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    Synthesis of beta-L-2'-deoxy nucleosides
    1.
    发明申请
    Synthesis of beta-L-2'-deoxy nucleosides 审中-公开
    β-L-2'-脱氧核苷的合成

    公开(公告)号：US20050059632A1

    公开(公告)日：2005-03-17

    申请号：US10882893

    申请日：2004-06-30

    申请人： Richard Storer ,  Adel Moussa ,  Jingyang Wang ,  Narayan Chaudhuri ,  Steven Mathieu ,  Alistair Stewart

    发明人： Richard Storer ,  Adel Moussa ,  Jingyang Wang ,  Narayan Chaudhuri ,  Steven Mathieu ,  Alistair Stewart

    IPC分类号： A61K31/7072 ,  A61K31/7076 ,  C07H13/08 ,  C07H19/00 ,  C07H19/048 ,  C07H19/073 ,  C07H19/22 ,  C12Q20060101

    CPC分类号： C07H19/09 ,  C07H9/04 ,  C07H9/06 ,  C07H13/04 ,  C07H13/08 ,  C07H15/203 ,  C07H19/06 ,  C07H19/073 ,  Y02P20/55

    摘要： An improved process for the preparation of 2′-modified nucleosides and 2′-deoxy-nucleosides, such as, β-L-2′-deoxy-thymidine (LdT), is provided. In particular, the improved process is directed to the synthesis of a 2′-deoxynucleoside that may utilize different starting materials but that proceeds via a chloro-sugar intermediate or via a 2,2′-anhydro-1-furanosyl-nucleobase intermediate. Where an 2,2′-anhydro-1-furanosyl base intermediate is utilized, a reducing agent, such as Red-Al, and a sequestering agent, such as 15-crown-5 ether, that cause an intramolecular displacement reaction and formation of the desired nucleoside product in good yields are employed. An alternative process of the present invention utilizes a 2,2′-anhydro-1-furanosyl base intermediate without a sequestering agent to afford 2′-deoxynucleosides in good yields. The compounds made according to the present invention may be used as intermediates in the preparation of other nucleoside analogues, or may be used directly as antiviral and/or antineoplastic agents.

    摘要翻译： 提供了用于制备2'-修饰的核苷和2'-脱氧核苷的改进方法，例如β-L-2'-脱氧胸苷（LdT）。 特别地，改进的方法涉及可以利用不同起始原料但通过氯糖中间体或通过2,2'-脱水-1-呋喃糖基 - 核碱基中间体进行的2'-脱氧核苷的合成。 当使用2,2'-脱水-1-呋喃糖基碱中间体时，可以使用诸如Red-Al的还原剂和诸如15-冠醚5的多价螯合剂，其引起分子内置换反应和形成 使用所需的产率良好的核苷产物。 本发明的另一种方法是利用不含螯合剂的2,2'-脱水-1-呋喃糖基碱中间产物得到2'-脱氧核苷。 根据本发明制备的化合物可以用作制备其它核苷类似物的中间体，或者可以直接用作抗病毒和/或抗肿瘤剂。

    Industrially scalable nucleoside synthesis
    4.
    发明申请
    Industrially scalable nucleoside synthesis 失效
    工业可扩展的核苷合成

    公开(公告)号：US20050004357A1

    公开(公告)日：2005-01-06

    申请号：US10833925

    申请日：2004-04-28

    申请人： Adel Moussa ,  Jing Wang ,  Richard Storer

    发明人： Adel Moussa ,  Jing Wang ,  Richard Storer

    IPC分类号： A61K20060101 ,  C07H19/00 ,  C07H19/04 ,  C07H19/048 ,  C07H19/22

    CPC分类号： C07H19/073

    摘要： An industrially scalable two-step process for preparing a β-L-2′-deoxy-nucleoside that results in a predominance of the β- over the γ-anomeric form of the compound is described. An optional third step may be used to prepare 3′-prodrugs of desirable β-L-2′-deoxy-nucleosides for the delivery of these pharmaceuticals effective for treating viral diseases. The synthetic process is applicable in particular to the formation of β-L-2′-deoxy-cytidine, a pharmaceutically acceptable salt or prodrug thereof. The process can provide a relatively uncontaminated product that may require no further isolation or purification, thereby making the synthesis easily scalable for industrial manufacture.

    摘要翻译： 描述了一种用于制备β-L-2'-脱氧核苷的工业可扩展的两步法，其导致β-位于化合物的γ-异头体形式之上。 可选的第三步可用于制备所需的β-L-2'-脱氧核苷的3'-前药，用于递送有效治疗病毒性疾病的这些药物。 合成方法特别适用于形成β-L-2'-脱氧胞苷，其药学上可接受的盐或前药。 该方法可以提供可能不需要进一步分离或纯化的相对未污染的产品，从而使合成容易扩展到工业制造。

    Industrially scalable nucleoside synthesis
    5.
    发明授权
    Industrially scalable nucleoside synthesis 失效
    工业可扩展的核苷合成

    公开(公告)号：US07595390B2

    公开(公告)日：2009-09-29

    申请号：US10833925

    申请日：2004-04-28

    申请人： Adel Moussa ,  Jing Yang Wang ,  Richard Storer

    发明人： Adel Moussa ,  Jing Yang Wang ,  Richard Storer

    IPC分类号： C07H19/073

    CPC分类号： C07H19/073

    摘要： An industrially scalable two-step process for preparing a β-L-2′-deoxy-nucleoside that results in a predominance of the β- over the α-anomeric form of the compound is described. An optional third step may be used to prepare 3′-prodrugs of desirable β-L-2′-deoxy-nucleosides for the delivery of these pharmaceuticals effective for treating viral diseases. The synthetic process is applicable in particular to the formation of β-L-2′-deoxy-cytidine, a pharmaceutically acceptable salt or prodrug thereof. The process can provide a relatively uncontaminated product that may require no further isolation or purification, thereby making the synthesis easily scalable for industrial manufacture.

    摘要翻译： 描述了一种用于制备β-L-2'-脱氧核苷的工业可扩展的两步法，其导致β-位于化合物的α-端基异构体形式的优势。 可选的第三步可用于制备所需的β-L-2'-脱氧核苷的3'-前药，用于递送有效治疗病毒性疾病的这些药物。 合成方法特别适用于形成β-L-2'-脱氧胞苷，其药学上可接受的盐或前药。 该方法可以提供可能不需要进一步分离或纯化的相对未污染的产品，从而使合成容易扩展到工业制造。

    Substituted phenylindoles for the treatment of HIV
    6.
    发明授权
    Substituted phenylindoles for the treatment of HIV 有权
    用于治疗HIV的取代的苯基吲哚

    公开(公告)号：US07365090B2

    公开(公告)日：2008-04-29

    申请号：US10637949

    申请日：2003-08-07

    申请人： Marino Artico ,  Paolo LaColla ,  Romano Silvestri ,  Adel Moussa ,  Jean-Pierre Sommadossi ,  Richard Storer

    发明人： Marino Artico ,  Paolo LaColla ,  Romano Silvestri ,  Adel Moussa ,  Jean-Pierre Sommadossi ,  Richard Storer

    IPC分类号： A61K31/405 ,  C07D209/14

    CPC分类号： C07D403/04 ,  C07D209/42 ,  C07D403/12

    摘要： This invention is in the area of phenylindoles that are useful for the treatment of HIV infection, and, in particular, phenylindoles that exhibit significant activity against resistant strains of HIV. The phenylindoles have at least two substituents other than hydrogen on the benzo ring of the indole function, preferably at the 4′ and 5′, 5′ and 6′ or the 5′ and 7′ positions, optionally in combination with disubstitution at positions 3″ and 5″ on the phenyl ring of the compound, and carboxamide containing moieties at position-2 on the indole group of the compound. Methyl is a preferred group for substitution on the phenyl ring. Preferred substituents for the benzo ring of the indole function include but are not limited to chlorine, fluorine, bromine, iodine, CF3, methoxy, CN, and NO2.

    摘要翻译： 本发明在可用于治疗HIV感染的苯基吲哚的区域中，特别是对抗HIV抗性菌株显示出显着活性的苯基吲哚。 苯吲哚在吲哚官能团的苯并环上具有至少两个除氢之外的取代基，优选在4'和5'，5'和6'或5'和7'位置，任选地与3位的取代基组合 “和5”，化合物的吲哚基上的位置-2的含羧酰胺的部分。 甲基是在苯环上取代的优选基团。 吲哚官能团的苯并环的优选取代基包括但不限于氯，氟，溴，碘，CF 3，甲氧基，CN和NO 2。

    Process for preparing a synthetic intermediate for preparation of branched nucleosides
    8.
    发明申请
    Process for preparing a synthetic intermediate for preparation of branched nucleosides 有权
    制备分支核苷合成中间体的方法

    公开(公告)号：US20070203334A1

    公开(公告)日：2007-08-30

    申请号：US11644304

    申请日：2006-12-22

    申请人： Benjamin Mayes ,  Adel Moussa

    发明人： Benjamin Mayes ,  Adel Moussa

    IPC分类号： C07H19/048 ,  C07D309/30 ,  C07D305/12 ,  C07H19/22

    CPC分类号： C07H15/24 ,  C07D307/33 ,  C07D309/30 ,  C07H19/048 ,  C07H19/22

    摘要： A process is provided for the preparation of a key intermediate in the preparation of 2′-branched nucleoside compounds. The process includes contacting a protected precursor 3,4-O-isopropylidene-2-C-substituted-D-arabinono-1,5-lactone with a fluorinating agent under anhydrous conditions and converting the precursor into a protected 2-deoxy-2-halo-2-C-disubstituted ribono-1,5-lactone and optionally into a 2-deoxy-2-halo-2-C-disubstituted ribono-1,4-lactone.

    摘要翻译： 提供了制备2支支化核苷化合物的关键中间体的方法。 该方法包括在无水条件下将受保护的前体3,4-O-异亚丙基-2-C取代的-MacLCAPS> D - 阿拉蛋酸-1,5-内酯与氟化剂接触并将前体转化为 保护的2-脱氧-2-卤-2- C - 二取代的ribono-1,5-内酯，任选地加入到2-脱氧-2-卤代-2- C-二取代的核糖内-1,4-内酯中。

    Process for preparing a synthetic intermediate for preparation of branched nucleosides
    9.
    发明授权
    Process for preparing a synthetic intermediate for preparation of branched nucleosides 有权
    制备分支核苷合成中间体的方法

    公开(公告)号：US07781576B2

    公开(公告)日：2010-08-24

    申请号：US11644304

    申请日：2006-12-22

    申请人： Benjamin Alexander Mayes ,  Adel Moussa

    发明人： Benjamin Alexander Mayes ,  Adel Moussa

    IPC分类号： C07H19/48 ,  C07H19/22

    CPC分类号： C07H15/24 ,  C07D307/33 ,  C07D309/30 ,  C07H19/048 ,  C07H19/22

    摘要： A process is provided for the preparation of a key intermediate in the preparation of 2′-branched nucleoside compounds. The process includes contacting a protected precursor 3,4-O-isopropylidene-2-C-substituted-D-arabinono-1,5-lactone with a fluorinating agent under anhydrous conditions and converting the precursor into a protected 2-deoxy-2-halo-2-C-disubstituted ribono-1,5-lactone and optionally into a 2-deoxy-2-halo-2-C-disubstituted ribono-1,4-lactone.

    摘要翻译： 提供了制备2支支化核苷化合物的关键中间体的方法。 该方法包括在无水条件下将受保护的前体3,4-O-异亚丙基-2-C-取代的D-阿拉伯酮-1,5-内酯与氟化剂接触，并将前体转化为受保护的2-脱氧-2- 卤代-2- C-二取代的核糖-1,5-内酯，任选地加入2-脱氧-2-卤代-2- C-二取代的核糖内-1,4-内酯。