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：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。