Disclosed are a class of compounds having a highly selective inhibition of ROS1, and the use thereof in the preparation of drugs for treating diseases related to abnormal ROS1 kinase expression. Specifically disclosed are compounds represented by formula (IV) and a pharmaceutically acceptable salt thereof.

##STR00001##

The present disclosure relates to novel compounds for use in therapeutic treatment of a disease associated with peptidylarginine deiminases (PADs), such as peptidylarginine deiminase type 4 (PAD4). The present disclosure also relates to processes and intermediates for the preparation of such compounds, methods of using such compounds and pharmaceutical compositions comprising the compounds described herein.

The present invention provides a compound represented by Formula (I):

##STR00001##

wherein ring A is a substituted or unsubstituted heterocycle; ring C is a benzene ring or the like; R.sup.1 is halogen or the like; R.sup.2a and R.sup.2b are each independently hydrogen or the like; R.sup.3 is substituted or unsubstituted alkyl or the like; R.sup.4 is hydrogen or the like; and n is an integer of 1 to 3.

The present invention provides a compound represented by Formula (I):

##STR00001##

wherein ring A is a substituted or unsubstituted heterocycle; ring C is a benzene ring or the like; R.sup.1 is halogen or the like; R.sup.2a and R.sup.2b are each independently hydrogen or the like; R.sup.3 is substituted or unsubstituted alkyl or the like; R.sup.4 is hydrogen or the like; and n is an integer of 1 to 3.

Disclosed in the present invention are a fused pyridone compound, and a preparation method therefor and a use thereof. Specifically, the present invention discloses a compound of formula (I-B), an optical isomer thereof and a pharmaceutically acceptable salt thereof, and the use of the compound as a KRAS inhibitor.

##STR00001##

Disclosed in the present invention are a fused pyridone compound, and a preparation method therefor and a use thereof. Specifically, the present invention discloses a compound of formula (I-B), an optical isomer thereof and a pharmaceutically acceptable salt thereof, and the use of the compound as a KRAS inhibitor.

##STR00001##

This invention relates to macrocyclic deaza-purinones derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.

This invention relates to macrocyclic deaza-purinones derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.

The invention provides a compound of formula (0):

##STR00001## or a pharmaceutically acceptable salt, N-oxide or tautomer thereof; wherein: n is 1 or 2; X is CH or N; Y is selected from CH and C—F; Z is selected from C—R.sup.z and N; R.sup.1 is selected from: -(Alk.sup.1).sub.t-Cyc.sup.1; wherein t is 0 or 1; Optionally substituted C.sub.1-6 acyclic hydrocarbon groups R.sup.2 is selected from hydrogen; halogen; and C.sub.1-3 hydrocarbon groups optionally substituted with one or more fluorine atoms; R.sup.3 is hydrogen or a group L.sup.1-R.sup.7; R.sup.4 is selected from hydrogen; methoxy; and optionally substituted C.sub.1-3 alkyl; and R.sup.4a is selected from hydrogen and a C.sub.1-3 alkyl group; wherein R.sup.z, Alk.sup.1, Cyc.sup.1, L.sup.1 and R.sup.7 are defined herein; provided that the compound is other than 6-benzyl-3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and 3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and salts and tautomers thereof.

The compounds are inhibitors of ERK1/2 kinases and will be useful in the treatment of ERK1/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.

The invention provides a compound of formula (0):

##STR00001## or a pharmaceutically acceptable salt, N-oxide or tautomer thereof; wherein: n is 1 or 2; X is CH or N; Y is selected from CH and C—F; Z is selected from C—R.sup.z and N; R.sup.1 is selected from: -(Alk.sup.1).sub.t-Cyc.sup.1; wherein t is 0 or 1; Optionally substituted C.sub.1-6 acyclic hydrocarbon groups R.sup.2 is selected from hydrogen; halogen; and C.sub.1-3 hydrocarbon groups optionally substituted with one or more fluorine atoms; R.sup.3 is hydrogen or a group L.sup.1-R.sup.7; R.sup.4 is selected from hydrogen; methoxy; and optionally substituted C.sub.1-3 alkyl; and R.sup.4a is selected from hydrogen and a C.sub.1-3 alkyl group; wherein R.sup.z, Alk.sup.1, Cyc.sup.1, L.sup.1 and R.sup.7 are defined herein; provided that the compound is other than 6-benzyl-3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and 3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and salts and tautomers thereof.

The compounds are inhibitors of ERK1/2 kinases and will be useful in the treatment of ERK1/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.