Abstract: Provided is a low-tint (meth) acrylate aryl ester. This production method for (meth) acrylate aryl ester causes a specific hydroxyl group-containing aromatic compound and a (meth) acrylate anhydride to react, in the presence of a hindered phenol and a specific phosphite, and produces a (meth) acrylate aryl ester.

Abstract: Esters and a process for making esters from organic acids by means of reacting a carboxylic acid with dialkylcarbonate in an alcohol-containing solvent without any extrinsic acid or base catalyst is described. A benefit of the preparation process is that it can make the separation and extraction of ester products simpler and more facile vis-à-vis conventional isolation techniques.

Abstract: A method for synthesising a second ester from a first ester, the method including the following steps: a) placing a first ester and a catalyst in the presence of dihydrogen such as to obtain a first alcohol and a second alcohol; b) extracting the second alcohol from the reaction medium; c) reacting the first alcohol with the catalyst of step a) in order to obtain a second ester and dihydrogen; and d) recirculating the dihydrogen obtained in step c) by injecting same into step a).

Abstract: Provided herein are compounds of the formula: in which n is an integer equal to or greater than 1; R2 is selected from hydrogen and optionally substituted alkyl that is saturated or unsaturated, and branched or unbranched; and R1, R3, and R4, independently for each occurrence, are selected from optionally substituted alkyl that is saturated or unsaturated, and branched or unbranched, wherein compositions comprising the compounds are characterized by particular combinations of values for estolide number, kinematic viscosity, and pour point. Also provided are compositions containing the compounds and methods of making both the compounds and compositions thereof.

Abstract: Isophoronediamine, is prepared by A) subjecting isophoronenitrile directly in one stage to aminating hydrogenation to give isophoronediamine in the presence of ammonia, hydrogen, a hydrogenation catalyst and an optional additive, and in the presence or absence of an organic solvent; or B) first converting isophoronenitrile fully or partly in at least two or more than two stages to isophoronenitrile imine, and subjecting the isophoronenitrile imine to aminating hydrogenation to give isophoronediamine as a pure substance or in a mixture with another component and/or isophoronenitrile, in the presence of at least ammonia, hydrogen and a catalyst.

Abstract: A biomass resource-derived 1,5-pentamethylene diamine produces a polyamide resin composition having a good color tone. The 1,5-pentamethylene diamine in which a total of the contents of an acetamide, 2,3,4,5-tetrahydropyridine, 2-piperidone, ?-amino-?-caprolactam, lysine and ornithine that the 1,5-pentamethylene diamine contains as impurities is less than or equal to 150 weight ppm.

Abstract: A process for preparation of diethyl 2-aetamido-2-(4-octyl phenyl)ethyl malonate (III), a key intermediate of fingolimod hydrochloride comprising reaction of 2-(4-octylphenyl)ethyl iodide (IV) with diethyl acetamido malonate in presence of a base and an iodinating agent and in an organic solvent. The compound of formula (III) thus obtained provided fingolimod hydrochloride (Ia) having associated impurities below the regulatory limits.

Abstract: Process for the manufacture of an amino ester of formula (I) R1—O—C(O)—(CH2)n—NH2 (I) in which n is an integer from 10 to 15 from an unsaturated ester responding to formula (II) R1—O—C(O)—(CH2)m—CH?CH—R2 (II) in which R1 is either H or a saturated alkyl group containing from 1 to 5 carbon atoms; R2 is either H or an alkyl group containing from 1 to 10 carbon atoms, either saturated or containing 1 or 2 unsaturations and bearing optionally a hydroxyl, a carboxylic or an ester group, and m is equal to 7, 8, 9, 10 or 11; said process comprising: submitting the unsaturated ester of formula (II) to a catalytic cross-metathesis reaction with a pentenenitrile chosen among 2-pentenenitrile or 3-pentenenitrile in order to obtain a ester-nitrile responding to formula (III) R1—O—C(O)—(CH2)m—CH?CH—(CH2)p—CN (III) in which m is equal to 7, 8, 9, 10 or 11 and p is equal to 0 or 1, and submitting the obtained ester-nitrile of formula (III) to an hydrogenation in order to obtain the amino ester of formula (I).

Abstract: ?-Substituted ?-amino acids, ?-substituted ?-amino acid derivatives, and ?-substituted ?-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates, capable of passing through the blood-brain barrier, and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs and (bio)isosteres and methods of using the compounds for treating tumors are also disclosed. The ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs and (bio)isosteres exhibit an improved selectivity toward tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo.

Abstract: The present invention provides N-substituted glycinium bis(fluorosulfonyl)imide compounds and methods for producing and using the same. In particular, the N-substituted glycinium bis(fluorosulfonyl)imide compound is of the formula: wherein each of R1, R2 and R3 is independently selected from the group consisting of alkyl, aryl, aralkyl, cycloalkyl, (cycloalkyl)alkyl, heteroaryl, (heteroaryl)alkyl, heterocyclyl, and (heterocyclyl)alkyl; or R1 and R2 together with the nitrogen atom to which they are attached to form a nitrogen-heterocyclyl, or a nitrogen-heteroaryl.

Abstract: The present invention provides an N-substituted glycinium (fluorosulfonyl)(trifluoromethylsulfonyl)imide compounds and methods for producing and using the same. In particular, the N-substituted glycinium (fluorosulfonyl)(trifluoromethylsulfonyl)imide compound is of the formula: wherein each of R1, R2 and R3 is independently selected from the group consisting of alkyl, aryl, aralkyl, cycloalkyl, (cycloalkyl)alkyl, heteroaryl, (heteroaryl)alkyl, heterocyclyl, and (heterocyclyl)alkyl; or R1 and R2 together with the nitrogen atom to which they are attached to form a nitrogen-heterocyclyl, or a nitrogen-heteroaryl.

Abstract: There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.

Abstract: ?-Substituted ?-amino acids, ?-substituted ?-amino acid derivatives, and ?-substituted ?-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

Abstract: The present invention generally relates to devices and methods for crystallizing a compound. In certain industries, crystallization techniques require additional filtration steps in order to obtain products of relatively high yield and/or high purity. In some embodiments, the devices and methods described herein facilitate continuous production of high yield and/or high purity products without the need for additional filtration steps. In some embodiments, the devices and methods comprise flowing a fluid comprising a compound (e.g., a crystallizable compound, a solidifiable compound) over a substrate such that the compound crystallizes and/or precipitates on the substrate. In some embodiments, the crystallized compound can be recovered (e.g., at a high purity in solution). In certain embodiments, the substrate is orientated substantially vertically (e.g., such that flow of the fluid is driven by gravity). In some cases, the substrate comprises a plurality of crystallization promoting structures.

Abstract: Alternative continuous downstream processes for the production of 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophthalamide (“Compound A”) are described. Compound A is a key intermediate in the production of iodixanol and iohexol, which are two of the biggest commercially available non-ionic x-ray contrast media agents.

Abstract: The present invention provides novel creatine analogs useful for treating any creatine deficiency disorders and methods of treating and preventing creatine deficiencies utilizing the present compounds and the pharmaceutical compositions or formulations thereof. Certain embodiments seek to increase the lipophilicty of novel creatine analogs with the goal of improving their bioavailability.

Abstract: A process for preparing alkanesulfonic acids from sulfur trioxide and an alkane, wherein sulfur trioxide, the alkane and dialkylsulfonoyi peroxide (DASP) react as components, characterized in that the following steps are performed: a) sulfur trioxide is charged in a high-pressure reactor in a condensed phase; b) a temperature of at least 25° C. is set; c) the gaseous alkane is introduced to the high-pressure reactor until a pressure of at least 10 bar is reached; d) dialkylsulfonoyi peroxide (DASP) is added; and e) after a duration of at least 5 hours, the produced alkanesulfonic acid is withdrawn.

Abstract: The invention relates to a method for the preparation of imidodisulfuryl compounds in a continuous reaction at elevated temperatures.

Abstract: The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.

Abstract: A process for the preparation of dihalodiphenylsulfones such as 4,4?-dichlorodiphenyl sulfone or 4,4?-bis-(4-chlorophenylsulfonyl)biphenyl with high regioselectivity, at low temperature and in the absence of toxic reagents by reacting together at least one acid, at least one fluorinated anhydride and at least one halobenzene. The invented process is particularly suited for the manufacture of 4,4?-dichlorodiphenyl sulfone.

Abstract: A continuous process is described for the one-pot synthesis of compounds, such as metal salts and metal complexes, as well as optionally for the protection of the compounds thus obtained by coating and/or impregnation with suitable compounds.

Abstract: A compound of the formula (I) ALK-SO2—O—O—SO2OX, wherein ALK is a branched or unbranched alkyl group, especially a methyl, ethyl, propyl, butyl, isopropyl, isobutyl group, or a higher alkyl group, and X=hydrogen, zinc, aluminium, an alkali or alkaline earth metal.

Abstract: Described herein are compositions and compounds having one or more aziridinyl groups, and methods of making the same. The compounds can also have one or more nitrogen atoms that each can be positively charged. The composition and compounds can inactivate one or more nucleic acid molecules (e.g. a DNA and/or a RNA from a pathogen) in a sample. The sample can comprise a blood or blood product (e.g., donated blood). The compositions and compounds can inactivate any nucleic acid present in a blood or blood product, thereby making the blood or blood product safe for use (e.g., in a transfusion).

Abstract: IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPs (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kd of less than 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposed are also disclosed.

Abstract: The present invention relates to compounds of the general formula (I) having a selective FKBP51 ligand scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said selective FKBP51 ligand compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.

Abstract: The invention provides EBNA1 inhibitors, and pharmaceutical compositions comprising the same, that are useful for the treatment of diseases caused by EBNA1 activity such as, but not limited to, cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and/or rheumatoid arthritis. The compounds and compositions of the invention are further useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. The compounds and compositions of the invention are further useful for the treatment of diseases caused by lytic EBV infection.

Abstract: The invention relates to pyrrole carboxamides bearing a fluoromethyl-moiety as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.

Abstract: Hybrid compounds of curcumin and melatonin as neuroprotectants are provided. The hybrid compounds are useful for the treatment and/or prevention of Alzheimer's disease (AD), as well as other neurodegenerative diseases. The hybrid compounds exhibited superior and potent neuroprotection in an AD model.

Abstract: Methods of treating and/or preventing viral diseases and disorders, such as those ameliorated by inhibition of PDE-4, are disclosed.

Abstract: To provide a compound having an effect for preventing photolysis of a liquid crystal composition, and having a high solubility in the liquid crystal composition, a liquid crystal composition containing the compound, and a liquid crystal display device including the composition. The compound is represented by formula (1), the liquid crystal composition contains the compound, and the liquid crystal display device includes the composition. In formula (1), R1, R2, R3 and R4 are independently hydrogen or alkyl having 1 to 4 carbons; ring A1 and ring A2 are independently 1,4-cyclohexylene, 1,4-phenylene or the like; Z1, Z2 and Z3 are independently a single bond, alkylene or the like; and n is 0, 1 or 2.

Abstract: The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.

Abstract: The present invention provides heterocyclic derivatives that 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: Ivabradine hydrochloride Form IV, its pharmaceutical composition, process for its preparation, and its use as therapeutically active ingredient and pharmaceutical compositions containing Ivabradine hydrochloride Form IV.

Abstract: The present invention relates to a novel process for preparing 3,5-bis(haloalkyl)pyrazole derivatives.

Abstract: A new process for the preparation of 5-fluoro-1H-pyrazoles of the general formula (I) as described herein, resulting from the reaction of an olefin with hydrazine in the presence of water and a base.

Abstract: The present invention provides a compound of the Formula: wherein X is selected from the group consisting of, R is selected from the group consisting of H and CH3; R1 is selected from the group consisting of H, CH3, F, Cl, OCH3, C(O)OH, C(O)NH2 or a pharmaceutically acceptable salt thereof.

Abstract: Provided is pyrazole derivatives as a TNIK (Traf2- and NCK-interacting kinase), IKK? (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor; the pyrazole derivative according to the present invention effectively inhibits TNIK, IKK? and TBK1, and thus is useful not only as an anticancer agent for the treatment of various cancers including colorectal cancer, breast cancer, CNS cancer, colon cancer, non-small cell lung cancer, kidney cancer, prostate cancer, ovarian cancer, uterus cancer, stomach cancer, liver cancer, skin cancer, lung cancer, brain cancer, bladder cancer, esophageal cancer, pancreatic cancer, thyroid cancer, head and neck cancer, squamous cell carcinoma, osteosarcoma, B-cell or T-cell lymphoma, acute or chronic leukemia and multiple myeloma, but as a therapeutic agent for chronic inflammation.

Abstract: The invention relates to the synthesis of a therapeutic agent which is effective against American trypanosomiasis (Chagas disease) caused by the protozoa Tripanosoma cruzi and transmitted by blood-sucking insects of the genera Triatoma or Rhodnius. This synthesis method is carried out in one step, in a solid state. It is a clean, simple, economical, rapid, easily implemented method, does not involve acid or base catalysts in the synthesis process, and is also environmentally friendly. It is a synthesis method for producing N-benzyl-2-(2-nitro-1-H-imidazol-1-yl)acetamide from the N-benzyl-2-hydroxyacetamide and 2-nitro-1H-imidazol reaction mixture, using microwave irradiation as an activation source in order to produce the N-benzyl-2-(2-nitro-1H-imidazol-1-yl)acetamide.

Abstract: The present invention is directed to bendamustine esters and bendamustine amides and their use for the treatment of cancer.

Abstract: The invention discloses compounds of formula I wherein Y is a group of formula A, B, C, D, or E: and W, Q, n, R1, R2, R3, U1-U5, J and K have the meanings given in the description. The compounds of formula I are TRPV1 antagonists and are useful as active ingredients of pharmaceutical compositions for the treatment of pain and other conditions ameliorated by the inhibition of the vanilloid receptor TRPV1.

Abstract: The present invention includes methods/processes and intermediates for preparing compounds having structural Formula (I): wherein X is alkyl, substituted alkyl, alkenyl, substituted alkenyl, heteroalkyl, substituted heteroalkyl, heteroalkenyl, or substituted heteroalkenyl.

Abstract: The present invention relates to novel compounds, e.g. for use as a medicament. In particular, the present invention relates to novel medicaments, preferably in the treatment and/or prevention of systemic diseases, autoimmune diseases, or inflammatory diseases, for example multiple sclerosis and psoriasis.

Abstract: The present invention relates to 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine acetate in crystalline form and to methods for the preparation thereof. In addition the present invention relates to solid pharmaceutical compositions for oral administration comprising an effective amount of the crystalline 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine acetate. Moreover, the present invention relates to the use of crystalline 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine acetate for the preparation of pharmaceutical compositions.

Abstract: In accordance with the present subject matter, there is provided a process for preparing a furan derivative, the process comprising the steps of contacting a sugar with a monophasic organic solvent to obtain a reaction mixture; and subjecting the reaction mixture to a temperature in the range from 100° C. to 180° C., in presence of an acid catalyst, for a time period in the range of 0.5 min to 4.0 h to obtain at least 70% conversion of the sugar to a single furan derivative, wherein the acid catalyst is selected from the group consisting of homogenous acid catalyst, heterogenous solid acid catalyst, and combinations thereof There is also provided a process for preparation of a heterogenous solid acid catalyst.

Abstract: The present invention relates to compounds of the following general formula (I), or to a pharmaceutically acceptable salt thereof, as well as to the uses thereof as a drug, in particular for treating cancerous or precancerous hyperproliferative conditions, and to the pharmaceutical compositions containing same.

Abstract: The present invention relates to a compound of the following formula (I): or a pharmaceutically acceptable salt thereof, for use in the prevention or treatment of obsessions and/or compulsions in an individual.

Abstract: The present invention provides a new compound which has NK1 receptor antagonist activity, whose CYP3A4 inhibitory activity is reduced compared to aprepitant, and which are useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. That is, the present invention relates to carboxymethyl piperidine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof. Wherein, ring A is a benzene ring or the like; ring B is a pyridine ring or the like; R1 is C1-6 alkyl or C1-6 alkoxy; R2 and R3 are a hydrogen atom or methyl; and n is an integral number from 0 to 5.

Abstract: The present invention is directed to substituted indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.

Abstract: This 2-pyridone compound represented by formula [1] or a tautomer of said compound, or a pharmaceutically acceptable salt of said compound or said tautomer, or a solvate of said compound or the like has a superior UK-activating effect and is useful as a pharmaceutical.

Abstract: The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.