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    • 7. 发明申请
    • Diuretic aerosols and methods of making and using them
    • 利尿剂及其使用方法
    • US20040105818A1
    • 2004-06-03
    • US10712365
    • 2003-11-12
    • Alexza Molecular Delivery Corporation
    • Nathan R. EveryRon L. HaleAmy T. LuJoshua D. Rabinowitz
    • A61L009/04A61K031/58
    • A61K9/0073A61K9/007A61K31/58
    • Described herein are diuretic condensation aerosols and methods of making and using them. Kits for delivering a condensation aerosol are also described. The diuretic aerosols typically comprise diuretic condensation aerosol particles that comprise a diuretic compound. In some variations the diuretic compound is selected from the group consisting of bumetanide, ethacrynic acid, furosemide, muzolimine, spironolactone, torsemide, triamterene, tripamide, BG 9928, and BG 9719. Methods of treating edema using the described aerosols are also provided. In general, the methods typically comprise the step of administering a therapeutically effective amount of diuretic condensation aerosol to a person with edema. The diuretic condensation aerosol may be administered in a single inhalation, or may be administered in more than one inhalation. Methods of forming a diuretic condensation aerosol are also described. The methods typically comprise the steps of providing a diuretic composition, vaporizing the composition to form a vapor, and then condensing the diuretic composition vapor.
    • 本文描述的是利尿凝结气溶胶及其制备和使用方法。 还描述了用于递送冷凝气雾剂的组件。 利尿剂气溶胶通常包含利尿剂缩合气溶胶颗粒,其包含利尿剂。 在一些变体中,利尿剂化合物选自布美他尼,依西醋酸,呋塞米,多佐立胺,螺内酯,托塞米明,扑热息痛,三酰胺,BG 9928和BG 9719.还提供了使用所述气溶胶治疗水肿的方法。 通常,所述方法通常包括向具有水肿的人施用治疗有效量的利尿冷凝气雾剂的步骤。 利尿冷凝气雾剂可以在单次吸入中施用,或者可以在多于一次的吸入中施用。 还描述了形成利尿冷凝气雾剂的方法。 所述方法通常包括提供利尿组合物,蒸发组合物以形成蒸气,然后冷凝利尿组合物蒸气的步骤。
    • 8. 发明申请
    • 16,17-carbocyclic condensed steroid compounds having selective estrogenic activity
    • 具有选择性雌激素活性的16,17-碳环缩合类固醇化合物
    • US20040102426A1
    • 2004-05-27
    • US10297706
    • 2002-12-06
    • Hubert Jan Jozef Loozen
    • A61K031/58A61K031/56C07J053/00
    • C07J53/002
    • The invention discloses a steroid compound having the formula (1), wherein dotted bonds represent optional double bonds; R6 is H, nullCH2, or nullCH3, or nullCH2nullCH3; R7 is H C1-4-alkyl, C2-5 alkenyl or C2-5-alkynyl, wherein the alkyl, alkenyl or alkynyl group may be substituted with 1 to 3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; R11 is H, C1-4-alkyl, C2-4-alkenyl, C2-4-alkynyl or C1-4-alkylidene, wherein the alkyl, alkenyl, alkynyl or alkylidene group may be substituted with 1 to 3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; E represents together with carbon atoms 16 and 17 of the steroid skeleton a four to seven-membered ring, said ring being null and in cis-configuration with respect to the steroid skeleton, optionally comprising one or two endocyclic bonds; or a prodrug thereof. Such compounds can be used in therapy and for methods for selective modification of the activity of estrogen receptors. 1
    • 本发明公开了具有式(1)的类固醇化合物,其中虚线键代表任选的双键; R 6是H,= CH 2或-CH 3或-CH 2 -CH 3; R 7是C 1-4 - 烷基,C 2-5烯基或C 2-5炔基,其中烷基,烯基或炔基可以被独立地选自氟或氯原子的1至3个卤素原子取代; R 11是H,C 1-4 - 烷基,C 2-4 - 烯基,C 2-4 - 炔基或C 1-4 - 亚烷基,其中烷基,烯基,炔基或亚烷基可以被1至3个独立地选自 该组氟或氯原子; E与类固醇骨架的碳原子16和17一起形成4至7元环,所述环为α并且相对于类固醇骨架为顺式构型,任选包含一个或两个内环键; 或其前药。 这些化合物可用于治疗和选择性修饰雌激素受体活性的方法。