Nucleotide analogs
First Claim
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1. A compound having the structure of formula (1) ##STR36## wherein B is 5-fluorocytosin-1-yl, 5-methylcytosin-1-yl, or a heterocyclic base having the structure (a) ##STR37## R is --S(O)2 N(R3)2 ;
- each R1 is independently hydrogen, cyano, nitro, alkyl, O-alkyl, --C(O)R3, --S(O)2 OH, --N(R3)2 or --CHO;
each R3 is independently hydrogen, alkyl, phenyl, phenyl substituted with C1-20 alkyl, --CH2 C6 H5 or --CH2 CH2 C6 H5, but when R1 is --N(R3)2, one R3 is hydrogen and the other R3 is C2-6 alkyl or when R1 is --N(R3)2, both R3 are the same and are C2-6 alkyl;
R6 is --NH2, --NHR7, --NHR8, --N═
CHN(R7)2 or --N═
C(CH3)N(R7)2 ;
R7 is C1 -C6 alkyl;
R8 is a protecting group; and
each R9 independently is N or CH.
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Abstract
Nucleotide phosphonate esters characterized by the presence of an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise an ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for their synthesis and use are described.
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Citations
1 Claim
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1. A compound having the structure of formula (1) ##STR36## wherein B is 5-fluorocytosin-1-yl, 5-methylcytosin-1-yl, or a heterocyclic base having the structure (a) ##STR37## R is --S(O)2 N(R3)2 ;
- each R1 is independently hydrogen, cyano, nitro, alkyl, O-alkyl, --C(O)R3, --S(O)2 OH, --N(R3)2 or --CHO;
each R3 is independently hydrogen, alkyl, phenyl, phenyl substituted with C1-20 alkyl, --CH2 C6 H5 or --CH2 CH2 C6 H5, but when R1 is --N(R3)2, one R3 is hydrogen and the other R3 is C2-6 alkyl or when R1 is --N(R3)2, both R3 are the same and are C2-6 alkyl; R6 is --NH2, --NHR7, --NHR8, --N═
CHN(R7)2 or --N═
C(CH3)N(R7)2 ;R7 is C1 -C6 alkyl; R8 is a protecting group; and each R9 independently is N or CH.
- each R1 is independently hydrogen, cyano, nitro, alkyl, O-alkyl, --C(O)R3, --S(O)2 OH, --N(R3)2 or --CHO;
Specification