Abstract: A method of treating a urinary tract fungal infection in a human comprising systemically administering a therapeutically effective amount of a liposomal polyene including nystatin and amphotericin wherein the fungal infection is selected from the group consisting of aspergillosis, candidiasis (e.g., C. parapsilosis, C. albicans, C. tropicalis, C. glabrata, C. lusitaniae), zygomycosis, cryptococcosis, histoplasmosis, blastomycosis, cladosporiosis, fusariosis, Bipolaris hawaiiensis, Dactylaria gallopava, torulopsosis, Acremonium kiliense, Cryptococcus neoformans, and Histoplasma capsulatum.

Abstract: Migrastatin and a migrastatin analog can be produced by fermentation of Streptomyces platensis NRRL 18993 and used in pharmaceutical formulations to treat cancer and/or inhibit metastasis of cancer cells.

Abstract: There is described a novel class of ring contracted 14-membered macrolides, and pharmaceutically acceptable salts, esters and prodrugs thereof, having antibacterial activity, compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier as well as 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. There are also described synthetic processes for preparing the compounds of the invention.

Abstract: 6-O-Carbamoyl ketolide antibacterials of the formula: 1

Abstract: Novel 9-amino-14-membered macrolides 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 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: This invention relates to a moisturizing skin ointment composition consisting of polymyxin B Sulfate, bacitracin zinc, neomycin (the combination of which totals 1 ounce), hydrocortisone acetate (1 ounce) and white petrolatum (13 ounces). When combined and water evaporated, an external ointment that penetrates the skin and alleviates dry skin conditions, itching and minor scrapes and scratches is created. The properties of the antibiotic products help to promote healing of minor scrapes and scratches as well as preventing the spread of dry skin conditions. The properties of the hydrocortisone aids in the alleviation of itching associated with dry skin. Because this ointment penetrates the dermis almost immediately, the moisturizing properties of petrolatum allows the full benefit of the antibiotic products and hydrocortison to remain on/in the skin through several washings thereby alleviating the need to reapply several times a day.

Abstract: The present invention provides novel macrolide compounds of the formulas 1

Abstract: Acid-labile active compounds are prepared in suppository form, particularly for rectal administration.

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 recognizes that marine organisms comprise nucleic acid molecules that encode polypeptides that catalyze the synthesis of bioactive compounds, such as polyketides including bryopyran rings, such as bryostatins. One aspect of the present invention is a composition including at least one nucleic acid molecule that encodes at least one polypeptide that catalyzes at least one step in the synthesis of at least one polyketide such as a bryopyran ring, wherein said at least one nucleic acid molecule is derived from at least one marine organism. A second aspect of the present invention is a composition including a library of nucleic acid molecules of the present invention. These nucleic acid molecules can be used in a combinatorial biosynthesis of polyketides, bryopyran rings and bryostatins.

Abstract: Screening methods and methods of treatment taking advantage of the mode of action of apoptolidin and its analogs are described.

Abstract: The subject invention concerns eryloside F, a novel disaccharide of the steroidal carboxylic acid penasterol. This compound can be isolated from an extract of the marine sponge Erylus formosus. The compound is a potent thrombin receptor antagonist and, furthermore, inhibits human platelet aggregation. Longer chain penasterol oligosaccharides were also isolated and characterized but these had weaker activity than eryloside F. The subject invention also concerns methods for inhibiting thrombin receptor activity and methods for inhibiting platelet aggregation through the administration of eryloside F, or a salt, derivative or analog thereof.

Abstract: The present invention concerns an unexpected synergistic combination of known antineoplastic agents which provides unexpectedly greater efficacy than the single agents alone. Accordingly, the present invention provides a method of treating neoplasia in a subject in need of treatment, by administering to the subject an amount of paclitaxel effective to treat the neoplasia, in combination with an amount of discodermolide effective to treat the neoplasia, wherein a synergistic antineoplastic effect results. The present invention further provides a synergistic combination of antineoplastic agents, comprising an effective antineoplastic amount of paclitaxel and an effective antineoplastic amount of discodermolide.

Abstract: Methods 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 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: The invention relates to dispersible tablets containing macrolides as active ingredients either on their own or associated with other active ingredients, in addition to a method for the production thereof. The dispersible tablets are characterized in that the macrolide is chosen from a group that is made up of pristinamycin, azithromycin, roxithromycin, clarithromycin and spiramycin, and is present in a basic form in proportions ranging from 20-60% of the total weight of said tablets. The dispersible tablets are also characterized in that they contain at least one disintegrator in proportions ranging from 1-25% of the total weight of said tablets in addition to at least one sweetening agent.

Abstract: The invention is directed toward a sterile bone structure for application to a bone defect site to promote new bone growth at the site comprising a partially demineralized cortical bone structure, said bone structure comprising a cross sectional surface are ranging from 85% to 95% of the original bone surface area before demineralization with the remaining partially demineralized cortical bone structure having an outer demineralized layer ranging in thickness from about 0.05 mm to about 0.14 mm and a mineralized core.

Abstract: Use: medicine, oncology in particular.

Abstract: The present invention generally relates to an in vitro analysis of anti-Leishmania activity of the anti-parasitic agent azithromycin, and more particularly the invention uses a novel source of macrophages, which are monocyte-derived bone marrow macrophages, to show the efficacy of azithromycin anti-parasitic therapy.

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

Abstract: Methods for the treatment of glaucoma are provided by the present invention. The compounds described cause a perturbation of the actin cytoskeleton in the trabecular meshwork or the modulation of its interactions with the underlying membrane. Perturbation of the cytoskeleton and the associated adhesions reduces the resistance of the trabecular meshwork to fluid flow and thereby reduces intraocular pressure.

Abstract: A controlled-release dosage form of azithromycin having an improved side effect profile; a process for preparing the dosage form; and a method of treating a microbial infection, comprising administering azithromycin in such a controlled-release dosage form to a mammal, including a human patient, in need of such treatment.

Abstract: A method of treating a hyperproliferative disorder in a subject in need of such treatment, comprising administering to said subject, in combination, a treatment effective amount of: (a) a ceramide-generating retinoid such as fenretinide or a pharmaceutically acceptable salt thereof; and (b) at least one (and in certain embodiments at least two) ceramide degredation inhibitor, such as compounds selected from the group consisting of (i) glucosylceramide synthesis inhibitors and/or 1-acylceramide synthesis inhibitors, (ii) sphingosine-1-phosphate synthesis inhibitors, and (iii) protein kinase C inhibitors. A preferred glucosyl ceramide synthesis inhibitor is 1-phenyl-2-palmitoylamino-3-morpholino-1-propanol. A preferred sphingosine-1-phosphate synthesis inhibitor is D-erythro-N,N-dimethylsphingosine. A preferred protein kinase C inhibitor is L-threo-dihydrosphingosine.

Abstract: A method is disclosed for improving the pharmacokinetics of a drug which is metabolized by cytochrome P450 monooxygenase.

Abstract: This invention relates to compounds of the formula 1

Abstract: The present invention relates to a novel macrolide derivative 2′-propionate-clarithromycin dodecyl sulfate (I), and to a method for preparing the same as well as to a pharmaceutical composition containing the same as antibiotics.

Abstract: An anthelmintic composition comprising:

Abstract: The present invention relates to methods for prevention and treatment of bone-related or nutrition-related disorders using a GLP molecule or GLP activator either alone or in combination with another therapeutic. The present invention also encompasses methods of diagnosing or monitoring the progression of a disorder. The invention also encompasses methods of monitoring the effectiveness of treatment of the invention.

Abstract: A method for treating dermatoses including transient acantholytic dermatitis, acne miliaris necrotica, acne varioliformis, perioral dermatitis, and acneiform eruptions is disclosed. The method includes topical application of a dermatological composition containing an avermectin compound to the affected areas of a patient.

Abstract: Method fore enhancing in a mammalian cell the activity of an enzyme associated with a lysosomal storage disorder by administering a competitive inhibitor of the enzyme in an amount effective to enhance the activity of the enzyme. Preferred compounds for use in the method are imino sugars and related compounds.

Abstract: The present invention provides a method and composition of medications used to treat inflammatory bowel disease. The invention further provides combinations of anti-atypical mycobacterial agents effective against the atypical mycobacterial strains. It also provides a method of potentiating the anti-atypical mycobacterial agents in treatment of inflammatory bowel disease by immunising patients with extracts of non-pathogenic mycobacteria.

Abstract: This invention relates to a method for coating a medical device comprising the steps of applying to at least a portion of the surface of said medical device, an antimicrobial coating layer and a non-pathogenic bacterial coating layer, wherein the antimicrobial and non-pathogenic bacterial coating layers inhibit the growth of pathogenic bacterial and flngal organisms. The non-pathogenic bacterium used in the bacterial coating layer is resistant to the antimicrobial agent. Furthermore, the non-pathogenic bacterium layer includes at least one of the following: viable whole cells, non-viable whole cells, or cellular structures or extracts. The antimicrobial agent and non-pathogenic bacterium are used to develop a kit comprising these compositions in one container or in separate containers. The kit is used to coat a catheter prior to implantation in a mammal.

Abstract: This invention relates to a pharmaceutical composition comprising at least one anthelmintically active compound which is an avermectin or milbemycin, in the form of a complex with at least one cyclodextrin.

Abstract: The present application relates to the use of fibers in a skincare composition or a make-up composition for the skin, to make the complexion matte, smooth and/or uniform, and/or to fade out skin relief defects. The fibers are in particular polyamide fibers having a length of from 1 &mgr;m to 10 mm and a shape factor of from 5 to 150. The composition used gives the skin a covering index of greater than 0.1 and preferably greater than 0.13. The invention also relates to a cosmetic treatment process for fading the complexion matte, smooth and/or uniform, and/or for fading out microreliefs, wrinkles, fine lines and pores in the skin, comprising the application to the skin of fibers in a cosmetic composition.

Abstract: A long-acting antiparasitic formulation suitable for topical application including:

Abstract: The present invention provides novel macrolide compounds of the formulas 1

Abstract: A subject of the invention is the compounds of formula (I): R1=H, OH, alkyl, alkenyl or alkynyl optionally substituted or alkoxy, R2=H, Hal, R3=H, alkyl, Hal, Rg and Rh: H, alkyl, aryl heterocycle, R5=H or O-alkyl, R6=alkyl or CH2—O-alkyl, R7=H or alkyl. The compounds of formula (I) have antibiotic properties.

Abstract: Agents for inducing apoptosis comprising a tetrocarcin derivative represented by the following formula (I) or a salt thereof as an active ingredient (- - - - represents a single bond or a double bond; j and k represent 0 or 1; R1 to R3, R7 to R10 and R14 represent a hydrogen atom, a lower alkyl group and the like; R4, R11, R12, R13 and R15 to R18 represent a hydrogen atom, a hydroxyl group, a lower alkyl group and the like; R5 and R6 represents a hydrogen atom, a hydroxyl group, a lower alkyl group, a group represented by the following formula (B) (R32 represents a formyl group and the like, R33 to R35 represent a hydrogen atom, a hydroxyl group, a lower alkyl group and the like); R19 represents a hydroxyl group, a lower alkoxyl group, a lower alkanoyloxy group and the like). The agents are useful as medicaments for preventive and/or therapeutic treatment of diseases resulting from increased expression of Bcl-2 family proteins, for example, cancers, AIDS and the like.

Abstract: A method of treatment of seborrheic dermatitis includes the application, in the form of either a lotion or a cream, of a mixture including a therapeutically effective amount of ivermectin in water preferably in a concentration of about 750 micrograms per milliliter (mcg/ml), in the case of a lotion, and with a pharmaceutically acceptable carrier if used as a cream. Such a lotion or cream is applied nightly preferably for a period of seven days and then employed on a maintenance basis one to four times per month.

Abstract: Methods for treating or preventing bacterial or protozoal infections in mammals by administering a single dose of an antibiotic composition comprising a mixture of azalide isomers and a pharmaceutically acceptable vehicle are disclosed. Methods for increasing acute or chronic injection-site toleration in mammals by administering a single dose of antibiotic compositions comprising a mixture of azalide isomers and a pharmaceutically acceptable vehicle are also disclosed. A combination comprising: an antibiotic composition comprising a mixture of azalide isomers, a pharmaceutically acceptable carrier, and instructions for use in a single-dose administration is also disclosed.

Abstract: The invention is directed to a method of treating cancer or a bacterial or protozoal infection in a mammalian subject in need of such treatment. The method comprises the adjunctive administration of pharmaceutically effective amounts of a macrolide antibiotic and a Substance P antagonist. The invention also encompasses a method of preventing or treating emesis associated with macrolide antibiotic administration. The invention further encompasses novel compositions comprising a macrolide antibiotic and a Substance P antagonist.

Abstract: The bioavailability of azithromycin can be increased by co-administering azithromycin with a p-glycoprotein (p-gp) inhibitor. The azithromycin and p-gp inhibitor can be administered together in a composition or as separate components. If administered separately, they can be embodied as a kit.

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: 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: This invention is directed to the treatment of inflammatory and autoimmune diseases by administering proteasome inhibitors, ubiquitin pathway inhibitors, agents that interfere with the activation of NF-&kgr;B via the ubiquitin proteasome pathway, or mixtures thereof. The invention is further directed to the treatment of inflammatory and autoimmune diseases by administering an effective combination of a glucocorticoid and a proteasome inhibitor, ubiquitin pathway inhibitor, agent that interferes with the activation of NF-&kgr;B via the ubiquitin proteasome pathway, or mixture thereof. Pharmaceutical compositions comprising a combination of a glucocorticoid and a proteasome inhibitor, ubiquitin pathway inhibitor, agent that interferes with the activation of NF-&kgr;B via the ubiquitin proteasome pathway, or mixture thereof are also contemplated within the scope of the invention.

Abstract: The invention relates to a method of preparing compounds of the formula 1 and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are antibacterial agents that may be used to treat various bacterial and protozoa infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial protozoa 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: An improved medicinal composition includes an effective amount of an antihistamine pharmaceutical and an effective amount of a nutraceutical in a pharmaceutically acceptable base. At least one of the pharmaceutical and the nutraceutical treats a condition caused by an immune response to a virus, a microorganism, or an atmospheric pollutant or allergen. The medicinal composition may additionally include a pain relieving pharmaceutical or a decongestant. The nutraceutical is preferably an immune booster, an anti-oxidant, a liver protectant, or a combination thereof. Methods of using these compositions to treat conditions caused by an immune response are also disclosed.

Abstract: When selamectin is administered to a female animal over a period commencing during pregnancy and ending during lactation, endo- and ecto-parasite infestations are either treated or prevented in that animal's offspring, avoiding the problems of treating the offspring directly. This leads to improvements in the compliance of dosing and hence the efficacy of treatment and reduces the number of doses to be administered leading to economic benefits and greater convenience.

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: The present invention includes a formulation which comprises an antibacterial substance and an antiulcer substance, wherein at least either of them is formulated into a gastrointestinal mucosa-adherent solid preparation. The formulation of the present invention shows long retention time in the gastrointestinal tract because of adhesion to the gastrointestinal tract mucosa, synergetically enhances the pharmaceutical effects of an antibacterial substance, specially antibiotic against Helicobacter pylori (HP) and an antiulcer substance, with very low doses of active ingredients, particularly the anti-HP antibiotic with low prevalence of side effects. The present agent is useful as an antiulcer agent, showing potent anti-HP activity.