Abstract: The present invention features imidazolidinone compounds and pharmaceutical compositions of imidazolidinone compounds. The compounds of the invention are utilized in methods of treating a deubiquitination-related disorder in a subject and inhibiting p97-associated deubiquitination.

Abstract: Novel N-phenylacetamide compounds of formula (I): and cosmetic and pharmaceutical compositions containing same are useful for treating disorders of the sebaceous gland, e.g., acne, or have cosmetic applications.

Abstract: The present invention provides a compound represented by formula (I): wherein n is an integer selected from 1 to 20, Q is A is cyano or the like; B is hydrogen, halogen, or the like; X1 and X2 are each independently selected from O and S; E is a C1-4 alkyl group; and R1, R2, R3 and R4 are each independently selected from a hydrogen atom and a C1-C6 alkyl group, and a drug, a pharmaceutical composition containing the compound, and the like.

Abstract: The present invention relates to new compounds, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

Abstract: The present invention generally relates to various nucleases and uses thereof, and in some cases, to the UPF0054 protein superfamily. Members of the UPF0054 protein superfamily, such as the E. coli protein YbeY, may possess RNase activity and may be involved in certain important cellular processes. Disruption of YbeY activity can lead to increased sensitivity to antibiotics. Accordingly, certain embodiments of the invention are directed to systems and methods for screening target compounds for activity against UPF0054 superfamily proteins. In some embodiments, the screening method allows to target compositions to be determined that show selective activity against UPF0054 superfamily proteins. Other embodiments of the invention provide for nucleases capable of site-specific cleavage of nucleic acids.

Abstract: The present invention provides compounds having formula (I): or pharmaceutically acceptable salts and N-oxides thereof, wherein the subscript m is an integer from 0-4; Ar is an optionally substituted aryl; B is an optionally substituted aryl; L1 is an optionally substituted linking group selected from the group consisting of C1-4 alkylene, C1-4 heteroalkylene, C2-4 alkenylene and —CH2N(Ru)X5—; and L2 is a bond or C1-3 alkylene. The compounds act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity.

Abstract: The present invention is related to the composition and methods of manufacture of orally-dissolvable, edible films as a vehicle for the non-invasive administration of nitroglycerin and/or other active drugs through the mucosal tissues of the oral cavity. The films include a water soluble film-forming polymer such as pullulan. Methods for producing the films are also disclosed.

Abstract: Creatinine, creatinine precursors or the pharmaceutically acceptable salts thereof are activated to function as an antibacterial agent which has broad spectrum activity and is beneficially used in a variety of applications, such as antimicrobial wound dressings, compositions for topical delivery of the antibacterial agent and for preventing and/or inhibiting the occurrence or spread of bacterial infection, as well as the growth of odor-causing bacteria, to name a few.

Abstract: This invention relates to a novel process for the preparation of optically pure L-(+)-ergothioneine. The process for the chemical synthesis of L-ergothioneine comprises steps which consist of reacting L-histidine alkyl ester with an acid halide, chloroformate or pyrocarbonate in the presence of a base, hydrolysis of the alkyl-(S,Z)-2,4,5-triamidopent-4-enoate to obtain a (S)-alkyl 2,5-diamido-4-oxopentanoate, acid catalyzed hydrolysis of the (S)-alkyl 2,5-diamido-4-oxopentanoate followed by reaction with a metal thiocyanate to obtain the thiohistidine, protection of the sulfur of thiohistidine as the tert-butyl thioether, dialkylation of the primary amine to obtain a tertiary amine, quaternization of the tertiary amine, and removal of the protecting group to obtain the desired (S)-3-(2-mercapto-1H-imidazol-5-yl)-2-(trialkylammonio)propanoate (I). This process affords a better yield and is capable of practical application at large scale.

Abstract: The use of a substance selected from the group consisting of taurine, a taurine precursor, a taurine metabolite, a taurine derivative, a taurine analog and a substance required for the taurine biosynthesis, for manufacturing a pharmaceutical composition for preventing or inhibiting the undesirable side-effects caused to a human or an animal organism by an active ingredient that induces a high level of extracellular GABA or increases GABA receptor activation.

Abstract: The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.

Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.

Abstract: The present application relates to N-chlorinated oxazolidinone, hydantoin and imidazolidinone compounds of Formula I or pharmaceutically acceptable salts thereof, and associated compositions and methods of use as antimicrobial agents.

Abstract: The present invention provides compounds and methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.

Abstract: Imidazol-4-one or imidazole-4-thione compounds of formula (I): wherein X, R1, R2, R3, R4, R5, and R6 are defined herein. Also disclosed is a method for treating a cannabinoid receptor-mediated disorder with these compounds.

Abstract: Compounds of formula (I) or a salt thereof are provided: wherein R1, R2, R3, R4, R5, R6, R15, R7, R8 and m are as defined in the description. Uses of the compounds as medicaments, and in the manufacture of medicament for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder are also disclosed. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.

Abstract: The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.

Abstract: A method is described for treating attention deficit hyperactivity disorder (ADHD), by administering to the individual an anti-epileptic mood stabiliser at a dose which is sub-therapeutic for mood stabilisation, optionally in combination with a psychostimulant. Also described is a method of improving reading comprehension and/or fluency in an individual suffering from learning difficulties which method comprises administering to the individual an anti-epileptic mood stabiliser.

Abstract: Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.

Abstract: Compounds of formula (I) or a salt thereof are provided: wherein R6, R7, R8, R9, X, Ar, n, and m are as defined in the description. Uses of the compounds as medicaments, and in the manufacture of medicament for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder are also disclosed. The invention further discloses pharmaceutical compositions and combinations comprising the compounds.

Abstract: The invention relates to tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents.

Abstract: Compounds of the formula (I), in which R, X, R1, R2, R3 and R4 have the meanings indicated in Claim (1), are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours.

Abstract: Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.

Abstract: The present invention provides methods of reducing angiogenesis in an individual. The methods generally involve administering to the individual an effective amount of a nicotinic acetyl choline receptor antagonist. The methods are useful to treat conditions associated with or resulting from angiogenesis, particularly pathological angiogenesis. The invention further provides methods of treating a condition associated with or resulting from angiogenesis.

Abstract: The present invention relates to a novel compound of the formula I: and/or all stereoisomeric forms of the compound of the formula I and/or mixtures of these forms in any ratio, and/or a physiologically tolerated salt of the compound of the formula I, in which R1 to R5 and V1, V2 have the meanings stated in the claims and specification. The inventive compounds are suitable as inhibitors of metalloproteases, especially of ADAMTS proteases and TNF-? converting enzyme (TACE), and for the treatment of disorders such as but not limited to osteoarthrosis and rheumatoid arthritis.

Abstract: The present invention relates to polysubstituted imidazolone derivatives, to the pharmaceutical compositions comprising them and to the therapeutic uses thereof in the human and animal health fields. The present invention also relates to a process for preparing these derivatives.

Abstract: Compounds of formula (I) or a salt thereof are provided: wherein R1, R2, R3, R4, R5, R6, R7, R9, R10, X, n, p and m are as defined in the description. Uses of the compounds as medicaments, and in the manufacture of medicament for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder are also disclosed. The invention further discloses pharmaceutical compositions and combinations comprising the compounds.

Abstract: An electrical stimulation method for the treatment of peripheral neuropathy is disclosed. In a preferred embodiment, the method utilizes an electrical stimulation device that includes a plurality of channels of electrodes each of which includes a first and second electrode positioned in electrical contact with tissue of a target region suffering from peripheral neuropathy. Agonist/antagonist muscles involved in abduction/adduction, flexion/extension, supination/pronation, protraction/retraction, and/or eversion/inversion in the peripheral body regions are stimulated with a patterned series of electrical pulses through channels of electrodes in accordance with a procedure for treating peripheral neuropathy.

Abstract: Compounds of formula (I) and salts and solvates are provided. Uses of the compounds as medicaments, and in the manufacture of medicament for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder are also disclosed. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.

Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.

Abstract: This invention provides methods for the use of substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition diseases and disorders including asthma, stroke, atherosclerosis, multiple sclerosis, Parkinson's disease, arthritic disorders, rheumatic disorders, central nervous system damage resulting from stroke, central nervous system damage resulting from ischemia, central nervous system damage resulting from trauma, inflammation caused or potentiated by prostaglandins, inflammation caused or potentiated by leukotrienes, inflammation caused or potentiated by platelet activation factor, pain caused or potentiated by prostaglandins, pain caused or potentiated by leukotrienes, and pain caused or potentiated by platelet activation factor.

Abstract: Therapeutic and prophylactic treatments of aquatic species and aquatic diseases through the controlled introduction of a heterocyclic N-halamine into an aquatic habitat.

Abstract: The present invention provides a 10,11-dihydrospiro[dibenzo[a,d][7]annulene -5,4?-imidazol]-5?(1?H)-one compound of formula I Also provided are methods and compositions for the inhibition of ?-secretase (BACE) and the treatment of ?-amyloid deposits and neurofibrillary tangles.

Abstract: A compound of the formula or a pharmaceutically acceptable salt thereof, is disclosed herein. Methods and compositions related thereto are also disclosed.

Abstract: This invention relates to novel compounds having the structural formula I below and to their pharmaceutically acceptable salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.

Abstract: The invention relates to non-peptidic molecules which modulate, especially inhibit, the interaction of protein kinase A (PKA) and A kinase anchor proteins (AKAP) and to a host or target organism that comprises said non-peptidic compounds or recognition molecules directed to said compounds, such as e.g. antibodies or chelating agents. The invention also relates to a pharmaceutical agent, especially for use in the treatment of diseases that are associated with a disturbance of the cAMP signal path, especially insipid diabetes, hypertonia, pancreatic diabetes, duodenal ulcer, asthma, heart failure, obesity, AIDS, edema, hepatic cirrhosis, schizophrenia and others. The invention also relates to the use of the inventive molecules.

Abstract: Compounds of the formula I which are useful for treating or preventing inflammatory and immune cell-mediated diseases.

Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particularly those mediated by certain calcium channel subtype targets.

Abstract: Described herein are new bicyclic arylimidazolones having nootropic action (i.e., protecting and stimulating cerebral functions), analgesic action and anti hyperalgesic action; also described is the process for their preparation and pharmaceutical compositions comprising them, useful for the treatment of cognitive deficits, and of various types of pain.

Abstract: The invention relates to a fungicidally active agent containing at least one other defined fungicide in addition to the fungicide N-[2-(1,3-dimethylbutyl)-3-thienyl]-1-methyl-3-(trifluormethyl)-1H-pyrazol-4-carboxamide (penthiopyrad). The invention also relates to a method for controlling pathogenic fungi using one such agent, and to the use of said agent for controlling pathogenic fungi.

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: The present invention is directed to novel imidazolidin-2-one derivatives having a structure according to Formula I wherein a, b, R1, R2, R3, and R4 are as defined above, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.

Abstract: This invention is directed to a tetrahydro-indazole cannabinoid modulator compound of formula I: and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.

Abstract: The invention relates to compound of the formula I wherein the substituents are as defined in the specification; in free base form or in acid addition salt form; to its preparation, to its use as medicament and to medicaments comprising it.

Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated ?-amyloid deposits or ?-amyloid levels in a patient.

Abstract: The present invention relates to a compound of formula (I) having CCR2 receptor antagonistic properties, particularly anti-inflammatory properties.

Abstract: Combination therapy comprising RXR modulators and glucose reabsorption inhibitors useful for the treatment of diabetes and Syndrome X are disclosed.

Abstract: The present invention provides a 2-amino-5-[substituted-4-(difluoromethoxy)phenyl]-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.

Abstract: A method for controlling yeast-to-filamentous growth transition in fungi comprising contacting a fungal cell with an anti-fungal small molecule in an amount effective to reduce or inhibit the yeast-to-filamentous growth transition, wherein the anti-fungal small molecule is 5-(p-Bromobenzylidine)-?-isopropyl-4-oxo-2-thioxo-3-thiozolidineacetic acid or an analog thereof. A method for treating fungal infections comprising contacting one or more fungal cells with an anti-fungal small molecule in an amount effective to control the fungal infection, wherein the anti-fungal small molecule is 5-(p-Bromobenzylidine)-?-isopropyl-4-oxo-2-thioxo-3-thiozolidineactic acid or an analog thereof.

Abstract: The present invention provides a 2-amino-5-[4-(difluoromethoxy)phenyl]-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.