公开(公告)号：US09493502B2

公开(公告)日：2016-11-15

申请号：US13981694

申请日：2012-01-20

申请人： Hongguang Du ,  Guocheng Liu ,  Zhongren Ding ,  Shuming Wang

发明人： Hongguang Du ,  Guocheng Liu ,  Zhongren Ding ,  Shuming Wang

IPC分类号： C07H19/167 ,  A61K31/7076 ,  C07H19/16

CPC分类号： C07H19/16 ,  A61K31/7076 ,  C07H19/167

摘要： The present invention relates to the compounds of the formulae (I) and (I-1) and the process for preparing the same, uses of the compounds for the treatment of diseases associated with platelet aggregation and in the manufacture of a medicament for the treatment of diseases associated with platelet aggregation, and relates to a pharmaceutical composition and a pharmaceutical formulation containing the compounds, wherein the definitions of R1, R2, R3 and R2a in the formulae are the same as those in the description.

公开(公告)号：US09265752B2

公开(公告)日：2016-02-23

申请号：US12667915

申请日：2008-07-03

申请人： Shuming Wang ,  Huiyong Xue ,  Li Wang ,  Enhong Zhang ,  Hongjun Lian ,  Xiaoyan Shi ,  Guohua Chi ,  Yucheng Lu ,  Xiquan Liu ,  Li Song ,  Xuying Zhong ,  Hongguang Du

发明人： Shuming Wang ,  Huiyong Xue ,  Li Wang ,  Enhong Zhang ,  Hongjun Lian ,  Xiaoyan Shi ,  Guohua Chi ,  Yucheng Lu ,  Xiquan Liu ,  Li Song ,  Xuying Zhong ,  Hongguang Du

IPC分类号： A61K9/70 ,  A61K31/381 ,  A61P25/16

CPC分类号： A61K9/7023 ,  A61K9/7053 ,  A61K9/7061 ,  A61K9/7069 ,  A61K31/381

摘要： A Rotigotine-containing composition having a matrix mixture system formed from a polyvinylpyrrolidone and a combination of an acrylic pressure-sensitive adhesive with a silicone pressure-sensitive adhesive. The polyvinylpyrrolidone may be present in an amount of about 1-10% by weight in matrix mixture system. The acrylic pressure-sensitive adhesive may be present in an amount of about 1-25% by weight in the matrix mixture system. The silicone pressure-sensitive adhesive may be present in an amount of about 65-98% by weight in the matrix mixture system. The composition further includes 1-40% of Rotigotine on the basis of the total weight of the composition. The composition provides improved properties in the solubility, release and initial penetration level of Rotigotine. Also disclosed is a transdermal patch that includes the Rotigotine-containing composition, as well as methods of manufacturing and using the Rotigotine-containing composition.

摘要翻译： 一种含有罗替那定的组合物，其具有由聚乙烯吡咯烷酮形成的基质混合物体系和丙烯酸类压敏粘合剂与硅氧烷压敏粘合剂的组合。 聚乙烯吡咯烷酮的存在量可以在基质混合体系中约1-10％（重量）。 丙烯酸类压敏粘合剂可以在基质混合物体系中以约1-25重量％的量存在。 在基质混合物体系中，硅氧烷压敏粘合剂可以以约65-98重量％的量存在。 该组合物还包括基于组合物总重量的1-40％的罗替戈汀。 该组合物提供了罗替戈汀的溶解度，释放和初始渗透水平的改善的性质。 还公开了包括含有罗替多汀的组合物的透皮贴剂，以及制造和使用含有罗替尼汀的组合物的方法。

公开(公告)号：US20140005138A1

公开(公告)日：2014-01-02

申请号：US13981694

申请日：2012-01-20

申请人： Hongguang Du ,  Guocheng Liu ,  Zhongren Ding ,  Shuming Wang

发明人： Hongguang Du ,  Guocheng Liu ,  Zhongren Ding ,  Shuming Wang

IPC分类号： C07H19/16

CPC分类号： C07H19/16 ,  A61K31/7076 ,  C07H19/167

摘要： The present invention relates to the compounds of the formulae (I) and (I-1) and the process for preparing the same, uses of the compounds for the treatment of diseases associated with platelet aggregation and in the manufacture of a medicament for the treatment of diseases associated with platelet aggregation, and relates to a pharmaceutical composition and a pharmaceutical formulation containing the compounds, wherein the definitions of R1, R2, R3 and R2a in the formulae are the same as those in the description.

摘要翻译： 本发明涉及式（I）和（I-1）的化合物及其制备方法，该化合物用于治疗与血小板聚集有关的疾病的用途以及制备用于治疗的药物 涉及与血小板聚集有关的疾病，涉及含有该化合物的药物组合物和药物制剂，其中式中R1，R2，R3和R2a的定义与说明书中相同。

公开(公告)号：US20110027345A1

公开(公告)日：2011-02-03

申请号：US12667915

申请日：2008-07-03

申请人： Shuming Wang ,  Huiyong Xue ,  Li Wang ,  Enhong Zhang ,  Hongjun Lian ,  Xiaoyan Shi ,  Guohua Chi ,  Yucheng Lu ,  Xiquan Liu ,  Li Song ,  Xuying Zhong ,  Hongguang Du

发明人： Shuming Wang ,  Huiyong Xue ,  Li Wang ,  Enhong Zhang ,  Hongjun Lian ,  Xiaoyan Shi ,  Guohua Chi ,  Yucheng Lu ,  Xiquan Liu ,  Li Song ,  Xuying Zhong ,  Hongguang Du

IPC分类号： A61K31/381 ,  A61K9/00 ,  A61K9/70 ,  A61P25/16

CPC分类号： A61K9/7023 ,  A61K9/7053 ,  A61K9/7061 ,  A61K9/7069 ,  A61K31/381

摘要： The present invention relates to a composition containing Rotigotine and the use thereof in the manufacture of a Rotigotine-containing transdermal patch, wherein said composition is based on a matrix mixture system formed from a combination of an acrylic pressure-sensitive adhesive with a silicone pressure-sensitive adhesive, and polyvinylpyrrolidone which are present in a particular weight ratio, wherein (1) the acrylic pressure-sensitive adhesive is present in an amount of about 1-25% by weight in the matrix mixture system, (2) the silicone pressure-sensitive adhesive is present in an amount of about 65-98% by weight in the matrix mixture system, and (3) the polyvinylpyrrolidone is present in an amount of about 1-10% by weight in the matrix mixture system, and comprises 1-40% of Rotigotine on the basis of the total weight of the composition. The present invention further relates to an improved transdermal patch containing Rotigotine comprising said composition. Said patch has improved properties in the solubility, release and initial penetration level of Rotigotine.

摘要翻译： 本发明涉及含有罗替高汀的组合物及其在制造含罗替尼汀的透皮贴剂中的用途，其中所述组合物是基于由丙烯酸压敏粘合剂与硅氧烷压敏粘合剂组合形成的基质混合物体系， 敏感性粘合剂和聚乙烯吡咯烷酮，其特征在于：（1）所述丙烯酸类压敏粘合剂在所述基质混合物体系中以约1-25％（重量）的量存在，（2） 在基质混合体系中，敏感粘合剂的存在量为约65-98重量％，（3）在基质混合体系中，聚乙烯吡咯烷酮的存在量为约1-10重量％，并且包含1- 基于组合物总重量的罗替高汀为40％。 本发明还涉及包含所述组合物的含有罗替高汀的改良透皮贴剂。 所述贴剂具有改善的罗替戈汀的溶解度，释放和初始渗透水平的性质。