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公开(公告)号:US08097592B2
公开(公告)日:2012-01-17
申请号:US12296056
申请日:2007-04-04
申请人: Masakazu Imamura , Keita Nakanishi , Ryota Shiraki , Kenichi Onda , Daisuke Sasuga , Masamichi Yuda
发明人: Masakazu Imamura , Keita Nakanishi , Ryota Shiraki , Kenichi Onda , Daisuke Sasuga , Masamichi Yuda
CPC分类号: C07D207/16 , C07D409/10
摘要: A cocrystal of (1S)-1,5-anhydro-1-[3-(1-benzothien-2-ylmethyl)-4-fluorophenyl]-D-glucitol and L-proline. It is a cocrystal of known compound A, which has a constant quality, is superior in storage stability, has no moisture absorptivity, and is suitable as a crystal of a drug substance used for preparing pharmaceuticals.
摘要翻译: (1S)-1,5-脱水-1- [3-(1-苯并噻吩-2-基甲基)-4-氟苯基] -D-葡萄糖醇和L-脯氨酸的共结晶体。 已知的化合物A的共晶体具有恒定的质量,储存稳定性优异,不具有吸湿性,并且适合作为用于制备药物的药物的晶体。
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公开(公告)号:US20090143316A1
公开(公告)日:2009-06-04
申请号:US12296056
申请日:2007-04-04
申请人: Masakazu Imamura , Keita Nakanishi , Ryota Shiraki , Kenichi Onda , Daisuke Sasuga , Masamichi Yuda
发明人: Masakazu Imamura , Keita Nakanishi , Ryota Shiraki , Kenichi Onda , Daisuke Sasuga , Masamichi Yuda
IPC分类号: A61K31/7004 , C07H17/02 , A61P3/10
CPC分类号: C07D207/16 , C07D409/10
摘要: A cocrystal of (1S)-1,5-anhydro-1-[3-(1-benzothien-2-ylmethyl)-4-fluorophenyl]-D-glucitol and L-proline. It is a cocrystal of known compound A, which has a constant quality, is superior in storage stability, has no moisture absorptivity, and is suitable as a crystal of a drug substance used for preparing pharmaceuticals.
摘要翻译: (1S)-1,5-脱水-1- [3-(1-苯并噻吩-2-基甲基)-4-氟苯基] -D-葡萄糖醇和L-脯氨酸的共结晶体。 已知的化合物A的共晶体具有恒定的质量,储存稳定性优异,不具有吸湿性,并且适合作为用于制备药物的药物的晶体。
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公开(公告)号:US20070249587A1
公开(公告)日:2007-10-25
申请号:US11576889
申请日:2005-10-05
申请人: Yasuhiro Yonetoku , Kenji Negoro , Kenichi Onda , Masahiko Hayakawa , Daisuke Sasuga , Takahiro Nigawara , Kazuhiko Iikubo , Hiroyuki Moritomo , Shigeru Yoshida , Takahide Ohishi
发明人: Yasuhiro Yonetoku , Kenji Negoro , Kenichi Onda , Masahiko Hayakawa , Daisuke Sasuga , Takahiro Nigawara , Kazuhiko Iikubo , Hiroyuki Moritomo , Shigeru Yoshida , Takahide Ohishi
IPC分类号: A61K31/517 , A61K31/519 , A61K31/55 , A61P3/10 , C07D403/02 , C07D471/04 , C07D495/04
CPC分类号: C07D471/04 , C07D495/04 , C07D513/04
摘要: There are provided novel pyrimidine derivatives which has been fused with an aromatic heterocycle selected from thiophene, thiazole and pyridine or pharmaceutically acceptable salts thereof; and a pharmaceutical composition comprising said compound as an active ingredient. These compounds exhibit excellent promoting activity on insulin secretion and activity against hyperglycemia. Hence, the pharmaceutical compositions comprising such compounds as active ingredients, based on these actions, are useful for treating and/or preventing insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes), insulin-resistant diseases, obesity, and the like.
摘要翻译: 提供已经与选自噻吩,噻唑和吡啶的芳族杂环或其药学上可接受的盐融合的新的嘧啶衍生物; 以及包含所述化合物作为活性成分的药物组合物。 这些化合物对胰岛素分泌表现出优异的促进活性和抗高血糖的活性。 因此,基于这些作用,包含这些化合物作为活性成分的药物组合物可用于治疗和/或预防胰岛素依赖性糖尿病(1型糖尿病),非胰岛素依赖性糖尿病(2型糖尿病),胰岛素抵抗 疾病,肥胖等。
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公开(公告)号:US07557112B2
公开(公告)日:2009-07-07
申请号:US11576889
申请日:2005-10-05
申请人: Yasuhiro Yonetoku , Kenji Negoro , Kenichi Onda , Masahiko Hayakawa , Daisuke Sasuga , Takahiro Nigawara , Kazuhiko Iikubo , Hiroyuki Moritomo , Shigeru Yoshida , Takahide Ohishi
发明人: Yasuhiro Yonetoku , Kenji Negoro , Kenichi Onda , Masahiko Hayakawa , Daisuke Sasuga , Takahiro Nigawara , Kazuhiko Iikubo , Hiroyuki Moritomo , Shigeru Yoshida , Takahide Ohishi
IPC分类号: A61P3/10 , C07D495/04 , C07D279/12 , C07D417/04 , C07D413/04 , A61K31/541 , A61K31/5355 , A61K31/519
CPC分类号: C07D471/04 , C07D495/04 , C07D513/04
摘要: There are provided novel pyrimidine derivatives which has been fused with an aromatic heterocycle selected from thiophene, thiazole and pyridine or pharmaceutically acceptable salts thereof; and a pharmaceutical composition comprising said compound as an active ingredient. These compounds exhibit excellent promoting activity on insulin secretion and activity against hyperglycemia. Hence, the pharmaceutical compositions comprising such compounds as active ingredients, based on these actions, are useful for treating and/or preventing insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes), insulin-resistant diseases, obesity, and the like.
摘要翻译: 提供已经与选自噻吩,噻唑和吡啶的芳族杂环或其药学上可接受的盐融合的新的嘧啶衍生物; 以及包含所述化合物作为活性成分的药物组合物。 这些化合物对胰岛素分泌表现出优异的促进活性和抗高血糖的活性。 因此,基于这些作用,包含这些化合物作为活性成分的药物组合物可用于治疗和/或预防胰岛素依赖性糖尿病(1型糖尿病),非胰岛素依赖型糖尿病(2型糖尿病),胰岛素抵抗 疾病,肥胖等。
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公开(公告)号:US07947690B2
公开(公告)日:2011-05-24
申请号:US11577648
申请日:2005-10-17
申请人: Yasuhiro Yonetoku , Kenji Negoro , Kenichi Onda , Masahiko Hayakawa , Daisuke Sasuga , Takahiro Nigawara , Kazuhiko Iikubo , Hiroyuki Moritomo , Shigeru Yoshida , Takahide Ohishi
发明人: Yasuhiro Yonetoku , Kenji Negoro , Kenichi Onda , Masahiko Hayakawa , Daisuke Sasuga , Takahiro Nigawara , Kazuhiko Iikubo , Hiroyuki Moritomo , Shigeru Yoshida , Takahide Ohishi
IPC分类号: A61K31/519 , A61K31/497 , C07D495/04 , A61P3/10 , C07D487/04 , C07D471/04 , C07D239/72 , A61K31/517
CPC分类号: C07D239/70 , C07D239/94 , C07D495/04
摘要: The present invention provides a condensed pyrimidine compound represented by formula (I) or pharmaceutically acceptable salt thereof: where A represents a ring where at least one carbon atom within said ring is optionally substituted with one or more groups selected from the group consisting of lower alkyl, —O-(lower alkyl), halogen atom, carboxyl, —CO2-(lower alkyl), and carbamoyl, R1 represents: (1) phenyl substituted with at least three halogen atoms, which may have at least one additional substituent, or (2) cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl, each of which is optionally substituted; and R2 represents a group represented by formula (II) or an optionally substituted cyclic amino: wherein R21 and R22 may be identical or different and each represents —H, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, phenyl, heteroaryl, non-aromatic heterocyclyl, or —O-(lower alkyl), each of which is optionally substituted.
摘要翻译: 本发明提供由式(I)表示的稠合嘧啶化合物或其药学上可接受的盐:其中A表示环,其中所述环中至少一个碳原子任选被一个或多个选自以下的基团取代:低级烷基 ,-O-(低级烷基),卤素原子,羧基,-CO 2 - (低级烷基)和氨基甲酰基,R 1表示:(1)被至少三个卤素原子取代的苯基,其可以具有至少一个另外的取代基,或 (2)环丙基,环丁基,环戊基,环己基或环庚基,其各自任选被取代; 并且R 2表示由式(II)表示的基团或任选取代的环状氨基:其中R 21和R 22可以相同或不同,并且各自表示-H,低级烷基,低级烯基,低级炔基,环烷基,苯基,杂芳基, 芳族杂环基或-O-(低级烷基),其各自任选被取代。
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公开(公告)号:US20080070896A1
公开(公告)日:2008-03-20
申请号:US11577648
申请日:2005-10-17
申请人: Yasuhiro Yonetoku , Kenji Negoro , Kenichi Onda , Masahiko Hayakawa , Daisuke Sasuga , Takahiro Nigawara , Kazuhiko Iikubo , Hiroyuki Moritomo , Shigeru Yoshida , Takahide Ohishi
发明人: Yasuhiro Yonetoku , Kenji Negoro , Kenichi Onda , Masahiko Hayakawa , Daisuke Sasuga , Takahiro Nigawara , Kazuhiko Iikubo , Hiroyuki Moritomo , Shigeru Yoshida , Takahide Ohishi
IPC分类号: A61K31/519 , A61K31/497 , A61K31/5377 , A61K31/551 , A61P3/00 , C07D285/36 , C07D413/14 , C07D495/04 , C07D487/04 , C07D403/04 , C07D239/70 , A61K31/554 , A61K31/55 , A61K31/517
CPC分类号: C07D239/70 , C07D239/94 , C07D495/04
摘要: There are provided new pyrimidine derivatives condensed with a non-aromatic ring selected from dihydrothiophene, dihydrofuran, cycloalkane moiety, and the like or pharmaceutically acceptable salts thereof; and a pharmaceutical composition comprising said compound as an active ingredient. These compounds exhibit excellent promoting activity on insulin secretion and activity against hyperglycemia. Hence, the pharmaceutical compositions comprising such compounds as active ingredients, based on these actions, are useful for treating and/or preventing insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes), insulin-resistant diseases, obesity, and the like.
摘要翻译: 提供了与选自二氢噻吩,二氢呋喃,环烷烃部分等的非芳香环稠合的新的嘧啶衍生物或其药学上可接受的盐; 以及包含所述化合物作为活性成分的药物组合物。 这些化合物对胰岛素分泌表现出优异的促进活性和抗高血糖的活性。 因此,基于这些作用,包含这些化合物作为活性成分的药物组合物可用于治疗和/或预防胰岛素依赖性糖尿病(1型糖尿病),非胰岛素依赖性糖尿病(2型糖尿病),胰岛素抵抗 疾病,肥胖等。
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公开(公告)号:US20100256113A1
公开(公告)日:2010-10-07
申请号:US12680301
申请日:2008-09-25
申请人: Kenichi Onda , Kenichiro Imamura , Fumie Sato , Hiroyuki Moritomo , Yasuharu Urano , Yuki Sawada , Naoki Ishibashi , Keita Nakanishi , Kazuhiro Yokoyama , Shigetada Furukawa , Kazuhiro Momose
发明人: Kenichi Onda , Kenichiro Imamura , Fumie Sato , Hiroyuki Moritomo , Yasuharu Urano , Yuki Sawada , Naoki Ishibashi , Keita Nakanishi , Kazuhiro Yokoyama , Shigetada Furukawa , Kazuhiro Momose
IPC分类号: A61K31/4709 , C07D215/233 , C07D405/12 , C07D401/12 , C07D413/12 , A61K31/47 , A61K31/506 , A61K31/5377 , A61K31/496 , A61K31/4725 , A61K31/55 , A61K31/553
CPC分类号: C07D401/12 , C07D215/233 , C07D401/06 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D491/107
摘要: As a result of extensive studies on NAD(P)H oxidase inhibitors, the present inventors found that a quinolone derivative having, at the 2-position, an alkyl group substituted with a heteroatom or the like has an excellent NAD(P)H oxidase inhibitory activity, and accomplished the present invention. The compound of the present invention has a reactive oxygen species production inhibitory activity based on the NAD(P)H oxidase inhibitory activity, and therefore can be used as an agent for preventing and/or treating diabetes, impaired glucose tolerance, hyperlipidemia, fatty liver, diabetic complications and the like.
摘要翻译: 作为对NAD(P)H氧化酶抑制剂的广泛研究的结果,本发明人发现,在2位具有被杂原子等取代的烷基的喹诺酮衍生物具有优异的NAD(P)H氧化酶 抑制活性,完成了本发明。 本发明的化合物具有基于NAD(P)H氧化酶抑制活性的活性氧产生抑制活性,因此可用作糖尿病预防和/或治疗药物,糖耐量异常,高脂血症,脂肪肝 ,糖尿病并发症等。
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公开(公告)号:US08367702B2
公开(公告)日:2013-02-05
申请号:US12680301
申请日:2008-09-25
申请人: Kenichi Onda , Kenichiro Imamura , Fumie Sato , Hiroyuki Moritomo , Yasuharu Urano , Yuki Sawada , Naoki Ishibashi , Keita Nakanishi , Kazuhiro Yokoyama , Shigetada Furukawa , Kazuhiro Momose
发明人: Kenichi Onda , Kenichiro Imamura , Fumie Sato , Hiroyuki Moritomo , Yasuharu Urano , Yuki Sawada , Naoki Ishibashi , Keita Nakanishi , Kazuhiro Yokoyama , Shigetada Furukawa , Kazuhiro Momose
IPC分类号: A61K31/04 , C07D215/38
CPC分类号: C07D401/12 , C07D215/233 , C07D401/06 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D491/107
摘要: As a result of extensive studies on NAD(P)H oxidase inhibitors, the present inventors found that a quinolone derivative having, at the 2-position, an alkyl group substituted with a heteroatom or the like has an excellent NAD(P)H oxidase inhibitory activity, and accomplished the present invention. The compound of the present invention has a reactive oxygen species production inhibitory activity based on the NAD(P)H oxidase inhibitory activity, and therefore can be used as an agent for preventing and/or treating diabetes, impaired glucose tolerance, hyperlipidemia, fatty liver, diabetic complications and the like.
摘要翻译: 作为对NAD(P)H氧化酶抑制剂的广泛研究的结果,本发明人发现,在2位具有被杂原子等取代的烷基的喹诺酮衍生物具有优异的NAD(P)H氧化酶 抑制活性,完成了本发明。 本发明的化合物具有基于NAD(P)H氧化酶抑制活性的活性氧产生抑制活性,因此可用作糖尿病预防和/或治疗药物,糖耐量异常,高脂血症,脂肪肝 ,糖尿病并发症等。
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公开(公告)号:US20100244396A1
公开(公告)日:2010-09-30
申请号:US12748803
申请日:2010-03-29
申请人: Kenichi Onda , Kensuke Ohkubo
发明人: Kenichi Onda , Kensuke Ohkubo
IPC分类号: B60G3/14
CPC分类号: B60G3/285 , B60G2200/182 , B60G2200/422 , B60G2204/15 , B60G2204/43 , B60G2206/60
摘要: A trailing arm type suspension improves the handling (driving stability) and the response (driving response) of an automobile by increasing the installation rigidity of a suspension member to a vehicle body frame. In the trailing arm type suspension including a pair of right and left trailing arms which extend in the vehicle longitudinal direction, a reinforcing bar for connecting a suspension member in the vehicle rear side of the trailing arm to a connecting part of a vehicle body frame in the vehicle front side of the suspension member, is disposed between a fuel tank and the trailing arm, and the reinforcing bar and the trailing arm overlap each other as viewed from the side of the vehicle.
摘要翻译: 拖臂式悬架通过将悬挂构件的安装刚性增加到车身框架来改善汽车的操纵(行驶稳定性)和响应(行驶响应)。 在包括在车辆纵向方向上延伸的一对左右拖臂的拖臂型悬架中,用于将拖曳臂的车辆后侧中的悬挂构件连接到车身框架的连接部分的钢筋 悬挂构件的车辆前侧设置在燃料箱和后臂之间,并且从车辆侧观察钢筋和后臂彼此重叠。
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公开(公告)号:US07053502B2
公开(公告)日:2006-05-30
申请号:US10809863
申请日:2004-03-26
申请人: Nobuyuki Aihara , Takeshi Onaka , Norikazu Tokunaga , Kenichi Onda , Satoru Masuyama , Shigekazu Zemba
发明人: Nobuyuki Aihara , Takeshi Onaka , Norikazu Tokunaga , Kenichi Onda , Satoru Masuyama , Shigekazu Zemba
IPC分类号: H02J1/12
CPC分类号: H02J9/061 , Y10T307/516 , Y10T307/615 , Y10T307/625
摘要: A power supply provided with: an AC/DC converter which receives AC power, converts the AC power into DC power, and outputs the DC power; a DC/DC converter which receives the DC power from the AC/DC converter, and controls a level of an output voltage of the DC/DC converter to be equal to a level of a voltage to be used by a load while the DC/DC converter supplies the output voltage to the load; a DC converter which is connected to an input of the DC/DC converter; and a DC power storage means which supplies electric power to the DC/DC converter through the DC converter.
摘要翻译: 一种电源,具有:AC / DC转换器,其接收AC电力,将AC电力转换为DC电力,并输出DC电力; DC / DC转换器,其接收来自AC / DC转换器的DC电力,并且将DC / DC转换器的输出电压的电平控制为等于由负载使用的电压的电平,同时DC / DC转换器将输出电压提供给负载; DC转换器,连接到DC / DC转换器的输入端; 以及通过DC转换器向DC / DC转换器供电的直流电力存储单元。
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