2-AMINOPROPANE-1,3-DIOL DERIVATIVE, ITS PHARMACEUTICAL APPLICATION AND INTERMEDIATE SUBSTANCES FOR THEIR SYNTHESIS

FIELD: organic chemistry, chemical technology, medicine, pharmacy. SUBSTANCE: invention describes derivative of 2-aminopropane-1,3-diol of the general formula (I): where R1, R2, R3, R4 are similar or different and each means hydrogen atom or alkanoyl with linear or branched chain containing from 1 t...

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Hauptverfasser: TESIMA KODZI, KHOSINO JUKIO, KHANANO TOKUSI, AOKI ¿SIJUKI, FUDZITA TETSURO, ADATI KUNITOMO
Format: Patent
Sprache:eng
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Zusammenfassung:FIELD: organic chemistry, chemical technology, medicine, pharmacy. SUBSTANCE: invention describes derivative of 2-aminopropane-1,3-diol of the general formula (I): where R1, R2, R3, R4 are similar or different and each means hydrogen atom or alkanoyl with linear or branched chain containing from 1 to 6 carbon atoms and its pharmaceutically acceptable acid addition salt or hydrate. Invention relates also to pharmaceutical composition exhibiting immunosuppressive activity, to 2-amino-2-{2-[4-(1-hydroxy-5-phenyl-pentyl)phenyl]ethyl}-propane-1,3-diol or its derivative where amino-group is protected with aliphatic acyl group and/or hydroxy-group is protected with tert.-butyldimethylsilyl-group and also to 2-amino-2-[2-(4-formylphenyl)ethyl]-propane-1,3-diol, its derivative where amino-group and/or hydroxy-group are protected with aliphatic group and/or hydroxy-group is protected with tert.-butyldimethylsilyl-group. Owing to low toxicity, high safety and immunosuppressive effect these derivatives can be used as agents preventing or suppressing rejection response in transplantation of organs and for prophylaxis and treatment of different autoimmune sicknesses and different allergic sicknesses. EFFECT: valuable medicinal properties of compounds. 9 cl, 2 dwg, 1 tbl