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    • 7. 发明申请
    • ANTIFUNGAL COMPOUND AND USES THEREOF
    • 抗真菌化合物及其用途
    • WO2014086285A1
    • 2014-06-12
    • PCT/CN2013/088483
    • 2013-12-04
    • THE UNIVERSITY OF HONG KONG
    • SENEVIRATNE, Chaminda JayampathKAO, Yi Tsun RichardSAMARANAYAKE, Lakshman PereraYUEN, Kwok YungYANG, DanWANG, YuWONG, Sze Wah, Sarah
    • C07D309/34A61K31/351A61P31/10A61P31/18
    • A61K31/351A01N43/40A01N59/00A61K9/0019A61K9/08A01N25/34
    • Disclosed herein is a novel antifungal compound, derivatives that are used b treat fungal infections. In a specific embodiment, the compound is a small molecule. In a specific embodiment, the compound described herein inhibits yeast to hypha transition under robust hyphal inducing conditions at lower concentration of the molecule. Also disclosed is a composition comprising the antifungal compound. In a specific embodiment, the composition is a pharmaceutical composition Also disclosed is a method of treating and/or preventing fungal infection using the disclosed compound. The disclosed compound exhibits antifungal activity against wide range of fungal species at slightly higher concentrations. Antifungal compound disclose d herein is use d as anti-biofilm agent against fungal infections. In a specific embodiment, the disclosed compound is effective for systemic fungal infections. In a certain embodiment, the disclosed compound is a broad-spectrum antifungal agent for treating topical local and/or systemic fungal infections. In a specific embodiment, the disclosed compound is used in the prevention or treatment of mycotic infections caused by various fungal pathogens.
    • 本文公开了一种新型抗真菌化合物,其用于治疗真菌感染的衍生物。 在一个具体实施方案中,化合物是小分子。 在一个具体的实施方案中,本文所述的化合物在分子浓度较低的条件下,在稳定的菌丝诱导条件下抑制酵母进行菌丝体转化。 还公开了包含抗真菌化合物的组合物。 在具体实施方案中,组合物是药物组合物。还公开了使用所公开的化合物治疗和/或预防真菌感染的方法。 所公开的化合物在稍高的浓度下对广泛的真菌种类显示出抗真菌活性。 本文中公开的抗真菌化合物d是使用d作为抗真菌感染的抗生物膜剂。 在一个具体实施方案中,所公开的化合物对全身真菌感染是有效的。 在某个实施方案中,所公开的化合物是用于治疗局部局部和/或系统性真菌感染的广谱抗真菌剂。 在具体实施方案中,所公开的化合物用于预防或治疗由各种真菌病原体引起的霉菌感染。
    • 8. 发明申请
    • METHOD FOR SYNTHESIZING 5ß, 6ß-EPOXIDES OF STEROIDS BY A HIGHLY ß-SELECTIVE EPOXIDATION OF Δ5-UNSATURATED STEROIDS CATALYZED BY KETONES
    • 通过KETONES催化的DELTA5-不饱和的STEROIDS的高选择性环氧化合成Steroids的5β,6-环氧化物的方法
    • WO2003074545A1
    • 2003-09-12
    • PCT/CN2003/000140
    • 2003-02-24
    • THE UNIVERSITY OF HONG KONG
    • YANG, DanJIAO, Guansheng
    • C07J21/00
    • C07J71/00
    • A general, efficient, and environmentally friendly method is provided for producing mostly ß-epoxides of Δ 5 -unsaturated steroids using certain ketones as the catalyst along with an oxidizing agent, or by using certain dioxiranes. In another aspect of the invention, a method is provided for producing mostly 5ß, 6ß-epoxides of steroids from Δ 5 -unsaturated steroids having a substituent at the 3α-position by an epoxidation reaction using a ketone along with an oxidizing agent under conditions effective to generate epoxides, or using a dioxirane under conditions effective to generate epoxides. A whole range of Δ 5 -unsaturated steroids, bearing different functional groups such as hydroxy, carbonyl, acetyl of ketal group as well as different side chains, were conveniently converted to the corresponding synthetically and biologically interesting 5ß, 6ß-epoxides with excellent ß-selectivities and high yields.
    • 提供一般的,有效的和环境友好的方法来生产大部分DELTA5-不饱和类固醇的β-环​​氧化物,其中使用某些酮作为催化剂以及氧化剂,或通过使用某些二恶烷。 在本发明的另一方面,提供了一种用于通过环氧化反应使用酮与氧化剂在3α-位上具有取代基的DELTA5-不饱和类固醇生成大部分5β,6β-环氧化物的方法, 产生环氧化物,或在有效产生环氧化物的条件下使用二氧杂环烷。 具有不同官能团(如羟基,羰基,缩酮乙酰基以及不同侧链)的全部范围的DELTA5-不饱和类固醇可方便地转化为具有优异ß选择性的相应的合成和生物学上有趣的5β,6β-环氧化物 产量高。