Abstract: The invention relates to inhibitors of PI5P4K inhibitors useful in the treatment of cancers, neurodegenerative diseases, inflammatory disorders, and metabolic diseases, having the Formula: wherein A, X, Y, Z, Q, R1, R2, R3, R4, R5, and n are described herein.

Abstract: The invention generally relates to the use of nuclear transport modulators, e.g., CRM1 inhibitors, of Formula (I) for treating epilepsy in a subject. Subjects can have unprovoked seizures without prior warning that affect one or both hemispheres of the brain. The disclosed methods can reduce the severity and occurrence of these unprovoked epileptic seizures and can result in resolution of epilepsy. The method comprises administering to the subject an effective amount of a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: The present disclosure relates to compositions including a phenylbutyrate compound and a bile acid, and methods of processing such compositions.

Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof. Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.

Abstract: Disclosed are pharmaceutical compositions comprising tedizolid phosphate, methods of preparing such pharmaceutical compositions, and methods of treating bacterial infections with such pharmaceutical compositions. Specifically, a pharmaceutical composition comprising tedizolid phosphate, an acid; and a suspending agent; and wherein the pH of the composition upon constitution with water is between about pH 2-4.5, is provided, wherein the acid is not citric acid or malic acid.

Abstract: Disclosed are methods of treating non-alcoholic steatohepatitis (NASH) and methods of preventing NASH-induced hepatocellular carcinoma (HCC), such methods including administering O-(3-piperidino-2-hydroxy-1-propyl)-nicotinic amidoxime (BGP15), alone or in combination with a inhibitor of the interleukin-6 receptor transsignaling response, particularly gp130Fc.

Abstract: The present invention discloses a nitrogen-containing heterocyclic substituted benzoxazine oxazolidinone compound, a preparation method and use thereof in the manufacture of a medicament for treating and/or preventing infectious diseases caused by Mycobacterium tuberculosis. Specifically, the present invention relates to a compound represented by formula (I) and stereoisomer thereof, pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the compounds of the present invention, use thereof, a method for preparing the compound, in which X1, X2, R1 and R2 are described in the specification.

Abstract: The present invention relates to tetrazolylpropyl derivatives of formula (I) wherein one of V1 and V2 represents CR3 and the other one of V1 and V2 represents N, Q represents a 6-membered aromatic cycle as defined in the specification, and R1, R2, R3, R4, and R5 are defined as disclosed in the specification, to compositions comprising such compounds, to the use of said compounds as fungicides, as well as to particular intermediates useful in the synthesis of said tetrazolylpropyl derivatives.

Abstract: The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.

Abstract: A condensed ring group azacyclobutyl triazole derivative, a preparation method therefor and use thereof in medicine are provided. In particular, a condensed ring group azacyclobutyl triazole derivative as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, use thereof as a therapeutic agent, in particular as an oxytocin antagonist, and for treating or preventing a disease or a condition that is known or can exhibit a beneficial effect of inhibiting oxytocin are provided. The definition for each substituent in general formula (I) is the same as that in the description.

Abstract: The present embodiments provide for substituted triazolylpyridine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for modulating the activity of histone demethylase enzymes. Additionally, the subject compounds and compositions are useful for the treatment of cancer or other neoplastic diseases, or maladies associated with abnormal histone demethylase activity. Accordingly, the substituted triazolylpyridine derivative compounds described herein are useful in methods and medicaments for treating cancer.

Abstract: The present disclosure relates to compositions and pharmaceutical formulations comprising at least one active pharmaceutical ingredient chosen from nitrocatechol derivatives of formula I as defined herein and salts, esters, hydrates, solvates and derivatives thereof and methods of making said compositions and pharmaceutical formulations.

Abstract: New classes of thiadiazole and oxadiazole compounds for use in LC mixtures are disclosed. In an embodiment, the new classes of thiadiazoles and oxadiazoles comprise at least one phenyl ring attached to the heterocyclic ring, where no alkyl, alkenyl or alkynyl tails are attached to the phenyl ring, but one alkyl, alkenyl or alkynyl tail is attached to the other end of the molecule, and a fluoro or cyano group appears in the para position of the phenyl ring. These compounds are disclosed as being effective at inducing smectic A phases in liquid crystal mixtures, particularly in liquid crystal mixtures also possessing a smectic C phase, more particularly in materials possessing a chiral smectic C (ferroelectric) phase.

Abstract: Disclosed is a method of preparing an intermediate for an oxazolidinone derivative, which enables 5-bromo-2-(2-methyl-2H-tetrazol-5-yl)pyridine to be produced at high yield and high purity, thus exhibiting high preparation efficiency under optimal processing conditions and making it suitable for industrial mass production.

Abstract: The invention relates to pyridazinone and pyridone compounds having formula (I) or (I?), and pharmaceutically acceptable salts, hydrates, and solvates thereof wherein R1/R4 and X and X3 are as defined in the claims. The invention further relates to their use as inhibitors of copper-containing amine oxidases. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds, pharmaceutically acceptable salts, hydrates, or solvates thereof.

Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is —O—, —S—, —(C?O)—, —(C?S)—, —SO.sub.

Abstract: The present invention relates to a crystalline form of the compound (S)-3-{4-[5-(2-cyclopentyl-6-methoxy-pyridin-4-yl)-[1,2,4]oxadiazol-3-yl]-2-ethyl-6-methyl-phenoxy}-propane-1,2-diol.

Abstract: The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.

Abstract: Provided herein are radiolabelled compounds useful for imaging GSK-3 kinase. An exemplary radiolabelled compound provided herein is useful as a radiotracer for imaging GSK-3 kinase using PET imaging. Methods for preparing the radiolabelled compounds and diagnostic methods using the radiolabelled compounds are also provided.

Abstract: Compounds having the following formula: or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, wherein X is N or C—R7, are useful as kinase modulators, including IRAK-4 modulation.

Abstract: The present invention relates to compounds of formula (I): wherein A1, A2, A3, A4, G1, L, Y1, Y2, Y3, Y4, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to intermediates for preparing compounds of formula (I), to compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.

Abstract: Disclosed are compounds of Formula (I), including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic diseases. Provided herein are substituted imidazole-pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase enzymes. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as pancreatic cancer, prostate cancer, breast cancer, bladder cancer, lung cancer, gastric cancer, leukemia and/or melanoma and the like.

Abstract: The present disclosure relates to compositions and pharmaceutical formulations comprising at least one active pharmaceutical ingredient chosen from nitrocatechol derivatives of formula I as defined herein and salts, esters, hydrates, solvates and derivatives thereof and methods of making said compositions and pharmaceutical formulations.

Abstract: A compound of formula (I) where R1, R2, X, Y, n, m, R3, R4, R5, R6 and R7 are as defined herein, for use in the prophylaxis or treatment of a central and peripheral nervous system disorder, wherein the compound of formula (I) is administered prior to sleep, before bedtime or at bedtime.

Abstract: Disclosed are heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. The compounds are useful for treating a mammal suffering from any one of a range of therapeutic indications, including Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism, trichotillomania, and hypothermia.

Abstract: Disclosed are compounds and methods of using them to treat a disorder selected from the group consisting of addiction, pain, obesity, schizophrenia, epilepsy, mania and manic depression, anxiety, Alzheimer's disease, learning deficit, cognition deficit, attention deficit, memory loss, Lewy Body Dementia, Attention Deficit Hyperactivity Disorder (ADHD), Parkinson's disease, Huntington's disease, Tourette's syndrome, amyotrophic lateral sclerosis, inflammation, stroke, spinal cord injury, dyskinesias, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, autism, mutism, trichotillomania, hypothermia, and disorders of sleep.

Abstract: Disclosed herein are compounds and compositions useful in the treatment of GLS1 mediated diseases, such as cancer, having the structure of Formula I: Methods of inhibition GLS1 activity in a human or animal subject are also provided.

Abstract: The invention relates to the use of an oxodiazolyl compound (I) for the preparation of a medicament for the prevention or treatment of central and peripheral nervous system associated disorders, wherein said medicament is administered according to a dosing regimen having a dosing periodicity ranging from about twice a day to about once every other day.

Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is —O—, —S—, —(C?O)—, —(C?S)—, —SO.sub.

Abstract: The present invention relates to benzamide derivatives represented by formula (I) or pharmaceutically acceptable salts thereof.

Abstract: The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.

Abstract: Heterocyclic compounds and salts according to formula (I), which are pyrimidinone derivatives, described herein exhibit human neutrophil elastase inhibitory properties, and useful for treating diseases or conditions in which HNE is implicated.

Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water.

Abstract: One aspect of the present invention relates to substituted pyridines and pharmaceutically acceptable salts thereof that are active against a range of mammalian maladies. Another aspect of the invention relates to a pharmaceutical composition, comprising a compound of the present invention or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable excipient. The present invention also relates to methods of treating a range of mammalian maladies or conditions, including but not limited to hyperlipidemia, hypercholesterolemia, atherosclerosis, coronary artery disease, congestive heart failure, cardiovascular disease, hypertension, coronary heart disease, angina, pellagra, Hartnup's syndrome, carcinoid syndrome, arterial occlusive disease, obesity, hypothyroidism, vasoconstriction, osteoarthritis, rheumatoid arthritis, diabetes, Alzheimer's disease, lipodystrophy, or dyslipidemia, raising serum high-density lipoprotein (HDL) levels, and lowering serum low-density lipoprotein (LDL) levels.

Abstract: The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests.

Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, -L2-, and -L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to ?-amyloid (“A?”) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimer's disease, are also disclosed.

Abstract: Means for improving the solubility of luliconazole is provided. A crystal of luliconazole represented by the following formula is provided, wherein the crystal has such a crystal habit that (011) plane is a specific crystal growth plane. The crystal is characterized in that I(011) with respect to a sum total of I(001), I(100), I(10-1), I(011), I(110), I(11-1), I(10-2), I(11-2), I(020), I(021), I(20-2), I(121), I(013), I(11-3), and I(221) is not less than 25%, provided that integrated intensities of diffraction peaks, which correspond to the (001), (100), (10-1), (011), (110), (11-1), (10-2), (11-2), (020), (021), (20-2), (121), (013), (11-3), and (221) planes, are designated as I(001), I(100), I(10-1), I(011), I(110), I(11-1), I(10-2), I(11-2), I(020), I(021), I(20-2), I(121), I(013), I(11-3), and I(221) respectively in relation to the diffraction peaks detected in a range of 2?=5 to 35° in a powder X-ray diffractometry using CuK? radiation.

Abstract: Disclosed are amino triazole compounds substituted by a carboxylate functional group or an bioisosteric polar functional group. Compounds having the carboxylate moiety or carboxylate bioisostere inhibit acidic mammalian chitinase. Also provided are methods of using the compounds to treat asthma reactions caused by allergens.

Abstract: Compositions and processes for controlling nematodes are described herein, e.g., nematodes that infest plants or animals. The compounds include oxazoles, oxadiazoles and thiadiazoles.

Abstract: The present invention is directed to compounds of the Formula I as well as pharmaceutically acceptable salts thereof, that are useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the Formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula I.

Abstract: The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.

Abstract: The invention is concerned with a compound of formula (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compound of formula (I) as well as pharmaceutical compositions containing such compounds. The compound of formula (I) are SCD1 inhibitors and may be useful in treating cancer.

Abstract: A compound of formula (I): where A1, A2, A3, A4, A5, A6, G1, L, R1, R2, R3, R4, Y1, Y2 and Y3 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, molluscicidal and nematicidal compositions comprising compounds of formula (I) and to methods of using compounds of formula (I) to combat and control insect, acarine, mollusc and nematode pests.

Abstract: A method for preparing a fluorinated organic compound (II) from an organic compound (I) comprising at least one nucleofugal group Nu, and also a preparation of different specific organic compounds, in particular a fluoro-methylpyrazole compound. The method comprises: a reaction, in the presence of water, of the organic compound (I) and at least one salt providing at least one fluoride anion; and a replacement of at least one nucleofugal group Nu of the compound (I) with a fluorine atom, in order to obtain the fluorinated organic compound (II).

Abstract: The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.

Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract: To provide a polymeric compound having superior charge-providing properties, the polymeric compound contains at least one unit represented by the following general formula (5). In the general formula (5), R1 represents a hydrogen atom or an alkyl group; R2 to R4 each represent a hydrogen atom, an alkyl group, an alkoxy group, a hydroxyl group or a halogen atom, or R3 and R4 may combine each other to form a ring; and A represents a divalent linking group.

Abstract: Provided is a pharmaceutical composition comprising candesartan or ester thereof and chlorthalidone, and use thereof, wherein the weight ratio of candesartan or ester thereof to chlorthalidone is 5.3:1 to 1:6.25. The pharmaceutical composition has a synergistic antihypertensive effect, and can enhance the antihypertensive effect and extend duration of antihypertension.

Abstract: The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.