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1. 发明申请

US20120197016A1 SCREENING METHODS OF MODULATING ADRENERGIC RECEPTOR GENE EXPRESSIONS IMPLICATED IN MELANOGENESIS 审中-公开
标题翻译：调控嗜酸性粒细胞趋化因子基因表达的筛选方法
公开(公告)号：US20120197016A1
公开(公告)日：2012-08-02
申请号：US13278465
申请日：2011-10-21
申请人： Leo Timothy Laughlin, II , Tomohiro Hakozaki , Wenzhu Zhao , Jiazhen Wang , John Crist Bierman
发明人： Leo Timothy Laughlin, II , Tomohiro Hakozaki , Wenzhu Zhao , Jiazhen Wang , John Crist Bierman
IPC分类号： C12Q1/02 , C07C257/18 , C07C233/51 , C07D471/10 , C07D405/14 , C07D209/88 , C07D459/00 , G01N21/64 , C07C229/52
CPC分类号： G01N33/566 , G01N2500/10
摘要： Embodiments of screening methods for determining test agents effective for modifying the appearance of pigmented skin are provided. The screening method may comprise the steps of contacting a cell, a cell culture, or bulk cells with the test agent, wherein the cell, the cell culture, or the bulk cells comprise ADRβ1 receptors, and determining based on the binding interaction of the test agent with the ADRβ1 receptors whether the test agent is an effective ADRβ1 receptor antagonist suitable for modifying the appearance of pigmented skin, wherein a test agent is considered to be an effective ADRβ1 receptor antagonist when it defines a half maximal inhibitory concentration of less than about 1000 ppm.
摘要翻译：提供了用于确定有效改善着色皮肤外观的试验剂的筛选方法的实施方案。筛选方法可以包括使细胞，细胞培养物或体细胞与测试试剂接触的步骤，其中细胞，细胞培养物或体细胞包含ADR和bgr1受体，并且基于具有ADR＆bgr.1受体的测试剂是否是测试剂是适合于改变着色皮肤外观的有效ADR＆bgr1受体拮抗剂，其中测试剂被认为是有效ADR＆bgr1受体拮抗剂，当它定义一半最大抑制浓度小于约1000ppm。

2. 发明授权

US10267796B2 Screening methods of modulating adrenergic receptor gene expressions implicated in melanogenesis 有权
公开(公告)号：US10267796B2
公开(公告)日：2019-04-23
申请号：US13278465
申请日：2011-10-21
申请人： Leo Timothy Laughlin, II , Tomohiro Hakozaki , Wenzhu Zhao , Jiazhen Wang , John Crist Bierman
发明人： Leo Timothy Laughlin, II , Tomohiro Hakozaki , Wenzhu Zhao , Jiazhen Wang , John Crist Bierman
IPC分类号： C12Q1/02 , C07C257/18 , C07C233/51 , C07D471/10 , C07D405/14 , C07D209/88 , C07D459/00 , G01N21/64 , C07C229/52 , G01N33/566
摘要： Embodiments of screening methods for determining test agents effective for modifying the appearance of pigmented skin are provided. The screening method may comprise the steps of contacting a cell, a cell culture, or bulk cells with the test agent, wherein the cell, the cell culture, or the bulk cells comprise ADRβ1 receptors, and determining based on the binding interaction of the test agent with the ADRβ1 receptors whether the test agent is an effective ADRβ1 receptor antagonist suitable for modifying the appearance of pigmented skin, wherein a test agent is considered to be an effective ADRβ1 receptor antagonist when it defines a half maximal inhibitory concentration of less than about 1000 ppm.

3. 发明授权

US08921346B2 Preparation method of drospirenone 有权
标题翻译：屈螺酮的制备方法
公开(公告)号：US08921346B2
公开(公告)日：2014-12-30
申请号：US13579229
申请日：2010-03-16
申请人： Jiazhen Wang
发明人： Jiazhen Wang
IPC分类号： A61K31/34 , C07D307/94 , C07J53/00
CPC分类号： C07J53/008
摘要： The present invention discloses the preparation method of drospirenone. 3β,5-dyhydroxy-6β,7β,15β, 16β-dimethylene- 5β-androstane-17,20-epoxy is taken as the raw material. It is subject to oxidization of the hydroxyl at the 3rd position, ketalization of 3-ketone group, condensation reaction and deesterification to obtain carboxylic acid lactone, sulfonation of the hydroxyl at the 5th position, and deketalization and desulphonation in the reaction system of glacial acetic acid and sodium acetate to produce the 3-keto-4-alkenyl compound, thus obtaining drospirenone. The preparation method of the invention has high intensification, reaction specificity, less by-products and high yield of products in each step, thus overcoming the disadvantages of low yield and unstable quality.
摘要翻译：本发明公开了屈螺酮的制备方法。 3＆bgr; 5-dyhydroxy-6＆bgr; 7＆bgr; 15＆bgr; 16＆bgr-二亚甲基-5＆bgr-雄甾烷-17,20-环氧树脂作为原料。第3位羟基氧化，3-酮基缩酮化，缩合反应脱酯，得到羧酸内酯，第5位羟基磺化，冰醋酸反应体系中的脱酮和脱磺酸酸和乙酸钠，得到3-酮-4-烯基化合物，得到屈螺酮。本发明的制备方法在每个步骤中具有高强化，反应特异性，副产物少，成品率高，克服了低产量和质量不稳定的缺点。

4. 发明申请

US20120316333A1 PREPARATION METHOD OF DROSPIRENONE 有权
标题翻译：氟哌酮的制备方法
公开(公告)号：US20120316333A1
公开(公告)日：2012-12-13
申请号：US13579229
申请日：2010-03-16
申请人： Jiazhen Wang
发明人： Jiazhen Wang
IPC分类号： C07J75/00
CPC分类号： C07J53/008
摘要： The present invention discloses the preparation method of drospirenone. 3β,5-dyhydroxy-6β,7β,15β,16β-dimethylene-5β-androstane-17,20-epoxy is taken as the raw material. It is subject to oxidization of the hydroxyl at the 3rd position, ketalization of 3-ketone group, condensation reaction and deesterification to obtain carboxylic acid lactone, sulfonation of the hydroxyl at the 5th position, and deketalization and desulphonation in the reaction system of glacial acetic acid and sodium acetate to produce the 3-keto-4-alkenyl compound, thus obtaining drospirenone. The preparation method of the invention has high intensification, reaction specificity, less by-products and high yield of products in each step, thus overcoming the disadvantages of low yield and unstable quality.
摘要翻译：本发明公开了屈螺酮的制备方法。 3＆bgr; 5-dyhydroxy-6＆bgr; 7＆bgr; 15＆bgr; 16＆bgr。 - 亚甲基-5＆bgr-雄甾烷-17,20-环氧树脂作为原料。第3位羟基氧化，3-酮基缩酮化，缩合反应脱酯，得到羧酸内酯，第5位羟基磺化，冰醋酸反应体系中的脱酮和脱磺酸酸和乙酸钠，得到3-酮-4-烯基化合物，得到屈螺酮。本发明的制备方法在每个步骤中具有高强化，反应特异性，副产物少，成品率高，克服了低产量和质量不稳定的缺点。

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