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    Reactive oxygen generating enzyme inhibitor with nitric oxide bioactivity and uses thereof
    2.
    发明申请
    Reactive oxygen generating enzyme inhibitor with nitric oxide bioactivity and uses thereof 失效
    具有一氧化氮生物活性的活性氧发生酶抑制剂及其应用

    公开(公告)号：US20050239807A1

    公开(公告)日：2005-10-27

    申请号：US10829940

    申请日：2004-04-23

    申请人： Jonathan Stamler ,  Eric Toone ,  Joshua Hare

    发明人： Jonathan Stamler ,  Eric Toone ,  Joshua Hare

    IPC分类号： A61K31/519 ,  C07D487/02 ,  C07D487/04

    CPC分类号： C07D487/04 ,  A61K31/519

    摘要： A reactive oxygen generating enzyme inhibitor with NO donor bioactivity, e.g., nitrated allopurinol, e.g., 1,5-bis(3-nitrooxypropyyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidine-4-one is useful to treat heart failure, stable angina, ischemic disorder, ischemic reperfusion injury, atherosclerosis, sickle cell disease, diabetes, Alzheimer's disease, Parkinson's disease, ALS and asthma and to obtain proper contraction of heart, skeletal and smooth muscle. Where the disorder is heart failure, administration of the enzyme inhibitor mediates amelioration of acute coronary symptoms and/or myocardial infarction.

    摘要翻译： 具有NO供体生物活性的活性氧产生酶抑制剂，例如硝化别嘌呤醇，例如1,5-双（3-硝基氧基丙基）-1,5-二氢-4H-吡唑并[3,4-d]嘧啶-4-酮 可用于治疗心力衰竭，稳定型心绞痛，缺血障碍，缺血再灌注损伤，动脉粥样硬化，镰状细胞病，糖尿病，阿尔茨海默氏病，帕金森病，ALS和哮喘，并获得心脏，骨骼和平滑肌的适当收缩。 在疾病是心力衰竭的地方，酶抑制剂的施用介导急性冠状动脉症状和/或心肌梗死的改善。

    C-nitroso compounds and use thereof
    3.
    发明申请
    C-nitroso compounds and use thereof 失效
    C-亚硝基化合物及其用途

    公开(公告)号：US20050203295A1

    公开(公告)日：2005-09-15

    申请号：US11052777

    申请日：2005-02-09

    申请人： Jonathan Stamler ,  Eric Toone

    发明人： Jonathan Stamler ,  Eric Toone

    IPC分类号： A61K31/00 ,  A61K31/194 ,  A61K31/195 ,  A61K31/222 ,  A61K31/553 ,  A61K31/635 ,  A61K38/00 ,  A61L27/00 ,  A61L31/00 ,  A61P7/02 ,  A61P9/10 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  C07C207/00 ,  C07C291/08 ,  C07D231/12 ,  C07D267/04 ,  C07D279/02 ,  C07D267/02

    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变其碳酸pKα的药物而获得。当这种药物是非甾体抗炎药物时，所得的C-亚硝基化合物起COX- 1和COX-2抑制剂，没有与COX-1抑制相关的有害作用，但具有与COX-1和COX-2抑制相关的有利效果。 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。

    Methods of treating cardio pulmonary diseases with NO group compounds
    4.
    发明申请
    Methods of treating cardio pulmonary diseases with NO group compounds 审中-公开
    用NO组化合物治疗心肺疾病的方法

    公开(公告)号：US20070191478A1

    公开(公告)日：2007-08-16

    申请号：US11231162

    申请日：2005-09-20

    申请人： Jonathan Stamler ,  Eric Toone ,  Andrew Gow

    发明人： Jonathan Stamler ,  Eric Toone ,  Andrew Gow

    IPC分类号： A61K31/21

    CPC分类号： C12N5/0641 ,  A61K31/197 ,  A61K31/21 ,  A61K33/00 ,  A61K33/04 ,  A61M2202/0275 ,  A61K2300/00

    摘要： Treatment of pulmonary disorders associated with hypoxemia and/or smooth muscle constriction and/or inflammation comprises administering into the lungs as a gas a compound with an NO group which does not form NO2/NOx in the presence of oxygen or reactive oxygen species at body temperature. Treatment of cardiac and blood disorders, e.g., angina, myocardial infarction, heart failure, hypertension, sickle cell disease and clotting disorders, comprises administering into the lungs as a gas, a compound which reacts with cysteine in hemoglobin and/or dissolves in blood and has an NO group which is bound in said compound so that it does not form NO2/NOx in the presence of oxygen or reactive oxygen species at body temperature. Exemplary of the compound administered in each case is ethyl nitrite. Treatment of patient in need of improved oxygenation, blood flow of and/or thinning of blood comprises providing in the patient a therapeutic amount of red blood cells loaded with nitrosylated hemoglobin. A method is directed to screening drugs that increase level of nitrosoglutathione in airway lining fluid.

    摘要翻译： 与低氧血症和/或平滑肌收缩和/或炎症相关的肺部疾病的治疗包括以肺部作为气体给予具有不形成NO 2的NO组的化合物 在体温存在氧或活性氧的情况下。 治疗心脏和血液疾病，例如心绞痛，心肌梗死，心力衰竭，高血压，镰状细胞病和凝血障碍，包括作为气体给予肺，与血红蛋白中的半胱氨酸反应和/或溶解于血液中的化合物和 具有在所述化合物中结合的NO基团，使得其在体温存在氧或活性氧的情况下不形成NO 2 / NO x 2 x。 在每种情况下施用的化合物的实例是亚硝酸乙酯。 治疗需要改善氧合，血流和/或血液变薄的患者包括在患者体内提供加载有亚硝基化血红蛋白的治疗量的红细胞。 一种方法是用于筛选增加气道衬里液中亚硝基谷胱甘肽水平的药物。

    Carbon nanotubules for storage of nitric oxide
    6.
    发明申请
    Carbon nanotubules for storage of nitric oxide 审中-公开
    用于储存一氧化氮的碳纳米管

    公开(公告)号：US20050152891A1

    公开(公告)日：2005-07-14

    申请号：US10980616

    申请日：2004-11-03

    申请人： Eric Toone ,  Jonathan Stamler

    发明人： Eric Toone ,  Jonathan Stamler

    IPC分类号： A61K33/00 ,  A61K45/06 ,  A61L29/10 ,  A61L29/16 ,  A61L31/08 ,  A61L31/16 ,  A61K33/44

    CPC分类号： A61K33/00 ,  A61K45/06 ,  A61L29/103 ,  A61L29/16 ,  A61L31/084 ,  A61L31/16 ,  A61L2300/114 ,  A61L2300/416 ,  A61L2300/432 ,  A61L2300/45 ,  A61L2300/624

    摘要： Delivering nitric oxide to a treatment site, such as in the area of an implanted stent, over a period of hours or days is desirable; however, the storage and release of nitric oxide in medically-relevant situations and amounts is a challenge, in part due to the gaseous nature of nitric oxide and its instability in the presence of oxygen. The present invention provides a method of preparing compositions of matter, particularly those comprising nanotubules, containing nitric oxide or gases with nitric oxide-like biological activity, where the gas is non-covalently bound to the composition. These compositions allow for the storage of nitric oxide or a related gas, followed by controlled release of the gas. Compositions disclosed in the present invention include polymers, articles, pills, capsules, and medical devices.

    摘要翻译： 将一氧化氮递送至治疗部位，例如在植入支架的区域中，需要数小时或数天; 然而，一氧化氮在医学相关的情况和量中的储存和释放是一个挑战，部分是由于一氧化氮的气体性质及其在氧气存在下的不稳定性。 本发明提供了一种制备物质组合物的方法，特别是包含含有一氧化氮或具有一氧化氮样生物活性的气体的纳米管的组合物，其中气体与组合物非共价结合。 这些组合物允许一氧化氮或相关气体的储存，然后控制释放气体。 本发明公开的组合物包括聚合物，制品，丸剂，胶囊和医疗装置。

    C-Nitroso compounds and use thereof
    7.
    发明申请
    C-Nitroso compounds and use thereof 有权
    C-亚硝基化合物及其用途

    公开(公告)号：US20070258942A1

    公开(公告)日：2007-11-08

    申请号：US11822770

    申请日：2007-07-10

    申请人： Jonathan Stamler ,  Eric Toone

    发明人： Jonathan Stamler ,  Eric Toone

    IPC分类号： A61K31/785 ,  A61F2/06 ,  A61K47/00 ,  A61P41/00

    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 about 20, vascular relaxing effect is obtained at nanomolar concentrations without ghitathione. 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在约15至约20范围内的碳酸获得时，在毫摩尔浓度下获得血管松弛效果，而没有使用谷胱甘肽。 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。

    C-nitroso compounds and use thereof
    8.
    发明申请
    C-nitroso compounds and use thereof 失效
    C-亚硝基化合物及其用途

    公开(公告)号：US20050187166A1

    公开(公告)日：2005-08-25

    申请号：US11052141

    申请日：2005-02-08

    申请人： Jonathan Stamler ,  Eric Toone

    发明人： Jonathan Stamler ,  Eric Toone

    IPC分类号： A61K31/00 ,  A61K31/195 ,  C07C207/00 ,  C07C207/04 ,  C07C219/06 ,  C07C245/04 ,  A61K38/05 ,  A61K31/21 ,  A61K31/535 ,  A61K31/54 ,  A61K31/55 ,  A61K31/553 ,  A61K31/554

    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 about 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。 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。

    Stable no-delivering compounds
    10.
    发明申请
    Stable no-delivering compounds 有权
    稳定的不输送化合物

    公开(公告)号：US20060217439A1

    公开(公告)日：2006-09-28

    申请号：US11376756

    申请日：2006-03-14

    申请人： Eric Toone ,  Jonathan Stamler

    发明人： Eric Toone ,  Jonathan Stamler

    IPC分类号： A61K31/21 ,  C07C331/02

    CPC分类号： A61L2/23 ,  A61L2/20 ,  A61L29/16 ,  A61L2300/114 ,  A61L2300/216 ,  C07C381/00

    摘要： Disclosed are novel NO-releasing compounds which comprise a stabilized S-nitrosyl group and a free alcohol or a free thiol group. Also disclosed is a method of preparing the NO-releasing compounds. The method comprises reacting a polythiol or a thioalcohol with a nitrosylating agent. Also disclosed are medical devices coated with the disclosed compounds, methods of delivering NO to treatments sites in a subject by utilizing the medical devices and methods of sterilizing surfaces.

    摘要翻译： 公开了包含稳定的S-亚硝酰基和游离醇或游离巯基的新型NO释放化合物。 还公开了制备释放NO的化合物的方法。 该方法包括使多硫醇或硫代醇与亚硝酰化剂反应。 还公开了涂覆有所公开的化合物的医疗装置，通过利用医疗装置和灭菌表面的方法将NO递送到受试者的治疗部位的方法。