insect neuropeptide 3

Abstract

The present invention relates to natural or natural-like analogs of the insect pyroglutamic peptide [Hy]-NADEDQQQSVDFTPRL-[NH2] (SEQ ID NO: 2) having activity against insects, such as Hemipteran, Dipteran, Lepidopteran, Blattodean and / or Coleopteran insects, such as aphids, moths and fruit flies, and the use of these natural or natural-like analogs as insect control agents (e.g., insecticides) and plant protectants.

Description

Technical Field

[0001] This invention relates to natural or natural-like analogues of insect pyrogenic peptides having activity against insects (e.g., Hemiptera, Diptera, Lepidoptera, Blattodea and / or Coleoptera, such as aphids, moths and fruit flies), and their use as insect control agents (e.g. insecticides) 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] Artificial attempts have been made to provide modified synthetic analogs of such insect neuropeptides for use as targeted insecticides, with promising results. However, despite the ideality and effectiveness of these modified peptides, bringing them to market may be challenging in many regions where their use is heavily regulated.

[0006] The present invention aims to solve one or more of the above-mentioned problems and to provide novel natural pyrokinin neuropeptides and their natural variants or analogs for use as insect control agents and plant protectants. Summary of the Invention

[0007] The inventors have discovered novel pyrogen peptides and their natural variants or analogs that have insecticidal activity against insects (e.g., hemiptera, dipterans, lepidopterans, cockroaches, and / or coleopterans) and are therefore potentially 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) or a salt or solvate thereof:

[0009] R 1 -Y 1 -ZY 2 -R 2

[0010] (I)

[0011] in:

[0012] R 1 It is hydrogen (which can be named "H-" or "Hy-"), C 1-4 Alkyl (e.g., methyl, ethyl, propyl, butyl), formyl, acyl, fatty acyl, sugar moiety, phosphate ester or sulfate ester, or R 1 The following formula contains a pyroglutamic acid group:

[0013]

[0014] Furthermore, any alkyl, formyl, acyl, or fatty acyl group may optionally be selected from one or more oxo or C-terminated groups. 1-6 Alkyl or sugar moiety, phosphate ester or sulfate ester group substitution;

[0015] Y 1 Peptides that either do not exist or contain one or two amino acids;

[0016] Z is a peptide based on the following formula.

[0017] NADEDQQQSVDFTPRL(SEQ ID NO:1);

[0018] Y 2 Peptides that either do not exist or contain one or two amino acids;

[0019] 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).

[0020] In another aspect, a composition is provided comprising a compound or salt thereof as defined herein, 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.

[0021] On the other hand, the use of compounds or salts thereof as defined herein, or compositions thereof, as insect control agents is provided. This use can be as an insecticide against insects encoding pyrogens. This use can be as an insecticide against Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera, preferably Hemiptera, Diptera, and / or Lepidoptera, and most preferably Lepidoptera such as moths.

[0022] On the other hand, a method for increasing insect mortality is provided, comprising contacting an insect colony with a compound or a salt thereof as defined herein, or a composition as defined herein. Suitably, the insects are insects encoding pyrogens, such as hemiptera, dipterans, lepidopterans, cockroaches, and / or coleopterans, preferably hemiptera, dipterans, and / or lepidopterans, most preferably lepidopterans, such as moths.

[0023] In another aspect, 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. Preferably, the insects are Lepidoptera, such as moths.

[0024] On the other hand, the use of compounds as defined herein, salts thereof, or compositions thereof, as plant protectants is provided for protecting plants from insects encoding the pyrogens. Preferably, the insects are lepidopteran insects, such as moths.

[0025] In another aspect, the use of compounds or salts thereof as defined herein, or compositions thereof as defined herein, as plant protectants for protecting plants from the influence of hemiptera, dipterans, lepidopterans, cockroaches and / or coleopterans, preferably hemiptera, dipterans and / or lepidopterans, most preferably lepidopterans, such as moths.

[0026] On the other hand, a method for inhibiting plant infection by insects encoding pyrogens 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 the plant has no or substantially no insects encoding pyrogens.

[0027] On the other hand, a method for inhibiting plant infestation by Hemiptera, Diptera, Coleoptera, Blattodea, 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, most preferably Lepidoptera insects, such as moths.

[0028] On the other hand, methods are provided for reducing insect infestation of plants by insects encoding pyrogens, or for reducing the insect load on plants encoding pyrogens, the methods comprising contacting the plants with compounds as defined herein or salts thereof or compositions as defined herein.

[0029] On the other hand, methods are provided for reducing plant infection by Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera insects, or for reducing the insect load on plants by Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera, comprising contacting the plant with a compound as defined herein or a salt thereof, or a composition as defined herein. Preferably, the insects are selected from Hemiptera, Diptera, and / or Lepidoptera, most preferably Lepidoptera, such as moths. In one embodiment, the compounds, compositions, and agents of the present invention suitably have activity against the moth species Diamondback moth. In one embodiment, the compounds, compositions, and agents of the present invention suitably have activity against the moth species Fall Armyworm. In one embodiment, the compounds, compositions, and agents of the present invention suitably have activity against the inchworm species White-spotted Armyworm.

[0030] Suitable insects encoding pyrogen peptides include Hemiptera, Diptera, Lepidoptera, Blattodea, and / or Coleoptera, with Hemiptera, Diptera, and / or Lepidoptera being preferred. In a preferred embodiment, the insect encoding the pyrogen peptide is a Lepidoptera, such as a moth.

[0031] On the other hand, a method for producing the insecticidal compound according to the first aspect is provided, the method comprising:

[0032] (a) An insecticidal compound of chemical formula (I) or a precursor thereof.

[0033] In one embodiment, the chemical synthesis includes the methods described in the examples. In one embodiment, the chemical synthesis includes... Figure 2 The methods and steps are shown.

[0034] 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

[0035] 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] 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.

[0038] The term amino acid is an abbreviation for α-amino[α-amino]carboxylic acid. Each molecule contains a central carbon atom, called the α-carbon, to which an amino group 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 R below:

[0039]

[0040] Unless otherwise stated, the amino acid residues in the peptides of this invention are in the L-configuration. 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 as above by their full names or according to standard three-letter or one-letter amino acid codes.

[0041] 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.

[0042] 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.

[0043] 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).

[0044] 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-).

[0045] 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 groups may optionally be substituted and include groups 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 propyl-1-alkenyl (-CH=CHCH3).

[0046] In the chemical structures drawn in this article, or The existence of indicates a connection point or free radical, for example, the free radical discussed in relation to various functional groups.

[0047] 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.

[0048] 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.

[0049] As used herein, “plant” refers to the whole plant or a part thereof, including fresh fruits, vegetables, and seeds. A plant or a 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.

[0050] 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, canola, castor beans, or olives, gourds, etc. Algae, such as cucumbers, melons, or squash; fiber plants, such as cotton, flax; 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).

[0051] 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.

[0052] 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.

[0053] "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).

[0054] The terms “effective amount” and “effective dose” used in this article refer to the amount required to achieve the desired result.

[0055] 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 phyla Arthropoda, Tardigrades, 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.

[0056] 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.

[0057] 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.

[0058] 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%.

[0059] The compounds of the present invention

[0060] Specific compounds of the present invention include, for example, compounds of formula (I), wherein, unless otherwise stated, R 1 Y 1 Y 2 R 2 Each of the substituents and any associated substituents shall have the meaning as defined in any of the paragraphs (1) to (12) above or below: -

[0061] (1)R 1 Selected from hydrogen, acyl or fatty acyl, or phosphate or sulfate, or R 1 The following formula contains a pyroglutamic acid group:

[0062]

[0063] The acyl or fatty acyl group may optionally be replaced by a sugar moiety, phosphate ester, or sulfate ester.

[0064] (2)R 1 Selected from hydrogen, formyl, acetyl (Ac), propionyl, butanoyl, palmitoyl, butyryl, cerotoyl, decyl, dodecanoyl, dodecanoyl, tunganoyl, heptanoyl, hexanoyl, eicosanoyl, eicosanoyl, tetracosanoyl, linoleyl, thiooctanoyl, myristoyl, nonanoyl, octadecanoyl, octanoyl, palmitoyl, stearoyl, undecanoyl, and pentanoyl.

[0065] (3)R 1 Selected from hydrogen, acetyl or palmitoyl, or R 1 The following formula contains a pyroglutamic acid group:

[0066]

[0067] (4)R 1 Selected from hydrogen or palmitoyl.

[0068] (5)R 1 It is hydrogen.

[0069] (6)R 1 The following formula contains a pyroglutamic acid group:

[0070]

[0071] (7)Y 1 Peptides that either do not exist or contain one or two amino acid residues.

[0072] (8)Y 1 It does not exist.

[0073] (9)Y 2 Peptides that either do not exist or contain one or two amino acid residues.

[0074] (10)Y 2 It does not exist.

[0075] (11)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).

[0076] (12)R 2 It is NH2.

[0077] 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 (4) or (5) above.

[0078] Appropriately, Y 1 Or Y 2 It is as defined in any of the paragraphs (7) to (10) above. Most appropriately, Y 1 Or Y 2 It is as defined in paragraphs (8) or (10) above.

[0079] Appropriately, R 2 It is as defined in paragraphs (11) or (12) above. Most appropriately, R 2 It is as defined in paragraph (12) above.

[0080] In a preferred embodiment, R 1 It's hydrogen, Y1 and Y 2 It does not exist, and R 2 It is NH2.

[0081] In a preferred embodiment, R 1 It's hydrogen, Y 2 It does not exist, Y 1 It is one or two amino acids, and R 2 It is NH2.

[0082] In a preferred embodiment, R 1 It's hydrogen, Y 1 It does not exist, Y 2 It is one or two amino acids, and R 2 It is NH2.

[0083] Further explanation of the compounds of the present invention

[0084] R 1 and R 2

[0085] 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 With Y 1 The nitrogen atom bond of the N-terminal amino group, R 2 With Y 2 The C-terminal carbonyl carbon atom is bonded.

[0086] 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. Therefore, suitably, R 1 It can be an aromatic group, a heteroaromatic group, an aliphatic group, or a lipophilic group.

[0087] 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, cetyl, decyl, dodecylenoyl, dodecyl, tungyl, heptayl, hexanoyl, eicosyl, eicosylenoyl, tetracosyl, linoleyl, thiocyl, myristyl, nonanoyl, octadecyl, octanoyl, palmitoleyl, stearoyl, undecyl, and pentanoyl. Therefore, suitably, R 1 The group can be palmitoyl ([Palm]), that is:

[0088]

[0089] 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 R 1b -C(O)-, for example, acetyl (Ac), i.e.:

[0090]

[0091] In some embodiments, R 1 The group can be replaced by the sugar portion.

[0092] In some embodiments, one or more amino acid residues in peptides Y and Z can be naturally modified with a sugar moiety, i.e., the amino acid residues can be "saccharide analogues". For example, the sugar can be part of a Ser or Thr side chain modification (glycosylation) or a Lys or Arg side chain modification (glycosylation).

[0093] 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, lysose, 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. Sugars can exist as N-terminal modifications or as part of Ser side-chain modifications. In some embodiments, R 1 The group can be replaced by a phosphate ester or a sulfate ester.

[0094] In some embodiments, one or more amino acid residues in peptides Y and Z may be naturally modified with phosphate or sulfate esters. For example, phosphate or sulfate esters may be part of a side-chain modification, i.e., the amino acid may be phosphorylated or sulfated.

[0095] R 1 Selected from hydrogen (which may not be specified in a particular peptide sequence, or may 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 R 1e Each is independently selected from hydrogen or C. 1-4 Alkyl (e.g., methyl, ethyl, propyl, butyl), preferably hydrogen or methyl.

[0096] 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.

[0097] When R 1 = "H" (or "Hy"); it 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.

[0098] In some embodiments, the N-terminal glutamine (Gln or Q) or N-terminal glutamate (Glu or E) residues may undergo a transformation to form a pyroglutamate terminal group [pyr]:

[0099]

[0100] This conversion can occur in biological systems through reaction with certain enzymes at the N-terminal glutamine (Q) or glutamate (E) residues. This conversion can also be achieved synthetically.

[0101] Therefore, Y 1 Peptides (if present) or Z-peptides may also contain an N-terminal [pyr] group:

[0102]

[0103] The N-terminal [pyr] group can be formed by the cyclization of an N-terminal glutamine (Gln or Q) or N-terminal glutamate (Glu or E) residue to form a pyroglutamic acid terminal group. Since this transformation 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) residue.

[0104] Appropriately, R 2 It is NH2, NR 2a H, NR 2a R 2b OR 2a ;where R 2a and R 2b Each as defined herein. Preferred R 2 It is NH2.

[0105] Specific examples of the pyrogen peptide according to the present invention include:

[0106]

[0107] Or its salts or solvates.

[0108] In some embodiments, the compounds of the present invention may be in the form of salts or solvates (e.g., hydrates).

[0109] The compounds of the present invention can be provided in combination with one or more other active insecticides, such as those described herein.

[0110] Y 1 and Y 2

[0111] A peptide may contain one or two additional peptide groups located between terminal R1 and R2 groups at the N and C ends, respectively. Suitably, these groups are Y... 1 and Y 2 Groups. If present, these groups are located on either side of the Z-peptide group.

[0112] In one embodiment, Y 1 and Y 2 The functional group is not present.

[0113] In one embodiment, the compound contains only Y. 1 Group. In one embodiment, the compound contains only Y. 2 Group.

[0114] In one embodiment, the compound contains Y 1 and Y 2 Group.

[0115] Suitablely, when present, the Y group contains one or two amino acids. Suitablely, the Y group may contain any amino acid, suitably selected from M, R, G, and K.

[0116] In one embodiment, the Y group is selected from: GR, RG, KR, RK, K, R, M, and G. In another embodiment, the Y group is selected from: RG, KR, and K.

[0117] In one embodiment, the compound contains only Y. 2 Group, wherein Y 2 The groups are selected from RG, KR, and K.

[0118] Modified amino acids or non-natural amino acid analogues

[0119] In a preferred embodiment, the insecticidal compound does not contain any modified amino acids or non-natural amino acid analogs.

[0120] Specifically, preferably, peptide Y 1 (If present) does not contain any modified amino acids or non-natural amino acid analogues, and peptide Y 2 (If present) it does not contain any modified amino acids or non-natural amino acid analogs. Therefore, in some embodiments, peptide Y 1 and Y 2 It contains only unmodified amino acid residues, and appropriately only natural amino acid residues.

[0121] Specifically, peptide Z does not contain any modified amino acids or non-natural amino acid analogs. Therefore, in some embodiments, peptide Z contains only unmodified amino acid residues, suitably only natural amino acid residues.

[0122] active

[0123] Suitablely, the compounds of the present invention have anti-insect activity. Suitablely, this activity is against hemiptera, dipterans, lepidopterans, cockroaches, and / or coleopterans.

[0124] In preferred embodiments, the compounds of the present invention possess activity against lepidopteran insects. Therefore, the compounds of the present invention can be particularly useful against lepidopteran insects and can be particularly applied in the related uses and methods described herein. Particularly preferred lepidopteran insects are moths.

[0125] The compounds of the present invention generally increase insect mortality, for example, when in contact with suitable insects or ingested by suitable insects. Therefore, the compounds of the present invention described herein (and compositions containing them) can be considered insecticides and can be referred to as “insect control agents”.

[0126] Suitablely, the compounds of the present invention thereby indirectly increase plant health, including increased plant growth, yield, etc., by preventing plant infestation by insects and reducing the insect load on plants. Therefore, the compounds of the present invention (and compositions containing them) described herein can also be considered "plant protectants".

[0127] Not wishing to be bound by theory, any or all of the described effects can be mediated by agonist activity at pykaloid receptors in target insects. Pykaloid receptors believed to be present in target insects include GPCR pykaloid receptor 1 and pykaloid receptor 2, PK1-R, and PK2-R. The compounds of the present invention are suitable for binding to one or more pykaloid receptors in target insects. Suitably, the compounds of the present invention have agonist activity upon binding to pykaloid receptors in target insects. Suitably, the compounds of the present invention bind to pykaloid receptor 1 and / or pykaloid receptor 2. Suitably, the compounds of the present invention are agonists of pykaloid receptor 1 and / or pykaloid receptor 2.

[0128] Insect control agents

[0129] 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.

[0130] 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.

[0131] 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 an entire plant. Suitablely, insect mortality can be measured by performing an artificial lepidopteran diet assay as described in the examples herein.

[0132] Insect control agents can be used to reduce the size of insect populations, or to inhibit the growth of insect populations or to inhibit the feeding of insect populations (e.g., compared to other insect populations that are not exposed to the same agent).

[0133] The insect control composition is a composition comprising an insect control agent (i.e., the compound of the present invention as described).

[0134] Plant protectant

[0135] 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.

[0136] 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.

[0137] 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, Coleoptera, Blattodea, and / or Lepidoptera.

[0138] Plant protection compositions are compositions comprising plant protection agents (i.e., the compounds of the present invention as described herein).

[0139] plant

[0140] 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.

[0141] Suitable plants or parts thereof that can be protected by the compounds or compositions thereof of the present invention or the pharmaceuticals 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 nut (Arecacatechu), 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), *Rubus* spp., pepper (Piper nigrum), black thorn (Acaciamearnsii), blueberry (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* 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) Medica, Citrus (Citrus veticulata), clover species (Trifolium spp.), clove (Syzygium aromaticum), coconut (Cocos nucifera), taro species (Colocasia spp.); yellow-fleshed taro species (Xanthosoma spp.), coffee species (Coffee spp.), kola species (Cola spp.), Brassica napus, maize (Zea mays), wild lettuce (Valerianellalocusta), cotton species (Gossypium spp.), cowpea (Vigna unguiculate), blueberry species (Vaccinium spp.), lepidium sativum, cucumber (Cucumis sativus), currant spp. (Ribes spp.), reticulated custard apple (Annona reticulata), taro (Colocasia esculenta), date palm (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* (Pelargonium); species of the genus *Geranium* (Geranium) (Ginger) (Zingiber officinalis), species of the genus *Langenaria* (Calamus) (Language) (Calamus) (Cucurbita) spp.), chickpea (Cicer arietinum), grapefruit (Citrus paradise), grape (Vitisvinifera), needlegrass (Lygeum spartum), orchardgrass (Dactylis glomerata), peanut (Arachis hypogaea), guava (Psidium guajava), hazelnut (Corylus avellane), Indian hemp (Crotalaria juncea), agave (Agave fourcroydes), ragweed (Lawsonia inermis), hops (Humulus lupulus), horseradish (Armoracia Rusticana), indigofera tinctorial, 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 (Myristica fragrans), agave (Agaveatrovirens), citrus (Citrus reticulata), mango (Mangifera indica), cassava (Manihotesculenta), 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 (Elaeis guineensis), okra (Abelmoschus) esculentus), olive (Olea europaea), sweet orange (Citrus sinensis), sour orange (Citrus aurantium), orchardgrass (Dactylis glomerate), and species of the genus Metroxylon (Metroxylon spp.).*Borassus flabellifer*, *Carica papaya*, *Pastinaca sativa*, *Pyrus communis*, *Pisum sativum*, *Carya illinoensis*, *Capsicum annuum*, *Diospyros kaki*; *Diospyros virginiana*, *Cajanus cajan*, *Ananas comosus*, *Pistacia* spp., *Prunus domestica*, *Punica granatum*, *Citrus grandis*, *Solamum tuberosum*, *Ipomoea batatas*, *Cucurbita* spp., *Chrysanthemum cineraraiefolium*, *Aspidosperma* spp.), quince (Cydonia oblonga), cinchona species (Cinchona spp.), quinoa (Chenopodium quinoa), radish (Raphanus sativus) (including horseradish (Cochlearia armoracia)), ramie (Boehmeria nivea), creeping bentgrass species (Agrostis spp.), ramie (Boehmeria nivea), rhubarb species (Rheum spp.), rice (Oryza sativa); gleaming rice (Oryza glaberrima), rose species (Rose spp.), Brazilian rubber tree (Heveabrasiliensis), rye (Secale cereal), ryegrass species (Lolium spp.), safflower (Carthamustinctorius), sago palm species (Metroxylon spp.).Red Bean Grass (Onobrychis viciifolia), Wild Lettuce (Valerianella locusta), Brahman Ginseng (Tragopogon porrifolius), Sapodilla (Achrassapota), Citrus (Citrus reticulata), Brussels Sprouts (Brassica ileracea capitate), Black Brahman Ginseng (Scorzonera hispanica), Sesame (Sesamumindicum), Avocado (Butyrospermum paradoxum), Agave sislana, Lime (Citrus aurantifolia), Soybean (Glycinemax), Spelt Wheat (Triticum spelta), Spinach (Spinacia oleracea), Rye (Secalecereal), Cucurbita spp., Fragaria spp., Sudan Grass (Sorghumbicolor Sudanense), Sugarcane (Saccharum officinarum), Sunflower (Helianthus) annuus, jujube (Crotalaria juncea), lemon (Citrus limetta), sweet potato (Ipomoea batatas), citrus (Citrus reticulata), arrow-leaved yellow-bodied taro (Xanthosoma sagittifolium), cassava (Manihot esculenta), taro (Colocasia esculenta), tea tree (Camellia sinensis), Ethiopian thrush (Eragrostisabyssinica), cat's tail grass (Phleum pratense), tobacco (Nicotiana tabacum), tomato (Lycopersicumesculentum), lotus species (Lotus spp.), kudzu species (Aleurites spp.), turnip (Brassicarapa), ground peach (Urena lobate), vanilla (Vanilla planifolia), broad bean (Vicia sativa), walnut species (Juglans spp.), watermelon (Citrullus) lanatus), black thorn (Acacia mearnsii), wheat species (Triticum spp.), barley species (Hordeum spp.), and yam species (Dioscorea spp.).Paraguayan tea (Ilex paraguariensis).

[0142] 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, Coleoptera, Blattodea, and / or Lepidoptera insects, or plants or portions thereof that attract Hemiptera, Diptera, Coleoptera, Blattodea, and / or Lepidoptera insects. Suitably, the plants or portions thereof that are infested by Hemiptera, Diptera, Coleoptera, Blattodea, and / or Lepidoptera insects, or plants or portions thereof that attract Hemiptera, Diptera, Coleoptera, Blattodea, and / or Lepidoptera insects, are any of the above.

[0143] Suitablely, the plant or part thereof that is infested by or attracts hemipteran insects is any of those listed above.

[0144] Suitablely, the plant or part thereof that is infested by or attracts dipteran insects is any of those listed above.

[0145] Appropriately, the plant or part thereof that is infested by or attracts lepidopteran insects is any of those listed above.

[0146] Appropriately, the plant or part thereof that is infested by or attracts beetles is any of those listed above.

[0147] Suitablely, the plant or part thereof that is infested by or attracts cockroaches is any of those listed above.

[0148] 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 (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); strawberry (fragararia species), blueberry (Vaccinium species), blackberry (Rubus species), raspberry (Rubus species), citrus (citrus species), olive (Olea species), durian (Durio species), and longan (Dimocarpus species). spp.), lychee (L. chinensis species), persimmon (Diospyros spp. species); legumes and peas (including but not limited to species of common bean, cowpea, pea, lentil, soybean, chickpea, pigeon pea, 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, squash, zucchini (species of cucumber), and tubers (species of nightshade), or parts thereof.

[0149] 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, squash, zucchini (cucumber species), citrus (citrus species), and tubers (potatoes) (solepis species), or portions thereof. In one embodiment, the plant is a vegetable crop, suitably a Brassica species.

[0150] In one embodiment, the plant or a portion thereof is selected from plants or parts thereof that have been infected or attracted by dipteran insects, such as: cereals (wheat species); oats (oat species); rye (rye species); barley (barley species), rice (rice species), and corn (corn species); legumes and peas (including but not limited to those from the genera *Phaseolus*, *Vigna*, *Pisum*, *Lens*, *Glycine*, *Cicer*, *Cajanus*, *Arachis*, etc.); and fruit crops (including apples (*Malus* species), pears (*Pyrus* species), and strawberries (*Strawberry* species). Species, including blueberries (Vaccinium species), blackberries (Rubus species), raspberries (Rubus species), cherries, plums, apricots, peaches, nectarines (Prunus species), blackcurrants, redcurrants, whitecurrants, currants (Rubus species), kiwifruit (Actinidia species), papaya (Carica species), avocado (Avocado species), mango (Mango), longan (Longan species), litchi (L. chinensis), grapes (Vitis species), figs (Fig species), passion fruit (Passiflora species), Asian pears (Pyrus species), citrus (Citrus species), and olives (Olive species); vegetable crops, including Allium species. Eggplant, tomato (spp.), and pepper (spp.), lettuce (spp.), brassica (spp.), cucumber, cucurbits, squash, and zucchini (spp.); umbelliferous root crops, including carrot (spp.), parsnip (spp.), or parts thereof.

[0151] In one embodiment, the plant or a portion thereof is selected from plants or parts thereof that have been infected or attracted by 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 (pear species); tree nuts (including, for example, almonds (P. amygdalus)) and pistachios (Pistachios pumila). Walnuts (Juglandaceae), hazelnuts (Corylus species); avocados, including alligator pears (Lauraceae), blueberries (Vaccinium species), citrus fruits (Citrus species), olives (Olive species), durians (Durian species), longans (Longan species), litchis (L. chinensis), persimmons (Diospyros species); legumes and peas (including but not limited to species of the genera *Vigna*, *Vigna*, *Vigna*, *Lysimachia*, *Glycine*, *Chickpea*, *Pistacia*, and *Peanut*), beets (sugar) beet (Beta vulgaris)), sugarcane (succulents), lettuce (species of lettuce), brassica (species of brassica) (including rapeseed), onion (species of allium), tomato (species of nightshade), pepper (species of capsicum), asparagus, cucurbits, squash, zucchini (species of cucumber), and tuberous (potato) (species of nightshade), cauliflower (Brassica oleracea Botrytis), or parts thereof.

[0152] insect

[0153] The compounds, compositions, and agents of the present invention suitably possess the insecticidal activity described above.

[0154] 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*.

[0155] Other examples come from the order Anoplura (Phthiraptera), such as species of the genera *Damalinia*, *Haematopinus*, *Linognathus*, *Pediculus*, *Ptirus pubis*, and *Trichodectes*.

[0156] Other examples come from the subclass Chilopoda, such as species of the genera *Geophilus* and *Scutigera*.

[0157] Other examples come from the order Coleoptera, such as the cucumber beetle (Acalymma vittatum), bean weevil (Acanthoscelides obtectus), species of the genus *Adoretus* spp., 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* spp., flower weevil species (Anthonomus spp.), dermestid beetle species (Anthrenus spp.), fine wasp species (Apion spp.), slender flower beetle species (Apogonia spp.), micro-hairy round springtail species (Atomaria spp.), felt beetle species (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.), powder 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 *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 (Agriotes spp. species).

[0158] Other examples come from the order Colchiformes, such as the armed jerboa (Onychiurus armatus).

[0159] Other examples come from the class Diplopoda, such as the spotted worm (Blaniulus guttulatus).

[0160] 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.), species of the genera *Eurygaster*, *Heliopeltis*, *Horcias nobilellus*, *Leptocorisa*, *Leptoglossus phyllopus*, *Lygus*, *Macropes excavatus*, Miridae, *Monalonion atratum*, *Nezaras*, *Oebalus*, Pentomidae, *Piesmaquadrata*, *Piezodorus*, *Psallus*, *Pseudacysta* persea), species of the genus Rhodnius (Rhodnius spp.).), black and brown round shield scale (Sahlbergellasingularis), 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 (Chaetosiphonfragaefolii), Java scale (Chionaspis tegalensis), rice green bug (Chlorita onukii), walnut gall aphid (Chromaphis juglandicola), cottony cushion scale (Chrysomphalus) Ficus, corn leafhopper (Cicadulinambila), gall aphid (Coccomytilus halli), and species of the genus Coccus spp.* *Cryptomyzus ribis*, *Dalbulus spp.*, *Dialeurodes* spp., *Diaphorina* spp., *Diaspis* spp., *Drosicha* spp., *Dysaphis* spp., *Dysmicoccus* spp., *Empoasca* spp., *Eriosoma* spp., *Erythroneura* spp., *Euscelis bilobatus*, *Ferrisia* spp., *Geococcus coffeae*, and *Hieroglyphus* spp.), persimmon scale (Homalodiscacoagulata), rice leafhopper (Hyalopterus arundinis), species of the genera *Icerya*, *Idiocerus*, *Idioscopus*, striped leafhopper (Laodelphaxstriatellus), wax scale (Lecanium), scale insect (Lepidosaphes), cabbage aphid (Lipaphis erysimi), long-tubed aphid (Macrosiphum), sugarcane gall aphid (Mahanarva), sugarcane woolly aphid (Melanaphis sacchari), small-headed aphid (Metcalfiella), two-spined rice leafhopper (Metopolophium dirhodum), edge-horned aphid (Monellia) The following aphids are listed: costalis, walnut flat-horned aphid (Monelliopsis pecanis), *Myzus* spp., nut black aphid (Nasonovia ribisnigri), *Nephotettix* spp., brown planthopper (Nilaparvata lugens), *Oncometopia* spp., long-horned aphid (Orthezia praelonga), whitefly (Parabemisia myricae), wood aphid (Paratrioza spp.), scale insect (Parlatoria spp.), and gall aphid (Pemphigus spp.).The following species are listed: * Peregrinus maidis* (corn leaf beetle), *Phenacoccus* spp., *Phloeomyzus passerinii* (pear scale), *Phorodon humuli* (hops aphid), *Phylloxera* spp. (root phylloxera), *Pinnaspis aspidistrae* (shield scale), *Planococcus* spp., *Protopulvinaria pyriformis* (pear-shaped mealybug), *Pseudaulacaspispentagona* (five-cornered shield scale), *Pseudococcus* spp., *Psylla* spp., *Pteromalus* spp., *Pyrilla* spp., *Quadraspidiotus* spp., and *Quesada* (giant shield scale). 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*, *Tenalaphara malayensis*, *Tinocallis caryaefoliae*, *Tomaspis* spp., *Toxoptera* spp., *Trialeurodes* spp., and *Trioza* Species of the genera *Typhlocyba*, *Unaspis*, *Viteus vitifolii*, and *Zygina*.

[0161] 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.*.

[0162] Other examples come from the order Isopoda, such as Armadillidium vulgare, Oniscus asellus, and Porcellio scaber.

[0163] Other examples come from the order Isoptera, such as species of the genera *Coptotermes*, *Cornitermes cumulans*, *Cryptotermes*, *Incisitermes*, *Microtermes obesi*, *Odontotermes*, and *Reticulitermes*.

[0164] 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.), Citrus psyllid (Ecdytolopha aurantium), small sugarcane borer (Elasmopalpus lignosellus), African giant moth (Eldana saccharina), species of the genera *Ephestia* (Ephestia spp.), species of the genera *Epinotia* (Epinotia spp.), grape flower leaf roller (Epiphyas postvittana), species of the genera *Etiella* (Etiella spp.), and species of the genera *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*. The following species are listed: molesta, eggplant borer (Leucinodes orbonalis), Leucoptera spp., Lithocolletis spp., Lithophaneantennata, Lobesia spp., Loxagrotis albicosta, Lymantria spp., Lyonetia spp., Malocosomaneustria, Maruca testulalis, Mamestra brassicae, Mods spp., Mythimna separata, Nymphula spp., Oiketicus spp., Orria spp., and Orthaga 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*, soybean borer (Pseudoplusia includens), purple 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* spp., *Stathmopodas* spp., *Stomopteryx subsecivella*, *Synanthedon* spp., *Tecia solanivora*, *Thermesia gemmatalis*, *Tineapellionella*, *Tineola bisselliella*, *Tortrix* spp., *Trichophaga tapetzella*, *Trichoplusia* spp., *Tutaabsoluta*, and *Virachola* spp.

[0165] 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).

[0166] Other examples come from the order Blattodea, such as the oriental cockroach (Blatta orientalis), the German cockroach (Blattella germanica), the American cockroach (Periplaneta america), species of the genus Periplaneta (Periplanetaspp.), the brown-spotted cockroach (Supella longipalpa), and termites of the suborder Isoptera, such as termites of the family Termitidae.

[0167] Other examples come from the order Fleas, such as species of the genera *Ceratophyllus*, *Ctenocephalides*, *Tunga penetrans*, and *Xenopsyllacheopis*.

[0168] Other examples come from orders within the class Syntagma, such as species of the genus *Scutigerella*.

[0169] 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*.

[0170] In a preferred embodiment, the compounds, compositions, and agents of the present invention suitably have activity against insects of the orders Hemiptera, Diptera, Coleoptera, Blattodea, and / or Lepidoptera. In a preferred embodiment, the compounds, compositions, and agents of the present invention suitably have activity against Lepidoptera. In a preferred embodiment, the compounds, compositions, and agents of the present invention suitably have activity against moths. In one embodiment, the compounds, compositions, and agents of the present invention suitably have activity against the moth species *Plutella xylostella*. In one embodiment, the compounds, compositions, and agents of the present invention suitably have activity against the moth species *Prunella vulgaris*. In one embodiment, the compounds, compositions, and agents of the present invention suitably have activity against the moth / inchworm species *Spodoptera litura*.

[0171] Hemiptera insects

[0172] 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.

[0173] 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.

[0174] 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.

[0175] 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).

[0176] 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.

[0177] Aphids may belong to genera such as Aphis nigra (e.g., pea aphid), Aphis (e.g., cotton aphid, soybean aphid, beet aphid), Diuraphis (e.g., wheat Diuraphis noxia), Aphis spp. (e.g., rose aphid, potato aphid), Aphis spp. (e.g., peach aphid), Aphis spp. (e.g., cereal aphid), or Aphis spp. (e.g., wheat aphid).

[0178] 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.

[0179] 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).

[0180] The cotton aphid (also known as the melon aphid) is a pest of the cucurbitaceae family and cotton.

[0181] Besides aphids, insects can belong to, for example, the family Coccidioidae, such as the genus Coccidioidae (e.g., Coccidioidae).

[0182] 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).

[0183] These insects may belong to the family Psyllidaceae, such as the genus Pachypsylla (e.g., Pachypsylla venusta).

[0184] As examples of Hemiptera insects outside the suborder Sternophora, these insects may belong to the family Cestridae, such as the genus Cestrum (bedbugs), such as temperate bedbugs.

[0185] 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*).

[0186] 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.

[0187] These insects may belong to the family Psyllidaceae, such as the genus Psyllid (e.g., Citrus Psyllid).

[0188] These insects may belong to the family Pseudatomoscelis, such as the genus Pseudatomoscelis (e.g., the cotton flea), the genus Pseudatomoscelis (e.g., the grass flea Lygus hesperus), or the genus Tupiocoris (e.g., the spotted Tupiocoris notatus). For example, the cotton flea (cotton flea) is a pest of cotton.

[0189] These insects may belong to the family Stink Bugs, such as those in the genera *Euschistus* (e.g., *Euschistus servus*), *Euschistus heroes*, *Euschistus*, *Murgantia histrionica*, *Euschistus servus*, *Euschistus heroes*, *Euschistus servus*, *Murgantia histrionica*, *Euschistus servus*, *Euschistus servus*, or *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.

[0190] These insects may belong to the family Pyrrocoris, such as the genus Pyrrocoris (e.g., the wingless red bug (Pyrrocoris apterus)).

[0191] 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).

[0192] These insects may belong to the family Psyllidaceae, such as the genus *Acanthocasuarina* (e.g., *Acanthocasuarina muellerianae*).

[0193] In one embodiment, the insect may be selected from the following species: tea-winged bug, hero bug, hilare bug, cotton aphid, brown bug, brown stink bug, peach aphid, southern green stink bug, brown planthopper, cotton jumping mirid bug, and long red trapeze bug.

[0194] In one embodiment, the insect belongs to the peach aphid species.

[0195] Diptera insects

[0196] The compounds, compositions, and agents of the present invention can have activity against dipteran insects.

[0197] In particular, they may be active against Drosophila species, such as fruit flies, including those in the genus *Drosophila*, such as *Drosophila suzukiensis*. They may also be active against fruit flies, including species in the genera *Anastrepha*, *Flyflies*, *Flyflies*, *Flyflies spp.*, *Flyflies spp.*, and *Tephritis*.

[0198] The families Drosophila and Fructus are generally referred to as fruit flies.

[0199] 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:

[0200] Plant miners (e.g., *Phytomyza angelicastri*);

[0201] Melani (e.g., the black-bellied leafminer (Melani agromyza));

[0202] The genus *Antherigona* (e.g., species of the genus *Antherigona*);

[0203] The genus *Delia radicum* (e.g., the cabbage ground fly (*Delia radicum*));

[0204] The genus *Contarinia* (e.g., *Contarinia sorghicola*);

[0205] 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

[0206] Lepidoptera

[0207] The compounds, compositions, and agents of the present invention can have activity against lepidopteran insects.

[0208] In particular, they may be active against insects of the genera *Heliothis*, *Plutella*, *Spodoptera*, *Cydia*, and *Trichoplusia*. Suitably, the compounds, compositions, and agents of the present invention may be active against the following species: *Heliothis*, *H. virescens*, species of *Spodoptera*, and codling moth (*Trichoplusia spp.*), larvae of *Heliothis* species, including *Peltigera virescens* and *Spodoptera littoralis* (which represents several species of moths in the subfamily Heliothisinae and the genus *Spodoptera* and is a global agricultural pest), diamondback moth (*Trichoplusia spp.*, one of the most important Brassica pests worldwide), and *Trichoplusia spp.*

[0209] In one embodiment, the compounds, compositions, and agents of the present invention may have activity against the diamondback moth. In one embodiment, the compounds, compositions, and agents of the present invention may have activity against the fall armyworm. In one embodiment, the compounds, compositions, and agents of the present invention may have activity against the white armyworm.

[0210] Coleoptera

[0211] The compounds, compositions, and agents of the present invention can have activity against Coleoptera insects.

[0212] In particular, they may be active against the following genera of insects: Bruchus, Ceutorhynchus, Psylliodes, Leptinotarsa, Sitona, Meligethes, Atomaria, and Agrates. Suitably, 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.)

[0213] Blattales

[0214] The compounds, compositions, and agents of the present invention may have activity against cockroaches.

[0215] In particular, they may have activity against isoptera. Suitably, the compounds, compositions, and agents of the present invention may have activity against termite species.

[0216] Suitablely, the compounds, compositions and agents of the present invention may have activity against the following species: Oriental cockroach (Blatta orientalis), German cockroach (Blattella germanica), American cockroach (Periplaneta america), species of the genus Periplaneta (Periplaneta spp.), and brown-banded cockroach (Supella longipalpa).

[0217] Household pests

[0218] The compounds, compositions, and agents of this invention can also be active against household pests such as cockroaches and termites (e.g., termites of the family Termiteidae). 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 (e.g., 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.

[0219] 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.

[0220] Methods and uses of the present invention

[0221] Methods to increase insect mortality

[0222] 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, Coleoptera, Blattodea, and / or Lepidoptera.

[0223] 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.

[0224] 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.

[0225] 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.

[0226] 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.

[0227] In one particular embodiment, a method is provided to increase the mortality rate of beet aphids (Aphis fabae), cotton aphids (Aphisgossypii), pea aphids (Acyrthosiphon pisum), peach aphids (Myzus persicae), cotton leafhoppers (Amrascabiguttula), or rice constrictor aphids (Rhopalosiphum padi), the method comprising contacting the beet aphids, cotton aphids, pea aphids, peach aphids, cotton leafhoppers, rice constrictor aphids, or insect populations with a compound or composition or combination as defined herein.

[0228] 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.

[0229] 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.

[0230] 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.

[0231] 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.

[0232] 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 or combination as defined herein.

[0233] 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 populations with a compound or composition or combination as defined herein.

[0234] 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.

[0235] In one embodiment, a method for increasing the mortality rate of cockroaches is provided, the method comprising contacting cockroaches or a colony of cockroaches with a compound or composition or combination as defined herein.

[0236] Methods to suppress or reduce plant or site infection

[0237] The present invention also provides a method for inhibiting insect infestation of plants or plant parts, wherein the insects are suitably Hemiptera, Diptera, Coleoptera, Blattodea, and / or Lepidoptera, the method comprising contacting the plant or plant parts with the compound, composition, or combination thereof.

[0238] 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.

[0239] 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.

[0240] 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.

[0241] 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.

[0242] In one embodiment, a method is provided for inhibiting the infestation of plants by beet aphids, cotton aphids, pea aphids, peach aphids, or cereal aphids, the method comprising contacting the plant with a compound or composition or combination as defined herein.

[0243] 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.

[0244] 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.

[0245] In one embodiment, a method for inhibiting the infestation of a plant by a tea winged bug is provided, the method comprising contacting the plant with a compound or composition or combination as defined herein.

[0246] 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.

[0247] 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.

[0248] 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.

[0249] 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.

[0250] 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.

[0251] In one embodiment, a method for inhibiting the infestation of plants by cockroaches is provided, the method comprising contacting the plant with a compound or composition or combination as defined herein.

[0252] 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, Coleoptera, Blattodea, and / or Lepidoptera, the method comprising contacting the site with said compound, composition, or combination.

[0253] 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.

[0254] 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.

[0255] Alternatively, the plant or part or location of the plant may have been colonized or infested by insects, preferably Hemiptera, Diptera, Coleoptera, Blattodea and / or Lepidoptera.

[0256] 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, Coleoptera, Blattodea, and / or Lepidoptera.

[0257] Methods to reduce insect consumption

[0258] 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, Coleoptera, Blattodea, and / or Lepidoptera.

[0259] Methods to protect plants from insects

[0260] This 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, Coleoptera, Blattodea, and / or Lepidoptera insects or their infestation, wherein the method comprises the step of applying the insecticidal compound or composition or combination of the invention directly or indirectly to the plant or plant part. Suitable indirect application may include applying the compound or composition or combination of the invention to the field or place where the plant is growing or intended to grow.

[0261] 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, Coleoptera, Blattodea, and / or Lepidoptera, 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 plants or harvested parts of plants, or the location where they are intended to be stored.

[0262] Appropriately, the insects can be Hemiptera, Diptera, Coleoptera, Blattodea, and / or Lepidoptera.

[0263] Methods of contact with insects

[0264] 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.

[0265] 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.

[0266] Suitablely, the insect can be from the orders Hemiptera, Diptera, Coleoptera, Blattodea, and / or Lepidoptera. More suitablely, the insect belongs to the order Lepidoptera. Most suitablely, the insect is a moth, such as the diamondback moth, fall armyworm, or whiteleg moth.

[0267] Application of compounds or compositions

[0268] 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.

[0269] However, for insects harmful to humans, such as those in the family Bedbugidae (e.g., bedbugs of the genus *Cyprinus*, 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 nuisance kissing bug), the substrate can act as a vector for human diseases. The substrate can be a household surface or item, such as bedding, mattresses, or any other suitable household surface. The compound or composition can be applied to the substrate in a form suitable for insect ingestion.

[0270] 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.

[0271] 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.

[0272] The compounds or compositions or combinations disclosed herein may be applied to a plant or a part of a plant, either directly or indirectly, by spraying, misting, foaming, fumigation, hydroponics, hydroponics, coating, immersion, injection, and / or coating, optionally after harvest. Suitable contact may include, for example, feeding or spraying. In some embodiments, contact is made by ingestion. Contact may include injecting a plant (e.g., a tree) or a part thereof with a composition as defined herein using systems and methods such as those described in WO 2020 / 021041, WO 2023 / 161802, WO 2022 / 264053, WO 2022 / 189386, WO 2022 / 165248, WO 2021 / 152093, WO 2020 / 212612, and WO 2020 / 021041 (the entire contents of which are incorporated herein by reference).

[0273] 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.

[0274] Used as a plant protectant

[0275] 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, Coleoptera, Blattodea, and / or Lepidoptera. The plant protectants are further described above.

[0276] Used as an insect control agent

[0277] 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.

[0278] 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, Coleoptera, Blattodea and / or Lepidoptera insects, or in methods for inhibiting or reducing insect infestation (suitably Hemiptera, Diptera, Coleoptera, Blattodea and / or Lepidoptera insects) or reducing the insect load on plants.

[0279] The present invention also provides the use of the compounds or compositions or combinations thereof described herein as insect control agents, specifically through their bioinhibitory effects on Hemiptera, Diptera, Coleoptera, Blattodea and / or Lepidoptera insects, their biocidal effects on Hemiptera, Diptera, Coleoptera, Blattodea and / or Lepidoptera insects, and / or their pest-killing effects on Hemiptera, Diptera, Coleoptera, Blattodea and / or Lepidoptera insects.

[0280] 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, pests are insects of the orders Hemiptera, Diptera, Coleoptera, Blattodea, and / or Lepidoptera. 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.

[0281] "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 pyrogens.

[0282] Suitablely, the compound or composition or combination can be used as an insect control agent, wherein the insect is a Diptera. Suitablely, the compound can be used as an insect control agent, wherein the insect belongs to the Drosophila genus. Suitablely, the compound can be used as an insect control agent, wherein the insect is Drosophila suzuki.

[0283] Suitablely, the compounds, compositions, or combinations defined herein may be used as insect control agents, wherein the insect is a hemiptera. Suitablely, the compounds, compositions, or combinations defined herein may be used as insect control agents, wherein the insect is an aphid. Suitablely, the compounds, compositions, or combinations defined herein may be used as insect control agents, wherein the insect belongs to the genus *Hemiptera*. Suitablely, the compounds, compositions, or combinations defined herein may be used as insect control agents, wherein the insect is the peach aphid.

[0284] Suitablely, the compounds, compositions, or combinations defined herein may be used as insect control agents, wherein the insect is a hemiptera. Suitablely, the compounds, compositions, or combinations defined herein may be used as insect control agents, wherein the insect belongs to the genus *Rhododendron*. Suitablely, the compounds, compositions, or combinations defined herein may be used as insect control agents, wherein the insect is a *Rhododendron*.

[0285] Suitablely, the compounds, compositions, or combinations defined herein can be used as insect control agents, wherein the insect belongs to the order Lepidoptera. Suitablely, the compounds, compositions, or combinations defined herein can be used as insect control agents, wherein the insect belongs to the genus Diamondback moth. Suitablely, the compounds, compositions, or combinations defined herein can be used as insect control agents, wherein the insect is the diamondback moth.

[0286] Suitablely, the compounds, compositions, or combinations defined herein can be used as insect control agents, wherein the insect belongs to the order Lepidoptera. Suitablely, the compounds, compositions, or combinations defined herein can be used as insect control agents, wherein the insect belongs to the genus *Hemiberlesiae*. Suitablely, the compounds, compositions, or combinations defined herein can be used as insect control agents, wherein the insect is *Pseudomonas aeruginosa*.

[0287] Suitablely, the compounds, compositions, or combinations defined herein can be used as insect control agents, wherein the insect belongs to the order Lepidoptera. Suitablely, the compounds, compositions, or combinations defined herein can be used as insect control agents, wherein the insect belongs to the genus *Spodoptera*. Suitablely, the compounds, compositions, or combinations defined herein can be used as insect control agents, wherein the insect is *Spodoptera*.

[0288] Suitablely, the compounds or compositions or combinations defined herein can be used as insect control agents, wherein the insect belongs to the order Coleoptera.

[0289] Suitablely, the compounds or compositions or combinations defined herein can be used as insect control agents, wherein the insect belongs to the order Blattodea. Suitablely, the compounds or compositions or combinations defined herein can be used as insect control agents, wherein the insect is a cockroach or a termite.

[0290] Methods to control insect fertility

[0291] 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, Coleoptera, or Lepidoptera, 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. Suitably, in some embodiments, the Lepidoptera insect is the fall armyworm.

[0292] A method for controlling the fertility of hemiptera insects is also provided, comprising contacting the compounds or compositions of the present invention with a substrate (e.g., plants or soil). Suitably, hemiptera insects are any of those disclosed herein, such as aphids.

[0293] 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.

[0294] A method for controlling the fertility of lepidopteran insects is 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.

[0295] 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.

[0296] A method for controlling the fertility of cockroaches is also provided, comprising contacting the compound or composition of the invention with a substrate (e.g., plant or soil). Suitably, cockroaches are any of the insects disclosed herein.

[0297] 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.

[0298] 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.

[0299] 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.

[0300] 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.

[0301] A method for controlling the fertility of Blattodea insects 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, Blattodea insects are any of the insects disclosed herein. Suitably, the combinations comprise compounds of the present invention and kinins or analogues thereof.

[0302] 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.

[0303] 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.

[0304] 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.

[0305] 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.

[0306] 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.

[0307] 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.

[0308] 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.

[0309] 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.

[0310] 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.

[0311] A method for controlling the fertility of cockroaches or insect colonies is also provided, comprising contacting the combinations described herein or the compositions of the present invention with cockroaches or insect colonies. Suitably, the cockroaches are any of the insects disclosed herein. Suitably, the combinations comprise compounds of the present invention and kinins or analogues thereof.

[0312] 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).

[0313] Combination with other insecticides

[0314] The compounds of the present invention can be used in combination with one or more other insecticides or insecticidal compounds (such as those described herein). Combinations comprising the compounds of the present invention or their salts or solvates in combination with one or more other active insecticides or insecticidal compounds are also provided.

[0315] The compositions of the present invention may also contain one or more other active insecticides or active insecticidal compounds.

[0316] Suitablely, the insecticide may be selected from insect neuropeptides or analogues thereof, such as kinins, AKH peptides, DH31 peptides, DH44 peptides, pyrogalin, or CAPA peptides (e.g., CAPA-1, CAPA-2, or CAPA-3 analogues). In certain embodiments, an additional insecticide is a kinin, such as SB-P-69 ([Hy]-NFSPWG-[NH2], SEQ ID NO:14). 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; and sulfamethoxam.

[0317] Suitable, the additional insecticide or insecticidal compound may be included in the composition of the present invention.

[0318] 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.

[0319] 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.

[0320] 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:

[0321]

[0322] In one embodiment, the compound of the present invention is used in combination with another pyrogenic peptide, such as...

[0323]

[0324]

[0325] In one embodiment, the compound of the present invention is used in combination with a kinin, such as...

[0326]

[0327] In one embodiment, the compounds of the present invention are used in combination with CAPA peptides (e.g., CAPA2 peptide).

[0328] In one embodiment, the compound of the present invention is used in combination with an AKH peptide, such as...

[0329]

[0330] Suitablely, any combination of the above compounds may be included in the compositions of the present invention.

[0331] The choice of adjuvant or additional pesticides usually depends on the specific target species.

[0332] Beneficial insect species

[0333] The compounds and compositions 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 honeybees, such as those of the genus Bumblebee, such as the European bumblebee. Important predatory species include ladybugs (Ladybugs), such as the two-spotted ladybug.

[0334] "Essentially 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.

[0335] Composition

[0336] 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.

[0337] The compositions of the present invention, or compositions used according to the present invention, generally comprise a combination of the said compound with one or more auxiliary components (e.g., solvents, carriers, diluents, adjuvants, preservatives, dispersants, emulsifiers, or synergists). Suitably, the composition may be an agricultural composition, an insect control composition (e.g., an insecticide composition), or a plant protection composition.

[0338] 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.

[0339] The composition typically comprises the compounds described herein mixed with one or more auxiliary components such as solvents, carriers, diluents, adjuvants, preservatives, dispersants, emulsifiers, or synergists.

[0340] The composition may also comprise a combination with one or more other active insecticides described herein.

[0341] 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. The composition may be an aqueous composition. Further details will be explained below.

[0342] 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 insects); 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.

[0343] As used herein, “agricultural use” includes not only the use of the insecticidal compounds of the present invention, combinations thereof, or compositions thereof, and optional agrochemicals as defined above (e.g., pest control agents, growth regulators, nutrients / fertilizers, insect repellents, defoliants, etc.) suitable and / or intended for use on field-grown crops (e.g., agriculture), but also the use of the compounds of the present invention, combinations thereof, or compositions thereof, and the agrochemicals as defined above intended for use on greenhouse-grown crops (e.g., horticulture / floristry) or hydroponic cultivation systems, and even the use of the compounds of the present invention, combinations thereof, or compositions thereof, and agrochemicals as defined above suitable and / or intended for use on non-crop purposes, such as use in private gardens, household use (e.g., household herbicides or insecticides), or use by pest control personnel (e.g., weed control, etc.).

[0344] 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.

[0345] 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.

[0346] As used herein, a composition refers to a composition 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. It will be clear from the further description herein that the compositions used herein comprise biological insect control agents or biological insecticides, and these terms are used interchangeably in this application. Therefore, the compositions used herein comprise 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, adjuvants, surfactants, wetting agents, dispersants, oils, binders, thickeners, penetrants, buffers, acidifiers, antisettling agents, antifreeze agents, photoprotectants, defoamers, biocides, and / or drift control agents.

[0347] Suitablely, the compositions of the present invention are aqueous compositions.

[0348] 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.

[0349] 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 up to 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 specific embodiments, 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.

[0350] 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.

[0351] 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.

[0352] Adjuvants can enhance product performance, for example, by improving the delivery efficiency of the active ingredient, reducing the level of the desired active ingredient, or expanding the range of efficacy.

[0353] 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.

[0354] 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.

[0355] Adjuvants that regulate spray retention may dissipate the kinetic energy of droplets during impact, meaning the likelihood of bouncing or runoff is reduced. Such adjuvants include alkyl polyglucosides, alkoxylated alcohols, and polyoxyethylene monobranched alcohols (e.g., polyoxyethylene (8) monobranched alcohols).

[0356] Adjuvants that modulate wetting properties (i.e., wetting agents) can reduce surface tension and contact angle, thereby improving coverage. Such adjuvants include polyoxyethylene dehydrated sorbitol monolaurate (e.g., polyoxyethylene (8) dehydrated sorbitol monolaurate), surfactant blends, and alkyl polyglucosides.

[0357] Adjuvants that regulate sediment formation can influence the evaporation of water from droplets, thereby providing a more uniform distribution. Such adjuvants include alkoxylated polyol esters, polyoxyethylene sorbitan monolaurates (e.g., polyoxyethylene (12) sorbitan monolaurate), and alkyl polyglucosides.

[0358] Adjuvants that modulate absorption 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).

[0359] 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 cuticle of insects), as the carrier oil often acts as an adjuvant.

[0360] Oils suitable for OD dispersions include flaxseed oil, rapeseed oil, and soybean oil.

[0361] 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 amphoteric polymeric dispersants and adjuvants.

[0362] 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.

[0363] The composition may also contain adhesives or dyes.

[0364] 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.

[0365] 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.

[0366] As used herein, “carrier” refers to 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 media, 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.

[0367] 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 or combination thereof of the present invention. Therefore, the present invention suitably provides a composition or formulation comprising a plurality of liposomes, said liposomes comprising a compound or combination thereof of the present invention, soybean lecithin (preferably 25 mg / ml), and glycerol (preferably 3%).

[0368] 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.

[0369] 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.

[0370] 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 medium) to provide the (concentrated) liquid composition of the present invention, which has stability that allows the composition of the present invention to be properly 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 a suitable liquid concentrate, dry powder, tablet, capsule suspension, slurry, or “wet cake,” which can be appropriately diluted, dispersed, suspended, emulsified, or otherwise reconstituted by the end user 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.

[0371] 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.

[0372] Commercially available basic formulations can also be used to formulate the compounds described in this specification, for example... FMPC (Akzo Nobel).

[0373] 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.

[0374] 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.

[0375] The composition may also contain one or more other attractants, sterilizing agents, acaricides, nematicides, fungicides, growth regulators, or herbicides.

[0376] 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.

[0377] Examples of such agrochemicals will be clear to those skilled in the art; for example, including but not limited to: glyphosate, paraquat, metolachlor, acetochlor, mesotrione, 2,4-D, atrazine, glufosinate, sulfadiazine, quizalofop-p-ethyl, pendimethalin, chlorpyrifos, trifluralin, bromobenzonitrile, chlorpyrifos, fluroxypyr, nicosulfuron, bensulfuron-methyl, imidacloprid, dicamba, imidacloprid, thiamethoxam, fipronil, chlorpyrifos, deltamethrin, deltamethrin, 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, chlorantraniliprole, and other known agrochemicals or any suitable combination thereof.

[0378] Methods for producing insecticidal compounds

[0379] 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.

[0380] The insecticidal compounds of this invention can be synthesized using any suitable chemical method.

[0381] 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.

[0382] In one embodiment of the invention, the insecticidal compound is a peptide of the following formula: [Hy]-NADEDQQQSVDFTPRL-[NH2] (SEQ ID NO:2). Suitably, this peptide can be synthesized by the methods defined in the examples. Suitably by Figure 2 The methods defined in [the document / reference].

[0383] In another aspect of the invention, an isolated insecticidal compound produced by the method of the invention is provided. Suitably, an isolated insecticidal compound of formula (I) is produced by the method of the invention.

[0384] In another aspect of the invention, a method for producing the composition disclosed herein is provided, the method comprising at least the steps of: (a) obtaining at least one insecticidal compound of formula (I), and (b) formulating the insecticidal compound into a composition.

[0385] In another aspect of the invention, a method for producing and / or manufacturing variants of the insecticidal compound of formula (I) is provided. This may include the steps of: (i) modifying peptide Z of formula (I) by adding, substituting, or deleting at least one amino acid; and (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.

[0386] 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:

[0387] a) Modify peptide Z by adding, replacing, or deleting at least one amino acid;

[0388] 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;

[0389] 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.

[0390] d) When the insecticidal activity is improved compared to insecticidal compounds containing unmodified peptide Z, the variant is further manufactured, isolated, and purified.

[0391] Suitablely, the steps of obtaining at least one insecticidal compound include (a) chemically synthesizing the insecticidal compound.

[0392] 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.

[0393] 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.

[0394] 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.

[0395] 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.

[0396] Any section headings used herein are for typographical purposes only and should not be construed as limiting the scope of the subject matter. Attached Figure Description

[0397] Aspects and embodiments of the invention will now be discussed with reference to the accompanying drawings, in which:

[0398] Figure 1 The chemical structure of SB-P-80 is shown;

[0399] Figure 2 The chemical synthetic route for synthesizing SB-P-80 is shown;

[0400] Figure 3 The experimental setup for determining artificial feed for Lepidoptera was shown.

[0401] Figure 4 The activity data of unformulated SB-P-80 against fall armyworm are shown after 168 hours. One larva was measured per cell (n=10).

[0402] Figure 5 Data on the activity of peptide SB-P-80 against diamondback moth were presented after laboratory spray assays performed via FERA.

[0403] Figure 6 The data show the activity of unformed peptide SB-P-80 against fall armyworm after leaf disc assay.

[0404] Figure 7 Field trial data show the % control of peptide SB-P-80 against diamondback moth (Caragana korshinskii) in gray mold of cabbage (cauliflower);

[0405] Figure 8Field trial data show the % control of peptide SB-P-80 against the cabbage looper in botrytis cinerea (cauliflower).

[0406] Example

[0407] The invention will now be demonstrated and further described through the following non-limiting examples.

[0408] General Program

[0409] 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 resins, will be noted where appropriate. Peptide-grade DMF was purchased from Rathburn.

[0410] Peptides are synthesized on either the Biotage Initiator+Alstra microwave-assisted peptide synthesizer or the CEM LibertyPrime microwave-assisted peptide synthesizer, as specified.

[0411] High-resolution mass spectrometry (HRMS) was performed on a Bruker microTOF-Q II (ESI+).

[0412] Peptides were purified using a Phenomenex Gemini C18 column (5 μm, 250 x 21.2 mm) 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 solvents consisting of A (H₂O + 0.1% TFA) and B (MeCN + 0.1% TFA), followed by lyophilization of the fractions using a ChristAlpha 2-4LO plus lyophilizer.

[0413] The purified peptides were analyzed using a Phenomenex (Aeris, 5 μm, peptide XB-C18, 150 x 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 in 5% solution B and a 5-minute wash in 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 in 5% solution B and a 5-minute wash in 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.

[0414] 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 3000LC. Analysis was performed on a Reprosil Gold 120C18, 3 μm 150 x 4 mm column using a linear gradient from buffer A (95 / 5H₂O / MeCN, containing 0.1% v / v TFA) to buffer B (95 / 5MeCN / 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.

[0415] High-resolution mass spectrometry (HRMS) analysis of the purified peptides was performed on a Bruker microTOF-Q II (ESI+) spectrometer.

[0416] Proton nuclear magnetic resonance spectra used to calculate peptide content ( 1H 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, δ 7.26; CD3OD, δ 3.31 and D2O, δ 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).

[0417] General procedure for automated peptide synthesis

[0418] Biotage initiator + Alstra synthesizer:

[0419] Fmoc-protected amino acids were prepared in DMF as 0.2 M (0.1 mmol synthesis), 0.5 M (0.2 mmol synthesis), or 0.7 M (0.5 mmol synthesis) 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 synthesis), 0.5 M (0.2 mmol synthesis), or 0.7 M (0.5 mmol synthesis) 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 for 2 minutes under microwave heating. 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.

[0420] CEM Liberty Blue Synthesizer

[0421] Fmoc-protected amino acids were prepared as 0.2 M NBP (Tamisolve) solutions. Five equivalents of amino acid (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. Except for Fmoc-Cys(Trt)-OH, Fmoc-His(Trt)-OH, and Fmoc-Arg(Pbf)-OH, the coupling reaction and Fmoc deprotection 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.

[0422] General procedure for TFA cleavage of peptides

[0423] 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.

[0424] 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.

[0425] The specific synthetic route of SB-P-80 is as follows: Figure 2 As shown. For the synthesis of SB-P-80, the double coupling method was used for 9Ser, 11Asp, and 13Thr. The extended 6-min coupling was used for 3Asp, 4Glu, 5Asp, 6Gln, and 7Gln, and the 7-min arginine coupling was used for 15Arg.

[0426] Unless otherwise stated herein, peptides are synthesized according to the general procedure described above, the exemplary procedure described below, or ordered directly.

[0427] Mortality assessment methods

[0428] Lepidoptera artificial feed determination

[0429] 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 x 10⁻⁶. -4 M, each peptide was aliquoted into 10 pools. Once the feed solidified 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 setup for the Lepidoptera artificial feed assay was as follows: Figure 3 As shown. SB-P-80 was used to test the activity of artificial feeds for Lepidoptera, and compared with a negative control mediator and the insecticide dichlorodiphenyltrichloroethane (DDT). The activity of SB-P-80 is shown in the figure. Figure 4 As shown; unlike broad-spectrum chemical insecticides such as DDT, SB-P-80 has higher activity, is also environmentally friendly, and targets specific pests.

[0430] Lepidoptera spray measurement

[0431] FERA conducted a laboratory spraying trial in which each treatment was applied to four cabbage plants at a concentration of 2 x 10⁻⁶. - 4 The peptide SB-P-80 (with and without Silwet-408) was sprayed from above using a laboratory spray chamber at a rate of 200 L / ha. Plants were allowed to air dry, then twenty diamondback moth larvae (2nd / 3rd instar) were added to each plant, which was then covered with a ventilated bag and secured with elastic bands. The plants were placed in plastic containers and watered from below. The plants were then placed under experimental conditions: a CE chamber set at 20°C and 65% RH with a 16-hour light:8-hour dark lighting scheme. Insect mortality was assessed 7 days after peptide spraying and compared with the chemical insecticide "Gazelle". SB-P-80 was shown to be highly effective at killing insects, with effects comparable to the chemical product. Results are as follows: Figure 5 As shown.

[0432] Lepidoptera leaf disc determination

[0433] The leaf disc assay was adapted from IRAC sensitivity test method 018 (https: / / irac-online.org / methods / plutella-xylostella-larvae / ?ext=pdf).

[0434] Place 9cm diameter filter paper into a Piper dish and moisten it, ensuring there is no water reservoir to prevent potential larval damage. Select Brassica leaves of suitable size for the Piper dish and immerse them in 2 x 10 cm water.-4 M-peptide solution. Gently shake the leaves to remove excess liquid, repeating this process ten times per treatment. Then, each leaf in each replicate was infected with one L1 larva, as the larvae are highly aggressive and exhibit cannibalistic tendencies. Piper dishes were sealed with folded tissue and stacked using rubber bands to minimize the risk of larval escape. The dishes were placed in a humidified chamber at 25°C with a relative humidity of approximately 60% and a light-dark cycle of 16:8. Observations were made daily for 6 to 10 days, depending on the degree of leaf consumption. Leaf immersion assays were performed using SB-P-80 and compared with a negative control and the currently commercial insecticide chlorantraniliprole. The activity of SB-P-80 against fall armyworm was as follows: Figure 6 As shown; unlike broad-spectrum chemical insecticides, SB-P-80 has good activity, is environmentally friendly, and targets specific pests.

[0435] field trials

[0436] Collins Agricultural Consultants, Inc. conducted field trials in the United States, studying the effects of concentrations of 1x10⁻⁶ over 2-27 days. -4 The efficacy of M's insecticidal peptide SB-P-80 against the diamondback moth (Cabbage looper) on cabbage (cauliflower) crops. Two applications were administered 7 days apart, where DAA represents the number of days after the first application (A) and DAB represents the number of days after the second application (B). The experiment observed that SB-P-80 exhibited excellent insecticidal activity under these conditions. Figure 7 As shown.

[0437] Collins Agricultural Consultants in the United States conducted further field trials in a similar manner, studying the effects of concentrations of 1 x 10⁻⁶ over 2-27 days. -4 The insecticidal peptide SB-P-80 of M is effective against the cabbage looper (spotted armyworm) on cabbage (cauliflower) crops. Experiments showed that SB-P-80 achieved excellent insecticidal activity under these conditions, such as... Figure 8 As shown.

[0438] References

[0439] 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.

[0440] ○Koyama T,Terhzaz S,Naseem MT,Nagy S,Rewitz K,Dow JAT,Davies SA,Halberg KV.Anutrient-responsive hormonal circuit mediates an inter-tissueprogram regulating metabolic homeostasis in adult Drosophila.Nat Commun.2021

[0441] ○Kean L,Cazenave W,Costes L,Broderick KE,Graham S,Pollock VP,DaviesSA,Veenstra JA,Dow JA.Two nitridergic peptides are encoded by the genecapability in Drosophila melanogaster.Am J Physiol Regul Integr CompPhysiol.2002

[0442] ○Yeoh JGC,Pandit AA,Zandawala M, DR,Davies SA,Dow JAT.DINeR:Database for Insect Neuropeptide Research.Insect Biochem Mol Biol.2017

[0443] ○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

[0444] ○Audsley N and Down RE,G protein coupled receptors as targets fornext generation pesticides.Insect Biochem Molec 67:27-37(2015).

[0445] ○Halberg KA,Terhzaz S,Cabrero P,Davies SAand Dow JAT,Tracing theevolutionary origins of insect renal function.Nat Commun 6(2015).

[0446] ○Dow JA,Insights into the Malpighian tubule from functionalgenomics.J Exp Biol 212:435-445(2009).

[0447] ○Huesmann GR,Cheung CC,Loi PK,Lee TD,Swiderek KM and Tublitz NJ,Amino acid sequence of CAP2b,an insect cardioacceleratory peptide from thetobacco hawkmoth Manduca sexta.FEBS Lett 371:311-314(1995).

[0448] ○Davies SA,Cabrero P,Povsic M,Johnston NR,Terhzaz S and Dow JAT,Signaling by drosophila capa neuropeptides.Gen Comp Endocr 188:60-66(2013).

[0449] ○Terhzaz S,Teets NM,Cabrero P,Henderson L,Ritchie MG,Nachman RJ,DowJAT,Denlinger DL and Davies SA,Insect capa neuropeptides impact desiccationand cold tolerance.Proc Natl Acad Sci 201501518(2015).

[0450] ○Terhzaz S,Alford L,Yeoh JGC,Marley R,Dornan AT,Dow JAT and DaviesSA,Renal neuroendocrine control of desiccation and cold tolerance byDrosophila suzukii.Pest Manag Sci 74:800-810(2017).

[0451] ○Predel R,Wegener C,Biology of the CAPApeptides in insects.Cell MolLife Sci 63:2477-2490(2006).

[0452] ○Lamango NS,Nachman RJ,Hayes TK,Strey Aand Isaac RE,Hydrolysis ofinsect neuropeptides by an angiotensin converting enzyme from the housefly,M.domestica.Peptides 18:47-52(1997).

[0453] ○Terhzaz S,Cabrero P,Robben JH,Radford JC,Hudson BD,Milligan G,DowJAand Davies SA,Mechanism and function of Drosophila capa GPCR:a desiccationstress-responsive receptor with functional homology to human neuromedinUreceptor.PLoS One 7(1):e29897(2012).

[0454] ○Blackman RL and Eastop VF,Aphids on the World’s Crops:AnIdentification Guide,John Wiley&Sons Ltd,Chichester,UK.(2000).

[0455] ○Dow JAT,Maddrell SHP,Gortz A,Skaer NJV,Brogan S and Kaiser K,TheMalpighian tubules of Drosophila melanogaster–a novel phenotype for studiesof fluid secretion and its control.J Exp Biol 197:421-428(1994).

[0456] ○Davies SA,Huesmann GR,Maddrell SH,O’Donnell MJ,Skaer NJ,Dow JAT andTublitz NJ,CAP2b,a cardioacceleratory peptide,is present in Drosophila andstimulates tubule fluid secretion via cGMP.Am J Physiol 269:R1321–R1326(1995).

[0457] Annu Rev Entomol 55:351-374(2010) ○Beyenbach KW,Skaer H and Dow JA,The developmental,molecular,andtransport biology of Malpighian tubules.

[0458] ○Sadeghi A.,Van Damme,EJMand Smagghe G.(2009)Evaluation of thesusceptibility of the pea aphid,Acyrthosiphon pisum,to a selection of novel biorational insecticides using an artificial diet.Journal ofInsect Science 9:65.

[0459] ○Van Emden F(2009).Artificial diet for aphids–thirty years'experience.REDIA,XCII:163-167

Claims

1. Insecticidal compounds of the formula: [Hy]-NADEDQQQSVDFTPRL-[NH2] (SEQ ID NO: 2) or salts or solvates thereof, or combinations thereof, for use as insect control agents or as plant protectants against lepidopteran insects to protect plants or parts thereof.

2. Use of the compound or composition as claimed in claim 1, wherein the use is directed to: Diamondback moth, fall armyworm, or striped armyworm.

3. A method for increasing the mortality rate of lepidopteran insects, the method comprising contacting lepidopteran insects or insect colonies with an insecticidal compound of the formula: [Hy]-NADEDQQQSVDFTPRL-[NH2] (SEQ ID NO: 2) or a salt or solvate thereof, or a combination thereof.

4. A method for inhibiting or preventing lepidopteran 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 expected to grow, with an insecticidal compound or a combination thereof of the formula: [Hy]-NADEDQQQSVDFTPRL-[NH2] (SEQ ID NO: 2) or a salt or solvate thereof.

5. The method of claim 4, wherein the compound or composition is contacted with the plant or part thereof, or the location where the plant is growing or is intended to grow, when the plant or part thereof is free of or substantially free of lepidopteran insects.

6. A method for reducing or treating lepidopteran insect infestation on plants or reducing the lepidopteran insect load on plants, the method comprising contacting the plant or a portion thereof, or the location where the plant is growing, with an insecticidal compound or a combination thereof of the formula: [Hy]-NADEDQQQSVDFTPRL-[NH2] (SEQ ID NO: 2) or a salt or solvate thereof.

7. The method of claim 4 or 5, wherein the location where the plant is growing or is expected to grow includes an agricultural location suitable for growing plants.

8. The method of any one of claims 3, 4 or 6, wherein the insects are: diamondback moth, fall armyworm or striped armyworm.

9. The method of any one of claims 3, 4 or 6, wherein contact with the lepidopteran insect or insect colony, plant or part thereof, or location comprises treating the lepidopteran insect or insect colony, plant or part thereof, or location with the compound or composition by: irrigation, feeding, spraying, foaming, hydroponics, coating, immersion, injection and / or coating.

10. The method of any one of claims 3, 4 or 6, wherein the lepidopteran insect or insect colony, plant or part thereof, or location is contacted with an effective concentration of the compound.

11. The method of claim 10, wherein the concentration is 10 -3 M to 10 -9 Between M.

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