Abstract: A chiral catalyst comprising a 3,4-disubstituted pyridine, or a salt, N functionalized derivative, dimer or oligomer thereof, wherein the 3-substituent is substantially hindered from rotation about the bond (sp2-sp2 biaryl axis) linking it to pyridine and the 4-substituent is an aliphatic or aromatic amine linked by a single bond to the pyridine, the pyridine nitrogen being functionalized or unfunctionalized, preferably comprising a compound of formula I 1

Abstract: Thiazole esters are suitable for detecting the presence of leukocytes in urine. Such thiazole esters are suitable for use in compositions, diagnostic devices, and methods for detecting the presence of leukocytes. In one embodiment, a thiazole ester is of the formula: or a salt or solvated salt thereof, in which A is an N-blocked amino acid residue or an N-blocked peptide chain, preferably N-blocked alanine or N-blocked polyalanine; and R1 is unsubstituted or substituted heteroaryl; alkenyl substituted with unsubstituted or substituted aryl; or alkenyl substituted with unsubstituted or substituted heteroaryl. For example, R1 may be thienyl, pyridyl, furyl, styryl, pyrrolyl, or indolyl. In still another embodiment, the thiazole ester includes unsubstituted or substituted fused hydrocarbyl rings as a substituent. In one embodiment, fused hydrocarbyl rings include naphthyl. In another embodiment, fused hydrocarbyl rings include anthryl.

Abstract: A process for the preparation of a compound of Formula (IA) or a pharmaceutically acceptable salt thereof: wherein R1 is an aryl, pyridyl, thiazolyl, phenoxymethyl or pyrimidyl group, optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C1-6alkoxy, C1-6alkyl, hydroxymethyl, tifluoromethyl, —NR6R6, and —NHSO2R6, where each R6 is independently hydrogen or C1-4alkyl; R2 is hydrogen or C1-6alkyl; R3 is CO2R7 where R7 is hydrogen or C1-6alkyl; R4 and R5 are independently hydrogen, C1-6alkyl or —CO2C1-6alkyl; and Y is N or CH comprising the step of preparing a diamide of Formula (II) or a pharmaceutically acceptable salt thereof: wherein R1 is an aryl, pyridyl, thiazolyl, phenoxymethyl or pyrimidyl group, optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C1-6alkoxy, C1-6alkyl, hydroxymethyl, trifluoromethyl, —NR6R6, and —NHSO2R6, where each R6 is independently hydrogen or C1-4

Abstract: A class of N-arylheteroarylalkyl imidazol-2-one compounds is described for use in treatment of arteriosclerosis.

Abstract: New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.

Abstract: The present invention relates to novel N-cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.

Abstract: Novel ethanes substituted with i) a phenyl, ii) a thiazole, and iii) a pyridyl moiety are PDE4 inhibitors.

Abstract: A heterocyclic compound has the following formula (I) wherein Y represents a substituted or unsubstituted ethylene group or a trimethylene group, W represents the group —SO2R1, X represents an oxygen atom or sulfur atom or the group —NR2 or —CHR3, R represents a hydrogen atom or a methyl group and Z represents a pyridyl group.

Abstract: A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a):

Abstract: Novel fluorescent derivitization reagents are described that are suitable for coupling to biomolecules that contain aldehyde or ketone functional groups. The method of treating a sample with the derivativization reagents is described. The reagents are particularly useful for labeling glycoproteins or glycopeptides, nucleic acids, and lipopolysaccharides in electrophoresis gels.

Abstract: 1

Abstract: A pharmaceutical composition for antagonizing adenosine at adenosine A3 receptors which comprises a 1,3-azole compound substituted on the 4- or 5-position, or both, by a pyridyl which may be substituted is provided and can be used as a prophylactic and therapeutic agent for asthma, allergosis, inflammation, and so on.

Abstract: Thiazole esters are suitable for detecting the presence of leukocytes in urine. Such thiazole esters are suitable for use in compositions, diagnostic devices, and methods for detecting the presence of leukocytes.

Abstract: Novel 2-thiothiazolidin-5-one compounds useful as intermediates for fungicidal 2-imidazolin-5-ones are disclosed.

Abstract: 5-Arylidene-4-oxo-2-thioxo-3-thiazolidinecarboxylic acids of formula I 1

Abstract: There is provided heterocyclic compounds of the following formula (I): 1

Abstract: Thiazole esters are suitable for detecting the presence of leukocytes in urine. Such thiazole esters are suitable for use in compositions, diagnostic devices, and methods for detecting the presence of leukocytes. In one embodiment, a thiazole ester is of the formula: or a salt or solvated salt thereof, in which A is an N-blocked amino acid residue or an N-blocked peptide chain, preferably N-blocked alanine or N-blocked polyalanine; and R1 is unsubstituted or substituted heteroaryl; alkenyl substituted with unsubstituted or substituted aryl; or alkenyl substituted with unsubstituted or substituted heteroaryl. For example, R1 may be thienyl, pyridyl, furyl, styryl, pyrrolyl, or indolyl. In still another embodiment, the thiazole ester includes unsubstituted or substituted fused hydrocarbyl rings as a substituent. In one embodiment, fused hydrocarbyl rings include naphthyl. In another embodiment, fused hydrocarbyl rings include anthryl.

Abstract: Para-aryl or heteroaryl substituted phenyl amides which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.

Abstract: The present invention provides an agent for inhibiting cytokine production or cell adhesion, comprising at least one compound selected from the group consisting of thiazole derivatives represented by the following general formula: [wherein R1 is a phenyl group which may have a lower alkoxy group(s) as a substituent(s) on the phenyl ring, and R2 is a group represented by the following general formula: [wherein R3's, which may be the same or different, are each a carboxyl group, a lower alkoxy group or the like) or the like] and salts thereof.

Abstract: 1,3-Oxazoline and 1,3-thiazoline derivatives, their preparation, and their use as pesticides 1,3-Oxazoline and 1,3-thiazoline derivatives of the formula (I) where the symbols have the following meanings: A is phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyrazolyl or thienyl, E is a single bond, (C1-C4)alkylene, —O—CH2— or —CH2—O—; G is a radical selected from the group consisting of Z is oxygen or sulfur. Compounds of the formula (I) have, in particular, a very good acaricidal and insecticidal action with regard to the spectrum of action and the potency.

Abstract: The present invention relates to 4-haloalkyl-3-heterocyclylpyridines and 4-haloalkyl-5-heterocyclylpyrimidines of the formula (I), to processes for their preparation, to compositions comprising them, and to the use of these compounds for controlling animal pests, in particular insects, spider mites, ectoparasites and helminths. In the formula (I), Q is a 5-membered heterocyclic group which is optionally substituted by halogen or organic radicals, Y is halo-C1-C8-alkyl, X is CH or N and m is 0 or 1.

Abstract: Disclosed is a novel class of thiazole, thiadiazole, and oxadiazole compounds which are substituted at their nuclear carbons by aromatic moieties. These compounds exhibit antifungal activity against a variety of fungi including strains which have proven to be resistant to treatment with known antifungal agents such as Fluconazole.

Abstract: A compound selected from the group consisting of a compound of the formula wherein the substituents are defined as in the specification having antagonist properties to histamine H3-receptors.