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    Nucleotide analogues as precursor molecules for antivirals
    2.
    发明授权
    Nucleotide analogues as precursor molecules for antivirals 有权
    核苷酸类似物作为抗病毒药物的前体分子

    公开(公告)号：US08884011B2

    公开(公告)日：2014-11-11

    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 ,  C07F9/6561

    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。

    Method to treat infections using anti-infective agents
    3.
    发明授权
    Method to treat infections using anti-infective agents 有权
    使用抗感染剂治疗感染的方法

    公开(公告)号：US08450318B2

    公开(公告)日：2013-05-28

    申请号：US12531971

    申请日：2008-03-18

    申请人： Monika Mazik ,  Jan Balzarini

    发明人： Monika Mazik ,  Jan Balzarini

    IPC分类号： A01N43/58 ,  A01N43/40 ,  A61K31/50 ,  A61K31/435

    CPC分类号： A61K31/15 ,  A61K31/167 ,  A61K31/4375 ,  A61K31/44 ,  A61K47/55

    摘要： Molecules having a spacer unit, linker and recognition unit(s) are used for the treatment of various diseases, disorders and conditions. The compounds are useful in treating infectious diseases and diseases, disorders or conditions related thereto. Further, the methods for treating diseases, disorders or conditions involve recognition and binding of carbohydrate structures.

    摘要翻译： 具有间隔单元，连接体和识别单元的分子用于治疗各种疾病，病症和病症。 该化合物可用于治疗感染性疾病及其相关疾病，病症或病症。 此外，用于治疗疾病，病症或病症的方法涉及碳水化合物结构的识别和结合。

    Antiviral therapies
    6.
    发明授权
    Antiviral therapies 有权
    抗病毒治疗

    公开(公告)号：US08735416B2

    公开(公告)日：2014-05-27

    申请号：US13453184

    申请日：2012-04-23

    申请人： Jan Balzarini ,  Monika Mazik

    发明人： Jan Balzarini ,  Monika Mazik

    IPC分类号： A61K31/69

    CPC分类号： C07D239/42 ,  A61K31/165 ,  A61K31/30 ,  A61K31/409 ,  A61K31/444 ,  A61K31/69 ,  A61K31/715 ,  A61K38/168 ,  C07D213/74

    摘要： The field of the invention relates to the use of carbohydrate binding compounds as a medicine, their use to treat or prevent viral infections, their use to manufacture a medicine to treat or prevent viral infections and their use in a vaccination strategy. The present invention relates to the use of said compounds to manufacture a medicine to treat or prevent viral infections of subject, more in particular infections with viruses having glycosilated envelope proteins such as Retroviridae (i.e., Lentivirinae), like HIV (human immunodeficiency virus), Flaviviridae, like HCV (hepatitis C virus), Hepadnaviridae, like HBV (hepatitis B virus), Coronaviridae, like SARS corona virus, and Orthomyxoviridae, like influenza A, B, or C.

    摘要翻译： 本发明的领域涉及使用碳水化合物结合化合物作为药物，其用于治疗或预防病毒感染的用途，其用于制造药物以治疗或预防病毒感染及其在疫苗接种策略中的应用。 本发明涉及所述化合物用于制备治疗或预防受试者的病毒感染的药物的用途，更具体地，涉及具有糖基化包膜蛋白的病毒感染，例如逆转录病毒科（例如Lentivirina），如HIV（人类免疫缺陷病毒）， 黄病毒科，如HCV（丙型肝炎病毒），Hepadnaviridae，如HBV（乙型肝炎病毒），冠状病毒科，如SARS冠状病毒和正粘病毒科，如A，B或C型流感。

    Compositions for the treatment or prophylaxis of viral infections
    7.
    发明授权
    Compositions for the treatment or prophylaxis of viral infections 有权
    用于治疗或预防病毒感染的组合物

    公开(公告)号：US08513215B2

    公开(公告)日：2013-08-20

    申请号：US12676394

    申请日：2008-08-27

    申请人： Jan Balzarini ,  Maria Jose Camarasa ,  Sonsoles Velazquez

    发明人： Jan Balzarini ,  Maria Jose Camarasa ,  Sonsoles Velazquez

    IPC分类号： C07H19/24

    CPC分类号： C07K9/003 ,  A61K47/542 ,  A61K47/64 ,  C07H19/24 ,  C07H23/00 ,  C07K5/0808

    摘要： A compound of the general formula (III): wherein X is O, S, NH or CH2; Y is O, S or NH; Z is O, S or CH2; R1 is C1-8 alkyl, especially C1-6 alkyl, preferably n-alkyl, e.g., n-pentyl or n-hexyl; at least one of R2 and R3 is H—[R4-R5]n—R6—, in which: H—[R4-R5]n— comprises an oligopeptide, R4 being an amino acid and R5 being an amino acid selected from proline, alanine, hydroxyproline, dihydroxyproline, thiazolidinecarboxylic acid (thioproline), dehydroproline, pipecolic acid (L-homoproline), azetidinecarboxylic acid, aziridinecarboxylic acid, glycine, serine, valine, leucine, isoleucine and threonine, R6 is a neutral, non-polar amino acid moiety that is bonded to R5 by a peptide bond, and n is 1, 2, 3, 4 or 5; and the other of R3 and R2 is H—[R4-R5]n-R6— or H; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 通式（III）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; R1是C1-8烷基，特别是C1-6烷基，优选正烷基，例如正戊基或正己基; R2和R3中的至少一个是H- [R4-R5] n-R6-，其中：H- [R4-R5] n-包含寡肽，R4是氨基酸，R5是选自脯氨酸 ，丙氨酸，羟脯氨酸，二羟脯氨酸，噻唑烷羧酸（硫脯氨酸），脱氢脯氨酸，哌可酸（L-高脯氨酸），氮杂环丁烷羧酸，氮丙啶羧酸，甘氨酸，丝氨酸，缬氨酸，亮氨酸，异亮氨酸和苏氨酸，R6是中性，非极性氨基 通过肽键与R5结合的酸部分，n为1,2,3,4或5; R3和R2中的另一个是H- [R4-R5] n-R6-或H; 或其药学上可接受的盐。

    Anti-Viral Pyrimidine Nucleoside Derivatives
    9.
    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。

    Hiv Prodrugs Cleavable by Cd26
    10.
    发明申请
    Hiv Prodrugs Cleavable by Cd26 审中-公开
    Hiv前驱物可被Cd26切割

    公开(公告)号：US20080214648A1

    公开(公告)日：2008-09-04

    申请号：US10555712

    申请日：2004-05-10

    申请人： Herman Augustinus De Kock ,  Piet Tom Bert Paul Wigerinck ,  Jan Balzarini

    发明人： Herman Augustinus De Kock ,  Piet Tom Bert Paul Wigerinck ,  Jan Balzarini

    IPC分类号： A61K31/40 ,  C07D493/04 ,  C07D207/12 ,  A61P31/18 ,  A61K31/34

    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 new prodrugs which are conjugates of a therapeutic compound and a peptide wherein the conjugate is cleavable by dipeptidyl-peptidases, more preferably by CD26, also known as DPPIV (dipeptidyl aminodipeptidase IV). The present prodrugs have the formula the stereoisomeric forms and salts thereof, wherein n is 1 to 5; Y is proline, alanine, hydroxyproline, dihydroxyproline, thiazolidinecarboxylic acid (thioproline), dehydroproline, pipecolic acid (L-homoproline), azetidinecarboxylic acid, aziridinecarboxylic acid, glycine, serine, valine, leucine, isoleucine and threonine; X is selected from any amino acid in the D- or L-configuration; X and Y in each repeat of [Y-X] are chosen independently from one another and independently from other repeats; Z is a direct bond or a bivalent straight or branched saturated hydrocarbon group having from 1 to 4 carbon atoms; R1 is an aryl, heteroaryl, aryloxy, heteroaryloxy, aryloxyC1-4alkyl, heterocycloalkyloxy, heterocycloalkylC1-4alkyloxy, heteroaryloxyC1-4alkyl, heteroarylC1-4alkyloxy; R2 is arylC1-4alkyl; R3 is C1-10alkyl, C2-6alkenyl or C3-7cycloalkylC1-4alkyl; R4 is hydrogen or C1-4alkyl. The present invention furthermore provides the use of said prodrugs as medicines as well as a method of producing said prodrugs.

    摘要翻译： 本发明提供了新的前体药物，其是治疗化合物和肽的缀合物，其中缀合物可被二肽基肽酶切割，更优选通过CD26，也称为DPPIV（二肽基氨基二肽酶IV））。 本发明的前药具有式的立体异构形式及其盐，其中n为1至5; Y是脯氨酸，丙氨酸，羟脯氨酸，二羟脯氨酸，噻唑烷羧酸（硫脯氨酸），脱氢脯氨酸，哌可酸（L-高脯氨酸），氮杂环丁烷羧酸，氮丙啶羧酸，甘氨酸，丝氨酸，缬氨酸，亮氨酸，异亮氨酸和苏氨酸; X选自D-或L-构型中的任何氨基酸; [Y-X]的每个重复中的X和Y彼此独立地独立地选自其它重复; Z是直接键或具有1至4个碳原子的二价直链或支链饱和烃基; R 1是芳基，杂芳基，芳氧基，杂芳氧基，芳氧基C 1-4烷基，杂环烷氧基，杂环烷基C 1-4烷氧基，杂芳氧基C 1-4烷基，杂芳基C 1-4烷氧基; R 2是芳基C 1-4烷基; R 3是C 1-10烷基，C 2-6链烯基或C 3-7环烷基C SUB 1-4烷基; R 4是氢或C 1-4烷基。 本发明还提供所述前体药物作为药物的用途以及制备所述前体药物的方法。