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41 条记录 (耗时 0.034 秒)

    ANTI-VIRAL PYRIMIDINE NUCLEOSIDE ANALOGUES
    32.
    发明申请
    ANTI-VIRAL PYRIMIDINE NUCLEOSIDE ANALOGUES 有权
    抗虚拟吡啶类核苷类似物

    公开(公告)号：US20110015147A1

    公开(公告)日：2011-01-20

    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： A61K31/7068 ,  C07H19/09 ,  A61P31/12

    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。

    NOVEL NUCLEOTIDE ANALOGUES AS PRECUSOR MOLECULES FOR ANTIVIRALS
    33.
    发明申请
    NOVEL NUCLEOTIDE ANALOGUES AS PRECUSOR MOLECULES FOR ANTIVIRALS 有权
    新型核苷酸类似物作为抗病毒剂的分子分子

    公开(公告)号：US20100099869A1

    公开(公告)日：2010-04-22

    申请号：US12514285

    申请日：2007-11-08

    申请人： Bruno Canard ,  Karine Alvarez ,  Karine Barral ,  Jean-Louis Romette ,  Johan Neyts ,  Jan Balzarini

    发明人： Bruno Canard ,  Karine Alvarez ,  Karine Barral ,  Jean-Louis Romette ,  Johan Neyts ,  Jan Balzarini

    IPC分类号： C07F9/02

    CPC分类号： C07F9/65616

    摘要： This invention relates to a purine or pyrimidine phosphonate compound of formula (I) or pharmaceutically acceptable salt thereof; wherein B, X, and R1-R3 are as defined in classes and subclasses herein. These compounds may be used as antiviral precursors. The invention also relates to therapeutic compositions of these compounds and their use for the preparation of a medication for testing and/or preventing a viral infection in a patient. The invention also provides methods for making these compounds. In particular, the invention provides an H-phosphinate precursor intermediate of formula (II) wherein B is a purine or pyrimidine base as defined herein and R1 is selected from the group comprising a hydrogen atom, and a methyl, ethyl, hydroxymethyl, hydroxyethyl and C1-6haloalkyl group.

    摘要翻译： 本发明涉及式（I）的嘌呤或嘧啶膦酸酯化合物或其药学上可接受的盐; 其中B，X和R 1 -R 3如本文中的类别和子类所定义。 这些化合物可以用作抗病毒前体。 本发明还涉及这些化合物的治疗组合物及其用于制备用于测试和/或预防患者病毒感染的药物的用途。 本发明还提供了制备这些化合物的方法。 特别地，本发明提供了式（II）的H-次膦酸盐前体中间体，其中B是如本文所定义的嘌呤或嘧啶碱基，R 1选自氢原子和甲基，乙基，羟甲基，羟乙基和 C 1-6卤代烷基。

    Prodrugs Cleavable by Cd26
    34.
    发明申请
    Prodrugs Cleavable by Cd26 失效
    前药可被Cd26切割

    公开(公告)号：US20070275900A1

    公开(公告)日：2007-11-29

    申请号：US10555930

    申请日：2004-05-10

    申请人： Jan Balzarini

    发明人： Jan Balzarini

    IPC分类号： A61K38/04 ,  A61P25/00

    CPC分类号： C07D493/04 ,  A61K38/00 ,  A61K47/64 ,  C07H15/252 ,  C07K5/06052 ,  C07K5/06113 ,  C07K5/0808 ,  C07K5/1008 ,  C07K5/101 ,  C07K5/1019 ,  C07K5/1021 ,  C07K7/06 ,  C07K9/003

    摘要： The present invention provides a new prodrug technology and new prodrugs in order to increase the solubility, to modulate plasma protein binding or to enhance the biovailability of a drug. In the present invention the prodrugs are conjugates of a therapeutic compound and a peptide (eg tetrapeptide or hexapeptide) wherein the conjugate is cleavable by dipeptidyl-peptidases, more preferably by CD26, also known as DPPIV (dipeptidyl aminodipeptidase IV). The present invention furthermore provides a method of producing said prodrugs, to enhance brain and lymphatic delivery of drugs and/or to extend drug half-lives in plasma.

    摘要翻译： 本发明提供新的前药技术和新的前体药物，以增加溶解度，调节血浆蛋白结合或提高药物的生物利用度。 在本发明中，前药是治疗化合物和肽（例如四肽或六肽）的缀合物，其中缀合物可被二肽基肽酶切割，更优选由CD26（也称为DPPIV（二肽基氨基二肽酶IV））切割。 本发明还提供了一种制备所述前药的方法，以增强药物的脑和淋巴递送和/或延长血浆中的药物半衰期。

    Heterocyclic compounds for use in the treatment of viral infections
    35.
    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
    40.
    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