Dimeric compounds and their use as anti-viral agents
    71.
    发明授权
    Dimeric compounds and their use as anti-viral agents 有权
    二聚体化合物及其作为抗病毒剂的用途

    公开(公告)号:US07504434B2

    公开(公告)日:2009-03-17

    申请号:US11695268

    申请日:2007-04-02

    IPC分类号: A61K31/351

    摘要: The invention relates to compounds of general formula (I), in which: R is an amino or guanidino group; R2 is acetyl or trifluoroacetyl; n and q are either the same or different and selected from 0, 1 or 2; and X is an optionally substituted phenyl, optionally substituted naphthyl or optionally substituted phenyl-Y-optionally substituted phenyl in which Y is selected from a covalent bond, CH2, CH2CH2, O or SO2, or a pharmaceutically acceptable derivative thereof, with the proviso that when X is phenyl or naphthyl, n and q are both 2 and when X is phenyl-Y-phenyl in which Y is a covalent bond, then n and q are not both 0, methods for their preparation, pharmaceutical formulations containing them or their use in the prevention or treatment of a viral infection.

    摘要翻译: 本发明涉及通式(I)的化合物,其中:R是氨基或胍基; R2是乙酰基或三氟乙酰基; n和q相同或不同,选自0,1或2; CH 2,CH 2 CH 2,O或SO 2,或其药学上可接受的衍生物,其中Y是任选取代的苯基,任选取代的萘基或任选取代的苯基-Y-任选取代的苯基,其中Y选自共价键, 当X是苯基或萘基时,n和q都是2,当X是其中Y是共价键的苯基-Y-苯基时,n和q都不是0,它们的制备方法,含有它们的药物制剂或它们 用于预防或治疗病毒感染。

    Antiviral agents
    77.
    发明授权
    Antiviral agents 失效
    抗病毒剂

    公开(公告)号:US07078403B1

    公开(公告)日:2006-07-18

    申请号:US10018963

    申请日:2000-06-16

    IPC分类号: A61K31/53

    摘要: Disclosed herein are compounds of formula II: wherein Alk, Z, X1, X2, R1, —R10 and R11 are defined herein, and their salts and pharmaceutically acceptable derivatives thereof, as well as other compounds of the general formula Het-A-Alk-W-Ar-C(X2)═NO-X2 where Het, A, W and Ar are also defined herein. These compounds are useful in treating picornavirus infections in mammals. Novel intermediates of these compounds, as well as pharmaceutical compositions and methods of use, are also disclosed herein.

    摘要翻译: 本文公开了式II的化合物:其中Alk,Z,X 1,X 2,R 1,R 10, 本文定义的本文及其盐及其药学上可接受的衍生物,以及通式Het-A-Alk-W-Ar-C(X

    6-Carboxamido dihydropyran derivatives
    78.
    发明授权
    6-Carboxamido dihydropyran derivatives 失效
    6-羧甲酰氨基二氢吡喃衍生物

    公开(公告)号:US5990156A

    公开(公告)日:1999-11-23

    申请号:US945676

    申请日:1998-01-12

    摘要: Compounds of formula (I), ##STR1## wherein R.sup.1 represents OR.sup.5, SR.sup.5, NR.sup.5 R.sup.6, N(OR.sup.5)R.sup.6 or N(NR.sup.5 R.sup.6)R.sup.6 ; X represents OH, N.sub.3, NR.sup.3 R.sup.4 or NR.sup.4 CO.sub.2 R.sup.15 ; Y represents H or NHR.sup.2 ; R.sup.2 represents a group SO.sub.2 R.sup.7 or COR.sup.7 ; R.sup.3 represents H, C.sub.1-6 alkyl or C(.dbd.NR.sup.8)NR.sup.9 R.sup.10 ; R.sup.4 represents H or C.sub.1-6 alkyl; R.sup.5 represents H, C.sub.1-20 alkyl, C.sub.3-8 cycloalkyl, C.sub.2-20 alkenyl, C.sub.2-20 alkynyl, CHR.sup.11 COR.sup.12 or C.sub.1-20 alkyl substituted by one or more groups selected from NR.sup.13 R.sup.14, NR.sup.13 COR.sup.14, CO.sub.2 R.sup.13, OR.sup.13, C.sub.3-8 cycloalkyl and optionally substituted aryl; each R.sup.6 independently represents H, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.2-6 alkenyl, C.sub.2-20 alkynyl, aryl or C.sub.1-4 alkyl substituted by one or more groups selected from NR.sup.13 R.sup.14, COR.sup.13, C.sub.3-8 cycloalkyl, CN, N.sub.3, OR.sup.13 and optionally substituted aryl; or R.sup.5 and R.sup.6 together form a C.sub.2-6 hydrocarbon chain which may optionally contain a group NR.sup.13 which chain is optionally substituted by 1, 2, 3 or 4 groups selected from oxo and C.sub.1-6 alkyl groups which groups may optionally be substituted by hydroxy or optionally substituted aryl; R.sup.7 represents C.sub.1-6 alkyl optionally substituted by one or more halogen atoms, C.sub.3-8 cycloalkyl or optionally substituted aryl; R.sup.8, R.sup.9 and R.sup.10 each independently represent H, C.sub.1-6 alkyl, amino, hydroxy, cyano or nitro; R.sup.11 represents the side chain of a D- or L-amino acid; R.sup.12 represents NR.sup.13 R.sup.14, OR.sup.13 or R.sup.13 ; each R.sup.13 and each R.sup.14 independently represents H, C.sub.1-6 alkyl or optionally substituted arylC.sub.1-4 alkyl; R.sup.15 represents C.sub.1-6 alkyl; and their pharmaceutically acceptable derivatives are neuraminidase inhibitors useful in the treatment of viral infections.

    摘要翻译: PCT No.PCT / AU96 / 00289 Sec。 371日期:1998年1月12日 102(e)日期1998年1月12日PCT提交1996年5月13日PCT公布。 出版物WO96 / 36628 日期:1996年11月21日,式(I)的化合物,其中R1表示OR5,SR5,NR5R6,N(OR5)R6或N(NR5R6)R6; X表示OH,N 3,NR 3 R 4或NR 4 CO 2 R 15; Y表示H或NHR 2; R2表示SO2R7或COR7; R 3表示H,C 1-6烷基或C(= NR 8)NR 9 R 10; R4表示H或C1-6烷基; R5表示H,C 1-20烷基,C 3-8环烷基,C 2-20烯基,C 2-20炔基,CHR 11 COR 12或被一个或多个选自NR 13 R 14,NR 13 COR 14,CO 2 R 13,OR 13,C 3-8环烷基和任选取代的芳基取代的C 1-20烷基; 每个R 6独立地表示被一个或多个选自NR 13 R 14,COR 13,C 3-8环烷基,CN,N 3,OR 13的基团取代的H,C 1-6烷基,C 3-8环烷基,C 2-6烯基,C 2-20炔基,芳基或C 1-4烷基, 取代芳基; 或R 5和R 6一起形成C 2-6烃链,其可以任选地含有NR 13,该链任选被1,2,3或4个选自氧代和C 1-6烷基的基团取代,所述基团可任选地被羟基或 任选取代的芳基; R 7表示任选被一个或多个卤素原子取代的C 1-6烷基,C 3-8环烷基或任选取代的芳基; R8,R9和R10各自独立地表示H,C1-6烷基,氨基,羟基,氰基或硝基; R11表示D-或L-氨基酸的侧链; R12表示NR13R14,OR13或R13; 每个R 13和每个R 14独立地表示H,C 1-6烷基或任选取代的芳基C 1-4烷基; R 15表示C 1-6烷基; 其药学上可接受的衍生物是可用于治疗病毒感染的神经氨酸酶抑制剂。