http://rdf.ncbi.nlm.nih.gov/pubchem/patent/RU-2067976-C1

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filingDate 1991-11-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 1996-10-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d399812ddcddb9742c960cd49f3e6646
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publicationDate 1996-10-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber RU-2067976-C1
titleOfInvention Aryl derivatives or their pharmaceutically acceptable salts and methods of their synthesis
abstract FIELD: organic chemistry. SUBSTANCE: product: derivatives of aryl of the formula (I) where Ar 1 - phenyl or naphthyl that can be substituted if necessary with one or two substituents taken from halogen atom or hydroxy-group, CN, trifluoromethyl, C 1-4 -alkyl, C 1-4 -alkylamino-, di-((C 1-4 -alkyl)-amino-group, amino-(C 1-4 )-alkyl, carboxy-(C 1-4 )-alkoxy-, (C 1-4 )-alkoxycarbonyl-(C 1-4 )-alkoxy- and di-((C 1-4 )-alkyl)-amino-(C 2-4 )-alkoxy-group; X 1 means hydroxy - or thio-group, sulfonyl, difluoromethylene, imino-group or (C 1-4 )-alkylene where (C 1-4 )-alkylene group can be substituted if necessary with one or two substituents taken from hydroxy-group, (C 1-4 )-alkyl, (C 1-4 )-alkoxy-group and phenyl; or X 1 means the group of the formula -O-CH 2 -; or where A 1 means 5- or 6-membered monocyclic heterocyclic fragment containing one or two nitrogen heteroatom or their hydrogenated derivative. Heterocyclic fragment can be substituted if necessary with one oxo-substituent and X 1 is linear bond to Ar 2 or X 1 is carbonyl or C 1-4 -alkylene; Ar 2 and Ar 3 that can be similar or different and each is phenylene that if necessary can be substituted with halogen atom; X 2 means hydroxy, thio, sulfonyl-group; R 1 means (C 1-4 )-alkyl; R 2 and R 3 together form the group of the formula -A 1 -X 3 -A 2 - that together with carbon atom to which A 1 and A 2 were bound form ring with 6 atoms where A 1 and A 2 can be similar or different and every is C 1 -C 3 -alkylene and X 3 is hydroxy-group, and ring can be substituted with one (C 1-4 )-alkyl; pharmaceutically acceptable salts and methods of their synthesis. Method 1: reagent 1: compound of the formula X 3 . Reagent 2: compound of the formula (II) (Ar 1 -X 1 -Ar 2 -X 2 -H. Reagent 1: compound of the formula (III) . Method 2: . Reagent 2: compound of the formula: Ar 1 -X 1 -A 2 -Z. Method 3. Reagent 1: compound of the formula (IV) . Reagent 2: R 1 - Z where R 1 ,R 2 ,R 3 ,X 1 ,X 2 ,Ar 1 ,Ar 2 and Ar 3 have value indicated above. Compounds of the formula (I) decrease leukotriene B 4 by 50% ((IC 50 )). All tested samples show activity at indices IC 50 at the range of concentration from 0.03 to 0.5 mcmole. Synthesized compounds were used for treatment different inflammatory and/or allergic diseases. EFFECT: improved methods of synthesis. 5 tbl
priorityDate 1990-11-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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