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Modified cyclopentane and cyclopentene compounds suitable for use as neuraminidase inhibitors

机译：适合用作神经氨酸酶抑制剂的改性环戊烷和环戊烯化合物

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摘要

Compounds I-III wherein U is CH, O, or S; Z is mono- or di-substituted carbon; R is (CH2)nCO2H, (CH2)nSO3H, (CH2)nPO3H2, (CH2)nNO2, CH(SCH3)3, esters; R1 is H, hydroxyalkyl, aminoalkyl, alkoxyalkyl; RR1 is O; n is 0-4; R2, R3 is H, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkyl; R4 is (CH2)nOH, (CH2)nNH2, substituted alkyl were prepd. as neuraminidase inhibitors. Thus, (1R,3R,4R,1'S)-(-)-(1'-acetylamino-2 '-ethyl)butyl-4-(aminoimino)methylaminocyclopentan-1-carboxylic acid was prepd. and tested in vitro as neuraminidase inhibitor (IC501.mu.M).

机译：化合物I-III，其中U是CH，O或S; Z是单或二取代的碳; R为（CH2）nCO2H，（CH2）nSO3H，（CH2）nPO3H2，（CH2）nNO2，CH（SCH3）3的酯; R1为H，羟烷基，氨基烷基，烷氧基烷基; RR1为O; n为0-4; R2，R3为H，羟烷基，氨基烷基，烷氧基烷基，卤代烷基; R 4为（CH 2）n OH，（CH 2）n NH 2，取代烷基。作为神经氨酸酶抑制剂。因此，制备了（1R，3R，4R，1′S）-（-）-（1′-乙酰氨基-2′-乙基）丁基-4-（氨基亚氨基）甲基氨基环戊烷-1-羧酸。并作为神经氨酸酶抑制剂（IC50 ＜1μM）在体外测试。

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公开/公告号LTPA2018513I1

专利类型
公开/公告日2018-10-10

原文格式PDF
申请/专利权人 BIOCRYST PHARMACEUTICALS INC.;
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申请/专利号LTPA2018513C
发明设计人
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申请日2018-09-13
分类号A61K;A61K31/195;A61K31/196;A61K31/215;A61K31/385;A61K31/4164;A61K31/423;A61P31/12;A61P43;C07C;C07C229/32;C07C229/48;C07C233/47;C07C247/14;C07C271/24;C07C279/16;C07C279/24;C07C309/66;C07C323/41;C07C323/43;C07C323/59;C07C323/60;C07D;C07D233/54;C07D233/56;C07D261/20;C07D339/08;C07D521;
国家 LT
入库时间 2022-08-21 12:51:26

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