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    Anti-Viral Pyrimidine Nucleoside Derivatives
    4.
    发明申请
    Anti-Viral Pyrimidine Nucleoside Derivatives 有权
    抗病毒嘧啶核苷衍生物

    公开(公告)号：US20100222295A1

    公开(公告)日：2010-09-02

    申请号：US12226044

    申请日：2007-05-09

    申请人： Christopher McGuigan ,  Jan Balzarini ,  Marco Migliore

    发明人： Christopher McGuigan ,  Jan Balzarini ,  Marco Migliore

    IPC分类号： A61K31/7068 ,  C07H19/23 ,  A61P31/12

    CPC分类号： A61K31/7068 ,  A61K31/7052 ,  A61K31/706 ,  A61K31/7064 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04

    摘要： A compound for use in the treatment or prophylaxis of viral infections such, for example as chicken pox or shingles caused by the Varicella Zoster virus, said compound having the general formula (II): wherein X is O, S, NH or CH2, Y is O, S or NH, Z is O, S or CH2, R1 is C1-6 alkyl, preferably n-alkyl, e.g., n-pentyl or n-hexyl, and one of R2 and R3 is OH, and the other of R3 and R2 is a neutral, non-polar amino acid moiety, or a pharmaceutically acceptable salt or hydrate thereof. Said neutral, non-polar amino acid moiety R2 or R3 may be (IV): in which R4, R5, R6 and R7 are each independently H or C1-2 alkyl. In preferred embodiments, one of R2 or R3 is valine, leucine, isoleucine or alanine, particularly valine.

    摘要翻译： 用于治疗或预防病毒感染的化合物，例如由水痘带状疱疹病毒引起的水痘或带状疱疹，所述具有通式（II）的化合物：其中X是O，S，NH或CH 2，Y 是O，S或NH，Z是O，S或CH 2，R 1是C 1-6烷基，优选正烷基，例如正戊基或正己基，R 2和R 3之一是OH，另一个是 R3和R2是中性的，非极性的氨基酸部分，或其药学上可接受的盐或水合物。 所述中性，非极性氨基酸部分R 2或R 3可以是（Ⅳ）：其中R 4，R 5，R 6和R 7各自独立地为H或C 1-2烷基。 在优选的实施方案中，R2或R3之一是缬氨酸，亮氨酸，异亮氨酸或丙氨酸，特别是缬氨酸。

    Anti-viral pyrimidine nucleoside analogues
    6.
    发明授权
    Anti-viral pyrimidine nucleoside analogues 有权
    抗病毒嘧啶核苷类似物

    公开(公告)号：US08551965B2

    公开(公告)日：2013-10-08

    申请号：US12889980

    申请日：2010-09-24

    申请人： Christopher McGuigan ,  Jan Balzarini

    发明人： Christopher McGuigan ,  Jan Balzarini

    IPC分类号： A61K31/706 ,  A61K31/498 ,  A61K31/4985 ,  C07D403/02 ,  C07D405/04 ,  C07H19/23 ,  C07H19/24

    CPC分类号： C07H19/24 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/706 ,  C07D403/02 ,  C07D405/04 ,  C07D487/04 ,  C07D491/04 ,  C07D498/04 ,  C07H19/06 ,  C07H19/10 ,  C07H19/14 ,  C07H19/23

    摘要： A compound of formula (I) wherein Ar can be one six-membered or two fused six-membered aromatic rings; R8 and R9 can be hydrogen, alkyl, cycloalkyl, halogens, amino, alkylamino, dialkylamino, nitro, cyano, alkyoxy, aryloxy, thiol, alkylthiol, arythiol, or aryl; Q can be O, S or CY2, where Y may be H, alkyl or halogens; X can be O, NH, S, N-alkyl, (CHR2)m where m is 1 to 10, and CY2; Z can be O, S, NH, or N-alkyl; U″ is H and U′ can be H or CH2; wherein: T can be OH, H, halogens, O-alkyl, O-acyl, O-aryl, CN, NH2. or N3; T′ and T″ can be H or halogen; and W can be H or a phosphate group. Compounds show anti-viral activity, for example with respect to varicella zoster virus.

    摘要翻译： 式（I）的化合物，其中Ar可以是一个六元或两个稠合的六元芳环; R 8和R 9可以是氢，烷基，环烷基，卤素，氨基，烷基氨基，二烷基氨基，硝基，氰基，烷氧基，芳氧基，硫醇，烷基硫醇，仲胺或芳基; Q可以是O，S或CY2，其中Y可以是H，烷基或卤素; X可以是O，NH，S，N-烷基，（CHR2）m，其中m是1-10，CY2; Z可以是O，S，NH或N-烷基; U“是H，U'可以是H或CH2; 其中：T可以是OH，H，卤素，O-烷基，O-酰基，O-芳基，CN，NH 2。 或N3; T'和T“可以是H或卤素; W可以是H或磷酸基。 化合物显示出抗病毒活性，例如关于水痘带状疱疹病毒。

    Anti-viral pyrimidine nucleoside derivatives
    7.
    发明授权
    Anti-viral pyrimidine nucleoside derivatives 有权
    抗病毒嘧啶核苷衍生物

    公开(公告)号：US08329664B2

    公开(公告)日：2012-12-11

    申请号：US12226044

    申请日：2007-05-09

    申请人： Christopher McGuigan ,  Jan Balzarini ,  Marco Migliore

    发明人： Christopher McGuigan ,  Jan Balzarini ,  Marco Migliore

    IPC分类号： A01N43/04 ,  A61K31/70

    CPC分类号： A61K31/7068 ,  A61K31/7052 ,  A61K31/706 ,  A61K31/7064 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04

    摘要： A compound for use in the treatment or prophylaxis of viral infections such, for example as chicken pox or shingles caused by the Varicella Zoster virus, said compound having the general formula (II): wherein X is O, S, NH or CH2, Y is O, S or NH, Z is O, S or CH2, R1 is C1-6 alkyl, preferably n-alkyl, e.g., n-pentyl or n-hexyl, and one of R2 and R3 is OH, and the other of R3 and R2 is a neutral, non-polar amino acid moiety, or a pharmaceutically acceptable salt or hydrate thereof. Said neutral, non-polar amino acid moiety R2 or R3 may be (IV): in which R4, R5, R6 and R7 are each independently H or C1-2 alkyl. In preferred embodiments, one of R2 or R3 is valine, leucine, isoleucine or alanine, particularly valine.

    摘要翻译： 用于治疗或预防病毒感染的化合物，例如由水痘带状疱疹病毒引起的水痘或带状疱疹，所述具有通式（II）的化合物：其中X是O，S，NH或CH 2，Y 是O，S或NH，Z是O，S或CH 2，R 1是C 1-6烷基，优选正烷基，例如正戊基或正己基，R 2和R 3之一是OH，另一个是 R3和R2是中性的，非极性的氨基酸部分，或其药学上可接受的盐或水合物。 所述中性，非极性氨基酸部分R 2或R 3可以是（Ⅳ）：其中R 4，R 5，R 6和R 7各自独立地为H或C 1-2烷基。 在优选的实施方案中，R2或R3之一是缬氨酸，亮氨酸，异亮氨酸或丙氨酸，特别是缬氨酸。

    Heterocyclic compounds for use in the treatment of viral infections
    8.
    发明申请
    Heterocyclic compounds for use in the treatment of viral infections 审中-公开
    用于治疗病毒感染的杂环化合物

    公开(公告)号：US20070191373A1

    公开(公告)日：2007-08-16

    申请号：US10551569

    申请日：2004-04-21

    申请人： Christopher McGuigan ,  Jan Balzarini ,  Erik De Clerq

    发明人： Christopher McGuigan ,  Jan Balzarini ,  Erik De Clerq

    IPC分类号： A61K31/53

    CPC分类号： C07D491/04

    摘要： 6-substituted-3-substituted-3H-furo[2,3-d]pyrimidin-2-one and 6-substituted-2-substituted-furo[2,3-d]pyrimidine novel compounds are useful in the treatment of viral infection, in particular cytomegalovirus viral infection. The substituents are independently selected from alkyl, aryl, alkenyl and alkynyl. The preferred substituent at the 6 position is alkyl.

    摘要翻译： 6-取代-3-取代-3H-呋喃并[2,3-d]嘧啶-2-酮和6-取代-2-取代呋喃并[2,3-d]嘧啶新化合物可用于治疗病毒 感染，特别是巨细胞病毒感染。 取代基独立地选自烷基，芳基，烯基和炔基。 6位优选的取代基是烷基。

    Chemical compounds
    9.
    发明授权
    Chemical compounds 失效
    化合物

    公开(公告)号：US06455513B1

    公开(公告)日：2002-09-24

    申请号：US09382084

    申请日：1999-08-24

    申请人： Christopher McGuigan ,  Jan Balzarini

    发明人： Christopher McGuigan ,  Jan Balzarini

    IPC分类号： C07F96561

    CPC分类号： C07H19/10 ,  A61K31/675 ,  C07F9/6512 ,  C07H19/20

    摘要： Aryl substituted phosphoryl derivatives of the formula In which Ar is phenyl, naphthyl, or pyridyl, Y is O or S, X1 is O, NR3, S, CR3R4, CR3W1 or CW1W2, X2 and X6 are a bond or X6 is CH2 and X2 is O, NR3, S, CR3R4, CR3W1 or CW1W2, R3 and R4 are H, alkyl or phenyl, groups, W1 and W2 are heteroatoms, X3 is alkylene, X4 is oxygen or CH2, X5 is a bond or CH2, Z is O, NR5, S, alkyl or phenyl, R5 is H, alkyl or phenyl, J is H, alkyl, phenyl, or a heterocyclic or polycyclic group, Q is O, NR6, S, CR6R7, CR6W3 or CW3W4, R6 and R7 are H, alkyl, or phenyl, and W3 and W4 are hetero atoms, T1 and T2 are H or CH2R8, R8 is H, OH or F, or T1 and T2 together are —CH═CH— or —C(R9)(R10)C(R11)(R12)—, R9 is H, halogeno, CN, NH2, CO-alkyl, or alkyl, R10, R11, and R12 are H, N3, halogen, CN, NH2, CO-alkyl, or alkyl, and B is a purine or pyrimidine base, have antiviral activity, as for example against HIV. Particularly preferred are thymine and adenine derivatives of amino acid phenoxyphosphoroamides. A typical embodiment is 2′,3′-dideoxy-2,′3′-didehydrothymidine 5′-(phenyl methoxy alaninyl) phosphoroamidate which can be prepared from phenyl methoxy alaninyl phosphorochloridate and 2′,3′-dideoxy-2′,3′-didehydrothymidine.

    摘要翻译： 芳基取代的下式的磷酰基衍生物其中Ar为苯基，萘基或吡啶基，Y为O或S，X1为O，NR3，S，CR3R4，CR3W1或CW1W2，X2和X6为键或X6为CH2，X2为 O，NR3，S，CR3R4，CR3W1或CW1W2，R3和R4是H，烷基或苯基，W1和W2是杂原子，X3是亚烷基，X4是氧或CH2，X5是键或CH2，Z是O ，NR5，S，烷基或苯基，R5是H，烷基或苯基，J是H，烷基，苯基或杂环或多环基团，Q是O，NR6，S，CR6R7，CR6W3或CW3W4，R6和R7是 H，烷基或苯基，W3和W4是杂原子，T1和T2是H或CH2R8，R8是H，OH或F，或者T1和T2一起是-CH = CH-或-C（R9） ）C（R 11）（R 12） - ，R 9为H，卤代，CN，NH 2，CO-烷基或烷基，R 10，R 11和R 12为H，N 3，卤素，CN，NH 2， ，B是嘌呤或嘧啶碱基，具有抗病毒活性，例如抗HIV。 特别优选的是氨基酸苯氧基磷酰胺的胸腺嘧啶和腺嘌呤衍生物。 典型的实施方案是2'，3'-二脱氧-2''3'-二脱氢胸苷5' - （苯基甲氧基乙酰基）氨基磷酸酯，其可以由苯基甲氧基乙烯基磷酰氯