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    Method of treating herpes simplex viral infection employing pyrimidine derivatives
    12.
    发明授权
    Method of treating herpes simplex viral infection employing pyrimidine derivatives 失效
    使用嘧啶衍生物治疗单纯疱疹病毒感染的方法

    公开(公告)号：US5010060A

    公开(公告)日：1991-04-23

    申请号：US342277

    申请日：1989-04-24

    申请人： Robert W. Lambert ,  Joseph A. Martin ,  Gareth J. Thomas

    发明人： Robert W. Lambert ,  Joseph A. Martin ,  Gareth J. Thomas

    IPC分类号： C07D405/04 ,  A61K31/505 ,  A61P31/12 ,  C07D405/14 ,  C07D409/14 ,  C07H19/06

    CPC分类号： C07H19/06

    摘要： Compounds of the formula ##STR1## wherein R.sup.1 is halogen, C.sub.1-4 -alkyl, halo-(C.sub.1-4 -alkyl) or C.sub.2-4 -alkanoyl,R.sup.2 is hydrogen, hydroxy, C.sub.1-4 -alkoxy, C.sub.1-4 -alkylthio or phenyl-(C.sub.1-4 -alkoxy) or, when X is O, also acyloxy,R.sup.3 is hydrogen or C.sub.1-4 -alkyl,R.sup.4 is a carbocyclic group or a heterocyclic group,R.sup.5 is hydrogen or fluorine,m stands for zero, 1 or 2,X is O or NH and Y is a direct bond, --CH.dbd.CH--, --C.tbd.C-- or a group of the formula of--(Z).sub.n --A-- (a) in which A is a C.sub.1-8 -alkylene group which is optionally substituted by one or two phenyl groups, is O, S, SO or SO.sub.2 and n stands for zero or 1, with the proviso that R.sup.1 is different from iodine, when R.sup.2 is hydroxy or benzoyloxy, R.sup.3 is hydrogen, R.sup.4 is unsubstituted phenyl, R.sup.5 is hydrogen, m stands for zero, X is O, and Y is a direct bond,and tautomers thereof, which possess antiviral activity and can therefore be used in the form of medicaments for the control and prevention of viral infections are described. The compounds of formula I can be prepared according to known methods.

    Amino acid derivatives having antiviral activity
    14.
    发明授权
    Amino acid derivatives having antiviral activity 失效
    具有抗病毒活性的氨基酸衍生物

    公开(公告)号：US5583248A

    公开(公告)日：1996-12-10

    申请号：US417315

    申请日：1995-04-05

    申请人： Joseph A. Martin ,  Gareth J. Thomas

    发明人： Joseph A. Martin ,  Gareth J. Thomas

    IPC分类号： A61K31/095 ,  A61K20060101 ,  A61K31/13 ,  A61K31/16 ,  A61K31/27 ,  A61K31/275 ,  A61K31/47 ,  A61P31/12 ,  C07C20060101 ,  C07C7/00 ,  C07C233/18 ,  C07C233/22 ,  C07C237/08 ,  C07C237/12 ,  C07C237/24 ,  C07C255/19 ,  C07C255/21 ,  C07C255/29 ,  C07C271/16 ,  C07C271/20 ,  C07C271/22 ,  C07C271/48 ,  C07C321/20 ,  C07C323/25 ,  C07C323/26 ,  C07C323/60 ,  C07D215/48 ,  C07D263/06 ,  C07C233/58

    CPC分类号： C07C271/22 ,  C07C237/24 ,  C07C255/29 ,  C07C323/60 ,  C07D215/48 ,  C07C2101/14

    摘要： Compounds of the formula: ##STR1## wherein R.sup.1 is alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, aralkanoyl, heterocyclylcarbonyl or a group of the formula: ##STR2## R.sup.2 is alkyl, cycloalkylalkyl or aralkyl; R.sup.3 is hydrogen and R.sup.4 is hydroxy or R.sup.3 and R.sup.4 together are oxo; R.sup.5 is alkoxycarbonyl or alkylcarbamoyl; R.sup.6 and R.sup.7 together are trimethylene or tetramethylene optionally substituted by alkyl or on adjacent carbon atoms by tetramethylene; R.sup.8 is alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, aroyl, aralkanoyl or heteroeyelylearbonyl; and R.sup.9 is alkyl, cycloalkyl, cycloalkylalkyl, aralkyl, cyanoalkyl, carbamoyl-alkyl, alkylthioalkyl, alkoxyalkyl or alkoxycarbonylalkyl:and pharmaceutically acceptable acid addition salts of those compounds of formula I which are basic, inhibit aspartyl proteases of viral origin and can be used in the form of medicaments for the prophylaxis or treatment of viral infections. They can be manufactured according to generally known methods.

    摘要翻译： 下式的化合物：其中R 1是烷氧基羰基，芳烷氧基羰基，烷酰基，芳烷酰基，杂环基羰基或下式基团：（ⅰ）R 2是烷基，环烷基烷基或芳烷基; R3是氢，R4是羟基或R3和R4一起是氧代; R5是烷氧基羰基或烷基氨基甲酰基; R6和R7一起是三甲基或四亚甲基，任选被烷基或相邻碳原子上被四亚甲基取代; R8是烷氧基羰基，芳烷氧基羰基，烷酰基，芳酰基，芳烷酰基或杂烯基羰基; 并且R 9为烷基，环烷基，环烷基烷基，芳烷基，氰基烷基，氨基甲酰基 - 烷基，烷硫基烷基，烷氧基烷基或烷氧基羰基烷基，以及那些碱式的式I化合物的药学上可接受的酸加成盐，可抑制病毒来源的天冬氨酰蛋白酶， 用于预防或治疗病毒感染的药物的形式。 它们可以根据通常已知的方法制造。

    Pyrimidine derivatives
    15.
    发明授权
    Pyrimidine derivatives 失效
    嘧啶衍生物

    公开(公告)号：US4851519A

    公开(公告)日：1989-07-25

    申请号：US080021

    申请日：1987-07-31

    申请人： Robert W. Lambert ,  Joseph A. Martin ,  Gareth J. Thomas

    发明人： Robert W. Lambert ,  Joseph A. Martin ,  Gareth J. Thomas

    IPC分类号： C07D405/04 ,  A61K31/505 ,  A61P31/12 ,  C07D405/14 ,  C07D409/14 ,  C07H19/06

    CPC分类号： C07H19/06

    摘要： Compounds of the formula ##STR1## wherein R.sup.1 is halogen, C.sub.1-4 -alkyl, halo-(C.sub.1-4 -alkyl) or C.sub.2-4 -alkanoyl,R.sup.2 is hydrogen, hydroxy, C.sub.1-4 alkoxy, C.sub.1-4 -alkylthio or phenyl-(C.sub.1-4 -alkoxy) or , when X is O, also acyloxy,R.sup.3 is hydrogen or C.sub.1-4 -alkyl,R.sup.4 is a carbocyclic group or a heterocyclic group,R.sup.5 is hydrogen or fluorine,m stands for zero, 1 or 2,X is O or NH and Y is a direct bond, --CH.dbd.CH--, --C.tbd.C-- or a group of the formula of--(Z).sub.n --A-- (a)in which A is a C.sub.1-8 alkylene group which is optionally substituted by one or two phenyl groups,Z is O, S, SO or SO.sub.2 and n stands for zero or 1, with the proviso that R.sup.1 is different from iodine, when R.sup.2 is hydroxy or benzoyloxy, R.sup.3 is hydrogen,R.sup.4 is unsubstituted phenyl, R.sup.5 is hydrogen, m stands for zero, X is O, and Y is a direct bond, and tautomers thereof, which possess antiviral activity and can therefore be used in the form of medicaments for the control and prevention of viral infections are described. The compounds of formula I can be prepared according to known methods.

    摘要翻译： 式Ⅰ化合物其中R1是卤素，C1-4烷基，卤代（C1-4烷基）或C2-4-烷酰基，R2是氢，羟基，C1-4烷氧基，C1-4烷硫基 或苯基 - （C 1-4 - 烷氧基），或者当X是O时也是酰氧基，R 3是氢或C 1-4 - 烷基，R 4是碳环基或杂环基，R 5是氢或氟，m代表0 ，1或2，X是O或NH，Y是直接键，-CH = CH-，-C 3BOND C-或 - 式（Z）nA（a）的基团，其中A是C1 -8亚烷基，其任选被一个或两个苯基取代，Z是O，S，SO或SO 2，n代表0或1，条件是R1不同于碘，当R2是羟基或苯甲酰氧基时，R3是 氢，R4是未取代的苯基，R5是氢，m代表0，X是O，Y是直接键，其互变异构体具有抗病毒活性，因此可以以用于控制和预防的药物的形式使用 描述了病毒感染。 式I化合物可以根据已知方法制备。

    Pyrimidine derivatives
    17.
    发明授权
    Pyrimidine derivatives 失效
    嘧啶衍生物

    公开(公告)号：US4882316A

    公开(公告)日：1989-11-21

    申请号：US79741

    申请日：1987-07-30

    申请人： Robert W. Lambert ,  Joseph A. Martin ,  Gareth J. Thomas

    发明人： Robert W. Lambert ,  Joseph A. Martin ,  Gareth J. Thomas

    IPC分类号： C07D405/06 ,  A61K31/505 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61P31/12 ,  C07D405/04 ,  C07H19/06 ,  C12N9/99

    CPC分类号： C07H19/06

    摘要： Compounds of the formula ##STR1## wherein R.sup.1 is halogen, C.sub.1-4 -alkyl or halo-(C.sub.1-4 - alkyl), R.sup.2 is hydrogen, hydroxy or acyloxy, R.sup.3 and R.sup.4 each are hydrogen or C.sub.1-4 -alkyl, R.sup.5 is aryl or aryloxy, X is O or NH and Y is --CO--CH.sub.2 --, --CH(OH)--CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --S--, --SO-- or --SO.sub.2 --,and tautomers thereof are described. Compounds of formula I and their tautomers possess antiviral activity and can be used in the form of medicaments for the control and prevention of viral infections.

    摘要翻译： 其中R 1是卤素，C 1-4 - 烷基或卤代（C 1-4 - 烷基），R 2是氢，羟基或酰氧基，R 3和R 4各自是氢或C 1-4 - 烷基， R5是芳基或芳氧基，X是O或NH，Y是-CO-CH2-，-CH（OH）-CH2-，-CH2-CH2-，-S-，-SO-或-SO2-，及其互变异构体 被描述。 式I化合物及其互变异构体具有抗病毒活性，可用于控制和预防病毒感染的药物形式。

    Cyclic compounds
    18.
    发明授权
    Cyclic compounds 失效
    环状化合物

    公开(公告)号：US4302398A

    公开(公告)日：1981-11-24

    申请号：US175724

    申请日：1980-08-06

    申请人： Cedric H. Hassall ,  Michael J. Broadhurst ,  Gareth J. Thomas

    发明人： Cedric H. Hassall ,  Michael J. Broadhurst ,  Gareth J. Thomas

    IPC分类号： C07C41/18 ,  C07C43/23 ,  C07C45/56 ,  C07D317/26 ,  C07F5/02 ,  C07C50/16 ,  C07C107/02

    CPC分类号： C07F5/025 ,  C07C45/567 ,  C07D317/26

    摘要： The present invention relates to naphthacene derivatives. More particularly, the invention is concerned with a process for the manufacture of hexahydronaphthacene derivatives and with certain of said derivatives per se. The invention is also concerned with novel intermediates occurring in said process and with the preparation thereof.There are presented hexahydronaphthacene derivatives of the formula ##STR1## wherein R.sup.1 represents a lower alkyl or esterified carboxy group or a group of the formula ##STR2## , in which R.sup.2 and R.sup.3 together form an oxo group or a protected oxo group and X represents a hydrogen atom or a hydroxy or acyloxy group, or--(CH.sub.2).sub.n --OY bin which n stands for 1 or 2 and Y represents a hydrogen atom or an alkyl or acyl group.Also presented are intermediates and a process to produce the compounds of formula I.

    摘要翻译： 本发明涉及并四苯衍生物。 更具体地说，本发明涉及制备六氢萘并萘衍生物的方法以及某些所述衍生物本身。 本发明还涉及在所述方法和其制备中发生的新型中间体。 本发明提供下式的六氢萘并衍生物，其中R 1表示低级烷基或酯化羧基或下式的基团：其中R 2和R 3一起形成氧代基或被保护的氧代基，X代表 表示氢原子或羟基或酰氧基，或 - （CH 2）n -OY b，其中n表示1或2，Y表示氢原子或烷基或酰基。 还提出了产生式I化合物的中间体和方法。

    Anthracycline glycosides
    20.
    发明授权
    Anthracycline glycosides 失效
    蒽环类苷

    公开(公告)号：US4591636A

    公开(公告)日：1986-05-27

    申请号：US682448

    申请日：1984-12-17

    申请人： Michael J. Broadhurst ,  Cedric H. Hassall ,  Gareth J. Thomas

    发明人： Michael J. Broadhurst ,  Cedric H. Hassall ,  Gareth J. Thomas

    IPC分类号： C07D317/72 ,  C07D339/06 ,  C07F5/02 ,  C07H15/252

    CPC分类号： C07D317/72 ,  C07D339/06 ,  C07F5/025 ,  C07H15/252

    摘要： The invention relates to compounds of the formula ##STR1## wherein R is lower alkyl or a carboxy group or a group of the formula--(CH.sub.2).sub.n --OY a in which n stands for 1 or 2 and Y is hydrogen or alkyl and R.sup.Y and R.sup.z each are hydrogen or one of R.sup.Y and R.sup.z is hydrogen and the other is hydroxy,and pharmaceutically acceptable acid addition salts thereof.These compounds and salts possess antibiotic and antitumor activity and can be used as medicaments in the form of pharmaceutical preparations.

    摘要翻译： 本发明涉及下式化合物其中R是低级烷基或羧基或式 - （CH 2）n -OY a的基团，其中n代表1或2，Y是氢或烷基， RY和Rz各自为氢或RY和Rz之一为氢，另一个为羟基，及其药学上可接受的酸加成盐。 这些化合物和盐具有抗生素和抗肿瘤活性，可用作药物制剂形式的药物。