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    Serotonin potentiation by oleamide analogs
    2.
    发明授权
    Serotonin potentiation by oleamide analogs 有权
    油酰胺类似物的5-羟色胺增强作用

    公开(公告)号：US06734204B1

    公开(公告)日：2004-05-11

    申请号：US09647447

    申请日：2000-09-28

    申请人： Dale L. Boger

    发明人： Dale L. Boger

    IPC分类号： A61K3140

    CPC分类号： A61K31/164 ,  A61K31/16 ,  A61K31/165 ,  Y10S514/973

    摘要： Analogs related to oleamide are employed for potentiating the 5-HT2A and 5-HT1A responses to serotonin (5-HT). With respect to the potentiation of the 5-HT2A receptor response, it is disclosed that, of the naturally occurring fatty acids, the primary amide of oleic acid (oleamide) is the most effective potentiating agent of serotonin and that the potentiating activity of oleamide analogs is highly dependent upon their structural features. In particular, the presence, position, and stereochemistry of the 9-cis double bond is required and even subtle structural variations reduce or eliminate activity. Secondary or tertiary amides may replace the primary amide but follow a well-defined relationship requiring small amide substituents suggesting that the carboxamide serves as a hydrogen bond acceptor but not donor. Alternative modifications at the carboxamide as well as modifications of the methyl terminus or the hydrocarbon region spanning the carboxamide and double bond typically eliminate activity. With respect to the potentiation of the 5-HT1A receptor response, it is disclosed that the potentiation activity of oleamide analogs is more tolerant and accommodates a wider range of structural modifications. One genus of analogs is disclosed that inhibits rather than potentiates the 5-HT2A, but not the 5-HT1A, receptor response. Such analogs permit the selective modulation of serotonin receptor subtypes and have opposing effects on the different subtypes.

    摘要翻译： 与油酰胺相关的类似物用于增强5-羟色胺（5-HT）的5-HT2A和5-HT1A应答。 关于5-HT2A受体反应的增强，公开了天然存在的脂肪酸，油酸（油酰胺）的主要酰胺是5-羟色胺的最有效的增效剂，并且油酰胺类似物的增强活性 高度依赖于它们的结构特征。 特别地，需要9-顺式双键的存在，位置和立体化学，甚至微妙的结构变化减少或消除活性。 仲或叔酰胺可以替代初级酰胺，但遵循明确的关系，需要小的酰胺取代基，表明羧酰胺用作氢键受体而不是供体。 甲酰胺的替代修饰以及甲基末端或跨越甲酰胺和双键的烃区的修饰通常消除活性。 关于5-HT1A受体反应的增强，公开了油酰胺类似物的增强活性更耐受并适应更广泛的结构修饰。 公开了一类类似物，其抑制而不是增强5-HT2A，而不是5-HT1A受体反应。 这样的类似物允许5-羟色胺受体亚型的选择性调节并且对不同亚型具有相反的作用。

    Prophylactic therapeutic and industrial antioxidant compositions enhanced with stabilized atomic hydrogen/free electrons and methods to prepare and use such compositions
    3.
    发明授权
    Prophylactic therapeutic and industrial antioxidant compositions enhanced with stabilized atomic hydrogen/free electrons and methods to prepare and use such compositions 失效
    用稳定的原子氢/自由电子增强的预防性治疗和工业抗氧化剂组合物以及制备和使用这些组合物的方法

    公开(公告)号：US06649193B1

    公开(公告)日：2003-11-18

    申请号：US09591194

    申请日：2000-06-09

    申请人： Miroslav Colic

    发明人： Miroslav Colic

    IPC分类号： A61K900

    CPC分类号： B82Y5/00 ,  A61K9/127 ,  A61K31/714 ,  A61K33/00 ,  A61K36/15 ,  A61K36/82 ,  A61K36/87 ,  A61K41/0004 ,  A61K47/6949 ,  Y10S424/06 ,  Y10S514/836 ,  Y10S514/97 ,  Y10S514/973 ,  A61K31/70 ,  A61K2300/00

    摘要： The invention is directed to therapeutic antioxidant compositions which are enhanced by the stabilized atomic hydrogen; one of the most potent antioxidants. Such products can be used for prophylactic and therapeutic purposes in treatment of cancer, diabetes, autoimmune diseases, neurodegenerative diseases, cardiovascular diseases, skin diseases etc. The products described can be used independently or in combination with other drugs and treatment modalities. The products can also be used as dietetic products to aid in desired weigh loss. The described products can also be used to prevent oxidative and free radical damage to food and oxidation-prone industrial products. The invention also describes the methods to produce and stabilize atomic hydrogen and prepare and use such stabilized/encaged atomic hydrogen enhanced antioxidant compositions.

    摘要翻译： 本发明涉及通过稳定的原子氢增强的治疗性抗氧化剂组合物; 最有效的抗氧化剂之一。 这些产品可用于治疗癌症，糖尿病，自身免疫性疾病，神经退行性疾病，心血管疾病，皮肤疾病等中的预防和治疗目的。所述产品可以独立使用或与其他药物和治疗方式组合使用。 该产品也可用作饮食产品，以帮助所需的体重减轻。 所述产品也可用于防止氧化和自由基损伤食物和易氧化的工业产品。 本发明还描述了制备和稳定原子氢的方法，并且制备和使用这种稳定/包裹的原子氢增强抗氧化剂组合物。

    Hydrogen peroxide disinfectant with increased activity
    5.
    发明申请
    Hydrogen peroxide disinfectant with increased activity 有权
    过氧化氢消毒剂具有增加的活性

    公开(公告)号：US20020192297A1

    公开(公告)日：2002-12-19

    申请号：US10028373

    申请日：2001-12-28

    发明人： Jose A. Ramirez ,  Michael J. Rochon

    IPC分类号： A61K033/42 ,  A61K033/40

    CPC分类号： A01N59/00 ,  Y10S424/06 ,  Y10S514/97 ,  Y10S514/973 ,  A01N25/30 ,  A01N25/22 ,  A01N2300/00

    摘要： An acidic aqueous hydrogen peroxide solution is provided with improved disinfectant activity. Concentrated solutions preferably contain up to about 8 wt./wt. % H202 and as-used concentrations contain about 0.5 % wt./wt. % H202. The solution also contains from 0.05 to 8.0 wt./wt. % of at least one phosphorous-based acid, e.g. phosphoric acid and/or a phosphonic acid with from 1 to 5 phosphonic acid groups, and from 0.02 to 5 wt./wt. % of at least one anionic surfactant. The surfactant is selected from C8 to C16 alkyl aryl sulfonic acids, sulfonated C12 to C22 carboxylic acids, C8 to C22 alkyl diphenyl oxide sulfonic acids, naphthalene sulfonic acids, C8 to C22 alkyl sulfonic acids, and alkali metal and ammonium salts thereof, and alkali metal C8 to C18 alkyl sulfates, and mixtures thereof. Most preferably the solution has an emulsifier and/or hydrotrope, e.g. an alkylated sulfonated diphenyl oxide salt, an alkyl aryl polyoxyethylene surfactant, and/or a polyoxyethylene surfactant. The solution may also contain corrosion inhibitors and/or lower alcohols.

    摘要翻译： 提供酸性过氧化氢水溶液具有改善的消毒剂活性。 浓缩溶液优选含有高达约8重量/重量 ％H 2 O 2和所用浓度含有约0.5重量％ ％H202。 该溶液还含有0.05至8.0wt./wt。 至少一种基于磷的酸的％，例如。 磷酸和/或具有1至5个膦酸基团的膦酸和0.02至5重量/重量的膦酸。 ％的至少一种阴离子表面活性剂。 表面活性剂选自C 8〜C 16烷基芳基磺酸，磺化C12〜C22羧酸，C8〜C22烷基二苯基氧化物磺酸，萘磺酸，C8〜C22烷基磺酸及其碱金属和铵盐，碱 金属C8至C18烷基硫酸盐，及其混合物。 最优选地，溶液具有乳化剂和/或水溶助长剂，例如。 烷基化磺化二苯基氧化物盐，烷基芳基聚氧乙烯表面活性剂和/或聚氧乙烯表面活性剂。 该溶液还可含有腐蚀抑制剂和/或低级醇。

    Hydrogen peroxide disinfectant with increased activity
    6.
    发明申请
    Hydrogen peroxide disinfectant with increased activity 审中-公开
    过氧化氢消毒剂具有增加的活性

    公开(公告)号：US20020142051A1

    公开(公告)日：2002-10-03

    申请号：US10067809

    申请日：2002-02-08

    发明人： Michael J. Rochon

    IPC分类号： A01N039/00

    CPC分类号： A01N59/00 ,  Y10S424/06 ,  Y10S514/97 ,  Y10S514/973 ,  A01N25/30 ,  A01N25/22 ,  A01N2300/00

    摘要： An acidic aqueous hydrogen peroxide solution is provided with improved disinfectant activity. Concentrated solutions preferably contain up to about 8 wt./wt. % H2O2 and as-used concentrations contain about 0.5% wt./wt. % H2O2. The solution also contains from 0.05 to 8.0 wt./wt. % of at least one phosphorous-based acid, e.g. phosphoric acid and/or a phosphonic acid with from 1 to 5 phosphonic acid groups, and from 0.02 to 5 wt./wt. % of at least one anionic surfactant. The surfactant is selected from C8 to C16 alkyl aryl sulfonic acids, sulfonated C12 to C22 carboxylic acids, C8 to C22 alkyl diphenyl oxide sulfonic acids, naphthalene sulfonic acids, C8 to C22 alkyl sulfonic acids, and alkali metal and ammonium salts thereof, and alkali metal C8 to C18 alkyl sulfates, and mixtures thereof. Most preferably the solution has an emulsifier, e.g. a polyoxyethylene surfactant. The solution also preferably contains a hydrotrope, e.g. an alkylated sulfonated diphenyl oxide salt. The solution may also contain corrosion inhibitors and/or lower alcohols.

    摘要翻译： 提供酸性过氧化氢水溶液具有改善的消毒剂活性。 浓缩溶液优选含有高达约8重量/重量 ％H 2 O 2和所使用的浓度含有约0.5重量％ ％H2O2。 该溶液还含有0.05至8.0wt./wt。 至少一种基于磷的酸的％，例如。 磷酸和/或具有1至5个膦酸基团的膦酸和0.02至5重量/重量的膦酸。 ％的至少一种阴离子表面活性剂。 表面活性剂选自C 8〜C 16烷基芳基磺酸，磺化C12〜C22羧酸，C8〜C22烷基二苯基氧化物磺酸，萘磺酸，C8〜C22烷基磺酸及其碱金属和铵盐，碱 金属C8至C18烷基硫酸盐，及其混合物。 最优选地，溶液具有乳化剂，例如 聚氧乙烯表面活性剂。 该溶液还优选含有水溶助长剂，例如。 烷基化磺化二苯醚盐。 该溶液还可含有腐蚀抑制剂和/或低级醇。

    Salts of thrombin inhibitors
    7.
    发明授权
    Salts of thrombin inhibitors 失效
    凝血酶抑制剂的盐

    公开(公告)号：US06407067B1

    公开(公告)日：2002-06-18

    申请号：US09559047

    申请日：2000-04-27

    申请人： Bernd Schäfer

    发明人： Bernd Schäfer

    IPC分类号： A61F206

    CPC分类号： C07K5/06078 ,  A61K38/00 ,  Y10S514/97 ,  Y10S514/973

    摘要： Compounds having thrombin inhibiting activity of the general formula I or II where n is 0.5, 1, 2 and HX is  and HX is optionally substituted once or twice by methyl, ethyl or hydroxyl, and the tautomers and stereoisomers thereof, which compounds have greater thermal stability betaines, and salts of mineral acids or C1-C4-carboxylic acids.

    摘要翻译： 具有通式I或II的凝血酶抑制活性的化合物为0.5,1,2和HX，HX任选被甲基，乙基或羟基取代一次或两次，以及其互变异构体和立体异构体，该化合物具有较高的热稳定性甜菜碱， 和无机酸或C 1 -C 4羧酸的盐。

    Hydrogen peroxide disinfectant with increased activity
    8.
    发明授权
    Hydrogen peroxide disinfectant with increased activity 有权
    过氧化氢消毒剂具有增加的活性

    公开(公告)号：US06346279B1

    公开(公告)日：2002-02-12

    申请号：US09356345

    申请日：1999-07-19

    申请人： Michael J. Rochon

    发明人： Michael J. Rochon

    IPC分类号： A01N5900

    CPC分类号： A01N59/00 ,  Y10S424/06 ,  Y10S514/97 ,  Y10S514/973 ,  A01N25/30 ,  A01N25/22 ,  A01N2300/00

    摘要： An acidic aqueous hydrogen peroxid solution is provided, with improved disinfectant activity. Concentrated solutions preferably contain up to about 8% and as-used concentrations contain about 0.5% peroxide. The solution also contains from 0.1 to 5.0% of at least one acid compound, e.g. phosphoric and/or a phosphonate with from 1 to 5 phosphonic acid groups, and from 0.02 to 5% of at least one anionic surfactant. The surfactant is selected from C8 to C16-alkyl aryl sulphonic acids, sulphonated C12 to C22 carboxylic acids, C8 to C22-alkyl diphenyl oxide sulphonic acids, naphthalene sulphonic acids, C8 to C22 alkyl sulphonic acids, and alkali metal and ammonium salts thereof, and alkali metal C8 to C18 alkyl sulphates, and mixtures thereof. Most preferably the solution has an emulsifier, e.g. a salt of an alkylated diphenyl oxide. The solution may also contain corrosion inhibitors and/or lower alcohols.

    摘要翻译： 提供酸性过氧化氢水溶液，具有改善的消毒剂活性。 浓缩溶液优选含有高达约8％且所用浓度含有约0.5％的过氧化物。 该溶液还含有0.1至5.0％的至少一种酸化合物，例如， 具有1至5个膦酸基团的磷酸酯和/或膦酸酯，和0.02至5％的至少一种阴离子表面活性剂。 表面活性剂选自C 8至C 16烷基芳基磺酸，磺化的C 12至C 22羧酸，C 8至C 22烷基二苯基氧基磺酸，萘磺酸，C 8至C 22烷基磺酸及其碱金属和铵盐， 和碱金属C8至C18烷基硫酸盐，及其混合物。 最优选地，溶液具有乳化剂，例如 烷基化二苯基氧化物的盐。 该溶液还可含有腐蚀抑制剂和/或低级醇。

    AQUEOUS SOLVENT FOR CORTICOSTEROIDS
    9.
    发明申请
    AQUEOUS SOLVENT FOR CORTICOSTEROIDS 失效
    水溶性溶剂

    公开(公告)号：US20020013305A1

    公开(公告)日：2002-01-31

    申请号：US09347974

    申请日：1999-07-06

    发明人： CALVIN HANNA

    IPC分类号： A61K031/56

    CPC分类号： A61K47/14 ,  A61K9/0014 ,  A61K31/56 ,  A61K47/10 ,  A61K47/44 ,  Y10S514/952 ,  Y10S514/97 ,  Y10S514/973 ,  Y10S514/975

    摘要： A solvent comprising a combination of water and organic solvent(s) capable of dissolving a therapeutically effective amount of medicament(s) not readily soluble in aqueous solvents, said organic solvents including alcohol and glycol, and said medicaments including hydrocortisone.

    摘要翻译： 一种包含能够溶解治疗有效量的不易溶于水溶剂的药物的水和有机溶剂的组合的溶剂，所述有机溶剂包括醇和二醇，所述药物包括氢化可的松。