Abstract: 3-(2-amino-ethyl)-5-[3-(4-substituted-phenyl)-alkylidene)-thiazolidine-2,4-dione and 1-(2-amino-ethyl)-3-alkylidene-1,3-dihydro-indol-2-one and derivatives thereof are provided for use as selective SphK2 inhibitors and for use in the treatment of human diseases, such as cancer.

Abstract: This invention relates to methods of reversing and inhibiting liver fibrosis and hepatitis using a small indolinone molecule Hesperadin and related compounds. Methods of identifying such agents and using them to inhibit the expression of collagens and ECM proteins including MMPs and TIMPs in purified hepatic stellate cells are provided. In vivo data of Hesperadin in inhibiting induced collagen production are presented. This method of specifically targeting drugs to hepatic stellate cells in vivo, provides a novel therapy for liver diseases.

Abstract: The invention is compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.

Abstract: Compounds of general formula I: wherein R1a, R1b, R2, R3a, R3b and X are as defined herein are tyrosine kinase inhibitors and are useful for the treatment of various diseases and conditions, for example cancer.

Abstract: The present invention relates to the improvement in organic electroluminescent devices by using compounds of the formula (1), in particular as hole-injection or hole-transport materials in a hole-injection or hole-transport layer.

Abstract: A compound of Formula (1), is disclosed wherein P1 and P2 are alcohol protecting groups or 1,3-diol protecting group, R is selected from: wherein R4a is selected from alkyl, aryl, arylalkyl and cycloalkyl, Rc is selected from H, alkyl, aryl, alkaoxy, haloalkyl, monohaloalkyloxy, and dihaloalkyloxy, Rd is selected from alkyl, aryl, arylalkyl, CF3, halo and NO2 and X is selected from O, N—H, N-alkyl and S, Ra and Rb are same or different and each represents hydrogen, an alkyl group of 1 to 12 carbon atoms, an aryl group of 6 to 12 carbon atoms, or an aralkyl group of 7 to 12 carbon atoms.

Abstract: The present invention provides oxazine compounds, method of using and method of making oxazine compounds and its pharmaceutical use.

Abstract: The present invention relates to a cellulose acetate film for optical compensation and a retardation enhancer used therein, and relates to a cellulose acetate film which has a high retardation value in the thickness direction (Rth).

Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerization inhibitors.

Abstract: The present invention relates to chemical-pharmaceutical industry and medicine. The present invention relates to N-[3-(4-nitrophenylamino)-indole-2-ilmethylene]aminoguanidine hydrochloride of formula (2) having anti-inflammatory and chondroprotective activity. The compound does not exhibit adverse effects.

Abstract: The invention relates to pharmaceutical compositions comprising casein kinase 1 delta (CK1?) and to the use of said inhibitors in the treatment of neurodegenerative disorders such as Alzheimer's disease.

Abstract: Protein tyrosine phosphatase (PTP) Shp2 is a non-receptor PTP that involved in cell signaling and regulation of cell proliferation, differentiation, and migration. Shp2 mediates activation of kinases that are involved in the pathogenesis of human carcinoma. A high throughput screen identified compounds that inhibit the PTP Shp2. Several compounds were identified that selectively inhibit Shp2 over Shp1 with low to sub-micromolar activity. Also disclosed are methods of inhibiting a protein tyrosine phosphatase in a cell and treating cancer through selective inhibition of Shp2.

Abstract: An indole compound having a carbamoyl group, a ureido group and a substituted oxy group having the following formula (1) or a salt thereof: In the formula (1), R1 represents a hydrogen atom, an alkyl group, a hydroxy group, or an alkoxy group; R2 represents a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; R3 represents a halogen atom, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group, a heterocyclic group an alkoxy group, an alkenyloxy group, an alkynyloxy group, a cycloalkyloxy group, an aryloxy group or a heterocyclic oxy group; m represents 0, 1, 2, or 3.

Abstract: Some embodiments of this invention include methods for treating disease and methods for administering a compound of Formula (I). In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of Formula (I). Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I).

Abstract: Disclosed are novel methods for the synthesis of N-substituted indol-3-yl-alkylamide compounds which act as P2X7R antagonists, said methods involving the rearrangement of an oxime intermediate.

Abstract: The present invention relates to 3-Aminosulfonyl Substituted Indole Derivatives of Formula (I): The invention also relates to compositions comprising at least one 3-Aminosulfonyl Substituted Indole Derivative, and methods of using the 3-Aminosulfonyl Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.

Abstract: Compounds of general formula I: wherein R1a, R1b, R2, R3a, R3b and X are as defined herein are tyrosine kinase inhibitors and are useful for the treatment of various diseases and conditions, for example cancer.

Abstract: The present invention relates to chemical-pharmaceutical industry and medicine. The present invention relates to N-[3-(4-nitrophenylamino)-indole-2-ilmethylene]aminoguanidine hydrochloride of formula (2) having anti-inflammatory and chondroprotective activity. The compound does not exhibit adverse effects.

Abstract: Hydrazone compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.

Abstract: Compounds of formula (I): wherein: R1 represents a hydrogen atom or a —COOR group, R2 represents a group G or a linear or branched (C1-C6)alkyl group substituted by a group G, wherein G represents a —(CH2)n-A-(CH2)m—B—(CR4R5)p—(CH2)o—R6 group as defined in the description, R3 represents a hydrogen atom, an alkyl group or an NO2 group. Medicinal products containing the same which are useful in treating hypertension and cardiovascular pathologies.

Abstract: The present invention provides oxazine compounds, method of using and method of making oxazine compounds and its pharmaceutical use.

Abstract: The present invention relates to methods of treating a subject with malaria comprising administering a 2-aminoindole compound represented by Formula: (I)—The values and preferred values of the variables in Structural Formula I are defined herein.

Abstract: The present invention provides compounds of formula or pharmaceutically acceptable salts, esters or stereoisomers thereof, wherein R1 to R4, A and Y have the meanings given herein, as well as methods for making those compounds and their use as medicament, in particular as medicament for the treatment of cancer.

Abstract: The present invention provides a new class of excited state intramolecular charge transfer (ESIPT) dye compounds based on mono or dihydroxy substituted 1,3-bisiminoisoindole motif and metal complexes containing such compounds as ligands. The present invention also provides OLEDs containing the compound and/or metal complex as the emissive material.

Abstract: The present application discloses compounds of the formula: and pharmaceutical compositions containing same and their use for treating and preventing various pathologies, including obesity, appetite disorders, excess weight and diabetes.

Abstract: This invention is directed to indolone derivatives which are antagonists for the GALR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier.

Abstract: Disclosed is a compound represented by the general formula (1) or a salt thereof. The compound or a salt thereof has an inhibitory activity on IKK? and is therefore useful as preventive and/or therapeutic agent for a disease associated with IKK?. In the formula, R1 represents a hydrogen atom, a lower alkyl group, an aryl group, a hydroxy group, or the like; R2 represents a halogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, or the like; and m represents 0, 1, 2, or the like.

Abstract: The present invention is related to derivatives of benzenesulfonamide represented by formula (I), and the pharmaceutical composition thereof. In addition, the benzenesulfonamide derivatives disclosed in the present invention can serve as potential cell cycle inhibitors, and thereby these benzenesulfonamide derivatives and the pharmaceutical composition thereof can be antitumor drug candidates, which might aim at cell cycle. Particularly, the benzenesulfonamide derivatives disclosed in the present invention may function as antitumor drugs to treat solid cancers.

Abstract: Protein tyrosine phosphatase (PTP) Shp2 is a non-receptor PTP that involved in cell signaling and regulation of cell proliferation, differentiation, and migration. Shp2 mediates activation of kinases that are involved in the pathogenesis of human carcinoma. A high throughput screen identified compounds that inhibit the PTP Shp2. Several compounds were identified that selectively inhibit Shp2 over Shp1 with low to sub-micromolar activity. Also disclosed are methods of inhibiting a protein tyrosine phosphatase in a cell and treating cancer through selective inhibition of Shp2.

Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R0; R1; R2; R3; R4; R5; R6; A1; A2; A3; A4, Q, T and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional N-aminoindole or N-amino-azaindoles of the formula I from 2-halo-phenylacetylenes or (2-sulfonato)phenyl-acetylenes and N,N-disubstituted hydrazines, useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.

Abstract: Methods of treating or suppressing oxidative stress disorders including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-heterocyclylaminoalkyl-(p-quinone) derivatives.

Abstract: The present invention relates to a series of substituted aza-indole derivatives of the formula I: wherein R, R1, R2, R3, R4, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5?-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.

Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification.

Abstract: Compounds of Formula I wherein A1, B1, C1, D1, E1, F1 and L1 are as defined herein, which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein, such as leukemia and lymphoma, are disclosed.

Abstract: The present invention relates to heterocyclyl-substituted sulfonamides with 5-HT6 receptor affinity, and compositions thereof, and the use of said compounds for the treatment or prophylaxis of various disorders.

Abstract: The object is to provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. The solving means is a 1,3-dihydroisobenzofuran derivative represented by the following general formula (1) or salt thereof, or their solvate.

Abstract: The present invention relates to synthetic studies on novel indole derivatives having a carbamoyl group, a ureido group and a substituted oxy group or a salt thereof, and pharmaceutical actions of the derivatives. The compound and a salt thereof represented by the general formula (1) has an IKK? inhibitory activity and is useful as a preventive and/or therapeutic agent for diseases considered to be associated with IKK?.

Abstract: The invention relates to a nitrogen heterocycle compound of formula 1: Also disclosed are a method of synthesizing the compound and use of the compound for treating various diseases and conditions.

Abstract: To provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A 2-oxochromene derivative represented by the following general formula (1) or salt thereof, or their solvate.

Abstract: [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. [Means for Solving Problems] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic action, and as a result, they have found that various amide derivatives having a carboxylic group or an equivalent thereof exhibit an excellent EP4 receptor antagonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor antagonistic action, it is useful as an agent for preventing and/or treating chronic renal insufficiency or diabetic nephropathy.

Abstract: This invention is directed to indolone derivatives which are antagonists or the GALR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier.

Abstract: Provided herein are isolated compounds of formula I: processes for their preparation and isolation, as well as pharmaceutical compositions which comprise these therapeutic agents, and methods of use therefore the treatment and/or control of conditions associated with or mediated by effects of histone deacetylase.

Abstract: Compounds of formula (I): wherein: R1 represents a hydrogen atom or a —COOR group, R2 represents a group G or a linear or branched (C1-C6)alkyl group substituted by a group G, wherein G represents a —(CH2)n-A-(CH2)m—B—(CR4R5)p—(CH2)o-R6 group as defined in the description, R3 represents a hydrogen atom, an alkyl group or an NO2 group.

Abstract: The present application is directed to novel P2X7R antagonists that are N-indol-3-yl-acetamide and N-azaindol-3-yl-acetamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity.

Abstract: A hair and/or scalp treatment composition comprising an amino-oxo-indole-ylidene compound of general formula (I): (I) formula should be here in which: R1, R2, R3 and R4 are each, independently, hydrogen or a monovalent organic group selected from alkyl, alkenyl, alkynyl, aryl, alkylenearyl, cycloalkyl, cycloalkenyl, and heterocyclyl.

Abstract: Provided are compounds which are indole derivatives, as well as pharmaceutical compositions containing the compounds. Also provided are methods of using the indole compounds for preventing or treating a disease, or a condition that predisposes to a disease, wherein the disease or condition is associated with activation of the serine/threonine kinase B (Akt) in an animal. The method comprises administering to the animal a preventive or treatment effective amount of the indole compound. Further provided is a method for increasing apoptosis of an animal cell comprising contacting the cell with the indole compound.

Abstract: Hydrazone compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.

Abstract: A crystalline form of N-(3-cyano-4-methyl-1H-indol-7-yl)-3-cyanobenzenesulfonamide having a diffraction peak at a diffraction angle (2?±0.2°) of 19.1° in a powder X-ray diffraction.

Abstract: The present invention relates to new beta-agonists of general formula (I) wherein the groups R1 and R2 have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers, solvates, hydrates, mixtures thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, methods of preparing these compounds and their use as pharmaceutical compositions.

Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R0; R1; R2; R3; R4; R5; R6; A1; A2; A3; A4, Q, T and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional N-aminoindole or N-amino-azaindoles of the formula I from 2-halo-phenylacetylenes or (2-sulfonato)phenyl-acetylenes and N,N-disubstituted hydrazines, useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.