公开(公告)号：US20100113391A1

公开(公告)日：2010-05-06

申请号：US12596643

申请日：2008-04-17

申请人： Yuji Koga ,  Takao Okuda ,  Takashi Kamikubo ,  Michihito Kageyama ,  Hiroyuki Moritomo

发明人： Yuji Koga ,  Takao Okuda ,  Takashi Kamikubo ,  Michihito Kageyama ,  Hiroyuki Moritomo

IPC分类号： A61K31/695 ,  C07D215/22 ,  C07D239/80 ,  C07F7/02 ,  C07D243/14 ,  A61K31/47 ,  A61K31/517 ,  A61K31/5513 ,  A61P7/02

CPC分类号： C07D217/24 ,  C07D239/96 ,  C07D243/14 ,  C07D401/06 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D413/06 ,  C07D417/06

摘要： [Problem]Provided is a compound, which exhibits a P2Y12 inhibitory action and is useful as a medical drug, particularly, as a platelet aggregation inhibitor.[Means for Solution]The inventors have eagerly investigated P2Y12 inhibitors. As a result, the inventors have found that a bicyclic heterocyclic compound such as quinazolinedione, isoquinolone, and the like having an amino group substituted with lower alkyl, cycloalkyl, or lower alkylene-cycloalkyl at the specific position exhibits an excellent platelet aggregation inhibitory action, thereby completing the present invention. Since the compound of the invention exhibits excellent P2Y12 inhibitory action and platelet aggregation inhibitory action, it is useful as a platelet aggregation inhibitor.

摘要翻译： [问题]提供了表现出P2Y12抑制作用的化合物，可用作医药，特别是作为血小板聚集抑制剂。 解决方法本发明人急切地研究P2Y12抑制剂。 结果发现，在具体位置具有被低级烷基，环烷基或低级亚烷基 - 环烷基取代的氨基的喹唑啉二酮，异喹诺酮等双环杂环化合物显示优异的血小板聚集抑制作用， 从而完成了本发明。 由于本发明化合物表现出优异的P2Y12抑制作用和血小板聚集抑制作用，因此作为血小板聚集抑制剂是有用的。

公开(公告)号：US20090197834A1

公开(公告)日：2009-08-06

申请号：US12293055

申请日：2007-03-14

申请人： Yuji Koga ,  Takao Okuda ,  Susumu Watanuki ,  Takashi Kamikubo ,  Fukushi Hirayama ,  Hiroyuki Moritomo ,  Jiro Fujiyasu ,  Michihito Kageyama ,  Toshio Uemura ,  Jun Takasaki

发明人： Yuji Koga ,  Takao Okuda ,  Susumu Watanuki ,  Takashi Kamikubo ,  Fukushi Hirayama ,  Hiroyuki Moritomo ,  Jiro Fujiyasu ,  Michihito Kageyama ,  Toshio Uemura ,  Jun Takasaki

IPC分类号： A61K31/675 ,  C07D215/22 ,  A61K31/47 ,  C07F9/60

CPC分类号： C07D513/04 ,  C07D215/22 ,  C07D215/56 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/14 ,  C07D487/04 ,  C07F7/1804 ,  C07F9/60

摘要： [Problem] To provide a compound having excellent platelet aggregation inhibitory activity.[Means for Resolution] It was found that quinolone derivatives characterized in that these have lower alkyl, cycloalkyl or the like at the 1-position; —N(R0)C(O)-lower alkylene-CO2R0, lower alkylene-CO2R0, lower alkenylene-CO2R0, —O-lower alkylene-CO2R0, —O-(lower alkylene which may be substituted with —CO2R0)-aryl or —O-lower alkenylene-CO2R0 (wherein R0 is H or lower alkyl) at the 3-position; halogen at the 6-position; and amino group substituted with a substituent group having a ring structure at the 7-position, respectively, or pharmaceutically acceptable salts thereof, has excellent P2Y12 inhibitory activity. In addition, it was confirmed that these quinolone derivatives also have excellent platelet aggregation inhibitory activity. Based on the above, these quinolone derivatives or pharmaceutically acceptable salts thereof are useful as platelet aggregation inhibitors.

摘要翻译： 提供具有优异血小板聚集抑制活性的化合物。 [解决方法]发现喹诺酮衍生物的特征在于它们在1-位具有低级烷基，环烷基等; -N（R 0）C（O） - 低级亚烷基-CO 2 R 0，低级亚烷基-CO 2 R 0，低级亚烯基-CO 2 R O，-O-低级亚烷基-CO 2 R O，-O-（可被-CO 2 R 0取代的低级亚烷基） - 芳基或 O-低级亚烯基-CO 2 R 0（其中R 0是H或低级烷基）在3-位; 6位卤素; 分别被具有7位具有环结构的取代基取代的氨基或其药学上可接受的盐具有优异的P2Y12抑制活性。 此外，证实这些喹诺酮衍生物也具有优异的血小板聚集抑制活性。 基于上述，这些喹诺酮衍生物或其药学上可接受的盐可用作血小板聚集抑制剂。

公开(公告)号：US08629126B2

公开(公告)日：2014-01-14

申请号：US13364815

申请日：2012-02-02

申请人： Yuji Koga ,  Takao Okuda ,  Susumu Watanuki ,  Takashi Kamikubo ,  Fukushi Hirayama ,  Hiroyuki Moritomo ,  Jiro Fujiyasu ,  Michihito Kageyama ,  Toshio Uemura ,  Jun Takasaki

发明人： Yuji Koga ,  Takao Okuda ,  Susumu Watanuki ,  Takashi Kamikubo ,  Fukushi Hirayama ,  Hiroyuki Moritomo ,  Jiro Fujiyasu ,  Michihito Kageyama ,  Toshio Uemura ,  Jun Takasaki

IPC分类号： A61K31/675 ,  A61K31/47

CPC分类号： C07D513/04 ,  C07D215/22 ,  C07D215/56 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/14 ,  C07D487/04 ,  C07F7/1804 ,  C07F9/60

摘要： Disclosed are quinolone derivatives characterized in that these have lower alkyl, cycloalkyl or the like at the 1-position; —N(R0)C(O)-lower alkylene-CO2R0, lower alkylene-CO2R0, lower alkenylene-CO2R0, —O-lower alkylene-CO2R0, —O-(lower alkylene which may be substituted with —CO2R0)-aryl or —O-lower alkenylene-CO2R0 (wherein R0 is H or lower alkyl) at the 3-position; halogen at the 6-position; and amino group substituted with a substituent group having a ring structure at the 7-position, respectively, or pharmaceutically acceptable salts thereof, has excellent P2Y12 inhibitory activity. The quinolone derivatives have excellent platelet aggregation inhibitory activity. A method of using the compounds is also disclosed.

摘要翻译： 公开了喹诺酮衍生物，其特征在于它们在1-位具有低级烷基，环烷基等; -N（R 0）C（O） - 低级亚烷基-CO 2 R 0，低级亚烷基-CO 2 R 0，低级亚烯基-CO 2 R O，-O-低级亚烷基-CO 2 R O，-O-（可被-CO 2 R 0取代的低级亚烷基） - 芳基或 O-低级亚烯基-CO 2 R 0（其中R 0是H或低级烷基）在3-位; 6位卤素; 分别被具有7位具有环结构的取代基取代的氨基或其药学上可接受的盐具有优异的P2Y12抑制活性。 喹诺酮衍生物具有优异的血小板聚集抑制活性。 还公开了使用该化合物的方法。

公开(公告)号：US08133882B2

公开(公告)日：2012-03-13

申请号：US12293055

申请日：2007-03-14

申请人： Yuji Koga ,  Takao Okuda ,  Susumu Watanuki ,  Takashi Kamikubo ,  Fukushi Hirayama ,  Hiroyuki Moritomo ,  Jiro Fujiyasu ,  Michihito Kageyama ,  Toshio Uemura ,  Jun Takasaki

发明人： Yuji Koga ,  Takao Okuda ,  Susumu Watanuki ,  Takashi Kamikubo ,  Fukushi Hirayama ,  Hiroyuki Moritomo ,  Jiro Fujiyasu ,  Michihito Kageyama ,  Toshio Uemura ,  Jun Takasaki

IPC分类号： A61K31/675 ,  A61K31/47 ,  C07D215/22 ,  C07F9/60

CPC分类号： C07D513/04 ,  C07D215/22 ,  C07D215/56 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/14 ,  C07D487/04 ,  C07F7/1804 ,  C07F9/60

摘要： Provided are quinolone derivatives having a lower alkyl or cycloalkyl at the 1-position; —N(R0)C(O)-lower alkylene-CO2R0, lower alkylene-CO2R0, lower alkenylene-CO2R0, —O-lower alkylene-CO2R0, —O-(lower alkylene which may be substituted with —CO2R0)-aryl or —O-lower alkenylene-CO2R0 (wherein R0 is H or lower alkyl) at the 3-position; halogen at the 6-position; and amino group substituted with a substituent group having a ring structure at the 7-position, respectively, or pharmaceutically acceptable salts thereof. Pharmaceutical composition containing the quinolone derivatives and methods of using the compositions are provided.

摘要翻译： 提供在1-位具有低级烷基或环烷基的喹诺酮衍生物; -N（R 0）C（O） - 低级亚烷基-CO 2 R 0，低级亚烷基-CO 2 R 0，低级亚烯基-CO 2 R O，-O-低级亚烷基-CO 2 R O，-O-（可被-CO 2 R 0取代的低级亚烷基） - 芳基或 O-低级亚烯基-CO 2 R 0（其中R 0是H或低级烷基）在3-位; 6位卤素; 分别被具有7-位上的环结构的取代基取代的氨基或其药学上可接受的盐。 提供了含有喹诺酮衍生物的药物组合物和使用该组合物的方法。

公开(公告)号：US07879878B2

公开(公告)日：2011-02-01

申请号：US12347428

申请日：2008-12-31

申请人： Susumu Watanuki ,  Yuji Koga ,  Hiroyuki Moritomo ,  Issei Tsukamoto ,  Daisuke Kaga ,  Takao Okuda ,  Fukushi Hirayama ,  Yumiko Moritani ,  Jun Takasaki

发明人： Susumu Watanuki ,  Yuji Koga ,  Hiroyuki Moritomo ,  Issei Tsukamoto ,  Daisuke Kaga ,  Takao Okuda ,  Fukushi Hirayama ,  Yumiko Moritani ,  Jun Takasaki

IPC分类号： A61K31/47 ,  A61K31/44 ,  C07D215/00

CPC分类号： C07D237/28 ,  A61K31/4709 ,  A61K31/4725 ,  C07D215/56 ,  C07D405/04 ,  C07F9/5765 ,  C07F9/60 ,  C07F9/650947

摘要： A platelet aggregation inhibitor comprising a quinolone derivative or a pharmaceutically acceptable salt thereof as an active ingredient, and a novel quinolone derivative or a pharmaceutically acceptable salt thereof useful as a platelet aggregation inhibitor.

摘要翻译： 包含喹诺酮衍生物或其药学上可接受的盐作为活性成分的血小板聚集抑制剂和用作血小板聚集抑制剂的新型喹诺酮衍生物或其药学上可接受的盐。

公开(公告)号：US20060148806A1

公开(公告)日：2006-07-06

申请号：US10562128

申请日：2004-07-22

申请人： Susumu Watanuki ,  Yuji Koga ,  Hiroyuki Moritomo ,  Issei Tsukamoto ,  Daisuke Kaga ,  Takao Okuda ,  Fukushi Hirayama ,  Yumiko Moritani ,  Jun Takasaki

发明人： Susumu Watanuki ,  Yuji Koga ,  Hiroyuki Moritomo ,  Issei Tsukamoto ,  Daisuke Kaga ,  Takao Okuda ,  Fukushi Hirayama ,  Yumiko Moritani ,  Jun Takasaki

IPC分类号： A61K31/503 ,  C07D471/02 ,  C07D487/02 ,  A61K31/4745

CPC分类号： C07D237/28 ,  A61K31/4709 ,  A61K31/4725 ,  C07D215/56 ,  C07D405/04 ,  C07F9/5765 ,  C07F9/60 ,  C07F9/650947

摘要： A platelet aggregation inhibitor comprising a quinolone derivative or a pharmaceutically acceptable salt thereof as an active ingredient, and a novel quinolone derivative or a pharmaceutically acceptable salt thereof useful as a platelet aggregation inhibitor.

公开(公告)号：US07488739B2

公开(公告)日：2009-02-10

申请号：US10562128

申请日：2004-07-22

申请人： Susumu Watanuki ,  Yuji Koga ,  Hiroyuki Moritomo ,  Issei Tsukamoto ,  Daisuke Kaga ,  Takao Okuda ,  Fukushi Hirayama ,  Yumiko Moritani ,  Jun Takasaki

发明人： Susumu Watanuki ,  Yuji Koga ,  Hiroyuki Moritomo ,  Issei Tsukamoto ,  Daisuke Kaga ,  Takao Okuda ,  Fukushi Hirayama ,  Yumiko Moritani ,  Jun Takasaki

IPC分类号： A61K31/47 ,  C07D215/233 ,  C07D237/28 ,  C07D407/02

CPC分类号： C07D237/28 ,  A61K31/4709 ,  A61K31/4725 ,  C07D215/56 ,  C07D405/04 ,  C07F9/5765 ,  C07F9/60 ,  C07F9/650947

摘要： A platelet aggregation inhibitor comprising a quinolone derivative or a pharmaceutically acceptable salt thereof as an active ingredient, and a novel quinolone derivative or a pharmaceutically acceptable salt thereof useful as a platelet aggregation inhibitor.

摘要翻译： 包含喹诺酮衍生物或其药学上可接受的盐作为活性成分的血小板聚集抑制剂和用作血小板聚集抑制剂的新型喹诺酮衍生物或其药学上可接受的盐。

公开(公告)号：US20060194844A1

公开(公告)日：2006-08-31

申请号：US10564520

申请日：2004-07-15

申请人： Keizo Sugasawa ,  Yuji Koga ,  Kazuyoshi Obitsu ,  Takao Okuda ,  Koichiro Harada ,  Hideki Kubota ,  Fukushi Hirayama ,  Masaki Abe ,  Ken-ichi Suzuki

发明人： Keizo Sugasawa ,  Yuji Koga ,  Kazuyoshi Obitsu ,  Takao Okuda ,  Koichiro Harada ,  Hideki Kubota ,  Fukushi Hirayama ,  Masaki Abe ,  Ken-ichi Suzuki

IPC分类号： C07D417/02 ,  A61K31/4439 ,  A61K31/426

CPC分类号： C07D417/14 ,  C07D417/04

摘要： 2-Acylaminothiazole derivatives or salts thereof which have a platelet increasing activity based on an excellent human c-mpl-Ba/F3 cell growth function and a function of accelerating formation of megakaryocytic colonies and which are useful for treating thrombocytopenia are provided.

摘要翻译： 提供了基于优异的人c-mpl-Ba / F3细胞生长功能具有血小板增加活性的2-酰基氨基噻唑衍生物或其盐，并且具有促进巨核细胞集落形成并且可用于治疗血小板减少症的功能。

公开(公告)号：US07361658B2

公开(公告)日：2008-04-22

申请号：US10564520

申请日：2004-07-15

申请人： Keizo Sugasawa ,  Yuji Koga ,  Kazuyoshi Obitsu ,  Takao Okuda ,  Koichiro Harada ,  Hideki Kubota ,  Fukushi Hirayama ,  Masaki Abe ,  Ken-ichi Suzuki

发明人： Keizo Sugasawa ,  Yuji Koga ,  Kazuyoshi Obitsu ,  Takao Okuda ,  Koichiro Harada ,  Hideki Kubota ,  Fukushi Hirayama ,  Masaki Abe ,  Ken-ichi Suzuki

IPC分类号： A61K31/4427 ,  A61K31/4523 ,  A61K31/496 ,  C07D403/12 ,  C07D401/12 ,  C07D211/26 ,  C07D401/14

CPC分类号： C07D417/14 ,  C07D417/04

摘要： 2-Acylaminothiazole derivatives or salts thereof which have a platelet increasing activity based on an excellent human c-mpl-Ba/F3 cell growth function and a function of accelerating formation of megakaryocytic colonies and which are useful for treating thrombocytopenia are provided.

摘要翻译： 提供了基于优异的人c-mpl-Ba / F3细胞生长功能具有血小板增加活性的2-酰基氨基噻唑衍生物或其盐，并且具有促进巨核细胞集落形成并且可用于治疗血小板减少症的功能。

公开(公告)号：US09248676B2

公开(公告)日：2016-02-02

申请号：US14816592

申请日：2015-08-03

申请人： Yuji Koga ,  Masatoshi Izuchi

发明人： Yuji Koga ,  Masatoshi Izuchi

IPC分类号： B41J19/00 ,  B41J23/04 ,  B41J9/14 ,  B41J13/00 ,  B41J23/14 ,  B41J25/34 ,  B41J11/48 ,  B41J25/00 ,  B41J2/01

CPC分类号： B41J25/006 ,  B41J2/01 ,  B41J11/485 ,  B41J13/0018 ,  B41J13/009 ,  B41J19/202 ,  B41J23/02 ,  B41J23/14 ,  B41J25/001 ,  B41J25/34

摘要： A printer has a carriage being movable between a first end and a second end of a reciprocating path; and a driving force transmitting path selecting mechanism provided at the second end of the reciprocating path. The selecting mechanism has: a common driving force outputting member; a plurality of force receiving members; a selecting member; and a position retainer for keeping the position of the selecting member. The selecting member connects the force outputting member to one of the plurality of force receiving members, and moves in association with the carriage when the carriage moves in a vicinity of the second end in a first direction extending from the first end to the second end. The position retainer keeps the position of the selecting member when the carriage moves in a second direction extending from the second end to the first end. The force receiving member connected to the force outputting member via the selecting member is selected in accordance with a movement of the carriage along the reciprocating path.