Classifications

• • A—HUMAN NECESSITIES
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
  • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
  • A01N43/72—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms
  • A01N43/84—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms six-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,4
• • A—HUMAN NECESSITIES
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
  • A01N37/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
  • A01N37/36—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing at least one carboxylic group or a thio analogue, or a derivative thereof, and a singly bound oxygen or sulfur atom attached to the same carbon skeleton, this oxygen or sulfur atom not being a member of a carboxylic group or of a thio analogue, or of a derivative thereof, e.g. hydroxy-carboxylic acids
  • A01N37/38—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing at least one carboxylic group or a thio analogue, or a derivative thereof, and a singly bound oxygen or sulfur atom attached to the same carbon skeleton, this oxygen or sulfur atom not being a member of a carboxylic group or of a thio analogue, or of a derivative thereof, e.g. hydroxy-carboxylic acids having at least one oxygen or sulfur atom attached to an aromatic ring system
  • A01N37/40—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing at least one carboxylic group or a thio analogue, or a derivative thereof, and a singly bound oxygen or sulfur atom attached to the same carbon skeleton, this oxygen or sulfur atom not being a member of a carboxylic group or of a thio analogue, or of a derivative thereof, e.g. hydroxy-carboxylic acids having at least one oxygen or sulfur atom attached to an aromatic ring system having at least one carboxylic group or a thio analogue, or a derivative thereof, and one oxygen or sulfur atom attached to the same aromatic ring system
• • A—HUMAN NECESSITIES
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
  • A01N37/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
  • A01N37/44—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing at least one carboxylic group or a thio analogue, or a derivative thereof, and a nitrogen atom attached to the same carbon skeleton by a single or double bond, this nitrogen atom not being a member of a derivative or of a thio analogue of a carboxylic group, e.g. amino-carboxylic acids
• • A—HUMAN NECESSITIES
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
  • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
  • A01N43/02—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms
  • A01N43/04—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom
  • A01N43/06—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom five-membered rings
  • A01N43/12—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom five-membered rings condensed with a carbocyclic ring
• • A—HUMAN NECESSITIES
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
  • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
  • A01N43/34—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
  • A01N43/36—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom five-membered rings
  • A01N43/38—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom five-membered rings condensed with carbocyclic rings
• • A—HUMAN NECESSITIES
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
  • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
  • A01N43/34—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
  • A01N43/40—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
• • A—HUMAN NECESSITIES
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
  • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
  • A01N43/34—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
  • A01N43/40—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
  • A01N43/42—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
• • A—HUMAN NECESSITIES
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
  • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
  • A01N43/48—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
  • A01N43/50—1,3-Diazoles; Hydrogenated 1,3-diazoles
• • A—HUMAN NECESSITIES
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
  • A01N61/00—Biocides, pest repellants or attractants, or plant growth regulators containing substances of unknown or undetermined composition, e.g. substances characterised only by the mode of action
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23B—PRESERVATION OF FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES; CHEMICAL RIPENING OF FRUIT OR VEGETABLES
  • A23B2/00—Preservation of foods or foodstuffs, in general
  • A23B2/70—Preservation of foods or foodstuffs, in general by treatment with chemicals
  • A23B2/725—Preservation of foods or foodstuffs, in general by treatment with chemicals in the form of liquids or solids
  • A23B2/729—Organic compounds; Microorganisms; Enzymes
  • A23B2/742—Organic compounds containing oxygen
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23B—PRESERVATION OF FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES; CHEMICAL RIPENING OF FRUIT OR VEGETABLES
  • A23B2/00—Preservation of foods or foodstuffs, in general
  • A23B2/70—Preservation of foods or foodstuffs, in general by treatment with chemicals
  • A23B2/725—Preservation of foods or foodstuffs, in general by treatment with chemicals in the form of liquids or solids
  • A23B2/729—Organic compounds; Microorganisms; Enzymes
  • A23B2/762—Organic compounds containing nitrogen
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23B—PRESERVATION OF FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES; CHEMICAL RIPENING OF FRUIT OR VEGETABLES
  • A23B2/00—Preservation of foods or foodstuffs, in general
  • A23B2/70—Preservation of foods or foodstuffs, in general by treatment with chemicals
  • A23B2/725—Preservation of foods or foodstuffs, in general by treatment with chemicals in the form of liquids or solids
  • A23B2/729—Organic compounds; Microorganisms; Enzymes
  • A23B2/771—Organic compounds containing hetero rings
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23B—PRESERVATION OF FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES; CHEMICAL RIPENING OF FRUIT OR VEGETABLES
  • A23B4/00—Preservation of meat, sausages, fish or fish products
  • A23B4/14—Preserving with chemicals not covered by groups A23B4/02 or A23B4/12
  • A23B4/18—Preserving with chemicals not covered by groups A23B4/02 or A23B4/12 in the form of liquids or solids
  • A23B4/20—Organic compounds; Microorganisms; Enzymes
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23B—PRESERVATION OF FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES; CHEMICAL RIPENING OF FRUIT OR VEGETABLES
  • A23B5/00—Preservation of eggs or egg products
  • A23B5/08—Preserving with chemicals
  • A23B5/12—Preserving with chemicals in the form of liquids or solids
  • A23B5/14—Organic compounds; Microorganisms; Enzymes
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23K—FODDER
  • A23K20/00—Accessory food factors for animal feeding-stuffs
  • A23K20/10—Organic substances
  • A23K20/116—Heterocyclic compounds
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
  • A61K31/404—Indoles, e.g. pindolol
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
  • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
  • A61K31/4406—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
  • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
  • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
  • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
  • A61L2/00—Disinfection or sterilisation of materials or objects, in general; Accessories therefor
  • A61L2/16—Disinfection or sterilisation of materials or objects, in general; Accessories therefor using chemical substances
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
  • A61L9/00—Disinfection, sterilisation or deodorisation of air
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
  • A61P31/04—Antibacterial agents
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
  • A61P31/10—Antimycotics
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
  • A61L2103/00—Materials or objects being the target of disinfection or sterilisation
  • A61L2103/05—Living organisms or biological materials

Definitions

• the present invention relates in general to the uses of nicotinamide adenine dinucleotide (“NAD”) synthetase inhibitors, and in particular, but not limited, to the use of NAD synthetase inhibitors in treating the environment against microbial contamination, in agriculture, e.g., in raising foodcrops and food animals, and in medicine, e.g., to disinfect, sterilize, or decontaminate equipments, devices, rooms, and people.
• NAD nicotinamide adenine dinucleotide
• Spore-forming bacteria can be lethal.
• Bacillus anthracis causes the deadly disease, anthrax.
• antibiotic-resistant strains e.g., engineered strains that are not recognized by B. anthracis antibodies or common bacteria engineered to carry the virulence gene (see, e.g., T. C. Dixon et al., "Anthrax," New England Journal of medicine, 341 (11), 815- 826, Sept. 1999).
• the foregoing shows that there exists a need for a novel treatment against spore-forming bacteria, particularly B. anthracis or bacteria carrying the virulence gene of B. anthracis.
• the present invention ameliorates some of the disadvantages of the prior art.
• the present invention provides a method for increasing production of food animals comprising administering to the food animal an effective amount of at least one inhibitor of NAD synthetase of a microbe capable of infecting the food animal.
• the present invention further provides a method for the treatment or prevention of infection by a spore-forming bacterium in an animal comprising treating an environment of the animal with an effective amount of at least one inhibitor of NAD synthetase of the spore-forming bacterium.
• the present invention further provides a method for killing the vegetative cell of a spore- forming bacterium in an environment comprising treating the environment with an effective amount of at least one inhibitor of NAD synthetase of the bacterium.
• the present invention also provides a method for treating a fungal or bacterial disease in a plant comprising treating the plant or the environment of the plant with an effective amount of at least one inhibitor of NAD synthetase of the fungus or bacterium.
• the present invention further provides a method for disinfecting, sterilizing, or decontaminating an object comprising treating the object with an effective amount of at least one inhibitor of NAD synthetase of a microbe.
• Fig. 1 depicts a step in the biosynthesis of NAD.
• Fig. 2 depicts the dose response of an inhibitor of a NAD synthetase to inhibit the growth of Bacillus subtilis.
• NAD synthetase is an enzyme which catalyzes the last step in the biosynthesis of NAD. See Figure 1.
• NAD is an essential cellular cofactor required for numerous oxidation-reduction reactions in all bacteria, in fungi and molds, and in insects. Since all of these organisms require NADs for survival and growth, inhibitors of NAD synthetase have numerous practical applications.
• the present invention provides, in an embodiment, a method for increasing production of a food animal comprising administering to the food animal an effective amount of at least one inhibitor of NADs of a microbe capable of infecting the food animal.
• the present invention provides a method for the treatment or prevention of infection by a spore-forming bacterium in an animal comprising treating an environment of the animal with an effective amount of at least one inhibitor of NADs of the spore-forming bacterium.
• the present invention provides a method for killing the vegetative cell of a spore-forming bacterium in an environment comprising treating the environment with an effective amount of at least one inhibitor of NADs of the bacterium.
• An example of a spore-forming bacterium is a biological warfare agent, e.g., Bacillus anthracis.
• the present invention provides a method for treating a fungal or bacterial disease in a plant comprising treating the plant or an environment of the plant with an effective amount of at least one inhibitor of NADs of the fungus or bacterium.
• the present invention provides a method for a treating plant comprising the treating the plant, or an environment thereof, with a pesticidal effective amount of at least one inhibitor of NADs of a pest.
• An example of the plant is a food crop.
• the present invention provides a method for disinfecting, sterilizing, or decontaminating an object comprising treating the object with an effective amount of at least one inhibitor of NADs of a microbe.
• the microbe is a microorganism, e.g., bacterium or fungus.
• An example of a fungus is mold or yeast.
• Any suitable object can be disinfected, sterilized, or decontaminated.
• suitable objects include an article of clothing, an animal, an organ of an animal, a structure, an equipment, a furniture, an environment, a food crop, a chicken, a chicken skin, and an egg, e.g., egg shell.
• the environment being disinfected, sterilized, or decontaminated can be land, air, or water, or a combination thereof.
• An example of the environment includes a medical environment.
• a medical device, medical equipment, hospital, or surgical room can be disinfected. Medical personnel also can be disinfected or decontaminated.
• medical devices such as implantable medical devices, e.g., catheters can be disinfected, sterilized, or decontaminated. Medical equipment such as a surgical equipment may also be disinfected, sterilized, or decontaminated.
• the organs of animals, including human can be disinfected or decontaminated.
• An example of an organ is the digestive tract.
• the present invention provides a method for controlling insect population in an environment comprising treating the environment with an effective amount of at least one inhibitor of NADs of the insect. Any suitable environment can be treated.
• a household environment or an agricultural environment can be treated.
• the inhibitor or antimicrobial agent may be mixed with animal feed at a typical concentration of 1-500 mg per kg of feed. Alternatively, similar concentrations may be added to the animals' drinking water. Further alternatively, the antimicrobial agent may be administered as an oral pill or may be injected, either intramuscularly or intravenously.
• the method of the present invention in an embodiment is useful in the prophylaxis or therapy of biological warfare agents, including, but not limited to, the spore-forming bacterium such as Bacillus anthracis or a microorganism carrying the virulent gene of a spore-forming bacteria such as Bacillus anthracis.
• NADs In Bacillus anthracis and other spore- forming bacteria, NADs is required for outgrowth of the germinated spore. Since inhibitors of NADs also prevent vegetative growth, this represents two different points of attack on the life cycle of these bacteria and should provide extremely effective prophylaxis and/or therapy.
• the antimicrobial agent in a suitable vehicle is sprayed onto growing plants to either prevent or treat fungal and/or bacterial diseases.
• application may be made by deposition of solutions or solid preparations on the soil near growing plants.
• NADs inhibitors as pesticides for controlling pests and insects in the household and/or for agricultural uses
• NADs inhibitors with pesticidal or insecticidal activities and in a suitable vehicle are sprayed in areas of homes that are commonly treated with existing insecticidal preparations.
• the pesticidal or insecticidal agent in a suitable vehicle is sprayed onto growing plants to either prevent or treat infestation by insects.
• pesticidal or insecticidal application to plants may be made by deposition on the soil near growing plants.
• a solution of the microbicidal compound in a suitable vehicle would be painted, sprayed, or soaked (by immersion into a solution) onto the surface of the object.
• a solution of the microbicidal agent in a suitable vehicle may be sprayed onto or soaked into the ground, or a solid form may be mixed with the soil.
• the microbicidal agent may also be added to contaminated water supplies in sufficient concentration (1-100 micromolar) to cause sterilization.
• a solution of the microbicidal compound in a suitable vehicle may be painted, sprayed, or soaked (by immersion into a solution) onto the surface of the food.
• a solution of the microbicidal compound in a suitable vehicle may be painted, sprayed, or soaked (by immersion into a solution) onto the surface of the food.
• Numerous related beneficial applications are possible, including decontamination of chicken skins, e.g., to reduce Salmonella typhimurium, egg shells (carriers of Salmonella), and disinfection of other foods.
• disinfecting and decontamination including, microbicidal concentrations of NADs inhibitors have the potential for use in a variety of situations benefiting from sterilization or decontamination, including the treatment of clothing, surfaces of structures, equipment, furniture, and natural environmental surfaces such as the ground and water supplies.
• a typical application for disinfection of implantable devices would involve soaking the device in a solution of the microbicidal compound.
• the implantable device may be manufactured to contain a releasable or bioactive form of the microbicidal compound, either by mechanical entrapment in the polymeric material composing the surface of the device or by covalent chemical attachment to the polymeric material composing the surface of the device.
• the organ may be immersed in a solution of the microbicidal agent contained in a suitable vehicle.
• Whole body washing can be accomplished by thoroughly wiping the body with a solution of the microbicidal agent, or by immersion of the body in a suitable solution.
• Control of dental caries and/or gum disease may be accomplished by washing of the oral cavity with a suitable solution of the microbicidal agent, or by incorporation into a toothpaste used in brushing the teeth.
• Numerous medical applications and devices requiring disinfection or decontamination are possible such as pacemakers, def ⁇ brillators, artificial hearts or parts thereof, whole body washing of infected patients, treatment of transplantable organs for transplantation, decontamination of surgical rooms and surgical equipment, and control of dental caries or gum disease.
• inhibitors of germination may cause damage to the spore and should be bactericidal to the vegetative cell.
• these inhibitors may be used to decontaminate a variety of environments including, but not limited to, environmental surfaces and drinking water.
• the inhibitor can be carried in a suitable vehicle and sprayed onto the plants to either prevent or treat fungal and/or bacterial diseases.
• application may be made by deposition of solutions or solid preparations on the soil near growing plants.
• any suitable inhibitor of the NADs can be used.
• suitable inhibitors of NADs include those compounds disclosed within International Publication Nos. WO 99/36422, WO
• Ri - R 7 each, independently, is H, an unsubstituted or a substituted cyclic or aliphatic group, a branched or an unbranched group; the linker is a cyclic or aliphatic, branched or an unbranched alkyl, alkenyl, or an alkynyl group; and the linker may also contain heteroatoms. In a preferred embodiment, all of R x - R 7 are not H simultaneously.
• a particular example of the inhibitor of NAD synthetase has the Structure 4:
• X is a C, N, O or S within a monocyclic or bicyclic moiety
• a and B represent the respective sites of attachment for the linker.
• X is a C or N within a monocyclic or bicyclic moiety
• R R 7 each, independently, is H, an unsubstituted or substituted cyclic or aliphatic, branched or unbranched hydrocarbon
• the linker is cyclic or aliphatic, branched or unbranched alkyl, alkenyl, or alkynyl.
• n in the above formulas is from 5 to 9, and preferably from 6 to 9.
• the linker has the formula A-(C, Heteroatom)n-B, wherein n is from 5 to 9.
• the inhibitor of NAD synthetase has the Structure 2':
• Aryl 1 is indolyl or phenyl
• Aryl 2 is phenyl, pyridinyl, indolyl, or quinolinyl
• R 1 -R 3 are independently selected from the group consisting of H, aryloxy, hydroxyaryl, aryl C C 6 alkoxy, - alkoxy, -C O alkoxycarbonyl, C C 6 alkyl, C ⁇ -C 6 alkylcarbonyl, arylcarbonyl, nitro, halo, carboxy, halo C r C 6 alkyl, perhalo C C 6 alkyl, triphenylmethoxy, phenylcarbonylamino, C C 6 alkoxycarbonyl C 2 -C 6 alkenyl, arylcarbonyl C 2 -C 6 alkenyl, benzofuranyl carbonyl, C C 6 alkylbenzylfuranyl carbonyl, arylaminocarbonyl, arylcarbonyloxy, aminocarbonyl, C ⁇ -C 6 alkoxycarbonylamino, phthalidimido, morpholino, pyr
• R 3 -R are independently H.
• Aryl 1 is indolyl. In some other embodiments, Aryl 1 is phenyl. In certain embodiments, Aryl 2 is phenyl. In certain other embodiments, Aryl 2 is pyridinyl. In further embodiments, Aryl 2 is quinolinyl. In other embodiments, Aryl 2 is indolyl.
• R ⁇ -R 3 are independently selected from the group consisting of H, phenoxy, hydroxyphenyl, benzyloxy, methoxy, methoxycarbonyl, isopropyl, butyl, acetyl, phenylcarbonyl, nitro, fluoro, carboxy, trif ⁇ uoromethyl, triphenylmethoxy, phenylcarbonylamino, methoxycarbonyl ethenyl, phenylcarbonyl ethenyl, benzofuranyl carbonyl, butylbenzylfuranyl carbonyl, phenylaminocarbonyl, phenylcarbonyloxy, aminocarbonyl, methoxycarbonylamino, phthalidimido, morpholino, pyrrolidinyl, phenylhydantoinyl, and acetylpipe
• R 1 -R 3 are independently selected from the group consisting of H, phenoxy, hydroxyphenyl, benzyloxy, acetyl, phenylcarbonyl, nitro, phenylcarbonyl ethenyl, benzofuranyl carbonyl, butylbenzylfuranyl carbonyl, phenylaminocarbonyl, phenylcarbonyloxy, aminocarbonyl, and methoxycarbonylamino.
• inhibitors of NAD synthetase has the Structure 300: Structure 300 wherein Y is C, N, O, S, ester, amide, or ketone, n is an integer of from 1 to 12, a is an integer from 1-3, and R R 5 each, independently, is H, unsubstituted or substituted cyclic group or an aliphatic group, a branched or an unbranched group, or an alkyl, alkenyl, or alkynyl, or an aryl group.
• a further example of the inhibitor of NAD synthetase has the Structure 400:
• Y is C, N, O, S, ester, amide, or ketone
• Z is C, N, O, or S
• AA is a natural or unnatural stereoisomer of an a-, ⁇ -, ⁇ -, or ⁇ -amino acid in which the carboxyl carbonyl is attached to Z, and the amino grouping may be a primary, secondary, tertiary, or quaternary ammonium compound
• n is an integer of from 1 to 12
• R R 5 each, independently, is H, unsubstituted or substituted cyclic group or an aliphatic group, a branched or an unbranched group, or an alkyl, alkenyl, alkynyl, aryl, aryl alkyl, or aryl alkoxy group.
• R R 2 may also be H, hydroxyl, ketone, nitro, amino, amidino, guanidino, carboxylate, amide, ester, sulfonate, halogen, alkoxy, or aryloxy group.
• inhibitors of NAD synthetase are 5940, 5949, 5951, 5409, 5948, 5270, 5939, 5947, 5953, and 5274:
• alkyl refers to a branched or unbranched saturated hydrocarbon group of 1 to 24 carbon atoms, such as methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, t-butyl, octyl, decyl, tetradecyl, hexadecyl, eicosyl, tetracosyl and the like.
• cycloalkyl intends a cyclic alkyl group of from three to eight, preferably five or six carbon atoms.
• alkoxy intends an alkyl group bound through a single, terminal ether linkage; that is, an “alkoxy” group may be defined as -OR where R is alkyl as defined above.
• a "lower alkoxy” group intends an alkoxy group containing from one to six, more preferably from one to four, carbon atoms.
• alkylene refers to a difunctional saturated branched or unbranched hydrocarbon chain containing from 1 to 24 carbon atoms, and includes, for example, methylene (-CH 2 -), ethylene (-CH 2 -CH 2 -), propylene (-CH 2 -CH 2 -CH 2 -), 2- methylpropylene [-CH 2 -CH(CH 3 )-CH 2 -], hexylene [-(CH 2 ) 6 -] and the like.
• cycloalkylene refers to a cyclic alkylene group, typically a 5- or 6- membered ring.
• alkene intends a mono-unsaturated or di-unsaturated hydrocarbon group of 2 to 24 carbon atoms.
• alkynyl refers to a branched or unbranched unsaturated hydrocarbon group of 2 to 24 carbon atoms wherein the group has at least one triple bond.
• cyclic intends a structure that is characterized by one or more closed rings.
• the cyclic compounds discussed herein may be saturated or unsaturated and may be heterocyclic.
• heterocyclic it is meant a closed- ring structure, preferably of 5 or 6 members, in which one or more atoms in the ring is an element other than carbon, for example, sulfur, nitrogen, etc.
• bicyclic as used herein intends a structure with two closed rings.
• the two rings in a bicyclic structure can be the same or different. Either of the rings in a bicyclic structure may be heterocyclic.
• an effective amount of a compound as provided herein is meant a sufficient amount of the compound to provide the desired treatment or preventive effect.
• the exact amount required will vary from subject to subject, depending on the species, age, and general condition of the subject, the severity of the disease that is being treated, the particular compound used, its mode of administration, and the like. An appropriate effective amount may be determined by one of ordinary skill in the art using only routine experimentation. It is preferred that the effective amount be essentially non-toxic to the subject, but it is contemplated that some toxicity will be acceptable in some circumstances where higher dosages are required.
• pharmaceutically acceptable carrier a material that is not biologically or otherwise undesirable, i.e., the material may be administered to an individual along with the compounds of the invention without causing any undesirable biological effects or interacting in a deleterious manner with any of the other components of the pharmaceutical composition in which it is contained.
• NAD synthetase enzyme is defined as the enzyme that catalyzes the final reaction in the biosynthesis of NAD, namely, the transformation of NaAD into NAD.
• catalytic sites are defined as those portions of the NAD synthetase enzyme that bind to substrates, and cofactors, including nicotinic acid adenine dinucleotide (NaAD), NAD, adenosine triphosphate (ATP), adenosine monophosphate (AMP), pyrophosphate, magnesium and ammonia in yeast.
• receptor site or "receptor subsite” relates to those portions of the yeast NAD synthetase enzyme in which the yeast NAD synthetase enzyme inhibitors disclosed herein are believed to bind.
• the terms "catalytic site,” “receptor site” and “receptor subsite” may be used interchangeably.
• inhibitors of NAD synthetase particularly for killing an yeast are: 14
• the methods of the invention comprise the use of a compound having the general structure of Structure 2 as set forth above, wherein n is an integer of from 1 to 12, R t - R 7 each, independently, is H, an unsubstituted or a substituted cyclic or aliphatic group, a branched or an unbranched group, and wherein the linker is a cyclic or aliphatic, branched or an unbranched alkyl, alkenyl, or an alkynyl group and wherein the linker may also contain heteroatoms.
• heteroatoms it is meant that one or more atoms is an element other than carbon, e.g., O, N, S, or other atoms.
• R R 7 may also be one of the following groups: an H, alkyl, alkenyl, alkynyl, or an aryl.
• Ri -R 7 may further be a hydroxyl, ketone, nitro, amino, amidino, guanidino, carboxylate, amide, sulfonate, or halogen or the common derivatives of these groups.
• n may also be an integer of from 3 to 10, more preferably 5 to 9 and, still more preferably 6 to 9.
• the tethered active molecule, e.g., in this example denoted "aryl,” moieties may be the same or different.
• the invention comprises the use of a compound of Structure 4 set forth above, wherein X is a C, N, O, or S with a monocyclic or bicyclic moiety, A and B represent the respective sites of attachment of the linker, n in an integer of from 1 to 12, Ri-R 7 each, independently, is H, an unsubstituted or a substituted cyclic group, or an aliphatic group, or a branched or an unbranched group, and the linker is a saturated or unsaturated cyclic group or an aliphatic branched or unbranched alkyl, alkenyl or alkynyl group, and wherein the linker may also contain heteroatoms.
• Ri-R 7 may also be one of the following groups: an H. alkyl, alkenyl, alkynyl, or an aryl group.
• R R 7 may also be a hydroxyl, ketone, nitro, amino, amidino, guanidino, carboxylate, amide, sulfonate, or halogen or the common derivatives of these groups.
• n may be an integer of from 3 to 10, more preferably 5 to 9 and, still more preferably 6 to 9.
• the methods of the invention comprise administering a compound of Structure 6:
• X is C, N, O or S
• Y is C, N, O, S, carboxy, ester, amide, or ketone
• a and B represent the respective sites of attachment for a linker
• n is an integer of from 1 to 12
• Ri-R 7 each, independently, is an H, unsubstituted or substituted cyclic group or an aliphatic group, a branched or an unbranched group
• the linker is a saturated or unsaturated cyclic or aliphatic group, branched or unbranched alkyl, alkenyl, or alkynyl group and wherein the linker may also contain heteroatoms.
• Ri-R 7 may also be one of the following groups: an H, alkyl, alkenyl, alkynyl, or an aryl.
• R R 7 may further be a hydroxyl, ketone, nitro, amino, amidino, guanidino, carboxylate, amide, sulfonate, or halogen or the common derivatives of these groups.
• n may also be an integer of from 3 to 10, more preferably 5 to 9 and, still more preferably 6 to 9.
• the tethered active molecule, e.g., in this example denoted "aryl," moieties may be the same or different.
• the methods of the invention comprise administering a compound of Structure 7:
• X is C, N, O or S
• Y is C, N, O, S, carboxy, ester, amide, or ketone
• a and B represent the respective sites of attachment for a linker
• n is an integer of from 1 to 12
• Ri-R ⁇ 5 each, independently, is H, unsubstituted or substituted cyclic group or an aliphatic group, a branched or an unbranched group
• the linker is a saturated or unsaturated cyclic or aliphatic group, branched or unbranched alkyl, alkenyl, or alkynyl group and wherein the linker may also contain heteroatoms.
• R R ⁇ 5 may also be one of the following groups: an H, alkyl, alkenyl, or alkynyl, or an aryl group.
• Ri-Rg may also be H, hydroxyl, ketone, nitro, amino, amidino, guanidino, carboxylate, amide, sulfonate, or halogen and the common derivatives of these groups.
• n may also be an integer of from 3 to 10, more preferably 5 to 9 and, still more preferably 6 to 9.
• the methods of the invention comprise administering a compound of Structure 8:
• n is an integer of from 1 to 12
• Ri is H, methoxy, benzyloxy, or nitro
• R 2 is 3- pyridyl, N-methyl-3-pyridyl, 3-quinolinyl, N-methyl-3 -quinolinyl, 3- (dimethylan ⁇ ino)phenyl, 3 -(trimethylammonio)phenyl, 4-(dimethylamino)phenyl, 4(trimethylammonio)phenyl, 4-(dimethylamino)phenylmethyl, or 4- (trimethylammonio)phenylmethyl.
• n may also be an integer of from 3 to 10, more preferably 5 to 9 and, still more preferably 6 to 9.
• the methods of the invention comprise administering a compound of Structure 10:
• n is an integer of from 1 to 12
• Ri is an H, CO 2 H, -OCH 3 , or -OCH 2 Ph
• R 3 is H or CO 2 H
• Y is N-linked pyxidine-3-carboxylic acid, N-linked pyridine, N-linked quinoline, or N-linked isoquinoline.
• n may also be an integer of from 3 to 10, more preferably 5 to 9 and, still more preferably 6 to 9.
• the methods of the invention comprise the use of a compound of Structure 12:
• n is an integer of from 1 to 12
• Ri is H, F, or NO 2
• R 2 is H, CH 3 , CF 3 , NO 2 , phenyl, n-butyl, isopropyl, F, phenyloxy, triphenylmethyl, methoxycarbonyl, methoxy, carboxy, acetyl, or benzoyl
• R 3 is H or CF 3
• Y is N-linked pyridine-3-carboxylic acid, N-linked pyridine, N-linked quinoline, or N-linked isoquinoline.
• n may also be an integer of from 3 to 10, more preferably 5 to 9 and, still more preferably 6 to 9.
• the methods of the invention comprise administering a compound of Structure 14 :
• n is an integer of from 1 to 12
• Ri is H, phenyloxy, isopropyl, acetyl, or benzoyl
• R 2 is H or CF 3
• Y is 3-(dimethylamino)phenyl, 3-(trimelthylammonio)phenyl, 4- (dimethylamino)phenyl, 4-(trimethylammonio)phenyl, 2-(phenyl)phenyl, diphenylmethyl, 3-pyridyl, 4-pyridyl, or pyridine-3-methyl.
• n may also be an integer of from 3 to 10, more preferably 5 to 9 and, still more preferably 6 to 9.
• the invention comprises administering compounds of the structures denoted in Tables 102-128 as Compounds 1- 274 can be synthesized utilizing the methods disclosed previously in WO 99/36422.
• Fragments I-X each represent an active molecule, as defined previously herein, which can be included in the compounds of the present invention as further described in the respective Tables.
• the point of attachment for the linker compound is at the nitrogen.
• the symbol T " or X " designates generally the presence of an anion.
• the type of anion in the compounds of this invention is not critical.
• the compounds of this invention may be comprised of any such moieties known generally to one of skill in the art or that follow from the synthesis methods disclosed in WO 99/36422.
• the methods of the invention comprise administering a compound corresponding to Structure 100:
• R' is as defined below (Illustration 1):
• n is an integer of from 1 to 12. n may also be from 3 to 10, more preferably 5 to 9 and, still more preferably 6 to 9.
• the methods of the invention comprise the use of a compound corresponding to the structures set out in Structure 100 and as further defined in Table 100.
• n may also be an integer of from 1 to 12, from 3 to 10, from 5 to 9 and, still further, from 6 to 9.
• R' corresponds to a Fragment as previously defined in Illustration 1 and n indicates the number of linker groups separating the two tethered active molecule groups in the compound.
• Fragments A - G are set out.
• the group denoted R in A-G can be a benzyl group, a methyl group or a hydrogen.
• the point of attachment of the linker group to Fragments A-G is at the nitrogen group.
• the methods of the invention comprise administering a compound corresponding to compounds of Structure 101.
• n is an integer of from 1 to 12, more preferably from 3 to 10, more preferably from 5 to 9 and, still more preferably from 6 to 9.
• the point of attachment of the linker group for both Ri and R' is at the respective nitrogen groups of each illustrated fragment.
• R' is:
• RI is:
• R group in Fragments A-G is a benzyl group, a methyl group or a hydrogen.
• the compounds may include the Fragments illustrated below (Illustration 2).
• the methods of the invention comprise the use of a compound corresponding to the structures set out in Structure 102.
• n is an integer of from 1 to 12, from 3 to 10, more preferably from 5 to 9, and still more preferably from 6 to 9.
• the compounds herein correspond to Structure 102, as further set out in Table 102.
• R' corresponds to a Fragment as previously shown in
• Illustration 1 corresponds to a Fragment as previously defined in Illustration 2, and n indicates the number of linker groups separating Groups R' and A in the respective compounds.
• Groups I, II, VII, and VIII each have a benzyl group and Groups I*, IIP, VII*, and VIII* each have a hydrogen, respectively, in the position designated R in Fragment A of Illustration 2.
• the methods of the invention comprise the use of a compound corresponding to the structures set out in Structure 104.
• n is an integer of from 1 to 12, from 3 to 10, more preferably from 5 to 9, and still more preferably from 6 to 9.
• the compounds herein correspond to Structure 104, as further set out in Table 104.
• R' corresponds to a Fragment as defined in Illustration 1
• B corresponds to a Fragment as defined in Illustration 2
• n indicates the number of linker groups separating Groups R' and B in the respective compounds.
• Groups I, VII, and VIII each have a benzyl group and Groups I*, VII*, and VIII* each have a hydrogen, respectively, in the position designated R in Fragment B of Illustration 2.
• the methods of the invention comprise the use of a compound corresponding to the structures set out in Structure 106.
• n is an integer of from 1 to 12, from 3 to 10, more preferably from 5 to 9, and still more preferably from 6 to 9.
• the compounds herein correspond to Structure 106, as further set out in Table 106.
• R' corresponds to a Fragment as previously defined in Illustration 1
• C corresponds to a Fragment as previously defined in Illustration 2
• n indicates the number of linker groups separating Groups R' and C in the respective compounds.
• Groups I, II, VII, and VIII each have a benzyl group and Groups I*, III*, VII*, and VIII* each have a hydrogen, respectively, in the position designated R in Fragment C of Illustration 2.
• the methods of the invention comprise the use of a compound corresponding to the structures set out in Structure 108.
• n is an integer of from 1 to 12, from 3 to 10, more preferably from 5 to 9, and still more preferably from 6 to 9.
• the compounds herein correspond to Structure 108, as further set out in Table 1 8.
• R' corresponds to a Fragment as previously defined in Illustration 1
• D corresponds to a fragment as previously defined in Illustration 2
• n indicates the number of linker groups separating Groups R' and D in the compound.
• Groups I, VII, and VIII each have a benzyl group and Groups I*, VII*, and VIII* each have a hydrogen, respectively, in the position designated R in Fragment D of Illustration 2.
• the methods of the invention comprise the use of a compound corresponding to the structures set out in Structure 110.
• n is an integer of from 1 to 12, from 3 to 10, more preferably from 5 to 9, and still more preferably from 6 to 9.
• the compounds herein correspond to Structure 110, as further set out in Table 110.
• R' corresponds to a Fragment as previously defined in Illustration 1
• E corresponds to a Fragment as previously defined in Illustration 2
• n indicates the number of linker groups separating Groups R' and E in the respective compounds.
• Groups I, VII, and VIII each have a benzyl group and Groups I*, VII*, and VIII* each have a hydrogen, respectively, in the position designated R in Fragment E of Illustration 2.
• the methods of the invention comprise administering a compound corresponding to the structures set out in Structure 112.
• n is an integer of from 1 to 12, from 3 to 10, more preferably from 5 to 9, and still more preferably from 6 to 9.
• the compounds herein correspond to Structure 112, as further set out in Table 112.
• R' corresponds to a Fragment as previously defined in
• Illustration 1 F corresponds to a Fragment as previously defined in Illustration 2, and n indicates the number of linker groups separating Groups R' and F in the respective 1 5 compounds.
• Groups 1, VII, and VIII each have a benzyl group and Groups I*, VII*, and VIII* each have a hydrogen, respectively, in the position designated R in Fragment F of Illustration 2.
• the methods of the invention comprise the use of a compound corresponding to the structures set out in Structure 114.
• n is an integer of from 1 to 12, from 3 to 10, more preferably from 5 to 9, and still more preferably from 6 to 9.
• the compounds herein correspond to Structure 114, as further set out in Table 114.
• R' corresponds to a Fragment as previously defined in Illustration 1
• G corresponds to a Fragment as previously defined in Illustration 2
• n indicates the number of linker groups separating Groups R' and G in the respective compounds.
• Groups I, VII, and VIII each have a benzyl group and Groups I*, VII*, and VIII* each have a hydrogen, respectively, in the position designated R in Fragment G of Illustration 2.
• the methods of the invention comprise the use of a compound corresponding to the structures set out in Structure 116.
• n is an integer of from 1 to 12, from 3 to 100, more preferably from 5 to 9, and still more preferably from 6 to 9.
• the compounds herein correspond to Structure 116, as further set out in Table 116.
• R' corresponds to a Fragment as previously defined in
• Illustration 1 corresponds to a Fragment as previously defined in Illustration 2, and n indicates the number of linker groups separating Groups R' and A in the respective compounds.
• Groups I and II each have a methyl group and Groups I* and III* each have a hydrogen, respectively, in the position designated R in Fragment A of Illustration 2.
• the method of invention comprise the use of a compound corresponding to the structures set out in Structure 118.
• n in an integer of from 1 to 12, from 3 to 10, more preferably from 5 to 9, and still more preferably from 6 to 9.
• the compounds herein correspond to Structure 118, as further set out in Table 118.
• R' corresponds to a Fragment as previously defined in Illustration 1
• B corresponds to a Fragment as previously defined in Illustration 2
• n indicates the number of linker groups separating Groups R' and B in the respective compounds.
• Groups I and II each have a methyl group and Groups I* and III* each have a hydrogen, respectively, in the position designated R in Fragment B of Illustration 2.
• the methods of the invention comprise the use of a compound corresponding to the structures set out in Structure 120.
• n is an integer of from 1 to 12, from 3 to 10, more preferably from 5 to 9, and still more preferably from 6 to 9.
• the compounds herein correspond to Structure 120, as further set out in Table 120.
• R' corresponds to a Fragment as previously defined in Illustration 1
• C corresponds to a Fragment as previously defined in Illustration 2
• n indicates the number of linker groups separating Groups R' and C in the respective compounds.
• Groups I and II each have a methyl group and Groups I*and II * each have a hydrogen, respectively, in the position designated R in Fragment C of Illustration 2.
• the methods of the invention comprise the use of a compound corresponding n Structure 122.
• n is an integer of from 1 to 12, from 3 to 10, more preferably from 5 to 9, and still more preferably from 6 to 9.
• the compounds herein correspond to Structure 122, as further set out in Table 122.
• R' corresponds to a Fragment as previously defined in Illustration 1
• D corresponds to a Fragment as previously defined in Illustration 2
• n indicates the number of linker groups separating Groups R' and D in the respective compounds.
• Groups I and II each have a methyl group and Groups I and III each have a hydrogen, respectively, in the position designated R in Fragment D of Illustration 2.
• the methods of the invention comprise administering a compound corresponding to the structures set out in Structure 124.
• n is an integer of from 1 to 12, from 3 to 10, more preferably from 5 to 9, and still more preferably from 6 to 9.
• the compounds herein correspond to Structure 124, as further set out in Table 124.
• R' corresponds to a Fragment as previously defined in
• Illustration 1 E corresponds to a Fragment as previously defined in Illustration 2, and n indicates the number of linker groups separating Groups R' and E in the respective compounds.
• Groups I and II each have a methyl group and Groups I* and III* each have a hydrogen, respectively, in the position designated R in Fragment E of Illustration 2.
• the methods of the invention comprise the use of a compound corresponding to the structures set out in Structure 126.
• n is an integer of from 1 to 12, from 3 to 10, more preferably from 5 to 9, and still more preferably from 6 to 9.
• the compounds herein correspond to Structure 126, as further set out in Table 126.
• R' corresponds to a Fragment as previously defined in Illustration 1
• F corresponds to a Fragment as previously defined in Illustration 2
• n indicates the number of linker groups separating Groups R' and F in the respective compounds.
• Groups I and II each have a methyl group and Groups P and IP each have a hydrogen, respectively, in the position designated R in Fragment F of Illustration 2.
• the methods of the invention comprise administering a compound corresponding to the structures set out in Structure 128.
• n is an integer of from 1 to 12, from 3 to 10, more preferably from 5 to 9, and still more preferably from 6 to 9.
• the compounds herein correspond to Structure 128, as further set out in Table 128.
• R' corresponds to a Fragment as previously defined in Illustration 1
• G corresponds to a Fragment as previously defined in Illustration 1
• n indicates the number of linker groups separating Groups R' and G in the respective compounds.
• Groups I and II each have a methyl group and Groups I* and IIP each have a hydrogen, respectively, in the position designated R in Fragment G of Illustration 2.
• Ph phenyl
• Ipropyl- isopropyl
• OPh ⁇ O-Phenyl isopropyl
• diNO 2 - dinifro.
• the compounds administered in the methods of the present invention correspond to compounds of the Structure 130 wherein n is an integer of from 1 to 12, from 3 to 10, from 5 to 9 and, still further, from 6 to 9. Further embodiments of the compounds corresponding to Structure 130 are set out in Table 130.
• the compounds used according to the methods of the present invention correspond to compounds of the Structure 132 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further from 6 to 9 and wherein and R is 5-H, 6-CF 3 , 5-CH 3 , 5,7-diF, 5,7-diNO 2 , 5-Butyl, 5-ipropyl, 5-Phenyl, 5-
• the compounds employed according to the methods of the present invention correspond to compounds of the Structure 134 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein R is 5-H, 6-CF 3 , 5-CH 3 , 5,7-diF, 5,7-diNO 2 ,5-Butyl, 5-iPropyl, 5- Phenyl, 5-NO 2 , 5-Trityl, 5-F, 5-OPh, 5-COPh, 5-CF 3 , 5-COCH 3 , 5-OCH 3 , 5-COOCH 3 , or 5-COOH.
• STRUCTURE 134 is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein R is 5-H, 6-CF 3 , 5-CH 3 , 5,7-diF, 5,7-diNO 2 ,5-Butyl, 5-iPropyl, 5- Phenyl, 5-NO 2 , 5-Tr
• the compounds employed according to the methods of the present invention correspond to compounds of the Structure 136 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein R is 5-H, 6-CF 3 , 5-CH 3 , 5,7-diF, 5,7-diNO 2 , 5-Butyl, 5-iPropyl, 5- Phenyl, 5-NO 2 , 5-Trityl, 5-F, 5-OPh, 5-COPh, 5-CF 3 , 5-COCH 3 , 5-OCH 3 , 5-COOCH 3 , or 5-COOH.
• STRUCTURE 136 is set out in Table 136.
• the compounds employed according to the methods of the present invention correspond to compounds of the Structure 138 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein R is 5-CF 3 , 5-OPh, 5-iPropyl, 5-COCH 3 , or 5-COPh and Y is 3-N,N- dimethylaminophenyl (3-N,N-diCH 3 ), 4-N,N-dimethylaminophenyl (4-N,N-diCH 3 ), or 2Ph.
• Further embodiments of the compounds corresponding to Structure 138 are set out in Table 138.
• STRUCTURE 138 is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein R is 5-CF 3 , 5-OPh, 5-iPropyl, 5-COCH 3 , or 5-COPh and Y is 3-N,N- dimethylaminophenyl (3-N,
• Table 138 COMPOUNDS 606-650 CORRESPONDING TO STRUCTURE 138
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 140 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein R is 5-CF 3 , 5-OPh, 5-iPropyl, 5-COCH 3 or 5-COPh, and Z is CH(Ph) 2 or 3-Pyridyl. Further embodiments of the compounds corresponding to Structure 140 are set out in Table 140.
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 142 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from
• R is 6-CF 3 , 5-OPh, 5-iPropyl, 5-COCH 3 , or 5-COPh.
• R is 6-CF 3 , 5-OPh, 5-iPropyl, 5-COCH 3 , or 5-COPh.
• the compounds administered according tO the methods of the present invention correspond to compounds of the Structure 144 wherein n is an integer of from 1 to 12, more preferably, from 3 to IO, from 5 to 9 and, still further, 1 0 from 6 to 9 and wherein R is 6-CF 3 , 5-OPh, 5-iPropyl, 5-COCH 3 , or 5-COPh. Further embodiments of the compounds corresponding to Structure 144 are set out in Table 144.
• the compounds employed according to the methods of the present invention correspond to compounds of the Structure 146 wherein n is an integer of from 1 to 12, from 3 to 10, from 5 to 9 and, still further, from 6 to 9. Further embodiments of the compounds corresponding to Structure 146 are set out in Table 146.
• STRUCTURE 146 :
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 148, as further defined in Table 148.
• the compounds employed according to the methods of the present invention correspond to compounds of the Structure 150 wherein n is an integer of from 1 to 12, from 3 to 10, from 5 to 9 and, still further, from 6 to 9. Further embodiments of the compounds corresponding to Structure 150 are set out in Table 150.
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 152 wherein n is an integer of from 1 to 12, from 3 to 10, from 5 to 9 and, still further, from 6 to 9. Further embodiments of the compounds corresponding to Structure 152 are set out in Table 152.
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 154 wherein n is an integer of from 1 to 12, more preferably, from 3 to 1O, from 5 to 9 and, still further, from 6 to 9 and wherein Z is CH(DiPh), 4-(N,N-dimethylamino) ⁇ henyl, CH 2 CH 2 -(3- ⁇ yridy ⁇ ), or (2-phenyl)-phenyl.
• STRUCTURE 154 is an integer of from 1 to 12, more preferably, from 3 to 1O, from 5 to 9 and, still further, from 6 to 9 and wherein Z is CH(DiPh), 4-(N,N-dimethylamino) ⁇ henyl, CH 2 CH 2 -(3- ⁇ yridy ⁇ ), or (2-phenyl)-phenyl.
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 156 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein R is -OCH 3 or -OCH 2 Ph. Further embodiments of the compounds corresponding to Structure 156 are set out in Table 156.
• the compounds employed according to the methods of the present invention correspond to compounds of the Structure 158 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein R is -OCH 3 or -OCH 2 Ph. Further embodiments of the compounds corresponding to Structure 158 are set out in Table 158.
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 160 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein R is -OCH 3 or -OCH 2 Ph. Further embodiments of the compounds corresponding to Structure 160 are set out in Table 160.
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 162 wherein n is an integer of from lto 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein R is -OCH 3 or -OCH 2 Ph. Further embodiments of the compounds corresponding to Structure 162 are set out in Table 162.
• the compounds employed according to the methods of the present invention correspond to compounds of the Structure 164 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein R is -OCH 3 or -OCH 2 Ph. Further embodiments of the compounds corresponding to Structure 164 are set out in Table 164.
• the compounds employed according to the methods of the present invention correspond to cohipounds of the Structure 166 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein R is -OCH 3 or -OCH 2 Ph. Further embodiments of the compounds corresponding to Structure 166 are set out in Table 166.
• the compounds used according to the methods of the present invention correspond to compounds of the Structure 168 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein R is -OCH 3 or -OCH 2 Ph. Further embodiments of the compounds corresponding to Structure 168 are set out in Table 168.
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 170 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein R is -OCH 3 or -OCH 2 Ph. Further embodiments of the compounds corresponding to Structure 170 are set out in Table 170.
• the compounds employed according to the methods of the present invention correspond to compounds of the Structure 172 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein R is -OCH 3 and -OCH 2 Ph. Further embodiments of the compounds corresponding to Structure 172 are set out in Table 172.
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 174 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein R is -OCH 3 and -OCH 2 Ph. Further embodiments of the compounds corresponding to Structure 174 are set out in Table 174.
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 176 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein Z is 3-quinoline, 3-(N,N-dimethylamino)phenyl, or 4-(N,N- dimethylamino)phenyl. Further embodiments of the compounds corresponding to Structure 176 are set out in Table 176.
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 178 wherein n is an integer of from 1 to 12, from 3 to 10, from 5 to 9 and, still further, from 6 to 9. Further embodiments of the compounds corresponding to Structure 178 are set out in Table 178.
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 180 wherein n is an integer of from 1 to 12, from 3 to 10, from 5 to 9 and, still further, from 6 to 9. Further embodiments of the compounds corresponding to Structure 180 are set out in Table 180.
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 182 wherein n is an integer of from 1 to 12, from 3 to 10, from 5 to 9 and, still further, from 6 to 9. Further embodiments of the compounds corresponding to Structure 182 are set out in Table 182.
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 184 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein and R is 6-CF 3 , 5-OPh, 5-CH(CH 3 ) 2 , 5-COCH 3 or 5-COPh. Further embodiments of the compounds corresponding to Structure 184 are set out in Table 184.
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 186 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein R is 6-CF 3 , 5-OPh, 5-CH(CH 3 ) 2 , 5-COCH 3 or 5-COPh. Further embodiments of the compounds corresponding to Structure 186 are set out in Table 186.
• the compounds employed according to the methods of the present invention correspond to compounds of the Structure 188 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein and R is 6-CF 3 , 5-OPh, 5-CH(CH 3 ) 2 , 5-COCH 3 or 5-COPh. Further embodiments of the compounds corresponding to Structure 188 are set out in Table 188.
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 190 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein R is 6-CF 3 , 5-OPh, 5-CH(CH 3 ) 2 , 5-COCH 3 or 5-COPh. Further embodiments of the compounds corresponding to Structure 190 are set out in Table 190.
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 192 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein and R is 6-CF 3 , 5-OPh 5-CH(CH 3 ) 2 , 5-COCH 3 or 5-COPh. Further embodiments of the compounds corresponding to Structure 192 are set out in Table 192.
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 194 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and R 1 is an H or -OCH 2 Ph and R 2 is H or COOCH 3 . Further embodiments of the compounds corresponding to Structure 194 are set out in Table 194.
• the compounds employed according to the methods of the present invention correspond to compounds of the Structure 196 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 198 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein R 1 is H or a -OCH 2 Ph and R 2 is H, or COOCH 3 .
• n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein R 1 is H or a -OCH 2 Ph and R 2 is H, or COOCH 3 .
• Further embodiments of the compounds corresponding to Structure 198 are set out in Table 198.
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 200 wherein n is an integer of from 1 to 12, more preferably, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein R 1 is H or a -OCH 2 Ph and R 2 is H or COOCH 3 . Further embodiments of the compounds corresponding to Structure 200 are set out in Table 200.
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 202 A.
• Further embodiments of the compounds corresponding to Structure 206 are set out in Table 206.
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 208 wherein n is an integer of from 1 to 12, from 3 to 10, from 5 to 9 and, still further, from 6 to 9 and wherein R is 4-NO 2 ; 2-CONHPh; 2-NO 2 ; 2-COCH 3 ; 3-OCH3; 4-COCH 3 ; 3-OCOPh, 2-
• the compounds employed according to the methods of the present invention correspond to compounds of the Structure 210 wherein R is NH 2 ; NMe 2 ; NMe 3 -I; NH 2 .HC1; NMe 2 .HCl. Further embodiments of the compounds corresponding to Structure 210 are set out in Table 210.
• STRUCTURE 210 is set out in Table 210.
• the compounds employed according to the methods of the present invention correspond to compounds of the Structure 212 wherein R' is PhCONH or Ph 3 C and R" is H or COOCH 3 . Further embodiments of the compounds corresponding to Structure 212 are set out in Table 212.
• the compounds administered according to the methods of the present invention correspond to compounds of the Structure 214 wherein R is 4- hydroxyphenyl or 3-hydroxy-4-methylphenyl. Further embodiments of the compounds corresponding to Structure 214 are set out in Table 214.
• Y is C, N, 0, S, ester, amide, or ketone
• n is an integer of from 1 to 12
• a is an integer from 1-3
• R ⁇ -R 5 each, independently, is an H, unsubstituted or substituted cyclic group or an aliphatic group, a branched or an unbranched group, or an alkyl, alkenyl, or alkynyl, an aryl, an arylalkyl, or arylalkoxy group.
• Ri -R 2 may also be an H, hydroxyl, ketone, nitro, amino, amidino, guanidino, carboxylate, amide, ester, sulfonate, halogen, alkoxy, or aryloxy group.
• the (CH 2 ), linker may be saturated or unsaturated and contain cyclic or aliphatic groups, branched or unbranched alkyl, alkenyl, or alkyl substituents, and wherein the linker may also contain heteroatoms.
• the aryl group is an aromatic grouping which may contain one or more rings, and the quaternary nitrogen may be part of the ring (as, for example, in pyridines and quinolines) or outside the ring (as, for example, in anilines and aminonaphthalenes).
• the value for n may also be an integer of from 3 to 10, more preferably 5 to 9 and, still more preferably 6 to 9. Specific examples include Structure 1300
• Y is C, N, 0, S, ester, amide, or ketone
• Z is C, N, 0, or S
• AA is a natural or unnatural stereoisomer of an -, ⁇ -, 7-, or ⁇ -amino acid in which the carboxyl carbonyl is attached to Z, and the amino grouping may be a primary, secondary, tertiary, or quaternary ammonium compound
• n is an integer of from 1 to 12
• R R 5 each, independently, is an H, unsubstituted or substituted cyclic group or an aliphatic group, a branched or an unbranched group, or an alkyl, alkenyl, or alkynyl, or an aryl group.
• R R 2 may also be an H, hydroxyl, ketone, nitro, amino, amidino, guanidino, carboxylate, amide, ester, sulfonate, halogen, alkoxy, or aryloxy group.
• the (CH 2 ) n linker may be saturated or unsaturated and contain cyclic or aliphatic groups, branched or unbranched alkyl, alkenyl, or.alkynyl substituents, and wherein the linker may also contain heteroatoms.
• the value for n may also be an integer of from 3 to 10, more preferably 5 to 9 and, still more preferably 6 to 9. Specific examples include Structure 1230:
• the NADs enzyme inhibitor is a compound that selectively binds with catalytic sites or subsites on a yeast NADs enzyme to reduce or eliminate the production of NAD by the yeast.
• the host is a mammal. In a further embodiment, the host is a plant.
• the compounds of the present invention can be in pharmaceutical compositions in the form of solid, semi-solid or liquid dosage forms, such as, for example, tablets, suppositories, pills, capsules, powders, liquids, suspensions, lotions, creams, gels, or the like, preferably in unit dosage form suitable for single administration of a precise dosage.
• the compositions will include, as noted above, an effective amount of the selected composition, possibly in combination with a pharmaceutically acceptable carrier and, in addition, may include other medicinal agents, pharmaceutical agents, carriers, adjuvants, diluents, and the like.
• Parenteral administration of the compounds of the present invention, if used, is generally characterized by injection.
• Injectables can be prepared in conventional forms, either as liquid solutions or suspensions, solid forms suitable for solution of suspension in liquid prior to injection, or as emulsions.
• parenteral administration includes intradermal, subcutaneous, intramuscular, intraperitoneal, iiuravenous and infrafracheal routes.
• One approach for parenteral administration involves use of a slow release or sustained release system such that a constant dosage is maintained.
• a pharmaceutically acceptable carrier which can also include a suitable adjuvant.
• the yeast NAD synthetase enzyme inhibitor compounds of the invention herein are preferably presented to animals or humans orally, rectally, intramuscularly, intravenously, infravesicularly or topically (including inhalation).
• the dosage preferably comprises between about 0.1 to about 15g per day and wherein the dosage is administered from about 1 to about 4 times per day.
• the preferred dosage may also comprise between 0.001 and 1 g per day, still preferably about 0.01, 0.05, 0.1, and 0.25, 0.5, 0.75 and 1.0 g per day.
• the dosage may be administered in an amount of about 1, 2.5, 5.0, 7.5,10.0, 12.5 and 15.0 g per day.
• the dosage may be administered at a still preferable rate of about 1, 2, 3, 4 or more times per day.
• it may be preferable to administer the compounds invention continuously, as with, for example, intravenous administration.
• the exact amount of the compound required will vary from subject to subject, depending on the species, age, weight and general condition of the subject, the particular compound used, its mode of administration and the like. Thus, it is not possible to specify an exact amount for every compound. However, an appropriate amount can be determined by one of ordinary skill in the art using only routine experimentation given the teachings herein.
• the inhibitors of NAD synthetase according to the present invention can be employed in a variety of processes for the treatment of humans, animals and plants as well as decontamination, sterilization and/or disinfectant techniques.
• the present invention further provides a method for preventing germination of spore-forming bacteria and/or the vegetative growth of bacteria, fungi and/or molds comprising administering an effective amount of at least one inhibitor of NAD synthetase, e.g. prophylactically or therapeutically, e.g., to at least one of a human, a mammal, or an animal.

Landscapes

• Life Sciences & Earth Sciences (AREA)
• Health & Medical Sciences (AREA)
• Engineering & Computer Science (AREA)
• General Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Zoology (AREA)
• Wood Science & Technology (AREA)
• Plant Pathology (AREA)
• Dentistry (AREA)
• Pest Control & Pesticides (AREA)
• Agronomy & Crop Science (AREA)
• Environmental Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• Polymers & Plastics (AREA)
• Food Science & Technology (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• General Chemical & Material Sciences (AREA)
• Epidemiology (AREA)
• Organic Chemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Microbiology (AREA)
• Communicable Diseases (AREA)
• Oncology (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Animal Husbandry (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Agricultural Chemicals And Associated Chemicals (AREA)
• Enzymes And Modification Thereof (AREA)
• Cultivation Of Plants (AREA)

Applications Claiming Priority (3)

Publications (1)

Family

ID=22814976

Family Applications (1)

Country Status (7)

Families Citing this family (10)

Family Cites Families (4)

• 2001
  • 2001-07-13 CA CA002415900A patent/CA2415900A1/en not_active Abandoned
  • 2001-07-13 JP JP2002513271A patent/JP2004510704A/ja active Pending
  • 2001-07-13 AU AU2001280548A patent/AU2001280548A1/en not_active Abandoned
  • 2001-07-13 EP EP01958943A patent/EP1301074A2/de not_active Withdrawn
  • 2001-07-13 IL IL15357501A patent/IL153575A0/xx unknown
  • 2001-07-13 WO PCT/US2001/022203 patent/WO2002007516A2/en not_active Ceased
  • 2001-07-13 BR BR0112514-1A patent/BR0112514A/pt not_active Application Discontinuation

Non-Patent Citations (1)

Also Published As

Similar Documents

Legal Events