- CYCLIC DINUCLEOTIDES AS ANTICANCER AGENTS
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The present invention is directed to compounds of the formulae I, II and III as shown below wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
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Paragraph 1384; 1387; 1388
(2019/02/13)
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- 6-methyl 7-position-denitrified purine nucleoside compounds and application thereof
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The invention discloses6-methyl 7-position-denitrified purine nucleoside compounds and an application thereof and belongs to the field of medicinal chemistry. The 6-methyl 7-position-denitrified purine nucleoside compounds or pharmaceutically acceptable salts of the compounds having characteristics of a structure shown as formula I are a kind of novel-structured compounds designed and synthesized according to protein structure characteristics of RNA virus polymerase, and the compounds can inhibit RNA viruses, thereby being capable of serving as potential drugs for preventing and treating infection of RNA viruses such as HCV (hepatitis c virus), influenza virus, HRV (rhinovirus), RSV, Ebola virus, DENV (Dengue virus), enterovirus and the like.
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Paragraph 0146; 0147; 0148; 0150; 0151
(2017/09/02)
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- ANTIVIRAL AGENTS
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Compounds of structural formula (I): and pharmaceutically acceptable salts thereof; as defined herein, are described for use in the prevention and/or treatment of HCV infections. Novel compounds of the formula (I) and pharmaceutical formulations containin
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Page/Page column 12
(2012/01/15)
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- Chemoselective staudinger strategy in the practical, fit for purpose, gram-scale synthesis of an HCV RNA polymerase inhibitor
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The use of a late-stage selective Staudinger reaction in the preparation of the novel HCV RNA polymerase inhibitor is described. Georg Thieme Verlag Stuttgart - New York.
- Campeau, Louis-Charles,O'Shea, Paul D.
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scheme or table
p. 57 - 60
(2011/02/25)
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- Sugar-modified derivatives of cytostatic 6-(het)aryl-7-deazapurine nucleosides: 2′-c-methylribonucleosides, arabinonucleosides and 2′-deoxy-2′-fluoroarabinonucleosides
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A series of novel sugar-modified derivatives of cytostatic 6-hetaryl-7-deazapurine ribonucleo-sides: 2′-C-methylribonucleosides, arabinonucleosides and 2′-deoxy-2′-fluoroarabinonucleo-sides bearing an alkyl, aryl and hetaryl group in position 6 were prepared by palladium catalyzed cross-coupling reactions of corresponding (protected) 6-chloro-(7-fluoro)-7-deazapurine nucleosides with (het)arylboronic, hetarylstannanes and trimethylaluminium eventually followed by deprotection. Key intermediate 6-chloro-7-deazapurine 2′-C-methyl-β-D-ribofuranoside was prepared via a stereoselective nucleobase anion glycosylation with toluoyl-protected 1,2-anhydro-2-C-methylribofuranose. The 1,2-anhydro sugar was synthesized in 3 steps starting from readily available 2-C-methylribonolactone. The 6-chloro-7-deazapurine arabinofuranoside intermediate was obtained by epimerization from 3′,5′-protected 6-chloro-7-deazapurine ribofuranoside via 2′-hydroxyl oxidation followed by reduction. None of the prepared compounds showed any considerable cytostatic or antiviral activity.
- Naus, Petr,Perlikova, Pavla,Pohl, Radek,Hocek, Michal
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experimental part
p. 957 - 988
(2012/06/16)
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- Total synthesis of 2'-deoxy-2'-arafluoro-tubercidin, -toyocamycin, -sangivamycin and certain related nucleosides
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A total synthesis of novel nucleosides 2'-deoxy-2'-arafluoro-tubercidin 12, -toyocamycin 23, -sangivamycin 24 and -thiosangivamycin 25 has been accomplished for the first time starting from 4-chloropyrrolopyrimidine 4, and 2-bromo-5-(ethoxymethyleneamino)pyrrole-3,4-dicarbonitrile 16.The sodium-salt glycosylation of secondary amines 4 and 16 with 3,5-di-O-benzoyl-2-deoxy-2-fluoro-α-D-arabinofuranosyl bromide 5 gave the major β-nucleosides 6 and 17 along with minor amounts of α-anomers 7 and 18.Ammonolysis of compound 6 gave the tubercidin analogue 12.The annulation of epimers 17 and 18 furnished the bromotoyocamycin 21 and its α-anomer 22, respectively.Compound 21 was converted into analogues of toyocamycin 23, sangivamycin 24 and thiosangivamycin 25.Similar functional-group manipulation of substrates 7 and 22 provided the α-anomers of compounds 12, 23, 24 and 25.Among the nucleosides tested, the sangivamycin 24 and thiosangivamycin 25 analogues have shown some interesting anti-(human cytomegalovirus) activity and it was observed that compound 25 is more active than compound 24, but less potent than 9-(1,3-dihydroxypropan-2-yloxymethyl)guanine in vitro.
- Bhattacharya, Birendra K.,Rao, T. Sudhakar,Revankar, Ganapathi R.
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p. 1543 - 1550
(2007/10/02)
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