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    Nitrosated and nitrosylated compounds and compositions and their use for treating respiratory disorders
    1.
    发明授权
    Nitrosated and nitrosylated compounds and compositions and their use for treating respiratory disorders 失效
    亚硝化和亚硝化化合物及其组合物及其用于治疗呼吸系统疾病的用途

    公开(公告)号：US06579863B1

    公开(公告)日：2003-06-17

    申请号：US09689851

    申请日：2000-10-13

    申请人： David S. Garvey ,  L. Gordon Letts ,  H. Burt Renfroe ,  Stewart K. Richardson

    发明人： David S. Garvey ,  L. Gordon Letts ,  H. Burt Renfroe ,  Stewart K. Richardson

    IPC分类号： A61K3156

    CPC分类号： C07D451/06 ,  C07C313/36 ,  C07D311/22 ,  C07D451/10 ,  C07D471/04 ,  C07J5/00 ,  C07J7/00 ,  C07J31/00 ,  C07J71/00 ,  C07J71/0031

    摘要： Disclosed are (i) compounds of a steroid, a &bgr;-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO2 group or a group which stimulates endogenous production of NO or EDRF in vivo; (ii) compositions of steroids, &bgr;-agonists, anticholinergics, mast cell stabilizers and PDE inhibitors, which can optionally be substituted with at least one NO or NO2 moiety or a group which stimulates endogenous production of NO or EDRF in vivo, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or that stimulates endogenous production of NO or EDRF in vivo; and (iii) uses for them in preventing and/or treating respiratory disorders.

    摘要翻译： 公开的是（i）直接或间接连接到NO或NO 2基团或刺激NO或EDRF的内源性产生的基团的类固醇，β-激动剂，抗胆碱能药，肥大细胞稳定剂和磷酸二酯酶（PDE）抑制剂的化合物 体内; （ii）类固醇，β-激动剂，抗胆碱能药物，肥大细胞稳定剂和PDE抑制剂的组合物，其可任选地被至少一个NO或NO 2部分或刺激体内NO或EDRF内源性产生的基团取代;以及化合物 捐赠，转移或释放一氧化氮作为带电物质，即亚硝酸盐（NO +）或硝酰基（NO-），或作为中性物质，一氧化氮（NO））或刺激体内NO或EDRF的内源性产生; 和（iii）用于预防和/或治疗呼吸系统疾病。

    N-(2-fluoro-1,1,2,2-tetrachloroethylthio)-N-phenyl methane sulfonamides and their use in controlling pests
    2.
    发明授权
    N-(2-fluoro-1,1,2,2-tetrachloroethylthio)-N-phenyl methane sulfonamides and their use in controlling pests 失效
    N-（2-氟-1,1,2,2-四氯乙硫基）-N-苯基甲磺酰胺及其在防治害虫中的应用

    公开(公告)号：US4193933A

    公开(公告)日：1980-03-18

    申请号：US657019

    申请日：1976-02-09

    申请人： Peter F. Epstein ,  Willis C. McGuire

    发明人： Peter F. Epstein ,  Willis C. McGuire

    IPC分类号： C07C119/00

    CPC分类号： C07C313/36

    摘要： Compounds of the formula ##STR1## in which R.sub.1 is a lower alkyl, lower haloalkyl or lower alkenyl group, R.sub.2 is hydrogen, halogen, lower alkoxy, lower alkyl, cyano, or a nitro group, and n is an integer between 1 and 5, R.sub.2 being the same or different when n is greater than 1; and their use in controlling pests, e.g. acarids, fungi, helminths and protozoa which cause coccidiosis.

    摘要翻译： 其中R 1为低级烷基，低级卤代烷基或低级烯基，R 2为氢，卤素，低级烷氧基，低级烷基，氰基或硝基的式“IMAGE”化合物，n为1至5的整数 当n大于1时，R2相同或不同; 及其在防治害虫方面的应用。 螨虫，真菌，蠕虫和引起球虫病的原生动物。

    Nitrosated and nitrosylated compounds and compositions and their use for treating respiratory disorders
    4.
    发明授权
    Nitrosated and nitrosylated compounds and compositions and their use for treating respiratory disorders 失效
    亚硝化和亚硝化化合物及其组合物及其用于治疗呼吸系统疾病的用途

    公开(公告)号：US07345037B2

    公开(公告)日：2008-03-18

    申请号：US11604677

    申请日：2006-11-28

    申请人： David S. Garvey ,  L. Gordon Letts ,  H. Burt Renfroe ,  Stewart K. Richardson

    发明人： David S. Garvey ,  L. Gordon Letts ,  H. Burt Renfroe ,  Stewart K. Richardson

    IPC分类号： A61K31/40 ,  C07D451/00

    CPC分类号： C07D451/06 ,  C07C313/36 ,  C07D311/22 ,  C07D451/10 ,  C07D471/04 ,  C07J5/00 ,  C07J7/00 ,  C07J31/00 ,  C07J71/00 ,  C07J71/0031

    摘要： Disclosed are (i) compounds of a steroid, a β-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO2 group or a group which stimulates endogenous production of NO or EDRF in vivo; (ii) compositions of steroids, β-agonists, anticholinergics, mast cell stabilizers and PDE inhibitors, which can optionally be substituted with at least one NO or NO2 moiety or a group which stimulates endogenous production of NO or EDRF in vivo, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO.) or that stimulates endogenous production of NO or EDRF in vivo; and (iii) uses for them in preventing and/or treating respiratory disorders.

    摘要翻译： 公开的是（i）直接或间接连接到NO或NO 2基团或基团上的基团的类固醇，β-激动剂，抗胆碱能药，肥大细胞稳定剂和磷酸二酯酶（PDE）抑制剂的化合物 其在体内刺激NO或EDRF的内源性产生; （ii）类固醇，β-激动剂，抗胆碱能药物，肥大细胞稳定剂和PDE抑制剂的组合物，其可任选地被至少一个NO或NO 2个部分取代，或刺激内源性产生NO 或EDRF，以及作为带电物质，即亚硝酸盐（硝酸）或硝酰基（NO +）的一氧化氮，或NOX + 作为中性物种，一氧化氮（NO））或者在体内刺激NO或EDRF的内源性产生; 和（iii）用于预防和/或治疗呼吸系统疾病。

    Nitrosated and nitrosylated compounds and compositions and their use for treating respiratory disorders
    5.
    发明申请
    Nitrosated and nitrosylated compounds and compositions and their use for treating respiratory disorders 失效
    亚硝化和亚硝化化合物及其组合物及其用于治疗呼吸系统疾病的用途

    公开(公告)号：US20070155781A1

    公开(公告)日：2007-07-05

    申请号：US11604677

    申请日：2006-11-28

    申请人： David Garvey ,  L. Letts ,  H. Renfroe ,  Stewart Richardson

    发明人： David Garvey ,  L. Letts ,  H. Renfroe ,  Stewart Richardson

    IPC分类号： A61K31/46 ,  C07D451/02

    CPC分类号： C07D451/06 ,  C07C313/36 ,  C07D311/22 ,  C07D451/10 ,  C07D471/04 ,  C07J5/00 ,  C07J7/00 ,  C07J31/00 ,  C07J71/00 ,  C07J71/0031

    摘要： Disclosed are (i) compounds of a steroid, a β-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO2 group or a group which stimulates endogenous production of NO or EDRF in vivo; (ii) compositions of steroids, β-agonists, anticholinergics, mast cell stabilizers and PDE inhibitors, which can optionally be substituted with at least one NO or NO2 moiety or a group which stimulates endogenous production of NO or EDRF in vivo, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO.) or that stimulates endogenous production of NO or EDRF in vivo; and (iii) uses for them in preventing and/or treating respiratory disorders.

    摘要翻译： 公开的是（i）直接或间接连接到NO或NO 2基团或基团上的基团的类固醇，β-激动剂，抗胆碱能药，肥大细胞稳定剂和磷酸二酯酶（PDE）抑制剂的化合物 其在体内刺激NO或EDRF的内源性产生; （ii）类固醇，β-激动剂，抗胆碱能药物，肥大细胞稳定剂和PDE抑制剂的组合物，其可任选地被至少一个NO或NO 2个部分取代，或刺激内源性产生NO 或EDRF，以及作为带电物质，即亚硝酸盐（硝酸）或硝酰基（NO +）的一氧化氮，或NOX + 作为中性物种，一氧化氮（NO））或者在体内刺激NO或EDRF的内源性产生; 和（iii）用于预防和/或治疗呼吸系统疾病。

    Novel Method for Directly Nitration of OH-, SH-and NHR-Functions in Organic Molecules by Means of in Situ Generated Carbonic Acid Dinitrate
    7.
    发明申请
    Novel Method for Directly Nitration of OH-, SH-and NHR-Functions in Organic Molecules by Means of in Situ Generated Carbonic Acid Dinitrate 审中-公开
    通过原位生成的硝酸二苯酯在有机分子中直接硝化OH-，SH-和NHR-功能的新方法

    公开(公告)号：US20120232257A1

    公开(公告)日：2012-09-13

    申请号：US13390311

    申请日：2010-10-04

    申请人： Nikolas Pietrzik

    发明人： Nikolas Pietrzik

    IPC分类号： C07C201/02 ,  C07H5/04 ,  C07H1/00 ,  C07C203/04 ,  C07D251/06 ,  C08B5/02 ,  C07H7/02

    CPC分类号： C07B43/02 ,  C07C313/36 ,  C07D251/06 ,  C07H9/04

    摘要： The invention relates to a nitration method having the following principles: a phosgene species is converted with two equivalent silver nitrates into a double-mixed anhydride of carbonic acid and nitric acid, known here as carbonic acid dinitrate (I). Said operation is carried out in situ, and the formed dinitrate decomposes spontaneously. In addition to carbon dioxide, nitrate ions and nitronium ions are formed, said ions comprising electrophiles which are necessary for nitration. The solution which is used is acetonitrile, and is insignificant if the alcohol species is dissolved or suspended. The necessary equivalent silver nitrates are introduced into the system and optionally heated or cooled to the desired temperature. Subsequently, the acid chloride is introduced slowly, drop by drop or slowly little by little. Phosgene, diphosgene, triphosgene and chloroformic acid ester can be used as carbonic acid dichloride and monochloride, and their thiocarbonic acid analogues. A brown colouration and precipitated silver chloride display the formation of the carbonic acid reactants, said brown colouration rapidly discolouring due to an immediate reaction of the nitronium ions with the substrate with is to be nitrated. Towards the end of the addition of phosgene, the brown colouration remains for longer and longer until it no longer disappears. Then, it is stirred for another hour at room temperature. In the event of high acid-sensitive educts, non-nucleophilic nitrogen bases such as DBU can be added to the system in order to intercept the formation of nitric acid.

    摘要翻译： 本发明涉及一种具有以下原理的硝化方法：将光气物质用两当量的硝酸银转化成碳酸和硝酸的双重混合酸酐，这里称为硝酸二苯酯（I）。 所述操作在原位进行，形成的硝酸酯自发分解。 除了二氧化碳之外，还形成硝酸根离子和硝鎓离子，所述离子包含硝化所必需的亲电体。 使用的溶液是乙腈，如果醇类物质溶解或悬浮，则不重要。 将必需的相当的硝酸银引入体系中，并任选地加热或冷却至所需温度。 随后，缓慢逐滴引入酰氯，或逐渐缓缓地引入。 光气，双光气，三光气和氯甲酸酯可用作二氯化碳和一氯化碳及其硫代碳酸类似物。 棕色着色和沉淀的氯化银显示碳酸反应物的形成，棕色着色由于硝基离子与底物立即反应而迅速变色将被硝化。 在加入光气结束时，棕色着色会持续更长时间，直至不再消失。 然后在室温下再搅拌1小时。 在酸敏感性离析物高的情况下，可以向体系中加入非亲核性氮碱如DBU，以拦截硝酸的形成。

    Nitric oxide donors, compositions and methods of use related applications
    9.
    发明申请
    Nitric oxide donors, compositions and methods of use related applications 审中-公开
    一氧化氮供体，组合物和使用方法相关应用

    公开(公告)号：US20030203915A1

    公开(公告)日：2003-10-30

    申请号：US10407420

    申请日：2003-04-07

    发明人： Xinqin Fang ,  David S. Garvey ,  Ricky D. Gaston ,  Chia-En Lin ,  Ramani R. Ranatunga ,  Stewart K. Richardson ,  Tiansheng Wang ,  Weiheng Wang ,  Shiow-Jyi Wey

    IPC分类号： A61K031/496 ,  A61K031/505 ,  A61K031/325 ,  A61K031/215

    CPC分类号： C07D213/74 ,  C07C313/36 ,  C07C2602/08 ,  C07C2602/42 ,  C07C2603/74 ,  C07D211/54 ,  C07D217/02 ,  C07D233/96 ,  C07D239/47 ,  C07D241/08 ,  C07D241/24 ,  C07D295/155 ,  C07D317/22 ,  C07D453/02 ,  C07F9/383 ,  C07F9/4018

    摘要： The invention describes novel nitric oxide donors and novel compositions comprising at least one nitric oxide donor. The invention also provides novel compositions comprising at least one nitric oxide donor, and, optionally, at least one therapeutic agent. The compounds and compositions of the invention can also be bound to a matrix. The invention also provides methods for treating cardiovascular diseases, for the inhibition of platelet aggregation and platelet adhesion caused by the exposure of blood to a medical device, for treating pathological conditions resulting from abnormal cell proliferation; transplantation rejections, autoimmune, inflammatory, proliferative, hyperproliferative, vascular diseases; for reducing scar tissue or for inhibiting wound contraction, particularly the prophylactic and/or therapeutic treatment of restenosis by administering the nitric oxide donor optionally in combination with at least one therapeutic agent. The invention also provides methods for treating inflammation, pain, fever, gastrointestinal disorders, respiratory disorders and sexual dysfunctions. The nitric oxide donors donate, transfer or release nitric oxide, and/or elevate endogenous levels of endothelium-derived relaxing factor, and/or stimulate endogenous synthesis of nitric oxide and/or are substrates for nitric oxide synthase and are capable of releasing nitric oxide or indirectly delivering or transferring nitric oxide to targeted sites under physiological conditions. The therapeutic agent can optionally be substituted with at least one NO and/or NO2 group (i.e., nitrosylated and/or nitrosated). The invention also provides novel compositions and kits comprising at least one nitric oxide donor and/or at least one therapeutic agent.

    摘要翻译： 本发明描述了新一代氧化氮供体和包含至少一种一氧化氮供体的新型组合物。 本发明还提供包含至少一种一氧化氮供体和任选的至少一种治疗剂的新型组合物。 本发明的化合物和组合物也可以结合到基质上。 本发明还提供治疗心血管疾病的方法，用于抑制由血液暴露于医疗器械引起的血小板聚集和血小板粘附，用于治疗由异常细胞增殖引起的病理状况; 移植排斥，自身免疫，炎症，增殖，过度增殖，血管疾​​病; 用于减少瘢痕组织或抑制伤口收缩，特别是通过给予任选与至少一种治疗剂组合的一氧化氮供体的再狭窄的预防和/或治疗性治疗。 本发明还提供了治疗炎症，疼痛，发热，胃肠道疾病，呼吸障碍和性功能障碍的方法。 一氧化氮供体捐赠，转移或释放一氧化氮，和/或提升内源性内源性松弛因子水平，和/或刺激一氧化氮的内源性合成和/或是一氧化氮合成酶的底物，并能够释放一氧化氮 或在生理条件下将一氧化氮间接递送或转移到靶位点。 治疗剂可任选地被至少一种NO和/或NO 2基团取代（即亚硝基化和/或亚硝基化）。 本发明还提供了包含至少一种一氧化氮供体和/或至少一种治疗剂的新型组合物和试剂盒。

    Nitrosated and nitrosylated compounds and compositions and their use for treating respiratory disorders
    10.
    发明申请
    Nitrosated and nitrosylated compounds and compositions and their use for treating respiratory disorders 有权
    亚硝化和亚硝化化合物及其组合物及其用于治疗呼吸系统疾病的用途

    公开(公告)号：US20030199529A1

    公开(公告)日：2003-10-23

    申请号：US10428936

    申请日：2003-05-05

    发明人： David S. Garvey ,  L. Gordon Letts ,  H. Burt Renfroe ,  Stewart K. Richardson

    IPC分类号： A61K031/522 ,  A61K031/4545 ,  A61K031/4412 ,  A61K031/21 ,  C07D473/16 ,  C07D41/02 ,  C07C23/10

    CPC分类号： C07D451/06 ,  C07C313/36 ,  C07D311/22 ,  C07D451/10 ,  C07D471/04 ,  C07J5/00 ,  C07J7/00 ,  C07J31/00 ,  C07J71/00 ,  C07J71/0031

    摘要： Disclosed are (i) compounds of a steroid, a null-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO2 group or a group which stimulates endogenous production of NO or EDRF in vivo; (ii) compositions of steroids, null-agonists, anticholinergics, mast cell stabilizers and PDE inhibitors, which can optionally be substituted with at least one NO or NO2 moiety or a group which stimulates endogenous production of NO or EDRF in vivo, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NOnull) or nitroxyl (NOnull), or as the neutral species, nitric oxide (NOnull) or that stimulates endogenous production of NO or EDRF in vivo; and (iii) uses for them in preventing and/or treating respiratory disorders.

    摘要翻译： 公开的是（i）直接或间接连接到NO或NO 2基团或刺激NO或EDRF的内源性产生的基团的类固醇，β-激动剂，抗胆碱能药，肥大细胞稳定剂和磷酸二酯酶（PDE）抑制剂的化合物 体内; （ii）类固醇，β-激动剂，抗胆碱能药物，肥大细胞稳定剂和PDE抑制剂的组合物，其可以任选地被至少一个NO或NO 2部分或刺激体内NO或EDRF的内源性产生的基团取代;以及化合物 捐赠，转移或释放一氧化氮作为带电物种，即亚硝酸盐（NO +）或硝酰基（NO - ），或作为中性物质，一氧化氮（NO）或刺激内源性产生NO 或EDRF; 和（iii）用于预防和/或治疗呼吸系统疾病。