http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-099312-A1

Outgoing Links

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filingDate 2015-02-06-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f7d28162ce6673187193220041f81fcc
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_192fbc2ea13c1f938ed948bc748ea26f
publicationDate 2016-07-13-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-099312-A1
titleOfInvention DERIVATIVES OF NUCLEOSIDS REPLACED WITH 4-DIFLUOROMETIL AS INHIBITORS OF THE REPLICATION OF THE INFLUENZA RNA
abstract The application discloses nucleoside derivatives as inhibitors of influenza RNA replication. In particular, the application discloses the use of purine and pyrimidine nucleoside derivatives as inhibitors of influenza RNA replication and pharmaceutical compositions containing such compounds. Claim 1: An influenza RNA replication inhibitor compound of formula (1) characterized in that: Y is H or P (= X) (R) (R); R is O-R¹ or NHR¹; R¹ is -C (R²ᵃ) (R²ᵇ) C (= O) OR³; R is N (R⁴) C (R²ᵃ) (R²ᵇ) C (= O) OR³, -OP (= O) (OH) OP (= O) (OH) OH, or -OR³; R¹ is H, lower haloalkyl, or aryl, wherein the aryl is phenyl or naphthylenyl, optionally substituted with one or more of lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, halo, lower haloalkyl, -N (R¹ᵃ) ₂, acylamino, -SO₂N (R¹ᵃ) ₂, -C (= O) R¹ᵇ, -SO₂ (R¹ᶜ), -NHSO₂ (R¹ᶜ), nitro, cyano, or R¹; each R¹ᵃ is independently H or lower alkyl; each R¹ᵇ is independently -OR¹ᵃ or -N (R¹ᵃ) ₂; each R¹ᶜ is lower alkyl; each R²ᵃ and R²ᵇ is independently H, lower alkyl, (CH₂) ʳN (R¹ᵃ) ₂, lower hydroxyalkyl, -CH₂SH, - (CH₂) S (O) ₚMe, - (CH₂) ₙNHC (= NH) NH₂, (1H- indole-3-yl) methyl, (1H-indol-4-yl) methyl, - (CH₂) ₘC (= O) R¹ᵇ, aryl and lower arylalkyl, wherein the aryl is optionally substituted with one or more hydroxy, alkyl lower, lower alkoxy, halo, nitro or cyano; m is 0, 1, or 2; n is 1, 2, or 3; p is 1 or 2; r is 1 or 2; or R²ᵃ is H and R²ᵇ and R⁴ together form (CH₂) ₙ; each R³ is independently H, lower alkyl, lower haloalkyl, phenyl or phenyl-lower alkyl, wherein the phenyl and the phenyl-lower alkyl are optionally substituted with lower alkoxy; or R³ and R¹ together form CH₂; each R⁴ is independently H, lower alkyl; or R²ᵇ and R⁴ together form (CH₂) ₃; Rʷ, Rʸ, and Rᶻ are each independently H, OH or F; Rˣ is H, OH, or F; or R³ and Rˣ together form a union; or R¹ and Rˣ together form a union; X is O or S; the Base is uracil, cytosine, guanine, adenine, thymine, or heterocycloalkyl, each of which may be optionally substituted with one or more of hydroxy, lower alkyl, lower alkoxy, halo, nitro or cyano; with the proviso that if Rʷ is H, Rʸ is H, and Rᶻ is H, then Rˣ is not H; and with the proviso that formula (1) is not ((2R, 3R, 4R, 5R) -5- (4-amino-2-oxopyrimidin-1 (2H) -yl) -2- (difluoromethyl) -4 -fluoro-3-hydroxytetrahydrofuran-2-yl) methyl tetrahydrogen triphosphate; or a pharmacologically acceptable salt thereof.
priorityDate 2014-02-06-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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Total number of triples: 52.