Abstract: There are described novel 11-O-substituted ketolide derivatives of clarithromycin 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: The invention is directed to biologically active lipophilic compositions comprising a biologically active covalently attached to, or encapsulated within, a lipid. Preferably, a biologically active agent is both covalently attached to a lipid and encapsulated within a lipid composition. Preferred lipid components include triglycerides and fatty acids. The resulting composition is preferably adapted for oral administration.

Abstract: There are provided granules having a good taking property wherein an active ingredient, at least one kind of soluble additive having an average particle size of smaller than 50 &mgr;m and at least one kind of disintegrator are contained.

Abstract: The invention relates to novel compounds from the class of the macrolide antibiotic oleandomycin of the general formula (I) wherein R1 has the individual meaning of —CH2CH3 group, of a fragment of the formula (II), together with R2 has the meaning of a fragment of the formula (III) or together with R4 has the meaning of a fragment of the formula (IV) or a fragment of the formula (V) R2 together with R3 has the meaning of a ketone or together with R1 has the meaning of a fragment of the formula (III), R3 has the individual meaning of OH group or together with R2 has the meaning of a ketone, R4 has the individual meaning of a methyl group, or together with R1 has the meaning of a fragment of the formula (IV) or of a fragment of the formula (V), R5 has the individual meaning of hydrogen or a benzyloxycarbonyl group, R6 has the individual meaning of hydrogen, a methyl group or a benzyloxycarbonyl group, to intermediates for the preparation thereof, to a process for

Abstract: Improved daily ration mammal feeds are provided which include minor amounts of heartworm preventative drugs, ensure that a mammal consuming the feed receives quantities of drug sufficient to establish and maintain substantially constant concentrations of the drug in the pet's bloodstream. The feeds may be produced by extrusion with addition of minor quantities of heartworm preventative drug so as to uniformly distribute the drug throughout the extruded product. Ivermectin levels of from about 2-1500 &mgr;g/kg of extruded feed are preferred.

Abstract: Synergistic combinations of a squalene epoxidase inhibitor such as terbinafine and a macrolide T-cell immunomodulator or immunosuppressant such as 33-epichloro, 33-desoxyascomycin are provided, which are useful in particular in the treatment of diseases involving fungal or suspected fungal infection, for immunomodulation or immunosuppression in conditions in which fungal or suspected fungal colonisation of e.g. the skin plays a role, such as atopic dermatitis and seborrhoeic dermatitis, and in situations of fungal resistance.

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: There are described novel 4′substituted 16-membered macrolides and pharmaceutically acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier.

Abstract: Improved ivermectin-containing daily ration extruded feeds for domesticated household pets such as cats and dogs are provided so that a pet consuming the feeds receives quantities of ivermectin sufficient to establish and maintain substantially constant concentrations of the drug in the pet's bloodstream. The feeds are produced by extrusion with addition of minor quantities of ivermectin so as to uniformly distribute the drug throughout the extruded product. Ivermectin levels of from about 2-1500 &mgr;g/kg of extruded feed are preferred.

Abstract: Disclosed are multibinding compounds which include macrolide antibiotics, aminoglycosides, lincosamides, oxazolidinones, streptogramins, tetracycline and/or other compounds at which bind to bacterial ribosomal RNA and/or to one or more proteins involved in ribosomal protein synthesis in the bacterium, which are useful in treating bacterial infections. The compounds adversely affect protein expression and have an antibacterial effect. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is macrolide antibiotic, aminoglycoside, lincosamide, oxazolidinone, streptogramin, tetracycline or other compound which binds to bacterial ribosomal RNA and/or one or more proteins involved in ribosomal protein synthesis in the bacterium.

Abstract: The invention relates to insecticidal mixtures of spinosyns and agonists or antagonists of nicotinic acetylcholine receptors for protecting plants against attack by pests.

Abstract: Aqueous antibiotic compositions comprising a mixture of an azalide compound, propylene glycol, and one or more acids, and methods for preparing such compositions, are disclosed.

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: There is disclosed the formulation of a poorly soluble macrolide antibiotic, such as clarithromycin together with &bgr;-cyclodextrin, and optionally a dicarboxylic acid wherein the particles of the formulation are prepared using microfluidization techniques in a particle size in the range of from 5 to 15 microns.

Abstract: The invention involves methods and materials for treating and preventing non-invasive fungus-induced mucositis. Specifically, the invention involves administrating an antifungal agent such that it contact mucus in an amount, at a frequency, and for a duration effective to prevent, reduce, or eliminate non-invasive fungus-induced rhinosinusitis. This invention also provides methods and materials for diagnosing non-invasive fungus-induced rhinosinusitis and culturing non-invasive fungus from a mammalian mucus sample as well as specific antifungal formulations and medical devices for treating and preventing non-invasive fungus-induced rhinosinusitis. In addition, the invention provides methods and materials for treating and preventing other non-invasive fungus-induced mucositis conditions such as chronic otitis media, chronic colitis, and Crohn's disease. Further, the invention involves methods and materials for treating and preventing chronic asthma symptoms.

Abstract: The invention relates to cosmetic and dermatological formulations having a) a content of a compound or several compounds from the group consisting of flavonoids, or having b) a content of an active compound combination comprising a compound or several compounds chosen from the group consisting of flavonoids in combination with a compound or several compounds chosen from the group consisting of cinnamic acid derivatives and c) if appropriate an additional content of a compound or several compounds from the group consisting of antioxidants.

Abstract: The present invention relates to combined preparations comprising a morpholinyl anthracycline administered in combination anticancer agents chosen from an allylating agent, an antimetabolite, a topoisomerase II inihbitor, a topoisomerase I inhibitor, an antimitotic drug and a platinum derivative, which are useful anticancer therapy, particularly in the treatment of a primary or metastatic liver cancer.

Abstract: The present invention relates to composition and methods for administering compositions in solutions for killing adult lice and the ova comprising water, PVM/MA Decadiene crosspolymers, propylene glycol, a mixture of cetyl and stearyl alcohols, Ceteareth-20; stearlkonium chloride; benzyl alcohol; hexylene glycol; pentylene glycol, isopropyl alcohol; a mixture of spinosyn A and spinosyn D in a weight ratio of 80:20, BHT; and sodium hydroxide.

Abstract: Disclosed is an oral controlled release macrolide pharmaceutical formulation. In a preferred embodiment, the formulation comprises a citrate salt of a preferred macrolide, clarithromycin. Also disclosed are methods for preparing, isolating and characterizing soluble and stable citrate salt of macrolides and use thereof in all solid dosage forms of macrolides.

Abstract: An antibiotic product for delivering at least Amoxicillin or Clarithromycin that is comprised of three dosage forms with different release profiles with each of Amoxicillin and Clarithromycin being present in at least one of the dosage forms.

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: Compositions having synergistic effective amounts of one or more antibacterial agents, a nitroimidazole, and an antifungal agent effective against a Candida species. The compositions are particularly useful in the treatment of genitourinary infections.

Abstract: A stable derivative of apoptolidin retains sufficient potency to be useful as an antitumor drug.

Abstract: Compound JK represented by the general formula (1): 1

Abstract: The invention relates to processes for preparing compounds of formula 1 1

Abstract: A kit for treating acne vulgaris are disclosed. The treatment includes topical application of a dermatological composition containing an avermectin compound to the affected areas of a patient alone, or in conjunction with other conventional methods of treating acne vulgaris. The dermatological composition of the kit contains an avermectin compound in a pharmaceutically acceptable carrier, including water, glycols, alcohols, lotions, creams, gels, emulsions, sprays, soaps, body washes, facial cleansers, and facial masks.

Abstract: A local injection prescription that disperses a malignant tumor to decrease the size of the tumor or terminate the tumor. The local injection prescription is produced by dissolving an organic compound having a lactone nucleus in lower alcohol and water.

Abstract: The present invention relates to methods of providing crystalline and crystal-like forms of daptomycin, a lipopeptide antibiotic with potent bactericidal activity against gram-positive bacteria, including strains that are resistant to conventional antibiotics. The present invention relates to methods of purifying daptomycin.

Abstract: Non-naturally-occurring compositions for use in amelioration of disruption of energy metabolism secondary to stress are described. These compositions comprise a flavonoid or derivative thereof and a synergist. Synergists include, but are not limited to, amino acids, carbohydrates, carnitines, flavonoids, nucleosides, and tocopherols and/or derivatives thereof. Methods of making these compositions and methods of ameliorating disruption of energy metabolism secondary to stress, comprising administering such synergistic compositions, are also disclosed.

Abstract: The present invention provides two new classes of polyene macrolide amide derivatives useful for treating or preventing fungal infections. The new polyene macrolide amide derivatives exhibit antifungal activity and are more water-soluble than conventional polyene antibiotics, such as amphotericin B and amphotericin B methyl ester.

Abstract: The invention provides a method of treating or preventing rosacea, comprising topical administration, of a pharmaceutical preparation comprising a nonsteroidal anti-inflammatory drug (NSAID).

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: A pharmaceutical composition comprising at least one antifungal agent and at least one chelator, and a method for administering the pharmaceutical composition to a patient having a fungal infection. Another aspect provides a pharmaceutical composition comprising at least one chelator, at least one antifungal agent and at least one monoclonal antibody, wherein the monoclonal antibody is operatively attached to the chelator, and a method of administering this composition to a patient having a fungal infection.

Abstract: Antibiotic compositions comprising an equilibrium mixture of azalide isomers, water, and one or more acids, and methods for preparing such compositions, are disclosed. The antibiotic compositions can be advantageously stabilized by adding one or more water-miscible co-solvents. In a preferred embodiment, the one or more co-solvents is propylene glycol.

Abstract: Acne-affected skin has been found to be accompanied by the presence of matrix-degrading enzymes such as MMPs and neutrophil elastase, induction of neutrophils, and a reduction in procollagen biosynthesis. This invention treats scarring and inflammation accompanying acne by administering, topically or systemically, at least one of (i) an inhibitor of the matrix degrading enzymes and (ii) a cytokine inhibitor that alleviates inflammation and thus also alleviate neutrophil infiltration. Alleviating the matrix degradation and renormalizing procollagen biosynthesis allows for reduced inflammation and better natural repair of acne-affected skin. Inhibiting cytokines alleviates induction of MMPs in resident skin cells, and also alleviates inflammation with its concommitant induction of neutrophils from the blood stream bringing MMPs and elastase into the acne lesion.

Abstract: The invention provides novel erythromycin derivatives in which methyl groups on the macrolactone ring have been substituted with —H, -Et, and/or —OH. The invention also provides reagents such as isolated polynucleotides, vectors comprising the polynucleotides and host cells transformed with the vectors for making the novel compounds. Methods for making the compounds utilizing genetic engineering techniques are also disclosed.

Abstract: Mammalian hair growth is reduced by applying an inhibitor of telomerase to the skin.

Abstract: The present invention is directed to methods for preventing or treating inflammatory bowel disease by administering a composition comprising a therapeutically or prophylactically effective amount of a composition comprising between about 60% to 90% iduronylglycosaminoglycan sulfate and between about 10% to 40% dermatan sulfate, or a pharmaceutically acceptable salt, solvate, hydrate, or clathrate thereof. In a particular embodiment, a therapeutically or prophylactically effective amount of a composition comprising sulodexide, or a pharmaceutically acceptable salt, solvate, hydrate, or clathrate thereof is administered. The composition to be administered may also comprise one or more additional active ingredients selected from the group consisting of steroids, aminosalicylates, short-chain fatty acids, thioguanine derivatives, antibiotics, biological agents, antidepressants, and pain-relievers.

Abstract: A method for treating a human patient includes screening for Crohn's disease by simultaneously contacting a human serum sample with an antigen composition comprising a 35 kD protein expressed by a recombinant p35 clone specific to sera from Johne's disease and a 36 kD protein expressed by a recombinant p36 clone specific to sera from Crohn's disease. A bound antibody-antigen complex to the antigen composition is detected, the bound antibody-antigen complex detecting a presence of Mycobacterium avium ss. paratuberculosis (MAP). If the screening results are positive, the patient is administered a regimen of an antibiotic effective in and sufficient for eradicating a presence of MAP. Preferably a probiotic and specific carbohydrate diet are also administered. In a related method Crohn's disease is screened for by performing an ELISA analysis for serum antibodies to MAP, and, for patients screening positive for MAP, the antibiotic regimen is administered.

Abstract: A composition is provided that has a viscosity of less than about 15,000 cP and a pH of about 3.0 to 9.0 for treating a skin disorder in a human subject. The composition is a lotion that consists essentially of (a) a therapeutically-effective amount of at least one compound useful for treating such disorder, (b) a pharmaceutically-acceptable, lightly cross-linked polyacrylic acid polymer compatible with the compound, (c) a pharmaceutically acceptable base to adjust pH, (d) up to about 25% ww of at least one water miscible solvent, (e) optionally a preservative, (f) water, and (g) an oil phase component and suitable surfactant. The composition is useful for treating an inflammatory skin disorder, acne, or rosacea.

Abstract: The invention relates to compounds of the general formula 1

Abstract: The present invention provides novel soy formulations comprising 3-23 milligrams of at least one isoflavone per gram of the formulation. The soy formulations may additionally comprise 0.4 to 1.2 grams of protein per gram of the formulation. In another aspect, the present invention provides novel soy formulations comprising diadzin, genistin and glycitin in a ratio of 3:1:2 to 3:4.5:1, preferably approximately 2:1:1 such that diadzin is a major isoflavone component. The present invention further provides dietary supplements and food products comprising a soy formulation of the present invention. In another aspect the present invention provides pharmacological compositions comprising a soy formulation of the present invention. The pharmacological compositions may additionally comprise a medicinal composition.

Abstract: The invention relates to a novel pharmaceutical composition comprising an effective amount of bio-active fraction from cow urine distillate as a bioavailability facilitator and pharmaceutically acceptable additives selected from anticancer compounds, antibiotics, drugs, therapeutic and nutraceutic agents, ions and similar molecules which are targeted to the living systems.

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: This invention relates to compounds of formula (1) and to pharmaceutically acceptable salts thereof. The compounds of formula (1) are potent antibacterial agents that may be used to treat various bacterial infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula (1) and to methods of treating bacterial infections by administering the compounds of formula (1). The invention also relates to methods of preparing the compounds of formula (1) and to intermediates useful in such preparation.

Abstract: The present invention relates to methods and compositions for inhibiting cell survival and/or promoting cell death following exposure to cytotoxic agents and stress such as radiation or chemotherapy exposure through inhibition of V-H+-ATPase. In particular, the formation and/or acidification of acidic vesicular organelles (AVOs) may be prevented or decreased by inhibiting the activity of vacuolar proton ATPase (“V-H+-ATPase”). The methods and compositions of the invention are based on the observation that (i) following irradiation surviving cancer cells accumulate AVOs and that their acidification is mediated by V-H+-ATPase; (ii) surviving colonies of cells contain higher levels of AVOs; and (iii) inhibition of V-H+-ATPase decreases the clonogenic survival of cells irradiated or exposed to chemotherapeutic agents. These observations led to the conclusion that V-H+-ATPase activity and AVO function serve to protect cells from radiation and chemotherapy damage.

Abstract: Compounds and compositions for stabilizing microtubules are disclosed. Also disclosed are methods of inhibiting, preventing, regulating, modulating, attenuating, stabilizing, or affecting microtubule formation or function. Methods of treating, preventing or inhibiting diseases and disorders associated with microtubule formation, function, or both by administering a microtubule stabilizing agent such as coumarin is also disclosed.

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: Long-acting antiparasitic formulations of doramectin, suitable for injection, are described herein.

Abstract: Macrolide compounds produced by culturing Saccharopolyspora species LW107129 (NRRL 30141) have insecticidal and acaricidal activity and are useful intermediates for preparing spinosyn analogs.