Abstract: The present invention generally relates to compounds as a dual kinase-demethylase inhibitor useful for the treatment of diseases mediated by a kinase and/or a histone demethylase, such as inflammation, cancer, viral and bacterial infections, neurological and immunological disorders. Pharmaceutical compositions and methods for treating those diseases are within the scope of this invention.

Abstract: Disclosed is an organic light-emitting device using a compound capable of emitting delayed fluorescence and capable of undergoing intramolecular hydron transfer. The compound includes, for example, a compound represented by the general formula. X1 to X3 each represent O or S; R1 to R6 each represent nH or a substituent; n, n1 to n3 each represent an integer of 1 to 3.

Abstract: The invention relates to novel pyrido-phenanthroline derivatives, to the production and use thereof in the field of medicine, in particular for cancer therapy.

Abstract: The present invention generally relates to compounds as a dual kinase-demethylase inhibitor useful for the treatment of diseases mediated by a kinase and/or a histone demethylase, such as inflammation, cancer, viral and bacterial infections, neurological and immunological disorders. Pharmaceutical compositions and methods for treating those diseases are within the scope of this invention.

Abstract: The disclosure provides new, stable, pharmaceutically acceptable salt forms of 1-(4-fluoro-phenyl)-4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one, together with methods of making and using them, and pharmaceutical compositions comprising them.

Abstract: The invention described herein pertains to selective Janus kinase (JAK) inhibitors and methods of use thereof. Also described are methods for treating diseases involved abnormal JAK/STAT signaling pathway in mammals using the described selective JAK inhibitors or a pharmaceutical formulation thereof.

Abstract: Disclosed is an imidazole[4,5-f][1,10]phenanthroline derivative conforming to the chemical structural formula of: Wherein X and Y are independently selected from the group consisting of Z-substituted aryl ring, Z-substituted heteroaryl ring, unsubstituted aryl ring, or unsubstituted heteroaryl ring, and wherein Z is independently selected from the group consisting of aryl, C1-4 alkoxy, amino, nitro, trifluoromethyl, cyano, halo atom, or C1-24 aliphatic hydrocarbyl. The present invention further discloses a method of preparing the imidazole[4,5-f][1,10]phenanthroline derivative and the use thereof.

Abstract: There is provided a production method for the purpose of improving the solubility of an arginine-residue imidazopyrroloquinoline in water and making the purity thereof high. There is provided a compound represented by general formula (1): wherein n is 1, 2, 3 or 4; and M is an alkali metal or ammonium.

Abstract: The present invention relates to novel tricyclic compounds of formula (I) and (II) More particularly, the present invention relates to novel tricyclic compounds of formula (I) and (II) and process of preparation of these compounds from 4,5-di-methyl-o-phenylinediamine. Further, the present invention relates to a process for preparation of tricyclic compound hunanamycin A.

Abstract: A triazole derivative represented by General Formula (G0) is provided. In the General formula (G0), A represents a substituted or unsubstituted carbazolyl group, a substituted or unsubstituted dibenzothiophenyl group, or a substituted or unsubstituted dibenzofuranyl group, E represents substituted or unsubstituted triazolo [4,3 f]phenanthridine or substituted or unsubstituted triazolo [3,4-?]isoquinoline, and Ar represents a substituted or unsubstituted arylene group having 6 to 13 carbon atoms.

Abstract: The invention provides novel nicotinic acetylcholine receptor agonists, for example, phantasmidine and derivatives thereof, for example a compound of formula (I). Also disclosed are methods of treating disorders responsive to nicotinic acetylcholine receptor agonists such as Alzheimer's disease, schizophrenia, Myasthenia Gravis, Tourette's syndrome, Parkinson's disease, epilepsy, pain, and cognitive dysfunction by treatment with the nicotinic acetylcholine for agonists.

Abstract: New phenanthroline derivatives as drug as well as methods for producing said compounds are provided.

Abstract: Compounds of formula I: wherein variables A1, A2, B, m, n, J, R4, G1, G2, G3 and Y are as described herein, which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Abstract: Compounds of Formula (I) wherein n, A, R1, R2, R3 and R5 are defined herein, are useful for the treatment of cytomegalovirus disease and/or infection.

Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.

Abstract: In accordance with the present invention, tetracyclic caboline derivatives that inhibit the expression of VEGF post-transcriptionally have been identified, and methods for their use provided. In one aspect of the invention, these compounds useful in the inhibition of VEGF production, in the inhibition of angiogenesis, and/or in the treatment of cancer, diabetic retinopathy or exudative macular degeneration are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the inhibition of angiogenesis, and/or the treatment of cancer, diabetic retinopathy or exudative macular degeneration using the compounds of the invention.

Abstract: The present invention relates to a norepinephrine and selective serotonin receptor blocker and the use thereof. The norepinephrine and selective serotonin receptor blocker is a compound of formula I, or isomers, pharmaceutically acceptable salts or solvates thereof, wherein R1 is selected from the group consisting of C1-6 alkyl, C1-6 alkoxy, C6-10 aralkyl, C6-10 arylalkoxy, C1-6 haloalkyl and C1-6 haloalkoxy; and R2 is one or more groups each independently selected from the group consisting of hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, nitro, cyano, amino, hydroxyl, C1-6 haloalkyl, and C1-6 haloalkoxy. R3 is one or more groups each independently selected from the group consisting of hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, nitro, cyano, amino, hydroxyl, C1-6 haloalkyl, and C1-6 haloalkoxy. The compound of the present invention is effective norepinephrine and selective serotonin receptor blocker.

Abstract: An arylamine-based compound is represented by Formula 1 below. The arylamine-based compound is included in an organic light emitting diode.

Abstract: The present invention relates to a compound derived from indole corresponding to the following formula II: wherein X represents N, CR8 or N+R8, wherein R8 represents a hydrogen atom, a hydroxyl or alkyl or methoxy group optionally substituted with a phenyl group; R2, R3 and R4 independently represent a hydrogen atom or a halogen atom or an optionally substituted alkyl, amine, alkene, ester, sulfonamide, ether or benzyl group; R5 represents a hydrogen atom or an optionally substituted, saturated or unsaturated alkyl group, amine, benzyl group; R6 represents an optionally substituted C1-C3 alkyl group; R7 represents a hydrogen atom or an optionally substituted C1-C3 alkyl group and R7 is absent when the ring A is in the b position, and A represents a ring; R9 and R10 represent together a carbon bond or independently represent an R11 OR11, SR11 group; wherein R11 represents a hydrogen atom, an optionally substituted, saturated or unsaturated, C1-C3 alkyl group, which may contain one or more sulfur, oxygen or

Abstract: The present invention relates to a norepinephrine and selective serotonin receptor blocker and the use thereof. The norepinephrine and selective serotonin receptor blocker is a compound of formula I, or isomers, pharmaceutically acceptable salts or solvates thereof, wherein R1 is selected from the group consisting of C1-6 alkyl, C1-6 alkoxy, C6-10 aralkyl, C6-10 arylalkoxy, C1-6 haloalkyl and C1-6 haloalkoxy; and R2 is one or more groups each independently selected from the group consisting of hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, nitro, cyano, amino, hydroxyl, C1-6 haloalkyl, and C1-6 haloalkoxy. R3 is one or more groups each independently selected from the group consisting of hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, nitro, cyano, amino, hydroxyl, C1-6 haloalkyl, and C1-6 haloalkoxy. The compound of the present invention is effective norepinephrine and selective serotonin receptor blocker.

Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?2B. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.

Abstract: Use of substituted isoquinolinones, isoquinolinediones, isoquinolinetriones and dihydroisoquinolinones of the general formula (I) or their respective salts where the radicals in the general formula (I) correspond to the definitions given in the description, for enhancing stress tolerance in plants to abiotic stress, for strengthening plant growth and/or for increasing plant yield, and selected processes for preparing the compounds mentioned above.

Abstract: The present invention provides novel quinolone 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 invention relates to a process for obtaining compounds derived from tetrahydro-?-carboline, specifically tadalafil and intermediate products from the synthesis, comprising the reaction between piperonal and an alkyl ester of D-tryptophan as a salt, and in the absence of any other component, followed by haloacetylation and a final cyclization with methylamine.

Abstract: A compound for an organic optoelectronic device represented by Chemical Formula 1 wherein, in Chemical Formula 1, variables A, Y1 to Y4, X1, m, R1 to R4, L1 to L3, n1 to n3, Ar1 and Ar2 are described in the specification.

Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor ?2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.

Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.

Abstract: A method of staining a poly(amino acid) by contacting a poly(amino acid) with an overall neutral or overall cationic complex of at least one of transition metal ion, and a plurality of donor ligands each of which is fully coordinated to the transition metal ion and is either a nitrogen donor ligand or a cyclometalated donor ligand, such that at least one of the donor ligands is a cyclometalated donor ligand. Nitrogen donor ligands will contain heteroaryl ring systems having from 10 to 40 ring atoms, wherein each nitrogen donor ligand is substituted with from 0 to 4 R1 groups. Cyclometalated donor ligands will likewise contain heteroaryl ring systems having from 10 to 40 ring atoms, such that at least one ring atom is N, wherein each cyclometalated donor ligand is substituted with from 0 to 4 R1 groups. R1, R2, R3 and R4 groups are defined herein.

Abstract: The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.

Abstract: The present invention relates to compounds of following general formula (I): and to the pharmaceutically acceptable salts of same, the tautomers of same, the stereoisomers or mixture of stereoisomers in any proportions of same, such as a mixture of enantiomers, notably a racemic mixture, as well as to methods for preparing same and uses of same, notably as an antineoplastic agent.

Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.

Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.

Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:

Abstract: The invention provides novel nicotinic acetylcholine receptor agonists, for example, phantasmidine and derivatives thereof, for example a compound of formula (I). Also disclosed are methods of treating disorders responsive to nicotinic acetylcholine receptor agonists such as Alzheimer's disease, schizophrenia, Myasthenia Gravis, Tourette's syndrome, Parkinson's disease, epilepsy, pain, and cognitive dysfunction by treatment with the nicotinic acetylcholine for agonists.

Abstract: Disclosed is a novel process for the preparation of pharmacologically interesting indolopyridine derivatives containing tetracyclic tetrahydro-11-carboline-hydantoines linked to a basic side chain and the corresponding salts, which can be used as Eg5 inhibitors, with very high overall chemical yield and enantiomeric purity.

Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b>]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are 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: This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are 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: A heterocyclic compound includes a compound represented by Formula 1.

Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles 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: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles 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: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles 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: The present invention provides therapeutically effective 2,4,5-trisubstituted imidazole compounds, methods of preparing the same, and compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-microbial agents. The anti-microbial properties of the compounds include anti-bacterial and/or anti-fungal activity.

Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Abstract: The invention provides derivatives and analogues of triazatetracyclo[7.7.0.01,13,02,7]-hexadeca-2,4,6,10,12-pentaenes, 5,7,11-triazatetracyclo[8.7.0.01,6,012,17]-heptadeca-6,8,12,14,16-pentaenes, pharmaceutical compositions comprising these compounds and methods for treatment of hepatitis C viral infections using these compounds.

Abstract: The present invention provides therapeutically effective 2,4,5-trisubstituted imidazole compounds, methods of preparing the same, and compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-microbial agents. The anti-microbial properties of the compounds include anti-bacterial and/or anti-fungal activity.

Abstract: [Problem] To provide a compound useful as medicine having PDE4B inhibitory activity, in particular, as an active ingredient of a composition for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like. [Measures for Solution] The present inventors examined compounds having PDE4B inhibitory activity and found that a tricyclic or tetracyclic imidazo[1,2-a]pyridine derivative or salts thereof had a superior PDE4B inhibitory activity, thereby completing the present invention. The imidazo[1,2-a]pyridine derivative can be used as an agent for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like.

Abstract: The present invention relates to imidazole derivatives having vinyl group represented by general formula (I) which possess electron transporting character, have a high glass transition temperature (Tg), and high decomposition temperature (Td): wherein all symbols are defined as recited in the specification. The present invention also relates to a use of the imidazole derivatives having vinyl group as a guest emitter or electron transporter in luminescent elements.

Abstract: Optionally substituted chromenoisoquinolines and analogs and derivatives thereof are described herein. In addition, syntheses of these compounds are described herein. In addition, uses of these compounds as dopamine receptor binding compounds are described herein.

Abstract: This application relates to tricyclic compounds of Formula I: including all stereoisomers, mixtures of stereoisomers, and salts thereof. This application also relates to compositions comprising compounds of Formula I and uses therefore.