公开(公告)号：US06747023B1

公开(公告)日：2004-06-08

申请号：US09762888

申请日：2001-02-12

申请人： Syozo Kobayashi ,  Satoshi Komoriya ,  Noriyasu Haginoya ,  Masanori Suzuki ,  Toshiharu Yoshino ,  Takayasu Nagahara ,  Tsutomu Nagata ,  Haruhiko Horino ,  Masayuki Ito ,  Akiyoshi Mochizuki

发明人： Syozo Kobayashi ,  Satoshi Komoriya ,  Noriyasu Haginoya ,  Masanori Suzuki ,  Toshiharu Yoshino ,  Takayasu Nagahara ,  Tsutomu Nagata ,  Haruhiko Horino ,  Masayuki Ito ,  Akiyoshi Mochizuki

IPC分类号： C07D51304

CPC分类号： C07D207/08 ,  C07D207/12 ,  C07D207/22 ,  C07D211/34 ,  C07D211/70 ,  C07D213/56 ,  C07D213/61 ,  C07D213/73 ,  C07D213/75 ,  C07D213/82 ,  C07D213/84 ,  C07D213/89 ,  C07D233/18 ,  C07D233/64 ,  C07D233/88 ,  C07D239/42 ,  C07D239/48 ,  C07D243/08 ,  C07D277/40 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

摘要： Described in the present invention are a sulfonyl derivative represented by the following formula (I): Q1—Q2—T1—Q3—SO2—QA  (I) [wherein Q1 represents a saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group, 5- or 6-membered heterocyclic group, dicyclic fused ring or tricyclic fused ring group which may have a substituent; Q2 represents a single bond, an oxygen atom, a sulfur atom, a linear or branched C1-6 alkylene group or the like; QA represents an arylalkenyl group which may have a substituent or a heteroarylalkenyl group which may have a substituent; and T1 represents a carbonyl group or the like] and a medicament comprising the same. The compound has strong FXa inhibitory action, provides prompt, sufficient and long-lasting anti-thrombus effects when orally administered, and has low side effects and is therefore useful as an excellent anticoagulant.

摘要翻译： 在本发明中描述的是由下式（I）表示的磺酰基衍生物：其中Q 1表示饱和或不饱和的5或6元环烃基，5或6元杂环基，双环稠合 可以具有取代基的环或三环稠环; Q 2表示单键，氧原子，硫原子，直链或支链C 1-6亚烷基等; Q表示芳基烯基 其可以具有取代基或可以具有取代基的杂芳基烯基; 和T 1表示羰基等]和包含该羰基的药物。 该化合物具有强的FXa抑制作用，在口服给药时提供及时，充足和持久的抗血栓作用，副作用小，因此可用作优异的抗凝血剂。

公开(公告)号：US06525042B1

公开(公告)日：2003-02-25

申请号：US09508680

申请日：2000-03-28

申请人： Syozo Kobayashi ,  Satoshi Komoriya ,  Masayuki Ito ,  Tsutomu Nagata ,  Akiyoshi Mochizuki ,  Noriyasu Haginoya ,  Takayasu Nagahara ,  Haruhiko Horino

发明人： Syozo Kobayashi ,  Satoshi Komoriya ,  Masayuki Ito ,  Tsutomu Nagata ,  Akiyoshi Mochizuki ,  Noriyasu Haginoya ,  Takayasu Nagahara ,  Haruhiko Horino

IPC分类号： C07D24302

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; R2 and R3 are each independently hydrogen, halogeno or the like; R4 and R5 are each dependently 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 X1 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.

摘要翻译： 由通式（I）表示的磺酰基衍生物，它们的盐和两者的溶剂合物：和它们作为药物的应用：[其中R1是氢，羟基，硝基等; R2和R3各自独立地为氢，卤代等; R4和R5各自为氢，卤代等; Q1是任选取代的饱和或不饱和的5-或6-元环烃基等; Q2是单键，氧等; Q3是例如由式（a）表示的基团：T1是羰基等; X1和X2各自独立地是亚甲基或氮]。 这些化合物显示出有力的Fxa抑制活性，并且作为优异的抗凝血剂，其通过口服给药快速发挥令人满意且持久的抗血栓形成作用，并且几乎不引起不良反应。