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    Anti-Viral Pyrimidine Nucleoside Derivatives
    1.
    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 derivatives
    2.
    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。

    Anti-viral pyrimidine nucleoside analogues
    5.
    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。

    Chemical compounds
    9.
    发明授权
    Chemical compounds 失效

    公开(公告)号：US07018989B2

    公开(公告)日：2006-03-28

    申请号：US10216940

    申请日：2002-08-12

    申请人： Christopher McGuigan ,  Jan Balzarini

    发明人： Christopher McGuigan ,  Jan Balzarini

    IPC分类号： C07F9/6561 ,  C07F9/6558 ,  C07F9/6512 ,  A61K31/675 ,  A61P31/18

    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 phenoxyphosphoroamidates. 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.

    Antiviral purine derivatives
    10.
    发明授权
    Antiviral purine derivatives 失效
    抗病毒嘌呤衍生物

    公开(公告)号：US06638919B2

    公开(公告)日：2003-10-28

    申请号：US09825554

    申请日：2001-03-27

    申请人： Christopher McGuigan ,  Jan Balzarini

    发明人： Christopher McGuigan ,  Jan Balzarini

    IPC分类号： A61K31675

    CPC分类号： C07F9/65616

    摘要： Compounds of the formula wherein Ar is aryl, R1 and R2 are hydrogen alkyl, alkyl substituted with phenyl, and aryl, O, NH, NR4 and S, R5 is hydrogen, alkyl or aryl or alkylene when taken with R1, and R3 is hydrogen, alkyl, alkyl substituted with phenyl, aryl, a heterocyclic group or a polycyclic group, are antiviral agents. A typical embodiment is (1S,4R)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol O-[phenyl-(methoxy-L-alaninyl)]phosphate.

    摘要翻译： 化合物Ar是芳基，R 1和R 2是氢烷基，被苯基取代的烷基和芳基，O，NH，NR 4和S，R 5是氢，烷基或芳基 或者当R 1取代时为亚烷基，R 3为氢，烷基，被苯基，芳基，杂环基或多环取代的烷基为抗病毒剂。 典型的实施方案是（1S，4R）-4- [2-氨基-6-（环丙基氨基）-9H-嘌呤-9-基] -2-环戊烯-1-甲醇O- [苯基 - （甲氧基-L-丙氨酰基 ）]磷酸盐。