4 - hydroxy - 3 - 1.8 - naftiridin carboxamidas, Pharmaceutical composition, formulation, use thereof for preparing antiviral Medicine and Method for inhibiting viral DNA Polymerase

摘要

4-hydroxy-1,8-naphthyridin-3-carboxamides, comprising a compound of formula (4) or a pharmaceutically acceptable salt, where R1 is (a) Cl, (b) Br, (c) CN, (d) NO2, or (e) F; R2, R3 and R4 are independently selected from: (a) H, (b) halo, (c) aryl, (d) S (O) mR6, (e) (C = O) R6, (f) (C = O) OR6, (g) cyano, (h) het, where said het is attached by means of a carbon atom, (i) OR10, (j) Ohet, (k) NR7R8, (l) SR10, (m) Shet, (n) NHCOR12, (o) NHSO2R12, or (p) C1-7alkyl which may be partially unsaturated and is optionally substituted by one or more substituents from the group R11, OR13, SR10, SR13, NR7R8, halo, (C = O) C1-7alkyl, or SOmR9, R6 is (a) C1-7alkyl, (b) NR7R8,(c) aryl or (d) het, where het is attached via a carbon atom; R7 and R8 are independently, (a) H, (b) aryl, (c) C1-7alkyl which may be partially unsaturated and is optionally substituted by one or more substituents selected from NR10R10, R11, SOmR9, CONR10R10, or halo or ; (d) R7 and R8 together with the nitrogen to which they are attached forming a het; R9 is (a) aryl, (b) het, (c) C3-8cycloalkyl, (d) methyl, or (e) C2-7alkyl which can be partially unsaturated and is optionally substituted by one or more substituents selected from NR10R10, R11, SH, CONR10R10, or halo; R10 is (a) H, (b) methyl, or (c) C2-7alkyl optionally substituted by OH;(2; (c) nnnnnnnnnnnnnnnnnnnn2; (c + (= O) arilo, O (E) C (= O) c1-7oquilo optional replacement Nr7r8, arilo, het, CO2H, and O (CH2) n2r14; R14 is (a) h, or (b) c1-7 tar; each n is an independent 1, 2, 3, 4, or 5; each m is an independent 0, 1, or 2; m is sodium, potassium, or lithium; arilo is a phenyl radical or a bi periodic carbon radical with at least one aromatic ring shaped;When an arilo is replaced by one or more alternatives selected from halo, oh, Ciano, co2r14, CF3, c1-6alcoxi and c1-6oqui, these alternatives can then be replaced by one to three sr14, nr14r14, or14 or co2r14, het is a four (4) heterocycle,5 (5) 6 (6) or 7 (7) saturated or unsaturated members, with 1, 2 or 3 different atoms selected from the oxygen, sulfur or Nitrosobenzene group, can choose to combine with benzene ring, or any heterocyclic or double cyclic group; Any of these HETS can be replaced by one or more alternatives selected from the group of halogenated substances, oh, Ciano, fenilo, co2r14, CF3, c1-6alcoxilo, oxo, oxima and c1-6oquilo, which can then be replaced by one or three sr14, nr14, or14 or co2r14, pharmaceutical ingredients, formulations,2. Methods of using antiretroviral drugs and inhibiting polymerase DNA virus;