Abstract: The invention provides novel methods for preparing substituted indoline compounds and their synthetic precursors.

Abstract: The present invention concerns substituted indoline derivatives, methods to prevent or treat dengue viral infections by using said compounds and also relates to said compounds for use as a medicine, more preferably for use as a medicine to treat or prevent dengue viral infections. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of dengue viral infections. The invention also relates to processes for preparation of the compounds.

Abstract: Methods and compositions are described for enhancing tissue regeneration or wound repair in a mammalian subject comprising a composition comprising (a) a proline hydroxylase inhibitor component or molecule that increases or upregulates HIF1a and (b) a carrier component comprising a hydrogel.

Abstract: Disclosed are compositions and methods for treatment of a disease or disorder of the eye and adnexa of the eye, including dry eye disease and Sjögren's syndrome, by administering a composition comprising an indole and a flavonoid either as an admixture or as a synthetic heterodimer thereof.

Abstract: The present disclosure relates to prostate specific membrane antigen (PSMA) targeted compounds conjugated to near-infra red (NIR) dyes and methods for a method for synthesizing a compound of the formula:

Abstract: Methods and compositions are described for enhancing tissue regeneration or wound repair in a mammalian subject comprising a composition comprising (a) a proline hydroxylase inhibitor component or molecule that increases or upregulates HIF1a and (b) a carrier component comprising a hydrogel.

Abstract: Methods and compositions are described for enhancing tissue regeneration or wound repair in a mammalian subject comprising a composition comprising (a) a proline hydroxylase inhibitor component or molecule that increases or upregulates HIF1a and (b) a carrier component comprising a hydrogel.

Abstract: Provided is a method for producing a compound represented by a formula (6), the method comprising: a step of mixing a compound represented by a formula (4) and a compound represented by a formula (5) to form a salt consisting of the compound represented by the formula (4) and the compound represented by the formula (5); and a step of removing a protecting group P1 of the salt. In the following formulae, P1 is a protecting group and P2 is a protecting group.

Abstract: The present invention describes nanoprodrugs of non-steroidal anti-inflammatory drug (NSAIDs) and nanoprodrugs of ?-lipoic acid-containing and NSAIDs. These nanoprodrugs have antioxidant properties and stimuli-responsiveness, which can be used to treat various disease conditions.

Abstract: The photoelectric conversion device described herein includes a working electrode having a dye-supported metal oxide electrode in which a dye is supported on a metal oxide layer. The dye includes a structure represented by general formula (I) wherein A is a structure having a maximum absorption wavelength ?max of 350 to 500 nm in a methanol solution; B is a cyanine skeleton having a maximum absorption wavelength ?max of 500 to 700 nm in a methanol solution; Z1 is any one divalent linking group selected from —CONR—, —NRCO—, —SO2NR—, and —NRSO2—; R in Z1 is a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or an arylalkyl group having 7 to 20 carbon atoms; Y1 and Y2 are each independently an alkylene group having 1 to 8 carbon atoms, or a single bond, and may be the same or different; r is 1 or 2; m and n are each independently an integer of 0 to 2; and (m+n) is 1 or more.

Abstract: The present invention provides methods and intermediates for the preparation of (1aR,12bS)-8-cyclohexyl-11-fluoro-N-((1-methylcyclopropyl)sulfonyl)-1a-((3-methyl-3,8-diazabicyclo[3.2.1]oct-8-yl)carbonyl)-1,1a,2,12b-tetrahydrocyclopropa[d]indolo[2,1-a][2]benzazepine-5-carboxamide (formula I), including pharmaceutically acceptable salts. The compound has activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

Abstract: The invention relates to a compound of formula (I) wherein A1, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

Abstract: A pharmaceutical composition, a method of producing same, and a method of providing cancer therapy therein comprising a pharmaceutically acceptable excipient or carrier and a compound Formula 3 as follows: or a pharmaceutically acceptable salt or prodrug thereof, wherein: R1, R2, R3 and R4 are optionally substituted and are hydrogen, haloalkyl, aryl, fused aryl, carbocyclic, a heterocyclic group, a heteroaryl group, C1-10 alkyl, alkenyl, alkynyl, arylalkyl, arylalkenyl, arylalkynyl, heteroarylalkyl, heteroarylalkenyl, carbocycloalkyl, heterocycloalkyl, hydroxyalkyl, aminoalkyl, carboxyalkyl, nitroalkyl, cyanoalkyl, acetamidoalkyl, acyloxyalkyl, hydroxyl, alkoxy, acetoxy, amino, alkylamino, acetamido.

Abstract: The invention provides compositions and methods for wound healing and scar reduction. The compositions and methods of the invention include at least one EP4 agonist set forth herein. Wounds and or scars that can be treated by the compositions and methods of the invention can arise from events such as surgery, trauma, disease, mechanical injury, burn, radiation, poisoning, and the like.

Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

Abstract: The invention provides indole and indoline derivatives and slats thereof, compositions comprising them and uses thereof for the treatment of diseases and disorders.

Abstract: Novel use of small molecules, particularly indolyl and indolinyl hydroxamates is disclosed herein. The indolyl and indolinyl hydroxamates are useful as lead compounds for manufacturing a medicament or a pharmaceutical composition for treating a patient suffering from heart failure or neuronal injury.

Abstract: Disclosed are selective histone deactylase inhibitors (HDACi) that having Formula (I). Methods of making and using these inhibitors for the treatment of cancer, in particular melanoma are also disclosed.

Abstract: The present invention relates to processes and intermediates useful for the manufacture of spiroindolone compounds such as (1?R,3?S)-5,7?-dichloro-6?-fluoro-3?-methyl-2?,3?,4?,9?-tetrahydrospiro[indoline-3,1?-pyrido[3,4-b]indol]-2-one and salts and hydrates and solvates thereof.

Abstract: The present invention relates to a process for preparing silodosin with high optical purity up to 99.9% enantiomeric excess (e.e.) or above. The process makes use of a method step, in which the enantiomers contained in a racemic mixture of a compound represented by the general formula V: wherein * denotes the asymmetric center, R1 is a protecting group, and R2 is cyano or carbamoyl, are separated.

Abstract: Provided are compositions for inhibiting a biological activity of an aldoketo reductase family 1, member C3 (AKR1 C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1 C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects.

Abstract: The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.

Abstract: The object of the invention is to provide a technique of suppressing tumorigenesis in IPS cells and inducing differentiation into target differentiated cells. In use of a statin and a differentiation inducer, iPS cells are differentiated into target differentiated cells, whereby iPS cells can be differentiated into differentiated cells in which tumorigenesis is suppressed.

Abstract: The synthesis and evaluation of gastroprotective effect of different tryptamine derivatives. Tryptamine derivatives have been synthesized by formation of amide or ester with some known anti oxidant molecules. These derivatives show excellent antioxidant property in vitro. Among all the derivatives the compound SEGA (3a), that was prepared by the combination of serotonin with gallic acid shows the greater antioxidant property than the other synthesized compounds both in vivo and in vitro. SEGA(3a) shows the gastroprotective effect against NSAIDs (indomethacin or diclofenac)-induced gastropathy in dose dependent manner and also accelerates the healing from injury. It prevents the NSAIDs-induced mitochondrial oxidative stress in vivo. This derivative prevents NSAID-induced mitochondrial oxidative stress-mediated apoptosis in vivo by preventing the activation of caspase 9 and caspase-3 and restores NSAIDs-mediated collapse of mitochondroial transmembrane potential and dehydrogenase activity.

Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.

Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1-R7, X1, X2, R, Q, and n are as defined herein.

Abstract: Indolyl or indolinyl compounds of formula (I): wherein bond, n, R1, R2, R3, R4, R5, and R6, are defined herein. Also disclosed is a method for treating cancer with these compounds.

Abstract: The present invention describes single drug entities, formed by connecting an antibiotic moiety via a linker with a non-steroidal anti-inflammatory drug (NSAID) moiety. Upon topical application to the eye, the conjugate hybrid would undergo enzymatic and/or hydrolytic cleavage to release the individual antibiotic and NSAID drug.

Abstract: A protecting group for 1-nitrogen atom of an indole group including a sulfonylethyl carbamate group, wherein the protecting group is represented by the following General Formula (I) and capable of being removed from the 1-nitrogen atom of the indole group in an aprotic solvent: where R represents an alkyl group, a derivative of the alkyl group, a phenyl group or a derivative of the phenyl group.

Abstract: The present invention relates, in a first aspect, to a process preparing vilazodone hydrochloride that comprises the reaction of 3-(4-chloro-1-hydroxy-butyl)-1H-indol-5-carbonitrile with 5-piperazin-1-yl-benzofuran-2-carboxylate methyl hydrochloride with the formation of a 1,4-piperazine, with subsequent dehydration, hydrogenation and treatment with ammonia, to obtain vilazodone in free base form that is then converted into the hydrochloride thereof.

Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.

Abstract: The present invention relates, in a first aspect, to a process preparing vilazodone hydrochloride that comprises the reaction of 3-(4-chloro-1-hydroxy-butyl)-1H-indol-5-carbonitrile with 5-piperazin-1-yl-benzofuran-2-carboxylate methyl hydrochloride with the formation of a 1,4-piperazine, with subsequent dehydration, hydrogenation and treatment with ammonia, to obtain vilazodone in free base form that is then converted into the hydrochloride thereof.

Abstract: An agent in foam form for coloring keratin-containing fibers, in particular human hair, under induction by atmospheric oxygen and methods for coloring keratin-containing fibers using such agent is provided. In an embodiment, the agent comprises, in a cosmetically acceptable carrier, at an alkaline pH of 8 to 10.5, (a) as a color-forming component in the form of a dye precursor of a nature-analogous dye an indole and/or indoline derivative, (b) an alkalizing agent, and (c) a propellant, the agent containing no additional oxidizing agent for the color-forming components.

Abstract: The present invention relates to an indole derivative, The indole derivative according to the present invention effectively inhibits the activity of diacylglycerol acyltransferase (DGAT) which induces metabolic diseases, such as obesity, diabetes, hyperlipidemia, or fatty liver and the like in lipid metabolism, thereby effectively regulating lipid metabolism and energy metabolism, and thus can be useful in pharmaceutical compositions for preventing or treating metabolic disease.

Abstract: The present invention relates to compounds derived from taurine with non-steroidal anti inflammatory activity. In a first embodiment, the present invention relates to compounds derived from taurine, in which taurine is bound directly by means of an amide bond or through an spacing group, to a compound selected from the group of non-steroidal anti inflammatory compounds, cited as derived from taurine presenting the Formula (I): in which R means the component with non-steroidal anti inflammatory activity. In a second embodiment, the invention provides a process for obtaining the compounds of Formula (I) by reaction of taurine with a compound belonging to the group of non-steroidal anti inflammatory (NSAIs), in order to obtain a compound derived from taurine by direct bond or through a spacing group of the taurine to the NSAI. The invention also relates to the pharmaceutical compositions comprising at least one compound derived from taurine presenting non-steroidal anti inflammatory activity.

Abstract: The present invention relates to photolabile or photoreleasable compounds including a caging moiety linked to an effector moiety, wherein the compounds are capable of releasing the effector moiety on irradiation, typically by flash irradiation with UV light. These compounds are particularly suitable for focal 2-photon uncaging The photoreleasable compounds can be used to deliver effector moieties such as carboxylic acids, preferably, neuroactive amino acids to sites where their activity is required. In preferred embodiments of the invention, the caging moiety is based on 4-carboxymethoxy-5,7-dinitroinlinyl and derivatives thereof.

Abstract: Described herein are antimicrobial compounds identified via a high-throughput inhibitor screen of the in vitro activity of MipZ, which is an ATPase that regulates division site placement in Caulobacter crescentus. The compounds and their analogs are active against bacterial membranes and thus represent a novel class of antimicrobial compounds. The antimicrobial compounds are effective against both actively growing bacterial cells as well as bacterial cells in the stationary phase. The antimicrobial compounds are also effective against bacteria in biofilms.

Abstract: The present invention provides type C crystal of compound I, type B crystal of compound II, or type C crystal of compound III set forth in this specification.

Abstract: Novel p75 receptor antagonist compounds and compositions and uses thereof for the prevention and treatment of p75-associated disorders, such as neurodegenerative diseases, are described.

Abstract: The present invention relates to indole and indazole compounds of Formula (I) that activate 5? adenosine monophosphate-activated protein kinase (AMPK). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating or preventing diseases, conditions, or disorders ameliorated by activation of AMPK.

Abstract: The present invention relates, in a first aspect, to a process preparing vilazodone hydrochloride that comprises the reaction of 3-(4-chloro-1-hydroxy-butyl)-1H-indol-5-carbonitrile with 5-piperazin-1-yl-benzofuran-2-carboxylate methyl hydrochloride with the formation of a 1,4-piperazine, with subsequent dehydration, hydrogenation and treatment with ammonia, to obtain vilazodone in free base form that is then converted into the hydrochloride thereof.

Abstract: Compounds of the invention are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions.

Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.

Abstract: This invention discloses a method of preservation of a food product comprising the step of adding 1) a first component comprising between 10 ppm and 1% of a biocidal salt of N?—(C1-C22) alkanoyl di-basic amino acid alkyl (C1-C22) ester cationic biocidal molecule with an anionic counterion, and 2) a second component comprising from 10 ppm to 1% by weight an acyl monoglyceride, directly to a food product. The preferred cationic biocidal molecule comprises N?-lauroyl-L-arginine ethyl ester (“LAE”). The invention also discloses the method of preservation of a food product using salts of a N?—(C1-C22) alkanoyl di-basic amino acid alkyl (C1-C22) ester cationic biocidal molecule and an anionic counterion with or without a monoglyceride of a fatty acid, whereby the packaging film is compounded with the salts and the optional monoglyceride of a fatty acid.

Abstract: The present invention relates to indole or indazole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole or indazole compounds as an active ingredient.

Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.

Abstract: Disclosed are pyruvate kinase M2 activators which are compounds of Formula (I), including those of Formula (II), wherein A1, A2, L, R, R1 to R3, X1 to X3, k, n, and m are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer. A1-NR-L-A2 (I).

Abstract: The present invention relates to a cationic 6-aminoindoline of general formula (I), the addition salts thereof with an acid and the solvates thereof: the present invention is also directed towards a method for synthesizing this cationic 6-aminoindoline, the compositions, the uses, the hair dyeing methods and the devices using this cationic 6-aminoindoline.

Abstract: Method of identifying and using compounds which inhibit the expression or activity of micro-RNAs for preventing and/or attenuating ageing, and/or for hydrating skin. An in vitro method for screening for candidate compounds for preventing and/or attenuating ageing of the skin, and/or for hydrating the skin, includes the following steps: a. bringing at least one test compound in contact with a sample of keratinocytes; b. measuring the expression or the activity of at least one microRNA in the keratinocytes; c. selecting the compounds for which an inhibition of at least 20%, preferably at least 30%, preferably at least 40% of the expression or an inhibition of at least 20%, preferably at least 30%, preferably at least 40% of the activity of at least one microRNA is measured in the keratinocytes treated in a. compared with the untreated keratinocytes.

Abstract: An (aza)indole derivative substituted in position 5, of formula (I) in which X, Y, Z, G1, G2, G3, R1, W, and R2 have the meanings given in the description, a pharmaceutical composition comprising it, and also intermediate compounds and a preparation process therefor.