Abstract: The present invention relates to a novel process for the preparation of (R)-3-((1-methylpyrrolidin-2-yl)methyl)-5-(2-(phenylsulfonyl)ethyl)-1H-indole and its intermediates thereof.

Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.

Abstract: The present application relates to novel 3-cyanoalkyl- and 3-hydroxyalkyl-substituted indole derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of cardiovascular diseases.

Abstract: The present invention relates to compounds of formula (I) below in which: —R1 and R3 represent, independently of one another, a methoxy group optionally substituted by one or more fluorine atoms, —R2 and R4 represent, independently of one another, a hydrogen atom or a methoxy group optionally substituted by one or more fluorine atoms, —A represents a ring chosen from the group comprising aryl and heteroaryl groups, said ring possibly being substituted by or fused to a heterocycle, —X represents a nitrogen atom or a CH group, and —Z1 represents a hydrogen atom or a halogen atom, preferably fluorine, and —Z2 represents a hydrogen atom, a halogen atom, preferably fluorine, a C1 to C4 alkyl group, an aryl group or a —CN, —SO2NR12R13, —SO2R9, —COOR15 or —COR15 group, and also to the pharmaceutically acceptable salts thereof, the isomers thereof and the prodrugs thereof.

Abstract: The present invention is related to a process for the preparation of 5-benzyloxy-2-(4-benzyloxyphenyl)-3-methyl-1H-Indole (formula-1, a useful intermediate for the synthesis of bazedoxifene) using 4-benzyloxy propiophenone and 4-benzyloxy phenyl hydrazine hydrochloride.

Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.

Abstract: We have designed a molecular switch based on the photoinduced opening and thermal closing of a [1,3]oxazine ring. A substituted [1,3]oxazine compound described as having a general (i.e., unsubstituted) structure with fused indoline and benzooxazine fragments such that they share a common bond in the [1,3]oxazine compound: (i) the bond connecting positions 1 and 2 of the indoline fragment and (ii) the bond connecting positions 2 and 3 of the benzooxazine fragment. Irradiation by light of suitable wavelength and intensity of this photochromic compound induces cleavage of a [C—O] bond of the [1,3]oxazine ring to form a phenolate chromophore. The photogenerated (e.g., colored) isomer may revert thermally to the starting (e.g., colorless) oxazine. Alternatively, the switch may be between isomers of the compound that absorb at different wavelengths. Reversible coloration of silica or polymeric materials and switching optical signals may involve many cycles of interconversion between different colored states.

Abstract: Compounds of Formula (I), wherein n is 1 or 2, and R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein, their preparation, pharmaceutical compositions, and methods of use are disclosed.

Abstract: Provided is an indole long-chain alcohol, or a hydrate or an isomer thereof, represented by the following formula (I): wherein R1, R2, R3 and R4 each independently represent a hydrogen atom, a methyl group, an acetyl group, or a hydroxyl group, and n represents a number from 0 to 20; and a medicinal composition comprising the same. The indole long-chain alcohol (I) exhibits an excellent nerve growth promoting effect, as well as potent antioxidative and anti-tumor effects, and is therefore useful as a prophylactic and/or therapeutic agent for cerebral diseases including dementia diseases, and malignant tumors including brain tumors.

Abstract: Compounds and methods for treating cancer or inducing apoptosis in proliferating cells. The compounds are shown in formula I: wherein X is selected from hydroxyl, thiol, and amino; Y is selected from carboxyl and sulfonyl; R1, R2, R3, and R4 are selected from hydrogen, lower alkyl, and combinations thereof; R5, R6, and R7 are selected from hydrogen, halo, nitro, amino, methoxy, and combinations thereof; and pharmaceutically acceptable salts thereof.

Abstract: Aryl substituted sulfonamide compounds of formula (I): wherein bond, X, Y, R1, R2, R3, m, and n are defined herein. Also disclosed is a method for treating cancer with these compounds.

Abstract: A novel epoxy compound represented by the following general formula (I), and a production process thereof, is provided: Y—(CH2)3—Si(OR1)nR23-n??(I) (wherein, Y is represented by any of the following formulas: wherein, R1 and R2 represent alkyl groups having 1 to 5 carbon atoms, n represents an integer of 1 to 3, R3 and R4 represent hydrogen atoms, alkyl groups having 1 to 6 carbon atoms or trialkylsilyl groups having 1 to 4 carbon atoms, R5 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or a trialkylsilyl group having 1 to 4 carbon atoms, R6 to R12 represent hydrogen atoms, alkyl groups having 1 to 6 carbon atoms or trialkylsilyl groups having 1 to 4 carbon atoms, and R13 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a trialkylsilyl group having 1 to 4 carbon atoms or an aryl group).

Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.

Abstract: The presently disclosed subject matter is described to metalloenzyme inhibitors having metal binding moieties linked to a targeting moiety through a linking group or a direct bond, method of screening for metalloenzyme inhibitors, and methods for treating a metalloenzyme related disorder by administering a metalloenzyme inhibitor to a subject in need of treatment thereof.

Abstract: The invention relates to novel amino alcohols of the general formula (I) where X, R1, R2, R3, R4, R5 and R6 are each as defined in detail in the description, to a process for their preparation and to the use of these compounds as medicines, in particular as renin inhibitors.

Abstract: The present invention is directed to novel rhodium-phosphorus complexes of formula: [Rh(PP?)(solv)2]X the process for their preparation and their use as catalysts in the ring opening reaction of heteronorbornenes and other ?,?-unsaturated compounds.

Abstract: The present invention provides: a pharmaceutical composition for inhibiting amyloid-? protein accumulation comprising a compound of the formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient; a method for inhibiting amyloid-? protein accumulation, comprising a step of administering an effective amount of the compound of the formula (I) or a pharmaceutically acceptable salt thereof to a mammal which may be diagnosed with an amyloid-? protein-related disease; and so on.

Abstract: Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Abstract: The present invention relates to squarylium dyes including an anchoring group, to a method of synthesis of such dye, to an electronic device comprising such dye, and to uses of such dye.

Abstract: Disclosed are cyanine dyes that are useful for labelling and detecting biological and other materials. The dyes are of formula (I): in which groups R3 and R4 are attached to the Z1 ring structure and groups R5 and R6 are attached to the Z2 ring structure, and n=1, 2 or 3; Z1 and Z2 independently represent the carbon atoms necessary to complete a one ring, or two-fused ring aromatic system; at least one of groups R1, R2, R3, R4, R5, R6 and R7 is the group -E-F where E is a single bond or a spacer group and F is a target bonding group; one or more of groups R11, R12, R13 and R14 are independently selected from the group —(CH2)k—W, where W is sulphonic acid or phosphonic acid and k is an integer from 1 to 10.

Abstract: The present invention relates to novel amino arylsulfonamide compounds of the formula (I), their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them: The present invention also relates to a process for the preparation of above said novel compounds, their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The compounds of the invention are useful in the treatment of various disorders that are related to 5-HT6 receptor functions. Specifically, the compounds of this invention are also useful in the treatment of various CNS disorders, hematological disorders, eating disorders, obesity, anxiety, depression, diseases associated with pain, respiratory diseases, gastrointestinal, cardiovascular diseases and cancer.

Abstract: The invention relates to the use of non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment and prophylaxis of hormone-dependent, particularly estrogen-dependent, diseases. The invention further relates to suitable inhibitors and to a method for the production thereof.

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 provides a light emitting device material which enables a light emitting device having high efficiency and excellent chromatic purity and durability using a light emitting device material containing a pyrene compound represented by formula (1), wherein any one of R1 to R10 is a group represented by formula (2), or 1 to 4 substituents is/are group(s) represented by formula (3), and a light emitting device using the same.

Abstract: The present invention relates generally to substituted indoles and methods of using them.

Abstract: A method of performing a chemical reaction includes reacting a compound selected from the group consisting of an organohalide and an organo-pseudohalide, and a protected organoboronic acid represented by formula (I) in a reaction mixture: R1—B-T ??(I); where R1 represents an organic group, T represents a conformationally rigid protecting group, and B represents boron having sp3 hybridization. When unprotected, the corresponding organoboronic acid is unstable by the boronic acid neat stability test. The reaction mixture further includes a base having a pKB of at least 1 and a palladium catalyst. The method further includes forming a cross-coupled product in the reaction mixture.

Abstract: The present application relates to novel 7-sulfanylmethyl-, 7-sulfinylmethyl- and 7-sulfonylmethylindole derivatives, processes for the preparation thereof, the use thereof alone or in combinations for the treatment and/or prevention of diseases, and the use thereof for the manufacture of medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular disorders.

Abstract: The present invention relates generally to substituted indoles and methods of using them.

Abstract: Indole compounds of the formula: wherein L1, L2, R1, R2, Ra, Rb, Rc, Rd, and Re are defined herein. Also disclosed are methods of using of the indole compounds in inhibiting tubulin polymerization and treating cancer and other angiogenesis-related disorders.

Abstract: This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; R5 is H, alkyl, perfluoroalkyl, aryl optionally substituted with R5, alkanoyl, aroyl optionally substituted with R8; R6 is H, alkyl, alkylaryl, benzyl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R7 is H, alkyl, alkylaryl, aryl optionally substituted with R8; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SO3H, PO3H2, tetronic acid, etc.; R8 is H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.

Abstract: The invention relates to new compounds of formula (1) wherein R is hydrogen or a linear or branched C1-40alkyl; where X is O, S, or NR1 where R1 is a hydrogen, a linear or branched C1-40 alkyl, C2-40 alkenyl or C2-40 alkynyl group, an aryl, a heteroaryl or C1-40 alkylaryl or alkylheteroaryl group and where one or both of C and D is OR2, SR2, NR3R4 where R2, R3 and R4 are each independently hydrogen, a linear or branched C1-40 alkyl, C2-40 alkenyl or C2-40 alkynyl group, an aryl or C1-40 alkylaryl group or a linear or branched C1-40 alkyl NR5R6 chain where R5 and R6 are each independently hydrogen, a linear or branched C1-40 alkyl; or an optionally complex metal ion Mn+/n wherein n is an integer from 1 to 8; or where one or both of C and D are amino acids or nucleic acids attached via either N, O or S; and wherein m is an integer from 1 to 8; and wherein either: I) A is a known aryl or heteroaryl fluorescent group and B is hydrogen, a linear or branched C1-40 alkyl, C2-40 alkenyl or C2- 40 alkynyl group, an ar

Abstract: Novel compounds that have been found effective in inhibiting PDZ domain interactions, and particularly interactions of PDZ domains in MAGIs with the oncogenic (tumor suppressor) protein PTEN and interactions between the PDZ domain in the Dishevelled (Dvl) protein and other proteins such as the Frizzled (Fz) protein, have the general formula The invention also includes combinatorial libraries, arrays and methods for screening and studying proteins using such compounds. Compounds of the invention have produced apoptosis in certain cell lines that overexpress the Dishevelled protein (Dvl); inhibiting Wnt signaling.

Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.

Abstract: The invention provides indole-4,7-dione derivatives useful for the treatment of diseases in a mammal, pharmaceutical compositions containing the same and methods of using the same in the treatment of cancer and neoplastic diseases including human solid tumors and other mammalian tumors.

Abstract: The present invention relates generally to substituted phenyl indoles and methods of using them, for example as PAI-1 inhibitors.

Abstract: Organic compounds having nitrogen atoms protected with t-butoxycarbonyl are effectively deprotected by heating in a fluorinated alcohol solution.

Abstract: This invention relates to compounds having pharmacological activity, to compositions containing these compounds, and to a method of treatment employing the compounds and compositions. More particularly, this invention concerns certain indole derivatives and their salts and solvates. These compounds have H3 histamine receptor antagonist activity. This invention also relates to pharmaceutical compositions containing these compounds and to a method of treating disorders in which histamine H3 receptor blockade is beneficial.

Abstract: The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

Abstract: The invention relates to a photoelectric conversion device, using oxide semiconductor fine particles sensitized with a methine dye represented by the following formula (1) and a solar cell using the same, and a solar cell high in conversion efficiency can be obtained at low cost: in the formula (1), n represents an integer of 0 to 7; R1 represents an optionally-substituted aromatic residue or optionally-substituted aliphatic hydrocarbon residue, or an acyl group; X represents an optionally-substituted hydrocarbon residue which has 2 to 4 carbon atoms; Y represents a hydrogen atom, an optionally-substituted aromatic residue or aliphatic hydrocarbon residue, a carboxyl group or the like, and preferably represents a carboxyl group; Z represents an optionally-substituted aromatic residue or aliphatic hydrocarbon residue, or an acyl group; A1, A2 and A3 each independently represent a hydrogen atom, an optionally-substituted aromatic residue or aliphatic hydrocarbon residue or the like, and preferably represent

Abstract: 4-alkyl/4-alkenyl/4-alkynyl methyl/-1-arylcyclohexylamine compounds corresponding to the formula I a method for producing them, pharmaceutical compositions containing them, and methods of using them to treat or inhibit pain or other specified conditions associated with the ORL1 receptor.

Abstract: A medicament which has an activity of inhibiting production of tissue factor and comprises an LXR ligand as an active ingredient; and a medicament for treatment and/or prophylaxis of vascular restenosis following angioplasty, endarterectomy, percutaneous transluminal coronary angioplasty (PTCA) or stent implantation, or treatment and/or prophylaxis of blood coagulation diseases, diseases induced by platelet aggregation including stable or unstable angina pectoris, cardiovascular and cerebrovascular diseases including thromboembolism formation diseases accompanying diabetes, rethrombosis following thrombolysis, cerebral ischemic attack, infarction, stroke, ischemia-derived dementia, peripheral artery disease, thromboembolism formation diseases during use of an aorta-coronary artery bypass, glomerulosclerosis, renal embolism, tumor or cancer metastasis, which comprises an LXR ligand as an active ingredient.

Abstract: The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

Abstract: Provided is an indole long-chain alcohol, or a hydrate or an isomer thereof, represented by the following formula (I): wherein R1, R2, R3 and R4 each independently represent a hydrogen atom, a methyl group, an acetyl group, or a hydroxyl group, and n represents a number from 0 to 20; and a medicinal composition comprising the same. The indole long-chain alcohol (I) exhibits an excellent nerve growth promoting effect, as well as potent antioxidative and anti-tumor effects, and is therefore useful as a prophylactic and/or therapeutic agent for cerebral diseases including dementia diseases, and malignant tumors including brain tumors.

Abstract: This invention is directed to compounds of the formula (I): wherein one of R6, R7, R8 and R9 is and X, R1 to R12, m, n and o are as defined in the description, and pharmaceutically acceptable salts and/or esters thereof. The invention is also directed to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPAR? and/or PPAR? agonists.

Abstract: This invention pertains to certain 4-(1-(sulfonyl)-1H-indol-2-yl)-4-(hydroxy)-cyclohexa-2,5-dienone compounds, and analogs thereof, including compounds of the following formula, which are, inter alia, antiproliferative agents, anticancer agents, and/or thioredoxin/thioredoxin reductase inhibitors: formula (I) wherein: Ar is a 1-(sulfonyl)-1H-indol-2-yl group; the bond marked ? is independently: (a) a single bond; or: (b) a double bond; the bond marked ? is independently: (a) a single bond; or: (b) a double bond; the group —ORO is independently: (a) —OH; (b) an ether group (e.g., —OMe); or: (c) an acyloxy (i.e., reverse ester) group (e.g.

Abstract: An indole derivative represented by the following general formula (1): wherein at least one of R1, R2, R3, and R4 represents an alkoxy group containing 1 to 20 carbon atoms, and other groups of the R1, R2, R3, and R4 represent hydrogen, an alkyl group containing 1 to 6 carbon atoms, acetyl group, or hydroxyl group; and either one of X and Y represents —(CH2)nOH wherein n is an integer of 0 to 30, and the other one of the X and Y represents hydrogen atom; or a salt thereof; and a drug and an agent for promoting differentiation of a stem cell containing such indole derivative or its salt as an effective component, wherein the indole derivative (1) has action of inducing differentiation of neural stem cell specifically into a neuron, and this indole derivative is useful as a prophylactic or therapeutic drug for brain dysfunction or neuropathy caused by loss or degeneration of the neuron.

Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.

Abstract: The present invention provides novel 2,2-bis(4-hydroxyphenyl)-alkyl onium salts as illustrated by 2,2-bis(4-hydroxyphenyl)-tridecyl(1,2-dimethylimidazolium)bromide and a process for preparation thereof by hydroxyalkylating acetoacetate to the corresponding hyroxyalkylacetoacetate, dealkoxycarbonylating the hydroxyalkyl acetoacetate to ?-hydroxyalkan-2-one and contacting the ?-hydroxyalkan-2-one with phenol in the presence of an acidic catalyst to give 2,2-bis(4-hydroxyphenyl)alkanol, brominating the 2,2-bis(4-hydroxyphenyl)alkanol to 2,2-bis(4-hydroxyphenyl)alkyl bromide, quaternizing 1,2-dimethylimidazole with the 2,2-bis(4-hydroxyphenyl)alkyl bromide to 2,2-bis(4-hydroxyphenyl)alkyl(1,2-dimethylimidazolium)bromide. The products can be used as reactive modifiers for layered phyllosilicates that can be used in the preparation of polymer-nanocomposites, wherein the said polymers are prepared from 2,2-bis(4-hydroxyphenyl)propane as one of the reacting monomers.

Abstract: The compounds of the invention are represented by the following general structure or a pharmaceutically acceptable salt thereof, and compositions containing them, wherein the variables are defined herein, and their use to reduce or inhibit PTH secretion, including methods for reducing or inhibiting PTH secretion and methods for treatment or prophylaxis of diseases associated with bone disorders, such as osteoporosis, or associated with excessive secretion of PTH, such as hyperparathyroidism. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.