公开(公告)号：US20110166131A1

公开(公告)日：2011-07-07

申请号：US13045567

申请日：2011-03-11

申请人： Hisashi TAKAHASHI ,  Junichi Kuroyanagi ,  Rie Miyauchi ,  Masatoshi Nagamochi ,  Makoto Takemura ,  Isao Hayakawa

发明人： Hisashi TAKAHASHI ,  Junichi Kuroyanagi ,  Rie Miyauchi ,  Masatoshi Nagamochi ,  Makoto Takemura ,  Isao Hayakawa

IPC分类号： A61K31/5383 ,  C07D498/06 ,  A61P31/04

CPC分类号： C07D401/04 ,  C07D498/06

摘要： A quinolone antibacterial compound, or a salt or hydrate of the compound, for the treatment of infectious diseases, which exhibit potent antibacterial activity and higher selective toxicity against Gram-positive and Gram-negative bacteria, which do not cause side effects (e.g., convulsion), which exhibit higher safety, and which has a structure of formula (I):

摘要翻译： 用于治疗感染性疾病的喹诺酮类抗菌化合物或化合物的盐或水合物，其对革兰氏阳性和革兰氏阴性菌具有强力的抗菌活性和较高的选择性毒性，其不引起副作用（例如惊厥 ），其具有更高的安全性，并且具有式（I）的结构：

公开(公告)号：US20080045520A1

公开(公告)日：2008-02-21

申请号：US11596318

申请日：2005-05-13

申请人： Hisashi Takahashi ,  Junichi Kuroyanagi ,  Rie Miyauchi ,  Masatoshi Nagamochi ,  Makoto Takemura ,  Isao Hayakawa

发明人： Hisashi Takahashi ,  Junichi Kuroyanagi ,  Rie Miyauchi ,  Masatoshi Nagamochi ,  Makoto Takemura ,  Isao Hayakawa

IPC分类号： A61K31/4709 ,  A61K31/538 ,  A61P31/00 ,  A61P31/04 ,  C07D215/14 ,  C07D498/06

CPC分类号： C07D401/04 ,  C07D498/06

摘要： The present invention contemplates provision of a quinolone antibacterial agent and a drug for the treatment of infectious diseases, which exhibit potent antibacterial activity and higher selective toxicity against Gram-positive and Gram-negative bacteria, which do not cause side effects (e.g., convulsion), and which exhibit higher safety. A compound represented by the following formula (I): a salt of the compound, or a hydrate of the compound or the salt; and an antibacterial drug and an infectious disease treating drug containing the compound as an active ingredient.

摘要翻译： 本发明考虑提供喹诺酮抗菌剂和用于治疗感染性疾病的药物，其对革兰氏阳性和革兰氏阴性菌具有强力的抗菌活性和较高的选择性毒性，其不引起副作用（例如惊厥） ，而且安全性更高。 由下式（I）表示的化合物：化合物的盐或化合物或其盐的水合物; 以及含有该化合物作为活性成分的抗菌药物和感染性疾病治疗药物。

公开(公告)号：US08455482B2

公开(公告)日：2013-06-04

申请号：US13045567

申请日：2011-03-11

申请人： Hisashi Takahashi ,  Junichi Kuroyanagi ,  Rie Miyauchi ,  Masatoshi Nagamochi ,  Makoto Takemura ,  Isao Hayakawa

发明人： Hisashi Takahashi ,  Junichi Kuroyanagi ,  Rie Miyauchi ,  Masatoshi Nagamochi ,  Makoto Takemura ,  Isao Hayakawa

IPC分类号： A61K31/535

CPC分类号： C07D401/04 ,  C07D498/06

摘要： A quinolone antibacterial compound, or a salt or hydrate of the compound, for the treatment of infectious diseases, which exhibit potent antibacterial activity and higher selective toxicity against Gram-positive and Gram-negative bacteria, which do not cause side effects (e.g., convulsion), which exhibit higher safety, and which has a structure of formula (I):

摘要翻译： 用于治疗感染性疾病的喹诺酮类抗菌化合物或化合物的盐或水合物，其对革兰氏阳性和革兰氏阴性菌具有强力的抗菌活性和较高的选择性毒性，其不引起副作用（例如惊厥 ），其具有更高的安全性，并且具有式（I）的结构：

公开(公告)号：US07977327B2

公开(公告)日：2011-07-12

申请号：US11596318

申请日：2005-05-13

申请人： Hisashi Takahashi ,  Junichi Kuroyanagi ,  Rie Miyauchi ,  Masatoshi Nagamochi ,  Makoto Takemura ,  Isao Hayakawa

发明人： Hisashi Takahashi ,  Junichi Kuroyanagi ,  Rie Miyauchi ,  Masatoshi Nagamochi ,  Makoto Takemura ,  Isao Hayakawa

IPC分类号： A61K31/54

CPC分类号： C07D401/04 ,  C07D498/06

摘要： A quinolone antibacterial compound, or a salt or hydrate of the compound, for the treatment of infectious diseases, which exhibit potent antibacterial activity and higher selective toxicity against Gram-positive and Gram-negative bacteria, which do not cause side effects (e.g., convulsion), which exhibit higher safety, and which has a structure of formula (I):

摘要翻译： 用于治疗感染性疾病的喹诺酮类抗菌化合物或化合物的盐或水合物，其对革兰氏阳性和革兰氏阴性菌具有强力的抗菌活性和较高的选择性毒性，其不引起副作用（例如惊厥 ），其具有更高的安全性，并且具有式（I）的结构：

公开(公告)号：US08618094B2

公开(公告)日：2013-12-31

申请号：US12459612

申请日：2009-07-02

申请人： Hisashi Takahashi ,  Satoshi Komoriya ,  Takahiro Kitamura ,  Takashi Odagiri ,  Hiroaki Inagaki ,  Toshifumi Tsuda ,  Kiyoshi Nakayama ,  Makoto Takemura ,  Kenichi Yoshida ,  Rie Miyauchi ,  Masatoshi Nagamochi

发明人： Hisashi Takahashi ,  Satoshi Komoriya ,  Takahiro Kitamura ,  Takashi Odagiri ,  Hiroaki Inagaki ,  Toshifumi Tsuda ,  Kiyoshi Nakayama ,  Makoto Takemura ,  Kenichi Yoshida ,  Rie Miyauchi ,  Masatoshi Nagamochi

IPC分类号： C07D401/10 ,  C07D498/06 ,  A61K31/4709 ,  A61K31/5383

CPC分类号： C07D498/06 ,  C07D209/02 ,  C07D209/56 ,  C07D401/04 ,  C07D401/14 ,  C07D491/048 ,  C07D491/052 ,  Y02P20/55

摘要： A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure.

摘要翻译： 提供了作为药物具有优异性能的喹诺酮合成抗菌剂，其不仅对革兰氏阴性菌具有很强的抗菌活性，而且对喹诺酮类抗菌剂具有低敏感性的革兰氏阳性球菌具有很强的抗菌活性，并且其表现出高安全性和优异的药代动力学 。 由式（I）表示的化合物或其盐或其水合物。 具体地，其中取代基R6和R7与它们所键合的碳原子一起形成式（I）的喹诺酮衍生物形成可以含有氧原子作为环组成原子的环状结构，所述环状结构形成5- 4,5,5-或5-6稠合双环吡咯烷基取代基，该取代基与含有吡啶并苯并恶嗪结构的喹诺酮母体骨架Q结合。

公开(公告)号：US20130029977A9

公开(公告)日：2013-01-31

申请号：US12459612

申请日：2009-07-02

申请人： Hisashi Takahashi ,  Satoshi Komoriya ,  Takahiro Kitamura ,  Takashi Odagiri ,  Hiroaki Inagaki ,  Toshifumi Tsuda ,  Kiyoshi Nakayama ,  Makoto Takemura ,  Kenichi Yoshida ,  Rie Miyauchi ,  Masatoshi Nagamochi

发明人： Hisashi Takahashi ,  Satoshi Komoriya ,  Takahiro Kitamura ,  Takashi Odagiri ,  Hiroaki Inagaki ,  Toshifumi Tsuda ,  Kiyoshi Nakayama ,  Makoto Takemura ,  Kenichi Yoshida ,  Rie Miyauchi ,  Masatoshi Nagamochi

IPC分类号： A61K31/4709 ,  C07D498/06 ,  A61K31/5383 ,  A61P1/12 ,  A61P29/00 ,  A61P31/04 ,  A61P31/00 ,  A61P33/00 ,  A61P17/00 ,  A61P15/00 ,  A61P17/10 ,  A61P11/08 ,  A61P11/00 ,  A61P13/08 ,  A61P13/02 ,  A61P27/02 ,  A61P1/02 ,  A61P37/00 ,  A61P31/06 ,  A61P31/08 ,  C07D401/10

CPC分类号： C07D498/06 ,  C07D209/02 ,  C07D209/56 ,  C07D401/04 ,  C07D401/14 ,  C07D491/048 ,  C07D491/052 ,  Y02P20/55

摘要： A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure.

公开(公告)号：US20120108582A1

公开(公告)日：2012-05-03

申请号：US12459612

申请日：2009-07-02

申请人： Hisashi Takahashi ,  Satoshi Komoriya ,  Takahiro Kitamura ,  Takashi Odagiri ,  Hiroaki Inagaki ,  Toshifumi Tsuda ,  Kiyoshi Nakayama ,  Makoto Takemura ,  Kenichi Yoshida ,  Rie Miyauchi ,  Masatoshi Nagamochi

发明人： Hisashi Takahashi ,  Satoshi Komoriya ,  Takahiro Kitamura ,  Takashi Odagiri ,  Hiroaki Inagaki ,  Toshifumi Tsuda ,  Kiyoshi Nakayama ,  Makoto Takemura ,  Kenichi Yoshida ,  Rie Miyauchi ,  Masatoshi Nagamochi

IPC分类号： A61K31/4709 ,  C07D498/06 ,  A61K31/5383 ,  A61P1/12 ,  A61P29/00 ,  A61P31/04 ,  A61P31/00 ,  A61P33/00 ,  A61P17/00 ,  A61P15/00 ,  A61P17/10 ,  A61P11/08 ,  A61P11/00 ,  A61P13/08 ,  A61P13/02 ,  A61P27/02 ,  A61P1/02 ,  A61P37/00 ,  A61P31/06 ,  A61P31/08 ,  C07D401/10

CPC分类号： C07D498/06 ,  C07D209/02 ,  C07D209/56 ,  C07D401/04 ,  C07D401/14 ,  C07D491/048 ,  C07D491/052 ,  Y02P20/55

摘要： A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure.

摘要翻译： 提供了作为药物具有优异性能的喹诺酮合成抗菌剂，其不仅对革兰氏阴性菌具有很强的抗菌活性，而且对喹诺酮类抗菌剂具有低敏感性的革兰氏阳性球菌具有很强的抗菌活性，并且其表现出高安全性和优异的药代动力学 。 由式（I）表示的化合物或其盐或其水合物。 具体地，其中取代基R6和R7与它们所键合的碳原子一起形成式（I）的喹诺酮衍生物形成可以含有氧原子作为环组成原子的环状结构，所述环状结构形成5- 4,5,5-或5-6稠合双环吡咯烷基取代基，该取代基与含有吡啶并苯并恶嗪结构的喹诺酮母体骨架Q结合。

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：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。