Abstract: A stable injectable composition includes a non-aqueous parasitic agent in a therapeutically effect amount, chosen from the group of avermectin, ivermectin, doramectin, abamectin, milbemycin and moxidecting, and an antigen in combination with a liquid carrier that also acts as an adjuvant for use with warm blooded animals and a method for treating parasitic diseases and preventing bacterial and viral diseases in warm blooded animals.

Abstract: There are described novel substituted tylosin analogs and pharmaceutically acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier. Also described is a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention, and processes for the preparation of such compounds.

Abstract: A compound represented by the following general formula (I) or a salt thereof: wherein R&agr; represents a C1-C10 alkyl group, a C3-C10 alkenyl group, a C7-C15 aralkyl group, a quinolinylalkyl group, a quinolinylalkenyl group, a C2-C10 alkylcarbonyl group, a C7-C15 aralkylcarbonyl group, a C4-C7 cycloalkylcarbonyl group, benzoyl group, an imidazolylcarbonyl group and the like; R1 represents hydrogen atom, a C1-C10 alkyl group, or a C2-C10 alkylcarbonyl group; and R2 represents hydrogen atom, a C1-C10 alkyl group, or a C2-C10 alkylcarbonyl group, provided that the compound wherein R&agr; represents a C2-C10 alkylcarbonyl group and both of R1 and R2 represent a C1-C10 alkyl group is excluded.

Abstract: Water-soluble compositions comprising a lipophilic compound and a solubilizing agent of the general formula: {X—OOC—[(CH2)n—COO]m}p—Y  (I) wherein: X is a residue of a hydrophobic moiety, Y is a residue of a hydrophilic moiety, p is 1 or 2, m is 0 or 1, and n is an integer greater than or equal to 0 are disclosed. The lipophilic compound is preferably selected from the group consisting of water-insoluble ubiquinones, ubiquinols, vitamins, provitamins, polyene macrolide antibiotics, and mixtures thereof. The hydrophobic moiety is preferably a sterol or a tocopherol and the hydrophilic moiety is preferably a polyalkylene glycol. In some embodiments, the sterol is cholesterol or sitosterol, the tocopherol is &agr;-(+)-tocopherol, the polyalkylene glycol is a polyethylene glycol or its methyl monoether having an average molecular weight between 400 and 1000, p is equal to 1 or 2, m is equal to 0 or 1 and n is an integer between 2 and 18.

Abstract: A stable, palatable solution of Ivermectin in water is provided for the mass medication of animals. The present formulation does not require the use of benzyl alcohol and is stable indefinitely in the concentrated form and for up to 30 days when mixed with water.

Abstract: The present application relates to injection formulations of avermectins and milbemycins based on a solvent mixture comprising sesame oil, medium-chain triglycerides, glycol esters or fatty acid esters and a further solvent from the group consisting of mono- or polyhydric aliphatic or aromatic alcohols and their derivatives (e.g. cyclic carbonates; acetates; acetals; ketals) or castor oil.

Abstract: Avermectin derivatives represented by the general formula (I) or salts thereof: wherein —X----Y— represents —CH═CH—, —CH2—C(═O)—, —CH2—CH2—, or —CH2—CH(R13)—; for example, 1) when —X----Y— represents —CH═CH—, R1 represents (R11)(R12)C [wherein R11 represents a substituted or unsubstituted lower alkyl group; a formyl group; a lower alkoxylcarbonyl group etc.

Abstract: This invention describes novel purified and isolated nucleic acid molecules or the fragments thereof, extracted from nematode or arthropod pests or recombinant, which encode P-glycoprotein homologs and regulate resistance to the macrocyclic lactone compounds. The invention further relates to the new P-glycoprotein homolog expression product of these nucleic acids. Also described herein are methods for detecting the gene encoding for resistance to the macrocyclic lactone compounds in nematode or arthropod pests which comprise comparing the nucleic acids extracted from a pest specimen to the nucleic acids encoding for resistance and the nucleic acids encoding for susceptibility to the macrocyclic lactone compounds.

Abstract: There are described novel 4′ substituted tylosin analogs and pharmaceutically acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier. Also described is a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention, and processes for the preparation of such compounds.

Abstract: A method for treatment of bacterial infections with rifalazil administered once-weekly or twice-weekly. A method for treatment of tuberculosis caused by Mycobacterium tuberculosis, infections caused by Mycobacterium avium complex, infections caused by Chlamydia pneumoniae and infections caused by Helicobacter pylori by administering to a patient suffering from the bacterial infection 1-100 mg of rifalazil once or twice a week. In this dose regimen, the treatment is fast, efficacious and eliminates undesirable secondary symptoms observed with daily doses of 1-50 mg of rifalazil.

Abstract: Sustained-release compositions comprising a macrolide compound, a surfactant, a co-solvent, and a solvent. The sustained-release compositions of this invention may be parenterally administered to animals, and are useful for preventing or treating helminth, acarid or arthropod endo- or ectoparasitic infection or infestation in warm-blooded animals for prolonged periods of time.

Abstract: The present invention relates to mixtures of avermectins, 22,23-dihydroavermectin B1 (ivermectin) and milbemycins from the class of the macrocyclic lactones with agonists or antagonists of the nicotinergic acetylcholine receptors of insects, if appropriate in the presence of other active compounds and diluents or excipients.

Abstract: A formulation for the treatment of a parasitic skin disease includes a parasiticide to kill the parasite. The formulation also includes a polymer effective to increase retention of the formulation on the skin, and to reduce absorption of the formulation into the skin. Alternatively, the formulation may include a polymer such as a beta-sheet breaker peptide which is effective to increase absorption of the insecticide into the head lice and/or the eggs of the head lice. The formulation also includes a vehicle for the polymer and the parasiticide.

Abstract: 20,23-disubstituted mycaminosyltylonolide derivatives and use of the same in the field of the prophylaxis and treatment of pasteurellosis are disclosed. The di-substituents are peperidino optionally substituted with one or two methyl groups. The derivatives have selective antibacterial activity against Pasteurella.

Abstract: The use of compounds of the milbemycin class as inhibitors of efflux pumps in microbes or other cells is described, along with pharmaceutical compositions incorporating a milbemycin. Also described is a method of screening for compounds which inhibit a CDR1, CDR2, BEN, or FLU1 efflux pump or a pump with components having a high level of protein level sequence similarity with the components of those efflux pumps.

Abstract: A parasiticidal formulation is provided. This formulation includes a pyrrolidone solvent, a bridging solvent, and an parasiticidal agent. One or more parasiticidal agents may be included in the formulation. Preferably, the formulation contains both closantel and ivermectin. Another aspect of the present invention is a method of making this parasiticidal formulation. This method includes mixing a pyrrolidone solvent and a bridging solvent to form a solvent solution and adding one or more parasiticidal agents to the solvent solution. A further aspect of the present invention is a method for administering the parasiticidal formulation of the present invention to an animal. This method of administration includes providing the parasiticidal formulation described above and applying this formulation to the skin of an animal, wherein the formulation is absorbed through the animal's skin.

Abstract: An anthelmintic composition including an Antibiotic S541 compound or a chemical derivative thereof, together with an insoluble anthelmintic compound. The composition is stabilized by between about 0.15% and about 5.0% of an antioxidant by weight of the total composition.

Abstract: A method of eliminating, reducing or preventing parasites in a fish population is provided by feeding emamectin or a salt thereof to the fish population at a daily dose of 25 &mgr;g to 400 &mgr;g per kg of fish biomass per day for a period of 3-14 days. Also provided is a kit for preparing a medicated fish feed for eliminating, reducing or preventing parasites in a fish population, the kit having a supply of emamectin or a salt thereof and printed instructions for feeding the emamectin or emamectin salt at a daily dose of 25 &mgr;g to 400 &mgr;g per kg of fish biomass per day for a period of 3-14 days.

Abstract: The invention concerns a method and a composition against parasites and particularly ectoparasites and, preferably also endoparasites of small mammals and in particular dogs and cats. The composition contains a compound (A) of formula (I) and a compound (B) consisting of an endectoparasiticide of the macrocylic lactone type.

Abstract: The present application relates to injection formulations of avermectins and milbemycins based on a solvent mixture comprising sesame oil, medium-chain triglycerides, glycol esters or fatty acid esters and a further solvent from the group consisting of mono- or polyhydric aliphatic or aromatic alcohols and their derivatives (e.g. cyclic carbonates; acetates; acetals; ketals) or castor oil.

Abstract: An active ingredient combination for the simultaneous control of ecto- and endoparasites, especially mites, ticks and nematodes, on productive livestock, domestic animals and pets, is described, which comprises the active ingredients (1) 1-[4-chloro-3-(3-chloro-5-trifluoromethyl-2-pyridyloxy)phenyl]-3-(2,6-difluorobenzoyl)urea and (2) a compound of formula (i)  wherein R1 is hydrogen or one of radicals R2 is —CH(CH3)—CH3, —CH(CH3)—C2H5, —C(CH3)═CH—CH(CH3)2 or cyclohexyl; R3 is hydrogen or hydroxy if the bond between atoms 22 and 23 represents a double bond, or is hydrogen or the group ═N—O—CH3 if a single bond is present between atoms 22 and 23; and R4 is HO— or HO—N═, in free form or in the form of a physiologically acceptable salt.

Abstract: Bicyclic leucomycins and pharmaceutically acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier, a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention, and processes for the preparation of such compounds.

Abstract: The present invention discloses compositions and methodologies for the utilization of probiotic organisms in therapeutic compositions. More specifically, the present invention relates to the utilization of one or more species or strains of lactic acid-producing bacteria, preferably strains of Bacillus coagulans, for the control of gastrointestinal tract pathogens, including antibiotic-resistant gastrointestinal tract pathogens, and their associated diseases by both a reduction in the rate of colonization and the severity of the deleterious physiological effects of the colonization of the antibiotic-resistant pathogen. In addition, the present invention relates to the utilization of therapeutic compounds comprised of lactic acid-producing bacteria and anti-microbial agents such as antibiotics, anti-fungal compounds, anti-yeast compounds, or anti-viral compounds.

Abstract: The invention relates to the use of cosmetic and dermatological formulations having

Abstract: The present invention provides novel sixteen-membered macrolide compounds that are useful as anti-infective agents or as intermediates thereto. The present invention also provides methods for the preparation of these compounds, and methods and formulations for their use. In one aspect of the present invention, sixteen-membered macrolide possessing a side chain Z are provided where Z is aliphatic, aryl, alkylaryl, halide, ═NOR3, ═NNHR3, or —W—R3 where W is O, S, NC(═O)R4, NC(═O)OR4, NC(═O)NHR4 or NR4 where R3 and R4 are each independently hydrogen, aliphatic, aryl or alkylaryl. In another aspect of the present invention, bicyclic compounds are provided where one of the cyclic-components is a sixteen-membered macrolide and the other is a cyclic moiety whose cyclic structure is formed by between 3 and 10 atoms. In another aspect of the present invention, sixteen-membered macrolide compounds that bind to the domain II region of the 23S RNA are provided.

Abstract: In particular this invention provides for spot-on compositions for the treatment or prophylaxis of parasite infestations in mammals or birds which comprise: (1) a composition comprising (A) an effective amount of a 1-phenylpyrazole derivative; and/or (B) an effective amount of a macrocyclic lactone antihelmintic or antiparasitic agent; (2) an acceptable liquid carrier vehicle; and (3) optionally, a crystallization inhibitor. The invention also provides for a method of treating parasitic infestations or for the prophylaxis of parasite infestations in mammals or birds which comprises topically applying to said mammal treating parasitic infestations or for the prophylaxis of parasite infestations in mammals or birds which comprises topically applying to said mammal or bird an effective amount of a composition according to the present invention.

Abstract: An improved termite bait composition comprises a powdered cellulosic attractant having a particle size in the range of approximately 1 to 100 micrometers and a termite killing agent. Also disclosed are a method for controlling termites by applying the termite bait composition to a termite infested area and a termite bait composition package for use in a termite bait station comprising the termite bait composition contained within a termite attractive package.

Abstract: The present invention is directed to a pesticidal composition of a water-soluble pesticide and processes for its manufacture. More specifically, the invention relates to a soluble granule (SG) pesticidal formulation comprising a water-soluble pesticide and a water-soluble filler. The present invention provides a pesticidal formulation with efficacy equal to the corresponding liquid formulation, yet with improved handler safety, such as lower eye irritation.

Abstract: Compounds of the formula: wherein X represents a single or a double bond; R1 is H or OH; provided that when X is a single bond, R1 is H or OH, and when X is a double bond, R1 is absent; R2 is H, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, alkoxy-alkyl or alkylthioalkyl containing from 1 to 6 carbon atoms in each alkyl or alkoxy group, wherein any of said alkyl, alkoxy alkenyl or alkynyl groups may be substituted by one or more halo atoms; or a C3-C8 cycloalkyl or C5-C8 cycloalkenyl group, either of which may be substituted by methylene or one or more C1-C4 alkyl groups or halo atoms; or a 3 to 6 membered oxygen or sulphur containing heterocyclic ring which may be saturated, or fully or partially unsaturated and which may be substituted by one or more C1-C4 alkyl groups or halo atoms; or a group of the formula SR5 wherein R5 is C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C3-C8 cycloalkyl, C5-C8 cycloalkenyl, phenyl or substituted phenyl wherein the substituent is C1-C4 alkyl, C1-C4 alkoxy or

Abstract: Antibacterial compositions comprising (1) a rifamycin derivative represented by the formula (I) or its physiologically acceptable salt, and (2) a proton pump inhibitor (a) or a bismuth preparation (b) wherein the components (1) and (2) are used in such amounts as producing a synergistic effect against Helicobacter pylori, drugs and remedies for digestive organ diseases which contain the antibacterial compositions, process for producing them, and pharmaceutical preparations related to the antibacterial compositions. The compositions can be administered to patients with digestive diseases caused by infection of Helicobacter pylori in a smaller dose and at a lower administration frequency as compared with conventional remedies.

Abstract: The present invention relates to a process for the production of clarithromycin from an aqueous medium in anhydrous form and in the form of a hydrate.

Abstract: A parasiticidal formulation is provided. This formulation includes a pyrrolidone solvent, a bridging solvent, and an parasiticidal agent. One or more parasiticidal agents may be included in the formulation. Preferably, the formulation contains both closantel and ivermectin. Another aspect of the present invention is a method of making this parasiticidal formulation. This method includes mixing a pyrrolidone solvent and a bridging solvent to form a solvent solution and adding one or more parasiticidal agents to the solvent solution. A further aspect of the present invention is a method for administering the parasiticidal formulation of the present invention to an animal. This method of administration includes providing the parasiticidal formulation described above and applying this formulation to the skin of an animal, wherein the formulation is absorbed through the animal's skin.

Abstract: A parasiticidal formulation is provided. This formulation includes a pyrrolidone solvent, a bridging solvent, and an parasiticidal agent. One or more parasiticidal agents may be included in the formulation. Preferably, the formulation contains both closantel and ivermectin. Another aspect of the present invention is a method of making this parasiticidal formulation. This method includes mixing a pyrrolidone solvent and a bridging solvent to form a solvent solution and adding one or more parasiticidal agents to the solvent solution. A further aspect of the present invention is a method for administering the parasiticidal formulation of the present invention to an animal. This method of administration includes providing the parasiticidal formulation described above and applying this formulation to the skin of an animal, wherein the formulation is absorbed through the animal's skin.

Abstract: The invention relates to certain stable microsphere compositions containing a fat, a wax or a mixture thereof; an active ingredient selected from LL-F28249&agr;-&lgr; compounds, 23-oxo or 23-imino derivatives of LL-F28249&agr;-&lgr; compounds, milbemycin compounds and avermectin compounds; an antioxidant and, optionally, an oil, a semi-soft fat, a fatty acid derivative or mixture thereof. The invention also relates to a method for introducing and maintaining levels of the active compound in the blood of warm-blooded animals for extended periods of time and for the prevention or treatment of infections and infestations caused by helminths, nematodes, acarids and endo- and ectoparasitic arthropods in warm-blooded animals by the parenteral administration of compositions of the invention.

Abstract: A method for treatment of bacterial infections with rifalazil administered once-weekly or twice-weekly. A method for treatment of tuberculosis caused by Mycobacterium tuberculosis, infections caused by Mycobacterium avium complex, infections caused by Chlamydia pneumoniae and infections caused by Helicobacter pylori by administering to a patient suffering from the bacterial infection 1-100 mg of rifalazil once or twice a week. In this dose regimen, the treatment is fast, efficacious and eliminates undesirable secondary symptoms observed with daily doses of 1-50 mg of rifalazil.

Abstract: Methods of modulating the export of a leaderless protein from a cell by contacting the cell with a compound that alters the binding of the leaderless protein and a transport molecule are provided. Transport molecules include gastrin binding protein/alpha subunit of mitochondrial fatty acid &bgr;-oxidation multienzyme complex (p70, GenBank Accession Nos. U04627/D16480), phosphotyrosine-independent ligand of the SH2 domain of p56lck (p62, GenBank Accession No. U46751), mitochondrial fatty acid &bgr;-oxidation trifunctional protein &bgr; subunit (TP-&bgr;) (p48, GenBank Accession No. D16481), actin related protein 3 (Arp3) (p48, GenBank Accession No. U29610), K-glypican (GenBank Accession No. X83577), tubulin (p50, GenBank Accession No. AF081484) and related polypeptides that are functionally equivalent in their role as leaderless protein trafficking components. Leaderless proteins include, for example, FGF-1, FGF-2, IL-1&agr;, IL-1&bgr;, CNTF, MIF, and HIV tat.

Abstract: This invention provides methods of inhibiting the export of a leaderless protein from a cell by contacting the cell with a cardiac glycoside or aglycone derivative. Leaderless proteins include FGF-1, FGF-2, IL-1&agr;, IL-1&bgr; and factor XIIIa. These methods are useful in treatment of conditions, including tumors and diabetes.

Abstract: A method for treating Pediculosis capitis infestation in a human patient which comprises orally administering to the human a total amount of ivermectin of between about 400 ug/kg and about 1200 ug/kg over a period of time of about one week, wherein equal portions of the total amount are administered according to an administration sequence selected from the group consisting of c) a first day and a second day, and d) a first day, a second day and a third day, during the one week time period. The invention is also a method for treating Pediculosis capitis infestation in a human patient which comprises orally administering to the human a total amount of ivermectin of between about 6 mg and 135 mg over a period of time of about one week, wherein equal portions of the total amount are administered according to an administration sequence selected from the group consisting of e) a first day and a second day, and f) a first day, a second day and a third day, during the one week time period.

Abstract: The present invention is drawn to a long acting injectable parasiticide composition comprising ivermectin in a 1% (w/w) concentration, benzilic alcohol, polyvinyl pyrrolidone, N-methyl-2-pyrrolidone in proportion of 40-65% (v/w) of the total formulation. The present invention is further drawn to methods of making using and using thereof.

Abstract: The present invention provides a method for controlling fungal growth, mycotic infections, yeast infections and parasitic infections using a therapeutically effective amount of a compound selected from Compounds (I-V). Further provided is a method for providing mdr inhibition using a therapeutically effective amount of a compound of formula (IA). Also provided is an antifungal composition comprising at least five percent (5%) by weight of a compound selected from Compounds (I-V).

Abstract: An antiparasitic medication for controlling and treating a wide variety of parasites in a herbivorous domesticated animal. The antiparasitic medication contains a mixture of ivermectin in a base of an alfalfa derivative. The antiparasitic medications are provided as pellets or fine granules or powders or other suitable feed application to avoid the use of injections in the animal, and to avoid stress and dangerous administration practices that could cause severe injury to both the care giver and the animal.

Abstract: A veterinary composition containing an effective amount of praziquantel, an effective amount of at least one macrolide anthelmintic selected from the group comprising the avermectins and the milbemycins, and a suitable organic solvent selected from the group consisting of glycerol formal, ethyl lactate, benzyl alcohol and N-methyl-2-pyrrolidone and the like wherein the composition is suitable for administration to warm-blooded non-human animals. The composition may be a solution or a paste and may be administered to the recipient animal by injection, drench or as an oral paste. A method of treating endo- and ectoparasites in non-human animals is also claimed.

Abstract: Gastrointestinal disorders involving Helicobacter pylorid are treated by administering spiramycin or spiramycin/metronidazole combinations. In addition, administration of anti-ulcer agents may be carried out before, during or after such administration of spiramycin or spiramycin/metronidazole combinations. Pharmaceutical compositions for such administrations are also disclosed.

Abstract: The present invention relates to mixtures of avermectins, 22,23-dihydroavermectins B.sub.1 (ivermectins) and milbemycins from the class of the macrocyclic lactones in combination with cyclic depsipeptides, optionally in the presence of praziquantel or epsiprantel, for increasing the endoparasiticidal action in endoparasiticidal compositions.

Abstract: This invention provides methods of inhibiting the export of a leaderless protein from a cell by contacting the cell with a cardiac glycoside or aglycone derivative. Leaderless proteins include FGF-1, FGF-2, IL-1.alpha., IL-1.beta. and factor XIIIa. These methods are useful in treatment of conditions, including tumors and diabetes.

Abstract: Methods of inhibiting the export of a leaderless protein from a cell by contacting the cell with a compound that inhibits the binding of the leaderless protein and a transport molecule are provided. Leaderless proteins include FGF-1, FGF-2, IL-1.alpha., IL-1.beta., CNTF and HIV-tat. These methods are useful in treatment of various conditions, including tumors and diabetes.

Abstract: This invention provides methods of inhibiting the export of a leaderless protein from a cell by contacting the cell with a cardiac glycoside or aglycone derivative. Leaderless proteins include FGF-1, FGF-2, IL-1.alpha., IL-1.beta. and factor XIIIa. These methods are useful in treatment of conditions, including tumors and diabetes.

Abstract: The present invention is drawn to injectable parasitical compositions comprising ivermectin in a 1% (w/w) concentration, benzyl alcohol, polyvinyl pyrrolidone, between 40-65% (v/w) concentration N-methyl-2-pyrrolidone, adjuvants and glycerin until reaching 100% final weight, and methods of making and using the composition.

Abstract: A method of therapy wherein there is administered to a person in need of such therapy a pharmacologically effective amount of a rupununine having the formula: ##STR1##

Abstract: The invention is directed to the use of tilmicosin and other compounds of U.S. Pat. No. 4,820,695 for the treatment of viral infection in swine.