153172-33-9Relevant articles and documents
8-Aza-immucillins as transition-state analogue inhibitors of purine nucleoside phosphorylase and nucleoside hydrolases
Evans, Gary B.,Furneaux, Richard H.,Gainsford, Graeme J.,Hanson, John C.,Kicska, Gregory A.,Sauve, Antony A.,Schramm, Vern L.,Tyler, Peter C.
, p. 155 - 160 (2003)
The 8-aza-immucillins (8-aza-9-deazapurines linked from C9 to C1 of 1,4-dideoxy-1,4-iminoribitol) have been designed as transition-state analogues of the reactions catalyzed by purine nucleoside phosphorylase and nucleoside hydrolases. Syntheses of the 8-aza-immucillin analogues of inosine and adenosine are described. They are powerful inhibitors of the target enzymes with equilibrium dissociation constants as low as 42 pM.
PROCESS FOR MANUFACTURE OF FORODESINE
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Page/Page column 8, (2016/08/10)
This invention describes a novel process for the manufacture of Forodesine (I).
ANTIVIRAL AZASUGAR-CONTAINING NUCLEOSIDES
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Page/Page column 97, (2014/06/11)
Disclosed are compounds comprising an azasugar attached to a heterocyclic base, including pharmaceutically acceptable salts thereof, suitable for use in inhibiting viral RNA polymerase activity or viral replication, and treating viral infections. The compounds are characterized, in part, by favorable pharmacokinetics for the active pharmaceutical ingredient, particularly in conjunction with enteral administration, including, in particular, oral administration. Also disclosed are pharmaceutical compositions comprising one or more compounds mentioned above, or pharmaceutically acceptable salts thereof, as well as methods for preparing same. Also provided are methods for inhibiting viral RNA polymerase activity, viral replication, and treating viral infections.
COMPOSITIONS AND METHODS FOR INHIBITING VIRAL POLYMERASE
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, (2013/11/05)
Provided are compounds of Formula (I) as described herein. Compounds of Formula (I) are useful in methods of inhibiting viral RNA polymerase activity and viral replication. Also provided are pharmaceutical compositions comprising compounds of Formula (I), as well as methods of treating viral infections using compounds of Formula (I).
Process for preparing 2-pyrrolidinyl-1H-pyrrolo[3,2-d]pyrimidine inhibitors of nucleoside metabolism
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Page column 18, (2008/06/13)
A process of preparing a compound of the formula (I) wherein B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H halogen or SCH3; R is an optionally substituted alkyl, aralkyl or aryl group; and Z is selected from OH, hydrogen, halogen, hydroxy, SQ or OQ, Q is an optionally substituted all, aralkyl or aryl group; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof, which comprises reacting a compound of the formula (II) ?with an anion produced by abstraction of the bromine or iodine atom from a compound of formula (XIX), ?to form a compound of formula (XX) The compound of formula (XX) is N- and O-deprotected to obtain the compound of formula (I).
Synthesis of transition state analogue inhibitors for purine nucleoside phosphorylase and N-riboside hydrolases
Evans, Gary B.,Furneaux, Richard H.,Gainsford, Graeme J.,Schramm, Vern L.,Tyler, Peter C.
, p. 3053 - 3062 (2007/10/03)
Syntheses of the 'Immucillins', potent aza-C-nucleoside inhibitors of purine nucleoside phosphorylase are reported as well as those of 5-deoxy-, 5- deoxyfluoro- and 2-deoxy- analogues and others having modified bases. (C) 2000 Elsevier Science Ltd.
Synthesis of transition state inhibitors for N-riboside hydrolases and transferases
Furneaux, Richard H.,Limberg, Gerrit,Tyler, Peter C.,Schramm, Vern L.
, p. 2915 - 2930 (2007/10/03)
A number of 1,4-dideoxy-1,4-imino-1-(S)-(substituted phenyl)-D-ribitols bearing aromatic OH, NH2, NO2, CO2H and halogeno moieties, and a 3-pyridyl analogue have been synthesized. The key step is die condensation of aryllithium or aryl Grignard reagents with the imine 3; derived from the protected 1,4-dideoxy-1,4-imino-D-ribitol 4.
A new class of C-nucleoside analogues. 1-(S)-aryl-1,4-dideoxy-1,4-imino-D-ribitols, transition state analogue inhibitors of nucleoside hydrolase
Horenstein,Zabinski,Schramm
, p. 7213 - 7216 (2007/10/02)
The first members of new class of N-glycohydrolase transition state analogue inhibitors, 1,4-dideoxy-1,4-imino-1-(S)-phenyl-D-ribitol, 1, and 1,4-dideoxy-1,4-imino-1-(S)-(4-imidazolyl)-D-ribitol, 2, have been synthesized. The compounds represent a new typ
