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1.发明申请COMPOUNDS WITH A SULPHONAMIDE GROUP AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS 审中-公开具有磺酰胺基团的化合物和含有这些化合物的药物组合物公开(公告)号：US20090023896A1
公开(公告)日：2009-01-22
申请号：US12142332
申请日：2008-06-19
CPC分类号： C07J41/0044 , C07J41/0038 , C07J41/005
摘要： This invention relates to compounds that as prodrugs and/or vehicles make it possible for an active ingredient to be taken up into erythrocytes and/or an active ingredient to bind to erythrocytes, whereby the uptake of the compounds into erythrocytes and/or the binding of the compounds to erythrocytes is made possible by a group —SO2NR1R2, whereby R1 and R2, independently of one another, mean a hydrogen atom, an acyl group, an alkyl group, a cycloalkyl group, an aryl group, a cyano group or a hydroxy group. By the prodrugs according to the invention, active ingredients, such as endogenous substances, natural substances and synthetic substances with therapeutically valuable properties with a high “first pass” effect are made available orally to a reasonable extent or are decisively improved relative to oral activity.
摘要翻译： 本发明涉及作为前药和/或载体的化合物，使活性成分能够摄入红细胞和/或活性成分以结合红细胞，由此将化合物摄入红细胞和/或结合 对于红细胞的化合物可以通过基团-SO 2 NR 1 R 2来实现，其中R 1和R 2彼此独立地表示氢原子，酰基，烷基，环烷基，芳基，氰基或羟基 组。 通过根据本发明的前药，可以以合理的方式口服提供活性成分，例如内源物质，天然物质和具有高“第一道”效果的治疗有价值的性质的合成物质，或者相对于口服活性而言是有显着改善的。
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2.发明授权Compounds with sulphonamide group and pharmaceutical compositions containing these compounds 失效具有磺酰胺基团的化合物和含有这些化合物的药物组合物公开(公告)号：US07507725B2
公开(公告)日：2009-03-24
申请号：US10296973
申请日：2001-05-08
IPC分类号： A61K31/56
CPC分类号： C07J41/0044 , C07J41/0038 , C07J41/005
摘要： The invention relates to compounds which, acting as a prodrug and/or support, enable an active agent to be taken up by the erythrocytes and/or an active agent to bind to the erythrocytes. The uptake of these compounds by and/or the binding thereof to the erythrocytes is made possible by a group of formula —SO2NR1R2, wherein R1 and R2, independently of each other, mean a hydrogen atom, an acyl group, an alkyl group, a cycloalkyl group, an aryl group, a cyano group or a hydroxy group. The inventive prodrugs enable active agents such as endogenic substances, natural substances and synthetic substances with therapeutically useful properties which have a high “first path” effect, to be administered orally effectively or significantly improve the oral activity thereof.
摘要翻译： 本发明涉及作为前药和/或支持物的化合物，使活性剂能够被红细胞和/或活性剂吸收以结合红细胞。 这些化合物通过和/或其与红细胞的结合的吸收通过式-SO 2 NR 1 R 2的基团可以实现，其中R 1和R 2彼此独立地表示氢原子，酰基，烷基， 环烷基，芳基，氰基或羟基。 本发明的前药使得具有高“第一途径”效果的具有治疗有用性质的内源性物质，天然物质和合成物质等活性剂能够有效口服或显着改善其口服活性。
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