Dinucleoside phosphinates and their pharmaceutical compositions

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United States of America Patent

PATENT NO 5466677
SERIAL NO

08204020

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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A dinucleotide analogue of formula ##STR1## where B.sup.1 and B.sup.2 are each independently a monovalent nucleoside base radical; R.sup.1 is R.sup.1.sub.a or Z; R.sup.1.sub.a, R.sup.2, R.sup.3 and R.sup.4 are each independently hydrogen, halogen or hydroxy; R.sup.5 is R.sup.5.sub.a or Z; R.sup.6 is hydrogen or R.sup.6.sub.a ; R.sup.7 is hydrogen, alkyl-N,N-dialkylphosphoramidyl or R.sup.7.sub.a, R.sup.8 is R.sup.8.sub.a or Z, or the indicated R.sup.7 O and R.sup.8 together denote an isopropylidenedioxy group; R.sup.5.sub.a and R.sup.8.sub.a are each independently hydrogen, halogen, hydroxy, --OR.sup.10, --OCOR.sup.10 or silyloxy substituted by three C.sub.1 -C.sub.15 hydrocarbyl groups; R.sup.6.sub.a and R.sup.7.sub.a are each independently a C.sub.1 -C.sub.10 aliphatic radical, a C.sub.6 -C.sub.15 aromatic radical, a C.sub.7 -C.sub.30 araliphatic radical, --COR.sup.11, --SO.sub.2 R.sup.11 or silyl substituted by three C.sub.1 -C.sub.15 hydrocarbyl groups; R.sup.9 is hydrogen, a C.sub.1 -C.sub.8 aliphatic radical, a C.sub.3 -C.sub.8 cycloaliphatic radical, a C.sub.6 -C.sub.15 aromatic radical, a C.sub.7 -C.sub.13 araliphatic radical, an alkali metal ion or an ammonium ion; R.sup.10 and R.sup.11 are each independently a C.sub.1 -C.sub.10 aliphatic radical, a C.sub.3 -C.sub.8 cycloaliphatic radical, a C.sub.6 -C.sub.15 aromatic radical or a C.sub.7 -C.sub.16 araliphatic radical; R.sup.x and R.sup.y are independently hydrogen, halogen, hydroxy, a C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.6 -C.sub.15 aryl, C.sub.7 -C.sub.16 aralkyl, C.sub.1 -C.sub.10 alkoxy, C.sub.2 -C.sub.10 alkenoxy, C.sub.6 -C.sub.10 aryloxy or C.sub.7 -C.sub.16 aralkyloxy group, which is substituted or unsubstituted, or --OCOR.sup.z ; R.sup.z is a substituted or unsubstituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.6 -C.sub.15 aryl or C.sub.7 -C.sub.16 aralkyl group; and Z is C.sub.6 -C.sub.10 aryloxythiocarbonyloxy, the C.sub.6 -C.sub.10 aryl group being substituted or unsubstituted.

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Patent Owner(s)

Patent OwnerAddress
CIBA-GEIGY CORPORATIONPATENT DEPARTMENT 520 WHITE PLAINS ROAD P O BOX 2005 TARRYTOWN NY 10591

International Classification(s)

Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Baxter, Anthony D Northwich, GB2 6 634
Baylis, Eric K Stockport, GB2 12 738
Collingwood, Stephen P Westhoughton, GB2 6 626
De, Mesmaeker Alain Kanerkinden, CH 42 1436
Schmit, Chantal Basel, CH 3 627
Taylor, Roger J Stretford, GB2 5 629

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