Abstract: The present invention relates to compounds of formula I wherein R1? is CH3; R1 is methyl, ethyl, CF3, cyclopropyl, CH2OH or R1? and R1 may form together with the carbon atom to which they are attached a 1,1-dioxo-thiolan-3-yl ring; R2 is hydrogen, methyl, ethyl, isopropyl, tertbutyl, cyclopropyl, CH2OH or C(CH3)2OH; R3 is Cl, F, CF3, cyano, methyl or cyclopropyl; R4 is hydrogen, methyl or F; or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof for use in the treatment of psychiatric disorders such as schizophrenia, bipolar disorder, obsessive-compulsive disorder or autism spectrum disorder.

Abstract: The invention relates to medicine and can be used for treating a range of diseases in the treatment of which interferon is used. The agent for inducing endogenous interferon is comprised of the compound 6-(3-methoxycarbonyl phenyl) amino-2,4 (1H, 3H)-pyrimidinedione C12H11N3O4 of general formula: (I). The preparation exhibits greater activity both when injected and when administered orally.

Abstract: One aspect of the disclosure relates to derivatives of aryl and heterocyclic ureido aryl and heterocyclic carboxamido isobutyric acids, dichlorophenyl urea, curcumin, and 1,3-diazetidine-2,4-dione, and pharmaceutical compositions thereof. The derivatives disclosed herein can modulate development of adipocytes and various cancer cells, including resistant cancer cells and cancer stem cells. Another aspect of the disclosure relates to the use of the derivatives and pharmaceutical compositions disclosed herein in treatment of obesity and various cancers.

Abstract: The present invention relates to diaminotriazine compounds and to their use as herbicides. It also relates to agrochemical compositions for crop protection and to a method for controlling unwanted vegetation. wherein p is 1 or 2; q is 0, 1, 2 or 3 provided that p+q is 1, 2, 3 or 4; Q is inter alia a chemical bond, O, S(O)m, CRq1Rq2, NRq3, C(O), C(O)O, Ar is phenyl, which is unsubstituted or carries 1, 2, 3, 4 or 5 radicals RA Ra is inter alia hydrogen, halogen, OH, CN, amino, NO2, C1-C6-alkyl, etc; Rb is inter alia halogen, OH, CN, amino, NO2, C1-C6-alkyl, etc.; R1 and R2 are inter alia H, OH, S(O)2NH2, CN, C1-C6-alkyl, etc; X is a radical selected from the group consisting of CR3R4R5, phenyl, which is unsubstituted or carries 1, 2, 3, 4 or 5 radicals RAr; NR3aR3b, OR3c, S(O)kR3d, k being 1, 2 or 3; and including their agriculturally acceptable salts.

Abstract: This invention provides a novel disubstituted 1,2,4-triazine compound or a pharmaceutically acceptable salt thereof, which has an aldosterone synthetase inhibitory activity and is useful for preventing and/or treating various diseases or conditions associated with aldosterone; a method for preparing it; use of it; as well as a pharmaceutical composition comprising it as an active ingredient. A compound of the general formula [I]: wherein RA is, for example, a group of the following formula (A-1): wherein ring A1 is, for example, a cycloalkyl group which may be substituted, and RB is, for example, a monocyclic cycloalkyl group, or a pharmaceutically acceptable salt thereof.

Abstract: This invention pertains generally to compounds of Formula I as described herein and compositions containing such compounds, as well as methods of using such compounds to treat bacterial infections. In certain aspects, the invention provides methods and compositions comprising these compounds for treating infections caused by Gram-negative bacteria.

Abstract: The present invention is directed to compounds of Formula I: and pharmaceutically acceptable salts, prodrugs, solvates, hydrates, tautomers, or isomers or thereof, wherein R1, R2, R2?, L, X, W, Y1, Y2, Y3, and Y4 are described herein.

Abstract: The present invention provides a category of cyano-substituted asymmetric cyanine dyes having the following general structural Formula I and its synthesizing method. The cyano-substituted asymmetric cyanine dyes in present invention are easily synthesized and have long emission wavelength, high molar extinction coefficient, high sensitivity, good light stability, high fluorescence quantum yield after binding with nucleic acid, and low cell toxicity, which is beneficial for application as fluorescent dyes and could also be used in the field of identifying nucleic acid molecules, clinical diagnostics, and immunoassay testing etc.

Abstract: The invention describes compounds that inhibit both HDAC and GSK3? (i.e., HDAC/GSK3? dual inhibitors). The invention further describes compositions containing these HDAC/GSK3? dual inhibitors, as well as methods and kits using these HDAC/GSK3? dual inhibitors to treat various medical conditions. The invention also provides methods and kits using a HDAC inhibitor and a GSK3? to treat various medical conditions, and compositions containing a HDAC inhibitor and a GSK3?. Medical conditions treatable with various embodiments of the invention include but are not limited to cancers and tumors.

Abstract: Compositions and processes for producing high purity acesulfame potassium are described. One process comprises the steps of forming a cyclic sulfur trioxide adduct; hydrolyzing the cyclic sulfur trioxide adduct to form an acesulfame-H composition comprising acesulfame-H; neutralizing the acesulfame-H in the acesulfame-H composition to form a crude acesulfame potassium composition comprising acesulfame potassium and less than 2800 wppm acetoacetamide-N-sulfonic acid, wherein the neutralizing step is conducted or maintained at a pH at or below 11.0; and treating the crude acesulfame potassium composition to form the finished acesulfame potassium composition comprising acesulfame potassium and less than 37 wppm acetoacetamide-N-sulfonic acid.

Abstract: Compositions and processes for producing high purity acesulfame potassium are described. One process comprises the steps of providing a crude acesulfame potassium composition comprising acesulfame potassium and acetoacetamide, concentrating the crude acesulfame potassium composition to form a water stream and an intermediate acesulfame potassium composition comprising acesulfame potassium and less than 33 wppm acetoacetamide, and separating the intermediate acesulfame potassium composition to form the finished acesulfame potassium composition comprising acesulfame potassium and less than 33 wppm acetoacetamide. The concentrating step is conducted at a temperature below 90° C. and the separating step is conducted at a temperature at or below 35° C.

Abstract: A process for producing acesulfame potassium, the process comprising the steps of providing a cyclizing agent composition comprising a cyclizing agent and a solvent and having an initial temperature, cooling the cyclizing agent composition to form a cooled cyclizing agent composition having a cooled temperature less than 35° C., reacting an acetoacetamide salt with the cyclizing agent in the cooled cyclizing agent composition to form a cyclic sulfur trioxide adduct composition comprising cyclic sulfur trioxide adduct; and, forming from the cyclic sulfur trioxide adduct in the cyclic sulfur trioxide adduct composition the finished acesulfame potassium composition comprising non-chlorinated acesulfame potassium and less than 39 wppm 5-chloro-acesulfame potassium. The cooled temperature is at least 2° C. less than the initial temperature.

Abstract: The present invention relates to a process for the synthesis of 5-hydroxymethyl furfural (HMF) comprising the steps of: 1) dehydrating at least one saccharide selected from monosaccharides having 6 carbon atoms and disaccharides, oligosaccharides or polysaccharides formed from units having 6 carbon atoms or mixtures thereof in the presence of at least one quaternary ammonium salt R3R?N+X?; in which: —R, which is the same or different, represents a C1-C16 substituted or unsubstituted alkyl group; —R? belongs to the group consisting of: hydrogen, C1-C16 substituted or unsubstituted alkyl group, monocyclic substituted or unsubstituted aryl group; —X? represents an anion selected from chloride, bromide, iodide, fluoride, hydroxide, BF4? and PF6?; at a temperature of between 80 and 120° C.

Abstract: The present invention relates to a coumarin derivative of Formula (L) for detection of cysteine and process for preparation thereof. The present invention further relates to a process of detection of cysteine residues present in protein as well as the cysteine released by the enzymatic action of aminoacylase 1 by using coumarin derivative of Formula (L).

Abstract: Subject of the invention is a method for enantioselective production of an isoflavane from an isoflavone, comprising the steps: (a) selectively reducing the isoflavone, such that the 4-keto group of the isoflavone is converted to a 4-hydroxy group, and the 2,3-double bond of the isoflavone is converted to a 2,3-single bond, thereby obtaining a 4-hydroxy intermediate, and (b) reacting the 4-hydroxy intermediate with a chiral reagent, such that a chiral group is covalently attached to the C4-position of the 4-hydroxy intermediate, thereby obtaining a chiral intermediate. The invention also relates to intermediates of formulae (IV), (V), (VI) and (VII) obtainable in the inventive process.

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: Described herein are compounds that inhibit wild-type RET and its resistant mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.

Abstract: Compounds of the formulas: wherein: R1-R4, X1, Y1, and A are as defined herein are provided. Pharmaceutical compositions of the compounds are also provided. In some aspects, these compounds are are useful for the treatment of a disease or disorder. In some embodiments, the disease or disorder is a proliferative disease such as cancer.

Abstract: The present invention provides Quinazolin-THF-amines as PDE I inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.

Abstract: The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-HI's, function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-HI's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.

Abstract: A compound of general formula (I) in which R1, R2, R3 and R5, identical or different, each represent a hydrogen atom or a hydroxyl group, optionally protected by a protecting group. R4 represents a hydrogen atom or an —OR7 group, in which R7 represents a hydrogen atom, a protecting group or a gallate group. R6 represents a hydroxyl group, optionally protected by a protecting group. R?1, R?2, R?3 and R?4, identical or different, each represent a hydrogen atom or a substituent not comprising a mesomeric electron withdrawing group conjugated with the furan ring. A substituent from R?1, R?2, R?3 and R?4 representing the covalent bond with the pyran ring or one of the salts of same. A method for obtaining such a compound includes a step of depolymerization of condensed tannins in the presence of an acid by means of a nucleophile derived from furan.

Abstract: The present invention relates to a process for the preparation of a compound of formula (A), Further, the present invention relates to the respective compound (A) as such and to its use in the preparation of antifungal agent.

Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.

Abstract: The present invention provides muscarinic M4 receptor agonists of formula (I) and pharmaceutically acceptable salts thereof, wherein m, n, p, q, R, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases such as schizophrenia, Alzheimer's disease and various cognitive disorders as well as in the treatment or alleviation of pain.

Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors.

Abstract: The present invention relates to a process for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate of the formula (I) and to a process for purifying the crude product of the compound of the formula (I) for use as pharmaceutically active compound, where, for purification, methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate sulphinyldimethane (1:1), i.e. a compound of the formula (II), is isolated as intermediate or is generated as intermediate in this purification process, if appropriate present in a mixture.

Abstract: Amine compounds having activity against inflammation, fungi, unicellular parasitic microorganisms, and cancer are described. The compounds contain a monocyclic, bicyclic, or tricyclic aromatic ring having one, two, or three ring nitrogen atoms.

Abstract: The present invention provides compounds useful as inhibitors of PDK1. The present invention also provides compositions thereof, and methods of treating PDK1-mediated diseases.

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one 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, melanoma, and the like.

Abstract: Provided are a hydroxyethyl sulfonate of a cyclin-dependent protein kinase inhibitor, a crystalline form thereof and a preparation method therefor. Specifically, 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperidin-4-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one hydroxyethyl sulfonate (compound of formula (I)), a crystal form I thereof and a preparation method therefor are provided. Crystal form I of the compound of formula (I) has good chemical and crystalline stability, low toxicity, and low residual crystallization solvent. Therefore, the crystal form I can be used in improved clinical therapy.

Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; Y is OR1 or NR2R3, and R1, R2, R3 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.

Abstract: Provided herein are spirocycle compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL and/or ABHD6. Furthermore, the subject compounds and compositions are useful for the treatment of pain.

Abstract: In one aspect, the invention provides compounds of Formula I: (I) and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, Y, Za are defined as set forth in the disclosure. The invention also provides compounds of any one of Formulae II to VII, IA to IC, and IIA to IIC, and pharmaceutically acceptable salts and solvates thereof. Other aspects of the invention include the use of compounds of Formulae I to VII, IA to IC, and IIA to IIC, and pharmaceutically acceptable salts and solvates thereof for the treatment of disorders responsive to modulation of one or more opioid receptors. In certain embodiments, the Compounds of the Invention are useful for treating pain.

Abstract: A method of stabilizing riboflavin by affixing the riboflavin to at least one substrate for the riboflavin by covalent bonding, hydrogen bonding, Van der Waals forces, or a combination thereof, to form an optically-activated complex, is provided. When activated by absorption of light in the ultraviolet (UV) to visible region of the electromagnetic spectrum the riboflavin in the complex re-emits light of longer wavelength in the blue-green-yellow region of the electromagnetic spectrum.

Abstract: The invention provides a mercaptoalkylglycoluril represented by the general formula (I): wherein R1 and R2 each independently represent a hydrogen atom, a lower alkyl group, or a phenyl group; R3, R4, and R5 each independently represent a hydrogen atom or a mercaptoalkyl group selected from a mercaptomethyl group, a 2-mercaptoethyl group, and a 3-mercaptopropyl group; and n is 0, 1, or 2. The invention further provides an epoxy resin composition comprising an epoxy resin and the mercaptoalkylglycoluril, and a method for producing a laminate or a multilayer printed circuit board using the same.

Abstract: The present invention relates to compounds useful as inhibitors of the PAR-2 signaling pathway. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of GPCRs in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such GPCRs; and the comparative evaluation of new inhibitors of the PAR-2 signaling pathway. The compounds of this invention have formula I: wherein the variables are as defined herein.

Abstract: Novel compounds of Formula I and their use in therapeutic treatments.

Abstract: Disclosed are chemical entities of formula (I) wherein X, Y, Z, R1, R3, R4, R5 and R6 are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of formula I.

Abstract: The invention provides compounds of the Formula (I) or a pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1, R2, R4, Ra, and the subscripts m, p, and q are as described herein. The compounds or their pharmaceutically acceptable salts can modulate the body's production of cyclic guanosine monophosphate (“cGMP”), and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose.

Abstract: The present disclosure provides a method for efficiently producing and providing compounds having a spirooxindole skeleton, for example compounds having a spirooxindole skeleton and having antitumor activity that inhibit the interaction between Mdm2 protein and p53 protein, or intermediates thereof, using an asymmetric catalyst. Compounds having optically active tricyclic dispiroindole skeletons are obtained through catalytic asymmetric 1,3-dipolar cycloaddition reactions using ketimine as a reaction substrate and using a chiral ligand and a Lewis acid.

Abstract: Disclosed are an antiviral compound and a use thereof in the preparation of a medicament for the treatment of virus infections. Specifically, the present invention relates an imidazole derivative for treating respiratory syncytial virus infection.

Abstract: Crystals of a dispiropyrrolidine compound or a salt thereof which inhibits the action of Mdm2 are provided. The present invention provides crystals of (3?R,4?S,5?R)—N-[(3R,6S)-6-carbamoyltetrahydro-2H-pyran-3-yl]-6?-chloro-4?-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2?-oxo-1?,2?-dihydrodispiro[cyclohexane-1,2?-pyrrolidine-3?,3?-indole]-5?-carboxamide or a salt thereof which inhibits Mdm2 and has anti-tumor activity. The present invention also provides a medicament comprising the same.

Abstract: The invention provides a method of treating drug and alcohol abuse, depression, anxiety, or a compulsive disorder in a subject comprising administering to the subject a compound having the formula: or a pharmaceutically acceptable salt or solvate thereof, wherein R, R1, R2, R3, R4, R5, and X are as defined in the specification.

Abstract: In general, the present invention features improved methods useful for the synthesis of analogs of halichondrin B, such as eribulin and pharmaceutically acceptable salts thereof (e.g., eribulin mesylate).

Abstract: The present disclosure provides processes for the preparation of a compound of formula I: which is useful as an antiviral agent. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.

Abstract: Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using heterocycle amines. Some of the disclosed embodiments include heterocycle amines useful to treat inflammatory disorders.

Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where m, p, q, W, Z, Y, X1, X2, R1, R2 R3 and R4 are as defined herein.

Abstract: This invention relates to new carbocyanine dye compositions, pharmaceutical compositions comprising such compositions, methods of detecting via near infrared fluorescent imaging incipient cancer cells and selective destruction of cancer cells identified by administration of such pharmaceutical compositions. A method of detecting and destroying cancer cells includes introducing a gold dye into an organism suspected of having a cancer cell. The gold dye is a carbocyanine dye covalently attached to a gold nanoparticle. A near infrared light is shined on a region suspected of having the cancer cell. Fluorescence from the gold dye is detected. A beam of radio frequency energy is directed at the region to induce hyperthermia in the cancer cell. The carbocyanine dye has the most basic structure of MHI-148 and structures 6 and 22 with a Aun—[CH2(CH2)9CH2—(OCH2CH2)4O]COCH2CH2-phenyl-O group on a cyclohexene ring that imparts activity to the cancer cell binding and destruction processes.

Abstract: Disclosed is a compound of formula (I): (R1 R2N)SinH2n(NR3R4) (I) wherein subscript n, R1, R2, R3 and R4 are as defined herein. Also disclosed are a method of making, intermediates useful therein, method of using, and composition comprising the compound of formula (I).

Abstract: Disclosed is a compound of formula (I): (R1R2N)SinH2n+1 (I), wherein subscript n is an integer from 3 to 9; and each R1 and R2 independently is (C1-C6)alkyl, (C3-C6)cycloalkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, or phenyl; or R1 is H and R2 is (C1-C6)alkyl, (C3-C6)cycloalkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, or phenyl; or R1 and R2 are bonded together to be -R1a R2a wherein -R1a-R2a- is (C2-C6)alkylene. Also disclosed are a method of making, intermediates useful therein, method of using, and composition comprising the compound of formula (I).