- 4-N-BENZAZOLYLAMINO DERIVATIVES OF 3-Y-3-BUTEN-2-ONE
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Ethoxymethylene derivatives of 2,4-pentanedione (Ia), 3-oxobutanenitrile (Ib), methyl (Ic) or ethyl (Id) 3-oxobutanoate give with 4- or 5-aminobenzimidazole or benzotriazole, respectively, under mild conditions products of nucleophilic substitution II-V.Structure of these compounds was discussed on the basis of their spectral measurements -IR, UV, 1H, 13C NMR and mass spectra.
- Milata, Viktor,Ilavsky, Dusan,Goljer, Igor,Lesko,Jan
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- Synthesis of N-aryl and N-heteroaryl hydroxylamines via partial reduction of nitroarenes with soluble nanoparticle catalysts
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Polystyrene-supported ruthenium nanoparticles enable the selective hydrazine-mediated reduction of nitroarenes to hydroxylamine products in high yield and selectivity. Key to obtaining the hydroxylamine product in good yield was the use of organic solvents capable of solubilizing the polystyrene-supported nanoparticle catalyst. N-aryl and N-heteroaryl hydroxylamines are generated under exceptionally mild conditions and in the presence of a various easily reduced functional groups.
- Tyler, Jefferson H.,Nazari, S. Hadi,Patterson, Robert H.,Udumula, Venkatareddy,Smith, Stacey J.,Michaelis, David J.
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supporting information
p. 82 - 86
(2016/12/23)
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- JNK MODULATORS
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Compounds of formula I modulate JNK: wherein X1 and X2 are each simultaneously N or CH;X3 is CH—R2 or N—SO2R, where R is lower alkyl;R1 is aryl or heteroaryl, substituted with 0-3 lower alkyl radicals;R2 is where R3 is H, lower acyl, or an amino acid, or a pharmaceutically acceptable salt thereof.
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Page/Page column 14
(2010/07/04)
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- 3, 4-DI-SUBSTITUTED CYCLOBUTENE- 1, 2 -DIONES AS CXCR2 RECEPTOR ANTAGONISTS
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The present invention relates to compounds of formula (I) wherein R1, R2, Ar, p, R4 and R5 are as defined herein, which are useful for creating diseases which respond to CXCR2 receptor mediators. Pharmaceutical
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Page/Page column 47
(2010/06/20)
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- THIADIAZOLES AS CXC- AND CC- CHEMOKINE RECEPTOR LIGANDS
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Disclosed are novel compounds of Formula (IA) and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and ischemia reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of Formula (IA).
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Page/Page column 182
(2010/02/12)
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- ISOTHIAZOLE DIOXIDES AS CXC- AND CC- CHEMOKINE RECEPTOR LIGANDS
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Disclosed are novel compounds of the formula (IA): and the pharmaceutically acceptable salts and solvates thereof. D and E are different groups wherein one is N and the other is CR50. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.
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Page/Page column 185
(2010/02/13)
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- THIADIAZOLEDIOXIDES AND THIADIAZOLEOXIDES AS CXC- AND CC-CHEMOKINE RECEPTOR LIGANDS
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Disclosed are novel compounds of the formula (IA) and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, acute pain, acute and chronic inflammatory pain, and neuropathic pain using a compound of formula (IA).
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Page 211-212
(2008/06/13)
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- 3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
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There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.
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- 3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
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There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.
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Page 105-106
(2008/06/13)
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- IL-8 receptor antagonists
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This invention relates to novel benzo-2-triazole substituted compounds, pharmaceutical compositions, processes for their preparation, and use thereof in treating IL-8, GROα, GROβ, GROγ and NAP-2 mediated diseases.
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- Novel Dimroth Rearrangements of the Benzotriazole System: 4-Amino-1-(arylsulfonyl)benzotriazoles to 4-benzotriazoles
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A variety of mono- and diarylsulfonyl-substituted 4-aminobenzotriazoles were prepared.Thermal rearrangements of 4-amino-1-(arylsulfonyl)benzotriazoles to 4-benzotriazoles were observed and confirmed by separation of the rearrangement products.Their structures were characterized by spectral methods and by X-ray crystallography.The rearrangement rates were studied by variable-temperature NMR experiments.Crossover experiments support an intramolecular mechanism involving a heterolytic benzotriazole ring cleavage to form a diazo intermediate followed by recyclization to the 4-amino group.
- Katritzky, Alan R.,Ji, Fu-Bao,Fan, Wei-Qiang,Gallos, John K.,Greenhill, John V.,et al.
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p. 190 - 195
(2007/10/02)
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- 1,2,3-triazolo[4,5-h]quinolines. III. Preparation and antimicrobial evaluation of 4-ethyl-4,7-dihydro-1(2)-R-1(2)H triazolo[4,5-h]quinolin-7-one-6-carboxylic acids as anti-infectives of the urinary tract
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Some 4-ethyl-1(2)-R-1(2)H-4,7-dihydro-triazolo[4,5-h]-quinolin-7-one-6-carb oxylic acids were prepared as novel analogues of oxolinic acid, in order to discover the influence of the annelation position of the triazole ring on the antimicrobial activity th
- Sanna,Carta,Paglietti,Zanetti,Fadda
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p. 1001 - 1019
(2007/10/02)
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