C07D491/113

Prodrugs of fumarates and their use in treating various diseases

The present invention provides compounds of formula (I), and pharmaceutical compositions thereof. ##STR00001##

Prodrugs of fumarates and their use in treating various diseases

The present invention provides compounds of formula (I), and pharmaceutical compositions thereof. ##STR00001##

Antiviral compounds highly effective as HCV-NS5A inhibitor
09820972 · 2017-11-21 · ·

Provided are compounds antiviral compounds represented by formula Ia and Ib: ##STR00001##
that are highly potent as HCV NS5A inhibitors, where the structural variables are as defined herein. These compounds are useful in, for example, inhibiting Hepatitis C virus and treating Hepatitis C virus infections.

Antiviral compounds highly effective as HCV-NS5A inhibitor
09820972 · 2017-11-21 · ·

Provided are compounds antiviral compounds represented by formula Ia and Ib: ##STR00001##
that are highly potent as HCV NS5A inhibitors, where the structural variables are as defined herein. These compounds are useful in, for example, inhibiting Hepatitis C virus and treating Hepatitis C virus infections.

Prodrugs of Fumarates and Their Use in Treating Various Diseases

The present invention provides compounds of formula (I),

##STR00001##

wherein:

R.sub.1 is unsubstituted C.sub.1-C.sub.6 alkyl;

L.sub.a is substituted or unsubstituted C.sub.1-C.sub.6 alkyl linker, substituted or unsubstituted C.sub.3-C.sub.10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and

R.sub.2 and R.sub.3 are each, independently, H, substituted or unsubstituted C.sub.1-C.sub.6 alkyl, or substituted or unsubstituted C.sub.6-C.sub.10aryl;

or alternatively, R.sub.2 and R.sub.3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S.

The invention also provides pharmaceutical compositions and methods for treating neurological diseases, such as multiple sclerosis.

Prodrugs of Fumarates and Their Use in Treating Various Diseases

The present invention provides compounds of formula (I),

##STR00001##

wherein:

R.sub.1 is unsubstituted C.sub.1-C.sub.6 alkyl;

L.sub.a is substituted or unsubstituted C.sub.1-C.sub.6 alkyl linker, substituted or unsubstituted C.sub.3-C.sub.10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and

R.sub.2 and R.sub.3 are each, independently, H, substituted or unsubstituted C.sub.1-C.sub.6 alkyl, or substituted or unsubstituted C.sub.6-C.sub.10aryl;

or alternatively, R.sub.2 and R.sub.3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S.

The invention also provides pharmaceutical compositions and methods for treating neurological diseases, such as multiple sclerosis.

Fluorene derivative or pharmaceutically acceptable salt thereof, preparation method therefor, and pharmaceutical composition comprising same as effective ingredient for preventing or treating HCV-related disease

The present invention relates to a fluorene derivative or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition comprising the same as an effective ingredient for preventing or treating HCV-related disease. A fluorene derivative according to the present invention is identified to exhibit an antiviral performance against not only HCV, but also highly against HCV mutants, particularly double mutants and thus can be used in a pharmaceutical composition for prevention or treatment of HCV-caused liver disease, such as acute hepatitis C, chronic hepatitis C, liver cirrhosis, hepatocellular cancer, etc., particularly, liver disease caused by mutants of HCV. The derivative can be useful in a pharmaceutical composition for prevention or treatment of HCV-related liver disease by which the problem of resistant mutation against conventional therapeutic agents is solved.

Fluorene derivative or pharmaceutically acceptable salt thereof, preparation method therefor, and pharmaceutical composition comprising same as effective ingredient for preventing or treating HCV-related disease

The present invention relates to a fluorene derivative or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition comprising the same as an effective ingredient for preventing or treating HCV-related disease. A fluorene derivative according to the present invention is identified to exhibit an antiviral performance against not only HCV, but also highly against HCV mutants, particularly double mutants and thus can be used in a pharmaceutical composition for prevention or treatment of HCV-caused liver disease, such as acute hepatitis C, chronic hepatitis C, liver cirrhosis, hepatocellular cancer, etc., particularly, liver disease caused by mutants of HCV. The derivative can be useful in a pharmaceutical composition for prevention or treatment of HCV-related liver disease by which the problem of resistant mutation against conventional therapeutic agents is solved.

Fused ring compounds as hepatitis C virus inhibitors, pharmaceutical compositions and uses thereof

Provided are fused tricyclic compounds effective to inhibit the function of the NS5A protein of formula (I), wherein X, X′, Y, Y′, A, A′, Q.sup.1, Q.sup.2, R.sup.1-R.sup.4, X.sup.4, R.sup.5a, f and W are defined as in the description. Also provided herein are pharmaceutical compositions thereof, and uses in the manufacture of a medicament for treating HCV infection or a HCV disorder thereof. ##STR00001##

Fused ring compounds as hepatitis C virus inhibitors, pharmaceutical compositions and uses thereof

Provided are fused tricyclic compounds effective to inhibit the function of the NS5A protein of formula (I), wherein X, X′, Y, Y′, A, A′, Q.sup.1, Q.sup.2, R.sup.1-R.sup.4, X.sup.4, R.sup.5a, f and W are defined as in the description. Also provided herein are pharmaceutical compositions thereof, and uses in the manufacture of a medicament for treating HCV infection or a HCV disorder thereof. ##STR00001##