公开(公告)号：US20090324581A1

公开(公告)日：2009-12-31

申请号：US12299483

申请日：2007-05-09

申请人： Nobuo Machinaga ,  Toshiharu Yoshino ,  Jun Chiba ,  Jun Watanabe ,  Takashi Suzuki ,  Youichi Kimura

发明人： Nobuo Machinaga ,  Toshiharu Yoshino ,  Jun Chiba ,  Jun Watanabe ,  Takashi Suzuki ,  Youichi Kimura

IPC分类号： A61K39/395 ,  C07D409/12 ,  A61K31/405 ,  A61K31/538 ,  C07D413/12 ,  A61K31/4709 ,  A61K31/397 ,  C07D409/14

CPC分类号： C07D409/12 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/4709 ,  A61K31/538 ,  A61K45/06 ,  C07D209/08 ,  C07D401/06 ,  C07D403/12 ,  C07D409/06 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12

摘要： To provide a novel compound which has S1P receptor agonistic activity, exhibits excellent immunosuppressing effect, gives less adverse side effects, and can be orally administered.The invention provides a compound represented by general formula (I) (wherein A is a single bond, —O—, or —CH2—; R1 represents a hydrogen atom or a C1-C6 alkyl group, and V represents any one group selected from among the following groups (1) to (3): (1) -G1-, (2) -G2-N(R2)-G3-, and (3) a group represented by formula 2, wherein each of Z1 and Z2 represents a hydrogen atom or a C1-C6 alkyl group, Z3 represents a hydrogen or the like, Q represents —CH2—O— or the like, and Y represents a group represented by formula 3, a salt thereof, or a solvate thereof.

摘要翻译： 为了提供具有S1P受体激动活性的新化合物，显示出优异的免疫抑制作用，给予较少的副作用，并且可以口服给药。 本发明提供由通式（I）表示的化合物（其中A是单键，-O-或-CH 2 - ; R 1表示氢原子或C 1 -C 6烷基，V表示选自 在以下组（1）〜（3）中：（1）-G1，（2）-G2-N（R2）-G3-，（3）由式2表示的基团，其中Z1和Z2 表示氢原子或C1-C6烷基，Z3表示氢等，Q表示-CH2-O-等，Y表示由式3表示的基团，其盐或其溶剂合物。

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：US20070129371A1

公开(公告)日：2007-06-07

申请号：US10539995

申请日：2003-12-24

申请人： Yumi Nakamoto ,  Toshiharu Yoshino ,  Hiroyuki Naito ,  Tsutomu Nagata ,  Kenji Yoshikawa ,  Makoto Suzuki

发明人： Yumi Nakamoto ,  Toshiharu Yoshino ,  Hiroyuki Naito ,  Tsutomu Nagata ,  Kenji Yoshikawa ,  Makoto Suzuki

IPC分类号： A61K31/519 ,  A61K31/503 ,  A61K31/501 ,  A61K31/517 ,  A61K31/497 ,  A61K31/498

CPC分类号： C07D417/12 ,  C07D213/75

摘要： A compound represented by the following formula (1): Q1—Q2—To—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 have a substituent, or the like; Q2 is a single bond or the like; Q3 represents the following group: —C(R3a)(R4a)—{C(R3b)(R4b)}m1—{C(R3c)(R4c)}m2—{C(R3d)(R4d)}m3—{C(R3e)(R4e)}m4—C (R3f)(R4f)— (in which, R3a to R4e represent hydrogen or the like); T0 represents a carbonyl group or the like; and T1 represents —COCONR— or the like]; or salt thereof, solvate thereof, or N-oxide thereof. The compound is useful as a preventive and/or therapeutic agent for 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.

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：US07192968B2

公开(公告)日：2007-03-20

申请号：US10240725

申请日：2001-04-05

申请人： Toshiharu Yoshino ,  Tsutomu Nagata ,  Noriyasu Haginoya ,  Kenji Yoshikawa ,  Hideyuki Kanno ,  Masatoshi Nagamochi

发明人： Toshiharu Yoshino ,  Tsutomu Nagata ,  Noriyasu Haginoya ,  Kenji Yoshikawa ,  Hideyuki Kanno ,  Masatoshi Nagamochi

IPC分类号： C07D237/26 ,  C07D471/02 ,  C07D209/02 ,  A61K31/495 ,  A61K31/44

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

摘要： The invention relates a compound represented by the formula (1): Q1-Q2-C(═O)—N(R1)-Q3-N(R2)-T1-Q4  (1) wherein R1 and R2 represent H or the like; Q1 represents an aromatic ring, heterocyclic ring or the like; Q2 represents a single bond, aromatic ring, heterocyclic ring or the like; Q3 represents a group or the like, Q4 represents an aromatic ring, heterocyclic ring or the like; and T1 represents —CO— or —SO2—, and a medicine which comprises the compound and is useful for thrombosis and embolism.

摘要翻译： 本发明涉及由式（1）表示的化合物：<？in-line-formula description =“In-line Formulas”end =“lead”？> Q-1 -Q2 -C（-O）-N（R 1） - Q 3 -N（R 2） - T O （1）<？in-line-formula description =“In-line Formulas”end =“tail”？>其中R 1 和R 2代表H等; Q 1表示芳环，杂环等; Q 2表示单键，芳环，杂环等; Q 3表示一个或多个基团，Q 4表示芳环，杂环等; 和T 1表示-CO - 或-SO 2 - ，以及包含该化合物并用于血栓形成和栓塞的药物。

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：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：US07935824B2

公开(公告)日：2011-05-03

申请号：US12465329

申请日：2009-05-13

申请人： Toshiharu Yoshino ,  Tsutomu Nagata ,  Noriyasu Haginoya ,  Kenji Yoshikawa ,  Hideyuki Kanno ,  Masatoshi Nagamochi

发明人： Toshiharu Yoshino ,  Tsutomu Nagata ,  Noriyasu Haginoya ,  Kenji Yoshikawa ,  Hideyuki Kanno ,  Masatoshi Nagamochi

IPC分类号： C07D513/04

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

摘要： The invention relates a compound represented by the formula (1): Q1-Q2-C(═O)—N(R1)-Q3-N(R2)-T1-Q4  (1) wherein R1 and R2 represent H or the like; Q1 represents an aromatic ring, heterocyclic ring or the like; Q2 represents a single bond, aromatic ring, heterocyclic ring or the like; Q3 represents a group or the like, Q4 represents an aromatic ring, heterocyclic ring or the like; and T1 represents —CO— or —SO2—, and a medicine which comprises the compound and is useful for thrombosis and embolism.

摘要翻译： 本发明涉及式（1）表示的化合物：其中R1和R2表示H等的Q1-Q2-C（= O）-N（R1）-Q3-N（R2）-T1-Q4（1） ; Q1表示芳环，杂环等; Q2表示单键，芳香环，杂环等; Q 3表示基团等，Q 4表示芳香环，杂环等; 并且T1表示-CO-或-SO2-，以及包含该化合物并用于血栓形成和栓塞的药物。

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。}