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    Methods for the treatment of male and female sexual dysfunction
    2.
    发明申请
    Methods for the treatment of male and female sexual dysfunction 审中-公开
    男性和女性性功能障碍的治疗方法

    公开(公告)号：US20050059645A1

    公开(公告)日：2005-03-17

    申请号：US10910964

    申请日：2004-08-02

    申请人： Nicholas Bodor

    发明人： Nicholas Bodor

    IPC分类号： A61K20060101 ,  A61K9/00 ,  A61K31/58 ,  A61K31/704 ,  A61K31/724

    CPC分类号： A61K9/006 ,  A61K9/0056 ,  A61K47/6951 ,  B82Y5/00

    摘要： Methods for the treatment of female sexual dysfunction, including treatment of associated postmenopausal symptoms, are provided using very low doses of 17β-[(1-methyl-1,4-dihydro-3-pyridinyl)carbonyloxy]estra-1,3,5(10)-trien-3-ol, also known as E2-CDS, which do not elevate average steady-state peripheral estradiol levels to above about 50-60 pg/ml. Also, methods for the treatment of male sexual dysfunction are provided using very low doses of E2-CDS which do not substantially elevate average peripheral estradiol levels to above average normal peripheral levels in the male mammal.

    摘要翻译： 使用非常低剂量的17β-[（1-甲基-1,4-二氢-3-吡啶基）羰基氧基]雌-1,3,5,5-三唑并[3,4-a]所示的方法来治疗女性性功能障碍，包括治疗相关的绝经后症状。 （10） - 三烯-3-醇，也称为E2-CDS，其不将平均稳态外周雌二醇水平提高至高于约50-60pg / ml。 此外，使用非常低剂量的E2-CDS提供了治疗男性性功能障碍的方法，其在雄性哺乳动物中基本上不将平均周围雌二醇水平提高至高于平均正常外周水平。

    Percutaneous penetration enhancer of oleic acid and 2-ethyl-1,3-hexanediol
    4.
    发明授权
    Percutaneous penetration enhancer of oleic acid and 2-ethyl-1,3-hexanediol 失效
    油酸和2-乙基-1,3-己二醇的经皮穿透增强剂

    公开(公告)号：US4983396A

    公开(公告)日：1991-01-08

    申请号：US412730

    申请日：1989-09-26

    申请人： Nicholas Bodor ,  Thorsteinn Loftsson

    发明人： Nicholas Bodor ,  Thorsteinn Loftsson

    IPC分类号： A61K9/70 ,  A61K31/21 ,  A61K31/565 ,  A61K47/10 ,  A61K47/12

    CPC分类号： A61K31/565 ,  A61K31/21 ,  A61K47/10 ,  A61K47/12 ,  A61K9/7023 ,  Y10S514/947

    摘要： Pharmaceutical preparations comprised of a pharmaceutically active ingredient and a carrier which comprises a percutaneous penetration enhancer comprised of 2-ethyl-1, 3-hexanediol alone or in combination with oleic acid is disclosed. The 2-ethyl-1, 3-hexanediol may be present in an amount in the range of about 50% to 100% based on the weight of the carrier. The oleic acid may be used in combination with 2-ethyl-1, 3-hexanediol in an amount of about 1 to 40% based on the weight of the carrier to provide a synergistic effect with respect to percutaneous penetration enhancement. The compound 2-ethyl-1, 3-hexanediol as used alone and/or in combination with the oleic acid has been found to significantly enhance the delivery of a drug, to a patient, from a transdermal delivery system.

    摘要翻译： 公开了包含药物活性成分和载体的药物制剂，其包含单独或与油酸组合的由2-乙基-1,3-己二醇组成的经皮穿透增强剂。 基于载体的重量，2-乙基-1,3-己二醇的存在量可以在约50％至100％的范围内。 油酸可以与2-乙基-1,3-己二醇组合使用，其量为载体重量的约1至40％，以提供经皮渗透增强方面的协同效应。 已经发现单独使用和/或与油酸组合使用的化合物2-乙基-1,3-己二醇显着增强了从透皮递送系统向患者递送药物。

    Enhancement of activity and/or duration of action of selected anti-inflammatory steroids for topical or other local application
    6.
    发明申请
    Enhancement of activity and/or duration of action of selected anti-inflammatory steroids for topical or other local application 有权
    增强选择的抗炎类固醇的局部或其他局部应用的活性和/或作用持续时间

    公开(公告)号：US20050020551A1

    公开(公告)日：2005-01-27

    申请号：US10868955

    申请日：2004-06-17

    申请人： Nicholas Bodor

    发明人： Nicholas Bodor

    IPC分类号： A61K31/565 ,  A61K31/573 ,  A61K45/06 ,  A61P29/00 ,  A61K31/56

    CPC分类号： A61K31/565 ,  A61K31/573 ,  A61K45/06 ,  Y10S514/944 ,  Y10S514/945 ,  Y10S514/951 ,  Y10S514/96 ,  Y10S514/966 ,  A61K2300/00

    摘要： Methods and compositions for enhancing the activity and/or duration of action of soft anti-inflammatory steroids of the haloalkyl 17α-alkoxy-11β-hydroxyandrost-4-en-3-one-17β-carboxylate type and the corresponding Δ1,4 compounds and of anti-inflammatory steroids of the hydrocortisone and prednisolone type are described. The enhancing agents have the formula: wherein R is H or C1-C4 alkyl; Z1 is carbonyl or β-hydroxymethylene; X1 is —O— or —S—; R5 is —OH, —OR6, —OCOOR6 or —OCOR7 wherein R6 is C1-C4 alkyl and R7 is C1-C4 alkyl, fluoromethyl or chloromethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated; with the proviso that when R is C1-C4 alkyl, then R5 is —OH.

    摘要翻译： 用于增强卤代烷基17α-烷氧基-11β-羟基雄甾-4-烯-3-酮-17β-羧酸盐类型的软性抗炎类固醇的活性和/或作用持续时间的方法和组合物以及相应的Δ1.4 >化合物和氢化可的松和泼尼松龙类型的抗炎类固醇。 增效剂具有下式：其中R是H或C 1 -C 4烷基; Z1是羰基或β-羟基亚甲基; X1为-O-或-S-; R5是-OH，-OR6，-OCOOR6或-OCOR7，其中R6是C1-C4烷基，R7是C1-C4烷基，氟甲基或氯甲基; 环A中的虚线表示1,2-键饱和或不饱和; 条件是当R是C 1 -C 4烷基时，则R 5是-OH。

    Sulfur-substituted phenylacetamides
    7.
    发明授权
    Sulfur-substituted phenylacetamides 失效
    硫取代苯乙酰胺

    公开(公告)号：US4859707A

    公开(公告)日：1989-08-22

    申请号：US525634

    申请日：1983-08-23

    申请人： Thorsteinn Loftsson ,  Nicholas Bodor

    发明人： Thorsteinn Loftsson ,  Nicholas Bodor

    IPC分类号： C07C317/44 ,  C07C323/60

    CPC分类号： C07C323/60 ,  C07C317/44 ,  Y10S514/821

    摘要： This invention relates to sulfur-substituted phenylacetamides of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 may be the same or different and are H or CH.sub.3 ; R.sub.4 is SR.sub.5, ##STR2## R.sub.5 and R.sub.6 may be the same or different and are lower alkyl containing 1-4 carbon atoms and R.sub.5 and R.sub.6 may be taken together with S to form a 5-7 member ring; and X.sup.- is a pharmaceutically acceptable anion, which exhibit arrhythmia activity.

    摘要翻译： 本发明涉及下式的硫代苯基乙酰胺：其中R 1，R 2和R 3可以相同或不同，为H或CH 3; R 4是SR 5，R 5和R 6可以相同或不同，是含有1-4个碳原子的低级烷基，R 5和R 6可与S一起形成5-7元环; X-是药学上可接受的阴离子，其表现出心律失常活性。

    Glycosides and Salts Thereof
    8.
    发明申请
    Glycosides and Salts Thereof 审中-公开
    糖苷及其盐

    公开(公告)号：US20080249165A1

    公开(公告)日：2008-10-09

    申请号：US11659453

    申请日：2005-08-05

    申请人： Janos Kuszmann ,  Istvan Kurucz ,  Gabor Medgyes ,  Nicholas Bodor

    发明人： Janos Kuszmann ,  Istvan Kurucz ,  Gabor Medgyes ,  Nicholas Bodor

    IPC分类号： A61K31/351 ,  C07D407/12 ,  A61P11/00 ,  C07D407/14

    CPC分类号： C07H3/10 ,  A61K9/0073

    摘要： The invention relates to new polysulfated glycosides of formula (I), the salts thereof formed with alkali metals or alkaline-earth metals, as well as the pharmaceutical compositions containing these compounds as active ingredients. Furthermore the invention provides a method of preventing, treating or alleviating the symptoms of acute and chronic inflammatory disorders of the airways of mammals—including asthma and asthma-related pathologies.

    摘要翻译： 本发明涉及式（I）的新型多硫酸糖苷，其与碱金属或碱土金属形成的盐以及含有这些化合物作为活性成分的药物组合物。 此外，本发明提供了预防，治疗或缓解哺乳动物气道（包括哮喘和哮喘相关病症）的急性和慢性炎症性疾病症状的方法。

    Transporter enhanced corticosteroid activity
    9.
    发明申请
    Transporter enhanced corticosteroid activity 有权
    转运蛋白增强皮质类固醇活性

    公开(公告)号：US20080004246A1

    公开(公告)日：2008-01-03

    申请号：US11802403

    申请日：2007-05-22

    申请人： Nicholas Bodor

    发明人： Nicholas Bodor

    IPC分类号： A61K31/573 ,  A61P27/02 ,  A61P29/00

    CPC分类号： C07J5/0053 ,  A61K31/568 ,  C07J3/005 ,  A61K2300/00

    摘要： Methods and compositions for enhancing the activity and/or duration of action of loteprednol etabonate and other soft anti-inflammatory steroids of the haloalkyl 17α-alkoxycarbonyloxy-11β-hydroxyandrost-4-en-3-one-17β-carboxylate type and the corresponding Δ1,4-compounds are described. The enhancing agents have the formula: wherein Z1 is carbonyl, β-hydroxymethylene or methylene; R2 is H, —OH or —OCOR3 wherein R3 is C1-C5 alkyl; Y is —OH, —SH or —OCOR4 wherein R4 is C1-C5 alkyl, cyclopentylethyl or diethylaminoethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated.

    摘要翻译： 卤代烷基17α-烷氧基羰基氧基-11β-羟基雄甾-4-烯-3-酮-17β-羧酸酯类型的对苯二甲酸乙二醇酯和其它软性抗炎类固醇的活性和/或作用持续时间的方法和组合物， 描述了化合物。 增强剂具有下式：其中Z 1是羰基，β-羟基亚甲基或亚甲基; R 2是H，-OH或-OCOR 3，其中R 3是C 1 -C 3 - 5 烷基; Y是-OH，-SH或-OCOR 4，其中R 4是C 1 -C 5烷基， 环戊基乙基或二乙基氨基乙基; 环A中的虚线表示1,2-键饱和或不饱和。