Compound and drug containing the same

Abstract

To provide a compound that is useful for the treatment and prophylaxis of rabies.SOLUTION: The present disclosure provides a compound represented by formula XXIF or formula XXIB, a solvate, or a pharmaceutically acceptable salt thereof, where R1, R3, and R4 independently represent hydrogen, or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, or carbonyl; R2A and R2B independently represent hydrogen, or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, or carbonyl, or R2A and R2B, together with the nitrogen atom to which they are attached, form a non-aryl heterocycle or heteroaryl ring, where the non-aryl heterocycle and the heteroaryl ring are independently and optionally substituted.SELECTED DRAWING: None

Description

[Technical Field]

[0001] The present disclosure relates to novel fused tricyclic compounds or their enantiomers, or pharmaceutically acceptable salts or solvates thereof that are useful as pharmaceuticals. More specifically, the present disclosure relates to pharmaceutical compositions containing the fused tricyclic compounds or their enantiomers, or pharmaceutically acceptable salts or solvates thereof. The present disclosure also relates to therapeutic agents containing the fused tricyclic compounds or their enantiomers, or pharmaceutically acceptable salts or solvates thereof. [Background technology]

[0002] Rabies is an infectious disease caused by the rabies virus, and the mortality rate in humans after onset is nearly 100%. While more than 15 million people worldwide receive post-exposure vaccinations each year to prevent rabies, approximately 55,000 people die from rabies worldwide each year. An effective treatment for rabies has not yet been established, and its development is still needed. Summary of the Invention [Means for solving the problem]

[0003] The present disclosure provides compounds and methods for the treatment of rabies and other diseases.

[0004] As a result of intensive research, the present inventors have found that compounds represented by the following formulae IF, IB, IIF, IIB, XXIF, XXIB, XXIIF or XXIIB and related structural formulae, or pharmaceutically acceptable salts thereof (hereinafter sometimes referred to as "the compound(s) of the present disclosure" or "the present (disclosed) compound(s)") solve the above-mentioned problems, and have completed the present disclosure. That is, the present disclosure is as follows:

[0005] This disclosure provides the following:

[0006] [Term 1] Formula XXIF: [ka] or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1, R3, and R4 are each independently hydrogen, an optionally substituted hydrocarbon group, an optionally substituted heterocycle, an optionally substituted carbonyl, or an optionally substituted functional group; R 2A and R 2B are each independently hydrogen, an optionally substituted hydrocarbon group, an optionally substituted heterocycle, an optionally substituted carbonyl, or an optionally substituted functional group, or R 2A and R 2B taken together with the nitrogen atom to which they are attached form a heterocycle, wherein each heterocycle is independently optionally substituted; A compound or its enantiomer, or a salt thereof, or a solvate thereof. [Term 1B] Formula XXIF: [ka] or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1, R3 and R4 are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted carbonyl; R 2A and R 2Bare each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted carbonyl, or R 2A and R 2B together with the nitrogen atom to which they are attached form a non-aryl heterocycle or heteroaryl ring, wherein said non-aryl heterocycle and said heteroaryl ring are each independently optionally substituted; Item 1. The compound according to item 1, an enantiomer thereof, a salt thereof, or a solvate thereof. [Term 2] Formula XXIB: [ka] or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1, R3, and R4 are each independently hydrogen, an optionally substituted hydrocarbon group, an optionally substituted heterocycle, an optionally substituted carbonyl, or an optionally substituted functional group; R 2A and R 2B are each independently hydrogen, an optionally substituted hydrocarbon group, an optionally substituted heterocycle, an optionally substituted carbonyl, or an optionally substituted functional group, or R 2A and R 2B taken together with the nitrogen atom to which they are attached form a heterocycle, wherein each heterocycle is independently optionally substituted; A compound or its enantiomer, or a salt thereof, or a solvate thereof. [Term 2B] Formula XXIB: [ka] or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1, R3 and R4 are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted carbonyl; R 2A and R 2B are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted carbonyl, or R 2A and R 2B together with the nitrogen atom to which they are attached form a non-aryl heterocycle or heteroaryl ring, wherein said non-aryl heterocycle and said heteroaryl ring are each independently optionally substituted; Item 3. The compound according to Item 2, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item 3] The alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, and carbonyl of R1, R3, and R4 are each independently substituted with the same or different substituents selected from Substituent Group I up to the maximum substitutable number, as needed; R 2A and R 2Bwherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, carbonyl, and the non-aryl heterocycle and the heteroaryl ring are each independently substituted with from 1 to the maximum possible number of identical or different substituents selected from Substituent Group I as needed, or an enantiomer thereof, or a salt thereof, or a solvate thereof, according to any one of the above items. [Item 4] R1, R3 and R4 are each independently hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted carbonyl; R 2A and R 2B are each independently hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted carbonyl, or R 2A and R 2B and R 1 and R 2 are each independently substituted or unsubstituted, and R 3 and R 4 are each independently substituted or unsubstituted, and R 5 and R 6 are each independently substituted or unsubstituted, and R 6 and R 7 and R 8 and R 9 and R 10 and R 11 and R 12 and R 13 and R 14 and R 15 and R 16 and R 17 and R 18 and R 19 and R 20 and R 21 are each independently substituted or unsubstituted, and R 2 and R 30 and R 22 and R 23 and R 24 and R 25 are each independently substituted or unsubstituted, and R 2 and R 30 and R 26 and R 27 and R 28 and R 29 and R 30 and R 21 are each independently substituted or unsubstituted, and R 2 ... [Item 4B] R1, R3 and R4 are each independently hydrogen, optionally substituted C 1-12 Alkyl, optionally substituted C 3-10 Cycloalkyl, optionally substituted 5- to 10-membered heterocycloalkyl, optionally substituted C 6-10 aryl, optionally substituted 5- to 10-membered heteroaryl, or optionally substituted carbonyl; R 2A and R 2B each independently represents hydrogen, optionally substituted C 1-12Alkyl, optionally substituted C 3-10 Cycloalkyl, optionally substituted 5- to 10-membered heterocycloalkyl, optionally substituted C 6-10 aryl, optionally substituted 5- to 10-membered heteroaryl, or optionally substituted carbonyl, or R 2A and R 2B and R 1 and R 2 are each independently substituted or unsubstituted, and R 3 and R 4 are each independently substituted or unsubstituted, and R 5 and R 6 are each independently substituted or unsubstituted, and R 6 and R 7 and R 8 and R 9 and R 10 and R 11 and R 12 and R 13 and R 14 and R 15 and R 16 and R 17 and R 18 and R 19 and R 20 and R 21 are each independently substituted or unsubstituted, and R 2 and R 30 and R 22 and R 23 and R 24 and R 25 are each independently substituted or unsubstituted, and R 2 and R 30 and R 26 and R 27 and R 28 and R 29 and R 30 and R 21 are each independently substituted or unsubstituted, and R 2 ... [Item 5] R1, R3 and R4 are each independently hydrogen, optionally substituted alkyl, optionally substituted arylalkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, formyl, optionally substituted alkylcarbonyl, optionally substituted alkoxycarbonyl, optionally substituted arylcarbonyl, optionally substituted aryloxycarbonyl, optionally substituted heteroarylcarbonyl, optionally substituted heteroaryloxycarbonyl, optionally substituted cycloalkylcarbonyl, optionally substituted cycloalkyloxycarbonyl, optionally substituted heterocycloalkylcarbonyl, optionally substituted heterocycloalkyloxycarbonyl, carbamoyl, optionally substituted alkylcarbamoyl, optionally substituted alkoxycarbamoyl, optionally substituted arylcarbamoyl, optionally substituted heteroarylcarbamoyl, optionally substituted cycloalkylcarbamoyl, or optionally substituted heterocycloalkylcarbamoyl, wherein the above groups of R1, R3 and R4 are optionally substituted with the same or different substituents selected from Substituent Group II, up to the maximum substitutable number; R 2A and R 2Bare each independently hydrogen, optionally substituted alkyl, optionally substituted arylalkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, formyl, optionally substituted alkylcarbonyl, optionally substituted alkoxycarbonyl, optionally substituted arylcarbonyl, optionally substituted aryloxycarbonyl, optionally substituted heteroarylcarbonyl, optionally substituted heteroaryloxycarbonyl, optionally substituted cycloalkylcarbonyl, optionally substituted cycloalkyloxycarbonyl, optionally substituted heterocycloalkylcarbonyl, optionally substituted heterocycloalkyloxycarbonyl, carbamoyl, optionally substituted alkylcarbamoyl, optionally substituted alkoxycarbamoyl, optionally substituted arylcarbamoyl, optionally substituted heteroarylcarbamoyl, optionally substituted cycloalkylcarbamoyl, or optionally substituted heterocycloalkylcarbamoyl, wherein R 2A and R 2B The above groups are optionally substituted with one to the maximum possible number of identical or different substituents selected from Substituent Group II, or R 2A and R 2B and R 1 and R 2 are, taken together with the nitrogen atom to which they are attached, to form a 5- to 6-membered non-aryl heterocycle or heteroaryl ring, and the non-aryl heterocycle and the heteroaryl ring are optionally substituted with 1 to the maximum possible number of identical or different substituents selected from Substituent Group II, or an enantiomer thereof, a salt thereof, or a solvate thereof, according to any one of the above items. [Item 5B] R1, R3 and R4 are each independently hydrogen, optionally substituted C 1-12 Alkyl, optionally substituted C 6-10 Aryl C 1-12 Alkyl, optionally substituted C 3-10Cycloalkyl, optionally substituted 5- to 10-membered heterocycloalkyl, formyl, optionally substituted C 1-12 Alkylcarbonyl, optionally substituted C 1-12 Alkoxycarbonyl, optionally substituted C 6-10 Arylcarbonyl, optionally substituted C 6-10 Aryloxycarbonyl, optionally substituted 5- to 10-membered heteroarylcarbonyl, optionally substituted 5- to 10-membered heteroaryloxycarbonyl, optionally substituted C 3-10 Cycloalkylcarbonyl, optionally substituted C 3-10 Cycloalkyloxycarbonyl, optionally substituted 5-10 membered heterocycloalkylcarbonyl, optionally substituted 5-10 membered heterocycloalkyloxycarbonyl, carbamoyl, optionally substituted C 1-12 Alkylcarbamoyl, optionally substituted C 1-12 Alkoxycarbamoyl, optionally substituted C 6-10 arylcarbamoyl, optionally substituted 5- to 10-membered heteroarylcarbamoyl, optionally substituted C 3-10 cycloalkylcarbamoyl, or optionally substituted 5- to 10-membered heterocycloalkylcarbamoyl, wherein the above groups of R1, R3, and R4 are optionally substituted with 1 to the maximum substitutable number of identical or different substituents selected from Substituent Group III; R 2A and R 2B each independently represents hydrogen, optionally substituted C 1-12 Alkyl, optionally substituted C 6-10 Aryl C 1-12 Alkyl, optionally substituted C 3-10 Cycloalkyl, optionally substituted 5- to 10-membered heterocycloalkyl, formyl, optionally substituted C 1-12 Alkylcarbonyl, optionally substituted C 1-12 Alkoxycarbonyl, optionally substituted C 6-10Arylcarbonyl, optionally substituted C 6-10 Aryloxycarbonyl, optionally substituted 5- to 10-membered heteroarylcarbonyl, optionally substituted 5- to 10-membered heteroaryloxycarbonyl, optionally substituted C 3-10 Cycloalkylcarbonyl, optionally substituted C 3-10 Cycloalkyloxycarbonyl, optionally substituted 5-10 membered heterocycloalkylcarbonyl, optionally substituted 5-10 membered heterocycloalkyloxycarbonyl, carbamoyl, optionally substituted C 1-12 Alkylcarbamoyl, optionally substituted C 1-12 Alkoxycarbamoyl, optionally substituted C 6-10 arylcarbamoyl, optionally substituted 5- to 10-membered heteroarylcarbamoyl, optionally substituted C 3-10 cycloalkylcarbamoyl, or optionally substituted 5- to 10-membered heterocycloalkylcarbamoyl, where R 2A and R 2B The above groups are optionally substituted with one to the maximum substitutable number of identical or different substituents selected from Substituent Group III, or R 2A and R 2B and R 1 and R 2 are, taken together with the nitrogen atom to which they are attached, to form a 5- to 6-membered non-aryl heterocycle, wherein the non-aryl heterocycle is optionally substituted with one to the maximum possible number of identical or different substituents selected from Substituent Group V, or an enantiomer thereof, a salt thereof, or a solvate thereof, according to any one of the above items. [Item 6] R1 and R4 are each independently hydrogen, optionally substituted alkyl, optionally substituted arylalkyl, optionally substituted cycloalkyl, formyl, optionally substituted alkylcarbonyl, optionally substituted alkoxycarbonyl, optionally substituted arylcarbonyl, optionally substituted aryloxycarbonyl, optionally substituted cycloalkylcarbonyl, optionally substituted cycloalkyloxycarbonyl, optionally substituted heterocycloalkylcarbonyl, optionally substituted heterocycloalkyloxycarbonyl, carbamoyl, optionally substituted alkylcarbamoyl, optionally substituted alkoxycarbamoyl, optionally substituted arylcarbamoyl, optionally substituted heteroarylcarbamoyl, optionally substituted cycloalkylcarbamoyl, or optionally substituted heterocycloalkylcarbamoyl, wherein the above groups of R1 and R4 are optionally substituted with 1 to the maximum possible number of identical or different substituents selected from Substituent Group III. A compound according to any one of the above items, or an enantiomer thereof, or a salt or solvate thereof. [Item 6B] R1 and R4 are each independently hydrogen, optionally substituted C 1-12 Alkyl, optionally substituted C 6-10 Aryl C 1-12 Alkyl, optionally substituted C 3-10 Cycloalkyl, formyl, optionally substituted C 1-12 Alkylcarbonyl, optionally substituted C 1-12 Alkoxycarbonyl, optionally substituted C 6-10 Arylcarbonyl, optionally substituted C 6-10 Aryloxycarbonyl, optionally substituted C 3-10 Cycloalkylcarbonyl, optionally substituted C 3-10Cycloalkyloxycarbonyl, optionally substituted 5-10 membered heterocycloalkylcarbonyl, optionally substituted 5-10 membered heterocycloalkyloxycarbonyl, carbamoyl, optionally substituted C 1-12 Alkylcarbamoyl, optionally substituted C 1-12 Alkoxycarbamoyl, optionally substituted C 6-10 arylcarbamoyl, optionally substituted 5- to 10-membered heteroarylcarbamoyl, optionally substituted C 3-10 A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein the compound is a cycloalkylcarbamoyl or an optionally substituted 5- to 10-membered heterocycloalkylcarbamoyl, wherein the above groups of R1 and R4 are optionally substituted with 1 to the maximum possible number of identical or different substituents selected from Substituent Group III. [Item 7] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1 and R4 are each independently hydrogen, optionally substituted alkyl, optionally substituted arylalkyl, formyl, optionally substituted alkylcarbonyl, optionally substituted alkoxycarbonyl, optionally substituted arylcarbonyl, optionally substituted aryloxycarbonyl, or carbamoyl, optionally substituted alkylcarbamoyl, wherein the above groups of R1 and R4 are optionally substituted with 1 to the maximum possible number of identical or different substituents selected from Substituent Group III. [Item 7B] R1 and R4 are each independently hydrogen, optionally substituted C 1-12 Alkyl, optionally substituted C 6-10 Aryl C 1-12 Alkyl, formyl, optionally substituted C 1-12 Alkylcarbonyl, optionally substituted C 1-12 Alkoxycarbonyl, optionally substituted C 6-10 Arylcarbonyl, optionally substituted C 6-10Aryloxycarbonyl, or carbamoyl, optionally substituted C 1-12 A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein the above groups R1 and R4 are optionally substituted with one to the maximum possible number of identical or different substituents selected from Substituent Group III. [Item 8] R1 and R4 are each independently hydrogen; alkyl; alkyl substituted with from 1 to the maximum number of identical or different substituents selected from the group consisting of amino, substituted amino, substituted oxy, substituted carbonyl, cycloalkyl and substituted cycloalkyl; arylalkyl; arylalkyl substituted with from 1 to the maximum number of identical or different substituents selected from the group consisting of halogen, alkyl, substituted alkyl, hydroxy, substituted oxy, amino, substituted amino, and nitro; formyl; substituted carbonyl; or substituted oxycarbonyl, wherein the substituted amino, substituted oxy, substituted alkyl, substituted carbonyl, substituted cycloalkyl, substituted carbonyl, and substituted oxycarbonyl in R1 and R4 each independently have from 1 to the maximum number of identical or different substituents selected from substituent group IV, or a compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Item 8B] R1 and R4 are each independently hydrogen; C 1-12 Alkyl; Amino, Substituted Amino, Substituted Oxy, Substituted Carbonyl, C 3-10 Cycloalkyl and substituted C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkyl 1-12 Alkyl; C 6-10 Aryl C 1-6 Alkyl; halogen, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkyl, substituted alkyl, hydroxy, substituted oxy, amino, substituted amino, and nitro 6-10 Aryl C 1-6A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein the substituted amino, substituted oxy, substituted alkyl, substituted carbonyl, substituted cycloalkyl, substituted carbonyl, and substituted oxycarbonyl in R1 and R4 each independently have from one to the maximum possible number of identical or different substituents selected from Substituent Group IV. [Item 9] R1 and R4 are each independently hydrogen; alkyl; alkyl substituted with from 1 to the maximum number of identical or different substituents selected from the group consisting of amidinoamino, alkoxy, alkoxycarbonyl, carbamoyl, carboxy, hydroxy, trialkylsilyloxy, and cycloalkyl; arylalkyl; arylalkyl substituted with from 1 to the maximum number of identical or different substituents selected from the group consisting of halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, amino, substituted amino, nitro, and hydroxy; formyl; alkylcarbonyl; arylalkylcarbonyl; arylalkyloxycarbonyl; alkoxycarbonyl; arylcarbonyl; aryloxycarbonyl; carbamoyl; alkylcarbamoyl; or arylalkylcarbamoyl, wherein each of the substituted aminos independently has from 1 to the maximum number of identical or different substituents selected from substituent group IV. The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Item 9B] R1 and R4 are each independently hydrogen; C 1-12 Alkyl; Amidinoamino, C 1-6 Alkoxy, C 1-6 Alkoxycarbonyl, carbamoyl, carboxy, hydroxy, triC 1-6 Alkylsilyloxy, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkyl 1-12 Alkyl; C 6-10 Aryl C 1-6 Alkyl; halogen, C1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of haloalkoxy, amino, substituted amino, nitro, and hydroxy. 6-10 Aryl C 1-6 Alkyl; Formyl; C 1-12 Alkylcarbonyl; C 6-10 Aryl C 1-6 Alkylcarbonyl; C 6-10 Aryl C 1-6 Alkyloxycarbonyl; C 1-12 Alkoxycarbonyl; C 6-10 Arylcarbonyl; C 6-10 Aryloxycarbonyl; Carbamoyl; C 1-12 alkylcarbamoyl; or C 6-10 Aryl C 1-6 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein the substituted amino is alkylcarbamoyl, wherein the substituted amino has from 1 to the maximum possible number of identical or different substituents selected from Substituent Group IV. [Item 10] R3 is hydrogen; alkyl; alkyl substituted with from 1 to the maximum number of the same or different substituents selected from the group consisting of amino, substituted amino, carboxy, substituted oxycarbonyl, carbamoyl, substituted aminocarbonyl, hydroxy, substituted oxy, cycloalkyl, and substituted cycloalkyl; arylalkyl; or arylalkyl substituted with from 1 to the maximum number of the same or different substituents selected from the group consisting of halogen, alkyl, substituted alkyl, carboxy, substituted oxycarbonyl, and hydroxy, and substituted oxy, wherein the substituted amino, substituted oxy, substituted oxycarbonyl, substituted aminocarbonyl, substituted alkyl, substituted cycloalkyl, substituted carbonyl, and substituted oxycarbonyl in R3 each independently have from 1 to the maximum number of the same or different substituents selected from substituent group IV, or a compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Item 11] R3 is hydrogen; alkyl; alkyl substituted with one to the maximum number of identical or different substituents selected from the group consisting of amidinoamino, alkoxycarbonyl, carbamoyl, carboxy, hydroxy, trialkylsilyloxy, amino, alkoxycarbonylamino, and cycloalkyl; arylalkyl; or arylalkyl substituted with one to the maximum number of identical or different substituents selected from the group consisting of halogen, alkyl, alkoxycarbonyl, and hydroxy, or an enantiomer thereof, or a salt or solvate thereof, according to any one of the above items. [Item 11B] R3 is hydrogen; C 1-12 Alkyl; Amidinoamino, C 1-6 Alkoxycarbonyl, carbamoyl, carboxy, hydroxy, triC 1-6 Alkylsilyloxy, Amino, C 1-6 Alkoxycarbonylamino, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkyl 1-12 Alkyl; C6-10 Aryl C 1-6 Alkyl; or halogen, C 1-6 Alkyl, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkoxycarbonyl and hydroxy 6-10 Aryl C 1-6 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R is alkyl. [Section 12]R 2A and R 2B are each independently hydrogen; alkyl; alkyl substituted with from one to the maximum number of the same or different substituents selected from the group consisting of formyl, substituted carbonyl, hydroxy, substituted oxy, amino, substituted amino, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, and substituted heterocycloalkyl; arylalkyl; arylalkyl substituted with from one to the maximum number of the same or different substituents selected from the group consisting of halogen, alkyl, substituted alkyl, hydroxy, and substituted oxy; heteroarylalkyl; substituted heteroarylalkyl; cycloalkyl; or substituted cycloalkyl, wherein R 2A and R 2B The substituted carbonyl, substituted oxy, substituted amino, substituted cycloalkyl, substituted heterocycloalkyl, substituted heteroarylalkyl, and substituted alkyl in each independently have from one to the maximum possible number of substituents selected from Substituent Group IV, which may be the same or different, or R 2A and R 2B are taken together with the nitrogen atom to which they are attached to form a non-aryl heterocycle, and the non-aryl heterocycle is optionally substituted with one, or up to the maximum permissible number of, identical or different substituents selected from Substituent Group VI, or a compound or enantiomer thereof, or a salt or solvate thereof according to any one of the preceding items. [Section 13]R 2A and R 2Bare each independently hydrogen; alkyl; alkyl substituted with from one to the maximum number of identical or different substituents selected from the group consisting of amidinoamino, alkoxy, alkoxycarbonyl, carbamoyl, carboxy, hydroxy, amino, alkoxycarbonylamino, cycloalkyl, and heterocycloalkyl; arylalkyl; arylalkyl substituted with from one to the maximum number of identical or different substituents selected from the group consisting of halogen, alkyl, haloalkyl, alkoxy, and hydroxy; heteroarylalkyl; alkoxycarbonyl-substituted heteroarylalkyl; or cycloalkyl; or 2A and R 2B and R 1 and R 2 are, taken together with the nitrogen atom to which they are attached, to form a 5- to 6-membered non-aryl heterocycle, wherein the non-aryl heterocycle is optionally substituted with one, or up to the maximum possible number of, identical or different substituents selected from Substituent Group VI, or a compound or an enantiomer thereof, or a salt or solvate thereof, according to any one of the above items. [Section 13B]R 2A and R 2B are each independently hydrogen; C 1-12 Alkyl; Amidinoamino, C 1-6 Alkoxy, C 1-6 Alkoxycarbonyl, carbamoyl, carboxy, hydroxy, amino, C 1-6 Alkoxycarbonylamino, C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkyl and 5- to 10-membered heterocycloalkyl 1-12 Alkyl; C 6-10 Aryl C 1-6 Alkyl; halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkoxy and hydroxy 6-10 Aryl C 1-6 Alkyl; 5-10 membered heteroaryl C 1-6Alkyl; C 1-6 Alkoxycarbonyl-substituted 5- to 10-membered heteroaryl C 1-6 Alkyl; or C 3-10 cycloalkyl or R 2A and R 2B and R 1 and R 2 are, taken together with the nitrogen atom to which they are attached, to form a 5- to 6-membered non-aryl heterocycle, wherein the non-aryl heterocycle is optionally substituted with one, or up to the maximum possible number of, identical or different substituents selected from Substituent Group VI, or a compound or an enantiomer thereof, or a salt or solvate thereof, according to any one of the above items. [Item 14] R1 is alkyl; alkyl, arylalkyl substituted with from 1 to the maximum number of identical or different substituents selected from the group consisting of amidinoamino, carbamoyl, carboxy, hydroxy, and cycloalkyl; or arylalkyl substituted with from 1 to the maximum number of identical or different substituents selected from the group consisting of halogen, alkyl, haloalkyl, alkoxy, substituted amino, and hydroxy, wherein the substituted amino has from 1 to the maximum number of identical or different substituents selected from substituent group IV, or a compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Section 14B] R1 is C 1-12 Alkyl; amidinoamino, carbamoyl, carboxy, hydroxy, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkyl 1-12 Alkyl; C 6-10 Aryl C 1-6 Alkyl; or halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkoxy, substituted amino, and hydroxy 6-10 Aryl C 1-6The compound according to any one of the preceding items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein the substituted amino is alkyl, and wherein the substituted amino has from 1 to the maximum possible number of identical or different substituents selected from Substituent Group IV. [Section 15]R 2A is hydrogen and R 2B is alkyl; alkyl substituted with from 1 to the maximum possible number of identical or different substituents selected from the group consisting of amidinoamino, carbamoyl, carboxy, hydroxy, and cycloalkyl; arylalkyl; arylalkyl substituted with from 1 to the maximum possible number of identical or different substituents selected from the group consisting of halogen, alkyl, haloalkyl, alkoxy, and hydroxy; or cycloalkyl; or an enantiomer thereof, or a salt or solvate thereof according to any one of the above items. [Section 15B]R 2A is hydrogen and R 2B is C 1-12 Alkyl; amidinoamino, carbamoyl, carboxy, hydroxy, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkyl 1-12 Alkyl; C 6-10 Aryl C 1-6 Alkyl; halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkoxy and hydroxy 6-10 Aryl C 1-6 Alkyl; or C 3-10 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, which is cycloalkyl. [Item 16] R3 is alkyl; alkyl substituted with one to the maximum number of identical or different substituents selected from the group consisting of amidinoamino, carbamoyl, carboxy, hydroxy, and cycloalkyl; arylalkyl; or arylalkyl substituted with one to the maximum number of identical or different substituents selected from the group consisting of alkyl and hydroxy, or a compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Section 16B] R3 is C 1-12 Alkyl; amidinoamino, carbamoyl, carboxy, hydroxy, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkyl 1-12 Alkyl; C 6-10 Aryl C 1-6 Alkyl; or C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkyl and hydroxy 6-10 Aryl C 1-6 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R is alkyl. [Item 17] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R4 is hydrogen, alkyl, alkylcarbonyl, arylalkylcarbonyl, arylalkyloxycarbonyl, alkoxycarbonyl, carbamoyl, or arylalkylcarbamoyl. [Item 17B] R4 is hydrogen, C 1-12 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl C 1-6 Alkyl carbonyl, C 6-10 Aryl C 1-6 Alkyloxycarbonyl, C 1-12 Alkoxycarbonyl, carbamoyl, or C 6-10 Aryl C 1-6The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, which is alkylcarbamoyl. [Item 17C] R1 is hydrogen, methyl, ethyl, isobutyl, isopentyl, amidinoaminopropyl, tert-butoxyethyl, tert-butoxypropyl, (tert-butoxycarbonyl)ethyl, carbamoylmethyl, carboxyethyl, hydroxyethyl, hydroxypropyl, cyclopentylmethyl, cyclohexylmethyl, benzyl, phenylethyl, naphthalenylmethyl, fluorobenzyl, chlorobenzyl, dichlorobenzyl, methylbenzyl, tert-butylbenzyl, (trifluoromethyl)benzyl, methoxybenzyl, ethoxybenzyl, tert -butoxybenzyl, aminobenzyl, (cyclopentylcarbonylamino)benzyl, (cyclopentylmethylamino)benzyl, (dimethylamino)benzyl, (carbamoylethylcarbonylamino)benzyl, (carboxyethylcarbonylamino)benzyl, nitrobenzyl, hydroxybenzyl, 3-methylbutanoyl, isobutylcarbonyl, 2-phenylacetyl, isopropyloxycarbonyl, benzoyl, or phenyloxycarbonyl, or an enantiomer thereof, or a salt or solvate thereof according to any one of the preceding items. [Section 17D]R 2A is hydrogen and R 2Bis methyl, isopropyl, isobutyl, n-pentyl, isopentyl, n-hexyl, heptyl, amidinoaminopropyl, tert-butoxyethyl, tert-butoxycarbonylmethyl, carbamoylmethyl, carbamoylethyl, carboxyethyl, hydroxyethyl, aminobutyl, ((tert-butoxycarbonyl)amino)butyl, cyclohexylmethyl, (tetrahydro-2H-pyran-2-yl)methyl, benzyl, phenylethyl, naphthalenylmethyl, naphthalenylethyl ethyl, fluorobenzyl, chlorobenzyl, dichlorobenzyl, (fluorophenyl)ethyl, methylbenzyl, (trifluoromethyl)benzyl, methoxybenzyl, tert-butoxybenzyl, hydroxybenzyl, α-hydroxymethylphenethyl, β-hydroxyphenethyl, pyridinylmethyl, (1H-indol-3-yl)ethyl, (1-(tert-butoxycarbonyl)-1H-indol-3-yl)ethyl, cyclopentyl, or cyclohexyl; or 2A and R 2B and R 1 and R 2 are each independently substituted or unsubstituted alkyl, and R 3 and R 4 are each independently substituted or unsubstituted alkyl, and R 5 and R 6 are each independently substituted or unsubstituted alkyl, and R 6 and R 7 and R 8 and R 9 and R 10 and R 11 and R 12 and R 13 and R 14 and R 15 and R 16 and R 17 and R 18 and R 19 and R 20 and R 21 are each independently substituted or unsubstituted alkyl, and R 2 and R 22 and R 23 and R 24 and R 25 and R 26 and R 27 and R 28 and R 29 and R 30 and R 31 and R 32 and R 33 and R 34 and R 35 and R 36 and R 37 and R 38 and R 39 and R 40 and R 41 and R 42 and R 43 and [Item 17E] R3 is n-propyl, isobutyl, isopentyl, amidinoaminopropyl, (methoxycarbonyl)ethyl, (tert-butoxycarbonyl)ethyl, carbamoylmethyl, carboxyethyl, hydroxymethyl, hydroxyethyl, (tert-butyldimethylsilyloxy)ethyl, aminobutyl, ((tert-butoxycarbonyl)amino)butyl, cyclohexylmethyl, cyclohexylethyl, benzyl, phenylethyl, phenylpropyl, phenylbutyl, naphthalenylmethyl, naphthalenylethyl, chlorobenzyl, methylbenzyl, (methylphenyl)ethyl, (isopropylphenyl)ethyl, or hydroxybenzyl, or an enantiomer thereof, or a salt thereof, or a solvate thereof, according to any one of the above items. [Item 17F] R4 is hydrogen, methyl, ethyl, isobutyl, formyl, acetyl, 3-methylbutanoyl, 2-phenylacetyl, methoxycarbonyl, ethoxycarbonyl, 2-methylpropyloxycarbonyl, tert-butoxycarbonyl, benzoyl, benzyl, benzyloxycarbonyl, aminocarbonyl, N-benzylaminocarbonyl, propylcarbamoyl, N-isobutylaminocarbonyl, or N-benzylaminocarbonyl, or a compound or enantiomer thereof according to any one of the above items, or a salt thereof, or a solvate thereof. [Item 17G] The compound is a compound selected from the group consisting of compound numbers IB-1 to IB-995 and IF-1 to IF-931. The compound or its enantiomer, or a salt thereof, or a solvate thereof according to any one of the above items. [Section 18] Formula XXIIF: [ka] or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1 and R3 are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted carbonyl; R 2A and R 2B are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted carbonyl, or R 2A and R 2Btogether with the nitrogen atom to which they are attached form a non-aryl heterocycle or heteroaryl ring, wherein said non-aryl heterocycle and said heteroaryl ring are each independently optionally substituted; A compound or its enantiomer, or a salt thereof, or a solvate thereof. [Section 19] Formula XXIIB: [ka] or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1 and R3 are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted carbonyl; R 2A and R 2B are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted carbonyl, or R 2A and R 2B together with the nitrogen atom to which they are attached form a non-aryl heterocycle or heteroaryl ring, wherein said non-aryl heterocycle and said heteroaryl ring are each independently optionally substituted; A compound or its enantiomer, or a salt thereof, or a solvate thereof. [Item 20] The alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, and carbonyl of R1 and R3 are each independently substituted with the same or different substituents selected from Substituent Group I up to the maximum substitutable number, as needed; R 2A and R 2B wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, carbonyl, and the non-aryl heterocycle and the heteroaryl ring are each independently substituted with from 1 to the maximum possible number of identical or different substituents selected from Substituent Group I as needed, or an enantiomer thereof, or a salt thereof, or a solvate thereof, according to any one of the above items. [Item 21] R1 and R3 are each independently hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted carbonyl; R 2A and R 2B are each independently hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted carbonyl, or R 2A and R 2B and R 1 and R 2 are each independently substituted or unsubstituted, and R 3 and R 4 are each independently substituted or unsubstituted, and R 5 and R 6 are each independently substituted or unsubstituted, and R 6 and R 7 and R 8 and R 9 and R 10 and R 11 and R 12 and R 13 and R 14 and R 15 and R 16 and R 17 and R 18 and R 19 and R 20 and R 21 are each independently substituted or unsubstituted, and R 2 and R 30 and R 22 and R 23 and R 24 and R 25 are each independently substituted or unsubstituted, and R 2 and R 30 and R 26 and R 27 and R 28 and R 29 and R 30 and R 21 are each independently substituted or unsubstituted, and R 2 ... [Item 22] R1 and R3 are each independently hydrogen, optionally substituted alkyl, optionally substituted arylalkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, formyl, optionally substituted alkylcarbonyl, optionally substituted alkoxycarbonyl, optionally substituted arylcarbonyl, optionally substituted aryloxycarbonyl, optionally substituted heteroarylcarbonyl, optionally substituted heteroaryloxycarbonyl, optionally substituted cycloalkylcarbonyl, optionally substituted cycloalkyloxycarbonyl, optionally substituted heterocycloalkylcarbonyl, optionally substituted heterocycloalkyloxycarbonyl, carbamoyl, optionally substituted alkylcarbamoyl, optionally substituted alkoxycarbamoyl, optionally substituted arylcarbamoyl, optionally substituted heteroarylcarbamoyl, optionally substituted cycloalkylcarbamoyl, or optionally substituted heterocycloalkylcarbamoyl, wherein the above groups of R1 and R3 are optionally substituted with the same or different substituents selected from Substituent Group II, up to the maximum substitutable number; R 2A and R 2Bare each independently hydrogen, optionally substituted alkyl, optionally substituted arylalkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, formyl, optionally substituted alkylcarbonyl, optionally substituted alkoxycarbonyl, optionally substituted arylcarbonyl, optionally substituted aryloxycarbonyl, optionally substituted heteroarylcarbonyl, optionally substituted heteroaryloxycarbonyl, optionally substituted cycloalkylcarbonyl, optionally substituted cycloalkyloxycarbonyl, optionally substituted heterocycloalkylcarbonyl, optionally substituted heterocycloalkyloxycarbonyl, carbamoyl, optionally substituted alkylcarbamoyl, optionally substituted alkoxycarbamoyl, optionally substituted arylcarbamoyl, optionally substituted heteroarylcarbamoyl, optionally substituted cycloalkylcarbamoyl, or optionally substituted heterocycloalkylcarbamoyl, wherein R 2A and R 2B The above groups are optionally substituted with one to the maximum possible number of identical or different substituents selected from Substituent Group II, or R 2A and R 2B and R 1 and R 2 are, taken together with the nitrogen atom to which they are attached, to form a 5- to 6-membered non-aryl heterocycle, wherein the non-aryl heterocycle is optionally substituted with one to the maximum possible number of identical or different substituents selected from Substituent Group II, or an enantiomer thereof, a salt thereof, or a solvate thereof, according to any one of the above items. [Item 23] R1 and R3 are each independently hydrogen, optionally substituted C 1-12 Alkyl, optionally substituted C 6-10 Aryl C 1-12 Alkyl, optionally substituted C 3-10 Cycloalkyl, optionally substituted 5- to 10-membered heterocycloalkyl, formyl, optionally substituted C 1-12Alkylcarbonyl, optionally substituted C 1-12 Alkoxycarbonyl, optionally substituted C 6-10 Arylcarbonyl, optionally substituted C 6-10 Aryloxycarbonyl, optionally substituted 5- to 10-membered heteroarylcarbonyl, optionally substituted 5- to 10-membered heteroaryloxycarbonyl, optionally substituted C 3-10 Cycloalkylcarbonyl, optionally substituted C 3-10 Cycloalkyloxycarbonyl, optionally substituted 5-10 membered heterocycloalkylcarbonyl, optionally substituted 5-10 membered heterocycloalkyloxycarbonyl, carbamoyl, optionally substituted C 1-12 Alkylcarbamoyl, optionally substituted C 1-12 Alkoxycarbamoyl, optionally substituted C 6-10 arylcarbamoyl, optionally substituted 5- to 10-membered heteroarylcarbamoyl, optionally substituted C 3-10 cycloalkylcarbamoyl, or optionally substituted 5- to 10-membered heterocycloalkylcarbamoyl, wherein the above groups of R1 and R3 are optionally substituted with 1 to the maximum substitutable number of identical or different substituents selected from Substituent Group III; R 2A and R 2B each independently represents hydrogen, optionally substituted C 1-12 Alkyl, optionally substituted C 6-10 Aryl C 1-12 Alkyl, optionally substituted C 3-10 Cycloalkyl, optionally substituted 5- to 10-membered heterocycloalkyl, formyl, optionally substituted C 1-12 Alkylcarbonyl, optionally substituted C 1-12 Alkoxycarbonyl, optionally substituted C 6-10 Arylcarbonyl, optionally substituted C 6-10Aryloxycarbonyl, optionally substituted 5- to 10-membered heteroarylcarbonyl, optionally substituted 5- to 10-membered heteroaryloxycarbonyl, optionally substituted C 3-10 Cycloalkylcarbonyl, optionally substituted C 3-10 Cycloalkyloxycarbonyl, optionally substituted 5-10 membered heterocycloalkylcarbonyl, optionally substituted 5-10 membered heterocycloalkyloxycarbonyl, carbamoyl, optionally substituted C 1-12 Alkylcarbamoyl, optionally substituted C 1-12 Alkoxycarbamoyl, optionally substituted C 6-10 arylcarbamoyl, optionally substituted 5- to 10-membered heteroarylcarbamoyl, optionally substituted C 3-10 cycloalkylcarbamoyl, or optionally substituted 5- to 10-membered heterocycloalkylcarbamoyl, where R 2A and R 2B The above groups are optionally substituted with one to the maximum substitutable number of identical or different substituents selected from Substituent Group III, or R 2A and R 2B and R 1 and R 2 are, taken together with the nitrogen atom to which they are attached, to form a 5- to 6-membered non-aryl heterocycle, wherein the non-aryl heterocycle is optionally substituted with one to the maximum possible number of identical or different substituents selected from Substituent Group III, or an enantiomer thereof, a salt thereof, or a solvate thereof, according to any one of the above items. [Item 24] R1 and R3 are each independently hydrogen, optionally substituted alkyl, optionally substituted arylalkyl, optionally substituted cycloalkyl, formyl, optionally substituted alkylcarbonyl, optionally substituted alkoxycarbonyl, optionally substituted arylcarbonyl, optionally substituted aryloxycarbonyl, optionally substituted cycloalkylcarbonyl, optionally substituted cycloalkyloxycarbonyl, optionally substituted heterocycloalkylcarbonyl, optionally substituted heterocycloalkyloxycarbonyl, carbamoyl, optionally substituted alkylcarbamoyl, optionally substituted alkoxycarbamoyl, optionally substituted arylcarbamoyl, optionally substituted heteroarylcarbamoyl, optionally substituted cycloalkylcarbamoyl, or optionally substituted heterocycloalkylcarbamoyl, wherein the above groups of R1 and R3 are optionally substituted with 1 to the maximum possible number of identical or different substituents selected from Substituent Group III. A compound according to any one of the above items, or an enantiomer thereof, or a salt or solvate thereof. [Item 25B] R1 and R3 are each independently hydrogen, optionally substituted C 1-12 Alkyl, optionally substituted C 6-10 Aryl C 1-12 Alkyl, optionally substituted C 3-10 Cycloalkyl, formyl, optionally substituted C 1-12 Alkylcarbonyl, optionally substituted C 1-12 Alkoxycarbonyl, optionally substituted C 6-10 Arylcarbonyl, optionally substituted C 6-10 Aryloxycarbonyl, optionally substituted C 3-10 Cycloalkylcarbonyl, optionally substituted C 3-10Cycloalkyloxycarbonyl, optionally substituted 5-10 membered heterocycloalkylcarbonyl, optionally substituted 5-10 membered heterocycloalkyloxycarbonyl, carbamoyl, optionally substituted C 1-12 Alkylcarbamoyl, optionally substituted C 1-12 Alkoxycarbamoyl, optionally substituted C 6-10 arylcarbamoyl, optionally substituted 5- to 10-membered heteroarylcarbamoyl, optionally substituted C 3-10 A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein the compound is a cycloalkylcarbamoyl or an optionally substituted 5- to 10-membered heterocycloalkylcarbamoyl, wherein the above groups of R1 and R3 are optionally substituted with 1 to the maximum possible number of identical or different substituents selected from Substituent Group III. [Item 25] R1 is a C substituted with one to the maximum number of identical or different substituents selected from the group consisting of hydrogen; alkyl; amino, substituted amino, hydroxy, substituted oxy, formyl, substituted carbonyl, and cycloalkyl, and substituted cycloalkyl. 1-12 A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein the compound is alkyl; arylalkyl; arylalkyl substituted with from one to the maximum possible number of identical or different substituents selected from the group consisting of halogen, alkyl, substituted alkyl, hydroxy, substituted oxy, amino, substituted amino, and nitro; formyl; or substituted carbonyl, wherein the substituted amino, substituted oxy, substituted carbonyl, substituted cycloalkyl, and substituted alkyl in R1 each independently have from one to the maximum possible number of identical or different substituents selected from substituent group IV. [Item 26] R1 is hydrogen; alkyl; amidinoamino, alkoxycarbonyl-substituted amidinoamino, alkoxy, alkoxycarbonyl, carbamoyl, carboxy, hydroxy, trialkylsilyloxy, and cycloalkyl, substituted with one or more of the same or different substituents up to the maximum number of substitutions possible. 1-12 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, is alkyl; arylalkyl; arylalkyl substituted with from one to the maximum possible number of identical or different substituents selected from the group consisting of halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, amino, substituted amino, nitro, and hydroxy; formyl; alkylcarbonyl; arylalkylcarbonyl; alkoxycarbonyl; arylcarbonyl; aryloxycarbonyl; carbamoyl; alkylcarbamoyl; or arylalkylcarbamoyl, wherein the substituted amino has from one to the maximum possible number of identical or different substituents selected from substituent group IV. [Item 27B] R1 is hydrogen; C 1-12 Alkyl; Amidinoamino, C 1-6 Alkoxycarbonyl-substituted amidinoamino, C 1-6 Alkoxy, C 1-6 Alkoxycarbonyl, carbamoyl, carboxy, hydroxy, triC 1-6 Alkylsilyloxy, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkyl 1-12 Alkyl; C 6-10 Aryl C 1-6 Alkyl; halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of haloalkoxy, amino, substituted amino, nitro, and hydroxy. 6-10 Aryl C 1-6 Alkyl; Formyl; C1-12 Alkylcarbonyl; C 6-10 Aryl C 1-6 Alkylcarbonyl; C 1-12 Alkoxycarbonyl; C 6-10 Arylcarbonyl; C 6-10 Aryloxycarbonyl; Carbamoyl; C 1-12 Alkylcarbamoyl; or C 6-10 Aryl C 1-6 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein the substituted amino is alkylcarbamoyl, wherein the substituted amino has from 1 to the maximum possible number of identical or different substituents selected from Substituent Group IV. [Section 27C] R1 is C 1-12 Alkyl; Amidinoamino, C 1-6 Alkoxycarbonyl-substituted amidinoamino, C 1-6 Alkoxy, C 1-6 Alkoxycarbonyl, carbamoyl, carboxy, hydroxy, triC 1-6 Alkylsilyloxy, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkyl 1-12 Alkyl; C 6-10 Aryl C 1-6 Alkyl; or halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of haloalkoxy, amino, substituted amino, nitro, and hydroxy. 6-10 Aryl C 1-6 The compound according to any one of the preceding items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein the substituted amino is alkyl, and wherein the substituted amino has from 1 to the maximum possible number of identical or different substituents selected from Substituent Group IV. [Item 28] R3 is hydrogen; alkyl; formyl; substituted carbonyl; or alkyl substituted with from 1 to the maximum number of the same or different substituents selected from the group consisting of hydroxy, substituted oxy, substituted carbonyl, amino, substituted amino, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, and substituted heterocycloalkyl; arylalkyl; arylalkyl substituted with from 1 to the maximum number of the same or different substituents selected from the group consisting of halogen, nitro, hydroxy, substituted oxy, amino, substituted amino, alkyl, and substituted alkyl; heteroarylalkyl; or substituted heteroarylalkyl, wherein the substituted carbonyl, substituted oxy, substituted amino, cycloalkyl, substituted heterocycloalkyl, substituted alkyl, and substituted heteroarylalkyl in R3 each independently have from 1 to the maximum number of the same or different substituents selected from substituent group IV, or a compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Item 29B] R3 is hydrogen; alkyl; formyl; alkylcarbonyl; arylalkylcarbonyl; or alkyl substituted with one to the maximum number of the same or different substituents selected from the group consisting of hydroxy, trialkylsilyloxy, alkoxy, alkoxycarbonyl, alkoxycarbonylamino, cycloalkyl, carboxy, amino, amidinoamino, alkoxycarbonyl-substituted amidinoamino, carbamoyl, and heterocycloalkyl; arylalkyl; arylalkyl substituted with one to the maximum number of the same or different substituents selected from the group consisting of halogen, nitro, hydroxy, amino, monoalkylamino, dialkylamino, alkyl, haloalkyl, alkoxy, haloalkoxy, carboxyalkylcarbonylamino, carbamoylalkylcarbonylamino, cycloalkylcarbonylamino, and cycloalkylalkylamino; heteroarylalkyl; or alkoxycarbonyl-substituted heteroarylalkyl, and any one of the compounds described in any one of the above items, or their enantiomers, or their salts, or their solvates. [Item 29C] R3 is hydrogen; C 1-12 Alkyl; Formyl; C 1-6 Alkylcarbonyl; C 6-10 Aryl C 1-6 Alkylcarbonyl; or hydroxy, triC 1-6 Alkylsilyloxy, C 1-6 Alkoxy, C 1-6 Alkoxycarbonyl, C 1-6 Alkoxycarbonylamino, C 3-6 Cycloalkyl, carboxy, amino, amidinoamino, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkoxycarbonyl-substituted amidinoamino, carbamoyl, and 5- to 6-membered heterocycloalkyl 1-12 Alkyl; C 6-10 Aryl C 1-6 Alkyl; halogen, nitro, hydroxy, amino, mono C 1-6 Alkylamino, DiC 1-6 Alkylamino, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, C 1-6 Haloalkoxy, Carboxy C 1-6 Alkylcarbonylamino, Carbamoyl C 1-6 Alkylcarbonylamino, C 3-6 cycloalkylcarbonylamino, and C 3-6 Cycloalkyl C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkylamino 6-10 Aryl C 1-12 Alkyl; 5-10 membered heteroaryl C 1-6 Alkyl; or C 1-6 Alkoxycarbonyl-substituted 5- to 10-membered heteroaryl C 1-6 The compound according to any one of the above items, wherein R is alkyl, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Section 29D] R3 is C 1-12 Alkyl; Hydroxy; TriC1-6 Alkylsilyloxy, C 1-6 Alkoxy, C 1-6 Alkoxycarbonyl, C 1-6 Alkoxycarbonylamino, C 3-6 Cycloalkyl, carboxy, amino, amidinoamino, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkoxycarbonyl-substituted amidinoamino, carbamoyl, and 5- to 6-membered heterocycloalkyl 1-12 Alkyl; C 6-10 Aryl C 1-6 Alkyl; or halogen, nitro, hydroxy, amino, mono C 1-6 Alkylamino, DiC 1-6 Alkylamino, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, C 1-6 Haloalkoxy, Carboxy C 1-6 Alkylcarbonylamino, Carbamoyl C 1-6 Alkylcarbonylamino, C 3-6 cycloalkylcarbonylamino, and C 3-6 Cycloalkyl C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkylamino 6-10 Aryl C 1-12 The compound according to any one of the above items, wherein R is alkyl, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Section 29]R 2A and R 2Bare each independently hydrogen; alkyl; formyl; substituted carbonyl; alkyl substituted with from one to the maximum number of the same or different substituents selected from the group consisting of hydroxy, substituted oxy, substituted carbonyl, amino, substituted amino, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, and substituted heterocycloalkyl; arylalkyl; arylalkyl substituted with from one to the maximum number of the same or different substituents selected from the group consisting of halogen, nitro, hydroxy, substituted oxy, amino, substituted amino, alkyl, and substituted alkyl; heteroarylalkyl; or substituted heteroarylalkyl, wherein R 2A and R 2B The substituted carbonyl, substituted oxy, substituted amino, substituted cycloalkyl, substituted heterocycloalkyl, substituted alkyl, and substituted heteroarylalkyl in each independently have from one to the maximum possible number of substituents selected from Substituent Group IV, which may be the same or different, or R 2A and R 2B are taken together with the nitrogen atom to which they are attached to form a non-aryl heterocycle, and the non-aryl heterocycle is optionally substituted with one, or up to the maximum permissible number of, identical or different substituents selected from Substituent Group VI, or a compound or enantiomer thereof, or a salt or solvate thereof according to any one of the preceding items. [Section 30B]R 2A and R 2Bare each independently hydrogen; alkyl; formyl; alkylcarbonyl; arylalkylcarbonyl; alkyl substituted with from one to the maximum number of the same or different substituents selected from the group consisting of hydroxy, trialkylsilyloxy, alkoxy, alkoxycarbonyl, alkoxycarbonylamino, cycloalkyl, carboxy, amino, amidinoamino, alkoxycarbonyl-substituted amidinoamino, carbamoyl, and heterocycloalkyl; arylalkyl; arylalkyl substituted with from one to the maximum number of the same or different substituents selected from the group consisting of halogen, nitro, hydroxy, amino, monoalkylamino, dialkylamino, alkyl, haloalkyl, alkoxy, carboxyalkylcarbonylamino, carbamoylalkylcarbonylamino, cycloalkylcarbonylamino, and cycloalkylalkylamino; heteroarylalkyl; or alkoxycarbonyl-substituted heteroarylalkyl; or R 2A and R 2B are taken together with the nitrogen atom to which they are attached to form a non-aryl heterocycle, and the non-aryl heterocycle is optionally substituted with one, or up to the maximum permissible number of, identical or different substituents selected from Substituent Group VI, or a compound or enantiomer thereof, or a salt or solvate thereof according to any one of the preceding items. [Section 30C]R 2A and R 2B are each independently hydrogen; C 1-12 Alkyl; Formyl; C 1-6 Alkylcarbonyl; C 6-10 Aryl C 1-6 Alkylcarbonyl; Hydroxy, TriC 1-6 Alkylsilyloxy, C 1-6 Alkoxy, C 1-6 Alkoxycarbonyl, C 1-6 Alkoxycarbonylamino, C 3-10 Cycloalkyl, carboxy, amino, amidinoamino, C 1-6C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkoxycarbonyl-substituted amidinoamino, carbamoyl, and 5- to 6-membered heterocycloalkyl 1-12 Alkyl; C 6-10 Aryl C 1-12 Alkyl; halogen, nitro, hydroxy, amino, mono C 1-6 Alkylamino, DiC 1-6 Alkylamino, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, Carboxy C 1-6 Alkylcarbonylamino, Carbamoyl C 1-6 Alkylcarbonylamino, C 3-6 cycloalkylcarbonylamino, and C 3-6 Cycloalkyl C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkylamino 6-10 Aryl C 1-12 Alkyl; 5-10 membered heteroaryl C 1-12 Alkyl; or C 1-6 Alkoxycarbonyl-substituted 5- to 10-membered heteroaryl C 1-12 alkyl or R 2A and R 2B together with the nitrogen atom to which they are attached form a 5-6 membered non-aryl heterocycle, wherein the non-aryl heterocycle is not substituted with halogen, nitro, hydroxy, amino, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, C 1-6 Alkoxycarbonyl, C 3-6 cycloalkylcarbonylamino, and C 3-6 Cycloalkyl C 1-6 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, which may be substituted with one or more identical or different substituents selected from the group consisting of alkylamino, ... [Section 30D]R 2Aand R 2B are each independently hydrogen; C 1-12 Alkyl; Hydroxy; TriC 1-6 Alkylsilyloxy, C 1-6 Alkoxy, C 1-6 Alkoxycarbonyl, C 1-6 Alkoxycarbonylamino, C 3-10 Cycloalkyl, carboxy, amino, amidinoamino, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkoxycarbonyl-substituted amidinoamino, carbamoyl, and 5- to 6-membered heterocycloalkyl 1-12 Alkyl; C 6-10 Aryl C 1-12 Alkyl; halogen, nitro, hydroxy, amino, mono C 1-6 Alkylamino, DiC 1-6 Alkylamino, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, Carboxy C 1-6 Alkylcarbonylamino, Carbamoyl C 1-6 Alkylcarbonylamino, C 3-6 cycloalkylcarbonylamino, and C 3-6 Cycloalkyl C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkylamino 6-10 Aryl C 1-12 Alkyl; 5-10 membered heteroaryl C 1-12 Alkyl; or C 1-6 Alkoxycarbonyl-substituted 5- to 10-membered heteroaryl C 1-12 alkyl or R 2A and R 2B together with the nitrogen atom to which they are attached form a 5-6 membered non-aryl heterocycle, wherein the non-aryl heterocycle is not substituted with halogen, nitro, hydroxy, amino, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, C 1-6 Alkoxycarbonyl, C3-6 cycloalkylcarbonylamino, and C 3-6 Cycloalkyl C 1-6 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, which may be substituted with one or more identical or different substituents selected from the group consisting of alkylamino, ... [Item 30] R1 is alkyl; alkyl substituted with from 1 to the maximum number of identical or different substituents selected from the group consisting of amidinoamino, carbamoyl, carboxy, hydroxy, and cycloalkyl; arylalkyl; or arylalkyl substituted with from 1 to the maximum number of identical or different substituents selected from the group consisting of halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, substituted amino, and hydroxy, wherein the substituted amino has from 1 to the maximum number of identical or different substituents selected from substituent group IV, or a compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Section 31B] R1 is C 1-12 Alkyl; amidinoamino, carbamoyl, carboxy, hydroxy, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkyl 1-12 Alkyl; C 6-10 Aryl C 1-6 Alkyl; or halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of haloalkoxy, substituted amino, and hydroxy. 6-10 Aryl C 1-6 The compound according to any one of the preceding items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein the substituted amino is alkyl, and wherein the substituted amino has from 1 to the maximum possible number of identical or different substituents selected from Substituent Group IV. [Section 31] R 2A is hydrogen and R 2B is alkyl; alkyl substituted with from 1 to the maximum possible number of identical or different substituents selected from the group consisting of amidinoamino, carbamoyl, carboxy, hydroxy, and cycloalkyl; arylalkyl; or arylalkyl substituted with from 1 to the maximum possible number of identical or different substituents selected from the group consisting of halogen and alkyl, or an enantiomer thereof, or a salt or solvate thereof according to any one of the above items. [Section 32B]R 2A is hydrogen and R 2B is C 1-12 Alkyl; amidinoamino, carbamoyl, carboxy, hydroxy, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkyl 1-12 Alkyl; C 6-10 Aryl C 1-6 Alkyl; or halogen and C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkyl 6-10 Aryl C 1-6 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R is alkyl. [Item 32] R3 is alkyl; alkyl substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of amidinoamino, carbamoyl, carboxy, hydroxy, and cycloalkyl; arylalkyl, or a compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Section 32B] R3 is C 1-12 Alkyl; alkyl substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of amidinoamino, carbamoyl, carboxy, hydroxy, and cycloalkyl; C 6-10 Aryl C 1-6A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein the compound is alkyl; or arylalkyl substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkyl and hydroxy. [Item 32C] R1 is methyl, n-propyl, isobutyl, isopentyl, amidinoaminopropyl, tert-butoxycarbonyl-substituted amidinoaminopropyl, tert-butoxyethyl, tert-butoxypropyl, (tert-butoxycarbonyl)ethyl, carboxyethyl, hydroxyethyl, hydroxypropyl, aminopropyl, 2-(tert-butyl-dimethylsilyloxy)ethyl, cyclopentylmethyl, cyclohexylmethyl, benzyl, phenylethyl, naphthalenylmethyl, fluorobenzyl, chlorobenzyl, dichlorobenzyl, methylbenzyl, (tert-butyl)benzyl, methoxybenzyl, ethoxybenzyl, (tert-butoxy)benzyl, (trifluoromethoxy)benzyl, (dimethylamino)benzyl, nitrobenzyl, or hydroxybenzyl, or a compound or enantiomer thereof according to any one of the above items, or a salt or solvate thereof. [Section 32D]R 2A and R 2Bare each independently isopropyl, isobutyl, sec-butyl, pentyl, isopentyl, n-hexyl, heptyl, amidinoaminopropyl, tert-butoxycarbonyl-substituted amidinoaminopropyl, tert-butoxyethyl, tert-butoxycarbonylmethyl, (tert-butoxycarbonyl)ethyl, carbamoylethyl, carboxyethyl, hydroxyethyl, aminopropyl, aminobutyl, ((tert-butoxycarbonyl)amino)butyl, cyclopentylmethyl, cyclohexylmethyl, (1,2,3,4-tetrahydronaphthalenyl)methyl, ( (tetrahydro-2H-pyranyl)methyl, benzyl, phenylethyl, naphthalenylmethyl, (naphthalenyl)ethyl, β-hydroxyphenethyl, α-(hydroxymethyl)phenethyl, fluorobenzyl, chlorobenzyl, dichlorobenzyl, (fluorophenyl)ethyl, methylbenzyl, (trifluoromethyl)benzyl, methoxybenzyl, (tert-butoxy)benzyl, hydroxybenzyl, pyridinylmethyl, quinolinylethyl, (1-(tert-butoxycarbonyl)-1H-indolyl)ethyl, cyclopentyl, or cyclohexyl; or 2A and R 2B The compound according to any one of the preceding items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein: are taken together with the nitrogen atom to which they are attached to form a pyrrolidine ring or a piperidine ring. [Item 32E] R3 is n-propyl, isobutyl, isopentyl, amidinoaminopropyl, tert-butoxycarbonyl-substituted amidinoaminopropyl, (methoxycarbonyl)ethyl, (tert-butoxycarbonyl)ethyl, carboxyethyl, hydroxyethyl, aminopropyl, (tert-butyldimethylsilyloxy)ethyl, ((tert-butoxycarbonyl)amino)butyl, cyclopentylmethyl, cyclohexylmethyl, cyclohexylethyl, benzyl, phenylethyl, phenylpropyl, phenylbutyl, naphthalenylmethyl, naphthalenylethyl, chlorobenzyl, methylbenzyl, (methylphenyl)ethyl, (isopropylphenyl)ethyl, (tert-butoxy)benzyl, or hydroxybenzyl, or an enantiomer thereof, or a salt thereof, or a solvate thereof, according to any one of the above items. [Item 32F] The compound is a compound selected from the group consisting of compound numbers IIB-1 to IIB-1129 and IIF-1 to IIF-1047. The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Item 33] An antiviral agent against a virus of the genus Lyssavirus, comprising the compound according to any one of the above items or a pharmaceutically acceptable salt thereof. [Item 34] The antiviral agent according to any one of the above items, wherein the Lyssavirus virus includes rabies virus. [Item 35] A pharmaceutical composition comprising the compound according to any one of the above items or a pharmaceutically acceptable salt thereof. [Item 36] The pharmaceutical agent according to any one of the above items, which is a preventive or therapeutic agent for rabies. [Item 37] A pharmaceutical composition comprising the compound according to any one of the above items or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. [Item 38] A pharmaceutical composition for preventing or treating rabies, comprising the compound according to any one of the above items or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. [Item 39] An anticancer agent comprising the compound according to any one of the above items or a pharmaceutically acceptable salt thereof. [Item 40] The pharmaceutical agent according to any one of the above items, which is a preventive or therapeutic agent for cancer. [Item 41] A pharmaceutical composition for preventing or treating cancer, comprising the compound according to any one of the above items or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. [Item 42] A method for preventing or treating rabies, comprising administering to a patient in need of prevention or treatment a prophylactically or therapeutically effective amount of a compound described in any one of the above items or a pharmaceutically acceptable salt thereof, an antiviral agent described in any one of the above items, a medicine described in any one of the above items, or a pharmaceutical composition described in any one of the above items. [Item 43] Use of the compound according to any one of the above items or a pharmaceutically acceptable salt thereof, or the antiviral agent according to any one of the above items, for the manufacture of a medicament for preventing or treating rabies. [Item 44] A method for preventing or treating cancer, comprising administering to a patient in need of prevention or treatment a prophylactically or therapeutically effective amount of a compound described in any one of the above items or a pharmaceutically acceptable salt thereof, an anticancer agent described in any one of the above items, a medicine described in any one of the above items, or a pharmaceutical composition described in any one of the above items. [Item 45] Use of the compound according to any one of the above items or a pharmaceutically acceptable salt thereof, or the anticancer agent according to any one of the above items, for the manufacture of a medicament for preventing or treating cancer.

[0007] The present disclosure also provides the following:

[0008] [Term A1] Formula IF: [ka] or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1, R2, and R3 are each independently optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl, optionally substituted cycloalkylalkyl, or optionally substituted heterocycloalkylalkyl; R4 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocycloalkylalkyl, optionally substituted alkylcarbonyl, optionally substituted alkoxycarbonyl, optionally substituted arylcarbonyl, optionally substituted heteroarylcarbonyl, or optionally substituted carbamoyl; A compound or its enantiomer, or a salt thereof, or a solvate thereof. [Term A2] Formula IB [ka] or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1, R2, and R3 are each independently optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl, optionally substituted cycloalkylalkyl, or optionally substituted heterocycloalkylalkyl; R4 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocycloalkylalkyl, optionally substituted alkylcarbonyl, optionally substituted alkoxycarbonyl, optionally substituted arylcarbonyl, optionally substituted heteroarylcarbonyl, or optionally substituted carbamoyl; A compound or its enantiomer, or a salt thereof, or a solvate thereof. [Item A3] R1, R2, and R3 are each independently an optionally substituted alkyl, an optionally substituted arylalkyl, an optionally substituted heteroarylalkyl, or an optionally substituted cycloalkylalkyl; R4 is hydrogen, optionally substituted alkyl, optionally substituted alkylcarbonyl, optionally substituted arylcarbonyl, optionally substituted alkoxycarbonyl, or optionally substituted carbamoyl; A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item A3a] R1, R2, and R3 are each independently an optionally substituted alkyl, an optionally substituted arylalkyl, an optionally substituted heteroarylalkyl, or an optionally substituted cycloalkylalkyl; R4 is hydrogen, optionally substituted alkyl, optionally substituted alkylcarbonyl, optionally substituted arylcarbonyl, or optionally substituted alkoxycarbonyl; A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item A4] R1, R2 and R3 are each independently an optionally substituted C 1-6 Alkyl, optionally substituted C6-10 Aryl C 1-6 Alkyl, optionally substituted 5-10 membered heteroarylC 1-6 Alkyl or optionally substituted C 3-6 Cycloalkyl C 1-6 is alkyl, R4 is hydrogen, optionally substituted C 1-6 Alkyl, optionally substituted C 1-6 Alkylcarbonyl, optionally substituted C 6-10 Arylcarbonyl, optionally substituted C 1-6 Alkoxycarbonyl or optionally substituted C 1-6 alkylcarbamoyl, A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item A4b] R1, R2 and R3 are each independently an optionally substituted C 1-6 Alkyl, optionally substituted C 6-10 Aryl C 1-6 Alkyl, optionally substituted 5-10 membered heteroarylC 1-6 Alkyl or optionally substituted C 3-6 Cycloalkyl C 1-6 is alkyl, R4 is hydrogen, optionally substituted C 1-6 Alkyl, optionally substituted C 1-6 Alkylcarbonyl, optionally substituted C 6-10 arylcarbonyl, or optionally substituted C 1-6 is an alkoxycarbonyl, A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item A5] R1, R2 and R3 are each independently C 1-6 Alkyl, hydroxy-substituted C 1-6 Alkyl, carbamoyl substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, amidinoamino substituted C 1-6Alkyl, carboxy-substituted C 1-6 Alkyl, C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkoxycarbonyl-substituted 5- to 10-membered heteroaryl C 1-6 Alkyl, C 1-4 Alkyl-substituted C 6-10 Aryl C 1-6 Alkyl, hydroxy-substituted C 6-10 Aryl C 1-6 Alkyl, halogen-substituted C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkoxy-substituted C 6-10 Aryl C 1-6 Alkyl, (optionally substituted amino)-C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkoxycarbonyl-substituted C 1-6 Alkyl, C 1-4 Alkoxycarbonylamino-substituted C 1-6 Alkyl, 5-6 membered heterocycloalkyl substituted C 1-6 Alkyl, or C 3-6 Cycloalkyl C 1-6 is alkyl, A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item A5a] R1, R2 and R3 are each independently C 1-6 Alkyl, hydroxy-substituted C 1-6 Alkyl, carbamoyl substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, amidinoamino substituted C 1-6 Alkyl, carboxy-substituted C 1-6 Alkyl, C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkoxycarbonyl-substituted 5- to 10-membered heteroaryl C 1-6 Alkyl, C 1-4 Alkyl-substituted C 6-10 Aryl C 1-6Alkyl, hydroxy-substituted C 6-10 Aryl C 1-6 Alkyl, halogen-substituted C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkoxy-substituted C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkoxycarbonyl-substituted C 1-6 Alkyl, C 1-4 Alkoxycarbonylamino-substituted C 1-6 Alkyl, 5-6 membered heterocycloalkyl substituted C 1-6 Alkyl, or C 3-6 Cycloalkyl C 1-6 is alkyl, A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item A5b] R4 is hydrogen, optionally substituted C 1-6 Alkyl, optionally substituted C 1-6 Alkylcarbonyl, optionally substituted C 6-10 Aryl C 1-6 Alkylcarbonyl, optionally substituted C 6-10 Arylcarbonyl, optionally substituted C 1-6 Alkoxycarbonyl, optionally substituted C 6-10 Aryl C 1-6 Alkoxycarbonyl, carbamoyl, optionally substituted C 1-6 Alkylcarbamoyl or optionally substituted C 6-10 Aryl C 1-6 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, which is alkylcarbamoyl. [Item A5c] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1, R2, and R3 are each independently an optionally substituted alkyl or an optionally substituted arylalkyl. [Item A5d] R1, R2 and R3 are each independently an optionally substituted C 1-6 Alkyl or optionally substituted C 6-10 Aryl C 1-6 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R is alkyl. [Item A5e] R1, R2 and R3 are each independently C 1-6 Alkyl, C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkyl-substituted C 6-10 Aryl C 1-6 Alkyl, halogen-substituted C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkoxy-substituted C 6-10 Aryl C 1-6 Alkyl, or (optionally substituted amino)-C 6-10 Aryl C 1-6 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R is alkyl. [Item A5f] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R2 is naphthalen-1-ylmethyl or optionally substituted benzyl. [Item A5g] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1 and R3 are each independently alkyl or optionally substituted benzyl, and R2 is optionally substituted benzyl. [Item A5h] R1 and R3 are each independently C 1-6 Alkyl, benzyl, C 1-4 Alkyl-substituted benzyl, chloro-substituted benzyl, C 1-4 alkoxy-substituted benzyl, or The compound according to any one of the preceding items, wherein R is amino-substituted benzyl, and R2 is benzyl, or chloro-substituted benzyl, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Item A5i] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1 and R3 are each independently isobutyl, isopentyl, 4-(dimethylamino)benzyl, 4-methylbenzyl, 4-methoxybenzyl, 3-chlorobenzyl, 4-chlorobenzyl, or 3,4-dichlorobenzyl, and R2 is benzyl, 3-chlorobenzyl, or 3,4-dichlorobenzyl. [Item A6] R4 is hydrogen, C 1-6 Alkyl, C 1-6 Alkyl carbonyl, C 6-10 Arylcarbonyl, C 6-10 Aryl C 1-6 Alkyl carbonyl, C 1-6 Alkoxycarbonyl, C 6-10 Aryl C 1-6 Alkoxycarbonyl, carbamoyl, C 1-6 Alkylcarbamoyl or C 6-10 Aryl C 1-6 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, which is alkylcarbamoyl. [Item A6b] R4 is hydrogen, C 1-6 Alkyl, C 1-6 Alkyl carbonyl, C 6-10 Arylcarbonyl, or C 1-6 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, which is alkoxycarbonyl. [Term A7] R4 is hydrogen, C 1-4 Alkyl, C 1-4 Alkylcarbonyl, C6 arylcarbonyl, C6 arylC 1-4 Alkyl carbonyl, C 1-4 Alkoxycarbonyl, C6 arylC 1-4 Alkoxycarbonyl, carbamoyl, C 1-4Alkylcarbamoyl or C6 arylC 1-4 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, which is alkylcarbamoyl. [Item A7b] R4 is hydrogen, C 1-4 Alkyl, C 1-4 Alkylcarbonyl, C6 arylcarbonyl, or C 1-4 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, which is alkoxycarbonyl. [Item A8] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R4 is hydrogen, methyl, ethyl, acetyl, benzoyl, methoxycarbonyl, tert-butoxycarbonyl, or propylcarbamoyl. [Item A8b] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R4 is hydrogen, methyl, ethyl, acetyl, benzoyl, methoxycarbonyl, or tert-butoxycarbonyl. [Term A9] R2 is C 1-4 Alkyl, hydroxy-substituted C 1-4 Alkyl, carbamoyl substituted C 1-4 Alkyl, amino substituted C 1-4 Alkyl, amidinoamino substituted C 1-4 Alkyl, carboxy-substituted C 1-4 Alkyl, C 6-10 Aryl C 1-4 Alkyl, C 1-4 Alkoxycarbonyl-substituted 5- to 10-membered heteroaryl C 1-4 Alkyl, C 1-4 Alkyl-substituted C 6-10 Aryl C 1-4 Alkyl, hydroxy-substituted C 6-10 Aryl C 1-4 Alkyl, halogen-substituted C 6-10 Aryl C 1-4 Alkyl, C 1-4 Alkoxy-substituted C 6-10 Aryl C1-4 Alkyl, C 1-4 Alkoxycarbonyl-substituted C 1-4 Alkyl, C 1-4 Alkoxycarbonylamino-substituted C 1-4 Alkyl, 5-6 membered heterocycloalkyl substituted C 1-4 Alkyl, or C 5-6 Cycloalkyl C 1-4 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R is alkyl. [Item A9b] R2 is isopropyl, 1-methylpropyl, isobutyl, isopentyl, n-hexyl, hydroxymethyl, 2-hydroxyethyl, carbamoylmethyl, 3-amino-3-oxopropyl, 4-aminobutyl, 3-(amidinoamino)propyl, 2-carboxyethyl, benzyl, phenethyl, naphthalen-1-ylmethyl, 2-(naphthalen-1-yl)ethyl, 2-(1-(tert-butoxycarbonyl)-1H-indol-3-yl)ethyl, 3-methylbenzyl, 4 4-(tert-butoxycarbonyl)amino)butyl, 2-(tert-butoxycarbonyl)methyl, 4-hydroxybenzyl, 4-fluorobenzyl, 3-chlorobenzyl, 4-chlorobenzyl, 3,4-dichlorobenzyl, 4-(tert-butoxy)benzyl, 2-(tert-butoxy)-2-oxoethyl, 4-((tert-butoxycarbonyl)amino)butyl, (tetrahydro-2H-pyran-2-yl)methyl, or cyclohexylmethyl, or an enantiomer thereof, or a salt thereof, or a solvate thereof, according to any one of the preceding items. [Item A10] R2 is isobutyl, 2-hydroxyethyl, 3-amino-3-oxopropyl, 4-aminobutyl, 2-carboxyethyl, benzyl, phenethyl, naphthalen-1-ylmethyl, 2-(naphthalen-1-yl)ethyl, 2-(1-(tert-butoxycarbonyl)-1H-indol-3-yl)ethyl, 3-methylbenzyl, 4-methylbenzyl, 4-hydroxybenzyl, 3-chlorobenzyl, 4-chlorobenzyl, 3,4-dichlorobenzyl, 4-(tert-butoxy)benzyl, 2-(tert-butoxy)-2-oxoethyl, 4-((tert-butoxycarbonyl)amino)butyl, (tetrahydro-2H-pyran-2-yl)methyl, or cyclohexylmethyl, or a compound or enantiomer thereof according to any one of the above items, or a salt or solvate thereof. [Item A10b] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R2 is 1-methylpropyl, isopropyl, isobutyl, isopentyl, n-hexyl, benzyl, 4-hydroxybenzyl, 4-fluorobenzyl, 2-carboxyethyl, carbamoylmethyl, carbamoylethyl, 3-(amidinoamino)propyl, hydroxymethyl, 2-hydroxyethyl, phenethyl, naphthalen-1-ylmethyl, or cyclohexylmethyl. [Item A11] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R2 is isopropyl, isobutyl, isopentyl, benzyl, 4-hydroxybenzyl, 4-fluorobenzyl, 2-carboxyethyl, carbamoylmethyl, 3-(amidinoamino)propyl, 2-hydroxyethyl, phenethyl, naphthalen-1-ylmethyl, or n-hexyl. [Item A11b] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R2 is 1-methylpropyl, isopropyl, isobutyl, benzyl, 4-hydroxybenzyl, 2-carboxyethyl, 3-(amidinoamino)propyl, or naphthalen-1-ylmethyl. [Term A12] R1 is C1-6 Alkyl, hydroxy-substituted C 1-4 Alkyl, carbamoyl substituted C 1-4 Alkyl, amino substituted C 1-6 Alkyl, amidinoamino substituted C 1-4 Alkyl, carboxy-substituted C 1-4 Alkyl, C 1-4 Alkoxycarbonyl-substituted C 1-4 Alkyl, C 6-10 Aryl C 1-4 Alkyl, hydroxy-substituted C 6-10 Aryl C 1-4 Alkyl, C 1-4 Alkoxy-substituted C 6-10 Aryl C 1-4 Alkyl, halo-substituted C 6-10 Aryl C 1-4 Alkyl, or C 5-6 Cycloalkyl C 1-4 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R is alkyl. [Item A12b] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1 is methyl, isopropyl, isobutyl, isopentyl, n-hexyl, 3-amino-3-oxopropyl, 3-(tert-butoxy)-3-oxopropyl, benzyl, naphthalen-1-ylmethyl, 2-carboxyethyl, carbamoylmethyl, 3-(amidinoamino)propyl, 4-fluorobenzyl, 4-hydroxybenzyl, 4-(tert-butoxy)benzyl, 3,4-dichlorobenzyl, naphthalen-1-ylmethyl, phenethyl, hydroxymethyl, 2-hydroxyethyl, or cyclohexylmethyl. [Item A13] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1 is methyl, isobutyl, isopentyl, 3-(tert-butoxy)-3-oxopropyl, benzyl, naphthalen-1-ylmethyl, 4-hydroxybenzyl, 4-(tert-butoxy)benzyl, 3,4-dichlorobenzyl, or cyclohexylmethyl. [Item A14] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1 is isopropyl, isobutyl, isopentyl, n-hexyl, cyclohexylmethyl, benzyl, phenethyl, naphthalen-1-ylmethyl, 4-hydroxybenzyl, 4-fluorobenzyl, 2-carboxyethyl, carbamoylmethyl, carbamoylethyl, 3-(amidinoamino)propyl, hydroxymethyl, or hydroxyethyl. [Item A14b] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1 is isobutyl, isopentyl, cyclohexylmethyl, benzyl, phenethyl, naphthalen-1-ylmethyl, 4-hydroxybenzyl, 4-fluorobenzyl, 2-carboxyethyl, carbamoylmethyl, 3-(amidinoamino)propyl, or hydroxyethyl. [Item A14c] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1 is isobutyl, benzyl, 4-hydroxybenzyl, 2-carboxyethyl, 3-(amidinoamino)propyl, or naphthalen-1-ylmethyl. [Item A15] R3 is C 1-4 Alkyl, hydroxy-substituted C 1-4 Alkyl, carbamoyl substituted C 1-4 Alkyl, C 1-4 Alkoxycarbonyl-substituted C 1-4 Alkyl, amino substituted C 1-4 Alkyl, amidinoamino substituted C 1-4 Alkyl, carboxy-substituted C 1-4 Alkyl, C 6-10 Aryl C 1-4 Alkyl, C 1-4 Alkyl-substituted C 6-10 Aryl C 1-4 Alkyl, hydroxy-substituted C 6-10 Aryl C 1-4 Alkyl, or C 5-6 Cycloalkyl C 1-4The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R is alkyl. [Item A15b] Isopropyl, isobutyl, isopentyl, n-hexyl, hydroxymethyl, 2-hydroxyethyl, carbamoylmethyl, 3-amino-3-oxopropyl, 4-aminobutyl, 3-(amidinoamino)propyl, 2-carboxyethyl, benzyl, phenethyl, naphthalen-1-ylmethyl, 4-hydroxybenzyl, 4-fluorobenzyl, 3-methylbenzyl, 4-methylbenzyl, 3-methoxy-3-oxopropyl, 4-((tert-butoxycarbonyl)amino)butyl, or cyclohexylmethyl, or an enantiomer thereof, or a salt thereof, or a solvate thereof, according to any one of the above items. [Item A16] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R3 is isobutyl, isopentyl, 3-amino-3-oxopropyl, 3-methoxy-3-oxopropyl, 4-aminobutyl, 2-carboxyethyl, benzyl, phenethyl, 3-methylbenzyl, 4-methylbenzyl, 4-hydroxybenzyl, 4-((tert-butoxycarbonyl)amino)butyl, or cyclohexylmethyl. [Item A17] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R3 is isopropyl, isobutyl, isopentyl, n-hexyl, cyclohexylmethyl, benzyl, phenethyl, naphthalen-1-ylmethyl, 4-hydroxybenzyl, 4-fluorobenzyl, 2-carboxyethyl, carbamoylmethyl, carbamoylethyl, 3-(amidinoamino)propyl, hydroxymethyl, or hydroxyethyl. [Item A17b] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R3 is isobutyl, isopentyl, benzyl, phenethyl, 4-hydroxybenzyl, 2-carboxyethyl, carbamoylmethyl, 3-(amidinoamino)propyl, hydroxymethyl, or naphthalen-1-ylmethyl. [Item A17c] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R3 is isobutyl, benzyl, 4-hydroxybenzyl, 2-carboxyethyl, 3-(amidinoamino)propyl, or naphthalen-1-ylmethyl. [Item A18] The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R4 is hydrogen or alkyl. [Item A18a] R4 is hydrogen or C 1-6 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R is alkyl. [Item A18b] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R4 is hydrogen or ethyl. [Item A19] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R4 is hydrogen. [Term A20] R1 is C 1-6 Alkyl or C 6-10 Aryl C 1-6 alkyl, and R2 and R3 are each independently C 1-6 Alkyl or optionally substituted C 6-10 Aryl C 1-6 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R is alkyl. [Item A21] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1 is isobutyl, isopentyl, or benzyl, R2 is isobutyl, benzyl, phenethyl, 3-methylbenzyl, 4-methylbenzyl, or 3,4-dichlorobenzyl, and R3 is isobutyl, benzyl, phenethyl, 3-methylbenzyl, or 4-methylbenzyl. [Item A22] The compound according to any one of the above items, wherein the compound is a compound of formula IF, R1 is isobutyl, R2 is benzyl, and R3 is benzyl, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Item A23] The compound according to any one of the above items, or its enantiomer, or a salt or solvate thereof, wherein the compound is a compound of formula IF, wherein R1 is benzyl, R2 is benzyl, and R3 is isobutyl. [Item A24] The compound according to any one of the above items, wherein the compound is a compound of formula IF, R1 is isobutyl, R2 is benzyl, and R3 is 3-methylbenzyl, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Item A25] The compound according to any one of the above items, wherein the compound is a compound of formula IF, R1 is benzyl, R2 is 3,4-dichlorobenzyl, and R3 is isobutyl, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Section A26] The compound of the formula IF may be 18,IF-19,IF-20,IF-22,IF-23,IF-24,IF-25,IF-26,IF-27,IF-28,IF-29,IF-30,IF-31,IF-32,IF-33,IF-34,IF-35,IF-36,IF-38,IF IF-39, IF-40, IF-41, IF-42, IF-43, IF-44, IF-45, IF-46, IF-47, IF-49, IF-50, IF-54, IF-57, IF-58, IF-68, IF-69, IF-70, IF-71, IF-72, IF-73, IF-74, IF-76, IF-77, IF-80, and IF-81 to IF-884, or an enantiomer thereof, or a salt thereof, or a solvate thereof according to any one of the preceding items. [Item A26b] The compound of formula IF is (3S * ,3aS* ,6S * ,7R * ,7aS * )-N,7-Dibenzyl-1-isobutyloctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aS * ,6S * ,7R * ,7aS * )-1,7-dibenzyl-N-isobutyloctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aS * ,6S * ,7R * ,7aS * )-N,1-dibenzyl-7-isobutyloctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aS * ,6S * ,7R * ,7aS * )-N,7-Dibenzyl-1-isopentyloctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aS * ,6S * ,7R * ,7aS * )-N-benzyl-1-isobutyl-7-phenethyloctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aS * ,6S * ,7R * ,7aS * )-N-benzyl-1-isobutyl-7-(3-methylbenzyl)octahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aS * ,6S * ,7R * ,7aS *)-N-benzyl-1-isobutyl-7-(4-methylbenzyl)octahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aS * ,6S * ,7R * ,7aS * )-7-benzyl-1-isobutyl-N-(3-methylbenzyl)octahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aS * ,6S * ,7R * ,7aS * )-1-benzyl-N-(3,4-dichlorobenzyl)-7-isobutyloctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide or (3S * ,3aS * ,6S * ,7R * ,7aS * 2. The compound according to any one of the preceding items, wherein the compound is N,7-dibenzyl-4-ethyl-1-isobutyloctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, or an enantiomer thereof, a salt thereof, or a solvate thereof. [Section A27] The compound of formula IB is IB-1, IB-2, IB-3, IB-4, IB-5, IB-6, IB-7, IB-8, IB-9, IB-10, IB-11, IB-12, IB-13, IB-14, IB-15, IB-16, IB-17, IB-18, IB-19, IB-20,IB-21,IB-22,IB-23,IB-24,IB-25,IB-26,IB-27,IB-28,IB-29,IB-30,IB-31,IB-32,IB-33,IB-34,IB-35,IB-36,IB-37,IB-38,IB-39,IB The compound according to any one of the preceding items, which is a compound selected from the group consisting of IB-40, IB-41, IB-42, IB-43, IB-44, IB-45, IB-46, IB-47, IB-49, IB-50, IB-54, IB-57, IB-58, IB-64, IB-68, IB-69, IB-70, IB-71, IB-72, IB-73, IB-74, IB-75, IB-76, IB-77, IB-78, IB-79, IB-80, and IB-81 to IB-923, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Item A27b] The compound of formula IB is (3S * ,3aS * ,6R * ,7R * ,7aS * )-7-benzyl-N,1-diisobutyloctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-1-benzyl-N,7-diisobutyloctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-N-benzyl-1,7-diisobutyloctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R *,7R * ,7aS * )-N,7-Dibenzyl-1-isopentyloctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-1-benzyl-7-isobutyl-N-phenethyloctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-N-benzyl-1-isobutyl-7-(3-methylbenzyl)octahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide or (3S * ,3aS * ,6R * ,7R * ,7aS * 2. The compound according to any one of the preceding items, which is 7-benzyl-1-isobutyl-N-(3-methylbenzyl)octahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Term A28] Formula IIF: [ka] or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1, R2, and R3 are each independently optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl, optionally substituted cycloalkylalkyl, or optionally substituted heterocycloalkylalkyl; A compound or its enantiomer, or a salt thereof, or a solvate thereof. [Term A29] Formula IIB: [ka] or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1, R2, and R3 are each independently optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl, optionally substituted cycloalkylalkyl, or optionally substituted heterocycloalkylalkyl; A compound or its enantiomer, or a salt thereof, or a solvate thereof. [Item A30] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1, R2, and R3 are each independently an optionally substituted alkyl, an optionally substituted arylalkyl, an optionally substituted heteroarylalkyl, or an optionally substituted cycloalkylalkyl. [Item A31] R1, R2 and R3 are each independently an optionally substituted C 1-6 Alkyl, optionally substituted C 6-10 Aryl C 1-6 Alkyl, optionally substituted 5-10 membered heteroarylC 1-6 Alkyl or optionally substituted C 3-6 Cycloalkyl C 1-6 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R is alkyl. [Item A32] R1, R2 and R3 are each independently C 1-6 Alkyl, hydroxy-substituted C 1-6 Alkyl, carbamoyl substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, amidinoamino substituted C 1-6Alkyl, carboxy-substituted C 1-6 Alkyl, C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkoxycarbonyl-substituted 5- to 10-membered heteroaryl C 1-6 Alkyl, C 1-4 Alkyl-substituted C 6-10 Aryl C 1-6 Alkyl, hydroxy-substituted C 6-10 Aryl C 1-6 Alkyl, halogen-substituted C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkoxy-substituted C 6-10 Aryl C 1-6 Alkyl, (optionally substituted amino)-C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkoxycarbonyl-substituted C 1-6 Alkyl, C 1-4 Alkoxycarbonylamino-substituted C 1-6 Alkyl, 5-6 membered heterocycloalkyl substituted C 1-6 Alkyl, or C 3-6 Cycloalkyl C 1-6 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R is alkyl. [Item A32a] R1, R2 and R3 are each independently C 1-6 Alkyl, hydroxy-substituted C 1-6 Alkyl, carbamoyl substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, amidinoamino substituted C 1-6 Alkyl, carboxy-substituted C 1-6 Alkyl, C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkoxycarbonyl-substituted 5- to 10-membered heteroaryl C 1-6 Alkyl, C 1-4 Alkyl-substituted C 6-10 Aryl C 1-6Alkyl, hydroxy-substituted C 6-10 Aryl C 1-6 Alkyl, halogen-substituted C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkoxy-substituted C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkoxycarbonyl-substituted C 1-6 Alkyl, C 1-4 Alkoxycarbonylamino-substituted C 1-6 Alkyl, 5-6 membered heterocycloalkyl substituted C 1-6 Alkyl, or C 3-6 Cycloalkyl C 1-6 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R is alkyl. [Item A32b] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1, R2, and R3 are each independently an optionally substituted alkyl, or an optionally substituted arylalkyl. [Item A32c] R1, R2 and R3 are each independently an optionally substituted C 1-6 Alkyl or optionally substituted C 6-10 Aryl C 1-6 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R is alkyl. [Item A33] R2 is C 1-4 Alkyl, hydroxy-substituted C 1-4 Alkyl, carbamoyl substituted C 1-4 Alkyl, amino substituted C 1-4 Alkyl, amidinoamino substituted C 1-4 Alkyl, carboxy-substituted C 1-4 Alkyl, C 6-10 Aryl C 1-4 Alkyl, C 1-4 Alkoxycarbonyl-substituted 5- to 10-membered heteroaryl C 1-4 Alkyl, C 1-4Alkyl-substituted C 6-10 Aryl C 1-4 Alkyl, hydroxy-substituted C 6-10 Aryl C 1-4 Alkyl, halogen-substituted C 6-10 Aryl C 1-4 Alkyl, C 1-4 Alkoxy-substituted C 6-10 Aryl C 1-4 Alkyl, C 1-4 Alkoxycarbonyl-substituted C 1-4 Alkyl, C 1-4 Alkoxycarbonylamino-substituted C 1-4 Alkyl, 5-6 membered heterocycloalkyl substituted C 1-4 Alkyl, or C 5-6 Cycloalkyl C 1-4 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R is alkyl. [Item A33b] R2 is isopropyl, 1-methylpropyl, isobutyl, isopentyl, n-hexyl, hydroxymethyl, 2-hydroxyethyl, carbamoylmethyl, 3-amino-3-oxopropyl, 4-aminobutyl, 3-(amidinoamino)propyl, 2-carboxyethyl, benzyl, phenethyl, naphthalen-1-ylmethyl, 2-(naphthalen-1-yl)ethyl, 2-(1-(tert-butoxycarbonyl)-1H-indol-3-yl) ethyl, 3-methylbenzyl, 4-methylbenzyl, 4-hydroxybenzyl, 4-fluorobenzyl, 3-chlorobenzyl, 4-chlorobenzyl, 3,4-dichlorobenzyl, 4-(tert-butoxy)benzyl, 2-(tert-butoxy)-2-oxoethyl, 3-(tert-butoxy)-3-oxopropyl, 4-((tert-butoxycarbonyl)amino)butyl, (tetrahydro-2H-pyran-2-yl)methyl, cyclohexylmethyl, or [ka] The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein [Item A34] R2 is isobutyl, 2-hydroxyethyl, 3-amino-3-oxopropyl, 4-aminobutyl, 2-carboxyethyl, benzyl, phenethyl, naphthalen-1-ylmethyl, 2-(naphthalen-1-yl)ethyl, 2-(1-(tert-butoxycarbonyl)-1H-indol-3-yl)ethyl, 3-methylbenzyl, 4-methylbenzyl, 4-hydroxybenzyl, 3-chlorobenzyl, 4-chlorobenzyl, 3,4-dichlorobenzyl, 4-(tert-butoxy)benzyl, 2-(tert-butoxy)-2-oxoethyl, 4-((tert-butoxycarbonyl)amino)butyl, (tetrahydro-2H-pyran-2-yl)methyl, or cyclohexylmethyl, or a compound or enantiomer thereof according to any one of the above items, or a salt or solvate thereof. [Item A35] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R2 is isopropyl, isobutyl, isopentyl, benzyl, 4-hydroxybenzyl, 4-fluorobenzyl, 2-carboxyethyl, carbamoylmethyl, 3-(amidinoamino)propyl, hydroxyethyl, phenethyl, naphthalen-1-ylmethyl, or n-hexyl. [Item A35b] R2 is isopropyl, 1-methylpropyl, isobutyl, 3-(amidinoamino)propyl, 2-carboxyethyl, benzyl, naphthalen-1-ylmethyl, 4-hydroxybenzyl, 4-(tert-butoxy)benzyl, 3-(tert-butoxy)-3-oxopropyl, or [ka] The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein [Item A36] R1 is C 1-6 Alkyl, hydroxy-substituted C 1-4 Alkyl, carbamoyl substituted C 1-4 Alkyl, amino substituted C 1-6Alkyl, amidinoamino substituted C 1-4 Alkyl, carboxy-substituted C 1-4 Alkyl, C 1-4 Alkoxycarbonyl-substituted C 1-4 Alkyl, C 6-10 Aryl C 1-4 Alkyl, hydroxy-substituted C 6-10 Aryl C 1-4 Alkyl, C 1-4 Alkoxy-substituted C 6-10 Aryl C 1-4 Alkyl, halo-substituted C 6-10 Aryl C 1-4 Alkyl, or C 5-6 Cycloalkyl C 1-4 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R is alkyl. [Item A36b] R1 is methyl, isopropyl, isobutyl, isopentyl, n-hexyl, 2-hydroxyethyl, carbamoylmethyl, 3-amino-3-oxopropyl, 3-(amidinoamino)propyl, 2-carboxyethyl, benzyl, phenethyl, naphthalen-1-ylmethyl, 4-hydroxybenzyl, 4-fluorobenzyl, 3,4-dichlorobenzyl, 4-(tert-butoxy)benzyl, 3-(tert-butoxy)-3-oxopropyl, hydroxymethyl, cyclohexylmethyl, or [ka] The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein [Item A37] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1 is methyl, isobutyl, isopentyl, 3-(tert-butoxy)-3-oxopropyl, benzyl, naphthalen-1-ylmethyl, 4-hydroxybenzyl, 4-(tert-butoxy)benzyl, 3,4-dichlorobenzyl, or cyclohexylmethyl. [Item A38] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1 is isobutyl, isopentyl, cyclohexylmethyl, benzyl, phenethyl, naphthalen-1-ylmethyl, 4-hydroxybenzyl, 4-fluorobenzyl, 2-carboxyethyl, carbamoylmethyl, 3-(amidinoamino)propyl, or hydroxyethyl. [Item A38b] R1 is isobutyl, 3-(amidinoamino)propyl, 2-carboxyethyl, benzyl, naphthalen-1-ylmethyl, 4-hydroxybenzyl, 4-(tert-butoxy)benzyl, 3-(tert-butoxy)-3-oxopropyl, or [ka] The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein [Item A39] R3 is C 1-4 Alkyl, hydroxy-substituted C 1-4 Alkyl, carbamoyl substituted C 1-4 Alkyl, C 1-4 Alkoxycarbonyl-substituted C 1-4 Alkyl, amino substituted C 1-4 Alkyl, amidinoamino substituted C 1-4 Alkyl, carboxy-substituted C 1-4 Alkyl, C 6-10 Aryl C 1-4 Alkyl, C 1-4 Alkyl-substituted C 6-10 Aryl C 1-4 Alkyl, hydroxy-substituted C 6-10 Aryl C 1-4 Alkyl, or C 5-6 Cycloalkyl C 1-4 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R is alkyl. [Item A39b] R3 is isopropyl, isobutyl, isopentyl, n-hexyl, hydroxymethyl, 2-hydroxyethyl, carbamoylmethyl, 3-amino-3-oxopropyl, 4-aminobutyl, 3-(amidinoamino)propyl, 2-carboxyethyl, benzyl, phenethyl, naphthalen-1-ylmethyl, 3-methylbenzyl, 4-methylbenzyl, 4-hydroxybenzyl, 4-fluorobenzyl, 4-(tert-butoxy)benzyl, 3-methoxy-3-oxopropyl, 3-(tert-butoxy)-3-oxopropyl, 4-((tert-butoxycarbonyl)amino)butyl, cyclohexylmethyl, or [ka] The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein [Item A40] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R3 is isobutyl, isopentyl, 3-amino-3-oxopropyl, 3-methoxy-3-oxopropyl, 4-aminobutyl, 2-carboxyethyl, benzyl, phenethyl, 3-methylbenzyl, 4-methylbenzyl, 4-hydroxybenzyl, 4-((tert-butoxycarbonyl)amino)butyl, or cyclohexylmethyl. [Item A41] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R3 is isobutyl, isopentyl, benzyl, phenethyl, 4-hydroxybenzyl, 2-carboxyethyl, carbamoylmethyl, 3-(amidinoamino)propyl, hydroxymethyl, or naphthalen-1-ylmethyl. [Item A41b] R3 is isobutyl, 2-carboxyethyl, 3-(amidinoamino)propyl, benzyl, naphthalen-1-ylmethyl, 4-hydroxybenzyl, 4-(tert-butoxy)benzyl, 3-(tert-butoxy)-3-oxopropyl, or [ka] The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein [Item A42] R1 is C 1-6 Alkyl or C 6-10 Aryl C 1-6 alkyl, and R2 and R3 are each independently C 1-6 Alkyl or optionally substituted C 6-10 Aryl C 1-6 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R is alkyl. [Item A42b] R1, R2 and R3 are each independently C 1-6 Alkyl or optionally substituted C 6-10 Aryl C 1-6 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R is alkyl. [Item A42c] R1, R2 and R3 are each independently C 1-6 Alkyl, C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkyl-substituted C 6-10 Aryl C 1-6 Alkyl, halogen-substituted C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkoxy-substituted C 6-10 Aryl C 1-6 Alkyl, or (optionally substituted amino)-C 6-10 Aryl C 1-6 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R is alkyl. [Section A42d] R1 is C 1-6 Alkyl or C6 arylC 1-4 alkyl, and R2 is C 1-6 Alkyl, or C 1-4 alkyl-substituted benzyl, and R3 is C 1-6Alkyl or C6 arylC 1-4 The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R is alkyl. [Item A43] R1 is isobutyl, benzyl, 4-(dimethylamino)benzyl, 4-methylbenzyl, 4-tert-butylbenzyl, 4-methoxybenzyl, 3-chlorobenzyl, 4-chlorobenzyl, or 3,4-dichlorobenzyl; R2 is isobutyl, benzyl, naphthalen-1-ylmethyl, 4-methylbenzyl, 4-chlorobenzyl, or 3,4-dichlorobenzyl; and R3 is isobutyl, isopentyl, or benzyl. A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Item A43b] A compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1 is isobutyl, isopentyl, or benzyl, R2 is isobutyl, benzyl, phenethyl, 3-methylbenzyl, 4-methylbenzyl, or 3,4-dichlorobenzyl, and R3 is isobutyl, benzyl, phenethyl, 3-methylbenzyl, or 4-methylbenzyl. [Item A44] The compound according to any one of the above items, wherein the compound is a compound of formula IIF, R1 is isobutyl, R2 is 4-methylbenzyl, and R3 is benzyl, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Item A45] The compound according to any one of the above items, wherein the compound is a compound of formula IIB, R1 is benzyl, R2 is isobutyl, and R3 is isobutyl, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Item A46] An antiviral agent against lyssaviruses, comprising the compound according to any one of the above items or a pharmaceutically acceptable salt thereof. [Item A47] The antiviral agent according to any one of the above items, wherein the Lyssavirus virus includes rabies virus. [Item A48] A pharmaceutical comprising the compound according to any one of the above items or a pharmaceutically acceptable salt thereof, or the antiviral agent according to any one of the above items. [Item A49] The pharmaceutical agent according to any one of the above items, which is a preventive or therapeutic agent for rabies. [Item A50] A pharmaceutical composition comprising the compound according to any one of the above items or a pharmaceutically acceptable salt thereof, or the antiviral agent according to any one of the above items, and a pharmaceutically acceptable carrier. [Item A51] A pharmaceutical composition for preventing or treating rabies, comprising the compound according to any one of the above items or a pharmaceutically acceptable salt thereof, or the antiviral agent according to any one of the above items, and a pharmaceutically acceptable carrier. [Item A52] A compound according to any one of the above items or a pharmaceutically acceptable salt thereof for use as an antiviral agent against a virus of the genus Lyssavirus, preferably rabies virus, or for preventing or treating rabies. [Item A53] A method for preventing or treating rabies, comprising administering to a patient in need of prevention or treatment a prophylactically or therapeutically effective amount of a compound described in any one of the above items or a pharmaceutically acceptable salt thereof, an antiviral agent described in any one of the above items, a medicine described in any one of the above items, or a pharmaceutical composition described in any one of the above items. [Item A54] Use of a compound according to any one of the above items or a pharmaceutically acceptable salt thereof, or an antiviral agent according to any one of the above items, for the manufacture of a medicament for the prevention or treatment of rabies.

[0009] It is contemplated that the present disclosure may provide one or more of the above-described features in combinations other than those explicitly stated. Still further embodiments and advantages of the present disclosure will be recognized by those skilled in the art upon reading and understanding the following detailed description, if necessary. [Effects of the Invention]

[0010] The compounds of the present disclosure exhibit excellent antiviral activity against Lyssaviruses, including rabies virus, and are therefore useful as therapeutic and / or preventive agents for rabies. [Brief explanation of the drawings]

[0011] [Figure 1] FIG. 1 shows an ORTEP diagram of the results of X-ray crystal structure analysis of the synthetic example IF-1. [Figure 2] FIG. 2 shows a chromatogram of the racemic mixture of Synthesis Example IF-1 separated using a chiral column, CHIRALPAK IG (5 μm, 4.6×150 mm), with a mobile phase of methanol:diethylamine (100:0.1). [Figure 3] FIG. 3 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 4] FIG. 4 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 5] FIG. 5 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 6] FIG. 6 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 7] FIG. 7 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 8] FIG. 8 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 9] FIG. 9 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 10] FIG. 10 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 11] FIG. 11 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 12] FIG. 12 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 13] FIG. 13 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 14] FIG. 14 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 15] FIG. 15 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 16] FIG. 16 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 17] FIG. 17 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 18] FIG. 18 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 19] FIG. 19 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 20] FIG. 20 shows the 1H-NMR chart of the exemplary compound of the present disclosure (the formula is shown in the figure). [Figure 21] FIG. 21 shows the 1H-NMR chart of the exemplary compound of the present disclosure (the formula is shown in the figure). [Figure 22] FIG. 22 shows the 1H-NMR chart of the exemplary compound of the present disclosure (the formula is shown in the figure). [Figure 23] FIG. 23 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 24] FIG. 24 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 25] FIG. 25 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 26] FIG. 26 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 27] FIG. 27 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 28] FIG. 28 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 29] FIG. 29 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 30]FIG. 30 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 31] FIG. 31 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 32] FIG. 32 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 33] FIG. 33 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 34] FIG. 34 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 35] FIG. 35 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 36] FIG. 36 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 37] FIG. 37 shows 1H-NMR charts of exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 38] FIG. 38 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 39] FIG. 39 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 40] FIG. 40 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 41] FIG. 41 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 42] FIG. 42 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 43] FIG. 43 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 44] FIG. 44 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 45] FIG. 45 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 46] FIG. 46 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 47] FIG. 47 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 48] FIG. 48 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 49] FIG. 49 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 50] FIG. 50 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 51] FIG. 51 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 52] FIG. 52 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 53] FIG. 53 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 54] FIG. 54 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 55] FIG. 55 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 56] FIG. 56 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 57] FIG. 57 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 58] FIG. 58 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 59] FIG. 59 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 60] FIG. 60 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 61] FIG. 61 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 62] FIG. 62 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 63]FIG. 63 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 64] FIG. 64 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 65] FIG. 65 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 66] FIG. 66 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 67] FIG. 67 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 68] FIG. 68 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 69] FIG. 69 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 70] FIG. 70 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 71] FIG. 71 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 72] FIG. 72 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 73] FIG. 73 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 74] FIG. 74 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 75] FIG. 75 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 76] FIG. 76 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). [Figure 77] FIG. 77 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 78] FIG. 78 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 79] FIG. 79 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 80] FIG. 80 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (formulas shown in the figure). [Figure 81] FIG. 81 shows the 1H-NMR chart of the exemplary compounds of the present disclosure (the formulas are shown in the figure). DETAILED DESCRIPTION OF THE INVENTION

[0012] The present disclosure is described in further detail below. Throughout this specification, singular expressions should be understood to include the plural concept unless otherwise specified. Thus, singular articles (e.g., "a," "an," "the," etc. in English) should be understood to include the plural concept unless otherwise specified. Furthermore, it should be understood that terms used in this specification are used in the sense commonly used in the art unless otherwise specified. Therefore, unless otherwise defined, all technical and scientific terms used in this specification have the same meaning as commonly understood by one of ordinary skill in the art to which this disclosure belongs. In case of conflict, the present specification (including definitions) will control.

[0013] (definition) First, we explain the terms and general techniques used in this disclosure.

[0014] In this specification, the term "group" refers to a monovalent group unless otherwise specified. Examples of non-monovalent groups include alkylene groups (divalent). In addition, in the following explanations of substituents, etc., the term "group" may be omitted.

[0015] In this specification, when defined as "optionally substituted" or "substituted," the number of substituents is not particularly limited as long as substitution is possible, and is one or more. Furthermore, unless otherwise specified, the description of each substituent also applies when that substituent is a part of or a substituent for another substituent.

[0016] As used herein, the "maximum number of possible substitutions" refers to the maximum number of substituents that a group can have, and may vary for each group. For example, the maximum number of possible substitutions is 3 for a methyl group, 5 for an ethyl group, 7 for a benzyl group, and 10 for a naphthalenylethyl group.

[0017] In the present specification, any part of a group modified with "optionally substituted" or "substituted" may be substituted. For example, in "optionally substituted arylalkyl" and "substituted arylalkyl," the aryl moiety, the alkyl moiety, or both the aryl and alkyl moieties may be substituted.

[0018] In the present specification, the substituent in the case of "optionally substituted" may be one or more of the same or different substituents selected from any of the following substituent groups I to VI. The type of atom in the substituent participating in the bond is not particularly limited depending on the type of substituent, but when the atom to which the substituent is bonded is an oxygen atom, nitrogen atom, or sulfur atom, it is limited to and selected from those in which the bonding point in the following substituent is a carbon atom.

[0019] Substituent group I is halogen, hydroxy, oxo, carboxy, amino, imino, hydroxyamino, hydroxyimino, formyl, formyloxy, carbamoyl, sulfamoyl, sulfanyl, sulfino, sulfo, thioformyl, thiocarboxy, dithiocarboxy, thiocarbamoyl, cyano, nitro, nitroso, azido, hydrazino, ureido, amidino, amidinoamino, unsubstituted or substituted alkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted alkynyl, unsubstituted or substituted aryl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted heteroaryl, unsubstituted or substituted heterocycloalkyl, unsubstituted or substituted alkyloxy, unsubstituted or substituted alkenyloxy, unsubstituted or substituted alkynyloxy, unsubstituted or substituted aryl-L X -oxy, unsubstituted or substituted cycloalkyl-LX -oxy, unsubstituted or substituted heteroaryl-L X -oxy, unsubstituted or substituted heterocycloalkyl-L X -oxy, unsubstituted or substituted alkyloxyalkyl, unsubstituted or substituted alkenyloxyalkyl, unsubstituted or substituted alkynyloxyalkyl, unsubstituted or substituted aryloxyalkyl, unsubstituted or substituted cycloalkyloxyalkyl, unsubstituted or substituted heteroaryloxyalkyl, unsubstituted or substituted heterocycloalkyloxyalkyl, unsubstituted or substituted alkyloxyalkyloxy, unsubstituted or substituted alkenyloxyalkyloxy, unsubstituted or substituted alkynyloxyalkyloxy, unsubstituted or substituted aryloxyalkyloxy, unsubstituted or substituted cycloalkyloxyalkyloxy, unsubstituted or substituted heteroaryloxyalkyloxy, unsubstituted or substituted heterocycloalkyloxyalkyloxy, unsubstituted or substituted alkylcarbonyl, unsubstituted or substituted alkenylcarbonyl, unsubstituted or substituted alkynylcarbonyl, unsubstituted or substituted aryl-L X -carbonyl, unsubstituted or substituted cycloalkyl-L X -carbonyl, unsubstituted or substituted heteroaryl-L X -carbonyl, unsubstituted or substituted heterocycloalkyl-L X -carbonyl, unsubstituted or substituted alkylcarbonyloxy, unsubstituted or substituted alkenylcarbonyloxy, unsubstituted or substituted alkynylcarbonyloxy, unsubstituted or substituted aryl-L X -carbonyloxy, unsubstituted or substituted cycloalkyl-L X -carbonyloxy, unsubstituted or substituted heteroaryl-L X -carbonyloxy, unsubstituted or substituted heterocycloalkyl-L X -carbonyloxy, unsubstituted or substituted alkylcarbonylamino, unsubstituted or substituted alkenylcarbonylamino, unsubstituted or substituted alkynylcarbonylamino, unsubstituted or substituted aryl-L X -carbonylamino, unsubstituted or substituted cycloalkyl-LX -carbonylamino, unsubstituted or substituted heteroaryl-L X -carbonylamino, unsubstituted or substituted heterocycloalkyl-L X -carbonylamino, unsubstituted or substituted alkylcarbonylthio, unsubstituted or substituted alkenylcarbonylthio, unsubstituted or substituted alkynylcarbonylthio, unsubstituted or substituted aryl-L X -carbonylthio, unsubstituted or substituted cycloalkyl-L X -carbonylthio, unsubstituted or substituted heteroaryl-L X -carbonylthio, unsubstituted or substituted heterocycloalkyl-L X -carbonylthio, unsubstituted or substituted alkylcarbonylimino, unsubstituted or substituted alkenylcarbonylimino, unsubstituted or substituted alkynylcarbonylimino, unsubstituted or substituted aryl-L X -carbonylimino, unsubstituted or substituted cycloalkyl-L X -carbonylimino, unsubstituted or substituted heteroaryl-L X -carbonylimino, unsubstituted or substituted heterocycloalkyl-L X -carbonylimino, unsubstituted or substituted alkylthio, unsubstituted or substituted alkenylthio, unsubstituted or substituted alkynylthio, unsubstituted or substituted aryl-L X -thio, unsubstituted or substituted cycloalkyl-L X -thio, unsubstituted or substituted heteroaryl-L X -thio, unsubstituted or substituted heterocycloalkyl-L X -thio, unsubstituted or substituted alkylamino, unsubstituted or substituted alkenylamino, unsubstituted or substituted alkynylamino, unsubstituted or substituted alkynylamino, unsubstituted or substituted aryl-L X -amino, unsubstituted or substituted cycloalkyl-L X -amino, unsubstituted or substituted heteroaryl-L X -amino, unsubstituted or substituted heterocycloalkyl-L X-amino, unsubstituted or substituted alkylsulfonyl, unsubstituted or substituted alkenylsulfonyl, unsubstituted or substituted alkynylsulfonyl, unsubstituted or substituted aryl-L X -sulfonyl, unsubstituted or substituted cycloalkyl-L X -sulfonyl, unsubstituted or substituted heteroaryl-L X -sulfonyl, unsubstituted or substituted heterocycloalkyl-L X -sulfonyl, unsubstituted or substituted alkylsulfonylamino, unsubstituted or substituted alkenylsulfonylamino, unsubstituted or substituted alkynylsulfonylamino, unsubstituted or substituted aryl-L X -sulfonylamino, unsubstituted or substituted cycloalkyl-L X -sulfonylamino, unsubstituted or substituted heteroaryl-L X -sulfonylamino, unsubstituted or substituted heterocycloalkyl-L X -sulfonylamino, unsubstituted or substituted alkylimino, unsubstituted or substituted alkenylimino, unsubstituted or substituted alkynylimino, unsubstituted or substituted aryl-L X -imino, unsubstituted or substituted cycloalkyl-L X -imino, unsubstituted or substituted heteroaryl-L X -imino, unsubstituted or substituted heterocycloalkyl-L X -imino, unsubstituted or substituted alkyloxyimino, unsubstituted or substituted alkenyloxyimino, unsubstituted or substituted alkynyloxyimino, unsubstituted or substituted aryl-L X -oximino, unsubstituted or substituted cycloalkyl-L X -oximino, unsubstituted or substituted heteroaryl-L X -oximino, unsubstituted or substituted heterocycloalkyl-L X -oximino, unsubstituted or substituted alkyloxycarbonyl, unsubstituted or substituted alkenyloxycarbonyl, unsubstituted or substituted alkynyloxycarbonyl, unsubstituted or substituted aryl-L X -oxycarbonyl, unsubstituted or substituted cycloalkyl-L X-oxycarbonyl, unsubstituted or substituted heteroaryl-L X -oxycarbonyl, unsubstituted or substituted heterocycloalkyl-L X -oxycarbonyl, unsubstituted or substituted alkyloxycarbonylamino, unsubstituted or substituted alkenyloxycarbonylamino, unsubstituted or substituted alkynyloxycarbonylamino, unsubstituted or substituted aryl-L X -oxycarbonylamino, unsubstituted or substituted cycloalkyl-L X -oxycarbonylamino, unsubstituted or substituted heteroaryl-L X -oxycarbonylamino, unsubstituted or substituted heterocycloalkyl-L X -oxycarbonylamino, unsubstituted or substituted alkylsulfanyl, unsubstituted or substituted alkenylsulfanyl, unsubstituted or substituted alkynylsulfanyl, unsubstituted or substituted aryl-L X -sulfanyl, unsubstituted or substituted cycloalkyl-L X -sulfanyl, unsubstituted or substituted heteroaryl-L X -sulfanyl, unsubstituted or substituted heterocycloalkyl-L X -sulfanyl, unsubstituted or substituted alkylsulfinyl, unsubstituted or substituted alkenylsulfinyl, unsubstituted or substituted alkynylsulfinyl, unsubstituted or substituted aryl-L X -sulfinyl, unsubstituted or substituted cycloalkyl-L X -sulfinyl, unsubstituted or substituted heteroaryl-L X -sulfinyl, unsubstituted or substituted heterocycloalkyl-L X -sulfinyl, unsubstituted or substituted alkylcarbamoyl, unsubstituted or substituted alkenylcarbamoyl, unsubstituted or substituted alkynylcarbamoyl, unsubstituted or substituted aryl-L X -carbamoyl, unsubstituted or substituted cycloalkyl-L X -carbamoyl, unsubstituted or substituted heteroaryl-L X -carbamoyl, unsubstituted or substituted heterocycloalkyl-L X-carbamoyl, unsubstituted or substituted alkylsulfamoyl, unsubstituted or substituted alkenylsulfamoyl, unsubstituted or substituted alkynylsulfamoyl, unsubstituted or substituted aryl-L X -sulfamoyl, unsubstituted or substituted cycloalkyl-L X -sulfamoyl, unsubstituted or substituted heteroaryl-L X -sulfamoyl, and unsubstituted or substituted heterocycloalkyl-L X -sulfamoyl, where L X is a single bond or unsubstituted or substituted alkylene; The substituted alkyl, substituted alkenyl, substituted alkynyl, substituted aryl, substituted cycloalkyl, substituted heteroaryl, substituted heterocycloalkyl, and substituted alkylene moieties (in whole or in part) in the above substituent groups each independently represent halogen, hydroxy, oxo, carboxy, amino, imino, hydroxyamino, hydroxyimino, formyl, formyloxy, carbamoyl, sulfamoyl, sulfanyl, sulfino, sulfo, thioformyl, thiocarboxy, dithiocarboxy, thiocarbamoyl, cyano, nitro, nitroso, azido, hydrazino, ureido, amidino, amidinoamino, alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, alkyloxy, alkenyloxy, alkynyloxy, aryl-L X -oxy, cycloalkyl-L X -oxy, heteroaryl-L X -oxy, heterocycloalkyl-L X-oxy, alkyloxyalkyl, alkenyloxyalkyl, alkynyloxyalkyl, aryloxyalkyl, cycloalkyloxyalkyl, heteroaryloxyalkyl, heterocycloalkyloxyalkyl, alkyloxyalkyloxy, alkenyloxyalkyloxy, alkynyloxyalkyloxy, aryloxyalkyloxy, cycloalkyloxyalkyloxy, heteroaryloxyalkyloxy, heterocycloalkyloxyalkyloxy, alkylcarbonyl, alkenylcarbonyl, alkynylcarbonyl, aryl-L X -carbonyl, cycloalkyl-L X -carbonyl, heteroaryl-L X -carbonyl, heterocycloalkyl-L X -carbonyl, alkylcarbonyloxy, alkenylcarbonyloxy, alkynylcarbonyloxy, aryl-L X -carbonyloxy, cycloalkyl-L X -carbonyloxy, heteroaryl-L X -carbonyloxy, heterocycloalkyl-L X -carbonyloxy, alkylcarbonylamino, alkenylcarbonylamino, alkynylcarbonylamino, aryl-L X -carbonylamino, cycloalkyl-L X -carbonylamino, heteroaryl-L X -carbonylamino, heterocycloalkyl-L X -carbonylamino, alkylcarbonylthio, alkenylcarbonylthio, alkynylcarbonylthio, aryl-L X -carbonylthio, cycloalkyl-L X -carbonylthio, heteroaryl-L X -carbonylthio, heterocycloalkyl-L X -carbonylthio, alkylcarbonylimino, alkenylcarbonylimino, alkynylcarbonylimino, aryl-L X -carbonylimino, cycloalkyl-L X -carbonylimino, heteroaryl-L X-carbonylimino, heterocycloalkyl-L X -carbonylimino, alkylthio, alkenylthio, alkynylthio, aryl-L X -thio, cycloalkyl-L X -thio, heteroaryl-L X -thio, heterocycloalkyl-L X -thio, alkylamino, alkenylamino, alkynylamino, alkynylamino, aryl-L X -amino, cycloalkyl-L X -amino, heteroaryl-L X -amino, heterocycloalkyl-L X -amino, alkylsulfonyl, alkenylsulfonyl, alkynylsulfonyl, aryl-L X -sulfonyl, cycloalkyl-L X -sulfonyl, heteroaryl-L X -sulfonyl, heterocycloalkyl-L X -sulfonyl, alkylsulfonylamino, alkenylsulfonylamino, alkynylsulfonylamino, aryl-L X -sulfonylamino, cycloalkyl-L X -sulfonylamino, heteroaryl-L X -sulfonylamino, heterocycloalkyl-L X -sulfonylamino, alkylimino, alkenylimino, alkynylimino, aryl-L X -imino, cycloalkyl-L X -imino, heteroaryl-L X -imino, heterocycloalkyl-L X -imino, alkyloxyimino, alkenyloxyimino, alkynyloxyimino, aryl-L X -Oximino, cycloalkyl-L X -oximino, heteroaryl-L X -Oximino, heterocycloalkyl-L X -Oximino, alkyloxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, aryl-L X -oxycarbonyl, cycloalkyl-LX -oxycarbonyl, heteroaryl-L X -oxycarbonyl, heterocycloalkyl-L X -oxycarbonyl, alkyloxycarbonylamino, alkenyloxycarbonylamino, alkynyloxycarbonylamino, aryl-L X -oxycarbonylamino, cycloalkyl-L X -oxycarbonylamino, heteroaryl-L X -oxycarbonylamino, heterocycloalkyl-L X -oxycarbonylamino, alkylsulfanyl, alkenylsulfanyl, alkynylsulfanyl, aryl-L X -sulfanyl, cycloalkyl-L X -sulfanyl, heteroaryl-L X -sulfanyl, heterocycloalkyl-L X -sulfanyl, alkylsulfinyl, alkenylsulfinyl, alkynylsulfinyl, aryl-L X -sulfinyl, cycloalkyl-L X -sulfinyl, heteroaryl-L X -sulfinyl, heterocycloalkyl-L X -sulfinyl, alkylcarbamoyl, alkenylcarbamoyl, alkynylcarbamoyl, aryl-L X -carbamoyl, cycloalkyl-L X -carbamoyl, heteroaryl-L X -carbamoyl, heterocycloalkyl-L X -carbamoyl, alkylsulfamoyl, alkenylsulfamoyl, alkynylsulfamoyl, aryl-L X -sulfamoyl, cycloalkyl-L X -sulfamoyl, heteroaryl-L X -sulfamoyl, and heterocycloalkyl-L X -sulfamoyl, wherein the aryl group has one to the maximum possible number of identical or different substituents selected from the group consisting of aryl, aryl, aryl- ...

[0020] Substituent group II is halogen, hydroxy, oxo, carboxy, amino, imino, hydroxyamino, hydroxyimino, formyl, formyloxy, carbamoyl, sulfamoyl, sulfanyl, sulfino, sulfo, thioformyl, thiocarboxy, dithiocarboxy, thiocarbamoyl, cyano, nitro, nitroso, azido, hydrazino, ureido, amidino, amidinoamino, unsubstituted or substituted C 1-12 Alkyl, unsubstituted or substituted C 2-12 Alkenyl, unsubstituted or substituted C 2-12 Alkynyl, unsubstituted or substituted C 6-10 Aryl, unsubstituted or substituted C 3-10 Cycloalkyl, unsubstituted or substituted 5-10 membered heteroaryl, unsubstituted or substituted 5-10 membered heterocycloalkyl, unsubstituted or substituted C 1-12 Alkyloxy, unsubstituted or substituted C 2-12 Alkenyloxy, unsubstituted or substituted C 2-12 Alkynyloxy, unsubstituted or substituted C 6-10 Aryl-L X -oxy, unsubstituted or substituted C 3-10 Cycloalkyl-L X -oxy, unsubstituted or substituted 5- to 10-membered heteroaryl-L X -oxy, unsubstituted or substituted 5- to 10-membered heterocycloalkyl-L X -oxy, unsubstituted or substituted C 1-12 Alkyloxy C 1-12 Alkyl, unsubstituted or substituted C 2-12 Alkenyloxy C 1-12 Alkyl, unsubstituted or substituted C 2-12 Alkynyloxy C 1-12 Alkyl, unsubstituted or substituted C 6-10 Aryloxy C 1-12 Alkyl, unsubstituted or substituted C 3-10 Cycloalkyloxy C 1-12 Alkyl, unsubstituted or substituted 5-10 membered heteroaryloxyC 1-12 Alkyl, unsubstituted or substituted 5-10 membered heterocycloalkyloxyC 1-12 Alkyl, unsubstituted or substituted C1-12 Alkyloxy C 1-12 Alkyloxy, unsubstituted or substituted C 2-12 Alkenyloxy C 1-12 Alkyloxy, unsubstituted or substituted C 2-12 Alkynyloxy C 1-12 Alkyloxy, unsubstituted or substituted C 6-10 Aryloxy C 1-12 Alkyloxy, unsubstituted or substituted C 3-10 Cycloalkyloxy C 1-12 Alkyloxy, unsubstituted or substituted 5-10 membered heteroaryloxyC 1-12 Alkyloxy, unsubstituted or substituted 5-10 membered heterocycloalkyloxyC 1-12 Alkyloxy, unsubstituted or substituted C 1-12 Alkylcarbonyl, unsubstituted or substituted C 2-12 Alkenylcarbonyl, unsubstituted or substituted C 2-12 Alkynylcarbonyl, unsubstituted or substituted C 6-10 Aryl-L X -carbonyl, unsubstituted or substituted C 3-10 Cycloalkyl-L X -carbonyl, unsubstituted or substituted 5- to 10-membered heteroaryl-L X -carbonyl, unsubstituted or substituted 5- to 10-membered heterocycloalkyl-L X -carbonyl, unsubstituted or substituted C 1-12 Alkylcarbonyloxy, unsubstituted or substituted C 2-12 Alkenylcarbonyloxy, unsubstituted or substituted C 2-12 Alkynylcarbonyloxy, unsubstituted or substituted C 6-10 Aryl-L X -carbonyloxy, unsubstituted or substituted C 3-10 Cycloalkyl-L X -carbonyloxy, unsubstituted or substituted 5- to 10-membered heteroaryl-L X -carbonyloxy, unsubstituted or substituted 5- to 10-membered heterocycloalkyl-L X -carbonyloxy, unsubstituted or substituted C 1-12 Alkylcarbonylamino, unsubstituted or substituted C2-12 Alkenylcarbonylamino, unsubstituted or substituted C 2-12 Alkynylcarbonylamino, unsubstituted or substituted C 6-10 Aryl-L X -carbonylamino, unsubstituted or substituted C 3-10 Cycloalkyl-L X -carbonylamino, unsubstituted or substituted 5- to 10-membered heteroaryl-L X -carbonylamino, unsubstituted or substituted 5- to 10-membered heterocycloalkyl-L X -carbonylamino, unsubstituted or substituted C 1-12 Alkylcarbonylthio, unsubstituted or substituted C 2-12 Alkenylcarbonylthio, unsubstituted or substituted C 2-12 Alkynylcarbonylthio, unsubstituted or substituted C 6-10 Aryl-L X -carbonylthio, unsubstituted or substituted C 3-10 Cycloalkyl-L X -carbonylthio, unsubstituted or substituted 5- to 10-membered heteroaryl-L X -carbonylthio, unsubstituted or substituted 5- to 10-membered heterocycloalkyl-L X -carbonylthio, unsubstituted or substituted C 1-12 Alkylcarbonylimino, unsubstituted or substituted C 2-12 Alkenylcarbonylimino, unsubstituted or substituted C 2-12 Alkynylcarbonylimino, unsubstituted or substituted C 6-10 Aryl-L X -carbonylimino, unsubstituted or substituted C 3-10 Cycloalkyl-L X -carbonylimino, unsubstituted or substituted 5- to 10-membered heteroaryl-L X -carbonylimino, unsubstituted or substituted 5- to 10-membered heterocycloalkyl-L X -carbonylimino, unsubstituted or substituted C 1-12 Alkylthio, unsubstituted or substituted C 2-12 Alkenylthio, unsubstituted or substituted C 2-12 Alkynylthio, unsubstituted or substituted C 6-10Aryl-L X -thio, unsubstituted or substituted C 3-10 Cycloalkyl-L X -thio, unsubstituted or substituted 5- to 10-membered heteroaryl-L X -thio, unsubstituted or substituted 5- to 10-membered heterocycloalkyl-L X -thio, unsubstituted or substituted C 1-12 Alkylamino, unsubstituted or substituted C 2-12 Alkenylamino, unsubstituted or substituted C 2-12 Alkynylamino, unsubstituted or substituted C 2-12 Alkynylamino, unsubstituted or substituted C 6-10 Aryl-L X -amino, unsubstituted or substituted C 3-10 Cycloalkyl-L X -amino, unsubstituted or substituted 5- to 10-membered heteroaryl-L X -amino, unsubstituted or substituted 5- to 10-membered heterocycloalkyl-L X -amino, unsubstituted or substituted C 1-12 Alkylsulfonyl, unsubstituted or substituted C 2-12 Alkenylsulfonyl, unsubstituted or substituted C 2-12 Alkynylsulfonyl, unsubstituted or substituted C 6-10 Aryl-L X -sulfonyl, unsubstituted or substituted C 3-10 Cycloalkyl-L X -sulfonyl, unsubstituted or substituted 5-10 membered heteroaryl-L X -sulfonyl, unsubstituted or substituted 5- to 10-membered heterocycloalkyl-L X -sulfonyl, unsubstituted or substituted C 1-12 Alkyl sulfonyl amino, unsubstituted or substituted C 2-12 Alkenylsulfonylamino, unsubstituted or substituted C 2-12 Alkynylsulfonylamino, unsubstituted or substituted C 6-10 Aryl-L X -sulfonylamino, unsubstituted or substituted C 3-10 Cycloalkyl-L X -sulfonylamino, unsubstituted or substituted 5-10 membered heteroaryl-LX -sulfonylamino, unsubstituted or substituted 5- to 10-membered heterocycloalkyl-L X -sulfonylamino, unsubstituted or substituted C 1-12 Alkylimino, unsubstituted or substituted C 2-12 Alkenylimino, unsubstituted or substituted C 2-12 Alkynylimino, unsubstituted or substituted C 6-10 Aryl-L X -imino, unsubstituted or substituted C 3-10 Cycloalkyl-L X -imino, unsubstituted or substituted 5- to 10-membered heteroaryl-L X -imino, unsubstituted or substituted 5- to 10-membered heterocycloalkyl-L X -imino, unsubstituted or substituted C 1-12 Alkyloxyimino, unsubstituted or substituted C 2-12 Alkenyloxyimino, unsubstituted or substituted C 2-12 Alkynyloxyimino, unsubstituted or substituted C 6-10 Aryl-L X -oximino, unsubstituted or substituted C 3-10 Cycloalkyl-L X -oximino, unsubstituted or substituted 5-10 membered heteroaryl-L X -oximino, unsubstituted or substituted 5- to 10-membered heterocycloalkyl-L X -oximino, unsubstituted or substituted C 1-12 Alkyloxycarbonyl, unsubstituted or substituted C 2-12 Alkenyloxycarbonyl, unsubstituted or substituted C 2-12 Alkynyloxycarbonyl, unsubstituted or substituted C 6-10 Aryl-L X -oxycarbonyl, unsubstituted or substituted C 3-10 Cycloalkyl-L X -oxycarbonyl, unsubstituted or substituted 5-10 membered heteroaryl-L X -oxycarbonyl, unsubstituted or substituted 5- to 10-membered heterocycloalkyl-L X -oxycarbonyl, unsubstituted or substituted C 1-12Alkyloxycarbonylamino, unsubstituted or substituted C 2-12 Alkenyloxycarbonylamino, unsubstituted or substituted C 2-12 Alkynyloxycarbonylamino, unsubstituted or substituted C 6-10 Aryl-L X -oxycarbonylamino, unsubstituted or substituted C 3-10 Cycloalkyl-L X -oxycarbonylamino, unsubstituted or substituted 5-10 membered heteroaryl-L X -oxycarbonylamino, unsubstituted or substituted 5- to 10-membered heterocycloalkyl-L X -oxycarbonylamino, unsubstituted or substituted C 1-12 Alkylsulfanyl, unsubstituted or substituted C 2-12 Alkenylsulfanyl, unsubstituted or substituted C 2-12 Alkynylsulfanyl, unsubstituted or substituted C 6-10 Aryl-L X -sulfanyl, unsubstituted or substituted C 3-10 Cycloalkyl-L X -sulfanyl, unsubstituted or substituted 5- to 10-membered heteroaryl-L X -sulfanyl, unsubstituted or substituted 5- to 10-membered heterocycloalkyl-L X -sulfanyl, unsubstituted or substituted C 1-12 Alkylsulfinyl, unsubstituted or substituted C 2-12 Alkenylsulfinyl, unsubstituted or substituted C 2-12 Alkynylsulfinyl, unsubstituted or substituted C 6-10 Aryl-L X -sulfinyl, unsubstituted or substituted C 3-10 Cycloalkyl-L X -sulfinyl, unsubstituted or substituted 5- to 10-membered heteroaryl-L X -sulfinyl, Unsubstituted or substituted 5-10 membered heterocycloalkyl-L X -sulfinyl, unsubstituted or substituted C 1-12 Alkylcarbamoyl, unsubstituted or substituted C 2-12 Alkenylcarbamoyl, unsubstituted or substituted C2-12 Alkynylcarbamoyl, unsubstituted or substituted C 6-10 Aryl-L X -carbamoyl, unsubstituted or substituted C 3-10 Cycloalkyl-L X -carbamoyl, unsubstituted or substituted 5- to 10-membered heteroaryl-L X -carbamoyl, unsubstituted or substituted 5- to 10-membered heterocycloalkyl-L X -carbamoyl, unsubstituted or substituted C 1-12 Alkyl sulfamoyl, unsubstituted or substituted C 2-12 Alkenylsulfamoyl, unsubstituted or substituted C 2-12 Alkynylsulfamoyl, unsubstituted or substituted C 6-10 Aryl-L X -sulfamoyl, unsubstituted or substituted C 3-10 Cycloalkyl-L X -sulfamoyl, unsubstituted or substituted 5- to 10-membered heteroaryl-L X -sulfamoyl, and unsubstituted or substituted 5- to 10-membered heterocycloalkyl-L X -sulfamoyl, where L X is a single bond or an unsubstituted or substituted C 1-12 is alkylene, Substituent C in the above substituent group 1-12 Alkyl, substituted C 2-12 Alkenyl, substituted C 2-12 Alkynyl, substituted C 6-10 Aryl, substituted C 3-10 The cycloalkyl, substituted 5-10 membered heteroaryl, substituted 5-10 membered heterocycloalkyl, and substituted alkylene moieties (in whole or in part) each independently represent halogen, hydroxy, oxo, carboxy, amino, imino, hydroxyamino, hydroxyimino, formyl, formyloxy, carbamoyl, sulfamoyl, sulfanyl, sulfino, sulfo, thioformyl, thiocarboxy, dithiocarboxy, thiocarbamoyl, cyano, nitro, nitroso, azido, hydrazino, ureido, amidino, amidinoamino, C 1-12 Alkyl, C 1-12 Haloalkyl, C2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, C 3-10 Cycloalkyl, 5-10 membered heteroaryl, 5-10 membered heterocycloalkyl, C 1-12 Alkyloxy, C 1-12 Haloalkyloxy, C 2-12 Alkenyloxy, C 2-12 Alkynyloxy, C 6-10 Aryl-L X -Oxy, C 3-10 Cycloalkyl-L X -oxy, 5- to 10-membered heteroaryl-L X -oxy, 5- to 10-membered heterocycloalkyl-L X -Oxy, C 1-12 Alkyloxyalkyl, C 2-12 Alkenyloxyalkyl, C 2-12 Alkynyloxyalkyl, C 6-10 Aryloxyalkyl, C 3-10 Cycloalkyloxyalkyl, 5-10 membered heteroaryloxyalkyl, 5-10 membered heterocycloalkyloxyalkyl, C 1-12 Alkyloxy alkyloxy, C 2-12 Alkenyloxyalkyloxy, C 2-12 Alkynyloxyalkyloxy, C 6-10 Aryloxyalkyloxy, C 3-10 Cycloalkyloxyalkyloxy, 5-10 membered heteroaryloxyalkyloxy, 5-10 membered heterocycloalkyloxyalkyloxy, C 1-12 Alkyl carbonyl, C 2-12 Alkenylcarbonyl, C 2-12 Alkynylcarbonyl, C 6-10 Aryl-L X -carbonyl, C 3-10 Cycloalkyl-L X -carbonyl, 5-10 membered heteroaryl-L X -carbonyl, 5-10 membered heterocycloalkyl-L X -carbonyl, C 1-12 Alkylcarbonyloxy, C 2-12Alkenylcarbonyloxy, C 2-12 Alkynylcarbonyloxy, C 6-10 Aryl-L X -carbonyloxy, C 3-10 Cycloalkyl-L X -carbonyloxy, 5-10 membered heteroaryl-L X -carbonyloxy, 5- to 10-membered heterocycloalkyl-L X -carbonyloxy, C 1-12 Alkylcarbonylamino, C 2-12 Alkenylcarbonylamino, C 2-12 Alkynylcarbonylamino, C 6-10 Aryl-L X -carbonylamino, C 3-10 Cycloalkyl-L X -carbonylamino, 5-10 membered heteroaryl-L X -carbonylamino, 5-10 membered heterocycloalkyl-L X -carbonylamino, C 1-12 Alkylcarbonylthio, C 2-12 Alkenylcarbonylthio, C 2-12 Alkynylcarbonylthio, C 6-10 Aryl-L X -carbonylthio, C 3-10 Cycloalkyl-L X -carbonylthio, 5-10 membered heteroaryl-L X -carbonylthio, 5- to 10-membered heterocycloalkyl-L X -carbonylthio, C 1-12 Alkylcarbonylimino, C 2-12 Alkenylcarbonylimino, C 2-12 Alkynylcarbonylimino, C 6-10 Aryl-L X -carbonylimino, C 3-10 Cycloalkyl-L X -carbonylimino, 5-10 membered heteroaryl-L X -carbonylimino, 5- to 10-membered heterocycloalkyl-L X -carbonylimino, C 1-12 Alkylthio, C 2-12 Alkenylthio, C2-12 Alkynylthio, C 6-10 Aryl-L X - Thio, C 3-10 Cycloalkyl-L X -thio, 5- to 10-membered heteroaryl-L X -thio, 5- to 10-membered heterocycloalkyl-L X - Thio, C 1-12 Alkylamino, C 2-12 Alkenylamino, C 2-12 Alkynylamino, C 2-12 Alkynylamino, C 6-10 Aryl-L X -Amino, C 3-10 Cycloalkyl-L X -amino, 5- to 10-membered heteroaryl-L X -amino, 5- to 10-membered heterocycloalkyl-L X -Amino, C 1-12 Alkylsulfonyl, C 2-12 Alkenylsulfonyl, C 2-12 Alkynylsulfonyl, C 6-10 Aryl-L X -sulfonyl, C 3-10 Cycloalkyl-L X -sulfonyl, 5-10 membered heteroaryl-L X -sulfonyl, 5- to 10-membered heterocycloalkyl-L X -sulfonyl, C 1-12 Alkyl sulfonyl amino, C 2-12 Alkenylsulfonylamino, C 2-12 Alkynylsulfonylamino, C 6-10 Aryl-L X -sulfonylamino, C 3-10 Cycloalkyl-L X -sulfonylamino, 5-10 membered heteroaryl-L X -sulfonylamino, 5- to 10-membered heterocycloalkyl-L X -sulfonylamino, C 1-12 Alkylimino, C 2-12 Alkenylimino, C 2-12 Alkynylimino, C 6-10 Aryl-L X -Imino, C 3-10Cycloalkyl-L X -imino, 5-10 membered heteroaryl-L X -imino, 5- to 10-membered heterocycloalkyl-L X -Imino, C 1-12 Alkyloxyimino, C 2-12 Alkenyloxyimino, C 2-12 Alkynyloxyimino, C 6-10 Aryl-L X -Oximino, C 3-10 Cycloalkyl-L X -oximino, 5-10 membered heteroaryl-L X -oximino, 5-10 membered heterocycloalkyl-L X -Oximino, C 1-12 Alkyloxycarbonyl, C 2-12 Alkenyloxycarbonyl, C 2-12 Alkynyloxycarbonyl, C 6-10 Aryl-L X -oxycarbonyl, C 3-10 Cycloalkyl-L X -oxycarbonyl, 5-10 membered heteroaryl-L X -oxycarbonyl, 5- to 10-membered heterocycloalkyl-L X -oxycarbonyl, C 1-12 Alkyloxycarbonylamino, C 2-12 Alkenyloxycarbonylamino, C 2-12 Alkynyloxycarbonylamino, C 6-10 Aryl-L X -oxycarbonylamino, C 3-10 Cycloalkyl-L X -oxycarbonylamino, 5-10 membered heteroaryl-L X -oxycarbonylamino, 5-10 membered heterocycloalkyl-L X -oxycarbonylamino, C 1-12 Alkylsulfanyl, C 2-12 Alkenylsulfanyl, C 2-12 Alkynylsulfanyl, C 6-10 Aryl-L X -Sulfanyl, C 3-10 Cycloalkyl-L X-sulfanyl, 5-10 membered heteroaryl-L X -sulfanyl, 5-10 membered heterocycloalkyl-L X -Sulfanyl, C 1-12 Alkylsulfinyl, C 2-12 Alkenylsulfinyl, C 2-12 Alkynylsulfinyl, C 6-10 Aryl-L X -sulfinyl, C 3-10 Cycloalkyl-L X -sulfinyl, 5-10 membered heteroaryl-L X -sulfinyl, 5-10 membered heterocycloalkyl-L X -sulfinyl, C 1-12 Alkylcarbamoyl, C 2-12 Alkenylcarbamoyl, C 2-12 Alkynylcarbamoyl, C 6-10 Aryl-L X -Carbamoyl, C 3-10 Cycloalkyl-L X -carbamoyl, 5- to 10-membered heteroaryl-L X -carbamoyl, 5- to 10-membered heterocycloalkyl-L X -Carbamoyl, C 1-12 Alkyl sulfamoyl, C 2-12 Alkenylsulfamoyl, C 2-12 Alkynylsulfamoyl, C 6-10 Aryl-L X -sulfamoyl, C 3-10 Cycloalkyl-L X -sulfamoyl, 5- to 10-membered heteroaryl-L X -sulfamoyl, and 5- to 10-membered heterocycloalkyl-L X -sulfamoyl, wherein the aryl group has from 1 to the maximum possible number of substituents selected from the group consisting of aryl, aryl, aryl- ...

[0021] Substituent group III consists of halogen, hydroxy, carboxy, amino, carbamoyl, nitro, amidinoamino, alkyl, aryl, cycloalkyl, heteroaryl, alkyloxy, alkylcarbonyl, cycloalkylcarbonyl, alkylcarbonylamino, cycloalkylcarbonylamino, alkylamino, cycloalkylalkylamino, alkyloxycarbonyl, and trialkylsilyloxy, and these groups in the substituent group are optionally substituted with from one to the maximum possible number of identical or different substituents selected from the group consisting of halogen, hydroxy, carboxy, amino, carbamoyl, nitro, alkyl, haloalkyl, alkyloxy, haloalkyloxy, and alkyloxycarbonyl. The substituent group III is preferably the substituent group III′, which includes halogen, hydroxy, carboxy, amino, carbamoyl, nitro, amidinoamino, C 1-12 Alkyl, C 6-10 Aryl, C 3-10 Cycloalkyl, 5-10 membered heteroaryl, C 1-12 Alkyloxy, C 1-12 Alkyl carbonyl, C 3-10 Cycloalkylcarbonyl, C 1-12 Alkylcarbonylamino, C 3-10 Cycloalkylcarbonylamino, C 1-12 Alkylamino, C 3-10 Cycloalkyl C 1-6 Alkylamino, C 1-12 Alkyloxycarbonyl, and TriC 1-6 alkylsilyloxy, and these groups in the above substituent group are halogen, hydroxy, carboxy, amino, carbamoyl, nitro, C 1-12 Alkyl, C 1-12 Haloalkyl, C 1-12 Alkyloxy, C 1-12 Haloalkyloxy, and C 1-12 It may be substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkyloxycarbonyl.

[0022] Substituent group IV consists of halogen, hydroxy, carboxy, amino, carbamoyl, nitro, amidino, alkyl, aryl, cycloalkyl, heteroarylheterocycloalkyl, arylalkyl, cycloalkylalkyl, alkyloxy, aryloxy, alkylcarbonyl, cycloalkylcarbonyl, alkyloxycarbonyl, and trialkylsilyloxy, and these groups in the substituent group are optionally substituted with from one to the maximum possible number of identical or different substituents selected from the group consisting of halogen, hydroxy, carboxy, amino, carbamoyl, nitro, alkyl, haloalkyl, alkyloxy, haloalkyloxy, and alkyloxycarbonyl. Substituent group IV is preferably substituent group IV′, which includes halogen, hydroxy, carboxy, amino, carbamoyl, nitro, amidino, C 1-6 Alkyl, C 6-10 Aryl, C 3-10 Cycloalkyl, 5-10 membered heteroaryl, 5-10 membered heterocycloalkyl, C 6-10 Aryl C 1-6 Alkyl, C 3-10 Cycloalkyl C 1-6 Alkyl, C 1-6 Alkyloxy, C 6-10 Aryloxy, C 1-6 Alkyl carbonyl, C 3-10 Cycloalkylcarbonyl, C 1-6 Alkyloxycarbonyl, and TriC 1-6 alkylsilyloxy, and each of these groups in the substituent group is independently selected from halogen, hydroxy, carboxy, amino, carbamoyl, nitro, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkyloxy, C 1-6 Haloalkyloxy, and C 1-6 It may be substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkyloxycarbonyl.

[0023] Substituent group V is selected from the group consisting of halogen, hydroxy, carboxy, amino, formyl, carbamoyl, cyano, nitro, amidino, amidinoamino, alkyl, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, alkyloxy, aryloxy, cycloalkyloxy, heteroaryloxy, heterocycloalkyloxy, alkyloxyoxy, alkylamino, arylamino, cycloalkylamino, heteroarylamino, heterocycloalkylamino, formyl, alkylcarbonyl, arylcarbonyl, cycloalkylcarbonyl, heteroarylcarbonyl, heterocycloalkylcarbonyl, alkyloxycarbonyl, aryloxycarbonyl, and cycloalkyloxycarbonyl. and heterocycloalkyloxycarbonyl, alkylcarbamoyl, arylcarbamoyl, cycloalkylcarbamoyl, heteroarylcarbamoyl, and heterocycloalkylcarbamoyl, wherein each of these groups in the aforementioned substituent group is independently optionally substituted with from one to the maximum possible number of the same or different substituents selected from the group consisting of halogen, hydroxy, carboxy, amino, formyl, carbamoyl, cyano, nitro, amidino, amidinoamino, alkyl, alkyloxy, haloalkyl, haloalkyloxy, alkylamino, formyl, alkylcarbonyl, alkyloxycarbonyl, and alkylcarbamoyl. The substituent group V is preferably a substituent group V′, which is a group selected from the group consisting of halogen, hydroxy, carboxy, amino, formyl, carbamoyl, cyano, nitro, amidino, amidinoamino, C 1-12 Alkyl, C 6-10 Aryl, C 3-10 Cycloalkyl, 5-10 membered heteroaryl, 5-10 membered heterocycloalkyl, C 1-12 Alkyloxy, C 6-10 Aryloxy, C 3-10 Cycloalkyloxy, 5-10 membered heteroaryloxy, 5-10 membered heterocycloalkyloxy, C 1-12 Alkylamino, C 6-10 Arylamino, C 3-10Cycloalkylamino, 5-10 membered heteroarylamino, 5-10 membered heterocycloalkylamino, formyl, C 1-12 Alkyl carbonyl, C 6-10 Arylcarbonyl, C 3-10 Cycloalkylcarbonyl, 5-10 membered heteroarylcarbonyl, 5-10 membered heterocycloalkylcarbonyl, C 1-12 Alkyloxycarbonyl, C 6-10 Aryloxycarbonyl, C 3-10 Cycloalkyloxycarbonyl, 5-10 membered heteroaryloxycarbonyl, 5-10 membered heterocycloalkyloxycarbonyl, C 1-12 Alkylcarbamoyl, C 6-10 Arylcarbamoyl, C 3-10 cycloalkylcarbamoyl, 5- to 10-membered heteroarylcarbamoyl, and 5- to 10-membered heterocycloalkylcarbamoyl, wherein each of these groups in the above substituent groups independently represents halogen, hydroxy, carboxy, amino, formyl, carbamoyl, cyano, nitro, amidino, amidinoamino, C 1-6 Alkyl, C 1-6 Alkyloxy, C 1-6 Haloalkyl, C 1-6 Haloalkyloxy, C 1-6 Alkylamino, Formyl, C 1-6 Alkyl carbonyl, C 1-6 Alkyloxycarbonyl, and C 1-6 It may be substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkylcarbamoyl.

[0024] Substituent group VI consists of halogen, hydroxy, carboxy, amino, formyl, carbamoyl, cyano, nitro, amidino, amidinoamino, alkyl, alkyloxy, haloalkyl, haloalkyloxy, alkylamino, formyl, alkylcarbonyl, alkyloxycarbonyl, and alkylcarbamoyl. Substituent group VI is preferably substituent group VI′, which includes halogen, hydroxy, carboxy, amino, formyl, carbamoyl, cyano, nitro, amidino, amidinoamino, C 1-6 Alkyl, C 1-6 Alkyloxy, C 1-6 Haloalkyl, C 1-6 Haloalkyloxy, C 1-6 Alkylamino, Formyl, C 1-6 Alkyl carbonyl, C 1-6 Alkyloxycarbonyl, and C 1-6 It consists of alkylcarbamoyl.

[0025] In the present specification, examples of substituents in the case of being "substituted as needed" include substituent group α and substituent group β. Substituent group α may be substituent group α1, substituent group α2, or substituent group α3, and substituent group β may be substituent group β1, substituent group β2, or substituent group β3. Substituents in the case of being "substituted as needed" may be selected from substituent group α1, and may be substituted with 1 to 5 identical or different substituents. The type of atom in the substituent participating in the bond is not particularly limited by the type of substituent, but when the atom to which the substituent is bonded is an oxygen atom, nitrogen atom, or sulfur atom, the substituents listed below are limited to those in which the atom to which the substituent is bonded is a carbon atom. The substituent group α1 is 1) Halogen atoms 2) Hydroxyl group 3) Carboxyl group 4) Cyano group 5) C 1-6 Alkyl 6) C 2-6 Alkenyl 7) C 2-6 Alkynyl 8) C 1-6 Alkoxy 9) C 1-6 Alkylthio 10) C 1-6 Alkyl carbonyl 11)C 1-6 Alkyl sulfonyl (However, each of the substituents 5) to 11) may be substituted with 1 to 5 identical or different substituents selected from the substituent group β1.) 12)C 3-10 alicyclic group 13)C 3-10 Alicyclic oxy 14)C 6-10 Aryloxy 15) 5- or 6-membered heteroaryloxy 16) 4-10 membered non-aryl heterocyclic oxy 17)C 3-10 Alicyclic Thio 18)C 6-10 Arylthio 19) 5- or 6-membered heteroarylthio 20) 4-10 membered non-aryl heterocyclic thio 21)C 6-10 Aryl 22) 5- or 6-membered heteroaryl 23) 4-10 membered non-aryl heterocycles 24)C 3-10 Alicyclic carbonyl 25)C 6-10 arylcarbonyl 26) 5- or 6-membered heteroarylcarbonyl 27) 4-10-membered non-aryl heterocyclic carbonyl 28)C 3-10 Alicyclic sulfonyl 29)C 6-10 Arylsulfonyl 30) 5- or 6-membered heteroarylsulfonyl 31) 4-10-membered non-aryl heterocycle sulfonyl (However, each of the substituents in 12) to 31) is 1 to 5 of the substituent group β1 or the above 5) C 1-6 (optionally substituted by alkyl) 32)-NR 10a R 11a 33)-SO2-NR 10b R 11b 34)-NR 10c -C(=O)R 11c 35)-NR 10d -C(=O)OR 11d 36)-NR 12a -C(=O)NR 10e R 11e 37)-NR 10i -SO2-R 11i 38)-NR 12c -SO2-NR 10j R 11j 39)-C(=O)OR 10k 40)-C(=O)NR 10l R 11k 41)-C(=O)NR 10m OR 11l 42)-C(=O)NR 12d -NR 10n R 11m 43)-C(=NR 13a )R 10s 44)-C(=NR 13c )NR 10t R 11q 45)-C(=NR 13d )NR 12f -NR 10u R 11r 46)-NR 17c -C(=NR 13k )R 17d 47)-NR 12g -C(=NR 13e )-NR 10v R 11s 48)-NR 14 -C(=NR 13f )-NR 12h -NR 10w R 11t 49)-OC(=O)R 10x 50)-OC(=O)OR 10y 51)-OC(=O)NR 10z1 R11u 52)-NR 12i -NR 10z2 R 11v 53)-NR 10z3 OR 11w 54) Protecting group are listed, The substituent group β1 is 1) halogen atoms, 2) hydroxyl group, 3) carboxyl group, 4) a cyano group, 5) C 3-10 alicyclic group, 6) C 1-6 Alkoxy, 7) C 3-10 Alicyclic oxy, 8) C 1-6 Alkylthio, 9) 5- or 6-membered heteroarylthio, 10) C 6-10 aryl, 11) 5- or 6-membered heteroaryl, 12) 4- to 10-membered non-aryl heterocycles, 13)C 1-6 alkylcarbonyl, 14)C 3-10 alicyclic carbonyls, 15)C 6-10 arylcarbonyl, 16) 5- or 6-membered heteroarylcarbonyl, 17) 4-10 membered non-aryl heterocycle carbonyl, 18)-NR 15a R 16a , 19)-SO2-NR 15b R 16b , 20)-NR 15c -C(=O)R 16c 21)-NR 17a -C(=O)NR 15d R 16d , 22)-C(=O)NR 15e R 16e , 23)-C(=NR 13g )R 15f , 24)-C(=NR 13h )NR 15g R 16f 25)-NR 16g -C(=NR 13i )R 15h 26)-NR 17b -C(=NR 13j )-NR 15i R 16h 27) Protecting group (However, in the substituent group β1, each of the substituents 5) to 17) is a halogen atom, a hydroxyl group, a cyano group, a carboxyl group, -NR 18a R 18b and optionally substituted with 1 to 5 substituents selected from the group consisting of: R 13a , R 13a2 , R 13c , R 13c2 , R 13d , R 13d2 , R 13e , R 13f , R 13g , R 13g2 , R 13h , R 13h2 , R 13i , R 13j , R 13k are each independently the same or different and represent a hydrogen atom, a hydroxyl group, or C 1-6 Alkyl, C 1-6 Alkoxy, or C 1-6 is an alkoxycarbonyl, R 10a , R 10b , R 10c , R 10d , R 10e , R 10i , R 10j , R 10k , R 10l , R 10m , R 10n , R 10s , R 10s2 , R 10t , R 10t2 , R10u , R 10u2 , R 10v , R 10w , R 10x , R 10y , R 10z1 , R 10z2 , R 10z3 , R 11a , R 11b , R 11c , R 11d , R 11e , R 11i , R 11j , R 11k , R 11l , R 11m , R 11q , R 11q2 , R 11r , R 11r2 , R 11s , R 11t , R 11u , R 11v , R 11w , R 12a , R 12c , R 12d , R 12f , R 12f2 , R 12g , R 12h , R 12i , R 14 , R 15a , R 15b , R 15c , R 15d , R 15e , R 15f , R 15f2 , R 15g , R 15g2 , R 15h , R 15i , R 16a , R 16b , R 16c , R 16d , R 16e , R 16f , R 16f2 , R 16g , R 16h , R 17a , R 17b , R 17c , R 17d are each independently the same or different and represent a hydrogen atom, C 1-6 Alkyl (C 1-6 Alkyl is a hydroxyl group, a cyano group, C 1-6Alkoxy, -NR 18a R 18b may be substituted with 1 to 3 identical or different substituents selected from the following, or C 1-6 is an alkoxycarbonyl, R 18a and R 18b are each independently the same or different and represent a hydrogen atom or C 1-6 It is alkyl. In an exemplary embodiment, the hydrogen of any hydroxyl group in the substituent groups α1 and β1 may be substituted with a protecting group.

[0026] As used herein, the term "optionally substituted" preferably includes the following substituents. The substituent group α2 is preferably 1) Halogen atoms 2) Hydroxyl group 3) Carboxyl group 4) Cyano group 5) C 1-6 Alkyl 6) C 1-6 Alkoxy 7) C 1-6 Alkylthio 8) C 1-6 Alkyl carbonyl (However, each of the substituents 5) to 8) may be substituted with 1 to 5 identical or different substituents selected from the substituent group β2.) 9) C 3-10 alicyclic group 10) C 3-10 Alicyclic oxy 11)C 6-10 Aryloxy 12) 5- or 6-membered heteroaryloxy 13) 4-10 membered non-aryl heterocyclic oxy 14)C 3-10 Alicyclic Thio 15)C 6-10 Arylthio 16) 5- or 6-membered heteroarylthio 17) 4-10 membered non-aryl heterocyclic thio 18)C 6-10 Aryl 19) 5- or 6-membered heteroaryl 20) 4-10 membered non-aryl heterocycles 21)C 3-10 Alicyclic carbonyl 22)C 6-10 arylcarbonyl 23) 5- or 6-membered heteroarylcarbonyl 24) 4-10-membered non-aryl heterocyclic carbonyl (However, each of the substituents in 9) to 24) is 1 to 5 of the substituent group β2 or the above 1) C 1-6 (optionally substituted by alkyl) 25)-NR 10a R 11a 26)-SO2-NR 10b R 11b 27)-NR 10c -C(=O)R 11c 28)-NR 12a -C(=O)NR 10d R 11d 29)-NR 10e -SO2-R 11e 30)-NR 12b -SO2-NR 10f R 11f 31)-C(=O)NR 10g R 11g 32)-C(=NR 13a )R 10h 33)-C(=NR 13b )NR 10i R 11h 34)-NR 11f2 -C(=NR 13c )R 10g2 35)-NR 12c -C(=NR 13d )-NR 10j R 11i are listed, The substituent group β2 is preferably 1) Halogen atoms 2) Hydroxyl group 3) Cyano group 4) C 3-10 alicyclic group 5) C 1-6 Alkoxy 6) C 1-6 Alkylthio 7) 5- or 6-membered heteroarylthio 8) 5- or 6-membered heteroaryl 9) 4-10 membered non-aryl heterocycle 10) C 1-6 Alkyl carbonyl 11)C 3-10 Alicyclic carbonyl 12)C 6-10 arylcarbonyl 13) 5- or 6-membered heteroarylcarbonyl 14) 4-10-membered non-aryl heterocyclic carbonyl 15)-NR 15a R 16a 16)-NR 15b -C(=O)R 16b 17)-NR 17a -C(=O)NR 15c R 16c 18)-C(=O)NR 15d R 16d 19)-C(=NR 13e )R 15e 20)-C(=NR 13f )NR 15f R 16e 21)-NR 16f -C(=NR 13g )R 15g 22)-NR 17b -C(=NR 13h )-NR 15h R 16g 23)-C(=N-OR 13e2 )R 15e2 24)-C(=N-OR 13f2 )NR 15f2 R 16e2 (However, in the substituent group β2, each of the substituents 4) to 14) is a halogen atom, a hydroxyl group, a cyano group, a carboxyl group, -NR 18a R 18b and optionally substituted with 1 to 5 substituents selected from the group consisting of: R 13a , R 13a2 , R 13b , R 13b2 , R 13c , R 13d , R 13e , R 13e2 , R 13f , R 13f2 , R 13g , R 13h are each independently the same or different and represent a hydrogen atom, a hydroxyl group, or C 1-6 Alkyl, C 1-6 Alkoxy, or C 1-6 is an alkoxycarbonyl, R 10a , R 10b , R 10c , R 10d , R 10e , R 10f , R 10g , R 10g2 , R 10h , R 10h2 , R 10i , R 10i2 , R 10j , R 11a , R 11b , R 11c , R 11d , R 11e , R 11f , R 11f2 , R 11g , R 11h , R 11h2 , R 11i , R 12a , R 12b , R 12c , R 15a , R 15b , R 15c , R 15d , R 15e , R 15e2 , R15f , R 15f2 , R 15g , R 15h , R 16a , R 16b , R 16c , R 16d , R 16e , R 16e2 , R 16f , R 16g , R 17a , R 17b are each independently the same or different and represent a hydrogen atom, C 1-6 Alkyl (C 1-6 Alkyl is a hydroxyl group, a cyano group, C 1-6 Alkoxy, -NR 18a R 18b may be substituted with 1 to 3 identical or different substituents selected from the following, or C 1-6 is an alkoxycarbonyl, R 18a , R 18b are each independently the same or different and represent a hydrogen atom or C 1-6 It is alkyl. In an exemplary embodiment, the hydrogen of any hydroxyl group in substituent groups α2 and β2 may be substituted with a protecting group.

[0027] As used herein, the substituents "optionally substituted" include the following more preferred substituents. The substituent group α3 is more preferably 1) Halogen atoms 2) Hydroxyl group 3) Cyano group 4) C 1-6 Alkyl 5) C 1-6 Alkoxy 6) C 1-6 Alkylthio 7) C 1-6 Alkyl carbonyl (However, each of the substituents 4) to 7) may be substituted with 1 to 5 identical or different substituents selected from the substituent group β3.) 8) C 3-10 alicyclic group 9) 5- or 6-membered heteroaryloxy 10) 4-10 membered non-aryl heterocyclic oxy 11) 5- or 6-membered heteroarylthio 12) 4-10 membered non-aryl heterocyclic thio 13)C 6-10 Aryl 14) 5- or 6-membered heteroaryl 15) 4-10 membered non-aryl heterocycles (However, each of the substituents in 8) to 15) is 1 to 5 of the substituent group β3 or the above 1) C 1-6 (optionally substituted by alkyl) 16)-NR 10a R 11a 17)-NR 11b -C(=O)R 10b 18)-NR 12a -C(=O)NR 10c R 11c 19)-C(=O)NR 10d R 11d 20)-C(=NR 13a )R 10e 21)-C(=NR 13b )NR 10f R 11e 22)-NR 11f -C(=NR 13c )R 10g 23)-NR 12b -C(=NR 13d )-NR 10h R 11g are listed, The substituent group β3 is more preferably 1) halogen atoms, 2) hydroxyl group, 3) a cyano group, 4)-NR 15a R 16a , 5)-NR 15b -C(=O)R 16b , 6)-NR17a -C(=O)NR 15c R 16c , 7)-C(=O)NR 15d R 16d , 8)-C(=NR 13e )R 15e , 9)-C(=NR 13f )NR 15f R 16e , 10)-NR 16f -C(=NR 13g )R 15g , 11)-NR 17b -C(=NR 13h )-NR 15h R 16g and R 13a , R 13a2 , R 13b , R 13b2 , R 13c , R 13d , R 13e , R 13e2 , R 13f , R 13f2 , R 13g , R 13h are each independently the same or different and represent a hydrogen atom, a hydroxyl group, or C 1-6 Alkyl, C 1-6 Alkoxy, or C 1-6 is an alkoxycarbonyl, R 10a , R 10b , R 10c , R 10d , R 10e , R 10f , R 10e2 , R 10f2 , R 10g , R 10h , R 11a , R 11b , R 11c , R 11d , R 11e , R 11e2 , R 11f , R 11g , R 12a , R 12b , R 15a , R15b , R 15c , R 15d , R 15e , R 15e2 , R 15f , R 15f2 , R 15g , R 15h , R 16a , R 16b , R 16c , R 16d , R 16e , R 16e2 , R 16f , R 16g , R 17a , R 17b are each independently the same or different and represent a hydrogen atom, C 1-6 Alkyl (C 1-6 Alkyl is a hydroxyl group, a cyano group, C 1-6 Alkoxy, -NR 18a R 18b may be substituted with 1 to 3 identical or different substituents selected from the following, or C 1-6 is an alkoxycarbonyl, R 18a , R 18b are each independently the same or different and represent a hydrogen atom or C 1-6 It is alkyl. In an exemplary embodiment, the hydrogen of any hydroxyl group in substituent groups α3 and β3 may be substituted with a protecting group.

[0028] In an exemplary embodiment, the hydroxyl group in the above substituent groups (e.g., α (α1, etc.), β (β1, etc.), I to VI) may be further protected with a silyl protecting group. In an exemplary embodiment, the amino group in the above substituent groups I to VI may be further protected with a nitrogen protecting group.

[0029] As used herein, "C 1-6 " means that the number of carbon atoms is 1 to 6. The same applies to other numbers, for example, "C 1-4 " means that the number of carbon atoms is 1 to 4, and "C 1-3" means that the number of carbon atoms is 1 to 3. In this specification, descriptions limiting the number of carbon atoms are merely preferred numerical ranges, and it is intended that groups having substituents with carbon atoms other than the specified number of carbon atoms also fall within the scope of the present disclosure.

[0030] As used herein, the term "hydrocarbon group," also referred to as a hydrocarbyl group, refers to a group formed by removing at least one hydrogen from a "hydrocarbon" containing at least one carbon and at least one hydrogen.

[0031] In this specification, the term "functional group" refers to any group that imparts some functionality, and includes a carboxyl group, a nitrile group, a carbonyl group, a hydroxy group, an amino group, an imino group, a nitro group, a halogen group, as well as an alkyl group, and in a broad sense also includes groups formed by bonds such as acid anhydrides, ester bonds, amide bonds, and ether bonds.

[0032] As used herein, the term "heteroatom" refers to an atom other than carbon or hydrogen atoms, such as an oxygen atom, nitrogen atom, or sulfur atom. A group containing a heteroatom may be referred to as a hetero... group (e.g., a heteroaryl group (meaning that an aryl group contains at least a heteroatom)) or a hetero... group (e.g., a heterocyclic group (meaning that a ring group (carbocyclic group) contains at least one heteroatom)).

[0033] As used herein, a "halogen atom" refers to an atom belonging to the halogen group, such as a fluorine atom, a chlorine atom, a bromine atom, or an iodine atom. A fluorine atom or a chlorine atom is preferred. A fluorine atom is more preferred. A "halogen atom" may also be referred to as "halogen" or "halo".

[0034] As used herein, a "hydroxyl group" refers to a monovalent group of -OH. This group may also be called a "hydroxy group" or "hydroxy."

[0035] As used herein, a "carboxyl group" refers to a monovalent group of -COOH. This group may also be referred to as a "carboxy group," "carboxy," or "carboxyl."

[0036] As used herein, a "cyano group" is a monovalent radical of -CN.

[0037] As used herein, "amino" refers to the monovalent radical -NH. This group may also be referred to as an "amino group."

[0038] As used herein, "alkyl" refers to a straight-chain or branched-chain saturated aliphatic hydrocarbon group. 1-12 "Alkyl" refers to an alkyl group having 1 to 12 carbon atoms, examples of which include C 1-6 Examples of alkyl include, but are not limited to, alkyl, heptyl, isoheptyl, octyl, isooctyl, nonyl, isononyl, decyl, isodecyl, undecyl, isoundecyl, dodecyl, and isododecyl. 1-6 "Alkyl" is an alkyl group having 1 to 6 carbon atoms, and preferred examples include "C 1-4 alkyl" and more preferably "C 1-3 alkyl," and more preferably "C 1-2 "C alkyl". 1-4 Specific examples of "alkyl" include methyl, ethyl, propyl, isopropyl, n-butyl, isobutyl, tert-butyl, sec-butyl, etc. 1-6 Specific examples of "alkyl" include C 1-4 Examples include, but are not limited to, alkyl, n-pentyl, isopentyl, neopentyl, tert-pentyl, 1,2-dimethylpropyl, n-hexyl, and the like.

[0039] As used herein, "alkenyl" refers to a straight-chain or branched-chain unsaturated aliphatic hydrocarbon group containing at least one carbon-carbon double bond. 2-12"Alkenyl" refers to an alkenyl group having 2 to 12 carbon atoms, and examples thereof include, but are not limited to, heptenyl, isoheptenyl, octenyl, isooctenyl, nonenyl, isononenyl, decenyl, isodecenyl, undecenyl, isoundecenyl, dodecenyl, and isododecenyl. 2-6 "Alkenyl" refers to an alkenyl group having 2 to 6 carbon atoms, and preferred examples include "C 2-4 Alkenyl" is an example of "C 2-6 Specific examples of "alkenyl" include, but are not limited to, vinyl, 1-propenyl, 2-propenyl, 1-butenyl, 2-butenyl, 3-butenyl, 2-methyl-1-propenyl, 2-methyl-2-propenyl, and the like.

[0040] As used herein, "alkynyl" refers to a straight-chain or branched-chain unsaturated aliphatic hydrocarbon group containing at least one carbon-carbon triple bond. 2-12 "Alkynyl" refers to an alkynyl group having 2 to 12 carbon atoms, and examples thereof include, but are not limited to, heptynyl, isoheptynyl, octynyl, isooctynyl, nonynyl, isononynyl, decynyl, isodecynyl, undecynyl, isoundecynyl, dodecynyl, isododecynyl, and the like. 2-6 "Alkynyl" refers to an alkynyl group having 2 to 6 carbon atoms, and preferred examples include "C 2-4 Alkynyl" is an example of "C 2-6 Examples of "alkynyl" include, but are not limited to, ethynyl, 1-propynyl, 2-propynyl, 1-butynyl, 1-methyl-2-propynyl, 3-butynyl, 1-pentynyl, 1-hexynyl, and the like.

[0041] As used herein, "aryl" means a monovalent radical of a monocyclic or bicyclic aromatic hydrocarbon ring, and "C 6-10 "Aryl" means an aryl group having 6 to 10 carbon atoms. Examples of "aryl" include C6 aryl, C 10Examples of C6 aryl include, but are not limited to, phenyl, etc. Specific examples of C6 aryl include, but are not limited to, phenyl, etc. 10 Specific examples of aryl include, but are not limited to, 1-naphthyl, 2-naphthyl, and the like.

[0042] The aryl group as a substituent or part thereof may be fused with an alicyclic group. For example, a phenyl group may be fused with a cyclohexane ring to form a 1,2,3,4-tetrahydronaphthalenyl group, in which case any available carbon atom on the benzene ring is bonded to the parent skeleton or to a group or atom thereof close to the parent skeleton. The aryl group includes 5,6,7,8-tetrahydronaphthalen-1-yl and 5,6,7,8-tetrahydronaphthalen-2-yl.

[0043] As used herein, "arylalkyl" refers to an alkyl substituted with at least one aryl. 6-10 Aryl C 1-6 "Alkyl" has at least one C 6-10 Aryl-substituted C 1-6 It means alkyl. 6-10 Aryl C 1-6 Specific examples of alkyl include, but are not limited to, benzyl (phenyl-CH2-), phenethyl (phenyl-CH2CH2-), naphthalen-1-ylmethyl, naphthalen-2-ylmethyl, 2-(naphthalen-1-yl)ethyl, 2-(naphthalen-2-yl)ethyl, and the like.

[0044] As used herein, "(optionally substituted amino)-arylalkyl" refers to an arylalkyl substituted with an optionally substituted amino group, where the alkyl group or the aryl group, or both, are substituted with an amino group. The amino group of the arylalkyl group may be unsubstituted or may have 1, 2, or 3 substituents, such as an optionally substituted alkyl (e.g., unsubstituted C 1-6 Alkyl, C 3-6 Cycloalkyl-C 1-6 Alkyl, C3-6 (Optionally substituted amino)-C 6-10 Aryl C 1-6 Examples of alkyl include, but are not limited to, (di(alkyl)amino)benzyl, ((cycloalkylalkyl)amino)benzyl, ((cycloalkylcarbonyl)amino)benzyl, ((carbamoylalkyl)carbonylamino)benzyl, ((carboxyalkyl)carbonyl)aminobenzyl, (di(alkyl)amino)naphthalenylmethyl, ((cycloalkylalkyl)amino)naphthalenylmethyl, ((cycloalkylcarbonyl)amino)naphthalenylmethyl, ((carbamoylalkyl)carbonylamino)naphthalenylmethyl, or ((carboxyalkyl)carbonyl)aminonaphthalenylmethyl, and the like.

[0045] As used herein, the aryl moiety of "arylthio" has the same meaning as the aryl defined above. 6-10 As "arylthio", preferably "C6 or C 10 "C 6-10 Specific examples of "aryloxy" include, but are not limited to, phenylthio, 1-naphthylthio, 2-naphthylthio, and the like.

[0046] As used herein, "arylsulfonyl" refers to a sulfonyl substituted with the above-mentioned "aryl". 6-10 As "arylsulfonyl", preferably "C6 or C 10 "C 6-10 Specific examples of "arylsulfonyl" include, but are not limited to, phenylsulfonyl, 1-naphthylsulfonyl, 2-naphthylsulfonyl, and the like.

[0047] As used herein, "heteroaryl" refers to a monovalent monocyclic or bicyclic aromatic heterocyclic group containing 1 to 4 identical or different heteroatoms selected from the group consisting of oxygen, nitrogen, and sulfur atoms.

[0048] As used herein, "5- or 6-membered heteroaryl" refers to a monovalent group of a monocyclic aromatic heterocycle consisting of 5 to 6 atoms, containing 1 to 4 identical or different heteroatoms selected from the group consisting of oxygen, nitrogen, and sulfur atoms. Specific examples of "5- or 6-membered heteroaryl" include, but are not limited to, pyrrolyl, furyl, thienyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, oxadiazolyl, thiazolyl, isothiazolyl, thiadiazolyl, tetrazolyl, pyridyl, furyl, pyridazinyl, pyrimidinyl, and pyrazinyl.

[0049] As used herein, the term "5- to 10-membered heteroaryl" refers to a monovalent monocyclic or bicyclic aromatic heterocyclic group consisting of 5 to 10 atoms, containing 1 to 4 identical or different heteroatoms selected from the group consisting of oxygen atoms, nitrogen atoms, and sulfur atoms. Specific examples of "5- to 10-membered heteroaryl" include, but are not limited to, 5- or 6-membered heteroaryl, quinolyl, isoquinolyl, naphthyridinyl, quinoxalinyl, cinnolinyl, quinazolinyl, phthalazinyl, imidazopyridyl, imidazothiazolyl, imidazooxazolyl, benzothiazolyl, benzoxazolyl, benzimidazolyl, indolyl, isoindolyl, indazolyl, pyrrolopyridyl, thienopyridyl, furopyridyl, benzothiadiazolyl, benzoxadiazolyl, pyridopyrimidinyl, benzofuryl, benzothienyl, benzo[1,3]dioxole, thienofuryl, chromenyl, chromanyl, coumarinyl, quinolonyl, and the like.

[0050] As used herein, "heteroarylalkyl" refers to an alkyl substituted with at least one heteroaryl. 1-6 "Alkyl" refers to a C alkyl substituted with at least one 5- to 10-membered heteroaryl. 1-6 alkyl; 5-10 membered heteroaryl C 1-6Specific examples of alkyl include, but are not limited to, pyridin-2-ylmethyl, pyridin-4-ylmethyl, 2-(quinolin-8-yl)ethyl, 2-(quinolin-5-yl)ethyl, 2-(quinoxalin-5-yl)ethyl, 2-(1H-indol-3-yl)ethyl, and the like.

[0051] As used herein, the term "alicyclic group" refers to a monovalent group of a monocyclic, bicyclic, or tricyclic non-aromatic hydrocarbon ring, and includes groups having partially unsaturated bonds, partially bridged structures, partially spiro groups, and groups having one, two, or more carbonyl structures. The term "alicyclic group" encompasses cycloalkyl, cycloalkenyl, and cycloalkynyl. 3-20 As the "alicyclic group", preferably "C 3-10 alicyclic group," and more preferably "C 3-6 "C" is an alicyclic group. 3-20 Specific examples of the "alicyclic group" include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclohexadinyl, cycloheptadinyl, cyclooctadinyl, adamantyl, norbornyl, and the like.

[0052] The alicyclic group may be a fused ring of a non-aryl ring with an aryl and / or heteroaryl ring. For example, C 6-10 Cycloalkyl fused with aryl or 5- or 6-membered heteroaryl is included in the alicyclic group. Examples of fused alicyclic groups include monovalent groups obtained by removing one hydrogen atom from 1,2,3,4-tetrahydronaphthalene, indan, 1,2,3,4-tetrahydroanthracene, and 5,6,7,8-tetrahydroquinoline, and specific examples include 1,2,3,4-tetrahydronaphthalen-1-yl, 1,2,3,4-tetrahydronaphthalen-2-yl, indan-1-yl, indan-2-yl, 5,6,7,8-tetrahydroquinolin-5-yl, and 5,6,7,8-tetrahydroquinolin-6-yl. The fused alicyclic group is bonded to the parent skeleton from any one of the possible ring-constituting atoms on the non-aryl ring.

[0053] As used herein, "C 3-10 The "alicyclic group" is the same as the "C 3-20 Alicyclic group" 3-10 The term "alicyclic group" refers to a substituent in which the alicyclic group is a monovalent group.

[0054] As used herein, "alicyclic oxy" refers to a (alicyclic group)-O- group, and the alicyclic moiety has the same meaning as an alicyclic group. 3-6 "Alicyclic oxy" is (C 3-6 means an alicyclic group)-O- group, 3-6 The alicyclic moiety is C 3-6 It is synonymous with alicyclic group. 3-6 As the "alicyclic oxy", preferably "C 3-5 "C 3-6 Specific examples of "alicyclicoxy" include, but are not limited to, cyclopropyloxy, cyclobutyloxy, cyclopentyloxy, cyclohexyloxy, and the like.

[0055] As used herein, the term "alicyclic carbonyl" refers to a carbonyl substituted with the above-mentioned "alicyclic group." 3-10 As the "alicyclic carbonyl", preferably, "C 3-6 "C" is an alicyclic carbonyl. 3-10 Specific examples of the "alicyclic carbonyl" include, but are not limited to, cyclopropylcarbonyl, cyclobutylcarbonyl, cyclopentylcarbonyl, cyclohexylcarbonyl, and the like.

[0056] As used herein, "alicyclic thio" refers to the group (alicyclic group)-S-, wherein the alicyclic moiety is as defined above. 3-10 As the "alicyclic thio", preferably "C 3-6 "C 3-6 Specific examples of "alicyclic thio" include, but are not limited to, cyclopropylthio, cyclobutylthio, cyclopentylthio, cyclohexylthio, and the like.

[0057] As used herein, the term "alicyclic sulfonyl" refers to a sulfonyl group substituted with the above-mentioned "alicyclic group". 3-10 As "alicyclic sulfonyl", preferably "C 3-6 "C 3-10 Specific examples of "alicyclic sulfonyl" include, but are not limited to, cyclopropylsulfonyl, cyclobutylsulfonyl, cyclopentylsulfonyl, cyclohexylsulfonyl, and the like.

[0058] As used herein, "cycloalkyl" refers to a non-aromatic saturated hydrocarbon ring group, including those having a partially bridged structure, those having a partially spiro structure, and those having one, two, or more carbonyl structures. 3-20 "Cycloalkyl" means a monocyclic or bicyclic cycloalkyl having 3 to 20 carbon atoms. 3-6 "Cycloalkyl" means a monocyclic cycloalkyl having 3 to 6 carbon atoms. 3-6 Examples of cycloalkyl include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl.

[0059] The cycloalkyl group as a substituent or part thereof may be fused with an aryl and / or heteroaryl ring. For example, a cyclohexyl group may be fused with a benzene ring to form a 1,2,3,4-tetrahydronaphthalenyl group, in which case any available carbon atom on the cyclohexane ring is bonded to the parent skeleton or a group or atom close to the parent skeleton. Cycloalkyl groups include 1,2,3,4-tetrahydronaphthalen-1-yl, 1,2,3,4-tetrahydronaphthalen-2-yl, indan-1-yl, indan-2-yl, 5,6,7,8-tetrahydroquinolin-5-yl, and 5,6,7,8-tetrahydroquinolin-6-yl.

[0060] As used herein, "cycloalkylalkyl" refers to an alkyl substituted with at least one cycloalkyl. 3-6 Cycloalkyl C 1-6"Alkyl" has at least one C 3-6 Cycloalkyl-substituted C 1-6 It means alkyl. 3-6 Cycloalkyl C 1-6 Specific examples of alkyl include, but are not limited to, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, 2-cyclopropylethyl, 2-cyclobutylethyl, 2-cyclopentylethyl, 2-cyclohexylethyl, 3-cyclopropylpropyl, 3-cyclobutylpropyl, 3-cyclopentylpropyl, 3-cyclohexylpropyl, and the like.

[0061] As used herein, "heterocycloalkyl" refers to a non-aromatic saturated or partially unsaturated heterocycle composed of three or more atoms, including one, two, or more identical or different heteroatoms selected from the group consisting of oxygen, nitrogen, and sulfur atoms, and includes those having a partially bridged structure and those having a partially spiro-linked structure. "Heterocycloalkyl" encompasses "non-aryl heterocycles." Heterocycloalkyls can have a structure in which a non-aromatic heterocycle is fused with an aryl ring and / or a heteroaryl ring.

[0062] As used herein, the term "non-aryl heterocycle" refers to a monocyclic or bicyclic non-aromatic heterocycle consisting of three or more atoms, including one or two or more identical or different heteroatoms selected from the group consisting of oxygen, nitrogen, and sulfur atoms, and includes saturated non-aryl heterocycles, those having a partially unsaturated bond, those having a partially bridged structure, and those having a partially spiro-bonded structure. The non-aryl heterocycle may form a condensed ring with an aryl or heteroaryl. For example, C 6-10A heterocycle also includes a ring fused with an aryl or a 5- or 6-membered heteroaryl. The non-aryl heterocycle may contain one, two, or more carbonyls, thiocarbonyls, sulfinyls, or sulfonyls, and cyclic groups such as lactams, thiolactams, lactones, thiolactones, cyclic imides, cyclic carbamates, and cyclic thiocarbamates are also included in the non-aryl heterocycle. Here, the oxygen atom of the carbonyl, sulfinyl, and sulfonyl and the sulfur atom of the thiocarbonyl are not included in the number of ring members (ring size) and the number of heteroatoms constituting the ring.

[0063] In the present specification, the term "4- to 10-membered non-aryl heterocycle" refers to a substituent in which the "4- to 10-membered non-aryl heterocycle" is a monovalent group among the above-mentioned "non-aryl heterocycles".

[0064] As used herein, the non-aryl heterocyclic moiety of "non-aryl heterocyclic oxy" has the same meaning as the above-mentioned "non-aryl heterocycle". The "4- to 10-membered non-aryl heterocyclic oxy" is preferably a "4- to 6-membered non-aryl heterocyclic oxy". Specific examples of the "4- to 10-membered non-aryl heterocyclic oxy" include, but are not limited to, tetrahydrofuranyloxy, tetrahydropyranyloxy, azetidinyloxy, pyrrolidinyloxy, piperidinyloxy, etc.

[0065] As used herein, the non-aryl heterocyclic moiety of "non-aryl heterocyclic thio" has the same meaning as the above-mentioned "non-aryl heterocycle." The "4- to 10-membered non-aryl heterocyclic thio" is preferably a "4- to 6-membered non-aryl heterocyclic thio." Specific examples of the "4- to 10-membered non-aryl heterocyclic thio" include, but are not limited to, tetrahydropyranylthio, piperidinylthio, etc.

[0066] As used herein, "non-aryl heterocyclic carbonyl" refers to a carbonyl group substituted with the above-mentioned "non-aryl heterocycle". The "4- to 10-membered non-aryl heterocyclic carbonyl" is preferably a "4- to 6-membered non-aryl heterocyclic carbonyl". Specific examples of the "4- to 10-membered non-aryl heterocyclic carbonyl" include, but are not limited to, azetidinylcarbonyl, pyrrolidinylcarbonyl, piperidinylcarbonyl, morpholinylcarbonyl, etc.

[0067] As used herein, "non-aryl heterocyclic sulfonyl" refers to a sulfonyl group substituted with the above-mentioned "non-aryl heterocycle." The "4- to 10-membered non-aryl heterocyclic sulfonyl" is preferably a "4- to 6-membered non-aryl heterocyclic sulfonyl." Specific examples of the "4- to 10-membered non-aryl heterocyclic sulfonyl" include, but are not limited to, azetidinylsulfonyl, pyrrolidinylsulfonyl, piperidinylsulfonyl, morpholinylsulfonyl, etc.

[0068] As used herein, the term "5- to 6-membered heterocycloalkyl" refers to a heterocycloalkyl consisting of 5 to 6 ring atoms, including one or more identical or different heteroatoms selected from oxygen, nitrogen, and sulfur atoms.

[0069] As used herein, "heterocycloalkylalkyl" refers to an alkyl substituted with at least one heterocycloalkyl.

[0070] As used herein, "alkylcarbonyl" refers to a monovalent group of -C(=O)-alkyl. Preferred examples of alkylcarbonyl include C 1-6 Alkylcarbonyl is an example. 1-6Specific examples of alkylcarbonyl include, but are not limited to, acetyl (CHC(=O)-), n-propanoyl (CHCHC(=O)-), n-butanoyl (CHCHCHC(=O)-), n-pentanoyl (CH(CH)C(=O)-), n-hexanoyl (CH(CH)C(=O)-), n-heptanoyl (CH(CH)C(=O)-), and the like.

[0071] As used herein, "alkoxy" refers to a monovalent group of -O-alkyl. Preferred examples of alkoxy include C 1-6 Alkoxy (i.e., C 1-6 Alkyl-O-), C 1-4 Alkoxy (i.e., C 1-4 alkyl-O-) and the like. 1-4 Specific examples of alkoxy include methoxy (CHO-), ethoxy (CHCHO-), n-propoxy (CH(CH)O-), isopropoxy ((CHCHO-), n-butoxy (CH(CH)O-), isobutoxy ((CH)CHCHO-), tert-butoxy ((CH)CO-), sec-butoxy (CHCHCH(CH)O-), etc. 1-6 Specific examples of alkoxy include C 1-4 Examples include, but are not limited to, alkoxy, n-pentyloxy (CH3(CH2)4O-), isopentyloxy ((CH3)2CHCH2CH2O-), neopentyloxy ((CH3)3CCH2O-), tert-pentyloxy (CH3CH2C(CH3)2O-), 1,2-dimethylpropoxy (CH3CH(CH3)CH(CH3)O-), and the like.

[0072] As used herein, an "alkoxycarbonyl" is a monovalent radical of -C(=O)-O-alkyl. Examples of alkoxycarbonyl include C 1-6 Alkoxycarbonyl, preferably C 1-4 Examples include, but are not limited to, alkoxycarbonyl. 1-4Specific examples of alkoxycarbonyl include methoxycarbonyl, ethoxycarbonyl, n-propoxycarbonyl, isopropoxycarbonyl, n-butoxycarbonyl, sec-butoxycarbonyl, tert-butoxycarbonyl, and isobutoxycarbonyl. 1-6 Specific examples of alkoxycarbonyl include C 1-4 Examples include, but are not limited to, alkoxycarbonyl, n-pentyloxycarbonyl, isopentyloxycarbonyl, neopentyloxycarbonyl, tert-pentyloxycarbonyl, 1,2-dimethylpropyloxycarbonyl, n-hexyloxycarbonyl, and the like.

[0073] As used herein, "alkoxycarbonylamino" refers to a monovalent radical of -NH-C(=O)-O-alkyl. Examples of alkoxycarbonylamino include C 1-6 Alkoxycarbonylamino, preferably C 1-4 Examples include, but are not limited to, alkoxycarbonylamino. 1-4 Specific examples of alkoxycarbonylamino include methoxycarbonylamino, ethoxycarbonylamino, n-propoxycarbonylamino, isopropoxycarbonylamino, n-butoxycarbonylamino, sec-butoxycarbonylamino, tert-butoxycarbonylamino, and isobutoxycarbonylamino. 1-6 Specific examples of alkoxycarbonylamino include C 1-4 Examples include, but are not limited to, alkoxycarbonylamino, n-pentyloxycarbonylamino, isopentyloxycarbonylamino, neopentyloxycarbonylamino, tert-pentyloxycarbonylamino, 1,2-dimethylpropyloxycarbonylamino, n-hexyloxycarbonylamino, and the like.

[0074] As used herein, "haloalkyl" refers to a monovalent halogenated alkyl group in which one or more hydrogen atoms on the alkyl group are replaced with halogen atoms. The term "perhaloalkyl" refers to a haloalkyl group in which all hydrogen atoms on the alkyl group are replaced with halogen atoms. For example, perfluoroethyl is -CF2CF3, and perchloro-n-propyl is -CCl2CCl2CCl3. Examples of haloalkyl include C 1-6 Haloalkyl, C 1-4 Haloalkyl, C 1-3 Haloalkyl and the like. 1-3 Specific examples of alkyl include, but are not limited to, fluoromethyl, chloromethyl, bromomethyl, difluoromethyl, dichloromethyl, dibromomethyl, trifluoromethyl, trichloromethyl, tribromomethyl, fluorochloromethyl, difluorochloromethyl, fluorodichloromethyl, fluoroethyl, chloroethyl, bromoethyl, trifluoroethyl, trichloroethyl, tribromoethyl, perfluoroethyl, perchloroethyl, perbromoethyl, perfluoropropyl, perchloropropyl, perbromopropyl, perfluoroisopropyl, perchloroisopropyl, perbromoisopropyl, and the like. 1-4 Specific examples of alkyl include C 1-3 Examples include, but are not limited to, haloalkyl, perfluorobutyl, perchlorobutyl, perbromobutyl, perfluoroisobutyl, perfluoro-t-butyl, and the like. 1-6 Specific examples of alkyl include C 1-4 These include, but are not limited to, haloalkyl, perfluoro-n-pentyl, perfluoroisopentyl, perfluoroneopentyl, perfluorotert-pentyl, perfluoro-1,2-dimethylpropyl, and the like.

[0075] As used herein, "haloalkoxy" and "haloalkyloxy" refer to a monovalent group of -O-haloalkyl in which one or more hydrogen atoms on the alkyl group are replaced with halogen atoms. The term "perhaloalkoxy" refers to a haloalkoxy in which all hydrogen atoms on the alkyl group are replaced with halogen atoms. For example, perfluoroethoxy is -OCF2CF3, and perchloro-n-propoxy is -OCCl2CCl2CCl3. Preferred examples of haloalkoxy include C 1-6 Haloalkoxy, C 1-4 Haloalkoxy, C 1-3 Haloalkoxy and the like are included. 1-3 Specific examples of alkoxy include, but are not limited to, fluoromethoxy, chloromethoxy, bromomethoxy, difluoromethoxy, dichloromethoxy, dibromomethoxy, trifluoromethoxy, trichloromethoxy, tribromomethoxy, fluorochloromethoxy, difluorochloromethoxy, fluorodichloromethoxy, fluoroethoxy, chloroethoxy, bromoethoxy, trifluoroethoxy, trichloroethoxy, tribromoethoxy, perfluoroethoxy, perchloroethoxy, perbromoethoxy, perfluoropropoxy, perchloropropoxy, perbromopropoxy, perfluoroisopropoxy, perchloroisopropoxy, perbromoisopropoxy, and the like. 1-4 Specific examples of alkoxy include C 1-3 Examples include, but are not limited to, haloalkoxy, perfluorobutoxy, perchlorobutoxy, perbromobutoxy, perfluoroisobutoxy, perfluoro-t-butoxy, and the like. 1-6 Specific examples of alkoxy include C 1-4 These include, but are not limited to, haloalkoxy, perfluoro-n-pentyloxy, perfluoroisopentyloxy, perfluoroneopentyloxy, perfluorotert-pentyloxy, perfluoro-1,2-dimethylpropoxy, and the like.

[0076] As used herein, "alkylsulfonyl" refers to a sulfonyl group substituted with the above-mentioned "alkyl". 1-6As "alkylsulfonyl", preferably "C 1-4 "C alkylsulfonyl". 1-6 Specific examples of "alkylsulfonyl" include, but are not limited to, methylsulfonyl, propionylsulfonyl, butyrylsulfonyl, and the like.

[0077] As used herein, the alkyl moiety of "alkylthio" has the same meaning as the alkyl defined above. 1-6 An example of an alkylthio is "C 1-4 alkylthio", preferably "C 1-3 "C alkylthio" 1-6 Specific examples of "alkylthio" include, but are not limited to, methylthio, ethylthio, propylthio, butylthio, isopropylthio, isobutylthio, tert-butylthio, sec-butylthio, isopentylthio, neopentylthio, tert-pentylthio, 1,2-dimethylpropylthio, and the like.

[0078] As used herein, "arylcarbonyl" refers to a monovalent group of -C(=O)-aryl. Preferred examples of arylcarbonyl include C 6-10 Arylcarbonyl is an example. 6-10 Illustrative examples of arylcarbonyl include, but are not limited to, benzoyl (ie, phenyl-C(=O)-), 1-naphthylcarbonyl, 2-naphthylcarbonyl, and the like.

[0079] As used herein, the aryl moiety of "aryloxy" has the same meaning as the above-mentioned aryl. 6-10 As "aryloxy", preferably "C6 or C 10 "C aryloxy" is an example. 6-10 Specific examples of the "aryloxy group" include, but are not limited to, a phenoxy group, a 1-naphthyloxy group, and a 2-naphthyloxy group.

[0080] As used herein, a "heteroarylcarbonyl" is a monovalent radical of -C(=O)-heteroaryl.

[0081] As used herein, the term "heteroarylcarbonyl group" refers to a carbonyl group substituted with the above-mentioned "heteroaryl." Specific examples of the "5- or 6-membered heteroarylcarbonyl group" include, but are not limited to, a pyrazoylcarbonyl group, a triazoylcarbonyl group, a thiazoylcarbonyl group, a thiadiazoylcarbonyl group, a pyridylcarbonyl group, and a pyridazoylcarbonyl group.

[0082] As used herein, the heteroaryl portion of a "heteroaryloxy group" has the same meaning as the above-mentioned "heteroaryl." The 5- or 6-membered heteroaryl portion of a "5- or 6-membered heteroaryloxy group" has the same meaning as a "5-membered heteroaryl" or a "6-membered heteroaryl," respectively. Specific examples of "5- or 6-membered heteroaryloxy groups" include, but are not limited to, pyrazolyloxy groups, triazolyloxy groups, thiazoyloxy groups, thiadiazoyloxy groups, pyridyloxy groups, and pyridazoyloxy groups.

[0083] As used herein, the heteroaryl portion of a "heteroarylthio group" has the same meaning as the above-mentioned "heteroaryl." The 5- or 6-membered heteroaryl portion of a "5- or 6-membered heteroarylthio group" has the same meaning as a "5-membered heteroaryl" or a "6-membered heteroaryl," respectively. Specific examples of the "5- or 6-membered heteroarylthio group" include, but are not limited to, a pyrazoylthio group, a triazoylthio group, a thiazoylthio group, a thiadiazoylthio group, a pyridylthio group, and a pyridazoylthio group.

[0084] As used herein, the heteroaryl moiety of a "heteroarylsulfonyl group" has the same meaning as the above-mentioned "heteroaryl." A "5- or 6-membered heteroarylsulfonyl group" refers to a sulfonyl group substituted with a "5- or 6-membered heteroaryl." Specific examples of the "5- or 6-membered heteroarylsulfonyl group" include, but are not limited to, a pyrazoylsulfonyl group, a triazoylsulfonyl group, a thiazoylsulfonyl group, a thiadiazoylsulfonyl group, a pyridylsulfonyl group, and a pyridazoylsulfonyl group.

[0085] As used herein, "acyl" refers to -C(=O)-R acyl where R acyl is hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocycloalkyl. Specific examples of acyl include, but are not limited to, formyl, and the exemplified groups of alkylcarbonyl, arylcarbonyl, and heteroarylcarbonyl.

[0086] As used herein, an "optionally substituted carbonyl" group refers to a monovalent group of -C(=O)- (hydrogen or any group selected from the substituent group described herein). Examples of "optionally substituted carbonyl" groups include, but are not limited to, formyl, optionally substituted carbamoyl, alkylcarbonyl, alkoxycarbonyl, alkenylcarbonyl, alkenyloxycarbonyl, alkynylcarbonyl, alkynyloxycarbonyl, arylcarbonyl, aryloxycarbonyl, cycloalkylcarbonyl, cycloalkyloxycarbonyl, heteroarylcarbonyl, heteroaryloxycarbonyl, heterocycloalkylcarbonyl, heterocycloalkyloxycarbonyl, and the like. A carbonyl group substituted with hydrogen is a formyl group. A carbonyl group substituted with amino is a carbamoyl group.

[0087] As used herein, an "optionally substituted oxy" group refers to a monovalent group of -O- (hydrogen or any group selected from the substituent group described herein). Examples of "optionally substituted oxy" groups include, but are not limited to, hydroxy, optionally substituted alkyloxy, alkenyloxy, alkynyloxy, aryloxy, heteroaryloxy, heterocycloalkyloxy, alkylcarbonyloxy, alkenylcarbonyloxy, alkynylcarbonyloxy, arylcarbonyloxy, heteroarylcarbonyloxy, heterocycloalkylcarbonyloxy, and the like. An oxy group substituted with hydrogen is a hydroxy group.

[0088] As used herein, "carbamoyl" refers to the monovalent group -C(=O)-NH2.

[0089] As used herein, "amidinoamino" refers to the monovalent group -NH-C(=NH)-NH2.

[0090] As used herein, the term "a group substituted with a substituent" means that the group is substituted with at least one substituent. For example, "hydroxy-substituted C 1-6 "Alkyl" is C 1-6 It means that the alkyl is substituted with at least one hydroxy.

[0091] As used herein, "carbamoyl-substituted C 1-6 "Alkyl" means a C alkyl group substituted with at least one -C(=O)-NH group. 1-6 "Carbamoyl-substituted C 1-6 Examples of "alkyl" include carbamoyl-substituted C 1-4 "Carbamoyl-substituted C 1-4Specific examples of "alkyl" include, but are not limited to, 2-amino-2-oxoethyl (i.e., HNC(=O)-CH- or carbamoylmethyl), 3-amino-3-oxopropyl (i.e., HNC(=O)-CHCH- or carbamoylethyl), 4-amino-4-oxobutyl (i.e., HNC(=O)-(CH)- or carbamoylpropyl), 5-amino-5-oxopentyl (i.e., HNC(=O)-(CH)- or carbamoylbutyl), and the like. 1-6 Specific examples of "alkyl" include carbamoyl-substituted C 1-4 Examples include, but are not limited to, alkyl, 6-amino-6-oxohexyl (i.e., H2NC(=O)-(CH2)5-, or carbamoylpentyl), 7-amino-7-oxoheptyl (i.e., H2NC(=O)-(CH2)6-, or carbamoylhexyl), and the like.

[0092] As used herein, an "amidinoamino-substituted alkyl" or "guanidino-substituted alkyl" refers to an alkyl substituted with at least one -NH-C(=NH)-NH group, wherein the nitrogen atom of the amidinoamino group may be protected with a nitrogen-protecting group (e.g., a tert-butoxycarbonyl group). 1-6 Examples of "alkyl" include "amidinoamino-substituted C 1-4 Examples include, but are not limited to, "amidinoamino-substituted C alkyl" and the like. 1-4 Specific examples of "amidinoamino-substituted C alkyl" include, but are not limited to, (amidinoamino)methyl, 2-(amidinoamino)ethyl, 3-(amidinoamino)propyl, 4-(amidinoamino)butyl, and the like. 1-6 Specific examples of "alkyl" include amidinoamino-substituted C 1-4 Examples of amidinoamino groups protected with a nitrogen protecting group include, but are not limited to, alkyl, 5-(amidinoamino)pentyl, 6-(amidinoamino)hexyl, etc. Examples of amidinoamino groups protected with a nitrogen protecting group include, but are not limited to, [ka] In this specification, "amidinoamino" and "guanidino" have the same meaning.

[0093] As used herein, a "carboxy-substituted alkyl" is an alkyl substituted with at least one -COOH group. 1-6 Examples of "alkyl" include "carboxy-substituted C 1-4 "Carboxy-substituted C alkyl" and the like are included, but are not limited to these. 1-4 Specific examples of "alkyl" include, but are not limited to, carboxymethyl, 2-carboxyethyl, 3-carboxypropyl, 4-carboxybutyl, etc. 1-6 Specific examples of "alkyl" include carboxy-substituted C 1-4 Examples include, but are not limited to, alkyl, 5-carboxypentyl, 6-carboxyhexyl, and the like.

[0094] A "protecting group" refers to a group of atoms that, when attached to a reactive functional group in a molecule, masks, reduces, or prevents the reactivity of the functional group. The compounds of the present disclosure may be substituted with a protecting group at any position, such as any of R1 to R4 or their substituents or other substituents, as appropriate or necessary, and compounds containing such protecting groups are also within the scope of the present disclosure. Typically, the protecting group can be selectively removed during the synthetic process, if desired. Examples of protecting groups can be found in Greene and Wuts, Protective Groups in Organic Chemistry, 5th Edition, 2014, John Wiley & Sons, NY, and Harrison et al., Compendium of Synthetic Organic Methods, Vols. 1-8, John Wiley & Sons, NY, etc. As used herein, "protecting group" may fall within the definitions of 1) to 53) for substituent α and 1) to 26) for substituent β. In this case, in the substituent group α1, "54) protecting group" may be expressed as "54) protecting group other than 1) to 53)," and in the substituent group β1, "27) protecting group" may be expressed as "protecting group other than 1) to 26)." Representative nitrogen protecting groups include, but are not limited to, formyl, acetyl, trifluoroacetyl, benzyl, benzyloxycarbonyl ("CBZ"), tert-butoxycarbonyl ("Boc"), trimethylsilyl ("TMS"), 2-trimethylsilylethanesulfonyl ("TES"), trityl and substituted trityl groups, allyloxycarbonyl, 9-fluorenylmethyloxycarbonyl ("FMOC"), nitro-veratryloxycarbonyl ("NVOC"), and groups represented by "Protect" herein.Representative hydroxyl protecting groups include, but are not limited to, those in which the hydroxyl group is acylated (esterified) or alkylated, such as benzyl and trityl ethers, as well as alkyl ethers, tetrahydropyranyl ethers, trialkylsilyl ethers (e.g., TMS, triethylsilyl, t-butyldimethylsilyl (TBDMS), triisopropylsilyl (TIPS)), alkyldiarylsilyl ethers (e.g., t-butyldiphenylsilyl (TBDPS)), triarylsilyl ethers (e.g., triphenylsilyl), glycol ethers (e.g., ethylene glycol ether, propylene glycol ether, etc.), and allyl ethers.

[0095] An amino group possessed by a compound of the present disclosure (for example, an amino group possessed by the parent skeleton, an amino group as a substituent, an amino group in a substituent possessed by the compound, etc.) may be protected with a nitrogen-protecting group or a group represented by "Protect." An amino group in a substituent listed in a substituent group may be further protected with a nitrogen-protecting group or a group represented by "Protect," and the protected substituent may be used as a substituent.

[0096] The hydroxy group of the compound of the present disclosure (for example, a hydroxy group as a substituent, a hydroxy group in a substituent of the compound, a hydroxy group in the above-mentioned substituent group, etc.) may also be protected with a protecting group for the hydroxy group. The hydroxy group in the substituent listed in the substituent group may be further protected with a hydroxyl-protecting group described herein, and the protected substituent may be used as a substituent.

[0097] (Preferred embodiment) Preferred embodiments of the present disclosure will be described below. The embodiments provided below are provided for a better understanding of the present disclosure, and it is understood that the scope of the present disclosure should not be limited to the following description. Therefore, it is clear that those skilled in the art can make appropriate modifications within the scope of the present disclosure in light of the description herein. It is also understood that the following embodiments of the present disclosure can be used alone or in combination.

[0098] Compounds and Compositions of the Present Disclosure In one aspect, the compounds of the present disclosure have the following formula XXIF: [ka] or an enantiomer thereof, or a salt thereof, or a solvate thereof. R1, R3 and R4 are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted carbonyl; R 2A and R 2B are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted carbonyl, or R 2A and R 2B together with the nitrogen atom to which they are attached form a non-aryl heterocycle or a heteroaryl ring, wherein said non-aryl heterocycle and said heteroaryl ring are each independently optionally substituted. In this specification, R 2Aor R 2B is hydrogen, it is understood that the same definition as R2 described herein may be adopted.

[0099] In another aspect, the compounds of the present disclosure have the following formula XXIB: [ka] or an enantiomer thereof, or a salt thereof, or a solvate thereof. 2a , R 2B and R3 is defined as in formula XXIF described herein.

[0100] In yet another aspect, compounds of the present disclosure have the following formula XXIIF: [ka] or an enantiomer thereof, or a salt thereof, or a solvate thereof. 2A , R 2B and R3 is defined as in formula XXIF described herein.

[0101] In yet another aspect, compounds of the present disclosure have the following formula XIIB: [ka] or an enantiomer thereof, or a salt thereof, or a solvate thereof. In formula XXIIB, R1, R2, and R3 are defined as in formula XXIF described herein.

[0102] In one embodiment, the alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, and carbonyl of R1, R3, and, when present, R4, are each independently optionally substituted with 1 to the maximum possible number of identical or different substituents selected from Substituent Group I; R 2A and R 2B The alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, carbonyl, and the non-aryl heterocycle and heteroaryl ring are each independently substituted with from 1 to the maximum possible number of identical or different substituents selected from Substituent Group I as needed.

[0103] In one embodiment, R, R, and, if present, R, are each independently hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted carbonyl; R 2A and R 2B are each independently hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted carbonyl, or R 2A and R 2B together with the nitrogen atom to which they are attached form a non-aryl heterocycle or a heteroaryl ring, wherein said non-aryl heterocycle and said heteroaryl ring are each independently optionally substituted. Optionally, the substituent in this embodiment is R 2A and R 2Bare each independently hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl, and / or R 2A and R 2B taken together with the nitrogen atom to which they are attached form a non-aryl heterocycle, wherein each said non-aryl heterocycle is independently optionally substituted.

[0104] Alternatively, in another embodiment, (imine form), R and R are each independently hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted carbonyl; and R 2A and R 2B are each independently hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted carbonyl, or R 2A and R 2B together with the nitrogen atom to which they are attached form a non-aryl heterocycle or a heteroaryl ring, wherein said non-aryl heterocycle and said heteroaryl ring are each independently optionally substituted. Optionally, R and R are each independently hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl; R 2A and R 2Bare each independently hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl, and / or R 2A and R 2B taken together with the nitrogen atom to which they are attached form a non-aryl heterocycle, wherein each said non-aryl heterocycle is independently optionally substituted.

[0105] In one embodiment, R, R, and, if present, R, are each independently selected from hydrogen, optionally substituted C 1-12 Alkyl, optionally substituted C 3-10 Cycloalkyl, optionally substituted 5- to 10-membered heterocycloalkyl, optionally substituted C 6-10 aryl, optionally substituted 5- to 10-membered heteroaryl, or optionally substituted carbonyl; R 2A and R 2B each independently represents hydrogen, optionally substituted C 1-12 Alkyl, optionally substituted C 3-10 Cycloalkyl, optionally substituted 5- to 10-membered heterocycloalkyl, optionally substituted C 6-10 aryl, optionally substituted 5- to 10-membered heteroaryl, or optionally substituted carbonyl, or R 2A and R 2B together with the nitrogen atom to which they are attached form a non-aryl heterocycle or a heteroaryl ring, wherein said non-aryl heterocycle and said heteroaryl ring are each independently optionally substituted. In some cases, R 2A and R 2B each independently represents hydrogen, optionally substituted C 1-12 Alkyl, optionally substituted C 3-10 Cycloalkyl, optionally substituted 5- to 10-membered heterocycloalkyl, optionally substituted C 6-10aryl, or optionally substituted 5- to 10-membered heteroaryl, and / or R 2A and R 2B together with the nitrogen atom to which they are attached form a non-aryl heterocycle, wherein said non-aryl heterocycle is independently optionally substituted.

[0106] In one embodiment, R, R and, if present, R are each independently hydrogen, optionally substituted alkyl, optionally substituted arylalkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, formyl, optionally substituted alkylcarbonyl, optionally substituted alkoxycarbonyl, optionally substituted arylcarbonyl, optionally substituted aryloxycarbonyl, optionally substituted heteroarylcarbonyl, optionally substituted heteroaryloxycarbonyl, optionally substituted cycloalkylcarbonyl, optionally substituted cycloalkyloxycarbonyl, optionally substituted heterocycloalkylcarbonyl, optionally substituted heterocycloalkyloxycarbonyl, carbamoyl, optionally substituted alkylcarbamoyl, optionally substituted alkoxycarbamoyl, optionally substituted arylcarbamoyl, optionally substituted heteroarylcarbamoyl, optionally substituted cycloalkylcarbamoyl, or optionally substituted heterocycloalkylcarbamoyl, wherein the groups R, R and R are optionally substituted with 1 to a maximum of the possible number of identical or different substituents selected from Substituent Group II; R 2A and R 2Bare each independently hydrogen, optionally substituted alkyl, optionally substituted arylalkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, formyl, optionally substituted alkylcarbonyl, optionally substituted alkoxycarbonyl, optionally substituted arylcarbonyl, optionally substituted aryloxycarbonyl, optionally substituted heteroarylcarbonyl, optionally substituted heteroaryloxycarbonyl, optionally substituted cycloalkylcarbonyl, optionally substituted cycloalkyloxycarbonyl, optionally substituted heterocycloalkylcarbonyl, optionally substituted heterocycloalkyloxycarbonyl, carbamoyl, optionally substituted alkylcarbamoyl, optionally substituted alkoxycarbamoyl, optionally substituted arylcarbamoyl, optionally substituted heteroarylcarbamoyl, optionally substituted cycloalkylcarbamoyl, or optionally substituted heterocycloalkylcarbamoyl, wherein R 2A and R 2B The above groups are optionally substituted with one to the maximum possible number of identical or different substituents selected from Substituent Group II, or R 2A and R 2B form a 5- to 6-membered non-aryl heterocycle or heteroaryl ring together with the nitrogen atom to which they are bonded, wherein the non-aryl heterocycle and the heteroaryl ring are optionally substituted with one to the maximum possible number of identical or different substituents selected from Substituent Group II.

[0107] In one embodiment, R, R, and, if present, R, are each independently selected from hydrogen, optionally substituted C 1-12 Alkyl, optionally substituted C 6-10 Aryl C 1-12 Alkyl, optionally substituted C 3-10 Cycloalkyl, optionally substituted 5- to 10-membered heterocycloalkyl, formyl, optionally substituted C 1-12Alkylcarbonyl, optionally substituted C 1-12 Alkoxycarbonyl, optionally substituted C 6-10 Arylcarbonyl, optionally substituted C 6-10 Aryloxycarbonyl, optionally substituted 5- to 10-membered heteroarylcarbonyl, optionally substituted 5- to 10-membered heteroaryloxycarbonyl, optionally substituted C 3-10 Cycloalkylcarbonyl, optionally substituted C 3-10 Cycloalkyloxycarbonyl, optionally substituted 5-10 membered heterocycloalkylcarbonyl, optionally substituted 5-10 membered heterocycloalkyloxycarbonyl, carbamoyl, optionally substituted C 1-12 Alkylcarbamoyl, optionally substituted C 1-12 Alkoxycarbamoyl, optionally substituted C 6-10 arylcarbamoyl, optionally substituted 5- to 10-membered heteroarylcarbamoyl, optionally substituted C 3-10 cycloalkylcarbamoyl, or optionally substituted 5- to 10-membered heterocycloalkylcarbamoyl, wherein the above groups of R1, R3, and R4 are optionally substituted with 1 to the maximum substitutable number of identical or different substituents selected from Substituent Group III; R 2A and R 2B each independently represents hydrogen, optionally substituted C 1-12 Alkyl, optionally substituted C 6-10 Aryl C 1-12 Alkyl, optionally substituted C 3-10 Cycloalkyl, optionally substituted 5- to 10-membered heterocycloalkyl, formyl, optionally substituted C 1-12 Alkylcarbonyl, optionally substituted C 1-12 Alkoxycarbonyl, optionally substituted C 6-10 Arylcarbonyl, optionally substituted C 6-10Aryloxycarbonyl, optionally substituted 5- to 10-membered heteroarylcarbonyl, optionally substituted 5- to 10-membered heteroaryloxycarbonyl, optionally substituted C 3-10 Cycloalkylcarbonyl, optionally substituted C 3-10 Cycloalkyloxycarbonyl, optionally substituted 5-10 membered heterocycloalkylcarbonyl, optionally substituted 5-10 membered heterocycloalkyloxycarbonyl, carbamoyl, optionally substituted C 1-12 Alkylcarbamoyl, optionally substituted C 1-12 Alkoxycarbamoyl, optionally substituted C 6-10 arylcarbamoyl, optionally substituted 5- to 10-membered heteroarylcarbamoyl, optionally substituted C 3-10 cycloalkylcarbamoyl, or optionally substituted 5- to 10-membered heterocycloalkylcarbamoyl, where R 2A and R 2B The above groups are optionally substituted with one to the maximum substitutable number of identical or different substituents selected from Substituent Group III, or R 2A and R 2B form a 5- to 6-membered non-aryl heterocycle together with the nitrogen atom to which they are bonded, and the non-aryl heterocycle is optionally substituted with one to the maximum possible number of identical or different substituents selected from Substituent Group V. In some cases, R 2A and R 2B each independently represents hydrogen, optionally substituted C 1-12 Alkyl, optionally substituted C 6-10 Aryl C 1-12 Alkyl, optionally substituted C 3-10 cycloalkyl, optionally substituted 5- to 10-membered heterocycloalkyl, or formyl, where R 2A and R 2B The above groups may be optionally substituted with one to the maximum substitutable number of the same or different substituents selected from Substituent Group III.

[0108] In one embodiment, R and, if present, R are each independently hydrogen, optionally substituted alkyl, optionally substituted arylalkyl, optionally substituted cycloalkyl, formyl, optionally substituted alkylcarbonyl, optionally substituted alkoxycarbonyl, optionally substituted arylcarbonyl, optionally substituted aryloxycarbonyl, optionally substituted cycloalkylcarbonyl, optionally substituted cycloalkyloxycarbonyl, optionally substituted heterocycloalkylcarbonyl, optionally substituted heterocycloalkyloxycarbonyl, carbamoyl, optionally substituted alkylcarbamoyl, optionally substituted alkoxycarbamoyl, optionally substituted arylcarbamoyl, optionally substituted heteroarylcarbamoyl, optionally substituted cycloalkylcarbamoyl, or optionally substituted heterocycloalkylcarbamoyl, wherein the groups of R and R are optionally substituted with 1 to the maximum possible number of identical or different substituents selected from Substituent Group III. Optionally, R1 and, if present, R4 are each independently hydrogen, optionally substituted alkyl, optionally substituted arylalkyl, optionally substituted cycloalkyl, or formyl, wherein the above groups of R1 and R4 are optionally substituted with 1 to the maximum possible number of identical or different substituents selected from Substituent Group III.

[0109] In one embodiment, R and, if present, R are each independently selected from hydrogen, optionally substituted C 1-12 Alkyl, optionally substituted C 6-10 Aryl C 1-12 Alkyl, optionally substituted C 3-10 Cycloalkyl, formyl, optionally substituted C 1-12 Alkylcarbonyl, optionally substituted C 1-12 Alkoxycarbonyl, optionally substituted C6-10 Arylcarbonyl, optionally substituted C 6-10 Aryloxycarbonyl, optionally substituted C 3-10 Cycloalkylcarbonyl, optionally substituted C 3-10 Cycloalkyloxycarbonyl, optionally substituted 5-10 membered heterocycloalkylcarbonyl, optionally substituted 5-10 membered heterocycloalkyloxycarbonyl, carbamoyl, optionally substituted C 1-12 Alkylcarbamoyl, optionally substituted C 1-12 Alkoxycarbamoyl, optionally substituted C 6-10 arylcarbamoyl, optionally substituted 5- to 10-membered heteroarylcarbamoyl, optionally substituted C 3-10 cycloalkylcarbamoyl, or optionally substituted 5- to 10-membered heterocycloalkylcarbamoyl, wherein the above groups of R1 and R4 are optionally substituted with 1 to the maximum substitutable number of identical or different substituents selected from Substituent Group III.

[0110] In one embodiment, R1 and, if present, R4 are each independently hydrogen, optionally substituted alkyl, optionally substituted arylalkyl, formyl, optionally substituted alkylcarbonyl, optionally substituted alkoxycarbonyl, optionally substituted arylcarbonyl, optionally substituted aryloxycarbonyl, or carbamoyl, optionally substituted alkylcarbamoyl, wherein the above groups of R1 and R4 are optionally substituted with 1 to the maximum possible number of identical or different substituents selected from Substituent Group III.

[0111] In one embodiment, R and, if present, R are each independently selected from hydrogen, optionally substituted C 1-12 Alkyl, optionally substituted C 6-10 Aryl C 1-12 Alkyl, formyl, optionally substituted C 1-12Alkylcarbonyl, optionally substituted C 1-12 Alkoxycarbonyl, optionally substituted C 6-10 Arylcarbonyl, optionally substituted C 6-10 Aryloxycarbonyl, or carbamoyl, optionally substituted C 1-12 alkylcarbamoyl, wherein the above groups of R1 and R4 are optionally substituted with one to the maximum possible number of identical or different substituents selected from Substituent Group III.

[0112] In one embodiment, R1 and, if present, R4 are each independently alkyl substituted with from one to the maximum number of the same or different substituents selected from the group consisting of hydrogen, alkyl, amino, substituted amino, substituted oxy, substituted carbonyl, cycloalkyl, and substituted cycloalkyl, arylalkyl substituted with from one to the maximum number of the same or different substituents selected from the group consisting of halogen, alkyl, substituted alkyl, hydroxy, substituted oxy, amino, substituted amino, and nitro, formyl, substituted carbonyl, or substituted oxycarbonyl, wherein the substituted amino, substituted oxy, substituted alkyl, substituted carbonyl, substituted cycloalkyl, substituted carbonyl, and substituted oxycarbonyl in R1 and R4 each independently have from one to the maximum number of the same or different substituents selected from Substituent Group IV.

[0113] In one embodiment, R and, if present, R are each independently hydrogen, C 1-12 Alkyl, amino, substituted amino, substituted oxy, substituted carbonyl, C 3-10 Cycloalkyl and substituted C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkyl 1-12 Alkyl, C 6-10 Aryl C 1-6 Alkyl, halogen, C 1-6C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkyl, substituted alkyl, hydroxy, substituted oxy, amino, substituted amino, and nitro 6-10 Aryl C 1-6 alkyl, formyl, substituted carbonyl, or substituted oxycarbonyl, wherein the substituted amino, substituted oxy, substituted alkyl, substituted carbonyl, substituted cycloalkyl, substituted carbonyl, and substituted oxycarbonyl in R1 and R4 each independently have from 1 to the maximum possible number of identical or different substituents selected from Substituent Group IV.

[0114] In one embodiment, R and R are each independently hydrogen, optionally substituted alkyl, optionally substituted arylalkyl, optionally substituted cycloalkyl, formyl, optionally substituted alkylcarbonyl, optionally substituted alkoxycarbonyl, optionally substituted arylcarbonyl, optionally substituted aryloxycarbonyl, optionally substituted cycloalkylcarbonyl, optionally substituted cycloalkyloxycarbonyl, optionally substituted heterocycloalkylcarbonyl, optionally substituted heterocycloalkyloxycarbonyl, carbamoyl, optionally substituted alkylcarbamoyl, optionally substituted alkoxycarbamoyl, optionally substituted arylcarbamoyl, optionally substituted heteroarylcarbamoyl, optionally substituted cycloalkylcarbamoyl, or optionally substituted heterocycloalkylcarbamoyl, wherein the groups of R and R are optionally substituted with 1 to the maximum possible number of the same or different substituents selected from Substituent Group III.

[0115] In one embodiment, and R are each independently hydrogen, optionally substituted C 1-12 Alkyl, optionally substituted C 6-10 Aryl C 1-12 Alkyl, optionally substituted C 3-10Cycloalkyl, formyl, optionally substituted C 1-12 Alkylcarbonyl, optionally substituted C 1-12 Alkoxycarbonyl, optionally substituted C 6-10 Arylcarbonyl, optionally substituted C 6-10 Aryloxycarbonyl, optionally substituted C 3-10 Cycloalkylcarbonyl, optionally substituted C 3-10 Cycloalkyloxycarbonyl, optionally substituted 5-10 membered heterocycloalkylcarbonyl, optionally substituted 5-10 membered heterocycloalkyloxycarbonyl, carbamoyl, optionally substituted C 1-12 Alkylcarbamoyl, optionally substituted C 1-12 Alkoxycarbamoyl, optionally substituted C 6-10 arylcarbamoyl, optionally substituted 5- to 10-membered heteroarylcarbamoyl, optionally substituted C 3-10 cycloalkylcarbamoyl, or optionally substituted 5- to 10-membered heterocycloalkylcarbamoyl, wherein the above groups of R1 and R3 may be optionally substituted with 1 to the maximum substitutable number of the same or different substituents selected from Substituent Group III.

[0116] In one embodiment, R1 and, if present, R4 are each independently hydrogen, alkyl substituted with from one to the maximum number of identical or different substituents selected from the group consisting of alkyl, amidinoamino, alkoxy, alkoxycarbonyl, carbamoyl, carboxy, hydroxy, trialkylsilyloxy, and cycloalkyl, arylalkyl substituted with from one to the maximum number of identical or different substituents selected from the group consisting of halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, amino, substituted amino, nitro, and hydroxy, formyl, alkylcarbonyl, arylalkylcarbonyl, arylalkyloxycarbonyl, alkoxycarbonyl, arylcarbonyl, aryloxycarbonyl, carbamoyl, alkylcarbamoyl, or arylalkylcarbamoyl, wherein the substituted aminos each independently have from one to the maximum number of identical or different substituents selected from Substituent Group IV.

[0117] In one embodiment, R and, if present, R are each independently hydrogen, C 1-12 Alkyl, amidinoamino, C 1-6 Alkoxy, C 1-6 Alkoxycarbonyl, carbamoyl, carboxy, hydroxy, triC 1-6 Alkylsilyloxy, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkyl 1-12 Alkyl, C 6-10 Aryl C 1-6 Alkyl, halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of haloalkoxy, amino, substituted amino, nitro, and hydroxy. 6-10 Aryl C 1-6 Alkyl, formyl, C 1-12 Alkyl carbonyl, C 6-10Aryl C 1-6 Alkyl carbonyl, C 6-10 Aryl C 1-6 Alkyloxycarbonyl, C 1-12 Alkoxycarbonyl, C 6-10 Arylcarbonyl, C 6-10 Aryloxycarbonyl, carbamoyl, C 1-12 Alkylcarbamoyl, or C 6-10 Aryl C 1-6 alkylcarbamoyl, wherein the substituted amino has one to the maximum possible number of identical or different substituents selected from Substituent Group IV.

[0118] In one embodiment, R1 and, if present, R4 are each independently selected from the group consisting of C 1-12 Alkyl, amidinoamino, C 1-6 Alkoxycarbonyl-substituted amidinoamino, C 1-6 Alkoxy, C 1-6 Alkoxycarbonyl, carbamoyl, carboxy, hydroxy, triC 1-6 Alkylsilyloxy, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkyl 1-12 Alkyl, C 6-10 Aryl C 1-6 Alkyl, or halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of haloalkoxy, amino, substituted amino, nitro, and hydroxy. 6-10 Aryl C 1-6 alkyl, wherein the substituted amino may have from one to the maximum possible number of identical or different substituents selected from Substituent Group IV.

[0119] In one embodiment, R3 is hydrogen, alkyl, formyl, substituted carbonyl, or alkyl, arylalkyl, arylalkyl, heteroarylalkyl, or substituted heteroarylalkyl, each substituted with from 1 to the maximum possible number of the same or different substituents selected from the group consisting of hydroxy, substituted oxy, substituted carbonyl, amino, substituted amino, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, and substituted heterocycloalkyl, wherein the substituted carbonyl, substituted oxy, substituted amino, substituted cycloalkyl, substituted heterocycloalkyl, substituted alkyl, and substituted heteroarylalkyl in R3 each independently optionally have from 1 to the maximum possible number of the same or different substituents selected from substituent group IV. Optionally, R3 is hydrogen, alkyl, or alkyl substituted with from 1 to the maximum possible number of the same or different substituents selected from the group consisting of hydroxy, substituted oxy, substituted carbonyl, amino, substituted amino, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, and substituted heterocycloalkyl, arylalkyl, halogen, nitro, hydroxy, substituted oxy, amino, substituted amino, alkyl, and substituted alkyl, arylalkyl, heteroarylalkyl, or substituted heteroarylalkyl substituted with from 1 to the maximum possible number of the same or different substituents selected from the group consisting of substituted oxy, substituted amino, substituted cycloalkyl, substituted heterocycloalkyl, substituted alkyl, and substituted heteroarylalkyl in R3 each independently optionally have from 1 to the maximum possible number of the same or different substituents selected from substituent group IV.

[0120] In one embodiment, R3 can be hydrogen, alkyl, formyl, alkylcarbonyl, arylalkylcarbonyl, or alkyl, arylalkyl, heteroarylalkyl, or alkoxycarbonyl-substituted heteroarylalkyl substituted with one to the maximum number of the same or different substituents selected from the group consisting of hydroxy, trialkylsilyloxy, alkoxy, alkoxycarbonyl, alkoxycarbonylamino, cycloalkyl, carboxy, amino, amidinoamino, alkoxycarbonyl-substituted amidinoamino, carbamoyl, and heterocycloalkyl. Optionally, R3 may be hydrogen, alkyl, or alkyl substituted with from one to the maximum number of identical or different substituents selected from the group consisting of hydroxy, trialkylsilyloxy, alkoxy, alkoxycarbonyl, alkoxycarbonylamino, cycloalkyl, carboxy, amino, amidinoamino, alkoxycarbonyl-substituted amidinoamino, carbamoyl, and heterocycloalkyl, arylalkyl, heteroarylalkyl, or alkoxycarbonyl-substituted heteroarylalkyl substituted with from one to the maximum number of identical or different substituents selected from the group consisting of halogen, nitro, hydroxy, amino, monoalkylamino, dialkylamino, alkyl, haloalkyl, alkoxy, haloalkoxy, carboxyalkylcarbonylamino, carbamoylalkylcarbonylamino, cycloalkylcarbonylamino, and cycloalkylalkylamino.

[0121] In one embodiment, R3 is hydrogen, C 1-12 Alkyl, formyl, C1-6 Alkyl carbonyl, C 6-10 Aryl C 1-6 Alkylcarbonyl, or hydroxy, triC 1-6 Alkylsilyloxy, C 1-6 Alkoxy, C 1-6 Alkoxycarbonyl, C 1-6 Alkoxycarbonylamino, C 3-6 Cycloalkyl, carboxy, amino, amidinoamino, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkoxycarbonyl-substituted amidinoamino, carbamoyl, and 5- to 6-membered heterocycloalkyl 1-12 Alkyl, C 6-10 Aryl C 1-6 Alkyl, halogen, nitro, hydroxy, amino, mono C 1-6 Alkylamino, DiC 1-6 Alkylamino, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, C 1-6 Haloalkoxy, Carboxy C 1-6 Alkylcarbonylamino, Carbamoyl C 1-6 Alkylcarbonylamino, C 3-6 cycloalkylcarbonylamino, and C 3-6 Cycloalkyl C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkylamino 6-10 Aryl C 1-12 Alkyl, 5-10 membered heteroarylC 1-6 Alkyl, or C 1-6 Alkoxycarbonyl-substituted 5- to 10-membered heteroaryl C 1-6 It may also be alkyl. Optionally, R3 is hydrogen, C 1-12 Alkyl, or hydroxy, triC 1-6 Alkylsilyloxy, C 1-6 Alkoxy, C 1-6 Alkoxycarbonyl, C 1-6 Alkoxycarbonylamino, C3-6 Cycloalkyl, carboxy, amino, amidinoamino, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkoxycarbonyl-substituted amidinoamino, carbamoyl, and 5- to 6-membered heterocycloalkyl 1-12 Alkyl, C 6-10 Aryl C 1-6 Alkyl, halogen, nitro, hydroxy, amino, mono C 1-6 Alkylamino, DiC 1-6 Alkylamino, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, C 1-6 Haloalkoxy, Carboxy C 1-6 Alkylcarbonylamino, Carbamoyl C 1-6 Alkylcarbonylamino, C 3-6 cycloalkylcarbonylamino, and C 3-6 Cycloalkyl C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkylamino 6-10 Aryl C 1-12 Alkyl, 5-10 membered heteroarylC 1-6 Alkyl, or C 1-6 Alkoxycarbonyl-substituted 5- to 10-membered heteroaryl C 1-6 It may also be alkyl.

[0122] In one embodiment, R3 is C 1-12 Alkyl, hydroxy, triC 1-6 Alkylsilyloxy, C 1-6 Alkoxy, C 1-6 Alkoxycarbonyl, C 1-6 Alkoxycarbonylamino, C 3-6 Cycloalkyl, carboxy, amino, amidinoamino, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkoxycarbonyl-substituted amidinoamino, carbamoyl, and 5- to 6-membered heterocycloalkyl1-12 Alkyl, C 6-10 Aryl C 1-6 Alkyl, or halogen, nitro, hydroxy, amino, mono C 1-6 Alkylamino, DiC 1-6 Alkylamino, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, C 1-6 Haloalkoxy, Carboxy C 1-6 Alkylcarbonylamino, Carbamoyl C 1-6 Alkylcarbonylamino, C 3-6 cycloalkylcarbonylamino, and C 3-6 Cycloalkyl C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkylamino 6-10 Aryl C 1-12 It may also be alkyl.

[0123] In one embodiment, R3 is alkyl, arylalkyl substituted with from 1 to the maximum possible number of the same or different substituents selected from the group consisting of hydrogen, alkyl, amino, substituted amino, carboxy, substituted oxycarbonyl, carbamoyl, substituted aminocarbonyl, hydroxy, substituted oxy, cycloalkyl, and substituted cycloalkyl, or arylalkyl substituted with from 1 to the maximum possible number of the same or different substituents selected from the group consisting of halogen, alkyl, substituted alkyl, carboxy, substituted oxycarbonyl, and hydroxy, and substituted oxy, wherein the substituted amino, substituted oxy, substituted oxycarbonyl, substituted aminocarbonyl, substituted alkyl, substituted cycloalkyl, substituted carbonyl, and substituted oxycarbonyl in R3 each independently have from 1 to the maximum possible number of the same or different substituents selected from Substituent Group IV.

[0124] In one embodiment, R3 is alkyl substituted with from one to the maximum number of identical or different substituents selected from the group consisting of hydrogen, alkyl, amidinoamino, alkoxycarbonyl, carbamoyl, carboxy, hydroxy, trialkylsilyloxy, amino, alkoxycarbonylamino, and cycloalkyl, arylalkyl, or arylalkyl substituted with from one to the maximum number of identical or different substituents selected from the group consisting of halogen, alkyl, alkoxycarbonyl, and hydroxy.

[0125] In one embodiment, R3 is hydrogen, C 1-12 Alkyl, amidinoamino, C 1-6 Alkoxycarbonyl, carbamoyl, carboxy, hydroxy, triC 1-6 Alkylsilyloxy, Amino, C 1-6 Alkoxycarbonylamino, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkyl 1-12 Alkyl, C 6-10 Aryl C 1-6 Alkyl, or halogen, C 1-6 Alkyl, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkoxycarbonyl and hydroxy 6-10 Aryl C 1-6 It is alkyl.

[0126] In one embodiment, R 2A and R 2Bare each independently an alkyl substituted with from one to the maximum number of identical or different substituents selected from the group consisting of hydrogen, alkyl, formyl, substituted carbonyl, hydroxy, substituted oxy, amino, substituted amino, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, and substituted heterocycloalkyl, an arylalkyl substituted with from one to the maximum number of identical or different substituents selected from the group consisting of halogen, alkyl, substituted alkyl, hydroxy, and substituted oxy, a heteroarylalkyl, a substituted heteroarylalkyl, a cycloalkyl, or a substituted cycloalkyl; 2A and R 2B The substituted carbonyl, substituted oxy, substituted amino, substituted cycloalkyl, substituted heterocycloalkyl, substituted heteroarylalkyl and substituted alkyl in each independently have from one to the maximum possible number of substituents selected from Substituent Group IV, which may be the same or different, or R 2A and R 2B together with the nitrogen atom to which they are attached form a non-aryl heterocycle, wherein the non-aryl heterocycle is optionally substituted with one or up to the maximum possible number of identical or different substituents selected from Substituent Group VI.

[0127] In one embodiment, R 2A and R 2B are each independently hydrogen, alkyl substituted with from one to the maximum number of identical or different substituents selected from the group consisting of alkyl, amidinoamino, alkoxy, alkoxycarbonyl, carbamoyl, carboxy, hydroxy, amino, alkoxycarbonylamino, cycloalkyl, and heterocycloalkyl, arylalkyl substituted with from one to the maximum number of identical or different substituents selected from the group consisting of halogen, alkyl, haloalkyl, alkoxy, and hydroxy, heteroarylalkyl, alkoxycarbonyl-substituted heteroarylalkyl, or cycloalkyl; or R 2A and R 2Bform a 5- to 6-membered non-aryl heterocycle together with the nitrogen atom to which they are bonded, wherein the non-aryl heterocycle is optionally substituted with one or up to the maximum possible number of identical or different substituents selected from Substituent Group VI.

[0128] In one embodiment, R 2A and R 2B are each independently hydrogen, C 1-12 Alkyl, amidinoamino, C 1-6 Alkoxy, C 1-6 Alkoxycarbonyl, carbamoyl, carboxy, hydroxy, amino, C 1-6 Alkoxycarbonylamino, C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkyl and 5- to 10-membered heterocycloalkyl 1-12 Alkyl, C 6-10 Aryl C 1-6 Alkyl, halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkoxy and hydroxy 6-10 Aryl C 1-6 Alkyl, 5-10 membered heteroarylC 1-6 Alkyl, C 1-6 Alkoxycarbonyl-substituted 5- to 10-membered heteroaryl C 1-6 Alkyl or C 3-10 cycloalkyl or R 2A and R 2B form a 5- to 6-membered non-aryl heterocycle together with the nitrogen atom to which they are bonded, wherein the non-aryl heterocycle is optionally substituted with one or up to the maximum possible number of identical or different substituents selected from Substituent Group VI.

[0129] In one embodiment, R 2A and R 2Bare each independently an alkyl substituted with from one to the maximum number of the same or different substituents selected from the group consisting of hydrogen, alkyl, formyl, substituted carbonyl, hydroxy, substituted oxy, substituted carbonyl, amino, substituted amino, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, and substituted heterocycloalkyl, an arylalkyl substituted with from one to the maximum number of the same or different substituents selected from the group consisting of halogen, nitro, hydroxy, substituted oxy, amino, substituted amino, alkyl, and substituted alkyl, a heteroarylalkyl, or a substituted heteroarylalkyl; 2A and R 2B The substituted carbonyl, substituted oxy, substituted amino, substituted cycloalkyl, substituted heterocycloalkyl, substituted alkyl, and substituted heteroarylalkyl in each independently have from one to the maximum possible number of substituents selected from Substituent Group IV, which may be the same or different, or R 2A and R 2B together with the nitrogen atom to which they are attached form a non-aryl heterocycle, wherein the non-aryl heterocycle is optionally substituted with one or up to the maximum possible number of identical or different substituents selected from Substituent Group VI. In some cases, R 2A and R 2B are each independently an alkyl, arylalkyl, substituted with from one to the maximum number of the same or different substituents selected from the group consisting of hydrogen, alkyl, hydroxy, substituted oxy, substituted carbonyl, amino, substituted amino, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, and substituted heterocycloalkyl, an arylalkyl, heteroarylalkyl, or substituted heteroarylalkyl, substituted with from one to the maximum number of the same or different substituents selected from the group consisting of halogen, nitro, hydroxy, substituted oxy, amino, substituted amino, alkyl, and substituted alkyl, wherein R 2A and R 2BThe substituted oxy, substituted amino, substituted cycloalkyl, substituted heterocycloalkyl, substituted alkyl, and substituted heteroarylalkyl in each independently have from one to the maximum possible number of identical or different substituents selected from Substituent Group IV, or R 2A and R 2B together with the nitrogen atom to which they are attached form a non-aryl heterocycle, wherein the non-aryl heterocycle is optionally substituted with one or up to the maximum possible number of identical or different substituents selected from Substituent Group VI.

[0130] In one embodiment, R 2A and R 2B are each independently an alkyl, arylalkyl, halogen, nitro, hydroxy, amino, monoalkylamino, dialkylamino, alkyl, haloalkyl, alkoxy, carboxyalkylcarbonylamino, carbamoylalkylcarbonylamino, cycloalkylcarbonyl-substituted amidinoamino, carbamoyl, and heterocycloalkyl, each substituted with from one to the maximum number of identical or different substituents selected from the group consisting of hydrogen, alkyl, formyl, alkylcarbonyl, arylalkylcarbonyl, hydroxy, trialkylsilyloxy, alkoxy, alkoxycarbonyl, alkoxycarbonylamino, cycloalkyl, carboxy, amino, amidinoamino, alkoxycarbonyl-substituted amidinoamino, carbamoyl, and heterocycloalkyl; or an arylalkyl, heteroarylalkyl, or alkoxycarbonyl-substituted heteroarylalkyl, each substituted with from one to the maximum number of identical or different substituents selected from the group consisting of hydrogen, alkyl, formyl, alkylcarbonyl, arylalkylcarbonyl, hydroxy, trialkylsilyloxy, alkoxy, alkoxycarbonyl, alkoxycarbonylamino, cycloalkyl, carboxy, amino, amidinoamino, alkoxycarbonyl-substituted amidinoamino, carbamoyl, and heterocycloalkyl; 2A and R 2B together with the nitrogen atom to which they are attached form a non-aryl heterocycle, wherein the non-aryl heterocycle is optionally substituted with one or up to the maximum possible number of identical or different substituents selected from Substituent Group VI. In some cases, R 2A and R 2Bare each independently hydrogen, alkyl, arylalkyl, halogen, nitro, hydroxy, amino, monoalkylamino, dialkylamino, alkyl, haloalkyl, alkoxy, carboxyalkylcarbonylamino, carbamoylalkylcarbonylamino, cycloalkylcarbonylamino, and cycloalkylalkylamino, each substituted with from one to the maximum number of identical or different substituents selected from the group consisting of alkyl, hydroxy, trialkylsilyloxy, alkoxy, alkoxycarbonylamino, cycloalkyl, carboxy, amino, amidinoamino, alkoxycarbonyl-substituted amidinoamino, and heterocycloalkyl; or R 2A and R 2B together with the nitrogen atom to which they are attached form a non-aryl heterocycle, wherein the non-aryl heterocycle is optionally substituted with one or up to the maximum possible number of identical or different substituents selected from Substituent Group VI.

[0131] In one embodiment, R 2A and R 2B are each independently hydrogen, C 1-12 Alkyl, formyl, C 1-6 Alkyl carbonyl, C 6-10 Aryl C 1-6 Alkylcarbonyl, hydroxy, triC 1-6 Alkylsilyloxy, C 1-6 Alkoxy, C 1-6 Alkoxycarbonyl, C 1-6 Alkoxycarbonylamino, C 3-10 Cycloalkyl, carboxy, amino, amidinoamino, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkoxycarbonyl-substituted amidinoamino, carbamoyl, and 5- to 6-membered heterocycloalkyl 1-12 Alkyl, C6-10 Aryl C 1-12 Alkyl, halogen, nitro, hydroxy, amino, mono C 1-6 Alkylamino, DiC 1-6 Alkylamino, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, Carboxy C 1-6 Alkylcarbonylamino, Carbamoyl C 1-6 Alkylcarbonylamino, C 3-6 cycloalkylcarbonylamino, and C 3-6 Cycloalkyl C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkylamino 6-10 Aryl C 1-12 Alkyl, 5-10 membered heteroarylC 1-12 Alkyl or C 1-6 Alkoxycarbonyl-substituted 5- to 10-membered heteroaryl C 1-12 alkyl or R 2A and R 2B together with the nitrogen atom to which they are attached form a 5-6 membered non-aryl heterocycle, wherein the non-aryl heterocycle is not substituted with halogen, nitro, hydroxy, amino, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, C 1-6 Alkoxycarbonyl, C 3-6 cycloalkylcarbonylamino, and C 3-6 Cycloalkyl C 1-6 It may be substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkylamino. In some cases, R 2A and R 2B are each independently hydrogen, C 1-12 Alkyl, hydroxy, triC 1-6 Alkylsilyloxy, C 1-6 Alkoxy, C 1-6 Alkoxycarbonylamino, C 3-10Cycloalkyl, carboxy, amino, amidinoamino, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkoxycarbonyl-substituted amidinoamino and 5- to 6-membered heterocycloalkyl 1-12 Alkyl, C 6-10 Aryl C 1-12 Alkyl, halogen, nitro, hydroxy, amino, mono C 1-6 Alkylamino, DiC 1-6 Alkylamino, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, Carboxy C 1-6 Alkylcarbonylamino, Carbamoyl C 1-6 Alkylcarbonylamino, C 3-6 cycloalkylcarbonylamino, and C 3-6 Cycloalkyl C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkylamino 6-10 Aryl C 1-12 Alkyl, 5-10 membered heteroarylC 1-12 Alkyl or C 1-6 Alkoxycarbonyl-substituted 5- to 10-membered heteroaryl C 1-12 alkyl or R 2A and R 2B together with the nitrogen atom to which they are attached form a 5-6 membered non-aryl heterocycle, wherein the non-aryl heterocycle is not substituted with halogen, nitro, hydroxy, amino, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, C 1-6 Alkoxycarbonyl, C 3-6 cycloalkylcarbonylamino, and C 3-6 Cycloalkyl C 1-6 It may be substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkylamino.

[0132] In one embodiment, R2A and R 2B are each independently hydrogen, C 1-12 Alkyl, hydroxy, triC 1-6 Alkylsilyloxy, C 1-6 Alkoxy, C 1-6 Alkoxycarbonyl, C 1-6 Alkoxycarbonylamino, C 3-10 Cycloalkyl, carboxy, amino, amidinoamino, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkoxycarbonyl-substituted amidinoamino, carbamoyl, and 5- to 6-membered heterocycloalkyl 1-12 Alkyl, C 6-10 Aryl C 1-12 Alkyl, halogen, nitro, hydroxy, amino, mono C 1-6 Alkylamino, DiC 1-6 Alkylamino, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, Carboxy C 1-6 Alkylcarbonylamino, Carbamoyl C 1-6 Alkylcarbonylamino, C 3-6 cycloalkylcarbonylamino, and C 3-6 Cycloalkyl C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkylamino 6-10 Aryl C 1-12 Alkyl, 5-10 membered heteroarylC 1-12 Alkyl or C 1-6 Alkoxycarbonyl-substituted 5- to 10-membered heteroaryl C 1-12 alkyl or R 2A and R 2B together with the nitrogen atom to which they are attached form a 5-6 membered non-aryl heterocycle, wherein the non-aryl heterocycle is not substituted with halogen, nitro, hydroxy, amino, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, C 1-6Alkoxycarbonyl, C 3-6 cycloalkylcarbonylamino, and C 3-6 Cycloalkyl C 1-6 It may be substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkylamino.

[0133] In one embodiment, R1 is alkyl; alkyl substituted with from one to the maximum number of identical or different substituents selected from the group consisting of amidinoamino, carbamoyl, carboxy, hydroxy, and cycloalkyl; arylalkyl; or arylalkyl substituted with from one to the maximum number of identical or different substituents selected from the group consisting of halogen, alkyl, haloalkyl, alkoxy, substituted amino, and hydroxy, wherein the substituted amino has from one to the maximum number of identical or different substituents selected from Substituent Group IV. Alternatively, R1 is alkyl; arylalkyl; or arylalkyl substituted with from one to the maximum number of identical or different substituents selected from the group consisting of halogen, alkyl, haloalkyl, alkoxy, substituted amino, and hydroxy, wherein the substituted amino has from one to the maximum number of identical or different substituents selected from Substituent Group IV.

[0134] In one embodiment, R is C 1-12 Alkyl; amidinoamino, carbamoyl, carboxy, hydroxy, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkyl 1-12 Alkyl; C 6-10 Aryl C 1-6 Alkyl; or halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkoxy, substituted amino, and hydroxy 6-10 Aryl C 1-6alkyl, wherein the substituted amino has from one to the maximum possible number of identical or different substituents selected from Substituent Group IV. 1-12 Alkyl; C 6-10 Aryl C 1-6 Alkyl; or halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkoxy, substituted amino, and hydroxy 6-10 Aryl C 1-6 alkyl, wherein the substituted amino has from 1 to the maximum possible number of identical or different substituents selected from Substituent Group IV.

[0135] In one embodiment, R 2A is hydrogen and R 2B is alkyl; alkyl substituted with from one to the maximum number of identical or different substituents selected from the group consisting of amidinoamino, carbamoyl, carboxy, hydroxy, and cycloalkyl; arylalkyl; arylalkyl substituted with from one to the maximum number of identical or different substituents selected from the group consisting of halogen, alkyl, haloalkyl, alkoxy, and hydroxy, or cycloalkyl. Alternatively, R 2A is hydrogen and R 2B is alkyl; arylalkyl; arylalkyl substituted with from one to the maximum possible number of identical or different substituents selected from the group consisting of halogen, alkyl, haloalkyl, alkoxy, and hydroxy, or cycloalkyl.

[0136] In one embodiment, R 2A is hydrogen and R 2B is C 1-12 Alkyl; amidinoamino, carbamoyl, carboxy, hydroxy, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkyl1-12 Alkyl; C 6-10 Aryl C 1-6 Alkyl; halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkoxy and hydroxy 6-10 Aryl C 1-6 Alkyl; or C 3-10 cycloalkyl; or R 2A is hydrogen and R 2B is C 1-12 Alkyl; C 6-10 Aryl C 1-6 Alkyl; halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkoxy and hydroxy 6-10 Aryl C 1-6 Alkyl; or C 3-10 It is cycloalkyl.

[0137] In one embodiment, R3 is alkyl; alkyl substituted with one to the maximum number of identical or different substituents selected from the group consisting of amidinoamino, carbamoyl, carboxy, hydroxy, and cycloalkyl; arylalkyl; or arylalkyl substituted with one to the maximum number of identical or different substituents selected from the group consisting of alkyl and hydroxy. Alternatively, R3 is alkyl or arylalkyl.

[0138] In one embodiment, R3 is C 1-12 Alkyl; amidinoamino, carbamoyl, carboxy, hydroxy, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkyl 1-12 Alkyl; C 6-10 Aryl C 1-6 Alkyl; or C1-6 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of alkyl and hydroxy 6-10 Aryl C 1-6 Alternatively, in one embodiment, R3 is C 1-12 Alkyl, or C 6-10 Aryl C 1-6 It is alkyl.

[0139] In one embodiment, R4 is hydrogen, alkyl, alkylcarbonyl, arylalkylcarbonyl, arylalkyloxycarbonyl, alkoxycarbonyl, carbamoyl, or arylalkylcarbamoyl.

[0140] In one embodiment, R4 is hydrogen, C 1-12 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl C 1-6 Alkyl carbonyl, C 6-10 Aryl C 1-6 Alkyloxycarbonyl, C 1-12 Alkoxycarbonyl, carbamoyl, or C 6-10 Aryl C 1-6 It is alkylcarbamoyl.

[0141] In one embodiment, R1 is hydrogen, methyl, ethyl, isobutyl, isopentyl, amidinoaminopropyl, tert-butoxyethyl, tert-butoxypropyl, (tert-butoxycarbonyl)ethyl, carbamoylmethyl, carboxyethyl, hydroxyethyl, hydroxypropyl, cyclopentylmethyl, cyclohexylmethyl, benzyl, phenylethyl, naphthalenylmethyl, fluorobenzyl, chlorobenzyl, dichlorobenzyl, methylbenzyl, tert-butylbenzyl, (trifluoromethyl) benzyl, methoxybenzyl, ethoxybenzyl, tert-butoxybenzyl, aminobenzyl, (cyclopentylcarbonylamino)benzyl, (cyclopentylmethylamino)benzyl, (dimethylamino)benzyl, (carbamoylethylcarbonylamino)benzyl, (carboxyethylcarbonylamino)benzyl, nitrobenzyl, hydroxybenzyl, 3-methylbutanoyl, isobutylcarbonyl, 2-phenylacetyl, isopropyloxycarbonyl, benzoyl, or phenyloxycarbonyl.

[0142] In another embodiment, R1 is methyl, n-propyl, isobutyl, isopentyl, amidinoaminopropyl, tert-butoxycarbonyl-substituted amidinoaminopropyl, tert-butoxyethyl, tert-butoxypropyl, (tert-butoxycarbonyl)ethyl, carboxyethyl, hydroxyethyl, hydroxypropyl, aminopropyl, 2-(tert-butyl-dimethylsilyloxy)ethyl, cyclopentylmethyl, cyclohexylmethyl, benzyl, phenylethyl, naphthalenylmethyl, fluorobenzyl, chlorobenzyl, dichlorobenzyl, methylbenzyl, (tert-butyl)benzyl, methoxybenzyl, ethoxybenzyl, (tert-butoxy)benzyl, (trifluoromethoxy)benzyl, (dimethylamino)benzyl, nitrobenzyl, or hydroxybenzyl.

[0143] In one embodiment, R 2A is hydrogen and R 2Bis methyl, isopropyl, isobutyl, n-pentyl, isopentyl, n-hexyl, heptyl, amidinoaminopropyl, tert-butoxyethyl, tert-butoxycarbonylmethyl, carbamoylmethyl, carbamoylethyl, carboxyethyl, hydroxyethyl, aminobutyl, ((tert-butoxycarbonyl)amino)butyl, cyclohexylmethyl, (tetrahydro-2H-pyran-2-yl)methyl, benzyl, phenylethyl, naphthalenylmethyl, naphthalenylethyl ethyl, fluorobenzyl, chlorobenzyl, dichlorobenzyl, (fluorophenyl)ethyl, methylbenzyl, (trifluoromethyl)benzyl, methoxybenzyl, tert-butoxybenzyl, hydroxybenzyl, α-hydroxymethylphenethyl, β-hydroxyphenethyl, pyridinylmethyl, (1H-indol-3-yl)ethyl, (1-(tert-butoxycarbonyl)-1H-indol-3-yl)ethyl, cyclopentyl, or cyclohexyl; or 2A and R 2B together with the nitrogen atom to which they are attached form a pyrrolidine or piperidine ring.

[0144] In one embodiment, R 2A and R 2Bare each independently isopropyl, isobutyl, sec-butyl, pentyl, isopentyl, n-hexyl, heptyl, amidinoaminopropyl, tert-butoxycarbonyl-substituted amidinoaminopropyl, tert-butoxyethyl, tert-butoxycarbonylmethyl, (tert-butoxycarbonyl)ethylcarbamoylethyl, carboxyethyl, hydroxyethyl, aminopropyl, aminobutyl, ((tert-butoxycarbonyl)amino)butyl, cyclopentylmethyl, cyclohexylmethyl, (1,2,3,4-tetrahydronaphthalenyl)methyl, ( (tetrahydro-2H-pyranyl)methyl, benzyl, phenylethyl, naphthalenylmethyl, (naphthalenyl)ethyl, β-hydroxyphenethyl, α-(hydroxymethyl)phenethyl, fluorobenzyl, chlorobenzyl, dichlorobenzyl, (fluorophenyl)ethyl, methylbenzyl, (trifluoromethyl)benzyl, methoxybenzyl, (tert-butoxy)benzyl, hydroxybenzyl, pyridinylmethyl, quinolinylethyl, (1-(tert-butoxycarbonyl)-1H-indolyl)ethyl, cyclopentyl, or cyclohexyl; or 2A and R 2B together with the nitrogen atom to which they are attached form a pyrrolidine or piperidine ring.

[0145] In one embodiment, R3 is n-propyl, isobutyl, isopentyl, amidinoaminopropyl, (methoxycarbonyl)ethyl, (tert-butoxycarbonyl)ethyl, carbamoylmethyl, carboxyethyl, hydroxymethyl, hydroxyethyl, (tert-butyldimethylsilyloxy)ethyl, aminobutyl, ((tert-butoxycarbonyl)amino)butyl, cyclohexylmethyl, cyclohexylethyl, benzyl, phenylethyl, phenylpropyl, phenylbutyl, naphthalenylmethyl, naphthalenylethyl, chlorobenzyl, methylbenzyl, (methylphenyl)ethyl, (isopropylphenyl)ethyl, or hydroxybenzyl.

[0146] In one embodiment, R3 is n-propyl, isobutyl, isopentyl, amidinoaminopropyl, tert-butoxycarbonyl-substituted amidinoaminopropyl, (methoxycarbonyl)ethyl, (tert-butoxycarbonyl)ethyl, carboxyethyl, hydroxyethyl, aminopropyl, (tert-butyldimethylsilyloxy)ethyl, ((tert-butoxycarbonyl)amino)butyl, cyclopentylmethyl, cyclohexylmethyl, cyclohexylethyl, benzyl, phenylethyl, phenylpropyl, phenylbutyl, naphthalenylmethyl, naphthalenylethyl, chlorobenzyl, methylbenzyl, (methylphenyl)ethyl, (isopropylphenyl)ethyl, (tert-butoxy)benzyl, or hydroxybenzyl.

[0147] In one embodiment, R4 is hydrogen, methyl, ethyl, isobutyl, formyl, acetyl, 3-methylbutanoyl, 2-phenylacetyl, methoxycarbonyl, ethoxycarbonyl, 2-methylpropyloxycarbonyl, tert-butoxycarbonyl, benzoyl, benzyl, benzyloxycarbonyl, aminocarbonyl, N-benzylaminocarbonyl, propylcarbamoyl, N-isobutylaminocarbonyl, or N-benzylaminocarbonyl.

[0148] Compounds of the present disclosure, in some embodiments, have the following formula IF: [ka] or an enantiomer thereof, or a salt thereof, or a solvate thereof. R1, R2, and R3 are each independently optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl, optionally substituted cycloalkylalkyl, or optionally substituted heterocycloalkylalkyl; R4 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocycloalkylalkyl, optionally substituted alkylcarbonyl, optionally substituted alkoxycarbonyl, optionally substituted arylcarbonyl, optionally substituted heteroarylcarbonyl, or optionally substituted carbamoyl.

[0149] In one embodiment, R1, R2, and R3 are each independently optionally substituted alkyl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl, or optionally substituted cycloalkylalkyl.

[0150] In one embodiment, R, R and R are each independently an optionally substituted C 1-6 Alkyl, optionally substituted C 6-10 Aryl C 1-6 Alkyl, optionally substituted 5-10 membered heteroarylC 1-6 Alkyl or optionally substituted C 3-6 Cycloalkyl C 1-6 It is alkyl.

[0151] In one embodiment, R1, R2, and R3 are each independently optionally substituted alkyl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl, or optionally substituted cycloalkylalkyl, and R4 is hydrogen, optionally substituted alkyl, optionally substituted alkylcarbonyl, optionally substituted arylcarbonyl, optionally substituted alkoxycarbonyl, or optionally substituted alkylcarbamoyl.

[0152] In one embodiment, R1, R2 and R3 are each independently selected from the group consisting of C1-6 Alkyl, hydroxy-substituted C 1-6 Alkyl, carbamoyl substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, amidinoamino substituted C 1-6 Alkyl, carboxy-substituted C 1-6 Alkyl, C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkoxycarbonyl-substituted 5- to 10-membered heteroaryl C 1-6 Alkyl, C 1-4 Alkyl-substituted C 6-10 Aryl C 1-6 Alkyl, hydroxy-substituted C 6-10 Aryl C 1-6 Alkyl, halogen-substituted C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkoxy-substituted C 6-10 Aryl C 1-6 Alkyl, (optionally substituted amino)-C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkoxycarbonyl-substituted C 1-6 Alkyl, C 1-4 Alkoxycarbonylamino-substituted C 1-6 Alkyl, 5-6 membered heterocycloalkyl substituted C 1-6 Alkyl, or C 3-6 Cycloalkyl C 1-6 It is alkyl.

[0153] In one embodiment, R1, R2 and R3 are each independently selected from the group consisting of C 1-6 Alkyl, hydroxy-substituted C 1-6 Alkyl, carbamoyl substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, amidinoamino substituted C 1-6 Alkyl, carboxy-substituted C 1-6 Alkyl, C 6-10 Aryl C 1-6 Alkyl, C 1-4Alkoxycarbonyl-substituted 5- to 10-membered heteroaryl C 1-6 Alkyl, C 1-4 Alkyl-substituted C 6-10 Aryl C 1-6 Alkyl, hydroxy-substituted C 6-10 Aryl C 1-6 Alkyl, halogen-substituted C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkoxy-substituted C 6-10 Aryl C 1-6 Alkyl, (optionally substituted amino)-C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkoxycarbonyl-substituted C 1-6 Alkyl, C 1-4 Alkoxycarbonylamino-substituted C 1-6 Alkyl, 5-6 membered heterocycloalkyl substituted C 1-6 Alkyl, or C 3-6 Cycloalkyl C 1-6 It is alkyl.

[0154] In one embodiment, R1, R2, and R3 are each independently alkyl or optionally substituted arylalkyl.

[0155] In one embodiment, R1, R2 and R3 are each independently selected from the group consisting of C 1-6 Alkyl or optionally substituted C 6-10 Aryl C 1-6 It is alkyl.

[0156] In one embodiment, R1, R2 and R3 are each independently selected from the group consisting of C 1-6 Alkyl, C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkyl-substituted C 6-10 Aryl C 1-6 Alkyl, halogen-substituted C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkoxy-substituted C 6-10Aryl C 1-6 Alkyl, or (optionally substituted amino)-C 6-10 Aryl C 1-6 It is alkyl.

[0157] In one embodiment, R1, R2 and R3 are each independently selected from the group consisting of C 1-6 Alkyl, C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkyl-substituted C 6-10 Aryl C 1-6 Alkyl, chloro-substituted C 6-10 Aryl C 1-6 Alkyl, C 1-4 Alkoxy-substituted C 6-10 Aryl C 1-6 Alkyl, or (optionally substituted amino)-C 6-10 Aryl C 1-6 It is alkyl.

[0158] In one embodiment, R is C 1-6 Alkyl or C6 arylC 1-4 alkyl, and R2 is C 1-6 Alkyl, or C 1-4 alkyl-substituted benzyl, and R3 is C 1-6 Alkyl or C6 arylC 1-4 It is alkyl.

[0159] In one embodiment, R1 and R3 are each independently alkyl or optionally substituted benzyl, and R2 is optionally substituted benzyl.

[0160] In one embodiment, R and R are each independently selected from the group consisting of C 1-6 Alkyl, benzyl, C 1-4 Alkyl-substituted benzyl, chloro-substituted benzyl, C 1-4 alkoxy-substituted benzyl or amino-substituted benzyl, and R2 is benzyl or chloro-substituted benzyl.

[0161] In one embodiment, R1 and R3 are each independently isobutyl, isopentyl, 4-(dimethylamino)benzyl, 4-methylbenzyl, 4-methoxybenzyl, 3-chlorobenzyl, 4-chlorobenzyl, or 3,4-dichlorobenzyl, and R2 is benzyl, 3-chlorobenzyl, or 3,4-dichlorobenzyl.

[0162] In one embodiment, R1 is isobutyl, benzyl, 4-(dimethylamino)benzyl, 4-methylbenzyl, 4-tert-butylbenzyl, 4-methoxybenzyl, 3-chlorobenzyl, 4-chlorobenzyl, or 3,4-dichlorobenzyl; R2 is isobutyl, benzyl, naphthalen-1-ylmethyl, 4-methylbenzyl, 4-chlorobenzyl, or 3,4-dichlorobenzyl; and R3 is isobutyl, isopentyl, or benzyl.

[0163] In one embodiment, R is C 1-6 Alkyl, hydroxy-substituted C 1-4 Alkyl, carbamoyl substituted C 1-4 Alkyl, amino substituted C 1-6 Alkyl, amidinoamino substituted C 1-4 Alkyl, carboxy-substituted C 1-4 Alkyl, C 1-4 Alkoxycarbonyl-substituted C 1-4 Alkyl, C 6-10 Aryl C 1-4 Alkyl, hydroxy-substituted C 6-10 Aryl C 1-4 Alkyl, C 1-4 Alkoxy-substituted C 6-10 Aryl C 1-4 Alkyl, halo-substituted C 6-10 Aryl C 1-4 Alkyl, or C 5-6 Cycloalkyl C 1-4 It is alkyl.

[0164] In one embodiment, R1 is methyl, isopropyl, isobutyl, isopentyl, n-hexyl, 3-amino-3-oxopropyl, 3-(tert-butoxy)-3-oxopropyl, benzyl, naphthalen-1-ylmethyl, 2-carboxyethyl, carbamoylmethyl, 3-(amidinoamino)propyl, 4-fluorobenzyl, 4-hydroxybenzyl, 4-(tert-butoxy)benzyl, 3,4-dichlorobenzyl, naphthalen-1-ylmethyl, phenethyl, hydroxymethyl, 2-hydroxyethyl, or cyclohexylmethyl.

[0165] In one embodiment, R1 is methyl, isopropyl, isobutyl, isopentyl, n-hexyl, 2-hydroxyethyl, carbamoylmethyl, 3-amino-3-oxopropyl, 3-(amidinoamino)propyl, 2-carboxyethyl, benzyl, phenethyl, naphthalen-1-ylmethyl, 4-hydroxybenzyl, 4-fluorobenzyl, 3,4-dichlorobenzyl, 4-(tert-butoxy)benzyl, 3-(tert-butoxy)-3-oxopropyl, hydroxymethyl, cyclohexylmethyl, or [ka] is.

[0166] In one embodiment, R1 is methyl, isobutyl, isopentyl, 3-(tert-butoxy)-3-oxopropyl, benzyl, naphthalen-1-ylmethyl, 4-hydroxybenzyl, 4-(tert-butoxy)benzyl, 3,4-dichlorobenzyl, or cyclohexylmethyl.

[0167] In one embodiment, R1 is isopropyl, isobutyl, isopentyl, n-hexyl, cyclohexylmethyl, benzyl, phenethyl, naphthalen-1-ylmethyl, 4-hydroxybenzyl, 4-fluorobenzyl, 2-carboxyethyl, carbamoylmethyl, carbamoylethyl, 3-(amidinoamino)propyl, hydroxymethyl, or hydroxyethyl.

[0168] In one embodiment, R1 is isobutyl, isopentyl, cyclohexylmethyl, benzyl, phenethyl, naphthalen-1-ylmethyl, 4-hydroxybenzyl, 4-fluorobenzyl, 2-carboxyethyl, carbamoylmethyl, 3-(amidinoamino)propyl, or hydroxyethyl.

[0169] In one embodiment, R1 is isobutyl, benzyl, 4-hydroxybenzyl, 2-carboxyethyl, 3-(amidinoamino)propyl, or naphthalen-1-ylmethyl.

[0170] In one embodiment, R1 is isobutyl, 3-(amidinoamino)propyl, 2-carboxyethyl, benzyl, naphthalen-1-ylmethyl, 4-hydroxybenzyl, 4-(tert-butoxy)benzyl, 3-(tert-butoxy)-3-oxopropyl, or [ka] is.

[0171] In one embodiment, R1 is isobutyl, 3-hydroxypropyl, 3-amino-3-oxopropyl, 6-aminohexyl, 2-carboxyethyl, benzyl, naphthalen-1-ylmethyl, 4-hydroxybenzyl, or cyclohexylmethyl.

[0172] In one embodiment, R2 is C 1-4 Alkyl, hydroxy-substituted C 1-4 Alkyl, carbamoyl substituted C 1-4 Alkyl, amino substituted C 1-4 Alkyl, amidinoamino substituted C 1-4 Alkyl, carboxy-substituted C 1-4 Alkyl, C 6-10 Aryl C 1-4 Alkyl, C 1-4Alkoxycarbonyl-substituted 5- to 10-membered heteroaryl C 1-4 Alkyl, C 1-4 Alkyl-substituted C 6-10 Aryl C 1-4 Alkyl, hydroxy-substituted C 6-10 Aryl C 1-4 Alkyl, halogen-substituted C 6-10 Aryl C 1-4 Alkyl, C 1-4 Alkoxy-substituted C 6-10 Aryl C 1-4 Alkyl, C 1-4 Alkoxycarbonyl-substituted C 1-4 Alkyl, C 1-4 Alkoxycarbonylamino-substituted C 1-4 Alkyl, 5-6 membered heterocycloalkyl substituted C 1-4 Alkyl, or C 5-6 Cycloalkyl C 1-4 It is alkyl.

[0173] In one embodiment, R2 is naphthalen-1-ylmethyl or optionally substituted benzyl.

[0174] In one embodiment, R2 is isopropyl, 1-methylpropyl, isobutyl, isopentyl, n-hexyl, hydroxymethyl, 2-hydroxyethyl, carbamoylmethyl, 3-amino-3-oxopropyl, 3-(amidinoamino)propyl, 4-aminobutyl, 2-carboxyethyl, benzyl, phenethyl, naphthalen-1-ylmethyl, 2-(naphthalen-1-yl)ethyl, 2-(1-(tert-butoxycarbonyl)-1H -indol-3-yl)ethyl, 3-methylbenzyl, 4-methylbenzyl, 4-hydroxybenzyl, 4-fluorobenzyl, 3-chlorobenzyl, 4-chlorobenzyl, 3,4-dichlorobenzyl, 4-(tert-butoxy)benzyl, 2-(tert-butoxy)-2-oxoethyl, 4-((tert-butoxycarbonyl)amino)butyl, (tetrahydro-2H-pyran-2-yl)methyl, or cyclohexylmethyl.

[0175] In one embodiment, R2 is isopropyl, 1-methylpropyl, isobutyl, isopentyl, n-hexyl, hydroxymethyl, 2-hydroxyethyl, carbamoylmethyl, 3-amino-3-oxopropyl, 4-aminobutyl, 3-(amidinoamino)propyl, 2-carboxyethyl, benzyl, phenethyl, naphthalen-1-ylmethyl, 2-(naphthalen-1-yl)ethyl, 2-(1-(tert-butoxycarbonyl)-1H-indol-3-yl)methyl ... )ethyl, 3-methylbenzyl, 4-methylbenzyl, 4-hydroxybenzyl, 4-fluorobenzyl, 3-chlorobenzyl, 4-chlorobenzyl, 3,4-dichlorobenzyl, 4-(tert-butoxy)benzyl, 2-(tert-butoxy)-2-oxoethyl, 3-(tert-butoxy)-3-oxopropyl, 4-((tert-butoxycarbonyl)amino)butyl, (tetrahydro-2H-pyran-2-yl)methyl, cyclohexylmethyl, or [ka] is.

[0176] In one embodiment, R2 is isobutyl, 2-hydroxyethyl, 3-amino-3-oxopropyl, 4-aminobutyl, 2-carboxyethyl, benzyl, phenethyl, naphthalen-1-ylmethyl, 2-(naphthalen-1-yl)ethyl, 2-(1-(tert-butoxycarbonyl)-1H-indol-3-yl)ethyl, 3-methylbenzyl, 4-methylbenzyl, 4-hydroxybenzyl, 3-chlorobenzyl, 4-chlorobenzyl, 3,4-dichlorobenzyl, 4-(tert-butoxy)benzyl, 2-(tert-butoxy)-2-oxoethyl, 4-((tert-butoxycarbonyl)amino)butyl, (tetrahydro-2H-pyran-2-yl)methyl, or cyclohexylmethyl.

[0177] In one embodiment, R2 is 1-methylpropyl, isopropyl, isobutyl, isopentyl, n-hexyl, benzyl, 4-hydroxybenzyl, 4-fluorobenzyl, 2-carboxyethyl, carbamoylmethyl, carbamoylethyl, 3-(amidinoamino)propyl, hydroxymethyl, 2-hydroxyethyl, phenethyl, naphthalen-1-ylmethyl, or cyclohexylmethyl.

[0178] In one embodiment, R2 is isopropyl, 1-methylpropyl, isobutyl, 3-(amidinoamino)propyl, 2-carboxyethyl, benzyl, naphthalen-1-ylmethyl, 4-hydroxybenzyl, 4-(tert-butoxy)benzyl, 3-(tert-butoxy)-3-oxopropyl, or [ka] is.

[0179] In one embodiment, R2 is isopropyl, isobutyl, isopentyl, benzyl, 4-hydroxybenzyl, 4-fluorobenzyl, 2-carboxyethyl, carbamoylmethyl, 3-(amidinoamino)propyl, hydroxyethyl, phenethyl, naphthalen-1-ylmethyl, or n-hexyl.

[0180] In one embodiment, R2 is isobutyl, 2-hydroxyethyl, 3-amino-3-oxopropyl, 4-aminobutyl, 2-carboxyethyl, benzyl, phenethyl, naphthalen-1-ylmethyl, 3-methylbenzyl, 4-methylbenzyl, 4-hydroxybenzyl, cyclohexylmethyl, or 2-(1H-indol-3-yl)ethyl.

[0181] In one embodiment, R2 is 1-methylpropyl, isopropyl, isobutyl, benzyl, 4-hydroxybenzyl, 2-carboxyethyl, 3-(amidinoamino)propyl, or naphthalen-1-ylmethyl.

[0182] In one embodiment, R3 is C 1-4 Alkyl, hydroxy-substituted C 1-4 Alkyl, carbamoyl substituted C 1-4 Alkyl, C 1-4 Alkoxycarbonyl-substituted C 1-4 Alkyl, amino substituted C 1-4 Alkyl, amidinoamino substituted C 1-4 Alkyl, carboxy-substituted C 1-4 Alkyl, C 6-10 Aryl C 1-4 Alkyl, C 1-4 Alkyl-substituted C 6-10 Aryl C 1-4 Alkyl, hydroxy-substituted C 6-10 Aryl C 1-4 Alkyl, or C 5-6 Cycloalkyl C 1-4 It is alkyl.

[0183] In one embodiment, R3 is isopropyl, isobutyl, isopentyl, n-hexyl, 3-amino-3-oxopropyl, 3-methoxy-3-oxopropyl, 4-aminobutyl, 2-carboxyethyl, carbamoylmethyl, 3-(amidinoamino)propyl, benzyl, naphthalen-1-ylmethyl, phenethyl, hydroxymethyl, 2-hydroxyethyl, 4-fluorobenzyl, 3-methylbenzyl, 4-methylbenzyl, 4-hydroxybenzyl, 4-((tert-butoxycarbonyl)amino)butyl, or cyclohexylmethyl.

[0184] In one embodiment, R3 is isopropyl, isobutyl, isopentyl, n-hexyl, hydroxymethyl, 2-hydroxyethyl, carbamoylmethyl, 3-amino-3-oxopropyl, 4-aminobutyl, 3-(amidinoamino)propyl, 2-carboxyethyl, benzyl, phenethyl, naphthalen-1-ylmethyl, 3-methylbenzyl, 4-methylbenzyl, 4-hydroxybenzyl, 4-fluorobenzyl, 4-(tert-butoxy)benzyl, 3-methoxy-3-oxopropyl, 3-(tert-butoxy)-3-oxopropyl, 4-((tert-butoxycarbonyl)amino)butyl, cyclohexylmethyl, or [ka] is.

[0185] In one embodiment, R3 is isobutyl, isopentyl, 3-amino-3-oxopropyl, 3-methoxy-3-oxopropyl, 4-aminobutyl, 2-carboxyethyl, benzyl, phenethyl, 3-methylbenzyl, 4-methylbenzyl, 4-hydroxybenzyl, 4-((tert-butoxycarbonyl)amino)butyl, or cyclohexylmethyl.

[0186] In one embodiment, R3 is isopropyl, isobutyl, isopentyl, n-hexyl, cyclohexylmethyl, benzyl, phenethyl, naphthalen-1-ylmethyl, 4-hydroxybenzyl, 4-fluorobenzyl, 2-carboxyethyl, carbamoylmethyl, carbamoylethyl, 3-(amidinoamino)propyl, hydroxymethyl, or hydroxyethyl.

[0187] In one embodiment, R3 is isobutyl, isopentyl, benzyl, phenethyl, 4-hydroxybenzyl, 2-carboxyethyl, carbamoylmethyl, 3-(amidinoamino)propyl, hydroxymethyl, or naphthalen-1-ylmethyl.

[0188] In one embodiment, R3 is isobutyl, benzyl, 4-hydroxybenzyl, 2-carboxyethyl, 3-(amidinoamino)propyl, or naphthalen-1-ylmethyl.

[0189] In one embodiment, R3 is isobutyl, 2-carboxyethyl, 3-(amidinoamino)propyl, benzyl, naphthalen-1-ylmethyl, 4-hydroxybenzyl, 4-(tert-butoxy)benzyl, 3-(tert-butoxy)-3-oxopropyl, or [ka] is.

[0190] In one embodiment, R3 is isobutyl, hydroxymethyl, 3-amino-3-oxopropyl, 4-aminobutyl, 2-carboxyethyl, benzyl, 2-naphthylmethyl, 4-hydroxybenzyl, or cyclohexylmethyl.

[0191] In one embodiment, R is C 1-6 Alkyl or C 6-10 Aryl C 1-6 alkyl, and R2 and R3 are each independently C 1-6 Alkyl or optionally substituted C 6-10 Aryl C 1-6 It is alkyl.

[0192] In one embodiment, R1 is isobutyl, isopentyl or benzyl, R2 is isobutyl, benzyl, phenethyl, 3-methylbenzyl, 4-methylbenzyl or 3,4-dichlorobenzyl, and R3 is isobutyl, benzyl, phenethyl, 3-methylbenzyl or 4-methylbenzyl.

[0193] In one embodiment, R1 is isobutyl, R2 is benzyl, and R3 is benzyl.

[0194] In one embodiment, R1 is benzyl, R2 is benzyl, and R3 is isobutyl.

[0195] In one embodiment, R1 is isobutyl, R2 is benzyl, and R3 is 3-methylbenzyl.

[0196] In one embodiment, R1 is benzyl, R2 is 3,4-dichlorobenzyl, and R3 is isobutyl.

[0197] In one embodiment, R1 is isobutyl, R2 is 4-methylbenzyl, and R3 is benzyl.

[0198] In one embodiment, R1 is benzyl, R2 is isobutyl, and R3 is isobutyl.

[0199] In one embodiment, R4 is hydrogen, optionally substituted alkyl, optionally substituted alkylcarbonyl, optionally substituted arylcarbonyl, or optionally substituted alkoxycarbonyl.

[0200] In one embodiment, R4 is hydrogen, optionally substituted C 1-6 Alkyl, optionally substituted C 1-6 Alkylcarbonyl, optionally substituted C 6-10 Arylcarbonyl, optionally substituted C 1-6 Alkoxycarbonyl or optionally substituted C 1-6 It is alkylcarbamoyl.

[0201] In one embodiment, R4 is hydrogen, optionally substituted C 1-6 Alkyl, optionally substituted C 1-6 Alkylcarbonyl, optionally substituted C 6-10 arylcarbonyl, or optionally substituted C 1-6 It is an alkoxycarbonyl.

[0202] In one embodiment, R4 is hydrogen, C 1-6 Alkyl, C 1-6 Alkyl carbonyl, C 6-10 Arylcarbonyl, C 1-6 Alkoxycarbonyl, or C 1-6 It is alkylcarbamoyl.

[0203] In one embodiment, R4 is hydrogen, C 1-6 Alkyl, C 1-6 Alkyl carbonyl, C 6-10 Arylcarbonyl, or C 1-6 It is an alkoxycarbonyl.

[0204] In one embodiment, R4 is hydrogen, C 1-4 Alkyl, C 1-4 Alkylcarbonyl, C6 arylcarbonyl, C 1-4 Alkoxycarbonyl, or C 1-4 It is alkylcarbamoyl.

[0205] In one embodiment, R4 is hydrogen, C 1-4 Alkyl, C 1-4 Alkylcarbonyl, C6 arylcarbonyl, or C 1-4 It is an alkoxycarbonyl.

[0206] In one embodiment, R4 is hydrogen or alkyl.

[0207] In one embodiment, R4 is hydrogen or C 1-6 It is alkyl.

[0208] In one embodiment, R4 is hydrogen, methyl, ethyl, acetyl, benzoyl, methoxycarbonyl, tert-butoxycarbonyl, or propylcarbamoyl.

[0209] In one embodiment, R4 is hydrogen, methyl, ethyl, acetyl, benzoyl, methoxycarbonyl, or tert-butoxycarbonyl.

[0210] In one embodiment, R4 is hydrogen or ethyl. In a preferred embodiment, R4 is hydrogen.

[0211] When hydroxyl, amino, and / or carboxyl groups are present in R1, R2, R3, and / or R4, they may be independently protected with protecting groups, and such compounds are also within the scope of the present disclosure.

[0212] Compounds of the present disclosure, in some embodiments, have the following formula IB: [ka] or an enantiomer thereof, or a salt thereof, or a solvate thereof. In formula IB, R1, R2 and R3 are defined as in formula IF.

[0213] Compounds of the present disclosure, in some embodiments, have the following formula IIF: [ka] or an enantiomer thereof, or a salt thereof, or a solvate thereof. In formula IIF, R1, R2 and R3 are defined as in formula IF.

[0214] Compounds of the present disclosure, in some embodiments, have the following formula IIB: [ka] or an enantiomer thereof, or a salt thereof, or a solvate thereof. In formula IIB, R1, R2 and R3 are defined as in formula IF.

[0215] The compounds of the present disclosure are further described below. The compounds of the present disclosure may exist as stereoisomers such as tautomers and geometric isomers, and optical isomers, depending on the types of substituents, and the present disclosure also includes these. That is, when the compounds of the present disclosure have one or more asymmetric carbon atoms, diastereomers and optical isomers exist, and mixtures and isolated forms of these diastereomers and optical isomers are also included in the compounds of the present disclosure.

[0216] The present disclosure is also intended to encompass various hydrates, solvates and crystalline polymorphs.

[0217] Additionally, compounds of the present disclosure may contain isotopes (e.g., 2 H (or D), 3 H (or T), 11 C. 13 C. 14 C. 13 N, 15 N, 15 O. 35 S, 18 F, 125 I, etc.), and these compounds are also included in the compounds of the present disclosure.

[0218] Furthermore, prodrugs of the compounds of the present disclosure are also included within the scope of the present disclosure. In the present disclosure, prodrugs refer to derivatives that are hydrolyzed in vivo by acid hydrolysis or enzymatically to give compounds represented by the formulae IF, IB, IIF, IIB, XXIF, XXIB, XXIIF, or XXIIB, and related structural formulae thereof. For example, when the compounds represented by the formulae IF, IB, IIF, IIB, XXIF, XXIB, XXIIF, or XXIIB, and related structural formulae thereof, have functional groups such as hydroxyl groups, amino groups, or carboxyl groups or other substituents, prodrugs can be produced by modifying these groups according to conventional methods. Prodrug technology is described, for example, in C.G. Wermuth, "The Practice of Medicinal Chemistry," 4 th Ed., Academic Press, (2015), Chapter 28.

[0219] For example, in the case of a compound having a carboxyl group, the carboxyl group may be replaced by an alkoxycarbonyl group, an alkylthiocarbonyl group, or an alkylaminocarbonyl group.

[0220] Furthermore, for example, in the case of a compound having an amino group, examples include a compound in which the amino group is substituted with an alkanoyl group to become an alkanoylamino group, a compound in which the amino group is substituted with an alkoxycarbonyl group to become an alkoxycarbonylamino group, a compound in which the amino group is substituted with an alkoxycarbonylamino group, a compound in which the amino group is substituted with an alkanoyloxymethylamino group, or a compound in which the amino group is hydroxylamine.

[0221] Further, for example, in the case of a compound having a hydroxyl group, examples include a compound in which the hydroxyl group is substituted with the above-mentioned alkanoyl group to form an alkanoyloxy group, a compound which is a phosphate ester, or a compound which is an alkanoyloxymethyloxy group.

[0222] The alkyl moiety of the group used for making these prodrugs includes the above-mentioned alkyl groups, and the alkyl group may be substituted with, for example, an alkoxy group, etc. Preferred examples include the following:

[0223] For example, examples of compounds in which a carboxyl group is an alkoxycarbonyl group include alkoxycarbonyl such as methoxycarbonyl or ethoxycarbonyl, and alkoxycarbonyl substituted with an alkoxy group such as methoxymethoxycarbonyl, ethoxymethoxycarbonyl, 2-methoxyethoxycarbonyl, 2-methoxyethoxymethoxycarbonyl, or pivaloyloxymethoxycarbonyl.

[0224] As used herein, the term "pharmaceutically acceptable salt" refers to an acid addition salt and a base addition salt that are acceptable for pharmaceutically use. Specific examples of "pharmaceutically acceptable salts" include acetate, propionate, butyrate, formate, trifluoroacetate, maleate, fumarate, tartrate, citrate, stearate, succinate, ethylsuccinate, malonate, lactobionate, gluconate, glucoheptonate, benzoate, methanesulfonate, benzenesulfonate, paratoluenesulfonate (tosylate), lauryl sulfate, malate, ascorbate, mandelate, saccharate, xinafoate, pamoate, ketone ... Examples of acid addition salts include arsenate, adipate, cysteine ​​salt, N-acetylcysteine ​​salt, hydrochloride, hydrobromide, phosphate, sulfate, hydroiodide, nicotinate, oxalate, picrate, thiocyanate, undecanoate, acrylic acid polymer salt, and carboxyvinyl polymer salt; inorganic base addition salts such as lithium salt, sodium salt, potassium salt, and calcium salt; organic base addition salts such as morpholine and piperidine; and addition salts with amino acids such as aspartic acid and glutamic acid, but are not limited to these.

[0225] In one embodiment, the compounds of the present disclosure can be administered orally or parenterally, either directly or in the form of a formulation, medicament, or pharmaceutical composition using an appropriate dosage form. Specific examples of these dosage forms include, but are not limited to, tablets, capsules, powders, granules, liquids, suspensions, injections, patches, and poultices. These formulations can be manufactured by known methods using additives commonly used as pharmaceutical additives.

[0226] Depending on the purpose, these additives may include excipients, disintegrants, binders, fluidizing agents, lubricants, coating agents, solubilizers, solubilizers, thickeners, dispersants, stabilizers, sweeteners, flavors, etc. Specific examples of these additives include, but are not limited to, lactose, mannitol, crystalline cellulose, low-substituted hydroxypropyl cellulose, corn starch, partially pregelatinized starch, carmellose calcium, croscarmellose sodium, hydroxypropyl cellulose, hydroxypropyl methylcellulose, polyvinyl alcohol, magnesium stearate, sodium stearyl fumarate, polyethylene glycol, propylene glycol, titanium oxide, talc, etc.

[0227] The dosage of the compound of the present disclosure is appropriately selected depending on the subject to be administered, the administration route, the disease, the age, weight and symptoms of the subject.For example, in the case of oral administration, the lower limit is 0.01 mg (preferably 100 mg) and the upper limit is 10,000 mg (preferably 6,000 mg) per day for an adult, and this amount can be administered once a day or in divided doses.

[0228] In one embodiment, the compound of the present disclosure has antiviral activity against viruses of the genus Lyssavirus, including rabies virus, Lagos bat virus, Mokola virus, Duvenhage virus, European bat lyssavirus 1, European bat lyssavirus 2, and Australian bat lyssavirus, and preferably includes rabies virus.

[0229] In one embodiment, the compounds of the present disclosure are compounds capable of inhibiting or killing tumors or cancers. The tumor or cancer can be any of carcinomas, lymphomas, blastomas, sarcomas, and leukemias, including lung cancers such as squamous cell carcinoma, small cell lung cancer, non-small cell lung cancer, and lung adenocarcinoma, squamous cell carcinoma of the lung, peritoneal cancer, hepatocellular carcinoma, esophageal cancer, gastrointestinal cancer, pancreatic cancer, glioblastoma, uterine cancer such as cervical cancer, ovarian cancer, liver cancer, hepatocellular carcinoma, bladder cancer, hepatoma, breast cancer, colon cancer, colorectal cancer, epithelial or uterine carcinoma, salivary gland carcinoma, kidney cancer, liver cancer, prostate cancer, vulvar cancer, thyroid cancer, liver carcinoma, and various types of head and neck cancer, blood cancer (leukemia), prostate cancer, gastric cancer, fibroid cancer, glioma, melanoma, and the like.

[0230] The administration timing of the compounds of the present disclosure and the therapeutic agents thereof is not limited, and they may be administered to the subject simultaneously or at different times. The compounds of the present disclosure and the therapeutic agents may also be combined. The dosage of the therapeutic agents may be appropriately selected based on the clinically used dose. The compounding ratio of the compounds of the present disclosure and the therapeutic agents may be appropriately selected depending on the subject to be administered, the administration route, the target disease, symptoms, the combination, etc.

[0231] In one embodiment of the present disclosure, when using a pharmaceutical composition, the compounds of the present disclosure can be administered in combination at the same time or at different times. Such pharmaceutical compositions are also within the scope of the present disclosure.

[0232] Such medicines, formulations, and pharmaceutical compositions can be manufactured using any technique known in the art by mixing the compounds of the present disclosure and / or additional drugs (e.g., antirabies gamma globulin preparations, antibacterial agents, antiviral agents (e.g., ribavirin, amantadine, etc.), sedatives (e.g., ketamine, midazolam, etc.), etc.) together or separately, as a combination drug or as separate drugs, with any appropriate ingredients, and can be formulated using any technique known in the art into appropriate preparations, such as tablets, capsules, powders, granules, liquids, suspensions, injections, patches, and poultices. When the compound of the present disclosure and / or the additional drug (e.g., an antirabies gamma globulin preparation, an antibacterial agent, an antiviral agent (e.g., ribavirin, amantadine, etc.), a sedative (e.g., ketamine, midazolam, etc.), etc.) are prepared as separate drugs, they may be provided as a kit of two drugs, or one component may be provided as a single drug along with instructions (such as a package insert) instructing that the other component (which is an additional drug in the case of the compound of the present disclosure, and a compound of the present disclosure in the case of the additional drug (e.g., an antirabies gamma globulin preparation, an antibacterial agent, an antiviral agent (e.g., ribavirin, amantadine, etc.), a sedative (e.g., ketamine, midazolam, etc.), etc.)) be administered in combination at the same time or at different times.

[0233] When the compounds of the present disclosure are used as active ingredients in medicines, they are not intended for use only in humans, but can also be used in other animals other than humans (cats, dogs, cows, horses, bats, foxes, mongooses, raccoons, etc.).

[0234] (Methods for producing compounds of the present disclosure) Examples of methods for producing the compounds of the present disclosure will be described below, but the present disclosure is not limited to these.

[0235] The compounds of the present disclosure can be produced, for example, by the production methods described below, but are not limited thereto. These production methods can be appropriately improved based on the knowledge of those skilled in organic synthetic chemistry. In the production methods described below, the compounds used as raw materials may be used in the form of salts thereof, as long as they do not interfere with the reaction.

[0236] In the following production methods, even if the use of a protecting group is not specifically specified, if any functional group other than the reactive site is changed under the reaction conditions or if it is not suitable for post-reaction treatment, the target compound can be obtained by protecting the site other than the reactive site as necessary and deprotecting it after the reaction or a series of reactions. Protecting groups used in these processes include those described in the literature (Peter GM Wuts, "Greene's Protective Groups in Organic Synthesis", 5 th Ed., John Wiley & Sons, Inc., Hoboken, New Jersey (2014)) can be used. Introduction and removal of the protecting group can be carried out by a method commonly used in organic synthetic chemistry (for example, the methods described in the above-mentioned documents) or a method similar thereto.

[0237] The starting materials and intermediates in the following production methods are commercially available or can be obtained by synthesis from known compounds according to known methods or methods described in known literature. Furthermore, salts of these starting materials and intermediates may be used as long as they do not interfere with the reaction.

[0238] The intermediates and target compounds in the following production methods can also be converted into other compounds included in the present disclosure by appropriately converting their functional groups. The conversion of functional groups in this case can be carried out by a method commonly used in organic synthetic chemistry (for example, RC Larock, "Comprehensive Organic Transformations", 2 ndEd., John Wiley and Sons, Inc., New York (1999), or a method similar thereto.

[0239] In the following production methods, an inert solvent means a solvent that does not react with the raw materials, reagents, bases, acids, catalysts, ligands, etc. used in the reaction (hereinafter, sometimes referred to as "raw materials, etc. used in the reaction"). Even if the solvent used in each step reacts with the raw materials, etc. used in the reaction, it can be used as an inert solvent as long as the target reaction proceeds and the target compound is obtained.

[0240] An overview of the compound synthesis involved in this disclosure is shown below. The "B" and "F" after the Roman numerals in the compound numbers indicate that the nitrogen-containing five-membered ring is located at the "rear" and "front," respectively. In other words, a compound in which the -C(=O)NH-R2 group is bonded to the nitrogen-containing five-membered ring is called a "rear" compound, and a compound in which the -C(=O)NH-R2 group is not bonded to the nitrogen-containing five-membered ring is called a "front" compound.

[0241] Synthetic Scheme 1 Synthesis of Compound III Compound III can be produced, for example, by the following production method. (1) Route 1-1 Synthesis from Compound VII and Compound VIII [ka] (2) Route 1-2 Synthesis from Compound VII and Compound VIII via Amine Protection [ka] (3) Route 1-3 Synthesis from Compound XI and Compound XII [ka] where X Lrepresents a leaving group in a nucleophilic substitution reaction, examples of which include halogens (e.g., chlorine, bromine, and iodine), sulfates (-OSOH, etc.), and sulfonyl-O- groups (e.g., methanesulfonyl-O-, toluenesulfonyl-O-, etc.). (4) Route 1-4 Synthesis from Compound XI and Compound XIII [ka] (5) Route 1-5 Synthesis from Compound VII and Compound XIV [ka] Here, when R1 in compound III can be represented by -CH2-R1', R1 in compound III can be replaced with -CH2-R1', and compound III can be represented as compound III'. In the formula, R1 is as defined in item 1 or item A1 of the present specification, and "Protect" is a protecting group for an amino group. Examples of the protecting group for an amino group include an ethoxycarbonyl group, a tert-butoxycarbonyl group, an acetyl group, a benzoyl group, a trifluoroacetyl group, a benzyloxycarbonyl group, a 3- or 4-chlorobenzyloxycarbonyl group, a triphenylmethyl group, a methanesulfonyl group, a p-toluenesulfonyl group, a trimethylsilyl group, a benzyloxycarbonyl group, a 3- or 4-chlorobenzyloxycarbonyl group, a benzylsulfonyl group, a benzyl group, a 4-nitrobenzyl group, a 4-methoxybenzyl group, a methyl group, and an ethyl group.

[0242] The compounds used as starting materials may be commercially available or may be prepared by known methods.

[0243] Synthetic Scheme 2 Synthesis of Compound V The compound of formula V can be produced, for example, by the following production method. (1) Route 2-1 Synthesis from Compound XVI and Compound XVII [ka] In the formula, R8 represents alkoxy, aryloxy, hydroxy, or halogen, and examples thereof include ethoxy groups. This synthesis can be achieved by various reactions known to those skilled in the art. When R2 is aryl, compound V can be synthesized according to the method described in CW Cheung, ML Ploeger, and X. Hu, Nature Communications 2017, 8, 14878. (2) Route 2-2 Synthesis from Compound XVIII [ka] In the formula, R2 is as defined in Section 1 or Section A1 of this specification. The starting compound may be a commercially available compound or may be prepared by a known method.

[0244] Synthetic Scheme 3 Synthesis of Compound VI The compound of formula VI can be prepared from compound III and compound IV, for example, by the following method. [ka] In the formula, R1 and R3 are as defined in Section 1 or Section A1 of this specification.

[0245] Synthetic Scheme 4 Compounds of Formula IIF and Compounds of Formula IIB—Route 1 The compound of formula IIF and the compound of formula IIB can be produced by one-pot synthesis from three components, for example, according to known methods (e.g., methods described in Bioorg. Med. Chem. 23 (2015) 2629-2635, Tetrahedron 63 (2007) 6004-6014, Eur. J. Org. Chem. 2009, 2185-2189, and Eur. J. Org. Chem. 2011, 2354-2359). [ka] In the formula, R1, R2 and R3 are as defined in Section 1 or Section A1 of this specification.

[0246] Synthetic Scheme 5 Compounds of Formula IIF and Compounds of Formula IIB—Route 2 The compounds of formula IIF and IIB can be prepared, for example, from two components as follows. [ka] In the formula, R1, R2 and R3 are as defined in Section 1 or Section A1 of this specification.

[0247] Synthetic Scheme 6 Synthesis of Compound IF and Compound IB Step 6-1 Reduction of imines Compound IF (i.e., the compound of formula IF) or compound IB (i.e., the compound of formula IB) can be prepared from compound IIF (i.e., the compound of formula IIF) or compound IIB (i.e., the compound of formula IIB) by reduction, for example, as follows: wherein R4 in the following formula is H. [ka]

[0248] Step 6-2 Amine modification of the piperidine ring The amine of the piperidine ring in Compound IF or Compound IB can be modified, for example, by alkylation or amidation, as described below. [ka]

[0249] Synthetic Scheme 7 Synthesis of Compound V' The compound of formula V' can be produced, for example, by the following production method. (1) Route 7-1 Synthesis from Compound XVI and Compound XVII' [ka] The compound of formula V' can be synthesized under the same conditions as those of Route 2-1 in Synthesis Scheme 2. R8 represents alkoxy, aryloxy, hydroxy or halogen. (2) Route 7-2 Synthesis from Compound XVIII' [ka] In the formula, R 2A and R 2B is as defined in Section 1 of the present specification. The compounds used as starting materials may be commercially available or may be prepared by known methods.

[0250] Syntheti...

Claims

[Claim 1] The invention described in the specification.

Images