http://rdf.ncbi.nlm.nih.gov/pubchem/patent/RU-2067976-C1
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_0c8bffd30b513a7c8ac7d736fa3ef27f http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_0d78cd2835221849f6a74e6349185819 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D309-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D233-56 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D309-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D231-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D249-08 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D309-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D309-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-40 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-351 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D521-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-35 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P37-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P29-00 |
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 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f4dace9ec2f529f408b794af85b10259 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bb8b1429c9877a8aa319a49d123cd613 |
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> |
type | http://data.epo.org/linked-data/def/patent/Publication |
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