Abstract: The present invention relates to a novel method for preparing cabazitaxel from 10-deacetylbaccatin III, and a novel intermediate therefor, and more specifically, to: a method which allows cabazitaxel to be more easily prepared in a high yield and in a high purity within a short time compared with a conventional method by preparing cabazitaxel via a novel intermediate using 10-deacetylbaccatin III as a starting material, and thus is suitable for industrial mass production; and a novel intermediate therefor.

Abstract: A process is described for the preparation of 5-hydroxymethylfurfural (HMF), which comprises the following steps: provision or preparation of a starting mixture, comprising one, two or more starting compounds selected from the group consisting of hexoses, oligosaccharides comprising hexose units, and polysaccharides comprising hexose units, one, two or more organic salts with a melting point <180° C. and a boiling point >200° C. at 1013.25 hPa, optionally additionally one or more catalysts for the conversion of the one starting compound or at least one of the two or more starting compounds to 5-hydroxymethylfurfural (HMF), optionally water, optionally further substances, adjustment of reaction conditions such that an amount of the starting compound or starting compounds converts to HMF.

Abstract: Provided are methods of producing 2,5-furandicarboxylic acid (FDCA) from renewable sources such as seaweed, alginate, oligoalginate, pectin, oligopectin, polygalacturonate, galacturonate, and/or oligogalacturonate. The sugars in the renewable sources can be converted into one or more intermediates such as 4-deoxy-L-erythro-5-hexoseulose uronate (DEHU), 4-deoxy-L-threo-5-hexosulose uronate (DTHU), 5-hydroxymethyl furfural (HMF), 2,5-dihydroxymethyl furan (DHMF), and 5-formyl-2-furancarboxylic acid (FFA), which can be converted into FDCA by dehydration and cyclization to produce 5-formyl-2-furancarboxylic acid (FFA), followed by oxidation to produce FDCA. DEHU or DTHU may also be converted into FDCA by oxidation to produce 2,3-dihydroxy-5-oxohexanedioic acid (DOHA), which then undergoes dehydration and cyclization to produce FDCA.

Abstract: The present invention discloses eight new diterpenoids, i.e. Dysongensins A to H, extracted from the leaves and twigs of Dysoxylurn hongkongense, wherein AMBROX® which is applicable in the perfume industry is prepared from Dysongensin A via a series of chemical reactions, and the cytotoxicity of Dysongensins A to H against human cancer cell lines and their antiviral and anti-inflammatory activities are determined. Therefore, in the present invention, AMBROX® prepared from Dysongensin A is a new idea for application as an odorous compound in the perfume industry, and the novel diterpenoids can be prepared as a pharmaceutical compositions and/or a drug having antiviral, anti-inflammatory and/or anti-cancer activities.

Abstract: A catalyst system and a method for manufacturing cyclic carbonate by the same are provided. The catalyst system includes a transition metal salt containing a halo group, an acetate group, or a combination thereof, and an organic phosphine ligand. The molar ratio of the organic phosphine ligand to the transition metal salt is greater than 0 and less than or equal to 50.

Abstract: Specifically useful stereoisomers of 1,3-dioxane derivatives are described and their use in the treatment of a disease or condition dependent on PPAR modulation, such as diabetes, cancer, inflammation, neurodegenerative disorders and infections as well as their use in the treatment of a disease related to TP, such as cardiovascular diseases.

Abstract: The present invention provides a salt represented by the formula (I): wherein R1, R2, L1, Y, R3, R4, R5, R6, R7, n, s, and R8 represent variables outlined in the specification.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds. These compounds are useful for therapy or prophylaxis in a mammal, and in particular as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.

Abstract: There is provided inter alia a compound of formula (I): wherein R1, J, Ar, L, X, R3 and R4 are as defined in the specification, for use in the treatment of inflammatory disorders.

Abstract: A process for making (2S,5R)-5-ethynyl-1-{N-(4-methyl-1-(4-carboxy-pyridin-2-yl)piperidin-4-yl)glycyl}pyrrolidine-2-carbonitrile and salts thereof, and intermediates used in the process are disclosed.

Abstract: Compounds of formula (I) and their use as pharmaceutical.

Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.

Abstract: The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.

Abstract: Heteroaryl pyridone and aza-pyridone amide compounds with electrophilic functionality of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract: Described herein are compounds that are inhibitors of autotaxin. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such inhibitors, alone and in combination with other compounds, for treating autotaxin-dependent or autotaxin-mediated conditions or diseases.

Abstract: The present invention is directed to methods and compositions for suppressing lymphangiogenesis, angiogenesis and/or tumor growth. The methods comprise contacting the tumor with a compound that (i) stabilizes a protein kinase in the inactive state and (ii) is not an ATP competitive inhibitor of the protein kinase in the active state.

Abstract: The present invention is directed to pyranyl aryl methyl benzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

Abstract: The disclosure is in part directed to crystalline forms of an oxalate salt of 6-O-(4-dimethylaminoethoxy)cinnamoyl fumagillol.

Abstract: Provided is a superior, novel heterocyclic compound with improved solubility in oil such as sesame oil and benzyl benzoate, which has a broader treatment spectrum, causes less side effects, and is superior in tolerability and safety, and use thereof. A heterocyclic compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof.

Abstract: The present invention relates to a process for the preparation of dabigatran etexilate of the formula or pharmaceutically accepted salts thereof.

Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

Abstract: The present invention relates to a process for the preparation of a precursor for the synthesis of hexanoic acid derived statins and to the use of said precursor in the manufacture of a medicament.

Abstract: The present invention relates to new 4,6-diaminopyrimidine stimulators of soluble guanylate cyclase, pharmaceutical compositions thereof, and methods of use thereof

Abstract: Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract: The present invention relates to compounds according to Formulas I, IA or IB: to pharmaceutically acceptable composition, salts thereof, their synthesis and their use as SIK2 inhibitors including such compounds and methods of using said compounds in the treatment of various diseases and or disorders such as cancer, stroke, cardiovascular, obesity and type II diabetes.

Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.

Abstract: This application discloses a process to synthesize 8-({1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy)-methyl]-8-pheny-1.7-diaza-spiro[4.5]decan-2-one comprising reacting a compound of the Formula 27a-sulfonate with zinc in the presence of acetic acid.

Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Compounds having the structures are described, as are pharmaceutical-compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

Abstract: Provided are methods for preventing and treating injuries caused by exposure to biological warfare agents. The methods include administering to a subject in need thereof an effective amount of a TRPA1 antagonist or a pharmaceutically acceptable salt thereof. In an embodiment the TRPA1 antagonist is selected from the group consisting of compounds of formula I and compounds of formula II as described herein.

Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.

Abstract: This invention relates to novel compounds of the Formula A, B, or C, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier.

Abstract: Disclosed is an organic electroluminescent device (organic EL device) which is improved in luminous efficiency, sufficiently secures driving stability, and has a simple configuration. The organic EL device of this invention comprises a light-emitting layer between an anode and a cathode piled one upon another on a substrate and the light-emitting layer contains a phosphorescent dopant and an unsymmetrical indolocarbazole compound as a host material. The unsymmetrical indolocarbazole compound has a structure in which two or more groups having an indolocarbazole structure are linked together by a linking group and at least one of the groups has an isomeric indolocarbazole skeleton different from those of the other groups. Examples of the unsymmetrical indolocarbazole compound include compounds represented by the following formula (2) wherein A is a substituent, each of R1 to R3 is a hydrogen atom or a substituent, and L is a linking group composed of an aromatic group.

Abstract: Presently provided are IDO inhibitors and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.

Abstract: Compounds of formula (I) which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.

Abstract: The fused heterocyclic compound represented by formula (1) has excellent effectiveness in pest control. In the formula (1), J represents formula J1, J2, J3, J4, J5 or J6; A1; A2; A3; A4; A5; B1; B2; B4; B5; and B6 each represent a nitrogen atom, etc.; B3 represents NR5, etc.; R1 represents a C1-C6 chain hydrocarbon group, etc., optionally having one or more atoms or groups selected from group X; the pairs R2 and R3 and R5 and R6 are the same or different, and represent a C1-C6 chain hydrocarbon group, etc., optionally having one or more atoms or groups selected from group X; R4 represents a C1-C6 chain hydrocarbon group, etc., optionally having one or more atoms or groups selected from group W; and n represents 0, 1, or 2.

Abstract: Compounds Formula I: and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one of Fms protein kinase or Kit protein kinase.

Abstract: Solid and crystalline forms of tofacitinib hydrochloride and tofacitinib hydrobromide, processes for the preparation thereof and processes for the use thereof in preparing tofacitinib citrate are provided.

Abstract: The present invention relates to compounds of formula (X) or pharmaceutically acceptable salts thereof, wherein R1-R50, a, b, d, e, f, g, h, i, j, k, l, o, p, q, r, s, t, u, y, and z are defined herein. The novel dihydropyrrolopyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.

Abstract: Provided are certain fused tetra or penta-cyclic compounds and salts thereof, compositions thereof, and methods of use thereof.

Abstract: This invention relates to certain heteroaryl compounds for use as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of helminth infections and the treatment of parasitosis caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.

Abstract: Compounds useful as kinase inhibitors are provided herein, as well as salts, pharmaceutical compositions, methods of medical treatment and methods of synthesis thereof.

Abstract: A method of fabricating an organic device is provided comprising providing a first solution comprising an organic semiconductor or a precursor thereof; a solvent and a decomposable polymer additive, where the polymer additive is heated so that it decomposes into gas. The method is applicable to large scale fabrication of OLEDs, OPVs and OFET devices.

Abstract: The present invention provides a crystalline form of HPPH (2-((1?-n-hexyloxy)ethyl)-2-divinyl-pyropheophorbide-a): The crystalline form can be characterized by an X-ray powder diffraction (XRD) pattern and differential scanning calorimeter (DSC) pattern. The present invention also provides a method for preparing the crystalline form of HPPH.

Abstract: The present invention relates to indole carboxamide compounds of formula (I) or a salt thereof wherein R2, R3, R4, R6, R7, R8, R51 and R52 have the meanings as indicated herein, and are MT1 and/or MT2 receptor agonists useful for treating and/or preventing urological diseases.

Abstract: This invention is directed to methods of preparing certain spiro-oxindole derivatives, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Abstract: The present invention relates to a technique for preparing an anhydrosugar alcohol using hydrogenated sugar as a raw material and, more specifically, to a technique for preparing a high-purity anhydrosugar alcohol by adding an acid to hydrogenated sugar (for example, hexitol) to convert same to an anhydrosugar alcohol, then distilling the converted liquid, and crystallizing the distilled liquid in a solvent, the technique removing a crystallization solvent from a crystallization mother liquor generated during a crystallization step and then introducing the resultant product together with the distilled liquid and the converted liquid into a distillation step, thereby being capable of improving the total distillation yield of the anhydrosugar alcohol, improving distillation efficiency by improving the mobility of a distillate, and further reducing the amount of generated waste and treatment costs and thus highly efficiently preparing the high-purity anhydrosugar alcohol at reduced costs.

Abstract: Disclosed are thienopyrimidinone derivatives as antagonists that act on metabotropic glutamate receptor subtype 1. The thienopyrimidinone derivatives show pharmacological activity against metabotropic glutamate receptor-related diseases, including pain, such as neuropathic pain and migraine, psychiatric diseases, such as anxiety disorder and schizophrenia, urinary incontinence, and neurodegenerative diseases, such as Parkinson's disease and Alzheimer's disease. Also disclosed are methods for preparing the thienopyrimidinone derivatives, and pharmaceutical compositions containing the thienopyrimidinone derivatives as active ingredients.

Abstract: The invention discloses a D-biotin preparation method. In the prior art, with a synthesis method utilizing malonic acid diester as raw materials, impurities are also produced along with the obtained D-biotin. The D-biotin preparation method is characterized in that with the presence of dimethyl sulfoxide and inorganic base as catalysts, methane tricarboxylic acid trialkyl ester and (3aR, 8aS, 8bS)-1,3-dibenzyl-2-oxo-10H-iminazole [3,4-d] thiophene [1,2-a] sulfuryl halide are subjected to condensation reaction in methylbenzene solvent to obtain intermediate (3 aS,4S,6aR)-1,3-dibenzyl-4-(?,?,?-3-methoxycarbonylbutyl)-4H-1H-thiophene[3,4-d]iminazol e-2,4(1H)-ketone, and the D-biotin is obtained after the intermediate is treated by the aftertreatment method. By the D-biotin preparation method, production of the impurities is avoided, quality of the biotin is greatly improved on the existing basis, and side reaction is avoided too.

Abstract: The present invention provides for compounds of Formula I, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as therapeutic agents in the treatment of TGF?-mediated conditions, including cancer and fibrotic disorders. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.

Abstract: A method for producing a heterocyclic compound represented by general formula (2) from a heterocyclic compound represented by general formula (1) (in the formulae, X1 represents a halogen atom; each of Y1 and Y2 independently represents an oxygen atom, sulfur atom, or selenium atom; each of R1 and R2 independently represents a substituent; m and n respectively represent the number of substituents R1 and R2, each of m and n representing an integer of 0-4; and when m and n are 2 or higher, R1 and R2 may be the same or different and may bond to each other to form an optionally substituted ring).