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公开(公告)号:US6147114A
公开(公告)日:2000-11-14
申请号:US945356
申请日:1997-10-24
申请人: Tetsunori Fujisawa , Shinjiro Odake , Yasuo Morita , Tomoko Hongo , Hajime Ito , Junko Yasuda , Eiko Suda , Katsuhiro Igeta , Tadanori Morikawa
发明人: Tetsunori Fujisawa , Shinjiro Odake , Yasuo Morita , Tomoko Hongo , Hajime Ito , Junko Yasuda , Eiko Suda , Katsuhiro Igeta , Tadanori Morikawa
IPC分类号: A61K31/165 , C07C239/06 , C07C259/06 , C07C279/14 , C07C279/16 , C07C305/24 , C07C309/61 , C07C323/60 , C07F9/12 , A01N37/28 , C07C239/14
CPC分类号: C07C323/60 , A61K31/165 , C07C239/06 , C07C259/06 , C07C279/14 , C07C279/16 , C07C305/24 , C07C309/61 , C07F9/12
摘要: New compounds of the general formula (I) ##STR1## (wherein R.sup.1 is a hydrogen atom, or a hydroxyl, aryl (C.sub.1 -C.sub.6)alkylene or --A--SOn--B group (A is a (C.sub.1 -C.sub.6) alkylene group; B is a (C.sub.1 -C.sub.6) alkyl, (C.sub.1 -C.sub.6) acyl, aryl or heterocyclyl group; n is 0, 1 or 2), R.sup.2 is a hydrogen atom, or a (C.sub.1 -C.sub.6) alkyl, (C.sub.1 -C.sub.6) alkyloxy 10 or (C.sub.1 -C.sub.6) alkylthio group, R.sup.3 and R.sup.4 are identical or different, representing a hydrogen atom, or a (C.sub.1 -C.sub.6) alkyl, aryl or aryl(C.sub.1 -C.sub.6)alkylene group, R.sup.5 is a --Y--C or C group (Y is a (C.sub.1 -C.sub.6) alkylene group, an oxygen atom, an imino group or a (C.sub.1 -C.sub.6) alkyleneimino group, C is a sulfonic acid, phosphonic acid, amidino, (C.sub.1 -C.sub.6) acyl, acylimidoyl, diphosphonomethine or dicarboxymethine group), and R.sup.6 is a hydrogen atom, or a nonsubstituted or substituted benzyl, trialkylsilyl, tert-butyldiphenylsilyl, tetrahydropyranyl or tert-butyl group) or stereoisomers thereof, and pharmaceutically acceptable salts thereof and solvates thereof, and the process for the preparation thereof, and metalloproteinase inhibitors which comprise one or more compounds selected from those compounds as effective ingredients and inhibit matrix metalloproteinases (MMPs) and/or TNF-.alpha. converting enzyme. Furthermore, the preparation intermediates to obtain the compounds of the formula (I) and the process for the preparation.
摘要翻译: PCT No.PCT / JP96 / 01135 Sec。 371 1997年10月24日第 102(e)1997年10月24日PCT PCT 1996年4月25日PCT公布。 WO96 / 33968 PCT公开号 日期:1996年10月31日新化合物通式(Ⅰ)(其中R1是氢原子,或羟基,芳基(C1-C6)亚烷基或-A-SOn-B基团(A是(C1-C6) 亚烷基; B是(C1-C6)烷基,(C1-C6)酰基,芳基或杂环基; n是0,1或2),R2是氢原子或(C1-C6)烷基, C1-C6)烷氧基10或(C1-C6)烷硫基,R3和R4相同或不同,代表氢原子或(C1-C6)烷基,芳基或芳基(C1-C6)亚烷基,R5是 -YC或C基(Y是(C1-C6)亚烷基,氧原子,亚氨基或(C1-C6)亚烷基亚氨基),C是磺酸,膦酸,脒基,(C1-C6 )酰基,酰亚氨基,二亚膦酰基或二羧基甲基),R6为氢原子,或未取代或取代的苄基,三烷基甲硅烷基,叔丁基二苯基甲硅烷基,四氢吡喃基或叔丁基)或其立体异构体及其药学上可接受的盐及其溶剂合物 ,以及其准备过程 f和金属蛋白酶抑制剂,其包含一种或多种选自那些化合物的化合物作为有效成分并抑制基质金属蛋白酶(MMP)和/或TNF-α转化酶。 此外,制备中间体以获得式(I)化合物及其制备方法。
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公开(公告)号:US06284914B1
公开(公告)日:2001-09-04
申请号:US09492149
申请日:2000-01-27
申请人: Junko Fujisawa , Eiko Suda , Katsuhiro Igeta , Tadanori Morikawa , Tetsunori Fujisawa , Shinjiro Odake , Yasuo Morita , Tomoko Hongo , Hajime Ito
发明人: Junko Fujisawa , Eiko Suda , Katsuhiro Igeta , Tadanori Morikawa , Tetsunori Fujisawa , Shinjiro Odake , Yasuo Morita , Tomoko Hongo , Hajime Ito
IPC分类号: C07C23704
CPC分类号: C07C323/60 , A61K31/165 , C07C239/06 , C07C259/06 , C07C279/14 , C07C279/16 , C07C305/24 , C07C309/61 , C07F9/12
摘要: New compounds of general formulae (III), (IV) and (V).
摘要翻译: 通式(III),(IV)和(V)的新化合物。
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公开(公告)号:US08952010B2
公开(公告)日:2015-02-10
申请号:US13983540
申请日:2012-02-06
申请人: Hiroaki Inagaki , Tetsunori Fujisawa , Masao Itoh , Aki Yokomizo , Toshifumi Tsuda , Saito Higuchi , Biswajit Das , Rita Katoch , Dilip J. Upadhyay
发明人: Hiroaki Inagaki , Tetsunori Fujisawa , Masao Itoh , Aki Yokomizo , Toshifumi Tsuda , Saito Higuchi , Biswajit Das , Rita Katoch , Dilip J. Upadhyay
IPC分类号: A61K31/538 , A61K31/498 , C07D498/12 , C07D265/36 , C07D413/04 , C07D413/14 , C07D487/04 , C07D241/44 , A61K31/5383 , C07D471/04 , C07D519/00 , C07D498/04
CPC分类号: C07D487/04 , A61K31/5383 , C07D241/44 , C07D265/36 , C07D413/04 , C07D413/14 , C07D471/04 , C07D498/04 , C07D519/00 , Y02A50/475
摘要: A compound represented by the following formula (I) or a salt thereof: wherein R represents a hydrogen atom, a hydroxy group, or a halogen atom Ar1 represents a bicyclic heterocyclic group represented by the following formula: and Ar2 represents a bicyclic heterocyclic group represented by the following formulae:
摘要翻译: 由下式(I)表示的化合物或其盐:其中R表示氢原子,羟基或卤素原子Ar1表示由下式表示的双环杂环基:Ar2表示双环杂环基, 通过以下公式:
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公开(公告)号:US20100311966A1
公开(公告)日:2010-12-09
申请号:US12811004
申请日:2008-12-26
申请人: Tsuyoshi Soneda , Hiroshi Takeshita , Yoshiko Kagoshima , Yuko Yamamoto , Takafumi Hosokawa , Toshiyuki Konosu , Nobuhisa Masuda , Takuya Uchida , Issei Achiwa , Junichi Kuroyanagi , Tetsunori Fujisawa , Aki Yokomizo , Tetsuji Noguchi
发明人: Tsuyoshi Soneda , Hiroshi Takeshita , Yoshiko Kagoshima , Yuko Yamamoto , Takafumi Hosokawa , Toshiyuki Konosu , Nobuhisa Masuda , Takuya Uchida , Issei Achiwa , Junichi Kuroyanagi , Tetsunori Fujisawa , Aki Yokomizo , Tetsuji Noguchi
IPC分类号: C07D498/04 , C07D277/56 , C07D513/04 , C07D233/90 , C07D403/12 , C07D495/04 , C07D495/16
CPC分类号: C07D487/04 , C07D233/66 , C07D233/90 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/06 , C07D487/12 , C07D495/04 , C07D495/16 , C07D498/04 , C07D513/04 , C07D519/00
摘要: An antibiotic compound having a novel mechanism of action, weak cytotoxicity, high solubility in water, effective in inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and having antibacterial activity.
摘要翻译: 具有新的作用机理,细胞毒性低,在水中溶解度高的抗生素化合物,有效抑制DNA促旋酶GyrB和拓扑异构酶IV ParE亚基,具有抗菌活性。
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公开(公告)号:US20050113397A1
公开(公告)日:2005-05-26
申请号:US10502971
申请日:2003-01-30
申请人: Makoto Takemura , Hisashi Takahashi , Katsuhiro Kawakami , Hiroshi Takeshita , Youichi Kimura , Jun Watanabe , Yuichi Sugimoto , Akihiro Kitamura , Ryohei Nakajima , Kazuo Kanai , Tetsunori Fujisawa
发明人: Makoto Takemura , Hisashi Takahashi , Katsuhiro Kawakami , Hiroshi Takeshita , Youichi Kimura , Jun Watanabe , Yuichi Sugimoto , Akihiro Kitamura , Ryohei Nakajima , Kazuo Kanai , Tetsunori Fujisawa
IPC分类号: A61K31/437 , A61K31/4375 , A61K31/496 , A61K31/5377 , A61K31/541 , A61P31/00 , A61P31/10 , C07D471/04 , C07D471/14 , C07D491/14 , C07D519/00 , A61K31/4745 , A61K31/519 , C07D487/14
CPC分类号: C07D471/04 , A61K31/437 , A61K31/4375 , A61K31/496 , A61K31/5377 , A61K31/541 , C07D471/14 , C07D491/14
摘要: A compound reprsented by the following formula (I), its salts or nsolvates thereof capable of specifically or selectively expressig an antifungal activity in a broad spectrum based on the novel mechanism thereof of 1,6-β-glucan synthesis inhibition, and an antifungal agent containing any of them.
摘要翻译: 基于其1,6-β-葡聚糖合成抑制的新机理,通过下式(I)表示的化合物,其能够在宽谱中特异性或选择性表达抗真菌活性的盐或其溶剂化物,以及抗真菌剂 包含它们中的任何一个。
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公开(公告)号:US20140187542A1
公开(公告)日:2014-07-03
申请号:US13983540
申请日:2012-02-06
申请人: Hiroaki Inagaki , Tetsunori Fujisawa , Masao Itoh , Aki Yokomizo , Toshifumi Tsuda , Saito Higuchi , Biswajit Das , Rita Katoch , Dilip J. Upadhyay
发明人: Hiroaki Inagaki , Tetsunori Fujisawa , Masao Itoh , Aki Yokomizo , Toshifumi Tsuda , Saito Higuchi , Biswajit Das , Rita Katoch , Dilip J. Upadhyay
IPC分类号: C07D498/04 , C07D487/04 , C07D413/14
CPC分类号: C07D487/04 , A61K31/5383 , C07D241/44 , C07D265/36 , C07D413/04 , C07D413/14 , C07D471/04 , C07D498/04 , C07D519/00 , Y02A50/475
摘要: A compound represented by the following formula (I) or a salt thereof: wherein R represents a hydrogen atom, a hydroxy group, or a halogen atom Ar1 represents a bicyclic heterocyclic group represented by the following formula: and Ar2 represents a bicyclic heterocyclic group represented by the following formulae:
摘要翻译: 由下式(I)表示的化合物或其盐:其中R表示氢原子,羟基或卤素原子Ar1表示由下式表示的双环杂环基:Ar2表示双环杂环基, 通过以下公式:
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公开(公告)号:US08536197B2
公开(公告)日:2013-09-17
申请号:US12811004
申请日:2008-12-26
申请人: Tsuyoshi Soneda , Hiroshi Takeshita , Yoshiko Kagoshima , Yuko Yamamoto , Takafumi Hosokawa , Toshiyuki Konosu , Nobuhisa Masuda , Takuya Uchida , Issei Achiwa , Junichi Kuroyanagi , Tetsunori Fujisawa , Aki Yokomizo , Tetsuji Noguchi
发明人: Tsuyoshi Soneda , Hiroshi Takeshita , Yoshiko Kagoshima , Yuko Yamamoto , Takafumi Hosokawa , Toshiyuki Konosu , Nobuhisa Masuda , Takuya Uchida , Issei Achiwa , Junichi Kuroyanagi , Tetsunori Fujisawa , Aki Yokomizo , Tetsuji Noguchi
IPC分类号: C07D417/04 , C07D401/12 , A61K31/4164 , A61K31/4178
CPC分类号: C07D487/04 , C07D233/66 , C07D233/90 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/06 , C07D487/12 , C07D495/04 , C07D495/16 , C07D498/04 , C07D513/04 , C07D519/00
摘要: An antibiotic compound having a novel mechanism of action, weak cytotoxicity, high solubility in water, effective in inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and having antibacterial activity.
摘要翻译: 具有新的作用机理,细胞毒性低,在水中溶解度高的抗生素化合物,有效抑制DNA促旋酶GyrB和拓扑异构酶IV ParE亚基,具有抗菌活性。
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公开(公告)号:US20070191395A1
公开(公告)日:2007-08-16
申请号:US10589563
申请日:2005-02-16
IPC分类号: A61K31/519 , A61K31/437 , C07D207/06 , C07D471/04 , C07D487/12
CPC分类号: C07D471/04
摘要: A compound which can specifically or selectively expresses an antifungal activity with a broad spectrum, based on the functional mechanism of 1,6-β-glucan synthesis inhibition, is provided, and an antifungal agent which comprises such a compound, a salt thereof or a solvate thereof is provided. A compound represented by the following formula (I), a salt thereof or a solvate thereof.
摘要翻译: 提供了基于1,6-β-葡聚糖合成抑制的功能机理可以特异地或选择性地表达具有广谱的抗真菌活性的化合物,以及包含这种化合物,其盐或 提供其溶剂合物。 由下式(I)表示的化合物,其盐或其溶剂合物。
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