Abstract: The present invention relates to new tropine modulators of 5-HT3 receptor, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention is directed to a pharmaceutical composition comprising a therapeutically effective amount of misoprostol and an effective amount of an antibiotic. A suitable antibiotic is selected from the group consisting of doxycycline, gentamicin, tobramicin, ciprofloxacin, clindamycin, clarithromycin, azithromycin and metronidazole. Preferred antibiotics are doxycycline and ciprofloxacin. More preferably, the antibiotic is doxycycline. In its second aspect, the present invention is directed to a method for treating periodontal disease in a mammalian patient comprising administering to a mammalian patient in need of such treatment a therapeutically effective amount of misoprostol and an effective amount of an antibiotic. Typically, the mammalian patient is a human.

Abstract: A composition for inhalation which contains at least an effective amount of an antimicrobial aminoglycoside compound or a salt thereof, and an effective amount of a biofilm modifier which is a macrolide compound or a salt thereof.

Abstract: The invention relates to a method for treating ocular infections, by topical application twice a day in each eye to be treated, for less than four days, of a medicament essentially consisting of azithromycin in solution in a pharmaceutically acceptable vehicle of linear medium-chain fatty acid triglycerides, at the concentration of 1% to 2%.

Abstract: A nasal delivery device for and method of delivering substance to the middle meatus in a nasal cavity of a subject in the treatment of a condition, in particular an inflammatory or infectious condition, thereof, the delivery device comprising: a nosepiece unit (17) including a nosepiece (20) for fitting to a nostril of a subject and a nozzle (25) through which substance is in use delivered to the respective nasal cavity; and a delivery unit (29) for delivering substance through the nozzle of the nosepiece; wherein the delivery device is configured to provide for deposition of a significant fraction of the delivered dose on, around and in the vicinity of the middle meatus.

Abstract: This invention relates to a powder for oral suspension, and an oral suspension made there from, which comprises non-dihydrate azithromycin and an azithromycin conversion stabilizing excipient, wherein said excipient reduces the conversion of the form of azithromycin, when placed in suspension, to another form of azithromycin. This invention further relates to a method for reducing the conversion of a form of non-dihydrate azithromycin, in an oral suspension, by including at least one cyclodextrin in said oral suspension.

Abstract: The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes processes by which to make the compounds of the present invention.

Abstract: The present invention relates to a combination of pharmaceutical compositions adapted for oral administration one of which comprises a pharmaceutically active ingredient being acid resistant, and the other of which comprises a pharmaceutically active ingredient being acid labile. Said combination is in the form of a kit of parts which is administered in such way as to use food intake to optimize absorption of both the acid labile and the acid resistant active ingredient. Consequently, the kit of parts of the present invention when administered according to the invention provides improved bioavailability of both the acid-resistant and acid-labile active ingredient.

Abstract: Provided herein are pharmaceutical compositions comprising an anti-inflammatory macrolide compound suitable for aerosolized administration to the lungs by inhalation, and methods of treating inflammatory lung conditions, particularly those characterized by chronic inflammation, by administering an aerosolized anti-inflammatory macrolide compound to the lungs by inhalation. Also provided are unit dose formulations of an anti-inflammatory macrolide for aerosolized administration to the lungs by inhalation. Advantageously, the described methods and compositions allow for the targeted, localized delivery of anti-inflammatory macrolide compounds throughout the lungs without significant systemic absorption or deposition.

Abstract: The present invention relates to a method for treating non-infectious, inflammatory chronic posterior blepharitis in a subject. The present invention also relates to a method for treating chronic posterior blepharitis in a subject for over two weeks. The method comprises identifying a subject in need thereof, and topically administering to the eye of the subject a pharmaceutical formulation consisting essentially of an effective amount azithromycin. The present invention further relates to a method for treating dry eye secondary to blepharitis in a subject. The method comprises the steps of: identifying a subject suffering from dry eye secondary to posterior blepharitis, and topically administering to the eye of the subject a pharmaceutical formulation comprising an effective amount of azithromycin. The present invention further relates to method for reducing contact lens intolerance of a subject due to blepharitis or dry eye secondary to blepharitis.

Abstract: The present invention provides triazole macrocyclic compounds useful as therapeutic agents. More particularly, these compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. The compounds have the following structure: wherein T is the macrocyclic part.

Abstract: The present invention provides triazole macrocyclic compounds useful as therapeutic agents. More particularly, these compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.

Abstract: Provided are electrokinetically-altered fluids (gas-enriched (e.g., oxygen-enriched) electrokinetic fluids) comprising an ionic aqueous solution of charge-stabilized oxygen-containing nanostructures in an amount sufficient to provide, upon contact with a cell, modulation of at least one of cellular membrane potential and cellular membrane conductivity, and therapeutic compositions and methods for using same in treating cystic fibrosis or a symptom thereof. The electrokinetically-altered fluid compositions and methods include electrokinetically-altered fluids optionally in combination with other therapeutic agents (e.g., antibiotics, albuterol, budesonide, etc.). Particular embodiments comprise use and/or synergy with tobramycin for treating bacterial infection, and use and/or synergy with a bronchiodilator.

Abstract: The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

Abstract: The present invention provides a PEG-modified HAP having a high degree of safety and novel functions by modifying the surface of hydroxyapatite particles with a polyethylene glycol derivative, applications thereof, and a production process of the same. The PEG-modified HAP of the present invention is a substance in which hydroxyapatite having a particle diameter of 50 ?m to 10 nm is bonded to a polyethylene glycol derivative having a carboxyl group as a terminal functional group through —O(CO) bonds, and the carbon content thereof is 10 to 0.1%. In addition, the present invention is a substance composed of this substance and a pharmaceutical active ingredient or pharmaceutical additive, in which the weight ratio of the pharmaceutical active ingredient is 1 to 30%, and the substance is obtained by treating hydroxyapatite having a particle diameter of 50 ?m to 10 nm and an active ester of polyethylene glycol derivative having a carboxyl group as a terminal functional group in an anhydrous organic solvent.

Abstract: Microparticle-bioactive agent based treatments for local treatment of diseased tissues/organs are disclosed.

Abstract: The present invention discloses compounds of formulae (I), (II) or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

Abstract: The present invention discloses compounds of formula (I) or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit superior antibacterial properties, particularly against Haemophilus influenzae. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

Abstract: The invention is directed toward an osteoimplant for application to a bone defect site to promote new bone growth at the site which comprises a new bone growth inducing composition of demineralized allograft bone material mixed with an aqueous phosphate buffered gelatin which when lyophilized to remove water from the composition crosslinks the gelatin to form a solid structure and when rehydrated is flexible

Abstract: Disclosed herein are 10-desmethyl, 10 substituted-macrolides, their preparation, pharmaceutical compositions containing them, their use and methods of treatment using them. The 10-desmethyl macrolides are particularly useful as antibiotics.

Abstract: The present invention discloses compounds of formula I, II or X, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

Abstract: Described herein are novel macrolides, the preparation of novel macrolides, to the use of novel macrolides for preventing, treating, or ameliorating various conditions, and the use of novel macrolides as antibacterial agents.

Abstract: The present invention provides compounds having antimicrobial activity for preventing and treating diseases caused by microbial infections. Thus, the present invention relates to novel semi-synthetic 11,12-? lactone macrolides and ketolides having antimicrobial activity, processes for making compounds as well as pharmaceutical compositions containing said compounds as active ingredients and methods of treating microbial infections with the compounds.

Abstract: 15-fluoroketolides of the formula having improved activity and safety, compositions comprising them, and methods for their preparation and use in the treatment of bacterial infections.

Abstract: 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.

Abstract: The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

Abstract: This invention relates to combinations of an abl-, PDGF-Receptor- and/or Kit receptor-tyrosine kinase inhibitor with an organic compound capable of binding to ?1-acidic glycoprotein (AGP), as well as to pharmaceutical preparations and/or therapies, in relation to disease states which respond to inhibition of abl-, PDGF-Receptor- and/or Kit-receptor tyrosine kinase. In particular, the invention relates to products or combinations comprising an abl-, PDGF-Receptor- and/or Kit receptor-tyrosine kinase inhibitor with an organic compound capable of binding to AGP, either in fixed combination or for chronologically staggered or simultaneous administration, and the combined use of both classes of compounds, either in fixed combination or for chronologically staggered or simultaneous administration, for the treatment of proliferative diseases, especially tumor diseases, especially those that can be treated by inhibition of abl-, PDGF-Receptor- and/or Kit receptor-tyrosine kinase activity.

Abstract: Compositions and methods are provided for treating accumulation of exudative serous effusions caused by illnesses such as cancer, infection, and pancreatitis. In one embodiment, the method of the invention comprises administering to such mammal a macrolide in an amount effective to prevent or at least alleviate said exudative serous effusion accumulation.

Abstract: Compounds having a structure according to formula (I) where RA, RB, RC, RD, RE, and RF are as defined herein, are useful as prokinetic agents.

Abstract: This invention features a compound of the following formula: T-(-L-C)m, T is a transportophore, L is a bond or a linker having a molecular weight up to 240 dalton, C is a non-antibiotic therapeutic agent, and m is 1, 2, 3, 4, 5, 6, 7, or 8, in which the transportophore has an immune selectivity ratio of at least 2, the transportophore is covalently bonded to the non-antibiotic therapeutic agent via the bond or the linker, and the compound has an immune selectivity ratio of at least 2.

Abstract: The present disclosure related to a method of treating an infection by oral administration of a single dose of a fast dissolving form of azithromycin. The disclosure also relates to a method of reducing the adverse effects arising from treatment of a subject having an infection by administering a single dose of a fast dissolving form of azithromycin.

Abstract: The present invention relates to a method of forming shape-retentive and shape-conforming aggregate wound dressings and biomaterials composed of gel nanoparticles and wound or bodily fluid in which the aggregates are held together by non-covalent bond physical forces such as, without limitation, hydrophobic-hydrophilic interactions and hydrogen bonds. The method comprises introducing a dry powder of gel nanoparticles to a wound site in which the nanoparticles absorb some of the blood or wound exudate and coalesce in situ into the claimed shape-retentive aggregate dressing. The method also comprises introducing the dry nanoparticle powder in or on a wet bodily tissue in vivo to form the claimed shape-retentive biomaterial. In addition, the method also comprises incorporating biomedical agents to produce medicated aggregate dressings or biomaterials for a variety of medical applications. This invention also relates to uses of the method of formation of the shape-retentive aggregates of gel nanoparticles.

Abstract: The present disclosure provides compositions and methods for the treatment and elimination of chronic intracellular infections in cells or organisms. The compositions may include one or more acidic substances and one or more antimicrobial substances, administered in combination or separately. The methods may include administering an amount of one or more such compositions to an infected cell or organism for a period of time ranging from days to years, until the infection is substantially eliminated.

Abstract: The present invention relates to 14- or 15-membered macrolides substituted at the 4? position of formula (I) and pharmaceutically acceptable derivatives thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical microbial infections in a human or animal body.

Abstract: Substantially pure isostructural pseudopolymorphs of 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A having the Formula I: wherein S is an organic solvent which is at least partially miscible with water, x is 1, 1.25, 1.5 or 2, y is 0, 0.5, or 1, the pseudopolymorph being characterized by the monoclinic space group P21 and average unit cell parameters comprising: crystal axis lengths of a=15.5-17.0 ?, b=15.5-17.0 ?, and c=17.5-19.5 ?, and angles between the crystal axes of ?=?=90° and ?=106°-112°. In addition, this disclosure is directed to processes for the preparation of the substantially pure isostructural pseudopolymorphs of Formula I; to pharmaceutical compositions containing substantially pure isostructural pseudopolymorphs of Formula I; and to a method for the treatment of bacterial and protozoan infections, and inflammation-related diseases by administration of a pharmaceutical composition containing the substantially pure isostructural pseudopolymorphs of Formula I.

Abstract: Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II: aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.

Abstract: This invention provides for, inter alia, oral homogeneous veterinary pastes for the treating, controlling and preventing of endo- and ectoparasite infections in warm-blooded animals or birds, such as horses and household pets. This invention further provides for a process of preparing these veterinary pastes and for a method for increasing the bioavailability of the anthelmintic agents contained in the paste in the warm-blooded animal or bird. The inventive oral homogeneous anthelmintic pastes comprise a first anthelmintic agent, for example, prazequantel and/or pyrantel, and at least one marcrolide anthelmintic compound, a solvent, which dissolves both the first anthelmintic agent and second the macrolide anthelmintic compound, and a thickening agent.

Abstract: Methods for treating perioral dermatitis are described herein. The method includes administering topically a composition containing an effective amount of a systemic or topical antibiotic and a corticosteroid. The concentration of the antibiotic is from about 0.01% to about 5% by weight of the composition and the concentration of the corticosteroid is from about 0.01% to about 5% by weight of the composition. The composition can contain one or more pharmaceutically acceptable excipients and/or carriers. The compositions can be formulated as a lotion, cream, gel, ointment, paste, powder, solution, suspension, spray, foam, or patch.

Abstract: The invention relates to a capsule containing a heterogeneous mixture of active agents in the form of particles suspended in a liquid matrix and optionally active ingredients in the liquid matrix; the liquid matrix occupying less than the total internal volume of the capsule. The present invention further describes a capsule to allow the controlled-release of one or more active agents for specific desired benefits.

Abstract: The present invention relates to 14- or 15-membered macrolides substituted at the 4? position of formula (I) and pharmaceutically acceptable derivatives thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical microbial infections in a human or animal body.

Abstract: Compounds of Formula (I), and pharmaceutically acceptable salts, esters, and prodrugs thereof: (I) are disclosed, wherein A, B, D, L, X, Y, Z and R2?, are described herein. The compounds exhibit antibacterial properties. The compounds of Formula (I) can be employed to treat or prevent bacterial infections as compounds per se or in the form of pharmaceutically acceptable salts, esters, or prodrugs. The compounds and their salts, esters, and prodrugs can also be employed as ingredients in pharmaceutical compositions, optionally in combination with other antibacterial agents, for the treatment of bacterial infections. Processes for making the compounds are also disclosed.

Abstract: The invention relates to compositions and methods related to Toll-like receptor (TLR) polypeptides. In some embodiments, the invention relates to managing TLR3 related diseases. In further embodiments, the invention relates to methods of preventing and treating inflammation. In some embodiments, the invention relates to antagonists of TLR3, to amino acid sequences that act as dominant negative molecules, and to nucleic acid sequences that encode said amino acid sequences. In additional embodiments, the invention relates to the manipulation of biological materials to evaluate TLR3 activity.

Abstract: An ocular method comprising localized ocular administration of a pharmaceutically acceptable formulation and effective concentration of at least one neuro-stimulatory agent, which may include a macrolide, for a duration sufficient to at least partially restore corneal sensation, or at least one macrolide to reduce scarring after ocular surgery. The neuro-stimulatory agent may be one or more of a macrolide, macrolide analog, neurotrophin, or neuropoietic factor. The method is used in a patent following ocular surgery, such as vision-correction surgery, glaucoma surgery, or retinal detachment repair surgery.

Abstract: The invention describes novel nitrosated and/or nitrosylated compounds of the invention and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated compound of the invention, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one compound of the invention, and at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one compound of the invention, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for (a) treating bacterial infections; (b) treating viral infections; (c) treating fungal infections; and (d) treating lesions.

Abstract: An aspect of the disclosure includes a system for delivering therapeutic agents. In an embodiment, the system includes an implantable medical device comprising at least one reservoir that holds at least one therapeutic agent. Additionally the device includes a delivery mechanism that provides non-systemic in vivo delivery of the at least one therapeutic agent to a local area of an animal in a therapeutically-effective concentration, wherein the therapeutically-effective concentration is in excess of a concentration that would produce a toxic effect when administered systemically to the animal. Furthermore, the at least one therapeutic agent has short half-life. A further aspect of the disclosure includes a method of delivering a therapeutic agent in vivo at non-systemic high doses to a localized area of an animal.

Abstract: The present invention provides macrolide derivatives, which can be used as antibacterial agents. Compounds described herein can be used for treating or preventing conditions caused by or contributed to by gram-positive, gram-negative or anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Moraxalla spp., Chlamydia spp., Mycoplasm, Legionella spp., Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebacterium, Propionibeacterium, Bacillus, Enterobactericeae or any combination thereof. Also provided are processes for preparing compounds described herein, pharmaceutical compositions thereof, and methods of treating bacterial infections.

Abstract: The invention provides methods utilizing bridged macrolide or tylosin derivatives for the treatment of patients with inflammatory bowel diseases. The methods of the invention provide for the administration to a patient of a therapeutically effective amount of a bridged macrolide or a tylosin derivative, pharmaceutically acceptable derivatives thereof, and combinations thereof for a period of time sufficient to obtain a desired alleviation of one or more symptoms of the inflammatory bowel disease.

Abstract: The invention is directed to controlled release formulations containing drugs which are preferably considered sparingly soluble to insoluble and which are suitable for administration to a patient in need of treatment related thereto, and methods of manufacturing the same.

Abstract: A compound of formula (I) compositions comprising same, processes for their preparation and use of said compounds, particularly in the treatment of microbial infections.

Abstract: The present invention relates to new antibiotic macrolide compounds of the general formula I: with improved activity, to medicaments comprising such antibiotics, and to the use of such antibiotics for the treatment of infectious diseases, inflammatory diseases and human diseases or disorders which can be ameliorated by inhibition human phospdiesterases.