Abstract: The present invention relates to fungicidal compositions comprising, as active components, mefentrifluconazole and one or more of the following compounds: (Z)-N-allyloxy-1-(2,4-dichlorophenyl)-2-imidazol-1-yl-ethanimine, 3-chloro-4-(2,6-difluorophenyl)-6-methyl-5-phenyl-pyridazine, N?-(2,5-dimethyl-4-phenoxy-phenyl)-N-ethyl-N-methyl-formamidine, methyl (E)-2-[2-[(5-cyano-2-methyl-phenoxy)methyl]phenyl]-3-methoxy-prop-2-enoate, methyl (E)-2-[2-[(2,5-dimethylphenoxy)methyl]phenyl]-3-methoxy-prop-2-enoate, N-ethyl-2-[(3-ethynyl-8-methyl-6-quinolyl)oxy]butanamide, N-ethyl-2-[(3-ethynyl-8-methyl-6-quinolyl)oxy]-2-methylsulfanyl-acetamide, 2-[(3-ethynyl-8-methyl-6-quinolyl)oxy]-N-(2-fluoroethyl)butanamide, 2-[(3-ethynyl-8-methyl-6-quinolyl)oxy]-N-(2-fluoroethyl)-2-methoxy-acetamide, 2-[(3-ethynyl-8-methyl-6-quinolyl)oxy]-N-propyl-butanamide, 2-[(3-ethynyl-8-methyl-6-quinolyl) oxy]-2-methoxy-N-propyl-acetamide, 2-[(3-ethynyl-8-methyl-6-quinolyl)oxy]-2-methylsulfanyl-N-propyl-acetamide, 2-[(3-ethynyl-8-methyl-6-quino

Abstract: The present invention relates to a composition comprising a lithium salt of an N-substituted glycine compound and a carrier, wherein the lithium salt of the N-substituted glycine compound is of Formula (I): in which R1, R2, and R3 each are independently hydrogen, alkyl, alkenyl, alkynyl, aralkyl, carbocyclyl, aryl, or heteroaryl, or one of R1, R2, and R3 is absent. Also provided in the present invention is a method of mitigating at least one symptom of a neuropsychiatric disorder, comprising administering to a subject in need thereof the lithium salt of an N-substituted glycine compound of Formula (I).

Abstract: Methods of treating Alport syndrome and other diseases associated with a type IV collagen deficiency, and preventing hearing loss associated the same, are provided, comprising administering a compound having structure (I), or a pharmaceutically acceptable salt thereof, or administering a pharmaceutical composition comprising the compound of structure (I) or pharmaceutically acceptable salt thereof.

Abstract: The present application relates to novel substituted N-arylethyl-2-aminoquinoline-4-carboxamide derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of fibrotic and inflammatory disorders.

Abstract: The present application relates to novel substituted N-arylethyl-2-arylquinoline-4-carboxamide derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of fibrotic and inflammatory disorders.

Abstract: The present invention relates to a composition comprising a lithium salt of an N-substituted glycine compound and a carrier, wherein the lithium salt of the N-substituted glycine compound is of Formula (I): in which R1, R2, and R3 each are independently hydrogen, alkyl, alkenyl, alkynyl, aralkyl, carbocyclyl, aryl, or heteroaryl, or one of R1, R2, and R3 is absent. Also provided in the present invention is a method of mitigating at least one symptom of a neuropsychiatric disorder, comprising administering to a subject in need thereof the lithium salt of an N-substituted glycine compound of Formula (I).

Abstract: Methods of administering and pharmaceutical compositions of a biphenyl sulfonamide compound which is a dual angiotensin and endothelin receptor antagonist are disclosed for treating diseases.

Abstract: The present invention relates to radiolabeled LPA1 receptor antagonists or pharmaceutically acceptable salts thereof which are useful for the quantitative imaging of LPA1 receptors in mammals.

Abstract: The present disclosure concerns uses for isoxazole compounds or salts or analogs thereof for the treatment of wounds. The present disclosure also concerns devices for delivering a isoxazole compound or salts or an analogs thereof to a wound site.

Abstract: Methods are disclosed for treating dementia, including mild cognitive impairment, via administration of D-cycloserine, or a prodrug thereof, on a tolerance-inhibiting basis. Specifically, by administering D-cycloserine on a tolerance-inhibiting basis, tolerance to D-cycloserine is less likely than would occur via daily administration, enhancing benefits and reducing costs and side effects. Pharmaceutical compositions useful for the treatment of dementia are additionally disclosed.

Abstract: This invention provides an oral dosage regimen for the treatment of depression, a pharmaceutically acceptable medication dispensing package containing multiple dosage units of medicaments comprising an oral dosage regimen of D-cycloserine for the treatment of depression, a pharmaceutical composition comprising D-cycloserine formulated for oral administration providing a dosage of 1000 mg/day alone or in combination with antidepressant agents and uses thereof.

Abstract: Compositions and methods tor the treatment of depression and psychoses in humans are disclosed. More particularly, the invention is directed to formulations containing antipsychotic and/or antidepressant medications and also containing an NMDAR antagonist. The present invention is also directed to methods for the treatment of humans suffering from depression and other psychoses, including, schizophrenia, by administration of the inventive compositions in antidepressant and/or antipsychotic effective amounts.

Abstract: The present invention provides methods comprising applying to a crop of rice plants, the locus thereof, or propagation material thereof, a compound of formula (I): wherein —B1—B2—B3— is —C?N—O—, —C?N—CH2—, —C?CH2—O— or —N—CH2—CH2—; L is a direct bond or methylene; A1 and A2 are C—H, or one of A1 and A2 is C—H and the other is N; X1 is group X R1 is C1-C4alkyl, C1-C4haloalkyl or C3-C6cycloalkyl; R2 is chlorodifluoromethyl or trifluoromethyl; each R3 is independently bromo, chloro, fluoro or trifluoromethyl; R4 is hydrogen, halogen, methyl, halomethyl or cyano; R5 is hydrogen; or R4 and R5 together form a bridging 1,3-butadiene group; p is 2 or 3. Preferably the methods are for control of stemborer, leaffolder, hoppers, Gall midge, whorl maggot, Rice bugs, and/or Black bugs.

Abstract: The present invention provides a method of screening anti-plasmodial activity of Acriflavin, comprising assessing growth inhibition of plasmodium in vitro in chloroquine susceptible and cloroquine resistant plasmodium by Acriflavin; or measuring in-vivo plasmodium killing ability of Acriflavin; assessing localization of Acriflavin at different stages; and analyzing effect of Acriflavin on gyrase activity wherein said method utilizes Acriflavin in nano-molar range. The present invention relates to potency of Acriflavin (Acriflavin) as an anti-malarial agent both in vitro parasite culture as well as in vivo. More specifically, the invention relates to a method o determining anti-plasmodial activity, Acriflavin as potent anti-malarial agent and also relates to composition(s) comprising Acriflavin.

Abstract: The present invention relates to methods, preferably for controlling and/or preventing infestation of boll weevil in cotton, comprising applying to a crop of cotton plants, the locus thereof, or propagation material thereof, a compound of formula (I), wherein -B1-B2-B3- is —C?N—O—, —C?N—CH2—, —C?CH—O— or —N—CH2—CH2—; L is a direct bond or methylene; A1 and A2 are C—H, or one of A1 and A2 is C—H and the other is N; X1 is group X R1 is C1-C4alkyl, C1C4aloalkyl or C3-C6cycloalkyl; R2 is chlorodifluoromethyl or trifluoromethyl; each R3 is independently bromo, chloro, fluoro or trifluoromethyl; R4 is hydrogen, halogen, methyl, halomethyl or cyano; R5 is hydrogen; or R4 and R5 together form a bridging 1,3-butadiene group; p is 2 or 3.

Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.

Abstract: Methamphetamine is a highly addictive psychostimulant that causes profound damage to the brain and other body organs. Post mortem studies of human tissues have linked the use of this drug to diseases associated with aging, such as coronary atherosclerosis, but the molecular mechanism underlying these findings remains unknown. We report now that methamphetamine accelerates cellular senescence in vitro and activates transcription of genes involved in cell-cycle control and inflammation in vivo by stimulating production of the sphingolipid messenger ceramide. This pathogenic cascade is triggered by reactive oxygen species, generated through methamphetamine metabolism via cytochrome P450-2D6, which recruit nuclear factor (NF)-KB to induce expression of enzymes in the de novo pathway of ceramide biosynthesis. Inhibitors of ceramide formation prevent methamphetamine-induced senescence and attenuate systemic inflammation and health deterioration in rats self-administering the drug.

Abstract: The present invention relates to 5-oxoisoxazole derivatives of the formula I, the pharmaceutically usable salts thereof and the use thereof as medicinal substances.

Abstract: A pharmaceutical composition, medical food, dietary supplement or micronutrient for the treatment of a movement disorder comprising an NMDAR agonist or partial agonist as active ingredient therein in combination with a pharmaceutically acceptable carrier.

Abstract: Embodiments of the invention are directed to compounds that inhibit an activity of EP AC proteins and methods of using the same. The inventors have developed a sensitive and robust high throughput screening (HTS) assay for the purpose of identifying EPAC specific inhibitors (Tsalkova et al. (2012) PLOS ONE 7 (1):e30441).

Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: Methods for regulating glucagon release and of treating hypoglycemia, and for screening drug candidates for heating hypoglycemia. The methods are useful for treating diabetes melititus and screening drug candidates for potential efficacy.

Abstract: The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I.

Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.

Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.

Abstract: Embodiments of the invention include methods of treating, preventing, and/or reducing the risk of fibrosis in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction of the risk of fibrosis. In at least particular cases, the small molecules are inhibitors of STAT3.

Abstract: Compounds which modulate the CB2 receptor are disclosed. The compounds are useful for treating CB2 receptor-mediated diseases such as pain.

Abstract: The present invention relates to compositions and methods for diagnosing, preventing and treating intracranial aneurysm.

Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.

Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-?, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.

Abstract: The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic ?-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes. A spiroindoline compound represented by the general formula (1), or a salt thereof, or a solvate of the compound or the salt: [wherein ring A represents a nitrogen-containing 5-10 membered heteroaryl group; R1 and R2, which are the same or different, each represent a hydrogen atom, a halogen atom, a halo C1-6 alkyl group, a C6-10 aryl group, a cyano group, a C1-6 alkyl group optionally having a substituent, a C2-6 alkenyl group optionally having a substituent, etc.; R3 represents a hydrogen atom, a C1-6 alkyl group optionally having a substituent, etc.; and R4 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally having a substituent, etc.

Abstract: This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.

Abstract: Spiroindoline derivatives, process for their preparation and pharmaceutical compositions thereof, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially sex-hormone-related diseases in both men and women, in particularly those selected from the group of endometriosis, uterine fibroids, polycystic ovarian disease, hirsutism, precocious puberty, gonadal steroid-dependent neoplasia such as cancers of the prostate, breast and ovary, gonadotrope pituitary adenomas, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hypertrophy, contraception and infertility (e.g., assisted reproductive therapy such as in vitro fertilization). The present application relates in particular to spiroindoline derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists.

Abstract: A method of treating an ocular disorder in a subject includes administering to the subject a therapeutically effective amount of a primary amine compound of formula: wherein R1 is an aliphatic and/or aromatic compound.

Abstract: The present invention relates to compounds of formula (IA) wherein QA is QA1 or QA2 P is P1, heterocycyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, Z, 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 (IA), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (IA) and to methods of using the compounds of formula (IA) to control insect, acarine, nematode and mollusc pests.

Abstract: The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I: wherein R1, R2, R3, R5, X, A3, B1, s and n are defined herein, for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of contrast-induced nephropathy.

Abstract: Methods to treat infectious diseases are disclosed herein. Some embodiments of the invention include administration of one or more COX inhibitors (e.g., COX-1 or COX-2 inhibitors) to treat infectious diseases. Other embodiments of the invention include administration of one or more COX inhibitors (e.g., COX-1 or COX-2 inhibitors) and administration of one or more antibiotics to treat infectious diseases.

Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R6, A1, A2, X1, s and m are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: Systems and methods for longevity, anti-aging, fatigue management, obesity, weight loss, weight management, delivery of nutraceuticals, and treating hyperglycemia, Alzheimer's disease, sleep disorders, Parkinson's disease, Attention Deficit Disorder and nicotine addiction involve synchronizing and tailoring the administration of nutraceuticals, medications and other substances (for example, stimulants) in accordance with the body's natural circadian rhythms, meal times and other factors. Improved control of blood glucose levels, extended alertness, and weight control, and counteracting of disease symptoms when they are at their worst are possible.

Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

Abstract: The present invention relates to new sulfonamide URAT-1 inhibitor compounds of formula (I) or pharmaceutically acceptable salts thereof: to compositions containing them, to processes for their preparation and to intermediates used in such processes and to methods of treatment; wherein R1, R2, R3, R4, R5 and R6 are as defined in the description.

Abstract: Disclosed are (cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.

Abstract: Compounds of formula (I) and formula (II) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.

Abstract: Provided herein are sirtuin-modulating compounds of formula (II). The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.

Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).

Abstract: Described herein are compounds and compositions for the amelioration of arthritis or joint injuries by inducing mesenchymal stem cells into chondrocytes.

Abstract: The present invention relates to a method for treating ocular inflammatory diseases in a subject in need of such treatment, which comprises administering a pharmaceutical composition comprising a therapeutically effective amount of at least one agonist of Formyl peptide receptor 2.