Abstract: Benzoxazole and indole type KCa3.1 activators as well as the therapeutic uses of such compounds in human or animal subjects and their use in ex vivo preservation of organs or tissues.

Abstract: The invention provides compounds of Formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.

Abstract: Inhibitors of HIV-1 protease and compositions containing them are described. Use of the inhibitors and compositions containing them to treat HIV, AIDS, and AIDS-related diseases is described.

Abstract: Novel benzoarylureido compounds and a use thereof for prevention and/or treatment of the neurodegenerative brain disease are provided. The neurodegenerative brain diseases may include Alzheimer's disease, dementia, Parkinson's disease, stroke, amyloidosis, Pick's disease, Lou Gehrig's disease, Huntington's disease, Creutzfeld-Jakob disease, and the like.

Abstract: Various embodiments of the present invention relate to, among other things, compounds and methods of using those compounds to treat an HIV infection. The compounds of the various embodiments of the present invention provide, among other things, therapeutic agents having enhanced penetration capability across the blood-brain barrier, such that they can enter the CNS to treat an HIV-1 infection in the CNS.

Abstract: The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.

Abstract: Provided herein are heterocyclic compounds for treatment of CSF1R, FLT3, KIT, and/or PDGFR? kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.

Abstract: The invention relates to substituted benzothiazoles, benzoxazoles—and their counterparts having pyridine and pyrimidine rings replacing the benzene ring—that are PDE4 inhibitors useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula I: in which A and B are carbocycles or heterocycles.

Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.

Abstract: The present invention pertains to a compound represented by a formula (I) and a method for producing thereof (in the formula, Ax is an organic group having 2 to 30 carbon atoms that includes at least one aromatic ring selected from a group consisting of an aromatic hydrocarbon ring and an aromatic hetero ring, Ay is a hydrogen atom, an alkyl group having 1 to 18 carbon atoms, a cycloalkyl group, an alkenyl group having 2 to 18 carbon atoms, an organic group having 2 to 30 carbon atoms that includes at least one aromatic ring selected from a group consisting of an aromatic hydrocarbon ring and an aromatic hetero ring, or the like. Ax and Ay optionally bond to each other to form a ring, and Q is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like.).

Abstract: The invention is directed to compounds for selectively inhibiting glycosidases, uses of the compounds and pharmaceutical compositions including the compounds, and methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, and/or accumulation or deficiency of O-GlcNAc.

Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.

Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.

Abstract: The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.

Abstract: The present invention relates to a polymerizable compound represented by a formula (I). The present invention provides a polymerizable compound, a polymerizable composition, a polymer, and an optically anisotropic article that are capable of obtaining an optical film having a low melting point, having excellent solubility, capable of being manufactured at low cost, and capable of uniform polarized light conversion across a broad wavelength region. [In formula: Y1 to Y6 are independently a chemical single bond, —O—, —O—C(?O)—, —C(?O)—O— etc.; G1 and G2 are independently a divalent C1-C20 aliphatic group etc.; Z1 and Z2 are independently C2-C10 alkenyl group that is substituted with a halogen atom etc.; Ax is a C2-C30 organic group that includes at least one aromatic ring selected from a group consisting of an aromatic hydrocarbon ring and an aromatic hetero ring; Ay is a hydrogen atom, a C1-C20 alkyl group, a C2-C20 alkenyl group, a C3-C12 cycloalkyl group etc.; A1 is a trivalent aromatic group etc.

Abstract: The invention provides the process illustrated in scheme 1 for synthesizing heterocyclic compounds of formula I. In the process, an isothiocyanate of formula II is initially reacted with a primary amine or formula III to give a thiourea of formula IV. Subsequently, the thiourea of formula IV is converted to the corresponding heterocycle of formula I using a base and a sulfonyl chloride.

Abstract: The invention relates to 2,7-disubstituted benzoxazole and 2,4-disubstituted oxazolo[5,4-c]pyridine compounds of the formula I given below, as well as salts thereof, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, these compounds for use in the treatment (including prophylaxis) of the animal, especially human, body (especially with regard to a proliferative disease), the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment especially of a protein tyrosine kinase mediated disease (such as a tumor disease) or for the manufacture of a pharmaceutical preparation for use in the treatment of such a disease, a method for the treatment of such a disease and a pharmaceutical preparation for the treatment of a disease as mentioned. The compounds are of the formula I, wherein the symbols are as defined in the description. The compounds inhibit, for example, JAK2 and JAK3.

Abstract: The present invention relates to benzoxazole derivatives represented by the Formula 1, which has an inhibitory activity against interleukin-6 (IL-6), a method for preparation thereof, and a pharmaceutical composition containing the same. The compound represented by the Formula 1 according to the present invention has a superior inhibitory activity against interleukin-6, and therefore, can be practically applied for prevention and treatment of diseases caused by abnormal interleukin-6 activity.

Abstract: Inhibitors of HIV-1 protease and compositions containing them are described. Use of the inhibitors and compositions containing them to treat HIV, AIDS, and AIDS-related diseases is described.

Abstract: The invention relates to N-arylaminomethylenebenzothiophenones of General Formula (I) for use as a drug for the treatment of cardiovascular diseases: wherein E is S, O, or CH2, D is CH or NH, and Ar is a phenyl or naphtyl moiety substituted by an electron-withdrawing group, an unsubstituted heteroaryl residue, or a heteroaryl residue substituted by alkyl or an electron-withdrawing group.

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.

Abstract: The present invention is directed to substituted benzothiazole and benzoxazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.

Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.

Abstract: The invention provides compounds of Formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.

Abstract: The present invention provides a therapeutic agent for hyperlipidemia having an excellent effect of lowering the cholesterol and triglyceride level in blood plasma. The present invention relates to a prophylactic and/or therapeutic agent for hyperlipidemia, a prophylactic and/or therapeutic agent for obesity or diabetes mellitus, and a prophylactic and/or therapeutic agent for metabolic syndrome, each agent including a compound represented by the formula (1), or a salt thereof, and a statin, particularly pitavastatin, in combination.

Abstract: Provided herein are heterocyclic compounds for treatment of CSF1R, FLT3, KIT, and/or PDGFR? kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.

Abstract: The present invention relates to benzoxazole derivatives represented by the Formula 1, which has an inhibitory activity against interleukin-6 (IL-6), a method for preparation thereof, and a pharmaceutical composition containing the same. The compound represented by the Formula 1 according to the present invention has a superior inhibitory activity against interleukin-6, and therefore, can be practically applied for prevention and treatment of diseases caused by abnormal interleukin-6 activity.

Abstract: The present invention provides a compound represented by the formula which is useful as an agent for the prophylaxis or treatment of diseases related to the action of melatonin, or a salt thereof and the like.

Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the heterocyclic entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.

Abstract: A novel organic compound which can be preferably used as a phosphorescent host material is provided. A benzoxazolyl carbazole compound represented by the general formula [1] shown in the specification is provided.

Abstract: This application relates to a novel benzo-heterocycle derivative and more particularly, it relates a composition for preventing and treating cancer or for inhibiting metastasis comprising benzo-heterocycle derivative or pharmaceutically acceptable salts thereof as an active ingredient. The present inventors confirmed that KRS has an effect on cancer metastasis by facilitating cancer (or tumor) cell migration through interaction with 67LR, and also found that a substance inhibiting the interaction between KRS and 67LR can prevent and treat cancer by inhibiting cancer cell metastasis. Accordingly, the composition of the present invention can inhibit cancer metastasis, and thus provide a novel means for prevention and treatment of cancer.

Abstract: A process for preparing a compound of formula (I) or a salt or solvate thereof, by reacting a compound of formula (IV): with a compound of formula (V): to obtain the compound of formula (I): wherein each R1 is independently a halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl, C1-C6 haloalkoxy or C1-C6 alkylcarbonyl; R2 is C1-C6 alkyl, C1-C6 haloalkyl, or phenyl optionally substituted with at least one selected from the group consisting of a halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl, C1-C6 haloalkoxy, and nitro; R3 is C1-C6 alkyl, C3-C8 cycloalkyl, or a phenyl optionally substituted at least one selected from the group consisting of a halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl, and C1-C6 haloalkoxy; n is 0, 1, or 2; and X is S atom or O atom.

Abstract: The present invention relates to an optically active (R)-aryloxypropionic acid amide compound which has high selectivity and safety for protecting a crop such as rice, wheat, barley and soy bean, and exhibits excellent herbicidal activity against weeds, and a herbicidal composition comprising the same.

Abstract: The present invention relates to 5,6-ring annulated indole derivatives of the formula (I), compositions comprising at least one 5,6-ring annulated indole derivatives, and methods of using the 5,6-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.

Abstract: The invention relates to substituted benzothiazoles, benzoxazoles—and their counterparts having pyridine and pyrimidine rings replacing the benzene ring—that are PDE4 inhibitors useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula I: in which A and B are carbocycles or heterocycles.

Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.

Abstract: The invention relates to compounds of formula 1, the production and use thereof as a medicament for the treatment of diseases, particularly tumours and/or diseases caused, mediated or propagated by angiogenesis. The compounds of formula 1 are effective inhibitors of tyrosin kinases, particularly TIE-2 and VEGFR, and Raf-kinases.

Abstract: This invention provides an anorectic or anti-obesity composition comprising a compound of the formula (I): formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted lower alkyl, Y is —S(O)n- wherein n is 1 or 2, or —CO—, R2 is hydrogen or lower alkyl, R7 is hydrogen or lower alkyl, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, and Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like.

Abstract: An FGF21 production promoting agent containing, as an active ingredient, a compound represented by the following formula (1): wherein each of R1 and R2, which may be identical to or different from each other, represents, for example, a hydrogen atom; each of R3a, R3b, R4a, and R4b, which may be identical to or different from one another, represents, for example, a hydrogen atom or a halogen atom, or R3a and R3b or R4a and R4b may bond together to form an alkylenedioxy group; X represents an oxygen atom, a sulfur atom, or N—R5 (R5 represents, for example, a hydrogen atom or a C1-4 alkyl group); Y represents, for example, an oxygen atom, an S(O)l group (l is a number of from 0 to 2), or a carbonyl group; Z represents CH or N; n is a number of from 1 to 6; and m is a number from 2 to 6, a salt of the compound, or a solvate of the compound or the salt.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein the variables are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.

Abstract: Substituted heteroaromatic carboxamide and urea compounds corresponding to formula (i) processes for the preparation thereof, pharmaceutical compositions containing these compounds and also a method of using these compounds in pharmaceutical compositions for treating or inhibiting pain and other conditions mediated at least in part via the vanilloid receptor 1.

Abstract: Compounds of Formula I: (I) in which A, A1, R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and/or IL-13.

Abstract: Novel benzoarylureido compounds and a use thereof for prevention and/or treatment of the neurodegenerative brain disease are provided. The neurodegenerative brain diseases may include Alzheimer's disease, dementia, Parkinson's disease, stroke, amyloidosis, Pick's disease, Lou Gehrig's disease, Huntington's disease, Creutzfeld-Jakob disease, and the like.

Abstract: Vanilloid receptor ligand compounds corresponding to formula I: pharmaceutical compositions containing such compounds, a process for producing such compounds, and methods of using such compounds for treating or inhibiting pain and various other disorders or conditions.

Abstract: The present invention is directed to cyclopropyl proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.

Abstract: The invention provides compounds of Formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcN Ac.

Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.

Abstract: The present invention relates to novel anti-inflammatory and antiallergic compounds of the glucocorticosteroid series, methods of preparing such compounds, pharmaceutical compositions comprising them, combinations and therapeutic uses thereof. More particularly, the invention relates to glucocorticosteroids that are derivatives of pyrrolidine.

Abstract: Provided is a heterocyclic compound showing strong Raf inhibitory activity. A compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.