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公开(公告)号:US20090281072A1
公开(公告)日:2009-11-12
申请号:US12235189
申请日:2008-09-22
申请人: Shinya Nagashima , Hiroshi Nagata , Masashiro Iwata , Masaki Yokota , Hiroyuki Moritomo , Eiichi Nakai , Sadao Kuromitsu , Keiko Ohga , Makoto Takeuchi
发明人: Shinya Nagashima , Hiroshi Nagata , Masashiro Iwata , Masaki Yokota , Hiroyuki Moritomo , Eiichi Nakai , Sadao Kuromitsu , Keiko Ohga , Makoto Takeuchi
IPC分类号: A61K31/5377 , A61K31/551 , A61K31/397 , A61P11/06
CPC分类号: C07D403/12 , C07D239/48 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D451/04 , C07D453/02 , C07D471/10 , C07D487/08
摘要: A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided.A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.
摘要翻译: 提供了可用于预防或治疗其中涉及STAT6的呼吸系统疾病的化合物,特别是哮喘,慢性阻塞性肺病等。 具有可以被特定取代基取代的芳基氨基或芳基乙氨基的嘧啶衍生物或其盐在2-位被苄基取代的氨基或4-位上的氨基甲酰基和氨基甲酰基, 可以在5位被提供。
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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: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:US07449456B2
公开(公告)日:2008-11-11
申请号:US10518043
申请日:2003-06-26
申请人: Shinya Nagashima , Hiroshi Nagata , Masahiro Iwata , Masaki Yokota , Hiroyuki Moritomo , Eiichi Nakai , Sadao Kuromitsu , Keiko Ohga , Makoto Takeuchi
发明人: Shinya Nagashima , Hiroshi Nagata , Masahiro Iwata , Masaki Yokota , Hiroyuki Moritomo , Eiichi Nakai , Sadao Kuromitsu , Keiko Ohga , Makoto Takeuchi
IPC分类号: C07D239/48 , A61K31/506
CPC分类号: C07D403/12 , C07D239/48 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D451/04 , C07D453/02 , C07D471/10 , C07D487/08
摘要: A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided.A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.
摘要翻译: 提供了可用于预防或治疗其中涉及STAT6的呼吸系统疾病的化合物,特别是哮喘,慢性阻塞性肺病等。 具有可以被特定取代基取代的芳基氨基或芳基乙氨基的嘧啶衍生物或其盐在2-位被苄基取代的氨基或4-位上的氨基甲酰基和氨基甲酰基, 可以在5位被提供。
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公开(公告)号:US20050272753A1
公开(公告)日:2005-12-08
申请号:US10518043
申请日:2003-06-26
申请人: Shinya Nagashima , Hiroshi Nagata , Masahiro Iwata , Masaki Yokota , Hiroyuki Moritomo , Eiichi Nakai , Sadao Kuromitsu , Keiko Ohga , Makoto Takeuchi
发明人: Shinya Nagashima , Hiroshi Nagata , Masahiro Iwata , Masaki Yokota , Hiroyuki Moritomo , Eiichi Nakai , Sadao Kuromitsu , Keiko Ohga , Makoto Takeuchi
IPC分类号: A61P11/00 , A61P11/06 , A61P43/00 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D451/04 , C07D453/02 , C07D471/08 , C07D471/10 , C07D487/08 , A61K31/506 , A61K31/505 , C07D43/02
CPC分类号: C07D403/12 , C07D239/48 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D451/04 , C07D453/02 , C07D471/10 , C07D487/08
摘要: A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided. A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.
摘要翻译: 提供了可用于预防或治疗其中涉及STAT6的呼吸系统疾病的化合物,特别是哮喘,慢性阻塞性肺病等。 具有可以被特定取代基取代的芳基氨基或芳基乙氨基的嘧啶衍生物或其盐在2-位被苄基取代的氨基或4-位上的氨基甲酰基和氨基甲酰基, 可以在5位被提供。
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公开(公告)号:US06346532B1
公开(公告)日:2002-02-12
申请号:US09529096
申请日:2000-04-07
申请人: Tatsuya Maruyama , Takayuki Suzuki , Kenichi Onda , Masahiko Hayakawa , Hiroyuki Moritomo , Tetsuya Kimizuka , Tetsuo Matsui
发明人: Tatsuya Maruyama , Takayuki Suzuki , Kenichi Onda , Masahiko Hayakawa , Hiroyuki Moritomo , Tetsuya Kimizuka , Tetsuo Matsui
IPC分类号: A61K31495
CPC分类号: C07D231/12 , C07D213/30 , C07D213/56 , C07D213/81 , C07D215/48 , C07D233/26 , C07D235/16 , C07D235/30 , C07D239/26 , C07D241/12 , C07D257/04 , C07D277/36 , C07D277/82 , C07D401/04 , C07D513/04
摘要: Amide derivatives represented by general formula (I) or salts thereof wherein each symbol has the following meaning: ring B: an optionally substituted heteroaryl optionally fused with a benzene ring; X: a bond, lower alkylene or lower alkenylene optionally substituted by hydroxy or lower alkyl, carbonyl, or a group represented by —NH— (when X is lower alkylene optionally substituted by lower alkyl which may be bonded to the hydrogen atom bonded to a constituent carbon atom of ring B to form lower alkylene to thereby form a ring); A: a lower alkylene or a group represented by -(lower alkylene)—O—; R1a and R1b: the same or different and each hydrogen or lower alkyl; R2: hydrogen or halogeno; and Z: nitrogen or a group represented by ═CH—. The compounds are useful as a diabetes remedy which not only functions to both accelerate the secretion of insulin and enhance insulin sensitivity but has an antiobestic action and an antihyperlipemic action based on its selective stimulative action on a &bgr;3 receptor.
摘要翻译: 由通式(I)表示的酰胺衍生物或其盐,其中每个符号具有以下含义:环B:任选地与苯环稠合的任选取代的杂芳基; X:任选被羟基或低级烷基取代的低级亚烷基或低级亚烯基,羰基或由-NH-表示的基团(当X为任选被低级烷基取代的低级烷基时,该低级烷基可以键合到与 环B的构成碳原子形成低级亚烷基,从而形成环); A:低级亚烷基或由 - (低级亚烷基)-O-表示的基团。 R1a和R1b:相同或不同,各个氢或低级烷基; R2:氢或卤素; 和Z:氮或由= CH-表示的基团。 该化合物可用作糖尿病药物,其不仅可以加速胰岛素的分泌并增强胰岛素敏感性,而且具有基于其对β3受体的选择性刺激作用的抗胆碱作用和抗高脂血症作用。
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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:US20130029973A1
公开(公告)日:2013-01-31
申请号:US13639260
申请日:2011-04-27
申请人: Shunichiro Hachiya , Masanori Miura , Yoshimasa Imamura , Daisuke Kaga , Ippei Sato , Hiroyuki Moritomo , Koji Kato , Kazuhiro Terai , Yoh Terada
发明人: Shunichiro Hachiya , Masanori Miura , Yoshimasa Imamura , Daisuke Kaga , Ippei Sato , Hiroyuki Moritomo , Koji Kato , Kazuhiro Terai , Yoh Terada
IPC分类号: A61K31/381 , A61K31/5377 , A61K31/496 , A61K31/4535 , A61K31/444 , A61P7/00 , C07D409/12 , C07D413/14 , C07D413/12 , C07D409/14 , C07D333/66 , A61K31/55 , A61K31/4025
CPC分类号: C07D333/66 , A61K31/381 , A61K31/4025 , A61K31/4436 , A61K31/444 , A61K31/4535 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/55 , A61K31/63 , A61K31/7042 , C07D333/68 , C07D409/12
摘要: A compound has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating hyperphosphatemia, preventing hyperphosphatemia, or both. The compound is a tetrahydrobenzothiophene compound. A pharmaceutical composition for treating hyperphosphatemia includes the compound or salt thereof. A method of treating hyperphosphatemia includes administering to a subject an effective amount of the compound or salt thereof.
摘要翻译: 化合物具有肠道磷酸盐转运蛋白(NPT-IIb)抑制作用,可用作治疗高磷血症,预防高磷酸血症或二者的活性成分。 该化合物是四氢苯并噻吩化合物。 用于治疗高磷血症的药物组合物包括其化合物或其盐。 治疗高磷血症的方法包括给予受试者有效量的化合物或其盐。
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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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