Abstract: Disclosed herein are materials and methods for sensitizing multidrug resistant cancer cells that express ABCG2 and related proteins members of a family of ATP-binding transporter superfamily that mediate drug efflux found in some types of multidrug resistant cancer cells. A series of compounds, including (N-(4-chlorophenyl)-2-[(6-{[4,6-di(4-morpholinyl)-1,3,5-tri-azin-2-yl]amino}-1,3-benzothiazol-2-yl)sulfanyl]acetamide), specifically inhibits ABCG2 and can be used to boost the bio-avail-ability of one or more effective cancer killing drugs, making it possible to use certain widely used chemotherapeutic reagent to treat multidrug resistance cancers. Using these compounds in combination with chemotherapeutic drugs that are substrates for ABCG2 and related proteins may also find utility in treating cancer cells that are not currently identified as multi-drug resistant. Additionally, these compounds appear to accelerate the intercellular degradation of ABCG2 and related proteins.

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: Providing a novel control agent for soft rot and a novel control method for the same. A compound having no antibacterial activity against Erwinia carotovora but having a control activity against fungi on soil surface, specifically containing, as the active ingredient, a fungicide comprising any of a strobilurin compound such as azoxystrobin and kresoxim-methyl, an azole compound such as triflumizol, cyazofamid, amisulbrom, and thiophanate-methyl, a carboxamide compound such as penthiopyrad and boscalid, a sulfonamide compound such as flusulfamide, an organic chlorine compound such as chlorothalonil, a dicarboximide compound such as pro-cymidone and iprodione, a phenylpyrrole compound such as fludioxonil, an anilinopyrimidine compound such as mepanipyrim, and a guanidine compound such as iminoctadine is the control agent for plant soft rot, which is applied to plant cultivation soil.

Abstract: The present invention relates to novel cyclic N,N?-diarylureas and N,N?-diarylthioureas—androgen receptor antagonists, anti-cancer agent, pharmaceutical composition, medicament, and method for treatment of cancerous diseases, among them prostate cancer.

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 the activity of Cannabinoid Receptor 1 (CB1).

Abstract: The present disclosure relates to 4-(2-amino-1-hydroxyethyl)phenol derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the BETA2 adrenergic receptor.

Abstract: A composition comprising at least a pyridylethylbenzamide derivative of general formula (I) (a) and a compound capable of inhibiting the methionine biosynthesis (b) in a (a)/(b) weight ratio of from 0.01 to 20. A composition further comprising an additional fungicidal compound. A method for preventively or curatively combating the phytopathogenic fungi of crops by using this composition.

Abstract: Novel compounds are disclosed that have a Formula represented by the following: wherein X, R1, R2a, R2b, R2c, R3a R3b, R4a, R4b, R4c, and m1 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, cachexia, osteoporosis, sarcopenia, a decline in libido and/or sexual dysfunction.

Abstract: Compounds having a structure of Formula I: or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein, and wherein at least one of R1, R2, R3, R4 or R5 is F, are provided. Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provided.

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

Abstract: The invention provides a method of treating acute demyelinating optic neuritis in a patient suffering therefrom, which method comprises administering a compound to the patient, wherein the compound is phenytoin or an analog or prodrug thereof. The compound acts as a neuroprotectant by partial blocking of voltage-gated sodium channels in axonal other cell membranes thereby reducing the entry of sodium into the respective cell in vivo. The treatment is particularly concerned with preserving vision after onset of the acute demyelinating optic neuritis.

Abstract: Spray dried solid dispersions comprising a sparingly soluble drug and hydroxypropylmethylcellulose acetate succinate (HPMCAS) provide increased aqueous solubility and/or bioavailability in a use environment.

Abstract: A method for assessing if a subject has or is at risk of developing cardiac arrhythmia is described. The method includes determining the activity of Rap1A protein in a bodily sample of the subject and comparing the activity of Rap1A protein from the bodily sample of the subject to at least one Rap1A control. A decreased level of Rap1A activity in the bodily sample of the subject as compared to the at least one Rap1A control indicates that the subject is at risk of developing or has cardiac arrhythmia. Methods for evaluating the efficacy of treatment of a subject having decreased Rap1A activity with an antiarrhythmic agent are also described.

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: Provided is a method for determining the prognosis of cancer in a female patient with a solid tumor. The percentage of solid tumor cells expressing TUBB3 protein and the percentage of solid tumor cells expressing TUBB6 protein in a solid tumor sample from the patient is determined.

Abstract: The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizophrenia, substance abuse disorders, sleep disorders or epilepsy.

Abstract: Disclosed is a manufacturing method for a fine powder exhibiting improved solubility, little impurity contamination, and a high recovery rate. Material to be ground and a grinding medium are suspended and stirred in a liquefied inert gas dispersion medium such as dried ice, and the material to be ground is made into a sub-micron or nano-sized fine powder. A uniform fine powder can be obtained when the material to be ground is a mixture having two or more components. Impurity contamination can be reduced by using granular dry ice as the grinding medium.

Abstract: Pharmaceutical compositions that bind to a predicted FK506 Binding Protein 52 (FKBP52) interaction surface on the androgen receptor hormone binding domain, otherwise known as FKBP52 Targeting Agents (FTAs) are provided. These compositions of the present invention are found to specifically recognize the FKBP52 regulatory surface on the androgen receptor and inhibit FKBP52 from functionally interacting with the androgen receptor. Compositions comprising the pharmaceutical composition, as well as methods of use, treatment and screening are also provided.

Abstract: The invention refers to the use of androgen receptor antagonists for the treatment and/or prevention of fibroids, also known as uterine leiomyoma, leiomyomata. Particularly, the invention refers to the use of an androgen receptor antagonist being any one of the compounds according to the following list: cyproterone acetate, oxendolone, chlormadinone acetate, spironolactone, osaterone acetate, dienogest, flutamide, hydroxyflutamide, nilutamide, bicalutamide, RU 58841, LGD-2226, MDV3100, BMS-641988, BMS-779333, or 4-(3-{[6-(2-hydroxy-2-methylpropoxy)pyridin-3-yl]methyl}-4,4-dimethyl-5-oxo-2-thioxoimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrile (thioxoimidazolidine derivative) for the treatment of fibroids.

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

Abstract: Substituted di-arylhydantoin and di-arylthiohydantoins are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including CRPC and/or hormone-sensitive prostate cancer.

Abstract: Novel compounds are disclosed that have a Formula represented by the following: wherein X, R1, R2a, R2b, R2c, R3aR3b, R4a, R4b, R4c, and m1 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, cachexia, osteoporosis, sarcopenia, a decline in libido and/or sexual dysfunction.

Abstract: The present invention relates to novel substituted thioimidazolidinone compounds and pharmaceutical compositions comprising such compounds for treatment of androgen receptor-associated diseases or disorders, such as prostate cancer, benign prostatic hypertrophy, male hair loss, muscle loss, acne and hirsutism.

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: The present invention provides methods of treating baldness in a subject and generating new hair follicles, comprising epidermal disruption and administration of a compound that promotes a differentiation of an uncommitted epidermal cell into a hair follicle cell. The present invention also provides methods for hair removal and inducing hair pigmentation.

Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.

Abstract: Provided is a method for evaluating test agents as candidates for treating prostatic diseases, including benign prostatic hyperplasia and androgen dependent and androgen independent prostate cancer. The method comprises providing a mouse comprising a human prostate primary xenograft, where the xenograft contains blood vessels that include human endothelial cells, initiating androgen deprivation in the mouse, administering to the mouse a test agent within a period of 1-7 days after initiating the androgen deprivation, and determining a reduction in human epithelial cells in the xenografts and/or a reduction in number of the endothelial cells or blood vessels in the xenograft. Also provided is a method for treating an individual for human prostate cancer or benign prostatic hyperplasia.

Abstract: The present invention is directed to a wound composition comprising an effective amount of phenytoin and an effective amount of vitamin C. The present invention is further directed to a method of treating a wound in a patient comprising administering an effective amount of phenytoin and an effective amount of vitamin C to the wound.

Abstract: The subject matter of the present application is novel imidazolidine-2,4-dione derivatives of general formula (I) in which R1, R2, R3 and X are variables. These products have an anti-proliferative activity. They are particularly advantageous for treating pathological conditions and diseases associated with abnormal cell proliferation, such as cancers. The invention also relates to pharmaceutical compositions containing said products and to the use thereof for preparing a medicament.

Abstract: The present application relates to novel imidazolidine-2,4-dione derivatives of the general formula (I), where R1, R2, R3, R4, X, and Y are variables. Said materials have an antiproliferative activity. They are particularly useful for treating pathological conditions and diseases, such as cancer, that are linked to abnormal cell proliferation. The invention also relates to pharmaceutical compositions containing said materials and to the use thereof for preparing a drug.

Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.

Abstract: The present invention relates to active compound combinations consisting, firstly, of a known halogen-substituted derivative (component A) and, secondly, of further known pesticidally active compounds (component B), which active compound combinations are suitable for controlling animal and microbial pests.

Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R6 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.

Abstract: This invention is directed to a tetrahydro-cyclopentyl pyrazole 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: Compositions, such as pharmaceutical compositions, comprising specific diarylhydantoin and diarylthiohydantoin compounds, or salts or solvates thereof, are provided. Isolated and purified forms of the compounds are also described, as are unit dosage forms, compositions of substantially pure compound and kits comprising the compounds. The compounds and pharmaceutical compositions thereof may find use in the prevention and/or treatment of a variety of conditions, including prostate cancer, Parkinson's disease, Alzheimer's disease, and others.

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

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: This invention is directed to a hexahydro-cyclooctyl pyrazole 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: Novel active compound combinations comprising a carboxamide of the general formula (I) (group 1) in which A, R1, R2 and R3 are as defined in the description, and the active compound groups (2) to (23) listed in the description have very good fungicidal properties.

Abstract: According to the present invention, a compound represented by formula (I): wherein Q is: A is a hydrogen atom, a halogen atom, —ORa or a C1-4 alkyl group which may be substituted by one or more halogen atoms; E is independently selected from a C1-6 alkyl group; m is selected from integers from 0 to 3; R2 and R3 are independently selected from a C1-6 alkyl group; X1 and X2 are independently selected from O and S; Y is selected from an arylene group and a divalent 5- or 6-membered monocyclic or 8- to 10-membered condensed heterocyclic group, wherein the arylene group and the heterocyclic group may be substituted by 1 to 3 substituents independently selected from E1; E1 is independently selected from a hydroxyl group, a halogen atom, a C1-4 alkyl group, a cyano group, a C1-4 alkoky group, a carbamoyl group, a C1-4 alkylcarbamoyl group, a di(C1-4 alkyl)carbamoyl group, an amino group, a C1-4 alkylamino group, a di(C1-4 alkylamino group, a sulfamoyl group, a C1-4 alkylsulfamoyl group and a di(C1-4 alkyl)su

Abstract: Disclosed herein are materials and methods for sensitizing multidrug resistant cancer cells that express ABCG2 and related proteins members of a family of ATP-binding transporter superfamily that mediate drug efflux found in some types of multidrug resistant caner cells. A series of compounds, including (N-(4-chlorophenyl)-2-[(6-{[4,6-di(4-morpholinyl)-1,3,5-tri-azin-2-yl]amino}-1,3-benzothiazol-2-yl)sulfanyl]acetamide), specifically inhibits ABCG2 and can be used to boost the bio-avail-ability of one or more effective cancer killing drugs, making it possible to use certain widely used chemotherapeutic reagent to treat multidrug resistance cancers. Using these compounds in combination with chemotherapeutic drugs that are substrates for ABCG2 and related proteins may also find utility in treating cancer cells that are not currently identified as multi-drug resistant Additionally, these compounds appear to accelerate the intercellular degradation of ABCG2 and related proteins.

Abstract: Tannate compositions containing active pharmaceutical ingredients to be used for treating nausea, vomiting, pain, convulsions, and insomnia and manufacturing processes for preparing the tannate compositions.

Abstract: The invention relates to the use of at least one leukotriene inhibitor for preparing a pharmaceutical composition for the prophylaxis and/or treatment of lung diseases, more particularly of bronchopulmonary dysplasia, in prematurely born infants. The invention further relates to a pharmaceutical composition for the prophylaxis and/or treatment of lung diseases, more particularly of bronchopulmonary dysplasia, in prematurely born infants, the pharmaceutical composition comprising at least one leukotriene inhibitor. The invention additionally relates to a method for the treatment and/or prophylaxis of a lung disease, more particularly of a bronchopulmonary dysplasia, in a prematurely born infant, where the prematurely born infant is administered a pharmacologically active amount of at least one leukotriene inhibitor.

Abstract: The disclosure relates to inhibitors of Pim-1 and/or Pim-2 protein kinase, to compositions comprising one or more inhibitors of Pim-1 and/or Pim-2 protein kinase, and to methods for treating cancer.

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 of formula (I) wherein: R1 is a group selected from —CH2OH, —NHC(O)H and R7 is a hydrogen atom; or R1 together with R2 form the group —NH—C(O)—CH?CH— wherein the nitrogen atom is bound to the carbon atom in the phenyl ring holding R1 and the carbon atom is bound to the carbon is atom in the phenyl ring holding R2; R3 is selected from hydrogen and halogen atoms or groups selected from —SO—R5, —SO2—R5, —NH—CO—NH2, —CO—NH2, hydantoino, C1-4alkyl, C1-4alkoxy and —SO2NR5R6; R4 is selected from hydrogen atoms, halogen atoms and C1-4alkyl groups; R5 is a C1-4alkyl group or C3-5 cycloalkyl; R6 is independently selected from hydrogen atoms and C1-4alkyl groups; n, p and q are independently 0, 1, 2, 3 or 4: m and s are independently 0, 1, 2 or 3; r is 0, 1 or 2; with the provisos that: at least one of m and r is not 0; the sum n+m+p+q+r+s is 7, 8, 9, 10, 11, 12 or 13: the sum q+r+s is 2, 3, 4, 5 or 6 or a pharmaceutically-acceptable salt, solvate or stereoisomer thereof.

Abstract: The present invention provides a compound of formula (I) wherein: R1 is a group selected from —CH2OH, —NHC(O)H and R2 is a hydrogen atom; or R1 together with R2 form the group —NH—C(O)—CH?CH— wherein the nitrogen atom is bound to the carbon atom in the phenyl ring holding R1 and the carbon atom is bound to the carbon atom in the phenyl ring holding R2; R3 is selected from hydrogen and halogen atoms or groups selected from —SO—R5, —SO2—R5, —NH—CO—NH2, —CO—NH2, hydantoino, C1-4alkyl, C1-4alkoxy and —SO2NR5R6; R4 is selected from hydrogen atoms, halogen atoms and C1-4alkyl groups; R5 is a C1-4alkyl group or C3-8 cycloalkyl; R6 is independently selected from hydrogen atoms and C1-4alkyl groups; n, p and q are independently 0, 1, 2, 3 or 4; m and s are independently 0, 1, 2 or 3; r is 0, 1 or 2; with the provisos that at least one of m and r is not 0; the sum n+n+p+q+r+s is 7, 8, 9, 10, 11, 12 or 13; the sum q+r+s is 2, 3, 4, 5 or 6 or a pharmaceutically-acceptable salt, solvate or stereoisomer thereof.

Abstract: The present invention provides a method of optimizing therapeutic efficacy and reducing toxicity associated with 6-mercaptopurine drug treatment of an immune-mediated gastrointestinal disorder such as inflammatory bowel disease. The method of the invention includes the step of determining the level of one or more 6-mercaptopurine metabolites in the patient having an immune-mediated gastrointestinal disorder.

Abstract: Disclosed are molecules and their synthesis, for use in blocking gated ion channels such as voltage-gated sodium channels (VGSCs) and prostate voltage sodium channels (PVSCs). These inhibitors have superior blocking efficacy, for instance in displacing the radioligand [3H]-Batrachotoxin-B ([3H]-BTX-B) that binds to site 2 of a VGSC. The molecules of the invention comprise a moiety which increases the binding affinity of molecules for the protein binding site in prostate cancer cells (PCs), and which is also fluorescent. In one embodiment the invention molecules are an inhibition system that can be used to target over-abundant or hyperactive VGSCs selectively in pain, epilepsy or prostate cancer, inhibiting the proliferation of PCs. The fluorescent moiety also facilitates screening, tracking, and pharmacodynamic studies of the drug in a biological system both in vitro and in vivo.

Abstract: Small molecule choline kinase inhibitors, pharmaceutical compositions thereof, and screening methods for identifying and evaluating choline kinase inhibitors are provided. Safe and effective methods for treating subjects suffering from a disorder or disease characterized by neoplastic cell proliferation employing the choline kinase inhibitors are also provided.