Preparation of carrier bound vinyl nucleobases and their polymers, useful, e.g. as antiviral and anticancer agents, or for diagnostics or purification, comprises reaction of vinyl nucleobases with a carrier
Method for preparing carrier-fixed vinyl nucleobases comprises reacting vinyl nucleobases (I/II), preferably with long spacers on the heterocycle, with a carrier. Method for preparing carrier-fixed vinyl nucleobases comprises reacting vinyl nucleobases of formula (I) or (II), preferably having long...
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Main Authors | , |
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Format | Patent |
Language | English German |
Published |
24.04.2003
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Edition | 7 |
Subjects | |
Online Access | Get full text |
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Summary: | Method for preparing carrier-fixed vinyl nucleobases comprises reacting vinyl nucleobases (I/II), preferably with long spacers on the heterocycle, with a carrier. Method for preparing carrier-fixed vinyl nucleobases comprises reacting vinyl nucleobases of formula (I) or (II), preferably having long spacers on the heterocycle, with a carrier. R1 = H or vinyl; R2 = O, NH, N(alkyl, aryl or amino) or sulfur; R3 = H, halo, OH, amino (optionally substituted by 1 or 2 alkyl or aryl), N3, NO, NO2, alkyl or aryl (both optionally substituted by halo), NH-NH2, SH, alkylthio or arylthio; R4 and R5 = H, halo, OH, alkyl or aryl (both optionally substituted by halo), SH, alkylthio, arylthio, alkylamino, arylamino or vinyl; R6 = H, halo, OH, NH2 (optionally substituted by one or two alkyl), N3, NH-NH2 , SH, alkylthio, arylthio or CN; R7 = R3; R8 and R10 = R1; and R9 = H, halo, OH or NH2 (optionally substituted by 1 or 2 alkyl or aryl).
Die Erfindung betrifft am Träger fixierte neue artifizielle Polymerisationsprodukte der Vinylnukleobasen der allgemeinen Formel (I), ihre Herstellung als Homo- und Copolymerisate mit Vinylverbindungen der allgemeinen Formel (II) sowie ihre Anwendung. Diese nukleaseresistenten Homo- und Copolymere der allgemeinen Formel (III) zeigen im Komplex mit nativen Poly(desoxy)ribonukleotiden eine hohe therapeutische virostatische, cancerostatische sowie immunomodulatorische Aktivität und dienen auf Grund ihrer Fähigkeit zur Bindung spezifischer Nukleinsäuresequenzen als Diagnostika in der Medizin und als stationäre Phase bei Aufreinigungsverfahren. |
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Bibliography: | Application Number: DE2001147238 |