Insect neuropeptide analogs

By developing AKH peptides and analogues with specific structures as insecticides, the problems of environmental and non-target species damage caused by existing insecticides have been solved, achieving highly efficient insecticidal effects on insects encoding AKH peptides while protecting important pollinators.

CN122070296APending Publication Date: 2026-05-19SOLASTA BIO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SOLASTA BIO LTD
Filing Date
2024-10-23
Publication Date
2026-05-19

AI Technical Summary

Technical Problem

Existing insecticides are harmful to the environment and non-target species, making it difficult to achieve target-specific insecticidal effects, especially for insects encoding AKH peptides such as Hemiptera, Diptera, Lepidoptera, Blattodea, and Coleoptera.

Method used

AKH peptides and their analogues with specific structures were developed as insecticidal compounds. They were prepared by chemical synthesis and applied to insects to achieve insecticidal activity against these insects, while having almost no effect on important pollinators such as bees.

Benefits of technology

It provides highly effective insecticidal effects against insects encoding AKH peptides, such as Hemiptera, Diptera, Lepidoptera, Blattodea, and Coleoptera, while reducing harm to the environment and non-target species, especially to pollinators such as bees.

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Abstract

The present invention relates to insect neuropeptide compounds of the AKH family and analogs thereof having activity against insects, such as hemiptera, diptera, lepidoptera, cockroaches and / or coleopteran insects, such as aphids and fruit flies, and their use as insect control agents (e.g. Insecticides) and plant protection agents.
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Description

Technical Field

[0001] This invention relates to insect neuropeptide compounds and analogues having activity against insects, such as Hemiptera, Diptera, Lepidoptera, Blattodea and / or Coleoptera, such as aphids and fruit flies, and their use as insect control agents (e.g., pesticides) and plant protectants. Background Technology

[0002] With the global dependence on broad-spectrum insecticides and their damaging effects well documented, there is a growing need to develop more environmentally friendly, target-specific insecticides to protect valuable crops. The development and use of neuropeptides and their synthetic analogues offer a promising pathway to developing more environmentally friendly and target-specific insecticides.

[0003] In insects, neuropeptides are regulatory peptides that function in growth and development, behavior and reproduction, metabolism and homeostasis, and muscle movement. The insect neuropeptide family is large and includes insect kinins and CAPA (CAPA, CAP2b, CAPA3) neuropeptides, AKH peptides, and pyrogens.

[0004] Due to their high specificity, insect neuropeptides and their homologous receptors (G-protein coupled receptors, GPCRs) can be developed for use in pesticides to selectively reduce the fitness of target pest insects while minimizing harmful environmental impacts and minimizing harm to other non-target species such as pollinators, whose populations have declined sharply due to the use of pest control / pesticides.

[0005] It is known that AKH regulates lipid homeostasis. Gäde G, Auerswald LGen Comp Endocrinol. [General and Comparative Endocrinology] 1 June 2003; 132(1):10-20. doi: 10.1016 / s0016-6480(03)00159-x.

[0006] This invention provides lipid metabolism hormone (AKH) peptides and analogues. Summary of the Invention

[0007] The inventors have discovered novel AKHs and AKH analogues that have insecticidal activity against insects that encode AKHs (e.g., Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera) and thus have the potential to be used as pest control agents or insecticides while having little or no effect on important pollinator species (e.g., bees).

[0008] Therefore, in a first aspect, the present invention provides an insecticidal compound having the following formula (I): R 1-L 1 -Y 1 -YZY 2 -R 2 (I) in: R 1 It is hydrogen (which can be named "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, (poly)alkylene glycol, heterocyclic group, phosphate group or sulfate group; Where R 1a R 1b R 1c R 1d and R 1e Each is independently selected from hydrogen or C. 1-4 Alkyl groups (e.g., methyl, ethyl, propyl, butyl); And any alkyl, formyl, acyl, fatty acyl, benzyl, benzoyl, heteroaryl, trifluoroacetyl, -NHC 1-18 Alkyl, -NHC 6-16 Aryl, -NH-C 1-6 Alkyl-C 6-10 The aryl, (poly)alkylene glycol, or C(O) heterocyclic group may optionally be substituted by one or more groups selected from the following: halogen, oxo, C 1-6 Alkyl, C 1-6 Halogenated alkyl group, sugar moiety, phosphate group or sulfate group; L 1 It does not exist or: –(C=O)C 1-16 -alkylene-NH-, where Indicates Y 1 Attachment points of Y or Z; (C 1-20)alkylene (C 2-20 ) imidene group, (poly)alkylene glycols; Where L 1 Optionally substituted by one or more groups selected from the following: oxo (=O), halogen, cyano, =NR 1a NR 1a R 1b OR 1a S = S; where R 1a and R 1b Each is independently hydrogen or C 1-2 alkyl; Y 1 Peptides that either do not exist or contain one or two amino acids; Y is a peptide containing 1 to 12 amino acids; wherein Y optionally contains a (poly)alkylene glycol linker in the peptide sequence; Y 2 Peptides that either do not exist or contain one or two amino acids; Z is a peptide according to formula (Zi). Z 1 -Z 2 -F # -Z 4 -Z 5 -Z 6 -W # -Z 8 -Z 9 (Zi) in: Z 1 Does not exist or selected from L # I # or V # ; Z 2 Selected from T # or N # ; Z 4 Selected from S # or T # ; Z 5 Selected from P # R # S # or T # ; Z 6 Selected from D # S # N # T # or G # ; Z 8Does not exist or selected from G # or T # ; Z 9 Does not exist or selected from G # N # Q # or T # ; in" # This indicates that the residue is independently an unmodified amino acid, a modified amino acid, or a non-natural amino acid analogue listed; and R 2 It is NH2, NR 2a H, NR 2a R 2b OH or OR 2a ;where R 2a and R 2b If they exist, they are each independently C. 1-6 -alkyl (e.g., methyl, ethyl, propyl, butyl, pentyl, or hexyl), C 3-6 -Alkenyl, C 6-16- Aryl, C 6-16- Aryl-C 1-6 -alkyl, C 1-6 -alkylene-C 6-16 -Aryl or C 1-6 - Haloalkyl groups, each of which may optionally be substituted by one or more groups selected from: halogen, C 1-6 -alkyl or C 1-6- Halogenated alkyl groups.

[0009] In another aspect, the present invention provides an insecticidal compound having the following formula (II): R 1 -L 1 -YZR 2 (II) in: R 1 It is hydrogen (which can be named "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 1eAcyl, 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, (poly)alkylene glycol, heterocyclic group, phosphate group or sulfate group; Where R 1a R 1b R 1c R 1d and R 1e Each is independently selected from hydrogen or C. 1-4 Alkyl groups (e.g., methyl, ethyl, propyl, butyl); And any alkyl, formyl, acyl, fatty acyl, benzyl, benzoyl, heteroaryl, trifluoroacetyl, -NHC 1-18 Alkyl, -NHC 6-16 Aryl, -NH-C 1-6 Alkyl-C 6-10 The aryl, (poly)alkylene glycol, or C(O) heterocyclic group may optionally be substituted by one or more groups selected from the following: halogen, oxo, C 1-6 Alkyl, C 1-6 Halogenated alkyl group, sugar moiety, phosphate group or sulfate group; L 1 It does not exist or: –(C=O)C 1-16 -alkylene-NH-, where Indicates the attachment point to Y or Z; (C 1-20 )alkylene (C 2-20 ) imidene group, (poly)alkylene glycols; Where L 1 Optionally substituted by one or more groups selected from the following: oxo (=O), halogen, cyano, =NR 1a NR 1a R 1b OR 1a S = S; where R 1a and R 1b Each is independently hydrogen or C 1-2 alkyl; Y is a peptide containing 1 to 12 amino acids; wherein Y optionally contains a (poly)alkylene glycol linker in the peptide sequence; Z is a peptide according to formula (Zi). Z 1 -Z 2 -F# -Z 4 -Z 5 -Z 6 -W # -Z 8 -Z 9 (Zi) in: Z 1 Does not exist or selected from L # I # or V # ; Z 2 Selected from T # or N # ; Z 4 Selected from S # or T # ; Z 5 Selected from P # R # S # or T # ; Z 6 Selected from D # S # N # T # or G # ; Z 8 Does not exist or selected from G # or T # ; Z 9 Does not exist or selected from G # N # Q # or T # ; in" # This indicates that the residue is independently an unmodified amino acid, a modified amino acid, or a non-natural amino acid analogue listed; and R 2 It is NH2, NR 2a H, NR 2a R 2b OH or OR 2a ;where R 2a and R 2b If they exist, they are each independently C. 1-6 -alkyl (e.g., methyl, ethyl, propyl, butyl, pentyl, or hexyl), C 3-6 -Alkenyl, C 6-16- Aryl, C 6-16- Aryl-C 1-6 -alkyl, C 1-6-alkylene-C 6-16 -Aryl or C 1-6 - Haloalkyl groups, each of which may optionally be substituted by one or more groups selected from: halogen, C 1-6 -alkyl or C 1-6- Halogenated alkyl groups.

[0010] Suitablely, compounds having formulas (I) and (II) contain at least one modified amino acid or a non-natural amino acid analogue, such as in Y 1 Y, Y 2 In and / or in the Z group. At least one modified amino acid or non-natural amino acid analogue may be as defined anywhere herein.

[0011] mark" # "" indicates that the residue in question can be a modified version of an amino acid, or that the residue can be replaced by a non-natural amino acid analogue. For example, S # The residue can be a serine, a modified serine (e.g., D-serine, β-serine), or a non-natural amino acid (e.g., [Aib]).

[0012] In another aspect, a composition is provided comprising a compound as defined herein, or a salt or solvation thereof, mixed with one or more solvents, carriers, diluents, adjuvants, preservatives, dispersants, emulsifiers, or synergists. Suitably, the composition is an agricultural composition, an insect control composition, or a plant protection composition.

[0013] On the other hand, the use of compounds as defined herein, or their salts or solvates, or compositions as defined herein, as insect control agents is provided. This use can be as an insecticide against insects encoding AKH peptides. This use can be as an insecticide against Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera, preferably Hemiptera, Diptera, and / or Lepidoptera.

[0014] On the other hand, a method for increasing insect mortality is provided, comprising contacting an insect colony with a compound as defined herein or a salt or solvate thereof, or a composition as defined herein. Suitably, the insects are insects encoding AKH peptides, such as Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera, preferably Hemiptera, Diptera, and / or Lepidoptera.

[0015] On the other hand, a method for increasing the mortality rate of Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera insects is provided, the method comprising contacting a population of Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera insects with a compound as defined herein or a salt thereof or a composition as defined herein.

[0016] On the other hand, the use of compounds as defined herein, or their salts or solvates, or compositions as defined herein, as plant protectants for protecting plants from insects encoding AKH peptides is provided.

[0017] In another aspect, the use of compounds as defined herein or their salts or solvates, or compositions as defined herein, as plant protectants for protecting plants from the influence of insects of the orders Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera, preferably Hemiptera, Diptera, and / or Lepidoptera.

[0018] On the other hand, a method for inhibiting plant infection by insects encoding AKH peptides is provided, the method comprising contacting the plant with a compound as defined herein or a salt or solvate thereof, or a composition as defined herein. Suitably, the compound or composition is applied to the plant when the plant has no or substantially no insects encoding AKH peptides.

[0019] On the other hand, a method for inhibiting plant infestation by Hemiptera, Diptera, and / or Lepidoptera insects is provided, the method comprising contacting the plant with a compound as defined herein or a salt thereof, or a composition as defined herein. Suitably, the compound or composition is applied to the plant when there are no or substantially no Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera insects. Preferably, the insects are selected from Hemiptera, Diptera, and / or Lepidoptera insects.

[0020] On the other hand, methods are provided for reducing the infection of plants by insects encoding AKH, or for reducing the load of insects encoding AKH on plants, the method comprising contacting the plant with a compound as defined herein or a salt or solvate thereof or a composition as defined herein.

[0021] On the other hand, methods are provided for reducing plant infection by Hemiptera, Diptera, Lepidoptera, Blattodea and / or Coleoptera insects, or methods for reducing the load of Hemiptera, Diptera, Lepidoptera, Blattodea and / or Coleoptera insects on plants, the methods comprising contacting the plants with a compound as defined herein or a salt thereof or a composition as defined herein.

[0022] Suitable insects encoding AKH peptides include Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera, with Hemiptera, Diptera, and / or Lepidoptera being preferred.

[0023] On the other hand, a method for producing the insecticidal compound according to the first aspect is provided, the method comprising: (a) Chemically synthesized insecticidal compounds of formula (I) or (II) or their precursors.

[0024] In one embodiment, chemical synthesis includes the methods described in the examples.

[0025] On the other hand, the use of compounds or compositions as defined herein as insect control agents or plant protectants for insect protection of plants or parts thereof is provided.

[0026] On the other hand, compounds or compositions as defined herein are provided for use with the following purposes: a) Diptera insects, preferably selected from: Drosophila melanogaster or Drosophila suzuki; b) Hemiptera insects, such as aphids, preferably selected from: beet aphids, pea aphids, peach aphids, cotton leafhoppers, blackcurrant long-tubed aphids, or cereal constrictor aphids; and / or c) Lepidoptera, preferably selected from: diamondback moth, fall armyworm, or tussock moth; and / or d) Blattodea insects, preferably of which the German cockroach is.

[0027] On the other hand, a method for increasing insect mortality is provided, which involves contacting insects or insect populations with a compound or composition as defined herein.

[0028] On the other hand, a method for inhibiting or preventing insect infestation of a plant is provided, the method comprising contacting the plant or a portion thereof, or the location where the plant is growing or is intended to grow, with a compound or composition as defined herein. Suitably, the compound or composition is contacted with the plant or a portion thereof, or the location where the plant is growing or is intended to grow, when there are no or substantially no insects present in the plant or a portion thereof.

[0029] On the other hand, a method for reducing or treating insect infestation of plants or reducing insect load on plants is provided, the method comprising contacting the plant or a portion thereof, or the location where the plant is growing, with a compound or composition as defined herein.

[0030] Suitablely, the location where plants are growing or are expected to grow may include agricultural locations suitable for growing plants, preferably including fields.

[0031] Appropriately, insects are: a) Diptera insects, preferably selected from: Drosophila melanogaster or Drosophila suzuki; b) Hemiptera insects, such as aphids, preferably selected from beet aphids, pea aphids, peach aphids, cotton leafhoppers, blackcurrant long-tubed aphids or cereal constrictor aphids; c) Lepidoptera insects, preferably selected from: diamondback moth, striped armyworm or fall armyworm; d) Coleoptera insects; and / or d) Blattodea insects, preferably of which the German cockroach is.

[0032] More appropriately, insects are: a) Diptera insects, preferably selected from: Drosophila melanogaster or Drosophila suzuki; b) Hemiptera insects, such as aphids, preferably selected from beet aphids, pea aphids, peach aphids, cotton leafhoppers, blackcurrant long-tubed aphids, or cereal constrictor aphids; and / or c) Lepidoptera insects, preferably selected from diamondback moth, fall armyworm or tussock moth.

[0033] Suitablely, contact with insects or insect colonies, plants or parts thereof, or locations includes treating insects or insect colonies, plants or parts thereof, or locations with compositions as defined herein by means of: irrigation, feeding, spraying, misting, foaming, fogging, hydroponics, hydroponics, coating, immersion, injection, and / or coating. Contact may include injecting plants (e.g., trees) or parts thereof with compositions as defined herein using systems and methods such as those described in WO 2020 / 021041, WO 2023 / 161802, WO 2022 / 264053, WO 2022 / 189386, WO2022 / 165248, WO 2021 / 152093, WO 2020 / 212612, and WO 2020 / 021041 (the entire contents of which are incorporated herein by reference).

[0034] Suitablely, the insect or insect colony, plant or part thereof, or location is brought into contact with an effective concentration of the compound as defined herein, preferably at 10 -3 M to 10 -9 The concentrations between M.

[0035] Further features of aspects and embodiments of the invention will now be defined under the following headings. Any feature in any section may be combined with any aspect of the embodiments in any feasible combination. Detailed Implementation definition

[0036] Throughout this specification and claims, the conventional three-letter and single-letter codes for naturally occurring amino acids are used, 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).

[0037] In this text, if a single-letter code is accompanied by a "#" symbol, it indicates that it can be in its natural form, a modified form, or can be replaced by non-protein amino acids. For example, "A # "This includes unmodified alanine, modified alanine (e.g., N-methylalanine), or indicator alanine residues that can be replaced by another non-natural amino acid analog (e.g., α-aminoisobutyric acid (Aib)). Suitably, the residues can be in their naturally occurring or modified forms. Suitably, individual residues in the peptide can be replaced by non-protein amino acids."

[0038] The term "amino acid" as used in this article can refer to naturally occurring amino acids or any other amino acids, including synthetic amino acids and non-protein amino acids. "Naturally occurring" in this article refers to the 20 amino acids encoded by the standard genetic code, sometimes called protein amino acids.

[0039] The term amino acid is an abbreviation for α-amino[α-amino]carboxylic acid. Each molecule contains a central carbon (C) atom, called the α-carbon, to which an amino and a carboxyl group are attached. The other two bonds of the α-carbon atom are usually satisfied by hydrogen (H) atoms and side chains, as shown in the following R:

[0040] The modified amino acid in this invention can be an α-alkylated amino acid, wherein the α hydrogen atom has been replaced by C. 1-6 Alkyl groups (e.g., methyl or ethyl groups) are substituted. Preferably, the α-alkylated amino acid is an α-methylated amino acid, such as α-methyl-L-serine (given the symbol [α-Me)S]: α-Methyl-L-serine

[0041] Alternatively, the recognized three-letter codes and other abbreviations for amino acids can be used, such as hydroxyproline (Hyp: L-hydroxyproline or (2S,4R)-4-hydroxyproline), octahydroindole-2-carboxylic acid (Oic), sarcosine (Sar), ortholeucine (Nle), α-aminoisobutyric acid (Aib), naphthylalanine (Nal), thiazolidin-4-carboxylic acid (Thz), phenylglycine (Phg), etc.

[0042] The term "Nal" indicates that an amino acid residue has been replaced by a naphthylalanine residue:

[0043] The term "Thz" indicates that an amino acid residue has been replaced by a thiazolidin-4-carboxylic acid residue, such as (R)-thiazolidin-4-carboxylic acid. (R)-Thiazolidin-4-carboxylic acid

[0044] Ahx indicates 6-aminohexanoic acid (also known as 6-aminocaproic acid or ε-aminocaproic acid). Ado indicates 12-aminododecanoic acid.

[0045] The symbol "n-me" preceding the amino acid code is used to indicate an N-methylated amino acid residue. Thus, for example, "[n-me-V]" indicates N-methylvaline, "[n-me-A]" indicates N-methylalanine, and "[n-me-L]" indicates N-methylleucine.

[0046] The symbol "tBu" following the amino acid code indicates an amino acid residue modified with a tert-butyl group. Therefore, for example, "Ser(tBu)" indicates tert-butylserine.

[0047] The symbol "Boc" following the amino acid code indicates an amino acid residue modified with a tert-butoxycarbonyl group.

[0048] The symbol "Trt" following the amino acid code indicates an amino acid modified with triphenylmethyl, also known as a triphenylmethyl group.

[0049] The sarcosine residue ([Sar]) is an alternative name for the N-methylglycine residue ([n-me-G]). .

[0050] When used in the general formula or sequence in this specification, especially when the remainder of the formula or sequence is indicated by a single-letter code, such other amino acids may be indicated in square brackets “[]” (e.g., “[Aib]”).

[0051] Unless otherwise stated, the amino acid residues in the peptides of this invention are in the L-configuration. However, D-configuration amino acids may be incorporated as modifications. In this context, the amino acid code written in lowercase letters may be used to indicate the D-configuration of the amino acid, for example, [a] indicates the D-configuration of alanine.

[0052] β-amino acid residues can also be used in the compounds of this invention. Such residues can be represented by the symbol "β", followed by the conventional code of the corresponding α-amino acid. Thus, [βhL] (or [B3L]) represents a residue of β-homoleucine (3-amino-5-methylhexanoic acid), [βA] represents a residue of β-alanine (3-aminopropionic acid), [βhA] (or [B3A]) represents a residue of β-homoalanine, [βhV] represents a residue of β-homovaline (sometimes called β-leucine (3-amino-4-methylvaleric acid)), [βhF] (or [B3F]) represents a residue of β-homo-phenylalanine, and [βhP] (or [B3P]) represents a residue of β-homoproline.

[0053] Amino acid "peptide analogs" are analogs in which the side chain is linked to the nitrogen atom of the peptide backbone, rather than to the α-carbon as in protein peptides. These residues can be represented by the symbol "peptide analog," followed by the regular code for the corresponding α-amino acid. Examples of peptide analogs include peptides of phenylalanine. Peptides of phenylalanine. The aforementioned residues may also have the symbols [peptide-F], [peptide-Phe], or [NPhe], indicating a peptide containing phenylalanine.

[0054] "Biotin-modified" amino acid analogs are amino acid residues incorporated with a biotin moiety as part of their side chain. For example, the symbol "[Biotin-K]" indicates a lysine residue modified at the side chain to include a biotin moiety. The biotin moiety can also be attached to amino acid side chains via a linker group (such as PEG or an amino-terminated PEG group). For example, an aspartic acid (or glutamine) side chain modified with a PEG-linked biotin moiety: (The above residues are given the symbol [Biotin-PEG-D])

[0055] Alternatively or additionally, the biotin portion may be at the terminal position. Therefore, R1 can be biotin. The symbol [biotin]- denotes the terminal biotin portion, for example, the partial sequence [biotin]-S has the following formula:

[0056] Amino acid modification can involve, for example, the covalent linking of two specific amino acid side chains via an intramolecular reaction between side chains, thereby creating a cyclic amide structure in the peptide sequence. Such structures can be formed via intramolecular amide formation through a condensation reaction between certain amino acid residues on the side chains (particularly arginine or lysine) and the side chains of aspartic acid or glutamic acid. Suitablely, the residues linked via intramolecular side chain reactions are adjacent to each other, separated by one residue or two residues.

[0057] Specific examples of residues linked intramolecularly via their side chain (K) and glutamic acid (E) can undergo amide formation via a condensation reaction. In a specific example, lysine and glutamic acid are separated by a single amino acid residue (e.g., leucine), as shown below: [Circular-KLE] Such groups can have the symbol [cyclic-KLE], with the bold text indicating that the K and E residues are linked via their side chains to form a cyclic amide structure.

[0058] As used herein, the terms “polypeptide,” “protein,” and “peptide” are used interchangeably and refer to a polymer of amino acids of any length, including both coding and non-coding amino acids. As used herein, amino acid residues will be indicated by their full names or according to standard three-letter or one-letter amino acid codes, as above.

[0059] Symbol C x-xx This refers to the number of carbon atoms in a functional group. The number at the "x" position indicates the minimum number of carbon atoms, and the number at the "xx" position indicates the maximum number of carbon atoms. For example, C 1-6 -alkyl refers to an alkyl group having 1 to 6 carbon atoms as defined herein.

[0060] The symbols i, n, or t used in this article are associated with various alkyl groups in a conventional manner. Specifically, the suffix indicates the arrangement of atoms and represents a straight-chain ('n') or branched ('i' or 't') alkyl group.

[0061] As used herein, the term "alkyl" refers to a saturated straight-chain or branched monovalent hydrocarbon group, wherein the alkyl group may optionally be substituted. The number of carbon atoms in an alkyl group can be specified using the symbols described above; for example, when there are 1 to 8 carbon atoms, the term C can be used. 1-8 -alkyl. Examples of alkyl groups include methyl (Me, -CH3), ethyl (Et, -CH2CH3), 1-propyl (n-Pr, n-propyl, -CH2CH2CH3), 2-propyl (i-Pr, isopropyl, -CH(CH3)2) and 1-butyl (n-Bu, n-butyl, -CH2CH2CH2CH3).

[0062] An "alkylene", "alkenylene", or "alkynylene" group is an alkyl, alkenyl, or alkynyl group located between two other chemical groups and used to connect these two other chemical groups. Therefore, "C 1-6 "alkylene" refers to a straight-chain saturated divalent hydrocarbon group with one to six carbon atoms or a branched saturated divalent hydrocarbon group with three to six 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-).

[0063] As used herein, the term "alkenyl" refers to a straight-chain or branched monovalent hydrocarbon group having at least one unsaturated site (i.e., a carbon-carbon double bond). Alkenyl radicals may optionally be substituted and include radicals having "cis" and "trans" orientations or alternatively "E" and "Z" orientations. The number of carbon atoms in an alkenyl group can be specified using the notation described above; for example, when there are 2 to 8 carbon atoms, the term C can be used. 2-8 -Alkenyl. Examples of alkenyl groups include, but are not limited to, vinyl (-CH=CH2) and propenyl (-CH=CHCH3).

[0064] In the chemical structures drawn in this article, " "or" The presence of “” indicates an attachment point or free radical, such as the free radical discussed in relation to various functional groups.

[0065] The term "aryl" refers to a ring or polycyclic aromatic ring having 5 to 12 carbon atoms. The term aryl includes both monovalent and divalent substances. Aryl groups include groups having a single ring and groups having more than one ring, such as fused rings or spiro rings. In the case of groups having more than one ring, at least one of these rings is aromatic. The number of carbon atoms in an aryl group can be specified using the notation described above; for example, when there are 6 to 16 carbon atoms, the term C can be used. 6-16 -Aryl. The aryl group may optionally be substituted. Examples of aryl groups include phenyl, naphthyl, biphenyl, phenanthrene, tetraphenyl, 1,2,3,4-tetrahydronaphthyl, 1H-indenyl, 2,3-dihydro-1H-indenyl, and fluorene. The preferred aryl group is fluorene.

[0066] The term "heteroaryl" or "heteroaromatic" refers to an aromatic monocyclic, bicyclic, or polycyclic compound containing one or more (e.g., 1-4, particularly 1, 2, or 3) heteroatoms selected from nitrogen, oxygen, or sulfur. The term heteroaryl includes both monovalent and divalent compounds. Examples of heteroaryl groups are monocyclic and bicyclic groups containing five to twelve ring members, more typically five to ten. A heteroaryl group can be, for example, a 5- or 6-membered monocyclic or a 9- or 10-membered bicyclic, such as a bicyclic structure formed by fused 5- and 6-membered rings or two fused 6-membered rings. Each ring may contain up to about four heteroatoms typically selected from nitrogen, sulfur, and oxygen. Typically, a heteroaryl ring will contain up to 3 heteroatoms, more typically up to 2, such as a single heteroatom. In one embodiment, the heteroaryl ring contains at least one cyclic nitrogen atom. The nitrogen atom in a heteroaryl ring can be basic, as in the case of imidazole or pyridine, or substantially non-basic, as in the case of indole or pyrrole nitrogen. Generally, the number of basic nitrogen atoms present in a heteroaryl group (including any amino substituents in the ring) will be less than five.

[0067] Examples of heteroaryl groups include furanyl, pyrroleyl, thiopheneyl, oxazolyl, isoxazolyl, imidazolyl, pyrazolyl, thiazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, triazolyl, tetrazolyl, pyridyl, pyrimidinyl, pyrazinyl, 1,3,5-triazenoyl, benzofuranyl, indolyl, isoindolyl, benzothiopheneyl, benzooxazolyl, benzoimidazolyl, benzothiazolyl, benzothiazolyl, indolyl, purinyl, benzofuranyl, quinolinyl, isoquinolinyl, quinazolinyl, and quinoxolinyl. The terms "heteroaryl" also encompass certain aromatic bicyclic or polycyclic systems, wherein at least one ring is an aromatic ring and one or more other rings are non-aromatic, saturated, or partially saturated rings, provided that at least one ring contains one or more heteroatoms selected from nitrogen, oxygen, or sulfur. Examples of heteroaryl groups in some denomeric aromatic families include, for example, tetrahydroisoquinolinyl, tetrahydroquinolinyl, 2-oxo-1,2,3,4-tetrahydroquinolinyl, dihydrobenzothiophene, dihydrobenzofuranyl, 2,3-dihydro-benzo[1,4]dioxinyl, benzo[1,3]m-dioxacyclopentenyl, 2,2-dioxo-1,3-dihydro-2-benzothiophene, 4,5,6,7-tetrahydrobenzofuranyl, indololinyl, 1,2,3,4-tetrahydro-1,8-naphthidyl, 1,2,3,4-tetrahydropyrido[2,3-b]pyrazinyl, and 3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazinyl. A particularly preferred heteroaryl group is the indole group, which can be linked to the peptide via a CH2C(O) linker and is named "[Ind]".

[0068] Examples of five-membered heteroaryl groups include, but are not limited to, pyrrole, furanyl, thiophene, imidazolyl, furazonyl, oxazolyl, oxadiazolyl, oxatriazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, triazolyl, and tetrazolyl.

[0069] Examples of six-membered heteroaryl groups include, but are not limited to, pyridyl, pyrazinyl, pyridinyl, pyrimidinyl, and triazinyl.

[0070] The bicyclic heteroaryl group can be, for example, selected from the following groups: A benzene ring fused with a 5- or 6-membered ring containing 1, 2, or 3 heteroatoms; A pyridine ring fused with a 5- or 6-membered ring containing 1, 2, or 3 heteroatoms; A pyrimidine ring fused with a 5- or 6-membered ring containing one or two heteroatoms; Pyrrole rings fused with 5- or 6-membered rings containing 1, 2, or 3 heteroatoms; A pyrazole ring fused with a 5- or 6-membered ring containing 1 or 2 heteroatoms; Pyrazine rings fused with 5- or 6-membered rings containing 1 or 2 heteroatoms; Imidazole rings fused with 5- or 6-membered rings containing 1 or 2 heteroatoms; Oxazole rings fused with 5- or 6-membered rings containing 1 or 2 heteroatoms; An isoxazole ring fused with a 5- or 6-membered ring containing 1 or 2 heteroatoms; Thiazole rings fused with 5- or 6-membered rings containing 1 or 2 heteroatoms; An isothiazole ring fused with a 5- or 6-membered ring containing 1 or 2 heteroatoms; Thiophene rings fused with 5- or 6-membered rings containing 1, 2, or 3 heteroatoms; Furan rings fused with 5- or 6-membered rings containing 1, 2, or 3 heteroatoms; Cyclohexyl rings fused with 5- or 6-membered heteroaromatic rings containing 1, 2, or 3 cyclic heteroatoms; and A cyclopentyl ring fused with a 5- or 6-membered heteroaromatic ring containing 1, 2, or 3 heteroatoms.

[0071] 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, isoyindolyl, indoleazinyl, indololinyl, isoyindololinyl, purine (e.g., adenine, guanine), indazole, benzodioxanepentenyl, and pyrazolopyridyl groups. A preferred bicyclic heteroaryl group is the indolyl group.

[0072] Specific examples of bicyclic heteroaryl groups containing two fused six-membered rings include, but are not limited to, quinolinyl, isoquinolinyl, chromanyl, thiochromanyl, chromenyl, isochromenyl, chromanyl, isochromanyl, benzodioxane, quinazinyl, benzooxazinyl, benzodiazinyl, pyridinylpyridinyl, quinoxolinyl, quinazolinyl, terpineyl, phthalazinyl, naphthidyl, and pteridylyl groups.

[0073] 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 fluorine, chlorine, bromine, and iodine.

[0074] The term "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, when there are 1 to 8 carbon atoms, the term C can be used. 1-8 - Haloalkyl. Examples of haloalkyl groups include trifluoromethyl (-CF3).

[0075] The term "comprising" is used in this specification and claims, and does not exclude other elements or steps. Indefinite or definite articles, such as "a" or "an," or "the," are used when referring to a singular noun, and this includes the plural form of the noun unless otherwise stated.

[0076] As used herein, the term "about" when referring to a measurable value such as a parameter, quantity, duration, etc., means a variation of + / -10% or less, preferably + / -5% or less, more preferably + / -1% or less, and even more preferably + / -0.1% or less, provided that such variation is suitable for implementation in the disclosed invention. It should be understood that the value referred to by the modifier "about" is itself specifically and preferably disclosed.

[0077] As used herein, “plant” refers to the whole plant or a part thereof, including fresh fruits, vegetables, and seeds. A plant or plant part can be a living plant or a part thereof. Furthermore, the term “plant” as used herein encompasses the whole plant, the ancestors and descendants of plants, and plant parts, including seeds, buds, stems, leaves, roots (including tubers), flowers, and tissues and organs, each of which contains the target gene / nucleic acid. The term “plant” also encompasses plant cells, suspension cultures, callus tissue, embryos, meristematic regions, gametophytes, sporophytes, pollen, and microspores, each of which also contains the target gene / nucleic acid.

[0078] As used herein, “crop” refers to a plant species or variety cultivated for harvest as food, livestock feed, fuel raw material, or for any other economic purpose. As non-limiting examples, the crop may include corn, cereals such as wheat, rye, barley, and oats, sorghum, rice, sugar beets and forage beets, fruits such as pome fruits (e.g., apples and pears), citrus fruits (e.g., oranges, lemons, limes, grapefruits, or tangerines), stone fruits (e.g., peaches, nectarines, or plums), nuts (e.g., almonds or walnuts), soft fruits (e.g., cherries, strawberries, blackberries, or raspberries), plantains or grapevines, legumes such as beans, lentils, peas, and soybeans, oilseed crops such as sunflowers, safflowers, rapeseed, castor beans, or olives, and gourds. Plants such as cucumbers, melons, or squash; fiber plants such as cotton, flax, or hemp; fuel crops such as sugarcane, miscanthus, or switchgrass; vegetables such as potatoes, tomatoes, peppers, lettuce, spinach, onions, carrots, eggplants, asparagus, or cabbage; ornamental plants such as flowers such as petunias, geraniums, roses, tulips, lilies, or chrysanthemums; shrubs; broad-leaved trees such as poplars or willows; and evergreen trees such as conifers; grasses such as lawns, turf, or pasture; or other useful plants such as coffee, tea, tobacco, hops, pepper, rubber, or latex plants.

[0079] As used herein, “pests” refers to organisms that are harmful to plants, animals, humans or human affairs, including but not limited to crop pests such as insects (defined below), household pests or insects such as cockroaches and ants, and disease vectors such as malaria mosquitoes.

[0080] As used herein, “pest infection” or “pest disease” means any inflammatory condition, disease, or disorder in a living organism (such as a plant, animal, or human) caused by a pest.

[0081] "Active substance", "active ingredient" or "effective ingredient" may be used interchangeably herein to mean any biological, biochemical or chemical element and its derivatives, fragments or compounds based thereon, including microorganisms, that has a general or specific effect on pests on a subject, particularly on insect pests of plants, plant parts or plant products (whether naturally occurring or manufactured, including any impurities that are unavoidably generated during the manufacturing process).

[0082] The terms “effective amount” and “effective dose” used in this article refer to the amount required to achieve the desired result.

[0083] The term "insect" as used here is used in a broad, popular sense, encompassing all species within the superphylum Arthropoda (classification Systema Naturae, Brands, SJ 1989-2005. Systema Naturae 2000. Amsterdam, Netherlands [http: / / sn2000.taxonomy.nl / ]), including the phyla Arthropoda, Tardigrade, and Clawed Animals; it includes all different stages of the life cycle, such as, but not limited to, egg, larva, nymph, pupa, and adult. Suitable insect pests are defined elsewhere in this text.

[0084] As used herein, "insecticide compound" refers to a compound that is biologically active against insects (as defined above), including but not limited to compounds capable of killing insects, larvicides, insect growth regulators, behavior-modifying compounds, attractants, repellents, pheromones, allergens, egogens, and insect pathogenic fungi, viruses, and proteins. Insecticides preferably exert their biological activity through contact with insects without requiring ingestion by the insects. This includes not only ready-to-use compounds or compound formulations but also inactive precursors that can be activated by external factors. Insecticides may be combined with materials used in conjunction, such as synergists or safeners, flavorings, or odor compositions. Preferably, the compound is contained in a carrier as defined above. "Contained in a carrier" as used herein means bound to or contained in a carrier by, for example, but not limited to, embedding, encapsulation, and adsorption.

[0085] Unless the context otherwise requires, throughout this specification, including the following claims, the words “comprise” and “include”, and variations such as “comprises”, “comprising”, and “including”, shall be understood to implicitly include the stated whole or step or group of wholes or steps, but do not exclude any other whole or step or group of wholes or steps.

[0086] It must be noted that, as used in the specification and appended claims, the singular forms “a / an” and “the” include plural indicators unless the context clearly specifies otherwise. Scopes herein may be expressed as “about” a specific value, and / or up to “about” other specific values. When such scopes are expressed, another embodiment includes from one specific value and / or up to another specific value. Similarly, when a value is expressed as an approximation using the antecedent “about,” it will be understood that the specific value forms another embodiment. The term “about” associated with numerical values ​​is optional and indicates, for example, + / - 10%. The compounds of the present invention

[0087] Specific compounds of the present invention include, for example, compounds of formula (I) or (II), wherein, unless otherwise stated, R 1 L 1 Y 1 Y, Z, Y 2 R 2 Each of these, and any associated substituents, has the meaning as defined in any of paragraphs (1) to (52) above or below: - (1)R 1 Selected from: hydrogen -C(=N + Me2)NMe 2, Acyl group Fatty acyl, benzyl, benzoyl, heteroaryl Trifluoroacetyl, -NHC 1-18 alkyl, -NHC 6-16 Aryl, -NH-C 1-6 Alkyl-C 6-10 Aryl; Sugar portion; Biotin; 5- or 6-membered heterocyclic groups; or (Poly)alkylene glycols (e.g., polyethylene glycol, such as PEG-1 to PEG-16); Where R 1a R 1b R 1c R 1d and R 1e Each is independently selected from hydrogen or C. 1-4 Alkyl groups (e.g., methyl, ethyl, propyl, butyl); And any alkyl, formyl, acyl, fatty acyl, benzyl, benzoyl, heteroaryl, trifluoroacetyl, -NHC 1-18 Alkyl, -NHC 6-16 Aryl, -NH-C 1-6 Alkyl-C 6-10 The aryl, (poly)alkylene glycol, or heterocyclic group may optionally be substituted by one or more groups selected from the following: oxo, halogen, C 1-6 Alkyl, C 1-6 Halogenated alkyl groups or sugar moieties. (2)R 1 Selected from: hydrogen; The acyl group may be optionally replaced by the following: sugar moiety; Fatty acyl group; Heteroaryl groups, such as indole; -NHC 6-16 Aryl; Sugar portion; Biotin; 5- or 6-membered heterocyclic groups; or Having a style –(OCH2CH2) n -R p (poly)ethylene glycol, in which Indicates with L 1 The attachment point of Y or Z, where n is an integer from 1 to 16, and R p Selected from -NH2, -OH, or -OMe; And any acyl, fatty acyl, benzyl, benzoyl, heteroaryl, -NHC 6-16 The aryl, (poly)alkylene glycol, or heterocyclic group may optionally be a substituted group that is optionally replaced by one or more groups selected from: halogen, oxo, C 1-3 Alkyl or C 1-3 Halogenated alkyl groups. (3)R 1 Selected from: hydrogen; The acyl group may be optionally substituted with the following: sugar moiety, wherein the acyl group is selected from formyl, acetyl (Ac), propionyl, butanoyl. Selected from the following fatty acyl groups: palmitoyl, butyryl, waxyl, decanoyl, dodecanoyl, tunganoyl, heptanoyl, hexanoyl, eicosanoyl, eicosanoyl, limonoyl, myristoyl, nonanoyl, octadecanoyl, octanoyl, palmitoyl, stearoyl, undecanoyl, and pentanoyl; Indole, such as 3-indole: ; -NHC 6-16 Aryl; Monosaccharide or disaccharide portion; Biotin; 5-6 membered heterocyclic groups, such as pyrrolidone-2-one: ; Having a style –(OCH2CH2) n -R p (poly)ethylene glycol, in which Indicates with L1 The attachment point of Y or Z, where n is an integer from 4 to 12, and R p Selected from -NH2, -OH, or -OMe; And any acyl, fatty acyl, benzyl, benzoyl, heteroaryl, -NHC 6-16 The aryl, (poly)alkylene glycol, or heterocyclic group may optionally be a substituted group that is optionally replaced by one or more groups selected from: halogen, oxo, C 1-3 Alkyl or C 1-3 Halogenated alkyl groups. (4)R 1 Selected from: hydrogen; The acetyl group may be optionally replaced by either a monosaccharide or a disaccharide moiety; pyrrolidone-2-one, for example : Palmitoyl; or Having a style –(OCH2CH2) n -NH2 in (poly)ethylene glycol, wherein Indicates Y 1 The attachment point is Y or Z, and n is an integer from 6 to 10. (5)R 1 Selected from: hydrogen; pyrrolidone-2-one, for example ; Palmitoyl; or Having a style –(OCH2CH2)8-NH2 in (poly)ethylene glycol, wherein Indicates Y 1 Attachment points of Y or Z. (6)R 1 It is hydrogen or pyrrolidone-2-one, for example . (7)L 1 It does not exist or: –(C=O)C 1-12 -alkylene-NH-, –(C=O)-C 1-10 Alkylene-(C=O)- –(C=O)-C 0-10 Alkylene; C 1-10 Alkylene; -(C=O)- Any of L 1The group may optionally be replaced by one or more oxo (=O) groups; in Indicates Y 1 Attachment points of Y or Z. (8)L 1 It does not exist or: –(C=O)C 4-12 -alkylene-NH-, –(C=O)-C 1-4 Alkylene-(C=O)- –(C=O)-C 1-4 Alkylene; C 1-4 Alkylene; -(C=O)- Any of L 1 The group may optionally be replaced by one or more oxo (=O) groups; in Indicates Y 1 Attachment points of Y or Z. (9)L 1 It does not exist or: ; ; ; ;or ; in Indicates Y 1 Attachment points of Y or Z. (10)L 1 It does not exist or: ; in Indicates Y 1 Attachment points of Y or Z. (11)R 1 and L 1 As defined below: (i)R 1 It is hydrogen, and L 1 Not found or selected from: a) –(C=O)C 1-16 -alkylene-NH-, where Indicates Y 1 Attachment points of Y or Z; b)C 4-14 Alkylene; c) –(C=O)-C 1-10 Alkylene; Where L 1 Optionally substituted with one or more oxo (=O) groups; (ii)R 1 An acyl group optionally substituted with a monosaccharide or disaccharide; and L 1 Not found or selected from: a) –(C=O)C 1-16 -alkylene-NH-, where Indicates Y 1 Attachment points of Y or Z; b)C 4-14 Alkylene; and c) –(C=O)-C 1-10 Alkylene; (iii)R 1 It is a fatty acyl group; and L 1 Not found or selected from: a) –(C=O)C 1-16 -alkylene-NH-, where Indicates Y 1 Attachment points of Y or Z; b)C 4-14 Alkylene; c) –(C=O)-C 1-10 Alkylene; (iv)R 1 It is a heteroaryl group; and L 1 Not found or selected from: a) –(C=O)C 1-16 -alkylene-NH-, where Indicates Y 1 Attachment points of Y or Z; b)C 4-14 Alkylene; c) –(C=O)-C 1-10 Alkylene; (v) has the formula –(OCH2CH2) n -NH2 or –(OCH 2-CH2) n (poly)ethylene glycol with -OH groups, wherein Indicates with L 1 The attachment point of Y or Z, and n is an integer from 1 to 16; and L 1 Selected from: a)C 1-14 Alkylene; b) –(C=O)-C 1-10 Alkylene; Where L 1 Optionally substituted with one or more oxo (=O) groups; (vi)R 1 It is a heterocyclic group optionally substituted with one or more oxo groups; and; L 1 Not found or selected from: a) –(C=O)-C 1-4 Alkylene; b)C 1-10 Alkylene; and c)-(C=O)-; in Indicates the attachment point to Y or Z; (vii)R 1 It is -NHC 6-16 Aryl and L 1 yes –(C=O)C 1-10 -alkylene-(C=O)-; in Indicates the attachment point to Y or Z. (12)R 1 and L 1 As defined below: (i)R 1 It is hydrogen, and L 1 It does not exist; (ii)R 1 It is an acyl group, and L 1 It does not exist; (iii)R 1 It is selected from the following fatty acyl groups: palmitoyl, butyryl, waxyl, decanoyl, dodecanoyl, tunganoyl, heptanoyl, hexanoyl, eicosanoyl, eicosanoyl, limonoyl, myristoyl, nonanoyl, octadecanoyl, octanoyl, palmitoyl, stearoyl, undecanoyl, and pentanoyl; L 1 It does not exist; (iv)R 1 It is an indole group, such as 3-indole group: ;as well as L 1 yes –(C=O)-C 1-4 Alkylene; (v)R 1 It has a formula –(OCH2CH2) n -NH2 or –(OCH2CH2) n (poly)ethylene glycol with -OH groups, wherein Indicates with L 1 The attachment point, and n is an integer from 6 to 10; and L 1 yes –(C=O)-C 1-4 Alkylene, wherein Indicates Y 1 Attachment points of Y or Z; Where L 1 Optionally substituted with one or more oxo (=O) groups; (vi)R 1 It is a 5- or 6-membered heterocyclic group optionally substituted with one or more groups selected from the following: halogen, oxo, C 1-3 Alkyl groups or C groups optionally substituted with one or more oxo groups 1-3 Halogenated alkyl groups; and; L 1 Not found or selected from: a) –(C=O)-C 1-4 Alkylene; b)C 1-10 Alkylene; and c)-(C=O)-; in Indicates the attachment point to Y or Z; (vi)R 1 It is -NHC 6-16 Aryl and L 1 yes –(C=O)C 1-6 -alkylene-(C=O)-. (13)R 1 and L 1 As defined below: (i)R 1 It is hydrogen, and L 1 It does not exist; (ii)R 1 It is an acetyl group, and L 1 It does not exist; (iii)R 1 It is palmitoyl; L 1 It does not exist; (iv)R 1 It is a heteroaryl group; and L 1 Does not exist or –(C=O)-C 1-10 Alkylene; (v)R 1 It has a formula –(OCH2CH2) n -NH2 or –(OCH2CH2) n (poly)ethylene glycol with -OH groups, wherein Indicates with L 1 The attachment point, and n is an integer from 4 to 12; and L 1 yes –(C=O)-C 1-10 Alkylene, wherein Indicates Y 1 Attachment points of Y or Z; Where L 1 Optionally substituted with one or more oxo (=O) groups; (vi)R 1 It is a 5- or 6-membered heterocyclic group optionally substituted with one or more oxo groups; and; L 1 Not found or selected from: a) –(C=O)-C 1-4 Alkylene; b)C 1-10 Alkylene; and c)-(C=O)-; in Indicates the attachment point to Y or Z; (vi)R 1 It is -NHC 6-16 Aryl and L 1 yes –(C=O)C 1-6 -alkylene-(C=O)-. (14)R 1 and L 1 As defined below: (i)R 1 It is hydrogen, and L1 Does not exist (ii)R 1 An acyl group optionally substituted with a monosaccharide or disaccharide; and L 1 Not found or selected from: a) –(C=O)C 1-16 -alkylene-NH-, where Indicates Y 1 Attachment points of Y or Z; b)C 4-14 Alkylene; c) –(C=O)-C 1-10 Alkylene; (iii)R 1 It is a fatty acyl group; and L 1 Not found or selected from: a) –(C=O)C 1-16 -alkylene-NH-, where Indicates Y 1 Attachment points of Y or Z; b)C 4-14 Alkylene; c) –(C=O)-C 1-10 Alkylene; (iv)R 1 It is a heteroaryl group; and L 1 Not found or selected from: a) –(C=O)C 1-16 -alkylene-NH-, where Indicates Y 1 Attachment points of Y or Z; b)C 4-14 Alkylene; c) –(C=O)-C 1-10 Alkylene; d)-(C=O)- (v) has the formula –(OCH2CH2) n -NH2 or –(OCH 2- CH2) n (poly)ethylene glycol with -OH groups, wherein Indicates with L 1 The attachment point of Y or Z, and n is an integer from 1 to 16; and L 1 Selected from: a)C 1-14 Alkylene; b) –(C=O)-C 1-10 Alkylene; c)-(C=O)- (vi)R 1 It is pyrrolidone-2-one; and; L 1 Selected from: a) –(C=O)-C 1-4 Alkylene; b)-(C=O)-; in Indicates the attachment point to Y or Z; (vi)R 1 It is -NHC 6-16 Aryl and L 1 yes –(C=O)C 1-6 -alkylene-(C=O)-; in Indicates the attachment point to Y or Z. (15)R 1 and L 1 As defined below: (i)R 1 It is hydrogen, and L 1 Does not exist; or R 1 It is hydrogen and L 1 yes –(C=O)C5 alkylene-NH2, where Indicates Y 1 The attachment point of Y or Z, i.e., R 1 With L 1 Together they form a group: (6-Aminohexanoic acid); or R 1 It is hydrogen and L 1 yes –(C=O)C 11 alkylene-NH2, wherein Indicates Y 1 The attachment point of Y or Z, i.e., R 1 With L 1 Together they form a group: (12-Aminododecanoic acid) (ii)R 1 It is an acetyl group, and L 1 It does not exist; (iii)R 1 It is palmitoyl; L 1 It does not exist; (iv)R 1 It is an indole group; and L 1 Does not exist or –(C=O)-C1 alkylene; That is, R 1 With L 1 Together they form a group: (v)R 1 It has a formula –(OCH2CH2)8-NH2 in (poly)ethylene glycol, wherein Indicates with L 1 The attachment point, and L 1 yes –(C=O)-ethylidene, where Indicates Y 1 Attachment points of Y or Z; Where L 1 Optionally substituted with one or more oxo (=O) groups; (vi)R 1 It is pyrrolidone-2-one and L 1 It is -(C=O)-; that is, R 1 With L 1 Together they form a group: (16)R 1 and L 1 As defined below: (i)R 1 It is hydrogen, and L 1 Does not exist; or (ii)R 1 It is palmitoyl; L 1 It does not exist; (iii)R 1 It has a formula –(OCH2CH2)8-NH2 in (poly)ethylene glycol, wherein Indicates with L 1 The attachment point, and L 1 yes –(C=O)-ethylidene, where Indicates Y 1 Attachment points of Y or Z; Where L 1 Optionally substituted with one or more oxo (=O) groups; (iv)R 1 It is pyrrolidone-2-one and L 1 It is -(C=O)-; that is, R 1 With L 1 Together they form a pyroglutamic acid group [pyr]: . (17) Y is a peptide containing 1 to 12 amino acids. (18) Y is either a peptide that does not exist or contains 1 to 6 amino acid residues. (19) Y is either a peptide that does not exist or contains 1 to 3 amino acid residues. (20) Y is absent or residue Q is absent. # ;in" # "" indicates that the residue is a naturally occurring amino acid, a modified amino acid, or a non-natural amino acid analogue. (21) Y is absent or residue Q. (22)Z 1 Does not exist or selected from L or I # ; (23)Z 1 It is L # ; (24)Z 2 Selected from T # or N # ; (25)Z 2 It is T # ; (26)Z 4 Selected from S # or T # ; (27)Z 4 It is S # ; (28)Z 4 It is T # ; (29)Z 5 Selected from P # R # or S # ; (30)Z 5 Selected from P # or S # ; (31)Z 6 Selected from D # S# N # or G # ; (32)Z 6 Selected from D # or S # ; (33)Z 8 and Z 9 Neither exists or: Z 8 Selected from T # or G # ; Z 9 Does not exist or selected from G # N # or T # ; (34)Z 8 and Z 9 Neither exists or: Z 8 Selected from T # or G # ; Z 9 Does not exist or selected from G # or N # ; (35)Z 8 and Z 9 None of them exist. (36) Z is a peptide having a formula selected from the following: L # -T # -F # -S # -P # -D # -W # (Z A (SEQ ID NO: 1) L # -T # -F # -T # -S # -S # -W # -G # -G # (Z B (SEQ ID NO: 2) L # -T # -F # -T # -P # -N # -W # (ZC )(SEQ ID NO: 3) I # -T # -F # -S # -R # -D # -W # -T # -G # (Z D )(SEQ ID NO: 4) T # -F # -S # -R # -D # -W # -T # -G # (Z E )(SEQ ID NO: 5) V # -N # -F # -T # -P # -T # -W # -G # -Q # (Z F )(SEQ ID NO: 6) L # -N # -F # -S # -P # -G # -W # (Z G )(SEQ ID NO: 7) L # -T # -F # -T # -S # -S # -W # -G # (Z H )(SEQ ID NO: 8) L # -T # -F # -S # -S # -G # -W # (Z I )(SEQ ID NO: 9) L # -T # -F # -S # -S # -G # -W # -G # -N # (Z J )(SEQ ID NO: 10) V # -N # -F # -S # -P # -N # -W # -G # (Z K )(SEQ ID NO: 11) V # -N # -F # -S # -P # -G # -W # -G # -T # (Z L )(SEQ ID NO: 12) V # -N # -F # -S # -P # -N # -W # (Z M )(SEQ ID NO: 13) L # -N # -F # -S # -P # -G # -W # -G # (Z N )(SEQ ID NO: 14) L # -N # -F # -S​​​​​​​​​​​​# "" indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs. (37) Z is a peptide having a formula selected from the following: L # -TF # -SP # -D # -W(Z A1 (SEQ ID NO: 15) L # -TF # -TS # -S # -WGG(Z B1 (SEQ ID NO: 16) L # -TF # -TP # -N # -W(Z C1 (SEQ ID NO: 17) I # -TF # -SR # -D # -WTG(Z D1 (SEQ ID NO: 18) T # -FS # -RD # -WTG(Z E1 (SEQ ID NO: 19) V # -NF # -TP # -T # -WGQ(Z F1 (SEQ ID NO: 20) L # -NF # -SP # -G # -W(Z G1 (SEQ ID NO: 21) L # -TF # -TS # -S # -WG(Z H1 (SEQ ID NO: 22) L # -TF #-SS # -G # -W(Z I1 (SEQ ID NO: 23) L # -TF # -SS # -G # -WGN(Z J1 (SEQ ID NO: 24) V # -NF # -SP # -N # -WG(Z K1 (SEQ ID NO: 25) V # -NF # -SP # -G # -WGT(Z L1 (SEQ ID NO: 26) L # -NF # -ST # -G # -W(Z O1 (SEQ ID NO: 88) in" # "" indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs. (38) Z is a peptide having a formula selected from the following: L # -T # -F # -S # -P # -D # -W # (Z A (SEQ ID NO: 1) L # -T # -F # -T # -S # -S # -W # -G # -G # (Z B (SEQ ID NO: 2) I # -T # -F # -S# -R # -D # -W # -T # -G # (Z D (SEQ ID NO: 4) in" # "" indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs. (39) Z is a peptide having a formula selected from the following: L # -TF # -SP # -D # -W(Z A1 (SEQ ID NO: 15) L # -TF # -TS # -S # -WGG(Z B1 (SEQ ID NO: 16) I # -TF # -SR # -D # -WTG(Z D1 (SEQ ID NO: 18) in" # "" indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs. (40) Z is a peptide having a formula selected from the following: LTFSPDW (SEQ ID NO: 27); [n-me-L]TFSPDW (SEQ ID NO: 28); LT[n-me-F]SPDW (SEQ ID NO: 29); LTFTSSWGG (SEQ ID NO: 30); LTFTSSWG (SEQ ID NO: 31); LTFTPNW (SEQ ID NO: 32); ITFSRDWTG (SEQ ID NO: 33); LNFSTGW (SEQ ID NO: 34); LT[f]S-[Thz]-dW (SEQ ID NO: 35); TFSRDWTG (SEQ ID NO: 36); VNFTPTWGQ (SEQ ID NO: 37); LNFSPGW (SEQ ID NO: 38); LT-[Thi]-SP-[N-Me-D]-W (SEQ ID NO: 39); LTFT-[n-me-S]-[n-me-S]-WGG (SEQ ID NO: 40); LTFSSGWGN (SEQ ID NO: 41); LTFSSGW (SEQ ID NO: 42); VNFSPNW (SEQ ID NO: 43); VNFSPGWGT (SEQ ID NO: 44); LNFSPGWG (SEQ ID NO: 45); LN[Thi][n-me-S]PGW (SEQ ID NO: 46); LTFT[N-Me-Ser]S[Nal]GG. (SEQ ID NO: 47); or LTFT[N-Me-Ser][s][Nal]GG (SEQ ID NO: 104). (41) Z is a peptide having a formula selected from the following: LTFSPDW (SEQ ID NO: 27); LTFTSSWGG (SEQ ID NO: 30); LTFTSSWG (SEQ ID NO: 31); LTFTPNW (SEQ ID NO: 32); ITFSRDWTG (SEQ ID NO: 33); LTFT-[n-me-S]-[n-me-S]-WGG (SEQ ID NO: 40). (42) At least one of the modified amino acid or non-natural amino acid analog residues in peptides Y and Z is selected from: iN-methylated amino acids; ii. Non-protein amino acids, such as hydroxyproline (Hyp: L-hydroxyproline or (2S,4R)-4-hydroxyproline), octahydroindole-2-carboxylic acid (Oic), sarcosine (Sar), oroleucine (Nle), α-aminoisobutyric acid (Aib), thienylalanine (Thi) or thiazolidin-4-carboxylic acid (Thz), phenylglycine (Phg), γ-aminobutyric acid (gaba) or naphthylalanine (Nal); iii. D-amino acids iv. β-amino acids v. Peptide-like amino acid analogs; vi. Amino acids modified by sugars; or vii. Biotin-modified amino acids; Alternatively, the side chains of two amino acid residues can be linked together to form a cyclic structure (e.g., forming an intramolecular amide via a condensation reaction between the side chains of arginine or lysine and the side chains of aspartic acid or glutamic acid). (43) At least one of the modified amino acid or non-natural amino acid analog residues in peptides Y and Z is selected from: iN-methylated amino acids; ii. Peptide-like amino acid analogs; iii. Non-protein amino acids selected from hydroxyproline (Hyp: L-hydroxyproline or (2S,4R)-4-hydroxyproline), octahydroindole-2-carboxylic acid (Oic), sarcosine (Sar), oroleucine (Nle), α-aminoisobutyric acid (Aib), thiophene alanine (Thi), thiazolidin-4-carboxylic acid (Thz), or naphthyl alanine (Nal); iv. D-amino acids; Alternatively, the side chain of arginine or lysine can be linked to the side chain of one of aspartic acid or glutamic acid to form a cyclic amide; preferably, the arginine or lysine residue is adjacent to or separated from the aspartic acid or glutamic acid residue by one or two amino acid residues, for example, [cyclic-KXE], where "X" is any amino acid residue: ; R represents the amino acid side chain. (44) At least one of the modified amino acid or non-natural amino acid analog residues in peptides Y and Z is selected from: iN-methylated amino acids; ii. Aminoisobutyric acid (Aib). iii. Thiophene-alanine (Thi) iv. Thiazolidine-4-carboxylic acid (Thz); v. naphthylalanine (Nal); or vi. D-amino acids; The side chain of an arginine or lysine residue is connected to the side chain of an aspartic acid or glutamic acid residue to form an intramolecular cyclic amide; wherein the arginine or lysine residue is adjacent to or separated from the aspartic acid or glutamic acid residue by one amino acid residue, for example, [cyclic-KLE]. . (45) At least one of the modified amino acid or non-natural amino acid analog residues in peptides Y and Z is selected from: iN-methylated amino acids; ii. Thiophene-alanine (Thi) iii. Thiazolidine-4-carboxylic acid (Thz); iv. Naphthylalanine (Nal); or vD-amino acids. (46) At least one of the residues in peptides Y and Z is an N-methylated amino acid. (47)R 2 It is NH2, NR 2a H, NR 2a R 2b Or OH, where R 2a and R 2b If they exist, they are each independently C. 1-6 -alkyl (e.g., methyl, ethyl, propyl, butyl, pentyl or hexyl). (48) R2 is NH2 or OH. (49)Y 1 Peptides that either do not exist or contain one or two amino acid residues. (50)Y 1 It does not exist. (51)Y 2 Peptides that either do not exist or contain one or two amino acid residues. (52)Y 2 It does not exist.

[0088] Appropriately, R 1 It is as defined in any of the paragraphs (1) to (6) above. More appropriately, R 1 It is as defined in any of the paragraphs (3) to (6) above. Most appropriately, R 1 It is as defined in paragraphs (5) or (6) above.

[0089] Appropriately, L 1 It is as defined in any of the paragraphs (7) to (10) above. Most appropriately, L 1It is as defined in paragraphs (9) or (10) above.

[0090] Appropriately, R 1 and L 1 It is as defined in any of the paragraphs (11) to (16) above. More appropriately, R 1 and L 1 It is as defined in any of the paragraphs (14) to (16) above. Most appropriately, R 1 and L 1 It is as defined in paragraph (16) above.

[0091] Appropriately, Y is as defined in any of the paragraphs (17) to (21) above. More appropriately, Y is as defined in any of the paragraphs (18), (20) or (21) above. Most appropriately, Y is as defined in any of the paragraphs (20) or (21) above.

[0092] Appropriately, Z 1 It is as defined in paragraphs (22) or (23) above. Most appropriately, Z 1 It is as defined in paragraph (23) above.

[0093] Appropriately, Z 2 It is as defined in paragraphs (24) or (25) above. More appropriately, Z 2 It is as defined in paragraph (25) above.

[0094] Appropriately, Z 4 It is as defined in any of the paragraphs (26) to (28) above. More appropriately, Z 4 It is as defined in paragraphs (27) or (28) above.

[0095] Appropriately, Z 5 It is as defined in paragraphs (29) or (30) above. More appropriately, Z 4 It is as defined in paragraph (30) above.

[0096] Appropriately, Z 6 It is as defined in paragraphs (31) or (32) above. More appropriately, Z 6 It is as defined in paragraph (32) above.

[0097] Appropriately, Z 8 and Z 9 It is as defined in any of the paragraphs (33) to (35) above. More appropriately, Z 8 and Z9 It is as defined in paragraphs (34) or (35) above. Most appropriately, Z 8 and Z 9 It is as defined in paragraph (35) above.

[0098] Suitablely, Z is as defined in any of paragraphs (36) through (41). More suitablely, Z is a peptide as defined in any of paragraphs (37) through (41). Most suitablely, Z is a peptide as defined in paragraph (40) or (41).

[0099] In some embodiments, peptide Z and / or Y comprises at least one modified amino acid or a non-natural amino acid analogue. Suitably, at least one modified amino acid or non-natural amino acid analogue in peptide Z and / or Y is as defined in any of paragraphs (42) to (46) above. More suitably, at least one modified amino acid or non-natural amino acid analogue in peptide Z and / or Y is as defined in any of paragraphs (44) to (46) above. Most suitably, at least one modified amino acid or non-natural amino acid analogue in peptide Z and / or Y is as defined in paragraph (45) or (46) above.

[0100] In some embodiments, peptides Z and / or Y do not contain any modified amino acids or non-natural amino acid analogs.

[0101] Appropriately, R 2 It is as defined in paragraphs (47) or (48) above. Most appropriately, R 2 It is as defined in paragraph (48) above.

[0102] Appropriately, Y 1 It is as defined in either paragraph (49) or (50) above. Most appropriately, Y 1 It is as defined in paragraph (50) above.

[0103] Appropriately, Y 2 It is as defined in either paragraph (51) or (52) above. Most appropriately, Y 2 It is as defined in paragraph (52) above.

[0104] In the embodiments, Z is a peptide according to the formula (Z-ia) or (Z-ib): Z 1 -T # -F # -Z 4 -Z 5 -Z 6 -W# -Z 8 -Z 9 (Z-ia) Z 1 -N # -F # -Z 4 -Z 5 -Z 6 -W # -Z 8 -Z 9 (Z-ib) Z 1 Z 4 Z 5 Z 6 Z 8 and Z 9 As defined in this article; and where “ # "" indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs.

[0105] In the embodiments, the peptide portion YZ contains at least five unmodified amino acid residues.

[0106] Suitablely, at least two of the residues in the peptide moiety YZ are unmodified amino acids. More preferably, at least three of the residues in the peptide moiety YZ are unmodified amino acids.

[0107] In some embodiments, peptide YZ comprises 1, 2, 3, or 4 modified amino acids or non-natural amino acid analogs. In some embodiments, peptide YZ comprises 1, 2, or 3 modified amino acids or non-natural amino acid analogs. In some embodiments, peptide YZ comprises 1 or 2 modified amino acids or non-natural amino acid analogs. In some embodiments, peptide YZ comprises a single modified amino acid or non-natural amino acid analog.

[0108] In some embodiments, 1 to 6 residues in the peptide moiety YZ comprise modified amino acids or non-natural amino acid analogs. In some embodiments, 1 to 5 residues in the peptide moiety YZ comprise modified amino acids or non-natural amino acid analogs. In some embodiments, 1 to 4 residues in the peptide moiety YZ comprise modified amino acids or non-natural amino acid analogs. In some embodiments, 1 to 3 residues in the peptide moiety YZ comprise modified amino acids or non-natural amino acid analogs. In some embodiments, 1 to 2 residues in the peptide moiety YZ comprise modified amino acids or non-natural amino acid analogs.

[0109] In some embodiments, peptide YZ comprises no more than 5 modified amino acids or non-natural amino acid analogs. In some embodiments, peptide YZ comprises no more than 4 modified amino acids or non-natural amino acid analogs. In some embodiments, peptide YZ comprises no more than 3 modified amino acids or non-natural amino acid analogs.

[0110] In other embodiments, peptide YZ does not contain any modified amino acids or non-natural amino acid analogs, i.e., each residue is a listed protein amino acid residue.

[0111] In a preferred embodiment, Y 1 and Y 2 It does not exist.

[0112] In the embodiments, Z is a peptide having a formula selected from the following: LTFSPDW (SEQ ID NO: 27); [n-me-L]TFSPDW (SEQ ID NO: 28); LT[n-me-F]SPDW (SEQ ID NO: 29); LTFTSSWGG (SEQ ID NO: 30); LTFTPNW (SEQ ID NO: 32); ITFSRDWTG (SEQ ID NO: 33); LNFSTGW (SEQ ID NO: 34); LT[f]S-[Thz]-dW (SEQ ID NO: 35); TFSRDWTG (SEQ ID NO: 36); VNFTPTWGQ (SEQ ID NO: 37); LNFSPGW (SEQ ID NO: 38); LT-[Thi]-SP-[N-Me-D]-W (SEQ ID NO: 39); LTFT-[n-me-S]-[n-me-S]-WGG (SEQ ID NO: 40); LTFTSSWG (SEQ ID NO: 31); LTFSSGWGN (SEQ ID NO: 41); LTFSSGW (SEQ ID NO: 42); VNFSPNW (SEQ ID NO: 43); VNFSPGWGT (SEQ ID NO: 44); LNFSPGWG (SEQ ID NO: 45); LN[Thi][n-me-S]PGW (SEQ ID NO: 46); or LTFT[N-Me-Ser]S[Nal]GG (SEQ ID NO: 47) LTFT[N-Me-Ser][s][Nal]GG (SEQ ID NO: 104).

[0113] In some embodiments, Y, if present, does not contain any modified amino acids or non-natural amino acid analogs. In other embodiments, Y is absent or is a glutamine residue Q.

[0114] In some embodiments, Y is glutamine residue Q, or if Y is absent, then R 1 -L 1 - Formation of the pyroglutamic acid moiety: .

[0115] In a preferred embodiment, part of R 1 -L 1 -Y is selected from: • Pyroglutamic acid group-; • Palmitoyl-Q-; •[PEG8]-Q-; • Pyroglutamate group -Q-; •Hy-E; or •Hy-Q-.

[0116] In one embodiment, the compound of the present invention may be any of the AKH or peptide analogs listed herein. Specific examples of AKH peptides and analogs include compounds in the following table or their salts or solvates:

[0117] Specific examples of AKH peptides and analogues according to the present invention include compounds listed in the table below, or their salts or solvates: Further explanation of the compounds of the present invention

[0118] In some embodiments, the compounds of the present invention may be in the form of salts or solvates (e.g., hydrates).

[0119] The compounds of the present invention can be provided in combination with one or more other active insecticides, such as those described herein. R1 L 1 and R 2

[0120] The terminal groups at the N-terminus and C-terminus of the peptide backbone are designated as R, respectively. 1 and R 2 Therefore, R 1 Bonded to the nitrogen atom of the N-terminal amino group of Y (optionally via L) 1 and / or Y 1 ), and R 2 With Z or Y 2 The C-terminal carbonyl carbon atom is bonded.

[0121] In addition to containing at least one modified or non-natural amino acid residue, the compounds of the present invention may include further functionalization, suitably at the N or C terminus. Suitably, the compounds may be functionalized to increase stratum corneum permeability or increase stability. Suitably, the compounds may be functionalized with aromatic, aliphatic, or lipophilic groups. Thus, suitably, R 1 It can be an aromatic group, a heteroaromatic group, an aliphatic group, or a lipophilic group.

[0122] In some embodiments, the compound may be functionalized with a lipophilic group, such as a fatty acyl group. Fatty acyl groups include, but not limited to, palmitoyl, butyryl, waxyl, decanoyl, dodecanoyl, tunganoyl, heptayl, hexanoyl, eicosanoyl, eicosanoyl, limoyl, myristoyl, nonanoyl, octadecanoyl, octanoyl, palmitoleyl, stearoyl, undecanoyl, and pentanoyl. Therefore, suitably, R 1 The group can be palmitoyl ([Palm]), that is: .

[0123] In one embodiment, the compound may be functionalized with an aromatic group (e.g., a benzyl or benzoyl group), which may be a benzoic acid derivative or a benzophenone derivative. Therefore, suitably, R 1 The group can be an aromatic group (e.g., 4-benzoylbenzoic acid) or a derivative (e.g., 4-benzoylbenzoyl).

[0124] In one embodiment, the compound can be functionalized with an acyl group. The "acyl" group is of formula R. 3a -C(O)- group, where R 3a It is C 1-6 Alkyl groups, such as formyl, acetyl (Ac), propionyl, butyryl, or wherein R 3a It is benzoyl. Suitablely, R 3a The group can be R1b -C(O)-, for example, acetyl (Ac), i.e.: .

[0125] In some embodiments, R 1 The group can be a biotin moiety. Therefore, the biotin moiety can be incorporated into an amino acid residue (e.g., in a modified lysine side chain) or at the end.

[0126] In some embodiments, R 1 The group can be replaced by the sugar portion.

[0127] In some embodiments, one or more amino acid residues in peptides Y and Z may be naturally modified with a sugar moiety, i.e., the amino acid residues may be “saccharide analogues”. For example, the sugar may be part of a Ser or Thr side chain modification (glycosylation) or a Lys or Arg side chain modification (glycosylation).

[0128] The sugar moiety discussed in this article can be either a monosaccharide or a disaccharide. Examples of monosaccharides include glucose, 6-deoxyglucose, mannose, galactose, glucosamine, galactosamine, N-acetylglucosamine, N-acetylglucosamine, glucuronic acid, allose, arbutin, gulose, idole, fucose, tarose, ribose, deoxyribose, arabinose, xylose, lysolose, ribulose, xylulose, fructose, allulose, sorbose, or tagatose. Examples of disaccharides include sucrose, lactose, lactulose, isolaxose, maltose, isomaltulose, isomaltulose, trehalose, cellobiose, kosperidose, aspergillus niger, sophorose, laminarin, gentiobiose, thiomaltose, manniobiose, or their N-, C-, or S-glycosidic derivatives. Most preferably, the sugar moiety is selected from glucosamine or galactosamine.

[0129] Sugars can be N-terminal modified or as part of a Ser side chain modification. As part of the N-terminus, a spacer is typically added (e.g., succinic acid, Suc). R with such modifications... 1 -L 1 An example of the -Y sequence is: [sugar]-[Suc]-[sequence Y as defined herein]. The symbol "sugar" can be any of the sugars described herein, such as glucosamine or galactosamine.

[0130] Suitablely, the compound can be modified with a (poly)alkylene glycol polymer. This modification can be present in R... 1 L 1 Or in part Y. Appropriately, R 1The group can be a (poly)alkylene glycol. The presence of a polymer increases the ease of compound formulation. Preferred (poly)alkylene glycols include polyethylene glycol (PEG). Therefore, the compound can be PEGylated, suitably by the interaction of PEG with amino acid residues in Y at R. 1 Location or via connector L 1 Covalent attachment. The PEG group can have any suitable terminal group, such as NH2, OH, or OMe. The connector L1 can be... –(C=O)-C 1-4 alkylene groups, wherein This indicates the attachment point to Y.

[0131] The polyethylene glycol group present as the linker portion L1 or as part of a modified peptide chain can have the formula [–(C=O)-C 1-4 Alkylene-(OCH2CH2) n -], where n can preferably be an integer from 1 to 16, for example 8.

[0132] The particularly preferred terminal R1 PEG group is an NH2-terminated PEG8 group, which is obtained through... –(C=O)-ethylene linker group L1 is attached to the peptide, for example: . In the compounds described in this invention and examples, the above groups have the symbol [PEG8].

[0133] In some embodiments, one or more amino acid residues in peptides Y and Z may be naturally modified with phosphate or sulfate groups. For example, phosphate or sulfate groups may be part of a side-chain modification, i.e., the amino acid may be phosphorylated or sulfated.

[0134] R 1 Selected from hydrogen (which may not be specified in a particular peptide sequence, or can be designated as "H-" or "Hy-"), C 1-4 Alkyl groups (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 ;where R 1a R 1b R 1c R 1d and R1e Each is independently selected from hydrogen or C. 1-4 Alkyl groups (e.g., methyl, ethyl, propyl, butyl), preferably hydrogen or methyl.

[0135] In some embodiments, if R 1 It is -C(=N) + (R 1b (R) 1c ))NR 1d R 1e ;R 1a R 1b R 1c R 1d and R 1e Each is a methyl group, i.e., R 1 It is -C(=N) + Me2)NMe2.

[0136] When R 1 =“H” (or “Hy”;), which usually represents a free primary amino group at the N-terminus. The other hydrogen atom in the N-terminal amino group is usually unchanged, regardless of R. 1 How does it behave? An exception is when 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-terminal N-methylated leucine residue can be represented as R. 1 -[n-me-L]-, where R 1 Let it be H. However, it can also be simply represented as R. 1 -L-, where R 1 It is a methyl group, but no other hydrogen atom is shown.

[0137] In some embodiments, L 1 It can include Y 1 The carbonyl group adjacent to the N-terminus of the Y or Z group has a C=O structure. For example, L... 1 It can be –(C=O)C 1-12 -alkylene-NH-, –(C=O)-C 1-10 Alkylene-(C=O)- –(C=O)-C 1-10 Alkylene (e.g., -(C=O)-, i.e., C1 alkylene optionally substituted with oxy); wherein any L 1 The group is optionally substituted with one or more oxo (=O) groups; wherein Indicates Y 1 Y or Z attachment points

[0138] In some embodiments, when R 1 When it is hydrogen, L1 Does not exist or -(C=O)C 1-16 -alkylene-NH-, where Indicates Y 1 Attachment points of Y or Z, such as R 1 It is hydrogen and L 1 yes -(C=O)C 1-6 -alkylene-NH-, such as: .

[0139] In some embodiments, L 1 If it exists, then... –(C=O)C 1-10 -alkylene-NH-, where Indicates the attachment point to Y. For example, L 1 It can be -(C=O)C 1-6 -alkylene-NH-, such as: It can be considered a residue of 6-aminohexanoic acid (Ahx).

[0140] In some embodiments, when R 1 When it is hydrogen, L 1 Does not exist or -(C=O)C 1-16 -alkylene-NH-, where Indicates Y 1 Attachment points of Y or Z, such as R 1 It is hydrogen and L 1 yes –(C=O)C 11 alkylene-NH2, wherein Indicates Y 1 The attachment point of Y or Z, i.e. .

[0141] In some embodiments, L 1 If it exists, then... –(C=O)C 1-12 -alkylene-NH-, where Indicates Y 1 Attachment points for Y or Z. For example, L 1 It can be -(C=O)C 6-12 -alkylene-NH- (e.g., alkylene-NH-) –(C=O)C 11 alkylene-NH2), in which Indicates Y 1 The attachment point of Y or Z, i.e. It can be considered a residue of 12-aminododecanoic acid (Ado).

[0142] In some embodiments, L 1 It can be a C1 alkylene group that has been substituted with an oxonium, therefore L 1 It can be a C=O connector.

[0143] When L 1 When it exists, R 1 It can be hydrogen (H). For example, R 1 It is hydrogen and L 1 yes -(C=O)C 1-6 -alkylene-NH-, for example: .

[0144] In some embodiments, when R 1 It is -C(=N) + (R 1b (R) 1c ))NR 1d R 1e At that time, L 1 It does not exist, for example, R 1 It is -C(=N) + Me2)NMe2 and L 1 It does not exist. In such embodiments, R 1 The group, together with the N-terminal nitrogen, forms the following guanidine-based structure (represented as "NR" in the following structures):

[0145] Typically, when L 1 It is -(C=O)C 1-10 When -alkylene-NH-, R 1 It's H.

[0146] Typically, when R 1 It is -C(=N) + (R 1b (R) 1c ))NR 1d R 1e At that time, L 1 It does not exist. When R... 1 It is -C(=N) + (R 1b (R) 1c ))NR 1d R 1e "and L1 When it does not exist, R 1 The group, together with the N-terminal nitrogen of the peptide sequence Z, forms a guanidine-based group (discussed above). Preferably, "-C(=N)" + (R 1b (R) 1c ))NR 1d R 1e "is -C(=N" + Me2)NMe2.

[0147] In some embodiments, R 1 It can be a heterocyclic group linked to the peptide via a C=O linker. A specific example is a pyroglutamate salt group [pyr]. Such terminal residues can be formed by converting an N-terminal glutamine (Gln or Q) or N-terminal glutamate (Glu or E) residue to form a pyroglutamate terminal group [pyr]. This conversion can occur in biological systems through reactions with certain enzymes at the N-terminal glutamine (Q) or glutamate (E) residues. It can also be achieved synthetically. Because this conversion can occur under certain biological conditions, it is considered to be a modification of the naturally occurring N-terminal glutamine (Gln or Q) or N-terminal glutamate (Glu or E) residues.

[0148] Therefore, in some embodiments, L 1 and R 1 Together they can form a pyroglutamic acid terminal group, in which L 1 It is C=O and R 1 It is a pyrrolidone-2-one ring. Therefore, in the peptides described herein, the symbol [pyr] refers to the following structure: .

[0149] In some embodiments, R 2 It is NH 2、 NR 2a H 、 NR 2a R 2b OR 2a ;where R 2a and R 2b Each as defined herein. In some embodiments, R 2a and R 2b Each is independently selected from C 1-2 Alkyl group. Preferably R. 2 It is NH2.

[0150] In some embodiments, R2 is OH or OR 2a , where R 2a and R2b Each as defined in this article.

[0151] "Guidino" refers to the group containing R. 1 It is -C(=N) + Me2)NMe2 and the terminal structure formed by "guanidinyl-L-" is as follows: . Modified amino acids or non-natural amino acid analogues

[0152] In some embodiments, at least one of the residues in peptides Y and Z is a modified or non-natural amino acid analog. A modified or non-natural amino acid analog can be any analog known to those skilled in the art. Examples of modified or non-natural amino acid analogs include: iN-methylated amino acids; ii. Peptide analogues; iii. Sugar-modified analogues; iv. Biotin-modified analogues v.β amino acids, vi. D-configuration amino acids, vii. Non-protein amino acids, such as hydroxyproline (Hyp: L-hydroxyproline or (2S,4R)-4-hydroxyproline), octahydroindole-2-carboxylic acid (Oic), sarcosine (Sar), ortholeucine (Nle), α-aminoisobutyric acid (Aib), thiophene alanine (Thi), thiazolidin-4-carboxylic acid (Thz), phenylglycine (Phg), γ-aminobutyric acid (gaba), or naphthyl alanine (Nal), etc. viiiα-alkylated amino acids; Alternatively, the side chains of two amino acid residues can be linked together to form a cyclic structure (e.g., forming an intramolecular amide via a condensation reaction between the side chains of arginine or lysine and the side chains of aspartic acid or glutamic acid).

[0153] The compounds of the present invention may contain one or more modified amino acids or non-natural amino acid analogs in Y-peptide, Z-peptide, or both Y-peptide and Z-peptide.

[0154] In some embodiments, at least one of the residues in the Y portion is a modified or non-natural amino acid analog.

[0155] The compounds of the present invention may contain a variety of modified amino acids or non-natural amino acid analogs in the peptide sequence YZ.

[0156] In other embodiments, peptide YZ contains only unmodified amino acids, i.e., each residue is a listed protein amino acid residue. active

[0157] Suitablely, the compounds of the present invention have anti-insect activity. Suitablely, the activity is against insects of the orders Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera.

[0158] Suitablely, the compounds have activity against hemiptera, dipterans, and / or lepidopterans. Therefore, the compounds of the present invention can be found to have specific uses against hemiptera, dipterans, and / or lepidopterans (such as those described herein).

[0159] Compounds typically increase insect mortality, for example, when they come into local contact with suitable insects or are ingested by suitable insects. Therefore, the described compounds (and compositions containing them) can be considered insecticides and can be referred to as “insect control agents”.

[0160] Without wishing to be bound by theory, any or all of the effects described can be mediated by agonist activity at the AKH receptor in the target insect. Suitably, the compounds of the present invention have agonist activity when binding to the AKH receptor in the target insect.

[0161] It is believed that, especially compared to wild-type AKH, the peptide analogs described in this specification retain agonist activity while potentially exhibiting superior stability, particularly against proteases. Therefore, they are believed to have superior suitability as insecticides. Insect control agents

[0162] The term "insect control agent" refers to an agent used to increase insect mortality (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 an insect control agent. Therefore, the present invention appropriately provides the use of the compounds or compositions of the present invention as insect control agents, for example, against Diptera, Hemiptera, Coleoptera, Blattodea, and / or Lepidoptera. Thus, insect control agents can be applied to increase the mortality rate of a given insect or insect population.

[0163] The increase in mortality rate used herein refers to the increase in the percentage of dead insects compared to the percentage of dead insects in the same insect population that has not been exposed to other aspects of the insect control agent of the present invention.

[0164] Suitablely, insect mortality can be calculated as the number of dead insects per treatment area divided by the total number of insects. Suitablely, the treatment area can be a hole in a plate, or a single leaf or multiple leaves, or the entire plant. Suitablely, insect mortality can be measured by performing a leaf immersion assay as described in the examples herein.

[0165] Insect control agents can be used to reduce the size of insect populations, or to inhibit the growth of insect populations or to suppress the feeding of insect populations (e.g., compared to other insect populations that are not exposed to the same agent).

[0166] The insect control composition is a composition comprising an insect control agent (i.e., the compound of the present invention as described). Plant protectant

[0167] The term "plant protectant" refers to an agent used to protect plants or plant parts from insects (e.g., to prevent infection or colonization) or from being used as a food source by such insects (e.g., by excreting sap). Any compound or composition thereof of the present invention can be considered a plant protectant and can be used as a plant protectant. Accordingly, the present invention provides the use of the compounds or compositions of the present invention as plant protectants, for example, to protect plants from Diptera, Hemiptera, Coleoptera, Blattodea, and / or Lepidoptera insects.

[0168] Infection or colonization can occur by larvae (or nymphs), adults, or by insects acting as hosts or reservoirs for eggs. However, the terms "infection" and "colonization" should not be interpreted as requiring the presence of insects to be harmful to the plant.

[0169] Among other purposes, plant protectants can be applied to reduce the insect load on plants or plant parts, inhibit or reduce insect infestation of plants, suppress the increase of the insect load on plants or plant parts (e.g., reduce its rate), or maintain plants in an insect-free state (compared to species with other aspects of an insect population not exposed to the agent). Therefore, plant protectants can be applied to plants or plant parts already infested with Hemiptera, Diptera, Coleoptera, Blattodea, and / or Lepidoptera, or to plants or plant parts that are free of or substantially free of Hemiptera, Diptera, and / or Lepidoptera.

[0170] The plant protection composition is a composition comprising a plant protection agent (i.e., the compound of the present invention described herein). plant

[0171] The term “plant or part of a plant” or “plant or part thereof” as used in this article refers to any part of a plant, including but not limited to: leaves, stems, roots, flowers, buds, bulbs, and seeds.

[0172] Suitable plants or parts thereof that can be protected by the compounds or compositions thereof of the present invention or the pharmaceutical agents of the present invention include crops and plants of agricultural, horticultural, or economic significance. Suitable plants may include any of the following plants or parts thereof: Abaca (Musa textilis), alfalfa (Medicago sativa), almond (Prunus dulcis), fennel (Pimpinella anisum), wild apple (Malus sylvestris), apricot (Prunus armeniaca), areca (Areca catechu), root celery (Arracacia xanthorhiza), arrowroot (Maranta arundinacea), artichoke (Cynara scolymus), Jerusalem artichoke (Helianthus tuberosus), asparagus (Asparagus officinalis), avocado (Persea americona), American foxtail grass (Pennisetum americanum), underground pea (Vigna subterranean), plantain (Musa paradisiaca), barley (Hordeum vulgare), common bean (Phaseolus vulgaris), mung bean (Phaseolus vigna spp.), beet (Beta vulgaris), bergamot (Citrus bergamia), species of the genus Rubus (Rubus) spp.), pepper (Piper nigrum), black thorn (Acaciamearnsii), blueberry 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), kohlrabi (Brassica oleracea capitate), turnip (Brassica rapa), and Brassica species (Brassica spp.).Cocoa (Theobroma cacao), melon (Cucumis melo), caraway (Carumcarvi), cardamom (Elettaria cardamomum), artichoke (Cynara cardunculus), carob (Ceratonia siliqua), carrot (Daucus carota), cashew (Anacardium occidentale), cassava (Manihotesculenta), castor bean (Ricinus communis), cauliflower (Brassica oleracea botrytis), celery (Apium graveolens), chayote (Sechium edule), plum species (Prunus spp.), European chestnut (Castanea sativa), chickpea (Cicer arietinum), chicory (Cichorium intybus), chicory (Cichorium intybus), capsicum species (Capsicum spp.), cinnamon (Cinnamomum verum), lemongrass (Cymbopogon nardus), citron (Citrus) *Citrus veticulata*, *Trifolium* spp., *Syzygium aromaticum*, *Cocos nucifera*, *Colocasia* spp.; *Xanthosoma* spp., *Coffee* spp., *Cola* spp., *Brassica napus*, *Zea mays*, *Valerianellalocusta*, *Gossypium* spp., *Vigna unguiculate*, *Vaccinium* spp., *Lepidium sativum*, *Cucumis sativus*, *Ribes* spp., *Annona reticulata*, *Colocasia esculenta*, *Phoenix* dactylifera), Moringa (Moringa oleifera), and species of the genus Phaseolus (Phaseolus spp.).Garlic (Allium sativum), onion (Allium cepa), pea (Pisum sativum), durum wheat (Triticum durum), species of the genus *Xanthosoma*; species of the genus *Colocasia*, eggplant (Solanum melongena), chicory (Cichorium endivia), needlegrass (Lygeum spartum), fennel (Foeniculum vulgare), fenugreek (Trigonella foenumgraecum), fig (Ficus carica), European hazel (Corylus avellane), giant hemp (Furcraea macrophylla), flax (Linum usitatissimum), New Zealand hemp (Phormium tenax), species of the genus *Pelargonium*; species of the genus *Geranium*, ginger (Zingiber officinalis), species of the genus *Langenaria*; species of the genus *Cucurbita*. spp.), chickpeas (Cicer arietinum), grapefruit (Citrus paradise), grapes (Vitisvinifera), needlegrass (Lygeum spartum), orchardgrass (Dactylis glomerata), peanuts (Arachis hypogaea), guava (Psidium guajava), hazelnuts (Corylus avellane), hemp (Cannabissativa), Indian hemp (Crotalaria juncea), agave (Agave fourcroydes), ragweed (Lawsonia inermis), hops (Humulus lupulus), horseradish (Armoracia Rusticana), indigo (Indigoferatinctorial), jasmine species (Jasminum spp.), jute species (Corchorus spp.), kale (Brassica oleracea acephala), kapok (Ceiba pentandra), kenaf (Hibiscus cannabinus), kohlrabi (Brassica oleracea) gongylodes), species of the genus Lavandula (Lavandula spp.).Leek (Allium ampeloprasum), lemon (Citrus limon), lemongrass (Cymbopogon citratus), lentil (Lens culinaris), Lespedeza species (Lespendeza spp.), lettuce (Lactuca sativa), licorice (Glycyrrhiza glabra), lime (Citrus aurantifolia), mandarin orange (Citrus limetta), flax (Linum usitatissimum), lychee (Litchi chinensis), loquat (Eriobotrya japonica), lupinus species (Lupinus spp.), macadamia species (Macadamia spp.), nutmeg (Myristicafragrans), agave (Agave atrovirens), citrus (Citrus reticulata), mango (Mangiferaindica), cassava (Manihot esculenta), rye (Secale cereal), hawthorn (Mespilus) Germanica, melon (Cucumis melo), millet (Penicum miliaceum), sorghum (Eleusine coracana), foxtail millet (Setaria italica), barnyard grass (Echinochloa crusgalli), sorghum (Eleusine coracana); species of mint (Mentha spp.), mulberry (Morus spp.), white mulberry (Morus alba), umbrella grass (Agaricus spp.); species of Pleurotus (Pleurotus spp.), straw mushroom (Volvariella), black mustard (Brassica nigra); white mustard (Sinapis alba), peach (Prunus persica), New Zealand hemp (Phormium tenax), daisy (Guizotia abyssinica), nutmeg (Myristica fragrans), oat species (Avena spp.).Oil palm (Elaeisguineensis), okra (Abelmoschus esculentus), olive (Olea europaea), poppy (Papaversomniferum), sweet orange (Citrus sinensis), sour orange (Citrus aurantium), orchardgrass (Dactylis glomerate), sago palm species (Metroxylon spp.), fan-leaf sugar palm (Borassus flabellifer), papaya (Carica papaya), parsnip (Pastinaca sativa), pear (Pyrus communis), pea (Pisumsativum), pecan (Carya illinoensis), chili pepper (Capsicum annuum), persimmon (Diospyros kaki); American persimmon (Diospyros virginiana), pigeon pea (Cajanus cajan), pineapple (Ananas comosus), pistachio species (Pistacia spp.), European plum (Prunus domestica), pomegranate (Punica) granatum, pomelo (Citrus grandis), potato (Solamum tuberosum), sweet potato (Ipomoea batatas), Cucurbita spp., pyrethrum (Chrysanthemum cineraraiefolium), Aspidosperma spp., quince (Cydonia oblonga), Cinchona spp., quinoa (Chenopodium quinoa), radish (Raphanus sativus), ramie (Boehmeria nivea), Agrostis spp., ramie (Boehmeria nivea), Rheum spp., rice (Oryza sativa); glumed rice (Oryza glaberrima), rose spp., Brazilian rubber tree (Heveabrasiliensis), rye (Secale) cereal, species of ryegrass (Lolium spp.), red flower (Carthamustinctorius), species of sago palm (Metroxylon spp.).Onobrychis viciifolia, Valerianella locusta, Tragopogon porrifolius, Achrassapota, Citrus reticulata, Brussels sprouts (Brassica ileracea capitate), Scorzonera hispanica, Sesamum indicum, Butyrospermum paradoxum, Agave sislana, Citrus aurantifolia, Glycinemax, Triticum spelta, Spinacia oleracea, Secalecereal, Cucurbita spp., Fragaria spp., Sorghumbicolor Sudanense, Saccharum officinarum, Helianthus annuus, Crotalaria juncea, Citrus limetta, Ipomoea batatas, Citrus reticulata, Xanthosoma sagittifolium, Manihot esculenta, Colocasia esculenta, Camellia sinensis, Eragrostisabyssinica, Phleum pratense, Nicotiana tabacum, Lycopersicumesculentum, Lotus spp., Aleurites spp., Brassicarapa, Urena lobate, Vanilla planifolia, Vicia sativa, Juglans spp., Citrullus lanatus, black thorn (Acacia mearnsii), wheat species (Triticum spp.), barley species (Hordeum spp.), and yam species (Dioscorea spp.).Paraguayan tea (Ilex paraguariensis).

[0173] Suitably, the plants or portions thereof protected by the compounds, compositions, or agents of the present invention may be selected from plants or portions thereof that are infested by Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera, or plants or portions thereof that attract Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera. Suitably, the plants or portions thereof infested by Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera, or the Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera, may be any of those listed above.

[0174] Suitablely, the plant or part thereof that is infested by or attracts hemipteran insects is any of those listed above.

[0175] Suitablely, the plant or part thereof that is infested by or attracts dipteran insects is any of those listed above.

[0176] Appropriately, the plant or part thereof that is infested by or attracts lepidopteran insects is any of those listed above.

[0177] Appropriately, the plant or part thereof that is infested by or attracts beetles is any of those listed above.

[0178] In one embodiment, the plant or a part thereof is selected from plants or parts thereof that have been infected or attracted by hemipteran insects, such as: cereal crops such as wheat (species of the genus *Wheat*), oats (species of the genus *Oat*), rye (species of the genus *Rhizophora*), barley (species of the genus *Barley*), rice (species of the genus *Oryza*), and corn (species of the genus *Corn*); fruit and vegetable crops, including apple (species of the genus *Apple*); pear (species of the genus *Prunus*); strawberry (species of the genus *Fragaria*), blueberry (species of the genus *Vaccinium*), blackberry (species of the genus *Rubus*), raspberry (species of the genus *Rubus*), citrus (species of the genus *Citrus*), olive (species of the genus *Olea*), durian (species of the genus *Durio*), longan (species of the genus *Dimocarpus*), and lychee (species of the genus *Lychee*). chinensis), persimmon (Diospyros spp.); legumes and peas (including but not limited to species of common bean, cowpea, pea, lentil, soybean, chickpea, pigeon, and peanut), sugar beet (Beta vulgaris), sugarcane (species of sugarcane), lettuce (species of lettuce), brassica (species of brassica) (including rapeseed), onion (species of allium), tomato (species of nightshade), pepper (species of capsicum), asparagus, cucurbits, zucchini, squash (species of cucumber), cauliflower (cabbage), and tubers (potatoes) (species of nightshade), or parts thereof.

[0179] In one embodiment, the plant or a portion thereof is selected from plants or portions thereof that are susceptible to or attract aphid infestation (suitably, peach aphid infestation), including plants of the Solanaceae, Brassicaceae, and Leguminosae families, such as: cereal crops, such as wheat (wheat species, including winter wheat); fruit and vegetable crops, including peach (cherry species), strawberry (strawberry species), blueberry (blueberry species), blackberry (ruby species), raspberry (ruby species), Brassica (Brassica species) (e.g., rapeseed), lettuce (lettuce species), tomato (solepis species), pepper (capsicum species), legumes and peas (including but not limited to cowpea and pea species), cucurbits, zucchini, squash (cucumber species), citrus (citrus species), cauliflower (cabbage), and tubers (potatoes) (solepis species), or a portion thereof. In one embodiment, the plant is a vegetable crop, suitably a Brassica species.

[0180] In one embodiment, the plant or a portion thereof is selected from plants or parts thereof that have been infected by or attracted to dipteran insects, such as: cereals (wheat species); oats (oat species); rye (rye species); barley (barley species), rice (rice species), and corn (maize species); legumes and peas (including but not limited to those from the genera *Phaseolus*, *Vigna*, *Pisum*, *Lens*, *Glycine*, *Cicer*, and *Cajanus*). (e.g., peanuts (Arachis)); fruit crops (including apples (Malus species), pears (Pyrus species), strawberries (Strawberry species), blueberries (Blueberries species), blackberries (Rubus species), raspberries (Rubus species), cherries, plums, apricots, peaches, nectarines (Cherry species), blackcurrants, redcurrants, whitecurrants, currants (Rubus species), kiwifruit (Actinidia species), papaya (Carica species), avocado (Avocado species), mangoes, longans (Longan species), litchi (L. litchi). *Chinensis*, grapes (species of the genus *Vitis*), figs (species of the genus *Ficus*), passion fruit (species of the genus *Passiflora*), Asian pears (species of the genus *Pyrus*), citrus (species of the genus *Citrus*), and olives (species of the genus *Olivaceae*); vegetable crops, including allium species, eggplant, tomato (species of the genus *Solanum*) and pepper (species of the genus *Capsicum*), lettuce (species of the genus *Lactuca*), brassica (species of the genus *Brassica*), and cucumbers, cucurbits, zucchini, squash (species of the genus *Cucumis*); cauliflower (Brassica oleracea), umbelliferous root crops, including carrots (species of the genus *Daucus*), parsnip (species of the genus *Pastinaca*) or parts thereof.

[0181] In one embodiment, the plant or a part thereof is selected from plants or parts thereof that are susceptible to or attract lepidopteran insects, such as: cereal crops such as wheat (wheat species), oats (oat species), rye (rye species), barley (barley species), rice (rice species), and corn (corn species); fruit and vegetable crops, including apple (apple species); pear (plow species); tree nuts (including, for example, almonds (P. amygdalus), pistachios (pistachios), walnuts (Juglandaceae), hazelnuts (hazel species)); avocados, including avocado (Lauraceae), blueberries (blueberry species), citrus (citrus species), olives (olive species), durian (durian species), longan (longan species), and litchi (litchi (Lychee). chinensis), persimmon (species of the genus Diospyros); legumes and peas (including but not limited to species of the genera genus lentil, cowpea, pea, lentil, soybean, chickpea, pigeon pea, and peanut), sugar beet (Beta vulgaris), sugarcane (species of the genus sacchari), lettuce (species of the genus lettuce), brassica (species of the genus brassica) (including rapeseed), onion (species of the genus allium), tomato (species of the genus solanum), pepper (species of the genus capsicum), asparagus, cucurbits, zucchini, squash (species of the genus cucumber), cauliflower (cabbage), and tubers (species of the genus solanum), or parts thereof. insect

[0182] The compounds, compositions, and agents of the present invention suitably possess the insecticidal activity described above.

[0183] The compounds, compositions, and agents of this invention are effective against any insect. For example, arthropods, especially arachnids, such as species of the genera *Acarus* spp., *Aceria sheldoni*, *Aculops* spp., *Aculus* spp., *Amblyomma* spp., *Amphitetranychus viennensis*, *Argas* spp., *Boophilus* spp., *Brevipalpus* spp., *Bryobia praetiosa*, *Centruroides* spp., *Chorioptes* spp., *Dermanyssus gallinae*, *Dermatophagoides pteronyssius*, and *Dermatophagoides*. The following are species of ticks: *Dermacentor* spp., *Eotetranychus* spp., *Epitrimerus pyri*, *Eutetranychus* spp., *Eriophyes* spp., *Halotydeus destructor*, *Hemitarsonemus* spp., *Hyalomma* spp., *Ixodes* spp., *Latrodectus* spp., *Loxosceles* spp., *Metatetranychus* spp., *Nuphersa* spp., *Oligonychus* spp., and *Ornithodorus*. Species of the genera *Ornithonyssus*, *Panonychus*, *Phyllocoptruta oleivora*, *Polyphagotarsonemus latus*, *Psoroptes*, *Rhipicephalus*, *Rhizoglyphus*, and *Sarcoptes*.The species include: *Scorpio maurus*, *Stenotarsonemus* spp., *Tarsonemus* spp., *Tetranychus* spp., *Vaejovis* spp., and *Vasates lycopersici*.

[0184] Other examples come from the order Anoplura (Phthiraptera), such as species of the genera *Damalinia*, *Haematopinus*, *Linognathus*, *Pediculus*, *Ptirus pubis*, and *Trichodectes*.

[0185] Other examples come from the subclass Chilopoda, such as species of the genus *Geophilus* and species of the genus *Scutigera*.

[0186] Other examples come from the order Coleoptera, such as the cucumber beetle (Acalymma vittatum), bean weevil (Acanthoscelides obtectus), species of the genus *Adoretus*, European alder beetle (Agelastica alni), click beetle species (Agriotes spp.), black fungus beetle (Alphitobius diaperinus), summer solstice beetle (Amphimallon solstitialis), thieving beetle (Anobium punctatum), species of the genus *Anoplophora*, weevils (Anthonomus spp.), dermestid beetles (Anthrenus spp.), fine wasps (Apion spp.), slender flower beetles (Apogonia spp.), flea beetles (Atomaria spp.), felt beetles (Attagenus spp.), and four-striped bean weevil (Bruchidius). *Obtectus*, *Bruchus* spp., *Cassida* spp., *Cerotoma trifurcata*, *Ceutorrhynchus* spp., *Chaetocnema* spp., *Cleonus mendicus*, *Conoderus* spp., *Cosmopolites* spp., *Costelytra zealandica*, *Ctenicera* spp., *Curculio* spp., *Cryptorhynchus lapathi*, *Cylindrocopturus* spp., *Dermestes* spp., *Diabroticas* spp., and *Dichocrocis* spp. Species of the genera *Diloboderus*, *Epilachna*, *Epitrix*, *Faustinus*, *Gibbium psylloides*, *Hellula undalis*, *Heteronychusaratoria*, and *Heteronyx*.), Yellow-horned leaf beetle (Hylamorpha elegans), domestic longhorn beetle (Hylotrupes bajulus), alfalfa leaf weevil (Hypera postica), bark beetle species (Hypothenemus spp.), large-toothed saw beetle (Lachnosterna consanguinea), leaf beetle species (Lema spp.), potato beetle (Leptinotarsa ​​decemlineata), leaf moth species (Leucoptera spp.), rice water weevil (Lissorhoptrus oryzophilus), stem weevil species (Lixus spp.), ground beetle species (Luperodes spp.), powderpost beetle species (Lyctus spp.), large-custed grasshopper species (Megascelis spp.), black velvet gill beetle species (Melanotus spp.), blue beetle (Meligethes) *Aeneus*, species of the genera *Melolonthas*, *Migdolus*, *Monochamus*, *Naupactus xanthographus*, *Niptus hololeucus*, *Oryctesrhinoceros*, *Oryzaephilus surinamensis*, *Oryzaphagus oryzae*, *Otiorrhynchus*, *Oxycetonia jucunda*, *Phaedoncochleariae*, species of the genera *Phyllophaga*, *Phyllotreta*, *Popillia japonica*, *Premnotrypes*, and *Prostephanus*. Species of the genera *truncatus*, *Psylliodes*, *Ptinus*, *Rhizobius ventralis*, *Rhizopertha dominica*, *Sitophilus*, *Sphenophorus*, *Stegobium paniceum*, *Sternechus*, and *Symphyletes*.), ciliate weevil species (Tanymecus spp.), mealworm (Tenebrio molitor), ground beetle species (Tribolium spp.), spotted beetle species (Trogoderma spp.), seed weevil species (Tychius spp.), longhorn beetle species (Xylotrechus spp.), and ground beetle species (Zabrus spp.). Suitablely, the compounds, compositions, and agents of the present invention have activity against, for example, species selected from the order Coleoptera: bean weevil, cabbage seed weevil (Ceutorhynchus obstrictus), cabbage stem flea beetle (Psylliodeschrysocephalus), cabbage stem weevil (Ceutorhynchus pallidactylus), scarab beetle larvae (Melolontha melolontha), Colorado potato beetle (Leptinotarsa ​​decemlineata), pea and bean weevil (Sitona lineatus), pollen beetles (Meligethes spp.), dwarf beetle (Atomaria linearis), rapeseed winter stem weevil (Ceutorhynchus). (picitarsis), and nematodes (species of the genus *Agriotes* spp.).

[0187] Other examples come from the order Colchiformes, such as the armed jerboa (Onychiurus armatus).

[0188] Other examples come from the order Blattodea, such as the German cockroach (B. germanica), the Oriental cockroach (Blattaorientalis), the American cockroach (Periplaneta America), species of the genus Periplaneta (Periplaneta spp.), the brown-banded cockroach (Supella longipalpa), and those from the family Termiteidae.

[0189] Other examples come from the class Diplopoda, such as the spotted worm (Blaniulus guttulatus).

[0190] Other examples come from the order Diptera, such as species of the genera *Aedes*, *Agromyza*, *Anastrepha*, *Anopheles*, *Asphondylia*, *Bactrocera*, *Bibio hortulanus*, *Calliphora erythrocephala*, *Ceratitis capitata*, *Chironomus*, *Chrysomyia*, *Chrysops*, *Cochliomyia*, *Contarinia*, *Cordylobia anthropophaga*, and *Culex*. spp.), species of the genera *Culicoides*, *Culiseta*, *Cuterebra*, *Dacus oleae*, *Dasyneura*, *Delia*, *Dermatobia hominis*, *Drosophila*, *Echinocnemus*, *Fannias*, *Gasterophilus*, *Glossina*, *Haematopota*, *Hydrellia*, *Hylemyia*, *Hyppobosca*, and *Hypoderma*. Species of the genera *Liriomyza*, *Lucilia*, *Lutzomia*, *Mansonia*, *Musca*, *Nezara*, *Oestrus*, *Oscinella frit*, *Pegomyia*, *Phlebotomus*, and *Phorbia*.Species of the genera *Phormia*, *Prodiplosis*, *Psila rosae*, *Rhagoletis*, *Sarcophaga*, *Simulium*, *Stomoxys*, *Tabanus*, *Tannia*, *Tetanops*, and *Tipula*. Other examples of Heteroptera include: *Anasatristis*, *Antestiopsis* spp., *Boisea* spp., *Blissus* spp., *Calocoris* spp., *Campylommalivida*, *Cavelerius* spp., *Cimex* spp., *Collaria* spp., *Creontiades dilutus*, *Dasynus piperis*, *Dichelops furcatus*, *Diconocoris hewetti*, *Dysdercus* spp., and *Euschistus*. spp.), *Eurygaster* spp., *Heliopeltis* spp., *Horcias nobilellus*, *Leptocorisa* spp., *Leptoglossus phyllopus*, *Lygus* spp., *Macropesexcavatus*, Miridae, *Monalonion atratum*, *Nezaras* spp., *Oebalus* spp., Pentomidae, *Piesmaquadrata*, *Piezodorus* spp., *Psallus* spp., *Pseudacysta* persea), species of the genus Rhodnius (Rhodnius spp.).), black and brown round shield scale (Sahlbergella singularis), chestnut shield scale (Scaptocoris castanea), family Scotinophora spp., pear crowned lace bug (Stephanitis nashi), species of the genus Tibraca (Tibraca spp.), and species of the genus Triatoma (Triatoma spp.). Other examples come from the order Hemiptera, such as species of the genera *Acyrthosipon*, *Acrogonia*, *Aeneolamia*, *Agonoscena*, *Aleurodes*, *Aleurolobus barodensis*, *Aleurothrixus*, *Amrasca*, *Anuraphis cardui*, *Aonidiella*, *Aphanostigma pin*, *Aphis*, *Arboridia apicalis*, *Aspidiella*, *Aspidiotus*, and *Atanus*. spp.), eggplant whitefly (Aulacorthum solani), whitefly species (Bemisia spp.), sunflower aphid (Brachycaudus helichrysii), short-horned aphid species (Brachycolus spp.), cabbage aphid (Brevicoryne brassicae), edge ant lacewing (Calligypona marginata), bright-headed aphid (Carneocephala fulgida), long-haired gall aphid (Ceratovacuna lanigera), aphid family (Cercopidae), wax scale species (Ceroplastes spp.), apple gall aphid (Chaetosiphon fragaefolii), Java scale (Chionaspis tegalensis), rice green bug (Chlorita onukii), walnut gall aphid (Chromaphis juglandicola), cottony cushion scale (Chrysomphalus ficus), corn leafhopper (Cicadulina) mbila, Cocconytilus halli, and species of the genus Cocccus spp.* *Cryptomyzus ribis*, *Dalbulus spp.*, *Dialeurodes*, *Diaphorina*, *Diaspis*, *Drosicha*, *Dysaphis*, *Dysmicoccus*, *Empoasca*, *Eriosoma*, *Erythroneura*, *Euscelis bilobatus*, *Ferrisia*, *Geococcus coffeae*, and *Hieroglyphus*. spp.), persimmon scale (Homalodisca coagulata), rice leafhopper (Hyalopterus arundinis), species of the genera *Icerya*, *Idiocerus*, *Idioscopus*, striped leafhopper (Laodelphax striatellus), wax scale (Lecanium), scale insect (Lepidosaphes), cabbage aphid (Lipaphis erysimi), long-tubed aphid (Macrosiphum), sugarcane gall aphid (Mahanarva), sugarcane woolly aphid (Melanaphissacchari), species of the genera *Metcalfiella*, two-spined rice leafhopper (Metopolophium dirhodum), edge-horned aphid (Monellia) The following species are listed: costalis, walnut flat-horned aphid (Monelliopsis pecanis), myzus spp., Nephotettix spp., Nilaparvatalugens, Oncometopia spp., Orthezia praelonga, Parabemisia myricae, Paratrioza spp., Parlatoria spp., and Pemphigus spp.), Corn root leaf beetle (Peregrinus maidis), mealybug species (Phenacoccus spp.), pear scale (Phloeomyzus passerinii), hops aphid (Phorodonhumuli), root phylloxera species (Phylloxera spp.), shield scale (Pinnaspis aspidistrae), zoococcus species (Planococcus spp.), pear-shaped mealybug (Protopulvinaria pyriformis), five-horned shield scale (Pseudaulacaspis pentagona), mealybug species (Pseudococcus spp.), psyllid species (Psyllaspp.), ant wasp species (Pteromalus spp.), pear leaf aphid (Pyrilla spp.), four-horned shield scale (Quadraspidiotus spp.), giant shield scale (Quesada Species of the genera *gigas*, *Rastrococcus* spp., *Rhopalosiphum* spp., *Saissetia* spp., *Scaphoides titanus*, *Schizaphis graminum*, *Selenaspidus articulatus*, *Sogata* spp., *Sogatella furcifera*, *Sogatodes* spp., *Stictocephala festina*, *Tenalapharamalayensis*, *Tinocallis caryaefoliae*, *Tomaspis* spp., *Toxoptera* spp., *Trialeurodes* spp., and *Trioza* spp. Species of the genera *Typhlocyba*, *Unaspis*, *Viteus vitifolii*, and *Zygina*.

[0191] Other examples come from the order Hymenoptera, such as species of the genera *Acromyrmex*, *Athalia*, *Atta*, *Diprion*, *Hoplocampa*, *Lasius*, *Monomorium pharaonis*, *Solenopsis invicta*, *Tapinoma*, and *Vespaspp.*.

[0192] Other examples come from the order Isopoda, such as Armadillidium vulgare, Oniscus asellus, and Porcellio scaber.

[0193] Other examples come from the order Isoptera, such as species of the genera *Coptotermes*, *Cornitermes cumulans*, *Cryptotermes*, *Incisitermes*, *Microtermes obesi*, *Odontotermes*, and *Reticulitermes*.

[0194] Other examples come from Lepidoptera, such as *Acronicta major*, *Adoxophyes* spp., *Aedia leucomelas*, *Agrotis* spp., *Alabama* spp., *Amyelois transitella*, *Anarsia* spp., *Anticarsia* spp., *Argyroploces* spp., *Barathra brassicae*, *Borbo cinnara*, *Bucculatrix thurberiella*, *Bupalus piniarius*, *Busseola* spp., *Cacoecia* spp., and *Caloptilia*. Theivora, Capuareticulana, Carpocapsa pomonella, Carposina niponensis, Chematobia brumata, Chilo spp., Choristoneura spp., Clysia ambiguella, Cnaphalocerus spp., Cnephasia spp., Conopomorpha spp., Conotrachelus spp., Copitarsia spp., Cydiaspp., Dalacca noctuides, Diatraea saccharalis, Earias spp. spp.), Citrus psyllid (Ecdytolopha aurantium), small sugarcane borer (Elasmopalpus lignosellus), African giant moth (Eldana saccharina), species of the genus *Ephestia* (Ephestia spp.), species of the genus *Epinotia* (Epinotia spp.), grape flower leaf roller (Epiphyas postvittana), species of the genus *Etiella* (Etiella spp.), and species of the genus *Eulia* (Eulia spp.).The following species are listed: *Eupoecilia ambiguella*, *Euproctis* spp., *Euxoa* spp., *Feltia* spp., *Galleria mellonella*, *Gracillaria* spp., *Grapholitha* spp., *Hedylepta* spp., *Helicoverpa* spp., *Heliothis* spp., *Hofmannophila pseudospretella*, *Homoeosoma* spp., *Homona* spp., *Hyponomeuta padella*, *Kakivoria flavofasciata*, *Laphygma* spp., and *Laspeyresia*. * *Leucinodes orbonalis*, *Leucoptera* spp., *Lithocolletis* spp., *Lithophaneantennata*, *Lobesia* spp., *Loxagrotis albicosta*, *Lymantria* spp., *Lyonetia* spp., *Malacosomaneustria*, *Maruca testulalis*, *Mamestra brassicae*, *Mods* spp., *Mythimna separata*, *Nymphula* spp., *Oiketicus* spp., *Oria* spp., *Orthaga* spp. Species of the genera *Ostrinia* (corn borer), *Oulema oryzae* (rice leaf beetle), *Panolis flammea* (tobacco budworm), *Parnara* (swallowtail butterfly), *Pectinophora* (cotton bollworm), *Perileucoptera* (leaf miner), and *Phthorimaea* (potato tuber moth).Citrus leafminer (Phyllocnistiscitrella), species of the genus *Phyllonorycter*, species of the genus *Pieris*, apple moth (Platynota stultana), Indian meal borer (Plodia interpunctella), species of the genus *Plusia*, diamondback moth (Plutella xylostella), species of the genus *Prays*, species of the genus *Prodenia*, species of the genus *Protoparce*, species of the genus *Pseudaletia*, powdery armyworm (Pseudoplusia includens), purple-spotted meal borer (Pyrausta nubilalis), yellow cutworm (Rachiplusia nu), species of the genus *Schoenobius*, species of the genus *Scirpophaga*, and species of the genus *Scotia*. Species of the genera *Segetum*, *Sesamia* spp., *Sparganothis* spp., *Spodoptera frugiperda*, *Spodoptera* spp., *Stathmopoda* spp., *Stomopteryx subsecivella*, *Synanthedon* spp., *Tecia solanivora*, *Thermesia gemmatalis*, *Tinea pellionella*, *Tineolabisselliella*, *Tortrix* spp., *Trichophaga tapetzella*, *Trichoplusia* spp. (including *Trichoplusia ni*), *Tuta absoluta*, and *Virachola* spp. .

[0195] Other examples come from the order Orthoptera, such as the domestic cricket (Acheta domesticus), species of the genus Dichroplus spp., the mole cricket (Gryllotalpa spp.), the Madeira cockroach (Leucophaea maderae), species of the genus Locusta spp., species of the genus Melanoplus spp., the itch-inducing flea (Pulex irritans), and the desert locust (Schistocerca gregaria).

[0196] Other examples come from the order Fleas, such as species of the genera *Ceratophyllus*, *Ctenocephalides*, *Tunga penetrans*, and *Xenopsyllacheopis*.

[0197] Other examples come from orders within the class Syntagma, such as species of the genus *Scutigerella*.

[0198] Other examples come from the order Thysanoptera, such as *Anaphothrips obscurus*, *Baliothrips biformis*, *Drepanothris reuteri*, *Enneothrips flavens*, species of *Frankliniella*, *Heliothrips*, *Hercinothrips femoralis*, *Rhipiphorothrips cruentatus*, species of *Scirtothrips*, *Taeniothrips cardamoni*, and species of *Thrips*. Other examples come from the order Thysanura, such as *Lepisma saccharina* and *Thermobia domestica*.

[0199] In a preferred embodiment, the compounds, compositions, and agents of the present invention suitably have activity against hemiptera, dipterans, and / or lepidopteran insects. In a preferred embodiment, the compounds, compositions, and agents of the present invention suitably have activity against hemiptera insects. In a preferred embodiment, the compounds, compositions, and agents of the present invention suitably have activity against aphids. In one embodiment, the compounds, compositions, and agents of the present invention suitably have activity against the aphid species *Aphis pulcherrima*. Hemiptera insects

[0200] The compounds, compositions, and agents of the present invention suitably have activity against hemipteran insects, including aphids, planthoppers, leafhoppers, stink bugs, shield bugs, and cicadas. Suitably, the compounds, compositions, and agents of the present invention suitably have activity against aphids.

[0201] Hemiptera are defined as animals with a unique mouthpart in the form of a "beak," consisting of modified lower and upper jawbones forming a "stem" that fits inside a modified lower lip.

[0202] Many insects within these groups possess endogenous neuropeptides with sequence homology to the peptides described herein, suggesting that the compounds of the present invention may have activity against these insects.

[0203] These insects may belong to the suborder Thyracoidea, such as the superfamily Aphidoidea, superfamily Whitefly, superfamily Coccidioidea, superfamily Rhizophorae (including Rhizophorae or "Rhizophorae", and Coccidioidea or hairy needle aphids), or superfamily Psyllid (such as fleas).

[0204] Therefore, the insect could be an aphid, a member of the superfamily Aphididae. Aphids (Hemiptera: Aphididae) are one of the most important groups of agricultural pests and are the vectors for approximately 50% of insect-borne plant viruses. Within this superfamily, aphids may belong to the family Aphididae, which includes the following subfamilies: Aiceoninae, Anoeciinae, Aphidinae, Baltichaitophorinae, Calaphidinae, Chaitophorinae, Drepanosiphinae, Eriosomatinae, Greenideinae, Hormaphidinae, Israelaphidinae, and Macrophidinae. (Lachninae), Lizeriinae, Macropodaphidinae, Mindarinae, Neophyllaphidinae, Phloeomyzinae, Phllaphidinae, Pterastheniinae, Saltusaphidinae, Spicaphidinae, Taiwanaphidinae, Tamaliinae, and Thelaxinae.

[0205] Aphids may belong to genera such as Aphis nigra (e.g., pea aphid), Aphis (e.g., cotton aphid, soybean aphid), Diuraphis noxia (e.g., wheat diuraphis), Long-tubed aphid (e.g., rose long-tubed aphid, potato long-tubed aphid), Tubular aphid (e.g., peach aphid), Aphis arborescens (e.g., blackcurrant long-tubed aphid), Aphis granatum (e.g., cereal long-tubed aphid), or Aphis spp. (e.g., wheat long-tubed aphid).

[0206] The peach aphid (Peach potato aphid) is the world's most important aphid crop pest, distributed globally and hosting more than 400 species across 40 different plant families. For example, it is a major pest of crops including fruits and potatoes, and is also a vector for viruses.

[0207] The rose aphid (Rose aphid) is an important horticultural pest, especially in cultivated rose varieties, and is a vector for 12 plant viruses, including strawberry mild yellow edge virus.

[0208] The cotton aphid (also known as the melon aphid) is a pest of the Cucurbitaceae family and cotton.

[0209] Besides aphids, insects can belong to, for example, the family Aphididae, such as the genus Aphid (e.g., the coccidioidomycete).

[0210] These insects may belong to the family Amycidae, such as the genus *Bemisia tabaci* (e.g., the tobacco whitefly) or the genus *Trialeurodes* (e.g., the greenhouse whitefly).

[0211] These insects may belong to the family Psyllidaceae, such as the genus Pachypsylla (e.g., Pachypsylla venusta).

[0212] Examples of Hemiptera insects outside the suborder Sternophora, these insects may belong to the family Cestridae, such as the genus Cestrum (bed bugs), such as temperate bed bugs.

[0213] These insects may belong to the family Cicadidae, such as the genus *Cuerna* (e.g., *Cuerna arida*), the family Poaceae (e.g., *Graminella nigrifrons*), or the genus *Homalodisca* (e.g., *Homalodisca vitripennis*). The family Cicadidae also includes the cotton leafhopper (*Amrasca biguttula*).

[0214] These insects may belong to the family Planthopperidae, such as the genus *Brown Planthopper* (e.g., *Brown Planthopper*) or the genus *White-backed Planthopper* (e.g., *White-backed Planthopper*). For example, the brown planthopper (*Brown Planthopper*) is a pest of rice crops, especially in Asia.

[0215] These insects may belong to the family Psyllidaceae, such as the genus Psyllid (e.g., Citrus Psyllid).

[0216] These insects may belong to the family Pseudatomoscelis, such as the genus Pseudatomoscelis (e.g., cotton flea), the genus Lygus hesperus (e.g., grass flea), or the genus Tupiocoris (e.g., spotted Tupiocoris notatus). For example, the cotton flea (cotton flea) is a pest of cotton.

[0217] These insects may belong to the family Stink Bugs, such as those in the genera *Euschistus* (e.g., *Euschistus servus*), *Banasa* (e.g., *Banasa dimiata*), *Euschistus* (e.g., *Euschistus servus*, *Euschistus heroes*), *Murgantia* (e.g., *Murgantia histrionica*), *Euschistus* (e.g., *Euschistus servus*), *Euschistus servus* (e.g., *Euschistus servus*), or *Euschistus* (e.g., *Euschistus servus*). For example, *Euschistus servus* is a significant pest of cotton. *Euschistus servus* (brown stink bug) is a pest of many crops, including seeds, grains, nuts, and fruits, especially in the southern United States. *Euschistus servus* is a pest of grain and soybean crops, particularly in Brazil.

[0218] These insects may belong to the family Pyrrocoris, such as the genus Pyrrocoris (e.g., the wingless red bug (Pyrrocoris apterus)).

[0219] These insects may belong to the family Assassinidae, such as the genus *Rhodnius* (e.g., the long red trident bug) or the genus *Triatoma* (e.g., the infesting trident bug). The long red trident bug (*Rhodnius prolixus*) is a vector for a human disease (Chagas disease).

[0220] These insects may belong to the family Psyllidaceae, such as the genus Acanthocasuarina (e.g., Acanthocasuarina muellerianae).

[0221] In one embodiment, the insect may be selected from the following species: tea-winged bug, hero American bug (A. hilare), cotton aphid, brown stink bug, peach aphid, southern green stink bug, brown planthopper, cotton jumping mirid bug, and long red cone bug.

[0222] In one embodiment, the insect belongs to the brown planthopper species. In one embodiment, the compounds, compositions, and agents of the present invention may have activity against brown planthoppers.

[0223] In one embodiment, the insect belongs to the peach aphid species. In one embodiment, the compounds, compositions, and agents of the present invention may have activity against the peach aphid. Diptera insects

[0224] The compounds, compositions, and agents of the present invention can have activity against dipteran insects.

[0225] In particular, they may be active against Drosophila species, such as fruit flies, including those in the genus *Drosophila*, such as *Drosophila suzuki*. They may also be active against fruit flies, including species in the genera *Anastrepha*, *Fructus*, *Fructus*, *Fructus*, *Fructus*, and *Tephritis*.

[0226] The families Drosophila and Fructus are generally referred to as fruit flies.

[0227] The compounds, compositions, and agents may also be active against other important Diptera pests, such as flies of the family Ludwigiae (green bottle flies) and the following genera: Plant miners (e.g., Phytomyza angelicastri); Melani (e.g., the black-bellied leafminer (Melani agromyza)); The genus *Antherigona* (e.g., species of the genus *Antherigona*); Genus *Delia radicum* (e.g., *Delia radicum*, cabbage fly); The genus *Contarinia* (e.g., *Contarinia sorghicola*);

[0228] For more 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 Blattales

[0229] The compounds, compositions, and agents of the present invention may have activity against cockroaches, such as the German cockroach, the Oriental cockroach, the American cockroach, and the brown-banded cockroach.

[0230] In particular, they can be active against insects of the genus *Berberis*. Suitably, the compounds, compositions, and agents of the present invention can be active against the German cockroach species.

[0231] In one embodiment, the compounds, compositions, and agents of the present invention may have activity against the German cockroach. Lepidoptera

[0232] The compounds, compositions, and agents of the present invention can have activity against lepidopteran insects.

[0233] In particular, they may be active against insects of the genera *Heliothis*, *Plutella*, *Spodoptera*, *Trichoplusia*, and *Cydia*. Suitably, the compounds, compositions, and agents of the present invention may be active against the following species: *Heliothis*, *Plutella*, *H. virescens*, species of *Spodoptera*, fall armyworm, and codling moth (*Trichoplusia spp.*), larvae of *Heliothis* species, including *Peltigera virescens* and *Spodoptera spp.* (which represents many species of *Heliothis* and *Spodoptera spp.* and is a global agricultural pest), and diamondback moth (*Trichoplusia spp.*, the most important Brassica pest worldwide).

[0234] In one embodiment, the compounds, compositions, and agents of the present invention may have activity against the diamondback moth.

[0235] In one embodiment, the compounds, compositions, and agents of the present invention may have activity against the fall armyworm.

[0236] In one embodiment, the compounds, compositions, and agents of the present invention may have activity against the white-spotted armyworm. Coleoptera

[0237] The compounds, compositions, and agents of the present invention can have activity against Coleoptera insects.

[0238] In particular, they may be active against the following genera of insects: Bruchus, Ceutorhynchus, Psylliodes, Leptinotarsa, Sitona, Meligethes, Atomaria, and Agrates. Suitablely, the compounds, compositions, and agents of the present invention may have activity against the following species: bean weevil, cabbage seed weevil (Ceutorhynchus obstrictus), cabbage stem flea beetle (Psylliodes chrysocephalus), cabbage stem weevil (Ceutorhynchus pallidactylus), scarab beetle larvae (Melolontha melolontha), Colorado potato beetle (Leptinotarsa ​​decemlineata), pea and bean weevil (Sitonalineatus), pollen beetles (Meligethes spp.), dwarf beetle (Atomaria linearis), rapeseed winter stem weevil (Ceutorhynchus). picitarsis), and nematodes (species of the genus Agriotes spp.) Household pests

[0239] The compounds, compositions, and agents of this invention can also be active against household pests such as cockroaches and termites. Among more than 3,000 species, these may include the German cockroach (German cockroach), the Oriental cockroach (Oriental cockroach), the American cockroach (American cockroach), and the brown-banded cockroach (Brown-banded cockroach). Cockroaches are common household pests worldwide and can carry a variety of diseases. Controlling these and other household pests (such as ants) is envisioned by treating surfaces that insects have traversed, but particularly by using food baits containing the compounds, compositions, and agents of this invention, as well as by direct spraying of the compounds, compositions, and agents of this invention.

[0240] Therefore, another aspect of the invention may include baits comprising the compounds or compositions of the invention, suitably for use with household pests. Other aspects of the invention may include methods for controlling, reducing, suppressing, or increasing the mortality rate of household pests, comprising treating surfaces (e.g., wood) in contact with the household pests with the compounds or compositions of the invention, or bringing the household pests into contact with the compounds or compositions of the invention. Further details of such methods are described below. Optionally, treatment or contact may include suitable application methods as described elsewhere herein, such as by spraying. Therefore, sprayable formulations comprising the compounds or compositions of the invention are also suitably contemplated. Suitable formulations are described elsewhere herein. Methods and uses of the present invention Methods to increase insect mortality

[0241] This invention provides a method for increasing insect mortality, comprising contacting insects or insect populations with the compounds, compositions, or combinations described herein. The insects or insect populations may be Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera.

[0242] In one embodiment, a method for increasing the mortality rate of dipteran insects is provided, the method comprising contacting dipteran insects or a group of dipteran insects with the compounds or compositions or combinations of the present invention.

[0243] In one particular embodiment, a method for increasing the mortality rate of Drosophila suzuki is provided, comprising contacting Drosophila suzuki insects or insect populations with the compounds or compositions or combinations of the present invention.

[0244] In one embodiment, a method for increasing the mortality rate of hemiptera is provided, the method comprising contacting hemiptera or a population of hemiptera with a compound or composition or combination as defined herein.

[0245] In one particular embodiment, a method for increasing aphid mortality is provided, the method comprising contacting aphids or insect populations with a compound or composition or combination as defined herein.

[0246] In one particular embodiment, a method is provided to increase the mortality rate of beet aphids (Aphis fabae), pea aphids (Acyrthosiphon pisum), peach aphids (Myzus persicae), cotton leafhoppers (Amrasca biguttula), blackcurrant long-tubed aphids (Rhopalosiphum padi), or cereal constrictor aphids (Rhopalosiphum padi), the method comprising contacting the beet aphids, pea aphids, peach aphids, cotton leafhoppers, blackcurrant long-tubed aphids, or cereal constrictor aphids, or insect populations, with a compound or composition or combination as defined herein.

[0247] In one particular embodiment, a method for increasing the mortality rate of peach aphids is provided, the method comprising contacting peach aphid insects or insect colonies with a compound or composition or combination as defined herein.

[0248] In one particular embodiment, a method for increasing the mortality rate of tea-winged bugs is provided, the method comprising contacting the tea-winged bugs or a group of insects with a compound or composition or combination as defined herein.

[0249] In one particular embodiment, a method for increasing the mortality rate of the grain aphid is provided, the method comprising contacting the grain aphid insects or insect populations with a compound or composition or combination as defined herein.

[0250] In one particular embodiment, a method for increasing the mortality rate of brown planthoppers is provided, the method comprising contacting brown planthoppers or insect colonies with a compound or composition or combination as defined herein.

[0251] In one particular embodiment, a method for increasing the mortality rate of cotton leafhoppers is provided, the method comprising contacting cotton leafhoppers or insect colonies with a compound or composition or combination as defined herein.

[0252] In one embodiment, a method for increasing the mortality rate of lepidopteran insects is provided, the method comprising contacting lepidopteran insects or lepidopteran populations with a compound or composition or combination as defined herein.

[0253] In one particular embodiment, a method for increasing the mortality rate of diamondback moths is provided, the method comprising contacting diamondback moth insects or insect colonies with a compound or composition or combination as defined herein.

[0254] In one particular embodiment, a method for increasing the mortality rate of fall armyworm is provided, the method comprising contacting fall armyworm insects or insect colonies with a compound or composition as defined herein.

[0255] In one particular embodiment, a method for increasing the mortality rate of the white armyworm is provided, the method comprising contacting the white armyworm insects or insect colonies with a compound or composition as defined herein.

[0256] In one embodiment, a method for increasing the mortality rate of coleopteran insects is provided, the method comprising contacting the coleopteran insects or a group of coleopteran insects with a compound or composition or combination as defined herein.

[0257] In one embodiment, a method for increasing the mortality rate of cockroaches is provided, the method comprising contacting a colony of cockroaches or lepidopteran insects with a compound or composition or combination as defined herein.

[0258] In one particular embodiment, a method for increasing the mortality rate of German cockroaches is provided, the method comprising contacting German cockroaches or insect colonies with a compound or composition or combination as defined herein.

[0259] Methods to inhibit or reduce plant or site infection

[0260] The present invention also provides a method for inhibiting insect infestation of plants or plant parts, wherein the insects are suitably Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera, the method comprising contacting the plant or plant parts with the compound, composition, or combination thereof.

[0261] In one embodiment, a method for inhibiting dipteran insect infestation of plants is provided, the method comprising contacting the plant with a compound or composition or combination of the present invention.

[0262] In one particular embodiment, a method for inhibiting the infection of plants by the fruit fly *Drosophila suzuki* is provided, the method comprising contacting the plant with a compound or composition or combination of the present invention.

[0263] In one embodiment, a method for inhibiting hemiptera insect infestation of a plant is provided, the method comprising contacting the plant with a compound or composition or combination as defined herein.

[0264] In one embodiment, a method for inhibiting aphid infestation of plants is provided, the method comprising contacting the plant with a compound or composition or combination as defined herein.

[0265] In one embodiment, a method is provided for inhibiting the infestation of plants by beet aphids, pea aphids, peach aphids, cotton leafhoppers, blackcurrant long-tubed aphids, or cereal constrictor aphids, the method comprising contacting the plant with a compound or composition or combination as defined herein.

[0266] In one particular embodiment, a method for inhibiting the infestation of plants by the grain aphid is provided, the method comprising contacting the plant with a compound or composition or combination as defined herein.

[0267] In one embodiment, a method for inhibiting peach aphid infestation of plants is provided, the method comprising contacting the plant with a compound or composition or combination as defined herein.

[0268] In one embodiment, a method for inhibiting cotton leafhopper infestation of plants is provided, the method comprising contacting the plant with a compound or composition or combination as defined herein.

[0269] In one embodiment, a method for inhibiting brown planthopper infestation of plants is provided, the method comprising contacting the plant with a compound or composition or combination as defined herein. In one embodiment, a method for inhibiting tea winged bug infestation of plants is provided, the method comprising contacting the plant with a compound or composition or combination as defined herein.

[0270] In one embodiment, a method for inhibiting lepidopteran insect infestation of a plant is provided, the method comprising contacting the plant with a compound or composition or combination as defined herein.

[0271] In one embodiment, a method for inhibiting diamondback moth infestation of plants is provided, the method comprising contacting the plant with a compound or composition or combination as defined herein.

[0272] In one embodiment, a method for inhibiting fall armyworm infestation of plants is provided, the method comprising contacting the plants with a compound or composition or combination as defined herein.

[0273] In one embodiment, a method for inhibiting the infestation of plants by the white armyworm is provided, the method comprising contacting the plant with a compound or composition or combination as defined herein.

[0274] In one embodiment, a method for inhibiting the infestation of plants by coleopteran insects is provided, the method comprising contacting the plant with a compound or composition or combination as defined herein.

[0275] The present invention also provides a method for inhibiting plant growth or the infestation of a site intended for plant growth by insects, said insects being suitable to be hemiptera, diptera, lepidoptera, cockroaches and / or coleopterans, the method comprising contacting the site with said compound, composition or combination.

[0276] This method can be preventative. Therefore, for example, the compound can be applied to the plant or plant part or location when there are no or substantially no insects in the plant or plant part or field.

[0277] Suitablely, the location can be any agricultural site suitable for growing plants. Suitablely, the location can be any area or location suitable for plant growth or cultivation. Suitable locations may include farmland, brownfields, fields, greenhouses, hothouses, containers, aquaponics, and hydroponic systems, etc. In one embodiment, the location is a field.

[0278] Alternatively, the plant or part or location of the plant may have been colonized or infested by insects, preferably Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera.

[0279] Therefore, the present invention also provides a method for reducing insect infestation or insect load on plants or plant parts, the method comprising contacting the plant or plant parts with the compounds, compositions, or combinations described herein. The present invention also provides a method for reducing field insect infestation or insect load in fields, the method comprising contacting the field with the compounds, compositions, or combinations described herein. Suitable insects are Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera. Methods to reduce insect consumption

[0280] The present invention also provides a method for reducing insect feeding, the method comprising contacting an insect or insect colony with the compounds, compositions, or combinations described herein. This suitably reduces insect feeding on plants or plant parts. The insect or insect colony may be Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera. Methods to protect plants from insects

[0281] The present invention also provides methods for protecting plants or parts thereof from insect influence or infestation, particularly methods for protecting plants or plant parts from Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera insects or their infestation, wherein the method comprises the step of applying the insecticidal compound or composition or combination of the present invention directly or indirectly to the plant or plant part thereof. Suitable indirect application may include applying the compound or composition or combination of the present invention to the field or place where the plant is growing or intended to grow.

[0282] 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 infestations, particularly against Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera, or their infestations. The method comprises, under the condition of effectively protecting or treating the harvested plants or harvested parts of plants against insects, applying, directly or indirectly, the insecticidal compound or composition or combination of the present invention to the harvested plants or harvested parts of plants. Suitable indirect application may include applying the compound or composition or combination of the present invention to the storage location of the plant or harvested parts of plants, or the location where it is intended to be stored.

[0283] Appropriately, insects may belong to the orders Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera. More appropriately, insects may belong to the orders Hemiptera, Diptera, and / or Lepidoptera. Methods of contact with insects

[0284] In one embodiment, a method is provided for contacting insects with a compound (preferably an insect control agent, or even more preferably an insecticide), the method comprising applying the compound or composition or combination of the present invention to or onto a location where insects frequently appear.

[0285] Locations frequently visited by insects may be their natural habitats or areas where they are often active. These locations can then be treated with compounds or compositions as described above: as a non-limiting example, mosquito nets impregnated with encapsulated insecticides can be used as an application method. Alternatively, these locations can be created by applying visual lures or attractants targeting insects. Visual lures are known to those skilled in the art and include, but are not limited to, light sources, colored objects, and shapes or outlines that stand out against a contrasting background. As described above, insect attractants include, but are not limited to, pheromones, allergens, and egogens. Attractants may be present in the composition or may be applied separately from the compound or composition to ensure that insects are attracted to the location where the compound or composition is applied.

[0286] Appropriately, the insect can belong to the orders Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera. More appropriately, the insect belongs to the order Hemiptera. More appropriately, the insect is an aphid, such as the peach aphid. Application of compounds or compositions

[0287] The compounds, compositions, or combinations of the present invention can come into contact with insects or insect populations. Suitably, this can include applying the compounds, compositions, or combinations directly to the insects or insect populations. For example, it can be applied topically. Alternatively, the compounds, compositions, or combinations can be applied indirectly. For example, it can be applied to a substrate, location, or place where the insects or insect populations may come into contact. The substrate can be a plant or part of a plant, especially for Hemiptera, Diptera, Coleoptera, Lepidoptera, or Blattodea, which represent pests of plants (whether crops or horticultural plants), or it can be a field, location, or area suitable for plant growth. Therefore, suitably, the compounds, compositions, or combinations can be applied to plants or plant parts. Therefore, suitably, the compounds, compositions, or combinations can be applied to the location where the plant grows.

[0288] However, for insects harmful to humans, such as those in the family Bedbugidae (e.g., bedbugs of the genus *Cypripedium*, such as the temperate bedbug) or the family Assassinidae (e.g., bedbugs of the genus *Aspergillus*, such as the long red assassin bug, or aspergillus of the genus *Triatomine*, such as the harassing kissing bug), the substrate can be a household surface or item, such as bedding, mattresses, or any other suitable household surface (e.g., wood). The compound or composition can be applied to the substrate in a form suitable for insect ingestion.

[0289] Suitable contact may include, for example, feeding or spraying. Feeding may be suitably encouraged by bait or attractants, which may be included in the compositions of the present invention, as explained below.

[0290] These methods may include applying, directly or indirectly, the compounds, compositions, or combinations disclosed herein to a plant or a portion thereof, for example, at an application rate of more than 5 g of compound per hectare, for example, but not limited to, more than 10 g of compound per hectare, for example, more than 24 g of compound per hectare, for example, more than 50 g of compound per hectare, for example, more than 75 g of compound per hectare, for example, more than 100 g of compound per hectare, or particularly more than 200 g of compound per hectare. These methods may include applying, directly or indirectly, the compounds, compositions, or combinations disclosed herein to a plant or a portion thereof, for example, at an application rate of 5 to 100 g of compound composition or combination per hectare, for example, but not limited to, 5 to 200 g of compound composition or combination per hectare, particularly 5 to 50 g of compound composition or combination per hectare, for example, 5 to 30 g of compound composition or combination per hectare or 10 to 25 g per hectare.

[0291] The compounds or compositions or combinations disclosed herein may be applied to the plant or a part of the plant, either directly or indirectly, after harvest, by spraying, misting, foaming, fumigation, hydroponics, hydroponics, coating, immersion, and / or coating. Suitable contact may include, for example, feeding or spraying. In some embodiments, contact is made by ingestion.

[0292] Suitably, the compound can contact insects or insect colonies, or plants or plant parts, at any suitable effective concentration. Suitably, compositions and combinations can contain such effective concentrations of the compound. Suitably, the concentration of the compound is in the range of 10. -3 Up to 10 -9 Between M, appropriately within 10 -4 Up to 10 -6 Between M, appropriately within 10 -4 Up to 10 -5 Between M. Used as a plant protectant

[0293] This invention further provides the use of the compounds, compositions, or combinations described herein as plant protectants, particularly for protecting plants or plant parts against insects, appropriately targeting Hemiptera, Diptera, and / or Lepidoptera. The plant protectants are further described above. Used as an insect control agent

[0294] This invention provides the use of the compounds or compositions or combinations thereof described herein as insect control agents, specifically in methods for increasing insect mortality or inhibiting insect infestation of plants.

[0295] The present invention also provides the use of the compounds or compositions or combinations thereof described herein as insect control agents, particularly in methods for increasing the mortality rate of Hemiptera, Diptera, Lepidoptera, Blattodea and / or Coleoptera insects, or in methods for inhibiting or reducing insect infestation (suitably Hemiptera, Diptera, Lepidoptera, Blattodea and / or Coleoptera insects) or reducing the insect load on plants.

[0296] The present invention also provides the use of the compounds or compositions or combinations thereof described herein as insect control agents, specifically by means of their bioinhibitory effect on Hemiptera, Diptera, Coleoptera and / or Lepidoptera insects, their biocidal effect on Hemiptera, Diptera, Coleoptera and / or Lepidoptera insects, and / or their pest-killing effect on Hemiptera, Diptera, Coleoptera and / or Lepidoptera insects.

[0297] As used herein, “bioinhibition (effect)” or “bioinhibition use” includes any effect or use of the compounds or compositions or combinations described herein (optionally included in bioinhibitory, biocidal, fungicidal, or antifungal compositions as defined herein) for controlling, moderating, or interfering with the harmful activities of pests (e.g., plant pests or plant pathogens). Suitably, the pest belongs to the orders Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera. Suitably, this includes, but is not limited to, inhibiting the growth or activity of insects, altering insect behavior, and repelling or attracting insects in plants, plant parts, or other agriculturally relevant environments, such as for domestic use or in soil.

[0298] "Biotoxic activity" or "biological activity" may be used interchangeably herein, referring to the killing or severe incapacitating of pests. Suitably, it may be the same as insecticidal activity when the pest is an insect. Suitably, the compound, composition, or combination may be used as an insect control agent, wherein the insect encodes an AKH peptide.

[0299] Suitablely, the compound or composition or combination can be used as an insect control agent, wherein the insect belongs to the order Diptera. Suitablely, the compound can be used as an insect control agent, wherein the insect belongs to the genus Drosophila. Suitablely, the compound can be used as an insect control agent, wherein the insect is Drosophila suzuki.

[0300] Suitablely, compounds, compositions, or combinations as defined herein may be used as insect control agents, wherein the insect belongs to the order Hemiptera. Suitablely, compounds, compositions, or combinations as defined herein may be used as insect control agents, wherein the insect is an aphid. Suitablely, compounds, compositions, or combinations as defined herein may be used as insect control agents, wherein the insect belongs to the genus *Hemiptera*. Suitablely, compounds, compositions, or combinations as defined herein may be used as insect control agents, wherein the insect is the peach aphid.

[0301] Suitablely, compounds, compositions, or combinations as defined herein may be used as insect control agents, wherein the insect belongs to the order Hemiptera. Suitablely, compounds, compositions, or combinations as defined herein may be used as insect control agents, wherein the insect belongs to the genus Rhododendron. Suitablely, compounds, compositions, or combinations as defined herein may be used as insect control agents, wherein the insect is Rhododendron.

[0302] Suitablely, compounds or compositions as defined herein may be used as insect control agents, wherein the insect belongs to the family Cicadidae. Suitablely, compounds or compositions as defined herein may be used as insect control agents, wherein the insect is the cotton leafhopper.

[0303] Suitablely, compounds, compositions, or combinations as defined herein may be used as insect control agents, wherein the insect belongs to the order Lepidoptera. Suitablely, compounds, compositions, or combinations as defined herein may be used as insect control agents, wherein the insect belongs to the genus Diamondback moth. Suitablely, compounds, compositions, or combinations as defined herein may be used as insect control agents, wherein the insect is the diamondback moth.

[0304] Suitablely, the compounds or compositions or combinations defined herein may be used as insect control agents, wherein the insect belongs to the genus *Ophiopogon*. Suitablely, the compounds or compositions or combinations defined herein may be used as insect control agents, wherein the insect is *Pseudomonas spp.*

[0305] Suitablely, the compounds or compositions or combinations defined herein can be used as insect control agents, wherein the insect belongs to the order Coleoptera.

[0306] Suitablely, compounds or compositions or combinations as defined herein may be used as insect control agents, wherein the insect belongs to the order Blattodea. Suitablely, compounds or compositions or combinations as defined herein may be used as insect control agents, wherein the insect is a cockroach or termite. Methods to control insect fertility

[0307] This invention also provides insecticidal compounds, compositions, and combinations thereof for controlling the reproductive capacity of insect species as described herein. Suitably, the insects are selected from Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera, such as those described anywhere herein. Suitably, in some embodiments, the Hemiptera insect is the peach aphid. Suitably, in some embodiments, the Diptera insect is the fruit fly Suzuki. Suitably, in some embodiments, the Lepidoptera insect is the diamondback moth.

[0308] A method for controlling the fertility of hemipteran insects is also provided, comprising contacting the compounds or compositions of the present invention with a substrate (e.g., plants or soil). Suitably, hemipteran insects are any of those disclosed herein, such as aphids.

[0309] A method for controlling the fertility of dipteran insects is also provided, comprising contacting the compounds or compositions of the present invention with a substrate (e.g., plants or soil). Suitably, dipteran insects are any of those disclosed herein.

[0310] Methods for controlling the fertility of lepidopteran insects are also provided, comprising contacting the compounds or compositions of the present invention with a substrate (e.g., plants or soil). Suitably, lepidopteran insects are any of those disclosed herein.

[0311] A method for controlling the fertility of Coleoptera is also provided, comprising contacting the compounds or compositions of the present invention with a substrate (e.g., plants or soil). Suitably, Coleoptera are any of those disclosed herein.

[0312] A method for controlling the fertility of Blattodea insects is also provided, comprising contacting the compound or composition of the invention with a substrate (e.g., plant or soil). Suitably, Blattodea insects are any of the insects disclosed herein.

[0313] A method for controlling the fertility of hemipteran insects is also provided, comprising contacting the combination described herein with a substrate, such as plants or soil. Suitably, the hemipteran insects are any of those disclosed herein. Suitably, the combination comprises compounds of the present invention and kinins or analogues thereof.

[0314] A method for controlling the fertility of dipteran insects is also provided, comprising contacting the combination described herein with a substrate, such as plants or soil. Suitably, the dipteran insects are any of those disclosed herein. Suitably, the combination comprises compounds of the present invention and kinins or analogues thereof.

[0315] Methods for controlling the fertility of lepidopteran insects are also provided, comprising contacting the combinations described herein or the compositions of the present invention with a substrate (e.g., plants or soil). Suitably, the lepidopteran insects are any of those disclosed herein. Suitably, the combinations comprise compounds of the present invention and kinins or analogues thereof.

[0316] A method for controlling the fertility of Coleoptera is also provided, comprising contacting the combinations described herein or the compositions of the present invention with a substrate (e.g., plants or soil). Suitably, the Coleoptera are any of those disclosed herein. Suitably, the combinations comprise compounds of the present invention and kinins or analogues thereof.

[0317] A method for controlling the fertility of Blattodea insects is also provided, comprising contacting the combination described herein or the composition of the present invention with a substrate (e.g., plant or soil). Suitably, Blattodea insects are any of the insects disclosed herein. Suitably, the combination comprises the compounds of the present invention and kinins or analogues thereof.

[0318] A method for controlling the reproductive capacity of hemiptera insects or insect colonies is also provided, comprising contacting the compounds or compositions of the present invention with hemiptera insects or insect colonies. Suitably, hemiptera insects are any of those disclosed herein.

[0319] A method for controlling the reproductive capacity of dipteran insects or insect colonies is also provided, comprising contacting the compounds or compositions of the present invention with dipteran insects or insect colonies. Suitably, dipteran insects are any of those disclosed herein.

[0320] A method for controlling the reproductive capacity of lepidopteran insects or insect colonies is also provided, comprising contacting the compounds or compositions of the present invention with lepidopteran insects or insect colonies. Suitably, the lepidopteran insects are any of those disclosed herein.

[0321] A method for controlling the reproductive capacity of Coleoptera or insect colonies is also provided, comprising contacting the compounds or compositions of the present invention with Coleoptera or insect colonies. Suitably, the Coleoptera are any of those disclosed herein.

[0322] A method for controlling the reproductive capacity of cockroaches or insect colonies is also provided, the method comprising contacting the compounds or compositions of the present invention with cockroaches or insect colonies. Suitably, cockroaches are any of the insects disclosed herein.

[0323] A method for controlling the fertility of hemiptera insects or insect colonies is also provided, comprising contacting hemiptera insects or insect colonies with a combination as described herein. Suitably, the hemiptera insects are any of those disclosed herein. Suitably, the combination comprises the compounds of the present invention and kinins or analogues thereof.

[0324] A method for controlling the fertility of dipteran insects or insect colonies is also provided, comprising contacting dipteran insects or insect colonies with a combination as described herein. Suitably, the dipteran insects are any of those disclosed herein. Suitably, the combination comprises the compounds of the present invention and kinins or analogues thereof.

[0325] A method for controlling the fertility of lepidopteran insects or insect colonies is also provided, comprising contacting the combinations described herein or the compositions of the present invention with lepidopteran insects or insect colonies. Suitably, the lepidopteran insects are any of those disclosed herein. Suitably, the combinations comprise compounds of the present invention and kinins or analogues thereof.

[0326] A method for controlling the fertility of Coleoptera or insect colonies is also provided, comprising contacting the combinations described herein or the compositions of the present invention with Coleoptera or insect colonies. Suitably, the Coleoptera are any of those disclosed herein. Suitably, the combinations comprise compounds of the present invention and kinins or analogues thereof.

[0327] In the context of this invention, "controlling fertility" means reducing, suppressing, or eliminating the presence of an insect species during one or more of its growth stages. For example, the compositions of this invention can be used to control the growth of mites at any stage (e.g., egg, larval, nymph, and adult forms). Specific embodiments of the present invention

[0328] In specific embodiments, the compounds used to combat lepidopteran insects (e.g., diamondback moths) are selected from: •SB-P-86:[pyr]-LTFTSSWGG-[NH2] (SEQ ID NO: 55); •SB-P-88:[pyr]-ITFSRDWTG-[NH2] (SEQ ID NO: 57); •SB-P-117:[pyr]-LTFT[N-Me-S][N-Me-S]WGG-[NH2] (SEQ ID NO: 63); Or its salts or solvates.

[0329] In specific embodiments, the compound used to combat dipteran insects (such as *Drosophila suzukiensis* or *Drosophila melanogaster*) is: •SB-P-39:[palm]-QLTFSPDW-[NH2] (SEQ ID NO: 51); •SB-P-42:[pyr]-LTFSPDW-[NH2] (SEQ ID NO: 54) Or its salts or solvates.

[0330] In a specific embodiment, the compound used to combat cockroaches (such as the German cockroach) is: •[pyr]LTFTSSWG-[NH2] (SEQ ID NO: 67); •[pyr]LTFSSGWGN-[NH2] (SB-P-207, SEQ ID NO: 68); •[pyr]LTFSSGW-[NH2] (SB-P-208, SEQ ID NO: 69); Or its salts or solvates.

[0331] In specific embodiments, the compound used to combat lepidopteran insects (e.g., the German cockroach) is [pyr]VNFSPNW-[NH2] (SB-P-209, SEQ ID NO: 70) or a salt or solvation thereof.

[0332] In specific embodiments, the compound used to combat hemiptera (e.g., brown planthoppers) is [pyr]VNFSPGWGT-[NH2] (SB-P-161, SEQ ID NO: 71) or its salt or solvate. Combination with other insecticides

[0333] The compounds of the present invention can be used in combination with one or more other insecticides (such as those described herein). Combinations comprising the compounds of the present invention or their salts or solvates with one or more other active insecticides or insecticidal compounds are also provided.

[0334] The compositions of the present invention may also contain one or more other active insecticides or active insecticidal compounds.

[0335] Appropriately, the insecticide may be selected from insect neuropeptides or analogues thereof, such as kinins, other AKH peptides, DH31 peptides, DH44 peptides, pyrogalin or CAPA peptides (e.g., CAPA-1, CAPA-2 or CAPA-3 peptides or analogues).

[0336] Alternatively or alternatively, insecticides may be selected from chemical insecticides, such as: pyrethroids (permethrin, cypermethrin, deltamethrin); organophosphates (malathion, chlorpyrifos, diazinon); neonicotinoids (imidacloprid, thiamethoxam, thiamethoxam); carbamates (carbaryl, methomyl, propoxur); phytotoxicants (pyrethroids (derived from chrysanthemum), rotenone (derived from the roots of certain plants)); biological pest control agents (Bacillus thuringiensis (Bt) products, Beauveria bassiana (fungus), Metarhizium anisopliae (fungus)); insect growth regulators (IGRs) (tebufenozide, pyriproxyfen); fipronil; spinosad; abamectins (including abamectin and ivermectin); chitin synthesis inhibitors (diflubenzuron, flufenoxuron); piperonyl butyl ether; flonicamid; indoxacarb; dichlorodiphenyltrichloroethane; and sulfadiazine.

[0337] In certain embodiments, the additional insecticide is a kinin, such as SB-P-69 (Hy-NFSPWG-[NH2], SEQ ID NO: 74).

[0338] In a particular embodiment, the additional insecticide is an additional AKH peptide.

[0339] In a particular embodiment, the additional insecticide is DH31 peptide.

[0340] In a particular embodiment, the additional insecticide is DH44 peptide.

[0341] In specific embodiments, the additional insecticide is pyrogens, such as SB-P-048 (EQNVQSNGEPAYRVRTPRL-[NH2], SEQ ID NO: 75), SB-P-49 ([Hy]-SVPFKPRL-[NH2], SEQ ID NO: 76), and SB-P-51 ([Hy]-LRQLQSNGEPAYRVRTPRL-[NH2], SEQ ID NO: 77).

[0342] In certain embodiments, the additional insecticide is a CAPA peptide (e.g., CAPA-1, CAPA-2, or CAPA-3 peptide or the like).

[0343] Suitable, the additional insecticide or insecticidal compound may be included in the composition of the present invention.

[0344] The method of the present invention may also include contacting an insect colony or plant or a portion thereof with an additional insecticide or insecticidal compound (such as those described herein). Suitably, the additional insecticide or insecticidal compound is a kinin.

[0345] Suitablely, any reference herein to compounds of the present invention or compositions thereof may also refer to compounds of the present invention in combination with one or more insecticides or insecticidal compounds, or compositions containing such combinations.

[0346] Suitablely, combinations comprising the compounds of the present invention or their salts or solvates with one or more peptides listed in the following table are provided:

[0347] In one embodiment, the compound of the present invention is used in combination with a pykaloid, for example;

[0348] In one embodiment, the compound of the present invention is used in combination with a kinin, for example;

[0349] In one embodiment, the compounds of the present invention are used in combination with CAPA peptides (e.g., CAPA2 peptide).

[0350] In one embodiment, the compound of the present invention is used in combination with another AKH peptide, such as;

[0351] In certain embodiments, where the peptides of the present invention are to be used as insecticides against dipteran insects (e.g., Drosophila suzuki), they may be used in combination with kinins and / or pyrogens or their modified analogues.

[0352] In certain embodiments, where the peptides of the present invention are to be used as insecticides against hemiptera (e.g., peach aphids), they may be used in combination with kinins and / or pyrogens or their modified analogues.

[0353] In certain embodiments, where the peptides of the present invention are to be used as insecticides against lepidopteran insects (e.g., diamondback moth), they may be used in combination with kinins, CAPA peptides and / or pyrogens or their modified analogues.

[0354] The choice of adjuvant or additional pesticides usually depends on the specific target species. Specific combinations

[0355] In certain embodiments, a combination is provided comprising the peptides described in the embodiments and figures, particularly the compounds shown in the table below, or salts or solvates thereof: Beneficial insect species

[0356] The compounds, compositions, and combinations of the present invention are substantially nontoxic to beneficial insect species, including those that prey on pests and pollinator species. Important pollinator species include insects of the superfamily Apoidea, including bees, for example, those of the genus Apidae, such as the European bumblebee. Important predatory species include ladybugs, such as the two-spotted ladybug.

[0357] "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., pollinator species), specifically, they do not cause premature death of beneficial insect species (e.g., pollinator species). This also means that the compounds, compositions, and combinations of the present invention do not cause any harmful side effects on beneficial insect species (e.g., pollinator species), such as negatively affecting feeding behavior or mobility. Composition

[0358] The inventors have provided compositions comprising at least one insecticidal compound of the present invention or a combination thereof, which can specifically bind to insects. Importantly, through interaction with specific molecular structures of insects (e.g., receptors, suitably neural receptors), the compositions disclosed herein are capable of inhibiting, preventing, or reducing one or more biological activities of insects, thereby inhibiting, preventing, or reducing insect growth or reproductive capacity. In some embodiments, the compositions disclosed herein are capable of killing insects through specific interactions with at least one insecticidal compound contained in the composition, which is capable of specifically binding to insect receptors.

[0359] The compositions of the present invention, or compositions used according to the present invention, generally comprise a combination of the compound as described and one or more auxiliary components (e.g., solvent, carrier, diluent, auxiliary agent, preservative, dispersant, emulsifier, or synergist).

[0360] Suitablely, the composition may be an agricultural composition, an insect control composition (e.g., an insecticide composition), or a plant protection composition.

[0361] 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. Therefore, references to the application or use of any compound or combination herein should be construed as encompassing the application or use of suitable compositions thereof, unless the context requires otherwise.

[0362] The composition typically comprises the compounds described herein mixed with one or more auxiliary components, such as solvents, carriers, diluents, auxiliaries, preservatives, dispersants, emulsifiers, or synergists.

[0363] The composition may also include a combination with one or more other active insecticides described herein.

[0364] The present invention also provides a composition, such as an agricultural composition, an insect control composition, or a plant protection composition, comprising the compounds of the present invention or combinations thereof, mixed with one or more solvents, carriers, diluents, adjuvants, preservatives, dispersants, emulsifiers, or synergists. This composition may be an aqueous composition. Further details will be explained below.

[0365] As used herein, "agriculture" refers to products suitable for agricultural or agrochemical industry use, including horticultural, floricultural, and domestic and garden uses, as well as products for non-crop-related uses, such as those used by public health / pest control personnel to control unwanted insects and rodents; domestic uses, such as household fungicides and insecticides and pesticides; for protecting plants or parts of plants, crops, bulbs, tubers, fruits (e.g., from pests, diseases, or pest effects); for controlling, preferably promoting, or increasing plant growth; and / or for promoting the yield of plants, crops, or harvested plant parts (e.g., their fruits, flowers, seeds, etc.). Examples of such substances will be apparent to those skilled in the art, and preferably, in the context of this invention, include compounds with insecticidal activity (e.g., contact insecticides or systemic insecticides, including household insecticides). Other such agrochemicals may be pest control agents, growth regulators, nutrients / fertilizers, insect repellents, defoliants, etc.

[0366] As used herein, “agricultural use” includes not only the use of the insecticidal compounds, combinations thereof, or compositions thereof, and optional agrochemicals as defined above (e.g., pest control agents, growth regulators, nutrients / fertilizers, insect repellents, defoliants, etc.) of the present invention for field-grown crops (e.g., agriculture), but also the use of the compounds, combinations thereof, or compositions thereof, and the agrochemicals as defined above for greenhouse-grown crops (e.g., horticulture / floristry) or hydroponic systems, and even the use of the compounds, combinations thereof, or compositions thereof, and the agrochemicals as defined above for non-crop uses, such as uses in private gardens, household uses (e.g., household herbicides or insecticides), or uses by pest control personnel (e.g., weed control, etc.).

[0367] Suitably, the insect control compositions according to the invention are used for controlling insect colonies. Formulations of such compositions for controlling insect colonies are known to those skilled in the art and include, but are not limited to, liquid emulsifiable concentrates, wettable powders, solutions, suspension concentrates, emulsions, suspension emulsions, granules, and water-dispersible granules (Mulqueen, 2003). Preferably, the insect control compositions according to the invention comprise a combination of the insecticidal compound of the invention and optionally additional insecticidal compounds. Suitably, the insecticidal compound is contained in a carrier as described below.

[0368] The compositions of this invention may comprise pest-killing formulations or agricultural chemical formulations. As used herein, "pest-killing formulation" refers to any composition comprising a compound or combination of compounds intended to prevent, eliminate, repel, attract, or mitigate any pests. As used herein, "agricultural chemical formulation" refers to a composition for agricultural use that comprises a bioactive agent and optionally one or more additives that promote optimal dispersion, atomization, distribution, retention, and / or activity of the agricultural chemical. Such additives, by way of non-limiting example, are diluents, solvents, adjuvants, surfactants, wetting agents, spreading agents, oils, adhesives, penetrants, buffers, acidifiers, defoamers, or drift control agents.

[0369] The compositions used herein refer to compositions comprising at least one active substance (suitably an insecticidal compound of the present invention), optionally further comprising one or more additives that facilitate optimal dispersion, atomization, deposition, leaf wetting, distribution, retention, and / or absorption of said active substance. As will be clearly seen from the further description herein, the compositions used herein include biological insect control agents or biological insecticides, and these terms are used interchangeably in this application. Therefore, the compositions used herein include compositions containing at least one biomolecule as an active ingredient, substance, or element for controlling pests in plants or other agriculturally relevant environments (e.g., soil). Suitably, the at least one biomolecule comprises an insecticidal compound of the present invention or a combination thereof. Suitably, the pest is an insect. As a non-limiting example, the additives in the compositions disclosed herein may include, but are not limited to, diluents, solvents, auxiliaries, surfactants, wetting agents, dispersants, oils, binders, thickeners, penetrants, buffers, acidifiers, antisettling agents, antifreeze agents, photoprotectants, defoamers, biocides, and / or drift control agents.

[0370] Suitablely, the compositions of the present invention are aqueous compositions.

[0371] The compound content of the composition can vary over a wide range. The compound concentration of the composition is suitably an effective amount and can be from 0.0000001% to 95% by weight of the compound, preferably from 0.0001% to 1% by weight. As used herein, the terms "effective amount" and "effective dose" refer to the amount required to achieve the desired results.

[0372] In specific embodiments, the concentration of the compound of the present invention contained in the composition may be at least 0.0001% by weight. In specific embodiments, the concentration of the compound of the present invention contained in the composition may be as high as 50% by weight. In specific embodiments, the concentration of the compound of the present invention contained in the composition may be from 0.0001% to 50% by weight. In a particular embodiment, the present invention provides a composition containing at least one insecticidal compound of the present invention, wherein the concentration of at least one compound of the present invention in the composition ranges from 0.001% to 50% by weight. In yet another specific embodiment, the concentration of at least one compound of the present invention contained in the composition may be from 0.001% to 50% by weight. In yet another specific embodiment, the concentration of at least one compound of the present invention contained in the composition may be from 0.01% to 50% by weight. In yet another specific embodiment, the concentration of at least one compound of the present invention contained in the composition may be from 0.1% to 50% by weight.

[0373] The compositions of the present invention, or compositions used according to the present invention, may comprise a combination of more than one compound of the present invention, and / or a combination with other insecticidal compounds described herein. Therefore, the compositions of the present invention may, for example, comprise the first compound and the second compound of the present invention, or the first compound and the second insecticidal compound of the present invention. Suitably, the first and second compounds may be any of those described herein and may be present in the composition in any relative proportion.

[0374] The composition can be an aqueous composition, such as a brine composition. The aqueous composition may contain one or more buffers, such as phosphate buffers (e.g., phosphate-buffered saline) or Tris buffers. Alternatively, the composition can be an oil dispersion or emulsion, such as an oil and water emulsion. Alternatively, the composition can be, for example, a suspension, powder, foam, paste, granules, aerosol, impregnated natural and synthetic substances, or encapsulated in, for example, a polymer. The appropriate form of the composition for its intended use can be selected based on the target insect and its habitat.

[0375] Additives can enhance product performance, for example, by improving the delivery efficiency of the active ingredient, reducing the required level of the active ingredient, or expanding the scope of effectiveness.

[0376] Different types of adjuvants have different benefits and advantages, which are achieved by adjusting properties such as spray formation, spray retention, wetting, deposit formation, or absorption.

[0377] Adjuvants that modulate spray formation can influence spray quality by reducing spray drift and waste, thus allowing more product to reach the target. This can reduce usage, thereby improving environmental conditions and providing potentially more cost-effective solutions. Such adjuvants include blends of nonionic surfactants and emulsifiers.

[0378] Additives that regulate spray retention may dissipate the kinetic energy of droplets during impact, meaning the likelihood of bouncing or runoff is reduced. Such additives include alkyl polyglucosides, alkoxylated alcohols, and polyoxyethylene monobranched alcohols (e.g., polyoxyethylene (8) monobranched alcohols).

[0379] Additives that modulate wetting properties (i.e., wetting agents) can reduce surface tension and contact angle, thereby improving coverage. Such additives include polyoxyethylene dehydrated sorbitol monolaurate (e.g., polyoxyethylene (8) dehydrated sorbitol monolaurate), surfactant blends, and alkyl polyglucosides.

[0380] Additives that regulate sediment formation can influence the evaporation of water from droplets, thereby providing a more uniform distribution. Such additives include alkoxylated polyol esters, polyoxyethylene sorbitan monolaurates (e.g., polyoxyethylene (12) sorbitan monolaurate), and alkyl polyglucosides.

[0381] Absorption modifiers can enhance the penetration and absorption of active ingredients, such as through the cuticle of insects, thereby improving bioavailability. Such adjuvants include alkoxylated polyol esters and polyoxyethylene sorbitol monolaurates (e.g., polyoxyethylene (12) sorbitol monolaurate and polyoxyethylene (16) sorbitol monolaurate).

[0382] Dispersants can be aqueous or non-aqueous. Oil dispersion (OD) formulations typically contain a solid active ingredient dispersed in an oil. This oil can range from paraffinic solvent type to aromatic solvent type, as well as vegetable oils or methylated seed oils. Typically, the active ingredient is uniformly suspended in the oil phase. Although primarily used for water-sensitive active ingredients, OD formulations have extended to other active ingredients due to their superior spray retention, diffusion, foliar absorption, and enhanced penetration (e.g., through the insect cuticle), as the carrier oil often acts as an adjuvant.

[0383] Oils suitable for OD dispersions include flaxseed oil, rapeseed oil, and soybean oil.

[0384] Aqueous dispersants can be used, for example, to improve stability in a spray can after dilution in water, and may include modified styrene-acrylic polymers, as well as polymeric amphoteric dispersants and additives.

[0385] When OD formulations are diluted prior to spraying, emulsifiers can be used to emulsify the continuous oil phase into water. Emulsifiers can be selected based on their ability to spontaneously form emulsions. Their performance depends primarily on the properties of the surfactants and the collective effect of their arrangement at the oil / water interface. Examples include polyoxyethylene sorbitan hexaoleate (e.g., polyoxyethylene (40) sorbitan hexaoleate), emulsifier blends, and calcium alkyl aryl sulfonates.

[0386] The composition may also contain adhesives or dyes.

[0387] The compound may be provided as a concentrate for dilution prior to application. Alternatively, the compound may be provided as a solid for suspension or dissolution prior to formulation.

[0388] The compositions disclosed herein are in quite different solid or liquid forms. As solid compositions, references may be made to granules (containing up to 100% active substance) and particles, particularly particles obtained by extrusion, compression, impregnation with a granular carrier, or granulation using powder as a starting material (in the latter case, these particles contain between 0.5% and 80% active substance). Such solid compositions may optionally be used in liquid form with varying viscosity, depending on the desired type of application, such as by dilution in water. As liquid compositions, or those intended to be liquid compositions during application, references may be made to solutions, particularly water-soluble concentrates, emulsions, suspension concentrates, wettable powders (or spray powders), oils, and waxes. Suspension concentrates are used for spray application and are prepared to obtain stable fluid products that do not form sediments. They typically contain 10% to 75% active material, 0.5% to 15% surfactant, 0.1% to 10% thixotropic agent, 0% to 10% appropriate additives such as defoamers, corrosion inhibitors, stabilizers, penetrants, and binders, as a carrier of water or organic liquid in which the active material is insoluble or poorly soluble. Some organic solids or inorganic salts may be dissolved in the carrier to help prevent precipitation or act as antigelling agents for water.

[0389] As used herein, “carrier” means any solid, semi-solid, or liquid carrier in which an active substance (such as the insecticidal compounds or combinations of the present invention) may be suitably incorporated, included, immobilized, adsorbed, absorbed, bound, encapsulated, embedded, linked, or contained therein or on. Non-limiting examples of such carriers include nanocapsules, microcapsules, nanospheres, microspheres, nanoparticles, microparticles, liposomes, vesicles, beads, gels, weakly ionic resin particles, liposomes, snail delivery mediators, small particles, granules, nanotubes, buckyballs, water droplets as part of a water-in-oil emulsion, oil droplets as part of an oil-in-water emulsion, organic materials such as cork, wood, or other plant-derived materials (e.g., in seed husks, sawdust, pulp, spheres, beads, flakes, or any other suitable form), paper or cardboard, inorganic materials such as talc, clay, microcrystalline cellulose, silica, alumina, silicates, and zeolites, or even microbial cells (such as yeast cells) or suitable fractions or fragments thereof.

[0390] In one embodiment, the carrier is a liposome. In one embodiment, the composition of the present invention suitably comprises one or more liposomes, wherein each liposome comprises a compound of the present invention or a combination thereof. Therefore, the present invention suitably provides compositions or formulations comprising a plurality of liposomes, said liposomes comprising a compound of the present invention or a combination thereof. Suitably, the liposomes comprise a lipid component, suitably which may be soy lecithin and glycerol. Suitably, the liposomes are formed from soy lecithin and glycerol. Suitably, the liposomes are formed from 25 mg / ml glycerol and 3% glycerol. Suitably, the liposomes comprise an effective concentration of the compound of the present invention. Suitably, the liposomes comprise about 10 -4 M is a compound of the present invention or a combination thereof. Therefore, the present invention suitably provides a composition or formulation comprising a plurality of liposomes, said liposomes comprising a compound of the present invention or a combination thereof, soybean lecithin (preferably 25 mg / ml) and glycerol (preferably 3%).

[0391] Suitablely, liposomes can be manufactured by the Mozafari heating method (Mozafari, MR "Nanoliposomes: preparation and analysis." Liposomes: Methods and Protocols, Vol. 1: Pharmaceutical Nanocarriers (2010): 29-50). Suitablely, such a method includes: (a) mixing the compound of the invention with glycerol, preferably with a 50% glycerol solution; (b) mixing the mixture of step (a) with soybean lecithin, preferably with 350 mg of soybean lecithin in an aqueous solution; (c) heating the mixture of step (b) while stirring to form liposomes, preferably at about 60°C and about 800 RPM for about 40 minutes; (d) annealing the liposomes, preferably by placing the liposomes in water at 40°C for about 1-2 hours; and (e) sonicating the liposomes, preferably in an ultrasonic bath for about 30 minutes.

[0392] Suitablely, the liposomes have an average diameter of about 150 to 250 nm, suitablely about 175 nm to 225 nm, suitablely about 190 nm to 210 nm, and suitablely about 200 nm. Suitablely, the size of the liposomes is determined by using dynamic light scattering (DLS), for example, using Malvern Zetasizer Nano. Suitablely, the polydispersity index of the liposomes is between 0.25 and 0.35, suitablely 0.26 to 0.33, suitablely 0.26 to 0.31, suitablely 0.26 to 0.30, suitablely 0.26 to 0.29, suitablely 0.26 to 0.28, and suitablely about 0.26.

[0393] In the compositions of the present invention, the carrier containing one or more insecticidal compounds can be preserved, for example, in the form of wettable powder, wettable granules, emulsifiable concentrate, suspension concentrate, microemulsion, capsule suspension, dry microcapsule, tablet, or gel, or suspended, dispersed, emulsified, or otherwise incorporated into a suitable liquid medium (e.g., water or other suitable aqueous, organic, or oily media) to provide the (concentrated) liquid compositions of the present invention, which have stability that allows the compositions of the present invention to be suitably stored or (if necessary, further diluted) applied to the intended site of action. Suitably, the compositions of the present invention can be transported and / or stored prior to final use, optionally (and generally preferably) as suitable liquid concentrates, dry powders, tablets, capsule suspensions, slurries, or “wet cakes,” which can be suitably diluted, dispersed, suspended, emulsified, or otherwise reconstituted by the end user prior to final use. The compositions of the present invention allow application to the intended site of action using any suitable or desired manual or mechanical technique, such as spraying, pouring, dripping, brushing, coating, applying in the form of droplets, mist, or aerosol, or any other suitable technique. In one embodiment, the intended site of action is an intact, live insect, or more preferably, the surface of an insect.

[0394] This composition can be a bait composition for ingestion by target insects. The bait composition may contain one or more attractants, i.e., substances that entice insects to ingest the compound. Attractants 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 solutions of sucrose.

[0395] Commercially available basic formulations may also be used to formulate the compounds described in this specification, such as Armid. ® FMPC (Akzo Nobel).

[0396] The composition may contain one or more synergists, which are compounds that typically increase the efficacy of insecticides against their targets by inhibiting the ability of insect metabolic activators. Common synergists include piperityl butyl ether and MGK-264 (n-octylbicycloheptanedicarboximide) or peptidase inhibitors.

[0397] The composition may contain one or more agents that promote the stability of the insecticidal compound of the present invention. Suitably, one or more stability-promoting agents can prevent the degradation of the insecticidal compound of the present invention. Suitable agents for preventing the degradation of the insecticidal compound of the present invention can inhibit or reduce the activity of enzymes (suitably enzymes that degrade proteins, suitably such as proteases). Therefore, suitably, the composition may contain one or more protease inhibitors, suitably selected from: Bowman-Birk inhibitors, Kunitz inhibitors, cysteine ​​protease inhibitors, trypsin inhibitors, serine protease inhibitors, tannins, protease inhibitor-II (PI-II), and α-AI1.

[0398] The composition may also contain one or more other attractants, sterilizing agents, acaricides, nematicides, fungicides, growth regulators, or herbicides.

[0399] In some embodiments, the composition may comprise one or more other agricultural chemicals or agrochemicals, such as herbicides (e.g., contact or systemic herbicides, including household herbicides), fungicides (e.g., contact or systemic fungicides, including household fungicides), nematicides (e.g., contact or systemic nematicides, including household nematicides) and other pest control agents or biocides (e.g., agents that kill insects or snails); as well as fertilizers; growth regulators, such as plant hormones; micronutrients, safeners, pheromones; insect repellents; insect baits; and / or active ingredients for regulating (i.e., increasing, decreasing, inhibiting, enhancing, and / or triggering) gene expression (and / or other biological or biochemical processes) in target plants (e.g., plants to be protected or plants to be controlled), such as nucleic acids (e.g., single-stranded or double-stranded RNA, for example, used in the context of RNAi technology) and other factors, proteins, chemicals, etc., known for this purpose.

[0400] Examples of such agrochemicals will be clear to those skilled in the art; for example, including but not limited to: chlorantraniliprole, glyphosate, paraquat, metolachlor, acetochlor, mesotrione, 2,4-D, atrazine, glufosinate, sulfadiazine, quizalofop-p-ethyl, pendimethalin, chlorpyrifos, trifluralin, bromobenzonitrile, chloroxac, fluroxypyr, nicosulfuron, bensulfuron-methyl, imidacloprid, dicamba, imidacloprid, thiamethoxam, fipronil, chlorpyrifos, deltamethrin, trichlorfon Cypermethrin, endosulfan, methamidophos, carbofuran, thiamethoxam, cypermethrin, abamectin, fluroxypyr, spinosad, indoxacarb, bifenthrin, heptafluthrin, pyraclostrobin, thiamethoxam, tebuconazole, mancozeb, cyazofamid, fluazinam, azoxystrobin, flutriafol, chlorothalonil, copper fungicides, azoxystrobin, prothioconazole, difenoconazole, carbendazim, propiconazole, thiophanate-methyl, sulfur, cyazofamid, and other known agrochemicals or any suitable combination thereof. Methods for producing insecticidal compounds

[0401] The insecticidal compounds described herein can be produced by any method known in the art for producing peptides. In one embodiment, the insecticidal compounds can be produced by chemical methods or suitable chemical synthesis methods.

[0402] The insecticidal compounds of this invention can be synthesized using any suitable chemical method.

[0403] Suitable insecticidal compounds are peptides. Therefore, they are suitably synthesized via solid-state peptide synthesis. Suitablely, this synthesis can be performed using commercially available equipment, such as the Biotage Initiator+Alstra microwave-assisted peptide synthesizer or the CEM Liberty Prime microwave-assisted peptide synthesizer.

[0404] In another aspect of the invention, isolated insecticidal compounds produced by the method of the invention are provided. Suitably, isolated insecticidal compounds of formula (I) or (II) are produced by the method of the invention.

[0405] In another aspect of the invention, a method for producing the compositions disclosed herein is provided, the method comprising at least the steps of: (a) obtaining at least one insecticidal compound having formula (I) or (II); and (b) formulating the insecticidal compound into a composition.

[0406] In another aspect of the invention, a method for producing and / or manufacturing variants of an insecticidal compound of formula (I) is provided. This may include the steps of: (i) modifying a peptide Z having formula (I) by adding, substituting, or deleting at least one amino acid; (ii) evaluating the insecticidal activity of the variant thus produced, and—optionally—at least one property selected from the group consisting of biological stability, chemical stability, bioavailability, solubility (including the ability to form stable formulations), manufacturability, and production cost. When the insecticidal activity is reduced compared to unmodified peptide Z, steps (i) and (ii) are repeated until a variant with improved insecticidal activity is obtained. When the insecticidal activity is improved compared to unmodified peptide Z, the method may include further steps of manufacturing, isolating, and purifying the variant. Screening for insecticidal activity and other properties described above may be performed as described below or as commonly known to those skilled in the art.

[0407] In one embodiment, a method for manufacturing a variant of the insecticidal compound of the present invention is provided, the method comprising the following steps: a) Modify peptide Z by adding, replacing, or deleting at least one amino acid; b) Assess the insecticidal activity of the variant, and—optionally—at least one property selected from the group consisting of: biological stability, chemical stability, bioavailability, solubility (including the ability to form stable formulations), manufacturability and production cost; c) When the insecticidal activity is reduced compared to insecticidal compounds containing unmodified peptide Z, repeat steps (a) and (b) until a variant with enhanced insecticidal activity is obtained; d) When the insecticidal activity is improved compared to insecticidal compounds containing unmodified peptide Z, the variant is further manufactured, isolated, and purified.

[0408] Suitablely, the steps of obtaining at least one insecticidal compound include (a) chemically synthesizing the insecticidal compound.

[0409] Suitable compositions are as described above. Suitable manufacturing methods for formulating such compositions are known in the art and include, but are not limited to, high or low shear mixing, wet or dry milling, drop casting, encapsulation, emulsification, coating, shelling, pelletizing, extrusion granulation, fluidized bed granulation, co-extrusion, spray drying, spray cooling, atomization, addition or condensation polymerization, interfacial polymerization, in-situ polymerization, coagulation, spray encapsulation, cooled melt dispersion, solvent evaporation, phase separation, solvent extraction, sol-gel polymerization, fluidized bed coating, pot coating, melting, passive or active absorption or adsorption.

[0410] Features disclosed in the foregoing description, or in the following claims, or in the accompanying drawings, whether in their specific form or in terms of the means for performing the disclosed functions, or in the methods or processes for obtaining the disclosed results, may, as the case may, be used alone or in any combination of such features to implement various forms of the invention.

[0411] While the 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 this disclosure. Therefore, the exemplary embodiments of the invention set forth above are considered illustrative rather than restrictive. Various changes may be made to the described embodiments without departing from the spirit and scope of the invention.

[0412] To avoid any doubt, any theoretical explanations provided herein are offered solely for the purpose of enhancing the reader's understanding. The inventor does not wish to be bound by any of these theoretical explanations.

[0413] Any section headings used herein are for typographical purposes only and should not be construed as limiting the scope of the subject matter. Specific aspects and embodiments of the invention

[0414] The following paragraphs are not claims, but are used to define specific aspects and embodiments of the invention. Paragraph 1. An insecticidal compound having the following formula (I), or a salt or solvate thereof: R 1 -L 1 -Y 1 -YZY 2 -R 2 (I) in: R 1 It is hydrogen (which can be named "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 1-6Alkyl-C 6-10 Aryl, biotin, sugar moiety, (poly)alkylene glycol, heterocyclic group, phosphate group or sulfate group; Where R 1a R 1b R 1c R 1d and R 1e Each is independently selected from hydrogen or C. 1-4 Alkyl groups (e.g., methyl, ethyl, propyl, butyl). And any alkyl, formyl, acyl, fatty acyl, benzyl, benzoyl, heteroaryl, trifluoroacetyl, -NHC 1-18 Alkyl, -NHC 6-16 Aryl, -NH-C 1-6 Alkyl-C 6-10 The aryl, (poly)alkylene glycol, or heterocyclic group may optionally be substituted by one or more groups selected from the following: halogen, oxo, C 1-6 Alkyl, C 1-6 Halogenated alkyl group, sugar moiety, phosphate group or sulfate group; L 1 It does not exist or: –(C=O)C 1-16 -alkylene-NH-, where Indicates Y 1 Attachment points of Y or Z; (C 1-20 )alkylene; (C 2-20 ) imidene group; (poly)alkylene glycols; Where L 1 Optionally substituted by one or more groups selected from the following: oxo (=O), halogen, cyano, =NR 1a NR 1a R 1b OR 1a S = S; where R 1a and R 1b Each is independently hydrogen or C 1-2 alkyl; Y 1 Peptides that either do not exist or contain one or two amino acids; Y is a peptide containing 1 to 12 amino acids; wherein Y optionally contains a (poly)alkylene glycol linker in the peptide sequence; Y 2 Peptides that either do not exist or contain one or two amino acids; Z is a peptide according to formula (Zi). Z 1 -Z2 -F # -Z 4 -Z 5 -Z 6 -W # -Z 8 -Z 9 (Zi) in: Z 1 Does not exist or selected from L # I # or V # ; Z 2 Selected from T # or N # ; Z 4 Selected from S # or T # ; Z 5 Selected from P # R # S # or T # ; Z 6 Selected from D # S # N # T # or G # ; Z 8 Does not exist or selected from G # or T # ; Z 9 Does not exist or selected from G # N # Q # or T # ; in" # This indicates that the residue is independently an unmodified amino acid, a modified amino acid, or a non-natural amino acid analogue listed; and R 2 It is NH2, NR 2a H, NR 2a R 2b OR 2a ;where R 2a and R 2b If they exist, they are each independently C. 1-6 -alkyl (e.g., methyl, ethyl, propyl, butyl, pentyl, or hexyl), C 3-6 -Alkenyl, C 6-16- Aryl, C 6-16- Aryl-C 1-6 -alkyl, C1-6 -alkylene-C 6-16 -Aryl or C 1-6 - Haloalkyl groups, each of which may optionally be substituted by one or more groups selected from: halogen, C 1-6 -alkyl or C 1-6- Halogenated alkyl groups. Paragraph 2. Insecticidal compounds as described in paragraph 1, wherein Y is absent or residue Q is present. # ; in" # "This indicates that the residue is a naturally occurring amino acid, a modified amino acid, or a non-natural amino acid analogue; Paragraph 3. Insecticidal compounds as described in paragraph 1 or paragraph 2, wherein Y is absent or is residue Q. Paragraph 4. The insecticidal compound as described in any of the preceding paragraphs, wherein Y 1 and Y 2 None of them exist. Paragraph 5. An insecticidal compound as described in any of the preceding paragraphs, wherein Z is a peptide having the formula (Z-ia) or (Z-ib): Z 1 -T # -F # -Z 4 -Z 5 -Z 6 -W # -Z 8 -Z 9 (Z-ia) Z 1 -N # -F # -Z 4 -Z 5 -Z 6 -W # -Z 8 -Z 9 (Z-ib) Z 1 Z 4 Z 5 Z 6 Z 8 and Z 9 As defined in paragraph 1; in" # "" indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs. Paragraph 6. The insecticidal compound as described in any of the preceding paragraphs, wherein: Y is Q or does not exist. Z 1 Is it L or I?# Z 2 Selected from T # or N # Z 4 Selected from S # or T # Z 5 Selected from P # R # S # or T # ; Z 6 Selected from D # S # N # or G # ; Z 8 and Z 9 Neither exists or: Z 8 Selected from T # or G # ; Z 9 Does not exist or selected from G # N # or T # ; in" # "" indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs; Optional, of which Z 1 Is it L or I? # Z 2 Selected from T # or N # Z 4 Selected from S # or T # Z 5 Selected from P # R # or S # ; Z 6 Selected from D # or S # ; Z 8 and Z 9 Neither exists or: Z 8 Selected from T # or G # ; Z9 It is G # or N # ; in" # "" indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs; Further, optionally, wherein: Z 1 It is L # Z 2 It is T # Z 4 Selected from S # or T # ; Z 5 Selected from P # or S # ; Z 6 Selected from D # or S # ; Z 8 and Z 9 None of them exist in" # "" indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs. Paragraph 7. An insecticidal compound as described in any one of paragraphs 1 to 4, wherein Z is a peptide having a formula selected from: L # -T # -F # -S # -P # -D # -W # (Z A ) L # -T # -F # -T # -S # -S # -W # -G # -G # (Z B ) L # -T # -F # -T # -P # -N # -W # (Z C ) I # -T # -F # -S # -R # -D # -W # -T # -G # (Z D ) T # -F # -S # -R # -D # -W # -T # -G # (Z E ) V # -N # -F # -T # -P # -T # -W # -G # -Q # (Z F ) L # -N # -F # -S # -P # -G # -W # (Z G )or L # -N # -F # -S # -T # -G # -W # (Z H ) in" # "" indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs; Optionally, any one of Z is a peptide having a formula selected from the following: L # -TF # -SP # -D # -W(Z A1 ) L # -TF # -TS # -S #-WGG(Z B1 ) L # -TF # -TP # -N # -W(Z C1 ) I # -TF # -SR # -D # -WTG(Z D1 ) T # -FS # -RD # -WTG(Z E1 ) V # -NF # -TP # -T # -WGQ(Z F1 ) L # -NF # -SP # -G # -W(Z G1 )or L # -NF # -ST # -G # -W(Z H1 ) in" # "" indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs. Paragraph 8. An insecticidal compound as described in any of the preceding paragraphs, wherein Z is a peptide having a formula selected from: L # -T # -F # -S # -P # -D # -W # (Z A ) L # -T # -F # -T # -S # -S # -W # -G # -G # (Z B ) I # -T # -F # -S # -R # -D # -W # -T # -G # (Z D ) Optionally, Z is a peptide having the following formula: (Z A1 ) L # -TF # -SP # -D # -W(Z A1 ) L # -TF # -TS # -S # -WGG(Z B1 )or I # -TF # -SR # -D # -WTG(Z D1 ) in" # "" indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs. Paragraph 9. The insecticidal compound as described in any of the preceding paragraphs, wherein at least one residue of peptides Y and Z is a modified amino acid or a non-natural amino acid analog; optionally, wherein at least one of peptides Y and Z is: iN-methylated amino acids; ii. Non-protein amino acids, such as hydroxyproline (Hyp: L-hydroxyproline or (2S,4R)-4-hydroxyproline), octahydroindole-2-carboxylic acid (Oic), sarcosine (Sar), oroleucine (Nle), α-aminoisobutyric acid (Aib), thienylalanine (Thi), or thiazolidin-4-carboxylic acid (Thz), phenylglycine (Phg), or γ-aminobutyric acid (gaba); iii. D-amino acids iv. β-amino acids v. Peptide-like amino acid analogs; vi. Amino acids modified by sugars; or vii. Biotin-modified amino acids; Optionally, at least one of the residues in peptides Y and Z is: iN-methylated amino acids; ii. Peptide-like amino acid analogs; iii. Non-protein amino acids selected from hydroxyproline (Hyp: L-hydroxyproline or (2S,4R)-4-hydroxyproline), octahydroindole-2-carboxylic acid (Oic), sarcosine (Sar), oroleucine (Nle), α-aminoisobutyric acid (Aib), thienylalanine (Thi), or thiazolidin-4-carboxylic acid (Thz). iv. D-amino acids. Paragraph 10. The insecticidal compound as described in any of the preceding paragraphs, wherein at least one residue of peptides Y and Z is: iN-methylated amino acids; ii. Thiophene-alanine (Thi) iii. Thiazolidine-4-carboxylic acid (Thz); or iv. D-amino acids. Paragraph 11. The insecticidal compound as described in any of the preceding paragraphs, wherein 1 to 6 residues in the peptide moiety YZ are modified amino acids or non-natural amino acid analogs; Optionally, one to five residues in the peptide portion YZ contain modified amino acids or non-natural amino acid analogs; Optionally, one to four residues in the peptide portion YZ contain modified amino acids or non-natural amino acid analogs. Paragraph 12. An insecticidal compound as described in any of the preceding paragraphs, wherein the Z portion has a formula selected from the following: LTFSPDW; [n-me-L]TFSPDW; LT[n-me-F]SPDW; LTFTSSWGG; LTFTPNW; ITFSRDWTG; LNFSTGW; LT[f]S-[Thz]-dW; TFSRDWTG; VNFTPTWGQ; LNFSPGW; LT-[Thi]-SP-[N-Me-D]-W; or LTFT-[n-me-S]-[n-me-S]-WGG; Optionally, the Z portion has a formula selected from the following: LTFSPDW; LTFTSSWGG; ITFSRDWTG. Paragraph 13. The insecticidal compound as described in any of the preceding paragraphs, wherein R 1 Selected from: (i)Hydrogen; (ii) An acyl group optionally substituted with the following: sugar moiety; (iii) fatty acyl group; (iv) heteroaryl; (v)-NHC 6-16 Aryl; (vi) Sugar portion; (vii) Biotin; (viii) 5- or 6-membered heterocyclic groups; or (ix) has the formula –(OCH2CH2) n -R p (poly)ethylene glycol, in which Indicates with L 1 The attachment point of Y or Z, where n is an integer from 1 to 16, and R p Selected from -NH2, -OH, or -OMe; And any acyl, fatty acyl, benzyl, benzoyl, heteroaryl, -NHC 6-16 The aryl, (poly)alkylene glycol, or heterocyclic group may optionally be a substituted group that is optionally replaced by one or more groups selected from: halogen, oxo, C 1-3 Alkyl or C 1-3 Halogenated alkyl Optionally, where R 1 Selected from: hydrogen; The acyl group may be optionally substituted with the following: sugar moiety, wherein the acyl group is selected from formyl, acetyl (Ac), propionyl, butanoyl. Selected from the following fatty acyl groups: palmitoyl, butyryl, waxyl, decanoyl, dodecanoyl, tunganoyl, heptanoyl, hexanoyl, eicosanoyl, eicosanoyl, limonoyl, myristoyl, nonanoyl, octadecanoyl, octanoyl, palmitoyl, stearoyl, undecanoyl, and pentanoyl; Indole, such as 3-indole: ; -NHC 6-16 Aryl; Monosaccharide or disaccharide portion; Biotin; 5-6 membered heterocyclic groups, such as pyrrolidone-2-one: ; Having a style –(OCH2CH2) n -R p (poly)ethylene glycol, in which Indicates with L 1 The attachment point of Y or Z, where n is an integer from 4 to 12, and R p Selected from -NH2, -OH or -OMe And any acyl, fatty acyl, benzyl, benzoyl, heteroaryl, -NHC 6-16 The aryl, (poly)alkylene glycol, or heterocyclic group may optionally be a substituted group that is optionally replaced by one or more groups selected from: halogen, oxo, C 1-3 Alkyl or C 1-3 Halogenated alkyl groups. Paragraph 14. The insecticidal compound as described in any of the preceding paragraphs, wherein R 1 Selected from: hydrogen; The acetyl group may be optionally replaced by either a monosaccharide or a disaccharide moiety; pyrrolidone-2-one, for example ; Palmitoyl; or Having a style –(OCH2CH2) n -NH2 in (poly)ethylene glycol, wherein Indicates Y 1 The attachment point of Y or Z, and n is an integer from 6 to 10; Optionally, where R 1 Selected from: hydrogen; pyrrolidone-2-one, for example ; Palmitoyl; or Having a style –(OCH2CH2)8-NH2 in (poly)ethylene glycol, wherein Indicates Y 1 Attachment points of Y or Z. Paragraph 15. The insecticidal compound as described in any of the preceding paragraphs, wherein L 1 It does not exist or: –(C=O)C 1-12 -alkylene-NH-, –(C=O)-C 1-10 Alkylene-(C=O)- –(C=O)-C0-10 Alkylene; C 1-10 alkylene; or -(C=O)-; in Indicates Y 1 Attachment points of Y or Z; Any of L 1 The group may optionally be replaced by one or more oxo (=O) groups; L can be selected from 1 It does not exist or: –(C=O)C 4-12 -alkylene-NH-, –(C=O)-C 1-4 Alkylene-(C=O)- –(C=O)-C 1-4 Alkylene; C 1-4 alkylene; or -(C=O)-; Any of L 1 The group may optionally be replaced by one or more oxo (=O) groups; in Indicates Y 1 Attachment points of Y or Z. Further, in any of the L 1 It does not exist or: ; ; ; ;or ; in Indicates Y 1 Attachment points of Y or Z. Paragraph 16. The insecticidal compound as described in any of the preceding paragraphs, wherein R 2 It is NH2. Paragraph 17. The compound, or its salt or solvation, as described in paragraph 1, is selected from: Paragraph 18. A composition, such as an insect control composition or a plant protection composition, comprising a compound as described in any one of paragraphs 1 to 17 mixed with one or more solvents, carriers, diluents, adjuvants, preservatives, dispersants, emulsifiers or synergists; optionally wherein the composition is an aqueous composition. Paragraph 19. The composition as described in paragraph 18 further comprises one or more of kinin, additional AKH peptide, DH31 peptide, DH44 peptide, pyrogalin, or CAPA peptide (e.g., CAPA-1, CAPA-2, or CAPA-3 analogs). Paragraph. The use of any compound as described in any one of paragraphs 1 to 17 or the composition as described in paragraph 18 or 19 for any of the following purposes: i) Insect control agents; or ii) Plant protectants used to protect plants or parts thereof from insects; These insects are, by choice: a) Diptera insects, preferably selected from: Drosophila melanogaster or Drosophila suzuki; b) Hemiptera insects, such as aphids, preferably selected from: beet aphid, pea aphid, peach aphid, cotton leafhopper or cereal constrictor aphid; c) Lepidoptera insects, preferably selected from diamondback moth or fall armyworm; d) Coleoptera insects; and / or e) Blattodea insects, preferably of which the German cockroach is; Further, optionally, these insects are: a) Diptera insects, preferably selected from: Drosophila melanogaster or Drosophila suzuki; b) Hemiptera insects, such as aphids, preferably selected from: beet aphids, pea aphids, peach aphids, cotton leafhoppers, or cereal constrictor aphids; and / or c) Lepidoptera insects, preferably selected from diamondback moth or fall armyworm. Paragraph 21. A method for increasing insect mortality, the method comprising contacting insects or insect colonies with a compound as described in any one of paragraphs 1 to 17 or a composition as described in paragraphs 18 or 19. Paragraph 22. A method for inhibiting or preventing insect infestation of a plant, the method comprising contacting the plant or a portion thereof, or the location where the plant is growing or is intended to grow, with a compound as described in any one of paragraphs 1 to 17 or a composition as described in paragraphs 18 or 19; Optionally, the compound or composition may be brought into contact with the plant or its parts, or the location where the plant is growing or is intended to grow, when there are no or substantially no insects in the plant or its parts. 23. A method for reducing or treating insect infestation of plants or reducing insect load on plants, the method comprising contacting the plant or a portion thereof, or the location where the plant is growing, with a compound as described in any one of paragraphs 1 to 17 or a composition as described in paragraphs 18 or 19. 24. The method as described in any one of paragraphs 21 to 23, wherein one or more of the following are applicable: a) The location where the plant is growing or is expected to grow may include an agricultural location suitable for growing plants, preferably including a field; b) Contact with the insect or insect colony, plant or part thereof, or location includes treating the insect or insect colony, plant or part thereof, or location with the compound or composition by: irrigation, feeding, spraying, misting, foaming, fogging, hydroponics, hydroponics, coating, immersion and / or coating; and / or c) Contacting the insect or insect colony, plant or part thereof, or location with an effective concentration of the compound, preferably at 10 -3 M to 10 -9 The concentrations between M. 25. The method as described in any one of paragraphs 21 to 24, wherein the insects are: a) Diptera insects, preferably selected from: Drosophila melanogaster or Drosophila suzuki; b) Hemiptera insects, such as aphids, preferably selected from: beet aphid, pea aphid, peach aphid, cotton leafhopper or cereal constrictor aphid; c) Lepidoptera insects, preferably selected from diamondback moth or fall armyworm; d) Coleoptera insects; and / or e) Blattodea insects, preferably of which the German cockroach is; These insects are, by choice: a) Diptera insects, preferably selected from: Drosophila melanogaster or Drosophila suzuki; b) Hemiptera insects, such as aphids, preferably selected from: beet aphids, pea aphids, peach aphids, cotton leafhoppers, or cereal constrictor aphids; and / or c) Lepidoptera insects, preferably selected from diamondback moth or fall armyworm. Attached Figure Description

[0415] Aspects and embodiments of the invention will now be discussed with reference to the accompanying drawings, in which: Figure 1-4 The activity data of the unformulated peptide according to the invention, administered alone or in combination with another peptide, against Drosophila suzuki in the Café bioassay are shown. Figure 5 The activity data of the unformulated peptide according to the present invention against diamondback moth in a leaf immersion assay are shown. Figure 6 The results of oral toxicity to bees are shown, expressed as survival 96 hours after administration of the combination of SB-P-99, SB-P-39 and SB-P-51. Figure 7 The data show the fertility of the unformulated peptide according to the invention in oviposition assays in Drosophila suzuki for the analogue SB-P-112. Figure 8 The experimental setup for the café assay is shown. Figure 9 The experimental setup for the leaf immersion assay is shown. Figure 10 The data show the activity (control %) of various peptide compositions according to the present invention against Drosophila suzuki on blackberry plants in field trials conducted by Collins Agricultural Consultants. Figure 11 This shows the 1 x 10⁻⁶ peptides in a leaf immersion assay for the diamondback moth. -4 The administration of a single (unformulated) peptide of M and 10 -4 Activity of M peptide combination (mortality %) (top plot) and leaf remaining %) (bottom plot). Figure 12 The data show the activity (control %) of 1 x 10⁻⁴ M peptide SB-P-86 against diamondback moth (Caragana korshinskii) on cabbage (cauliflower) in a field trial conducted by Collins Agricultural Consultants in the United States. Figure 13 The data show the activity (control %) of the 1 x 10⁻⁴ M peptide SB-P-86 against the cabbage looper moth (Brassica napus) in a field trial conducted by Collins Agricultural Consultants in the United States. Figures 14 to 18 The activity data for the unformed peptides and peptide combinations discussed in this paper are shown. Figure 19 The chemical synthetic route for synthesizing SB-P-86 is shown; Figure 20 The experimental setup for determining artificial feed for Lepidoptera was shown. Figure 21 The activity data of unformulated SB-P-86 against fall armyworm are shown after 168 hours. One larva was measured per cell (n = 10). Figure 22 The reaction scheme for the synthesis of SB-P-42 at a scale of 0.5 mmol is shown. Figure 23 The HPLC trace of SB-P-42 is shown. Figure 24 The LCMS trace of SB-P-42 is shown. Figure 25 The reaction scheme for the synthesis of SB-P-49 at a scale of 0.5 mmol is shown. Figure 26 The HPLC trace of SB-P-49 is shown. Figure 27 The LCMS trace of SB-P-49 is shown. Figure 28 The activity data of the unformulated SB-P-42 (AKH) + SB-P-49 (pyrogens) combination against Drosophila Suzuki are shown after 96 hours using a Café assay. Figure 29 The reaction scheme for the synthesis of SB-P-39 at a scale of 0.5 mmol is shown. Figure 30 The HPLC trace of SB-P-39 is shown. Figure 31 The LCMS trace of SB-P-39 is shown. Figure 32 The reaction scheme for the synthesis of SB-P-51 at a scale of 0.5 mmol is shown. Figure 33 The HPLC trace of SB-P-51 is shown. Figure 34 The LCMS trace of SB-P-51 is shown. Figure 35 The reaction scheme for the synthesis of SB-P-112 is shown. Figure 36 The HPLC trace of SB-P-112 is shown. Figure 37 The LCMS trace of SB-P-112 is shown. Figure 38 The reaction scheme for the synthesis of SB-P-138 is shown. Figure 39 The HPLC trace of SB-P-138 is shown. Figure 40 The LCMS trace of SB-P-138 is shown. Figure 41 The reaction scheme for the synthesis of SB-P-161 is shown. Figure 42The HPLC trace of SB-P-161 is shown. Figure 43 The LCMS trace of SB-P-161 is shown. Figure 44 The reaction scheme for the synthesis of SB-P-179 is shown. Figure 45 The HPLC trace of SB-P-179 is shown. Figure 46 The LCMS trace of SB-P-179 is shown. Figure 47 The reaction scheme for the synthesis of SB-P-190 is shown. Figure 48 The HPLC trace of SB-P-190 is shown. Figure 49 The LCMS trace of the SB-P-190 is shown. Figure 50 The reaction scheme for the synthesis of SB-P-207 is shown. Figure 51 The HPLC trace of SB-P-207 is shown. Figure 52 The LCMS trace of SB-P-207 is shown. Figure 53 The reaction scheme for the synthesis of SB-P-208 is shown. Figure 54 The HPLC trace of SB-P-208 is shown. Figure 55 The LCMS trace of SB-P-208 is shown. Figure 56 The reaction scheme for the synthesis of SB-P-209 is shown. Figure 57 The HPLC trace of SB-P-209 is shown. Figure 58 The LCMS trace of SB-P-209 is shown. Figure 59 The reaction scheme for the synthesis of SB-P-233 is shown. Figure 60 The HPLC trace of SB-P-233 is shown. Figure 61 The LCMS trace of SB-P-233 is shown. Figure 62 The field stability results for SB-P-42 are shown. Figure 63 The field stability results for SB-P-112 are shown. Figure 64The results show the UV drying lamp stability of SB-P-42. Figure 65 The results show the UV drying lamp stability of SB-P-112. Figure 66 The results show the stability of SB-P-42 at 54°C. Figure 67 The results show the stability of SB-P-112 at 54°C. Figure 68 The study showed that, 7 days after application in a laboratory spray assay conducted via FERA, 2 x 10 -4 Activity data of M's SB-P-86 against diamondback moth. Figure 69 The activity data of the unformulated peptide combination according to the present invention against Drosophila suzuki in the Café bioassay are shown. Figure 70 This shows the activity data of SB-P-42+49 (combination) and SB-P-39+49 (combination) against *Drosophila suzuki* on strawberry plants in a field trial conducted by Impact Agronomics. The peptides were applied twice (A and B) at 7-day intervals. DAA: Days after application of A. DAB: Days after application of B. Figure 71 The data show the activity (control %) of various peptides and combinations of peptides according to the invention against the fruit fly *Drosophila suzuki* on blueberry plants in field trials conducted by Epa Agricultural Economics. Example

[0416] The invention will now be demonstrated and further described through the following non-limiting examples. General Program

[0417] Unless otherwise stated, all amino acids are in the l-configuration. Standard Fmoc protected amino acids were purchased from CEM Corporation or Pepceuticals. Suppliers of specialty amino acids, and similarly, peptide synthesis resin suppliers, will be noted where appropriate. Peptide-grade DMF was purchased from Rathburn.

[0418] Peptides are synthesized on either the Biotage Initiator+ Alstra microwave-assisted peptide synthesizer or the CEM LibertyPrime microwave-assisted peptide synthesizer, as specified.

[0419] High-resolution mass spectrometry (HRMS) was performed on a Bruker microTOF-Q II (ESI+).

[0420] Peptides were purified using a Phenomenex Gemini, C18, 5 μm, 250 × 21.2 mm column on a reverse-phase Dionex HPLC system equipped with a Dionex P680 pump and a Dionex UVD170U UV-vis detector (monitored at 214 nm and 280 nm). Gradient elution was performed using a solvent consisting of A (H₂O + 0.1% TFA) and B (MeCN + 0.1% TFA), followed by lyophilization of the fractions using a Christ Alpha 2-4 LO plus lyophilizer.

[0421] The purified peptides were analyzed using a Phenomenex (Aeris, 5µm, peptide XB-C18, 150 × 4.6 mm) column on a Shimadzu reversed-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), at a flow rate of 1 mL / min. The RP-HPLC gradient was run using a solvent system consisting of solution A (100% H₂O + 0.1% TFA) and solution B (100% MeCN + 0.1% TFA). Typically, two gradients are used to characterize each peptide: a gradient from 5% to 95% solution B over 20 minutes (with a 2-minute hold at 5% solution B and a 5-minute wash at 95% solution B at the beginning and end of the gradient) and a gradient from 5% to 95% solution B over 50 minutes (with a 5-minute hold at 5% solution B and a 5-minute wash at 95% solution B at the beginning and end of the gradient). In some cases, specialized gradients are used, and these are indicated where appropriate. Analytical RP-HPLC data are reported in column retention times (tR) in minutes (min). The analytical column is maintained at ambient temperature.

[0422] LC-MS analysis was performed on a Thermo Scientific LCQ Fleet quadrupole mass spectrometer with an m / z range of 50–2000 Da and an ESI source coupled to a Dionex Ultimate 3000 LC. Analysis was performed on a Reprosil Gold 120 C18, 3 µm 150 × 4 mm column using a linear gradient from buffer A (95 / 5 H₂O / MeCN, containing 0.1% v / v TFA) to buffer B (95 / 5 MeCN / H₂O, containing 0.1% v / v TFA) over 20 minutes (with a 2-minute hold in 0% solution B and a 5-minute wash in 100% solution B at the start and end of the gradient, respectively). A similar LC-MS gradient was used if a dedicated analytical RP-HPLC gradient was employed to characterize the compounds. Analytical RP-HPLC and LC-MS samples were injected as 25 µL stock solutions containing 0.1% v / v TFA in H2O / MeCN at a concentration of 1 mg / mL. The LC-MS column temperature was maintained at 30°C. High-resolution mass spectrometry (HRMS) analysis of the purified peptides was performed on a Bruker microTOF-Q II (ESI+) spectrometer.

[0423] Proton nuclear magnetic resonance spectra used to calculate peptide content ( 1 H NMR was recorded on 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, d 7.26; CD3OD, d 3.31 and D2O, d 4.79). Peak modes are described using the following abbreviations where appropriate: br = broad peak, s = singlet, d = doublet, t = triplet, q = tetrad, m = multiplet. The coupling constant J is reported in Hertz (Hz). General procedure for automated peptide synthesis Biotage initiator + Alstra synthesizer:

[0424] Fmoc-protected amino acids were prepared in DMF as 0.2 M (0.1 mmol synthesized), 0.5 M (0.2 mmol synthesized), or 0.7 M (0.5 mmol synthesized) solutions. Five equivalents of amino acid (relative to resin loading) were used during coupling cycles. Oxyma and diisopropylcarbodiimide (DIC) were prepared in DMF as 0.2 M (0.1 mmol synthesized), 0.5 M (0.2 mmol synthesized), or 0.7 M (0.5 mmol synthesized) solutions. Five equivalents of Oxyma and five equivalents of DIC (relative to resin loading) were used during coupling cycles. For Fmoc deprotection, a solution of 20% morpholine (containing 5% formic acid) in DMF was used. Except for Fmoc-Cys(Trt)-OH, Fmoc-His(Trt)-OH, and Fmoc-Arg(PBf)-OH, the coupling reactions were carried out at 90°C under microwave heating for 2 minutes. The coupling of Fmoc-Cys(Trt) and Fmoc-His(Trt)-OH was carried out at 50°C for 10 minutes. The coupling of Fmoc-Arg(Pbf)-OH was carried out at 90°C for two consecutive cycles (double coupling) for 2 minutes. Microwave-assisted deprotection of Fmoc was carried out at 90°C for 1 minute. CEM Liberty Blue Synthesizer

[0425] Fmoc-protected amino acids were prepared as 0.2 M NBP (Tamisolve) solutions. Five equivalents of amino acids (relative to resin loading) were used during coupling cycles. 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 resin loading) were used during coupling cycles. For Fmoc deprotection, a 20% pyrrolidine solution was used. Coupling reactions and Fmoc deprotection, except for Fmoc-Cys(Trt)-OH, Fmoc-His(Trt)-OH, and Fmoc-Arg(Pbf)-OH, were carried out under microwave heating at 90°C for 2 min and 1 min, respectively. Coupling of Fmoc-Cys(Trt) and Fmoc-His(Trt)-OH was carried out at 50°C for 5 min. Coupling of Fmoc-Arg(Pbf)-OH was carried out in two consecutive cycles at 75°C for 5 min. General procedure for TFA cleavage of peptides

[0426] Typically, peptide cleavage assays are performed by taking approximately 3 mg of dried resin beads and treating them with TFA / TIS / water (95:2.5:2.5) for 3 hours. The filtrate is drained, concentrated, and then ground in cold diethyl ether (Et2O). The ground material is dissolved in acetonitrile / water and then analyzed by RP-HPLC / LC-MS.

[0427] Peptides are typically cleaved off resin in large quantities by gently shaking the resin in a cleavage mixture of TFA / TIS / H2O (95:2.5:2.5) at room temperature for 3 hours, then draining the resin and blowing off the TFA with a steady stream of N2. Peptides containing cysteine ​​or tryptophan residues are cleaved off the resin for 3 hours using a cleavage mixture of TFA / TIS / H2O / DODT (94:2.5:1:2.5). In all cases, the crude peptides are milled with cold Et2O. Et2O is removed from the resulting crude peptide precipitate under a steady stream of nitrogen. The crude peptides are then redissolved in H2O / MeCN and purified by RP-HPLC. Synthesis of SB-P-86 Chemical structure of SB-P-86 [pyr]-LTFTSSWGG-[NH2] (SEQ ID NO: 55) The specific synthetic route of SB-P-86 is as follows: Figure 19 As shown. Synthesis of SB-P-99

[0428] SB-P-99 was synthesized on a CEM Liberty Blue synthesizer using the same general Fmoc-SPPS procedure described above. An extended 4-min coupling cycle was used for Leu2 and Trp8. Bicoupling steps were used for Thr3, D-Phe4, Ser5, and D-Asp7. 0.1 M OxymaPure was incorporated into the Fmoc deprotected mixture to mitigate the risk of asparagine formation during synthesis.

[0429] Following synthesis, the peptide was simultaneously cleaved with resin and its side chains deprotected in a mixture of 94 : 2.5 : 2.5 : 1 (v / v) TFA : TIS : H2O : DODT at room temperature for 2 h. After RP-HPLC purification, SB-P-99 with a purity of 90% was obtained, with an overall yield of 85%. Synthesis of SB-P-109 and SB-P-110

[0430] The synthesis of SB-P-109 and SB-P-110 was performed on a CEM Liberty Blue synthesizer using the same general Fmoc-SPPS procedure described above. For SB-P-109, a double coupling step was used for Val2, Asn3, Phe4, Thr5, and Thr7. An extended 4-minute coupling step was used for Gln10. For SB-P-110, a double coupling cycle was used for Leu2, Asn3, Phe4, and Ser5. An extended 4-minute coupling step was used for Trp8.

[0431] Following synthesis, the peptide was simultaneously cleaved with resin and deprotected from its side chains in a mixture of 94 : 2.5 : 2.5 : 1 (v / v) TFA : TIS : H2O : DODT at room temperature for 2 h. After grinding in ice-cold Et2O, the crude peptide was purified by semi-preparative RP-HPLC, yielding purities of 92% and 97% and overall yields of 7% and 5%, respectively. The peptide identity was confirmed by LC-MS. 1 H NMR was used to determine the peptide content in the lyophilized powder. Synthesis of SB-P-112

[0432] The synthesis of SB-P-112 was carried out on CEM Liberty Blue using Rink amide ProTide LL resin (f = 0.18 mmol / g). 0.1 M oxime was incorporated into the pyrrolidine deprotection mixture to prevent asparagine formation during synthesis. Extended 4-minute coupling cycles were used for Leu2, Fmoc-(NMe)Asp(OtBu)-OH, and Trp8. Dual coupling cycles were used for Thr3 and Ser5.

[0433] Following synthesis, the peptide was simultaneously cleaved and its side-chain deprotected in a mixture of 94 : 2.5 : 2.5 : 1 (v / v) TFA : TIS : H2O : DODT at room temperature for 2 h. After grinding in ice-cold Et2O, crude SB-P-112 was purified by RP-HPLC and obtained with a purity of 96% and an overall yield of 11%. The peptide identity was confirmed by LC-MS, and the peptide content in the lyophilized powder was determined to be 89% by 1H NMR. Mortality assessment methods Cafe assay – Suzuki's fruit fly

[0434] Based on the following measurement: Capillary feeder measurement of food intake in Drosophila melanogaster - PubMed (nih.gov)

[0435] Five Drosophila Suzukii of the same sex were anesthetized with CO2 and placed in 2.5 cm × 7.5 cm cylindrical plastic vials. The vials were capped with cotton plugs having two holes, each containing a pipette tip to support a capillary tube. Two 5 µl capillary tubes were filled with the treatment solution, weighed on a fine balance, and then placed into the vials through the pipette tips. The vials were placed in an incubator, and the flies were fed for 24 hours. After 24 hours, the capillary tubes were removed and weighed, and the difference between the start and end times was calculated to determine how much food had been consumed. Fresh capillary tubes (weighed and filled) were placed in the experimental area, and this process was repeated until the 96-hour mark. Mortality (the number of dead flies) was counted every 24 hours. The experimental setup is shown in [illustration]. Figure 8 middle.

[0436] The activity data of the unformulated peptide combination according to the present invention against Drosophila suzuki in the Café bioassay are shown in... Figure 69 middle. Leaf dip test – Aphids or diamondback moths

[0437] Based on IRAC sensitivity testing method 019 (https: / / irac-online.org / methods / aphids-adultnymphs / ).

[0438] Pour 1% agar solution into a 4 cm wide and 3 cm high petri dish (ensuring a 1 cm gap between the agar and the lid), and allow it to solidify. Immerse a 2.5 cm leaf disc in 3 ml of the treatment solution, ensuring the solution covers the entire leaf. Allow the leaf disc to dry for 1 hour, then place it on the solidified agar. Place insects (aphids or diamondback moths) on each leaf disc. Seal each unit with a tightly fitting, well-ventilated lid. Place the agar petri dish in a small plastic tray lined with damp paper, ensuring the water tray at the bottom of the incubator is filled with clean water, and place it in the incubator. Assess mortality at 72, 96, and 120 hours. The leaf immersion assay setup is as follows: Figure 9 As shown.

[0439] Results of leaf immersion assays for diamondback moth using peptides and combinations thereof according to the invention are shown below. Figure 11 middle. Further data and discussion Data on spotted winged fruit fly (SWD; fruit fly Suzuki)

[0440] The inventors have observed the superior insecticidal effect of peptide SB-P-39 (a member of the lipid metabolism hormone family) in experiments combining it with pyrogen (PK) peptide SB-P-51. This effect was observed when SB-P-39 and SB-P-51 were administered to SWD at equimolar concentrations via a capillary feeder (CaFe). Peptide SB-P-51 is naturally identical in sequence, and SB-P-39 is considered naturally similar because, although this peptide was engineered to resemble the naturally similar peptide, the palmitoyl group is naturally present. Figure 14 The internal in vivo SWD data is displayed.

[0441] Figure 14 When administered at equimolar concentrations as a combined treatment delivered to the SWD via CaFe assay, peptides SB-P-39 and SB-P-51 exhibited insecticidal activity. n = 115. The mediators were 5% combi-protec, 0.1% Tween-80, 0.5% DMSO, and 8% ACN. The test concentration was 1 × 10⁻⁶. -4 M.

[0442] Field and semi-field trials were conducted at the National Institute of Agricultural Plants (NIAB) site in Kent, England. Equimolar concentrations of SB-P-39 and SB-P-51 induced significant mortality in SWD in different laboratory settings; selection droplet assays ( Figure 15 (Left). NIAB also demonstrated a significant reduction in oocyte count in response to the SB-P-39 and SB-P-51 combination ( Figure 15 ,right).

[0443] Figure 15 Laboratory-based NIAB peptide testing in SWD; recording mortality rate and oocyte count.

[0444] NIAB extended their analysis to a semi-field study to assess larval damage on strawberry plants in plastic greenhouses. This assessment was achieved by storing fruit picked from the experiment after peptide application at 20°C for two days to allow eggs to hatch into larvae. Larval extraction was performed according to the NIAB protocol (fruits were immersed in a sugar solution for 20 min), and the number of larvae was counted. This indicated that the SB-P-39+SB-P-51 treatment reduced larval numbers. Overall, these data are highly encouraging, suggesting that the peptide will significantly reduce SWD damage to fruit. Figure 15 ).

[0445] Figure 16 The study showed a reduction in SWD in the number of larvae in response to the SB-P-39+SB-P-51 treatment under semi-field conditions.

[0446] The inventors have tested the insecticidal activity of SWD as a single agent treatment and in equimolar combinations with other natural identical and natural-like AKH peptides; given the significant effects of combinations of SB-P-39 and SB-P-51 PK with AKH peptides on SWD. Figure 17 As shown, the monotherapy effects of SB-P-41 and SB-P-42 were significantly enhanced by combination administration with PK peptides SB-P-48 and SB-P-49.

[0447] Figure 17 The insecticidal activity of peptides SB-P-41, SB-P-42, SB-P-48, and SB-P-49 is shown when administered as single agents via CaFe assay to SWD and in combination at equimolar concentrations as shown in the figure. The mediators were 5% combi-protec, 0.1% Tween-80, 0.5% DMSO, and 8% ACN. The test concentration was 1 × 10⁻⁶. -4 M. shows the mortality rate over 72 hours. Further field trial data Field trial dataset from Epai Agricultural Economics Company

[0448] In field trials conducted by Epa Agricultural Economics, SB-P-42+49 (combination) and SB-P-39+49 (combination) were used at a rate of 1 x 10 for each peptide. -4 The results of M on the fruit fly Suzuki on strawberries are shown in Figure 70 In a field trial conducted by Epa Agricultural Economics Company, the results of using various combinations of peptides according to the present invention against the fruit fly *Drosophila suzuki* on blueberries are shown in... Figure 71 In a field trial conducted by Collins Agricultural Consultants in the United States, the results of using various combinations of peptides according to the invention against the fruit fly *Drosophila suzuki* on blueberries are shown in the figure. Figure 10 middle. Collins Agricultural Consultants, USA, field trial dataset

[0449] In field trials conducted by Collins Agricultural Consultants in the United States, 1 x 10 -4 Results of the peptide SB-P-86 of M against the diamondback moth (water chestnut borer) on cabbage (cauliflower) are shown in... Figure 12 In a field trial conducted by Collins Agricultural Consultants in the United States, 1 x 10 -4 Results of M's SB-P-86 against the cabbage looper (Brassica napus) on cabbage (cauliflower) are shown in... Figure 13 middle. Diamondback moth data (FERA)

[0450] The results were validated by testing the diamondback moth peptide SB-P-86 with the contract research organization FERA Sciences. The peptide test showed that diamondback moths exhibited a significant induced mortality rate at the 120-hour time point. Figure 18 ). 2 × 10⁻⁶ was used in laboratory spray assays conducted by FERA. -4 Results of M's SB-P-86 application against diamondback moth 7 days later are shown. Figure 68 middle. Lepidoptera Mortality Measurement

[0451] Frontier lepidopteran artificial feed was prepared using 1% agar and then mixed with artificial feed powder. The peptide solution was divided into 10 equal portions, and the feed was poured directly onto them. The final peptide concentration was 1 × 10⁻⁶. -4 M, each peptide was aliquoted into 10 pools. Once the feed coagulated and cooled, one L1 larva was infecting each pool. The trays were heated and sealed, and the larvae were allowed to develop for 168 hours. Finally, pupation and mortality were scored. The Lepidoptera mortality test setup is shown in [image / description]. Figure 20 In this study, SB-P-86 was used to determine lepidopteran mortality rates, and the results were compared with a negative control vector and the insecticide dichlorodiphenyltrichloroethane (DDT). The activity of SB-P-86 was as follows: Figure 21 As shown; unlike broad-spectrum chemical insecticides (such as DDT), SB-P-86 has good activity, is environmentally friendly, and targets specific pests. Other specific combinations The combination of SB-P-42 (AKH) and SB-P-49 (pyrogalpine) Synthesis of SB-P-42 The chemical structure of SB-P-42 is: [Pyr]LTFSPDW-[NH2] (SEQ ID NO: 54)

[0452] The specific synthetic route of SB-P-42 is as follows: Figure 22 As shown. For the synthesis of 0.5 mmol of SB-P-42, a double coupling step was used for 3Thr, 5Ser, 7Asp, and 8Trp. An extended 6-min coupling step was used for 4Phe and 6Pro. Purification was performed at 60°C using a 30 to 50% B gradient over 20 min (monitored at 280 nm). Purity = 93%, Yield = 27%. Synthesis of SB-P-49 The chemical structure of SB-P-49 is: SVPFKPRL-[NH2] (SEQ ID NO: 76).

[0453] The specific synthetic route of SB-P-49 is as follows: Figure 25 As shown. For 1Ser, a prolonged 6-min single coupling cycle was used; for 4Phe, a double coupling cycle was used; and for 7Arg, a 7-min Arg coupling cycle was used. SB-P-49 was synthesized at a scale of 0.5 mmol. Purification was monitored at 254 nm using a 10%–30% B gradient over 20 min at 60°C. Purity = 97%, Yield = 25%. In vivo data / mortality data Cafe assay – Suzuki's fruit fly

[0454] Based on the following assay: Capillary feeder assay for measuring food intake in Drosophila melanogaster - PubMed (nih.gov). This is discussed in this article. Results are as follows. Figure 28 As shown. The combination of SB-P-39 (AKH) and SB-P-51 (pyrogalpine) Synthesis of SB-P-39 The chemical structure of SB-P-39 is: [palmitoyl]-QLTFSPDW-[NH2] (SEQ ID NO: 51).

[0455] The specific synthetic route of SB-P-39 is as follows: Figure 29 As shown. For the synthesis of SB-P-39 at a scale of 0.25 mmol, a double coupling cycle was used for 1Gln and 7Asp. When the synthesis was carried out at a scale of 0.5 mmol, the double coupling step was used for 1Gln, 3Thr, 5Ser, 7Asp, and 8Trp. In addition, a 6-min coupling cycle was used for 4Phe and 6Pro. N-terminal palmitoylation was manually achieved in Tamisolve at room temperature using 4 equivalents of palmitoyl chloride relative to the resin loading and 8 equivalents of DIPEA for 1 h. Purity = 87%, Yield = 41%. Synthesis of SB-P-51 The chemical structure of SB-P-51 is: LRQLQSNGEPAYRVRTPRL-[NH2] (SEQ ID NO: 77)

[0456] The specific synthetic route of SB-P-51 is as follows: Figure 32As shown. For the synthesis of SB-P-51, a double coupling cycle was used for 3Gln and 5Gln. Fmoc-Arg(Pbf)-OH was used at a concentration of 0.12 M, and an extended 7-min Arg coupling cycle was used for all Arg residues. Purification was performed using a 10% to 20% B gradient over 20 min, monitored at 280 nm and 60°C. Purity >99%, yield = 15%. In vivo data / mortality data Cafe assay – Suzuki's fruit fly

[0457] Based on the following assay: Capillary feeder assay for measuring food intake in Drosophila melanogaster - PubMed (nih.gov). This is discussed in this article. Results are as follows. Figure 14 As shown. Bee survival research The oral toxicity test protocol for bees, adapted from OECD test number 247: Bumblebee, Acute Oral Toxicity Test

[0458] The results of a specific combination of SB-P-39 and SB-P-51 are shown in Figure 6 middle. Further experiments Synthesis of SB-P-112

[0459] The specific synthetic route of SB-P-112 is as follows: Figure 35 As shown. The synthesis was performed in batches running at a scale of 5 × 0.5 mmol using Rink amide MBHA resin (f = 0.702 mmol / g) on ​​CEM Liberty Blue with an HT12 loader. The Fmoc-deprotection reaction was carried out at 90°C for 1 min. For all amino acids, coupling cycles were performed in TamiSolve at 90°C for 4 min using 5 equivalents of Fmoc-AA (relative to resin load) and 5 equivalents of DIC / Oxyma Pure (relative to resin load). Dual coupling cycles were used for Thr3, Ser5, and Pro6.

[0460] Following synthesis, the resins from all four runs were combined at room temperature, and then resin cleavage and side-chain deprotection were simultaneously performed in a 94:2.5:2.5:1 (v / v) mixture of TFA:TIS:H2O:DODT for 2 h. After grinding and lyophilization in ice-cold Et2O, the crude peptide was purified by RP-HPLC and its purity was assessed by HPLC and LCMS.

[0461] Purification was performed on a Prodigy system; “SBP112_254nm” method (20-40% B 20 mL / min 254 nm 27 min) tR = collected between 10.4 and 11.6 min; dissolved in 20% MeCN. Characterization was performed as follows. Analytical HPLC standard 35 min gradient tR = 15.3, purity = 90%. LCMS: standard 10 min gradient [M+H]+ = 995.4, MW = 994.4. Overall yield = 0.3 g, 20%. Yield per 0.5 mmol run = 0.1 g. Characterization of SB-P-112 is shown in... Figure 36 and Figure 37 middle. Synthesis of SB-P-138

[0462] The specific synthetic route of SB-P-138 is as follows: Figure 38 As shown. Synthesis was performed on CEM Liberty Blue using Rink amide ProTide resin (f = 0.18 mmol / g). The Fmoc-deprotection reaction was carried out at 90°C for 1 min. For all amino acids except Fmoc-Arg(Pbf)-OH, coupling cycles were performed in TamiSolve at 90°C for 2 min using 5 equivalents of Fmoc-AA (relative to resin loading) and 5 equivalents of DIC / Oxyma Pure (relative to resin loading). Arg coupling cycles were performed at 75°C using two consecutive 5-min coupling steps. The extended 4-min coupling method was used for Leu2, Thr5, and Nal8.

[0463] Following synthesis, resin cleavage and side-chain deprotection were simultaneously performed at room temperature in a mixture of 94 : 2.5 : 2.5 : 1 (v / v) TFA : TIS : H2O : DODT for 2 h. After grinding and lyophilization in ice-cold Et2O, the crude peptide was purified by RP-HPLC and its purity was then assessed by HPLC and LCMS.

[0464] Purification was performed on a Prodigy system; 20%-40% B, 20 mL / min, 254 nm, 30 min, tR = 10.7; dissolved in 20% MeCN. Characterization was performed as follows: Analytical HPLC: Standard 35 min gradient, tR = 15.5, purity = 98%. LCMS: Standard 10 min gradient, [M+H]+ = 1090.4, MW = 1089.5. Yield = 20 mg, 18%. Characterization of SB-P-138 is shown in... Figure 39and Figure 40 middle. Synthesis of SB-P-161

[0465] The specific synthetic route of SB-P-161 is as follows: Figure 41 As shown. The synthesis of SB-P-161 was carried out on a 0.25 mmol scale on Rink amide MBHA resin (loaded 0.702 mmol / g). The Fmoc-deprotection reaction was carried out in a solution of 20% pyrrolidine containing 0.1 M Oxyma Pure in TamiSolve at 90°C for 1 min. The coupling reaction was carried out in TamiSolve at 90°C for 2 min using 5 equivalents of Fmoc-AA (relative to resin load) and 5 equivalents of DIC / Oxyma Pure (relative to resin load). Except for 2Val, 3Asn, 4Phe, and 5Ser, which were coupled using a 4 min method, all amino acids were coupled using a single coupling method.

[0466] Peptide cleavage and overall deprotection were performed at room temperature using a mixture of 94 : 2.5 : 2.5 : 1 (v / v) TFA : TIS : H2O : DODT for 2 h. After grinding in ice-cold Et2O, the crude product was lyophilized. The peptide identity was confirmed by LC-MS and purified by RP-HPLC.

[0467] Purification: 10% to 30% B over 20 min, 280 nm; dissolved in 10 mL 10% B + 1 mL DMSO, 5 mL 10% B (for remaining powder); retention time 16.5 min. Characterization showed purity = 90.2%, yield = 114.1 mg, 42.5%. Characterization of SB-P-161 is shown in... Figure 42 and Figure 43 middle. Synthesis of SB-P-179

[0468] The specific synthetic route of SB-P-179 is as follows: Figure 44As shown. The synthesis of SB-P-179 was carried out on a 0.1 mmol scale on Rink amide MBHA resin (loaded 0.702 mmol / g). The Fmoc-deprotection reaction was carried out at 90°C for 1 min in a solution of 20% pyrrolidine in TamiSolve. The coupling reaction was carried out in TamiSolve at 90°C for 2 min using 5 equivalents of Fmoc-AA (relative to resin load) and 5 equivalents of DIC / Oxyma Pure (relative to resin load). A 4 min single coupling method was used for 2Leu and 5Ser, and a double coupling was performed for 3Asn and 4Phe.

[0469] Peptide cleavage and overall deprotection were performed at room temperature using a mixture of 94 : 2.5 : 2.5 : 1 (v / v) TFA : TIS : H2O : DODT for 2 h. After grinding in ice-cold Et2O, the crude product was lyophilized. The peptide identity was confirmed by LC-MS, indicating successful synthesis. Therefore, the crude product was purified by RP-HPLC, and its purity was assessed by RP-HPLC.

[0470] Purification: 10% to 30% B over 20 min, 280 nm; retention time 17.7 min. Characterization showed purity = 92.9%, yield = 33.9 mg, 31.3%. Characterization of SB-P-179 is shown in... Figure 45 and Figure 46 middle. Synthesis of SB-P-190

[0471] The specific synthetic route of SB-P-190 is as follows: Figure 47 As shown. Synthesis was performed on CEM Liberty Blue using Fmoc-2-ClTrt-Cl resin (f = 0.53 mmol / g). The Fmoc-deprotection reaction was carried out at 90°C for 1 min. For all amino acids except Fmoc-Arg(Pbf)-OH, coupling cycles were performed at 90°C for 2 min in TamiSolve using 5 equivalents of Fmoc-AA (relative to resin loading) and 5 equivalents of DIC / Oxyma Pure (relative to resin loading). Arg coupling cycles were performed using two consecutive 5-min coupling steps at 75°C. The double coupling step was used for Thr3, Ser5, Asp7, and Trp8. The extended 4-min coupling method was used for Pyr1, Leu2, Phe4, and Pro6.

[0472] Following synthesis, resin cleavage and side-chain deprotection were simultaneously performed at room temperature in a mixture of 94 : 2.5 : 2.5 : 1 (v / v) TFA : TIS : H2O : DODT for 2 h. After grinding and lyophilization in ice-cold Et2O, the crude peptide was purified by RP-HPLC and its purity was then assessed by HPLC and LCMS.

[0473] Purification was performed on a Prodigy system; 15-35% B at 240 nm for 30 min, method tR = 13.7 min; dissolved in 15% MeCN. Characterization showed purity => 99%, yield = 16.6 mg, 17%. Characterization of SB-P-190 is shown in... Figure 48 and Figure 49 middle. Synthesis of SB-P-207 The specific synthetic route of SB-P-207 is as follows: Figure 50 As shown. The synthesis of SB-P-207 (fall armyworm AKH) was carried out on a 0.25 mmol scale on Rink amide MBHA resin (loaded 0.702 mmol / g). The Fmoc-deprotection reaction was carried out at 90°C for 1 min in a solution of 20% pyrrolidine containing 0.1 M Oxyma Pure in TamiSolve. The coupling reaction was carried out in TamiSolve at 90°C for 2 min using 5 equivalents of Fmoc-AA (relative to resin load) and 5 equivalents of DIC / Oxyma Pure (relative to resin load). All amino acids were coupled using a single coupling method except for 2Leu, 3Thr, 4Phe, 5Ser, and 10Asn, which were bicoupled. 6Ser was coupled using a 4 min method.

[0474] Peptide cleavage and overall deprotection were performed at room temperature using a mixture of 94 : 2.5 : 2.5 : 1 (v / v) TFA : TIS : H2O : DODT for 2 h. After grinding in ice-cold Et2O, the crude product was lyophilized. The peptide identity was confirmed by LC-MS and purified by RP-HPLC.

[0475] Purification was performed on a Prodigy system; 20%-30% B, 20 mL / min, 254 nm, 30 min, tR = 9.3; dissolved in 20% MeCN. Characterization was performed as follows: Analytical HPLC: Standard 35 min gradient, tR = 14.0, purity = 94%. LCMS: Standard 10 min gradient, [M+H]+ = 1079.4, MW = 1078.2. Yield = 13 mg, 12%. Characterization of SB-P-207 is shown in... Figure 51 and Figure 52 middle. Synthesis of SB-P-208

[0476] The specific synthetic route of SB-P-208 is as follows: Figure 53 As shown. Synthesis was performed on CEM Liberty Blue using Rink amide ProTide resin (f = 0.18 mmol / g). The Fmoc-deprotection reaction was carried out at 90°C for 1 min. For all amino acids except Fmoc-Arg(Pbf)-OH, coupling cycles were performed in TamiSolve at 90°C for 2 min using 5 equivalents of Fmoc-AA (relative to resin loading) and 5 equivalents of DIC / Oxyma Pure (relative to resin loading). Arg coupling cycles were performed at 75°C using two consecutive 5 min coupling steps.

[0477] The double coupling cycle was used for Leu2, Phe4, Ser5, and Gly7, and the extended 2 × 4 min double coupling method was used for Thr3.

[0478] Purification was performed on a Prodigy system; 20%-40% B, 20 mL / min, 254 nm, 30 min, tR = 9.1; dissolved in 20% MeCN. Characterization was performed as follows: Analytical HPLC: Standard 35 min gradient, tR = 14.8, purity > 99%. LCMS: Standard 10 min gradient, [M+H]+ = 907.4, MW = 906.4. Yield = 22 mg, 25%. Characterization of SB-P-208 is shown in... Figure 54 and Figure 55 middle. Synthesis of SB-P-209

[0479] The specific synthetic route of SB-P-209 is as follows: Figure 56As shown. Purification was performed on a Prodigy system; 20%–40% B, 20 mL / min, 254 nm, 30 min, tR = 10.2; dissolved in 20% MeCN. Characterization showed purity = 98.4%, yield = 16.1 mg, 16.5%. Characterization of SB-P-209 is shown in... Figure 57 and Figure 58 middle. Synthesis of SB-P-233

[0480] The specific synthetic route of SB-P-233 is as follows: Figure 59 As shown. Purification was performed on a Prodigy system; 20%-40% B 20 mL / min 254 nm 20 min tR = 9.2; dissolved in 20% MeCN. Characterization was performed as follows. Analytical HPLC: Standard 35 min gradient tR = 14.7, purity => 99%. LCMS: Standard 10 min gradient [M+H]+ = 1066.4, MW = 1065.5. Yield = 2 mg, 2%. Characterization of SB-P-233 is shown in... Figure 60 and Figure 61 middle. Field simulation stability of plant growth

[0481] Peptide stock solutions were prepared into 1 mg / mL ddH2O solutions in Eppendorf tubes and placed in an EvoGro cabinet. Samples were taken for analysis at 48 h, 72 h, 1 week, and 2 weeks. For each sample, 250 µL was taken. Five drops of MeCN + 0.1% formic acid were added to this solution, and the samples were analyzed by LCMS and HPLC.

[0482] The field stability results of SB-P-42 are shown in Figure 62 The field stability results of SB-P-112 are shown in... Figure 63 middle. UV drying lamp stability

[0483] The peptide stock solution was prepared into a 1 mg / mL ddH2O solution in Eppendorf tubes and placed in a UV drying chamber. The temperature was recorded throughout the process using a thermometer and remained stable at 40°C. Samples were taken for analysis at 0 h, 24 h, 48 h, and 72 h. For each sample, 250 µL was taken. Five drops of MeCN + 0.1% formic acid were added to this solution, and the samples were analyzed by LCMS and HPLC.

[0484] The UV drying lamp stability results for SB-P-42 are shown in... Figure 64 The UV drying lamp stability results for SB-P-112 are shown in the figure. Figure 65 middle. 54°C stability

[0485] The peptide stock solution was prepared into a 1 mg / mL ddH2O solution in Eppendorf tubes and placed in a ThermoBlock set to 54°C. The temperature was recorded throughout the process using a thermometer. Samples were taken for analysis at 0 h, 48 h, 168 h, and 336 h. For each sample, 250 µL was taken. Five drops of MeCN + 0.1% formic acid were added to this solution, and the sample was analyzed by LCMS and HPLC.

[0486] The stability results of SB-P-42 at 54°C are shown in the figure. Figure 66 The stability results of SB-P-112 at 54°C are shown in the figure. Figure 67 middle. References

[0487] To more fully describe and disclose this invention and the prior art to which it pertains, numerous publications have been cited. Full citations of these references are provided below. The entire contents of each of these references are incorporated herein by reference. ○Koyama T, Terhzaz S, Naseem MT, Nagy S, Rewitz K, Dow JAT, DaviesSA, Halberg KV. A nutrient-responsive hormonal circuit mediates an inter-tissue program regulating metabolic homeostasis in adult Drosophila. NatCommun.2021 ○Gäde G, Auerswald LGen Comp Endocrinol. 2003 Jun 1;132(1):10-20.doi: 10.1016 / s0016-6480(03)00159-x ○Yeoh JGC, Pandit AA, Zandawala M, Nässel DR, Davies SA, Dow JAT.DINeR: Database for Insect Neuropeptide Research. Insect Biochem Mol Biol.2017 ○Ahn SJ, Corcoran JA, Vander Meer RK, Choi MY. Identification andCharacterization of GPCRs for Pyrokinin and CAPA Peptides in the BrownMarmorated Stink Bug, Halyomorpha halys (Hemiptera: Pentatomidae). FrontPhysiol.2020 ○Audsley N and Down RE, G protein coupled receptors as targets fornext generation pesticides. Insect Biochem Molec 67: 27-37 (2015). ○Halberg KA, Terhzaz S, Cabrero P, Davies SA and Dow JAT, Tracingthe evolutionary origins of insect renal function. Nat Commun 6 (2015). ○Terhzaz S, Teets NM, Cabrero P, Henderson L, Ritchie MG, NachmanRJ, Dow JAT, Denlinger DL and Davies SA, Insect capa neuropeptides impactdesiccation and cold tolerance. Proc Natl Acad Sci 201501518 (2015). ○Terhzaz S, Alford L, Yeoh JGC, Marley R, Dornan AT, Dow JAT andDavies SA, Renal neuroendocrine control of desiccation and cold tolerance byDrosophila suzukii. Pest Manag Sci 74: 800-810 (2017). ○Predel R, Wegener C, Biology of the CAPA peptides in insects. CellMol Life Sci 63: 2477-2490 (2006). ○Lamango NS, Nachman RJ, Hayes TK, Strey A and Isaac RE, Hydrolysisof insect neuropeptides by an angiotensin converting enzyme from thehousefly, M. domestica. Peptides 18: 47-52 (1997). ○Terhzaz S, Cabrero P, Robben JH, Radford JC, Hudson BD, Milligan G,Dow JA and Davies SA, Mechanism and function of Drosophila capa GPCR: adesiccation stress-responsive receptor with functional homology to humanneuromedinU receptor. PLoS One 7(1): e29897 (2012). ○IRAC susceptibility test method 019 ( https: / / irac-online.org / methods / aphids-adultnymphs / ). ○For standard molecular biology techniques, see Sambrook, J.,Russel, D.W.Molecular Cloning, A Laboratory Manual.3 ed. 2001, Cold SpringHarbor, New York: Cold Spring Harbor Laboratory Press。

Claims

1. An insecticidal compound having the following formula (I), or a salt or solvate thereof: R 1 -L 1 -Y 1 -Y-Z-Y 2 -R 2 (I) in: R 1 It is hydrogen (which can be named "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, (poly)alkylene glycol, heterocyclic group, phosphate group or sulfate group; Where R 1a R 1b R 1c R 1d and R 1e Each is independently selected from hydrogen or C. 1-4 Alkyl groups (e.g., methyl, ethyl, propyl, butyl). And any alkyl, formyl, acyl, fatty acyl, benzyl, benzoyl, heteroaryl, trifluoroacetyl, -NHC 1-18 Alkyl, -NHC 6-16 Aryl, -NH-C 1-6 Alkyl-C 6-10 The aryl, (poly)alkylene glycol, or heterocyclic group may optionally be substituted by one or more groups selected from the following: halogen, oxo, C 1-6 Alkyl, C 1-6 Halogenated alkyl group, sugar moiety, phosphate group or sulfate group; L 1 It does not exist or: –(C=O)C 1-16 -alkylene-NH-, where Indicates Y 1 Attachment points of Y or Z; (C 1-20 )alkylene; (C 2-20 ) imidene group; (poly)alkylene glycols; Where L 1 Optionally substituted by one or more groups selected from the following: oxo (=O), halogen, cyano, =NR 1a NR 1a R 1b OR 1a S = S; where R 1a and R 1b Each is independently hydrogen or C 1-2 alkyl; Y 1 Peptides that either do not exist or contain one or two amino acids; Y is a peptide containing 1 to 12 amino acids; wherein Y optionally contains a (poly)alkylene glycol linker in the peptide sequence; Y 2 Peptides that either do not exist or contain one or two amino acids; Z is a peptide according to formula (Zi). WITH 1 -WITH 2 -F # -WITH 4 -WITH 5 -WITH 6 -IN # -WITH 8 -WITH 9 (Zi) in: Z 1 Does not exist or selected from L # I # or V # ; Z 2 Selected from T # or N # ; Z 4 Selected from S # or T # ; Z 5 Selected from P # R # S # or T # ; Z 6 Selected from D # S # N # T # or G # ; Z 8 Does not exist or selected from G # or T # ; Z 9 Does not exist or selected from G # N # Q # or T # ; in" # This indicates that the residue is independently an unmodified amino acid, a modified amino acid, or a non-natural amino acid analogue listed; and R 2 It is NH2, NR 2a H, NR 2a R 2b OH or OR 2a ;where R 2a and R 2b If they exist, they are each independently C. 1-6 -alkyl (e.g., methyl, ethyl, propyl, butyl, pentyl, or hexyl), C 3-6 -Alkenyl, C 6-16- Aryl, C 6-16- Aryl-C 1-6 -alkyl, C 1-6 -alkylene-C 6-16 -Aryl or C 1-6 - Haloalkyl groups, each of which may optionally be substituted by one or more groups selected from: halogen, C 1-6 -alkyl or C 1-6- Halogenated alkyl groups.

2. The insecticidal compound of claim 1, wherein Y is absent or residue Q is absent. # ; in" # "" indicates that the residue is a naturally occurring amino acid, a modified amino acid, or a non-natural amino acid analogue.

3. The insecticidal compound of claim 1 or 2, wherein Y is absent or is residue Q.

4. The insecticidal compound as described in any of the preceding claims, wherein Y 1 and Y 2 It does not exist.

5. The insecticidal compound as claimed in any of the preceding claims, wherein Z is a peptide having the formula (Z-ia) or (Z-ib): Z 1 -T # -F # -Z 4 -Z 5 -Z 6 -W # -Z 8 -Z 9 (Z-ia) Z 1 -N # -F # -Z 4 -Z 5 -Z 6 -W # -Z 8 -Z 9 (Z-ib) Z 1 Z 4 Z 5 Z 6 Z 8 and Z 9 As defined in claim 1; in" # "" indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs.

6. The insecticidal compound as claimed in any of the preceding claims, wherein: Y is Q or does not exist. Z 1 Is it L or I? # Z 2 Selected from T # or N # Z 4 Selected from S # or T # Z 5 Selected from P # R # S # or T # ; Z 6 Selected from D # S # N # or G # ; Z 8 and Z 9 Neither exists or: Z 8 Selected from T # or G # ; Z 9 Does not exist or selected from G # N # or T # ; in" # "" indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs; Optional, of which Z 1 Is it L or I? # Z 2 Selected from T # or N # Z 4 Selected from S # or T # Z 5 Selected from P # R # or S # ; Z 6 Selected from D # or S # ; Z 8 and Z 9 Neither exists or: Z 8 Selected from T # or G # ; Z 9 It is G # or N # ; in" # "" indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs; Further, optionally, wherein: Z 1 It is L # Z 2 It is T # Z 4 Selected from S # or T # ; Z 5 Selected from P # or S # ; Z 6 Selected from D # or S # ; Z 8 and Z 9 None of them exist in" # "" indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs.

7. The insecticidal compound according to any one of claims 1 to 4, wherein Z is a peptide having a formula selected from: L # -T # -F # -S # -P # -D # -W # (Z A )(SEQ ID NO: 1) L # -T # -F # -T # -S # -S # -W # -G # -G # (Z B )(SEQ ID NO: 2) L # -T # -F # -T # -P # -N # -W # (Z C )(SEQ ID NO: 3) I # -T # -F # -S # -R # -D # -W # -T # -G # (Z D )(SEQ ID NO: 4) T # -F # -S # -R # -D # -W # -T # -G # (Z E )(SEQ ID NO: 5) V # -N # -F # -T # -P # -T # -W # -G # -Q # (Z F )(SEQ ID NO: 6) L # -N # -F # -S # -P # -G # -W # (Z G )(SEQ ID NO: 7) L # -T # -F # -T # -S # -S # -W # -G # (Z H ) (SEQ ID NO: 8) or L # -N # -F # -S # -T # -G # -W # (Z O )(SEQ ID NO: 87) in" # "" indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs; Optionally, any one of Z is a peptide having a formula selected from the following: L # -T-F # -S-P # -D # -W(Z A1 )(SEQ ID NO: 15) L # -T-F # -T-S # -S # -W-G-G(Z B1 )(SEQ ID NO: 16) L # -T-F # -T-P # -N # -W(Z C1 )(SEQ ID NO: 17) I # -T-F # -S-R # -D # -W-T-G(Z D1 )(SEQ ID NO: 18) T # -F-S # -R-D # -W-T-G(Z E1 )(SEQ ID NO: 19) V # -N-F # -T-P # -T # -W-G-Q(Z F1 )(SEQ ID NO: 20) L # -N-F # -S-P # -G # -W(Z G1 )(SEQ ID NO: 21) L # -T-F # -T-S # -S # -W-G(Z H1 ) (SEQ ID NO: 22) or L # -N-F # -S-T # -G # -W(Z O1 )(SEQ ID NO: 88) in" # "" indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs.

8. The insecticidal compound as claimed in any of the preceding claims, wherein Z is a peptide having a formula selected from: L # -T # -F # -S # -P # -D # -W # (Z A )(SEQ ID NO: 1) L # -T # -F # -T # -S # -S # -W # -G # -G # (Z B )(SEQ ID NO: 2) I # -T # -F # -S # -R # -D # -W # -T # -G # (Z D )(SEQ ID NO: 4) Optionally, Z is a peptide having the following formula: (Z A1 ) L # -T-F # -S-P # -D # -W(Z A1 )(SEQ ID NO: 15) L # -T-F # -T-S # -S # -W-G-G(Z B1 ) (SEQ ID NO: 16) or I # -T-F # -S-R # -D # -W-T-G(Z D1 )(SEQ ID NO: 18) in" # "" indicates that the listed residues are independently unmodified amino acids, modified amino acids, or non-natural amino acid analogs.

9. The insecticidal compound as claimed in any of the preceding claims, wherein at least one of the residues in peptides Y and Z is a modified amino acid or a non-natural amino acid analog; optionally, wherein at least one of peptides Y and Z is: iN-methylated amino acids; ii. Non-protein amino acids, such as hydroxyproline (Hyp: L-hydroxyproline or (2S,4R)-4-hydroxyproline), octahydroindole-2-carboxylic acid (Oic), sarcosine (Sar), oroleucine (Nle), α-aminoisobutyric acid (Aib), thienylalanine (Thi) or thiazolidin-4-carboxylic acid (Thz), phenylglycine (Phg), γ-aminobutyric acid (gaba) or naphthylalanine (Nal); iii. D-amino acids iv. β-amino acids v. Peptide-like amino acid analogs; vi. Amino acids modified by sugars; or vii. Biotin-modified amino acids; Optionally, at least one of the residues in peptides Y and Z is: vN-methylated amino acids; vi. Peptide-like amino acid analogs; vii. Non-protein amino acids, selected from hydroxyproline (Hyp: L-hydroxyproline or (2S,4R)-4-hydroxyproline), octahydroindole-2-carboxylic acid (Oic), sarcosine (Sar), oroleucine (Nle), α-aminoisobutyric acid (Aib), thiophene alanine (Thi), thiazolidin-4-carboxylic acid (Thz), or naphthyl alanine (Nal). viii. D-amino acids; Further, optionally, at least one of the residues in peptides Y and Z is: iN-methylated amino acids; ii. Peptide-like amino acid analogs; iii. Non-protein amino acids selected from hydroxyproline (Hyp: L-hydroxyproline or (2S,4R)-4-hydroxyproline), octahydroindole-2-carboxylic acid (Oic), sarcosine (Sar), ortholeucine (Nle), α-aminoisobutyric acid (Aib), thienylalanine (Thi), and thiazolidin-4-carboxylic acid (Thz). iv. D-amino acids.

10. The insecticidal compound as claimed in any of the preceding claims, wherein at least one of the residues in peptides Y and Z is: iN-methylated amino acids; ii. Thiophene-alanine (Thi) iii. Thiazolidine-4-carboxylic acid (Thz); iv. Naphthylalanine (Nal); or vD-amino acids; Optionally, at least one of the residues in peptides Y and Z is: iN-methylated amino acids; ii. Thiophene-alanine (Thi) iii. Thiazolidine-4-carboxylic acid (Thz); or iv. D-amino acids.

11. The insecticidal compound as claimed in any of the preceding claims, wherein 1 to 6 residues in the peptide moiety YZ are modified amino acids or non-natural amino acid analogs; Optionally, one to five residues in the peptide portion YZ contain modified amino acids or non-natural amino acid analogs; Optionally, one to four residues in the peptide portion YZ contain modified amino acids or non-natural amino acid analogs.

12. The insecticidal compound as claimed in any of the preceding claims, wherein the Z portion has a formula selected from: LTFSPDW (SEQ ID NO: 27); [n-me-L]TFSPDW (SEQ ID NO: 28); LT[n-me-F]SPDW (SEQ ID NO: 29); LTFTSSWGG (SEQ ID NO: 30); LTFTPNW (SEQ ID NO: 32); ITFSRDWTG (SEQ ID NO: 33); LNFSTGW (SEQ ID NO: 34); LT[f]S-[Thz]-dW (SEQ ID NO: 35); TFSRDWTG (SEQ ID NO: 36); VNFTPTWGQ (SEQ ID NO: 37); LNFSPGW (SEQ ID NO: 38); LT-[Thi]-SP-[N-Me-D]-W (SEQ ID NO: 39); LTFT-[n-me-S]-[n-me-S]-WGG (SEQ ID NO: 40); LN[Thi][n-me-S]PGW (SEQ ID NO: 46); LTFT[N-Me-Ser]S[Nal]GG (SEQ ID NO: 47); LTFT[N-Me-Ser][s][Nal]GG (SEQ ID NO: 105) VNFSPGWGT (SEQ ID NO: 44); LNFSPGWG (SEQ ID NO: 45); LTFTSSWG (SEQ ID NO: 31); LTFSSGWGN (SEQ ID NO: 41); LTFSSGW (SEQ ID NO: 42); or VNFSPNW (SEQ ID NO: 43); Optionally, the Z portion has a formula selected from the following: LTFSPDW (SEQ ID NO: 27); LTFTSSWGG (SEQ ID NO: 30); ITFSRDWTG (SEQ ID NO: 33).

13. The insecticidal compound as claimed in any of the preceding claims, wherein R 1 Selected from: (i)Hydrogen; (ii) An acyl group optionally substituted with the following: sugar moiety; (iii) fatty acyl group; (iv) heteroaryl; (v)-NHC 6-16 Aryl; (vi) Sugar portion; (vii) Biotin; (viii) 5- or 6-membered heterocyclic groups; or (ix) has the formula –(OCH2CH2) n -R p (poly)ethylene glycol, in which Indicates with L 1 The attachment point of Y or Z, where n is an integer from 1 to 16, and R p Selected from -NH2, -OH, or -OMe; And any acyl, fatty acyl, benzyl, benzoyl, heteroaryl, -NHC 6-16 The aryl, (poly)alkylene glycol, or heterocyclic group may optionally be a substituted group that is optionally replaced by one or more groups selected from: halogen, oxo, C 1-3 Alkyl or C 1-3 Halogenated alkyl Optionally, where R 1 Selected from: hydrogen; The acyl group may be optionally substituted with the following: sugar moiety, wherein the acyl group is selected from formyl, acetyl (Ac), propionyl, butyryl; Selected from the following fatty acyl groups: palmitoyl, butyryl, waxyl, decyl, dodecanoyl, dodecanoyl, tunganoyl, heptayl, hexanoyl, eicosanoyl, eicosanoyl, lipolytyl, myristyl, nonanoyl, octadecanoyl, octanoyl, palmitoyl, stearoyl, undecanoyl, and pentanoyl; Indole, such as 3-indole: ; -NHC 6-16 Aryl; Monosaccharide or disaccharide portion; Biotin; 5-6 membered heterocyclic groups, such as pyrrolidone-2-one: ;or Having a style –(OCH2CH2) n -R p (poly)ethylene glycol, in which Indicates with L 1 The attachment point of Y or Z, where n is an integer from 4 to 12, and R p Selected from -NH2, -OH or -OMe And any acyl, fatty acyl, benzyl, benzoyl, heteroaryl, -NHC 6-16 The aryl, (poly)alkylene glycol, or heterocyclic group may optionally be a substituted group that is optionally replaced by one or more groups selected from: halogen, oxo, C 1-3 Alkyl or C 1-3 Halogenated alkyl groups.

14. The insecticidal compound as claimed in any of the preceding claims, wherein R 1 Selected from: hydrogen; The acetyl group may be optionally replaced by either a monosaccharide or a disaccharide moiety; pyrrolidone-2-one, for example ; Palmitoyl; or Having a style –(OCH2CH2) n -NH2 in (poly)ethylene glycol, wherein Indicates Y 1 The attachment point of Y or Z, and n is an integer from 6 to 10; Optionally, where R 1 Selected from: hydrogen; pyrrolidone-2-one, for example ; Palmitoyl; or Having a style –(OCH2CH2)8-NH2 in (poly)ethylene glycol, wherein Indicates Y 1 Attachment points of Y or Z.

15. The insecticidal compound as claimed in any one of the preceding claims, wherein L 1 It does not exist or: –(C=O)C 1-12 -alkylene-NH-, –(C=O)-C 1-10 Alkylene-(C=O)- –(C=O)-C 0-10 Alkylene; C 1-10 alkylene; or -(C=O)-; in Indicates Y 1 Attachment points of Y or Z; Any of L 1 The group may optionally be replaced by one or more oxo (=O) groups; L can be selected from 1 It does not exist or: –(C=O)C 4-12 -alkylene-NH-, –(C=O)-C 1-4 Alkylene-(C=O)- –(C=O)-C 1-4 Alkylene; C 1-4 alkylene; or -(C=O)-; Any of L 1 The group may optionally be replaced by one or more oxo (=O) groups; in Indicates Y 1 Attachment points of Y or Z; Further, in any of the L 1 It does not exist or: ; ; ; ;or ; in Indicates Y 1 Attachment points of Y or Z.

16. The insecticidal compound as claimed in any one of the preceding claims, wherein R 2 It is NH2 or OH.

17. The compound of claim 1, or a salt or solvate thereof, wherein the compound, or a salt or solvate thereof, is selected from: [pyr]QLTFSPDW-[NH2] (SEQ ID NO: 48); [pyr][n-me-L]TFSPDW-[NH2] (SEQ ID NO: 49); [pyr]LT[n-me-F]SPDW-[NH2] (SEQ ID NO: 50); [palm]-QLTFSPDW-[NH2] (SEQ ID NO: 51); [peg8]-QLTFSPDW-[NH2] (SEQ ID NO: 52); Hy-QLTFSPDW-[NH2] (SEQ ID NO: 53); [pyr]-LTFSPDW-[NH2] (SEQ ID NO: 54); [pyr]-LTFTSSWGG-[NH2] (SEQ ID NO: 55); [pyr]-LTFTPNW-[NH2] (SEQ ID NO: 56); [pyr]-ITFSRDWTG-[NH2] (SEQ ID NO: 57); [pyr]-LT[f]S-[Thz]-[d]W-[NH2] (SEQ ID NO: 58); [pyr]-TFSRDWTG-[NH2] (SEQ ID NO: 59); [pyr]-VNFTPTWGQ-[NH2] (SEQ ID NO: 60); [pyr]-LNFSPGW-[NH2] (SEQ ID NO: 61); [pyr]-LT-[Thi]-SP-[N-me-D]-W-[NH2] (SEQ ID NO: 62); [pyr]-LTFT[n-me-S][n-me-S]WGG-[NH2] (SEQ ID NO: 63); [pyr]-LN[Thi][n-me-S]PGW-[NH2] (SEQ ID NO: 64); [pyr]-LTFT[N-Me-Ser][s][Nal]GG-[NH2] (SEQ ID NO: 65); [pyr]LNFSPGWGP-[NH2] (SEQ ID NO: 66); [pyr]LTFTSSWG-[NH2] (SEQ ID NO: 67); [pyr]LTFSSGWGN-[NH2] (SEQ ID NO: 68); [pyr]LTFSSGW-[NH2] (SEQ ID NO: 69); [pyr]VNFSPNW-[NH2] (SEQ ID NO: 70); [pyr]VNFSPGWGT-[NH2] (SEQ ID NO: 71); [pyr]-LTFSPDW-[OH] (SEQ ID NO: 72); [pyr]-LTFTSSWGG-[OH] (SEQ ID NO: 73); or [pyr]-LTFT[N-Me-Ser]S[Nal]GG-[NH2] (SEQ ID NO: 65).

18. A composition, such as an insect control composition or a plant protection composition, comprising a compound as described in any one of claims 1 to 17 mixed with one or more solvents, carriers, diluents, adjuvants, preservatives, dispersants, emulsifiers or synergists; optionally wherein the composition is an aqueous composition.

19. The composition of claim 18, further comprising one or more of kinin, additional AKH peptide, DH31 peptide, DH44 peptide, pyrogalin, or CAPA peptide (e.g., CAPA-1, CAPA-2, or CAPA-3 analogs).

20. The use of the compound as claimed in any one of claims 1 to 17 or the composition as claimed in claim 18 or 19 for any of the following purposes: i) Insect control agents; or ii) Plant protectants used to protect plants or parts thereof from insects; These insects are, by choice: a) Diptera insects, preferably selected from: Drosophila melanogaster or Drosophila suzuki; b) Hemiptera insects, such as aphids, preferably selected from: beet aphid, pea aphid, peach aphid, cotton leafhopper, blackcurrant long-tubed aphid or cereal constrictor aphid; c) Lepidoptera insects, preferably selected from: diamondback moth, striped armyworm or fall armyworm; d) Coleoptera insects; and / or e) Blattodea insects, preferably of which the German cockroach is; Further, optionally, these insects are: a) Diptera insects, preferably selected from: Drosophila melanogaster or Drosophila suzuki; b) Hemiptera insects, such as aphids, preferably selected from: beet aphids, pea aphids, peach aphids, cotton leafhoppers, blackcurrant long-tubed aphids, or cereal constrictor aphids; and / or c) Lepidoptera insects, preferably selected from diamondback moth, fall armyworm or tussock moth.

21. A method for increasing insect mortality, the method comprising contacting insects or insect colonies with a compound as described in any one of claims 1 to 17 or a composition as described in claim 18 or 19.

22. A method for inhibiting or preventing insect infestation of a plant, the method comprising contacting the plant or a portion thereof, or the location where the plant is growing or is intended to grow, with a compound as described in any one of claims 1 to 17 or a composition as described in claim 18 or 19; Optionally, the compound or composition may be brought into contact with the plant or its parts, or the location where the plant is growing or is intended to grow, when there are no or substantially no insects in the plant or its parts.

23. A method for reducing or treating insect infestation of plants or reducing insect load on plants, the method comprising contacting the plant or a portion thereof, or the location where the plant is growing, with a compound as described in any one of claims 1 to 17 or a composition as described in claim 18 or 19.

24. The method of any one of claims 21 to 23, wherein one or more of the following are applicable: a) The location where the plant is growing or is expected to grow may include an agricultural location suitable for growing plants, preferably including a field; b) Contact with the insect or insect colony, plant or part thereof, or location includes treating the insect or insect colony, plant or part thereof, or location with the compound or composition by: irrigation, feeding, spraying, misting, foaming, fogging, hydroponics, hydroponics, coating, immersion and / or coating; and / or c) Contacting the insect or insect colony, plant or part thereof, or location with an effective concentration of the compound, preferably at 10 -3 M to 10 -9 The concentrations between M.

25. The method of any one of claims 21 to 24, wherein the insects are: a) Diptera insects, preferably selected from: Drosophila melanogaster or Drosophila suzuki; b) Hemiptera insects, such as aphids, preferably selected from: beet aphid, pea aphid, peach aphid, cotton leafhopper, blackcurrant long-tubed aphid or cereal constrictor aphid; c) Lepidoptera insects, preferably selected from: diamondback moth, striped armyworm or fall armyworm; d) Coleoptera insects; and / or e) Blattodea insects, preferably of which the German cockroach is; These insects are, by choice: a) Diptera insects, preferably selected from: Drosophila melanogaster or Drosophila suzuki; b) Hemiptera insects, such as aphids, preferably selected from: beet aphids, pea aphids, peach aphids, cotton leafhoppers, blackcurrant long-tubed aphids, or cereal constrictor aphids; and / or c) Lepidoptera insects, preferably selected from diamondback moth, fall armyworm or tussock moth.