- Oligomer conjugates of heteropentacyclic nucleosides
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The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer.
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Page/Page column 35; 36; 37
(2015/12/09)
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- Nucleoside analogs with carboxamidine modified monocyclic base
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Novel nucleoside analog compounds are disclosed. The novel compounds or pharmaceutically acceptable esters or salts thereof may be used in pharmaceutical compositions, and such compositions may be used to treat an infection, an infestation, a neoplasm, or an autoimmune disease. The novel compounds may also be used to modulate aspects of the immune system, including modulation of Type 1 and Type 2 activity.
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Page/Page column 4
(2008/06/13)
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- Synthesis and antitumor activity of ribavirin imidates. A new facile synthesis of ribavirin amidine (1-β-D-ribofuranosyl-1,2,4-triazole-3-carboxamidine hydrochloride)
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Methyl 1-β-D-ribofuranosyl-1,2,4-triazole-3-carboximidate (4) and ethyl 1-β-D-ribofuranosyl-1,2,4-triazole-3-carboximidate (6) were synthesized and tested for antitumor and antiviral activity. A new facile synthesis of 1-β-D-ribofuranosyl-1,2,4-triazole-3-carboxamidine hydrochloride (5), starting with imidate 4, was also developed. The imidates 4 and 6 differed greatly in solubility and dosing requirements. Even so, both compounds exhibited significant activity in vivo against murine leukemia L1210. Nontoxic dosing with 4 also significantly diminished Friend leukemia induced splenomegaly. In contrast, neither imidate was active in vitro.
- Kini,Robins,Avery
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p. 1447 - 1449
(2007/10/02)
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