公开(公告)号：EP1331221A4

公开(公告)日：2005-11-23

申请号：EP01972648

申请日：2001-10-02

申请人： KISSEI PHARMACEUTICAL

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：EP1486485A4

公开(公告)日：2009-07-15

申请号：EP03744508

申请日：2003-03-04

申请人： KISSEI PHARMACEUTICAL

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.

公开(公告)号：EP1443041A4

公开(公告)日：2006-06-07

申请号：EP02777984

申请日：2002-10-29

申请人： KISSEI PHARMACEUTICAL

发明人： UCHIDA MASAHIKO ,  KOBAYASHI HIROAKI ,  KAI YUICHIRO ,  YOKOYAMA KENJI ,  TERAO YOSHIHIRO ,  MURANAKA HIDEYUKI

IPC分类号： A61K31/18 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P13/12 ,  A61P25/28 ,  A61P31/16 ,  C07C311/29 ,  C07D207/00 ,  C07D207/16 ,  C07D207/26 ,  C07D207/273 ,  C07D211/42 ,  C07D211/60 ,  C07D213/42 ,  C07D213/82 ,  C07D231/12 ,  C07D233/02 ,  C07D261/08 ,  C07D263/38 ,  C07D271/10 ,  C07D271/113 ,  C07D277/28 ,  C07D277/44 ,  C07D277/46 ,  C07D295/088 ,  C07D295/13 ,  C07D295/185 ,  C07D295/192 ,  C07D317/62 ,  C07D333/20 ,  C07C311/37 ,  A61K31/00 ,  C07D211/62 ,  C07D213/00 ,  C07D233/36 ,  C07D241/04 ,  C07D263/20 ,  C07D271/00 ,  C07D295/00 ,  C07D333/00

CPC分类号： C07D207/273 ,  A61K31/18 ,  C07C311/29 ,  C07D207/00 ,  C07D207/16 ,  C07D211/42 ,  C07D211/60 ,  C07D213/42 ,  C07D213/82 ,  C07D231/12 ,  C07D233/02 ,  C07D261/08 ,  C07D263/38 ,  C07D271/113 ,  C07D277/28 ,  C07D277/46 ,  C07D295/088 ,  C07D295/13 ,  C07D295/185 ,  C07D295/192 ,  C07D317/62 ,  C07D333/20

摘要： 5-Amidino-2-hydroxybenzenesulfonamide derivatives represented by the following general formula [I] exhibiting a potent and selective inhibitory activity on activated blood coagulation factor X and thus being useful as preventives or remedies for diseases in the onset of which activated blood coagulation factor X participates: [I] wherein R1 represents optionally substituted lower alkyl, optionally substituted lower alkoxy, optionally substituted alkenyl, cycloalkyl, lower acyl, etc.; Q represents hydrogen or optionally substituted lower alkyl; and Z represents hydrogen, hydroxy, etc.; pharmacologically acceptable salts thereof, medicinal compositions containing the same and intermediates in the production thereof. These compounds are useful as preventives or remedies for various diseases such as brain infarction, cerebral thrombosis, cerebral embolism, TIA, cerebral vascular jerk, Alzheimer’s diseases, myocardial infarction, heart attack, heart failure, thrombosis, pulmonary infarction and pulmonary embolism.

公开(公告)号：EP1415983A4

公开(公告)日：2006-01-18

申请号：EP02762759

申请日：2002-08-08

申请人： KISSEI PHARMACEUTICAL

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.