Abstract: An inhalation composition for the treatment of bacteria related diseases in the respiratory tract is provided. The inhalation composition may include a mixture of levofloxacin, betamethasone, and a micronized poloxamer composition (excipient/solubilizer). Micronized poloxamer composition may include poloxamer 188 and poloxamer 407. The manufacturing method for micronized poloxamer composition may include any suitable process, such as non-contact mixing technology. This technology may include an apparatus for applying low-frequency acoustic field, in order to facilitate the mixing process. Inhalation composition may be delivered to the respiratory tract employing suitable inhalation devices, such as metered-dose inhalers (MDIs), dry powder inhalers, aerosols, syringe, pipette, forceps, measured spoon, eyedropper, nebulizers, or any suitable medically approved delivery apparatus.

Abstract: The present invention relates to the detection of markers in exhaled breath, wherein the detection of the presence or absence of the marker(s) in exhaled breath is used to assess various clinical data, including patient adherence in taking the medication and patient enzymatic (metabolic) competence in metabolizing the medication. An embodiment of the invention comprises a parent therapeutic agent labeled with a marker, where upon metabolism (e.g., via enzymatic action) of the therapeutic agent, the marker becomes volatile or semi-volatile and is present in the breath. In certain related embodiments, the marker contain a deuterium label, which is also present in the breath upon metabolism of the therapeutic agent. In another embodiment of the invention, the therapeutic agent is associated with a taggant (that may be either labeled or unlabeled with deuterium), which in turn will generate a marker in the breath that is easily measurable.

Abstract: The invention relates to a medicament for the treatment of respiratory tract diseases selected from the group including rhinosinusitis, sinusitis, tonsillitis, bronchiolitis, pneumonia, and acute respiratory distress syndrome, wherein the medicament comprises glutaryl histamine or a pharmaceutically acceptable salt thereof in an effective amount. The invention also relates to use of glutaryl histamine or a pharmaceutically acceptable salt thereof for manufacture a medicament for the treatment of a respiratory tract disease. The medicament provides potentiating the effectiveness of antibacterial therapy for the treatment of respiratory tract diseases.

Abstract: The present invention provides solid pharmaceutical compositions for improved delivery of a wide variety of pharmaceutical active ingredients contained therein or separately administered. In one embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier including a substrate and an encapsulation coat on the substrate. The encapsulation coat can include different combinations of pharmaceutical active ingredients, hydrophilic surfactant, lipophilic surfactants and triglycerides. In another embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier being formed of different combinations of pharmaceutical active ingredients, hydrophilic surfactants, lipophilic surfactants and triglycerides. The compositions of the present invention can be used for improved delivery of hydrophilic or hydrophobic pharmaceutical active ingredients, such as drugs, nutritional agents, cosmeceuticals and diagnostic agents.

Abstract: The present invention provides an amorphous form of dolutegravir sodium, pharmaceutical compositions comprising same, methods for its preparation and use thereof as an antiretroviral agent.

Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.

Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as or pharmaceutically acceptable salts, or tautomerism isomers, or enantiomers, or diastereomers thereof. The invention also contains compositions including the compounds and methods of using the compounds.

Abstract: Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.

Abstract: The present invention relates to the field of antimicrobial agents. In particular, the present invention relates to the use of aerosolized fluoroquinolones formulated with divalent or trivalent cations and having improved pulmonary availability for the treatment and management of bacterial infections of the lung and upper respiratory tract.

Abstract: The composition for management of periodontal diseases includes a gel matrix having a polymer system and a plurality of microspheres dispersed in the polymer system. The polymer system contains about one-half a dose of medicament, while the micro spheres contain the remainder. Upon administration of the composition into the periodontal cavity, the medicament in the polymer system provides an initial therapeutic benefit, while the remainder of the medication is released over time via degradation of the microspheres. This biphasic pattern of medicament delivery provides increased efficacy of the medicament through sustained delivery of the same.

Abstract: The invention relates to benzoxazines useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract: It has been desired to develop a coating composition, which is used for an orally-administered preparation having an improved administering property, and/or an easily administrable preparation that does not affect dissolution property. The present invention provides a coating composition comprising: a first thickener selected from the group consisting of a carboxyvinyl polymer and sodium alginate; a polyvalent metal compound; at least one type of a second thickener selected from the group consisting of xanthan gum, guar gum and sodium alginate, with the proviso that when the first thickener is sodium alginate the second thickener is not sodium alginate; and sucralose.

Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein Ar, R1, R2, R3, G1, G2, and m are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating inflammatory disorders, cardiovascular disease, cancer, and other conditions associated with PI3K?.

Abstract: Compounds of formula I: wherein R4, R6 and R7 are defined herein, are useful as inhibitors of HIV replication.

Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R4, A1 and A2 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.

Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.

Abstract: The use of chemotherapeutic agents for the preparation of a medicament for the topical and/or local treatment of diseases caused by bacteria and/or for prophylaxis in humans or animals.

Abstract: The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.

Abstract: The present invention is directed to a compound of Formula (I): The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.

Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Abstract: Provided are certain compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections.

Abstract: The present invention relates to the field of antimicrobial agents. In particular, the present invention relates to the use of aerosolized fluoroquinolones formulated with divalent or trivalent cations and having improved pulmonary availability for the treatment and management of bacterial infections of the lung and upper respiratory tract.

Abstract: The composition for management of periodontal diseases includes a gel matrix having a polymer system and a plurality of microspheres dispersed in the polymer system. The polymer system contains about one-half a dose of medicament, while the microspheres contain the remainder. Upon administration of the composition into the periodontal cavity, the medicament in the polymer system provides an initial therapeutic benefit, while the remainder of the medication is released over time via degradation of the microspheres. This biphasic pattern of medicament delivery provides increased efficacy of the medicament through sustained delivery of the same.

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

Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, Z2, or Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, and Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: This invention relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an HIV integrase inhibitor.

Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein Ar, R1, R2, R3, G1, G2, and m are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating inflammatory disorders, cardiovascular disease, cancer, and other conditions associated with PI3K?.

Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.

Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.

Abstract: The present invention provides an imidazooxazine compound represented by Formula (I) or a salt thereof, wherein A, B, C, and D are as defined in the specification.

Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.

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: Compounds that modulate GluR5 activity and methods of using the same are disclosed.

Abstract: This invention relates to novel bi- and tricyclic indazole-substituted 1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.

Abstract: The invention relates to heterocyclic chromene-spirocyclic piperidine amides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Abstract: An agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that activates a serotonin 5-HT2C receptor, an agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that stimulates an androgen binding site, and a method of screening for a drug for the prophylaxis or treatment of abdominal pressure incontinence, which includes electrostimulating the abdominal muscles or a nerve controlling them of an animal to increase the abdominal pressure, and measuring the leak point pressure at that time.

Abstract: A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure.

Abstract: The present invention concerns products, such as compositions or medical devices, comprising one or more compounds of the Formula I, containing one or more free sulphhydryl groups, where R1 is hydrogen or an acetyl group, and R2 is a sulphhydryl group or a C1-C5 straight chained or branched hydrocarbon chain, optionally containing one or more heteroatoms selected from O, N and S, further containing one or more free sulphhydryl groups, for use in connection with Helicobacter pylori infections or other related infections, either as such or as combinations with antibiotics, whereby the compound(s) and optionally, when present, the antibiotic(s), are mixed with one or more pharmaceutically acceptable carriers providing sustained local release in the stomach or elsewhere in the upper aerodigestive tract.

Abstract: The present invention relates to methods and compositions for the treatment of pulmonary inflammation. In particular, methods and compositions using aerosol levofloxacin or ofloxacin to reduce pulmonary inflammation are provided.

Abstract: Use of a benzoyl derivative of 3-aminocarbazole to produce a drug for the preventive or therapeutic treatment of a disorder selected form the group comprising inflammatory processes, pain, fever, tumors, Alzheimer's disease and atherosclerosis. Method for the preventive or therapeutic treatment of a disorder selected from the group comprising inflammatory processes, pain, fever, tumors, Alzheimer's disease and atherosclerosis in which a therapeutically effective quantity of a benzoyl derivative of 3-aminocarbazole according to the invention is administered to an individual.

Abstract: Described herein are antibacterial compounds, methods for making the compounds, pharmaceutical compositions containing the compounds and methods of treating bacterial infections utilizing the compounds and pharmaceutical composition.

Abstract: The invention provides tricyclic sulfonamide compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

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: Multidrug resistance reversers of the d-tetrandrine family are used in conjunction with penicillins and other principle drugs used to treat MRSA.

Abstract: The invention provides tricyclic sulfonamide compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

Abstract: Disclosed herein are formulations of fluoroquinolones suitable for aerosolization and use of such formulations for aerosol administration of fluoroquinolone antimicrobials for the treatment of pulmonary bacterial infections. In particular, inhaled levofloxacin specifically formulated and delivered for bacterial infections of the lungs is described. Methods include inhalation protocols and manufacturing procedures for production and use of the compositions described.

Abstract: The present invention relates to methods and compositions for the treatment of pulmonary inflammation. In particular, methods and compositions using aerosol levofloxacin or ofloxacin to reduce pulmonary inflammation are provided.