Abstract: A compound of Formula (I): wherein A1, A2, A3, A4, A5, G1, 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 (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.

Abstract: Provided herein are tetrazolone FASN inhibitors of the formula (I): or a pharmaceutically acceptable form thereof; wherein the variables RA, 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 compound of formula (I): where A, B, C, G, m, n, o, p, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 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 (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.

Abstract: Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.

Abstract: This invention relates to a method for treating or preventing diseases associated with the deposition of ?-amyloid peptide in the brain, such as Alzheimer's disease, said method involving administration of a gamma-secretase inhibitor in an intermittent dosing regime to a patient in need thereof.

Abstract: The present invention relates to substituted pyrazoline compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.

Abstract: The present invention concerns a method for identifying a compound which inhibits the activation of RAC GTPase by DOCK5 protein comprising the steps of (i) coexpressing the DOCK5 and the RAC proteins in a cell, wherein said DOCK5 protein induces the conversion of inactive RAC, which inactive RAC is bound to GDP, to active RAC, which active RAC is bound to GTP, (ii) contacting or not said cell with said compound, (iii) determining the conversion of inactive RAC to active RAC in the presence or absence of said compound, and (iv) selecting the compound inhibiting the conversion of inactive RAC to active RAC. Said compound is useful for treating disease-associated bone loss.

Abstract: A 3,4-dihalogenoisothiazole derivative represented by the general formula [I] (wherein R1 is a halogen atom; A is an oxygen atom or a sulfur atom; and R is a C1-C6 alkyl group, a C2-C5 alkenyl group, a C2-C5 alkynyl group, a C3-C6 cycloalkyl group, a phenyl group or a 5- to 10-membered heterocyclic group containing at least one of oxygen atom, sulfur atom and nitrogen atom), or a salt thereof.

Abstract: This disclosure relates to novel benzothiadiazoles, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an ?2-adrenoceptor agonist.

Abstract: The invention relates to thiophene carboxamides of formula (I), wherein A, R1, R2, R3, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: The present invention relates to proteasome inhibitors and their use in methods of treating a subject for a pathogen infection or cancer. The methods involve administering to the subject a compound of Formula (I). (I) where: Q is Formula or Formula, where the crossing dashed line illustrates the bond formed joining Q to the rest of the compound of Formula (I). The remainder of substituents of the compound of Formula (I) are defined in the present application.

Abstract: The present invention relates to novel compounds which are antagonist or inverse agonists at an opioid receptor. Such compounds are useful in the treatment of obesity and related diseases and/or conditions in mammals, particularly humans. Methods of making and using such compounds are also disclosed.

Abstract: The invention relates to thiazolidine derivatives of the formula (I) wherein A, B, and R1 are as described in the description, to salts, especially pharmaceutically acceptable salts, of such compounds and to their use as medicaments, especially as orexin receptor antagonists.

Abstract: The present disclosure relates to novel 1,3,5 tri-substituted benzenes of general formula (I), (II) or (III) and the use of such compounds in the treatment of diseases associated with the deposition of -amyloid in the brain.

Abstract: Disclosed is a catalyst composition based on an indium salt and an organic ionic liquid, a process for making the catalyst composition, and uses thereof. The catalyst composition is particularly suitable for Lewis acid catalysed electrophilic aromatic substitution reactions, such as Friedel-Crafts alkylation reactions an Friedel-Crafts acylation reactions.

Abstract: To provide a novel and excellent method for treating and/or preventing prostatic cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and the like based on selective inhibitory activity against 17?HSD type 5. It was found that an N-sulfonylindole derivative, where the indole ring is substituted by a carboxy group, a carboxy-substituted lower alkyl group or a carboxy-substituted lower alkenyl group at its carbon atom, has potent selective inhibitory activity against 17?HSD type 5 and may become a therapeutic agent and/or preventive agent for benign prostatic hyperplasia, prostatic cancer and the like without accompanying adverse drug reactions due to a decrease in testosterone, and the present invention has thus been completed.

Abstract: The present disclosure provides methods and compositions for treating Impulse Control disorders including, for example, pathological gambling using ?2-adrenergic agonists, ?-adrenergic receptor antagonists, or both.

Abstract: The present invention relates to methods of screening for modulators of interleukin 32 (IL-32), to modulators of IL-32 and to their use.

Abstract: The present invention relates to substituted phenoxybenzamide compounds of general formula (I): in which R1, R2, R3, R4, R5, X, R6 and q are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

Abstract: A patch formulation for external use where a basic drug, an organic acid and an organic acid salt are combined as essential components is disclosed. The basic drug is preferably in the form of its acid addition salt. The organic acid is preferably a carboxylic acid having carbon atoms of 2 to 7, and more preferably at least one acid selected from the group consisting of acetic, lactic, tartaric, citric, malic, benzoic and salicylic acids. The organic acid salt is preferably a metal salt of a carboxylic acid, and more preferably sodium acetate.

Abstract: The invention relates to novel compounds and also to methods of treating at least one disease, disorder, or condition associated with amyloidosis using such compounds. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.

Abstract: The present invention provides compounds of formula I: wherein R1 is an alkyl, phenyl, heterocyclyl, cycloalkyl, alkoxy, ester, amino or amide group; R2 is a phenyl, heterocyclyl, alkyl, cycloalkyl or cycloalkylalkyl group; R3 is an alkyl, cycloalkyl, cycloalkylalkyl, amino or heterocyclyl group; R4 and R5 are hydrogen or alkyl or form a cycloalkyl ring; A is O or N; and m is zero or one; as inhibitors of GlyT1 and thus as useful for treating or preventing diseases such as schizophrenia; with the provision of pharmaceutical compositions, first and second medical uses and methods of treatment.

Abstract: The invention relates to the use of a combination of protein tyrosine phosphatase inhibitors and human growth hormone for the treatment of musculoskeletal diseases, particularly for the treatment of muscle atrophy.

Abstract: 1-Heterocyclylamino-2-hydroxy-3-amino-?-arylalkanes of formula (I) and the salts thereof have renin-inhibiting properties and can be used as antihypertensive, medicinally active ingredients.

Abstract: Disclosed herein are methods of treating a psychiatric disorder, such as a sleep disorder, an anxiety disorder, a mood disorder or a perceptual disturbance. In one example, a method of treating a sleep disorder or anxiety disorder includes selecting a subject with a sleep disturbance or anxiety disorder in the absence of an underlying physical disorder and administering a therapeutically effective amount of tizanidine, thereby reducing or inhibiting a symptom of the sleep disorder or anxiety disorder. In another example, a method of treating a mood disorder or a perceptual disturbance is disclosed. This method includes selecting a subject with a mood disorder or perceptual disturbance and administering a therapeutically effective amount of tizanidine, thereby reducing or inhibiting a symptom of the mood disorder or perceptual disturbance.

Abstract: Certain sulfonamide compounds are dual CCK1/CCK2 inhibitors useful in the treatment of CCK1/CCK2 mediated diseases.

Abstract: The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.

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: Compounds are provided which are useful in the treatment of androgen receptor-associated conditions, such as age-related diseases, which compounds have the structure wherein R1, R2, R3, R4, R4a, R4b, R4c, R4c1, Rd, Re, Rf, Rg, Rh, R5, R5?, R7, and R7? are defined herein; G is aryl, heterocycle or heteroaryl group, wherein said group is mono- or polycyclic, and which is optionally substituted; and n is an integer of 1 or 2, m is an integer of 1 or 2, Z is oxygen (—O—) or NR4b, a prodrug ester, all stereoisomers thereof and a pharmaceutically acceptable salt thereof. A method for treating androgen receptor-associated conditions such as age-related diseases is also provided.

Abstract: Provided is a triarylcarboxylic acid derivative, or an isomer, a prodrug, a hydrate, a solvate, a polymorph, or a pharmaceutically acceptable salt thereof, represented by the following general formula (I): wherein A is an optionally substituted aryl or heteroaryl, and B is an optionally substituted monocyclic heteroaryl; and a pharmaceutical composition comprising the same and a pharmaceutically acceptable carrier. The triarylcarboxylic acid derivative (I) exhibits potent xanthine oxidase inhibiting action and is therefore useful as a therapeutic agent for preventing or treating hyperuricemia, gout, inflammatory bowel disease, diabetic nephropathy and diabetic retinopathy.

Abstract: A heteroannelated anthraquinone derivative compound is provided. The heteroannelated anthraquinone derivative compound is represented by a formula (I): wherein R1 is a substituent being one selected from a group consisting of i) a first substituent being one selected from a group consisting of a hydryl group, an amino group, a nitro group, a hydroxyl group and a cyan group, ii) a second substituent being one selected from a group consisting of (CH2)nX, a straight (CH2)n alkyl group, a (CH2)n alkoxyl group, a branched (CH2)n alkyl group, a C3˜C12 nephthenic group, and a C3˜C12 cyclic alkoxyl group, wherein 1?n?12, and X is a halogen, iii) a third substituent being one selected from a group consisting of a straight C1˜C8 alkyl group with a double-bond, a C1˜C8 alkoxyl group with a double-bond, a branched C1˜C8 alkyl group with a double-bond and a C3˜C8 nephthenic group with a double-bond, and iv) a fourth substituent of a C5˜C12 heterocyclic group.

Abstract: The present invention relates to compounds of formula I wherein R1a to R1c, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.

Abstract: A heteroannelated anthraquinone derivative compound is provided. The heteroannelated anthraquinone derivative compound is represented by a formula (I): wherein R1 is a substituent being one selected from a group consisting of i) a first substituent being one selected from a group consisting of a hydryl group, an amino group, a nitro group, a hydroxyl group and a cyan group, ii) a second substituent being one selected from a group consisting of (CH2)nX, a straight (CH2)n alkyl group, a (CH2)n alkoxyl group, a branched (CH2)n alkyl group, a C3˜C12 nephthenic group, and a C3˜C12 cyclic alkoxyl group, wherein 1?n?12, and X is a halogen, iii) a third substituent being one selected from a group consisting of a straight C1˜C8 alkyl group with a double-bond, a C1˜C8 alkoxyl group with a double-bond, a branched C1˜C8 alkyl group with a double-bond and a C3˜C8 nephthenic group with a double-bond, and iv) a fourth substituent of a C5˜C12 heterocyclic group.

Abstract: The present invention provides heterocyclic derivatives hat modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.

Abstract: The invention relates to a preservative comprising at least one isothiazolone, at least one quaternary ammonium compound, and at least one stabilizer selected from the group of sulphite salts, hydrogen sulphite salts, sulphite-releasing compounds and hydrogen-sulphite-releasing compounds, the presence of algicidal triazine being ruled out. The preservative inhibits the growth of fungi, algae and bacteria on or in alkaline coating compositions. The invention furthermore relates to a process for the preparation of the preservative, to its use in a coating composition, and to the preserved composition.

Abstract: The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.

Abstract: A benzophenone derivative represented by the following formula: wherein R1 represents, for example, an optionally substituted heterocyclic group, or a substituted phenyl group; Z represents, for example, an alkylene group; R2 represents, for example, a carboxyl group optionally protected with alkyl; R3 represents, for example, an optionally protected hydroxyl group; R4 represents, for example, an optionally substituted cycloalkyloxy group; and R5 represents, for example, a hydrogen atom, or a salt thereof has anti-arthritic activity, inhibits bone destruction caused by arthritis, and provides high safety and excellent pharmacokinetics and thus is useful as therapeutic agent for arthritis. These compounds have inhibitory effect on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression of AP-1 is involved.

Abstract: This invention relates to compounds of Formula I and the use of compounds of Formula I as neuroprotective agents in the treatment of neuronal disorders of the central and peripheral nervous systems.

Abstract: The present invention discloses methods of using endothelial membrane protein 2 (EMP2) as a biomarker for stratification of endometrial premalignancy, diagnosing, staging and imaging of endometrial neoplasia. Further, methods for identifying pharmaceutical/therapeutic modalities are described, including compositions which modulate glycolipid-enriched lipid raft microdomains (GEMs).

Abstract: Methods, devices and kits for treating sleep disorders, anxiety disorders, and developmental disorders, and/or for inducing an arousable state of sedation in a subject, are described. For example, inhalation methods, devices and kits for treating insomnia, anxiety and/or ADHD using one or more ?2-adrenergic agonists such as dexmedetomidine or clonidine are described.

Abstract: The present invention relates to substituted pyrazoline compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.

Abstract: The invention relates to a modified release pharmaceutical composition in capsules with coated microspheres, combining two active ingredients with radically different plasma concentration times, namely a muscle relaxant (tizanidine) and a non-steroidal anti-inflammatory drug (meloxicam), and pharmaceutically acceptable excipients or vehicles; as well as a method for producing the composition and the use of said combination for the preparation of a drug having synergic therapeutic effect in the treatment of spasticity, disorders related to the skeletal muscle and/or muscular ailments, and moderate to severe pain in general.

Abstract: The present invention is directed to novel bicyclic heterocycles, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.

Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: This invention relates to compounds of Formula I and the use of compounds of Formula I as neuroprotective agents in the treatment of neuronal disorders of the central and peripheral nervous systems.

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: Methods are provided for treating autism spectrum disorders (ASD) using agents that activate the locus coeruleus-noradrenergic (LC-NA) system of the brain and for screening for compounds for treating ASD comprising determining whether or not the compounds activate the LC-NA system.

Abstract: The present invention relates in general to an inhibitor of a glutaminyl peptide cyclotransferase-like protein (QPCTL), and the use thereof for the treatment and/or prevention of an inflammatory disease or disorder selected from the group consisting of (a) chronic and acute inflammations, e.g. rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis; (b) other inflammatory diseases, e.g. neuropathic pain, graft rejection/graft failure/graft vasculopathy, HIV infections/AIDS, gestosis, tuberous sclerosis, Guillain-Barré syndrome, chronic inflammatory demyelinising polyradiculoneuropathy and multiple sclerosis; (c) neuroinflammation; and (d) neurodegenerative diseases, e.g. mild cognitive impairment (MCI), Alzheimer's disease, neurodegeneration in Down Syndrome, Familial British Dementia, and Familial Danish Dementia, which may result from neuroinflammation.

Abstract: Compounds of general formula (I): wherein R1, R2, R3, R4, X and Y are as defined herein are inhibitors of glutaminyl cyclase and are therefore useful in treating conditions that can be treated by modulation of glutaminyl cyclase activity.

Abstract: This invention relates to compounds of Formula I and the use of compounds of Formula I as neuroprotective agents in the treatment of neuronal disorders of the central and peripheral nervous systems.