http://rdf.ncbi.nlm.nih.gov/pubchem/patent/RU-2233326-C1
Outgoing Links
| Predicate | Object |
|---|---|
| classificationIPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D275-04 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C12N9-99 |
| filingDate | 2002-11-26-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2004-07-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c7b76d9b54a812c92a152c7c2f8f83f0 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6625c106b4edd072d9976b7ac169ffb7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_73fa2bf2e94c951226af943d8f4bcb0d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_61ae19164f7434a9b1c20c5ebb0db08a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_65ad42a39009ca8c657bbf6aa0f76bda |
| publicationDate | 2004-07-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | RU-2233326-C1 |
| titleOfInvention | Method for inhibition of caspase activity |
| abstract | FIELD: organic chemistry, biochemistry, biotechnology. n SUBSTANCE: invention relates to inhibition of activity of aspartate-specific cysteine protease (caspase) and can be used cellular biology, physiology and pharmacology for study and directed regulation of processes associated with induction, development and/or prophylaxis of the scheduled cellular death (apoptosis). Method for inhibition of activity of caspases is carried out by administration to medium nitrogen-containing compound, namely, derivative of 1,2-isothiazole-3-one of the general formula [1] indicated in the description wherein if R 1 means unsubstituted phenyl or phenyl comprising as a substituent chlorine atom, methyl, trifluoromethyl, ethoxycarbonyl or methoxy-group then R 2 means hydrogen atom, phenyl, ethoxycarbonyl, methoxy- or cyano-group, and R 3 means unsubstituted phenyl or phenyl comprising as a substituent chlorine atom, methyl, trifluoromethyl or methoxy-group; or R 2 and R 3 in common with adjacent carbon atoms form annelated benzene or pyridine cycle that can be substituted with halogen atom, nitro-, amino- or methoxy-group; or if R 1 means (C 1 -C 4 )-alkyl, benzyl, thiazolyl, pyridyl, benzothiazolyl or phenyl comprising as a substituent 4-F, 4-Br, 4-J, two (C 1 -C 4 )-alkyl groups, 4-aminocarbonyl, 4-[(dimethyl)amino]carbonyl, nitro-, amino-, 4-cyano-group, 2-3 methoxy-groups or methoxycarbonyl and methoxy-group simultaneously then R 2 -R 3 means -CH=CH-CH=N-; or if R 1 - R 4 means -NR 5 R wherein R means (C 1 -C 12 )-alkylene; R and R mean (C 1 -C 4 )-alkyl groups or NR 5 , and R 6 forms unsaturated nitrogen-containing heterocycle, such as pyrrolidine, piperidine, azepine then R 2 and R 3 in common with adjacent carbon atoms form annelated benzene cycle that can comprise 1-2 substituents taken among the group: halogen atom, (C 1 -C 4 )-alkyl, (C 1 -C 4 )-alkoxyl, nitro-, amino- or acylamino-group, or its biochemically acceptable salt. Invention provides effective reducing activity of caspases in the presence of other proteins (for the known isatin derivative the value IC 50 = 7.5 ± 3.5 mcM; in the presence of 10 mcM compounds used in the describing method, in particular, 2-phenyl- and 2-benzyl-6-nitro-1,2-benzoisothiazole-3-one activity of caspases is determined to be 4.84 ± 0.80 and 4.30 ± 0.64% of the parent value, respectively). n EFFECT: enhanced inhibition method, valuable biochemical properties of compounds. n 1 ex |
| isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-103169700-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-103172587-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-103172587-B http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-113473996-A |
| priorityDate | 2002-11-26-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 174.