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2.发明公开5-AMIDINO-2-HYDROXYBENZENESULFONAMIDE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AND INTERMEDIATES FOR THEIR PREPARATION 有权5-脒基-2- HYDROXYBENZOLSULFONAMIDDERIVATE，药物组合物含有这些化合物，以及用于中间产品及其
公开(公告)号：EP1331221A4
公开(公告)日：2005-11-23
申请号：EP01972648
申请日：2001-10-02
发明人： OKAZAKI KOSUKE , UCHIDA MASAHIKO , MUKAIYAMA HARUNOBU , KOBAYASHI HIROAKI , KAI YUICHIRO , TAKEUCHI HIDEKI , YOKOYAMA KENJI , TERAO YOSHIHIRO , HOYANO YUJI , SHIOHARA HIROAKI , KIKUCHI NORIHIKO
IPC分类号： A61P7/02 , A61P9/10 , C07C311/29 , C07C311/37 , C07C317/32 , C07D277/28 , A61K31/216 , A61K31/4245 , A61K31/426 , A61K31/5375 , C07D271/10 , C07D295/18
CPC分类号： A61K31/18 , A61K31/40 , A61K31/421 , A61K31/445 , A61K31/5377 , A61K31/55 , A61K31/553 , C07C311/29 , C07C311/37 , C07C317/32 , C07C2601/14
摘要： 5-Amidino-2-hydroxybenzenesulfonamide derivatives of the general formula [I] or their pharmacologically acceptable salts, exhibiting potent and selective inhibitory activity against activated blood coagulation factor X and being useful as preventive or therapeutic drugs for diseases whose onset is related to activated blood coagulation factor X; pharmaceutical compositions containing the same; their use in medicines; and intermediates for their preparation: [I] wherein R is hydrogen or optionally substituted lower alkyl; R is di(lower alkyl)amino, lower alkyl, cycloalkyl, optionally substituted aryl, optionally substituted heterocycloalkyl, or an optionally substituted aromatic heterocyclic group; T is oxygen, sulfur, sulfonyl, or the like; Q is hydrogen or optionally substituted lower alkyl; and Z is hydrogen, hydroxyl, or the like.
摘要翻译： 本发明涉及一种由通式表示的5-脒基-2-羟基苯磺酰胺衍生物：
worin - [R <1>是一个氢原子或在OPTIONALLY substituiertem低级烷基; [R <2>是二（低级烷基）氨基，低级烷基，环烷基，在OPTIONALLY substituiertem芳基，在任选取代的杂环基团，或在任选被取代的芳香族杂环基。 T为氧原子，硫原子，磺酰基等; Q处于OPTIONALLY substituiertem氢原子或低级烷基; 且Z为氢原子，羟基基团等，或它们的药学上可接受的盐，其施加一个有效的和选择性的活化血液凝固因子X抑制活性，是作为用于疾病的与在相关联的预防或治疗剂是有用 活化血液凝固第X因子，药物组合物包含相同的，它们并涉及其中间体的药物的用途。 -
公开(公告)号：EP2535342A4
公开(公告)日：2013-07-10
申请号：EP11742250
申请日：2011-02-09
发明人： JO KAZUMICHI , TAKEUCHI HIDEKI
IPC分类号： C07D495/04 , A61K31/519 , A61P5/04 , A61P15/08 , A61P15/16 , A61P15/18 , A61P35/00
CPC分类号： A61K31/519 , A61K9/0053 , A61K31/14 , C07D495/04 , C07B2200/13
摘要： An objective of the present invention is to improve the solubility of 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid. The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxy lic acid choline salt has excellent solubility and storage stability.
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4.发明公开CRYSTAL POLYMORPHISM OF 4 -{2-Ý(1S,2R)-2-HYDROXY-2-(4-HYDROXYPHENYL)-1-METHYLETHYLAMINO¨ETHOXY}-3-ISOPROPYL-3 ,5 -DIMETHYLBIPHENYLCARBOXYLIC ACID HYDROCHLORIDE 审中-公开5-（2 - [（1S，2R）-2-羟基-2-（4-羟基苯基）-1-甲基乙酰胺基]乙氧基} -3-异丙基-3,5-二甲基苯乙烯基碳酸钠
公开(公告)号：EP1876167A4
公开(公告)日：2010-07-07
申请号：EP06732125
申请日：2006-04-20
发明人： KASAI KIYOSHI , ISHIKAWA TAKEHIRO , OZAWA TETSUJI , KAMATA KOJI , SUZUKI RITSU , TAKEUCHI HIDEKI
IPC分类号： C07C217/18 , A61K31/195 , A61P1/14 , A61P1/18 , A61P3/04 , A61P3/06 , A61P3/10 , A61P13/02 , A61P25/24 , A61P43/00
CPC分类号： C07C217/22 , C07B2200/07 , C07B2200/13
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公开(公告)号：EP2275430A4
公开(公告)日：2011-04-06
申请号：EP09733364
申请日：2009-04-13
发明人： TAKEUCHI HIDEKI , TSURU EIJI
IPC分类号： C07H17/02 , A61K31/7056 , A61P3/10
CPC分类号： C07H17/02
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6.发明公开NOVEL CRYSTALS OF 5-HYDROXYCARBAMIMIDOYL-2-HYDROXYBENZENESULFONAMIDE DERIVATIVE 审中-公开甲5-羟基甲脒基-2- HYDROXYBENZOLSULFONAMIDDERIVATS的新晶体
公开(公告)号：EP1486485A4
公开(公告)日：2009-07-15
申请号：EP03744508
申请日：2003-03-04
发明人： MUKAIYAMA HARUNOBU , KAI YUICHIRO , TAKEUCHI HIDEKI , YOKOYAMA KENJI , TERAO YOSHIHIRO , AKAHANE SATOSHI
IPC分类号： A61P7/02 , C07C317/32 , A61K31/216
CPC分类号： C07C317/32
摘要： It is intended to provide crystals of [4-[2-[2-hydroxy-5-(N-hydroxycarbamimidoyl)benzenesulfonylamino]ethyl]-2'-methanesulfonylbiphenyl-3-yloxy]acetic acid n-butyl hydrochloride showing an excellent effect of inhibiting activated blood coagulation factor X and being useful as a preventive or a remedy for thrombotic or obstructive diseases; medicinal compositions containing the same; and use thereof.
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7.发明公开5-AMIDINO-N-(2-AMINOPHENETHYL)-HYDROXYBENZENESULFONAMIDE DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, AND INTERMEDIATE THEREFOR 审中-公开5脒基N-（2-氨基苯乙基）-N- HYDROXYBENZOLSULFONAMIDDERIVAT含有医疗用组合物和中间体为此
公开(公告)号：EP1415983A4
公开(公告)日：2006-01-18
申请号：EP02762759
申请日：2002-08-08
发明人： OKAZAKI KOSUKE , UCHIDA MASAHIKO , KOBAYASHI HIROAKI , KAI YUICHIRO , TAKEUCHI HIDEKI , YOKOYAMA KENJI , TERAO YOSHIHIRO , SUZUKI RITSU
IPC分类号： A61P7/02 , A61P9/00 , A61P9/10 , A61P11/00 , A61P13/12 , A61P25/28 , A61P31/16 , A61P37/06 , A61P43/00 , C07C311/29 , C07C311/27 , A61K31/18 , A61K31/198 , A61K31/216 , A61K31/223 , A61K31/275 , A61K31/41 , C07D257/04
CPC分类号： C07C311/29
摘要： A 5−amidino−N−(2−aminophenethyl)−2−hydroxybenzenesulfonamide derivative represented by the general formula [I] (wherein R 1 is hydrogen or lower alkyl; R 2 is hydrogen, optionally substituted lower alkyl, etc.; R 3 is di(lower alkyl)amino, lower alkyl, cycloalkyl, etc.; Q is hydrogen or optionally substituted lower alkyl; and Z is hydrogen, hydroxy, etc.) or a pharmacologically acceptable salt of the derivative, which have strong and selective inhibitory activity against activated blood coagulation factor X and are useful as a preventive or remedy for diseases in which the activated blood coagulation factor X participates; a medicinal composition containing the compound; a medicinal use of the compound; and an intermediate for the compound.
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