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公开(公告)号：US20120003303A1
公开(公告)日：2012-01-05
申请号：US13143408
申请日：2010-01-08
IPC分类号： A61K31/39 , A61P9/12 , A61K9/14 , C07D327/08 , A61K9/48
CPC分类号： A61K9/5078 , A61K9/2846 , A61K9/5026 , A61K9/5042
摘要： Pharmaceutical presentations of phenoxathiin-based MAO-A inhibitors are disclosed whereby the MAO receptors are protected from binding to active ingredient in the stomach. Particular phenoxathiin-based MAO-A inhibitors include those of the following formula: (I) wherein n is 0, 1 or 2; R1 is a branched or straight chain C1-5 alkyl or C3-6 cycloalkyl optionally substituted with hydroxyl, or one or more halogens; and X1, X2, X3, X4, and X5 are either all hydrogens or one or two of X1, X2, X3, X4, and X5 are halogen and the remainder are hydrogens, with the proviso that when n is 0 or 1 and each X is hydrogen, R1 is not methyl. A wide variety of enteric mechanisms may be utilized so as to provide release of the active ingredient essentially out of the environment of the stomach after ingestion as a pharmaceutical presentation, such as a tablet or capsule. Presentations include enteric coated tablets, enteric coated capsules, capsules containing enteric coated beads.
摘要翻译： 公开了基于吩草素的MAO-A抑制剂的药物显示，由此保护MAO受体免受胃中的活性成分的结合。 特别的基于苯基硫蛋白的MAO-A抑制剂包括下式的那些：（I）其中n为0,1或2; R1是任选被羟基或一个或多个卤素取代的支链或直链C 1-5烷基或C 3-6环烷基; 且X 1，X 2，X 3，X 4和X 5均为氢，或者X 1，X 2，X 3，X 4和X 5中的一个或两个为卤素，其余为氢，条件是当n为0或1时， X是氢，R1不是甲基。 可以使用各种各样的肠溶机制，以便在摄取后作为药物呈递，例如片剂或胶囊，提供活性成分基本上脱离胃外的环境。 介绍包括肠溶包衣片剂，肠溶衣胶囊，含有肠溶包衣珠粒的胶囊。
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公开(公告)号：US20130045253A1
公开(公告)日：2013-02-21
申请号：US13653470
申请日：2012-10-17
申请人： Andrew Chen , Hailiang Chen , James Cecil Free , Majid Keshtmand , Mohammed Abdul Rahman , Sally Look
发明人： Andrew Chen , Hailiang Chen , James Cecil Free , Majid Keshtmand , Mohammed Abdul Rahman , Sally Look
IPC分类号： A61K31/5415 , A61P25/22 , A61P25/24 , A61K9/00 , A61P25/18
CPC分类号： A61K31/39 , A61K9/145 , A61K9/2054 , A61K9/5078
摘要： Provided are methods for reducing the excipient load of pharmaceutical formulations containing 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin 10,10-dioxide as the active pharmaceutical ingredient, and compositions related thereto. In particular, provided is a pharmaceutical product comprising 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin 10,10-dioxide and a stabilizer admixed throughout a solid-form unilamellar matrix, wherein the ratio of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin 10,10-dioxide to stabilizer ranges from about 2:3 to about 1:10, and related methods of forming the pharmaceutical product.
摘要翻译： 提供了减少含有3-氟-7-（2,2,2-三氟乙氧基）苯氧硫蛋白10,10-二氧化物作为活性药物成分的药物制剂的赋形剂负荷的方法，以及与之相关的组合物。 特别地，提供了包含3-氟-7-（2,2,2-三氟乙氧基）苯氧硫蛋白10,10-二氧化物和整个固体形式的单层基质中混合的稳定剂的药物产品，其中3-氟 - 7-（2,2,2-三氟乙氧基）苯氧硫蛋白10,10-二氧化物至稳定剂的范围为约2:3至约1:10，以及形成药物产品的相关方法。
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公开(公告)号：US08313766B2
公开(公告)日：2012-11-20
申请号：US12860358
申请日：2010-08-20
申请人： Andrew Chen , Hailiang Chen , James Cecil Free , Majid Keshtmand , Mohammed Abdul Rahman , Sally A. Look
发明人： Andrew Chen , Hailiang Chen , James Cecil Free , Majid Keshtmand , Mohammed Abdul Rahman , Sally A. Look
IPC分类号： A61K33/16
CPC分类号： A61K31/39 , A61K9/145 , A61K9/2054 , A61K9/5078
摘要： Provided are methods for reducing the excipient load of pharmaceutical formulations containing 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin 10,10-dioxide as the active pharmaceutical ingredient, and compositions related thereto. In particular, provided is a pharmaceutical product comprising 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin 10,10-dioxide and a stabilizer admixed throughout a solid-form unilamellar matrix, wherein the ratio of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin 10,10-dioxide to stabilizer ranges from about 2:3 to about 1:10, and related methods of forming the pharmaceutical product.
摘要翻译： 提供了减少含有3-氟-7-（2,2,2-三氟乙氧基）苯氧硫蛋白10,10-二氧化物作为活性药物成分的药物制剂的赋形剂负荷的方法，以及与之相关的组合物。 特别地，提供了包含3-氟-7-（2,2,2-三氟乙氧基）苯氧硫蛋白10,10-二氧化物和整个固体形式的单层基质中混合的稳定剂的药物产品，其中3-氟 - 7-（2,2,2-三氟乙氧基）苯氧硫蛋白10,10-二氧化物至稳定剂的范围为约2:3至约1:10，以及形成药物产品的相关方法。
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公开(公告)号：US20120003274A1
公开(公告)日：2012-01-05
申请号：US13143403
申请日：2010-01-08
IPC分类号： A61K9/00 , A61K31/39 , A61P25/24 , C07D327/08
CPC分类号： C07D327/08
摘要： Pharmaceutical presentations or phenoxathiin-based MAO-A inhibitors are disclosed whereby the MAO receptors are capable of sustained release in the digestive tract. Particular phenoxathiin-based MAO-A inhibitors include those of the following formula: wherein n is 0, 1 or 2; R1 is a branched or straight chain C1-5 alkyl or C3-6 cycloalkyl optionally substituted with hydroxyl, or one or more halogens; and X1, X2, X3, X4, and X5 are either all hydrogens or one or two of X1, X2, X3, X4, and X5 are halogen and the remainder are hydrogens, with the proviso that when n is 0 or 1 and each X is hydrogen, R1 is not methyl. A wide variety or sustained release mechanisms can be utilized so as to provide gradual release of the active ingredient after ingestion as a pharmaceutical presentation, such as a tablet or capsule. Presentations include sustained release tablets, sustained release capsules, capsules containing sustained release beads.
摘要翻译： 公开了药物表现或基于phenoxathiin的MAO-A抑制剂，由此MAO受体能够在消化道中持续释放。 特别的基于苯基硫蛋白的MAO-A抑制剂包括下式的那些：其中n为0,1或2; R1是任选被羟基或一个或多个卤素取代的支链或直链C 1-5烷基或C 3-6环烷基; 且X 1，X 2，X 3，X 4和X 5均为氢，或者X 1，X 2，X 3，X 4和X 5中的一个或两个为卤素，其余为氢，条件是当n为0或1时， X是氢，R1不是甲基。 可以使用多种或持续释放机制，以便在摄取后作为药物呈递（例如片剂或胶囊）逐渐释放活性成分。 呈现包括持续释放片剂，缓释胶囊，含缓释珠粒的胶囊。
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公开(公告)号：US20110206769A1
公开(公告)日：2011-08-25
申请号：US12860358
申请日：2010-08-20
申请人： Andrew Chen , Hailiang Chen , James Cecil Free , Majid Keshtmand , Mohammed Abdul Rahman , Sally A. Look
发明人： Andrew Chen , Hailiang Chen , James Cecil Free , Majid Keshtmand , Mohammed Abdul Rahman , Sally A. Look
CPC分类号： A61K31/39 , A61K9/145 , A61K9/2054 , A61K9/5078
摘要： Provided are methods for reducing the excipient load of pharmaceutical formulations containing 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin 10,10-dioxide as the active pharmaceutical ingredient, and compositions related thereto. In particular, provided is a pharmaceutical product comprising 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin 10,10-dioxide and a stabilizer admixed throughout a solid-form unilamellar matrix, wherein the ratio of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin 10,10-dioxide to stabilizer ranges from about 2:3 to about 1:10, and related methods of forming the pharmaceutical product.
摘要翻译： 提供了减少含有3-氟-7-（2,2,2-三氟乙氧基）苯氧硫蛋白10,10-二氧化物作为活性药物成分的药物制剂的赋形剂负荷的方法，以及与之相关的组合物。 特别地，提供了包含3-氟-7-（2,2,2-三氟乙氧基）苯氧硫蛋白10,10-二氧化物和整个固体形式的单层基质中混合的稳定剂的药物产品，其中3-氟 - 7-（2,2,2-三氟乙氧基）苯氧硫蛋白10,10-二氧化物至稳定剂的范围为约2:3至约1:10，以及形成药物产品的相关方法。
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