http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2360292-T3

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filingDate 2004-12-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2011-06-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_352723694c5aef32b7e825abe396ef85
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a358461fbf7e031834b09df0c5ff8d86
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publicationDate 2011-06-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber ES-2360292-T3
titleOfInvention 1,2,3-TRIAZOL AMIDA DERIVATIVES AS INHIBITORS OF CYTOKIN PRODUCTION.
abstract A compound of formula (I) ** Formula ** in which: Ar1 is chosen from the following rings (i), (ii) or (iii): ** Formula ** in which one of A or B is nitrogen and the other is carbon, R1 is covalently bound to any of A or B, and when the nitrogen is N-R1 the double bond between A and B is not present; R1 is hydrogen, NO2, -N (Rc) 2, J-C (O) - N (Rc) - or J-S (O) m-N (Rc) -; or R1 is selected from C1-6 alkyl, C3-7 cycloalkyl, C1-5 alkoxy or C3-7 cycloalkoxy, C1-5 alkylthiol or C3-7 cycloalkylthiol, C1-5 acyl, C1-5 alkoxycarbonyl, C1-5 acyloxy, C1-5 acylamino, C2-5 alkenyl, C2-5 alkynyl, heterocycle, heteroaryl, ornitrile, each of the above whenever possible is optionally, partially or completely halogenated or is optionally further substituted with alkylsulfonylamino, alkoxy, amino, alkylamino, dialkylamino, hydroxyl, oxo, nitro, and nitrile; ** Formula ** R2 is chosen from hydrogen, halogen, C1-5 alkyl, C1-5 alkoxy, C1-5 alkyl C1-5 alkoxy, hydroxy, hydroxy C1-5 alkyl, oxo, C1-5 S alkyl (O) m -, or amino optionally mono- or di-substituted by C1-5 alkyl, aryl or C1-5 arylalkyl; wherein R1 'is selected from H, C1-5 alkyl (S) m-, C1-6 alkyl, C3-7 cycloalkyl, C1-5 alkoxy or C3-7 cycloalkoxy, C1-5 alkylthiol, C3-7 cycloalkylthiol , C1-5 acyl, C1-5 alkoxycarbonyl, C1-5 acyloxy, C2-5 alkenyl, C25 alkynyl, heterocycle, C1-6 heterocycloalkyl, heteroaryl, C1-6 heteroarylalkyl, or nitrile, each of the above whenever possible is optionally, partially or completely halogenated or is optionally further substituted with alkylsulfonylamino, alkoxy, amino, alkylamino, dialkylamino, hydroxy, oxo, nitro, and nitrile; R2 'is chosen from nitrile, C1-5 alkyl S (O) m-, JOC (O) -O-, NH2-C (O) - (CH2) n-, hydrogen, halogen, C1-5 alkyl, C1 alkoxy -5, C1-5 alkyl C1-5 alkoxy, hydroxy, C1-5 hydroxyalkyl or optionally mono- or di40 amino substituted by C1-5 alkyl, aryl or C1-5 arylalkyl; wherein c is a benzo ring fused to ring d which is a 5- to 7-membered heterocyclic ring; ** Formula ** Each Rx is chosen from C1-6 alkyl or C3-7 cycloalkyl each being optionally substituted by C1-3 alkyl and optionally, partially or completely halogenated, C1-4 acyl, aroyl, C1-4 alkoxy, which it can be optionally, partially or completely halogenated, halogen, C1-6 alkoxycarbonyl, carbocyclosulfonyl and -SO2-CF3; m and n are 0, 1 or 2 and in which Rc is chosen from hydrogen or C1-5 alkyl; J is chosen from C1-10 alkyl and carbocycle each optionally substituted by Rb; R3, R4, R6, R7 and R8 are each independently selected from hydrogen, halogen, C1-5 alkyl, C1-5 alkoxy, C1-5 alkyl C1-5 alkoxy, hydroxy, hydroxy C1-5 alkyl or optionally mono- or amino di-substituted by C1-5 alkyl, aryl or C1-5 arylalkyl; R5 is a bond, -O-, -S-, -N <, -NH-, C (O), a linear chain chosen from -NH (CR7R8) r-, - (CR7R8) r-, O (CR7R8) r-, -C (C) -C (CR7R8) r-, -S (CR7R8) r-, C (O) (CR7R8) r- and -C (O) NH (CR7R8) r-, in which r it is from 1 to 5 and each of the above R5 is further substituted by Ra, or R5 is a ring system chosen from aryl, heteroaryl or heterocyclyl each optionally substituted by Ra; Ra and Rb are each independently selected from hydrogen, C1-5 alkyl, C1-5 hydroxyalkyl, C2-5 alkenyl, C2-5 alkynyl, carbocycle, heterocycle, heteroaryl, C1-5 alkoxy, C1-5 thioalkyl, amino, alkylamino C15, C1-5 dialkylamino, C1-5 acyl, C1-5 alkoxycarbonyl, C1-5 acyloxy, C1-5 acylamino, each of the above is optionally, partially or completely halogenated, or Ra and Rb are chosen from C1- alkylsulfonylamino 5, hydroxy, oxo, halogen, nitro and nitrile, and X is O or S with the proviso that the carboxylate compounds of 1- [5- (5-tert-Butyl-2-methoxy-phenylcarbamoyl) -2-methyl-phenyl ] -1H-1,2,3-Triazol-4-methyl, 1- [5- (5-tert-Butyl-2-methoxy-phenylcarbamoyl) -2-methyl-phenyl] -1H-1,2 acid benzylamide , 1- [5- (5-tert-Butyl-2-methoxy-phenylcarbamoyl) -2-methyl-phenyl] -1H-3-triazol-4-carboxylic acid, 2-morpholin-4-yl-ethyl) -amide -1,2,3-triazol-4-carboxylic acid, and ((R) -1-phenyl-ethyl) -amide 1- [5- (5-tert-Butyl-2-methoxy-phenylcarbamoyl) -2-methyl- phenyl] -1H-1,2,3tri azol-4-carboxylic are not included; or pharmaceutically acceptable isomers or salts thereof, in which the isomer should be understood to include any of the compounds of formula (I) that contains one or more asymmetric carbon atoms and may appear as racemates and racemic mixtures, single enantiomers, mixtures of diastereomers and individual diastereomers.
priorityDate 2003-12-03-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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Total number of triples: 539.