Abstract: The invention relates to a compound of the formula wherein the substituents are as defined herein, and pharmaceutically acceptable salts of the compound of formula (1). The compounds of formula (1), and their salts, possess inflammation inhibiting properties and are therefore useful in the treatment and prevention of conditions related to inflammations, such as inflammatory joint diseases, or other diseases caused by chronic inflammation. This application relates to compounds of formula (1), methods for their preparation, pharmaceutical compositions comprising these compounds and their use for the preparation of medicaments for the treatment of humans and animals.

Abstract: The present invention relates to triazolopyridine compounds of general formula (I) which are Monopolar Spindle 1 kinase (Mps-1 or TTK) inhibitors: Formula (I), in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis proliferative of diseases, as well as to intermediate compounds useful in the preparation of said compounds.

Abstract: The invention relates to acylamino-phthalic acid amides and related compounds of formula (I) wherein A is —CON—R3R4, —NR5COR6, —NHR7, —OR8, —SR9, —CH2NR10R11, —(CH2)2-R12, —CH?CH—R12, —C?C—R12, optionally substituted phenyl, optionally substituted thiophenyl, or optionally substituted 1,2,3-triazol-4-yl, W is hydrogen, hydroxy or carboxymethoxy, Y is carboxy, methoxycarbonyl or 2H-tetrazol-5-yl, and the various substituents R have the meanings indicated in the description. These compounds are useful for the treatment and/or prophylaxis of skeletal muscle atrophy, schizophrenia and Alzheimer's disease, and as cognitive enhancers.

Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.

Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for killing or inhibiting the growth of a Candida or Aspergillus species or preventing or treating a mammal having candidiasis (oral and/or disseminated) or an Aspergillus infection.

Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I), where V, W, R1, R2, R3 and R4 are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.

Abstract: Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R?, R?, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.

Abstract: Provided herein are triazole FASN inhibitors of the formula (I): or a pharmaceutically acceptable form thereof; wherein the variables RA, X, RB, and RC are defined herein. Also provided herein are pharmaceutical compositions of the compounds provided herein as well as methods of their use for the treatment of various disorders such as hyperproliferative disorders, inflammatory disorders, obesity-related disorders and microbial infections.

Abstract: A method for treating a keratoconjunctival disorder, wherein the keratoconjunctival disorder comprises at least one disorder selected from the group consisting of a superficial punctate keratopathy, a corneal epithelial defect, corneal erosion, a corneal ulcer, a conjunctival epithelial defect, keratoconjunctivitis sicca, superior limbic keratoconjunctivitis, filamentary keratoconjunctivitis, keratitis and conjunctivitis, and wherein the method comprises orally administering from 3 mg/kg to 30 mg/kg per day of 2-phenyl-1,2-benzisoselenazol-3(2H)-one or a salt thereof to a patient in need thereof.

Abstract: Compounds of a certain formula I, in which R1, R2, R3, R4, R5 and R6 have the meanings indicated in the description, are effective compounds with anti-proliferative and/or apoptosis inducing activity.

Abstract: Biodegradable polymers incorporating biomolecules and methods of their use are provided. Certain aspects provide biomolecules crosslinked with diglycidyl esters. The disclosed compositions have numerous applications including cellular regeneration, wound healing, and cellular differentiation.

Abstract: Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.

Abstract: Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R1, R2, R3, R101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections.

Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

Abstract: Polyal-Drug conjugates comprising a variable rate-releasing linker are described along with methods of making such conjugates. Uses for such Polyal-Drug conjugates is also described.

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted heterocyclic amine derivative compound and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

Abstract: This invention provides novel caspase inhibitors useful for prophylaxis or treatment of a number of pathologies, including, for example, Huntington's disease. In certain embodiments the inhibitors include inhibitors of casepase-3 and/or casepase-6.

Abstract: The present invention is directed to CA IX inhibitors that conform to Formula I where the substituents X, A, B, D, E, E? and G are as defined above. Also described are Pt, 64Cu, 186Re, 188Re and 99mTc metal complexes of Formula I compounds which find use as candidate agents for imaging tumors.

Abstract: The invention provides a crystalline form of (2S,4R)-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-4-[(1H-[1,2,3]triazole-4-carbonyl)amino]pentanoic acid 5-methyl-2-oxo-[1,3]dioxol-4-ylmethyl ester or its tautomer. This invention also provides pharmaceutical compositions comprising the crystalline compound, processes and intermediates for preparing the crystalline compound, and methods of using the crystalline compound to treat diseases.

Abstract: The present invention relates to novel trifluoromethoxyphenyl-substituted tetramic acid derivatives of the formula (I), in which J, X, Y, A, B, D and G have the meanings given above, to a number of processes for their preparation, and to their use as pesticides and/or herbicides. The invention further provides selective herbicidal compositions which comprise, firstly, trifluoromethoxyphenyl-substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention further relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the additions of ammonium salts or phosphonium salts and optionally penetrants.

Abstract: According to some embodiments, the present invention provides compositions and methods for making and using multifunctional polymerized liposomes finding relevant application in medical sciences, particularly in bioimaging, diagnostics, drug delivery, and drug formulation. The compositions and methods involve lipids that are both polymerizable and have a “clickable” group that provides the ability to functionalize via a click reaction with various functional moieties useful for the above-listed applications.

Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.

Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.

Abstract: The present invention provides compounds, methods for the synthesis thereof and methods for the use thereof in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis.

Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.

Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

Abstract: Use of a monobactam antibiotic of formula (I) wherein the oxyimino group i.e. >C?N—O— has Z-orientation, or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of a bacterial infection in combination with a carbapenem antibiotic or a pharmaceutically acceptable salt thereof.

Abstract: Methods and compositions for treating disorders of the nail and nail bed. Such compositions contain a vehicle in which all components of the composition are dissolved, suspended, dispersed, or emulsified, a non-volatile solvent, a wetting agent, and a pharmaceutically active ingredient that is soluble in the non-volatile solvent and/or a mixture of the vehicle and the non-volatile solvent, which composition has a surface tension of 40 dynes/cm or less and has continuing spreadability, and which composition is effective in treating a disorder of the nail or nail bed.

Abstract: The present invention relates to method of enhancing the absorption of migraine medications and thereby treating migraines by co-administering to a subject in need thereof an effective amount of a ghrelin mimetic or pharmaceutically acceptable salt, hydrate or solvate thereof and at least one migraine medication selected from a serotonin 5-HT1B/1D receptor agonist, a tryptamine derivative, an ergoline derivative, a non-steroidal anti-inflammatory drug, or an analgesic, or any combination thereof.

Abstract: The present invention relates to substituted triazole compounds of the formula (I): and pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds for modulating SCD activity.

Abstract: Methods for preventing or treating an Apicomplexan parasite infection in a patient administering to a patient in need thereof an effective amount of a compound of Formulas I-IV.

Abstract: The present invention relates to substituted benzo-pyrimido-tetrazolo-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-pyrimido-tetrazolo-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

Abstract: Disclosed are Cathepsin-S reversible inhibitor compounds of the formula (I) which are useful in the treatment of autoimmune and other diseases. Also disclosed are pharmaceutical compositions containing the same, and methods of making and using the same.

Abstract: The present invention is concerned with novel 1,2,3-triazole-imidazole compounds of formula (I) wherein X, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of present invention have affinity and selectivity for the GABA A ?5 receptor. Further the present invention provides a method for the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as therapeutic agents.

Abstract: A process for purifying Rufinamide, comprising: a) providing a dispersion of crude 1-[(2,6-difluorophenyl)methyl]-1H-1,2,3-triazole-4-carboxamide in a solvent mixture containing at least a carboxylic acid, and dissolving it; b) slowly cooling the solution to precipitate Rufinamide crystalline form A; and c) recovering the solid.

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Abstract: This application discloses liquid compositions for administration to a patient comprising midazolam and a pharmaceutically acceptable carrier, wherein the pH of the composition is about 6 or higher, the composition comprises less than about 200 mg/ml cyclodextrin, and at least about 50% of the midazolam is present in solution. Uses of these compositions are also disclosed.

Abstract: This invention relates to tryptophan hydroxylase inhibitors, compositions comprising them, and methods of their use for the treatment, management and/or prevention of metastatic bone disease.

Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts thereof, wherein R1, R2, and R3 are as defined herein, are useful for treating flaviviridae viral infections.

Abstract: Provided herein are triazole FASN inhibitors of the formula (I): or a pharmaceutically acceptable form thereof; wherein the variables RA, X, RB, and RC are defined herein. Also provided herein are pharmaceutical compositions of the compounds provided herein as well as methods of their use for the treatment of various disorders such as hyperproliferative disorders, inflammatory disorders, obesity-related disorders and microbial infections.

Abstract: The present invention relates to allosteric binding compounds of formula (I), especially for the treatment of CNS disorders, together with pharmaceutical compositions and methods of treatment including these compounds.

Abstract: Disclosure is provided for carbamate compounds that prevent, remove and/or inhibit the formation of biofilms, compositions including these compounds, devices including these compounds, and methods of using the same.

Abstract: This invention refers to new 1,2,3-triazole and imidazole compounds included in the families of compounds represented by general formula VIII. This invention also refers to a pharmaceutical composition comprising at least one of the azole compounds represented by the general formula VIII, to the use of such compositions and to methods of treatment or inhibition of tuberculosis and leishmaniasis.

Abstract: The present invention is directed to pharmaceutical compositions comprising: (a) bendamustine, (b) a charged cyclopolysaccharide, and (c) a stabilizing agent having a charge opposite to that of the cyclopolysaccharide. Such composition provides unexpectedly desirable stability in reactive environments such as plasma, coupled with unexpectedly desirable anticancer activity. Such compositions are suitable for injection or infusion into patients in need for treatment with bendamustine.

Abstract: The subject invention is directed to the treatment of infections caused by fungi which are resistant to standard antifungal drugs such as fluconazole. The treatment method involves administering to the sufferer an effective amount of an agent that suppresses the activity of the fungal (H+)-ATPase pump (Pma1p). Such agents may take the form of: a) 2-phenyl-1,2-benzisoselenazol-3(2H)-one, commonly referred to as ebselen and depicted by Formula I, or b) 2-phenyl-1,2-benzisoselenazol-3(2H)-one 1-oxide, commonly referred to as ebselen se-oxide and depicted by Formula II, or pharmaceutically acceptable salts thereof. Opportunistic fungal infections include those which are systemic and those which are superficial and are caused by species of fungi belonging to the genus Candida, Aspergillus, Pneumocystis, Tinea, Blastomyces, Cryptococcus, Histoplasma, Sporotrichum, Malassezia, Hansenula, Rhodotorula, Trichosporon, as well as others.

Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with or mediated by G protein-coupled receptors, in particular G protein-coupled receptor 120.

Abstract: The present invention relates generally to novel macrocycles of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, B, C, D, L, M, W, Z1, Z2, Z3, Z4, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.

Abstract: Use of DIM and/or its derivatives for prevention, treatment and/or delay of age-related hearing loss in mammals.

Abstract: The current invention provides methods and compositions for treating sensorineural hearing loss including but not limited to acute acoustic trauma (AAT). The composition includes compounds which function as free radical traps such as phenyl butyl nitrone (PBN), free radical scavengers, such as edaravone, resveratrol, ebselen and iron chelator and compounds from the family of antioxidant compounds including, but not limited to, N-acetylcysteine (NAC), Acetyl-L-Carnitine (ALCAR), glutathione monoethylester, ebselen, D-methionine and carbamathione. The compositions of the current invention may be delivered by injections or orally.