particular embodiment, a method is provided for increasing the mortality rate of the two-spotted green leafhopper insect or insect population, comprising the step of contacting the two-spotted green leafhopper insect or insect population with a compound or composition defined herein.

[0377] In one embodiment, a method is provided for inhibiting plant parasitism by the two-spotted green leafhopper, comprising the step of contacting the plant with a compound or composition defined in the present invention.

[0378] In one particular embodiment, a method is provided for increasing the mortality rate of Halyomorph halys, comprising the step of contacting Halyomorph halys insects or populations of insects with a compound or composition defined herein.

[0379] In one embodiment, a method is provided for inhibiting plant parasitism by Hariomorpa haris, comprising the step of contacting a plant with a compound or composition defined in the present invention.

[0380] In one particular embodiment, a method is provided for increasing the mortality rate of *Hariomorpa haris* insects or insect populations, comprising the step of contacting them with a compound or composition defined herein.

[0381] In one particular embodiment, a method is provided for inhibiting plant parasitism by Hariomorpa haris, comprising the step of contacting a plant with a compound or composition defined in the present invention.

[0382] In one embodiment, a method is provided for inhibiting parasitism of plants by lepidopteran insects, comprising the step of contacting a plant with a compound or composition of the present invention.

[0383] In one embodiment, a method is provided for inhibiting plant parasitism by Plutella xirostella, comprising the step of contacting a plant with a compound or composition defined in the present invention.

[0384] In one particular embodiment, a method is provided for increasing the mortality rate of Plutella xirostera insects or insect populations, comprising the step of contacting the insects with a compound, composition, or combination defined herein.

[0385] In one particular embodiment, a method is provided for inhibiting plant parasitism by Plutella xirostella, comprising the step of contacting a plant with a compound or composition defined in the present invention.

[0386] In one embodiment, a method is provided for inhibiting plant parasitism by Spodoptera fulgiperda, comprising the step of contacting a plant with a compound or composition defined in the present invention.

[0387] In one particular embodiment, a method is provided for increasing the mortality rate of Spodoptera fulgiperda insects or insect populations, comprising the step of contacting the insects or insect populations with a compound, composition or combination defined herein.

[0388] In one particular embodiment, a method is provided for inhibiting plant parasitism by Spodoptera fulgiperda, comprising the step of contacting a plant with a compound or composition defined in the present invention.

[0389] Preferably, contact may include, for example, feeding or spraying. Preferably, feeding may be facilitated by a bait attractant that may be included in the composition of the present invention, as described below.

[0390] The method of the present invention may further include the step of contacting an insect population or plant with a further insecticide, such as those described herein. Preferably, the insecticide is a further kinin analog.

[0391] Application of the compound of the present invention The present invention provides a method for increasing insect mortality, comprising the step of contacting an insect or a group of insects with a compound described herein. The insect or group of insects may be Diptera, Hemiptera, or Lepidoptera. The insect or group of insects may be Blattodea.

[0392] The present invention further provides a method for reducing insect feeding, comprising the step of contacting an insect or a group of insects with a compound described herein. Preferably, it reduces insect feeding of a plant or a part of a plant. The insect or group of insects may also be insects of the genus Drosophila.

[0393] The compound can be applied directly to insects or insect populations. For example, the compound can be applied topically. Alternatively, the compound can be applied indirectly. For example, it can be applied to a substrate that may come into contact with insects or insect populations. The substrate may be a plant or plant part, and in particular a plant or plant part that represents hemipterans or diptera, which are pests of plants (crops or horticultural plants).

[0394] However, for insects that are representative of human pests that are vectors of human diseases, such as bed bugs (e.g., bed bugs of the genus *Lysimachia*) or assassin bugs (e.g., *Rhodonius* of the genus *Lysimachia*, or *Triatoma* of the genus *Rhodonius prolyxus*, or *Triatoma* of the genus *Triatoma*, etc.), the substrate may be a household surface or article such as bedding, mattresses, or any other suitable household surface (e.g., wood). The compound can be applied to the substrate in a form suitable for ingestion by insects.

[0395] The present invention further provides the use of the described compounds as plant protectants, specifically for protecting plants or plant parts from Hemiptera, Diptera, Blattodea and / or Lepidoptera insects, preferably Hemiptera, Diptera and / or Lepidoptera insects.

[0396] The present invention further provides a method for inhibiting parasitism of plants or plant parts by hemipteran, dipteran, bladderwrack and / or lepidopteran insects, preferably hemipteran, dipteran and / or lepidopteran insects, comprising the step of contacting a plant or plant part with a compound described herein.

[0397] This method may also be preventative. For example, the compound can be applied to the plant or plant part while the plant or plant part is free from, or substantially free from, hemipteran, dipteran, cockroach and / or lepidopteran insects, preferably hemipteran, dipteran and / or lepidopteran insects.

[0398] Alternatively, the plant or plant part may already be colonized or parasitized by insects of the order Hemiptera, Diptera, Blattodea and / or Lepidoptera, preferably Hemiptera, Diptera and / or Lepidoptera. Accordingly, the present invention further provides a method for reducing parasitism to a plant or plant part, or a method for reducing the load on a plant or plant part by insects, such as Hemiptera, Diptera and / or Lepidoptera, comprising the step of contacting the plant or plant part with the compound described.

[0399] In any of these embodiments, the compound may be provided as part of a composition such as an insect control composition (e.g., an insecticide composition) or a plant protection composition. Therefore, references to the application or use of the compound should be interpreted as encompassing the application or use of the appropriate composition, unless the context should otherwise indicate otherwise.

[0400] The composition typically comprises the compound described in combination with one or more auxiliary components such as solvents, carriers, diluents, adjuvants, preservatives, dispersants, emulsifiers, or synergists.

[0401] The composition may further comprise one or more additional active insecticides described herein.

[0402] The present invention further provides compositions comprising a compound of the present invention mixed with one or more solvents, carriers, diluents, auxiliaries, preservatives, dispersants, emulsifiers, or synergists, such as insect control compositions or plant protection compositions. The compositions may be aqueous compositions.

[0403] This method may be preventative. For example, the compound can be applied to a plant, a plant part, or the land while there are no or substantially no insects in the plant or plant part or the field.

[0404] Preferably, the site may be any agricultural land suitable for growing plants. Preferably, the site may be suitable for growing plants, or any area or place where plants grow. Suitable sites may include farmland, brownfields, fields, greenhouses, conservatories, containers, aquaponics and hydroponic systems, etc. In one embodiment, the site is a field.

[0405] Alternatively, the plant or part of the plant or the land may already be colonized or parasitized by insects, preferably Hemiptera, Diptera, Blattodea and / or Lepidoptera.

[0406] Accordingly, the present invention further provides a method for reducing insect infestation of plants or plant parts, or for reducing the insect load on plants or plant parts, comprising the step of contacting the plants or plant parts with the compounds, compositions, or combinations described herein. The present invention also provides a method for reducing insect infestation of fields, or for reducing the insect load on fields, comprising the step of contacting the fields with the compounds, compositions, or combinations described herein. Preferably, the insects are Hemiptera, Diptera, Blattodea and / or Lepidoptera.

[0407] Methods to reduce insect consumption The present invention further provides a method for reducing insect feeding, comprising the step of contacting an insect or a group of insects with a compound, composition, or combination described herein. Preferably, the method reduces insect feeding of a plant or part of a plant. The insect or group of insects may be hemipterans, diptera, bladderworts, and / or lepidopterans.

[0408] How to protect plants from insects The present invention further provides a method for protecting plants or parts thereof from insects or insect parasites, specifically a method for protecting plants or parts of plants from hemipteran, dipteran, cockroach, and / or lepidopteran insects or their parasites, the method comprising the step of directly or indirectly applying the insecticidal compound or composition or combination of the present invention to the plant or part of the plant. Preferably, the indirect application step may include applying the compound or composition or combination of the present invention to a field or place where plants are growing or where plants are intended to grow.

[0409] The present invention also provides a post-harvest treatment method for protecting or treating harvested plants or harvested parts of plants against insects or insect parasites, specifically Hemiptera, Diptera, Blattodea and / or Lepidoptera insects or their parasites, comprising the step of directly or indirectly applying an insecticidal compound or composition or combination of the present invention to the harvested plants or harvested parts of plants under conditions effective for protecting or treating the harvested plants or harvested parts of plants against insects. Preferably, the indirect application step may include applying the compound or composition or combination of the present invention to a place where the plants or harvested parts of plants are stored or intended to be stored.

[0410] Preferably, the insects may be from the orders Hemiptera, Diptera, Blattodea, and / or Lepidoptera.

[0411] The present invention provides the use of the compounds described herein as insect control agents in a method for increasing the mortality rate of insects encoding kinin peptides, or for inhibiting plant parasitism by insects encoding kinin peptides.

[0412] Methods for bringing insects into contact One embodiment provides a method for contacting insects with a compound, preferably an insecticide, and more preferably an insecticide, the method comprising the step of applying the compound, composition, or combination according to the present invention to a site or site frequently visited by insects.

[0413] The site frequently visited by insects may be a natural habitat for insects or a place regularly visited by insects. This site can then be treated with the compound or composition described above, and as a non-limiting example, a mosquito net impregnated with encapsulated insecticide can be used as a method of application. Alternatively, the site may be created by the application of a visual decoy or attractant for insects. Visual decoys are known to those skilled in the art and include, but are not limited to, light sources, colored objects, and shapes or silhouettes that stand out against a contrasting background. As mentioned above, insect attractants include, but are not limited to, pheromones, kairomones, and allomones. The attractant may be present in the composition or may be applied separately from the compound or composition or combination to ensure that insects are reliably attracted to the site to which the compound or composition or combination is applied.

[0414] Preferably, the insects may be from the orders Hemiptera, Diptera, Blattodea, and / or Lepidoptera.

[0415] Specific embodiments of the present invention In certain embodiments, compounds of formula (Ia) are found to have specific use as insecticides against dipteran insects (e.g., Drosophila melanogaster). Preferably, compounds of formula (Ia) are those listed in the following table: [Table 7] Or selected from one or more of its salts or solvates.

[0416] In certain embodiments, compounds of formula (Ib) are found to have specific use as insecticides against hemipteran insects (e.g., *Hymenomorpha harris* and *Camponotus persicae*). Preferably, compounds of formula (Ib) are those listed in the following table: [Table 8] Or selected from one or more of its salts or solvates.

[0417] In certain embodiments, compounds of formula (Ic) are found to have specific use as insecticides against lepidopteran insects (e.g., Plutella xirostera or Spodoptera fulgiperda). Preferably, compounds of formula (Ic) are those listed in the following table: [Table 9] Or selected from one or more of its salts or solvates.

[0418] In certain embodiments, the compounds used for use against lepidopteran insects (e.g., Spodoptera fulgiperda) are the compounds listed in the table below: [Table 10] Or selected from one of its salts or solvates.

[0419] In certain embodiments, the compounds used for use against Hemiptera insects (e.g., brown planthoppers) are the compounds listed in the table below: [Table 11] Or selected from one of its salts or solvates.

[0420] In certain embodiments, the compounds used for use against insects of the order Blattodea (e.g., German cockroaches) are the compounds listed in the table below: [Table 12] Or selected from one of its salts or solvates.

[0421] Application of compounds or compositions The compounds, compositions, or combinations of the present invention can be brought into contact with insects or insect populations, preferably including direct application of the compounds, compositions, or combinations to insects or insect populations. For example, the compounds can be applied locally. Alternatively, the compounds, compositions, or combinations can be applied indirectly. For example, they can be applied to substrates, land, or locations that are likely to come into contact with insects or insect populations. The substrate may be a plant or plant part, particularly a plant or plant part for hemipterans, diptera, or lepidoptera that represent pests of plants (crops or horticultural plants), or preferably a field, place, or area where plants grow. Therefore, preferably, the compounds, compositions, or combinations can be applied to plants or plant parts. Therefore, preferably, the compounds, compositions, or combinations can be applied to land where plants grow.

[0422] However, for insects that represent human pests and may be vectors of human diseases, such as bed bugs (e.g., bed bugs of the genus *Lysimachia*, etc.) or assassin bugs (e.g., *Rhodonius*, etc., or *Triatoma*, etc., such as the Brazilian assassin bug), the substrate may be a household surface or article such as bedding, mattresses, or any other suitable household surface. The compound or composition can be applied to the substrate in a form suitable for ingestion by insects.

[0423] Preferably, contact may include, for example, feeding or spraying. Preferably, feeding may be facilitated by a bait attractant that may be included in the composition of the present invention, as described below.

[0424] This method may include a step of directly or indirectly contacting or applying a compound, composition, or combination disclosed herein to a plant or a part of a plant at a rate higher than, for example, 5 g of the compound per hectare, 10 g of the compound per hectare, 24 g of the compound per hectare, 50 g of the compound per hectare, 75 g of the compound per hectare, 100 g of the compound per hectare, or in particular, 200 g of the compound per hectare, etc. These methods may include a step of directly or indirectly applying to a plant or a part of a plant a compound, composition, or combination disclosed herein at a rate of, for example, 5 g to 100 g of the compound, composition, or combination per hectare, for example, but not limited to, 5 g to 200 g of the compound, composition, or combination per hectare, in particular, 5 g to 50 g of the compound, composition, or combination per hectare, for example, 5 g to 30 g of the compound, composition, or combination per hectare, or 10 g to 25 g of the compound, composition, or combination per hectare.

[0425] The compounds, compositions, or combinations disclosed herein may be applied directly or indirectly to plants or parts of plants after harvest, optionally by spraying, atomizing, foaming, fogging, hydroculture, hydroponics, coating, dipping, and / or covering. Preferably, contact may include, for example, feeding or spraying. In some embodiments, contact is by feeding.

[0426] Preferably, the compound can be brought into contact with insects or insect populations, or plants or plant parts, at any effective concentration. Preferably, compositions and combinations may contain such effective concentrations of the compound. Preferably, the concentration of the compound is 10 -3 ~10 -9 M, appropriately 10 -4 ~10 -6 M, preferably 10 -4 ~10 -5 It is M.

[0427] Use as a plant protectant The present invention further provides the use of compounds, compositions, or combinations described herein as plant protectants, specifically for protecting plants or plant parts from insects, preferably Hemiptera, Diptera, Blattodea and / or Lepidoptera insects, and more preferably Hemiptera, Diptera and / or Lepidoptera insects. In the foregoing, plant protectants are further described herein.

[0428] Use as an insect control agent The present invention provides, in particular, the use of the compounds or compositions described herein, or combinations thereof, as insect control agents in methods for increasing insect mortality or inhibiting insect parasitism of plants.

[0429] The present invention also provides the use of the compounds described herein as insecticides in a method for increasing the mortality rate of hemipteran, dipteran, and / or lepidopteran insects, or in a method for inhibiting plant parasitism by hemipteran, dipteran, dipteran, cockroach, and / or lepidopteran insects. Preferably, the present invention relates in particular to the use of the compounds described herein as insecticides in a method for increasing the mortality rate of hemipteran insects, or in a method for inhibiting plant parasitism by hemipteran, dipteran, dipteran, cockroach, and / or lepidopteran insects.

[0430] The present invention also provides the use of the compounds or compositions described herein, or combinations thereof, as insect control agents, particularly by having a biological inhibitory effect on Hemiptera, Diptera, Blattodea and / or Lepidoptera insects, a biocicidal effect on Hemiptera, Diptera, Blattodea and / or Lepidoptera insects, and / or an insecticidal effect on Hemiptera, Diptera, Blattodea and / or Lepidoptera insects.

[0431] As used herein, “biosuppression (effect)” or “biosuppressive use” includes any effect or use of the compounds, compositions, or combinations described herein (which may be included in the biosuppression, biocidal, fungicidal, or fungistatic compositions as defined herein) for controlling, regulating, or interfering with the harmful activity of pests such as plant pests or plant pathogens. Preferably, the pests are insects of the orders Hemiptera, Diptera, Blattodea, and / or Lepidoptera. Preferably, this includes, but is not limited to, inhibiting the growth or activity of insects, altering the behavior of insects, and repelling or attracting insects in plants, plant parts, or other agricultural-related environments such as in household use or in soil.

[0432] As used interchangeably herein, “insecticidal activity” or “biocidal activity” means killing or severely incapacitating pests. Preferably, the insecticidal activity may be the same as that which applies when the pest is an insect. Preferably, the compound, composition, or combination may be intended for use as an insect control agent in which insects encode kinin peptides.

[0433] Preferably, the compound may be used as an insect control agent for insects of the order Diptera. Preferably, the compound may be used as an insect control agent for insects of the genus Drosophila. Preferably, the compound may be used as an insect control agent for insects of the genus Drosophila.

[0434] In some embodiments, the compound for use against dipteran insects is one of the specific compounds described herein.

[0435] Preferably, the compounds or compositions defined herein may be used as insect control agents for insects of the order Hemiptera.

[0436] Preferably, the compounds, compositions, or combinations defined herein may be used as insect control agents for insects that are aphids.

[0437] Preferably, the compounds or compositions defined herein may be used as insect control agents for insects of the genus *Campsis*. Preferably, the compounds or compositions defined herein may be used as insect control agents for insects of the genus *Campsis persicae*.

[0438] Preferably, the compounds or compositions defined herein may be used as insect control agents for insects of the family Cicadellidae. Preferably, the compounds or compositions defined herein may be used as insect control agents for insects of the species *Euphyllia japonica*.

[0439] Preferably, the compounds or compositions defined herein may be used as insect control agents for insects of the genus Halyomorpha. Preferably, the compounds or compositions defined herein may be used as insect control agents for insects of Halyomorpha harris.

[0440] In some embodiments, the compound for use against hemipteran insects is one of the specific compounds described herein.

[0441] Preferably, the compound may be used as an insect control agent for insects of the order Lepidoptera.

[0442] Preferably, the compounds or compositions defined herein may be used as insect control agents for insects of the genus Plutella. Preferably, the compounds or compositions defined herein may be used as insect control agents for insects of the genus Plutella xirostella.

[0443] In some embodiments, the compound for use against lepidopteran insects is one of the specific compounds described herein.

[0444] Preferably, the compounds, compositions, or combinations defined herein may be used as insect control agents for insects of the order Blattodea. Preferably, the compounds, compositions, or combinations defined herein may be used as insect control agents for insects of the order Cockroaches or termites.

[0445] Methods for controlling insect reproductive capacity The present invention also provides insecticidal compounds, compositions, and combinations described herein for controlling the reproductive capacity of insect species. Preferably, the insect is selected from hemipterans, diptera, or lepidoptera, for example, those described herein. Preferably, in some embodiments, the hemipteran insect is *Drosophila*. Preferably, in some embodiments, the diptera insect is *Drosophila melanogaster*. Preferably, in some embodiments, the lepidoptera insect is *Plutella xirostera*.

[0446] A method for controlling the reproductive capacity of hemipteran insects is also provided, which includes the step of contacting a compound or composition of the present invention with a substrate, such as a plant or soil. Preferably, the hemipteran insect is any of those disclosed herein, such as aphids.

[0447] A method for controlling the reproductive capacity of dipteran insects is also provided, which includes the step of bringing a compound or composition of the present invention into contact with a substrate, such as a plant or soil. Preferably, the dipteran insect is any of those disclosed herein.

[0448] A method for controlling the reproductive capacity of lepidopteran insects is also provided, which includes the step of contacting a compound or composition of the present invention with a substrate, such as a plant or soil. Preferably, the lepidopteran insect is any of those disclosed herein.

[0449] A method for controlling the reproductive capacity of cockroach insects is also provided, which includes the step of contacting a compound or composition of the present invention with a substrate, such as a plant or soil. Preferably, the cockroach insect is any of those disclosed herein.

[0450] A method for controlling the reproductive capacity of hemipteran insects is also provided, which includes the step of contacting a substrate, such as a plant or soil, with the combination described herein. Preferably, the hemipteran insect is one of those disclosed herein. Preferably, the combination includes the compounds of the present invention and kinin peptides or analogs thereof.

[0451] A method for controlling the reproductive capacity of dipteran insects is also provided, which includes the step of bringing the combination described herein into contact with a substrate, such as a plant or soil. Preferably, the dipteran insect is one of those disclosed herein. Preferably, the combination includes the compounds of the present invention and kinin peptides or analogs thereof.

[0452] A method for controlling the reproductive capacity of lepidopteran insects is also provided, which includes the step of contacting a substrate, such as a plant or soil, with the combination described herein or a composition of the present invention. Preferably, the lepidopteran insect is one of those disclosed herein. Preferably, the combination includes the compounds of the present invention and kinin peptides or analogs thereof.

[0453] A method for controlling the reproductive capacity of cockroach insects is also provided, which comprises the step of contacting a substrate, such as a plant or soil, with the combination described herein or a composition of the present invention. Preferably, the cockroach insect is one of those disclosed herein. Preferably, the combination comprises the compounds of the present invention and kinin peptides or analogs thereof.

[0454] A method for controlling the reproductive capacity of hemipteran insects or insect populations is also provided, which includes the step of contacting a hemipteran insect or insect population with a compound or composition of the present invention. Preferably, the hemipteran insect is any of those disclosed herein.

[0455] A method for controlling the reproductive capacity of a dipteran insect or insect population is also provided, which includes the step of contacting a compound or composition of the present invention with a dipteran insect or insect population. Preferably, the dipteran insect is any of those disclosed herein.

[0456] A method for controlling the reproductive capacity of lepidopteran insects or insect populations is also provided, which includes the step of contacting a lepidopteran insect or insect population with a compound or composition of the present invention. Preferably, the lepidopteran insect is any of those disclosed herein.

[0457] A method for controlling the reproductive capacity of hemipteran insects or insect populations is also provided, which includes the step of contacting the hemipteran insects or insect populations with the combination described herein. Preferably, the hemipteran insects are any of those disclosed herein. Preferably, the combination includes the compounds of the present invention and kinin peptides or analogs thereof.

[0458] A method for controlling the reproductive capacity of a dipteran insect or insect population is also provided, which includes the step of contacting the dipteran insect or insect population with the combination described herein. Preferably, the dipteran insect is any of those disclosed herein. Preferably, the combination includes the compounds of the present invention and kinin peptides or analogs thereof.

[0459] A method for controlling the reproductive capacity of lepidopteran insects or insect populations is also provided, which comprises the step of contacting a lepidopteran insect or insect population with the combination described herein or a composition of the present invention. Preferably, the lepidopteran insect is one of those disclosed herein. Preferably, the combination comprises the compounds of the present invention and kinin peptides or analogs thereof.

[0460] A method for controlling the reproductive capacity of a cockroach insect or insect population is also provided, which comprises the step of contacting a cockroach insect or insect population with the combination described herein or a composition of the present invention. Preferably, the cockroach insect is one of those disclosed herein. Preferably, the combination comprises the compound of the present invention and a kinin peptide or analog thereof.

[0461] In the context of the present invention, "controlling reproductive capacity" means reducing, inhibiting, or eliminating the presence of an insect species during one or more of its developmental stages. For example, the compositions of the present invention can be used to control the growth of mites at any stage, such as the egg, larval, nymphal, and adult forms.

[0462] Further combination with insecticides The compounds of the present invention can be used in combination with one or more further insecticides, for example, those described herein. Combinations are also provided that include the compounds of the present invention or their salts or solvates in combination with one or more additional active insecticides or insecticidal compounds.

[0463] The composition of the present invention may further comprise one or more additional active insecticides or active insecticidal compounds.

[0464] Preferably, the insecticide can be selected from insect neuropeptides or their analogues. Preferably, the insecticide is a further kinin analogue, AKH peptide, DH31 peptide, DH44 peptide, pyrokinin peptide and / or CAPA peptide (e.g., CAPA-1, CAPA-2, or CAPA-3 peptide or analogue).

[0465] Additional active insecticides can be selected from CAPA peptide, AKH peptide, DH31 peptide, and / or pyrokinin peptide.

[0466] Appropriately, the insecticide may be selected from insect neuropeptides or analogs thereof, such as further kinin peptides, AKH peptides, DH31 peptides, DH44 peptides, pyrokinin peptides, or CAPA peptides (e.g., CAPA-1, CAPA-2, or CAPA-3 peptides or analogs).

[0467] In addition or alternatively, insecticides include pyrethroids (permethrin, cypermethrin, deltamethrin); organophosphates (malathion, chlorpyrifos, diazinon); neonicotinoids (imidacloprid, clothianidin, thiamethoxam); carbamates (carbaryl, methomyl, propoxul); plant insecticides (pyrethrins (derived from chrysanthemum flowers), rotenones (derived from the roots of certain plants)); bio-pest control agents (Bacillus thuringiensis (Bt) products, Beauveria bassiana (fungus), Metarhizium anisopriae (Metarhizium) Chemical insecticides such as anisopliae (fungus), insect growth regulators (IGRs) (methoprene, pyriproxyfen), fipronil, spinosad, avermectin (including abamectin and ivermectin), chitin synthesis inhibitors (diflubenzuron, hexaflumurone), piperonyl butoxide, flonicamide, indoxacarb, chlorantraniliprole, dichlorodiphenyltrichloroethane, and sulfoxaflor can be selected.

[0468] In certain embodiments, further insecticides are further kinin peptides.

[0469] In certain embodiments, a further insecticide is the AKH peptide.

[0470] In certain embodiments, a further insecticide is the DH31 peptide.

[0471] In certain embodiments, a further insecticide is the DH44 peptide.

[0472] In certain embodiments, a further insecticide is a pyrokinin peptide.

[0473] In certain embodiments, further insecticides include CAPA peptides (e.g., CAPA-1, CAPA-2, or CAPA-3 peptides or analogues).

[0474] Preferably, the further insecticides or insecticidal compounds may be included in the composition of the present invention.

[0475] The method of the present invention may further include the step of contacting an insect population or a plant or a part thereof with a further insecticide or insecticidal compound, such as those described herein. Preferably, the further insecticide or insecticidal compound is a kinin peptide.

[0476] Preferably, any reference herein to the compounds of the present invention or compositions thereof may equally refer to a combination of the compounds of the present invention with one or more insecticides or insecticidal compounds, or a composition containing such a combination.

[0477] Preferably, combinations are provided that include the compound of the present invention or a salt or solvate thereof in combination with one or more of the peptides listed in the table below. [Table 13]

[0478] In one embodiment, the compound of the present invention is used in combination with, for example, the following pyrokinin peptide. [Table 14]

[0479] In one embodiment, the compound of the present invention is used in combination with, for example, the following further kinin peptides. [Table 15]

[0480] In one embodiment, the compound of the present invention is used in combination with a CAPA peptide (e.g., CAPA2 peptide).

[0481] In one embodiment, the compound of the present invention is used in combination with, for example, the following AKH peptide. [Table 16]

[0482] The selection of supplementary or additional insecticides typically depends on the specific target species.

[0483] Specific combinations Additional active insecticides can be selected from CAPA peptides, such as SDSKNT[n-me-A]LWFGPRL-[NH2](SEQ ID NO: 134)(SB-P-015), ASG[b3L]VAFPRV-[NH2](SEQ ID NO: 135)(2315), Palm-LVAFPRV-[NH2](SEQ ID NO: 136)(AH59), or [ahx]-LV[n-me-A]FPR[n-me-V]-[NH2](SEQ ID NO: 137)(AH270).

[0484] Preferably, the compound of the present invention is one or more additional active insecticides selected from the following: SDSKNT[n-me-A]LWFGPRL-[NH2] (Sequence ID 134)(SB-P-015) ASG[b3L]VAFPRV-[NH2] (SEQ ID NO: 135)(2315) Palm-LVAFPRV-[NH2] (SEQ ID NO: 136)(AH59) [ahx]-LV[n-me-A]FPR[n-me-V]-[NH2] (Sequence ID 137)(AH270) It can be offered in combination with [another product / service].

[0485] In certain embodiments, the peptides described in the examples and drawings, particularly SB-P-3:DPKYKFSSWG-[NH2](SEQ ID NO: 59) and SB-P-015:SDSKNT[n-me-A]LWFGPRL-[NH2](SEQ ID NO: 134); SB-P-3:DPKYKFSSWG-[NH2](SEQ ID NO: 59) and 2315:ASG[b3L]VAFPRV-[NH2](SEQ ID NO: 135); SB-P-3:DPKYKFSSWG-[NH2](SEQ ID NO: 59), SB-P-015:SDSKNT[n-me-A]LWFGPRL-[NH2](SEQ ID NO: 134), and 2315:ASG[b3L]VAFPRV-[NH2](SEQ ID NO: 135); SB-P-3:DPKYKFSSWG-[NH2] (SEQ ID NO: 59) and AH59:Palm-LVAFPRV-[NH2] (SEQ ID NO: 136) SB-P-3:DPKYKFSSWG-[NH2](SEQ ID NO: 59), SB-P-015:SDSKNT[n-me-A]LWFGPRL-[NH2](SEQ ID NO: 134), and AH59:Palm-LVAFPRV-[NH2](SEQ ID NO: 136); or SB-P-3:DPKYKFSSWG-[NH2](SEQ ID NO: 59) and AH270:[ahx]-LV[n-me-A]FPR[n-me-V]-[NH2](SEQ ID NO: 137); Alternatively, combinations comprising salts or solvates thereof are provided.

[0486] Beneficial insect species (e.g., pollinators) The compounds, compositions, and combinations of the present invention may be substantially non-toxic to beneficial insect species, including species that prey on pests and pollinators. Important pollinators include insects of the superfamily Apoidea, such as honeybees, such as those of the family Apidae, and those of the genus Bombus, such as the European bumblebee (Bombus terrestris). Important predatory species include ladybugs of the family Coccinellidae, such as the two-spotted ladybug (Adalia bipunctata).

[0487] Substantially non-toxic means that the compounds, compositions, and combinations of the present invention do not cause the death of beneficial insect species (e.g., pollinators), preferably, they do not cause the premature death of beneficial insect species (e.g., pollinators). It also means that the compounds, compositions, and combinations of the present invention do not cause harmful side effects to beneficial insect species (e.g., pollinators), for example, they do not have a negative effect on feeding behavior or mobility.

[0488] composition The present inventors have provided compositions comprising at least one insecticidal compound or combination thereof that can specifically bind to insects. Importantly, through this interaction with specific insect molecular structures such as receptors, preferably nerve receptors, the compositions disclosed herein can inhibit, prevent, or reduce one or more biological activities of insects so as to inhibit, prevent, or reduce the growth or reproductive capacity of insects. In certain embodiments, the compositions disclosed herein can specifically bind to insect receptors and can kill insects through specific interactions of at least one insecticidal compound contained in the composition.

[0489] The compositions of the present invention, or compositions for use in accordance with the present invention, typically comprise compounds described in combination with one or more auxiliary components such as solvents, carriers, diluents, adjuvants, preservatives, dispersants, emulsifiers, or synergists.

[0490] Preferably, the composition may be an agricultural composition, an insect control composition (e.g., an insecticide composition), or a plant protection composition.

[0491] In any of these embodiments, the compounds or combinations of compounds of the present invention may be provided as part of a composition such as an agricultural composition, an insect control composition (e.g., an insecticide composition), or a plant protection composition. Accordingly, references herein to the application or use of compounds or combinations should be interpreted as encompassing the application or use of the appropriate composition, unless the context should otherwise indicate otherwise.

[0492] The composition typically comprises one or more auxiliary components, such as solvents, carriers, diluents, adjuvants, preservatives, dispersants, emulsifiers, or synergists, as described herein.

[0493] The composition may further include combinations with one or more additional active insecticides described herein.

[0494] The present invention further provides compositions comprising a compound of the present invention mixed with one or more solvents, carriers, diluents, auxiliaries, preservatives, dispersants, emulsifiers, or synergists, or combinations thereof, such as agricultural compositions, insect control compositions, or plant protection compositions. The compositions may be aqueous compositions. Further details are described below.

[0495] As used herein, “agricultural use” means suitable for use in agriculture or the pesticide industry, including horticulture, floriculture and home and garden use, but also means non-crop-related uses such as use by public health / pest control workers to control undesirable insects and rodents, home use such as household fungicides and insecticides, and products intended to protect plants or parts of plants, crops, bulbs, tubers, fruits (e.g., from harmful organisms, diseases or pests); agents to control, preferably promote or increase, plant growth; and / or products intended to promote the yield of harvested plants, crops or parts of plants (e.g., their fruits, flowers, seeds, etc.). Examples of such substances will be obvious to those skilled in the art and preferably include compounds active as insecticides (e.g., contact insecticides or systemic insecticides, including household insecticides) in the context of the present invention. Other such pesticides may be pest and disease control agents, growth regulators, nutrients / fertilizers, repellents, defoliants, etc.

[0496] As used herein, “agricultural use” includes not only the use of the insecticidal compounds, combinations or compositions thereof, and optionally the pesticides defined above (e.g., pest and disease control agents, growth regulators, nutrients / fertilizers, repellents, defoliants, etc.) of the present invention, which are suitable for and / or intended for use on field crops (e.g., agriculture), but also the use of the compounds, combinations or compositions thereof and the pesticides defined above, which are suitable for and / or intended for use on greenhouse crops (e.g., horticulture / floriculture) or hydroponic systems, as well as the use of the compounds, combinations or compositions thereof and the pesticides defined above, which are suitable for and / or intended for use on non-agricultural crops, such as use in private gardens, home use (e.g., herbicides or insecticides for home use), or use by pest control workers (e.g., weed control, etc.).

[0497] Preferably, the insect control composition according to the present invention is for controlling insect populations. Formulations of such compositions for controlling insect populations are known to those skilled in the art and include, but are not limited to, liquid emulsifying concentrates, wettable powders, liquids, suspension concentrates, emulsions, sposemulsions, granules, and water-dispersible granules (Mulqueen, 2003). Preferably, the insect control composition according to the present invention comprises the insecticidal compound of the present invention and optionally a combination of further insecticidal compounds. Preferably, the insecticidal compound is contained in a carrier as described herein below.

[0498] The compositions of the present invention may include pest control formulations or agricultural chemical formulations. As used herein, “pest control formulation” means any composition comprising a compound or combination of compounds intended to prevent, control, repel, attract or mitigate any pest. As used herein, “agricultural chemical formulation” means a composition for agricultural use comprising a biologically active agent, optionally together with one or more additives that are advantageous for the optimal dispersion, atomization, distribution, retention and / or activity of the agricultural chemical. Non-limiting examples of such additives include diluents, solvents, adjuvants, surfactants, wetting agents, spreading agents, oils, fixatives, penetrating agents, buffers, acidifying agents, defoaming agents, and drift control agents.

[0499] As used herein, a composition means a composition comprising at least one active substance, preferably an insecticidal compound of the present invention, together with one or more additives that are advantageous to the optimal dispersion, micronization, deposition, leaf wetting, distribution, retention and / or uptake of the active substance. As used herein, a composition includes a biological insecticide or a biological insecticide, and as will become apparent from further description herein, these terms are used interchangeably in this application. Accordingly, as used herein, a composition includes a composition comprising at least one biomolecule as an active ingredient, substance or component for controlling pests in plants or other agricultural environments (e.g., in soil). Preferably, at least one biomolecule comprises an insecticidal compound of the present invention or a combination thereof. Preferably, the pest is an insect. Examples of additives in compositions disclosed herein include, but are not limited to, diluents, solvents, adjuvants, surfactants, wetting agents, spreading agents, oils, binders, thickeners, penetrating agents, buffers, acidifying agents, anti-settling agents, anti-freezing agents, photoprotective agents, defoaming agents, biocides, and / or drift control agents.

[0500] Preferably, the composition of the present invention is an aqueous composition.

[0501] The compound content of the composition can vary over a wide range. The compound concentration of the composition is preferably an effective amount. The compound concentration of the composition may be 0.0000001 to 95% by mass of the compound, preferably 0.0001 to 1% by mass. As used herein, the terms "effective amount" and "effective dose" mean the amount necessary to achieve the desired result.

[0502] In certain embodiments, the concentration of the compound of the present invention contained in the composition may be at least 0.0001% by mass. In certain embodiments, the concentration of the compound of the present invention contained in the composition may be up to 50% by mass. In certain embodiments, the concentration of the compound of the present invention contained in the composition may be 0.0001% by mass to 50% by mass. In certain embodiments, the present invention provides a composition comprising at least one insecticidal compound of the present invention, wherein the concentration of at least one compound of the present invention in the composition is in the range of 0.001% by mass to 50% by mass. In yet another particular embodiment, the concentration of at least one compound of the present invention contained in the composition may be 0.001% by mass to 50% by mass. In yet another particular embodiment, the concentration of at least one compound of the present invention contained in the composition may be 0.01% by mass to 50% by mass. In yet another particular embodiment, the concentration of at least one compound of the present invention contained in the composition may be 0.1% by mass to 50% by mass.

[0503] A composition of the present invention, or a composition for use in accordance with the present invention, may contain one or more compounds of the present invention in combination and / or in combination with other insecticidal compounds described herein. Therefore, a composition of the present invention may, for example, contain the first compound of the present invention and the second compound of the present invention, or the first compound of the present invention and the second insecticidal compound. Preferably, the first and second compounds may be any of those described herein and may be present in the composition in any relative ratio.

[0504] The composition may be an aqueous composition, such as a physiological saline composition. The aqueous composition may contain one or more buffers, such as a phosphate buffer (e.g., phosphate-buffered saline) or Tris buffer. Alternatively, the composition may be an oil dispersion or emulsion, such as an oil or water emulsion. Alternatively, the composition may be, for example, a suspension, powder, foam, paste, granules, aerosol, impregnated natural and synthetic substances, or encapsulated in polymeric substances. The appropriate form of the composition can be selected for the intended use, taking into account the target insect and its habitat.

[0505] Adjuvants can enhance product performance, for example, by increasing the efficiency of delivery of the active ingredient, reducing the required level of the active ingredient, or expanding the range of efficacy.

[0506] Different types of adjuvants offer a variety of benefits and advantages achieved by modulating properties such as spray formation, spray retention, wetting, deposition, or uptake.

[0507] Adjuvants that modulate spray formation can influence spray quality by reducing spray drift and waste, allowing more product to reach the target. This can lead to reduced usage rates, resulting in a better environmental profile and potentially more cost-effective solutions. Such adjuvants include nonionic surfactant and emulsifier blends.

[0508] Adjuvants that regulate spray retention can dissipate the kinetic energy of droplets during impact, meaning that the likelihood of bounce or runoff is reduced. Examples of such adjuvants include alkyl polyglucosides, alkoxylated alcohols, and polyoxyethylene monobranched alcohols (e.g., polyoxyethylene(8) monobranched alcohol).

[0509] Adjuvants (i.e., wetting agents) that modify wetting properties can reduce surface tension and contact angle, resulting in improved coverage. Examples of such adjuvants include polyoxyethylene sorbitan monolaurate (e.g., polyoxyethylene(8) sorbitan monolaurate), surfactant blends, and alkyl polyglucosides.

[0510] Adjuvants that regulate deposition formation can influence the evaporation of water from droplets and thus provide a more uniform distribution. Examples of such adjuvants include alkoxylated polyol esters, polyoxyethylene sorbitan monolaurate (e.g., polyoxyethylene (12) sorbitan monolaurate), and alkyl polyglucosides.

[0511] Adjuvants that regulate uptake can improve the penetration and uptake of active ingredients, for example, through the cuticle of insects, thereby increasing their bioavailability. Examples of such adjuvants include alkoxylated polyol esters and polyoxyethylene sorbitan monolaurates (e.g., polyoxyethylene(12) sorbitan monolaurate and polyoxyethylene(16) sorbitan monolaurate).

[0512] The dispersant may be aqueous or non-aqueous. Oil-dispersion (OD) formulations typically contain a solid active ingredient dispersed in an oil. The oil may vary from paraffinic to aromatic solvent-type oils and vegetable oils or methylated seed oils. Typically, the active ingredient is uniformly suspended in the oil phase. While OD formulations are primarily used for water-sensitive active ingredients, they have also come to be used for other active ingredients due to the often adjuvant action of the carrier oil, resulting in better spray retention, diffusion, leaf uptake, and improved penetration (e.g., across insect cuticles).

[0513] Suitable oils for use in OD dispersions include linseed oil, rapeseed oil, and soybean oil.

[0514] Aqueous dispersants can be used, for example, to improve stability in a spray tank after dilution with water, and may include modified styrene-acrylic polymers, as well as polymeric amphoteric dispersants and adjuvants.

[0515] Emulsifiers can be used to emulsify a continuous oil phase in water when the OD formulation is diluted before spraying. Emulsifiers can be selected based on their ability to spontaneously form an emulsion. The performance of an emulsifier is determined primarily by the properties of the surfactant and the collective effect of how they are positioned at the oil / water interface. Examples include polyoxyethylene sorbitol hexaoleate (e.g., polyoxyethylene (40) sorbitol hexaoleate), emulsifier blends, and calcium alkylarylsulfonate.

[0516] The composition may further include an adhesive or a dye.

[0517] The compound may be provided in the form of a concentrate for dilution before application. Alternatively, the compound may be provided in a solid form to be suspended or dissolved before formulation.

[0518] The compositions disclosed herein are themselves available in a wide variety of solid or liquid forms. Examples of solid compositions include powdery powders (with an active substance content of up to 100%) and granules, particularly granules obtained by extrusion, compression molding, impregnation of granular carriers, and granulation using powder as a starting material (in the latter case, the active substance content in these granules is 0.5 to 80%). Such solid compositions can be optionally used in a liquid form, varying in degree of viscosity, by dilution with water, for example, depending on the desired type of application. Examples of liquid compositions, or forms intended to constitute a liquid composition during application, include solutions, particularly water-soluble concentrates, emulsions, suspension concentrates, wettable powders (or spray powders), oils, and waxes. The suspension concentrates that can be applied by spraying are prepared to obtain a stable fluid product that does not form deposits, and typically contain 10-75% active substance, 0.5-15% surfactant, 0.1-10% thixotropic agent, 0-10% suitable additives such as defoamers, corrosion inhibitors, stabilizers, penetrants, and adhesives, and as a carrier, water or an organic liquid in which the active substance is insoluble or poorly soluble, and certain organic solids or inorganic salts may be dissolved in the carrier to help prevent sedimentation or as an inhibitor of water gelation.

[0519] As used herein, “carrier” means any solid, semi-solid, or liquid carrier that can suitably incorporate, include, immobilize, adsorb, absorb, bind, encapsulate, embed, adhere, or contain the active substance, such as the insecticidal compound or combination of the present invention, in or on its surface. Non-limiting examples of such carriers include nanocapsules, microcapsules, nanospheres, microspheres, nanoparticles, microparticles, liposomes, vesicles, beads, gels, weakly ionic resin particles, liposomes, spiral delivery vehicles, small granules, granules, nanotubes, buckyballs, water droplets as part of water-in-oil emulsions, oil droplets as part of oil-in-water emulsions, organic materials such as cork, wood or other plant-derived materials (e.g., in the form of seed husks, wood chips, pulp, spheres, beads, sheets or any other suitable form), inorganic materials such as paper or cardboard, talc, clay, microcrystalline cellulose, silica, alumina, silicates and zeolites, or microbial cells (such as yeast cells), or even suitable fractions or fragments thereof.

[0520] In one embodiment, the carrier is a liposome. In one embodiment, the composition of the present invention preferably comprises one or more liposomes, each liposome comprising the compound of the present invention or a combination thereof. Therefore, preferably, the present invention provides a composition or formulation comprising a plurality of liposomes, the liposomes comprising the compound of the present invention or a combination thereof. Preferably, the liposomes comprise a lipid component, preferably soy lecithin and glycerol. Preferably, the liposomes are formed from soy lecithin and glycerol. Preferably, the liposomes are formed from 25 mg / ml glycerol and 3% glycerol. Preferably, the liposomes contain an effective concentration of the compound of the present invention. Preferably, the liposomes are approximately 10 -4 M comprises the compound of the present invention or a combination thereof. Preferably, the present invention provides a composition or formulation comprising a plurality of liposomes, wherein the liposomes comprise the compound of the present invention or a combination thereof, soy lecithin (preferably 25 mg / ml), and glycerol (preferably 3%).

[0521] Preferably, liposomes can be produced by the Mozafari heating method (Mozafari, MR "Nanoliposomes: preparation and analysis." Liposomes: Methods and Protocols, Volume 1: Pharmaceutical Nanocarriers (2010): 29-50). Preferably, such a method includes (a) mixing the compound of the present invention with glycerol, preferably a 50% glycerol solution; (b) mixing the mixture from step (a) with soy lecithin, preferably 350 mg of soy lecithin in aqueous solution; (c) heating the mixture from step (b) with stirring, preferably at about 60°C and at about 800 RPM for about 40 minutes to form liposomes; (d) annealing the liposomes, preferably by standing them in water at 40°C for about 1-2 hours; and (e) sonicating the liposomes, preferably in an ultrasonic bath for about 30 minutes.

[0522] Preferably, the liposomes have an average diameter of approximately 150-250 nm, preferably approximately 175-225 nm, preferably approximately 190-210 nm, and preferably approximately 200 nm. Preferably, the size of the liposomes is determined by using dynamic light scattering (DLS), for example, using Malvern's Zetasizer Nano. Preferably, the liposomes have a polydispersity index of 0.25-0.35, preferably 0.26-0.33, preferably 0.26-0.31, preferably 0.26-0.30, preferably 0.26-0.29, preferably 0.26-0.28, and preferably approximately 0.26.

[0523] In the compositions of the present invention, a carrier containing one or more insecticidal compounds may be maintained, for example, as a wettable powder, wettable granules, emulsifiable concentrate, suspension concentrate, microemulsion, capsule suspension, dry microcapsule, tablet, or gel, or it may be suspended, dispersed, emulsified, or otherwise provided in a suitable liquid medium (e.g., water or another suitable aqueous, organic, or oily medium) to provide a (concentrated) liquid composition of the present invention that has stability that allows the composition of the present invention to be properly stored or applied to the intended site of action (after further dilution if necessary). Preferably, the compositions of the present invention may be transported and / or stored before final use as a suitable liquid concentrate, dry powder, tablet, capsule suspension, slurry, or "wet cake," which can be appropriately diluted, dispersed, suspended, emulsified, or otherwise reconstituted by the end user before final use. The compositions of the present invention can be applied to the intended site of action by any suitable or desired manual or mechanical technique, such as spraying, injecting, dropping, brushing, coating, drip coating, application as droplets, mist, or aerosol, or any other suitable technique. In one embodiment, the intended site of action is a living insect in its entirety, and more preferably the surface of an insect.

[0524] Commercially available base formulations, such as Armid® FMPC (Akzo Nobel), may also be suitable for use in formulating the compounds described herein.

[0525] The composition may contain one or more synergistic agents, i.e., compounds that increase the effectiveness of the insecticide against its target, often by inhibiting the ability of insects to metabolize the activator. Common synergistic agents include piperonyl butoxide and MGK-264 (n-octylbicycloheptanedicarboximide), or peptidase inhibitors.

[0526] The composition may contain one or more agents that promote the stability of the insecticidal compound of the present invention. Preferably, the one or more agents that promote stability can prevent the degradation of the insecticidal compound of the present invention. Suitable agents that prevent the degradation of the insecticidal compound of the present invention can inhibit or reduce the activity of enzymes, preferably enzymes that act to degrade proteins, preferably, for example, proteases. Therefore, preferably, the composition may contain one or more protease inhibitors, preferably selected from Bowman-Burk inhibitors, Kunitz inhibitors, cystatins, trypsin inhibitors, serpines, tannins, proteinase inhibitor-II (PI-II), and alpha-AI1.

[0527] The composition may further contain one or more additional attractants, sterilizers, mite exterminators, nematode exterminators, fungicides, growth regulators, or herbicides.

[0528] In some embodiments, the composition may include one or more further agricultural chemicals or pesticides, such as herbicides (e.g., contact herbicides or systemic herbicides, including household herbicides), fungicides (e.g., contact fungicides or systemic fungicides, including household fungicides), anthelmintics (e.g., contact anthelmintics or systemic anthelmintics, including household anthelmintics) and other pest control agents or biocides (e.g., agents for killing insects or snails); as well as fertilizers; growth regulators such as plant hormones; micronutrients, mitigants, pheromones; repellents; insect bait; and / or active ingredients used to regulate (i.e., increase, decrease, inhibit, enhance and / or induce) gene expression (and / or other biological or biochemical processes) in or by a target plant (e.g., a protected plant or a controlled plant), such as nucleic acids (e.g., single-stranded or double-stranded RNA, as used in the context of RNAi technology) and other factors, proteins, chemicals, etc., known for this purpose.

[0529] Examples of such pesticides are obvious to those skilled in the art, for example, glyphosate, paraquat, metrachlor, acetochlor, mesotrione, 2,4-D, atrazine, glufosinate, sulfosate, phenoxaprop, bendimethalin, picloram, trifluralin, bromoxynil, clodinahop, fluroxypyr, nicosulfuron, bensulfuron, imazetapyr, dicamba, imidacloprid, thiamethoxam, fipronil, chlorpyrifos, deltamethrin, lambda-cyhalothrin, endosulfan, methamidophos, carbofuran, ku Examples of known pesticides or any suitable combination thereof include, but are not limited to, rotianidin, cypermethrin, abamectin, diflufenican, spinosad, indoxacarb, bifenthrin, tefluthrin, azoxystrobin, thiamethoxam, tebuconazole, mancozeb, cyazofamide, fluazinam, pyraclostrobin, epoxyconazole, chlorothalonil, copper fungicides, trifloxystrobin, prothioconazole, difenoconazole, carbendazim, propiconazole, thiophanate, sulfur, boscalid, and other known pesticides.

[0530] The composition may be a bait composition for ingestion by target insects. The bait composition may contain one or more feeding stimulants, i.e., substances that attract insects and cause them to ingest the compound. Feeding stimulants may include artificial sweeteners, amino acids, other peptides or proteins, and carbohydrates (e.g., glucose, fructose, sucrose, maltose), etc. Examples include honey, syrup, and aqueous sucrose solutions.

[0531] Commercially available base formulations, such as Armid® FMPC (Akzo Nobel), may also be suitable for use in formulating the compounds described herein.

[0532] The composition may contain one or more synergistic agents, i.e., compounds that increase the effectiveness of the insecticide against its target, often by inhibiting the ability of insects to metabolize the activator. Common synergistic agents include piperonyl butoxide and MGK-264 (n-octylbicycloheptanedicarboximide), or peptidase inhibitors.

[0533] Combinations comprising the compound of the present invention or a salt or solvate thereof in combination with one or more additional active insecticides are also provided. The additional active insecticides may be selected from pyrethrins or pyrethroids or other peptide analogs. The insecticides may also include, for example, phosphates, carbamates, carboxylates, chlorinated hydrocarbons, phenylurea and substances produced by microorganisms. The additional active insecticides may also be further kinin analogs, AKH peptides, DH31 peptides, DH44 peptides, pyrrokinin peptides or CAPA peptides (e.g., CAPA-1, CAPA-2, or CAPA-3 analogs).

[0534] The composition may further comprise one or more additional active insecticides. The composition of the present invention, or a composition for use according to the present invention, may comprise the compound of the present invention in combination with further kinin analogs, AKH peptides, DH31 peptides, DH44 peptides, pyrrokinin peptides, or CAPA peptides (e.g., CAPA-1, CAPA-2, or CAPA-3 analogs).

[0535] Method for producing insecticidal compounds The insecticidal compounds described herein can be produced by any method known in the art for producing peptides. In one embodiment, the insecticidal compound can be produced by a chemical method, preferably by chemical synthesis.

[0536] The insecticidal compounds of the present invention can be synthesized using any suitable chemical method.

[0537] Preferably, the insecticidal compound is a peptide. Therefore, preferably, the insecticidal compound is synthesized by solid-phase peptide synthesis. Preferably, such synthesis can be carried out using commercially available equipment such as the Biotage Initiator + Alstra microwave-assisted peptide synthesizer or the CEM Liberty Prime microwave-assisted peptide synthesizer.

[0538] In a further aspect of the present invention, an insecticidal compound produced and isolated by the method of the present invention is provided. Preferably, it is an isolated insecticidal compound of formula (I) or (XX) produced by the method of the present invention.

[0539] In a further aspect of the present invention, a method for producing a composition disclosed herein is provided, comprising at least the steps of (a) obtaining at least one insecticidal compound of formula (I) or (XX), and (b) formulating the insecticidal compound into a composition.

[0540] A further aspect of the present invention provides a method for generating and / or producing variants of an insecticidal compound of formula (I). Such a method may include (i) modifying peptide Z of formula (I) or (XX) by adding, substituting, or deleting at least one amino acid, and (ii) evaluating the variant thus produced for its insecticidal activity and, optionally, at least one property selected from the group consisting of biostability, chemical stability, bioavailability, solubility (including the ability to form a stable formulation), productivity, and production cost. If the insecticidal activity is reduced compared to the insecticidal compound containing unmodified peptide Z, steps (i) and (ii) are repeated until a variant with improved insecticidal activity is obtained. If the insecticidal activity is improved compared to the insecticidal compound containing unmodified peptide Z, the method may include further steps of generating, isolating, and purifying the variant. Screening for insecticidal activity and other above-mentioned properties may be carried out as described below or as is generally known to those skilled in the art.

[0541] Preferably, the step of obtaining at least one insecticidal compound includes (a) a step of chemically synthesizing the insecticidal compound.

[0542] Preferred compositions are described herein. Preferred manufacturing methods for formulating compositions are known in the art and include, but are not limited to, high-shear or low-shear mixing, wet or dry grinding, drip casting, encapsulation, emulsification, coating, pilling, extrusion granulation, fluidized bed granulation, co-extrusion formation, spray drying, spray cooling, particle formation, addition or condensation polymerization, interfacial polymerization, insight polymerization, coacervation, spray encapsulation, cooling melt dispersion, solvent evaporation, phase separation, solvent extraction, sol-gel polymerization, fluidized bed coating, pan coating, melting, passive or active absorption or adsorption.

[0543] Features disclosed in the foregoing description, or in the following claims, or in the accompanying drawings, and expressed in a particular form or with respect to means for performing the disclosed functions, or methods or processes for obtaining the disclosed results, may be used, as appropriate, separately, or in any combination of such features, to realize the present invention in its various forms.

[0544] Although the present invention has been described in conjunction with the exemplary embodiments described above, many equivalent modifications and variations will be apparent to those skilled in the art upon referring to this disclosure. Therefore, the exemplary embodiments of the present invention described above are illustrative and not limiting. Various modifications can be made to the embodiments described without departing from the spirit and scope of the invention.

[0545] To avoid any doubt, any theoretical explanations provided herein are provided solely for the purpose of improving the reader's understanding. The inventors do not wish to be bound by any of these theoretical explanations.

[0546] Any section headings used herein are for structural purposes only and should not be construed as limiting the subject matter described herein.

[0547] The present invention includes combinations of the described embodiments and preferred features, unless such combinations are not permitted or are explicitly avoided.

[0548] Aspects and embodiments of the present invention will be described below with reference to the accompanying drawings. Further aspects and embodiments will be apparent to those skilled in the art. All references mentioned herein are incorporated herein by reference. [Brief explanation of the drawing]

[0549] [Figure 1] This figure shows the activity data of the unformulated peptide according to the present invention against Drosophila melanogaster. [Figure 2] This figure shows the activity data of the unformulated peptide according to the present invention against M. persicae. [Figure 3] This figure shows the activity data of the unformulated peptides according to the present invention, when combined with one or more other peptides, against M. persicae. [Figure 4] This figure shows the activity data of the unformulated peptides according to the present invention, when combined with one or more other peptides, against M. persicae. [Figure 5] This figure shows the activity data of the unformulated peptides according to the present invention, when combined with one or more other peptides, against M. persicae. [Figure 6] This figure shows the activity data of the unformulated peptide according to the present invention against Plutella xirostella. [Figure 7] Scheme 1: This diagram shows the synthesis pathway leading to SB-P-33. A general overview of the workflow involved is shown in the inset. The locations where a double coupling process is used are indicated by asterisks. [Figure 8] Scheme 2: This figure shows the synthesis path leading to SB-P-35. A general overview of the workflow involved is shown in the inset. [Figure 9]Scheme 3: This diagram shows the synthesis path leading to SB-P-36. A general overview of the workflow involved is shown in the inset. [Figure 10] Scheme 5: This diagram shows the synthesis path leading to SB-P-54. An overview of a typical workflow is shown in the inset. [Figure 11] This diagram shows the setup for a CAF assay experiment. [Figure 12] This diagram shows the setup for a leaf immersion assay experiment. [Figure 13] (Top to bottom): This figure shows annotated LC-MS traces of SB-P-70(a) in Schneider medium and SB-P-70(b) after 24 hours of tissue incubation. [Figure 14] This figure shows annotated LC-MS traces of SB-P-103(a) in Schneider medium and SB-P-103(b) after 24 hours of tissue incubation. [Figure 15] This figure shows the peptide integrity of SB-P-70 and SB-P-103 after incubation with insect tissue for 24 hours. [Figure 16] This figure shows the oral toxicity results for bees, expressed as the survival rate % 96 hours after application of SB-P-32, SB-P-065, SB-P-066, and a combination of SB-P-33 and SB-P-51 (pyrokinin). [Figure 17] This figure shows the chemical synthesis route for synthesizing SB-P-65. [Figure 18] This figure shows the HPLC trace of SB-P-65. [Figure 19] This figure shows the LC-MS trace of SB-P-65. [Figure 20] This figure shows the activity data of unformulated SB-P-65 against Mizus persicae after 120 hours. [Figure 21] This figure shows the activity data of unformulated SB-P-65 against Mizusu persicae over time. [Figure 22] This figure shows the chemical synthesis route for synthesizing SB-P-66. [Figure 23] This figure shows the HPLC trace of SB-P-66. [Figure 24] This figure shows the LC-MS trace of SB-P-66. [Figure 25] This figure shows the activity data of unformulated SB-P-66 against Mizus persicae after 120 hours. [Figure 26] This figure shows the activity data of unformulated SB-P-66 against Mizusu persicae over time. [Figure 27] This figure shows the chemical synthesis route for synthesizing SB-P-70. [Figure 28] This is a diagram showing the HPLC trace of SB-P-70. [Figure 29] This is a diagram showing the LC-MS trace of the SB-P-70. [Figure 30] This figure shows the activity data of unformulated SB-P-70 against Plutella and Xirostella after 96 hours. [Figure 31] This diagram shows the setup for a lepidopteran mortality assay experiment. [Figure 32] This figure shows the activity data of unformulated SB-P-70 against Spodoptera flugyperda after 168 hours. [Figure 33] This figure shows the activity data of SB-P-65 against *Mizus persicae* after 120 hours using commercially available Silwet-408 as an adjuvant. [Figure 34] This figure shows the activity data of unformulated SB-P-65 and SB-P-66 against naturally parasitizing Aphis fabae in field trials conducted by PGRO on climbing beans, 2 days after the first application (Application A) and 16 days after the second application (Application B). [Figure 35] This figure shows the activity data of unformulated SB-P-65 and SB-P-66 against naturally infested cotton aphids in field trials conducted by AgriScience on cotton, 3 days and 7 days after application (Application A). [Figure 36]This figure shows the activity data of unformulated SB-P-65 and SB-P-66 against cotton aphids in a time-series field trial conducted by AgriScience on melons. [Figure 37] This figure shows the activity data of unformulated SB-P-65 and SB-P-66 against naturally parasitizing Aphis fabae in field trials conducted by PGRO on climbing beans, 4 days and 8 days after application (Application A). [Figure 38] This figure shows the activity data of unformulated SB-P-66 against naturally occurring leafhoppers (Leafhoppers) in field trials over time. [Examples]

[0550] General procedure All amino acids are in their L-stereoconfiguration unless otherwise specified. Standard Fmoc-protected amino acids were purchased from CEM or Pepceutical. Specialized amino acid suppliers are indicated as appropriate, as are the suppliers of peptide synthesis resins. Peptide-grade DMF was purchased from Rathburn.

[0551] The peptides were synthesized as specified using either the Biotage Initiator + Alstra microwave-assisted peptide synthesizer or the CEM Liberty Prime microwave-assisted peptide synthesizer.

[0552] High-resolution mass spectrometry (HRMS) was performed using a Bruker microTOF-Q II (ESI+) system.

[0553] The peptides were purified using a reverse-phase Dionex HPLC system equipped with a Dionex P680 pump and a Dionex UVD170U UV-vis detector (monitoring at 214 nm and 280 nm) with a Phenomenex Gemini C18 5 μm 250 × 21.2 mm column. Gradient filtration was performed using solvents A (H2O + 0.1% TFA) and B (MeCN + 0.1% TFA), and the fractions were lyophilized using a Christ Alpha 2-4 LO plus freeze-dryer.

[0554] Pure peptides were analyzed at a flow rate of 1 mL / min using a Shimadzu reverse-phase HPLC (RP-HPLC) system equipped with a Shimadzu LC-20AT pump, SIL-20A autosampler, and SPD-20A UV-vis detector (monitoring at 214 nm and 280 nm), using a Phenomenex Aeris 5 μm, peptide XB-C18, 150 × 4.6 mm column. RP-HPLC gradients were performed using solvent systems consisting of solution A (100% H₂O + 0.1% TFA) and solution B (100% MeCN + 0.1% TFA). Typically, each peptide was characterized using two gradients: a 20-minute gradient from 5% to 95% solution B (incorporating a 2-minute hold in 5% solution B and a 5-minute wash in 95% solution B at the start and end of each gradient) and a 50-minute gradient from 5% to 95% solution B (incorporating a 5-minute hold in 5% solution B and a 5-minute wash in 95% solution B at the start and end of each gradient). In some cases, special gradients were used, and this is indicated where appropriate. Analytical RP-HPLC data report column retention time (tR) in minutes (min). The analytical column was maintained at room temperature.

[0555] LC-MS analysis was performed using a Thermo Scientific LCQ Fleet quadrupole mass spectrometer with a m / z range of 50–2000 Da, equipped with an ESI source coupled to a Dionex Ultimate 3000 LC. The analysis was performed using a 20-minute linear gradient from buffer A (95 / 5 H2O / MeCN containing 0.1% v / v TFA) to buffer B (95 / 5 MeCNH2O containing 0.1% v / v TFA) on a ReprosilGold 120 C18, 3 μm 150 × 4 mm column (incorporating a 2-minute hold in 0% solution B and a 5-minute wash in 100% solution B at the start and end of each gradient). When special analytical RP-HPLC gradients were used to characterize the compounds, similar LC-MS gradients were used. Analytical RP-HPLC and LC-MS samples were injected as a 25 μL stock solution containing 0.1% v / v TFA in H2O / MeCN at a concentration of 1 mg / mL. The LC-MS column oven temperature was maintained at 30°C.

[0556] High-resolution mass spectrometry (HRMS) of pure peptides was performed using a Bruker microTOF-Q II (ESI+) system.

[0557] Proton nuclear magnetic resonance spectra (1H NMR) for peptide content calculation were recorded using an AVANCE III 400 Bruker (400 MHz). Proton chemical shifts are expressed in parts per million (ppm, δ scale) and referenced to residual protium in the NMR solvent (CDCl3, δ 7.26; CD3OD, δ 3.31 and D2O, δ 4.79). Peak patterns are described using the following abbreviations where appropriate: br=broad, s=singlet, d=doublet, t=triplet, q=quadruplet, m=multiplet. The binding constant J is reported in Hertz (Hz).

[0558] General procedure for automated peptide synthesis Biotage initiator + Alstra synthesis system: Fmoc-protecting amino acids were prepared as 0.2 M (0.1 mmol synthesized), 0.5 M (0.2 mmol synthesized), or 0.7 M (0.5 mmol synthesized) solutions in DMF. Five equivalents of amino acids (relative to resin filling) were used during the coupling cycle. Oxyma and diisopropylcarbodiimide (DIC) were prepared as 0.2 M (0.1 mmol synthesized), 0.5 M (0.2 mmol synthesized), or 0.7 M (0.5 mmol synthesized) solutions in DMF. Five equivalents of Oxyma and five equivalents of DIC (relative to resin filling) were used during the coupling cycle. For Fmoc deprotection, a solution of 20% morpholine (containing 5% formic acid) in DMF was used. The coupling reaction was carried out at 90°C for 2 minutes under microwave heating, except for Fmoc-Cys(Trt)-OH, Fmoc-His(Trt)-OH, and Fmoc-Arg(PBf)-OH. Fmoc-Cys(Trt) and Fmoc-His(Trt)-OH coupling were performed at 50°C for 10 minutes. Fmoc-Arg(Pbf)-OH coupling was performed at 90°C for 2 minutes in two consecutive cycles (double coupling). Microwave-assisted Fmoc deprotection was performed at 90°C for 1 minute.

[0559] CEM Liberty Blue Synthesizer Fmoc-protecting amino acids were prepared as a 0.2 M solution in NBP (Tamisolve). Five equivalents of amino acids (relative to the resin filling) were used during the coupling cycle. Oxyma was prepared as a 0.5 M solution in NBP. DIC was prepared as a 5 M solution in NBP. Five equivalents of Oxyma and five equivalents of DIC (relative to the resin filling) were used during the coupling cycle. A 20% pyrrolidine solution was used for Fmoc deprotection. The coupling reaction and Fmoc deprotection were carried out under microwave heating at 90°C for 2 minutes and 1 minute, respectively, except for Fmoc-Cys(Trt)-OH, Fmoc-His(Trt)-OH, and Fmoc-Arg(Pbf)-OH. The coupling of Fmoc-Cys(Trt) and Fmoc-His(Trt)-OH was carried out at 50°C for 5 minutes. The coupling reaction between Fmoc and Arg(Pbf)-OH was performed at 75°C for 5 minutes in two consecutive cycles.

[0560] General procedure for TFA cleavage of peptides Typically, peptide cleavage tests were performed by taking approximately 3 mg of dry resin beads and treating them with TFA / TIS / water (95:2.5:2.5) for 3 hours. The filtrate was drained, concentrated, and then pulverized in cold diethyl ether (Et2O). The pulverized material was dissolved in acetonitrile / water and then analyzed by RP-HPLC / LC-MS.

[0561] Peptides were typically cleaved from the resin in bulk by gently agitating the resin in a TFA / TIS / H2O (95:2.5:2.5) cleavage cocktail at room temperature for 3 hours, then discharged and the TFA was blown off with a steady flow of N2 gas. Peptides containing cysteine ​​or tryptophan residues were cleaved from the resin for 3 hours using a TFA / TIS / H2O / DODT (94:2.5:1:2.5) cleavage cocktail. In all cases, the crude peptides were pulverized with cold Et2O. Et2O was removed from the resulting crude peptide pellet under a steady flow of nitrogen. The crude peptides were then redissolved in H2O / MeCN and purified by RP-HPLC.

[0562] Unless otherwise specified herein, peptides were synthesized or ordered directly according to the general procedures described above and the exemplary procedures described below.

[0563] SB-P-33 SB-P-33 was synthesized using a double coupling process incorporating CEM's Liberty Prime unit in Val3, Val4, Gln9, D-Arg10, His12, and Aib13 (Scheme 1 - Figure 7).

[0564] SB-P-35: The synthesis of SB-P-35 was carried out by Fmoc-SPPS in the CEM Liberty Prime unit. Fmoc removal was performed using a solution of 25% pyrrolidine in DMF. The coupling reaction was carried out using the DIC / Oxyma strategy at 110°C for 2 minutes. Acetyl capping was performed manually at room temperature using acetic anhydride / DIPEA in DMF (scheme shown in Figure 8).

[0565] SB-P-36: The synthesis of SB-P-36 was carried out by Fmoc-SPPS in the CEM Liberty Prime unit. Fmoc removal was performed using a solution of 25% pyrrolidine in DMF. The coupling reaction was carried out using the DIC / Oxyma strategy at 110°C for 2 minutes. Acetyl capping was performed manually at room temperature using acetic anhydride / DIPEA in DMF (scheme shown in Figure 9).

[0566] SB-P-54: The synthesis of this peptide was carried out using an automated Fmoc-SPPS method with a Biotage Initiator Alstra peptide synthesizer on Tentagel S RAM resin (f=0.22 mmol / g) (the scheme is shown in Figure 10).

[0567] The coupling process was performed at 90°C for 2 minutes using 4 equivalents (relative to the resin filling) of Fmoc-amino acids (0.2M) and DIC / Oxyma (0.5M). Fmoc deprotection was performed at 90°C for 1 minute in 20% morpholine / DMF (containing 5% formic acid additive). N-terminal acetyl capping was achieved by treatment with Ac2O (50 equivalents) and DIPEA (50 equivalents) at room temperature for 10 minutes.

[0568] SB-P-65 [ka] The specific synthesis route for SB-P-65 is shown in Figure 17. For the synthesis of 0.25 mmol of SB-P-65, a double coupling cycle was used for 2Gln, 5Val, 6Phe, and 8Ser. For 1Arg, an extended 7-minute Arg coupling cycle was used. For 0.5 mmol scale synthesis, an extended 6-minute single coupling cycle was used for 3Lys, 4Thr, 9Trp, and 10Gly. A double coupling cycle was used for 2Gln, 5Val, 6Phe, 7Ser, and 8Ser. For 1Arg, an extended 7-minute Arg coupling cycle was used. Purification was performed using a 10–20% B gradient and monitored at 240 nm and 60°C. Purity = 90%, yield = 41%.

[0569] SB-P-66 [ka] The specific synthesis route for SB-P-66 is shown in Figure 22. A double coupling cycle was used for 4Ser and 5Ser to synthesize SB-P-66 on an arbitrary scale. Purification was performed over 20 minutes using a 10–30% B gradient, monitored at 280 nm and 60°C. Purity = 91%, yield = 41%.

[0570] SB-P-70 [ka] The specific synthesis route for SB-P-70 is shown in Figure 27. SB-P-70 was synthesized on a 0.1 mmol scale using a double coupling assay for 1 Lys, 2 Val, 3 Lys, and 4 Phe. Purification was performed at room temperature over 30 minutes using a gradient from 20–80% B, monitored at 214 nm. Purity = 91%, yield = 42%.

[0571] SB-P-101 The synthesis of SB-P-101 was carried out on a CEM Liberty Blue surface using Rink Amide ProTide LL resin (f=0.18 mmol / g). The Fmoc deprotection reaction was performed at 90°C for 1 minute in a solution of 20% pyrrolidine in TamiSolve. The coupling reaction was performed at 90°C for 2 minutes using 5 equivalents of Fmoc-AA (relative to the resin packing) and 5 equivalents of DIC / Oxyma Pure (relative to the resin packing) in TamiSolve. For Fmoc-α-Me-Ser(tBu)-OH and Fmoc-(N-Me)-Phe-OH, an extended 4-minute coupling cycle was used. For Ser4, a double coupling step was used. The N-terminus of the peptide was acetylated after synthesis.

[0572] After synthesis, simultaneous resin cleavage and side chain deprotection of the peptide were performed at room temperature for 2 hours in a cocktail of 94:2.5:2.5:1(v / v)TFA:TIS:H2O:DODT. After grinding in ice-cold Et2O, half of the crude SB-P-101 was taken and purified by RP-HPLC to obtain >99% purity and 24% total yield.

[0573] Mortality rate assessment methods Cafe assay - Drosophila melanogaster Capillary feeder assay-based assays measure food intake in Drosophila melanogaster - PubMed (nih.gov) Five identical Drosophila melanogaster flies are anesthetized with CO2 and placed in a 2.5 cm x 7.5 cm cylindrical plastic vial. The vial is capped with a cotton stopper and has two holes, each with a pipette tip to support a capillary tube. Two 5 μl capillary tubes are filled with the treatment agent and weighed on a precision balance before being pipetted into the vial. The vial is placed in an incubator and the flies are fed for 24 hours. After 24 hours, the capillary tubes are removed, weighed, and the difference between the start and end values ​​is calculated to determine the amount of food consumed. New capillary tubes (weighed and filled) are placed in the active area, and this is repeated until 96 hours have passed. The mortality rate (number of dead flies) is counted every 24 hours. The experimental setup is shown in Figure 11.

[0574] Leaf immersion assay - Aphids or Plutella xirostella Based on IRAC susceptibility testing method 019 (https: / / irac-online.org / methods / aphids-adultnymphs / ). Fill a small dish measuring 4 cm wide and 3 cm high with a 1% agar solution (leaving a 1 cm gap between the agar and the lid), and let it stand to solidify. Immerse a 2.5 cm leaf disc in 3 ml of the treatment solution to coat the leaf with the treatment agent. Let the disc dry for 1 hour and place it on the solidified agar. Place insects (aphids or Plutella xirostella) on each leaf disc. Seal each unit with a tightly sealed, breathable lid. Place the agar dish on a small plastic tray lined with damp tissue paper, fill the water tray at the bottom of the incubator with clean water, and place it inside the incubator. Mortality rates are evaluated at 72 hours, 96 hours, and 120 hours. The leaf immersion assay setup is shown in Figure 12.

[0575] Biostability Biostability testing of Plutella xylostera tissues of SB-P-70 and SB-P-103 SB-P-70 and SB-P-103 were incubated in Schneider medium at 25°C with the intestinal and MT tissues and contents of P. xirostella larvae in their final stage. Control samples were prepared using peptides in Schneider medium without tissue, and tissues in Schneider medium without peptide. The state of the peptides after incubation with tissue was evaluated by LC-MS at 4 hours, 8 hours, 16 hours, and 24 hours (Figures 13 and 14).

[0576] In SB-P-70, proteolytic cleavage was confirmed to occur primarily between Ser5 and Ala6. After 24 hours, the peptide was completely degraded. In contrast, SB-P-103 remained 44% intact even after 24 hours of tissue incubation.

[0577] A leaf immersion assay for aphids was performed using SB-P-65 and compared with a negative control vehicle and the currently commercially available insecticide spirotetramat. The activity of SB-P-65 is shown in Figures 20 and 21. SB-P-65 exhibits good activity, and unlike broad-spectrum chemical insecticides such as spirotetramat, it is environmentally friendly and targets specific pests.

[0578] A leaf immersion assay for aphids was performed using SB-P-66 and compared with a negative control vehicle and the currently commercially available insecticide spirotetramat. The activity of SB-P-66 is shown in Figures 25 and 26. SB-P-66 exhibits good activity, and unlike broad-spectrum chemical insecticides such as spirotetramat, it is environmentally friendly and targets specific pests.

[0579] Leaf immersion assays of Plutella xirostella were performed using SB-P-70 and compared with a negative control vehicle and the currently commercially available insecticide chlorantraniliprole. The activity of SB-P-70 is shown in Figure 6. SB-P-70 exhibits good activity, and unlike broad-spectrum chemical insecticides such as chlorantraniliprole, it is environmentally friendly and targets specific pests.

[0580] Lepidopteran mortality assay for Spodoptera fulgiperda Frontier Lepidoptera artificial feed was prepared by preparing 1% agar and then mixing it with artificial feed powder. The peptide solution was divided equally into 10 cells, and the feed was poured directly onto them. The final peptide concentration was 1 × 10⁻⁴ M, and each peptide was divided equally into 10 cells. After the feed solidified and cooled, one L 1 Larvae were parasitized in each cell. The trays were sealed with heat, and the larvae were developed for 168 hours. Finally, pupation and mortality rates were scored. The setup for the lepidopteran mortality assay is shown in Figure 31. The lepidopteran mortality assay was performed using SB-P-70 and compared with a negative control vehicle and the insecticide dichlorodiphenyltrichloroethane (DDT). The activity of SB-P-70 is shown in Figure 32. SB-P-70 exhibits good activity, and unlike broad-spectrum chemical insecticides such as DDT, it is environmentally friendly and targets specific pests.

[0581] Honeybee survival experiment OECD Test No. 247: Adapted from the acute oral toxicity test of bumblebees, an oral testing protocol for honeybees. The survival of honeybees against peptides SB-P-065 and SB-P-066 was measured according to the protocol of OECD study 247. The results are shown in Figure 16.

[0582] An oral toxicity protocol for honeybees, adapted from OECD Test No. 247: Bumblebee, acute oral toxicity test, was implemented. The toxicity of SB-P-65 and SB-P-66 was compared to negative controls of sucrose or vehicle, and to the currently commercially available insecticide imidacloprid. The toxicity data are shown in Figure 16, and SB-P-65 and SB-P-66 are far less toxic to important pollinators such as honeybees compared to a wide range of chemical insecticides such as imidacloprid. array [Table 17A] [Table 17B]

[0583] References To more fully describe and disclose the present invention and the field of the art to which it pertains, numerous publications are cited. A complete citation of these references is provided below. Each of these references in its entirety is incorporated herein by reference. (References)

[0584] For standard molecular biology techniques, see Sambrook, J., and Russel, DW, *Molecular Cloning*, *A Laboratory Manual*, 3rd edition, 2001, Cold Spring Harbor, New York: Cold Spring Harbor Laboratory Press.

[0585] Numbered paragraphs The following numbered paragraphs define specific aspects and embodiments of the present invention. 1. Insecticidal compounds having the following formula (I), or their salts or solvates: R 1 -L 1 -YZR 2 (I) (In the formula, R 1 C is hydrogen (which can be represented as "H-" or "Hy-"), C 1~4 Alkyl (e.g., methyl, ethyl, propyl, butyl), formyl, -N(R 1a )-C(=N + (R 1b )(R 1c ))NR 1d R 1e , -C(=N + (R 1b )(R 1c ))NR 1d R 1e Acyl, fatty acyl, benzyl, benzoyl, heteroaryl or trifluoroacetyl, -NHC 1~18 Alkyl, -NHC 6~16 Ariel, -NHC1~6 Alkyl-C 6~10 It is an aryl, biotin, sugar moiety, or (poly)alkylene glycol; R 1a , R 1b , R 1c , R 1d and R 1e Each of them is either hydrogen or C 1~4 Independently selected from alkyl groups (e.g., methyl, ethyl, propyl, butyl); Any alkyl, formyl, acyl, fatty acyl, benzyl, benzoyl, heteroaryl, or trifluoroacetyl, -NHC 1~18 Alkyl, -NHC 6~16 aryl, -NH-C 1~6 Alkyl-C 6~10 Aryl or (poly)alkylene glycols contain halogens, C 1~6 Alkyl, C 1~6 It may be substituted with one or more groups selected from the haloalkyl or sugar moieties; L 1 It does not exist, or * -(C=O)C 1~16 Alkylene-NH-(in the formula, * (This represents a connection point to Y or Z). (C 1~20 ) Alkilen, (C 2~20 ) Alkenylene, (Poly)alkylene glycol; L 1 This may be substituted with one or more groups selected from oxo (=O), halogen, =N, and =S; Y is either absent or a peptide containing 1 to 16 amino acids; Y may contain a (poly)alkylene glycol linker in its peptide sequence; Z is expressed by the formula: F # -X 2 -X 3 -W # -X 5 It is a peptide, During the ceremony, X 2 is, S # , Y # , N # or H # Selected from; X 3 is, S # , A # , P # , V # , or T # Selected from; X 5 G # , A # Selected from; During the ceremony, `` # " indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs; R 2 NH2, NR 2a H, NR 2a R 2b , or OR 2a And; in the formula, R 2a and R 2b Each of them, if present, independently, C 1~6 Alkyl (e.g., methyl, ethyl, propyl, butyl, pentyl, or hexyl), C 3~6 Alkenil, C 6~16 Ariel, C 6~16 Aryl-C 1~6 Alkyl, C 1~6 Alkylene-C 6~16 Aryl, or C 1~6 These are haloalkyls, and each of them is a halogen, C 1~6 Alkyl, or C 1~6 (May be substituted with one or more groups selected from haloalkyl groups.) 2. Z is Z a , Z b or Z c A peptide selected from, During the ceremony, a)Z a The formula is: -F # -H # -S # -W # -G # It is the peptide of (SEQ ID NO: 1); b)Z b The formula is: -F # -X 2b -X 3b -W # -X 5b It is a peptide, During the ceremony, X 2b is the amino acid residue S # , Y # , N # Or H # Selected from; X 3b is the amino acid residue S # , A # , P # , V # , or T # Selected from (X 3b is the amino acid residue S # Or A # You may choose from the following options; X 5b is amino acid residue A # Or G # Select from, or c)Z c The formula is: -F # -S # -X 3c -W # -G # (Sequence 2) It is a peptide, In the formula, X 3c is amino acid residue A # , P # , V # Or T # Selected from; During the ceremony, `` # The insecticidal compound described in paragraph 1, wherein the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs. 3. The insecticidal compound described in paragraph 1 or 2, wherein Y is absent or a peptide containing 1 to 14 amino acids. 4. R 1 but, hydrogen; Acyls that may be substituted with sugar moieties; Fat acyl; heteroaryl; -NHC 6~16 Ariel; sugar part; Biotin; or formula * -(OCH2CH2) n -R p (Poly)ethylene glycol (in the formula, * L 1 , represents the connection point to Y or Z, n is an integer from 1 to 16, and Rp is selected from -NH2OH or -Ome. An insecticidal compound as described in any one of paragraphs 1 to 3. 5. R 1 but, hydrogen; An acyl which may be substituted with a sugar moiety, wherein the acyl group is selected from formyl, acetyl (Ac), propanoyl, and butanoyl; Fatty acyls selected from palmitoyl, butyryl, cerotoyl, decanoyl, docosenoyl, dodecanoyl, eleostearoyl, heptanol, hexanoyl, eicosanoyl, eicosenoyl, lignoceroyl, linoleoyl, lipoyl, myristreoyl, nonanoyl, octadecanoyl, octanoyl, palmitoyl, stearoyl, undecanoyl, and valeryl; Indrill; -NHC 6~16 Ariel; Monosaccharide or disaccharide portion; Biotin; -formula * -(OCH2CH2) n -R p (Poly)ethylene glycol (in the formula, * L 1 , represents the connection point to Y or Z, n is an integer from 4 to 12, and Rp is selected from -NH2OH or -Ome. An insecticidal compound as described in any one of paragraphs 1 to 4. 6. R 1An insecticidal compound according to any one of paragraphs 1 to 5, wherein is hydrogen or acetyl. 7. L 1 However, it does not exist, or -(C=O)C4~12alkylene-NH-(in the formula, * (This represents a connection point to Y or Z). An insecticidal compound described in any one of paragraphs 1 to 6, which is -(C=O)-C1~4alkylene-(C=O)-. 8. L 1 However, it does not exist, or [ka] (In the formula, * (represents a connection point to Y or Z); or [ka] The insecticidal compound described in any one of paragraphs 1 to 7. 9. L 1 An insecticidal compound described in any one of paragraphs 1 to 8, which does not exist. 10. An insecticidal compound according to any one of paragraphs 1 to 9, wherein the YZ portion comprises at least one modified amino acid or a non-natural amino acid analog. 11. Modified amino acids or unnatural amino acid analogs in peptides Y and Z, iN-methylated amino acids; ii. Non-proteinogenic amino acids, such as hydroxyproline (Hyp:L-hydroxyproline or (2S,4R)-4-hydroxyproline), octahydroindole-2-carboxylic acid (Oic), sarcosine (Sar), norleucine (Nle), α-aminoisobutyric acid (Aib), or thiazolidinedione-4-carboxylic acid (Thz); iii. α-alkylated (e.g., α-methylated) amino acids iv. D-amino acids; v. Beta-amino acids; vi. Peptoid amino acid analogs; vii. Sugar-modified amino acids; or viii. Biotin-modified amino acids An insecticidal compound selected from any one of paragraphs 1 to 10. 12. Modified amino acids or unnatural amino acid analogs in peptides Y and Z, iN-methylated amino acids; ii. Non-proteinogenic amino acids, such as hydroxyproline (Hyp:L-hydroxyproline or (2S,4R)-4-hydroxyproline), octahydroindole-2-carboxylic acid (Oic), sarcosine (Sar), norleucine (Nle), α-aminoisobutyric acid (Aib), or thiazolidinedione-4-carboxylic acid (Thz); iii. α-methylated amino acids; iv. D-amino acids; or v. Beta-amino acids An insecticidal compound selected from any one of paragraphs 1 to 11. 13. Modified amino acids or unnatural amino acid analogs in peptides Y and Z, iN-methylated amino acids; ii. Non-proteinogenic amino acids, such as hydroxyproline (Hyp:L-hydroxyproline or (2S,4R)-4-hydroxyproline), octahydroindole-2-carboxylic acid (Oic), sarcosine (Sar), norleucine (Nle), α-aminoisobutyric acid (Aib), or thiazolidinedione-4-carboxylic acid (Thz); iii. α-methylated amino acids; iv. D-amino acids An insecticidal compound selected from any one of paragraphs 1 to 12. 14. Modified amino acids or unnatural amino acids, iN-methylated amino acids; ii. α-aminoisobutyric acid (Aib); iii. Thiazolidine-4-carboxylic acid (Thz); iv. α-methylated amino acids vD-amino acids An insecticidal compound selected from any one of paragraphs 1 to 13. 15. R 2 However, NH2, NR2a H or NR 2a R 2b And R 2a and R 2b If each of them exists, independently, C 1~6 An insecticidal compound according to any one of paragraphs 1 to 14, wherein the compound is alkyl (e.g., methyl, ethyl, propyl, butyl, pentyl, or hexyl). 16. R 2 An insecticidal compound according to any one of paragraphs 1 to 15, wherein is NH2. 17. An insecticidal compound having the following formula (Ia). R 1 -L 1 -Y a -Z a -R 2 (Ia) (In the formula, R 1 , L 1 , and R 2 This is as provided for in any one of paragraphs 1 through 16; Y a is a Y base as defined in any one of paragraphs 1 to 16, and optionally, Y a It is either absent or a peptide containing 1 to 12 amino acids; Z a The formula is: -F # -H # -S # -W # -G # It is the peptide of (SEQ ID NO: 1) During the ceremony, `` # (The notation indicates that the residues "F", "H", "S", "W", and "G" are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs.) 18. Motif Y a -Z a At least one of the residues in the molecule is a modified amino acid or a non-natural amino acid analog, and optionally, however, S # If the residue is an α-aminoisobutyric acid group ([Aib]), then motif Y a -Z aThe insecticidal compound described in paragraph 19, further comprising at least one D-amino acid. 19. The "S" in the Z motif # The insecticidal compound according to paragraph 19 or 20, wherein the residue is a modified amino acid or a non-natural amino acid analog. 20. Y does not exist, or the following formula applies: Y a1 ---K # -Q # -R # It is a peptide, In the formula, Y a1 It is either absent or a peptide containing 1 to 9 amino acids; During the ceremony, `` # " indicates that the residue is one of the naturally occurring amino acids, modified amino acids, or unnatural amino acid analogs as defined in any one of paragraphs 13 to 16, as described in any one of paragraphs 19 to 21. 21. YZ is, formula: Y a1 ---K # -Q # -R # ---FH # -S # -WG(sequence number 13); or FH # -S # -WG (Sequence ID 138) It is a peptide, In the formula, Y a1 It is either absent or a peptide containing 1 to 9 amino acids; During the ceremony, `` # The notation " indicates that the residues "K", "Q", "R", "H", and "S" are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs; The insecticidal compound according to any one of paragraphs 17 to 20, wherein at least one of the residues "K", "Q", "R", "H", and "S" is a modified amino acid or a non-natural amino acid analog as defined in any one of paragraphs 13 to 16. 22. YZ is, formula: Y a1 ---KQR# ---FH # -S # -WG(sequence number 139); or FH # -S # -WG (Sequence ID 138) It is a peptide, In the formula, Y a1 It is either absent or a peptide containing 1 to 9 amino acids; During the ceremony, `` # The notation " indicates that the residues "R", "H", and "S" are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs; At least one of the residues "R", "H", and "S" is a modified amino acid or unnatural amino acid analog as defined in any one of paragraphs 13 to 16; Optional, Y a -Z is the formula: Y a1 ---KQR # ---FHS # -WG(sequence number 15); or FHS # -WG (Sequence ID 7) It is a peptide, In the formula, Y a1 It is either absent or a peptide containing 1 to 9 amino acids; During the ceremony, `` # This indicates that residues "R" and "S" are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs; The insecticidal compound according to any one of paragraphs 17 to 21, wherein at least one of the residues "R" (if present) and "S" is a modified amino acid or a non-natural amino acid analog as defined in any one of paragraphs 13 to 16. 23. Y a The "S" in the motif # The insecticidal compound according to any one of paragraphs 17 to 22, wherein the residue is N-methylserine ([n-me-S]) or D-serine ([s]). 24. Z a The part is the formula: FH[Aib]WG (Sequence ID 3) FHsWG(sequence number 4); or An insecticidal compound according to any one of paragraphs 1 to 23, comprising FH[n-me-S]WG (Sequence ID 5). 25. Formula: Ac-KQrFH[Aib]WG-[NH2](Sequence ID 18); Ac-NSVVLGKKQrFH[Aib]WG-[NH2](Sequence ID 19); Ac-FH[Aib]WG-[NH2](SEQ ID NO: 20) Ac-KQrFHsWG-[NH2](Sequence ID 21); Ac-FHsWG-[NH2](Sequence ID 22); NSVVLGKKQ[n-me-R]FH[n-me-S]WG-[NH2](Sequence ID 23) Compounds containing; Or its salt. 26. Insecticidal compounds having the following formula (Ib): R 1 -L 1 -Y b -Z b -R 2 (Ib) (In the formula, R 1 , L 1 , and R 2 This is as provided for in any one of paragraphs 1 through 25; Y b is a Y group as defined herein, and optionally, Y b It is either absent or a peptide containing 1 to 14 amino acids; Z b The formula is: -F # -X 2b -X 3b -W # -X 5b It is a peptide, During the ceremony, X 2b is the amino acid residue S # , Y # , N # or H #Selected from; X 3b is the amino acid residue S # , A # , P # , V # or T # Selected from; X 5b is amino acid residue A # Or G # Selected from; During the ceremony, `` # (The ') indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs as defined in any one of paragraphs 1 through 25. 27. Z b However, (ZbI)~(ZbVI)(Z b Sub-expression of): F # -S # -S # -W # -G # (Sequence code 24)(ZbI); F # -S # -S # -W # -A # (Sequence code 25)(ZbII); F # -N # -S # -W # -A # (Sequence number 26)(ZbIII); F # -Y # -S # -W # -G # (Sequence code 27)(ZbIV); F # -N # -A # -W # -A # (Sequence code 28)(ZbV); or F # -S # -A # -W # -G # (Sequence code 29)(ZbVI); A peptide having a formula selected from one of the following, Any residue marked with "#" in the formula is independently one of the unmodified amino acids, modified amino acids, or unnatural amino acid analogs listed in any one of paragraphs 1 to 26; Optionally, Z b However, (ZbI)~(ZbVI-I)(Z b Sub-expression of): F # -SS # -WG (Sequence ID 32)(ZbI-I); F # -SS # -WA (Sequence ID 33)(ZbII-I); F # -NS # -WA (Sequence ID 34)(ZbIII-I); F # -YS # -WG (Sequence ID 35)(ZbIV-I); F # -NA # -WA (sequence number 36)(ZbV-I); or F # -SA # -WG (Sequence ID 37)(ZbVI-I) A peptide having a formula selected from one of the following, The insecticidal compound according to paragraph 26, wherein any residue marked with "#" is independently an unmodified amino acid, modified amino acid, or unnatural amino acid analog as defined in any one of paragraphs 1 to 26. 28. The insecticidal compound according to paragraph 26 or 27, wherein the modified or unnatural amino acid analog is selected from N-methylated amino acids, aminoisobutyric acid (Aib), D-amino acids, or beta-amino acids. 29. Z b but, FSSWG (Sequence ID 40) FSSWA (Sequence ID 41) FNSWA (Sequence ID 42) FYAWG (Sequence ID 43) FN[Aib]WA (Sequence ID 44) FN-βA-WA (SEQ ID NO: 45) (n-me-F)-SsWG(Sequence ID 46) (N-me-F)-S-βA-WG (Sequence ID 47) (N-me-F)-S-(α-Me)S-WG(Sequence ID 48) Selected from; and / or Y b but, DPKYK(sequence number 51); AK; AR; SK; VP; PI; GPD; Sk; RQKTV(sequence number 52); PA; or ASDKHGRPKQT(Sequence ID 53) An insecticidal compound selected from any one of paragraphs 28 to 30. 30. Insecticidal compounds having the following formula (Ic): R 1 -L 1 - Y c -Z c -R 2 (I C) (In the formula, R 1 , L 1 , and R 2 This is as provided for in any one of paragraphs 1 through 29; Y c Y is a Y group as defined in any one of paragraphs 1 to 29, and optionally, Yc is either absent or a peptide containing 1 to 12 amino acids; Z c The formula is: -F # -S # -X 3c -W # -G # (Sequence 2) It is a peptide, In the formula, X 3c is amino acid residue A # , P# , V # or T # Selected from; During the ceremony, `` # (The symbol indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs.) 31. Z c However, the formula: -FSX 3c -WG(Sequence ID 118)(ZcI) It is a peptide, X 3c However, amino acid residue A # , P # , V # or T # Selected from; Optional, X 3c However, P # or V # The insecticidal compound described in paragraph 30. 32. Z c However, the formula selected from ZcI-I to ZcI-IV is: -FSA # -WG (Sequence ID 119)(ZcI-I) -FSP # -WG (Sequence ID 120)(ZcI-II) -FSV # -WG (Sequence ID 121)(ZcI-III) -FST # -WG (Sequence ID 122)(ZcI-IV) The insecticidal compound described in paragraph 30 or 31, which is a peptide. 33. An insecticidal compound according to any one of paragraphs 31 to 33, wherein one or more modified amino acids or unnatural amino acid analogs are independently selected from N-methylated amino acids, aminoisobutyric acid (Aib), thiazolidinedione-4-carboxylic acid (Thz), beta-amino acids, or D-amino acids. 34. Z c However, the formula: FSPWG (Sequence ID 101) FSAWG (Sequence ID 102) FSVWG (Sequence ID 103) FSTWG (Sequence ID 104) FS-βA-WG (SEQ ID NO: 105) FS-Thz-WG (Sequence ID 106) A peptide selected from; and / or Y c However, it does not exist, or VR; N; KVK; SFS; or Y An insecticidal compound selected from any one of paragraphs 30 to 33. 35. Select an insecticidal compound from the following: DPKYKFSSWG-[NH2] (SEQ ID NO: 59); AKFSSWG-[NH2] (SEQ ID NO: 60); ARFSSWA-[NH2] (Sequence ID 61); SKFNSWA-[NH2] (SEQ ID NO: 62); AKFSSWA-[NH2] (SEQ ID NO: 63); ARFNSWA-[NH2] (Sequence ID 64); VPFNSWA-[NH2] (SEQ ID NO: 65); PIFSSWG-[NH2] (Sequence ID 66); GPDFYAWG-[NH2] (Sequence ID 67); Ac-KQrFH[Aib]WG-[NH2] (Sequence ID 18); Ac-NSVVLGKKQrFH[Aib]WG-[NH2] (Sequence ID 19); Ac-FH[Aib]WG-[NH2] (Sequence ID 20); Ac-KQrFHsWG-[NH2] (Sequence ID 21); Ac-FHsWG-[NH2] (Sequence ID 22); NSVVLGKKQ[n-me-R]FH[n-me-S]WG-[NH2] (Sequence ID 23); Ac-SkFN-Aib-WA-[NH2] (Sequence ID 68); Ac-SK-[n-me-F]-N-(α-Me)Ser-WA-[NH2] (Sequence ID 69); Ac-PA-[n-me-F]-SsWG-[NH2] (Sequence ID 70); RQKTVFSSWG-[NH2] (Sequence ID 71); PAFSSWG-[NH2] (Sequence ID 72); ASDKHGRPKQTFSSWG-[NH2] (Sequence ID 73); VRFSPWG-[NH2] (Sequence ID 107); NFSPWG-[NH2] (SEQ ID NO: 108); KVKFSAWG-[NH2] (Sequence ID 109); SFSPWG-[NH2] (SEQ ID NO: 110); FSPWG-[NH2] (Sequence ID 111); YFSPWG-[NH2] (Sequence ID 112); KVKFSVWG-[NH2] (Sequence ID 113); KVKFSTWG-[NH2] (Sequence ID 114); Ac-PA-[n-me-F]-S-Ba-WG-[NH2] (Sequence ID 74); Ac-PA-[n-me-F]-S-(α-Me)S-WG-[NH2] (Sequence ID 75); Ava-FS-βA-WG-[NH2] (SEQ ID NO: 116); Ava-FS-Thz-WG-[NH2] (Sequence ID 117); or its salt or solvate. 36. A composition comprising a compound described in any one of paragraphs 1 to 35, mixed with one or more solvents, carriers, diluents, auxiliaries, preservatives, dispersants, emulsifiers, or synergists, for example, an insect control composition or a plant protection composition. 37. The composition described in paragraph 36, which is an aqueous composition. 38. The composition according to paragraph 36 or 37, further comprising one or more kinin peptides, AKH peptides, DH31 peptides, DH44 peptides, pyrokinin peptides, or CAPA peptides (e.g., CAPA-1, CAPA-2, or CAPA-3 analogs). 39. Use as an insecticide of any compound described in any one of paragraphs 1 to 35, or of a composition described in paragraphs 36, 37, or 38, wherein such use is optionally used against Diptera, Hemiptera, or Lepidoptera insects. 40. The aforementioned use is a) Diptera insects (where Z is the Z defined in paragraph 2) a It is the basis; b) Hemiptera insects (e.g., *Hymenomorpha harris* or *Hymenomorpha persicae* insects) (where Z is the Z defined in paragraph 2) b It is the basis; c) Lepidopteran insects (e.g., Plutella xirostera) (where Z is the Z defined in paragraph 2) c (It is the basis) The use described in paragraph 39 is for use as an insecticide against [unspecified]. 41. A method for increasing the mortality rate of insects, comprising the step of contacting an insect or an insect population with a compound described in any one of paragraphs 1 to 35, or a composition described in paragraph 36, 37, or 38, a) The insect population is a Diptera insect population, and Z is of the choice specified in paragraph 2. a It is the basis; b) The insect population is a group of hemipteran insects (e.g., *Hygromorpha harris* or *Camponotus persicae*), and optionally Z is the Z specified in paragraph 2. b It is the basis; c) The insect population is a group of lepidopteran insects (e.g., Plutella xirostera), and optionally Z is the Z defined in paragraph 2. c The basis, the method. 42. a) Diptera insects (optional, where Z is the Z defined in paragraph 2) a It is the basis; b) Hemiptera insects (e.g., *Hymenomorpha harris* or *Campomorpha persicae* insects) (optional, where Z is the Z defined in paragraph 2) b It is the basis; c) Lepidopteran insects (e.g., Plutella xirostera) (optional, where Z is the Z defined in paragraph 2) c Use as a plant protectant for protecting plants from (the base) the compounds described in any one of paragraphs 1 to 35, or the compositions described in paragraphs 36, 37, or 38. 43. A method for inhibiting insect parasitism of plants, comprising the step of contacting a plant with a compound described in any one of paragraphs 1 to 35, or a composition described in paragraphs 36, 37, or 38, a) The insect is a Diptera insect, and optionally Z is the Z specified in paragraph 2. a It is the basis; b) The insect is a hemipteran insect (e.g., *Hymenomorpha harris* or *Hymenomorpha persicae*), and optionally Z is the Z specified in paragraph 2. b It is the basis; c) The insect is a lepidopteran insect (e.g., Plutella xirostera), and optionally Z is the Z specified in paragraph 2. c It is the basis; A method of applying a compound to plants at a time when, by choice, there are no insects present or substantially no insects present on the plants. 44. A method for reducing insect infestation on plants or reducing the insect load on plants, comprising the step of contacting a plant with a compound described in any one of paragraphs 1 to 35, or a composition described in paragraphs 36, 37, or 38. a) The insect is a Diptera insect, and optionally Z is the Z specified in paragraph 2. a It is the basis; b) The insect is a hemipteran insect (e.g., *Hymenomorpha harris* or *Hymenomorpha persicae*), and optionally Z is the Z specified in paragraph 2. b It is the basis; c) The insect is a lepidopteran insect (e.g., Plutella xirostera), and optionally Z is the Z specified in paragraph 2. c The basis, the method.

Claims

1. An insecticidal compound having the following formula (XX), or a salt or solvate thereof: R 1 -L 1 -Y 1 -Y-Z-Y 2 -R 2 (XX) (In the formula, R 1 is hydrogen (which may be denoted as "H-" or "Hy-"), C 1～4 alkyl (e.g., methyl, ethyl, propyl, butyl), formyl, -N(R 1a )-C(=N + (R 1b )(R 1c ))NR 1d R 1e 、-C(=N + (R 1b )(R 1c ))NR 1d R 1e 、acyl, fatty acyl, benzyl, benzoyl, heteroaryl or trifluoroacetyl, -NHC 1～18 alkyl, -NHC 6～16 aryl, -NH-C 1～6 alkyl-C 6～10 aryl, biotin, sugar moiety or (poly)alkylene glycol, phosphate or sulfate; R 1a , R 1b , R 1c , R 1d and R 1e Each of them is either hydrogen or C 1～4 Independently selected from alkyl groups (e.g., methyl, ethyl, propyl, butyl); Any alkyl, formyl, acyl, fatty acyl, benzyl, benzoyl, heteroaryl or trifluoroacetyl, -NHC 1～18 Alkyl, -NHC 6～16 aryl, -NH-C 1～6 Alkyl-C 6～10 Aryl or (poly)alkylene glycols contain halogens, C 1～6 Alkyl, C 1～6 It may be substituted with one or more groups selected from haloalkyl groups, sugar moieties, phosphates, or sulfates; L 1 It does not exist, or * -(C=O)C 1～16 Alkylene-NH-(in the formula, * Y 1 , represents a connection point to Y or Z); (C 1～20 ) Alkilen, (C 2～20 ) Alkenylene, (Poly)alkylene glycol; L 1 This may be substituted with one or more groups selected from oxo (=O), halogen, =N, and =S; Y 1 It is either absent or a peptide containing one or two amino acids; Y is either absent or a peptide containing 1 to 16 amino acids; Y may contain a (poly)alkylene glycol linker in its peptide sequence; Y 2 It is either absent or a peptide containing one or two amino acids; Z is expressed by the formula: F # -X 2 -X 3 -W # -X 5 It is a peptide, During the ceremony, X 2 is, S # , Y # , K # , N # , or H # Selected from; X 3 is, S # , A # , P # , V # , or T # Selected from; X 5 G # , A # Selected from; During the ceremony, `` # " indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs; R 2 NH 2 , NR 2a H, NR 2a R 2b , OH or OR 2a And; in the formula, R 2a and R 2b Each of them, if present, independently, C 1～6 Alkyl (e.g., methyl, ethyl, propyl, butyl, pentyl, or hexyl), C 3～6 Alkenil, C 6～16 Ariel, C 6～16 Aryl-C 1～6 Alkyl, C 1～6 Alkylene-C 6～16 Aryl, or C 1～6 These are haloalkyls, and each of them is a halogen, C 1～6 Alkyl, or C 1～6 (May be substituted with one or more groups selected from haloalkyl groups.)

2. An insecticidal compound having the following formula (I), or a salt or solvate thereof: R 1 -L 1 -Y-Z-R 2 (I) (In the formula, R 1 is hydrogen (which may be denoted as "H-", or "Hy-"), C 1～4 alkyl (e.g., methyl, ethyl, propyl, butyl), formyl, -N(R 1a )-C(=N + (R 1b )(R 1c ))NR 1d R 1e 、-C(=N + (R 1b )(R 1c ))NR 1d R 1e 、acyl, fatty acyl, benzyl, benzoyl, heteroaryl or trifluoroacetyl, -NHC 1～18 alkyl, -NHC 6～16 aryl, -NH-C 1～6 alkyl-C 6～10 aryl, biotin, sugar moiety or (poly)alkylene glycol; R 1a , R 1b , R 1c , R 1d and R 1e Each of them is either hydrogen or C 1～4 Independently selected from alkyl groups (e.g., methyl, ethyl, propyl, butyl); Any alkyl, formyl, acyl, fatty acyl, benzyl, benzoyl, heteroaryl or trifluoroacetyl, -NHC 1～18 Alkyl, -NHC 6～16 aryl, -NH-C 1～6 Alkyl-C 6～10 Aryl or (poly)alkylene glycols contain halogens, C 1～6 Alkyl, C 1～6 It may be substituted with one or more groups selected from the haloalkyl or sugar moieties; L 1 It does not exist, or * -(C=O)C 1～16 Alkylene-NH-(in the formula, * (This represents a connection point to Y or Z). (C 1～20 ) Alkilen, (C 2～20 ) Alkenylene, (Poly)alkylene glycol; L 1 This may be substituted with one or more groups selected from oxo (=O), halogen, =N, and =S; Y is either absent or a peptide containing 1 to 16 amino acids; Y may contain a (poly)alkylene glycol linker in its peptide sequence; Z is expressed by the formula: F # -X 2 -X 3 -W # -X 5 It is a peptide, During the ceremony, X 2 is, S # , Y # , K # , N # , or H # Selected from (preferably X 2 is, S # , Y # , N # , or H # (Selected from) X 3 is, S # , A # , P # , V # , or T # Selected from; X 5 G # , A # Selected from; During the ceremony, `` # " indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs; R 2 NH 2 , NR 2a H, NR 2a R 2b , OH or OR 2a (preferably, R 2 NH 2 , NR 2a H, NR 2a R 2b OR 2a And); in the formula, R 2a and R 2b Each of them, if present, independently, C 1～6 Alkyl (e.g., methyl, ethyl, propyl, butyl, pentyl, or hexyl), C 3～6 Alkenil, C 6～16 Ariel, C 6～16 Aryl-C 1～6 Alkyl, C 1～6 Alkylene-C 6～16 Aryl or C 1～6 These are haloalkyls, and each of them is a halogen, C 1～6 Alkyl or C 1～6 (May be substituted with one or more groups selected from haloalkyl groups.)

3. Y 1 and Y 2 The insecticidal compound according to claim 1, wherein the insecticidal compound is absent.

4. Z, Z a , Z b or Z c A peptide selected from, During the ceremony, a)Z a The formula is: -F # -H # -S # -W # -G # It is the peptide of (SEQ ID NO: 1); b)Z b The formula is: -F # -X 2b -X 3b -W # -X 5b It is a peptide, During the ceremony, X 2b is the amino acid residue S # , Y # , K # , N # Or H # Selected from; X 3b is the amino acid residue S # , A # , P # , V # Or T # (Optional S # Or A # ) selected from; X 5b is amino acid residue A # Or G # Select from, or c)Z c The formula is: -F # -S # -X 3c -W # -G # (Sequence 2) It is a peptide, In the formula, X 3c is amino acid residue A # , P # , V # Or T # Selected from; During the ceremony, `` # The insecticidal compound according to any one of claims 1 to 3, wherein the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs.

5. The insecticidal compound according to any one of claims 1 to 4, wherein Y is absent or a peptide containing 1 to 14 amino acids.

6. R 1 but, hydrogen; Acyls that may be substituted with sugar moieties; Fatty acyl; heteroaryl; -NHC 6～16 Ariel; sugar part; Biotin; or formula * -(OCH 2 CH 2 ) n -R p (Poly)ethylene glycol (in the formula, * L 1 , Y 1 , represents a connection point to Y or Z, n is an integer from 1 to 16, and Rp is -NH 2 Selected from OH or -Ome; Optionally, R 1 but, hydrogen; An acyl which may be substituted with a sugar moiety, wherein the acyl group is selected from formyl, acetyl (Ac), propanoyl, and butanoyl; Fatty acyls selected from palmitoyl, butyryl, cerotoyl, decanoyl, docosenoyl, dodecanoyl, eleostearoyl, heptanol, hexanoyl, eicosanoyl, eicosenoyl, lignoceroyl, linoleoyl, lipoyl, myristreoyl, nonanoyl, octadecanoyl, octanoyl, palmitoyl, stearoyl, undecanoyl, and valeryl; Indrill; -NHC 6～16 Ariel; Monosaccharide or disaccharide portion; Biotin; -formula * -(OCH 2 CH 2 ) n -R p (Poly)ethylene glycol (in the formula, * L 1 , Y 1 , represents a connection point to Y or Z, n is an integer between 4 and 12, and Rp is -NH 2 Selected from OH or -Ome; Furthermore, R 1 The insecticidal compound according to any one of claims 1 to 5, wherein is hydrogen or acetyl.

7. L 1 However, it does not exist, or -(C=O)C 4～12 Alkylene-NH-(in the formula, * Y 1 , represents a connection point to Y or Z); -(C=O)-C 1～4 It is alkylene-(C=O)-; Optional, L 1 However, it does not exist, or 【Chemistry 1】 (In the formula, * Y 1 , representing a connection point to Y or Z); or 【Chemistry 2】 and; Furthermore, L 1 The insecticidal compound according to any one of claims 1 to 6, wherein the presence of [the specified element] is not required.

8. The insecticidal compound according to any one of claims 1 to 7, wherein the YZ portion comprises at least one modified amino acid or a non-natural amino acid analog.

9. Modified amino acids or unnatural amino acid analogs in peptides Y and Z, iN-methylated amino acids; ii. Non-proteinogenic amino acids, such as hydroxyproline (Hyp:L-hydroxyproline or (2S,4R)-4-hydroxyproline), octahydroindole-2-carboxylic acid (Oic), sarcosine (Sar), norleucine (Nle), α-aminoisobutyric acid (Aib), or thiazolidinedione-4-carboxylic acid (Thz); iii. α-alkylated (e.g., α-methylated) amino acids iv. D-amino acids; v. Beta-amino acids; vi. Peptoid amino acid analogs; vii. Sugar-modified amino acids; or viii. Biotin-modified amino acids An insecticidal compound selected from any one of claims 1 to 8.

10. Modified amino acids or unnatural amino acid analogs in peptides Y and Z, iN-methylated amino acids; ii. Non-proteinogenic amino acids, such as hydroxyproline (Hyp:L-hydroxyproline or (2S,4R)-4-hydroxyproline), octahydroindole-2-carboxylic acid (Oic), sarcosine (Sar), norleucine (Nle), α-aminoisobutyric acid (Aib), or thiazolidinedione-4-carboxylic acid (Thz); iii. α-methylated amino acids; iv. D-amino acids; or v. Beta-amino acids An insecticidal compound selected from any one of claims 1 to 9.

11. Modified amino acids or unnatural amino acid analogs in peptides Y and Z, iN-methylated amino acids; ii. Non-proteinogenic amino acids, such as hydroxyproline (Hyp:L-hydroxyproline or (2S,4R)-4-hydroxyproline), octahydroindole-2-carboxylic acid (Oic), sarcosine (Sar), norleucine (Nle), α-aminoisobutyric acid (Aib), or thiazolidinedione-4-carboxylic acid (Thz); iii. α-methylated amino acids; iv. D-amino acids An insecticidal compound selected from any one of claims 1 to 10.

12. Modified amino acids or unnatural amino acids, iN-methylated amino acids; ii. α-aminoisobutyric acid (Aib); iii. Thiazolidine-4-carboxylic acid (Thz); iv. α-methylated amino acids vD-amino acids An insecticidal compound selected from any one of claims 1 to 11.

13. R 2 However, NH 2 , NR 2a H, NR 2a R 2b , or OR 2a And; R 2a and R 2b If each of them exists, independently, C 1～6 Alkyl (e.g., methyl, ethyl, propyl, butyl, pentyl, or hexyl); Optionally, R 2 However, NH 2 , NR 2a H or NR 2a R 2b And R 2a and R 2b If each of them exists, independently, C 1～6 The insecticidal compound according to any one of claims 1 to 12, wherein the compound is alkyl (e.g., methyl, ethyl, propyl, butyl, pentyl, or hexyl).

14. R 2 NH 2 The insecticidal compound according to any one of claims 1 to 13.

15. Insecticide compounds having the following formula (Ia): R 1 -L 1 -Y a -Z a -R 2 (Ia) (In the formula, R 1 , L 1 , and R 2 This is as provided for in any one of claims 1 to 14; Y a is a Y base as defined in any one of claims 1 to 14, and optionally, Y a It is either absent or a peptide containing 1 to 12 amino acids; Z a The formula is: -F # -H # -S # -W # -G # It is the peptide of (SEQ ID NO: 1) During the ceremony, `` # (The notation indicates that the residues "F", "H", "S", "W", and "G" are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs.)

16. Motif Y a -Z a At least one of the residues in the molecule is a modified amino acid or a non-natural amino acid analog, and optionally, however, S # If the residue is an α-aminoisobutyric acid group ([Aib]), then motif Y a -Z a The insecticidal compound according to claim 15, further comprising at least one D-amino acid.

17. "S" in the Z motif # The insecticidal compound according to claim 15 or 16, wherein the residue is a modified amino acid or a non-natural amino acid analog.

18. Y does not exist, or the following expression: Y a1 ---K # -Q # -R # It is a peptide, In the formula, Y a1 It is either absent or a peptide containing 1 to 9 amino acids; During the ceremony, `` # " indicates that the residue is one of the naturally occurring amino acids, modified amino acids, or unnatural amino acid analogs as defined in either claim 13 or 14; Optionally, YZ is given by the formula: Y a1 ---K # -Q # -R # ---FH # -S # -WG(sequence number 13); or FH # -S # -WG (Sequence ID 138) It is a peptide, In the formula, Y a1 It is either absent or a peptide containing 1 to 9 amino acids; During the ceremony, `` # The notation " indicates that the residues "K", "Q", "R", "H", and "S" are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs; The insecticidal compound according to any one of claims 15 to 17, wherein at least one of the residues "K", "Q", "R", "H", and "S" is a modified amino acid or a non-natural amino acid analog as defined in any one of claims 13 or 14.

19. YZ is the formula: Y a1 ---KQR # ---FH # -S # -WG(sequence number 139); or FH # -S # -WG (Sequence ID 138) It is a peptide, In the formula, Y a1 It is either absent or a peptide containing 1 to 9 amino acids; During the ceremony, `` # The notation " indicates that the residues "R", "H", and "S" are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs; At least one of the residues "R", "H", and "S" is a modified amino acid or unnatural amino acid analog as defined in either claim 13 or 14; Optional, Y a -Z is the formula: Y a1 ---KQR # ---FHS # -WG(sequence number 15); or FHS # -WG (Sequence ID 7) It is a peptide, In the formula, Y a1 It is either absent or a peptide containing 1 to 9 amino acids; During the ceremony, `` # This indicates that residues "R" and "S" are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs; The insecticidal compound according to any one of claims 1 to 18, wherein at least one of the residues "R" (if present) and "S" is a modified amino acid or a non-natural amino acid analog as defined in any one of claims 13 to 16.

20. Y a The "S" in the motif # The insecticidal compound according to any one of claims 15 to 19, wherein the residue is N-methylserine ([n-me-S]) or D-serine ([s]).

21. Z a The part is the formula: FSSWG (Sequence ID 40) FH[Aib]WG (Sequence ID 3) FHsWG(sequence number 4); or It has FH[n-me-S]WG (Sequence ID 5), Optionally, Z a The part is the formula: FHsWG(sequence number 4); or The insecticidal compound according to any one of claims 1 to 20, comprising FH[n-me-S]WG (Sequence ID 5).

22. The following insecticidal compounds can be selected: Hy-DPKYKFSSWG-[NH 2 ] (Sequence ID 59); Hy-AKFSSWG-[NH 2 ] (Sequence ID 60); Hy-ARFSSWA-[NH 2 ] (Sequence ID 61); Hy-SKFNSWA-[NH 2 ] (Sequence ID 62); Hy-AKFSSWA-[NH 2 ] (Sequence ID 63); Hy-ARFNSWA-[NH 2 ] (Sequence ID 64); Hy-VPFNSWA-[NH 2 ] (Sequence ID 65); Hy-PIFSSWG-[NH 2 ] (Sequence ID 66); Hy-GPDFYAWG-[NH 2 ] (Sequence ID 67); Ac-KQrFH[Aib]WG-[NH 2 ] (Sequence ID 18); Ac-NSVVLGKKQrFH[Aib]WG-[NH 2 ] (Sequence ID 19); Ac-FH[Aib]WG-[NH 2 ] (Sequence ID 20); Ac-KQrFHsWG-[NH 2 ] (Sequence ID 21); Ac-FHsWG-[NH 2 ] (Sequence ID 22); Hy-NSVVLGKKQ[n-me-R]FH[n-me-S]WG-[NH 2 ] (Sequence ID 23); Ac-SkFN-Aib-WA-[NH 2 ] (Sequence ID 68); Ac-SK-[n-me-F]-N-(α-Me)Ser-WA-[NH 2 ] (Sequence ID 69); Ac-PA-[n-me-F]-SsWG-[NH 2 ] (Sequence ID 70); Hy-RQKTVFSSWG-[NH 2 ] (Sequence ID 71); Hy-PAFSSWG-[NH 2 ] (Sequence ID 72); Hy-ASDKHGRPKQTFSSWG-[NH 2 ] (Sequence ID 73); Hy-VRFSPWG-[NH 2 ] (Sequence ID 107); Hy-NFSPWG-[NH 2 ] (Sequence ID 108); Hy-KVKFSAWG-[NH 2 ] (Sequence ID 109); Hy-SFSPWG-[NH 2 ] (Sequence ID 110); Hy-FSPWG-[NH 2 ] (Sequence ID 111); Hy-YFSPWG-[NH 2 ] (Sequence ID 112); Hy-KVKFSVWG-[NH 2 ] (Sequence ID 113); Hy-KVKFSTWG-[NH 2 ] (Sequence ID 114); Ac-PA-[n-me-F]-S-βA-WG-[NH 2 ] (Sequence ID 74); Ac-PA-[n-me-F]-S-(α-Me)S-WG-[NH 2 ] (Sequence ID 75); ava-FS-βA-WG-[NH 2 ] (Sequence ID 116); Ava-FS-Thz-WG-[NH 2 ] (Sequence ID 117); Hy-GPAFSSWG-[NH 2 ] (Sequence ID 92); Hy-AAAFNSWG-[NH 2 ] (Sequence ID 93); Hy-NAAFSSWG-[nh2] (Sequence ID 94); Hy-NAAFNSWG-[NH 2 ] (Sequence ID 95); Hy-VPAFNSWG-[NH 2 ] (Sequence ID 96); Hy-TNTAFSSWG-[NH 2 ] (Sequence ID 97); Hy-PRFYSWG-[NH 2 ] (Sequence ID 98); Hy-GADFYAWG-[NH 2 ] (Sequence ID 99); Hy-DPAFNSWG-[NH 2 ] (Sequence ID 76); Hy-SSAFNSWG-[NH 2 ] (Sequence ID 77); Hy-RAFTSTGSSRSPAFSSWG-[NH 2 ] (Sequence ID 78); Hy-PASFSSWG-[NH 2 ] (Sequence ID 79); Hy-DAGFSSWG-[NH 2 ] (Sequence ID 80); Hy-SSGFSSWG-[NH 2 ] (Sequence ID 81); Hy-DPVFKSWG-[NH 2 ] (Sequence ID 82); Hy-DAAFSSWG-[NH 2 ] (Sequence ID 83); Hy-GSGFSSWG-[NH 2 ] (Sequence ID 84); Hy-DDDSDVSESGSKFSSWG-[NH 2 ] (Sequence ID 85); Hy-SFSSWG-[NH 2 ] (Sequence ID 86); Hy-GFSSWG-[NH 2 ] (Sequence ID 87); Hy-LDRSEGRVSKALFSSWG-[NH 2 ] (Sequence ID 88); Hy-WGQSSVGAVFSSWG-[NH 2 ] (Sequence ID 89); Hy-GAEFYSWG-[NH 2 ] (Sequence ID 90); Hy-FSSWG-[NH 2 ] (Sequence ID 91); or [Ac]-SK[n-me-F]N[βAla]WA-[NH 2 ] (Sequence ID 100); or its salt or solvate.

23. A composition comprising a compound according to any one of claims 1 to 22, mixed with one or more solvents, carriers, diluents, adjuvants, preservatives, dispersants, emulsifiers, or synergists, for example, an insect control composition or a plant protection composition, Optionally, the composition is an aqueous composition, and / or the composition further comprises one or more of the following: kinin peptide, AKH peptide, DH31 peptide, DH44 peptide, pyrokinin peptide, or CAPA peptide (e.g., CAPA-1, CAPA-2, or CAPA-3 analogues).

24. The use of a compound according to any one of claims 1 to 22, or a composition according to claim 23, as an insect control agent, wherein the use is optionally applied to Diptera, Hemiptera, or Lepidoptera insects; The use of the above is optional. a) Diptera insects (where Z is the Z defined in claim 4) a It is the basis; b) Hemiptera insects (e.g., *Hymenomorpha harris*, *Aphis fabae*, *Pea long-horned aphid*, *Two-spotted green leafhopper*, *Twisteria persicae*, or *Pleurocera spp.*) (where Z is the Z defined in claim 4) b It is the basis; c) Lepidopteran insects (e.g., Plutella xirostera or Spodoptera fulgiperda) (where Z is the Z defined in claim 4) c (It is the basis) It is used as an insecticide against [unspecified].

25. A method for increasing the mortality rate of insects, comprising the step of contacting an insect or an insect population with a compound according to any one of claims 1 to 22 or a composition according to claim 23, a) The insect population is a population of Diptera insects, and optionally Z is Z as defined in claim 4. a It is the basis; b) The insect population is a population of hemipteran insects (e.g., *Hymenomorpha harris*, *Aphis fabae*, *Pea aphid*, *Two-spotted green leafhopper*, *Twisteria persicae*, or *Pleuroceris*), and optionally Z is Z as defined in claim 4. b It is the basis; c) The insect population is a lepidopteran insect population (e.g., Plutella xirostera or Spodoptera fulgiperda), and optionally Z is Z as defined in claim 4. c The basis, the method.

26. a) Diptera insects (optional, where Z is the Z defined in claim 4) a It is the basis; b) Hemiptera insects (e.g., *Hymenomorpha harris*, *Aphis fabae*, *Pea aphid*, *Two-spotted green leafhopper*, *Twisteria persicae*, or *Pleuroceras spp.*) (optional, where Z is as defined in claim 4) b It is the basis; c) Lepidopteran insects (e.g., Plutella xirostera or Spodoptera fulgiperda) (optional, where Z is the Z defined in claim 4) c (It is the basis) Use of a compound according to any one of claims 1 to 22, or a composition according to claim 23, as a plant protectant for protecting plants from

27. A method for inhibiting insect parasitism of plants, comprising the step of contacting a plant with a compound according to any one of claims 1 to 22 or a composition according to claim 23, a) The insect is a Diptera insect, and optionally Z is Z as defined in claim 4. a It is the basis; b) The insect is a hemipteran insect (e.g., *Hymenomorpha harris*, *Aphis fabae*, *Pea aphid*, *Two-spotted green leafhopper*, *Twisteria persicae*, or *Pleuroceris*), and optionally Z is Z as defined in claim 4. b It is the basis; c) The insect is a lepidopteran insect (e.g., Plutella xirostera or Spodoptera fulgiperda), and optionally Z is Z as defined in claim 4. c It is the basis; A method of applying a compound to plants at a time when, by choice, there are no insects present or substantially no insects present on the plants.

28. A method for reducing insect infestation on plants or reducing insect load on plants, comprising the step of contacting a plant with a compound according to any one of claims 1 to 22 or a composition according to claim 23, a) The insect is a Diptera insect, and optionally Z is Z as defined in claim 4. a It is the basis; b) The insect is a hemipteran insect (e.g., *Hymenomorpha harris*, *Aphis fabae*, *Pea aphid*, *Two-spotted green leafhopper*, *Twisteria persicae*, or *Pleuroceris*), and optionally Z is Z as defined in claim 4. b It is the basis; c) The insect is a lepidopteran insect (e.g., Plutella xirostera or Spodoptera fulgiperda), and optionally Z is Z as defined in claim 4. c The basis, the method.

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