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    • 3. 发明授权
    • Amino acid derivatives
    • 氨基酸衍生物
    • US06018020A
    • 2000-01-25
    • US96570
    • 1998-06-12
    • Michael Richard AttwoodDavid Nigel HurstPhilip Stephen JonesPaul Brittain KayTony Michael RaynhamFrancis Xavier Wilson
    • Michael Richard AttwoodDavid Nigel HurstPhilip Stephen JonesPaul Brittain KayTony Michael RaynhamFrancis Xavier Wilson
    • C12N15/09A01N43/34A01N43/36A61K38/00A61P31/12A61P31/14C07C205/04C07C205/45C07C271/18C07D207/12C07D207/20C07D211/70C07D223/04C07D227/04C07D405/10C07D407/10C07D409/10C07K7/06A61K38/08
    • C07K7/06A61K38/00
    • The invention provides amino acid derivatives of the formula ##STR1## wherein E represents CHO or B(OH).sub.2 ;R.sup.1 represents lower alkyl (optionally substituted by halo, cyano, lower alkylthio, aryl-lower alkylthio, aryl or heteroaryl), lower alkenyl or lower alkynyl;R.sup.2 represents lower alkyl optionally substituted by hydroxy, carboxy, aryl, aminocarbonyl or lower cycloalkyl; andR.sup.3 represents hydrogen or lower alkyl; orR.sup.2 and R.sup.3 together represent di- or trimethylene optionally substituted by hydroxy;R.sup.4 represents lower alkyl (optionally substituted by hydroxy, lower cycloalkyl, carboxy, aryl, lower alkylthio, cyano-lower alkylthio or aryl-lower alkylthio), lower alkenyl, aryl or lower cycloalkyl;R.sup.5 represents lower alkyl (optionally substituted by hydroxy, lower alkylthio, aryl, aryl-lower alkylthio or cyano-lower alkylthio) or lower cycloalkyl;R.sup.6 represents hydrogen or lower alkyl;R.sup.7 represent lower alkyl (optionally substituted by hydroxy, carboxy, aryl or lower cycloalkyl) or lower cycloalkyl;R.sup.8 represents lower alkyl optionally substituted by hydroxy, carboxy or aryl; andR.sup.9 represents lower alkylcarbonyl, carboxy-lower alkylcarbonyl, arylcarbonyl, lower alkylsulphonyl, arylsulphonyl, lower alkoxycarbonyl or aryl-lower alkoxycarbonyl,and salts of acidic compounds of formula I with bases, which are viral proteinase inhibitors useful as antiviral agents, especially for the treatment or prophylaxis of infections caused by Hepatitis C, Hepatitis G and human GB viruses.
    • 本发明提供下式的氨基酸衍生物,其中E代表CHO或B(OH)2; R 1表示低级烷基(任选被卤素,氰基,低级烷硫基,芳基 - 低级烷硫基,芳基或杂芳基取代),低级烯基或低级炔基; R 2表示任选被羟基,羧基,芳基,氨基羰基或低级环烷基取代的低级烷基; 并且R 3表示氢或低级烷基; 或R 2和R 3一起表示任选被羟基取代的二 - 或三亚甲基; R4代表低级烷基(任选被羟基,低级环烷基,羧基,芳基,低级烷硫基,氰基 - 低级烷硫基或芳基 - 低级烷硫基取代),低级烯基,芳基或低级环烷基; R5代表低级烷基(任选被羟基,低级烷硫基,芳基,芳基 - 低级烷硫基或氰基 - 低级烷硫基取代)或低级环烷基; R6代表氢或低级烷基; R7代表低级烷基(任选被羟基,羧基,芳基或低级环烷基取代)或低级环烷基; R8代表任选被羟基,羧基或芳基取代的低级烷基; 并且R 9表示低级烷基羰基,羧基 - 低级烷基羰基,芳基羰基,低级烷基磺酰基,芳基磺酰基,低级烷氧基羰基或芳基 - 低级烷氧基羰基,以及式I酸性化合物与碱的碱,其为用作抗病毒剂的病毒蛋白酶抑制剂, 治疗或预防丙型肝炎,丙型肝炎和人类GB病毒引起的感染。
    • 5. 发明授权
    • Peptidyl inhibitors of viral proteases
    • 肽基蛋白酶抑制剂
    • US5866684A
    • 1999-02-02
    • US971036
    • 1997-11-14
    • Michael Richard AttwoodDavid Nigel HurstPhilip Stephen JonesPaul Brittain KayTony Michael RaynhamFrancis Xavier Wilson
    • Michael Richard AttwoodDavid Nigel HurstPhilip Stephen JonesPaul Brittain KayTony Michael RaynhamFrancis Xavier Wilson
    • C12N15/09A01N43/34A01N43/36A61K38/00A61P31/12A61P31/14C07C205/04C07C205/45C07C271/18C07D207/12C07D207/20C07D211/70C07D223/04C07D227/04C07D405/10C07D407/10C07D409/10C07K7/06A61K38/08
    • C07K7/06A61K38/00
    • The invention provides amino acid derivatives of the formula ##STR1## wherein E represents CHO or B(OH).sub.2 ;R.sup.1 represents lower alkyl (optionally substituted by halo, cyano, lower alkylthio, aryl-lower alkylthio, aryl or heteroaryl), lower alkenyl or lower alkynyl;R.sup.2 represents lower alkyl optionally substituted by hydroxy, carboxy, aryl, aminocarbonyl or lower cycloalkyl; andR.sup.3 represents hydrogen or lower alkyl; orR.sup.2 and R.sup.3 together represent di- or trimethylene optionally substituted by hydroxy;R.sup.4 represents lower alkyl (optionally substituted by hydroxy, lower cycloalkyl, carboxy, aryl, lower alkylthio, cyano-lower alkylthio or aryl-lower alkylthio), lower alkenyl, aryl or lower cycloalkyl;R.sup.5 represents lower alkyl (optionally substituted by hydroxy, lower alkylthio, aryl, aryl-lower alkylthio or cyano-lower alkylthio) or lower cycloalkyl;R.sup.6 represents hydrogen or lower alkyl;R.sup.7 represent lower alkyl (optionally substituted by hydroxy, carboxy, aryl or lower cycloalkyl) or lower cycloalkyl;R.sup.8 represents lower alkyl optionally substituted by hydroxy, carboxy or aryl; andR.sup.9 represents lower alkylcarbonyl, carboxy-lower alkylcarbonyl, arylcarbonyl, lower alkylsulphonyl, arylsulphonyl, lower alkoxycarbonyl or aryl-lower al koxycarbonyl,and salts of acidic compounds of formula I with bases, which are viral proteinase inhibitors useful as antiviral agents, especially for the treatment or prophylaxis of infections caused by Hepatitis C, Hepatitis G and human GB viruses.
    • 本发明提供式(I)的氨基酸衍生物,其中E表示CHO或B(OH)2; R 1表示低级烷基(任选被卤素,氰基,低级烷硫基,芳基 - 低级烷硫基,芳基或杂芳基取代),低级烯基或低级炔基; R 2表示任选被羟基,羧基,芳基,氨基羰基或低级环烷基取代的低级烷基; 并且R 3表示氢或低级烷基; 或R 2和R 3一起表示任选被羟基取代的二 - 或三亚甲基; R4代表低级烷基(任选被羟基,低级环烷基,羧基,芳基,低级烷硫基,氰基 - 低级烷硫基或芳基 - 低级烷硫基取代),低级烯基,芳基或低级环烷基; R5代表低级烷基(任选被羟基,低级烷硫基,芳基,芳基 - 低级烷硫基或氰基 - 低级烷硫基取代)或低级环烷基; R6代表氢或低级烷基; R7代表低级烷基(任选被羟基,羧基,芳基或低级环烷基取代)或低级环烷基; R8代表任选被羟基,羧基或芳基取代的低级烷基; 并且R 9表示低级烷基羰基,羧基 - 低级烷基羰基,芳基羰基,低级烷基磺酰基,芳基磺酰基,低级烷氧基羰基或芳基 - 低级烷氧基羰基,以及式I酸性化合物与碱的碱,其为用作抗病毒剂的病毒蛋白酶抑制剂, 治疗或预防丙型肝炎,丙型肝炎和人类GB病毒引起的感染。