知搜-全球专利检索

  1. 登录
  2. 注册

搜索结果

36 条记录 (耗时 0.034 秒)

    Stable neutral nitric oxide source
    1.
    发明授权
    Stable neutral nitric oxide source 有权
    稳定的中性一氧化氮源

    公开(公告)号：US08598368B2

    公开(公告)日：2013-12-03

    申请号：US12532918

    申请日：2008-04-16

    申请人： Eric J. Toone ,  Harinath Chakrapani

    发明人： Eric J. Toone ,  Harinath Chakrapani

    IPC分类号： C07D498/08

    CPC分类号： C07D261/20 ,  C07D498/08

    摘要： C-nitroso compound capable of releasing neutral nitric oxide is made stable by forming a Diels Alder adduct thereof which is functionalized at the Diels-Alder double bond to impart the stability. Treatment of the stabilized adduct with agent that removes functionalization and regenerates Diels Alder double bond triggers delivery of neutral nitric oxide via retro Diels-Alder reaction and homolytic scission.

    摘要翻译： 能够释放中性一氧化氮的C-亚硝基化合物通过形成其在Diels-Alder双键官能化的Diels Alder加合物而赋予稳定性。 用去除功能化并再生Diels Alder双键的试剂处理稳定的加合物，通过复古Diels-Alder反应和均质裂解触发中性一氧化氮的传递。

    C-nitroso compounds and use thereof
    3.
    发明授权
    C-nitroso compounds and use thereof 有权
    C-亚硝基化合物及其用途

    公开(公告)号：US07785616B2

    公开(公告)日：2010-08-31

    申请号：US11822770

    申请日：2007-07-10

    申请人： Jonathan S. Stamler ,  Eric J. Toone

    发明人： Jonathan S. Stamler ,  Eric J. Toone

    IPC分类号： A61K31/785

    CPC分类号： C07C245/04 ,  A61K31/00 ,  A61K31/195 ,  A61K31/785 ,  A61L31/10 ,  A61L31/16 ,  A61L2300/114 ,  A61L2300/606 ,  C07C207/00 ,  C07C207/04 ,  C07C219/06 ,  A61K2300/00

    摘要： A C-nitroso moiety derived from a carbon acid with a pKa less than about 25 is bound in a biocompatible polymer as an ester or ether to a pendant hydroxyl group, as an ester to a pendant carboxylic acid or as an amine or amide to a pendant amine moiety. The polymer with c-nitroso moiety bound thereto can be coated on a medical device and/or used for prophylaxis of a patient at risk for restenosis. A c-nitroso moiety bound as amide to polyisobutylene amine substituted styrene copolymer is described in detail.

    摘要翻译： 衍生自pKa小于约25的碳酸的C-亚硝基部分作为酯或醚与作为酯的侧链羟基的生物相容性聚合物结合到侧羧酸或作为胺或酰胺与 侧胺部分。 具有结合到其上的C-亚硝基部分的聚合物可以涂覆在医疗装置上和/或用于预防具有再狭窄风险的患者。 详细描述了作为酰胺与聚异丁烯胺取代的苯乙烯共聚物结合的C-亚硝基部分。

    C-nitroso compounds and use thereof
    5.
    发明授权
    C-nitroso compounds and use thereof 失效
    C-亚硝基化合物及其用途

    公开(公告)号：US07049308B2

    公开(公告)日：2006-05-23

    申请号：US10380172

    申请日：2001-09-27

    申请人： Jonathan S. Stamler ,  Eric J. Toone

    发明人： Jonathan S. Stamler ,  Eric J. Toone

    IPC分类号： C07D211/90 ,  C07D405/14 ,  C07D413/04 ,  C07D231/12 ,  A61P29/00

    CPC分类号： C07C245/04 ,  A61K31/00 ,  A61K31/195 ,  A61K31/785 ,  A61L31/10 ,  A61L31/16 ,  A61L2300/114 ,  A61L2300/606 ,  C07C207/00 ,  C07C207/04 ,  C07C219/06 ,  A61K2300/00

    摘要： A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. In another embodiment, a biocompatible polymer incorporates a C-nitroso moiety.

    摘要翻译： 一种分子量范围为225〜1000（口服给药时为225〜600）的C-亚硝基化合物，其中亚硝基连接到叔碳上，其通过具有pKa的碳酸的亚硝化而得到 小于约25，可用作NO供体。 当化合物从pKa小于约10的碳酸获得时，当以微摩尔浓度使用时，其提供血管松弛效果，并且该活性由以纳摩尔浓度获得的谷胱甘肽加强。 当化合物由pKa为约15至20的碳酸获得时，在没有谷胱甘肽的纳摩尔浓度下获得血管松弛效果。 在另一个实施方案中，生物相容性聚合物包含C-亚硝基部分。

    Polymers for delivering nitric oxide in vivo
    6.
    发明授权
    Polymers for delivering nitric oxide in vivo 失效
    用于在体内递送一氧化氮的聚合物

    公开(公告)号：US06673891B2

    公开(公告)日：2004-01-06

    申请号：US10164366

    申请日：2002-06-05

    申请人： Jonathan S. Stamler ,  Eric J. Toone ,  Richard S. Stack

    发明人： Jonathan S. Stamler ,  Eric J. Toone ,  Richard S. Stack

    IPC分类号： C08G7500

    CPC分类号： A61K31/785 ,  A61K47/61 ,  A61K47/6951 ,  A61L29/10 ,  A61L29/16 ,  A61L31/10 ,  A61L31/16 ,  A61L33/068 ,  A61L33/08 ,  A61L2300/114 ,  A61L2300/416 ,  A61L2300/42 ,  B82Y5/00 ,  C08B37/0012 ,  C08G75/00 ,  C08L5/16 ,  C09D105/16 ,  G06F19/00 ,  Y10T428/1393

    摘要： Disclosed are novel polymers derivatized with at least one —SNO group per 1200 atomic mass unit of the polymer. In one embodiment, the S-nitrosylated polymer has stabilized —S-nitrosyl groups. In another embodiment the S-nitrosylated polymer prepared by polymerizing a compound represented by the following structural formula: R is an organic radical. Each X′ is an independently chosen aliphatic group or substituted aliphatic group. Preferably, each X′ is the same and is a C2-C6 alkylene group, more preferably —CH2—, —CH2CH2—, —CH2CH2CH2— or —CH2CH2CH2CH2—. p and m are independently a positive integer such that p+m is greater than two. The polymers of the present invention can be used to coat medical devices to deliver nitric oxide in vivo to treatment sites.

    摘要翻译： 公开了每聚合物的每1200原子质量单位衍生自至少一个-SNO基团的新型聚合物。 在一个实施方案中，S-亚硝基化聚合物具有稳定的-S-亚硝酰基。 在另一个实施方案中，通过聚合由以下结构式表示的化合物制备的S-亚硝基化聚合物：R是有机基团。每个X'是独立选择的脂族基团或取代的脂族基团。 优选地，每个X'相同并且是C2-C6亚烷基，更优选-CH 2 - ， - CH 2 CH 2 - ， - CH 2 CH 2 CH 2 - 或-CH 2 CH 2 CH 2 CH 2 -P-，m独立地为正整数，使得p + m更大 本发明的聚合物可以用于涂覆医疗装置以将体内的一氧化氮输送到治疗部位。

    C-nitroso compounds and use thereof
    9.
    发明授权
    C-nitroso compounds and use thereof 失效
    C-亚硝基化合物及其用途

    公开(公告)号：US07030238B2

    公开(公告)日：2006-04-18

    申请号：US11052777

    申请日：2005-02-09

    申请人： Jonathan S. Stamler ,  Eric J. Toone

    发明人： Jonathan S. Stamler ,  Eric J. Toone

    IPC分类号： C07D265/02 ,  C07D267/04 ,  C07D279/02 ,  A61K31/5415 ,  A61K31/536

    CPC分类号： C07C207/00 ,  A61K31/00 ,  A61K31/195 ,  A61K2300/00

    摘要： A C-nitroso compound having a molecular weight ranging from about 225 to about 1,000 (from about 225 to about 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to about 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. The compound is preferably water-soluble and preferably contains a carbon alpha to the nitrosylated carbon which is part of a ketone group. In one embodiment, the C-nitroso compound is obtained by nitrosylation of a conventional drug or such drug modified to modify the carbon acid pKa thereof. When such drug is a nonsteroidal anti-inflammatory drug, the resulting C-nitroso compound functions as a COX-1 and COX-2 inhibitor without the deleterious effects associated with COX-1 inhibition but with the advantageous effects associated with COX-1 and COX-2 inhibition. One such C-nitroso compound is a nitrosoketoibuprofen. A specific example of this kind of compound is isolated as dimeric 2-[4′-(α-nitroso)isobutyrylphenyl]propionic acid. In another case, the C-nitroso compound contains the moiety where X is S, O or NR. One embodiment is directed to COX-2 inhibitors where a tertiary carbon atom and/or an oxygen atom and/or a sulfur atom is nitrosylated.

    摘要翻译： 单体基团的分子量范围为约225至约1,000（约225至约600）的C-亚硝基化合物，其中亚硝基连接到叔碳上，其通过碳的亚硝基化获得 pKa小于约25的酸可用作NO供体。 当化合物从pKa小于约10的碳酸获得时，当以微摩尔浓度使用时，其提供血管松弛效果，并且该活性由以纳摩尔浓度获得的谷胱甘肽加强。 当化合物由pKa为约15至约20的碳酸获得时，在没有谷胱甘肽的纳摩尔浓度下获得血管松弛效果。 该化合物优选是水溶性的并且优选地含有作为酮基的一部分的亚硝基化碳的碳α。 在一个实施方案中，C-亚硝基化合物通过常规药物的亚硝基化或经修饰以改性其碳酸pKa的药物而获得。 当这种药物是非甾体抗炎药物时，所得到的C-亚硝基化合物起COX-1和COX-2抑制剂的作用，而没有与COX-1抑制有关的有害作用，但具有与COX-1和COX相关的有益效果 -2抑制。 一种这样的C-亚硝基化合物是亚硝基基布洛芬。 这种化合物的具体实例被分离为二聚2- [4' - （α-亚硝基）异丁酰苯基]丙酸。 在另一种情况下，C-亚硝基化合物包含其中X是S，O或NR的部分。 一个实施方案涉及其中叔碳原子和/或氧原子和/或硫原子被亚硝酰化的COX-2抑制剂。