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:
The invention relates to the use of bicyclic nucleosides and nucleotides based on formula (II) for the treatment of infectious diseases, and in particular, viral infections.
摘要:
This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.
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; and n is an integer from 10 to 18 or a pharmaceutically acceptable derivative thereof, 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; R 2是乙酰基或三氟乙酰基; 且n为10至18的整数或其药学上可接受的衍生物,其制备方法,含有它们的药物制剂或其在预防或治疗病毒感染中的用途
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; X is CONH, NHCO or O; n is an integer from 2 to 6; and Y is C2–C8 alkyl C3-8 cycloalkyl, C1–C4 alkoxyalkyl, an amino acid or dipeptide, or a pharmaceutically acceptable derivative thereof, methods for their preparation, pharmaceutical formulations containing them or their use in the prevention or treatment of a viral infection
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:
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。
摘要:
Derivatives and analogues of 2-deoxy-2,3-didehydro-N-acetyl neuraminic acid, pharmaceutical formulations thereof, methods for their preparation and their use in the treatment of viral infections, in particular influenza, are described.