412 results about "Macrocyclic lactone" patented technology

Disclosed are mixtures and compositions for controlling invertebrate pests relating to combinations comprising (a) 3-bromo-N-[4-chloro-2-methyl-6-[(methylamino)carbonyl]phenyl]-1-(3-chloro-2-pyridinyl)-1H-pyrazole-5-carboxamide, and its N-oxides, and suitable salts thereof and a component (b) wherein the component (b) is at least one compound or agent selected from neonicotinoids, cholinesterase inhibitors, sodium channel modulators, chitin synthesis inhibitors, ecdysone agonists, lipid biosynthesis inhibitors, macrocyclic lactones, GABA-regulated chloride channel blockers, juvenile hormone mimics, ryanodine receptor ligands, octopamine receptor ligands, mitochondrial electron transport inhibitors, nereistoxin analogs, pyridalyl, flonicamid, pymetrozine, dieldrin, metaflumizone, biological agents, and suitable salts of the foregoing. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a mixture or composition of the invention.

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.

Hydrophilic dispersions of stable nano-sized particles are provided comprising: (a) a water-insoluble or water-soluble active compound, wherein said active compound is selected from the group consisting of a macrolide antibiotic, donepezil hydrochloride, an azole compound and a taxane; and (b) an amphiphilic polymer which wraps said active compound in a non-crystalline manner to form a nano-sized molecular entity in which no valent bonds are formed.

This invention provides a process for producing a macrocyclic lactone compound, which comprises cultivating Actinoplanes sp. FERM BP-3832, in the presence of L-proline, L-hydroxyproline or L-nipecotic acid, and then isolating a macrocylic lactone compound from the fermentation broth. The compounds produced by this process include a compound of the following formula:The present invention also relates to a pharmaceutical composition comprising the same, which is useful as immunosuppressive, antimycotic, antitumor agent or the like.

The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula:wherein R1, R2, R3, R5, R6 and R8 are each independently a member selected from the group consisting of H, C1-6 alkyl and OH; R4, R7 and R9 are each independently selected from the group consisting of C1-6 alkoxy and OH; R10 is a member selected from the group consisting of H, —OH, —OP(O)Me2,—O—(CH2)n—OH and —O—(CH2)m—O—(CH2)o— CH3, wherein subscripts n and m are each independently from 2 to 8 and subscript o is from 1 to 6; each of L1 and L4 are independently selected from the group consisting of:each of L2 and L3 are independently selected from the group consisting of:salts, hydrates, isomers, metabolites and prodrugs thereof.

A pharmaceutical gel composition is provided comprising (a) a therapeutically effective amount of one or more active pharmaceutical ingredients comprising one or more macrolide related immunosuppressants or pharmaceutically acceptable salts or esters thereof; (b) one or more gel forming agents; and (c) an effective amount of one or more skin penetration enhancers capable of percutaneous delivery of the macrolide related immunosuppressant through the skin. Also provided is a process for its preparation and methods for delivering a macrolide related immunosuppressant through the skin of a mammal in order to treat conditions situated on and beneath the skin.

PCT No. PCT / NZ96 / 00099 Sec. 371 Date Mar. 25, 1998 Sec. 102(e) Date Mar. 25, 1998 PCT Filed Sep. 19, 1996 PCT Pub. No. WO97 / 11709 PCT Pub. Date Apr. 3, 1997A composition comprising an anthelmintic chosen from the class of macrocyclic lactones including but not limited to the avermectins, ivermectin, doramectin, abamectin, milbemycin and moxidectin, together with a vegetable oil and a co-solvent chosen from the group comprising alcohols having four or more carbons atoms. The compositions of the inventions may be formulated as injections, drenches or for topical administration and are suitable for treating helminthiasis in animals.

There is disclosed the formulation of a poorly soluble macrolide antibiotic, such as clarithromycin together with beta-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.

A pharmaceutical ointment composition is provided comprising (a) a therapeutically effective amount of one or more active pharmaceutical ingredients comprising one or more macrolide related immunosuppressants or pharmaceutically acceptable salts or esters thereof; (b) an ointment base; and (c) an effective amount of one or more skin penetration enhancers capable of percutaneous delivery of the macrolide related immunosuppressant through the skin. Also provided is a process for its preparation and methods for delivering a macrolide related immunosuppressant or a pharmaceutically acceptable salt or ester thereof through the skin of a mammal in order to treat conditions situated on and beneath the skin.

Microencapsulated formulations of macrolide lactones (abamectin, milbemectin, milbemycins emamectin, avermectins, ivermectins) wherein the active ingredient is protected from UV-degradation, with exceptional release characteristics resembling those of an emulsion concentrate or, if desired, of long-lasting effect; further with appropriate rheological properties, and with reduced toxicity. The invention provides a unique microencapsulation process for the chemical stability and biological activity of mectins, e.g. abamectin, and provides microcapsules of mectins to be used in formulations CS, WG / CS, ZC, EC / CS and any formulation type containing microcapsules and combination with other biologically active ingredients.

The present disclosure is directed to novel macrolide antibiotics of Formula 1 and pharmaceutically acceptable salts and prodrugs thereof; and the chemical syntheses and medical uses of these novel macrolide antibiotics for the treatment and / or management of infections caused by various aerobic and anaerobic gram-positive and gram-negative microorganisms as well as various mycobacteria.

The present invention provides novel macrolide compounds of the formulas 1 wherein: R is hydroxyl or methoxy; R.sup.1 is selected from the group consisting of hydrogen, hydroxyl, halide, NH.sub.2, OR.sup.9, 2 where R.sup.9 is C.sub.1-C.sub.10 alkyl, C.sub.2-C.sub.10 alkenyl, C.sub.2-C.sub.10 alkynyl, aryl or heteroaryl and R.sup.10 and R.sup.11 are each independently hydrogen, C.sub.1-C.sub.10 alkyl, C.sub.2-C.sub.10 alkenyl, C.sub.2-C.sub.10 alkynyl, or aryl; R.sup.2 and R.sup.3 are each independently selected from the group consisting of hydrogen, C.sub.1-C.sub.10 alkyl, C.sub.2-C.sub.10 alkenyl, C.sub.2-C.sub.10 alkynyl, aryl, alkylaryl, alkenylaryl, alkynylaryl or R.sup.2 and R.sup.3 together form a cycloalkyl or a cycloaryl moiety; R.sup.4 is hydrogen or methyl; R.sup.5 is hydrogen, hydroxyl, oxo, or together with R.sup.6 and the carbons to which they are attached form a cyclic carbonate; R.sup.6 is hydrogen, hydroxyl, OR.sup.12 where R.sup.12 is C.sub.1-C.sub.10 alkyl, C.sub.2-C.sub.10 alkenyl, C.sub.2-C.sub.10 alkynyl, or together with R.sup.5 and the carbons to which they are attached form a cyclic carbonate; R.sup.7 is methyl, C.sub.3-C.sub.10 alkyl, C.sub.2-C.sub.10 alkenyl, C.sub.2-C.sub.10 alkynyl, alkylaryl, alkenylaryl, alkynylaryl, amidoalkylaryl, amidoalkenylaryl, or amidoalkynylaryl; R.sup.8 is C.sub.1-C.sub.10 alkyl, C.sub.2-C.sub.10 alkenyl, C.sub.2-C.sub.10 alkynyl, alkylaryl, alkenylaryl, alkynylaryl, amidoalkylaryl, amidoalkenylaryl, or amidoalkynylaryl; and, x is a single or a double bond.

This invention relates to compositions for combating ectoparasites and endoparasites in animals, comprising at least one 1-arylpyrazole, at least one macrocyclic lactone, at least one insect growth regulator, and at least one anthelmintic compound in combination with a pharmaceutically acceptable carrier. This invention also provides for an improved methods for eradicating, controlling, and preventing parasite infections and infestations in an animal comprising administering the compositions of the invention to the animal in need thereof.

The invention provides an aqueous pharmaceutical composition for administration as an aerosol to the respiratory tract, nose or oropharyngeal region comprising (i) a macrolide having a poor taste and poor chemical stability in aqueous solution; (ii) at least one salt selected from the group consisting of sodium gluconate, sodium aspartate, sodium acetate, sodium lactate, sodium succinate, sodium maleate, magnesium gluconate, magnesium aspartate, magnesium citrate, magnesium acetate, magnesium lactate, magnesium succinate, and magnesium maleate; or mixtures thereof and (iii) a taste-masking agent different from said salt; wherein (a) the concentration of said macrolide in the composition is in the range of about 0.25 wt.-% to about 15 wt.-%; (b) the molar ratio of said macrolide:said salt is in the range from about 1:0.5 to about 1:100; (c) the pH of the composition is in the range of about 3 to 9; and (d) the osmolality of the composition is in the range of about 150 mOsmol / kg to about 1500 mOsmol / kg. The invention further provides a method of generating an aerosol, preferably by means of a nebuliser, which uses such an aqueous pharmaceutical composition. The macrolide may be used alone or in combination with other drugs. The composition is suitable to treat inflammatory disorders and / or infections of the respiratory tract. It has an improved taste and stability.

Antimicrobial macrolide and ketolide compounds are provided having formulas XII: as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

The invention relates to an antibiotic streptomyces, fermentation product of which can inhibit broad spectrum fungus and protozoan, and field experiment can control crop fungus plant disease and root-knot nematode. The antibiotic streptomyces has good effect, no pollution nuisance and no residue. The antifungal agent has extremely low hazardness for the people and good performance and development prospect for medical and agricultural use. The invention is named as SIM001 antibiotic streptomyces which is Streptomyces antibioticus subspecies xi an, and is preserved as patent in the depositary institution appointed by patent office of state intellectual property office; the preservation data is April 14th, 2005, the name of the depositary institution is CGMCC, and the number of preservation is CGMCC No.1349. The whole cell hydrolysate of the antibiotic streptomyces contains L, L-DAP (Diaminopimelic acid) and no characteristic glucide; the cytoderm belongs to I type and glucide type C; one of the main antibacterial materials is polyene macrocyclic ketolide which belongs to the broad spectrum antifungal substance.

Methods for the purification of the macrolide moxidectin result in higher purity levels than can often otherwise be obtained. The crystalline moxidectin is then used in a wide variety of pharmaceutical and veterinary applications, including the prevention, treatment and control of parasites in plants, animals and humans.

The present invention relates to compositions comprising a combination of PKC activators and PKC inhibitors and methods to modulate α-secretase activity; improve or enhance cognitive ability; and / or reduce neurodegeneration in individuals suffering from diseases that impair cognitive ability, particularly Alzheimer's Disease. The invention also relates to methods for improving or enhancing cognitive ability. The present invention also provides methods for increasing the generation of non-amyloidogenic soluble APP (sAPP) comprising the activation of protein kinase C (PKC) in the brain and inhibiting PKC in peripheral tissues. Macrocyclic lactones (i.e. bryostatin class and neristatin class) are preferred PKC activators and Vitamin E is a preferred PKC inhibitor for use in the inventive composition.

The invention relates to novel methods for using macrolide anti-infective agents. The macrolide anti-infective agents demonstrate antibacterial activity against multi-drug resistant strains of bacteria and, in particular, methicillin-resistant Staphylococcus aureus (MRSA). Methods for inhibiting the activity of multi-drug resistant bacterial organisms and methods for treating a bacterial infection caused by such organisms are described herein.

A pharmaceutical cream composition is provided comprising (a) a therapeutically effective amount of one or more active pharmaceutical ingredients comprising one or more macrolide related immunosuppressants or pharmaceutically acceptable salts or esters thereof; (b) one or more cream forming agents; and (c) an effective amount of one or more skin penetration enhancers capable of percutaneous delivery of the macrolide related immunosuppressant through the skin. Also provided is a process for its preparation and methods for delivering a macrolide related immunosuppressant through the skin of a mammal in order to treat conditions situated on and beneath the skin.

Methods and systems for preventing or treating various ocular conditions are disclosed and described. In one aspect, for example, a method for noninvasively delivering a water insoluble macrolide into an eye of a subject for treatment of an ocular condition is provided. Such a method may include administering non-invasively a water soluble form of the macrolide directly into an eye of a subject having or at risk for having the ocular condition, wherein the water soluble form is converted into the water insoluble macrolide in the eye in order to treat the ocular condition.

The present invention provides a stable veterinary oral composition which comprises one or more surfactants, a water-miscible solvent, optionally an oil and an effective amount of each of a benzimidazole antihelmintic compound, such as triclabendazole and a macrocyclic lactone, such as moxidectin. Said composition is useful for treating and controlling endo- and ectoparasitic infection and infestation in a homeothermic animal.

A method of treating an ophthalmic condition or disease by administering a compound disclosed herein is provided. The compound can be administered systemically or locally and in a variety of ways, such as via a temporary device, an implant, an injection or an eye drop. The compound can also be administered with an additional therapeutic agent.

The present invention relates (a) to new compounds represented by Formula I: wherein M represents a macrolide subunit (macrolide moiety) derived from macrolide possessing the property of accumulation in inflammatory cells, S represents a steroid subunit (steroid moiety) derived from steroid drug with anti-inflammatory activity and L represents a linker molecule linking M and S, (b) to their pharmacologically acceptable salts, prodrugs and solvates, (c) to processes and intermediates for their preparation, and (d) to their use in the treatment of inflammatory diseases and conditions in humans and animals. Such compounds inhibit many cytokines and immune mediators involved in immune responses which cause inflammation, allergy, or alloimmunity, including without limitation IL-1, 2, 4, 5, 6, 10, 12, GMCSF, ICAM, and TNF-α. Importantly, anti-inflammatory steroids exert a direct anti-inflammatory effect through binding to the glucocorticosteroid receptor.

A method of inhibiting smooth muscle cell proliferation or cytokine production in a subject, comprising administering a compound disclosed herein to the subject, is provided. The compound can be administered systemically, locally, or a combination thereof. For example, the compound can be locally delivered from a temporary device or an implant, such as a vascular prosthesis.

The present invention discloses a combination of macrolides insecticide and insecticide of Sufluoxime, wherein the macrolides insecticide is spinosad, avermectin, the derivative thereof, etc., and the Sufluoxime is 1-(3-fluoro-4-chlorophenyl)-2-methylthioethanone-O-(2-hydroxymethyl-3-methyl) aether. The various surfactants and additives such as carrier, thickening agent, stabilizing agent, antifreeze agent, antifoaming agent, adhesive and the like are added to prepare an insecticidal composition in dosage forms of missible oil, aqueous emulsion, microemulsion, suspending agent, granular formulation, water dispersible powder or dispersible granula, etc. The insecticidal composition has characteristics of evident synergism, resistance delay, widening the spectrum of insect disinfestation, etc., and has disinfestation effect to the destructive insect in the disinfestation range of two normal insecticides.