Abstract: Provided herein are, inter alia, compositions that bind to a PDZ1 domain of MDA-9/Syntenin (syndecan binding protein: SDCBP), thereby inhibiting MDA-9/Syntenin activity, and methods of use of same. The compositions and methods provided herein are useful for treating cancer and preventing cancer metastasis, particularly in cancers that have increased MDA-9/Syntenin expression.

Abstract: A 1-cyclopropyl-6-fluoro-4-oxo-7-(4-((2-thioxobenzo[d]thiazol-3(2H)-1-3-carboxylic acid compound, its synthesis, and its use as an antimicrobial agent.

Abstract: Disclosed are methods for methods, compounds, and compositions for treating cancers characterized by therapeutic targeting of the BAP1 histone H2A deubiquitinase (DUB) complex, otherwise referred to herein as the BAP1 complex. In particular, the methods, compounds, and compositions disclosed herein relate to the use of therapeutic agents that inhibit the biological activity of the BAP1 complex for treating cancers such as myeloid neoplasms.

Abstract: Described herein are tetrahydro-pyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulation activity or function having the Formula I structure: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

Abstract: The present disclosure provides 1) an enantiomerically purified compound SRR G-1, or a derivative thereof, including specific crystal forms, salts and co-crystals that modulates G protein-coupled estrogen receptor activity, 2) pharmaceutical and cosmetic compositions comprising an enantiomerically purified SRR G-1, or a derivative thereof, and 3) methods of treating or preventing disease states and conditions and cosmetic conditions mediated through these receptors and related methods thereof in humans and animals.

Abstract: The invention relates to compound of the formula (I?) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.

Abstract: Disclosed in the present invention are a bis-?-carboline compound and a preparation method, a pharmaceutical composition and the use thereof. In particular, the bis-?-carboline compound and a pharmaceutical salt thereof are described as general formula I, and the bis-?-carboline compound is prepared through the condensation of ?-carboline intermediate and dihaloalkane. Also disclosed in the present invention are a pharmaceutical composition comprising an effective dose of the bis-?-carboline compound as shown in formula I and a pharmaceutically acceptable carrier, and the use of the bis-?-carboline compound in preparing drugs resistant to tumors such as melanoma, stomach cancer, lung cancer, breast cancer, kidney cancer, liver cancer, oral epidermoid carcinoma, cervical cancer, ovarian cancer, pancreatic cancer, prostate cancer, and colon cancer.

Abstract: Described herein are tetrahydro-pyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulation activity or function having the Formula I structure: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

Abstract: The present invention provides the following compound having anti-HIV activity of formula: wherein, A1 is C, CR1A or N; A2 is C, CR2A, or N; A3 is CR3A, CR3AR3B, N, NR3C, O, S, SO, or SO2; A4 is CR4A, CR4AR4B, N, NR4C, O, S, SO, or SO2; A5 is C, CR5A, or N; T1 ring is substituted or unsubstituted monocyclic carbocycle or substituted or unsubstituted monocyclic heterocycle; R1 is halogen, cyano, nitro or —X1—R11; R2 is substituted or unsubstituted alkyl and the like; n is 1 or 2; R3 is hydrogen, substituted or unsubstituted aromatic carbocyclyl; R4 is hydrogen or a carboxy protecting group; the other symbols are as specified in the description.

Abstract: The present invention provides compounds of Formula (I) for the treatment of parasitic diseases including malaria, as well as neurodegenerative diseases. Formula (I) wherein R3, R4, X and Y have the meaning given in claim 1.

Abstract: The invention related to pyrazolonaphthyridinone derivatives of formula (I) to their preparation and to their therapeutic use as selective inhibitors of type 2 methionine aminopeptidase (hMETAP2).

Abstract: The present invention belongs to the technical field of medicines, and relates to a crystal form of a compound used as a mineralocorticoid receptor antagonist and a preparation method therefor, and in particular, to a method for preparing a compound 2-chloro-4-[(3S,3aR)-3-cyclopentyl-7-(4-hydroxypiperidin-1-carbonyl)-3,3a,4,5-tetrahydro-2H-pyrazolo[3,4-f]quinolin-2-yl]benzonitrile of formula (1); a crystal form thereof, a preparation method for the crystal form, and the use of the crystal form in the preparation of drugs for the treatment and/or prevention of renal injury or cardiovascular diseases.

Abstract: Embodiments of bridged tetrahydroisoquinolines and methods for their use in selectively inhibiting nicotinamide adenine dinucleotide phosphate (NADPH) oxidase 2 are disclosed. The disclosed compounds have a structure according to general formula I or a pharmaceutically acceptable salt thereof: wherein “” represents a single or double bond, R1 is hydrogen, halogen, lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; Ra is hydrogen, —CH2R2, R3, or —SO2R4; R2 is lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R3 is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R4 is lower aliphatic, or substituted or unsubstituted aryl; and R5 is hydrogen, halogen, or lower aliphatic.

Abstract: The present invention relates to the pharmaceutical field, in particular to a phenanthridine derivative as shown in general formula (1) a pharmaceutical composition comprising the derivative, its preparation method, and its uses in manufacture of a medicament for the prevention or treatment of a disease related to the activity of Wnt signaling pathway, hepatitis C and hepatitis B.

Abstract: The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization and their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and Y have defined meanings.

Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

Abstract: Crystalline form, Form N-2, of N,Ndicyclopropyl-4-(1,5-dimethyl-1Hpyrazol-3-ylamino)-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide (Compound I) is provided. Also provided are a pharmaceutical composition and an oral dosage form comprising Form N-2 of Compound I as well as a method of using the Form N-2 of Compound I in the treatment of myeloproliferative disorders, which include polycythaemia vera, thrombocythaemia and primary myelofibrosis.

Abstract: An ionic liquid is used as liquid matrix for organic synthesis in homogeneous phase on soluble support, the ionic liquid being presented in liquid or solid form at ambient temperature, of formula A1+X1?, A1+ representing a cation, functional or non-functional, or a mixture of cations in which either none of the cations is functional or at least one of the cations is functional, and X1? an anion, functional or non-functional, or a mixture of anions in which either none of the anions is functional or at least one of the anions is functional.

Abstract: The present invention relates to inhibitors of the oncogenic protein kinase ALK of formula (I) as herein described and pharmaceutical compositions thereof, as well as to key intermediates towards their synthesis. The compounds of formula (I) are useful in the preparation of a medicament, in particular for the treatment of cancer.

Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where Q, R1, R2, R3, R4 and R5 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent ATM kinase mediated disease, including cancer. The specification further relates to crystalline forms of compounds of imidazo[4,5-c]quinolin-2-one compounds and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating ATM kinase mediated disease, including cancer, using such compounds and salts.

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

Abstract: Methods of using dyes and associated technology are provided. A dye, such as a monomeric dye or a dimeric dye, may be used in a nucleic acid gel staining application and/or a nucleic acid detection application. Such a dye and a salt that comprises an anion that is associated with a strong acid and a cation that is associated with a strong base may be used in such an application. A dimeric dye, such as a dimeric dye capable of forming a hairpin-like structure, may be used to stain and/or detect nucleic acids via a release-on-demand mechanism. A dimeric dye having low background fluorescence in the absence of nucleic acids and high fluorescence in the presence of nucleic acids, upon binding therewith, may be used to stain and/or detect nucleic acids.

Abstract: The present invention describes novel indenofluorene derivatives which can preferably be employed as matrix materials for phosphorescent dopants or as electron-transport materials, in particular for use in the emission and/or charge-transport layer of electroluminescent devices. The invention furthermore relates to polymers which comprise these compounds as structural units and to a process for the preparation of the compounds according to the invention and to electronic devices which comprise same.

Abstract: The present invention relates to an electronic device comprising at least one organic semiconducting material according to the following formula (I): wherein R1-4 are independently selected from H, halogen, CN, substituted or unsubstituted C1-C20-alkyl or heteroalkyl, C6-C20-aryl or C5-C20-heteroaryl, C1-C20-alkoxy or C6-C20-aryloxy, Ar is selected from substituted or unsubstituted C6-C20-aryl or C5-C20-heteroaryl, and R5 is selected from substituted or unsubstituted C6-C20-aryl or C5-C20-heteroaryl, H, F or formula (II).

Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.

Abstract: The present invention relates to a material for an organic electroluminescent device, including a phenanthrocarbazole-based compound having a specific structure, and an organic electroluminescent device including the same. More specifically, the phenanthrocarbazole-based compound is applied as a material for a phosphorescent and fluorescent organic electroluminescent device, thereby providing an organic light emitting device with improved light emitting efficiency, luminance, thermal stability, driving voltage, lifetime and the like.

Abstract: A heterocyclic compound represented by Formula 1 below, and an organic light-emitting diode including the heterocyclic compound, and a flat display device including the organic light-emitting diode. wherein Ar1 to Ar4, X1, X2, Y1, Y2, L1, and m are defined as in the specification.

Abstract: An organic photoelectric device may include an anode and a cathode configured to face each other, and an active layer between the anode and cathode, wherein the active layer includes a quinacridone derivative and a thiophene derivative having a cyanovinyl group.

Abstract: Provided is a novel compound which can be used for a transport layer or as a host material or a light-emitting material in a light-emitting element and with which a high-performance light-emitting element can be manufactured. A dibenzo[c,g]carbazole compound in which an aryl group having 14 to 30 carbon atoms and including at least anthracene is bonded to nitrogen of a dibenzo[c,g]carbazole derivative is synthesized. By use of the dibenzo[c,g]carbazole compound, a light-emitting element having very good characteristics can be obtained.

Abstract: The present invention relates to the compounds of the formula (1) and to organic electroluminescent devices, in particular blue-emitting devices, in which these compounds are used as host material or dopant in the emitting layer and/or as hole-transport material and/or as electron-transport material.

Abstract: The present invention is directed to novel compounds that are able to inhibit the interaction of paxillin or its paralogues, including leupaxin or Hic-5, with alpha.4 integrin or its binding partners that regulate signaling events downstream of the paxillin-.alpha.4 interaction. The present invention further relates to methods for therapeutic use of such compounds and pharmaceutical compositions of such compounds for the treatment of a disease or condition.

Abstract: Compounds of formula I may be used in optoelectronic devices wherein R1, R2 and R4 are, independently at each occurrence, H, a C1-C20 aliphatic radical, a C3-C20 aromatic radical, or a C3-C20 cycloaliphatic radical; R3 is H or a is, independently at each occurrence, 1 or 2; b is, independently at each occurrence, an integer ranging from 0-3; c is, independently at each occurrence, an integer ranging from 0-4; Ar is independently at each occurrence, H, or heteroaryl; and at least two of Ar are heteroaryl.

Abstract: The present invention relates to organic electroluminescent devices which comprise fluorene derivatives and spirobifluorene derivatives as matrix material for phosphorescent emitters.

Abstract: The invention relates to a polyester film incorporating at least one UV stabilizer of the formula I, in which R1 is hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkenyl, heterocycloalkyl, aryl, or heteroaryl, and R2 is a moiety which contains at least one ?-electron system, which contains a carbon atom and at least one further atom selected from carbon, oxygen, and nitrogen, where the moiety R2 contains at least one atom different from carbon, where the film includes at least one further UV absorber which does not correspond to the formula I. The invention further relates to a process for producing the film, and also to articles formed from the film.

Abstract: Inhibitors of p67phox protein are provided herein, as well as pharmaceutical compositions and methods relating thereto.

Abstract: The present invention relates to organic electroluminescent devices, in particular blue-emitting devices, in which compounds of the formulae (1) to (4) are used as host material or dopant in the emitting layer and/or as hole-transport material and/or as electron-transport material.

Abstract: Compounds comprising a 3,9-linked oligocarbazole moiety and a dibenzothiophene, dibenzofuran, dibenzoselenophene, aza-dibenzothiophene, aza-dibenzofuran, or aza-dibenzoselenophene are provided. The 3,9-linked oligocarbazole and dibenzo or aza-dibenzo moiety are separated by an aromatic spacer. The compounds may be used as non-emissive materials for phosphorescent OLEDs to provide devise having improved performance.

Abstract: There is provided an organic compound having excellent characteristics, including excellent electron-injecting/transporting performance, hole blocking ability, and high stability in the thin-film state, for use as material of an organic electroluminescent device having high efficiency and high durability. There is also provided a high-efficient and high-durable organic electroluminescent device using the compound. The compound is represented by general formula (1) having a substituted anthracene ring structure and a pyridoindole ring structure. The organic electroluminescent device includes a pair of electrodes, and one or more organic layers sandwiched between the pair of electrodes, and the compound is used as a constituent material of at least one organic layer.

Abstract: The present invention relates to a compound of the formula (1) and (2) The invention further relates to a process to produce the compound. The invention additionally relates and an electronic device containing the compound of the formula (1) or (2). The electronic device can be an organic electroluminescence devices, particularly a blue emitting device, in which compounds are used as host materials or dopants in the emitting layer and/or as hole transport materials and/or as electron transport materials.

Abstract: Disclosed herein are compounds represented by Formula 1, wherein R1, Ar1, X, Ar2, Ar3, and Het are described herein. Compositions and light-emitting devices related thereto are also disclosed.

Abstract: The present invention relates to compounds of formula (I) wherein R1, R2 and R3 are as defined in the description, to their pharmaceutical compositions and use thereof for the treatment of cancer expressing oncogenic ALK protein, particularly anaplastic large cell lymphoma (ALCL), diffuse large B cell lymphoma (DLBCL), inflammatory myofibroblastic tumors (IMT) and non-small cell lung cancer (NSCLC).

Abstract: The present invention encompasses compounds of general formula (1), wherein the groups R1 to R7, Qa, Qb, L, n and m are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, pharmaceutical preparations containing such compounds and their use as medicaments.

Abstract: Disclosed are a novel-structural compound including a 5-membered heterocycle, an organic electronic device using the same, and a terminal thereof.

Abstract: The invention discloses methods for preventing or treating addiction by administering to a subject in need thereof a PARP inhibitor.

Abstract: The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization and their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and Y have defined meanings.

Abstract: The present invention relates to novel carbazole derivatives and an organic light-emitting diode device using the same. These carbazole derivatives can simultaneously or singly be used as a hole transporting layer, a host or guest of an emitting layer or an electron transporting layer of an organic light-emitting diode device.

Abstract: The invention relates to novel hybrid cholinesterase inhibitors containing the melatonin or its oxidation products unit and tetrahydroacridine unit linked via a carbamate bond. Due to the high selectivity of action, which is expressed with high ratio of IC50 for acetylcholinesterase inhibition to IC50 for butyrylcholinesterase inhibition ([IC50(AChE)]/[IC50(BChE)]), the novel compounds may be used in relief and/or treatment of the neurodegenerative diseases, among them the Alzheimer's disease.

Abstract: Disclosed are a metal complex compound represented by the following Chemical Formula 1 or 3, and an organic light emitting diode device including the same. In Chemical Formulae 1 and 3, M1, M2, R1 to R14, y1 and y2 are as defined in the detailed description.

Abstract: The invention relates to a process for obtaining compounds derived from tetrahydro-?-carboline, specifically tadalafil and intermediate products from the synthesis, comprising the reaction between piperonal and an alkyl ester of D-tryptophan as a salt, and in the absence of any other component, followed by haloacetylation and a final cyclization with methylamine.

Abstract: An organic electroluminescent element including at least an emission layer sandwiched between an anode and a cathode, wherein the emission layer comprises at least a compound represented by Formula (A),