Abstract: The present invention relates to a novel process for the synthesis of 9,9-bis(hydroxymethyl)fluorene. The syntheses from fluorene to 9,9-bis(hydroxymethyl)fluorene via a hydroxymethylation and further to 9,9-bis(methoxymethyl)fluorene via a etherification are known. 9,9-bis(methoxymethyl)fluorene is a compound that is used as an electron donor for Ziegler-Natta catalysts. The present invention is related to an improvement in the synthesis of 9,9-bis(hydroxymethyl)fluorene leading to a decrease in the amount of solvent used and an easier work up while achieving high yield and purity.

Abstract: A fluorene-containing compound having a formula (I) where X and R are as defined in as defined in the specification.

Abstract: A process for preparing an arylpropene from a diarylpropane by gas phase thermolysis in the presence of boron containing zeolitic material comprising a membered ring (MR) pore system greater than 10 MR.

Abstract: A process for preparing an arylpropene from a diarylpropane by gas phase thermolysis in the presence of solid porous catalyst comprising silica having large pore volume and low acidity.

Abstract: The invention pertains to a method for providing a succinic acid solution, comprising the steps of—providing a first magnesium succinate containing medium with a magnesium succinate concentration of 18-23 wt. % to a first acidification reactor where it is contacted with hydrogen chloride to form a solution of succinic acid, magnesium chloride and hydrogen chloride,—providing a second magnesium succinate containing medium with a magnesium 3 succinate concentration of 25-50 wt. %, and contacting it in a second acidification reactor with the solution of succinic acid, magnesium chloride and hydrogen chloride withdrawn from the first acidification reactor, to form an aqueous mixture comprising magnesium chloride and succinic acid with a succinic acid concentration of at least 18 wt. %. the method according to the invention makes it possible to obtain a solution comprising succinic acid and magnesium 20 chloride with an increased succinic acid concentration.

Abstract: A process for the coupled production of sweet whey and lactic acid from acid whey is suggested, comprising the following steps: (a) providing acid whey having a lactic acid content of about 0.1 to about 1% by weight; (b) nanofiltration of the acid whey, obtaining a first permeate P1 and a first retentate R1; (c) optionally, redilution of the first retentate R1 with water to reconstitute the initial dry matter content, and preparation of the second nanofiltration step; (d) nanofiltration or nano-diafiltration of the retentate R1, obtaining a second permeate P2 and sweet whey as a second retentate R2; (e) combining the two permeates P1 and P2 and subjecting the mixture to reverse osmosis, obtaining a third permeate P3 which, substantially, only contains water, and a concentrate of lactic acid as a third retentate R3.

Abstract: Endogenous mechanisms leading to host protection and resolution of infections without immunosuppression are of wide interest. Here we elucidated the structures of four new host-protective molecules produced in neutrophil-endothelial co-cultures, and present in human and mouse tissues after sterile inflammation or infection. These bioactive molecules contained conjugated triene and diene double bonds with each carrying a 13-carbon position alcohol and were derived from n-3 docosapentaenoic acid (DPA, C22:5). These compounds, termed 13-series resolvins (RvT), demonstrated potent protective actions increasing mice survival during Escherichia coli infections. RvT also regulated human and mouse phagocyte responses stimulating bacterial phagocytosis and regulating inflammasome components. Their biosynthesis during neutrophil-endothelial cell interactions was initiated by endothelial cyclooxygenase-2 (COX-2) and increased by atorvastatin via S-nitrosylation of COX-2.

Abstract: 2-Acetoxyalkanoic acid esters are made in a reaction of a 3,6-dialkyl-1,4-dioxane-2,5-dione or a poly(?-hydroxyalkanoic acid), an acetate ester and an alcohol or phenol in the presence of a transesterification catalyst. Unlike previous methods for making 2-acetoxyalkanoic acid esters, this process proceeds in high yield and high selectivity to the desired product.

Abstract: The invention relates to a process for preparing an ester mixture, in which an n-butene-containing feed mixture having a composition which changes over time is first oligomerized and then converted by hydroformylation, hydrogenation and esterification to an ester mixture. In this process, an approximation of the actual viscosity of the ester mixture is determined. The problem that it addresses is that of specifying a comparatively simple process which enables conversion of an n-butene with a variable composition over time to an ester mixture having a viscosity which can be kept very substantially constant over a long period even when an inconstant C4 source which delivers fluctuating qualities over this period is utilized. This is achieved through controlled use of a second raw material, namely ethene. It has been found that the viscosity of n-butene-based ester mixtures can be influenced by controlled use of ethene in the preparation of the ester precursors.

Abstract: Methods and systems for producing alkyl hydroxyalkanoate from hydroxy carboxylic acid recovery bottoms. The methods generally comprise the steps of obtaining a hydroxy carboxylic acid recovery bottom, adding a mono-alcohol to the hydroxy carboxylic acid recovery bottom to obtain a first mixture, heating the first mixture in the presence of a catalyst to form a reaction product, distilling the reaction product, and recovering an alkyl hydroxyalkanoate fraction.

Abstract: The present invention concerns the use as perfuming ingredient (of the fruity type) of a compound of formula in the form of any one of its stereoisomers or of a mixture thereof, and wherein R1 represents a C1-3 alkyl or alkenyl group, R2 represents a methyl or ethyl group, R3 represents a C1-4 alkyl or alkenyl group, and the compound (I) has from 8 to 12 carbon atoms.

Abstract: A mixture of isomeric dipentyl terephthalates, pentyl radicals of which are n-pentyl radicals to an extent of less than 60 mol %, characterized by a low viscosity which does not increase significantly even at temperatures below 40° C. Plastisols comprising these mixtures have a low plastisol viscosity which moreover increases only to a minor degree with time.

Abstract: The present invention relates to a process for the preparation of selegiline base, an irreversible and selective inhibitor of the MAO-B enzymes and which is used in the treatment of Parkinson's Disease.

Abstract: A new process for preparing the fenfluramine molecule and new compositions containing fenfluramine obtainable with the claimed process.

Abstract: The present invention provides an improved process for the preparation of 3-(4-chlorophenyl)-3-cyanopropanoic acid (compound (A)) and further its transformation to Baclofen (I). The process comprises reaction of compound (II) with Glyoxylic acid to obtain 3-(4-chlorophenyl)-3-cyanoacrylic acid (III); followed by the ‘in-situ’ reduction of (III) in the presence of a reducing agent to provide the compound (A). Alternatively, the compound (A) is obtained by the process comprising reacting 2-(4-chlorophenyl)acetonitrile (II) with haloacetic acid (IV) in the presence of a base. The compound 3-(4-chlorophenyl)-3-cyanopropanoic acid (A) undergoes hydrogenation in the presence of a metal catalyst and ammonia solution to provide Baclofen (I).

Abstract: The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids comprising at least one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.

Abstract: A method for producing a compound of formula (I) or a pharmaceutically acceptable salt, solvate, tautomer or stereoisomer, such as compound 1 and compound 2 is disclosed. The method proceeds through an O-allylated tyrosine-based compound, such as compound 3 and preferably comprises [3,3] sigmatropic Claisen rearrangement and olefin cross metathesis reactions. In addition, a pharmaceutical composition comprising a compound of formula (I) a tumor necrosis factor (TNF) related apoptosis inducing ligand (TRAIL) and a pharmaceutically acceptable carrier or excipient is disclosed.

Abstract: Here described is a method of delivery of a drug to a stellate cell using a composition comprising a compound of formula I: wherein R1 and R2 are independently selected from C10 to C18 alkyl, C12 to C18 alkenyl, and oleoyl; R3 and R4 are independently selected from C1 to C6 alkyl and C2 to C6 alkanol; X is selected from —CH2—, —S—, and —O—, or X is absent; Y is selected from —(CH2)n, —S(CH2)n—, —O(CH2)n—, -thiophene-, -SO2(CH2)n—, and ester; n=1-4; a=1-4; b=1-4; c=1-4; and Z? is a counterion.

Abstract: Disclosed is a process for co-manufacture of ACRN and HCN with improved HCN selectivity and reduced solids formation in a shared product recovery section.

Abstract: Provided are a new aromatic cyanogen compound and a preparation method thereof. The present invention also relates to the use of such compound in antiviral drugs, in particular the use thereof in anti-HCV drugs.

Abstract: The present invention relates to a process for preparing a cyclic isocyanate (B) from a composition (Z) which comprises at least one component (A) which has at least one cycloalkane ring having at least 4 ring carbons, where the cycloalkane ring has two NH2 groups in ? or ? positions relative to one another as substituents and in more than 50 mol % of the total amount of component (A) the two NH2 groups in ? or in ? positions relative to one another assume a trans configuration relative to one another. This composition (Z) is, in the process of the invention, reacted with phosgene to give a composition (ZP) which comprises at least one cyclic isocyanate (B) having isocyanate groups. In addition, the invention relates to the use of the isocyanate mixture (M) as monomer in processes for preparing polymers, in particular for preparing polyurethanes and polyureas.

Abstract: A method for producing organic urea is provided that, by mixing and reacting liquid ammonia (NH3) and gaseous carbon dioxide (CO2) through the steps of ammonium carbamate formation (5), carbamate decomposition (7), urea synthesis (8) and evaporation (9) thereof, is carried out using organic ammonia from animal and plant biomass (2) and carbon dioxide recycled from the exhaust gases (6) from combined-cycle biogas boilers with plant biomass. The steps preceding the organic urea production include methanization (1), with a biomass “digester”, mixing with pig and chicken slurry and blood, pine needles and ash, and water, until obtaining: methane gas, air, gaseous ammonia and water vapor and PH regulator and catalyzing (3), where the obtained gases are condensed by cooling and the gaseous ammonia is separated to be stored at a pressure of 13 atmospheres. Organic urea and the chemical reactor AUS32 manufactured using from biomass are also detailed.

Abstract: The present invention provides a urea compound or a pharmacologically acceptable salt thereof that has a formyl peptide receptor like 1 (hereinafter may be abbreviated as FPRL1) agonist effect, a pharmaceutical composition containing the urea compound or the pharmacologically acceptable salt thereof, and a pharmaceutical use thereof. It has been found that a urea derivative represented by the general formula (I) below or a pharmacologically acceptable salt thereof has a superior FPRL1 agonist effect. Compound (I) or a pharmacologically acceptable salt thereof is highly useful for treatment, prevention, or suppression of inflammatory diseases, chronic airway diseases, cancers, septicemia, allergic symptoms, HIV retrovirus infection, circulatory disorders, neuroinflammation, nervous disorders, pains, prion diseases, amyloidosis, immune disorders and the like.

Abstract: The present application provides a process for preducing taurine, comprising the steps as follows: (a) mixing isethionic acid with taurine salt solution until the system pH reaches a certain value in a range from 5.0 to 9.5; (b) separating liquid phase and solid phase of the system; wherein said solid phase is the crude product of taurine, and said liquid phase is isethionate solution; (c) reacting ammonia solution with said liquid phase obtained from step (b) to obtain taurine salt solution. It uses isethionic acid to adjust the pH of the taurine salt solution, avoiding the problem causing by using sulphate acid to adjust the pH in the traditional process. By the recycling use of the cations in taurine salts, a new raw material or reagent does not need to be added which is benefit to reducing the use of dangerous chemical materials, simplifying the production process greatly, improving the utilization rate of raw materials, increasing the yield of the product and decreasing production cost significantly.

Abstract: Compounds that inhibit Myeloid Cell Leukemia-1 (Mcl-1) oncoprotein, and methods of using the same, are provided for treating disease.

Abstract: What is described is a method of synthesis of the compound of formula 1A, or a salt thereof, wherein R3 is a linear or branched alkene of 1, 2, 3, 4, 5 or 6 carbons; R4 and R5 are the same or different, each a hydrogen, or a linear or branched alkyl of 1, 2, 3, 4, 5 or 6 carbons; and L3 is a bond or an alkane of 1, 2, 3, 4, 5 or 6 carbons.

Abstract: Provided is a method for preparing pimavanserin including reacting an intermediate compound represented by Formula (II) with N-(4-fluorobenzyl)-1-methylpiperidin-4-amine or a salt thereof, or reacting an intermediate compound represented by Formula (IV) with 4-isobutoxybenzylamine or a salt thereof, wherein L represents a heteroaryl group, —OR1 or halogen, and wherein R1 represents C1 to C10 alkyl or aryl. The present disclosure provides the method for preparing pimavanserin without the use of isocyanate intermediate.

Abstract: The present invention is directed to phenylcyanoquinolinone compounds which may be useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

Abstract: The present invention relates to methods and compounds for regulating or enhancing erthropoiesis and iron metabolism, and for treating or preventing iron deficiency and anemia of chronic disease.

Abstract: A process for the preparation of a compound of formula IX: wherein R1 is difluoromethyl, and R3 is methyl or ethyl.

Abstract: The present invention relates to compounds of formula I, wherein the groups R, R1, R2, R3, m and n are defined herein, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.

Abstract: A compound for treating a protein kinase-related disease or disorder having a structure of formula (I) wherein L is NR8 or O; R1, R2, R3, R4, R5, R6 and R7 are defined herein. Compounds of formula (I) are useful for inhibition of protein kinases.

Abstract: The invention relates to novel methods of preparing cell-binding agent-cytotoxic agent conjugates, wherein the cytotoxic agent is an imine-containing cytotoxic agent bearing a maleimide group. In some embodiments, the cell-binding agent (CBA) is covalently linked to the cytotoxic agent through an engineered Cys, such as an engineered Cys in the heavy chain CH3 domain, at a position corresponds to the EU/OU numbering position 442 (or C442) on an antibody CBA. The invention also provides conjugates prepared by the methods of the present invention, compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the conjugates of the invention.

Abstract: Thermodynamically stable crystal modification of 2-chloro-3-(methylsulfanyl)-N-(1-methyl-1H-tetrazol-5-yl)-4-(trifluoromethyl)benzamide A thermodynamically stable crystal modification of the herbicidal active ingredient 2-chloro-3-(methylsulfanyl)-N-(1-methyl-1H-tetrazol-5-yl)-4-(trifluoromethyl)benzamide is described. This thermodynamically stable crystal modification has particular advantages in the stability of suspension formulations.

Abstract: Compositions of the invention comprise 1,2-dithiolane, dithiol and related compounds useful as therapeutic agents for the treatment and prevention of diseases and conditions associated with aberrant EGFR activity.

Abstract: The present invention pertains generally to the field of chemical synthesis, and more particularly to methods of chemical synthesis which include the step of preparing a substituted 10H-phenothiazine-3,7-diamine compound of Formula (1) by a step of selective alkylation by reductive amination, in which the corresponding unsubstituted diamine of Formula (4) is reacted with aldehyde/ketone, under reductive amination conditions. The present invention also relates to such methods which incorporate additional subsequent and/or preceding steps, for example, to prepare compounds of Formulae (2) and (3) from compounds of Formula (1), and to prepare compounds of Formula (4) from, for example, compounds of Formulae (5), (6), (7), (8), and (9). Compounds of Formula (1), Formula (2), and Formula (3) are useful, for example, in the treatment of diseases of protein aggregation, such as Alzheimer's disease.

Abstract: This invention relates to deuterated forms of meclizine, and pharmaceutically acceptable salts or hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering meclizine and other Constitutive Androstane Receptor agonists or FGFR3 antagonists.

Abstract: The present invention relates to an improved process for making hydroxyethyl piperazine compounds especially mono-hydroxyethyl piperazine. The improvement comprises reacting piperazine and an alkylene oxide, preferably ethylene oxide in a reactive distillation column.

Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.

Abstract: The present disclosure relates to a method for effecting catalytic selective oxidation in liquid phase comprising a perfluorinated solvent and an olefinic compound with molecular oxygen to produce an epoxide. The method may provide enhanced selectivity to the epoxide of greater than 60%. The olefinic compound may be ethylene, propylene, butenes, 1-octene, butadiene, allyl chloride, allyl alcohol, styrene, and the like. The perfluorinated solvent may be perfluoro methyldecalin, perfluorodecalin, perfluoroperhydrophenanthrene, perfluoro (butyltetrahydrofuran), isomers thereof, or a combination thereof. In some embodiments, the method includes catalytically epoxidizing, in a liquid phase comprising a perfluorinated solvent, propylene with molecular oxygen to produce propylene oxide.

Abstract: The design and synthesis of a novel bis-furan scaffold tailored for high efficiency at inhibiting transthyretin amyloid formation is reported. In vitro results show that the discovered compounds are more efficient inhibitors of amyloid formation than tafamidis, a drug currently used in the treatment of familial amyloid polyneuropathy (FAP), despite their lower molecular weight and lipophilicity. Moreover, ex vivo experiments with the strongest inhibitor in the series, conducted in human blood plasma from normal and FAP Val30Met-transthyretin carriers, disclose remarkable affinity and selectivity profiles. The promises and challenges facing further development of this compound are discussed under the light of increasing evidence implicating transthyretin stability as a key factor not only in transthyretin amyloidoses and several associated co-morbidities, but also in Alzheimer's disease.

Abstract: Disclosed is a continuous process for concentrating or separating of vitamin E, sterols and/or terpenes from oily or fatty mixtures of biological origin comprising the measures: a) providing a reaction mixture containing oily or fatty mixture of biological origin, at least a monohydric alcohol and at least an acidic catalyst, b) continuously conducting the reaction mixture through a reactor which has a heating zone in which the reaction mixture is heated to a temperature between 100° C. and 190° C.

Abstract: Described herein are ?9-THC prodrugs, methods of making ?9-THC prodrugs, formulations comprising ?9-THC prodrugs and methods of using ?9-THC. One embodiment described herein relates to the transdermal administration of a ?9-THC prodrug for treating and preventing diseases and/or disorders.

Abstract: Disclosed are compounds, for example, compounds of formula (I), (Formula (I) wherein R, R0, R1-R8, n, X, Y, Y?, and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition, for example, cancer.

Abstract: The invention relates to Pro-drugs, comprising red-ox-sensitive cleavage sites. The compounds may be utilized in medical practice for targeting of si RNA, antisense oligonucleotides or protein-based therapeutics to the cytoplasmatic compartment of cells both in vitro or in vivo, in a subject in need.

Abstract: The invention relates to compounds of formula IA and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof.

Abstract: The present invention relates to novel selective 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD1) inhibitors and the use thereof to prevent age-induced skin structure and function defects.

Abstract: This disclosure provides compounds and compositions and methods of using those compounds and compositions to treat diseases and disorders associated with excessive transforming growth factor-beta (TGF?) activity. This disclosure also provides methods of using the compounds in combination with one or more cancer immunotherapies.

Abstract: The present invention provides novel compounds of Formula (I) and Formula (II) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.

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.