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422 results about "1,2,4-Triazole" patented technology

1,2,4-Triazole (as ligand in coordination compounds, Htrz abbreviation is sometimes used) is one of a pair of isomeric chemical compounds with molecular formula C₂H₃N₃, called triazoles, which have a five-membered ring of two carbon atoms and three nitrogen atoms. 1,2,4-Triazole is a basic aromatic heterocycle. 1,2,4-Triazole derivatives find use in a wide variety of applications, most notably as antifungals such as fluconazole and itraconazole. 1,2,4-Triazoles can be prepared using the Einhorn–Brunner reaction or the Pellizzari reaction.

Nicotinamide acids, amides, and their mimetics active as inhibitors of PDE4 isozymes

InactiveUS20020111495A1Organic chemistryDiseasePyridazine
Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: wherein j is 0 or 1, k is 0 or 1, m is 0, 1, or 2; n is 1 or 2; A is selected from the partial Formulas: where q is 1, 2, or 3, W3 is -O-; -N(R9)-; or -OC(=O)-; R7 is selected from -H; -(C1-C6) alkyl, -(C2-C6) alkenyl, or -(C2-C6) alkynyl substituted by 0 to 3 substituents R10; -(CH2)u-(C3-C7) cycloalkyl where u is 0, 1 or 2, substituted by 0 to 3 R10; and phenyl or benzyl substituted by 0 to 3 R14; R8 is tetrazol-5-yl; 1,2,4-triazol-3-yl; 1,2,4-triazol-3-on-5-yl; 1,2,3-triazol-5-yl; imidazol-2-yl; imidazol-4-yl; imidazolidin-2-on-4-yl; 1,3,4-oxadiazolyl; 1,3,4-oxadiazol-2-on-5-yl; 1,2,4-oxadiazol-3-yl; 1,2,4-oxadiazol-5-on-3-yl; 1,2,4-oxadiazol-5-yl; 1,2,4-oxadiazol-3-on-5-yl; 1,2,5-thiadiazolyl; 1,3,4-thiadiazolyl; morpholinyl; parathiazinyl; oxazolyl; isoxazolyl; thiazolyl; isothiazolyl; pyrrolyl; pyrazolyl; succinimidyl; glutarimidyl; pyrrolidonyl; 2-piperidonyl; 2-pyridonyl; 4-pyridonyl; pyridazin-3-onyl; pyridyl; pyrimidinyl; pyrazinyl; pyridazinyl; indolyl; indolinyl; isoindolinyl; benzo[b]furanyl; 2,3-dihydrobenzofuranyl; 1,3-dihydroisobenzofuranyl; 2H-1-benzopyranyl; 2-H-chromenyl; chromanyl; benzothienyl; 1H-indazolyl; benzimidazolyl; benzoxazolyl; benzisoxazolyl; benzothiazolyl; benzotriazolyl; benzotriazinyl; phthalazinyl; 1,8-naphthyridinyl; quinolinyl; isoquinolinyl; quinazolinyl; quinoxalinyl; pyrazolo[3,4-d]pyrimidinyl; pyrimido[4,5-d]pyrimidinyl; imidazo[1,2-a]pyridinyl; pyridopyridinyl; pteridinyl; or 1H-purinyl; or A is selected from phosphorous and sulfur acid groups; W is -O-; -S(=O)t-, where t is 0, 1, or 2; or -N(R3)-; Y is =C(R1a)-, or -[N<custom-character file="US20020111495A1-20020815-P00900.TIF" wi="20" he="20" id="custom-character-00001"/>(O)k] where k is 0 or 1; R4, R5 and R6 are (1) -H; provided that R5 and R6 are not both -H at the same time, -F; -Cl; -(C2-C4) alkynyl; -R16; -OR16; -S(=O)pR16; -C(=O)R16, -C(=O)OR16, -C(=O)OR<highlight><sup
Owner:PFIZER INC

4-alkyl-2-aryl amino-5-(1,2,4-triazol-1-yl)thiazole and preparation method and application thereof

The invention relates to 4-alkyl-2-aryl amino-5-(1,2,4-triazol-1-yl)thiazole shown as a chemical structural formula I and a salt thereof. The chemical structural formula I is shown in the specifications, wherein R is selected from H, alkyl with 1-2 carbon atoms, or straight chain alkyl or branch chain alkyl with 3-4 carbon atoms; and X1, X2, X3, X4 and X5 is selected from hydrogen, alkyl with 1-2 carbon atoms, hydroxyl, methoxyl, oxethyl, trifluoromethyl, fluorine, chlorine, bromine, nitro or amino. A preparation method of the 4-alkyl-2-aryl amino-5-(1,2,4-triazol-1-yl)thiazole comprises the following steps of: feeding 2-(1,2,4-triazol-1-yl)-2-bromoalkylketone and aryl thiourea in the molar ratio of 1:1, and carrying out a reflux reaction in ethanol; and after reacting, distilling under reduced pressure to remove a solvent, adding ethyl acetate for washing, filtering, drying to obtain 4-alkyl-2-aryl amino-5-(1,2,4-triazol-1-yl)thiazole hydrobromide, neutralizing the hydrobromide with ammonia water, extracting with ethyl acetate, drying, and distilling under reduced pressure to obtain 4-alkyl-2-aryl amino-5-(1,2,4-triazol-1-yl)thiazole. The 4-alkyl-2-aryl amino-5-(1,2,4-triazol-1-yl)thiazole has high antitumor activity, and can be applied to preparation of an anticancer medicament.
Owner:HUNAN UNIV

Biospecific binding reactants labeled with new luminescent lanthanide chelates and their use

This invention relates to a luminescent lanthanide chelate comprising a lanthanide ion and a chelating ligand of formula (I)
wherein
R1 is selected from the group consisting H, —COOH, —COO, —CH2COOH and —CH2COO; G1 is a group consisting of one or two moieties each moiety being selected from the group consisting of ethynediyl, ethenylene, phenylene, biphenylene, naphthylene, pyridylene, pyrazinylene, pyrimidinylene, pyridazinylene, furylene, thienylene, pyrrolylene, imidazolylene, pyrazolylene, thiazolylene, isothiazolylene, oxazolylene, isoxazolylene, fyrazanylene, 1,2,4-triazol-3,5-ylene and oxadiazolylene; G2 for coupling to a biospecific binding reactant is selected from the group consisting of amino, aminooxy, carbonyl, aldehyde or mercapto groups and activated forms made of them; Z is selected from the group consisting of carboxyalkyl amine, ether, thioether, carbonyl and unsubstituted or substitute methyl (—CR2—) wherein group R2 is selected from the group consisting of H, methyl, ethyl and carboxylalkyl; and the lanthanide ion is europium(III), terbium(III), dysprosiym(III) or samarium(III). This invention further relates to a detectable molecule comprising the lanthanide chelate and the use of the molecule in a method of carrying out a biospecific binding assay.
Owner:INNOTRAC DIAGNOSTISC
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