Abstract: Pharmaceutical compositions in unit dose form comprising a hard or soft capsule containing a fill consisting of one or more inert ingredients, and one or more coatings on the capsule, wherein at least one coating comprises at least one active pharmaceutical ingredient.

Abstract: The subject application provides small compounds that are able to suppress autophagy in various cells. These compounds are useful in augmenting the existing treatments of various cancers and microbial/parasitic infections. Thus, the subject application also provides methods of treating various types of cancers and microbial/parasitic infections. Also provided by the subject application are methods of suppressing the expansion of autophagosomes within cells or individuals and inhibiting the lipidation of autophagy-related protein 8 (Atg8).

Abstract: An antimicrobial accessory may include a polymer an antimicrobial mixed in the polymer, and an antioxidant. The antioxidant may include, for example, at least one of citric acid, maltol, kojic acid, malic acid, or vitamin A. In some examples, the antioxidant may include an ascorbate peroxidase in combination with ascorbic acid, a glutathione peroxidase in combination with glutathione, or a superoxide dismutase in combination with a metal such as Ni, Cu, Mn, or Fe. In some examples, the antimicrobial accessory may include at least three polymer layers. For example, the antimicrobial accessory may include a first layer comprising a biodegradable polymer and an antimicrobial. The antimicrobial accessory may further include a sacrificial diffusion layer formed on a surface of the first layer. The sacrificial diffusion layer may include a biodegradable polymer, which may be the same biodegradable polymer as in the first layer or may be a different biodegradable polymer.

Abstract: An antimicrobial accessory may include a polymer an antimicrobial mixed in the polymer, and an antioxidant. The antioxidant may include, for example, at least one of citric acid, maltol, kojic acid, malic acid, or vitamin A. In some examples, the antioxidant may include an ascorbate peroxidase in combination with ascorbic acid, a glutathione peroxidase in combination with glutathione, or a superoxide dismutase in combination with a metal such as Ni, Cu, Mn, or Fe. In some examples, the antimicrobial accessory may include at least three polymer layers. For example, the antimicrobial accessory may include a first layer comprising a biodegradable polymer and an antimicrobial. The antimicrobial accessory may further include a sacrificial diffusion layer formed on a surface of the first layer. The sacrificial diffusion layer may include a biodegradable polymer, which may be the same biodegradable polymer as in the first layer or may be a different biodegradable polymer.

Abstract: The present invention pertains to novel 3, 10, and/or 12a-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

Abstract: The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

Abstract: A drug-eluting device comprising a drug-eluting matrix containing at least one elutable drug, a method of manufacturing a preformed drug-eluting device, and an implant kit comprising the same.

Abstract: This invention provides compounds of Formula (I); or a tautomer or pharmaceutically acceptable salts thereof useful as antibacterial agents.

Abstract: Bioactive, hydroforming luminal liner compositions are formed of high molecular weight crystalline, absorbable copolyesters dissolved in a liquid derivative of a polyether glycol that undergoes transformation into a tissue-adhering, resilient interior cover or liner for the controlled release of its bioactive payload at clinically compromised conduits in humans as in the case of bacteria- and yeast-infected vaginal canals, esophagi, and arteries following angioplasty.

Abstract: Bioactive hydroforming luminal liner compositions are formed of an absorbable crystalline amphiphilic polyether-ester-urethane dissolved in a liquid derivative of a polyether glycol that undergoes transformation into a tissue-adhering, resilient interior cover or liner for the controlled release of its bioactive payload at clinically compromised conduits in humans as in the case of bacteria- and yeast-infected vaginal canals, esophagi, and arteries following angioplasty.

Abstract: The instant invention provides methods and compositions for the treatment of cancer.

Abstract: Methods and compositions for treating Cryptosporidium parvum related disorders in a mammal are discussed. Several novel tetracycline compounds useful for treating Cryptosporidium parvum related disorders are also included.

Abstract: The invention pertains to prodrugs of 9-aminomethyl substituted tetracycline compounds, methods of using the compounds, and pharmaceutical compositions containing them.

Abstract: A therapeutic agent eluting element includes an elongate body member and one or more therapeutic agents elutable from the body member. The elongate body member is configured to be implanted subcutaneously along side of a therapy delivery element. The elongate body member may be formed from a polymeric material, and the agent eluting element may consist essentially of the body member and the one or more therapeutic agents. The therapeutic agent eluting element may be a part of a system or kit that includes a therapy delivery element and a tunneling tool, such as a dilator, sheath, catheter passer, or the like.

Abstract: The invention relates to low-molecular doxorubicin peptide derivatives containing MMP-2 or MMP-9 divisible peptide sequences and a protein-binding group.

Abstract: The invention provides Toll-like receptor (TLR) modulators, compositions comprising the same, and methods for using the same.

Abstract: Minocycline oral dosage forms containing a controlled release carrier are useful for the treatment of acne.

Abstract: The invention relates to novel spill resistant formulations comprising either a weak base or a weak acid as the pharmaceutical ingredient, a liquid base, a clay and a water soluble cellulose ether. The clay and cellulose ether allow for a broader pH range into which the pharmaceutically active agent may be dispersed or dissolved, and therefore allows for easier preparation and formulation of the pharmaceutical composition.

Abstract: Aromatized A-ring derivatives of tetracycline compounds are described.

Abstract: A delivery system for various functional compounds is disclosed. The delivery system incorporates a composition containing alumina. Various functional materials containing particular moieties may be adsorbed onto the alumina and used as desired. The functional compounds can be, for instance, pharmaceuticals, xenobiotics, anti-microbial agents, anti-viral agents, UV absorbers, odor control agents, fragrances, and the like. In one particular embodiment, for instance, certain dyes can be adsorbed onto the alumina surfaces. Once the dye is adsorbed onto the alumina surface, the resulting particles can be combined with a liquid vehicle for use in any suitable printing process.

Abstract: A method of producing a batch of a tetracycline-class component HPMC extended release pharmaceutical product having a desired dissolution profile, comprising: selecting a dissolution rate-controlling polymer comprising an HPMC component, the HPMC component having a selected % HP value; validating that the % HP in the selected HPMC component is such that a mean sample of the product complies with the desired dissolution profile over each time point in the dissolution profile, and preparing the product by preparing a formulation comprising a pharmaceutically effective amount of the tetracycline-class chemical and the selected HPMC component with the % HP value. There is also provided a method of predicting the dissolution rate profile over a number of dosage forms.

Abstract: The PhoU protein is a widely expressed protein in bacteria, but not in eukaryotes. The PhoU protein is required for persister formation in bacteria. The invention includes compositions to reduce persister formation and their use as therapeutic agents. The invention further includes methods for identification of compounds to reduce persister formation. The invention further includes kits for the identification of agents that modulate the activity and expression of PhoU.

Abstract: The present invention is directed to solid forms of the Raf kinase inhibitor 1-methyl-5-(2-(5-(trifluoromethyl)-1H-imidazol-2-yl)pyridin-4-yloxy)-N-(4-(trifluoromethyl)phenyl)-1H-benzo[d]imidazol-2-amine, as well as compositions thereof and uses of the same.

Abstract: The present invention relates to a metal triangulo compound. Provided is also a method of inducing apoptosis in a cell that comprises administering the metal triangulo compound. Provided is also a method of preventing carcinogenesis in a cell that comprises administering the metal triangulo compound.

Abstract: An aerosolizable formulation comprised of a drug, a carrier and pH affecting component is disclosed. The drug is dissolved in the formulation at a concentration above which it remains in solution at neutral pH. This increases the concentration of the drug in solution making it possible to administer larger amounts of drug with the same or a smaller volume of formulation. When the formulation is aerosolized to small particles and inhaled into human lungs in small volumes (e.g. 0.05 to 0.5 mL) the fluids in the lungs neutralize the formulation causing the drug to participate out of solution. This results in the drug being delivered at a controlled rate below the rate at which drug is administered from a formulation initially at a neutral pH.

Abstract: The invention provides a multi-compartmented container suitable for the delivery of pharmaceuticals, medicines, vitamins, and the like.

Abstract: Aromatized A-ring derivatives of tetracycline compounds are described.

Abstract: A drug delivery system is provided for treatment of oxidative stress. The drug delivery system can include a therapeutic agent and a matrix. The therapeutic agent can include an antioxidant or steroid. The matrix can include a hydrogel, particle, microparticle, or nanoparticle. A method of treating injury, including peripheral nerve injury or spinal cord injury, is also provided. The method includes injecting the drug delivery system at the site of injury.

Abstract: Implantable catheters are provided which comprise an antimicrobial agent incorporated in a coating or bulk distributed, in combination with a fibrinolytic agent incorporated in a top coating.

Abstract: The present invention pertains to novel 3, 10, and/or 12a-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

Abstract: The present invention pertains, at least in part, to substituted tetracycline compounds. The present invention also pertains to methods for treating rheumatoid arthritis in a subject, comprising administering to the subject a tetracycline compound of the invention.

Abstract: A therapeutic, cosmetic or cosmeceutic composition for topical application, capable of stabilizing an active ingredient and delivering the active ingredient, comprising a plurality of microcapsules having a core-shell structure. The microcapsules have a diameter of approximately 0.1 to 100 micron. The core of each microcapsule includes at least one active ingredient and is encapsulated within a microcapsular shell. The shell is comprised of at least one inorganic polymer obtained by a sol-gel process, and the shell protects the active ingredient before topical application and is designed to release the active ingredient from the microcapsules following application. The composition is useful in encapsulating active ingredients, such as benzoyl peroxide, that are unstable in other formulation, or are irritating to the skin.

Abstract: The present invention relates to a method of determining the microbial bioburden in a wound (in particular a diabetic ulcer) in a test subject, the method comprising the step of measuring the level of a cytokine in a wound sample, wherein a cytokine level lower than a reference level indicates a significant microbial bioburden in the wound (or a cytokine level higher than a reference level indicates an insignificant microbial bioburden in the wound). The invention provides methods of diagnosis, prognosis and treatment of wound infection, and devices and kits for use in such methods.

Abstract: The present invention relates to polymers modified to increase their resorbability. In particular, the polymers of the invention have phenyl ester side chains which are good leaving groups and which thereby increase the resorption rate of the polymer relative to the same polymer, for example, bearing a comparable amount of an alkyl ester side chain. Such polymers are generally water insoluble, but when modified are able to solublize drugs and upon degradation and resorption, release those in a physiological environment in a controlled and/or sustained manner.

Abstract: The present invention relates to the new crystalline solid form VI and VIII of tigecycline and processes for the production of form VI and VIII. It further relates to a new method for preparing Form I and Form III in high polymorphic purity.

Abstract: The present invention pertains to novel 7,9-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

Abstract: 7, 8 and 9-substituted tetracycline compounds, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7, 8 and 9-substituted tetracycline compounds are described.

Abstract: Methods are provided for evaluating osteoarthritis (OA), for example for diagnosing OA, to confirm a diagnosis of OA, to assess or prognose progression of OA, determining the severity of a subject who has OA, and determining a subject's risk of developing OA in the future, as are arrays and kits that can be used to practice the methods. In particular examples, the method includes determining an amount of activity (such as an amount of protein present or an amount of expression) of OA risk-related molecules, such as soluble vascular adhesion protein 1 (sVAP-1) or interleukin-15 (IL-15). Also provided are methods of identifying one or more compounds that alter the activity of an OA-related molecule, thereby identifying potential anti-osteoarthritis drugs.

Abstract: A method for treating a patient having ulcerative colitis, by administering a drug which containing an effective amount of tetracyclines is provided. The drug may also contain penicillins and/or metronidazoles.

Abstract: The present invention provides processes for the preparation of crystalline forms of Tigecycline.

Abstract: An aspect of the present invention provides for a medicament including a solution containing pleconaril or a pharmaceutically acceptable salt thereof, wherein at least one solvent including the solution is a pleconaril-dissolving hydrofluorocarbon.

Abstract: The present invention is for a method for treating aortic stenosis in a mammal in need thereof. The method comprises administering an effective amount of a non-antibacterial tetracycline formulation, to the mammal.

Abstract: A pharmaceutical or cosmetic carrier or composition for topical application characterized by rheological properties which render the carrier or composition semi-solid at rest and a liquid upon application of shear forces thereto. The composition or carrier are prepared by mixing 1-25 percent of a solidifying agent and 75-99 percent of a hydrophobic solvent, by weight, wherein at least one of them has therapeutic or cosmetic benefits, in the presence or absence of a biologically active substance.

Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetra-cycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-pro liferative agents in the treatment of diseases of humans or other animals.

Abstract: A topical pharmaceutical composition comprising an antibiotic is useful for the prevention of Lyme disease.

Abstract: Methods for disinfecting and removing smear layer from prepared tooth surfaces are provided. The methods involve irrigating the tooth surface with a disinfectant solution containing doxycycline or tetracycline, a surfactant such as polysorbate, and organic acid such as citric acid. The methods can be used in various dental treatments including, for example, endodontic and periodontic procedures as well as tooth restoration and reconstruction.

Abstract: The present invention is directed to polyphenolic polymers formed from dihydroxybenzoic acid (DHB) derivatives or from resorcinol derivatives, monomers which form such polymers, blends of the polymers with drugs and/or additional polymers, as well as medical devices formed from, coated with, impregnated by or coverings made with any of the foregoing polymers (with or without drugs) or blends (with or without drugs).

Abstract: Use of doxycycline, a non specific matrix metalloproteinase inhibitor, for treatment of idiopathic pulmonary fibrosis and a pharmaceutical composition comprising doxycycline or its congener in combination with another compound selected from the drug listed for treatment of idiopathic pulmonary fibrosis in a standard dose.

Abstract: The present invention relates to new phenylacetic acid inhibitors of cyclooxygenase activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Crystalline forms, including salts and polymorphs, of a compound useful in the treatment of tetracycline compound-responsive states are provided herein. The crystalline compounds are useful for the treatment or prevention of conditions and disorders such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds in general.