Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.

Abstract: Sphingosine-1-phosphate analogs that are potent, and selective agonists at one or more S1P receptors, specifically the S1P1 receptor type are provided. The disclosed compounds include an optional phosphate moiety as well as compounds with hydrolysis-resistant phosphate surrogates such as phosphonates, alpha-substituted phosphonates, and phosphothionates.

Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2). The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 and TYK2 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.

Abstract: Compositions comprising cyclic amino acids or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier. Said composition are for use in the treatment of pain. Pain includes both acute and chronic forms of pain. The preferred cyclic amino acid is 1-aminocyclobutane-1-carboxylic acid (ACBC).

Abstract: The present invention relates to a process for preparing 4-alkoxycarbonyl-3-aminothiophenes of the general formula (I) and/or their hydrochlorides of the formula (I)? in which R1 and R2 are each as defined in the description, and/or their mono- or bisacetylated or mono- or bisformylated form, by reacting enamines of the formula (II) in which R1 and R2 are each as defined in the description, and/or their mono- or bisacetylated or mono- or bisformylated form, with a chlorinating agent in the presence of one or more diluents, and also to a process for preparing the compounds of the formula (II).

Abstract: A photoelectric conversion device comprising an electrically conductive film, an organic photoelectric conversion film, and a transparent electrically conductive film, wherein the organic photoelectric conversion film contains a compound represented by the following formula (1) and an n-type organic semiconductor: wherein each of R1 and R2 independently represents a substituted aryl group, an unsubstituted aryl group, a substituted heteroaryl group or an unsubstituted heteroaryl group, each of R3 to R11 independently represents a hydrogen atom or a substituent provided that an acidic group is excluded, m represents 0 or 1, n represents an integer of 0 or more, R1 and R2, R3 and R4, R3 and R5, R5 and R6, R6 and R8, R7 and R8, R7 and R9, or R10 and R11 may be combined each other to form a ring, and when n is an integer of 2 or more, out of a plurality of R7's and R8's, a pair of R7's, a pair of R8's, or a pair of R7 and R8 may be combined each other to form a ring.

Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.

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: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

Abstract: The invention relates to compounds, in particular 2-amino-3,4,5,-trisubstituted thiophenes, pharmaceutical compositions containing them and the uses of said compounds and compositions for diseases related to sphingosine-1-phosphate (S1P) receptors, predominantly S1P3 receptors. The diseases include cardiovascular diseases, atherosclerosis, cancer, pulmonary oedema, autoimmune disorders and Adult Respiratory Distress Syndrome.

Abstract: The present invention provides a method of producing 2-alkyl-3-aminothiophene derivative represented by Formula (4), the method comprising oxidizing a compound represented by the following Formula (1) to produce a compound represented by the following Formula (3) and reducing the compound represented by the following Formula (3): wherein in Formula (1), Formula (3), and Formula (4), R represents an alkyl group, a cycloalkyl group, or a bicycloalkyl group; and X represents a hydroxyl group, a halogen atom acyloxy group, an alkylsulfonyl group, or an arylsulfonyl group.

Abstract: Crystalline duloxetine hydrochloride, compositions containing the same and methods for the production thereof.

Abstract: Crystalline duloxetine hydrochloride, compositions containing the same and methods for the production thereof.

Abstract: Crystalline duloxetine hydrochloride, compositions containing the same and methods for the production thereof.

Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.

Abstract: The present invention is an improved process for the preparation of a sodium/proton exchange inhibitor of sub-type 3 (NHE-3) useful in the treatment of sleep apnea and other related respiratory disorders.

Abstract: The present invention relates to compounds of formula (I) with the substituents as defined herein, and uses thereof.

Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flaviviridae viral infections.

Abstract: The invention discloses compounds of formula (I); wherein: R is a carboxylic acid or a derivative thereof; R1 is alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, alkylthio, halo or trihalomethyl; R2 is aryl, heteroaryl, arylalkyl or heteroarylalkyl; R3 is H or F; and L is a linking group comprising a chain of from 2 to 8 atoms linking R and the carbonyl group (A); and pharmaceutically acceptable derivatives thereof, useful for treating disorders mediated by peroxisome-proliferator-activated receptor (PPAR) subtype ? (PPAR?). The compounds of the invention are therefore useful in the treatment of metabolic syndrome, obesity, type-II diabetes, dyslipidemia, wound healing, inflammation, neurodegenerative disorders and multiple sclerosis.

Abstract: N-Substituted sulfoximines are effective at controlling insects.

Abstract: N-Substituted sulfoximines are effective at controlling insects.

Abstract: Provided are compounds that are modulators of CCR9 receptor activity, compositions containing the compounds and methods of use of the compounds and compositions. In certain embodiments, provided are methods for treating or ameliorating diseases associated with modulation of CCR9 receptor activity.

Abstract: The present invention relates to AMPA receptor potentiators of Formula I: formulations comprising them, methods for their use, and intermediates useful for their preparation.

Abstract: The present invention relates to a process for preparing 4-alkoxycarbonyl-3-aminothiophenes of the general formula (I) and/or their hydrochlorides of the formula (I)? in which R1 and R2 are each as defined in the description, and/or their mono- or bisacetylated or mono- or bisformylated form, by reacting enamines of the formula (II) in which R1 and R2 are each as defined in the description, and/or their mono- or bisacetylated or mono- or bisformylated form, with a chlorinating agent in the presence of one or more diluents, and also to a process for preparing the compounds of the formula (II).

Abstract: The present invention provides a method of producing a 2-alkyl-3-aminothiophene derivative represented by formula (2) by reducing at least one of the 2-alkenyl-3-aminothiophene derivatives represented by formulae (1a) to (1d), or a mixture thereof, or a salt thereof, without using a protecting group for an amino group: wherein in formulae (1a) to (1d), R1 to R4 each independently represents a hydrogen atom, an alkyl group of 1 to 12 carbon atoms or the like; and R5 and R6 each independently represents a hydrogen atom, a halogen atom, an alkyl group of 1 to 12 carbon atoms or the like. According to the invention, a 2-alkyl-3-aminothiophene derivative usable as an intermediate of agricultural chemicals can be produced by a cost-efficient industrial process, without the use of a high-cost protective group for an amino group.

Abstract: The present invention provides compositions comprising sucralose and 4-amino-5,6-dimethylthieno[2,3-d]pyrimidine-2(1H)-one or salts, solvates, and/or esters thereof and methods of making the compositions by spray drying. The present invention also provides ingestible compositions comprising compositions of the present invention and methods of making such foods. The present invention also includes a process of preparing 2-amino-thiophene derivatives, which are key intermediates for preparing 4-amino-5,6-dimethylthieno[2,3-d]pyrimidine-2(1H)-one.

Abstract: The present invention provides compounds of formula (I) wherein W, R1, R5 and R6 have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric enhancers of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain, and inflammatory pain, cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke, neurological disease or injury, sleep disorders, epilepsy and depression.

Abstract: The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by formula (1): wherein one of R1 and R2 represents a cyano group and the other represents a hydrogen atom; Ar1 represents a group selected from among the groups represented by formulas (2) to (4): and Ar2 represents an aromatic hydrocarbon group having a condensed ring which may be substituted by a halogen atom, or a group selected from among the groups represented by the following formulas (5) to (15): or a salt thereof.

Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flaviviridae viral infections.

Abstract: A process for the preparation of N-monosubstituted ?-aminoalcohol sulfonates of formula (Ia), (Ib): wherein R1 is C6-20-aryl or C4-12-heteroaryl, each optionally being substituted with one or more halogen atoms and/or one or more C1-4-alkyl or C1-4-alkoxy groups, R2 is C1-4-alkyl or C6-20-aryl, each aryl optionally being substituted with one or more halogen atoms and/or one or more C1-4-alkyl or C1-4-alkoxy groups and wherein R3 is selected from the group consisting of C1-18-alkyl, C6-20-cycloalkyl, C6-20-aryl and C7-20-aralkyl residues. The process has the steps of (a) reacting a methyl ketone, a primary amine, formaldehyde and a sulfonic acid, at a pressure above 1.5 bar, optionally in a organic solvent, the organic solvent optionally containing water, to afford N-monosubstituted ?-aminoketone sulfonates of formula (II): wherein R1, R2 and R3 are as defined above, and (b) asymmetrically hydrogenating.

Abstract: The compounds of formula I in which R1, R2, R3, R4 and R5 have the meanings as given in the description are novel effective antiinflammatory compounds.

Abstract: Protein tyrosine phosphatases (PTPases) such as PTP1B can play a role in regulating a wide variety of cellular responses such as insulin signaling. Substituted thiophene compounds such as, for example, 2-carboxyl, 3-carboxymethoxy, 5-aryl substituted thiophenes, can inhibit PTP1B and thereby induce greater insulin sensitivity. Accordingly, PTP1B inhibition can provide an alternate treatment for PTPase-mediated disorders such as diabetes.

Abstract: Disclosed is a method for commercially producing 2-alkenyl-3-aminothiophene derivatives, which are useful as intermediates for agricultural chemicals, at low cost. Specifically disclosed is a method for introducing alkenyl groups into the 2-position of 3-aminothiophene derivatives by reacting 3-aminothiophene derivatives represented by the general formula (2) below or salts thereof with a ketone represented by the general formula (1) below without using a protecting group.

Abstract: A photoacid generator has formula (1). A chemically amplified resist composition comprising the photoacid generator has advantages including a high resolution, focus latitude, long-term PED dimensional stability, and a satisfactory pattern profile shape. When the photoacid generator is combined with a resin having acid labile groups other than those of the acetal type, resolution and top loss are improved. The composition is suited for deep UV lithography.

Abstract: A photoacid generator has formula (1) wherein R is H, F, Cl, nitro, alkyl or alkoxy, n is 0 or 1, m is 1 or 2, r is an integer of 0-4, and r? is an integer of 0-5. A chemically amplified resist composition comprising the photoacid generator has advantages including a high resolution, focus latitude, long-term PED dimensional stability, and a satisfactory pattern profile shape. When the photoacid generator is combined with a resin having acid labile groups other than those of the acetal type, resolution and top loss are improved. The composition is suited for deep UV lithography.

Abstract: Novel amine compounds that can be utilized as hole transport materials, hole injection materials or the like of organic electroluminescence devices, electrophotographic receptors or the like, and their production processes are provided. The novel amine compound is represented by the following general formula (1). In the formula, R1 and R2 each independently represents hydrogen atom, a linear, branched or cyclic alkyl group or alkoxy group, an aryl group, an aryloxy group or a halogen atom; Ar1 and Ar2 each independently represents a substituted or unsubstituted aryl group or heteroaryl group, and may form a nitrogen-containing heterocyclic ring together with the nitrogen atom bonded thereto; and Ar3 each independently represents a substituted or unsubstituted phenyl group, naphthyl group, biphenylyl group, terphenylyl group, anthryl group, fluorenyl group or pyridyl group (except for amino-substituted groups); and M represents a single bond, an arylene group or a heteroarylene group.

Abstract: An organophotoreceptor that includes: (a) a charge transport material having the formula wherein A is selected from heterocyclic groups, naphthyl group, alkylsulfonylphenyl, stilbenyl or the group X, wherein X is represented by the formula B is selected from hydrogen, alkyl group, and an aryl group, with the proviso that when A is naphthyl, B is naphthyl; or where R1 is selected from the group consisting of N-pyrrolyl, N-pyrazolyl, N-tetrazolyl, N-indolyl, N-carbazolyl, N-triazolyl, N-imidazolyl, N-benzimidazolyl, N-indazolyl, and N-benzotriazolyl group, and R3 is a 9-fluorenone group. (b) a charge generating compound; and (c) an electrically conductive substrate.

Abstract: o-Aminophenol derivatives of the general formula (I) or physiologically compatible, water-soluble salts thereof, in which X is oxygen, sulfur or N—R4; R1, R2, R3 may be identical or different and, independently of one another, are hydrogen, a halogen atom, a cyano group, a C1-C4-alkoxy group, a C1-C6-alkyl group, a C1-C4-alkyl thioether group, a mercapto group, a nitro group, a trifluoromethane group, a —C(O)H group, a —C(O)CH3 group, a —C(O)CF3 group, an —Si(CH3)3 group, a C1-C4-hydroxyalkyl group or an aminomethyl group; R4 is hydrogen, a C1-C6-alkyl group, a C1-C4-hydroxy-alkyl group, a phenyl group or an acetyl group; and colorants containing said compounds for keratin fibers.

Abstract: This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cancer.

Abstract: Oncoproteins such as Ras and RhoB are known to induce cell division in an unrestrained manner when such proteins are localized at the inner surface of a cancer cell membrane. The localization is effected by the prenylation reaction, whereby a hydrophobic group (e.g. a farnesyl group) is attached to the protein in the presence of an enzyme (e.g. farnesyl protein transferase). Deactivation of the prenylation enzyme through covalent modification can therefore ultimately result in the mitigation and/or cessation of cancer cell growth. Various prenylation inhibitors having the necessary structural groups to bond covalently, or essentially irreversibly, to the prenylation enzyme include carbonyl or thiocarbonyl compounds (or masked versions of these compounds) and alpha oxo-epoxides bonded to a hydrophobic, substrate-mimicking group. The carbonyl or thiocarbonyl compounds also contain a nucleofugal atom or group to enhance the tendency to form covalent bonds.

Abstract: This invention relates to novel whitening agents for cellulosic substrates. The whitening agents are comprised of at least two components: at least one chromophore component and at least one polymeric component. Suitable chromophore components generally fluoresce blue, red, violet, or purple color when exposed to ultraviolet light, or they may absorb light to reflect these same shades. The whitening agents are further characterized by having a dispersion component value of the Hansen Solubility Parameter of less than or equal to about 17 MPa0.5. This invention also relates to laundry care compositions including but not limited to liquid and/or powder laundry detergent formulations and rinse added fabric softening (RAFS) compositions that comprise such whitening agents.

Abstract: This invention relates to novel whitening agents for cellulosic substrates. The whitening agents are comprised of at least two components: at least one chromophore component and at least one polymeric component. Suitable chromophore components generally fluoresce blue, red, violet, or purple color when exposed to ultraviolet light, or they may absorb light to reflect these same shades. The whitening agents are further characterized by having a dispersion component value of the Hansen Solubility Parameter of less than or equal to about 17 MPa0.5. This invention also relates to laundry care compositions including but not limited to liquid and/or powder laundry detergent formulations and rinse added fabric softening (RAFS) compositions that comprise such whitening agents.

Abstract: Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein A and J are defined herein, are useful in the treatment of tumors and cancers such as mastocytosis/mast cell leukemia, gastrointestinal stromal tumors (GIST), germ cell tumors, small cell lung carcinoma (SCLC), sinonasal natural killer/T-cell lymphoma, testicular cancer (seminoma), thyroid carcinoma, malignant melanoma, ovarian carcinoma, adenoid cystic carcinoma, acute myelogenous leukemia (AML), breast carcinoma, pediatric T-cell acute lymphoblastic leukemia, neuroblastoma, mast cell leukemia, angiosarcoma, anaplastic large cell lymphoma, endometrial carcinoma, and prostate carcinoma.

Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.

Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.

Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13 SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.

Abstract: A photoacid generator has formula (1). A chemically amplified resist composition comprising the photoacid generator has advantages including a high resolution, focus latitude, long-term PED dimensional stability, and a satisfactory pattern profile shape. When the photoacid generator is combined with a resin having acid labile groups other than those of the acetal type, resolution and top loss are improved. The composition is suited for deep UV lithography.

Abstract: The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.

Abstract: Thiophene derivatives are described herein. The described invention also includes methods of making such thiophene derivatives as well as methods of using the same in the treatment of diseases.