7-OXO-THIAZOLOPYRIDINE CARBONIC ACID DERIVATIVES AND THEIR USE IN THE TREATMENT, AMELIORATION OR PREVENTION OF A VIRAL DISEASE

摘要

The present invention relates to a compound having the general formula (A), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof,;;which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.

主权项

1. A compound having formula (A) wherein R* —X1—R1; X1 is NR4; X2 is O, S or NR4; X3 is O or S; X4 is O or S; R1 is —SO2—R4; R2 is a hydrocarbon group which contains from 5 to 20 carbon atoms and optionally 1 to 4 heteroatoms selected from O, N and S and which contains at least one ring, wherein the hydrocarbon group can be optionally substituted; R3 is —H, -(optionally substituted C1-6 alkyl), -(optionally substituted C3-7 cycloalkyl), -(optionally substituted aryl), or —C1-4 alkyl-(optionally substituted aryl); or if X2 is NR4, then R3 can also be —OH; R4 is —H, -(optionally substituted C1-6 alkyl), -(optionally substituted C3-7 cycloalkyl), -(optionally substituted aryl), —C1-4 alkyl-(optionally substituted C3-7 cycloalkyl), or —C1-4 alkyl-(optionally substituted aryl); or R4 and R1 can be joined together to form a 5- to 7-membered ring, which can optionally contain O, S or further N; or if X2 is NR4, then R4 and R3 can be joined together to form a 5- to 7-membered ring, which can optionally contain O, S or further N; R5 is —H, -(optionally substituted C1-6 alkyl), -(optionally substituted C3-7 cycloalkyl), -(optionally substituted aryl), —C1-4 alkyl-(optionally substituted C3-7 cycloalkyl), or —C1-4 alkyl-(optionally substituted aryl); and R6 is —H or —C1-6 alkyl; wherein the optional substituent of the alkyl group is selected from the group consisting of halogen, —CN, —NR6R6, —OH, and —O—C1-6 alkyl; wherein the optional substituent of the cycloalkyl group, the aryl group or the hydrocarbon group is selected from the group consisting of —C1-6 alkyl, halogen, —CF3, —CN, —X1—R5 and —C1-4 alkyl-aryl; or a pharmaceutically acceptable salt, solvate, polymorph, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof; wherein, the prodrug is a compound where X2 is O or S, and R3 is one of the following groups: wherein R6 is the same or different, wherein R9 is aryl or C3-7 cycloalkyl, p is 2-8.