http://rdf.ncbi.nlm.nih.gov/pubchem/patent/FI-116940-B
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_7d9751afd4757ecf6908e1d39b22accd |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-69 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-42 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-42 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P3-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-635 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-69 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D- |
filingDate | 2001-07-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 2006-04-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9ea560edeeaf1ebc7b9c5d43ab8abec2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_32fb54ece787443dd7898f1bbfedc8d2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_10f85b5eabf30245029fd2acb77db7cb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0ac7abfd98edee783971df2d6ccab29a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dd6985b52fc16e5e4e3c697ce3786d64 |
publicationDate | 2006-04-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | FI-116940-B |
titleOfInvention | Compounds Useful for the Treatment or Prevention of Alpha-2B Adrenoceptor Mediated Disease |
abstract | N-Pyrimidinyl para-aminobenzenesulfonamide derivatives (I) are new. N-Pyrimidinyl para-aminobenzenesulfonamide derivatives of formula (I) and their salts, except for 4-(1H-benzimidazol-2-ylmethylamino)-N-(4,6-dimethyl-2-pyrimidinyl)-benzenesulfonamide, 4-(1-methyl-1H-benzimidazol-2-ylmethylamino)-N-(4,6-dimethyl-2-pyrimidinyl)-benzenesulfonamide, 4-(1-ethyl-1H-benzimidazol-2-ylmethylamino)-N-(4,6-dimethyl-2-pyrimidinyl)-benzenesulfonamide and 4-(1H-benzimidazol-2-ylmethylamino)-N-(4-methyl-2-pyrimidinyl)-benzenesulfonamide, are new; [Image] R1-R5H, 1-4C alkyl, 1-4C alkoxy or halogen; Z : H, acetyl, trifluoromethoxybenzyl or trifluoromethylbenzyl; Y : Q or Q(1-2C)alkyl; X : H, 1-4C alkyl, phenyl or OH; Q : phenyl optionally substituted with 1-2 of halogen, 1-4C alkyl, 1-4C alkoxy, halomethyl, halomethoxy, CN, CONH2, NH2 or NO2; 2-benzimidazolyl, 2-imidazolyl or 2- or 3-indolyl optionally substituted 1-2 of 1-4C alkyl, 1-4C alkoxy or halogen, where one N atom is optionally substituted with 1-4C alkyl, 1-4C alkoxy or benzyl; pyridyl optionally substituted 1-2 of 1-4C alkyl, 1-4C alkoxy or halogen; or naphthyl optionally substituted 1-2 of 1-4C alkyl, 1-4C alkoxy or halogen. ACTIVITY : Cardiant; Antianginal; Vasotropic; Hypotensive; Cerebroprotective; Antimigraine; Gynecological; Anorectic; Antiinfertility. MECHANISM OF ACTION : Alpha-2B Adrenoceptor Antagonist. 4-(1-Isobutyl-1H-benzimidazol-2-ylmethylamino)-N-(4,6-dimethyl-2-pyrimidinyl)-benzenesulfonamide had a Ki of 160 nM for inhibiting binding of 3>H-rauwolscine to membrane preparations from Shionogi S115 cells stably transfected with human alpha-2B adrenoceptor. |
priorityDate | 2001-07-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 162.