Abstract: The present invention describes single drug entities, formed by connecting an antibiotic moiety via a linker with a non-steroidal anti-inflammatory drug (NSAID) moiety. Upon topical application to the eye, the conjugate hybrid would undergo enzymatic and/or hydrolytic cleavage to release the individual antibiotic and NSAID drug.

Abstract: The present invention relates to a pharmaceutical composition, in particular a composition formulated for enema administration, wherein the composition comprises metronidazole or a pharmacologically acceptable derivative thereof in an amount to effectively treat both acute and chronic pouchitis and/or proctitis.

Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.

Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.

Abstract: The present invention relates to novel bis-indolic derivatives, processes for their preparation, and their potential use as new antibacterial drugs.

Abstract: An anti-infection solution including (i) from 10% to 30% by weight with respect to the total volume of the solution of at least one compound of Formula (I): wherein: X represents a hydrogen or halogen atom or a hydroxy function, R1 represents: a 1-piperazinyl radical, which may be substituted in position 4 by a methyl, acetyl or 4-aminobenzyl group; a morpholino radical: a 1-pyrrolidinyl radical substituted in position 3 by a chlorine atom or by an amino, aminomethyl, (methylamino) methyl, (ethylamino) methyl or methoxy group; a 1-imidazolyl radical that can be substituted in position 4 by the methyl group, or a 1-piperidyl radical substituted in position 4 by a hydroxy or methoxy group, and R2 represents an alkyl radical, linear, branched or ring, including 1 to 10 carbon atoms, or at least one of its pharmaceutically acceptable salts, (ii) benzyl alcohol as a stabilizing agent, and at least one stabilizing agent, and (iii) at least one solubilization agent selected from the group consisting of carbolic

Abstract: Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.

Abstract: Phospholipid based powders for drug delivery applications are disclosed. The powders comprise a polyvalent cation in an amount effective to increase the gel-to-liquid crystal transition temperature of the particle compared to particles without the polyvalent cation. The powders are hollow and porous and are preferably administered via inhalation.

Abstract: The present invention provides compounds of formula (I), wherein G1 is oxygen; R1 is hydrogen; R2 is group P (P) L is a bond, methylene or ethylene; one of A1 and A2 is S, SO or SO2 and the other is —C(R4)R4—R3 is hydrogen or methyl; each R4 is independently hydrogen or methyl; Y1 is C—R6, CH or nitrogen; Y2 and Y3 are independently CH or nitrogen; wherein no more than two of Y1, Y2 and Y3 are nitrogen and wherein Y2 and Y3 are not both nitrogen; R5 is hydrogen, halogen, cyano, nitro, NH2, C1-C2alkyl, C1-C2haloalkyl, C3-C5cycloalkyl, C3-C5halocycloalkyl, C1-C2alkoxy, C1-C2haloalkoxy; R6 together with R5 forms a —CH?CH—CH?CH— bridge; X2 is C—X6 or nitrogen; X1, X3 and X6 are independently hydrogen, halogen or trihalomethyl, wherein at least two of X1, X3 and X6 are not hydrogen; X4 is trifluoromethyl, difluoromethyl or chlorodifluoromethyl.

Abstract: Artonin I is reported to treat multi-drug resistant Staphlococcus infections.

Abstract: The disclosure relates to piperazine derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to inhibitors of NADPH-oxidase.

Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.

Abstract: The present invention relates to compounds formula (I), wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5, R6, R17, R18, R19 and R20 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.

Abstract: Polymeric articles capable of releasing drugs at therapeutic levels over extended periods of time, and methods for producing the extended release articles.

Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.

Abstract: The invention relates to solid compositions that may be suitable for administering a therapeutic agent to a subject. The invention also relates to methods of making such solid compositions. The invention further relates to methods of treating a disease, condition, or disorder by administering to a subject such solid compositions.

Abstract: The invention relates to compounds of formula (I): where A1, A2, A3, A4, G1, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.

Abstract: Compositions and methods related to ophthalmic use of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymers and therapeutic uses are described herein.

Abstract: A method for treating cancer in a subject, comprising administering to a subject having cancer a therapeutically effective amount of (i) a fluoroquinolone derivative that inhibits tyrosyl-DNA-phosphodiesterase 1 (Tdp1) activity or (ii) a sulfonamide moiety-containing compound that inhibits tyrosyl-DNA-phosphodiesterase 1 (Tdp1) activity, thereby treating the cancer in the subject. In certain embodiments, the fluoroquinolone derivative or sulfonamide moiety-containing compound is co-administered with a topoisomerase I (TopI) inhibitor.

Abstract: The present invention provides compounds of formula (I): wherein A1, A2, A3 and A4 are independently of one another C—H, C—R5, or nitrogen; B1—B2—B3—B4 is —CH2—C?N—CH2—, —CH2—N—CH2—CH2—, —CH2—C?CH-0- or —CH?C—CH2-0-; G1 is oxygen or sulfur; L is a single bond or C1-C8alkylene; R1 is hydrogen, C1-C8alkyl, C1-C8alkylcarbonyl-, C1-C8alkoxy, C2-C8alkenyl, C2-C8alkynyl, C1-C8alkoxy-C1-C8alkyl, aryl or aryl substituted by one to three R6, or R1 is heterocyclyl or heterocyclyl substituted by one to three R6 or C1-C8alkoxycarbonyl-; R2 is hydrogen, C1-C8haloalkyl or C1-C8alkyl; R3 is C1-C8haloalkyl; R4 is aryl or aryl substituted by one to three R6, or R4 is heterocyclyl or heterocyclyl substituted by one to three R6; Y1 is CR7R8, C?O or C?S; Y2, Y3 and Y4 are independently CR7R8, C=0, C?S, N—R9, O, S, SO or SO2; wherein at least two adjacent ring atoms in the ring formed by Y1, Y2, Y3 and Y4 are heteroatoms; each R7 and R8 is independently hydrogen, halogen, C1-C8alkyl, or C1-C8haloalkyl; and R5, R6, R7, R8 and R9 a

Abstract: The present invention provides a combination product comprising a component A and a component B, wherein component A is a compound of formula (I) wherein A1, A2, L, p, R1, R2, R3, R4 and R5 are as defined in claim 1 and component B is a further therapeutic agent; wherein the combination product is for use in a method of therapeutic treatment.

Abstract: The invention relates to novel solid forms of fluoroquinolones, in particular to complex co-crystals and to solvates, hydrates and polymorphs thereof. These substances can be used to prepare a pharmaceutical composition containing same as an active ingredient, which can be used as an antibiotic. The compounds have a storage stability that is constant and above that of the salts or hydrates thereof.

Abstract: The invention describes novel triterpenoid 2-deoxy glycosides of general formula I, wherein at least one of the substituents X1 and R2 contains a 2-deoxy glycosidic group, method of preparation thereof, their cytotoxic activity and a pharmaceutical formulation containing these compounds.

Abstract: Disclosed are guanidine and biguanidine derivatives which have anti-viral and antibacterial activity. Also disclosed are pharmaceutical compositions containing such compounds as an active ingredient, and anti-viral and anti-bacterial methods utilizing such compounds. Methods of treating infections using the guanidine and biguanidine derivatives are also disclosed.

Abstract: The present invention relates to an aromatic substituted pentadienoic acid amides and there use in combination of specific amounts of aromatic amides i.e. 4-alkyl-5-(substituted phenyl)-2(E),4(E)-pentadienoic acid amides, its geometrical isomers or their dihydro or tetrahydro derivatives and an anti-infective drug useful in potentiating the bioefficacy of antiinfective drug. The combination of the present invention is useful in the treatment of certain infections and disease at lower concentration of anti-infectives necessary to inhibit the growth of microbial strains and may also find applications in reducing the resistance in microorganisms.

Abstract: The present disclosure relates to benzimidazole-benzamide derivatives, and the use thereof, e.g., to treat infections.

Abstract: The present invention relates to the use of certain quinolone antibiotics for controlling bacterial disorders of the oral cavity, in particular in veterinary medicine.

Abstract: The present invention relates to compounds of formula (I), where R1 and R2, identical or different, are each independently a hydrogen atom or a non-substituted or substituted (C1-C12) alkyl group; R3 is a hydrogen atom or a non-substituted or substituted (C1-C6) alkyl group; R4 is a non-substituted or substituted (C1-C12) alkyl group or an aryl or heteroaryl group, said aryl and heteroaryl groups being non-substituted or substituted; and R5 is a non-substituted or substituted (C1-C12) alkyl group; or R4 and R5 are bonded to one another by a saturated hydrocarbon chain having 3 or 4 carbon atoms, optionally in hydrated form or in the form of a salt that is acceptable for being administered to animals or plants, for the use thereof as a potentiator of the effect of an antimicrobial agent or for the use thereof as an antimicrobial agent.

Abstract: The invention provides an inflammation-responsive implantable device for the in situ delivery of one or more pharmaceutically active agents to a human or animal. The device comprises two differential release bioresponsive polymeric matrices (BPMs): an outer polymetric matrix and an inner polymeric matrix, both of which contain at least one pharmaceutically active agent or drug, typically an antibiotic and an anti-inflammatory agent, respectively. The therapeutically effective agent may be embedded in nanoparticles or nanobubbles. In response to inflammation, the pharmaceutically active agents are released, but at different rates: the rate of drug release from the inner polymeric matrix is lower than the rate of drug release from the outer polymeric matrix. Suitable polymers for forming the outer and inner polymeric matrices are hyaluronic acid and chitosan, respectively. A method of making the device and a method of treatment are also described.

Abstract: A composition which comprises a biologically active agent and a polymer that exhibits a reverse thermal gelation at a physiological temperature, in a carrier, and in which the active agent is in an undissolved form is disclosed herein. Further disclosed herein are methods utilizing the compositions for treating subjects, including non-human subjects, as well as kits for preparing and using a composition. The composition is preferably a sustained release formulation, and is particularly useful for treating animals, where single-dose treatment is desired.

Abstract: A pH responsive and mucoadhesive pharmaceutical dosage form for the release of a pharmaceutically active agent is described. The dosage form includes a mucoadhesive layer for site-specific mucoadhesion, a water-insoluble outer layer, and an intermediate layer including one or more pharmaceutically active agents for site-specific delivery. The different membranous layers perform different functions in order to create a drug delivery system which is able to deliver a drug to a specific site, for a particular period of time and with a specific drug release pattern. The dosage form can have two or more intermediate layers, each layer comprising an active agent. The mucoadhesive layer can also include an active agents. The dosage form is preferably an oral or buccal delivery form for release of the active agent into the gastro intestinal tract. The intermediate layer can be an electrospun fibrous membrane layer containing the active agent.

Abstract: Disclosed are novel formulations for the treatment of otic infections in an animal comprising a triazole anti-fungal compound, a quinolone antibiotic and a corticosteroid such as mometasone furoate monohydrate.

Abstract: This invention provides for biocompatible, biodegradable eye drop pharmaceutical formulations useful for the treatment of ocular indications. In particular, tocopherols and their esters of low water solubility, notably ?-tocopheryl acetate, are exceptional vehicles for biocompatible, nonirritating topical eye drop formulations that provide sustained release of active agents.

Abstract: The invention provides pharmaceutical compositions based on liquid vehicles whose density is substantially higher than that of aqueous physiological fluids. The compositions are useful as medicines in ophthalmology, in particular for the treatment of conditions affecting the posterior segment of an eye. They may be administered topically into the eye or in a minimally invasive manner by periocular injection. Preferred liquid carriers are selected from semifluorinated alkanes.

Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:

Abstract: Novel compositions and methods of reducing microbial resistance to antimicrobial agents and treating infections are disclosed. In particular, compositions and methods of inhibiting efflux pump activity, treating infection and methods of enhancing antimicrobial activity of antimicrobial agents are provided.

Abstract: The invention features compositions, methods, and kits useful for the treatment of filovirus-mediated diseases, e.g., hemorrhagic fever caused by Ebola virus, in an animal.

Abstract: This invention provides an oral veterinary pharmaceutical or nutraceutical composition comprising a physiologically tolerable gelled oil-in-water emulsion further comprising at least one component selected from taste enhancers, odour enhancers, digestive enzymes and veterinary drugs.

Abstract: A methods and compounds for inhibiting 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) are described. Also described are methods of inhibiting cell proliferation, treating cancer, and screening compounds to determine their ability to inhibit PFKFB3.

Abstract: The invention provides novel pharmaceutical compositions based on semifluorinated alkanes which are useful as carriers for a broad range of active ingredients. Preferred active ingredients include poorly water-soluble and/or hydrolytically sensitive drug substances. The compositions are designed as suspensions and have superior physical properties which make them highly useful as pharmaceutical delivery systems. The compositions may be administered topically into the eye, or injected via the subcutaneous or intramuscular route. The invention further provides kits comprising such compositions.

Abstract: The invention relates to respirable dry particles that contain one or more divalent metal cations, such as calcium, in an amount of less than 3% by weight, and to dry powders that contain the respirable particles. The dry particles can further contain an active agent, or can be used as carrier particles to deliver an active agent.

Abstract: The various embodiments herein provide a nano silicon carrier as a drug delivery mechanism. The nano silicon carrier comprises a diatom frustules loaded with a drug molecule to be released at the target site. The diatom frustules are of Hannaea arcus and Navicula inflexa species of diatom. The pore size of the diatom frustules is 1 to 100 nm. The diatom frustules are comb-like in structure. The diatom frustules are in the form of powdered diatomaceous earth. The drug delivery mechanism described in the embodiments herein is a controlled release mechanism. The nano silicon carrier described in the embodiments herein is also used for delivery of pesticides and herbicides in plants. The nano silicon carrier described in the embodiments herein is also used in hormone waste water treatment.

Abstract: Disclosed herein are compositions and methods for the treatment of otic diseases or conditions with antimicrobial agent compositions and formulations administered locally to an individual afflicted with an otic disease or condition, through direct application of these compositions and formulations onto or via perfusion into the targeted auris structure(s).

Abstract: In some embodiments, the invention provides an implant comprising a uniform mixture of degradable polymer, bone, and a drug. In some embodiments, the drug comprises an antibiotic. In some embodiments, diffusion of the drug from the implant at a therapeutic level is maintained for an amount of time longer than an amount of time that a pathogen is senescent. In some embodiments, diffusion of the drug from the implant at a therapeutic level is maintained for at least eight weeks, or at least ten weeks, or at least twelve weeks post-implantation. In some embodiments, the therapeutic level is maintained at an implantation site of the implant. In some embodiments, the implant is a solid, a paste, or a liquid. In some embodiments, the solid implant is carved or molded for insertion into a site of implantation in a vertebrate host prior to implantation. In some embodiments, the paste implant hardens following implantation. In some embodiments, the liquid implant is used to coat a prosthesis (e.g.

Abstract: It is an object of the present invention to provide antimicrobial metallodrugs comprising an antimicrobial peptide (“AMP”) and/or an antibiotic covalently bound to a metal binding moiety. These metallodrugs combine a metal binding domain which typically catalyzes oxido-reductase chemistry or acts as a Lewis-Acid catalyst, with a member of a diverse class of antimicrobial agents currently validated in preclinical and clinical settings for the treatment of a broad spectrum of pathogenic organisms.

Abstract: The present invention provides compositions and methods for increasing the delivery (i.e., bioavailability) of a compound to an ocular cell. Such compositions and methods can be used to treat an ocular clinical condition. Typically, increased bioavailability or delivery of the compound to ocular cells is achieved by utilizing a membrane transporter.

Abstract: An ophthalmic composition comprises an ophthalmic drug that has a low solubility in water and a surfactant, wherein the ophthalmic drug is present at a concentration from about 3 to about 7000 times the solubility of the drug in water. A volume of about 1-15 microliter is administered topically to an eye of a subject to treat or control a condition for which the drug is effective.

Abstract: Compositions and methods, including novel homogeneous microparticulate suspensions, are described for treating acute wounds, chronic wounds and/or a wound or epithelial tissue surface that contains bacterial biofilm, including unexpected synergy between bismuth-thiol (BT) compounds and certain antibiotics, to provide topical formulations including antiseptic formulations, for management and promotion of wound healing and in particular infected wounds. Previously unpredicted antibacterial properties and anti-biofilm properties of disclosed BT compounds and BT compound-plus-antibiotic combinations are also described, including preferential efficacies of certain such compositions for treating gram-positive bacterial infections, and distinct preferential efficacies of certain such compositions for treating gram-negative bacterial infections.

Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

Abstract: Compositions and methods related to ophthalmic use of polyvinyl capralactam-polyvinyl acetate-polyethylene glycol graft copolymers and therapeutic uses are described herein.