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公开(公告)号:US08598355B2
公开(公告)日:2013-12-03
申请号:US12992388
申请日:2009-05-12
申请人: Eisuke Nozawa , Ryotaro Ibuka , Kazuhiro Ikegai , Keisuke Matsuura , Tatsuya Zenkoh , Ryushi Seo , Susumu Watanuki , Michihito Kageyama
发明人: Eisuke Nozawa , Ryotaro Ibuka , Kazuhiro Ikegai , Keisuke Matsuura , Tatsuya Zenkoh , Ryushi Seo , Susumu Watanuki , Michihito Kageyama
IPC分类号: C07D215/38
CPC分类号: C07D401/06 , C07C233/47 , C07C233/87 , C07C235/42 , C07C235/52 , C07C235/66 , C07C271/14 , C07C271/22 , C07C2601/02 , C07C2602/08 , C07D207/34 , C07D209/08 , C07D213/64 , C07D215/48 , C07D217/04 , C07D231/14 , C07D235/24 , C07D263/58 , C07D333/68 , C07D333/70 , C07D401/12 , C07D403/12 , C07D405/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D417/06 , C07D471/04 , C07D491/048
摘要: [Problems] A compound, which is useful as an active ingredient of a pharmaceutical composition, for example, a pharmaceutical composition for treating chronic renal failure and/or diabetic nephropathy, is provided.[Solving Means] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic activity, and confirmed that the amide compound of the present invention has an EP4 receptor antagonistic activity, thereby completing the present invention. The amide compound of the present invention has an EP4 receptor antagonistic activity, and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating various EP4-related diseases, for example, chronic renal failure and/or diabetic nephropathy, and the like.
摘要翻译: [问题]提供了可用作药物组合物的活性成分例如用于治疗慢性肾衰竭和/或糖尿病性肾病的药物组合物的化合物。 本发明人对具有EP4受体拮抗作用的化合物进行了广泛的研究,证实本发明的酰胺化合物具有EP4受体拮抗作用,从而完成了本发明。 本发明的酰胺化合物具有EP4受体拮抗作用,可用作预防和/或治疗各种EP4相关疾病例如慢性肾衰竭和/或糖尿病性肾病的药物组合物的活性成分, 等等。
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公开(公告)号:US20100222361A1
公开(公告)日:2010-09-02
申请号:US12615968
申请日:2009-11-10
申请人: Keizo SUGASAWA , Susumu WATANUKI , Yuji KOGA , Hiroshi NAGATA , Ryutaro WAKAYAMA , Fukushi HIRAYAMA , Ken-ichi SUZUKI
发明人: Keizo SUGASAWA , Susumu WATANUKI , Yuji KOGA , Hiroshi NAGATA , Ryutaro WAKAYAMA , Fukushi HIRAYAMA , Ken-ichi SUZUKI
IPC分类号: A61K31/497 , A61P7/00
CPC分类号: C07D417/14 , A61K31/426 , A61K31/427 , A61K31/439 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/695 , C07D277/46 , C07D417/04 , C07D417/12 , C07D453/02
摘要: A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia.
摘要翻译: 基于促进巨核细胞集落形成的效果,具有对人c-mpl-Ba / F3细胞增殖的优异效果的2-酰基氨基噻唑衍生物或其药学上可接受的盐和增加血小板的活性。 用于治疗血小板减少症的化合物或其药学上可接受的盐。
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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.
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公开(公告)号:US08338429B2
公开(公告)日:2012-12-25
申请号:US12615968
申请日:2009-11-10
申请人: Keizo Sugasawa , Susumu Watanuki , Yuji Koga , Hiroshi Nagata , Ryutaro Wakayama , Fukushi Hirayama , Ken-ichi Suzuki
发明人: Keizo Sugasawa , Susumu Watanuki , Yuji Koga , Hiroshi Nagata , Ryutaro Wakayama , Fukushi Hirayama , Ken-ichi Suzuki
IPC分类号: A61K31/496 , C07D417/14
CPC分类号: C07D417/14 , A61K31/426 , A61K31/427 , A61K31/439 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/695 , C07D277/46 , C07D417/04 , C07D417/12 , C07D453/02
摘要: A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia.
摘要翻译: 基于促进巨核细胞集落形成的效果,具有对人c-mpl-Ba / F3细胞增殖的优异效果的2-酰基氨基噻唑衍生物或其药学上可接受的盐和增加血小板的活性。 用于治疗血小板减少症的化合物或其药学上可接受的盐。
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公开(公告)号:US20120136025A1
公开(公告)日:2012-05-31
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: A61K31/47 , A61P9/00 , A61P7/02 , C07D215/22
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。
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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。
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公开(公告)号:US20100222329A1
公开(公告)日:2010-09-02
申请号:US12615979
申请日:2009-11-10
申请人: Keizo Sugasawa , Susumu Watanuki , Yuji Koga , Hiroshi Nagata , Ryutaro Wakayama , Fukushi Hirayama , Ken-ichi Suzuki
发明人: Keizo Sugasawa , Susumu Watanuki , Yuji Koga , Hiroshi Nagata , Ryutaro Wakayama , Fukushi Hirayama , Ken-ichi Suzuki
IPC分类号: A61K31/427 , C07D417/14 , C07D417/12 , C07D453/02 , C07D417/04 , A61K31/55 , A61K31/5377 , A61K31/454 , A61K31/439 , A61K31/496 , A61P7/00
CPC分类号: C07D417/14 , A61K31/426 , A61K31/427 , A61K31/439 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/695 , C07D277/46 , C07D417/04 , C07D417/12 , C07D453/02
摘要: A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia.
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公开(公告)号:US07638536B2
公开(公告)日:2009-12-29
申请号:US10500964
申请日:2003-01-15
申请人: Keizo Sugasawa , Susumu Watanuki , Yuji Koga , Hiroshi Nagata , Kazuyoshi Obitsu , Ryutaro Wakayama , Fukushi Hirayama , Ken-ichi Suzuki
发明人: Keizo Sugasawa , Susumu Watanuki , Yuji Koga , Hiroshi Nagata , Kazuyoshi Obitsu , Ryutaro Wakayama , Fukushi Hirayama , Ken-ichi Suzuki
IPC分类号: A61K31/496 , A61K31/4545 , C07D417/14
CPC分类号: C07D417/14 , A61K31/426 , A61K31/427 , A61K31/439 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/695 , C07D277/46 , C07D417/04 , C07D417/12 , C07D453/02
摘要: A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia.
摘要翻译: 基于促进巨核细胞集落形成的效果,具有对人c-mpl-Ba / F3细胞增殖的优异效果的2-酰基氨基噻唑衍生物或其药学上可接受的盐和增加血小板的活性。 用于治疗血小板减少症的化合物或其药学上可接受的盐。
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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。
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公开(公告)号:US20050153977A1
公开(公告)日:2005-07-14
申请号:US10500964
申请日:2003-01-15
申请人: Keizo Sugasawa , Susumu Watanuki , Yuji Koga , Hiroshi Nagata , Kazuyoshi Obitsu , Ryutaro Wakayama , Fukushi Hirayama , Ken-ichi Suzuki
发明人: Keizo Sugasawa , Susumu Watanuki , Yuji Koga , Hiroshi Nagata , Kazuyoshi Obitsu , Ryutaro Wakayama , Fukushi Hirayama , Ken-ichi Suzuki
IPC分类号: A61K31/426 , A61K31/427 , A61K31/439 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/695 , A61P7/00 , A61P43/00 , C07D277/44 , C07D277/46 , C07D417/04 , C07D417/12 , C07D417/14 , C07D453/02
CPC分类号: C07D417/14 , A61K31/426 , A61K31/427 , A61K31/439 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/695 , C07D277/46 , C07D417/04 , C07D417/12 , C07D453/02
摘要: A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia.
摘要翻译: 基于促进巨核细胞集落形成的效果,具有对人c-mpl-Ba / F3细胞增殖的优异效果的2-酰基氨基噻唑衍生物或其药学上可接受的盐和增加血小板的活性。 用于治疗血小板减少症的化合物或其药学上可接受的盐。
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