Abstract: A bis(perfluoroether carboxylic acid alkyl)amino ester represented by the general formula: {CnF2n+1O[CF(CF3)CF2O]aCF(CF3)COO(CH2)b}2NR, wherein R is a hydrogen atom, an alkyl group having 1 to 12 carbon atoms, an aryl group, or an aralkyl group; preferably an alkyl group having 1 to 6 carbon atoms or an aryl group; n is an integer of 1 to 3; a is an integer of 0 to 20, preferably an integer of 1 to 6; and b is an integer of 1 to 12, preferably an integer of 1 to 4. The bis(perfluoroether carboxylic acid alkyl)amino ester having an amino group at the end of the ester group is produced by reacting a perfluoroether carboxylic acid fluoride compound of the formula: CnF2n+1O[CF(CF3)CF2O]aCF(CF3)COF and a bis(hydroxyalkyl)amine compound of the formula: HO(CH2)bNR(CH2)bOH at a molar ratio of 2:1 in the presence of an alkali metal fluoride.

Abstract: The present invention provides a process for the preparation of 4-dimethylaminocrotonic acid of Formula (II) or its salts, which is used as an intermediate for the preparation of afatinib or its salts.

Abstract: Non-lactone carbocyclic and heterocyclic antagonists and agonists of bacterial quorum sensing. Pharmaceutical composition containing antagonists. Methods employing antagonists and agonists for modulation of quorum sensing. Compounds are exemplified by those of formula: A-[Z]n-L1-[Y]q-W-[V]m-L2-HG, where A is an acyclic aliphatic group, and HG is an optionally substituted phenyl group. Compounds include those where m and n are both 0, W is —NH—, Y is present and is —CO—CH2—CO—, and L1 and L2 independently are —[CH2]p1— and —[CH2]p2—, where p1 and p2, independently, are 0 or integers ranging from 1-10.

Abstract: The present invention relates generally to therapeutics targeting the bacterium Porphyromonas gingivalis, including its protease Lysine gingipain (Kgp), and their use for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, as described herein, and pharmaceutically acceptable salts thereof.

Abstract: The present invention provides dihydroorotate dehydrogenase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders wherein the inhibition of Dihydroorotate dehydrogenase is known to show beneficial effect.

Abstract: A perfume composition comprising an effective amount of at least one alkadienenitrile selected from 4,8-undecadienenitrile and isomers thereof, 4,9-dodecadienenitrile and isomers thereof, and 4,10-tridecadienenitrile and isomers thereof. The isomers of 4,8-undecadienenitrile comprise Z,Z-4,8-undecadienenitrile, E,E-4,8-undecadienenitrile, and mixed Z/E isomers of 4,8-undecadienenitrile; the isomers of 4,9-dodecadienenitrile comprise Z,Z-4,9-dodecadienenitrile, E,E-4,9-dodecadienenitrile, and mixed Z/E isomers of 4,9-dodecadienenitrile; and the isomers of 4,10-tridecadienenitrile comprise Z,Z-4,10-tridecadienenitrile, E,E-4,10-tridecadienenitrile, and mixed Z/E isomers of 4,10-tridecadienenitrile. A composition comprising an effective amount of at least one alkadienenitrile selected from 4,8-undecadienenitrile and isomers thereof, 4,9-dodecadienenitrile and isomers thereof, and 4,10-tridecadienenitrile and isomers thereof. Processes for the preparation of the isomeric alkadienenitriles are provided.

Abstract: The present invention relates to novel ortho alkynyl anilines of formula (I) which are useful in synthesis of drug intermediates and natural products and process for preparation of these ortho alkynyl anilines of formula (I) via copper catalyzed Multi Component Reactions (MCR).

Abstract: The present invention provides sulfamoylbenzamide derivatives, and pharmaceutical compositions thereof. In certain embodiments, the compounds and pharmaceutical compositions of the invention inhibit pregenomic RNA encapsidation. In other embodiments, the compounds and pharmaceutical compositions of the invention are useful for treating Hepatitis B virus (HBV) infection.

Abstract: A Addition-fragmentation oligomers containing allylic disulfide groups are described. The oligomers may be added to polymerizable compositions to provide labile crosslinks that can cleave and reform during the polymerization process.

Abstract: A method for preparing peroxide, including a step of treating, in a reaction medium, a component having at least one tertiary alcohol grouping with a compound having at least one tertiary hydroperoxide function in the presence of a catalyst, said method being characterized in that the catalyst includes a sulphonic acid and a inorganic acid, the molar ratio between the sulphonic acid and the aforementioned component including at least one tertiary alcohol grouping ranges from 0.05 to 0.8, and the molar ratio between the inorganic acid and the aforementioned component including at least one tertiary alcohol grouping ranges from 0.05 to 0.8. Also, to the peroxide resulting directly from said preparation method.

Abstract: A compound represented by formula (1) (in the formula: ring-D represents a three- to eight-membered hydrocarbon ring; Ra represents an optionally substituted amino C1-6 alkyl group or the like; Rb1 and Rb2 each independently represent a hydrogen atom, a halogen atom, or the like; Rc represents an optionally substituted C6-10 aryl group or the like; Rd represents a hydrogen atom or the like; and ring-Q represents a (hetero)aryl group or the like which may be substituted with a carboxyl group or the like) or a pharmaceutically acceptable salt thereof exhibits an excellent FXIa inhibitory activity, and is useful as a therapeutic agent against thrombosis or the like.

Abstract: Peptides and compounds are provided that function as EWS-FLI1 protein inhibitors. The peptides and compounds have utility in the treatment of Ewing's sarcoma family of tumors. Also provided are methods of preparing the compounds and assays for identifying inhibitors of EWS-FLI1 protein.

Abstract: The invention relates to pyridone amide compounds of formula I and I? or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain.

Abstract: Novel base addition salts of nitroxoline with improved solubility and increased urine secretion under physiological conditions are described. Pharmaceutical compositions and methods of treatment using the pharmaceutical compositions are also described.

Abstract: The invention relates inter alia to compounds of the general formula (I) in which the A1-A4, T, n, W, Q, R1 and B1-B4 radicals are each as defined in the description. Also described are processes for preparing the compounds of the formula (I). The inventive compounds are especially suitable for controlling insects, arachnids and nematodes in agriculture, and ectoparasites in veterinary medicine.

Abstract: A compound with antitumor activities represented by formula I: In formula I, R1 is alkyl, alkoxy, or ethenyl; and R2 is alkyl, alkoxy, or halogen.

Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.

Abstract: Fexinidazole is prepared according to a method which comprises the following steps: a) reacting 1-methyl-2-hydroxymethyl-5-nitro-imidazole with methanesulfonyl chloride in the presence of a suspension of powdered alkaline carbonate in an anhydrous organic solvent suitable for performing nucleophile substitution reactions; b) adding to the resulting reaction medium a solution of 4-methyl-mercapto-phenol in the same organic solvent as referred to in step a); c) separating fexinidazole from the reaction mixture as its hydrochloride salt and d) converting said hydrochloride salt into fexinidazole and optionally, purifying the latter.

Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.

Abstract: This invention is related to the antifungal compounds having azole structure in Formula (1), and hydrates, solvates, pharmaceutically acceptable salts or geometric isomers thereof. Formula (1).

Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).

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 autoimmune diseases utilizing the compounds of the invention.

Abstract: The present invention is directed to a process for the preparation of phosphoric acid loaded covalent organic framework (PA@Tp-Azo and PA@Tp-Stb) with high stability and high proton conductivity.

Abstract: N-(Oxazol-2-yl)-aryl-carboxylic acid amides and use thereof as herbicides N-(Isoxazol-3-yl)arylcarboxamides and their use as herbicides are described. In this formula (I), A represents N or C—Y. R, R?, V, X, Y and Z represent radicals such as hydrogen, halogen and organic radicals such as substituted alkyl.

Abstract: The present invention provides MDM2 inhibitor compounds of Formula (I), or the pharmaceutically acceptable salts thereof, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor of Formula (I).

Abstract: A method of sealing an end of a polymer with a carbodiimide compound without liberating an isocyanate compound. A compound including a cyclic structure having one carbodiimide group whose first nitrogen and second nitrogen are bonded together by a bond group is used as an end-sealing agent for the polymer.

Abstract: The present invention relates to the following compounds for use in the treatment of a bacterial infection wherein the integers are as defined in the description. The invention also relates to compounds for use as medicaments, pharmaceutical compositions and some novel compounds.

Abstract: A method for lowering the sodium content of different carriers which may have different physical properties as well as varying degrees of sodium is provided. The method, which lowers the sodium content from the surface, subsurface as well as the binding layer of the carrier, includes contacting a carrier with water. A rinse solution is recovered from the contacting. The rinse solution includes leached sodium from the carrier. The sodium content in the rinse solution is then determined. The contacting, recovering and determining are repeated until a steady state in the sodium content is achieved.

Abstract: A novel Rh(I)-catalyzed approach to synthesizing functionalized (E,Z) dienal compounds has been developed via tandem transformation where a stereoselective hydrogen transfer follows a propargyl Claisen rearrangement. Z-Stereochemistry of the first double bond suggests the involvement of a six-membered cyclic intermediate whereas the E-stereochemistry of the second double bond stems from the subsequent protodemetallation step giving an (E,Z)-dienal. The reaction may be represented by the following sequence.

Abstract: The present invention relates to new types of processes for the improved preparation of homofarnesol, in particular of (3E,7E)-homofarnesol and homofarnesol preparations with an increased content of (3E,7E)-homofarnesol (also referred to as all E-homofarnesol).

Abstract: The present invention discloses the syntheses of new 3-hydroxyflavone salts with defined structures, which are suitable for sensor applications for sensing anions, cations, DNA chains and organic compounds soluble in highly polar solvent like water.

Abstract: The present invention provides a compound having an excellent efficacy for controlling weeds. A dihydropyrone compound of formula (I): wherein m is 1, 2 or 3; n is an integer of any one of 1 to 5; X represents O, S, S(O) or S(O)2; R1 represents a hydrogen atom or a methyl group; R2 and R3 represents a hydrogen atom, an C1-6 alkyl group and the like; when X represents S, S(O) or S(O)2, R4 represents an C1-6 alkyl group, a C1-6 haloalkyl group, an C6-10 aryl group or a five- to six-membered heteroaryl group, and X represents O, S, S(O) or S(O)2, R4 represents an C6-10 aryl group or a five- to six-membered heteroaryl group; G represents a hydrogen atom and the like; Z represents a halogen atom, a cyano group, a nitro group, a phenyl group, an C1-6 alkyl group and the like; is useful as an active ingredient for herbicides.

Abstract: A compound with antitumor activities is represented by formula A or formula B R1, R2, R3, and R4 are independently hydrogen, hydroxyl, alkoxy, halogen, formyl, unsubstituted or substituted alkyl, or unsubstituted or substituted cycloalkyl.

Abstract: The invention relates to a method for producing 2,3,5-trimethyl benzoquinone or a compound containing 2,3,5-trimethyl benzoquinone, the method comprising the following steps: Oxidation of 2,3,6-trimethylphenol with oxygen or an oxygen-containing gas in a two- or multi-phase reaction medium in the presence of a catalyst or catalyst system containing at least one copper (II)-halide to a mixture containing 2,3,5-trimethyl benzoquinone, characterized in that the reaction medium contains water and at least one secondary aliphatic acyclic alcohol having 6 or more, preferably 7 or more, carbon atoms.

Abstract: The present invention relates to compound of Formula I or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates to a process for manufacturing compounds of Formula I.

Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula (1a) or a salt thereof, wherein p, q, r, s, Q, R3 and R4 are as defined herein.

Abstract: A chiral synthesis of pyrrolidine compounds en route to selective neuronal nitric oxide synthase inhibitors, and representative inhibitor compounds heretofore unattainable.

Abstract: The present invention provides a compound selected from the group consisting of a compound of formula (I), pharmaceutically acceptable salts, esters, prodrugs, hydrates, solvates and isomers thereof; a use of the compound for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase, and a use of the compound for the manufacture of a medicament for the treatment, relief or prevention of the diseases; a pharmaceutical composition comprising the compound as an active ingredient; and a method for the treatment, relief or prevention of the diseases using the compound. The inventive compound is useful for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase.

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: 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: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.

Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.

Abstract: The present invention provides a compound which has an effect of inhibiting amyloid ? production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid ? proteins. A compound of the formula (I): wherein X is —C(R3a)(R3b)—, —C(R3a)(R3b)—C(R3c)(R3d)— or —C(R3a)?C(R3c)—, R1 is substituted or unsubstituted alkyl or the like, R2a, R2b, R3a, R3b, R3c and R3d are each independently hydrogen, halogen or the like, R4 is hydrogen or halogen, Ring B is substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.

Abstract: The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.

Abstract: A crystalline Form B of compound 1 can be used in pharmaceutically compositions. The pharmaceutical compositions can be used in methods of treating a disease (e.g., a disease of the central nervous system).

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrrolopyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.

Abstract: Generally, the present invention provides novel quinoline compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same.

Abstract: The present invention relates to substituted fused heterocyclic compounds. The substituted fused heterocyclic compounds are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of substituted fused heterocyclic compounds as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

Abstract: Compounds of formulae (I), (II), and (III), defined herein, are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.