公开(公告)号：EP1031563A4

公开(公告)日：2000-12-06

申请号：EP98945542

申请日：1998-09-30

申请人： DAIICHI SEIYAKU CO

发明人： KOBAYASHI SYOZO ,  KOMORIYA SATOSHI ,  ITO MASAYUKI ,  NAGATA TSUTOMU ,  MOCHIZUKI AKIYOSHI ,  HAGINOYA NORIYASU ,  NAGAHARA TAKAYASU ,  HORINO HARUHIKO

IPC分类号： C07D207/08 ,  C07D207/12 ,  C07D207/22 ,  C07D207/38 ,  C07D211/34 ,  C07D211/70 ,  C07D213/26 ,  C07D213/73 ,  C07D213/74 ,  C07D213/82 ,  C07D213/89 ,  C07D215/48 ,  C07D217/02 ,  C07D233/54 ,  C07D233/64 ,  C07D235/06 ,  C07D239/42 ,  C07D239/48 ,  C07D277/40 ,  C07D295/26 ,  C07D307/84 ,  C07D333/68 ,  C07D401/10 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D495/04 ,  C07D513/04 ,  C07D207/335 ,  A61K31/425 ,  A61K31/435 ,  A61K31/495 ,  A61K31/505 ,  A61K31/535 ,  C07D213/56

CPC分类号： C07D207/08 ,  C07C2601/14 ,  C07D207/12 ,  C07D207/22 ,  C07D207/38 ,  C07D211/34 ,  C07D211/70 ,  C07D213/26 ,  C07D213/73 ,  C07D213/74 ,  C07D213/82 ,  C07D213/89 ,  C07D215/48 ,  C07D217/02 ,  C07D233/64 ,  C07D235/06 ,  C07D239/42 ,  C07D239/48 ,  C07D277/40 ,  C07D295/26 ,  C07D307/84 ,  C07D333/68 ,  C07D401/10 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D495/04 ,  C07D513/04

摘要： Sulfonyl derivatives represented by general formula (I), salts of the same, and solvates of both; and application of them as drugs: [wherein R1 is hydrogen, hydroxyl, nitro or the like; R?2 and R3¿ are each independently hydrogen, halogeno or the like; R?4 and R5¿ are each independently hydrogen, halogeno or the like; Q1 is an optionally substituted saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group or the like; Q2 is a single bond, oxygen or the like; Q3 is, e.g., a group represented by formula (a); T1 is carbonyl or the like; and X?1 and X2¿ are each independently methylidyne or nitrogen]. These compounds exhibit potent Fxa inhibiting activities and serve as excellent anticoagulants which speedily exert satisfactory and persistent anti-thrombotic effects through oral administration and little cause adverse effects.

公开(公告)号：EP1405852A4

公开(公告)日：2006-07-26

申请号：EP02743653

申请日：2002-06-20

申请人： DAIICHI SEIYAKU CO

发明人： OHTA TOSHIHARU ,  KOMORIYA SATOSHI ,  YOSHINO TOSHIHARU ,  UOTO KOUICHI ,  NAKAMOTO YUMI ,  NAITO HIROYUKI ,  MOCHIZUKI AKIYOSHI ,  NAGATA TSUTOMU ,  KANNO HIDEYUKI ,  HAGINOYA NORIYASU ,  YOSHIKAWA KENJI ,  NAGAMOCHI MASATOSHI ,  KOBAYASHI SYOZO ,  ONO MAKOTO

IPC分类号： C07D401/12 ,  A61K20060101 ,  A61K31/428 ,  A61K31/429 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  A61P20060101 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P29/00 ,  C07D20060101 ,  C07D209/42 ,  C07D401/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D513/14 ,  C07D519/00 ,  C07K5/06 ,  C07K5/08

CPC分类号： C07D401/12 ,  C07D209/42 ,  C07D401/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04 ,  C07D513/14 ,  C07K5/06191 ,  C07K5/0827

摘要： Compounds represented by the following general formula (1), salts thereof, solvates of the same or N-oxides of the same: Q1-Q2-T0-N(R1)-Q3-N(R2)-T1-Q4 (1) wherein R1 and R2 represent each hydrogen, etc.; Q1 represents optionally substituted, saturated or unsaturated 5- or 6-membered hydrocarbyl, etc.; Q2 represents a single bond, etc.; Q3 represents the following group; (wherein Q5 represents C1-8 alkylene, etc.); and T0 and T1 represent each carbonyl, etc. These compounds are useful as preventives and/or remedies for brain infarction, cerebral embolism, myocardial infarction, angina, pulmonary infarction, pulmonary embolism, Buerger’s disease, bottom venous thrombosis, disseminated intravascular coagulation, thrombosis following artificial valve/joint replacement, thrombosis and reocclusion following circulation reconstruction, systemic inflammatory responsive syndrome (SIRS), multiple organ dysfunction (MODS), thrombosis in extracorporeal circulation or blood coagulation in collecting blood.

公开(公告)号：EP1577301A4

公开(公告)日：2009-11-11

申请号：EP03768266

申请日：2003-12-25

申请人： DAIICHI SEIYAKU CO

发明人： OHTA TOSHIHARU ,  KOMORIYA SATOSHI ,  YOSHINO TOSHIHARU ,  UOTO KOUICHI ,  NAKAMOTO YUMI ,  NAITO HIROYUKI ,  MOCHIZUKI A ,  NAGATA TSUTOMU ,  KANNO HIDEYUKI ,  HAGINOYA NORIYASU ,  YOSHIKAWA KENJI ,  NAGAMOCHI M ,  KOBAYASHI SYOZO ,  ONO MAKOTO

IPC分类号： C07D513/04 ,  C07D213/75

CPC分类号： C07D498/04 ,  C07D213/75 ,  C07D401/12 ,  C07D401/14 ,  C07D409/04 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/14 ,  C07D519/00

公开(公告)号：EP1270557A4

公开(公告)日：2008-12-03

申请号：EP01919784

申请日：2001-04-05

申请人： DAIICHI SEIYAKU CO

发明人： YOSHINO TOSHIHARU ,  NAGATA TSUTOMU ,  HAGINOYA NORIYASU ,  YOSHIKAWA KENJI ,  KANNO HIDEYUKI ,  NAGAMOCHI MASATOSHI

IPC分类号： C07D209/12 ,  C07D209/42 ,  C07D401/12 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D513/14 ,  C07D401/14 ,  C07D471/04

CPC分类号： C07D513/04 ,  C07D213/56 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04

摘要： Compounds of the general formula (1): Q1-Q2-C(=O)-N(R?1)-Q3-N(R2)-T1-Q4¿; and drugs which contain the compounds and are efficacious for thrombosis and embolism. In said formula, wherein R?1 and R2¿ are each H or the like; Q1 is an aromatic ring, a heterocycle, or the like; Q2 is a single bond, an aromatic ring, a heterocycle, or the like; Q3 is a group of the general formula (2), or the like; Q4 is an aromatic ring, a heterocycle, or the like; and T1 is -CO- or -SO¿2?-.

公开(公告)号：EP1415992A4

公开(公告)日：2006-07-26

申请号：EP02762760

申请日：2002-08-08

申请人： DAIICHI SEIYAKU CO

发明人： OHTA TOSHIHARU ,  KOMORIYA SATOSHI ,  YOSHINO TOSHIHARU ,  UOTO KOUICHI ,  NAKAMOTO YUMI ,  NAITO HIROYUKI ,  MOCHIZUKI AKIYOSHI ,  NAGATA TSUTOMU ,  KANNO HIDEYUKI ,  HAGINOYA NORIYASU ,  YOSHIKAWA KENJI ,  NAGAMOCHI MASATOSHI ,  KOBAYASHI SYOZO ,  ONO MAKOTO

IPC分类号： C07D401/12 ,  A61K20060101 ,  A61K31/428 ,  A61K31/429 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/50 ,  A61K31/501 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61P20060101 ,  A61P7/02 ,  A61P9/00 ,  C07D20060101 ,  C07D209/42 ,  C07D401/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D513/14 ,  C07D519/00 ,  C07K5/06 ,  C07K5/08

CPC分类号： C07D209/42 ,  C07D401/12 ,  C07D401/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D513/04 ,  C07K5/06191 ,  C07K5/0827

摘要： Compounds represented by the following general formula (1), salts thereof, solvates of the same or N-oxides of the same: Q1-Q2-T0-N(R1)-Q3-N(R2)-T1-Q4 (1) wherein R1 and R2 represent each hydrogen, etc.; Q1 represents optionally substituted, saturated or unsaturated 5- or 6-membered hydrocarbyl, etc.; Q2 represents a single bond, etc.; Q3 represents the following group; (wherein Q5 represents C1-8 alkylene, etc.); and T0 and T1 represent each carbonyl, etc. These compounds are useful as preventives and/or remedies for brain infarction, cerebral embolism, myocardial infarction, angina, pulmonary infarction, pulmonary embolism, Buerger’s disease, bottom venous thrombosis, disseminated intravascular coagulation, thrombosis following artificial valve/joint replacement, thrombosis and reocclusion following circulation reconstruction, systemic inflammatory responsive syndrome (SIRS), multiple organ dysfunction (MODS), thrombosis in extracorporeal circulation or blood coagulation in collecting blood.

摘要翻译： （1）表示的化合物，其盐，相同的溶剂化物或相同的N-氧化物：Q1-Q2-T0-N（R1）-Q3-N（R2）-T1-Q4（1） 其中R1和R2代表每个氢等; Q1表示任选取代的饱和或不饱和的5或6元烃基等; Q2代表单键等; Q3代表以下组别; （其中Q5表示C1-8亚烷基等）; 这些化合物可用作脑梗塞，脑栓塞，心肌梗塞，心绞痛，肺梗塞，肺栓塞，伯格氏病，下肢静脉血栓形成，弥散性血管内凝血，血栓形成等的预防剂和/或治疗剂 继循环重建，全身炎症反应综合征（SIRS），多器官功能障碍（MODS），体外循环中的血栓形成或血液凝固后的人工瓣膜/关节置换，血栓形成和再闭塞。

公开(公告)号：EP1031563A1

公开(公告)日：2000-08-30

申请号：EP98945542

申请日：1998-09-30

申请人： DAIICHI SEIYAKU CO

发明人： KOBAYASHI SHOZO ,  KOMORIYA SATOSHI ,  ITO MASAYUKI ,  NAGATA TSUTOMU ,  MOCHIZUKI AKIYOSHI ,  HAGINOYA NORIYASU ,  NAGAHARA TAKAYASU ,  HORINO HARUHIKO

IPC分类号： C07D207/08 ,  C07D207/12 ,  C07D207/22 ,  C07D207/38 ,  C07D211/34 ,  C07D211/70 ,  C07D213/26 ,  C07D213/73 ,  C07D213/74 ,  C07D213/82 ,  C07D213/89 ,  C07D215/48 ,  C07D217/02 ,  C07D233/54 ,  C07D233/64 ,  C07D235/06 ,  C07D239/42 ,  C07D239/48 ,  C07D277/40 ,  C07D295/26 ,  C07D307/84 ,  C07D333/68 ,  C07D401/10 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D495/04 ,  C07D513/04 ,  C07D207/335

CPC分类号： C07D207/08 ,  C07C2601/14 ,  C07D207/12 ,  C07D207/22 ,  C07D207/38 ,  C07D211/34 ,  C07D211/70 ,  C07D213/26 ,  C07D213/73 ,  C07D213/74 ,  C07D213/82 ,  C07D213/89 ,  C07D215/48 ,  C07D217/02 ,  C07D233/64 ,  C07D235/06 ,  C07D239/42 ,  C07D239/48 ,  C07D277/40 ,  C07D295/26 ,  C07D307/84 ,  C07D333/68 ,  C07D401/10 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D495/04 ,  C07D513/04

摘要： Described is a sulfonyl derivative represented by the following formula (I): Äwherein R represents a hydrogen atom, a hydroxyl group, a nitro group or the like, R and R each independently represents a hydrogen atom, a halogen atom or the like, R and R each independently represents a hydrogen atom, a halogen atom or the like, Q represents a saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group which may be substituted, or the like, Q represents a single bond, an oxygen atom or the like, Q represents any one of the following groups: T represents a carbonyl group or the like, and X and X each independently represents a methine group or a nitrogen atomÜ; or salt thereof; or solvate thereof. The sulfonyl derivative, salt or solvate according to the present invention is novel as an excellent anticoagulant and it has strong FXa inhibitory action, rapidly exhibits sufficient and long-lasting anti-thrombus effects after oral administration and has less side effects.

摘要翻译： 描述了由下式（I）表示的磺酰基衍生物：其中R 1表示氢原子，羟基，硝基等，R 2和R 3各自独立地表示 氢原子，卤素原子等，R 4和R 5各自独立地表示氢原子，卤素原子等，Q 1表示饱和或不饱和的5-或6-元环状 可以被取代的烃基等，Q 2表示单键，氧原子等，Q 3表示以下基团中的任一个： T 1表示羰基 X 1和X 2各自独立地表示次甲基或氮原子; 或其盐; 或其溶剂合物。 本发明的磺酰基衍生物，盐或溶剂合物作为优良的抗凝剂是新颖的，具有强的FXa抑制作用，在口服给药后迅速显示足够且持久的抗血栓作用，副作用较小。