Phosphonate nucleotide derivatives
First Claim
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1. A phosphonate nucleotide derivative represented by the following general formula (I) or a salt thereof, or a hydrate or a solvate thereof:
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wherein R1 represents hydrogen atom, a C1-C6 alkyl group, or a C7-C10 aralkyl group;
R2 represents a C1-C6 alkyl group, a C7-C10 aralkyl group, or phenyl group;
R3 and R4 independently represent an ethyl group substituted with one or more halogen atoms;
R5 represents hydrogen atom, a C1-C4 alkyl group, a C1-C4 hydroxyalkyl group or a C1-C4 alkyl group substituted with one or more halogen atoms; and
X represents —
CH—
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Abstract
A compound represented by the following general formula (I) which has an antiviral activity:
wherein R1 represents hydrogen atom, C1-C6 alkyl group, or C7-C10 aralkyl group; R2 represents C1-C6 alkyl group, C7-C10 aralkyl group, or phenyl group; R3 and R4 independently represent hydrogen atom, C1-C6 alkyl group, acyloxymethyl group, acylthioethyl group, or ethyl gorup substituted with at least one halogen atom; R5 represents hydrogen atom, C1-C4 alkyl gorup, C1-C4 hydroxyalkyl group, C1-C4 alkyl group substituted with at least one halogen atom; and X represents carbon atom or nitrogen atom.
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Citations
13 Claims
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1. A phosphonate nucleotide derivative represented by the following general formula (I) or a salt thereof, or a hydrate or a solvate thereof:
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wherein R1 represents hydrogen atom, a C1-C6 alkyl group, or a C7-C10 aralkyl group;
R2 represents a C1-C6 alkyl group, a C7-C10 aralkyl group, or phenyl group;
R3 and R4 independently represent an ethyl group substituted with one or more halogen atoms;
R5 represents hydrogen atom, a C1-C4 alkyl group, a C1-C4 hydroxyalkyl group or a C1-C4 alkyl group substituted with one or more halogen atoms; and
X represents —
CH—
.- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13)
2-amino-9-[2-[bis(2,2,2-trifluoroethyl)phosphonylmethoxy]ethyl]-6-(phenylamino)purine;
2-amino-9-[2-[bis(2,2,2-trifluoroethyl)phosphonylmethoxy]ethyl]-6-(N-methylphenylamino)purine;
2-amino-9-[2-[bis(2,2,2-trifluoroethyl)phosphonylmethoxy]propyl]-6-(phenylamino)purine;
2-amino-9-[2-[bis(2,2,2-trifluoroethyl)phosphonylmethoxy]propyl]-6-(N-methylphenylamino)purine; and
2-amino-9-[2-[bis(2,2,2-trifluoroethyl)phosphonylmethoxy]propyl]-6-(dimethylamino)purine.
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9. A pharmaceutical composition which comprises the compound or the salt thereof, or the hydrate or the solvate thereof according to claim 1 together with a pharmaceutically acceptable carrier.
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10. A method for therapeutic treatment of a viral infectious disease which comprises the step of administering a therapeutically effective amount of the compound or the salt thereof, or the hydrate or the solvate thereof according to claim 1 to a patient with the viral disease.
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11. The compound or the salt thereof, or the hydrate or the solvate thereof according to claim 2, wherein R2 is phenyl group.
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12. The compound or the salt thereof, or the hydrate or the solvate thereof according to claim 2, wherein R5 is a C1-C4 alkyl group.
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13. The compound or the salt thereof, or the hydrate or the solvate thereof according to claim 3, wherein R5 is a C1-C4 alkyl group.
Specification
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Current AssigneeMitsubishi Chemical Corporation (Mitsubishi Chemical Group Corp.)
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Original AssigneeMitsubishi Chemical Corporation (Mitsubishi Chemical Group Corp.)
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InventorsInoue, Naoko, Yuasa, Satoshi, Kamiya, Naohiro, Takashima, Hideaki, Sekiya, Kouichi, Ubasawa, Masaru
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Primary Examiner(s)Shah, Mukund J.
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Assistant Examiner(s)TRUONG, TAMTHOM NGO
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Application NumberUS08/973,762Time in Patent Office1,181 DaysField of Search544/277, 514/261US Class Current514/81CPC Class CodesC07F 9/6561 containing systems of two o...C07F 9/65616 containing the ring system ...
