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59 条记录 (耗时 0.019 秒)

    4′-thio-L-xylo furanosyl nucleosides, precursors thereof, preparation and use thereof
    2.
    发明授权
    4′-thio-L-xylo furanosyl nucleosides, precursors thereof, preparation and use thereof 有权
    4'-硫代-L-木糖呋喃糖基核苷，其前体，其制备和用途

    公开(公告)号：US07148223B2

    公开(公告)日：2006-12-12

    申请号：US11045085

    申请日：2005-01-31

    申请人： John A. Secrist, III ,  Kamal N. Tiwari ,  John A. Montgomery

    发明人： John A. Secrist, III ,  Kamal N. Tiwari ,  John A. Montgomery

    IPC分类号： A61K31/54 ,  C07D265/38

    CPC分类号： C07H19/06 ,  A61K31/4436 ,  A61K31/519 ,  A61K31/522 ,  A61K31/53 ,  C07H19/16

    摘要： Compounds represented by the formula 1: A is selected from the group consisting of wherein each R individually is H or acyl, Y is X, N3, NH2, monoalkylamino, or dialkylamino; Z is O or S; and X is selected from the group consisting of hydrogen, halo, hydroxy, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, thioaryl, thioalkyl, allylamino, cyano and nitro; tautomers thereof; and pharmaceutically acceptable salts thereof are provided along with methods for their fabrication. Various of these compounds can be used as anticancer agents, or antiviral agents or to inhibit DNA replication.

    摘要翻译： 由式1：A表示的化合物选自其中每个R各自为H或酰基，Y为X，N 3，NH 2，单烷基氨基， 或二烷基氨基; Z是O或S; 烷基，卤代烷基，烯基，卤代烯基，炔基，氨基，一烷基氨基，二烷基氨基，硫代芳基，硫代烷基，烯丙基氨基，氰基和硝基; 互变异构体 及其药学上可接受的盐及其制备方法。 这些化合物中的各种可以用作抗癌剂，抗病毒剂或抑制DNA复制。

    Method for synthesizing 2-chloro-9-(2-fluoro-β-D-arabinofuranosyl)-9H-purin-6-amine
    3.
    发明授权
    Method for synthesizing 2-chloro-9-(2-fluoro-β-D-arabinofuranosyl)-9H-purin-6-amine 有权
    合成2-氯-9-（2-氟-β-D-阿拉伯呋喃糖基）-9H-嘌呤-6-胺的方法

    公开(公告)号：US06949640B2

    公开(公告)日：2005-09-27

    申请号：US09889287

    申请日：2001-02-16

    申请人： John A. Montgomery ,  Anita T. Fowler ,  John A. Secrist, III

    发明人： John A. Montgomery ,  Anita T. Fowler ,  John A. Secrist, III

    IPC分类号： C07H19/16 ,  C07H19/19

    CPC分类号： C07H19/16

    摘要： 2-Chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-9H-purin-9-amine is synthesized by reacting a 2-chloro-6-substituted purine with a protected and activated 2-deoxy-2-fluoro-D-arabinofuranose; and reacting with a base such as ammonia to provide 2-chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-9H-purin-6-amine. When the purine reactant is substituted in the 6 position with a halogen, a reaction step with an alkoxide is carried out prior to the reaction with ammonia.

    摘要翻译： 2-氯-9-（2-脱氧-2-氟-β-D-阿拉伯呋喃糖基）-9H-嘌呤-9-胺通过使2-氯-6-取代的嘌呤与被保护的和活化的2-脱氧 -2-氟-D-阿拉伯呋喃糖; 并与碱如氨反应得到2-氯-9-（2-脱氧-2-氟-β-D-阿拉伯呋喃糖基）-9H-嘌呤-6-胺。 当嘌呤反应物在6位被卤素取代时，与氨反应之前，与醇盐进行反应步骤。

    Process for the production of (.+-.)3-deazaaristeromycin
    5.
    发明授权
    Process for the production of (.+-.)3-deazaaristeromycin 失效
    生产（+/-）3-脱氮霉素霉素的方法

    公开(公告)号：US4387228A

    公开(公告)日：1983-06-07

    申请号：US302845

    申请日：1981-09-16

    申请人： John A. Montgomery ,  Sarah D. Clayton

    发明人： John A. Montgomery ,  Sarah D. Clayton

    IPC分类号： C07D471/04

    CPC分类号： C07D471/04

    摘要： A process for the production of (.+-.)3-deazaaristeromycin, which is also known as (.+-.)-4-amino-1-[(1.alpha., 2.beta., 3.beta., 4.alpha.)-2,3-dihydroxy-4-(hydroxymethyl)-cyclopentyl]imidazo[4,5-c]pyridine, which comprises:(1) reacting 2,4-dichloro-3-nitropyridine with (.+-.)(1,4/2,3)-4-amino-2,3-dihydroxy-1-cyclopentanemethanol to give (.+-.)-(1,4/2,3)-4-(3-nitro-2-chloro-4-pyridylamino)-2,3-dihydroxy-1-cyclopentanemethanol (compound II);(2) subsequently reducing compound II to (.+-.)-(1,4/2,3)-4(3-amino-2-chloro-4-pyridylamino)-2,3-dihydroxy-1-cyclopentanemethanol (compound III);(3) acid catalyzed cyclization of compound III to (.+-.)-4-chloro-1-(1.alpha., 2.beta., 3.beta., 4.alpha.)-2,3-dihydroxy-4-(hydroxymethyl)cyclopentyl)imidazo[4,5-c]pyridine (compound IV);(4) displacing the chloro group of compound IV to produce (.+-.)-4-hydrazino-1-(1.alpha., 2.beta., 3.beta., 4.alpha.)-2,3-dihydroxy-4-(hydroxymethyl)cyclopentyl)-imidazo[4,5-c]pyridine (compound V);(5) cleaving said hydrazino compound V to produce (.+-.)-4-amino-1-[(1.alpha., 2.beta., 3.beta., 4.alpha.)-2,3-dihydroxy-4-(hydroxymethyl)cyclopentyl]imidazo[4,5-c]-pyridine (compound VI).

    摘要翻译： （+/-）3-脱氮霉素霉素的制备方法，其也称为（+/-） - 4-氨基-1 - [（1α，2β，3β，4α）-2,3 - 二羟基-4-（羟甲基） - 环戊基]咪唑并[4,5-c]吡啶，其包括：（1）使2,4-二氯-3-硝基吡啶与（+/-）（1,4 / 3）-4-氨基-2,3-二羟基-1-环戊烷甲醇，得到（+/-） - （1,4 / 2,3）-4-（3-硝基-2-氯-4-吡啶基氨基） - 2,3-二羟基-1-环戊烷甲醇（化合物II）; （2）随后将化合物II还原成（+/-） - （1,4 / 2,3）-4（3-氨基-2-氯-4-吡啶基氨基）-2,3-二羟基-1-环戊醇甲醇 化合物III）; （3）化合物III酸化催化环化为（+/-） - 4-氯-1-（1α，2β，3β，4α）-2,3-二羟基-4-（羟甲基）环戊基）咪唑 [4,5-c]吡啶（化合物IV）; （4）置换化合物IV的氯基以产生（+/-） - 4-肼基-1-（1α，2β，3β，4α）-2,3-二羟基-4-（羟甲基）环戊基 ） - 咪唑并[4,5-c]吡啶（化合物V）; （5）切割所述肼基化合物V以产生（+/-） - 4-氨基-1 - [（1α，2β，3β，4α）-2,3-二羟基-4-（羟甲基）环戊基] 咪唑并[4,5-c] - 吡啶（化合物VI）。

    Preparation of thioarabinofuranosyl compounds and use thereof
    8.
    发明授权
    Preparation of thioarabinofuranosyl compounds and use thereof 有权
    硫代呋喃并呋喃糖基化合物的制备及其用途

    公开(公告)号：US06576621B1

    公开(公告)日：2003-06-10

    申请号：US09493247

    申请日：2000-01-28

    申请人： John A. Secrist, III ,  Kamal N. Tiwari ,  John A. Montgomery

    发明人： John A. Secrist, III ,  Kamal N. Tiwari ,  John A. Montgomery

    IPC分类号： A61K900

    CPC分类号： C07D409/04 ,  A61K31/513 ,  A61K31/53 ,  C07H19/04

    摘要： Patients suffering from cancer are treated by being administered a compound represented by the following formula: wherein each R individually is H or an aliphatic or aromatic acyl group; A is selected from the group consisting of wherein X is selected from the group consisting of hydrogen, fluorine, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, cyano and nitro. The above compounds also inhibit DNA replication in mammalian cells,

    摘要翻译： 通过施用由下式表示的化合物来治疗患有癌症的患者：其中R独立地为H或脂族或芳族酰基; A选自X，其选自氢，氟， 烷氧基，烷基，卤代烷基，烯基，卤代烯基，炔基，氨基，单烷基氨基，二烷基氨基，氰基和硝基。 上述化合物还抑制哺乳动物细胞中的DNA复制，

    Hypoxanthine-guanine phosphoribosyl transferase
    10.
    发明授权
    Hypoxanthine-guanine phosphoribosyl transferase 失效
    次黄嘌呤 - 鸟嘌呤磷酸核糖转移酶

    公开(公告)号：US06248577B1

    公开(公告)日：2001-06-19

    申请号：US07552744

    申请日：1990-07-16

    申请人： Geetha Vasanthakumar ,  John A. Montgomery

    发明人： Geetha Vasanthakumar ,  John A. Montgomery

    IPC分类号： C12N1554

    CPC分类号： C12Y204/02008 ,  C12N9/1077

    摘要： The present invention describes the previously unreported cloning and isolation of HGPRT cDNA containing an open reading frame corresponding to the HGPRT of Plasmodium falciparum, present the complete nucleotide sequence of the Plasmodium falciparum HGPRT Dral/Pstl cDNA fragment, and the expression of this gene product in an E. coli strain deficient in purine salvage.

    摘要翻译： 本发明描述了以前未报道的克隆和分离含有对应于恶性疟原虫的HGPRT的开放阅读框的HGPRT cDNA，其存在恶性疟原虫HGPRT Dral / Pst1 cDNA片段的完整核苷酸序列，并且该基因产物的表达 缺乏嘌呤补救的大肠杆菌菌株。