Double-headed protease inhibitor

2:

• The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein
• A1 and A2 each independently represent an inhibitor residue formed by removing any one hydrogen atom or any one hydroxy group from an inhibitor molecule selected from the following inhibitor molecule group:
• or an inhibitor molecule represented by the following general formula (II):
• wherein:
• ring B and ring C each independently represent an aryl group or a heteroaryl group;
• R1 each independently represents a hydrogen atom or a —COO—(C1-C4 alkyl group);
• W represents a single bond or a C1-C4 alkylene group;
• X represents —C(═O)—, —O—C(═O)—, or —NG-SO2—;
• G represents a hydrogen atom, a C1-C4 alkyl group, or —COOR2;
• R2 represents a C1-C4 alkyl group optionally substituted with 1 to 5 aryl group(s);
• Y represents —NG2G4, —NG2-L1-COOH, —NG2-L1-C(═O)—NH2, —NG2-L1-C(═O)-NG3-L2-COOH, —NG2-L1-C(═O)—NG3-L2-C(═O)—NG3-L2-COOH, —NG2-L1-C(═O)—NG3-L2-C(═O)—NH2, —NG2-L3-OH, or —NG2-(CH2—CH2—O)q—CH2—CH2—COOH;
• q represents an integer of 1 to 6;
• G2 and G3 each independently represent a hydrogen atom, or a C1-C6 alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from the group consisting of a phenyl group optionally substituted with 1 to 5 —COOR3 group(s) and a —COOR3 group;
• G4 represents a hydrogen atom, a C1-C4 alkyl group, or a C1-C4 alkoxy-C1-C4 alkyl group;
• R3 each independently represents a hydrogen atom or a C1-C4 alkyl group optionally substituted with 1 to 5 aryl group(s);
• L1 and L2 each independently represent a C1-C6 alkylene group optionally substituted with 1 to 5 C1-C6 alkyl group(s) optionally substituted with 1 to 5 —COOR4 group(s), a C1-C6 alkylene group substituted with a C7-C12 aralkyl group optionally substituted with 1 to 5 substituent(s) independently selected from the group consisting of a hydroxy group and a carboxy group, a C1-C4 alkylene-phenylene group, or a phenylene-C1-C4 alkylene group;
• L3 represents a C1-C4 alkylene-phenylene group wherein the phenylene moiety is optionally substituted with 1 to 3 —COOR4 group(s);
• R4 each independently represents a hydrogen atom or a C1-C4 alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from the group consisting of an aryl group and a trimethylsilyl group;
• R5 and R6 each independently represent a hydrogen atom, a halogen atom, a C1-C4 alkyl group, a C1-C4 alkoxy group, a carboxy group, or —C(═O)—NG2G4;
• s and t each independently represent an integer of 1 to 4;
• two or more R5 and/or two or more R6 may be the same or different with each other;
• or
• any one of R5 and any one of R6 may be combined with each other to form a C1-C4 alkyleneoxy group;
• and
• Z represents a single bond, an arylene group, a heteroarylene group, or a C2-C30 alkylene group, provided that one or more methylene group(s) in the chain of said alkylene group may be replaced with group(s) independently selected from the group consisting of —C(═O)—, —NR7—, —O—, —SiR8R9-, —SOr—, an arylene group, and a heteroarylene group, R7 represents a hydrogen atom or a C1-C4 alkyl group, R8 and R9 each independently represent a C1-C4 alkyl group, and r represents an integer of 0 to 2.

4:

• The compound according to claim 2 or a pharmaceutically acceptable salt thereof, wherein
• A1 has a structure represented by;
• A2 has a structure represented by
• wherein:
• ring B1, ring B2, ring C1, and ring C2 each independently represent an aryl group;
• R1 each independently represents a hydrogen atom or a —COO—(C1-C4 alkyl group);
• W1 and W2 each independently represent a single bond or a C1-C4 alkylene group;
• X1 represents —C(═O)—, —O—C(═O)—, or —NG11-SO2—;
• X1′ represents —NGZ-SO2—;
• X2 represents —C(═O)—, —C(═O)—O—, or —SO2—NG12-;
• X2′ represents —SO2—NGZ-;
• G11 and G12 each independently represent a hydrogen atom, a C1-C4 alkyl group, or —COOR2;
• Z represents a single bond that links X1′ or X2′ to Z;
• R2 represents a C1-C4 alkyl group optionally substituted with 1 to 5 aryl group(s);
• Y1 represents —NG21-, —NG21-L11-C(═O)—, —NG21-L11-C(═O)—NH—, —NG21-L11-C(═O)—NG31-L21-C(═O)—, —NG21-L11-C(═O)—NG31-L21-C(═O)—NH—, —NG21-L3-O—, or -NG21-G4′-;
• Y1′ represents —NG21H, —NG21-L11-COOH, or —NG21-L11-C(═O)—NG31-L21-COOH;
• Y2 represents —NG22-, —C(═O)-L12-NG22-, —NH—C(═O)-L12-NG22-, —C(═O)-L22-NG32-C(═O)-L12-NG22-, —NH—C(═O)-L22-NG32-C(═O)-L12-NG22-, —O-L3-NG22-, or -G4′-NG22-;
• Y2′ represents HNG22-, HOOC-L12-NG22-, or HOOC-L22-NG32-C(═O)-L12-NG22-;
• G21, G31, G22, and G32 each independently represent a hydrogen atom, or a C1-C6 alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from the group consisting of a phenyl group optionally substituted with 1 to 5 —COOR3 group(s) and a —COOR3 group;
• G4′ represents a C1-C4 alkylene group or a C1-C4 alkyleneoxy-C1-C4 alkylene group;
• R3 each independently represents a hydrogen atom or a C1-C4 alkyl group optionally substituted with 1 to 5 aryl group(s);
• L11, L21, L12, and L22 each independently represent a C1-C6 alkylene group optionally substituted with 1 to 5 C1-C6 alkyl group(s) optionally substituted with 1 to 5 —COOR4 group(s), a C1-C4 alkylene-phenylene group, or a phenylene-C1-C4 alkylene group;
• L3 represents a C1-C4 alkylene-phenylene group wherein the phenylene moiety is optionally substituted with 1 to 3 —COOR4 group(s);
• R4 each independently represents a hydrogen atom or a C1-C4 alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from the group consisting of an aryl group and a trimethylsilyl group;
• R5 and R6 each independently represent a hydrogen atom, a halogen atom, a C1-C4 alkyl group, or a C1-C4 alkoxy group;
• s and t each independently represent an integer of 1 to 4;
• two or more R5 and/or two or more R6 may be the same or different with each other;
• or any one of R5 and any one of R6 may be combined with each other to form a C1-C4 alkyleneoxy group;
• and
• the symbol
• represents the point of attachment to Z;
• and
• Z represents a single bond, an arylene group, a heteroarylene group, or a C2-C30 alkylene group, provided that one or more methylene group(s) in the chain of said alkylene group may be replaced with group(s) independently selected from the group consisting of —C(═O)—, —NR7—, —O—, an arylene group, and a heteroarylene group, and R7 represents a hydrogen atom or a C1-C4 alkyl group.

5:

• The compound according to claim 4 or a pharmaceutically acceptable salt thereof, wherein
• A1 has a structure represented by;
• A2 has a structure represented by
• Z represents a single bond, a C6-C12 arylene group, —(CH2—CH2—O)m—CH2—CH2—, —(CH2—O—CH2)m—, —(CH2)m—(C6-C12 arylene)-(CH2)m—, or —(CH2)n—;
• m represents an integer of 1 to 6;
• and
• n represents an integer of 2 to 12.

6:

• The compound according to claim 4 or a pharmaceutically acceptable salt thereof, wherein
• A1 has a structure represented by;
• and
• A2 has a structure represented by

7:

• The compound according claim 4 or a pharmaceutically acceptable salt thereof, wherein
• A1 has a structure represented by;
• and
• A2 has a structure represented by;

9:

• The compound according to claim 8 or a pharmaceutically acceptable salt thereof, wherein
• R1 each independently represents a hydrogen atom or a tert-butoxycarbonyl group;
• W1 and W2 each independently represent a single bond or a C1-C4 alkylene group;
• X1 represents —C(═O)—, —O—C(═O)—, or —NG11-SO2—;
• X1′ represents —NGZ-SO2—;
• X2 represents —C(═O)—, —C(═O)—O—, or —SO2—NG12-;
• X2′ represents —SO2—NGZ-;
• G11 and G12 each independently represent a hydrogen atom, a C1-C4 alkyl group, or —COOR2;
• GZ represents a single bond that links X1′ or X2′ to Z;
• R2 represents a C1-C4 alkyl group optionally substituted with 1 to 5 aryl group(s);
• Y1 represents —NG21-, —NG21-L11-C(═O)—, —NG21-L11-C(═O)—NH—, —NG21-L11-C(═O)—NG31-L21-C(═O)—, —NG21-L11-C(═O)—NG31-L21-C(═O)—NH—, —NG21-L3-O—, or -NG21-G4′-;
• Y1′ represents —NG21H, —NG21-L11-COOH, or —NG21-L11-C(═O)—NG31-L21-COOH;
• Y2 represents —NG22-, —C(═O)-L12-NG22-, —NH—C(═O)-L12-NG22-, —C(═O)-L22-NG32-C(═O)-L12-NG22-, —NH—C(═O)-L22-NG32-C(═O)-L12-NG22-, —O-L3-NG22-, or -G4′-NG22-;
• Y2′ represents HNG22-, HOOC-L12-NG22-, or HOOC-L22-NG32-C(═O)-L12-NG22-;
• G21, G31, G22, and G32 each independently represent a hydrogen atom, or a C1-C6 alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from the group consisting of a phenyl group optionally substituted with 1 to 5 —COOR3 group(s) and a —COOR3 group;
• G4′ represents a C1-C4 alkylene group or a C1-C4 alkyleneoxy-C1-C4 alkylene group;
• R3 each independently represents a hydrogen atom, a benzyl group, or a tert-butyl group;
• L11, L21, L12, and L22 each independently represent a C1-C6 alkylene group optionally substituted with 1 to 5 C1-C6 alkyl group(s) optionally substituted with 1 to 5 —COOR4 group(s), a C1-C4 alkylene-phenylene group, or a phenylene-C1-C4 alkylene group;
• L3 represents a C1-C4 alkylene-phenylene group wherein the phenylene moiety is optionally substituted with 1 to 3 —COOR4 group(s);
• R4 each independently represents a hydrogen atom, a benzyl group, a 2-(trimethylsilyl)ethyl group, or a tert-butyl group;
• R5 and R6 each independently represent a hydrogen atom, a halogen atom, a C1-C4 alkyl group, or a C1-C4 alkoxy group;
• each R5 may be the same or different with each other;
• Z represents a single bond, a C6-C12 arylene group, —(CH2—CH2—O)m—CH2—CH2—, —(CH2—O—CH2)m—, —(CH2)m—(C6-C12 arylene)-(CH2)m—, or —(CH2)n—;
• m represents an integer of 1 to 6;
• and
• n represents an integer of 2 to 12.

10:

• The compound according to claim 9 or a pharmaceutically acceptable salt thereof, wherein
• R1 each independently represents a hydrogen atom or a tert-butoxycarbonyl group;
• W1 and W2 each independently represent a single bond or a C1-C4 alkylene group;
• X1 represents —C(═O)—, —O—C(═O)—, or —NG11-SO2—;
• X1′ represents —NGZ-SO2—;
• X2 represents —C(═O)—, —C(═O)—O—, or —SO2—NG12-;
• X2′ represents —SO2—NGZ-;
• G11 and G12 each independently represent a hydrogen atom, a C1-C4 alkyl group, or —COOR2;
• GZ represents a single bond that links X1′ or X2′ to Z;
• R2 represents a C1-C4 alkyl group optionally substituted with 1 to 3 aryl group(s);
• Y1 represents —NG21-, —NG21-L11-C(═O)—, —NG21-L11-C(═O)—NH—, —NG21-L11-C(═O)—NG31-L21-C(═O)—, —NG21-L11-C(═O)—NG31-L21-C(═O)—NH—, or —NG21-L3-O—;
• Y1′ represents —NG21H, —NG21-L11-COOH, or —NG21-L11-C(═O)—NG31-L21-COOH;
• Y2 represents —NG22-, —C(═O)-L12-NG22-, —NH—C(═O)-L12-NG22-, —C(═O)-L22-NG32-C(═O)-L12-NG22-, —NH—C(═O)-L22-NG32-C(═O)-L12-NG22-, or —O-L3-NG22-;
• Y2′ represents HNG22-, HOOC-L12-NG22-, or HOOC-L22-NG32-C(═O)-L12-NG22-;
• G21, G31, G22, and G32 each independently represent a hydrogen atom, or a C1-C6 alkyl group optionally substituted with 1 to 3 substituent(s) independently selected from the group consisting of a phenyl group optionally substituted with 1 to 3 —COOR3 group(s) and a —COOR3 group;
• R3 each independently represents a hydrogen atom, a benzyl group, or a tert-butyl group;
• L11, L21, L12, and L22 each independently represent a C1-C6 alkylene group optionally substituted with 1 to 5 C1-C6 alkyl group(s) optionally substituted with 1 to 5 —COOR4 group(s), a C1-C4 alkylene-phenylene group, or a phenylene-C1-C4 alkylene group;
• L3 represents a C1-C2 alkylene-phenylene group wherein the phenylene moiety is optionally substituted with 1 to 2 —COOR4 group(s);
• R4 each independently represents a hydrogen atom, a benzyl group, a 2-(trimethylsilyl)ethyl group, or a tert-butyl group;
• R5 and R6 each independently represent a hydrogen atom, a halogen atom, a C1-C4 alkyl group, or a C1-C4 alkoxy group;
• each R5 may be the same or different with each other;
• Z represents a single bond, a biphenylene group, —(CH2—CH2—O)m—CH2—CH2—, —(CH2—O—CH2)m—, —(CH2)m-biphenylene-(CH2)m—, or —(CH2)n—;
• m represents an integer of 1 to 6;
• and
• n represents an integer of 2 to 12.

11:

• The compound according to claim 10 or a pharmaceutically acceptable salt thereof, wherein
• R1 each represents a hydrogen atom;
• W1 and W2 each independently represent a single bond or a C1-C4 alkylene group;
• X1 represents —C(═O)— or —NG11-SO2—;
• X1′ represents —NGZ-SO2—;
• X2 represents —C(═O)— or —SO2—NG12-;
• X2′ represents —SO2—NGZ-;
• G11 and G12 each independently represent a hydrogen atom or —COOR2;
• GZ represents a single bond that links X1′ or X2′ to Z;
• R2 represents a C1-C4 alkyl group optionally substituted with one phenyl group;
• Y1 represents —NG21-;
• Y1′ represents —NG21H;
• Y2 represents —NG22-;
• Y2′ represents HNG22-;
• G21 and G22 each independently represent a hydrogen atom, or a C1-C3 alkyl group substituted with 1 to 3 carboxy group(s);
• R5 and R6 each independently represent a hydrogen atom, a fluorine atom, a methyl group, or a methoxy group;
• each R5 may be the same or different with each other;
• Z represents a single bond, [1,1′-biphenyl]-3,3′-diyl, —(CH2—CH2—O)m—CH2—CH2—, —(CH2—O—CH2)m—, —(CH2)m—([1,1′-biphenyl]-3,3′-diyl)-(CH2)m—, or —(CH2)n—;
• m represents an integer of 1 to 6;
• and
• n represents an integer of 2 to 12.

12:

• The compound according to claim 4 represented by the following formula (V):
• wherein:
• R1 each independently represents a hydrogen atom or a —COO—(C1-C4 alkyl group);
• W1 and W2 each independently represent a single bond or a C1-C4 alkylene group;
• X1 represents —C(═O)— or —NG11-SO2—;
• X2 represents —C(═O)— or —SO2—NG12-;
• G11 and G12 each independently represent a hydrogen atom, a C1-C4 alkyl group, or —COOR2;
• R2 represents a C1-C4 alkyl group optionally substituted with 1 to 5 aryl group(s);
• Y1 represents —NG21-, —NG21-L11-C(═O)—, —NG21-L11-C(═O)—NH—, —NG21-L11-C(═O)—NG31-L21-C(═O)—, —NG21-L11-C(═O)—NG31-L21-C(═O)—NH—, —NG21-L3-O—, or -NG21-G4′-;
• Y2 represents —NG22-, —C(═O)-L12-NG22-, —NH—C(═O)-L12-NG22-, —C(═O)-L22-NG32-C(═O)-L12-NG22-, —NH—C(═O)-L22-NG2-C(═O)-L12-NG22-, —O-L3-NG22-, or -G4′-NG22-;
• G21, G31, G22, and G32 each independently represent a hydrogen atom, or a C1-C6 alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from the group consisting of a phenyl group optionally substituted with 1 to 5 —COOR3 group(s) and a —COOR3 group;
• G4′ represents a C1-C4 alkylene group or a C1-C4 alkyleneoxy-C1-C4 alkylene group;
• R3 each independently represents a hydrogen atom or a C1-C4 alkyl group optionally substituted with 1 to 5 aryl group(s);
• L11, L21, L12, and L22 each independently represent a C1-C6 alkylene group optionally substituted with 1 to 5 C1-C6 alkyl group(s) optionally substituted with 1 to 5 —COOR4 group(s), a C1-C4 alkylene-phenylene group, or a phenylene-C1-C4 alkylene group;
• L3 represents a C1-C4 alkylene-phenylene group wherein the phenylene moiety is optionally substituted with 1 to 3 —COOR4 group(s);
• R4 each independently represents a hydrogen atom or a C1-C4 alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from the group consisting of an aryl group and a trimethylsilyl group;
• R5 each independently represents a hydrogen atom, a halogen atom, a C1-C4 alkyl group, or a C1-C4 alkoxy group;
• Z represents a single bond, a C6-C12 arylene group, —(CH2—CH2—O)m—CH2—CH2— —(CH2—O—CH2)m—, —(CH2)m—(C6-C12 arylene)-(CH2)m—, or —(CH2)n—;
• m represents an integer of 1 to 6;
• and
• n represents an integer of 2 to 12,
• or a pharmaceutically acceptable salt thereof.

14:

• The compound according to claim 13 or a pharmaceutically acceptable salt thereof, wherein
• R1 each independently represents a hydrogen atom or a tert-butoxycarbonyl group;
• W1 and W2 each independently represent a single bond or a C1-C2 alkylene group;
• X1 represents —C(═O)— or —NG11-SO2—;
• X2 represents —C(═O)— or —SO2—NG12-;
• G11 and G12 each represent a hydrogen atom;
• Y1 represents —NG21-, —NG21-L11-C(═O)—, —NG21-L11-C(═O)—NH—, —NG21-L11-C(═O)—NG31-L21-C(═O)—, —NG21-L11-C(═O)—NG31-L21-C(═O)—NH—, —NG21-L3-O—, or -NG21-G4′-;
• Y2 represents —NG22-, —C(═O)-L12-NG22-, —NH—C(═O)-L12-NG22-, —C(═O)-L22-NG32-C(═O)-L12-NG22-, —NH—C(═O)-L22-NG32-C(═O)-L12-NG22-, —O-L3-NG22-, or -G4′-NG22-;
• G21, G31, G22, and G32 each independently represent a hydrogen atom, or a C1-C3 alkyl group optionally substituted with 1 to 3 —COOR3 group(s);
• G4′ represents a C1-C2 alkylene group or a C1-C2 alkyleneoxy-C1-C2 alkylene group;
• R3 each independently represents a hydrogen atom or a tert-butyl group;
• L11, L21, L12, and L22 each independently represent a C1-C2 alkylene group;
• L3 represents a C1-C4 alkylene-phenylene group wherein the phenylene moiety is optionally substituted with 1 to 3 —COOR4 group(s);
• R4 each independently represents a hydrogen atom or a C1-C4 alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from the group consisting of an aryl group and a trimethylsilyl group;
• R5 each independently represents a hydrogen atom, a halogen atom, a C1-C4 alkyl group, or a C1-C4 alkoxy group;
• Z represents a single bond, a biphenylene group, —(CH2—CH2—O)m—CH2—CH2—, —(CH2—O—CH2)m—, —(CH2)m-biphenylene-(CH2)m—, or —(CH2)n—;
• m represents an integer of 1 to 6;
• and
• n represents an integer of 2 to 12.

15:

• The compound according to claim 14 or a pharmaceutically acceptable salt thereof, wherein
• R1 each represents a hydrogen atom;
• W1 and W2 each represent a single bond;
• X1 represents —C(═O)—;
• X2 represents —C(═O)—;
• Y1 represents —NG21-, —NG21-L3-O—, or —NG21-G4′-;
• Y2 represents —NG22-, —O-L3-NG22-, or -G4′-NG22-;
• G21 and G22 each independently represent a C1-C3 alkyl group substituted with 1 to 3 carboxy group(s);
• G4′ represents a C1-C2 alkylene group or a C1-C2 alkyleneoxy-C1-C2 alkylene group;
• L3 represents a C1-C2 alkylene-phenylene group wherein the phenylene moiety is optionally substituted with 1 to 2 —COOR4 group(s);
• R4 each independently represents a hydrogen atom or a C1-C4 alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from the group consisting of an aryl group and a trimethylsilyl group;
• R5 each independently represents a hydrogen atom, a fluorine atom, a methyl group, or a methoxy group;
• Z represents a single bond, [1,1′-biphenyl]-3,3′-diyl, —(CH2—CH2—O)m—CH2—CH2—, —(CH2—O—CH2)m—, —(CH2)m—([1,1′-biphenyl]-3,3′-diyl)-(CH2)m—, or —(CH2)n—;
• m represents an integer of 1 to 6;
• and
• n represents an integer of 2 to 12.

16:

• The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein
• A1 has a structure represented by:
• and
• A2 has a structure represented by
• wherein
• R1 each independently represents a hydrogen atom or a —COO—(C1-C4 alkyl group);
• W1 and W2 each independently represent a single bond or a C1-C4 alkylene group;
• X1 represents —C(═O)—, —O—C(═O)—, or —NG11-SO2—;
• X2 represents —C(═O)—, —C(═O)—O—, or —SO2—NG12-;
• G1 1 and G12 each independently represent a hydrogen atom or —COOR2;
• R2 represents a C1-C4 alkyl group optionally substituted with 1 to 5 aryl group(s);
• Y1 represents —NG21-, —NG21-L11-C(═O)—NH—, or —NG21-L11-C(═O)—NG31-L21-C(═O)—NH—;
• Y2 represents —NG22-, —NH—C(═O)-L12-NG22-, or —NH—C(═O)-L22-NG32-C(═O)-L12-NG22-;
• G21, G31, G22, and G32 each independently represent a hydrogen atom, or a C1-C6 alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from the group consisting of a phenyl group optionally substituted with 1 to 5 —COOR3 group(s) and a —COOR3 group;
• R3 each independently represents a hydrogen atom or a C1-C4 alkyl group optionally substituted with 1 to 5 aryl group(s);
• L11, L21, L12, and L22 each independently represent a C1-C6 alkylene group optionally substituted with 1 to 5 C1-C6 alkyl group(s) optionally substituted with 1 to 5 —COOR4 group(s), a C1-C4 alkylene-phenylene group, or a phenylene-C1-C4 alkylene group;
• R4 each independently represents a hydrogen atom or a C1-C4 alkyl group optionally substituted with 1 to 5 aryl group(s);
• R5 and R6 each independently represent a hydrogen atom, a C1-C4 alkyl group, or a C1-C4 alkoxy group, or R5 and R6 may be combined with each other to form a C1-C4 alkyleneoxy group;
• and
• the symbol
• represents the point of attachment to Z,
• Z represents —(CH2—CH2—O)m—CH2—CH2— or —(CH2)n—;
• m represents an integer of 1 to 6;
• and
• n represents an integer of 2 to 12.

18:

• The compound according to claim 1, represented by the following formula (VII):
• wherein:
• R1 each independently represents a hydrogen atom or a —COO—(C1-C4 alkyl group);
• W1 and W2 each independently represent a single bond or a C1-C4 alkylene group;
• X1 represents —O—C(═O)— or —NG11-SO2—;
• X2 represents —C(═O)—O— or —SO2—NG12-;
• G1 1 and G12 each independently represent a hydrogen atom or —COOR2;
• R2 represents a C1-C4 alkyl group optionally substituted with 1 to 5 aryl group(s);
• Y1 represents —NG21-, —NG21-L11-C(═O)—NH—, or —NG21-L11-C(═O)—NG31-L21-C(═O)—NH—;
• Y2 represents —NG22-, —NH—C(═O)-L12-NG22-, or —NH—C(═O)-L22-NG32-C(═O)-L12-NG22-;
• G21, G31, G22, and G32 each independently represent a hydrogen atom, or a C1-C6 alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from the group consisting of a phenyl group optionally substituted with 1 to 5 —COOR3 group(s) and a —COOR3 group;
• R3 each independently represents a hydrogen atom or a C1-C4 alkyl group optionally substituted with 1 to 5 aryl group(s);
• L11, L21, L12, and L22 each independently represent a C1-C6 alkylene group optionally substituted with 1 to 5 C1-C6 alkyl group(s) optionally substituted with 1 to 5 —COOR4 group(s), a C1-C4 alkylene-phenylene group, or a phenylene-C1-C4 alkylene group;
• R4 each independently represents a hydrogen atom or a C1-C4 alkyl group optionally substituted with 1 to 5 aryl group(s);
• Z represents —(CH2—CH2—O)m—CH2—CH2— or —(CH2)n—;
• m represents an integer of 1 to 6;
• and
• n represents an integer of 2 to 12,
• or a pharmaceutically acceptable salt thereof.

19:

• The compound according to claim 18 or a pharmaceutically acceptable salt thereof, wherein
• R1 each independently represents a hydrogen atom or a tert-butoxycarbonyl group;
• W1 and W2 each represent a C1-C4 alkylene group;
• X1 represents —O—C(═O)— or —NG11-SO2—;
• X2 represents —C(═O)—O— or —SO2—NG12-;
• G1 1 and G12 each independently represent a hydrogen atom or —COOR2;
• R2 represents a C1-C4 alkyl group optionally substituted with 1 to 3 phenyl group(s);
• Y1 represents —NG21-, —NG21-L11-C(═O)—NH—, or —NG21-L11-C(═O)—NG31-L21-C(═O)—NH—;
• Y2 represents —NG22-, —NH—C(═O)-L12-NG22-, or —NH—C(═O)-L22-NG32-C(═O)-L12-NG22-;
• G21, G31, G22 and G32 each independently represent a hydrogen atom, or a C1-C6 alkyl group optionally substituted with 1 to 3 substituent(s) independently selected from the group consisting of a phenyl group optionally substituted with 1 to 3 —COOR3 group(s) and a —COOR3 group;
• R3 each independently represents a hydrogen atom, a benzyl group, or a tert-butyl group;
• L11, L21, L1 2, and L22 each independently represent a C1-C6 alkylene group optionally substituted with 1 to 5 C1-C6 alkyl group(s) optionally substituted with 1 to 5 —COOR4 group(s), a C1-C4 alkylene-phenylene group, or a phenylene-C1-C4 alkylene group;
• R4 each independently represents a hydrogen atom, a benzyl group, or a tert-butyl group;
• Z represents —(CH2—CH2—O)m—CH2—CH2— or —(CH2)n—;
• m represents an integer of 1 to 6;
• and
• n represents an integer of 2 to 12.

20:

• The compound according to claim 19 or a pharmaceutically acceptable salt thereof, wherein
• R1 each independently represents a hydrogen atom or a tert-butoxycarbonyl group;
• W1 and W2 each represent a C1-C2 alkylene group;
• X1 represents —O—C(═O)— or —NG11-SO2—;
• X2 represents —C(═O)—O— or —SO2—NG12-;
• G1 1 and G12 each independently represent a hydrogen atom or —COOR2;
• R2 represents a C1-C4 alkyl group optionally substituted with one phenyl group;
• Y1 represents —NG21-, —NG21-L11-C(═O)—NH—, or —NG21-L11-C(═O)—NG31-L21-C(═O)—NH—;
• Y2 represents —NG22-, —NH—C(═O)-L12-NG22-, or —NH—C(═O)-L22-NG32-C(═O)-L12-NG22-;
• G21, G31, G22, and G32 each independently represent a hydrogen atom, or a C1-C3 alkyl group optionally substituted with 1 to 3 substituent(s) independently selected from the group consisting of a phenyl group optionally substituted with one —COOR3 group and a —COOR3 group;
• R3 each independently represents a hydrogen atom or a tert-butyl group;
• L11, L21, L12, and L22 each independently represent a C1-C2 alkylene group optionally substituted with 1 to 2 C1-C2 alkyl group(s) optionally substituted with 1 to 2 —COOR4 group(s), a C1-C2 alkylene-phenylene group, or a phenylene-C1-C2 alkylene group;
• R4 each independently represents a hydrogen atom or a tert-butyl group;
• Z represents —(CH2—CH2—O)m—CH2—CH2— or —(CH2)n—;
• m represents an integer of 1 to 6;
• and
• n represents an integer of 2 to 12.

21:

• The compound according to claim 20 or a pharmaceutically acceptable salt thereof, wherein
• R1 each represents a hydrogen atom;
• W1 and W2 each represent a C1-C2 alkylene group;
• X1 represents —NG11-SO2—;
• X2 represents —SO2—NG12-;
• G1 1 and G12 each independently represent a hydrogen atom or —COOR2;
• R2 represents a C1-C4 alkyl group optionally substituted with one phenyl group;
• Y1 represents —NG21-;
• Y2 represents —NG22-;
• G21 and G22 each independently represent a C1-C3 alkyl group substituted with 1 to 3 substituent(s) independently selected from the group consisting of a phenyl group substituted with one carboxy group and a carboxy group;
• Z represents —(CH2—CH2—O)m—CH2—CH2— or —(CH2)n—;
• m represents an integer of 1 to 6;
• and
• n represents an integer of 2 to 12.

22:

• The compound according to claim 1 represented by the following formula (VIII):
• wherein:
• R1 each independently represents a hydrogen atom or a —COO—(C1-C4 alkyl group);
• W1 and W2 each independently represent a single bond or a C1-C4 alkylene group;
• X1 represents —C(═O)— or —NG11-SO2—;
• X2 represents —C(═O)— or —SO2—NG12-;
• G11 and G12 each independently represent a hydrogen atom or —COOR2;
• R2 represents a C1-C4 alkyl group optionally substituted with 1 to 5 aryl group(s);
• Y1 represents —NG21-, —NG21-L11-C(═O)—NH—, or —NG21-L11-C(═O)—NG31-L21-C(═O)—NH—;
• Y2 represents —NG22-, —NH—C(═O)-L12-NG22-, or —NH—C(═O)-L22-NG32-C(═O)-L12-NG22-;
• G21, G31, G22, and G32 each independently represent a hydrogen atom, or a C1-C6 alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from the group consisting of a phenyl group optionally substituted with 1 to 5 —COOR3 group(s) and a —COOR3 group;
• R3 each independently represents a hydrogen atom or a C1-C4 alkyl group optionally substituted with 1 to 5 aryl group(s);
• L11, L21, L12, and L22 each independently represent a C1-C6 alkylene group optionally substituted with 1 to 5 C1-C6 alkyl group(s) optionally substituted with 1 to 5 —COOR4 group(s), a C1-C4 alkylene-phenylene group, or a phenylene-C1-C4 alkylene group;
• R4 each independently represents a hydrogen atom or a C1-C4 alkyl group optionally substituted with 1 to 5 aryl group(s);
• Z represents —(CH2—CH2—O)m—CH2—CH2— or —(CH2)n—;
• m represents an integer of 1 to 6;
• and
• n represents an integer of 2 to 12,
• or a pharmaceutically acceptable salt thereof.

23:

• The compound according to claim 22 or a pharmaceutically acceptable salt thereof, wherein
• R1 each independently represents a hydrogen atom or a tert-butoxycarbonyl group;
• W1 and W2 each independently represent a single bond or a C1-C2 alkylene group;
• X1 represents —C(═O)— or —NG11-SO2—;
• X2 represents —C(═O)— or —SO2—NG12-;
• G11 and G12 each represent a hydrogen atom;
• Y1 represents —NG21-, —NG21-L11-C(═O)—NH—, or —NG21-L11-C(═O)—NG31-L21-C(═O)—NH—;
• Y2 represents —NG22-, —NH—C(═O)-L12-NG22-, or —NH—C(═O)-L22-NG32-C(═O)-L12-NG22-;
• G21, G31, G22, and G32 each independently represent a hydrogen atom, or a C1-C3 alkyl group optionally substituted with 1 to 3 —COOR3 group(s);
• R3 each independently represents a hydrogen atom or a tert-butyl group;
• L11, L21, L12, and L22 each independently represent a C1-C2 alkylene group;
• Z represents —(CH2—CH2—O)m—CH2—CH2— or —(CH2)n—;
• m represents an integer of 1 to 6;
• and
• n represents an integer of 2 to 12.

24:

• The compound according to claim 23 or a pharmaceutically acceptable salt thereof, wherein
• R1 each represents a hydrogen atom;
• W1 and W2 each represent a single bond;
• X1 represents —C(═O)—;
• X2 represents —C(═O)—;
• Y1 represents —NG21-;
• Y2 represents —NG22-;
• G21 and G22 each independently represent a C1-C3 alkyl group substituted with 1 to 3 carboxy group(s);
• Z represents —(CH2—CH2—O)m—CH2—CH2—;
• and
• m represents an integer of 1 to 6.

25:

• The compound according to claim 1, selected from the group consisting of:
• (2S,2′S)-2,2′-((oxybis(ethane-2,1-diyl))bis((N-(4-((4-guanidinobenzoyl)oxy)benzyl)sulfamoyl)azanediyl))disuccinic acid;
• (2S,13S)-3,12-bis(N-(4-((4-guanidinobenzoyl)oxy)benzyl)sulfamoyl)-6,9-dioxa-3,12-diazatetradecane-1,2,13,14-tetracarboxylic acid;
• (2S,16S)-3,15-bis(N-(4-((4-guanidinobenzoyl)oxy)benzyl)sulfamoyl)-6,9,12-trioxa-3,15-diazaheptadecane-1,2,16,17-tetracarboxylic acid;
• (2S,19S)-3,18-bis(N-(4-((4-guanidinobenzoyl)oxy)benzyl)sulfamoyl)-6,9,12,15-tetraoxa-3,18-diazaicosane-1,2,19,20-tetracarboxylic acid;
• (2S,22S)-3,21-bis(N-(4-((4-guanidinobenzoyl)oxy)benzyl)sulfamoyl)-6,9,12,15,18-pentaoxa-3,21-diazatricosane-1,2,22,23-tetracarboxylic acid;
• (2S,25S)-3,24-bis(N-(4-((4-guanidinobenzoyl)oxy)benzyl)sulfamoyl)-6,9,12,15,18,21-hexaoxa-3,24-diazahexacosane-1,2,25,26-tetracarboxylic acid;
• (2S,2′S)-2,2′-(propane-1,3-diylbis((N-(4-((4-guanidinobenzoyl)oxy)benzyl)sulfamoyl)azanediyl))disuccinic acid;
• (2S,2′S)-2,2′-(butane-1,4-diylbis((N-(4-((4-guanidinobenzoyl)oxy)benzyl)sulfamoyl)azanediyl))disuccinic acid;
• (2S,2′S)-2,2′-(pentane-1,5-diylbis((N-(4-((4-guanidinobenzoyl)oxy)benzyl)sulfamoyl)azanediyl))disuccinic acid;
• 3,18-bis(((4-((4-guanidinobenzoyl)oxy)benzyl)oxy)carbonyl)-6,9,12,15-tetraoxa-3,18-diazaicosane-1,2,19,20-tetracarboxylic acid;
• 2,2′-(1,20-bis(4-((4-guanidinobenzoyl)oxy)phenyl)-3,18-dioxo-2,19-dioxa-4,17-diazaicosane-4,17-diyl)disuccinic acid;
• (3S,6S,25S,28S)-6,25-bis(carboxymethyl)-3,28-bis((((4-((4-guanidinobenzoyl)oxy)benzyl)oxy)carbonyl)amino)-4,7,24,27-tetraoxo-11,14,17,20-tetraoxa-5,8,23,26-tetraazatriacontane-1,30-dioic acid;
• (3S,6S,23S,26S)-6,23-bis(carboxymethyl)-3,26-bis((((4-((4-guanidinobenzoyl)oxy)benzyl)oxy)carbonyl)amino)-4,7,22,25-tetraoxo-5,8,21,24-tetraazaoctacosane-1,28-dioic acid;
• (3S,22S)-3,22-bis(2-((3-carboxybenzyl)(((4-((4-guanidinobenzoyl)oxy)benzyl)oxy)carbonyl)amino)acetamido)-4,21-dioxo-8,11,14,17-tetraoxa-5,20-diazatetracosane-1,24-dioic acid;
• (4S,7S,26S,29S)-4,7,26,29-tetrakis(carboxymethyl)-3,30-bis(((4-((4-guanidinobenzoyl)oxy)benzyl)oxy)carbonyl)-5,8,25,28-tetraoxo-12,15,18,21-tetraoxa-3,6,9,24,27,30-hexaazadotriacontane-1,32-dioic acid;
• (3S,22S)-3,22-bis((3-carboxybenzyl)(((4-((4-guanidinobenzoyl)oxy)benzyl)oxy)carbonyl)amino)-4,21-dioxo-8,11,14,17-tetraoxa-5,20-diazatetracosane-1,24-dioic acid;
• (2S,2′S)-2,2′-((((5,8,11,14-tetraoxa-2,17-diazaoctadecane-1,18-dioyl)bis(3,1-phenylene))bis(methylene))bis((((4-((4-guanidinobenzoyl)oxy)benzyl)oxy)carbonyl)azanediyl))disuccinic acid;
• (2S,2′S)-2,2′-((((5,8,11,14-tetraoxa-2,17-diazaoctadecane-1,18-dioyl)bis(3,1-phenylene))bis(methylene))bis((N-(4-((4-guanidinobenzoyl)oxy)benzyl)sulfamoyl)azanediyl))disuccinic acid;
• 3,12-bis(10-guanidino-13-oxo-6,7,8,13-tetrahydrodibenzo[b,f] [1,4]dioxecin-4-carbonyl)-6,9-dioxa-3,12-diazatetradecane-1,2,13,14-tetracarboxylic acid;
• (2S,13S)-3,12-bis(10-guanidino-13-oxo-6,7,8,13-tetrahydrodibenzo[b,f] [1,4]dioxecin-4-carbonyl)-6,9-dioxa-3,12-diazatetradecane-1,2,13,14-tetracarboxylic acid;
• (2R,13R)-3,12-bis(10-guanidino-13-oxo-6,7,8,13-tetrahydrodibenzo[b,f] [1,4]dioxecin-4-carbonyl)-6,9-dioxa-3,12-diazatetradecane-1,2,13,14-tetracarboxylic acid;
• (2S,13S)-3,12-bis(N-(4-((4-guanidinobenzoyl)oxy)benzyl)-N-methylsulfamoyl)-6,9-dioxa-3,12-diazatetradecane-1,2,13,14-tetracarboxylic acid;
• 3,3′-(((ethane-1,2-diylbis(oxy))bis(ethane-2,1-diyl))bis((N-(4-((4-guanidinobenzoyl)oxy)benzyl)sulfamoyl)azanediyl))dipentanedioic acid;
• (2S,2′S)-2,2′-((1,12-bis(4-((4-guanidinobenzoyl)oxy)phenyl)-5,8-dioxa-2,11-diazadodecanedisulfonyl)bis(azanediyl))disuccinic acid;
• (2S,13S)-3,12-bis(N-(3-((4-guanidinobenzoyl)oxy)benzyl)sulfamoyl)-6,9-dioxa-3,12-diazatetradecane-1,2,13,14-tetracarboxylic acid;
• (2S,2′S)-2,2′-((oxybis(ethane-2,1-diyl))bis((10-guanidino-13-oxo-6,7,8,13-tetrahydrodibenzo[b,f] [1,4]dioxecin-4-carbonyl)azanediyl))disuccinic acid;
• (2S,16S)-3,15-bis(10-guanidino-13-oxo-6,7,8,13-tetrahydrodibenzo[b,f] [1,4]dioxecin-4-carbonyl)-6,9,12-trioxa-3,15-diazaheptadecane-1,2,16,17-tetracarboxylic acid;
• (2S,2′S)-2,2′-(([1,1′-biphenyl]-3,3′-diylbis(methylene))bis((10-guanidino-13-oxo-6,7,8,13-tetrahydrodibenzo[b,f] [1,4]dioxecin-4-carbonyl)azanediyl))disuccinic acid;
• (2S,2′S)-2,2′-(((((oxybis(ethane-2,1-diyl))bis(oxy))bis(3-carboxy-5,1-phenylene))bis(methylene))bis((10-guanidino-13-oxo-6,7,8,13-tetrahydrodibenzo[b,f] [1,4]dioxecin-4-carbonyl)azanediyl))disuccinic acid;
• and
• (2S,2′S)-2,2′-((oxybis(ethane-2,1-diyl))bis((3-((4-guanidinobenzoyl)oxy)benzoyl)azanediyl))disuccinic acid,
• or a pharmaceutically acceptable salt thereof.

26:

• The compound according to claim 1, selected from the group consisting of:
• (2S,2′S)-2,2′-((oxybis(ethane-2,1-diyl))bis((N-(4-((4-guanidinobenzoyl)oxy)benzyl)sulfamoyl)azanediyl))disuccinic acid;
• (2S,13S)-3,12-bis(N-(4-((4-guanidinobenzoyl)oxy)benzyl)sulfamoyl)-6,9-dioxa-3,12-diazatetradecane-1,2,13,14-tetracarboxylic acid;
• (2S,2′S)-2,2′-(butane-1,4-diylbis((N-(4-((4-guanidinobenzoyl)oxy)benzyl)sulfamoyl)azanediyl))disuccinic acid;
• (2S,13S)-3,12-bis(10-guanidino-13-oxo-6,7,8,13-tetrahydrodibenzo[b,f] [1,4]dioxecin-4-carbonyl)-6,9-dioxa-3,12-diazatetradecane-1,2,13,14-tetracarboxylic acid;
• (2S,2′S)-2,2′-((oxybis(ethane-2,1-diyl))bis((10-guanidino-13-oxo-6,7,8,13-tetrahydrodibenzo[b,f] [1,4]dioxecin-4-carbonyl)azanediyl))disuccinic acid;
• (2S,16S)-3,15-bis(10-guanidino-13-oxo-6,7,8,13-tetrahydrodibenzo[b,f] [1,4]dioxecin-4-carbonyl)-6,9,12-trioxa-3,15-diazaheptadecane-1,2,16,17-tetracarboxylic acid;
• (2S,2′S)-2,2′-(([1,1′-biphenyl]-3,3′-diylbis(methylene))bis((10-guanidino-13-oxo-6,7,8,13-tetrahydrodibenzo[b,f] [1,4]dioxecin-4-carbonyl)azanediyl))disuccinic acid;
• and
• (2S,2′S)-2,2′-(((((oxybis(ethane-2,1-diyl))bis(oxy))bis(3-carboxy-5,1-phenylene))bis(methylene))bis((10-guanidino-13-oxo-6,7,8,13-tetrahydrodibenzo[b,f] [1,4]dioxecin-4-carbonyl)azanediyl))disuccinic acid,
• or a pharmaceutically acceptable salt thereof.