5-substituted isoquinoline derivatives

A compound represented by the following formula (1) or a salt thereof:

• wherein R1 represents hydrogen atom, a halogen atom, hydroxyl group, amino group, or a C1-6 alkoxyl group;
• R2 represents hydrogen atom, a halogen atom, a C1-6 alkyl group, —(C2-3 alkylene)O(G1), —(C2-3 alkylene)CO2(G1), —N(G2)(G3), —O(C2-3 alkylene)O(G1), —NH(C2-3 alkylene)O(G1), —NH(C2-3 alkylene)N(G2)(G3), a C2-3 alkenyl group, a C2-3 alkynyl group, a C1-6 alkoxyl group, —(C2-3 alkylene)SO2(C1-6 alkyl), —S(O)p(C1-6 alkyl), —O(C2-3 alkylene)SO2(C1-6 alkyl), or cyano group;
• G1, G2, and G3 independently represent hydrogen atom, or a C1-6 alkyl group;
• p represents an integer of from 0 to 2;
• R3 represents a group represented by the following formula (1-1), formula (1-2), or formula (1-3);
• wherein
• (i) when R3 represents a group represented by the formula (1-1):
• R1 is hydrogen atom, hydroxyl group, or amino group;
• R2 is a C1-6 alkyl group, —(C2-8 alkylene )O(G1), a C2-8 alkenyl group, —S(O)p(C1-6 alkyl), or cyano group;
• X represents propylene group, butylene group, —C(A5)(A51)-, —C(A5)(A51)-C(A6)(A61)-, or a single bond;
• A11, A21, A51, and A61 independently represent hydrogen atom, or a C1-6 alkyl group;
• A31 represents a C1-6 alkyl group substituted with hydroxyl group, or hydrogen atom;
• and
• groups in each of one or more combinations selected from the group consisting of combinations of A3 and A2, A3 and A1, A3 and A5, A3 and A6, A2 and A1, A2 and A5, A2 and A6, A1 and A5, A1 and A6, and A5 and A6 bind to each other to form a 5- or 6-membered ring, provided that a group or groups among A1, A2, A3, A5, and A6 not involved in the ring formation independently represent hydrogen atom, or a C1-6 alkyl group;
• (ii) when R3 represents a group represented by the formula (1-2):
• X represents propylene group, butylene group, —C(A5)(A51)-, —C(A5)(A51)-C(A6)(A61)-, or a single bond;
• A11, A21, A51, and A61 independently represent hydrogen atom, or a C1-6 alkyl group;
• A31 represents a C1-6 alkyl group substituted with hydroxyl group, or hydrogen atom;
• R4 represents hydrogen atom, or a C1-6 alkyl group;
• and
• A1, A2, A3, A5, and A6 independently represent hydrogen atom, or a C1-6 alkyl group;
• or
• groups in each of one or more combinations selected from the group consisting of combinations of A3 and A2, A3 and A1, A3 and A5, A3 and A6, A2 and A1, A2 and A5, A2 and A6, A1 and A5, A1 and A6, and A5 and A6 may bind to each other to form a 5- or 6-membered ring;
• and
• (iii) when R3 represents a group represented by the formula (1-3):
• Y represents a C2-6 alkylene group, a C2-6 alkylene group substituted with a C1-6 alkyl group, a C2-6 alkylene group substituted with phenyl group, a C2-6 alkylene group substituted with benzyl group, —(C1-6 alkylene)phenylene(C1-6 alkylene)-, 1,2-cyclohexylene group, or 1,3-cyclohexylene group;
• A4 represents hydrogen atom, or a C1-6 alkyl group, or may binds to any one of carbon atoms of the alkylene moiety of Y to form a 4- to 7-membered ring;
• R5 represents —(C2-6 alkylene)(cycloalkyl), —(C2-6 alkylene)(aryl), —(C2-6 alkylene)(heteroaryl), —(C2-6 alkylene)S(O)q(cycloalkyl), —(C2-6 alkylene)S(O)q(aryl), —(C2-6 alkylene)S(O)q(heteroaryl), —(C2-6 alkylene)N(G6)(cycloalkyl), —(C2-6 alkylene)N(G6)(aryl), —(C2-6 alkylene)N(G6)(heteroaryl), —(C2-6alkylene)CON(G6)(cycloalkyl), —(C2-6 alkylene)CON(G6)(aryl), or —(C2-6 alkylene)CON(G6)(heteroaryl);
• G6 represents hydrogen atom, or a C1-6 alkyl group;
• q represents an integer of from 0 to 2;
• wherein aryl is a phenyl group which may be substituted with one or more substituents selected from the group consisting of a halogen atom, a C1-6 alkyl group, CF3 group, a C1-6 alkoxyl group, cyano group, —N(G7)(G8), —CO2(G9), —S(O)r(G9), and —N(G9)SO2(C1-6 alkyl);
• G9 represents hydrogen atom, or a C1-6 alkyl group;
• G7 and G8 independently represents hydrogen atom, or a C1-6 alkyl group, or —N(G7)(G8) in said “aryl” as a whole may form a 4- to 7-membered ring which may contain oxygen atom, sulfur atom, or an N(G10) group, besides said nitrogen atom;
• G10 represents hydrogen atom, or a C1-6 alkyl group;
• wherein heteroaryl is selected from pyranyl, pyrazinyl, dioxolyl, furyl, thienyl, pyridyl, pyrimidyl, pyridazinyl, tetrazolyl, pyrrolyl, oxazolyl, thiazolyl, isoxazolyl, isothiazolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, and triazolyl, and these groups may optionally be substituted with one or more substituents selected from the group consisting of a C1-6 alkyl group which may be substituted with a halogen atom, and a halogen atom;
• and
• r represents an integer of from 0 to 2.