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1.发明授权Proline ester and preparation containing the same for percutaneous administration 失效脯氨酸酯和含有相同用于经皮给药的制剂公开(公告)号：US07323489B2
公开(公告)日：2008-01-29
申请号：US10527062
申请日：2003-09-08
IPC分类号： A61K31/40 , C07D207/00
CPC分类号： A61K9/7053 , A61K9/0014 , A61K9/7076 , A61K38/00 , C07K5/0222 , C07K5/06026
摘要： A proline ester represented by the following formula (I): wherein R1 represents a hydroxy-lower alkyl group, a lower alkoxy-lower alkyl group, or a lower alkoxy-lower alkoxy-lower alkyl group or a pharmaceutically acceptable salt thereof. The proline ester (I) of the present invention and a pharmaceutically acceptable salt thereof are useful as a prodrug of enalaprilat, which is a medicine useful for preventing or treating circulatory diseases such as hypertension, cardiac diseases (e.g., cardiac hypertrophy, cardiac failure, and myocardial infarct), nephritis, and apoplexy. Thus, a drug containing the ester or a salt thereof is preferably formulated to a percutaneous preparation, particularly a patch, from the viewpoint of medicinal activity and use.
摘要翻译： 由下式（I）表示的脯氨酸酯：其中R 1表示羟基 - 低级烷基，低级烷氧基 - 低级烷基或低级烷氧基 - 低级烷氧基 - 低级烷基，或 其药学上可接受的盐。 本发明的脯氨酸酯（I）及其药学上可接受的盐可用作依那普利的前药，它是可用于预防或治疗诸如高血压，心脏疾病（例如心脏肥大，心脏衰竭， 和心肌梗塞），肾炎和中风。 因此，从药物活性和用途的观点出发，优选将含有酯或其盐的药剂配制成经皮制剂，特别是贴剂。
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2.发明申请Proline ester and preparation containing the same for percutaneous administration 失效脯氨酸酯和含有相同用于经皮给药的制剂公开(公告)号：US20050288232A1
公开(公告)日：2005-12-29
申请号：US10527062
申请日：2003-09-08
申请人： Takayuki Furuishi , Kunihiro Minami
发明人： Takayuki Furuishi , Kunihiro Minami
IPC分类号： A61K9/00 , A61K9/70 , A61K38/00 , A61P9/04 , A61P9/12 , A61P43/00 , C07K5/02 , C07K5/062 , A61K38/04 , C07K5/04
CPC分类号： A61K9/7053 , A61K9/0014 , A61K9/7076 , A61K38/00 , C07K5/0222 , C07K5/06026
摘要： A proline ester represented by the following formula (I): wherein R1 represents a hydroxy-lower alkyl group, a lower alkoxy-lower alkyl group, or a lower alkoxy-lower alkoxy-lower alkyl group or a pharmaceutically acceptable salt thereof. The proline ester (I) of the present invention and a pharmaceutically acceptable salt thereof are useful as a prodrug of enalaprilat, which is a medicine useful for preventing or treating circulatory diseases such as hypertension, cardiac diseases (e.g., cardiac hypertrophy, cardiac failure, and myocardial infarct), nephritis, and apoplexy. Thus, a drug containing the ester or a salt thereof is preferably formulated to a percutaneous preparation, particularly a patch, from the viewpoint of medicinal activity and use.
摘要翻译： 由下式（I）表示的脯氨酸酯：其中R 1表示羟基 - 低级烷基，低级烷氧基 - 低级烷基或低级烷氧基 - 低级烷氧基 - 低级烷基，或 其药学上可接受的盐。 本发明的脯氨酸酯（I）及其药学上可接受的盐可用作依那普利的前药，它是可用于预防或治疗诸如高血压，心脏疾病（例如心脏肥大，心脏衰竭， 和心肌梗塞），肾炎和中风。 因此，从药物活性和用途的观点出发，优选将含有酯或其盐的药剂配制成经皮制剂，特别是贴剂。
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公开(公告)号：US20120264742A1
公开(公告)日：2012-10-18
申请号：US13509391
申请日：2010-11-11
IPC分类号： A61K47/14 , A61K31/135 , A61K31/439 , A61P25/04 , A61K47/34 , A61K47/30 , A61K47/36 , A61K31/55 , A61K47/32
CPC分类号： A61K9/0014 , A61K9/06 , A61K9/7038 , A61K9/7061 , A61K9/7084 , A61K31/135 , A61K31/439 , A61K31/485 , A61K31/55 , A61K47/14
摘要： A pharmaceutical composition for external use which is an organogel containing a fatty acid ester and a glycerolglycerin fatty acid ester, in particular, a novel transdermally absorbable pharmaceutical composition for external use which has a drug such as non-narcotic analgesics as an active ingredient made in organogel form containing a drug such as non-narcotic analgesics as an active ingredient, a fatty acid ester and a glycerolglycerin fatty acid ester, and a method for producing the composition. The pharmaceutical composition significantly improves skin permeability of drugs such as non-narcotic analgesics and allows a sufficient amount of drug to permeate the skin sustainably. Moreover, since the pharmaceutical composition is in organogel form, it can be easily applied to a preparation in practice. In addition, the pharmaceutical composition can provide efficient use and the like of drugs due to a high drug release rate and therefore is highly useful.
摘要翻译： 一种外用药物组合物，其是含有脂肪酸酯和甘油甘油脂肪酸酯的有机凝胶，特别是一种新颖的经皮吸收的外用药物组合物，其具有药物如非麻醉止痛剂作为活性成分 含有作为活性成分的非麻醉性镇痛药等的药物的有机凝胶形式，脂肪酸酯和甘油甘油脂肪酸酯等的制造方法。 药物组合物显着地改善药物如非麻醉止痛剂的皮肤渗透性，并允许足够量的药物可持续地渗透皮肤。 此外，由于药物组合物为有机凝胶形式，因此可以容易地应用于实践中的制剂。 此外，药物组合物由于药物释放率高而能够提供有效的药物使用等，因此是非常有用的。
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公开(公告)号：US09050247B2
公开(公告)日：2015-06-09
申请号：US13509391
申请日：2010-11-11
IPC分类号： A61K47/14 , A61K31/135 , A61P25/04 , A61K9/00 , A61K31/439 , A61K31/485 , A61K31/55 , A61K9/06 , A61K9/70
CPC分类号： A61K9/0014 , A61K9/06 , A61K9/7038 , A61K9/7061 , A61K9/7084 , A61K31/135 , A61K31/439 , A61K31/485 , A61K31/55 , A61K47/14
摘要： A pharmaceutical composition for external use which is an organogel containing a fatty acid ester and a glycerolglycerin fatty acid ester, in particular, a novel transdermally absorbabedle pharmaceutical composition for external use which has a drug such as non-narcotic analgesics as an active ingredient made in organogel form containing a drug such as non-narcotic analgesics as an active ingredient, a fatty acid ester and a glycerolglycerin fatty acid ester, and a method for producing the composition. The pharmaceutical composition significantly improves skin permeability of drugs such as non-narcotic analgesics and allows a sufficient amount of drug to permeate the skin sustainably. Moreover, since the pharmaceutical composition is in organogel form, it can be easily applied to a preparation in practice. In addition, the pharmaceutical composition can provide efficient use and the like of drugs due to a high drug release rate and therefore is highly useful.
摘要翻译： 一种外用药物组合物，其是含有脂肪酸酯和甘油甘油脂肪酸酯的有机凝胶，特别是一种外用的新型经皮吸收材料药物组合物，其具有药物如非麻醉止痛剂作为活性成分 含有作为活性成分的非麻醉性镇痛药等的药物的有机凝胶形式，脂肪酸酯和甘油甘油脂肪酸酯等的制造方法。 药物组合物显着地改善药物如非麻醉止痛剂的皮肤渗透性，并允许足够量的药物可持续地渗透皮肤。 此外，由于药物组合物为有机凝胶形式，因此可以容易地应用于实践中的制剂。 此外，药物组合物由于药物释放率高而能够提供有效的药物使用等，因此是非常有用的。
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