Boronated nucleoside, nucleotide and oligonucleotide compounds, compositions and methods for using same
AssigneeBoron Bilogicals, Inc.
InventorsBernard F. Spielvogel, Anup Sood, Iris H. Hall, Barbara Ramsay Shaw
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Abstract
A novel class of pharmaceutically active boronated nucleosides are provided. The nucleosides are boronated at a ring nitrogen of the purine or pyrimidine or analogues thereof. Also provided are phosphate esters of these nucleosides and oligomers thereof. Methods of making and using the boronated nucleosides are also disclosed.
Claims14
A boronated nucleoside comprising a nucleoside which is N-boronated on the nucleoside base with a boron-containing substituent selected from the group consisting of --BH.sub.2 CN, --BH.sub.3, and --BH.sub.2 COOR, wherein R is C1 to C18 alkyl.
A boronated nucleoside selected from the group consisting of 2'-deoxyguanosine-N7-cyanoborane, 2'-deoxyinosine-N7-cyanoborane, 2'-deoxyadenosine-N1-cyanoborane, 2'-deoxycytidine-N3-cyanoborane, and 2',3'-dideoxycytidine-N3-cyanoborane.
A pharmaceutical formulation comprising an effective anti-inflammatory or anti-tumor amount of a boronated nucleoside in a pharmaceutically acceptable carrier, said boronated nucleoside comprising a nucleoside which is N-boronated on the nucleoside base with a boron-containing substituent selected from the group consisting of --BH.sub.2 CN, --BH.sub.3, and --BH.sub.2 COOR, wherein R is C1 to C18 alkyl.
A method for treating a mammal suffering from inflammation comprising administering to said mammal an effective anti-inflammatory amount of a boronated nucleoside comprising a nucleoside which is N-boronated on the nucleoside base with a boron-containing substituent selected from the group consisting of --BH.sub.2 CN, --BH.sub.3, and --BH.sub.2 COOR, wherein R is C1 to C18 alkyl.
Dependencies are inferred from the claim text.