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    24-sulfoximine vitamin D3 compounds
    2.
    发明授权
    24-sulfoximine vitamin D3 compounds 有权
    24-亚磺酰亚胺维生素D3化合物

    公开(公告)号：US07973024B2

    公开(公告)日：2011-07-05

    申请号：US11442148

    申请日：2006-05-30

    申请人： Gary Posner ,  Mehmet Kahraman ,  Uttam Saha

    发明人： Gary Posner ,  Mehmet Kahraman ,  Uttam Saha

    IPC分类号： A61K31/593

    CPC分类号： C07C401/00

    摘要： The present invention provides novel sulfoximine compounds, compositions comprising these compounds and methods of using these compounds as inhibitors of CYP24. In particular, the compounds of the invention are useful for treating diseases which benefit from a modulation of the levels of 1α,25-dihydroxy vitamin D3, for example, cell-proliferative disorders.

    摘要翻译： 本发明提供新的磺酰亚胺化合物，包含这些化合物的组合物和使用这些化合物作为CYP24抑制剂的方法。 特别地，本发明的化合物可用于治疗受益于调节1α，25-二羟维生素D3水平的疾病，例如细胞增殖性疾病。

    Orally active, antimalarial, anticancer, artemisinin-derived trioxane dimers with high selectively, stability and efficacy and methods of making the same
    4.
    发明申请
    Orally active, antimalarial, anticancer, artemisinin-derived trioxane dimers with high selectively, stability and efficacy and methods of making the same 有权
    口服活性，抗疟药，抗癌，青蒿素衍生的三恶烷二聚体具有高选择性，稳定性和有效性及其制备方法

    公开(公告)号：US20060142377A1

    公开(公告)日：2006-06-29

    申请号：US10529513

    申请日：2003-09-26

    申请人： Gary Posner ,  Theresa Shapiro ,  Surojit Sur ,  Tanzina Labonte ,  Kristina Borstnik ,  Ik-Hyeon Paik ,  Andrew McRiner

    发明人： Gary Posner ,  Theresa Shapiro ,  Surojit Sur ,  Tanzina Labonte ,  Kristina Borstnik ,  Ik-Hyeon Paik ,  Andrew McRiner

    IPC分类号： A61K31/353 ,  A61K31/335 ,  C07D493/14

    CPC分类号： C07D493/18

    摘要： In only two steps and in 65% overall yield, natural trioxane artemisinin (I) was converted on gram scale into C-10-carba trioxane dimer (3). This new, very stable dimer was then transformed easily in one additional step into four different dimers (4-7). Alcohol and diol dimers (4 and 5) and ketone dimer (7) are 10 times more antimalarially potent in vitro than artemisinin (1), and alcohol and diol dimers (4 and 5) are strongly inhibitory but not cytotoxic toward several human cancer cell lines. Water-soluble carboxylic acid derivatives (8a-10c and 12) were easily prepared from dimers (4-6); they are thermally stable even at 60° C. for 24 hours, are more orally efficacious as antimalarials than either artelinic acid or sodium artesunate, and have potent and selective anticancer activities. Further derivitization of the alcohol dimers (4 and 17), diol dimer (5) and ketone (7) has produced a number of analogs also antimalarially active in vitro at sub-nanomolar concentrations (most notably: pyridine N-oxides (13, 15, 18, 23, 24 and 25), phosphoric acid triesters (26 and 27), sulfonamide (40) and cyclic carbonate (41)). In addition, dimers (13 and 19) are more efficacious (when administered both orally and i.v.) and less toxic (when administered intraperitoneally to mice as a single dose) than clinically-used sodium artesunate, thereby giving them a better antimalarial therapeutic index than sodium artesunate.

    摘要翻译： 只有两个步骤，65％的总产率，将天然的三恶烷青蒿素（I）按克标度转化为C-10-碳三三烷二聚物（3）。 然后将这种新的非常稳定的二聚体在一个额外的步骤中容易地转化成四种不同的二聚体（4-7）。 醇和二醇二聚体（4和5）和酮二聚体（7）在体外比青蒿素（1）具有10倍的抗疟药效力，醇和二醇二聚体（4和5）对几种人类癌细胞具有强烈的抑制作用但不具有细胞毒性 线条。 水溶性羧酸衍生物（8a-10c和12）容易由二聚体（4-6）制备; 它们甚至在60℃下热稳定24小时，作为抗疟药物比阿特金酸或青蒿琥酯钠更具口服效力，并且具有有效和选择性的抗癌活性。 醇二聚体（4和17），二醇二聚物（5）和酮（7）的进一步衍生产生了许多在亚纳摩尔浓度下体外抗疟活性的类似物（最引人注目的是：吡啶N-氧化物（13,15 ，18,23,24和25），磷酸三酯（26和27），磺酰胺（40）和环状碳酸酯（41））。 此外，二聚体（13和19）比临床使用的青蒿琥酯钠更有效（当口服和静脉内施用）和毒性较小（当以单剂量腹膜内给予小鼠时），从而给予它们更好的抗疟治疗指数 青蒿琥酯钠。

    Anti-cytomegalovirus activity of artemisinin-derived dimers
    6.
    发明授权
    Anti-cytomegalovirus activity of artemisinin-derived dimers 有权
    青蒿素衍生的二聚体的抗巨细胞病毒活性

    公开(公告)号：US08883765B2

    公开(公告)日：2014-11-11

    申请号：US13514645

    申请日：2010-12-08

    申请人： Ravit Arav-Boger ,  Gary Posner

    发明人： Ravit Arav-Boger ,  Gary Posner

    IPC分类号： A61K31/357 ,  C07D493/18 ,  C07F9/6561 ,  A61K31/683 ,  A61K45/06

    CPC分类号： A61K31/357 ,  A61K31/683 ,  A61K45/06 ,  C07D493/18 ,  C07F9/6561

    摘要： Artemisinin-derived monomers and artemisinin dimers are shown to exhibit in-vitro anti-cytomegalovirus (CMV) activity. Artemisinin dimers effectively inhibited CMV replication in human foreskin fibroblasts and human embryonic lung fibroblasts with no cytotoxicity at concentrations required for complete CMV inhibition. Artemisinin dimers were found to be potent and non-cytotoxic inhibitors of CMV replication, which indicates their use as therapeutic agents for the treatment of CMV infection in humans.

    摘要翻译： 青蒿素衍生的单体和青蒿素二聚体显示出体外抗巨细胞病毒（CMV）活性。 青蒿素二聚体有效抑制人包皮成纤维细胞和人胚胎肺成纤维细胞中的CMV复制，在完全CMV抑制所需的浓度下无细胞毒性。 青蒿素二聚体被发现是CMV复制的有效和非细胞毒性抑制剂，这表明它们用作治疗人类CMV感染的治疗剂。

    ANTI-CYTOMEGALOVIRUS ACTIVITY OF ARTEMISININ-DERIVED DIMERS
    7.
    发明申请
    ANTI-CYTOMEGALOVIRUS ACTIVITY OF ARTEMISININ-DERIVED DIMERS 有权
    阿司匹林衍生二聚体的抗细胞因子活性

    公开(公告)号：US20130109654A1

    公开(公告)日：2013-05-02

    申请号：US13514645

    申请日：2010-12-08

    申请人： Ravit Arav-Boger ,  Gary Posner

    发明人： Ravit Arav-Boger ,  Gary Posner

    IPC分类号： A61K31/357 ,  A61K45/06 ,  A61K31/683 ,  C07D493/18 ,  C07F9/6561

    CPC分类号： A61K31/357 ,  A61K31/683 ,  A61K45/06 ,  C07D493/18 ,  C07F9/6561

    摘要： Artemisinin-derived monomers and artemisinin dimers are shown to exhibit in-vitro anti-cytomegalovirus (CMV) activity. Artemisinin dimers effectively inhibited CMV replication in human foreskin fibroblasts and human embryonic lung fibroblasts with no cytotoxicity at concentrations required for complete CMV inhibition. Artemisinin dimers were found to be potent and non-cytotoxic inhibitors of CMV replication, which indicates their use as therapeutic agents for the treatment of CMV infection in humans.

    摘要翻译： 青蒿素衍生的单体和青蒿素二聚体显示出体外抗巨细胞病毒（CMV）活性。 青蒿素二聚体有效抑制人包皮成纤维细胞和人胚胎肺成纤维细胞中的CMV复制，在完全CMV抑制所需的浓度下无细胞毒性。 青蒿素二聚体被发现是CMV复制的有效和非细胞毒性抑制剂，这表明它们用作治疗人类CMV感染的治疗剂。