Ribonucleoside Analogues Against -Sars-Cov-2
AssigneeKatholieke Universiteit Leuven
InventorsPiet Herdewijn, Zihua Zheng, Elisabetta Groaz
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Abstract
The invention relates to nucleoside derivatives of formula (I), wherein R has the same meaning as that defined in the claims and the description. The present invention also relates to pharmaceutical compositions comprising such compounds and to uses of such compounds and compositions for the treatment or prevention of viral infections, more in particular infections caused by RNA virus, such as coronavirus infections.
Claims12
A compound with general formula (I), or a stereoisomer, tautomer, racemic, salt, hydrate, N-oxide form, or solvate or prodrug thereof;
- wherein R is selected from the group consisting of hydrogen, C1-6alkyl, C3-10cycloalkyl, C6-10aryl, C6-10arylC1-6alkyl, heterocyclyl and heteroaryl, wherein said C1-6alkyl, C3-10cycloalkyl, C6-10aryl, C6-10aryl C1-6alkyl, heterocyclyl and heteroaryl may be unsubstituted or substituted with halo, C1-6alkyl, heteroC1-6alkyl, C1-6alkyloxy, hetero C1-6alkyloxy, hydroxyl, amino, mono C1-6alkylamino, diC1-6alkylamino, C6-10aryl, carboxy, aminocarbonyl, nitro, and cyano.
(canceled)
A process for the preparation of a compound of formula (I) or a stereoisomer, tautomer, racemic, salt, hydrate, N-oxide form, or solvate or prodrug thereof
- wherein R is selected from the group consisting of hydrogen, C1-6alkyl, C3-10cycloalkyl, C6-10aryl, C6-10arylC1-6alkyl, heterocyclyl and heteroaryl, wherein said C1-6alkyl, C3-10cycloalkyl, C6-10aryl, C6-10aryl C1-6alkyl, heterocyclyl and heteroaryl may be unsubstituted or substituted with halo, C1-6alkyl, heteroC1-6alkyl, C1-6alkyloxy, hetero C1-6alkyloxy, hydroxyl, amino, mono C1-6alkylamino, diC1-6alkylamino, C6-10aryl, carboxy, aminocarbonyl, nitro, and cyano;
- the method comprising:
- a) halogenating of a compound of formula (A) to produce a compound of formula (B), wherein X is I, Br, Cl or F;
- and
- b) contacting a compound of formula (B) with a compound of formula (C) to produce the compound of formula (I).
Dependencies are inferred from the claim text.