http://rdf.ncbi.nlm.nih.gov/pubchem/patent/FI-116940-B

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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
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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>
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