Antiviral agents
    4.
    发明授权
    Antiviral agents 失效
    抗病毒剂

    公开(公告)号:US5449664A

    公开(公告)日:1995-09-12

    申请号:US808968

    申请日:1991-12-16

    摘要: Nucleoside compounds of the formula ##STR1## wherein: B is a purine or a pyrimidine;X and X' are H, OH or F, provided that at least one is H;Y and Y' are H, OH, OCH.sub.3 or F, provided that at least one is H;Y' and Z together form a cyclic phosphate ester, provided that Y is H; orZ is ##STR2## where n is zero, one, two or three; and Z' is N.sub.3 or OCH.sub.3 ; provided that when X' and Y' are OH and Z' is N.sub.3, B is not cytosine, andwhen X' and Y' are OH and Z' is OCH.sub.3, B is not uracil, adenine or cytosine;and the pharmaceutically acceptable esters, ethers and salts thereof, have been found to have potent antiviral activity with a high therapeutic ratio.

    摘要翻译: 式IMA的核苷化合物其中:B是嘌呤或嘧啶; X和X'是H,OH或F,条件是至少一个是H; Y和Y'是H,OH,OCH 3或F,条件是至少一个是H; Y'和Z一起形成环状磷酸酯,条件是Y是H; 或Z为,其中n为零,一,二或三; Z'为N 3或OCH 3; 条件是当X'和Y'为OH且Z'为N 3时,B不是胞嘧啶,当X'和Y'为OH且Z'为OCH 3时,B不是尿嘧啶,腺嘌呤或胞嘧啶; 已经发现其药学上可接受的酯,醚和盐具有高治疗比的有效的抗病毒活性。

    Substituted 9-(1-O- or 3-O-monosubstituted or 1,3-di-O-substituted
propoxymethyl)purines as antiviral agents
    5.
    发明授权
    Substituted 9-(1-O- or 3-O-monosubstituted or 1,3-di-O-substituted propoxymethyl)purines as antiviral agents 失效
    取代的9-(1-O-或3-O-单取代或1,3-二-O-取代的丙氧基甲基)嘌呤作为抗病毒剂

    公开(公告)号:US4609661A

    公开(公告)日:1986-09-02

    申请号:US744585

    申请日:1985-06-13

    摘要: Compounds useful as antiviral agents are defined by the following formula: ##STR1## wherein R.sup.1 is hydrogen, --C(Y)OR.sup.7 or --C(O)NHR.sup.7 wherein R.sup.7 is alkyl of one to twelve carbon atoms, alkenyl of two to twelve carbon atoms, cyclopentyl, cyclohexyl, phenyl or benzyl;R.sup.2 is --C(Y)OR.sup.7 or --C(O)NHR.sup.7 wherein R.sup.7 is as defined above;Y is oxygen or sulfur;R.sup.3 is hydrogen, halo, thio, lower alkylthio of one to six carbon atoms, azido, NR.sup.9 R.sup.10 wherein R.sup.9 and R.sup.10 are independently hydrogen or lower alkyl of one to six carbon atoms or --NHC(O)R.sup.8 wherein R.sup.8 is hydrogen, alkyl of one to nineteen carbon atoms or 1-adamantyl; and(a) R.sup.6 is hydrogen, halo, lower alkoxy of one to six carbon atoms, azido, thio, lower alkylthio of one to six carbon atoms, --NR.sup.9 R.sup.10 wherein R.sup.9 and R.sup.10 are as defined above or --NHC(O)R.sup.8 wherein R.sup.8 is as defined above and R.sup.4 together with R.sup.5 is a bond; or(b) R.sup.5 together with R.sup.6 is a keto group and R.sup.4 is hydrogen.

    摘要翻译: 可用作抗病毒剂的化合物由下式定义:其中R 1是氢,-C(Y)OR 7或-C(O)NHR 7,其中R 7是1至12个碳原子的烷基, 至十二个碳原子,环戊基,环己基,苯基或苄基; R 2是-C(Y)OR 7或-C(O)NHR 7,其中R 7如上所定义; Y是氧或硫; R3是氢,卤素,硫代,1-6个碳原子的低级烷硫基,叠氮基,NR9R10,其中R9和R10独立地是氢或1-6个碳原子的低级烷基或-NHC(O)R8,其中R8是氢, 一至十九个碳原子或1-金刚烷基; 和(a)R6是1-6个碳原子的氢,卤素,低级烷氧基,1-6个碳原子的叠氮基,硫代,低级烷硫基,-NR9R10,其中R9和R10如上所定义,或-NHC(O)R 8,其中 R8如上所定义,R4与R5一起是键; 或(b)R 5与R 6一起为酮基,且R 4为氢。

    Substituted 9-(1-0- or 3-0-monosubstituted or 1,3-Di-0-substituted
propoxymethyl)-purines as antiviral agents
    8.
    发明授权
    Substituted 9-(1-0- or 3-0-monosubstituted or 1,3-Di-0-substituted propoxymethyl)-purines as antiviral agents 失效
    取代的9-(1-0或3-0-单取代或1,3-二-O-取代的丙氧基甲基) - 嘌呤作为抗病毒剂

    公开(公告)号:US4556659A

    公开(公告)日:1985-12-03

    申请号:US406583

    申请日:1982-08-09

    摘要: Compounds useful as antiviral agents are defined by the following formula: ##STR1## wherein R.sup.1 is hydrogen, --C(Y)OR.sup.7 or --C(O)NHR.sup.7 wherein R.sup.7 is alkyl of one to twelve carbon atoms, alkenyl of two to twelve carbon atoms, cyclopentyl, cyclohexyl, phenyl or benzyl;R.sup.2 is --C(Y)OR.sup.7 or --C(O)NHR.sup.7 wherein R.sup.7 is as defined above;Y is oxygen or sulfur;R.sup.3 is hydrogen, halo, thio, lower alkylthio of one to six carbon atoms, azido, NR.sup.9 R.sup.10 wherein R.sup.9 and R.sup.10 are independently hydrogen or lower alkyl of one to six carbon atoms or --NHC(O)R.sup.8 wherein R.sup.8 is hydrogen, alkyl of one to nineteen carbon atoms or 1-adamantyl; and(a) R.sup.6 is hydrogen, halo, lower alkoxy of one to six carbon atoms, azido, thio, lower alkylthio of one to six carbon atoms, --NR.sup.9 R.sup.10 wherein R.sup.9 and R.sup.10 are as defined above or --NHC(O)R.sup.8 wherein R.sup.8 is as defined above and R.sup.4 together with R.sup.5 is a bond; or(b) R.sup.5 together with R.sup.6 is a keto group and R.sup.4 is hydrogen.

    摘要翻译: 可用作抗病毒剂的化合物由下式定义:其中R 1是氢,-C(Y)OR 7或-C(O)NHR 7,其中R 7是1至12个碳原子的烷基, 至十二个碳原子,环戊基,环己基,苯基或苄基; R 2是-C(Y)OR 7或-C(O)NHR 7,其中R 7如上所定义; Y是氧或硫; R3是氢,卤素,硫代,1-6个碳原子的低级烷硫基,叠氮基,NR9R10,其中R9和R10独立地是氢或1-6个碳原子的低级烷基或-NHC(O)R8,其中R8是氢, 一至十九个碳原子或1-金刚烷基; 和(a)R6是1-6个碳原子的氢,卤素,低级烷氧基,1-6个碳原子的叠氮基,硫代,低级烷硫基,-NR9R10,其中R9和R10如上所定义,或-NHC(O)R 8,其中 R8如上所定义,R4与R5一起是键; 或(b)R 5与R 6一起为酮基,且R 4为氢。

    Process for preparing guanine derivatives
    9.
    发明授权
    Process for preparing guanine derivatives 失效
    制备鸟嘌呤衍生物的方法

    公开(公告)号:US4803271A

    公开(公告)日:1989-02-07

    申请号:US59290

    申请日:1987-06-08

    摘要: Compounds useful as antiviral agents are defined by the following formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof whereinR.sup.1 is hydrogen or --C(O)R.sup.7 wherein R.sup.7 is hydrogen, alkyl of one to nineteen carbon atoms, hydroxyalkyl of one to eight carbon atoms, alkoxyalkyl of two to nine carbon atoms, alkenyl of two to nineteen carbon atoms, phenyl, 1-adamantyl or 2-carboxyethyl and the pharmaceutically acceptable alkali metal salts thereof;R.sup.2 is --C(O)R.sup.7 is as defined above;R.sup.3 is hydrogen, halo, thio, lower alkylthio of one to six carbon atoms, azido, NR.sup.9 R.sup.10 wherein R.sup.9 and R.sup.10 are independently hydrogen or lower alkyl of one to six carbon atoms or --NHC(O)R.sup.8 wherein R.sup.8 is hydrogen, alkyl of one to nineteen carbon atoms or 1-adamantyl; and(a) R.sup.6 is hydrogen, halo, lower alkoxy of one to six carbon atoms, azido, thio, lower alkylthio of one to six carbon atoms, --NR.sup.9 R.sup.10 and R.sup.9 and R.sup.10 are as defined above or --NHC(O)R.sup.8 is as defined above and R.sup.4 together with R.sup.5 is a bond; or(b) R.sup.5 together with R.sup.6 is a keto group and R.sup.4 is hydrogen.

    摘要翻译: 可用作抗病毒剂的化合物由下式定义:其中R 1是氢或-C(O)R 7,其中R 7是氢,一个至十九个碳原子的烷基,或其药学上可接受的酸加成盐, 1至8个碳原子的羟烷基,2至9个碳原子的烷氧基烷基,2至19个碳原子的烯基,苯基,1-金刚烷基或2-羧乙基及其药学上可接受的碱金属盐; R2是-C(O)R7如上所定义; R3是氢,卤素,硫代,1-6个碳原子的低级烷硫基,叠氮基,NR9R10,其中R9和R10独立地是氢或1-6个碳原子的低级烷基或-NHC(O)R8,其中R8是氢, 一至十九个碳原子或1-金刚烷基; 和(a)R6是1-6个碳原子的氢,卤素,低级烷氧基,1至6个碳原子的叠氮基,硫代,低级烷硫基,-NR9R10和R9和R10如上所定义或-NHC(O)R 8是 如上所定义,R 4与R 5一起是键; 或(b)R 5与R 6一起为酮基,且R 4为氢。

    Substituted 9-(1 or 3-monoacyloxy or 1,3-diacyloxy-2-propoxymethyl)
purines as antiviral agent
    10.
    发明授权
    Substituted 9-(1 or 3-monoacyloxy or 1,3-diacyloxy-2-propoxymethyl) purines as antiviral agent 失效
    取代9-(1或3-单酰氧基或1,3-二酰氧基-2-丙氧基甲基)嘌呤作为抗病毒剂

    公开(公告)号:US5250535A

    公开(公告)日:1993-10-05

    申请号:US451262

    申请日:1982-12-22

    摘要: Compounds useful as antiviral agents are defined by the following formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is hydrogen or --C(O)R.sup.7 wherein R.sup.7 is hydrogen, alkyl of one to nineteen carbon atoms, hydroxyalkyl of one to eight carbon atoms, alkoxyalkyl of two to nine carbon atoms, alkenyl of two to nineteen carbon atoms, phenyl, 1-adamantyl or 2-carboxyethyl and the pharmaceutically acceptable alkali metal salts thereof;R.sup.2 is --C(O)R.sup.7 wherein R.sup.7 is as defined above;R.sup.3 is hydrogen, halo, thio, lower alkylthio of one to six carbon atoms, azido, NR.sup.9 R.sup.10 wherein R.sup.9 and R.sup.10 are independently hydrogen or lower alkyl of one to six carbon atoms or --NHC(O)R.sup.8 wherein R.sup.8 is hydrogen, alkyl of one to nineteen carbon atoms or 1-adamantyl; and(a) R.sup.6 is hydrogen, halo, lower alkoxy of one to six carbon atoms, azido, thio, lower alkylthio of one to six carbon atoms, --NR.sup.9 R.sup.10 wherein R.sup.9 and R.sup.10 are as defined above or --NHC(O)R.sup.8 wherein R.sup.8 is as defined above and R.sup.4 together with R.sup.5 is a bond; or(b) R.sup.5 together with R.sup.6 is a keto group and R.sup.4 is hydrogen.

    摘要翻译: 可用作抗病毒剂的化合物由下式定义:其中R 1是氢或-C(O)R 7,其中R 7是氢,一个至十九个碳原子的烷基,或其药学上可接受的酸加成盐, 1至8个碳原子的羟烷基,2至9个碳原子的烷氧基烷基,2至19个碳原子的烯基,苯基,1-金刚烷基或2-羧乙基及其药学上可接受的碱金属盐; R 2是-C(O)R 7,其中R 7如上所定义; R3是氢,卤素,硫代,1-6个碳原子的低级烷硫基,叠氮基,NR9R10,其中R9和R10独立地是氢或1-6个碳原子的低级烷基或-NHC(O)R8,其中R8是氢, 一至十九个碳原子或1-金刚烷基; 和(a)R6是1-6个碳原子的氢,卤素,低级烷氧基,1-6个碳原子的叠氮基,硫代,低级烷硫基,-NR9R10,其中R9和R10如上所定义,或-NHC(O)R 8,其中 R8如上所定义,R4与R5一起是键; 或(b)R 5与R 6一起为酮基,且R 4为氢。