Abstract: The invention discloses a crystal of 4-(tert-butoxyamino)-6-(6-(trifluoromethyl)pyridin-2-yl)-N-(2-(trifluoromethyl)pyridin-4-yl)-1,3,5-triazin-2-amine compound, a mesylate salt and crystal thereof, a preparation method thereof, a composition containing thereof, and a use thereof for inhibiting activity of mutant IDH2 and treating cancer.

Abstract: Certain antiviral compounds, pharmaceutical compositions, and methods related thereto are disclosed.

Abstract: The present invention provides a method for treating or preventing heart failure with preserved ejection fraction (HFPEF), wherein the method comprises administering to a patient having or at risk of developing HFPEF a therapeutically effective amount of imeglimin.

Abstract: A compound of formula I or formula II, a pharmaceutically acceptable salt, or a tautomer thereof is disclosed. In formula I and II, n is 1-6.

Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof, and/or solvates, racemic mixtures, enantiomers, diasteromers, and tautomers thereof, wherein A, R1, R2, R3, R3?, R4, R4?, R5, R6, R7, R8, m, and n are as defined in the detailed description.

Abstract: The present invention relates to a herbicidal composition comprising specific quinolinecarboxylic acids selected from quinclorac and quinmerac. The invention also relates to methods and uses for controlling undesirable vegetation, in particular in crops.

Abstract: The invention relates to purely organic emitter molecules of a new type according to formula I and to the use thereof in optoelectronic devices, in particular in organic light-emitting diodes (OLEDs), comprising donor D: an aromatic or heteraromatic chemical group on which the HOMO is located and which optionally has at least one substitution; acceptor A: an aromatic or heteromatic chemical group on which the LUMO is located and which optionally has at least one substitution; bridge B1, bridge B2: organic groups that link the donor D and the acceptor A in a non-conjugated manner; wherein in particular the energy difference ?E(S1?T1) between the lowest excited singlet (S1) state of the organic emitter molecule and the triplet (T1) state of the organic emitter molecule lying thereunder is less than 2000 cm?1.

Abstract: Formulations and methods for reducing blood glucose and/or increasing insulin signaling in a subject have been developed. The formulations include SBI-477 and compounds based on SBI-477 i.e., SBI-477 analogs (collectively, SBI-477 compounds) and/or Mondo family inhibitors, in an effective amount to inhibit intracellular lipid accumulation and/or increase cellular glucose uptake when compared to levels in a control subject not administered the composition. Also disclosed are methods of reducing intracellular lipid accumulation and/or increase glucose uptake in a subject in need thereof. The method includes administering to the subject an effective amount of SBI-477 compounds and/or Mondo family inhibitor to reducing intracellular lipid accumulation and/or increase glucose uptake in the subject.

Abstract: The invention discloses a crystal of 4-(tert-butoxyamino)-6-(6-(trifluoromethyl)pyridin-2-yl)-N-(2-(trifluoromethyl)pyridin-4-yl)-1,3,5-triazin-2-amine compound, a mesylate salt and crystal thereof, a preparation method thereof, a composition containing thereof, and a use thereof for inhibiting activity of mutant IDH2 and treating cancer.

Abstract: The present invention relates to 2-amino-4-arylpyrimidine and 2-amino-4-aryltriazine compounds as inhibitors of heat shock protein 90 family of chaperone proteins. The invention also features pharmaceutical compositions and kits that include the compounds and compositions of the invention. The invention further relates to the medical use of these compounds and compositions for the treatment of a disorder in a subject. For example, the disorder is a neurodegenerative disease.

Abstract: The present invention relates to materials for organic electroluminescent devices, in particular carbazolyl compounds substituted by electron-deficient heteroaryl groups, for use as triplet matrix materials in organic electroluminescent devices, for example the compounds of formula (1). The invention further relates to a process for preparing the compounds of the invention and to electronic devices comprising these.

Abstract: The present invention provides a 2,4,6-trisubstituted s-triazine compound represented by general formula (I) or pharmaceutically acceptable salts, prodrugs or solvates thereof, a preparation method therefor, and use of these compounds in preparing drugs for preventing or treating diseases associated with protein kinase and vimentin dysregulation, and cell vacuolization, and in particular, drugs for treating or preventing cancer growth and metastasis, tissue fibrosis and atherosclerosis.

Abstract: Provided are compounds useful for treating cancer and methods of treating cancer, for example an advanced solid tumor, such as a glioma, or angioimmunoblastic T-cell lymphoma (AITL).

Abstract: Described herein are compositions and methods for increasing the survivability of one or more beneficial microorganisms.

Abstract: Provided are compounds useful for treating cancer and methods of treating cancer, for example an advanced solid tumor, such as a glioma, or angioimmunoblastic T-cell lymphoma (AITL).

Abstract: In one aspect, the invention relates methods for inhibiting or preventing muscle atrophy or increasing muscle mass by providing to a subject in need thereof an effective amount of ursolic acid, a derivative thereof, or an analog of the ursane scaffold. 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: The invention provides novel compounds and compositions comprising a 5-HT2B antagonist of formula I: and related methods for treating a person having a disorder characterized by undesirable 5-HT2B receptor signaling, such as migraine, irritable bowel syndrome (IBS), pulmonary arterial hypertension (PAH), fibrosis, hepatocellular cancer, a small intestinal neuroendocrine tumor, cardiovascular disorders, and gastrointestinal (GI) tract disorders.

Abstract: A wound drainage and hemostasis promoting medical device (1) are disclosed. A balloon (15) is temporary inflated and arranged outside a sheath (10), in contact with tissue surrounding a wound cavity for hemostasis promotion. The drainage device comprises a fluid communication channel for wound exudate from wound. The balloon is deflated and retracted into said sheath for removal from said wound cavity. Thus the medical device is percutaneously retractable from said confined wound.

Abstract: The invention provides novel compounds and compositions comprising a 5-HT2B antagonist of formula I: and related methods for treating a person having a disorder characterized by undesirable 5-HT2B receptor signaling, such as migraine, irritable bowel syndrome (IBS), pulmonary arterial hypertension (PAH), fibrosis, hepatocellular cancer, a small intestinal neuroendocrine tumor, cardiovascular disorders, and gastrointestinal (GI) tract disorders.

Abstract: Provided are compounds useful for treating cancer and methods of treating cancer, for example an advanced solid tumor, such as a glioma, or angioimmunoblastic T-cell lymphoma (AITL).

Abstract: The invention relates to substituted 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridines of formula (I), their use as medicament, and pharmaceutical preparations comprising them. The compounds of formula (I) act on the TASK-1 potassium channel. The compounds are particularly suitable for the treatment or prevention of atrial arrhythmias, for example atrial fibrillation (AF) or arterial flutter.

Abstract: A heteroarylamine compound includes protein kinase inhibition activity, a pharmaceutically acceptable salt thereof and a pharmaceutical composition for preventing and treating a disease caused by abnormal cell growth, which contains the compound as an active ingredient.

Abstract: The invention provides triazine compounds and methods of their use to modulate protein kinases and to treat diseases mediated by said protein kinases.

Abstract: The invention provides compounds, compositions and methods for treating myotonic dystrophy. The compounds can selectively bind to CUG repeats in RNA, or to CTG repeats in DNA, and inhibit replication of the nucleic acids.

Abstract: The invention provides rationally designed multi-targeting therapeutic agents for myotonic dystrophy type 1 (DM1), an incurable neuromuscular disease that originates in an abnormal expansion of CTG repeats (CTGexp) in the DMPK gene. The rationally designed small molecules target the DM1 pathobiology in three distinct ways: (1) binding the expanded trinucleotide repeat, CTGexp, and inhibiting its transcription to the toxic CUGexp RNA, (2) binding the CUGexp RNA and releasing sequestered muscleblind-like protein (MBNL1), and (3) cleaving the toxic CUGexp in an RNase-like manner. Importantly, the compounds can reduce the levels of CUGexp in DM1 model cells and reverse two separate CUGexp-induced phenotypes of DM1.

Abstract: The present application relates to novel substituted 6-fluoro-1H-pyrazolo[4,3-b]pyridines, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for preparing Medicaments for the treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.

Abstract: The present invention relates to triazine derivatives of formula (I) for their use in the treatment of type 1 diabetes mellitus, and to compositions comprising said triazine derivatives.

Abstract: For the separation, removal, isolation, purification, characterisation, identification or quantification of fibrinogen or a protein that is a fibrinogen analogue, an affinity adsorbent is used that is a compound of formula II wherein one X is N and the other is N, C—CI or C—CN; Y is O, S or NR2; Z is O, S or NR3; R2 and R3 are each H, alkyl, hydroxyalkyl, benzyl or ?-phenylethyl; n is 0 to 6; A is a support matrix, optionally linked to the triazine ring by a spacer; R7 is a group bearing a positive charge at neutral pH; W is an optional linker; V is an aromatic group; and R8 and R9 are each H, OH, alkyl, alkoxy, amino, NH2, acyloxy, acylamino, CO2H, sulphonic acid, carbamoyl, sulphamoyl, alkylsulphonyl or halogen or a cyclic structure such as a morpholino group, or R8 and R9 are linked to form such a cyclic structure.

Abstract: The present disclosure describes compositions providing for controlled release of nitric oxide (NO) and methods for production of these compositions. In some embodiments, the compositions may include a biodegradable polymer and a nitric oxide-releasing material at least partially encapsulated by the biodegradable polymer. Nitric oxide-releasing materials may include, for example, diazeniumdiolates and nitric oxide contained within a zeolite, metal-organic framework or other porous material. In general, the compositions are spun into a porous fiber, which may be further annealed by heating in order to densify the fiber. Annealing may prolong the NO release profile. Medical devices containing the compositions described herein are also contemplated by the present disclosure. Medical devices include, for example, textiles, bandages and articles of clothing.

Abstract: The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist. A compound represented by the formula (I): wherein Ra, Rb and Rc are, (a) Ra and Rb are taken together ?Z; and Rc is a group represented by R1c; or (b) Rb and Rc are taken together to form a bond; and Ra is a group represented by —Y—R1a; R1a and R1c are each independently hydrogen, substituted or unsubstituted alkyl, etc.; R2 and R3 are each independently substituted or unsubstituted aryl, etc.; R4a and R4b are each independently hydrogen, substituted or unsubstituted alkyl, etc.; X is —N(R5)—, etc.; R5 is hydrogen, substituted or unsubstituted lower alkyl, etc.; —Y— is —O—, etc.; ?Z is ?O, etc.; and n is an integer of 0 to 4.

Abstract: The present invention generally relates to prostaglandin transport. More specifically, the invention is directed to compounds that inhibit prostaglandin transport and subsequent COX-2 induction, and methods relating thereto.

Abstract: A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Abstract: The present invention relates to disubstituted 5-fluoro pyrimidine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).

Abstract: The present application relates to novel benzyl-substituted carbamates, to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders.

Abstract: The present invention relates to inhibitors of the activity of Complex (III) of the mitochondrial electron transport chain and use thereof in treatment and/or prevention of cancers presenting tumour-initiating cells. The present invention further relates to pharmaceutical compositions containing said inhibitors alone or in combination with other pharmaceutically active agents, and their use as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit.

Abstract: Microparticles containing an ultraviolet light absorbing polymer and 3-iodo-2-propynyl butylcarbamate (“IPBC”) resist discoloration by sunlight and other ultraviolet light sources. Methods for preparing the microparticles produce polymer-shielded, formaldehyde-free IPBC formulations which resist discoloration and leaching, and are especially useful in water-based applications. The microparticles include a polymer or a poly(vinyl formal) homopolymer that absorbs light over a range of ultraviolet wavelengths associated with IPBC discoloration. The microparticles may be utilized in paints, stains, stuccoes, adhesives, and plastics, for example.

Abstract: Provided are triazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.

Abstract: The invention relates to compounds of formula (I) wherein the radicals R1 to R6 have the meaning according to claim 1, and/or physiologically acceptable salts thereof, for the prophylactic or therapeutic treatment and/or monitoring of physiological and/or pathological conditions that are associated with the activity of AMP-activated protein kinase (AMPK). Another object of the invention concerns the use of said compounds for enhancing glucose homeostasis, improving podocytopathy and/or decreasing the production of reactive oxygen species (ROS). The invention also relates to a method for in-vitro diagnosing diabetic nephropathy and a method for screening compounds that reduce podocytopathy, in each case by applying synaptopodin as biomarker.

Abstract: The present invention provides compounds which are modulators of TNF-? signaling and methods of use thereof for treating a patient having a TNF-? mediated condition.

Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.

Abstract: The present invention relates to the field of HIV-1 infections, and in particular provides novel compounds containing triazine rings and suitable spacers. The compounds according to this invention are very suitable for the prevention and/or treatment of HIV-1 infection and in particular show improved activity against NNRTI-resistant viruses of HIV-1.

Abstract: The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of disease.

Abstract: The present invention relates to compounds according to the formula I: Where Ra is H or an optionally OH-substituted C1-C3 alkyl; R1 is OR1, an optionally substituted C4-12 carbocyclic group which may be saturated or unsaturated (including aromatic) or an optionally substituted heterocyclic group; R1 is an optionally substituted C1-C14 hydrocarbyl group or an optionally substituted heterocyclic group; R2, R3 and R4 are each independently H, an optionally substituted C1-C4 alkyl group (preferably CH3, CH2CH3 or CF3), halogen (preferably F, Cl, Br), OR, CN, NO2, a C1-C6 thioether, a C1-C6 thioester group, an optionally substituted CO2R group, an optionally substituted COR group or an optionally substituted OCOR group (preferably R4 is H); R is H or an optionally substituted C1-C6 alkyl group; RHET is an optionally substituted heterocyclic group; and pharmaceutically acceptable salts, solvates or polymorphs thereof.

Abstract: A pesticidal composition comprises one or more of the following compounds: 3-(thiazol-2-yl)pyridine 1-oxide compound of formula I or II, or N-(4-chloro-2-(pyridin-3-yl)thiazol-5-yl)-3-(methylthio)propanamide compound (C3), or any agriculturally acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, and Q, are as described herein. A method of controlling pests comprises applying the pesticidal composition near a population of pests.

Abstract: The present invention relates to chimeric chemical compounds which are used to recruit antibodies to cancer cells, in particular, prostate cancer cells or metastasized prostate cancer cells. The compounds according to the present invention comprise an antibody binding terminus (ABT) moiety covalently bonded to a cell binding terminus (CBT) and Toll-like receptor agonist (TLR) through a linker and a multifunctional connector group or molecule.

Abstract: Pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase.

Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

Abstract: Compounds and compositions useful for treating disorders related to KIT and PDFGR are described herein.

Abstract: The invention discloses methods and compositions for treating or preventing RAF kinase mediated diseases or conditions by administering a compound of Formula 1: or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein.

Abstract: The present invention relates to a corticotropin releasing hormone receptor type 1 (CRHR1) antagonist for use in the treatment of depressive symptoms and/or anxiety symptoms in a novel group of patients, i.e. patients having corticotropin releasing hormone (CRH) overactivity.