JP2002012555A5 - - Google Patents

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JP2002012555A5
JP2002012555A5 JP2001125659A JP2001125659A JP2002012555A5 JP 2002012555 A5 JP2002012555 A5 JP 2002012555A5 JP 2001125659 A JP2001125659 A JP 2001125659A JP 2001125659 A JP2001125659 A JP 2001125659A JP 2002012555 A5 JP2002012555 A5 JP 2002012555A5
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carbon atoms
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compound
pharmacologically acceptable
inhibitory activity
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JP4205314B2 (en
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シアリダーゼ阻害活性を有する化合物の薬理上許容されるエステル誘導体を有効成分として含有し、受容者の呼吸器へ投与されることを特徴とするインフルエンザ予防剤。  An influenza preventive agent comprising a pharmacologically acceptable ester derivative of a compound having a sialidase inhibitory activity as an active ingredient and administered to a recipient's respiratory tract. 請求項１において、シアリダーゼ阻害活性を有する化合物の薬理上許容されるエステル誘導体を受容者の呼吸器へ投与されることにより、シアリダーゼ阻害活性を有する化合物を受容者の呼吸器組織に滞留させることを特徴とするインフルエンザ予防剤。  The method of claim 1, wherein the compound having sialidase inhibitory activity is retained in the recipient's respiratory tissue by administering a pharmacologically acceptable ester derivative of the compound having sialidase inhibitory activity to the recipient's respiratory tract. Influenza preventive agent characterized. 請求項１又は２から選ばれるいずれか１項において、シアリダーゼ阻害活性を有する化合物が２−デオキシ−２，３−ジデヒドロ−Ｎ−アセチルノイラミン酸誘導体、シクロヘキセンカルボン酸誘導体、シクロペンタンカルボン酸誘導体またはピロリジン−２−カルボン酸誘導体であるインフルエンザ予防剤。  The compound having sialidase inhibitory activity according to any one of claims 1 and 2, wherein the compound having sialidase inhibitory activity is a 2-deoxy-2,3-didehydro-N-acetylneuraminic acid derivative, a cyclohexenecarboxylic acid derivative, a cyclopentanecarboxylic acid derivative, or Influenza preventive agent which is a pyrrolidine-2-carboxylic acid derivative. 請求項１又は２から選ばれるいずれか１項において、シアリダーゼ阻害活性を有する化合物が一般式
Figure 2002012555
［式中、Ｘはハロゲン原子、水酸基又は炭素数１乃至４個のアルコキシ基を示す。］、
一般式
Figure 2002012555
［式中、Ｒｂ１はアミノまたはグアニジノ基を示し、Ｒｂ２は炭素数１乃至１２個のアルキル基を示す。］、
一般式
Figure 2002012555
［式中、Ｒｃ１は水素原子または水酸基を示し、Ｒｃ２は炭素数１乃至８個のアルキル基を示し、Ｒｃ３はアミノまたはグアニジノ基を示す。］、
または一般式
Figure 2002012555
［式中、Ｒｄ１は炭素数２乃至５個のアルケニル基を示し、Ｒｄ２及びＲｄ３は炭素数１乃至６個のアルキル基または炭素数２乃至６個のアルケニル基を示し、Ｒｄ４は炭素数１乃至３個のアルキル基またはアリル基を示す。］で表される化合物であるインフルエンザ予防剤。3. The compound according to claim 1, wherein the compound having sialidase inhibitory activity is represented by the general formula:
Figure 2002012555
 [Wherein, X represents a halogen atom, a hydroxyl group or an alkoxy group having 1 to 4 carbon atoms. ],
General formula
Figure 2002012555
 [Wherein, R b1 represents an amino or guanidino group, and R b2 represents an alkyl group having 1 to 12 carbon atoms. ],
General formula
Figure 2002012555
 [Wherein, R c1 represents a hydrogen atom or a hydroxyl group, R c2 represents an alkyl group having 1 to 8 carbon atoms, and R c3 represents an amino or guanidino group. ],
Or general formula
Figure 2002012555
 [Wherein, R d1 represents an alkenyl group having 2 to 5 carbon atoms, R d2 and R d3 represent an alkyl group having 1 to 6 carbon atoms or an alkenyl group having 2 to 6 carbon atoms, and R d4 represents An alkyl group having 1 to 3 carbon atoms or an allyl group is shown. ] Influenza preventive agent which is a compound represented by this. 請求項１乃至４から選ばれるいずれか１項において、薬理上許容されるエステル誘導体がシアリダーゼ阻害活性を有する化合物の水酸基における炭素数６乃至２０個のアルカノイルエステルまたはシアリダーゼ阻害活性を有する化合物のカルボキシル基における炭素数８乃至２０個のアルキルエステルであるインフルエンザ予防剤。  The carboxylic acid group according to any one of claims 1 to 4, wherein the pharmacologically acceptable ester derivative is an alkanoyl ester having 6 to 20 carbon atoms in a hydroxyl group of the compound having sialidase inhibitory activity or a compound having sialidase inhibitory activity. Influenza preventive agent which is an alkyl ester having 8 to 20 carbon atoms. 請求項１乃至２から選ばれるいずれか１項において、薬理上許容されるエステル誘導体が、一般式  The pharmacologically acceptable ester derivative according to any one of claims 1 to 2, wherein the pharmacologically acceptable ester derivative is represented by the general formula:
Figure 2002012555
Figure 2002012555
 ［式中、Ｒ[Wherein R １1 及びＲAnd R ２2 は、同一又は異なって、水素原子又は炭素数６乃至２０個のアルカノイル基を示し、ＸAre the same or different and each represents a hydrogen atom or an alkanoyl group having 6 to 20 carbon atoms; １1 はハロゲン原子、水酸基、炭素数１乃至４個のアルコキシ基又は炭素数２乃至２０個のアルカノイルオキシ基を示し、ＲRepresents a halogen atom, a hydroxyl group, an alkoxy group having 1 to 4 carbon atoms or an alkanoyloxy group having 2 to 20 carbon atoms; ３3 は水素原子又は炭素数８乃至２０個のアルキル基を示す。但し、ＲRepresents a hydrogen atom or an alkyl group having 8 to 20 carbon atoms. However, R １1 及びＲAnd R ２2 が水素原子であり、かつＸIs a hydrogen atom and X １1 がハロゲン原子、水酸基又は炭素数１乃至４個のアルコキシ基である場合、ＲIs a halogen atom, a hydroxyl group or an alkoxy group having 1 to 4 carbon atoms, ３3 は炭素数８乃至２０個のアルキル基を示す。］で表される化合物であるインフルエンザ予防剤。Represents an alkyl group having 8 to 20 carbon atoms. ] Influenza preventive agent which is a compound represented by this. 請求項１乃至２から選ばれるいずれか１項において、薬理上許容されるエステル誘導体が、５−アセタミド−４−グアニジノ−９−Ｏ−オクタノイル−２、３、４、５−テトラデオキシ−７−Ｏ−メチル−Ｄ−グリセロ−Ｄ−ガラクト−ノン−２−エノピラソン酸水和物結晶であるインフルエンザ予防剤。  3. The pharmacologically acceptable ester derivative according to claim 1, wherein the pharmacologically acceptable ester derivative is 5-acetamido-4-guanidino-9-O-octanoyl-2, 3, 4, 5-tetradeoxy-7-. Influenza preventive agent which is O-methyl-D-glycero-D-galacto-non-2-enopyrazonic acid hydrate crystals. 請求項１乃至２から選ばれるいずれか１項において、薬理上許容されるエステル誘導体が、５−アセタミド−４−グアニジノ−９−Ｏ−オクタノイル−２、３、４、５−テトラデオキシ−７−Ｏ−メチル−Ｄ−グリセロ−Ｄ−ガラクト−ノン−２−エノピラソン酸水和物結晶であって、  3. The pharmacologically acceptable ester derivative according to claim 1, wherein the pharmacologically acceptable ester derivative is 5-acetamido-4-guanidino-9-O-octanoyl-2, 3, 4, 5-tetradeoxy-7-. O-methyl-D-glycero-D-galacto-non-2-enopyrazonic acid hydrate crystals, KBrKBr 法により下記の波長において赤外線吸収ピークを示す結晶であるインフルエンザ予防剤：Influenza preventive agent which is a crystal showing infrared absorption peak at the following wavelength by the method:
赤外線吸収スペクトル  Infrared absorption spectrum (KBr) (KBr) νν max cmmax cm -1-1 : 3412, 2929, 2856, 1676, 1401, 1320, 1285, 1205, 1137, 722: 3412, 2929, 2856, 1676, 1401, 1320, 1285, 1205, 1137, 722 。.
JP2001125659A 2000-04-25 2001-04-24 Influenza preventive Expired - Lifetime JP4205314B2 (en)

Priority Applications (1)

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JP2001125659A JP4205314B2 (en) 2000-04-25 2001-04-24 Influenza preventive

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JP2000124126 2000-04-25
JP2000-124126 2000-04-25
JP2001125659A JP4205314B2 (en) 2000-04-25 2001-04-24 Influenza preventive

Related Child Applications (1)

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JP2008197714A Division JP4827197B2 (en) 2000-04-25 2008-07-31 Influenza preventive

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JP2002012555A JP2002012555A (en) 2002-01-15
JP2002012555A5 true JP2002012555A5 (en) 2005-08-25
JP4205314B2 JP4205314B2 (en) 2009-01-07

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Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI491416B (en) * 2008-12-24 2015-07-11 Daiichi Sankyo Co Ltd A dry powder pharmaceutical composition for inhalation
JP2011136964A (en) * 2009-12-28 2011-07-14 Gifu Univ Neuraminic acid derivative, sialidase activity inhibitor and anti-influenza medicine
DE102011117128A1 (en) * 2011-10-28 2013-05-02 Christian-Albrechts-Universität Zu Kiel Compounds for the treatment of influenza
IN2014MN00971A (en) 2011-12-16 2015-05-22 Daiichi Sankyo Co Ltd

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