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。

公开(公告)号：US20100093785A1

公开(公告)日：2010-04-15

申请号：US12259496

申请日：2008-12-30

申请人： Toshiharu Ohta ,  Satoshi Komoriya ,  Toshiharu Yoshino ,  Kouichi Uoto ,  Yumi Nakamoto ,  Hiroyuki Naito ,  Akiyoshi Mochizuki ,  Tsutomu Nagata ,  Hideyuki Kanno ,  Noriyasu Haginoya ,  Kenji Yoshikawa ,  Masatoshi Nagamochi ,  Syozo Kobayashi ,  Makoto Ono

发明人： Toshiharu Ohta ,  Satoshi Komoriya ,  Toshiharu Yoshino ,  Kouichi Uoto ,  Yumi Nakamoto ,  Hiroyuki Naito ,  Akiyoshi Mochizuki ,  Tsutomu Nagata ,  Hideyuki Kanno ,  Noriyasu Haginoya ,  Kenji Yoshikawa ,  Masatoshi Nagamochi ,  Syozo Kobayashi ,  Makoto Ono

IPC分类号： A61K31/437

CPC分类号： C07D487/04 ,  A61K31/428 ,  A61K31/429 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  C07D209/42 ,  C07D401/12 ,  C07D401/14 ,  C07D417/12 ,  C07D417/14 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D513/14 ,  C07K5/06191 ,  C07K5/0827

摘要： A compound represented by the general formula (1): -Q1-Q2-T0-N(R1)-Q3-(R2)T1Q4   (1) wherein R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6-membered cyclic hydrocarbon group which may be substituted, or the like; Q2 is a single bond or the like; Q3 is a group in which Q5 is an alkylene group having 1 to 8 carbon atoms, or the like; and T0 and T1 are carbonyl groups or the like; a salt thereof, a solvate thereof, or an N-oxide thereof.The compound is useful as an agent for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.

摘要翻译： 由通式（1）表示的化合物：-Q1-Q2-T0-N（R1）-Q3-（R2）T1Q4（1）其中R1和R2是氢原子等; Q1是可以被取代的饱和或不饱和的5或6元环烃基，等等; Q2是单键等; Q 3为Q 5为碳原子数1〜8的亚烷基等的基团。 并且T0和T1是羰基等; 其盐，其溶剂合物或其N-氧化物。 该化合物可用作预防和/或治疗脑梗塞，脑栓塞，心肌梗死，心绞痛，肺梗塞，肺栓塞，Buerger病，深静脉血栓形成，弥散性血管内凝血综合征，瓣膜或关节置换后血栓形成 ，血管成形术后的血栓形成和再闭塞，全身炎症反应综合征（SIRS），多器官功能障碍综合征（MODS），体外循环期间的血栓形成或血液抽血时的凝血。

公开(公告)号：US20080015215A1

公开(公告)日：2008-01-17

申请号：US11850788

申请日：2007-09-06

申请人： Toshiharu Ohta ,  Satoshi Komoriya ,  Toshiharu Yoshino ,  Kouichi Uoto ,  Yumi Nakamoto ,  Hiroyuki Naito ,  Akiyoshi Mochizuki ,  Tsutomu Nagata ,  Hideyuki Kanno ,  Noriyasu Haginoya ,  Kenji Yoshikawa ,  Masatoshi Nagamochi ,  Syozo Kobayashi ,  Makoto Ono

发明人： Toshiharu Ohta ,  Satoshi Komoriya ,  Toshiharu Yoshino ,  Kouichi Uoto ,  Yumi Nakamoto ,  Hiroyuki Naito ,  Akiyoshi Mochizuki ,  Tsutomu Nagata ,  Hideyuki Kanno ,  Noriyasu Haginoya ,  Kenji Yoshikawa ,  Masatoshi Nagamochi ,  Syozo Kobayashi ,  Makoto Ono

IPC分类号： A61K31/4365 ,  A61P43/00 ,  A61P7/00 ,  A61P9/00

CPC分类号： C07D487/04 ,  A61K31/428 ,  A61K31/429 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  C07D209/42 ,  C07D401/12 ,  C07D401/14 ,  C07D417/12 ,  C07D417/14 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D513/14 ,  C07K5/06191 ,  C07K5/0827

摘要： A compound represented by the general formula (1): Q1-Q2-T0-N(R1)-Q3-N(R2)-T1-Q4  (1) wherein R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6-membered cyclic hydrocarbon group which may be substituted, or the like; Q2 is a single bond or the like; Q3 is a group in which Q5 is an alkylene group having 1 to 8 carbon atoms, or the like; and T0 and T1 are carbonyl groups or the like; a salt thereof, a solvate thereof, or an N-oxide thereof. The compound is useful as an agent for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.

摘要翻译： 由通式（1）表示的化合物：<？in-line-formula description =“In-line Formulas”end =“lead”？> Q ^{1 -N（R 1） - N（R 2） - N（R 2） - T （1）<？in-line-formula description =“In-line Formulas”end =“tail”？>其中R 1 < / SUP>和R 2是氢原子等; Q 1是可被取代的饱和或不饱和的5或6元环烃基，等等; Q 2是单键等; Q 3是其中Q 5是具有1〜8个碳原子的亚烷基等的基团; T 0和T 1是羰基等; 其盐，其溶剂合物或其N-氧化物。 该化合物可用作预防和/或治疗脑梗塞，脑栓塞，心肌梗死，心绞痛，肺梗塞，肺栓塞，Buerger病，深静脉血栓形成，弥散性血管内凝血综合征，瓣膜或关节置换后血栓形成 ，血管成形术后的血栓形成和再闭塞，全身炎症反应综合征（SIRS），多器官功能障碍综合征（MODS），体外循环期间的血栓形成或血液抽血时的凝血。}

公开(公告)号：US07576135B2

公开(公告)日：2009-08-18

申请号：US10540259

申请日：2003-12-25

申请人： Toshiharu Ohta ,  Satoshi Komoriya ,  Toshiharu Yoshino ,  Kouichi Uoto ,  Yumi Nakamoto ,  Hiroyuki Naito ,  Akiyoshi Mochizuki ,  Tsutomu Nagata ,  Hideyuki Kanno ,  Noriyasu Haginoya ,  Kenji Yoshikawa ,  Masatoshi Nagamochi ,  Syozo Kobayashi ,  Makoto Ono

发明人： Toshiharu Ohta ,  Satoshi Komoriya ,  Toshiharu Yoshino ,  Kouichi Uoto ,  Yumi Nakamoto ,  Hiroyuki Naito ,  Akiyoshi Mochizuki ,  Tsutomu Nagata ,  Hideyuki Kanno ,  Noriyasu Haginoya ,  Kenji Yoshikawa ,  Masatoshi Nagamochi ,  Syozo Kobayashi ,  Makoto Ono

IPC分类号： A61K31/13

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

摘要： A compound represented by formula (1): Q1-Q2-T0-N(R1)-Q3-N(R2)-T1-Q4  (1) [wherein R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6-membered cyclic hydrocarbon group which may be substituted, or the like; Q2 is a single bond or the like; Q3 represents the following group: (wherein Q5 is an alkylene group having 1 to 8 carbon atoms, or the like); and T0 and T1 are carbonyl groups or the like], a salt thereof, a solvate thereof, or an N-oxide thereof. The compound is useful as an agent for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after artificial valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.

摘要翻译： Q1-Q2-T0-N（R1）-Q3-N（R2）-T1由式（1）表示的化合物：<？in-line-formula description =“In-line formula”end =“lead” -Q4（1）<？in-line-formula description =“In-line Formulas”end =“tail”？> [其中R1和R2是氢原子等; Q1是可以被取代的饱和或不饱和的5或6元环烃基，等等; Q2是单键等; Q3表示以下基团：（其中Q5为碳原子数为1〜8的亚烷基等）; 并且T0和T1是羰基等]，其盐，其溶剂合物或其N-氧化物。 该化合物可用作预防和/或治疗脑梗塞，脑栓塞，心肌梗死，心绞痛，肺梗塞，肺栓塞，Buerger病，深静脉血栓形成，弥散性血管内凝血综合征，人工瓣膜或关节后血栓形成 血管成形术后的替代，血栓形成和再闭塞，全身炎症反应综合征（SIRS），多器官功能障碍综合征（MODS），体外循环期间的血栓形成或血液抽血时的凝血。

公开(公告)号：US20050020645A1

公开(公告)日：2005-01-27

申请号：US10773344

申请日：2004-02-09

申请人： Toshiharu Ohta ,  Satoshi Komoriya ,  Toshiharu Yoshino ,  Kouichi Uoto ,  Yumi Nakamoto ,  Hiroyuki Naito ,  Akiyoshi Mochizuki ,  Tsutomu Nagata ,  Hideyuki Kanno ,  Noriyasu Haginoya ,  Kenji Yoshikawa ,  Masatoshi Nagamochi ,  Syozo Kobayashi ,  Makoto Ono

发明人： Toshiharu Ohta ,  Satoshi Komoriya ,  Toshiharu Yoshino ,  Kouichi Uoto ,  Yumi Nakamoto ,  Hiroyuki Naito ,  Akiyoshi Mochizuki ,  Tsutomu Nagata ,  Hideyuki Kanno ,  Noriyasu Haginoya ,  Kenji Yoshikawa ,  Masatoshi Nagamochi ,  Syozo Kobayashi ,  Makoto Ono

IPC分类号： C07D209/42 ,  C07D513/04 ,  A61K31/44 ,  A61K31/40

CPC分类号： C07D513/04 ,  C07D209/42

摘要： A compound represented by the general formula (1): Q1-Q2-T0-N(R1)-Q3-N(R2)-T1-Q4  (1) wherein R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6-membered cyclic hydrocarbon group which may be substituted, or the like; Q2 is a single bond or the like; Q3 is a group in which Q5 is an alkylene group having 1 to 8 carbon atoms, or the like; and T0 and T1 are carbonyl groups or the like; a salt thereof, a solvate thereof, or an N-oxide thereof. The compound is useful as an agent for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.

摘要翻译： 由通式（1）表示的化合物：Q 1 -Q 2 -N（R 1）-Q 3 -N（R 2）-T 1 -Q 4（1）其中R 1和R 2都是氢原子等; Q 1是可被取代的饱和或不饱和的5或6元环烃基，等等; Q 2是单键等; Q 3为Q 5为碳原子数1〜8的亚烷基等的基团， T 0和T 1是羰基等; 其盐，其溶剂合物或其N-氧化物。 该化合物可用作预防和/或治疗脑梗塞，脑栓塞，心肌梗死，心绞痛，肺梗塞，肺栓塞，Buerger病，深静脉血栓形成，弥散性血管内凝血综合征，瓣膜或关节置换后血栓形成 ，血管成形术后的血栓形成和再闭塞，全身炎症反应综合征（SIRS），多器官功能障碍综合征（MODS），体外循环期间的血栓形成或血液抽血时的凝血。

公开(公告)号：US20050119486A1

公开(公告)日：2005-06-02

申请号：US10481262

申请日：2002-03-20

申请人： Toshiharu Ohta ,  Satoshi Komoriya ,  Toshiharu Yoshino ,  Kouichi Uoto ,  Yumi Nakamoto ,  Hiroyuki Naito ,  Akiyoshi Mochizuki ,  Tsutomu Nagata ,  Hideyuki Kanno ,  Noriyasu Haginoya ,  Kenji Yoshikawa ,  Masatoshi Nagamochi ,  Syozo Kobayashi ,  Makoto Ono

发明人： Toshiharu Ohta ,  Satoshi Komoriya ,  Toshiharu Yoshino ,  Kouichi Uoto ,  Yumi Nakamoto ,  Hiroyuki Naito ,  Akiyoshi Mochizuki ,  Tsutomu Nagata ,  Hideyuki Kanno ,  Noriyasu Haginoya ,  Kenji Yoshikawa ,  Masatoshi Nagamochi ,  Syozo Kobayashi ,  Makoto Ono

IPC分类号： C07D401/12 ,  A61K20060101 ,  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 ,  C07D405/00

CPC分类号： C07D487/04 ,  A61K31/428 ,  A61K31/429 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  C07D209/42 ,  C07D401/12 ,  C07D401/14 ,  C07D417/12 ,  C07D417/14 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D513/14 ,  C07K5/06191 ,  C07K5/0827

摘要： A compound represented by the general formula (1): Q1-Q2-T0-N(R1)-Q3-N(R2)-T1-Q4  (1) wherein R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6-membered cyclic hydrocarbon group which may be substituted, or the like; Q2 is a single bond or the like; Q3 is a group in which Q5 is an alkylene group having 1 to 8 carbon atoms, or the like; and T0 and T1 are carbonyl groups or the like; a salt thereof, a solvate thereof, or an N-oxide thereof. The compound is useful as an agent for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.

摘要翻译： 由通式（1）表示的化合物：<？in-line-formula description =“In-line Formulas”end =“lead”？> Q ^{1 -N（R 1） - N（R 2） - N（R 2） - T （1）<？in-line-formula description =“In-line Formulas”end =“tail”？>其中R 1 < / SUP>和R 2是氢原子等; Q 1是可被取代的饱和或不饱和的5或6元环烃基，等等; Q 2是单键等; Q 3是其中Q 5是具有1〜8个碳原子的亚烷基等的基团; T 0和T 1是羰基等; 其盐，其溶剂合物或其N-氧化物。 该化合物可用作预防和/或治疗脑梗塞，脑栓塞，心肌梗死，心绞痛，肺梗塞，肺栓塞，Buerger病，深静脉血栓形成，弥散性血管内凝血综合征，瓣膜或关节置换后血栓形成 ，血管成形术后的血栓形成和再闭塞，全身炎症反应综合征（SIRS），多器官功能障碍综合征（MODS），体外循环期间的血栓形成或血液抽血时的凝血。}

公开(公告)号：US20090281074A1

公开(公告)日：2009-11-12

申请号：US12250586

申请日：2008-10-14

申请人： Toshiharu OHTA ,  Satoshi Komoriya ,  Toshiharu Yoshino ,  Kouichi Outo ,  Yumi Nakamoto ,  Hiroyuki Naito ,  Akiyoshi Mochizuki ,  Tsutomu Nagata ,  Hideyuki Kanno ,  Noriyasu Haginoya ,  Kenji Yoshikawa ,  Masatoshi Nagamochi ,  Syozo Kobayashi ,  Makoto Ono

发明人： Toshiharu OHTA ,  Satoshi Komoriya ,  Toshiharu Yoshino ,  Kouichi Outo ,  Yumi Nakamoto ,  Hiroyuki Naito ,  Akiyoshi Mochizuki ,  Tsutomu Nagata ,  Hideyuki Kanno ,  Noriyasu Haginoya ,  Kenji Yoshikawa ,  Masatoshi Nagamochi ,  Syozo Kobayashi ,  Makoto Ono

IPC分类号： A61K31/397 ,  A61K31/437 ,  A61K31/502 ,  A61K31/5377 ,  A61K31/55

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

摘要： Drug compositions containing a substituted diamine compound represented by formula (1): Q1-Q2-r-N(R1)-Q3-N(R2)  (1) wherein Q3 represents the following group wherein Q5 represents an alkylene group having 4 carbon atoms, R3 represents a hydrogen atom, and R4 represents a 3-6 membered heterocyclic group which may be substituted; are useful for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after artificial valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.

摘要翻译： 含有式（1）表示的取代二胺化合物的药物组合物：Q1-Q2-rN（R1）-Q3-N（R2）（1）其中Q3表示以下基团，其中Q5表示具有4个碳原子的亚烷基，R3 表示氢原子，R4表示可以被取代的3-6元杂环基; 可用于预防和/或治疗脑梗死，脑栓塞，心肌梗死，心绞痛，肺梗塞，肺栓塞，Buerger病，深静脉血栓形成，弥散性血管内凝血综合征，人工瓣膜或关节置换后血栓形成，血栓形成和 血管成形术后再闭塞，全身炎症反应综合征（SIRS），多器官功能障碍综合征（MODS），体外循环期间的血栓形成或血液抽血时的凝血。

公开(公告)号：US07342014B2

公开(公告)日：2008-03-11

申请号：US10773344

申请日：2004-02-09

申请人： Toshiharu Ohta ,  Satoshi Komoriya ,  Toshiharu Yoshino ,  Kouichi Uoto ,  Yumi Nakamoto ,  Hiroyuki Naito ,  Akiyoshi Mochizuki ,  Tsutomu Nagata ,  Hideyuki Kanno ,  Noriyasu Haginoya ,  Kenji Yoshikawa ,  Masatoshi Nagamochi ,  Syozo Kobayashi ,  Makoto Ono

发明人： Toshiharu Ohta ,  Satoshi Komoriya ,  Toshiharu Yoshino ,  Kouichi Uoto ,  Yumi Nakamoto ,  Hiroyuki Naito ,  Akiyoshi Mochizuki ,  Tsutomu Nagata ,  Hideyuki Kanno ,  Noriyasu Haginoya ,  Kenji Yoshikawa ,  Masatoshi Nagamochi ,  Syozo Kobayashi ,  Makoto Ono

IPC分类号： A61K31/50 ,  A61K31/44 ,  A61K31/445 ,  C07D471/02 ,  C07D401/00

CPC分类号： C07D513/04 ,  C07D209/42

摘要： A compound represented by the general formula (1): Q1-Q2-T0-N(R1)-Q3-N(R2)-T1-Q4  (1) wherein R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6-membered cyclic hydrocarbon group which may be substituted, or the like; Q2 is a single bond or the like; Q3 is a group in which Q5 is an alkylene group having 1 to 8 carbon atoms, or the like; and T0 and T1 are carbonyl groups or the like; a salt thereof, a solvate thereof, or an N-oxide thereof. The compound is useful as an agent for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.

摘要翻译： 由通式（1）表示的化合物：<？in-line-formula description =“In-line Formulas”end =“lead”？> Q ^{1 -N（R 1） - N（R 2） - N（R 2） - T （1）<？in-line-formula description =“In-line Formulas”end =“tail”？>其中R 1 < / SUP>和R 2是氢原子等; Q 1是可被取代的饱和或不饱和的5或6元环烃基，等等; Q 2是单键等; Q 3是其中Q 5是具有1〜8个碳原子的亚烷基等的基团; T 0和T 1是羰基等; 其盐，其溶剂合物或其N-氧化物。 该化合物可用作预防和/或治疗脑梗塞，脑栓塞，心肌梗死，心绞痛，肺梗塞，肺栓塞，Buerger病，深静脉血栓形成，弥散性血管内凝血综合征，瓣膜或关节置换后血栓形成 ，血管成形术后的血栓形成和再闭塞，全身炎症反应综合征（SIRS），多器官功能障碍综合征（MODS），体外循环期间的血栓形成或血液抽血时的凝血。}

公开(公告)号：US20050245565A1

公开(公告)日：2005-11-03

申请号：US10481629

申请日：2002-06-20

申请人： Toshiharu Ohta ,  Satoshi Komoriya ,  Toshiharu Yoshino ,  Kouichi Uoto ,  Yumi Nakamoto ,  Hiroyuki Naito ,  Akiyoshi Mochizuki ,  Tsutomu Nagata ,  Hideyuki Kanno ,  Noriyasu Haginoya ,  Kenji Yoshikawa ,  Masatoshi Nagamochi ,  Syozo Kobayashi ,  Makoto Ono

发明人： Toshiharu Ohta ,  Satoshi Komoriya ,  Toshiharu Yoshino ,  Kouichi Uoto ,  Yumi Nakamoto ,  Hiroyuki Naito ,  Akiyoshi Mochizuki ,  Tsutomu Nagata ,  Hideyuki Kanno ,  Noriyasu Haginoya ,  Kenji Yoshikawa ,  Masatoshi Nagamochi ,  Syozo Kobayashi ,  Makoto Ono

IPC分类号： C07D401/12 ,  A61K20060101 ,  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 ,  C07D471/02 ,  A61K31/4745 ,  C07D43/02

CPC分类号： C07D401/12 ,  A61K31/428 ,  A61K31/429 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  C07D209/42 ,  C07D401/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D513/14 ,  C07K5/06191 ,  C07K5/0827

摘要： A compound represented by the general formula (1): Q1-Q2-T0-N(R1)-Q3-N(R2) -T1-Q4   (1) wherein R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6-membered cyclic hydrocarbon group which may be substituted, or the like; Q2 is a single bond or the like; Q3 is a group in which Q5 is an alkylene group having 1 to 8 carbon atoms, or the like; and T0 and T1 are carbonyl groups or the like; a salt thereof, a solvate thereof, or an N-oxide thereof. The compound is useful as an agent for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.

摘要翻译： 由通式（1）表示的化合物：<？in-line-formula description =“In-line Formulas”end =“lead”？> Q ^{1 -O（R 1） - N 3 - （R 2） - N（R 2） - T （1）<？in-line-formula description =“In-line Formulas”end =“tail”？>其中R 1 < / SUP>和R 2是氢原子等; Q 1是可被取代的饱和或不饱和的5或6元环烃基，等等; Q 2是单键等; Q 3是其中Q 5是具有1〜8个碳原子的亚烷基等的基团; T 0和T 1是羰基等; 其盐，其溶剂合物或其N-氧化物。 该化合物可用作预防和/或治疗脑梗塞，脑栓塞，心肌梗死，心绞痛，肺梗塞，肺栓塞，Buerger病，深静脉血栓形成，弥散性血管内凝血综合征，瓣膜或关节置换后血栓形成 ，血管成形术后的血栓形成和再闭塞，全身炎症反应综合征（SIRS），多器官功能障碍综合征（MODS），体外循环期间的血栓形成或血液抽血时的凝血。}