Abstract: Biaryl substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof, and a process for making such compounds and salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.

Abstract: The present invention relates to a compound represented by Formula (I): wherein Ar1, Ar2, R1 and R2 each represent a substituent, a salt thereof, or a solvate of the compound or the salt, and to a medicine containing the same. According to the present invention, a potent platelet aggregation suppressant which does not inhibit COX-1 and COX-2 is provided.

Abstract: The present invention is a 1,3,8 substituted xanthine derivative of formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined in the specification. Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.

Abstract: A novel achiral biaryl-type compound and a circular dichroism(CD) color fixing agent are provided. Furthermore, a method for determining an absolute configuration of a chiral compound is carried out by introducing the above achiral biaryl-type compound into the chiral compound.

Abstract: A fungicidally active compound of the formula: a) wherein Q is —NY—NH—, —N?N—, or X is oxygen, sulfur, sulfoxide, or sulfone; n is 0 or 1; Y is hydrogen, C1–C4 alkanoyl, C1–C4 haloalkanoyl, C1–C6 straight chain or branched alkoxycarbonyl, C1–C4 alkoxy(C1–C4)alkoxycarbonyl, C1–C4 alkyl, or C1–C4 haloalkyl; R1 is C1–C6 alkoxy, C3–C6 branched alkoxy, C3–C6 cycloalkoxy, phenoxy, benzyloxy, C2–C6 alkenyloxy, C2–C6 alkynyloxy, C1–C6 haloalkoxy, silyloxy, (C1–C6 alkoxy)-carbonylmethoxy, C1–C6 thioalkoxy, C1–C6 alkylamino, C1–C6 alkyl, C3–C6 branched alkyl, (C1–C6 alkoxy) C1–C6 alkoxy, or (C1–C6 alkoxy)carbonyl; R2 and R3 are each, independently, hydrogen, halogen, C1–C6 alkyl, C3–C6 branched alkyl, C1–C6 haloalkyl, C1–C6 alkoxy, C1–C6 haloalkoxy, cyano, or (C1–C6 alkoxy)carbonyl; R4 is C1–C6 alkyl; and Z1 and Z2 are each independently, carbon or nitrogen, with the proviso that when Z1 is carbon, X is oxygen, and R2 is hydrogen, then R3 cannot be hydrogen; b) wherein R5 is C1–C6 alkoxy; and R6 and

Abstract: A method of converting pure ?-anomer or ?/?-anomer mixtures of 1,2,3,5-tetra-O-acetyl-L-ribofuranose to methyl-1-(2,3,5-tri-O-acetyl-?-L-ribofuranosyl)-1,2,4-triazole-3-carboxylate an intermediate for levovirin, as well as, the novel pure ?-anomer, alpha 1,2,3,5-tetra-O-acetyl-L-ribofuiranose, are useful in manufacturing levovirin.

Abstract: New triterpenoid derivatives with various substituents at the C-17 position of 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid (CDDO) were synthesized. Among them, 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-onitrile (CNDDO), 1-(2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl) imidazole, 1-(2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl)-2-methylimidazole, 1-(2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl)-4-methylimidazole show extremely high inhibitory activity (IC50=0.01-1 pM level) against production of nitric oxide induced by interferon-? in mouse macrophages. These compounds can be used in the prevention or treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, rheumatoid arthritis, and other inflammatory diseases. All the new triterpenoid derivatives are more potent than previously known CDDO.

Abstract: The invention concerns a process for the preparation of N-aryl-aza-heterocycles of the general formula I by reaction of aza-heterocycles with activated aryl halides with use of caesium carbonate without addition of further catalysts at room temperature.

Abstract: This invention relates to compounds having the Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Het and R5-R8 are set in the specification. The invention also is directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

Abstract: Triazole derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

Abstract: Industrial and commercial processes for the preparation of 2-acyl-5-benzylfuran derivatives, 1,2,4-triazole-3-carboxylic acid ester derivatives or propenone derivatives having an anti-HIV activity; and useful crystals of the derivatives. A deblocking: (III-2), (IV-10), (VI-1), wherein R1, R2 and R4 are each independently hydrogen or the like; A is CR6 or N; R6 is hydrogen or the like; Q is a protecting group; and L is a leaving group.

Abstract: Chemokine receptor antagonists, in particular, bicyclic diamine compounds of Formula (I) that act as antagonists of chemokine CCR2 and CCR3 receptors including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leucocyte accumulation are described herein.

Abstract: The invention concerns novel azole or triazole derivatives of formula (I), wherein: X, Ar1, Ar3, A, R1, R5, R6, R7 and B are such as defined in the description, their preparation method and their use as antifungal medicines.

Abstract: A novel achiral biaryl-type compound and a circular dichroism(CD) color fixing agent are provided. Furthermore, a method for determining an absolute configuration of a chiral compound is carried out by introducing the above achiral biaryl-type compound into the chiral compound.

Abstract: This invention relates to the preparation of N,N′-carbonyldiazoles in a particularly advantageous manner by reacting corresponding azolide salts with phosgene in an aromatic compound or an ether as solvent. The azolide salts are preferably prepared by a novel process from an azole that is reacted with a compound of the formula M′R7 or MgR8Z′ in the presence of a solvent.

Abstract: This invention provides compounds of Formula (1), their N-oxides and agriculturally suitable salts wherein A, B, J, R1, R2, R3 and R4 and n are as defined in the disclosure. Also disclosed are methods for controlling arthropods comprising contacting the arthropods or their environment with an arthropodicidally effective amount of a compound of Formula (1) and compositions containing the compounds of Formula (1).

Abstract: The invention provides compounds of the formula I 1

Abstract: A novel achiral biaryl-type compound and a circular dichroism (CD) color fixing agent are provided. Furthermore, a method for determining an absolute configuration of a chiral compound is carried out by introducing the above achiral biaryl-type compound into the chiral compound.

Abstract: This invention relates to compounds having the Formula I: 1

Abstract: New triterpenoid derivatives with various substituents at the C-17 position of 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid (CDDO) were synthesized. Among them, 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-onitrile (CNDDO), 1-(2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl) imidazole, 1-(2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl)-2-methylimidazole, 1-(2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl)-4-methylimidazole show extremely high inhibitory activity (IC50=0.01-1 pM level) against production of nitric oxide induced by interferon-&ggr; in mouse macrophages. These compounds can be used in the prevention or treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, rheumatoid arthritis, and other inflammatory diseases. All the new triterpenoid derivatives are more potent than previously known CDDO.

Abstract: A compound of the formula (I): 1

Abstract: Diarylanines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C1-6 alkoxy, or NR6OR7; X is OR12, NR13R12, or NR14; inhibitors of MEK and are useful in the treatment of a variety of proliferative disease states, such as conditions related to the hyperactivity of MEK, as well as diseases modulated by the MEK cascade.

Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.

Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.

Abstract: A sulfamoyl compound of the general formulae (1): wherein R1 and R2 are each independently C1-4 alkyl, or R1 and R2 together are C4-6 alkylene or C4-6 alkyleneoxy, Y is H, halogen, C1-8 alkyl, C1-8 alkoxy, C1-8 alkylthio, C1-8 haloalkyl, C1-8 haloalkoxy or C1-8 haloalkylthio, A is a predetermined heterocyclic group, B is a predetermined heterocyclic group which is identical with or different from A, W is a chemical bond or O, V is O or S, D, E, F and G are each independently N, CR7, CR8, CR9 or CR10, and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are each independently predetermined group such as H, or an unsubstituted or substituted aliphatic, aromatic or heterocyclic group. The sulfamoyl compound is useful as an agricultural and horticultural fungicide.

Abstract: The present application describes nitrogen containing heteroaromatics with ortho-substituted P1's and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D is substituted ortho to G on E and may be CH2NH2, which are useful as inhibitors of factor Xa.

Abstract: The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment of a variety of immunomediated inflammatory disorders. More particularly, these compounds are potent and selective inhibitors of tryptase and are therefore effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis.

Abstract: This invention relates to the preparation of N,N′-carbonyldiazoles in a particularly advantageous manner by reacting corresponding azolide salts with phosgene in an aromatic compound or an ether as solvent. The azolide salts are preferably prepared by a novel process from an azole that is reacted with a compound of the formula M′R7 or MgR8Z′ in the presence of a solvent.

Abstract: Compounds of formula (I) are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.

Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.

Abstract: 1. A 1-naphthol compound represented by formula (I) below: wherein A represents the moiety of a compound having an acidic proton the pKa of a corresponding protonated form (AH) of which is 0 to 14, R1 represents an aliphatic group, aryl group, or heterocyclic group, R2 represents a substituent, n represents an integer of 0 to 5, X represents a hydrogen atom, halogen atom, R11—, R11O—, R11S—, R11OCOO—, R12COO—, R12(R13)NCOO—, R12CON(R13)—, —NO, —NO2, or —N═N—R11, wherein R11 represents an aliphatic group, aryl group, or heterocyclic group, and each of R12 and R13 independently represents a hydrogen atom, aliphatic group, aryl group, or heterocyclic group, and Y represents an oxygen atom or sulfur atom.

Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.

Abstract: A sulfamoyl compound of the general formulae (1): 1

Abstract: A method for treating a patient having chronic hepatitis C infection to eradicate detectable HCV-RNA involving a combination therapy using a therapeutically effective amount of ribavirin derivative of formula I and a therapeutically effective amount of interferon-alpha for a time period of from 20 up to 80 weeks.

Abstract: The present invention provides a solventless, continuous process, which includes:

Abstract: Antiviral compounds have the formula wherein m is zero, 1, 2 or 3; n is from 1 to 8, preferably 1, 2 or 3; most preferably 1 or 2; R is independently selected from the group consisting of  provided that all R may not be R1 is independently selected from the group consisting of hydroxyl and hydrogen; R2 is independently selected from the group consisting of oxygen and sulfur; or water soluble salts thereof.

Abstract: Substituted carbamoyltriazoles of the formula I as defined in the specification and the agriculturally useful salts thereof, processes for their preparation and their use as herbicides.