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公开(公告)号:US20110105460A1
公开(公告)日:2011-05-05
申请号:US13002373
申请日:2009-07-02
申请人: Seiji Yoshimura , Noriyuki Kawano , Tomoaki Kawano , Daisuke Sasuga , Takanori Koike , Hideyuki Watanabe , Hiroki Fukudome , Nobuyuki Shiraishi , Ryosuke Munakata , Hiroaki Hoshii , Kayoko Mihara
发明人: Seiji Yoshimura , Noriyuki Kawano , Tomoaki Kawano , Daisuke Sasuga , Takanori Koike , Hideyuki Watanabe , Hiroki Fukudome , Nobuyuki Shiraishi , Ryosuke Munakata , Hiroaki Hoshii , Kayoko Mihara
IPC分类号: A61K31/4196 , C07D401/12 , A61K31/4439 , C07D249/08 , C07D403/12 , A61K31/506 , C07D413/12 , A61K31/422 , A61K31/4245 , A61K31/5377 , C07D417/12 , A61K31/541 , C07D405/12 , A61K31/427 , C07D413/14 , C07D409/04 , C07D403/10 , C07D471/04 , A61K31/437 , A61P3/10 , A61P25/24 , A61P25/18 , A61P25/28
CPC分类号: C07D249/08 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/10 , C07D417/12
摘要: [Problem] A compound, which can be used for preventing or treating diseases, in which 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided.[Means for Solution] It was found that a triazole derivative, in which one of the 3- and 5-positions of the triazole ring has (di)alkylmethyl or cycloalkyl, each of which is substituted with —O— (aryl or a heterocyclic group, each of which may be substituted, or lower alkylene-cycloalkyl), and the other thereof has aryl, a heterocyclic group or cycloalkyl, each of which may be substituted, or a pharmaceutically acceptable salt thereof exhibits potent 11β-HSD1 inhibitory action. From the above, the triazole derivative of the present invention can be used for preventing or treating diabetes, insulin resistance, dementia, schizophrenia and depression.
摘要翻译: [问题]提供了一种可用于预防或治疗疾病的化合物,其中涉及11种β-羟基类固醇脱氢酶(11&bgr-HSD1),特别是糖尿病,胰岛素抵抗,痴呆,精神分裂症和抑郁症 。 [解决方案]发现三唑环的3-和5-位之一具有(二)烷基甲基或环烷基的三唑衍生物,其各自被-O-(芳基或杂环) 基团,其各自可以被取代,或低级亚烷基 - 环烷基),另一个具有可以被取代的芳基,杂环基或环烷基,或其药学上可接受的盐显示出有效的11β-HSD1抑制作用 。 由上可知,本发明的三唑衍生物可用于预防或治疗糖尿病,胰岛素抵抗,痴呆,精神分裂症和抑郁症。
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公开(公告)号:US08377923B2
公开(公告)日:2013-02-19
申请号:US13002373
申请日:2009-07-02
申请人: Seiji Yoshimura , Noriyuki Kawano , Tomoaki Kawano , Daisuke Sasuga , Takanori Koike , Hideyuki Watanabe , Hiroki Fukudome , Nobuyuki Shiraishi , Ryosuke Munakata , Hiroaki Hoshii , Kayoko Mihara
发明人: Seiji Yoshimura , Noriyuki Kawano , Tomoaki Kawano , Daisuke Sasuga , Takanori Koike , Hideyuki Watanabe , Hiroki Fukudome , Nobuyuki Shiraishi , Ryosuke Munakata , Hiroaki Hoshii , Kayoko Mihara
IPC分类号: A01N43/00 , A01N43/58 , A61K31/55 , C07D241/36 , C07D249/08 , C07D249/14
CPC分类号: C07D249/08 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/10 , C07D417/12
摘要: [Problem] A compound, which can be used for preventing or treating diseases, in which 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided.[Means for Solution] It was found that a triazole derivative, in which one of the 3- and 5-positions of the triazole ring has (di)alkylmethyl or cycloalkyl, each of which is substituted with —O— (aryl or a heterocyclic group, each of which may be substituted, or lower alkylene-cycloalkyl), and the other thereof has aryl, a heterocyclic group or cycloalkyl, each of which may be substituted, or a pharmaceutically acceptable salt thereof exhibits potent 11β-HSD1 inhibitory action. From the above, the triazole derivative of the present invention can be used for preventing or treating diabetes, insulin resistance, dementia, schizophrenia and depression.
摘要翻译: [问题]提供了一种可用于预防或治疗疾病的化合物,其中涉及11种β-羟基类固醇脱氢酶(11&bgr-HSD1),特别是糖尿病,胰岛素抵抗,痴呆,精神分裂症和抑郁症 。 [解决方案]发现三唑环的3-和5-位之一具有(二)烷基甲基或环烷基的三唑衍生物,其各自被-O-(芳基或杂环) 基团,其各自可以被取代,或低级亚烷基 - 环烷基),另一个具有可以被取代的芳基,杂环基或环烷基,或其药学上可接受的盐显示出有效的11β-HSD1抑制作用 。 由上可知,本发明的三唑衍生物可用于预防或治疗糖尿病,胰岛素抵抗,痴呆,精神分裂症和抑郁症。
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公开(公告)号:US20090082367A1
公开(公告)日:2009-03-26
申请号:US12293214
申请日:2007-03-14
申请人: Seiji Yoshimura , Ryota Shiraki , Tomoaki Kawano , Daisuke Sasuga , Mitsuru Hosaka , Hiroki Fukudome , Kazuo Kurosawa , Hirofumi Ishii , Takanori Koike
发明人: Seiji Yoshimura , Ryota Shiraki , Tomoaki Kawano , Daisuke Sasuga , Mitsuru Hosaka , Hiroki Fukudome , Kazuo Kurosawa , Hirofumi Ishii , Takanori Koike
IPC分类号: A61K31/4196 , C07D401/06 , A61K31/4439 , A61K31/497 , A61P3/10 , A61K31/4709 , C07D403/06
CPC分类号: C07D249/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/08 , C07D409/06 , C07D409/08 , C07D409/12 , C07D413/06 , C07D417/06
摘要: [Problem] To provide a compound which may be used in treating diseases in which 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is concerned, especially diabetes and insulin resistance.[Means for Solution] It was found that a triazole derivative or a pharmaceutically acceptable salt thereof, in which the 3-position of triazole ring is substituted with a trisubstituted methyl group and the 5-position is substituted with a lower alkyl, cycloalkyl or the like, has a strong 11β-HSD1-inhibitory activity. In addition, since the triazole derivative of the present invention shows excellent blood glucose-lowering action, it may be used in the treatment of diabetes and insulin resistance.
摘要翻译: [问题]提供可用于治疗其中涉及11β-羟类固醇脱氢酶1型(11beta-HSD1)的疾病的化合物,特别是糖尿病和胰岛素抵抗。 [解决方法]发现三唑环的3-位被三取代甲基取代的三唑衍生物或其药学上可接受的盐,并且5位被低级烷基,环烷基或 具有强的11beta-HSD1抑制活性。 此外,由于本发明的三唑衍生物显示出优异的降血糖作用,因此可用于治疗糖尿病和胰岛素抵抗。
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公开(公告)号:US20120277208A1
公开(公告)日:2012-11-01
申请号:US13513667
申请日:2010-12-09
申请人: Masahiko Hayakawa , Seiji Yoshimura , Daisuke Sasuga , Takanori Koike , Takahiro Nigawara , Mitsuaki Okumura , Keisuke Maki
发明人: Masahiko Hayakawa , Seiji Yoshimura , Daisuke Sasuga , Takanori Koike , Takahiro Nigawara , Mitsuaki Okumura , Keisuke Maki
IPC分类号: A61K31/497 , A61P3/04 , A61P3/10 , C07D241/20 , A61K31/4965 , C07D413/14 , A61K31/4439 , C07D405/14 , A61K31/5377 , C07D405/12 , A61K31/4155 , C07D403/14 , A61K31/506 , C07D409/14 , C07D403/12
CPC分类号: C07D213/75 , C07D213/80 , C07D231/40 , C07D241/20 , C07D277/20 , C07D277/46 , C07D285/08 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14
摘要: [Problem]A compound which is useful as a GK activator is provided.[Means for Solution]The present inventors have conducted studies on compounds having a GK activating action, which are promising as active ingredients of pharmaceutical compositions for the treatment of diabetes, type 2 diabetes mellitus, obesity, metabolic syndrome and related diseases caused by the aforementioned diseases, and as a result, they have confirmed that a benzamide compound of the present invention has an excellent GK activating action, thereby completing the present invention. That is, the benzamide compound of the present invention has a GK activating action and can be used as an agent for preventing and/or treating diabetes, type 2 diabetes mellitus, obesity, metabolic syndrome, and related diseases caused by the aforementioned diseases.
摘要翻译: [问题]提供了可用作GK活化剂的化合物。 [解决方案]本发明人对具有GK活化作用的化合物进行研究,这些化合物作为用于治疗糖尿病,2型糖尿病,肥胖,代谢综合征和由上述引起的相关疾病的药物组合物的活性成分是有希望的 疾病,结果证实本发明的苯甲酰胺化合物具有优异的GK活化作用,从而完成了本发明。 也就是说,本发明的苯甲酰胺化合物具有GK活化作用,可用作预防和/或治疗由上述疾病引起的糖尿病,2型糖尿病,肥胖症,代谢综合征和相关疾病的药剂。
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公开(公告)号:US08022208B2
公开(公告)日:2011-09-20
申请号:US12091099
申请日:2006-11-07
申请人: Fukushi Hirayama , Jiro Fujiyasu , Daisuke Kaga , Kenji Negoro , Daisuke Sasuga , Norio Seki , Ken-ichi Suzuki
发明人: Fukushi Hirayama , Jiro Fujiyasu , Daisuke Kaga , Kenji Negoro , Daisuke Sasuga , Norio Seki , Ken-ichi Suzuki
IPC分类号: C07D419/14 , C07D279/12 , C07D401/14 , C07D211/94 , C07D213/62 , C07D267/10 , A61K31/553 , A61K31/554 , A61K31/546 , A61K31/5355 , A61K31/497 , A61K31/445 , A61K31/444
CPC分类号: C07D213/75 , C07D211/76 , C07D213/64 , C07D239/36 , C07D241/18 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14
摘要: Problem: To provide compounds which have an anticoagulation effect based on their ability to inhibit the activated blood coagulation factor X and are useful as coagulation inhibitors or agents for prevention or treatment for diseases caused by thrombi or emboli.Means for Solution: Benzene derivatives or their salts having a characteristic chemical structure with a phenol ring and a benzene ring bonding to each other via an amide bond, in which the phenol ring further bonds to a benzene ring or a heteroaryl ring via an amide bond. They have an excellent effect of inhibiting the activated blood coagulation factor X, and especially have an excellent oral activity.
摘要翻译: 问题:提供基于其抑制活化凝血因子X的能力具有抗凝作用的化合物,并且可用作凝血抑制剂或用于预防或治疗由血栓或栓塞引起的疾病的药剂。 解决方法:苯衍生物或其具有特征化学结构的苯酚环和苯环通过酰胺键彼此键合,其中酚环还通过酰胺键与苯环或杂芳基环键合 。 它们具有抑制活化凝血因子X的优异效果,特别是具有优异的口服活性。
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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: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: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:US20050239780A1
公开(公告)日:2005-10-27
申请号:US10514636
申请日:2003-05-29
申请人: Akira Suga , Hideki Kubota , Masanori Miura , Daisuke Sasuga , Hiroshi Moritani
发明人: Akira Suga , Hideki Kubota , Masanori Miura , Daisuke Sasuga , Hiroshi Moritani
IPC分类号: A61P1/18 , A61P3/04 , A61P3/06 , A61P9/10 , A61P43/00 , C07D405/08 , C07D405/14 , C07D471/04 , C07D519/00 , A61K31/5377 , A61K31/496 , C07D471/02
CPC分类号: C07D405/08 , C07D405/14 , C07D471/04
摘要: The invention has succeeded in settling the aforementioned problems by finding that a novel tetrahydropyran derivative has excellent apo B-related lipoprotein secretion-inhibiting activity.
摘要翻译: 本发明通过发现新型四氢吡喃衍生物具有优异的载脂蛋白B相关脂蛋白分泌抑制活性而成功地解决了上述问题。
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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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