A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 47/48 (2006.01) A61K 31/4045 (2006.01) A61K 31/49 (2006.01) A61K 31/565 (2006.01) A61K 31/566 (2006.01) A61K 31/568 (2006.01) A61K 47/20 (2006.01) A61P 43/00 (2006.01) C07J 41/00 (2006.01)
Patent
CA 2410630
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.
L'invention concerne des composés qui permettent, en tant que promédicament ou support, l'absorption d'un principe actif dans les érythrocytes ou la liaison d'un principe actif aux érythrocytes. L'absorption des composés dans les érythrocytes ou leur liaison aux érythrocytes est rendue possible grâce à un groupe -SO¿2?NR?1¿R?2¿ où R?1¿ et R?2¿ représentent, indépendamment l'un de l'autre, un atome d'hydrogène, un groupe acyle, un groupe alkyle, un groupe cycloalkyle, un groupe aryle, un groupe cyano ou un groupe hydroxy. Grâce aux promédicaments selon l'invention, des principes actifs, tels que des substances endogènes, des substances naturelles et des substances synthétiques ayant des propriétés thérapeutiquement précieuses à effet de <= premier passage >= élevé, sont mises à disposition oralement de manière utile ou sont améliorées de manière significative quant à leur activité orale.
Elger Walter
Hedden Annemarie
Hillisch Alexander
Schollkopf Klaus
Schwarz Sigfrid
Marks & Clerk
Schering Ag
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