- MODIFIED CYCLIC DINUCLEOSIDE COMPOUNDS AS STING MODULATORS
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Provided herein are compounds of Formula (I), Formula (II) and/or Formula (III), or pharmaceutically acceptable salts of any of the foregoing, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salt
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Paragraph 0177
(2020/11/23)
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- 3'3'-CYCLIC DINUCLEOTIDE ANALOGUE COMPRISING A CYCLOPENTANYL MODIFIED NUCLEOTIDE AS STING MODULATOR
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The present disclosure relates to 3'3'-cyclic dinucleotides comprising a carbocyclic nucleotide and derivatives thereof, that can modulate the activity of the STING adaptor protein.
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- 3-DEAZANEPLANOCIN DERIVATIVES
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This invention describes the series of compounds based on the 3-deazaneplanocin A (DZNep) core structure designed to inhibit the function of Polycomb repressive complex 2 (PRC2) proteins.
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Page/Page column 30
(2010/04/27)
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- Chiral syntheses of 6′-β-fluoroaristeromycin, 6′-β-fluoro-5′-noraristeromycin and aristeromycin
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Carbocyclic nucleosides substituted at the C-6′ position are receiving increasing attention. Chiral synthetic accessibility to the biologically promising 6′-β-fluoroaristeromycin is lacking. Its preparation and that of the 5′-nor analogue are described. A
- Yin, Xue-Qiang,Schneller, Stewart W.
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p. 7535 - 7538
(2007/10/03)
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- Preparation of carbocyclic S-adenosylazamethionine accompanied by a practical synthesis of (-)-aristeromycin
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For the preparation of a carbocyclic nitrogen analogue of S-adenosylmethionine (carba-AdoazaMet, 4), a practical synthesis of (-)-aristeromycin (7) has been developed using variations of literature procedures. This approach called for a stereospecific synthesis of (3aR,6aR)-2,2-dimethyl-3a, 6a-dihydrocyclopenta[1,3]dioxol-4-one ((4R, 5R)-4,5-O-isopropylidene-2-cyclopentenone) (8), which was achieved by modifying reported procedures from D-(-)-ribose.
- Yang, Minmin,Ye, Wei,Schneller, Stewart W.
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p. 3993 - 3996
(2007/10/03)
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- A flexible synthesis of carbanucleosides and 5′-nor-1′-homo carbanucleosides from a common precursor
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Enzymatic resolution of (±)-1-acetoxy-4-(nitromethyl)-2-cyclopentene (4) provides entry into a facile 10-step route to carbanucleosides and a practical 7-step procedure to 5′-nor-1′-homo carbanucleosides. These routes are illustrated for adenine derivatives but they are adaptable to any heterocyclic base.
- Rajappan, Vasathakumar P,Yin, Xueqiang,Schneller, Stewart W
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p. 9889 - 9895
(2007/10/03)
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- An expeditious route to carbocyclic nucleosides: (-)-Aristeromycin and (-)-carbodine
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The readily available bicyclic lactone (-)-1 was transformed into diacetate (-)-2 which served in an expeditious route to (-)-aristeromycin (3a) and (-)-carbodine (3b) in acceptable yields.
- Burlina, Fabienne,Favre, Alain,Fourrey, Jean-Louis,Thomas, Martial
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p. 247 - 250
(2007/10/03)
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- Synthesis and incorporation of carbocyclic nucleosides into a hammerhead ribozyme domain-RNase resistance and catalytic activity
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A hammerhead ribozyme domain incorporating (-)-carbodine 8a and (-)-aristeromycin 8b at selected positions, manifests increased RNase resistance and exhibits significant catalytic activity.
- Burlina, Fabienne,Favre, Alain,Fourrey, Jean-Louis,Thomas, Martial
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p. 1623 - 1624
(2007/10/03)
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- Biocatalytical Transformations- VI. The 4-Acetamido-cyclopent-2-ene Carboxylate Route Revisited: Synthesis of (+)- and (-)-Aristeromycin
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Enantiomerically pure (+)-as well as (-)-aristeromycin can be synthesized starting from (+)- or (-)-butyl (or hexyl) 4-acetamido-cyclopent-2-ene carboxylate; these carboxylates are easily obtained from their corresponding racemates by hydrolysis with the lipase from Candida rugosa.
- Csuk, Rene,Doerr, Petra
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p. 5789 - 5798
(2007/10/02)
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- Highly asymmetric enzymatic hydrolysis and transesterification of meso-bis(acetoxymethyl)- and bis(hydroxymethyl)cyclopentane derivatives: An insight into the active site model of Rhizopus delemar lipase
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Rhizopus delemar lipase (RDL)-catalysed hydrolysis of meso-1,3-bis(acetoxymethyl)cyclopentane derivatives (7, 12) and Pseudomonas fluorescens lipase (PFL)-catalysed hydrolysis of 7 afforded the chiral monoacetates (15, 16) of > 99% ee. In explanation of these high enantioselectivities of RDL, the simple box-type active site model of enzyme was tentatively proposed. On the other hand, PFL-catalysed transesterification of meso-bis-(hydroxymethyl)cyclopentane (6) afforded (+)-16 of > 99% ee. The obtained (+) and (-)-16 were converted into the natural carbocyclic nucleoside(-)-aristeromycin (25), respectively.
- Tanaka,Yoshioka,Sakai
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p. 981 - 996
(2007/10/02)
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- Enantiospecific Syntheses of Aristeromycin and Neplanocin A
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The carbocylic nucleosides (-)-aristeromycin and (-)-neplanocin A were made enantiospecifically in nine steps and ten steps, respectively, from D-ribonic acid γ-lactone.Quenching of an organocuprate conjugate addition reaction with either acetic acid or methanesulfinyl chloride determines whether the divergent synthetic route branches toward (-)-aristeromycin or (-)-neplanocin A.An alternate synthesis of cyclopentenone 1, a common intermediate to these compounds, from D-gulonic acid γ-lactone is also described.
- Wolfe, Michael S.,Anderson, Blake L.,Borcherding, David R.,Borchardt, Ronald T.
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p. 4712 - 4717
(2007/10/02)
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- Enantioselective synthesis of the carbocyclic nucleosides (-)-aristeromycin and (-)-neplanocin A by a chemicoenzymatic approach
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An efficient synthesis of the carbocyclic nucleosides ( minus )-aristeromycin and ( minus )-neplanocin A has been developed in an enantioselective and stereocontrolled manner starting from the Diels-Alder adduct of cyclopentadiene and dimethyl acetylenedi
- Arita,Adachi,Ito,et al.
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p. 4049 - 4055
(2007/10/10)
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