Cyclic amide compounds and methods for treating rabies

Abstract

To provide a cyclic amide compound for treating rabies and a method therefor.SOLUTION: The present disclosure provides compounds that are useful for the treatment and prevention of rabies. The present disclosure provides compounds represented by Formula XXIF or Formula XXIB, solvates or pharmaceutically acceptable salts thereof, uses of these compounds, solvates or pharmaceutically acceptable salts thereof for the treatment or prevention of rabies, pharmaceutical compositions comprising these compounds, solvates or pharmaceutically acceptable salts thereof, and methods for the treatment and prevention of rabies using the same.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.

[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, XXIIB, XXIIIF, or XXIIIB, or pharmaceutically acceptable salts thereof (hereinafter sometimes referred to as "compounds of the present disclosure" or "the compound(s) of the disclosure") can solve the above-mentioned problems, and have completed the technical subject matter of the present disclosure. That is, the present disclosure is as follows:

[0005] This disclosure provides the following sections:

[0006] [Term 1A] Formula XXIF: [ka] or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1, R3 and R4 each independently represent hydrogen, optionally substituted hydrocarbon groups; an optionally substituted heterocycle; an optionally substituted carbonyl, or an optionally substituted functional group, R 2A and R 2B are each independently hydrogen, optionally substituted hydrocarbon groups; 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 each independently represent hydrogen, optionally substituted alkyl, optionally substituted alkenyl; optionally substituted alkynyl; optionally substituted cycloalkyl; optionally substituted heterocycloalkyl; optionally substituted aryl; optionally substituted heteroaryl, or is an 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 an 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 the non-aryl heterocycle and the 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 2A] Formula XXIB: [ka] or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1, R3 and R4 each independently represent hydrogen, optionally substituted hydrocarbon groups; an optionally substituted heterocycle; an optionally substituted carbonyl, or an optionally substituted functional group, R 2A and R 2B are each independently hydrogen, optionally substituted hydrocarbon groups; 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 each independently represent hydrogen, optionally substituted alkyl, optionally substituted alkenyl; optionally substituted alkynyl; optionally substituted cycloalkyl; optionally substituted heterocycloalkyl; optionally substituted aryl; optionally substituted heteroaryl, or is an 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 an 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 the non-aryl heterocycle and the 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 3A] 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 number of possible substitutions, as needed; R 2A and R 2B wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, carbonyl, the non-aryl heterocycle and the heteroaryl ring are each independently substituted as needed with one to the maximum possible number of identical or different substituents selected from Substituent Group I. A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item 4A] R1, R3 and R4 are each independently hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl; optionally substituted heterocycloalkyl; optionally substituted aryl; optionally substituted heteroaryl, or is an 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 an 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 the non-aryl heterocycle and the heteroaryl ring are each independently optionally substituted. A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item 4B] R1, R3 and R4 are each independently hydrogen, C substituted as needed 1-12 Alkyl, C substituted as needed 3-10 cycloalkyl, optionally substituted 5- to 10-membered heterocycloalkyl; C substituted as needed 6-10 aryl, an optionally substituted 5- to 10-membered heteroaryl; or is an optionally substituted carbonyl, R 2A and R 2B are each independently hydrogen, C substituted as needed 1-12 Alkyl, C substituted as needed 3-10 cycloalkyl, optionally substituted 5- to 10-membered heterocycloalkyl; C substituted as needed 6-10 aryl, an optionally substituted 5- to 10-membered heteroaryl; or an optionally substituted carbonyl; or R 2A and R 2B together with the nitrogen atom to which they are attached form a 5- to 10-membered non-aryl heterocycle or a 5- to 10-membered heteroaryl ring, wherein the non-aryl heterocycle and the heteroaryl ring are each independently optionally substituted. A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item 5A] R1, R3 and R4 are each independently hydrogen, optionally substituted alkyl, optionally substituted arylalkyl; optionally substituted heteroarylalkyl; optionally substituted cycloalkyl; optionally substituted heterocycloalkyl; optionally substituted aryl; 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; Here, the above groups of R1, R3 and R4 are optionally substituted with one to the maximum possible number of identical or different substituents selected from Substituent Group II; R 2A and R 2B 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; where R 2A and R 2B is 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 together with the nitrogen atom to which they are attached form a non-aryl heterocycle or heteroaryl ring; wherein the non-aryl heterocycle and the heteroaryl ring are each independently optionally substituted with one to the maximum possible number of identical or different substituents selected from Substituent Group II; A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item 5B] R1, R3 and R4 are each independently hydrogen, C substituted as needed 1-12 Alkyl, C substituted as needed 6-10 Aryl C 1-12 Alkyl, Optionally substituted 5- to 10-membered heteroaryl C 1-12 Alkyl, C substituted as needed 3-10 cycloalkyl, optionally substituted 5- to 10-membered heterocycloalkyl; C substituted as needed 6-10 aryl, Formyl, C substituted as needed 1-12 alkylcarbonyl, C substituted as needed 1-12 alkoxycarbonyl, C substituted as needed 6-10 arylcarbonyl, C substituted as needed 6-10 aryloxycarbonyl, optionally substituted 5- to 10-membered heteroarylcarbonyl; optionally substituted 5- to 10-membered heteroaryloxycarbonyl; C substituted as needed 3-10 cycloalkylcarbonyl, C substituted as needed 3-10 cycloalkyloxycarbonyl, optionally substituted 5- to 10-membered heterocycloalkylcarbonyl; optionally substituted 5- to 10-membered heterocycloalkyloxycarbonyl; Carbamoyl, C substituted as needed 1-12 alkylcarbamoyl, C substituted as needed 1-12 alkoxycarbamoyl, C substituted as needed 6-10 arylcarbamoyl, optionally substituted 5- to 10-membered heteroarylcarbamoyl; C substituted as needed 3-10 cycloalkylcarbamoyl, or optionally substituted 5- to 10-membered heterocycloalkylcarbamoyl; wherein the above groups of R1, R3 and R4 are optionally substituted with one to the maximum substitutable number of identical or different substituents selected from Substituent Group III; R 2A and R 2B are each independently hydrogen, C substituted as needed 1-12 Alkyl, C substituted as needed 6-10 Aryl C 1-12 Alkyl, C substituted as needed 3-10 cycloalkyl, optionally substituted 5- to 10-membered heterocycloalkyl; Formyl, C substituted as needed 1-12 alkylcarbonyl, C substituted as needed 1-12 alkoxycarbonyl, C substituted as needed 6-10 arylcarbonyl, C substituted as needed 6-10 aryloxycarbonyl, optionally substituted 5- to 10-membered heteroarylcarbonyl; optionally substituted 5- to 10-membered heteroaryloxycarbonyl; C substituted as needed 3-10 cycloalkylcarbonyl, C substituted as needed 3-10 cycloalkyloxycarbonyl, optionally substituted 5- to 10-membered heterocycloalkylcarbonyl; optionally substituted 5- to 10-membered heterocycloalkyloxycarbonyl; Carbamoyl, C substituted as needed 1-12 alkylcarbamoyl, C substituted as needed 1-12 alkoxycarbamoyl, C substituted as needed 6-10 arylcarbamoyl, optionally substituted 5- to 10-membered heteroarylcarbamoyl; C substituted as needed 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 possible number of identical or different substituents selected from Substituent Group III, or R 2A and R2B together with the nitrogen atom to which they are attached form a 5- to 10-membered non-aryl heterocycle or a 5- to 10-membered heteroaryl ring, wherein the non-aryl heterocycle and the 5- to 10-membered heteroaryl ring may each independently be substituted with one to the maximum possible number of identical or different substituents selected from Substituent Group V. A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item 6A] R1 and R4 are each independently hydrogen, optionally substituted alkyl, optionally substituted arylalkyl; optionally substituted heteroarylalkyl; optionally substituted cycloalkyl; optionally substituted heterocycloalkyl; 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 one to the maximum substitutable number of identical or different substituents selected from Substituent Group III. A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item 6B] R1 and R4 are each independently hydrogen, C substituted as needed 1-12 Alkyl, C substituted as needed 6-10 Aryl C 1-12 Alkyl, Optionally substituted 5- to 10-membered heteroaryl C 1-12 Alkyl, C substituted as needed 3-10 cycloalkyl, optionally substituted 5- to 10-membered heterocycloalkyl; Formyl, C substituted as needed 1-12 alkylcarbonyl, C substituted as needed 1-12 alkoxycarbonyl, C substituted as needed 6-10 arylcarbonyl, C substituted as needed 6-10 aryloxycarbonyl, C substituted as needed 3-10 cycloalkylcarbonyl, C substituted as needed 3-10 cycloalkyloxycarbonyl, optionally substituted 5- to 10-membered heterocycloalkylcarbonyl; optionally substituted 5- to 10-membered heterocycloalkyloxycarbonyl; Carbamoyl, C substituted as needed 1-12 alkylcarbamoyl, C substituted as needed 1-12alkoxycarbamoyl, C substituted as needed 6-10 arylcarbamoyl, optionally substituted 5- to 10-membered heteroarylcarbamoyl; C substituted as needed 3-10 cycloalkylcarbamoyl, or optionally substituted 5- to 10-membered heterocycloalkylcarbamoyl; wherein the above groups of R1 and R4 are optionally substituted with one to the maximum substitutable number of identical or different substituents selected from Substituent Group III. A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item 7A] R1 and R4 are each independently hydrogen, optionally substituted alkyl, optionally substituted arylalkyl; optionally substituted heteroarylalkyl; optionally substituted heterocycloalkyl; Formyl, optionally substituted alkylcarbonyl; optionally substituted alkoxycarbonyl; an optionally substituted arylcarbonyl, or optionally substituted aryloxycarbonyl; wherein the above groups of R1 and R4 are optionally substituted with one to the maximum substitutable number of identical or different substituents selected from Substituent Group III. A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item 7B] R1 and R4 are each independently hydrogen, C substituted as needed 1-12 Alkyl, C substituted as needed 6-10 Aryl C 1-12 Alkyl, Optionally substituted 5- to 10-membered heteroaryl C 1-12 Alkyl, optionally substituted 5- to 10-membered heterocycloalkyl; Formyl, C substituted as needed 1-12 alkylcarbonyl, C substituted as needed 1-12 alkoxycarbonyl, C substituted as needed 6-10 arylcarbonyl, C substituted as needed 6-10 aryloxycarbonyl, wherein the above groups of R1 and R4 are optionally substituted with one to the maximum substitutable number of identical or different substituents selected from Substituent Group III. A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item 7C] R1 and R4 are each independently hydrogen, C substituted as needed 1-12 Alkyl, C substituted as needed 6-10 Aryl C 1-6 Alkyl, Optionally substituted 5- to 10-membered heteroaryl C 1-6 Alkyl, optionally substituted 5- to 10-membered heterocycloalkyl; Formyl, C substituted as needed 1-12 alkylcarbonyl, C substituted as needed 1-12 alkoxycarbonyl, C substituted as needed 6-10 arylcarbonyl, C substituted as needed 6-10 aryloxycarbonyl, wherein the above groups of R1 and R4 are optionally substituted with one to the maximum substitutable number of identical or different substituents selected from Substituent Group III. A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section 8A] R1 is hydrogen; alkyl; alkyl substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of hydroxy, substituted oxy, formyl, substituted carbonyl, amino, substituted amino, and cycloalkyl, and substituted cycloalkyl; arylalkyl; arylalkyl substituted with 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; heteroarylalkyl; heteroarylalkyl substituted with 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; cycloalkyl; substituted cycloalkyl; heterocycloalkyl; substituted heterocycloalkyl; or a substituted carbonyl, wherein the substituted oxy, substituted carbonyl, substituted amino, substituted cycloalkyl, substituted heterocycloalkyl, and substituted alkyl each independently have from 1 to the maximum possible number of identical or different substituents selected from Substituent Group IV; A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section 8B] R1 is hydrogen; alkyl; Alkyl substituted with from 1 to the maximum possible number of identical or different substituents selected from the group consisting of hydroxy, alkoxy, haloalkoxy, formyl, carboxy, carbamoyl, alkylcarbonyl, alkoxycarbonyl, amino, amidinoamino, alkoxycarbonyl-substituted amidinoamino, alkoxycarbonylamino, cycloalkyl, and halocycloalkyl; arylalkyl; arylalkyl substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of halogen, alkyl, haloalkyl, hydroxy, alkoxy, haloalkoxy, arylalkoxy, amino, alkylamino, (alkyl)2amino, cycloalkylcarbonylamino, and nitro; heteroarylalkyl; heteroarylalkyl substituted with 1 to the maximum possible number of identical or different substituents selected from the group consisting of halogen, alkyl, haloalkyl, hydroxy, alkoxy, haloalkoxy, arylalkoxy, amino, alkylamino, (alkyl)2amino, cycloalkylcarbonylamino, and nitro; cycloalkyl; Halocycloalkyl; heterocycloalkyl; Alkyl carbonyl; Arylalkylcarbonyl; Alkoxycarbonyl; arylcarbonyl; or aryloxycarbonyl, A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section 8C] R1 is hydrogen; C 1-12 alkyl; C 1-12 Alkoxy, C 1-12 Haloalkoxy, formyl, carboxy, carbamoyl, C 1-12 Alkyl carbonyl, C 1-12 Alkoxycarbonyl, C1-12 Haloalkoxycarbonyl, amidinoamino, C 1-12 Alkoxycarbonyl-substituted amidinoamino, C 1-12 Alkoxycarbonylamino, hydroxy, C 3-10 Cycloalkyl, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of halocycloalkyl 1-12 alkyl; C 6-10 Aryl C 1-12 alkyl; Halogen, C 1-12 Alkyl, C 1-12 Haloalkyl, hydroxy, C 1-12 Alkoxy, C 1-12 Haloalkoxy, C 6-10 Aryl C 1-12 Alkoxy, Amino, C 1-12 Alkylamino, (C 1-12 Alkyl)2amino, C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkylcarbonylamino, nitro, and hydroxy 6-10 Aryl C 1-12 alkyl; 5-10 membered heteroaryl C 1-12 alkyl; Halogen, C 1-12 Alkyl, C 1-12 Haloalkyl, hydroxy, C 1-12 Alkoxy, C 1-12 Haloalkoxy, C 6-10 Aryl C 1-12 Alkoxy, Amino, C 1-12 Alkylamino, (C 1-12 Alkyl)2amino, C 3-10 5-10 membered heteroaryl C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkylcarbonylamino, nitro, and hydroxy 1-12 alkyl; C 3-10 cycloalkyl; 5-10 membered heterocycloalkyl; C 1-12 Alkyl carbonyl; C 6-10 Aryl C 1-12 Alkyl carbonyl; C 1-12 Alkoxycarbonyl; C 6-10 arylcarbonyl; or C 6-10 aryloxycarbonyl, A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section 8D] R1 is hydrogen; C 1-12 alkyl; C 1-6 Alkoxy, C 1-6 Haloalkoxy, formyl, carboxy, carbamoyl, C 1-6 Alkyl carbonyl, C 1-6 Alkoxycarbonyl, C 1-6 Haloalkoxycarbonyl, amidinoamino, C 1-6 Alkoxycarbonyl-substituted amidinoamino, C 1-6 Alkoxycarbonylamino, hydroxy, C 3-10 Cycloalkyl, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of halocycloalkyl 1-12 alkyl; C 6-10 Aryl C 1-6 alkyl; Halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, hydroxy, C 1-6 Alkoxy, C 1-6 Haloalkoxy, C 6-10 Aryl C 1-6 Alkoxy, Amino, C 1-6 Alkylamino, (C 1-6 Alkyl)2amino, C 3-10C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkylcarbonylamino, nitro, and hydroxy 6-10 Aryl C 1-6 alkyl; Halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, hydroxy, C 1-6 Alkoxy, C 1-6 Haloalkoxy, C 6-10 Aryl C 1-6 Alkoxy, Amino, C 1-6 Alkylamino, (C 1-6 Alkyl)2amino, C 3-10 5-10 membered heteroaryl C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkylcarbonylamino, nitro, and hydroxy 1-6 alkyl; C 3-10 cycloalkyl; 5-10 membered heterocycloalkyl; C 1-6 Alkyl carbonyl; C 6-10 Aryl C 1-6 Alkyl carbonyl; C 1-6 Alkoxycarbonyl; C 6-10 arylcarbonyl; or C 6-10 aryloxycarbonyl, A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section 9A] R3 is alkyl; alkyl substituted with from one to the maximum possible number of identical or different substituents selected from the group consisting of hydroxy, substituted oxy, substituted carbonyl, amino, substituted amino, cycloalkyl, and substituted cycloalkyl; 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, and substituted oxy; aryl; or and substituted aryl, wherein the substituted oxy, substituted carbonyl, substituted amino, substituted cycloalkyl, substituted alkyl, and substituted aryl each independently have from 1 to the maximum possible number of identical or different substituents selected from Substituent Group IV. A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section 9B] R3 is alkyl; alkyl substituted with from 1 to the maximum possible number of identical or different substituents selected from the group consisting of hydroxy, alkoxy, haloalkoxy, trialkylsilyloxy, carboxy, carbamoyl, alkoxycarbonyl, haloalkoxycarbonyl, amino, amidinoamino, alkoxycarbonyl-substituted amidinoamino, alkoxycarbonylamino, haloalkoxycarbonylamino, cycloalkyl, and halocycloalkyl; 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, hydroxy, alkoxy, and haloalkoxy; or is aryl, A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section 9C] R3 is C 1-12 alkyl; Hydroxy, C 1-12 Alkoxy, C 1-12 Haloalkoxy, TriC 1-12 Alkylsilyloxy, carboxy, carbamoyl, C 1-12 Alkoxycarbonyl, C 1-12 Haloalkoxycarbonyl, amino, amidinoamino, C 1-12Alkoxycarbonyl-substituted amidinoamino, C 1-12 Alkoxycarbonylamino, C 1-12 Haloalkoxycarbonylamino, C 3-10 Cycloalkyl, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of halocycloalkyl 1-12 alkyl; C 6-10 Aryl C 1-12 alkyl; Halogen, C 1-12 Alkyl, C 1-12 Haloalkyl, hydroxy, C 1-12 Alkoxy, and C 1-12 C substituted with 1 to the maximum possible number of identical or different substituents selected from the group consisting of haloalkoxy 6-10 Aryl C 1-12 alkyl; or C 6-10 is aryl, A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section 9D] R3 is C 1-12 alkyl; Hydroxy, C 1-6 Alkoxy, C 1-6 Haloalkoxy, TriC 1-6 Alkylsilyloxy, carboxy, carbamoyl, C 1-6 Alkoxycarbonyl, C 1-6 Haloalkoxycarbonyl, amino, amidinoamino, C 1-6 Alkoxycarbonyl-substituted amidinoamino, C 1-6 Alkoxycarbonylamino, C 1-6 Haloalkoxycarbonylamino, C 3-10 Cycloalkyl, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of halocycloalkyl 1-12 alkyl; C 6-10 Aryl C1-6 alkyl; Halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, hydroxy, C 1-6 Alkoxy, and C 1-6 C substituted with 1 to the maximum possible number of identical or different substituents selected from the group consisting of haloalkoxy 6-10 Aryl C 1-6 alkyl; or C 6-10 is aryl, A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section 10A]R 2A and R 2B are each independently hydrogen; alkyl; alkyl substituted with from one to the maximum possible number of identical or different substituents selected from the group consisting of hydroxy, substituted oxy, amino, substituted amino, cycloalkyl, and substituted cycloalkyl; 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, and substituted oxy; cycloalkyl; substituted cycloalkyl; heterocycloalkyl; or substituted heterocycloalkyl, wherein the substituted oxy, substituted amino, substituted alkyl, substituted cycloalkyl, and substituted heterocycloalkyl each independently have from 1 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; A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section 10B]R 2A and R 2B are each independently hydrogen; alkyl; alkyl substituted with from one to the maximum possible number of identical or different substituents selected from the group consisting of hydroxy, alkoxy, carboxy, alkoxycarbonyl, amino, amidinoamino, alkoxycarbonyl-substituted amidinoamino, alkoxycarbonylamino, cycloalkyl, and halocycloalkyl; 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, hydroxy, alkoxy, and haloalkoxy; cycloalkyl; alkyl-substituted cycloalkyl; or 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; A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section 10C]R 2A and R 2B are each independently hydrogen; C 1-12 alkyl; Hydroxy, C 1-12 Alkoxy, carboxy, C 1-12 Alkoxycarbonyl, amino, amidinoamino, C 1-12 Alkoxycarbonyl-substituted amidinoamino, and C 1-12 Alkoxycarbonylamino, C 3-10Cycloalkyl, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of halocycloalkyl 1-12 alkyl; C 6-10 Aryl C 1-12 Alkyl; halogen, C 1-12 Alkyl, C 1-12 Haloalkyl, hydroxy, C 1-12 Alkoxy, and C 1-12 C substituted with 1 to the maximum possible number of identical or different substituents selected from the group consisting of haloalkoxy 6-10 Aryl C 1-12 alkyl; C 3-10 cycloalkyl; C 1-12 Alkyl-substituted C 3-10 cycloalkyl; or a 5- to 10-membered heterocycloalkyl; 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 substitutable number of identical or different substituents selected from Substituent Group VI; A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section 10D]R 2A and R 2B are each independently hydrogen; C 1-12 alkyl; Hydroxy, C 1-6 Alkoxy, carboxy, C 1-6 Alkoxycarbonyl, amino, amidinoamino, C 1-6 Alkoxycarbonyl-substituted amidinoamino, and C 1-6 Alkoxycarbonylamino, C 3-10 Cycloalkyl, and C 3-10C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of halocycloalkyl 1-12 alkyl; C 6-10 Aryl C 1-6 alkyl; Halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, hydroxy, C 1-6 Alkoxy, and C 1-6 C substituted with 1 to the maximum possible number of identical or different substituents selected from the group consisting of haloalkoxy 6-10 Aryl C 1-6 alkyl; C 3-10 cycloalkyl; C 1-6 Alkyl-substituted C 3-10 cycloalkyl; or a 5- to 10-membered heterocycloalkyl; 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 substitutable number of identical or different substituents selected from Substituent Group VI; A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item 11A] R4 is hydrogen, alkyl, or substituted alkyl, wherein the substituted alkyl has one or up to the maximum possible number of identical or different substituents selected from the group consisting of halogen, carboxy, carbamoyl, amino, alkylamino, aryl, nitroaryl, and alkoxycarbonylamino; A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item 11B] R4 is hydrogen, C 1-12 Alkyl or substituted C 1-12 alkyl, wherein the substituted C 1-12Alkyl is halogen, carboxy, carbamoyl, amino, C 1-12 Alkylamino, C 6-10 Aryl, nitro C 6-10 Aryl, and C 1-12 alkoxycarbonylamino, having one or up to the maximum possible number of identical or different substituents selected from the group consisting of: A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item 11C] R4 is hydrogen or alkyl; A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item 11D] R4 is hydrogen or C 1-12 is alkyl, A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item 12A] R1 is hydrogen, methyl, propyl, isopropyl, isobutyl, sec-butyl, isopentyl, hexyl, amidinoaminopropyl, (tert-butoxycarbonyl-substituted amidinoamino)propyl, tert-butoxyethyl, tert-butoxypropyl, tert-butoxycarbonylethyl, carboxyethyl, hydroxyethyl, hydroxypropyl, tert-butoxycarbonylaminopropyl, cyclopentylmethyl, cyclohexylmethyl, cycloheptylmethyl, 5,6,7,8-tetrahydronaphthalenylmethyl, benzyl, phenylethyl, naphthalenylmethyl, fluorobenzyl, chlorobenzyl, methylbenzyl, dimethylbenzyl, tert-butylbenzyl, methoxybenzyl, ethoxy ... 1-tert-butoxycarbonyl-6-methyl-1H-indol-3-ylmethyl, 1-tert-butoxycarbonyl-6-fluoro-1H-indol-3-ylmethyl, 1-tert-butoxycarbonyl-6-fluoro-1H-indol-3-ylmethyl, nitrobenzyl, hydroxybenzyl, cyclohexyl, isovaleryl, phenylacetyl, benzoyl, isopropyloxycarbonyl, phenoxycarbonyl, or tetrahydro-2H-pyranyl; A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section 12B]R 2A is hydrogen, R 2Bis isopropyl, isobutyl, sec-butyl, pentyl, isopentyl, hexyl, heptyl, amidinoaminopropyl, (tert-butoxycarbonyl-substituted amidinoamino)propyl, (tert-butoxycarbonyl)ethyl, tert-butoxyethyl, methoxybutyl, carboxyethyl, hydroxyethyl, (tert-butoxycarbonylamino)propyl, cyclopentylmethyl, cyclohexylmethyl, cycloheptylmethyl, (1,2,3,4-tetrahydronaphthalenyl)methyl, 2,2,6,6-tetramethylpiperidinyl, benzyl, phenylethyl, naphthalenylmethyl, fluorobenzyl, chlorobenzyl, (fluorophenyl)ethyl, methylbenzyl, tert-butoxybenzyl, hydroxybenzyl, β-hydroxyphenethyl, α-hydroxymethylphenethyl, cyclopentyl, cyclohexyl, or methylcyclohexyl; or R 2A and R 2B together with the nitrogen atom to which they are attached form a pyrrolidine ring, A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item 12C] R3 is propyl, isobutyl, isopentyl, hexyl, amidinoaminopropyl, (tert-butoxycarbonyl-substituted amidinoamino)propyl, (tert-butoxycarbonyl)ethyl, carboxyethyl, hydroxyethyl, (tert-butyldimethylsilyloxy)ethyl, (tert-butoxycarbonylamino)propyl, cyclopentylmethyl, cyclohexylmethyl, cyclohexylethyl, benzyl, naphthalenylmethyl, phenylethyl, naphthalenylethyl, chlorobenzyl, methylbenzyl, (methylphenyl)ethyl, (isopropylphenyl)ethyl, tert-butoxybenzyl, hydroxybenzyl, or phenyl; A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item 12D] R4 is hydrogen or methyl; A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item 13A] R1 is alkyl, substituted arylalkyl, or substituted heteroarylalkyl, and R 2A is hydrogen and R 2B A compound according to any one of the preceding items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R is alkyl, arylalkyl, substituted arylalkyl, or optionally substituted cycloalkylalkyl, R is alkyl, and R is hydrogen. [Item 13B] R1 is alkyl, alkyl-substituted arylalkyl, chloro-substituted arylalkyl, alkoxy-substituted arylalkyl, or heteroarylalkyl substituted with Boc and alkyl, or heteroarylalkyl substituted with Boc and halogen, and R 2A is hydrogen and R 2B The compound or its enantiomer, or a salt or solvate thereof according to any one of the above items, wherein R is alkyl, arylalkyl, fluoro-substituted arylalkyl, chloro-substituted arylalkyl, or cycloalkylalkyl, and R is alkyl. [Item 13C] R1 is C 1-12 Alkyl, C 1-12 Alkyl-substituted C 6-10 Aryl C 1-12 Alkyl, chloro-substituted C 6-10 Aryl C 1-12 Alkyl, C 1-12 Alkoxy-substituted C 6-10 Aryl C 1-12 Alkyl, or Boc and C 1-12 5-10 membered heteroaryl C substituted with alkyl 1-12 5-10 membered heteroaryl C substituted with alkyl, or Boc and halogen 1-12 alkyl, and R 2A is hydrogen and R 2B is C 1-12 Alkyl, C 6-10 Aryl C 1-12 Alkyl, Fluoro-substituted C6-10 Aryl C 1-12 Alkyl, chloro-substituted C 6-10 Aryl C 1-12 Alkyl, or C 3-10 Cycloalkyl C 1-12 alkyl, and R3 is C 1-12 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 13D] R1 is isobutyl, isopentyl, methylbenzyl, t-butylbenzyl, chlorobenzyl, methoxybenzyl, 1-tert-butoxycarbonyl-6-methyl-1H-indol-3-ylmethyl or 6-fluoro-1H-indol-3-ylmethyl, and R 2A is hydrogen and R 2B The compound or its enantiomer, or a salt or solvate thereof according to any one of the preceding items, wherein R is isobutyl, benzyl, fluorobenzyl, chlorobenzyl, or cycloheptylmethyl, and R is isobutyl or isopentyl. [Item 14A] The compound according to any one of the above items, wherein the compound is a compound selected from the group consisting of compound numbers I-1 to I-50, II-1 to II-50, IF-51 to IF-800, and IB-51 to IB-832, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Item 14B] The compound according to any one of the above items, wherein the compound is a compound selected from the group consisting of compound numbers I-1 to I-50, II-1 to II-50, IF-51 to IF-411, and IB-51 to IB-425, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Item 15] 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 16] The Lyssavirus virus includes the rabies virus. The antiviral agent according to any one of the above items. [Item 17] A pharmaceutical composition comprising the compound according to any one of the above items or a pharmaceutically acceptable salt thereof. [Item 18] The pharmaceutical agent according to any one of the above items, which is a preventive or therapeutic drug for rabies. [Item 19] 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 20] 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 21] A method for preventing or treating rabies, comprising administering to a patient in need of prevention or treatment a therapeutically effective amount of a compound or a pharmaceutically acceptable salt thereof described in any one of the above items, 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 22] 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.

[0007] The present disclosure also provides the following sections:

[0008] [Term A1] Formula IF: [ka] or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1 and R2 are each independently optionally substituted alkyl, optionally substituted cycloalkyl, or optionally substituted heterocycloalkyl; R3 is optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted cycloalkyl, or optionally substituted heterocycloalkyl; and X is -NH-; 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 and R2 are each independently optionally substituted alkyl, optionally substituted cycloalkyl, or optionally substituted heterocycloalkyl; R3 is optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted cycloalkyl, or optionally substituted heterocycloalkyl; and X is -NH-; A compound or its enantiomer, or a salt thereof, or a solvate thereof. [Item A3] R1 and R2 are each independently an optionally substituted alkyl, an optionally substituted cycloalkyl, or an optionally substituted heterocycloalkyl, and R3 is an optionally substituted alkyl, an optionally substituted alkenyl, or an optionally substituted aryl. A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item A4] 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 R2 are each independently an optionally substituted alkyl, an optionally substituted cycloalkyl, or an optionally substituted heterocycloalkyl, and R3 is an optionally substituted alkyl or an optionally substituted aryl. [Item A5] 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 alkyl optionally substituted with a hydroxyl group, a carboxyl group, a carbamoyl group, an amino group, or an amidinoamino group, optionally substituted cycloalkylalkyl, optionally substituted arylalkyl, or optionally substituted heteroarylalkyl. [Item A6] R1, R2 and R3 are each independently an alkyl optionally substituted with a hydroxyl group, a carboxyl group, a carbamoyl group, an amino group or an amidinoamino group; an optionally substituted cycloalkylalkyl; an optionally substituted C 6-10 Aryl C 1-6 alkyl; or optionally substituted 5- to 10-membered heteroarylC 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 A7] R1, R2 and R3 are each independently an alkyl optionally substituted with a hydroxyl group, a carboxyl group, a carbamoyl group, an amino group or an amidinoamino group; an optionally substituted cycloalkylalkyl; an optionally substituted C6 arylC 1-6 alkyl; or optionally substituted 5- or 6-membered heteroarylC 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 A8] 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 alkyl optionally substituted with a hydroxyl group, a carboxyl group, a carbamoyl group, an amino group, or an amidinoamino group; optionally substituted cycloalkylalkyl; optionally substituted benzyl; or optionally substituted 5- or 6-membered heteroarylmethyl. [Item A9] 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 alkyl optionally substituted with a hydroxyl group, a carboxyl group, a carbamoyl group, an amino group, or an amidinoamino group; cycloalkylalkyl; optionally substituted benzyl; or optionally substituted 5- or 6-membered heteroarylmethyl. [Item A10] The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R1 is alkyl or optionally substituted benzyl. [Item A11] R1 and R2 are each independently a C substituted with a hydroxyl group, a carboxyl group, a carbamoyl group, an amino group or an amidinoamino group, as needed. 1-6 Alkyl; optionally substituted C 3-6 Cycloalkyl C 1-6 Alkyl; optionally substituted C 6-10 Aryl C 1-6 Alkyl; optionally substituted 5- to 10-membered heteroarylC 1-6 alkyl; or optionally substituted 4- to 6-membered heterocycloalkylC 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 A12] R1 and R2 are each independently a C substituted with a hydroxyl group, a carboxyl group, a carbamoyl group, an amino group or an amidinoamino group, as needed. 1-6 Alkyl; optionally substituted C 3-6 Cycloalkyl C 1-6alkyl; 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 A13] R2 is C, substituted as needed. 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 A14] R2 is an optionally substituted C6 aryl 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 A15] The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R2 is optionally substituted benzyl. [Item A16] R1 is optionally a C substituted with a hydroxyl group, a carboxyl group, a carbamoyl group, an amino group or an amidinoamino group. 1-6 Alkyl; optionally substituted C 3-6 Cycloalkyl C 1-6 Alkyl; optionally substituted C6 arylC 1-6 alkyl; or optionally substituted 5- or 6-membered heteroarylC 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 A17] R1 is optionally a C substituted with a hydroxyl group, a carboxyl group, a carbamoyl group, an amino group or an amidinoamino group. 1-6 The compound according to any one of the above items, wherein the compound is alkyl, or optionally substituted benzyl, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Item A18] R3 is alkyl optionally substituted with a hydroxyl group, a carboxyl group, a carbamoyl group, an amino group or an amidinoamino group; optionally substituted C 6-10 Arylalkyl; optionally substituted C2-6 alkenyl; or optionally substituted C 6-10 The 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 aryl. [Item A19] R3 is alkyl optionally substituted with a hydroxyl group, a carboxyl group, a carbamoyl group, an amino group or an amidinoamino group; or optionally substituted C 6-10 The 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 arylalkyl. [Item A20] The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R3 is alkyl. [Item A21] R3 is optionally a C substituted with a hydroxyl group, a carboxyl group, a carbamoyl group, an amino group or an amidinoamino group. 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 A22] R1 and R2 are each independently C 1-6 Alkyl; Hydroxy-substituted C 1-6 Alkyl; Carbamoyl-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 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; C 1-4 Alkoxycarbonyl-substituted C1-6 Alkyl; C 1-4 C substituted with alkyl-substituted amino 6-10 Aryl 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 A23] R2 is a hydroxy-substituted C 1-6 Alkyl; Carbamoyl-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 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; C 1-4 Alkoxycarbonyl-substituted C 1-6 Alkyl; C 1-4 C substituted with alkyl-substituted amino 6-10 Aryl 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 A24] R2 is C 6-10 Aryl 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; C1-4 Alkoxy-substituted C 6-10 Aryl C 1-6 Alkyl; or C 1-4 C substituted with alkyl-substituted amino 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 A25] R3 is C 1-6 Alkyl; Hydroxy-substituted C 1-6 Alkyl; Carbamoyl-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 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; C 1-4 Alkoxycarbonyl-substituted C 1-6 Alkyl; C 1-4 C substituted with alkyl-substituted amino 6-10 Aryl 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 A26] R3 is C 1-6 Alkyl; Hydroxy-substituted C 1-6 Alkyl; Carbamoyl-substituted C 1-6 Alkyl;Amidinoamino-substituted C 1-6 Alkyl; carboxy-substituted C 1-6 Alkyl; C 1-4 Alkoxycarbonyl-substituted C1-6 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 A27] R1 and R2 are each independently C 1-6 Alkyl; C 6-10 Aryl C 1-6 Alkyl; C 1-6 Alkyl-substituted C 6-10 Aryl C 1-6 Alkyl; C 1-6 Alkoxy-substituted C 6-10 Aryl C 1-6 Alkyl; C 1-6 Haloalkoxy-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 1-6 C substituted with alkyl-substituted amino 6-10 Aryl C 1-6 Alkyl; C 5-6 Cycloalkyl; C 1-6 Alkyl-substituted C 5-6 cycloalkyl; or optionally substituted 5- or 6-membered heterocyclyl, and R3 is C 1-6 Alkyl; C 6-10 Aryl C 1-6 Alkyl; C 1-6 Alkyl-substituted C 6-10 Aryl C 1-6 Alkyl; halogen-substituted C 6-10 Aryl C 1-6 Alkyl; C 1-6 Haloalkoxy-substituted C 6-10 Aryl C 1-6 Alkyl; C 1-6 Alkoxy-substituted C 6-10 Aryl C 1-6 Alkyl; Hydroxy-substituted C 6-10 Aryl C 1-6 Alkyl; C 1-6C substituted with alkyl-substituted amino 6-10 Aryl C 1-6 Alkyl; C 6-10 Aryl;C 1-4 Alkyl-substituted C 6-10 Aryl; or halogen-substituted C 6-10 The 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 aryl. [Item A28] R1 and R2 are each independently methyl; n-propyl; isobutyl; isopentyl; benzyl; methyl or t-butyl substituted benzyl; fluoro or chloro substituted benzyl; methoxy or ethoxy substituted benzyl; trifluoromethoxy substituted benzyl; hydroxy substituted benzyl; dimethylamino substituted benzyl; cyclohexyl; methyl substituted cyclohexyl; tetrahydro-2H-pyran-4-yl; or 2,2,6,6-tetramethylpiperidin-4-yl, and R3 is methyl; n-propyl; isobutyl; isopentyl; benzyl; methyl or t-butyl substituted benzyl; fluoro or chloro substituted benzyl; methoxy or ethoxy substituted benzyl; trifluoromethoxy substituted benzyl; hydroxy substituted benzyl; dimethylamino substituted benzyl; or phenyl, or an enantiomer thereof, or a salt or solvate thereof, according to any one of the above items. [Item A29] R2 is C6 aryl C 1-6 Alkyl; C 1-6 Alkyl-substituted C6 aryl C 1-6 Alkyl; C 1-6 Alkoxy-substituted C6 aryl C 1-6 Alkyl; C 1-6 Haloalkoxy-substituted C6 arylC 1-6 Alkyl; Hydroxy-substituted C6 arylC 1-6 Alkyl; halogen-substituted C6 arylC 1-6 Alkyl; or C 1-6 C6 aryl C substituted with alkyl-substituted amino 1-6The 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 A30] R2 is benzyl; methyl or t-butyl substituted benzyl; methoxy or ethoxy substituted benzyl; trifluoromethoxy substituted benzyl; hydroxy substituted benzyl; fluoro or chloro substituted benzyl; or dimethylamino substituted substituted benzyl, or an enantiomer thereof, or a salt thereof, or a solvate thereof, according to any one of the above items. [Item A31] R1 is C 1-6 Alkyl; C6 aryl C 1-6 Alkyl; C 1-6 Alkyl-substituted C6 aryl C 1-6 Alkyl; C 1-6 Alkoxy-substituted C6 aryl C 1-6 Alkyl; C 1-6 Haloalkoxy-substituted C6 arylC 1-6 Alkyl; Hydroxy-substituted C6 arylC 1-6 Alkyl; halogen-substituted C6 arylC 1-6 Alkyl; or C 1-6 C6 aryl C substituted with alkyl-substituted amino 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 is methyl; isobutyl; isopentyl; benzyl; methyl or t-butyl substituted benzyl; methoxy or ethoxy substituted benzyl; trifluoromethoxy substituted benzyl; hydroxy substituted benzyl; fluoro or chloro substituted benzyl; or dimethylamino substituted benzyl, or an enantiomer thereof, or a salt thereof, or a solvate thereof, according to any one of the above items. [Item A33] R3 is C 1-6 Alkyl; C6 aryl C 1-6 Alkyl; C 1-6 Alkyl-substituted C6 aryl C 1-6Alkyl; halogen-substituted C6 arylC 1-6 Alkyl; C 1-6 Haloalkoxy-substituted C6 arylC 1-6 Alkyl; C 1-6 Alkoxy-substituted C6 aryl C 1-6 Alkyl; Hydroxy-substituted C6 arylC 1-6 Alkyl; or C 1-6 C6 aryl C substituted with alkyl-substituted amino 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 A34] R3 is propyl; isobutyl; isopentyl; benzyl; methyl or t-butyl substituted benzyl; fluoro or chloro substituted benzyl; methoxy or ethoxy substituted benzyl; trifluoromethoxy substituted benzyl; hydroxy substituted benzyl; or dimethylamino substituted benzyl, or an enantiomer thereof, or a salt thereof, or a solvate thereof, according to any one of the above items. [Item A35] R3 is C 1-6 Alkyl; C6 aryl C 1-6 Alkyl; or halogen-substituted C6 arylC 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 A36] 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 propyl; isobutyl; isopentyl; benzyl; or chloro-substituted benzyl. [Item A37] R3 is 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 A38] R1 and R2 each independently represent methyl, ethyl, n-propyl, isopropyl, isobutyl, isopentyl, benzyl, 4-methylbenzyl, 4-(t-butyl)benzyl, 4-fluorobenzyl, 3-chlorobenzyl, 4-chlorobenzyl, 4-methoxybenzyl, 4-ethoxybenzyl, 4-hydroxybenzyl, 3-hydroxybenzyl, 4-(dimethylamino)benzyl, 4-(trifluoromethoxy)benzyl, cyclohexyl, trans-4-methylcyclohexyl, tetrahydro-2H-pyran-4-yl, or 2,2,6,6-tetramethylbenzyl. A compound according to any one of the preceding items, wherein R3 is methylpiperidin-4-yl, and R3 is methyl, ethyl, n-propyl, isopropyl, isobutyl, isopentyl, benzyl, 4-methylbenzyl, 4-(t-butyl)benzyl, 4-fluorobenzyl, 3-chlorobenzyl, 4-chlorobenzyl, 4-methoxybenzyl, 4-ethoxybenzyl, 4-hydroxybenzyl, 3-hydroxybenzyl, 4-(dimethylamino)benzyl, 4-(trifluoromethoxy)benzyl, or phenyl, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Item A39] R2 is isobutyl, isopentyl, benzyl, 4-fluorobenzyl, 4-chlorobenzyl, 4-hydroxybenzyl, 3-hydroxybenzyl, cyclohexyl, tetrahydro-2H-pyran-4-yl, or 2,2,6,6-tetramethylpiperidin-4-yl, or a compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [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 R2 is benzyl, 4-fluorobenzyl, 4-chlorobenzyl, 4-hydroxybenzyl, or 3-hydroxybenzyl. [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 R1 is methyl, isobutyl, isopentyl, benzyl, 4-methylbenzyl, 4-(t-butyl)benzyl, 3-chlorobenzyl, 4-chlorobenzyl, 4-methoxybenzyl, 4-ethoxybenzyl, 4-hydroxybenzyl, 4-(dimethylamino)benzyl, cyclohexyl, or trans-4-methylcyclohexyl. [Item A42] 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, benzyl, 4-methylbenzyl, 4-(t-butyl)benzyl, 3-chlorobenzyl, 4-chlorobenzyl, 4-methoxybenzyl, 4-ethoxybenzyl, 4-hydroxybenzyl, or 4-(dimethylamino)benzyl. [Item A43] 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 n-propyl, isobutyl, isopentyl, benzyl, 4-chlorobenzyl, or phenyl. [Item A44] The compound according to any one of the above items, or an enantiomer thereof, or a salt thereof, or a solvate thereof, wherein R3 is n-propyl, isobutyl, or isopentyl. [Item A45] 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 benzyl, R1 is isobutyl, methoxy-substituted benzyl, methyl-substituted benzyl, t-butyl-substituted benzyl, or chloro-substituted benzyl, and R3 is isobutyl. [Item A46] 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 benzyl, R1 is methoxy-substituted benzyl or chloro-substituted benzyl, and R3 is isobutyl. [Item A47] 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 benzyl, R1 is 4-methoxybenzyl or 3-chlorobenzyl, and R3 is isobutyl. [Item A48] The compound according to any one of the above items, wherein the compound is a compound of formula IF, R2 is benzyl, R1 is 4-methoxybenzyl, and R3 is isobutyl, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Item A49] The compound according to any one of the above items, wherein the compound is a compound of formula IB, R2 is benzyl, R1 is 4-methoxybenzyl, and R3 is isobutyl, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Item A50] 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 benzyl or chloro-substituted benzyl, and R1 and R3 are each independently isobutyl or isopentyl. [Item A51] 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 benzyl, R1 is isopentyl, and R3 is isobutyl. [Item A52] The compound according to any one of the above items, wherein the compound is a compound of formula IB, R2 is benzyl or 4-chlorobenzyl, and R1 and R3 are both isobutyl, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Item A53] The compound according to any one of the above items, wherein the compound is a compound of formula IB, R2 is benzyl, R1 is isobutyl, and R3 is isopentyl, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Item A54] The compound represented by the formula IF is (3S * ,3aR * ,6S * ,7R * ,7aR *)-N-benzyl-1-(4-chlorobenzyl)-7-isobutyl-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR * )-N-benzyl-1-(3-chlorobenzyl)-7-isobutyl-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR * )-N-benzyl-7-isobutyl-1-(4-methoxybenzyl)-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR * )-N-benzyl-7-isobutyl-1-(4-methylbenzyl)-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR * )-1-benzyl-N,7-diisobutyl-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR * )-7-benzyl-N-isobutyl-1-isopentyl-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR *)-7-(4-chlorobenzyl)-N,1-diisobutyl-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR * )-N-benzyl-1-(4-hydroxybenzyl)-7-isobutyl-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR * )-7-benzyl-1-isobutyl-N-isopentyl-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR * )-7-benzyl-N,1-diisobutyl-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR * )-N-benzyl-1,7-diisobutyl-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR * )-N-(4-chlorobenzyl)-1,7-diisobutyl-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR *)-N-benzyl-1-isobutyl-7-isopentyl-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR * )-N-benzyl-7-isobutyl-1-isopentyl-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR * )-N-benzyl-1-(4-(dimethylamino)benzyl)-7-isobutyl-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR * )-N-benzyl-1-(4-hydroxybenzyl)-7-isopentyl-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR * )-N-(4-fluorobenzyl)-7-isobutyl-1-isopentyl-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR * )-N-benzyl-7-isobutyl-4-oxo-1-(4-(trifluoromethoxy)benzyl)octahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR *)-N-benzyl-1-(4-ethoxybenzyl)-7-isobutyl-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR * )-1-benzyl-N-(4-hydroxybenzyl)-7-isobutyl-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR * )-N-(4-hydroxybenzyl)-7-isobutyl-1-(4-methoxybenzyl)-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR * )-1-(4-(dimethylamino)benzyl)-N-(3-hydroxybenzyl)-7-isobutyl-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR * )-1-(4-(dimethylamino)benzyl)-N-(4-hydroxybenzyl)-7-isobutyl-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR * )-1-benzyl-N-cyclohexyl-4-oxo-7-propyloctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR *)-1,7-dibenzyl-N-((1R,4S)-4-methylcyclohexyl)-4-oxooctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, (3S * ,3aR * ,6S * ,7R * ,7aR * )-1,7-dibenzyl-4-oxo-N-(2,2,6,6-tetramethylpiperidin-4-yl)octahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, and (3S * ,3aR * ,6S * ,7R * ,7aR * )-N-benzyl-1-isobutyl-4-oxo-7-phenyloctahydro-6H-3,6-methanopyrrolo[3,2-c]pyridine-6-carboxamide, or an enantiomer thereof, or a salt thereof, or a solvate thereof, according to any one of the above items. [Item A55] The compound represented by the formula IB is (3S * ,3aS * ,6R * ,7R * ,7aS * )-N,7-Dibenzyl-1-methyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-N-benzyl-1-(4-chlorobenzyl)-7-isobutyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-N-benzyl-1-(3-chlorobenzyl)-7-isobutyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS* ,6R * ,7R * ,7aS * )-N-benzyl-7-isobutyl-1-(4-methoxybenzyl)-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-N-benzyl-7-isobutyl-1-(4-methylbenzyl)-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-1-benzyl-N,7-diisobutyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-7-benzyl-N-isobutyl-1-isopentyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-7-(4-chlorobenzyl)-N,1-diisobutyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3R * ,3aS * ,6R * ,7R * ,7aS * )-7-benzyl-N,1-diisobutyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS *)-N-(4-chlorobenzyl)-1,7-diisobutyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-N-benzyl-1-(4-hydroxybenzyl)-7-isobutyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-7-benzyl-1-isobutyl-N-isopentyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-N-benzyl-1,7-diisobutyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-N-benzyl-1-isobutyl-7-isopentyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-N-benzyl-7-isobutyl-1-isopentyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS *)-N-benzyl-7-isobutyl-1-isopentyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-N-benzyl-1-(4-(dimethylamino)benzyl)-7-isobutyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-N-benzyl-1-(4-(tert-butyl)benzyl)-7-isobutyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-N-benzyl-1-(4-hydroxybenzyl)-7-isopentyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-N-(4-chlorobenzyl)-7-isobutyl-1-isopentyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-N-(4-fluorobenzyl)-7-isobutyl-1-isopentyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS *)-N-benzyl-7-isobutyl-5-oxo-1-(4-(trifluoromethoxy)benzyl)octahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-N-benzyl-1-(4-ethoxybenzyl)-7-isobutyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-1-benzyl-N-(4-hydroxybenzyl)-7-isobutyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-N-(4-hydroxybenzyl)-7-isobutyl-1-(4-methoxybenzyl)-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-1-(4-(dimethylamino)benzyl)-N-(3-hydroxybenzyl)-7-isobutyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-1-(4-(dimethylamino)benzyl)-N-(4-hydroxybenzyl)-7-isobutyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R* ,7aS * )-1-benzyl-N-cyclohexyl-5-oxo-7-propyloctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-1,7-dibenzyl-N-((1R,4S)-4-methylcyclohexyl)-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-1,7-dibenzyl-5-oxo-N-(2,2,6,6-tetramethylpiperidin-4-yl)octahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7R * ,7aS * )-N-benzyl-1-cyclohexyl-7-isobutyl-5-oxooctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7S * ,7aS * )-N-benzyl-1-cyclohexyl-5-oxo-7-phenyloctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, (3S * ,3aS * ,6R * ,7S * ,7aS * )-N-benzyl-5-oxo-7-phenyl-1-(tetrahydro-2H-pyran-4-yl)octahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, and (3S * ,3aS * ,6R * ,7S * ,7aS* )-N-benzyl-1-isobutyl-5-oxo-7-phenyloctahydro-3aH-3,6-methanopyrrolo[3,2-b]pyridine-3a-carboxamide, or an enantiomer thereof, or a salt thereof, or a solvate thereof, according to any one of the above items. [Item A56] An antiviral agent against lyssaviruses, comprising the compound according to any one of the above items, or a pharmaceutically acceptable salt thereof, or a solvate thereof. [Item A57] The antiviral agent according to Item 56, wherein the Lyssavirus virus includes rabies virus. [Item A58] A medicine containing the compound according to any one of the above items, or a pharmaceutically acceptable salt thereof, or a solvate thereof. [Item A59] The pharmaceutical according to Item 58, which is a preventive or therapeutic drug for rabies. [Item A60] A pharmaceutical composition comprising the compound according to any one of the above items, a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutically acceptable carrier. [Item A61] A pharmaceutical composition according to Item 60 for preventing or treating rabies. [Item A62] A method for preventing or treating rabies, comprising the step of administering to a subject in need of such prevention or treatment a compound described in any one of the above items or a pharmaceutically acceptable salt thereof or a solvate thereof, or a pharmaceutical composition described in item 60 or 61. [Item A63] Use of a compound according to any one of the above items or a pharmaceutically acceptable salt thereof, or a solvate thereof, for the manufacture of a medicament for the prevention or treatment of rabies. [Item A64] A compound according to any one of the above items, or a pharmaceutically acceptable salt thereof, or a solvate thereof, for use in the prevention or treatment of rabies.

[0009] The present disclosure further provides the following sections:

[0010] [Term B1A] 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; 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 B1B] 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; R 2A and R 2B together with the nitrogen atom to which they are attached form a non-aryl heterocycle or heteroaryl ring; wherein the non-aryl heterocycle and the 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 B2A] 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; 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 B2B] 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; R 2A and R 2B together with the nitrogen atom to which they are attached form a non-aryl heterocycle or heteroaryl ring; wherein the non-aryl heterocycle and the 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 B3A] 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 number of possible substitutions, as needed; R 2A and R 2Bwherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, carbonyl, the non-aryl heterocycle and the heteroaryl ring are each independently substituted as needed with one to the maximum possible number of identical or different substituents selected from Substituent Group I. A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item B4A] 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; R 2A and R 2B together with the nitrogen atom to which they are attached form a non-aryl heterocycle or heteroaryl ring; wherein the non-aryl heterocycle and the heteroaryl ring are each independently optionally substituted. A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item B4B] 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 R2B 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 5- to 10-membered non-aryl heterocycle or a 5- to 10-membered heteroaryl ring, wherein the non-aryl heterocycle and the heteroaryl ring are each independently optionally substituted. A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item B5A] R1, R3 and R4 are each independently hydrogen, optionally substituted alkyl, optionally substituted arylalkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, 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; Here, the above groups of R1, R3 and R4 are optionally substituted with one to the maximum possible number of identical or different substituents selected from Substituent Group II; R 2A and R 2B 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; where R 2A and R 2B is 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 together with the nitrogen atom to which they are attached form a non-aryl heterocycle or heteroaryl ring; wherein the non-aryl heterocycle and the heteroaryl ring are each independently optionally substituted with one to the maximum possible number of identical or different substituents selected from Substituent Group II; A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item B5B] 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 3-10 Cycloalkyl, optionally substituted 5- to 10-membered heterocycloalkyl, optionally substituted C 6-10 Aryl, 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 one 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 1-12Alkyl, 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 6-10 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 possible number of identical or different substituents selected from Substituent Group III, or R 2A and R 2B together with the nitrogen atom to which they are attached form a 5- to 10-membered non-aryl heterocycle or a 5- to 10-membered heteroaryl ring, wherein the non-aryl heterocycle and the 5- to 10-membered heteroaryl ring may each independently be substituted with one to the maximum possible number of identical or different substituents selected from Substituent Group V. A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item B6A] R1 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 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 one to the maximum substitutable number of identical or different substituents selected from Substituent Group III. A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item B6B] 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, 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 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 one to the maximum substitutable number of identical or different substituents selected from Substituent Group III. A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item B7A] R1 and R4 are each independently hydrogen, optionally substituted alkyl, optionally substituted arylalkyl, optionally substituted heterocycloalkyl, formyl, optionally substituted alkylcarbonyl, optionally substituted alkoxycarbonyl, optionally substituted arylcarbonyl, or optionally substituted aryloxycarbonyl; wherein the above groups of R1 and R4 are optionally substituted with one to the maximum substitutable number of identical or different substituents selected from Substituent Group III. A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item B7B] R1 and R4 are each independently hydrogen, optionally substituted C 1-12 Alkyl, optionally substituted C 6-10 Aryl C 1-6Alkyl, optionally substituted 5-10 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, wherein the above groups of R1 and R4 are optionally substituted with one to the maximum substitutable number of identical or different substituents selected from Substituent Group III. A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section B8A] R1 is hydrogen; alkyl; alkyl substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of hydroxy, substituted oxy, formyl, substituted carbonyl, amino, substituted amino, and cycloalkyl, and substituted cycloalkyl; arylalkyl; arylalkyl substituted with 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; cycloalkyl; substituted cycloalkyl; heterocycloalkyl; substituted heterocycloalkyl; or a substituted carbonyl, wherein the substituted oxy, substituted carbonyl, substituted amino, substituted cycloalkyl, substituted heterocycloalkyl, and substituted alkyl each independently have from 1 to the maximum possible number of identical or different substituents selected from Substituent Group IV; A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section B8B] R1 is hydrogen; alkyl; Alkyl substituted with from 1 to the maximum possible number of identical or different substituents selected from the group consisting of hydroxy, alkoxy, haloalkoxy, formyl, carboxy, carbamoyl, alkylcarbonyl, alkoxycarbonyl, amino, amidinoamino, alkoxycarbonyl-substituted amidinoamino, alkoxycarbonylamino, cycloalkyl, and halocycloalkyl; arylalkyl; arylalkyl substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of halogen, alkyl, haloalkyl, hydroxy, alkoxy, haloalkoxy, amino, alkylamino, (alkyl)2amino, cycloalkylcarbonylamino, and nitro; cycloalkyl; Halocycloalkyl; heterocycloalkyl; Alkyl carbonyl; Arylalkylcarbonyl; Alkoxycarbonyl; arylcarbonyl; or aryloxycarbonyl, A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section B8C] R1 is hydrogen; C 1-12 alkyl; C 1-6 Alkoxy, C 1-6 Haloalkoxy, formyl, carboxy, carbamoyl, C 1-6 Alkyl carbonyl, C 1-6 Alkoxycarbonyl, C 1-6 Haloalkoxycarbonyl, amidinoamino, C 1-6 Alkoxycarbonyl-substituted amidinoamino, C 1-6 Alkoxycarbonylamino, hydroxy, C 3-10 Cycloalkyl, and C 3-10C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of halocycloalkyl 1-12 alkyl; C 6-10 Aryl C 1-6 alkyl; Halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, hydroxy, C 1-6 Alkoxy, C 1-6 Haloalkoxy, Amino, C 1-6 Alkylamino, (C 1-6 Alkyl)2amino, C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkylcarbonylamino, nitro, and hydroxy 6-10 Aryl C 1-6 alkyl; C 3-10 cycloalkyl; 5-10 membered heterocycloalkyl; C 1-6 Alkyl carbonyl; C 6-10 Aryl C 1-6 Alkyl carbonyl; C 1-6 Alkoxycarbonyl; C 6-10 arylcarbonyl; or C 6-10 aryloxycarbonyl, A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section B9A] R3 is alkyl; alkyl substituted with from one to the maximum possible number of identical or different substituents selected from the group consisting of hydroxy, substituted oxy, substituted carbonyl, amino, substituted amino, cycloalkyl, and substituted cycloalkyl; 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, and substituted oxy; aryl; or and substituted aryl, wherein the substituted oxy, substituted carbonyl, substituted amino, substituted cycloalkyl, substituted alkyl, and substituted aryl each independently have from 1 to the maximum possible number of identical or different substituents selected from Substituent Group IV. A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section B9B] R3 is alkyl; alkyl substituted with from 1 to the maximum possible number of identical or different substituents selected from the group consisting of hydroxy, alkoxy, haloalkoxy, trialkylsilyloxy, carboxy, carbamoyl, alkoxycarbonyl, haloalkoxycarbonyl, amino, amidinoamino, alkoxycarbonyl-substituted amidinoamino, alkoxycarbonylamino, haloalkoxycarbonylamino, cycloalkyl, and halocycloalkyl; 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, hydroxy, alkoxy, and haloalkoxy; or is aryl, A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section B9C] R3 is C 1-12 alkyl; Hydroxy, C 1-6 Alkoxy, C 1-6 Haloalkoxy, TriC 1-6 Alkylsilyloxy, carboxy, carbamoyl, C 1-6 Alkoxycarbonyl, C 1-6 Haloalkoxycarbonyl, amino, amidinoamino, C 1-6Alkoxycarbonyl-substituted amidinoamino, C 1-6 Alkoxycarbonylamino, C 1-6 Haloalkoxycarbonylamino, C 3-10 Cycloalkyl, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of halocycloalkyl 1-12 alkyl; C 6-10 Aryl C 1-6 alkyl; Halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, hydroxy, C 1-6 Alkoxy, and C 1-6 C substituted with 1 to the maximum possible number of identical or different substituents selected from the group consisting of haloalkoxy 6-10 Aryl C 1-6 alkyl; or C 6-10 is aryl, A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section B10A]R 2A and R 2B are each independently hydrogen; alkyl; alkyl substituted with from one to the maximum possible number of identical or different substituents selected from the group consisting of hydroxy, substituted oxy, amino, substituted amino, cycloalkyl, and substituted cycloalkyl; 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, and substituted oxy; cycloalkyl; substituted cycloalkyl; heterocycloalkyl; or substituted heterocycloalkyl, wherein the substituted oxy, substituted amino, substituted alkyl, substituted cycloalkyl, and substituted heterocycloalkyl each independently have from 1 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; A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section B10B]R 2A and R 2B are each independently hydrogen; alkyl; alkyl substituted with from one to the maximum possible number of identical or different substituents selected from the group consisting of hydroxy, alkoxy, carboxy, alkoxycarbonyl, amino, amidinoamino, alkoxycarbonyl-substituted amidinoamino, alkoxycarbonylamino, cycloalkyl, and halocycloalkyl; 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, hydroxy, alkoxy, and haloalkoxy; cycloalkyl; alkyl-substituted cycloalkyl; or 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; A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section B10C]R 2A and R 2B are each independently hydrogen; C 1-12 alkyl; Hydroxy, C 1-6 Alkoxy, carboxy, C 1-6 Alkoxycarbonyl, amino, amidinoamino, C 1-6 Alkoxycarbonyl-substituted amidinoamino, and C 1-6 Alkoxycarbonylamino, C 3-10 Cycloalkyl, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of halocycloalkyl 1-12 alkyl; C 6-10 Aryl C 1-6 alkyl; Halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, hydroxy, C 1-6 Alkoxy, and C 1-6 C substituted with 1 to the maximum possible number of identical or different substituents selected from the group consisting of haloalkoxy 6-10 Aryl C 1-6 alkyl; C 3-10 cycloalkyl; C 1-6 Alkyl-substituted C 3-10 cycloalkyl; or a 5- to 10-membered heterocycloalkyl; 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 substitutable number of identical or different substituents selected from Substituent Group VI; A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item B11A] R4 is hydrogen, alkyl, or substituted alkyl, wherein the substituted alkyl has one or up to the maximum possible number of identical or different substituents selected from the group consisting of halogen, carboxy, carbamoyl, amino, alkylamino, aryl, nitroaryl, and alkoxycarbonylamino; A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item B11B] R4 is hydrogen or alkyl; A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item B11C] R4 is hydrogen or C 1-12 is alkyl, A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item B12A] R1 is hydrogen, methyl, propyl, isopropyl, isobutyl, sec-butyl, isopentyl, hexyl, (tert-butoxycarbonyl-substituted amidinoamino)propyl, tert-butoxyethyl, tert-butoxypropyl, tert-butoxycarbonylethyl, carboxyethyl, hydroxyethyl, hydroxypropyl, tert-butoxycarbonylaminopropyl, cyclopentylmethyl, cyclohexylmethyl, 5,6,7,8-tetrahydronaphthalenylmethyl, benzyl, 2-phenylethyl, naphthalenylmethyl, fluorobenzyl, chlorobenzyl, methylbenzyl, dimethylbenzyl, tert-butylbenzyl, methoxybenzyl, ethoxybenzyl, tert-butoxybenzyl, (trifluoromethoxy)benzyl, aminobenzyl, (dimethylamino)benzyl, (cyclopentylcarbonylamino)benzyl, nitrobenzyl, hydroxybenzyl, cyclohexyl, isovaleryl, phenylacetyl, benzoyl, isopropyloxycarbonyl, phenoxycarbonyl, or tetrahydro-2H-pyranyl; A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Section B12B]R 2A is hydrogen, R 2B is isopropyl, isobutyl, sec-butyl, pentyl, isopentyl, hexyl, heptyl, amidinoaminopropyl, (tert-butoxycarbonyl-substituted amidinoamino)propyl, (tert-butoxycarbonyl)ethyl, tert-butoxyethyl, carboxyethyl, hydroxyethyl, (tert-butoxycarbonylamino)propyl, cyclopentylmethyl, cyclohexylmethyl, (1,2,3,4-tetrahydronaphthalenyl)methyl, 2,2,6,6-tetramethylpiperidinyl, benzyl, phenylethyl, naphthalenylmethyl, fluorobenzyl, chlorobenzyl, (fluorophenyl)ethyl, methylbenzyl, tert-butoxybenzyl, hydroxybenzyl, β-hydroxyphenethyl, α-hydroxymethylphenethyl, cyclopentyl, cyclohexyl, or methylcyclohexyl; or R 2A and R 2B together with the nitrogen atom to which they are attached form a pyrrolidine ring, A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item B12C] R3 is propyl, isobutyl, isopentyl, hexyl, amidinoaminopropyl, (tert-butoxycarbonyl-substituted amidinoamino)propyl, (tert-butoxycarbonyl)ethyl, carboxyethyl, hydroxyethyl, (tert-butyldimethylsilyloxy)ethyl, (tert-butoxycarbonylamino)propyl, cyclopentylmethyl, cyclohexylmethyl, cyclohexylethyl, benzyl, naphthalenylmethyl, naphthalenylethyl, chlorobenzyl, (methylphenyl)ethyl, (isopropylphenyl)ethyl, tert-butoxybenzyl, hydroxybenzyl, or phenyl; A compound according to any one of the above items, an enantiomer thereof, a salt thereof, or a solvate thereof. [Item B12D] 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 methyl. [Item B13A] The compound according to any one of the above items, wherein the compound is a compound selected from the group consisting of compound numbers I-1 to I-50, II-1 to II-50, IF-51 to IF-411, and IB-51 to IB-425, or an enantiomer thereof, or a salt thereof, or a solvate thereof. [Item B12] An antiviral agent against lyssaviruses, comprising the compound according to any one of the above items or a pharmaceutically acceptable salt thereof. [Item B13] The antiviral agent according to any one of the above items, wherein the Lyssavirus virus includes rabies virus. [Item B14] A pharmaceutical composition comprising the compound according to any one of the above items or a pharmaceutically acceptable salt thereof. [Item B15] The pharmaceutical agent according to any one of the above items, which is a preventive or therapeutic agent for rabies. [Item B16] 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 B17] 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 B18] A method for preventing or treating rabies, comprising administering to a patient in need of prevention or treatment a therapeutically effective amount of a compound or a pharmaceutically acceptable salt thereof according to any one of the above items, an antiviral agent according to any one of the above items, a medicine according to any one of the above items, or a pharmaceutical composition according to any one of the above items. [Item B19] 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.

[0011] 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]

[0012] 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. DETAILED DESCRIPTION OF THE INVENTION

[0013] 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.

[0014] (definition) First, we explain the terms and general techniques used in this disclosure.

[0015] 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.

[0016] 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.

[0017] 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 11 for a naphthalenylethyl group.

[0018] 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.

[0019] 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.

[0020] 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-L X -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-L X -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-LX -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 Xis a single bond or unsubstituted or substituted alkylene, and 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 aforementioned 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, alkynylcarbonyl Amino, 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-L X -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 from 1 to the maximum possible number of substituents selected from the group consisting of aryl, aryl, aryl- ...

[0021] 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 3-10Cycloalkyl-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 C 1-12 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-LX -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 C 2-12 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 6-10 Aryl-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 C2-12 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-L X -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 C3-10 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 1-12 Alkyloxycarbonylamino, 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- to 10-membered heterocycloalkyl-L X -sulfinyl, unsubstituted or substituted C 1-12 Alkylcarbamoyl, unsubstituted or substituted C 2-12 Alkenylcarbamoyl, unsubstituted or substituted C 2-12 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-LX -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, C 2-12 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 3-10Cycloalkyloxyalkyl, 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 2-12 Alkenylcarbonyloxy, 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 1-12Alkylcarbonylthio, 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, C 2-12 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, C6-10 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 3-10 Cycloalkyl-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-LX -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- ...

[0022] 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, aryl, haloaryl, 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 1-12Alkylcarbonylamino, 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 6-10 Aryl, C 6-10 Haloaryl, 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.

[0023] 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 C1-6 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.

[0024] 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.

[0025] 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.

[0026] 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 13c , R 13d , R 13e , R 13f , R 13g , R 13h , 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 10t , R 10u , R 10v , R 10w , R 10x , R 10y , R 10z1 , R 10z2 , R10z3 , R 11a , R 11b , R 11c , R 11d , R 11e , R 11i , R 11j , R 11k , R 11l , R 11m , R 11q , R 11r , R 11s , R 11t , R 11u , R 11v , R 11w , R 12a , R 12c , R 12d , R 12f , R 12g , R 12h , R 12i , R 14 , R 15a , R 15b , R 15c , R 15d , R 15e , R 15f , R 15g , R 15h , R 15i , R 16a , R 16b , R 16c , R 16d , R 16e , R 16f , 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 1-6 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 the substituent groups α1 and β1 may be substituted with a protecting group.

[0027] 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 (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 13b , R 13c , R 13d , R 13e , R 13f , R 13g , R 13hare 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 10i , R 10j , R 11a , R 11b , R 11c , R 11d , R 11e , R 11f , R 11f2 , R 11g , R 11h , R 11i , R 12a , R 12b , R 12c , R 15a , R 15b , R 15c , R 15d , R 15e , R 15f , R 15g , R 15h , R 16a , R 16b , R 16c , R 16d , R 16e , 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 1-6It 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.

[0028] 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)NR10d 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)-NR 17a -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 13b , R 13c , R 13d , R 13e , R 13f , R13g , 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 10h , R 11a , R 11b , R 11c , R 11d , R 11e , R 11f , R 11g , R 12a , R 12b , R 15a , R 15b , R 15c , R 15d , R 15e , R 15f , R 15g , R 15h , R 16a , R 16b , R 16c , R 16d , R 16e , 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 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 substituent groups α3 and β3 may be substituted with a protecting group.

[0029] 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.

[0030] 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 are also within the scope of the present disclosure.

[0031] 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.

[0032] 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.

[0033] 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)).

[0034] As used herein, a "halogen atom" refers to an atom belonging to the halogen group, such as a fluorine atom, chlorine atom, bromine atom, or iodine atom. A fluorine atom or a chlorine atom is preferred. A "halogen atom" may also be referred to as "halogen" or "halo."

[0035] As used herein, a "hydroxyl group" refers to a monovalent group of -OH. This group may also be called a "hydroxy group" or "hydroxy."

[0036] 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."

[0037] As used herein, a "cyano group" is a monovalent radical of -CN.

[0038] As used herein, "amino" refers to the monovalent radical -NH. This group may also be referred to as an "amino group."

[0039] 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. 1-12 "Alkyl" is an alkyl group having 1 to 12 carbon atoms. 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". 1-4Specific examples of "alkyl" include methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, tert-butyl, sec-butyl, etc. 1-6 Specific examples of "alkyl" include C 1-4 Examples of alkyl include, but are not limited to, alkyl, n-pentyl, isopentyl, neopentyl, tert-pentyl, 1,2-dimethylpropyl, n-hexyl, and the like. 1-12 Specific examples of "alkyl" include C 1-6 Examples include, but are not limited to, alkyl, n-heptyl, isoheptyl, n-octyl, isooctyl, n-nonyl, n-decanyl, n-undecyl, n-dodecyl, and the like.

[0040] 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.

[0041] 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 "C alkynyl" is an example. 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.

[0042] 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 10 Examples 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.

[0043] 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.

[0044] 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 C6-10 Aryl-substituted C 1-6 It means alkyl. 6-10 Aryl C 1-6 Illustrative examples of alkyl include, but are not limited to, benzyl (i.e., phenyl-CH2-), phenethyl (i.e., phenyl-CH2CH2-), 1-phenylethyl, naphthalen-1-ylmethyl, naphthalen-2-ylmethyl, 2-(naphthalen-1-yl)ethyl, 2-(naphthalen-2-yl)ethyl, 1-(naphthalen-1-yl)ethyl, 1-(naphthalen-2-yl)ethyl, and the like.

[0045] 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, C 3-6 It may be substituted with cycloalkylcarbonyl or the like. (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.

[0046] 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.

[0047] 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.

[0048] 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.

[0049] 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.

[0050] 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.

[0051] 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 1-6 Specific 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, 1H-indol-3-ylmethyl, 2-(1H-indol-3-yl)ethyl, and the like.

[0052] 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. 3-20As 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.

[0053] 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.

[0054] As used herein, "C 3-10 The "alicyclic group" is defined as "C 3-20 Alicyclic group" 3-10 The term "alicyclic group" refers to a substituent in which the alicyclic group is a monovalent group.

[0055] 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 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 "C3-5 "C 3-6 Specific examples of "alicyclicoxy" include, but are not limited to, cyclopropyloxy, cyclobutyloxy, cyclopentyloxy, cyclohexyloxy, and the like.

[0056] 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.

[0057] 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.

[0058] 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.

[0059] 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 Specific examples of cycloalkyl include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl. 3-10 "Cycloalkyl" means a monocyclic or bicyclic cycloalkyl having 3 to 10 carbon atoms. 3-10 Specific examples of cycloalkyl include C 3-6 Examples include, but are not limited to, cycloalkyl, cycloheptyl, cyclooctyl, cyclononyl, cyclodecyl, bicyclo[4.1.0]heptyl, bicyclo[3.3.0]octyl, bicyclo[4.2.0]octyl, bicyclo[4.3.0]nonyl, decahydronaphthyl, and the like.

[0060] 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.

[0061] As used herein, "cycloalkylalkyl" refers to an alkyl substituted with at least one cycloalkyl. 3-10 Cycloalkyl C 1-6 "Alkyl" has at least one C 3-10 Cycloalkyl-substituted C 1-6 It means alkyl, and "C 3-6 Cycloalkyl C 1-6 "Alkyl" has at least one C 3-6Cycloalkyl-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. 3-10 Cycloalkyl C 1-6 Specific examples of alkyl include C 3-6 Cycloalkylmethyl, C 3-6 Examples include, but are not limited to, cycloalkylethyl, cycloheptylmethyl, cycloheptylethyl, cyclooctylmethyl, cyclooctylethyl, cyclononylmethyl, cyclononylethyl, cyclodecylmethyl, cyclodecylethyl and the like.

[0062] 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.

[0063] 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, C6-10 A 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. 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.

[0064] 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".

[0065] As used herein, the non-aryl heterocyclic moiety of "non-aryl heterocyclic oxy" has the same meaning as the above-mentioned "4- to 10-membered 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.

[0066] 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.

[0067] 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.

[0068] 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.

[0069] As used herein, "5- or 6-membered heterocycloalkyl" and "5- to 6-membered heterocycloalkyl" refer to a heterocycloalkyl consisting of 5 to 6 ring atoms containing one or more identical or different heteroatoms selected from oxygen atoms, nitrogen atoms, and sulfur atoms.

[0070] As used herein, "heterocycloalkylalkyl" refers to an alkyl substituted with at least one heterocycloalkyl.

[0071] As used herein, "alkylcarbonyl" refers to a monovalent group of -C(=O)-alkyl. Preferred examples of alkylcarbonyl include C 1-6 Examples include alkylcarbonyl. 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.

[0072] 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.

[0073] 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.

[0074] 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.

[0075] 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.

[0076] 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.

[0077] 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.

[0078] 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, n-propylthio, n-butylthio, isopropylthio, isobutylthio, tert-butylthio, sec-butylthio, isopentylthio, neopentylthio, tert-pentylthio, 1,2-dimethylpropylthio, and the like.

[0079] 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.

[0080] 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.

[0081] As used herein, a "heteroarylcarbonyl" is a monovalent radical of -C(=O)-heteroaryl.

[0082] 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.

[0083] 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.

[0084] 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.

[0085] 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 the above-mentioned "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.

[0086] 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.

[0087] 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.

[0088] 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.

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

[0090] As used herein, "amidinoamino" refers to the monovalent group -NH-C(=NH)-NH. An "amidinoamino" group may also be referred to as a "guanidino" group or a "guanidyl" group, and these terms are used interchangeably.

[0091] 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.

[0092] 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 1-4Examples of carbamoyl-substituted C include, but are not limited to, alkyl, 6-amino-6-oxohexyl (i.e., HNC(=O)-(CH)-, or carbamoylpentyl), 7-amino-7-oxoheptyl (i.e., HNC(=O)-(CH)-, or carbamoylhexyl), and the like. 1-4 Specific 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.

[0093] 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.

[0094] 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 Examples of carboxy-substituted C include, but are not limited to, alkyl, 5-carboxypentyl, 6-carboxyhexyl, and the like. 1-4 Specific examples of "alkyl" include, but are not limited to, carboxymethyl, 2-carboxyethyl, 3-carboxypropyl, 4-carboxybutyl, and the like.

[0095] As used herein, an "arylalkyl substituted with an alkyl-substituted amino" refers to an arylalkyl substituted with at least one alkyl-substituted amino. 1-6 Specific examples of alkyl-substituted amino include, but are not limited to, -NH(CH), -N(CH), -NH(CHCH), -N(CHCH), -NH((CH)CH), -N((CH)CH), -NH(CH(CH), -N(CH(CH), -NH((CH)CH), -N((CH)CH), -NH(CHCH(CH), -N(CHCH(CH), -NH((CH)CH), -N((CH)CH), -NH((CH)CH), -N((CH)CH), -NH((CH)CH), -N((CH)CH), -NH((CH)CH), -N((CH)CH), and the like. As used herein, "alkyl-substituted amino" is synonymous with "alkylamino."

[0096] 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.

[0097] 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.

[0098] 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 (such as a silyl ether) described herein, and the protected substituent may be used as a substituent.

[0099] (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.

[0100] 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; 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, R2A or R 2B is hydrogen, it is understood that the same definition as R2 described herein may be adopted.

[0101] In another aspect, compounds of the present disclosure have the 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.

[0102] In one embodiment, the alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, and carbonyl of R, R, and R are each independently optionally substituted with from 1 to the maximum possible number of identical or different substituents selected from Substituent Group I; 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 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 2Bare 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 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.

[0104] In one embodiment, R, R and R 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 1-12 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 5- to 10-membered non-aryl heterocycle or a 5- to 10-membered heteroaryl ring, wherein the non-aryl heterocycle and the heteroaryl ring are each independently optionally substituted.

[0105] In one embodiment, R1, R3, and R4 are each independently: hydrogen, optionally substituted alkyl, optionally substituted arylalkyl; optionally substituted heteroarylalkyl; optionally substituted cycloalkyl; optionally substituted heterocycloalkyl; optionally substituted aryl; 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; Here, the above groups of R1, R3 and R4 are optionally substituted with one to the maximum possible number of identical or different substituents selected from Substituent Group II; R 2A and R 2B 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; where R 2A and R 2B is 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 together with the nitrogen atom to which they are attached form a non-aryl heterocycle or heteroaryl ring; Here, the non-aryl heterocycle and the heteroaryl ring may each independently be substituted with one to the maximum possible number of identical or different substituents selected from Substituent Group II.

[0106] In one embodiment, R, R and R are each independently hydrogen, optionally substituted alkyl, optionally substituted arylalkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, 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 of R, R and R are optionally substituted with 1 to a maximum 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 is 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 together with the nitrogen atom to which they are attached form a non-aryl heterocycle or a heteroaryl ring, wherein the non-aryl heterocycle and the heteroaryl ring are each independently optionally substituted with one to the maximum possible number of identical or different substituents selected from Substituent Group II.

[0107] In one embodiment, R1, R3, and R4 are each independently: hydrogen, C substituted as needed 1-12 Alkyl, C substituted as needed 6-10 Aryl C 1-12 Alkyl, Optionally substituted 5- to 10-membered heteroaryl C1-12 Alkyl, C substituted as needed 3-10 cycloalkyl, optionally substituted 5- to 10-membered heterocycloalkyl; C substituted as needed 6-10 aryl, Formyl, C substituted as needed 1-12 alkylcarbonyl, C substituted as needed 1-12 alkoxycarbonyl, C substituted as needed 6-10 arylcarbonyl, C substituted as needed 6-10 aryloxycarbonyl, optionally substituted 5- to 10-membered heteroarylcarbonyl; optionally substituted 5- to 10-membered heteroaryloxycarbonyl; C substituted as needed 3-10 cycloalkylcarbonyl, C substituted as needed 3-10 cycloalkyloxycarbonyl, optionally substituted 5- to 10-membered heterocycloalkylcarbonyl; optionally substituted 5- to 10-membered heterocycloalkyloxycarbonyl; Carbamoyl, C substituted as needed 1-12 alkylcarbamoyl, C substituted as needed 1-12 alkoxycarbamoyl, C substituted as needed 6-10 arylcarbamoyl, optionally substituted 5- to 10-membered heteroarylcarbamoyl; C substituted as needed 3-10 cycloalkylcarbamoyl, or optionally substituted 5- to 10-membered heterocycloalkylcarbamoyl; wherein the above groups of R1, R3 and R4 are optionally substituted with one to the maximum substitutable number of identical or different substituents selected from Substituent Group III; R 2A and R 2B are each independently hydrogen, C substituted as needed 1-12 Alkyl, C substituted as needed 6-10 Aryl C 1-12 Alkyl, C substituted as needed 3-10 cycloalkyl, optionally substituted 5- to 10-membered heterocycloalkyl; Formyl, C substituted as needed 1-12 alkylcarbonyl, C substituted as needed 1-12 alkoxycarbonyl, C substituted as needed 6-10 arylcarbonyl, C substituted as needed 6-10 aryloxycarbonyl, optionally substituted 5- to 10-membered heteroarylcarbonyl; optionally substituted 5- to 10-membered heteroaryloxycarbonyl; C substituted as needed 3-10 cycloalkylcarbonyl, C substituted as needed 3-10 cycloalkyloxycarbonyl, optionally substituted 5- to 10-membered heterocycloalkylcarbonyl; optionally substituted 5- to 10-membered heterocycloalkyloxycarbonyl; Carbamoyl, C substituted as needed 1-12 alkylcarbamoyl, C substituted as needed 1-12 alkoxycarbamoyl, C substituted as needed 6-10 arylcarbamoyl, optionally substituted 5- to 10-membered heteroarylcarbamoyl; C substituted as needed 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 possible number of identical or different substituents selected from Substituent Group III, or R 2A and R 2B together with the nitrogen atom to which they are attached form a 5- to 10-membered non-aryl heterocycle or a 5- to 10-membered heteroaryl ring, Here, the non-aryl heterocycle and the 5- to 10-membered heteroaryl ring may each independently be substituted with one to the maximum possible number of identical or different substituents selected from Substituent Group V.

[0108] In one embodiment, R, R 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 3-10 Cycloalkyl, optionally substituted 5- to 10-membered heterocycloalkyl, optionally substituted C 6-10 Aryl, 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 3-10Cycloalkyloxycarbonyl, 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 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 6-10 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 1-12Alkoxycarbamoyl, 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 possible number of identical or different substituents selected from Substituent Group III, or R 2A and R 2B together with the nitrogen atom to which they are bonded, form a 5- to 10-membered non-aryl heterocycle or a 5- to 10-membered heteroaryl ring, wherein the non-aryl heterocycle and the 5- to 10-membered heteroaryl ring are each independently optionally substituted with one to the maximum possible number of identical or different substituents selected from Substituent Group V.

[0109] In one embodiment, R1 and R4 are each independently: hydrogen, optionally substituted alkyl, optionally substituted arylalkyl; optionally substituted heteroarylalkyl; optionally substituted cycloalkyl; optionally substituted heterocycloalkyl; 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; Here, the above groups of R1 and R4 are optionally substituted with the same or different substituents selected from Substituent Group III, up to the maximum substitutable number.

[0110] In one embodiment, R and 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 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.

[0111] In one embodiment, R1 and R4 are each independently: hydrogen, C substituted as needed 1-12 Alkyl, C substituted as needed 6-10 Aryl C 1-12 Alkyl, Optionally substituted 5- to 10-membered heteroaryl C 1-12 Alkyl, C substituted as needed 3-10 cycloalkyl, optionally substituted 5- to 10-membered heterocycloalkyl; Formyl, C substituted as needed 1-12 alkylcarbonyl, C substituted as needed 1-12 alkoxycarbonyl, C substituted as needed 6-10 arylcarbonyl, C substituted as needed 6-10 aryloxycarbonyl, C substituted as needed 3-10 cycloalkylcarbonyl, C substituted as needed 3-10 cycloalkyloxycarbonyl, optionally substituted 5- to 10-membered heterocycloalkylcarbonyl; optionally substituted 5- to 10-membered heterocycloalkyloxycarbonyl; Carbamoyl, C substituted as needed 1-12 alkylcarbamoyl, C substituted as needed 1-12 alkoxycarbamoyl, C substituted as needed 6-10 arylcarbamoyl, optionally substituted 5- to 10-membered heteroarylcarbamoyl; C substituted as needed 3-10 cycloalkylcarbamoyl, or optionally substituted 5- to 10-membered heterocycloalkylcarbamoyl; Here, the above groups of R1 and R4 are optionally substituted with the same or different substituents selected from Substituent Group III, up to the maximum substitutable number.

[0112] In one embodiment, R and 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 1-12 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 R4 are optionally substituted with 1 to the maximum substitutable number of identical or different substituents selected from Substituent Group III.

[0113] In one embodiment, R1 and R4 are each independently: hydrogen, optionally substituted alkyl, optionally substituted arylalkyl; optionally substituted heteroarylalkyl; optionally substituted heterocycloalkyl; Formyl, optionally substituted alkylcarbonyl; optionally substituted alkoxycarbonyl; an optionally substituted arylcarbonyl, or optionally substituted aryloxycarbonyl; Here, the above groups of R1 and R4 are optionally substituted with the same or different substituents selected from Substituent Group III, up to the maximum substitutable number.

[0114] In one embodiment, R1 and R4 are each independently hydrogen, optionally substituted alkyl, optionally substituted arylalkyl, optionally substituted heterocycloalkyl, formyl, optionally substituted alkylcarbonyl, optionally substituted alkoxycarbonyl, optionally substituted arylcarbonyl, or optionally substituted aryloxycarbonyl, 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.

[0115] In one embodiment, R1 and R4 are each independently: hydrogen, C substituted as needed 1-12 Alkyl, C substituted as needed 6-10 Aryl C 1-12 Alkyl, Optionally substituted 5- to 10-membered heteroaryl C 1-12 Alkyl, optionally substituted 5- to 10-membered heterocycloalkyl; Formyl, C substituted as needed 1-12 alkylcarbonyl, C substituted as needed 1-12 alkoxycarbonyl, C substituted as needed 6-10 arylcarbonyl, C substituted as needed 6-10 aryloxycarbonyl, Here, the above groups of R1 and R4 are optionally substituted with the same or different substituents selected from Substituent Group III, up to the maximum substitutable number.

[0116] In one embodiment, R1 and R4 are each independently: hydrogen, C substituted as needed 1-12 Alkyl, C substituted as needed 6-10 Aryl C 1-6 Alkyl, Optionally substituted 5- to 10-membered heteroaryl C 1-6 Alkyl, optionally substituted 5- to 10-membered heterocycloalkyl; Formyl, C substituted as needed 1-12 alkylcarbonyl, C substituted as needed 1-12 alkoxycarbonyl, C substituted as needed 6-10 arylcarbonyl, C substituted as needed 6-10 aryloxycarbonyl, Here, the above groups of R1 and R4 are optionally substituted with the same or different substituents selected from Substituent Group III, up to the maximum substitutable number.

[0117] In one embodiment, R and R are each independently selected from hydrogen, optionally substituted C 1-12 Alkyl, optionally substituted C 6-10 Aryl C 1-6 Alkyl, optionally substituted 5-10 membered heterocycloalkyl, formyl, optionally substituted C1-12 Alkylcarbonyl, optionally substituted C 1-12 Alkoxycarbonyl, optionally substituted C 6-10 Arylcarbonyl, optionally substituted C 6-10 Aryloxycarbonyl, 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.

[0118] In one embodiment, R1 is hydrogen; alkyl; alkyl substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of hydroxy, substituted oxy, formyl, substituted carbonyl, amino, substituted amino, and cycloalkyl, and substituted cycloalkyl; arylalkyl; arylalkyl substituted with 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; heteroarylalkyl; heteroarylalkyl substituted with 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; cycloalkyl; substituted cycloalkyl; heterocycloalkyl; substituted heterocycloalkyl; or and a substituted carbonyl, wherein the substituted oxy, substituted carbonyl, substituted amino, substituted cycloalkyl, substituted heterocycloalkyl, and substituted alkyl each independently have from 1 to the maximum possible number of identical or different substituents selected from Substituent Group IV.

[0119] In one embodiment, R1 is hydrogen, Alkyl, alkyl substituted with from one to the maximum possible number of identical or different substituents selected from the group consisting of hydroxy, substituted oxy, formyl, substituted carbonyl, amino, substituted amino, and cycloalkyl, and substituted cycloalkyl; aryl alkyl, arylalkyl substituted with 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; and cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, or substituted carbonyl, wherein the substituted oxy, substituted carbonyl, substituted amino, substituted cycloalkyl, substituted heterocycloalkyl, and substituted alkyl each independently have from 1 to the maximum possible number of identical or different substituents selected from Substituent Group IV.

[0120] In one embodiment, R1 is hydrogen; alkyl; Alkyl substituted with from 1 to the maximum possible number of identical or different substituents selected from the group consisting of hydroxy, alkoxy, haloalkoxy, formyl, carboxy, carbamoyl, alkylcarbonyl, alkoxycarbonyl, amino, amidinoamino, alkoxycarbonyl-substituted amidinoamino, alkoxycarbonylamino, cycloalkyl, and halocycloalkyl; arylalkyl; arylalkyl substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of halogen, alkyl, haloalkyl, hydroxy, alkoxy, haloalkoxy, arylalkoxy, amino, alkylamino, (alkyl)2amino, cycloalkylcarbonylamino, and nitro; heteroarylalkyl; heteroarylalkyl substituted with 1 to the maximum possible number of identical or different substituents selected from the group consisting of halogen, alkyl, haloalkyl, hydroxy, alkoxy, haloalkoxy, arylalkoxy, amino, alkylamino, (alkyl)2amino, cycloalkylcarbonylamino, and nitro; cycloalkyl; Halocycloalkyl; heterocycloalkyl; Alkyl carbonyl; Arylalkylcarbonyl; Alkoxycarbonyl; arylcarbonyl; or It is aryloxycarbonyl.

[0121] In one embodiment, R1 is hydrogen, Alkyl, an alkyl substituted with from one to the maximum possible number of identical or different substituents selected from the group consisting of hydroxy, alkoxy, haloalkoxy, formyl, carboxy, carbamoyl, alkylcarbonyl, alkoxycarbonyl, amino, amidinoamino, alkoxycarbonyl-substituted amidinoamino, alkoxycarbonylamino, cycloalkyl, and halocycloalkyl; aryl alkyl, arylalkyl substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of halogen, alkyl, haloalkyl, hydroxy, alkoxy, haloalkoxy, amino, alkylamino, (alkyl)2amino, cycloalkylcarbonylamino, and nitro; It is cycloalkyl, halocycloalkyl, heterocycloalkyl, alkylcarbonyl, arylalkylcarbonyl, alkoxycarbonyl, arylcarbonyl, or aryloxycarbonyl.

[0122] In one embodiment, R1 is hydrogen; C 1-12 alkyl; C 1-12 Alkoxy, C 1-12 Haloalkoxy, formyl, carboxy, carbamoyl, C 1-12 Alkyl carbonyl, C 1-12 Alkoxycarbonyl, C 1-12 Haloalkoxycarbonyl, amidinoamino, C 1-12 Alkoxycarbonyl-substituted amidinoamino, C 1-12 Alkoxycarbonylamino, hydroxy, C 3-10 Cycloalkyl, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of halocycloalkyl 1-12 alkyl; C 6-10 Aryl C 1-12 alkyl; Halogen, C 1-12 Alkyl, C 1-12 Haloalkyl, hydroxy, C 1-12 Alkoxy, C 1-12 Haloalkoxy, C 6-10 Aryl C 1-12 Alkoxy, Amino, C 1-12 Alkylamino, (C 1-12 Alkyl)2amino, C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkylcarbonylamino, nitro, and hydroxy 6-10 Aryl C 1-12 alkyl; 5-10 membered heteroaryl C 1-12 alkyl; Halogen, C 1-12 Alkyl, C 1-12 Haloalkyl, hydroxy, C 1-12 Alkoxy, C 1-12 Haloalkoxy, C 6-10 Aryl C 1-12 Alkoxy, Amino, C 1-12 Alkylamino, (C 1-12 Alkyl)2amino, C 3-105-10 membered heteroaryl C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkylcarbonylamino, nitro, and hydroxy 1-12 alkyl; C 3-10 cycloalkyl; 5-10 membered heterocycloalkyl; C 1-12 Alkyl carbonyl; C 6-10 Aryl C 1-12 Alkyl carbonyl; C 1-12 Alkoxycarbonyl; C 6-10 arylcarbonyl; or C 6-10 It is aryloxycarbonyl.

[0123] In one embodiment, R1 is hydrogen; C 1-12 alkyl; C 1-6 Alkoxy, C 1-6 Haloalkoxy, formyl, carboxy, carbamoyl, C 1-6 Alkyl carbonyl, C 1-6 Alkoxycarbonyl, C 1-6 Haloalkoxycarbonyl, amidinoamino, C 1-6 Alkoxycarbonyl-substituted amidinoamino, C 1-6 Alkoxycarbonylamino, hydroxy, C 3-10 Cycloalkyl, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of halocycloalkyl 1-12 alkyl; C 6-10 Aryl C 1-6 alkyl; Halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, hydroxy, C 1-6 Alkoxy, C 1-6 Haloalkoxy, C 6-10 Aryl C1-6 Alkoxy, Amino, C 1-6 Alkylamino, (C 1-6 Alkyl)2amino, C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkylcarbonylamino, nitro, and hydroxy 6-10 Aryl C 1-6 alkyl; Halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, hydroxy, C 1-6 Alkoxy, C 1-6 Haloalkoxy, C 6-10 Aryl C 1-6 Alkoxy, Amino, C 1-6 Alkylamino, (C 1-6 Alkyl)2amino, C 3-10 5-10 membered heteroaryl C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkylcarbonylamino, nitro, and hydroxy 1-6 alkyl; C 3-10 cycloalkyl; 5-10 membered heterocycloalkyl; C 1-6 Alkyl carbonyl; C 6-10 Aryl C 1-6 Alkyl carbonyl; C 1-6 Alkoxycarbonyl; C 6-10 arylcarbonyl; or C 6-10 It is aryloxycarbonyl.

[0124] In one embodiment, R1 is hydrogen, C 1-12 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkoxy, formyl, carboxy, carbamoyl, C 1-6 Alkyl carbonyl, C 1-6 Alkoxycarbonyl, C1-6 Haloalkoxycarbonyl, amidinoamino, C 1-6 Alkoxycarbonyl-substituted amidinoamino, C 1-6 Alkoxycarbonylamino, hydroxy, and C 3-10 Cycloalkyl, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of halocycloalkyl 1-12 Alkyl, C 6-10 Aryl C 1-6 Alkyl, Halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, hydroxy, C 1-6 Alkoxy, C 1-6 Haloalkoxy, Amino, C 1-6 Alkylamino, (C 1-6 Alkyl)2amino, C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of cycloalkylcarbonylamino, nitro, and hydroxy 6-10 Aryl C 1-6 Alkyl, C 3-10 Cycloalkyl, 5-10 membered heterocycloalkyl, C 1-6 Alkyl carbonyl, C 6-10 Aryl C 1-6 Alkyl carbonyl, C 1-6 Alkoxycarbonyl, C 6-10 Arylcarbonyl, or C 6-10 It is aryloxycarbonyl.

[0125] In one embodiment, R3 is Alkyl, alkyl substituted with from one to the maximum possible number of identical or different substituents selected from the group consisting of hydroxy, substituted oxy, substituted carbonyl, amino, substituted amino, cycloalkyl, and substituted cycloalkyl; aryl alkyl, 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, and substituted oxy; aryl, or and substituted aryl, wherein the substituted oxy, substituted carbonyl, substituted amino, substituted cycloalkyl, substituted alkyl, and substituted aryl each independently have from 1 to the maximum possible number of identical or different substituents selected from Substituent Group IV.

[0126] In one embodiment, R3 is Alkyl, an alkyl substituted with from 1 to the maximum possible number of identical or different substituents selected from the group consisting of hydroxy, alkoxy, haloalkoxy, trialkylsilyloxy, carboxy, carbamoyl, alkoxycarbonyl, haloalkoxycarbonyl, amino, amidinoamino, alkoxycarbonyl-substituted amidinoamino, alkoxycarbonylamino, haloalkoxycarbonylamino, cycloalkyl, and halocycloalkyl; aryl alkyl, arylalkyl substituted with from one to the maximum possible number of identical or different substituents selected from the group consisting of halogen, alkyl, haloalkyl, hydroxy, alkoxy, and haloalkoxy; or It is aryl.

[0127] In one embodiment, R3 is C 1-12 Alkyl, Hydroxy, C 1-6 Alkoxy, C 1-6 Haloalkoxy, TriC 1-6 Alkylsilyloxy, carboxy, carbamoyl, C 1-6 Alkoxycarbonyl, C 1-6 Haloalkoxycarbonyl, amino, amidinoamino, C 1-6 Alkoxycarbonyl-substituted amidinoamino, C 1-6 Alkoxycarbonylamino, C 1-6Haloalkoxycarbonylamino, C 3-10 Cycloalkyl, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of halocycloalkyl 1-12 Alkyl, C 6-10 Aryl C 1-6 Alkyl, Halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, hydroxy, C 1-6 Alkoxy, and C 1-6 C substituted with 1 to the maximum possible number of identical or different substituents selected from the group consisting of haloalkoxy 6-10 Aryl C 1-6 alkyl, or C 6-10 It is aryl.

[0128] In one embodiment, R 2A and R 2B are each independently hydrogen, Alkyl, alkyl substituted with from one to the maximum possible number of identical or different substituents selected from the group consisting of hydroxy, substituted oxy, amino, substituted amino, cycloalkyl, and substituted cycloalkyl; aryl alkyl, 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, and substituted oxy; cycloalkyl, substituted cycloalkyl, heterocycloalkyl, or substituted heterocycloalkyl; wherein the substituted oxy, substituted amino, substituted alkyl, substituted cycloalkyl, and substituted heterocycloalkyl each independently have from 1 to the maximum possible number of identical or different substituents selected from Substituent Group IV, or R 2A and R 2Btogether 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.

[0129] In one embodiment, R 2A and R 2B are each independently hydrogen, Alkyl, an alkyl substituted with from one to the maximum possible number of identical or different substituents selected from the group consisting of hydroxy, alkoxy, carboxy, alkoxycarbonyl, amino, amidinoamino, alkoxycarbonyl-substituted amidinoamino, alkoxycarbonylamino, cycloalkyl, and halocycloalkyl; aryl alkyl, arylalkyl substituted with from one to the maximum possible number of identical or different substituents selected from the group consisting of halogen, alkyl, haloalkyl, hydroxy, alkoxy, and haloalkoxy; cycloalkyl, alkyl-substituted cycloalkyl or 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.

[0130] In one embodiment, R 2A and R 2B are each independently hydrogen; C 1-12 alkyl; Hydroxy, C 1-12 Alkoxy, carboxy, C 1-12 Alkoxycarbonyl, amino, amidinoamino, C 1-12 Alkoxycarbonyl-substituted amidinoamino, and C 1-12 Alkoxycarbonylamino, C3-10 Cycloalkyl, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of halocycloalkyl 1-12 alkyl; C 6-10 Aryl C 1-12 Alkyl; halogen, C 1-12 Alkyl, C 1-12 Haloalkyl, hydroxy, C 1-12 Alkoxy, and C 1-12 C substituted with 1 to the maximum possible number of identical or different substituents selected from the group consisting of haloalkoxy 6-10 Aryl C 1-12 alkyl; C 3-10 cycloalkyl; C 1-12 Alkyl-substituted C 3-10 cycloalkyl; or a 5- to 10-membered heterocycloalkyl; 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.

[0131] In one embodiment, R 2A and R 2B are each independently hydrogen, C 1-12 Alkyl, Hydroxy, C 1-6 Alkoxy, carboxy, C 1-6 Alkoxycarbonyl, amino, amidinoamino, C 1-6 Alkoxycarbonyl-substituted amidinoamino, and C 1-6 Alkoxycarbonylamino, C 3-10 Cycloalkyl, and C 3-10 C substituted with one to the maximum possible number of identical or different substituents selected from the group consisting of halocycloalkyl 1-12Alkyl, C 6-10 Aryl C 1-6 Alkyl, Halogen, C 1-6 Alkyl, C 1-6 Haloalkyl, hydroxy, C 1-6 Alkoxy, and C 1-6 C substituted with 1 to the maximum possible number of identical or different substituents selected from the group consisting of haloalkoxy 6-10 Aryl C 1-6 Alkyl, C 3-10 cycloalkyl, C 1-6 Alkyl-substituted C 3-10 cycloalkyl, or 5- to 10-membered heterocycloalkyl, 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.

[0132] In one embodiment, R4 is hydrogen, alkyl, or substituted alkyl, wherein said substituted alkyl has one or up to the maximum possible number of identical or different substituents selected from the group consisting of halogen, carboxy, carbamoyl, amino, alkylamino, aryl, nitroaryl, and alkoxycarbonylamino.

[0133] In one embodiment, R4 is hydrogen, alkyl, or substituted alkyl, wherein said substituted alkyl is selected from the group consisting of halogen, carboxy, carbamoyl, amino, C 1-6 Alkylamino, C 6-10 Aryl, nitro-C 6-10 Aryl, and C 1-6 It has one or up to the maximum possible number of identical or different substituents selected from the group consisting of alkoxycarbonylamino.

[0134] In one embodiment, R4 is hydrogen, C 1-12 Alkyl or substituted C 1-12 alkyl, wherein the substituted C 1-12 Alkyl is halogen, carboxy, carbamoyl, amino, C 1-12 Alkylamino, C 6-10 Aryl, nitro-C 6-10 Aryl, and C 1-12 It has one or up to the maximum possible number of identical or different substituents selected from the group consisting of alkoxycarbonylamino.

[0135] In one embodiment, R4 is hydrogen or alkyl.

[0136] In one embodiment, R4 is hydrogen or C 1-12 It is alkyl.

[0137] In one embodiment, R1 is hydrogen, methyl, propyl, isopropyl, isobutyl, sec-butyl, isopentyl, hexyl, amidinoaminopropyl, (tert-butoxycarbonyl-substituted amidinoamino)propyl, tert-butoxyethyl, tert-butoxypropyl, tert-butoxycarbonylethyl, carboxyethyl, hydroxyethyl, hydroxypropyl, tert-butoxycarbonylaminopropyl, cyclopentylmethyl, cyclohexylmethyl, cycloheptylmethyl, 5,6,7,8-tetrahydronaphthalenylmethyl, benzyl, phenylethyl, naphthalenylmethyl, fluorobenzyl, chlorobenzyl, methylbenzyl, dimethylbenzyl, tert-butylbenzyl, methoxybenzyl , ethoxybenzyl, tert-butoxybenzyl, trifluoromethylbenzyl, (trifluoromethoxy)benzyl, benzyloxybenzyl, aminobenzyl, (dimethylamino)benzyl, (cyclopentylcarbonylamino)benzyl, 6-methyl-1H-indol-3-ylmethyl, 6-fluoro-1H-indol-3-ylmethyl, 1-tert-butoxycarbonyl-6-methyl-1H-indol-3-ylmethyl, 1-tert-butoxycarbonyl-6-fluoro-1H-indol-3-ylmethyl, nitrobenzyl, hydroxybenzyl, cyclohexyl, isovaleryl, phenylacetyl, benzoyl, isopropyloxycarbonyl, phenoxycarbonyl, or tetrahydro-2H-pyranyl.

[0138] In one embodiment, R1 is hydrogen, methyl, propyl, isopropyl, isobutyl, sec-butyl, isopentyl, hexyl, (tert-butoxycarbonyl-substituted amidinoamino)propyl, tert-butoxyethyl, tert-butoxypropyl, tert-butoxycarbonylethyl, carboxyethyl, hydroxyethyl, hydroxypropyl, tert-butoxycarbonylaminopropyl, cyclopentylmethyl, cyclohexylmethyl, 5,6,7,8-tetrahydronaphthalenylmethyl, benzyl, 2 -phenylethyl, naphthalenylmethyl, fluorobenzyl, chlorobenzyl, methylbenzyl, dimethylbenzyl, tert-butylbenzyl, methoxybenzyl, ethoxybenzyl, tert-butoxybenzyl, (trifluoromethoxy)benzyl, aminobenzyl, (dimethylamino)benzyl, (cyclopentylcarbonylamino)benzyl, nitrobenzyl, hydroxybenzyl, cyclohexyl, isovaleryl, phenylacetyl, benzoyl, isopropyloxycarbonyl, or phenoxycarbonyl.

[0139] In one embodiment, R 2A is hydrogen, R 2B is isopropyl, isobutyl, sec-butyl, pentyl, isopentyl, hexyl, heptyl, amidinoaminopropyl, (tert-butoxycarbonyl-substituted amidinoamino)propyl, (tert-butoxycarbonyl)ethyl, tert-butoxyethyl, methoxybutyl, carboxyethyl, hydroxyethyl, (tert-butoxycarbonylamino)propyl, cyclopentylmethyl, cyclohexylmethyl, cycloheptylmethyl, (1,2,3,4-tetrahydronaphthalenyl)methyl, 2,2,6,6-tetramethylpiperidinyl, benzyl, phenylethyl, naphthalenylmethyl, fluorobenzyl, chlorobenzyl, (fluorophenyl)ethyl, methylbenzyl, tert-butoxybenzyl, hydroxybenzyl, β-hydroxyphenethyl, α-hydroxymethylphenethyl, cyclopentyl, cyclohexyl, or methylcyclohexyl; or R 2A and R2B together with the nitrogen atom to which they are attached form a pyrrolidine ring.

[0140] In one embodiment, R 2A is hydrogen and R 2B is isopropyl, isobutyl, pentyl, isopentyl, hexyl, heptyl, (tert-butoxycarbonyl-substituted amidinoamino)propyl, tert-butoxyethyl, hydroxyethyl, (tert-butoxycarbonylamino)propyl, cyclopentylmethyl, cyclohexylmethyl, (1,2,3,4-tetrahydronaphthalenyl)methyl, 2,2,6,6-tetramethylpiperidinyl, benzyl, phenylethyl, naphthalenylmethyl, fluorobenzyl, chlorobenzyl, (fluorophenyl)ethyl, methylbenzyl, tert-butoxybenzyl, hydroxybenzyl, β-hydroxyphenethyl, α-hydroxymethylphenethyl, cyclopentyl, cyclohexyl, or methylcyclohexyl, or R 2A and R 2B together with the nitrogen atom to which they are attached form a pyrrolidine ring.

[0141] In one embodiment, R3 is propyl, isobutyl, isopentyl, hexyl, amidinoaminopropyl, (tert-butoxycarbonyl-substituted amidinoamino)propyl, (tert-butoxycarbonyl)ethyl, carboxyethyl, hydroxyethyl, (tert-butyldimethylsilyloxy)ethyl, (tert-butoxycarbonylamino)propyl, cyclopentylmethyl, cyclohexylmethyl, cyclohexylethyl, benzyl, naphthalenylmethyl, phenylethyl, naphthalenylethyl, chlorobenzyl, methylbenzyl, (methylphenyl)ethyl, (isopropylphenyl)ethyl, tert-butoxybenzyl, hydroxybenzyl, or phenyl.

[0142] In one embodiment, R3 is propyl, isobutyl, isopentyl, hexyl, (tert-butoxycarbonyl-substituted amidinoamino)propyl, (tert-butoxycarbonyl)ethyl, carboxyethyl, hydroxyethyl, (tert-butyldimethylsilyloxy)ethyl, (tert-butoxycarbonylamino)propyl, cyclopentylmethyl, cyclohexylmethyl, cyclohexylethyl, benzyl, naphthalenylmethyl, (naphthalenyl)ethyl, chlorobenzyl, (methylphenyl)ethyl, (isopropylphenyl)ethyl, tert-butoxybenzyl, hydroxybenzyl, or phenyl.

[0143] In one embodiment, R4 is hydrogen or C 1-6 In one embodiment, R4 is alkyl. In one embodiment, R4 is hydrogen or methyl. In one embodiment, R4 is hydrogen. In one embodiment, R4 is methyl.

[0144] In one embodiment, R is alkyl, substituted arylalkyl, or substituted heteroarylalkyl; R 2A is hydrogen and R 2B is alkyl, arylalkyl, substituted arylalkyl, or optionally substituted cycloalkylalkyl, R3 is alkyl, and R4 is hydrogen.

[0145] In one embodiment, R1 is alkyl, alkyl-substituted arylalkyl, chloro-substituted arylalkyl, alkoxy-substituted arylalkyl, or heteroarylalkyl substituted with Boc and alkyl, or heteroarylalkyl substituted with Boc and halogen; and R 2A is hydrogen and R 2B is alkyl, arylalkyl, fluoro-substituted arylalkyl, chloro-substituted arylalkyl, or cycloalkylalkyl, and R3 is alkyl.

[0146] In one embodiment, R is C 1-12 Alkyl, C1-12 Alkyl-substituted C 6-10 Aryl C 1-12 Alkyl, chloro-substituted C 6-10 Aryl C 1-12 Alkyl, C 1-12 Alkoxy-substituted C 6-10 Aryl C 1-12 Alkyl, or Boc and C 1-12 5-10 membered heteroaryl C substituted with alkyl 1-12 5-10 membered heteroaryl C substituted with alkyl, or Boc and halogen 1-12 alkyl, and R 2A is hydrogen and R 2B is C 1-12 Alkyl, C 6-10 Aryl C 1-12 Alkyl, Fluoro-substituted C 6-10 Aryl C 1-12 Alkyl, chloro-substituted C 6-10 Aryl C 1-12 Alkyl, or C 3-10 Cycloalkyl C 1-12 alkyl, and R3 is C 1-12 It is alkyl.

[0147] In one embodiment, R1 is isobutyl, isopentyl, methylbenzyl, t-butylbenzyl, chlorobenzyl, methoxybenzyl, 1-tert-butoxycarbonyl-6-methyl-1H-indol-3-ylmethyl, or 6-fluoro-1H-indol-3-ylmethyl; and R 2A is hydrogen and R 2B is isobutyl, benzyl, fluorobenzyl, chlorobenzyl, or cycloheptylmethyl, and R3 is isobutyl or isopentyl.

[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 and R2 are each independently optionally substituted alkyl, optionally substituted cycloalkyl, or optionally substituted heterocycloalkyl; R3 is optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted cycloalkyl, or optionally substituted heterocycloalkyl; X is —NH—.

[0149] In one embodiment, R and R are each independently optionally substituted alkyl, optionally substituted cycloalkyl, or optionally substituted heterocycloalkyl; R3 is optionally substituted alkyl, optionally substituted alkenyl, or optionally substituted aryl.

[0150] In one embodiment, R and R are each independently optionally substituted alkyl, optionally substituted cycloalkyl, or optionally substituted heterocycloalkyl; R3 is optionally substituted alkyl or optionally substituted aryl.

[0151] In one embodiment, R1, R2, and R3 are each independently an alkyl optionally substituted with hydroxyl, carboxyl, carbamoyl, amino, or amidinoamino group, an optionally substituted cycloalkylalkyl, an optionally substituted arylalkyl, or an optionally substituted heteroarylalkyl.

[0152] In one embodiment, R1, R2, and R3 each independently represent alkyl optionally substituted with hydroxyl, carboxyl, carbamoyl, amino, or amidinoamino groups, optionally substituted cycloalkylalkyl, optionally substituted C 6-10 Aryl C 1-6 Alkyl or optionally substituted 5-10 membered heteroarylC 1-6 It is alkyl.

[0153] In one embodiment, R, R, and R each independently represent an alkyl optionally substituted with a hydroxyl group, a carboxyl group, a carbamoyl group, an amino group, or an amidinoamino group, an optionally substituted cycloalkylalkyl, an optionally substituted C arylC 1-6 alkyl, or optionally substituted 5- or 6-membered heteroarylC 1-6 It is alkyl.

[0154] In one embodiment, R1, R2, and R3 are each independently alkyl optionally substituted with hydroxyl, carboxyl, carbamoyl, amino, or amidinoamino, optionally substituted cycloalkylalkyl, optionally substituted benzyl, or optionally substituted 5- or 6-membered heteroarylmethyl.

[0155] In one embodiment, R1, R2, and R3 are each independently alkyl, cycloalkylalkyl, optionally substituted with hydroxyl, carboxyl, carbamoyl, amino, or amidinoamino group, optionally substituted with hydroxyl, carboxyl, carbamoyl, amino, or amidinoamino group, or optionally substituted with 5- or 6-membered heteroarylmethyl.

[0156] In one embodiment, R1 and R2 are each independently selected from the group consisting of C 1-6 Alkyl, C 6-10 Aryl C 1-6 Alkyl, C 1-6 Alkyl-substituted C 6-10 Aryl C 1-6 Alkyl, C1-6 Alkoxy-substituted C 6-10 Aryl C 1-6 Alkyl, C 1-6 Haloalkoxy-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 1-6 C substituted with alkyl-substituted amino 6-10 Aryl C 1-6 Alkyl, C 5-6 Cycloalkyl, C 1-6 Alkyl-substituted C 5-6 cycloalkyl, or optionally substituted 5- or 6-membered heterocyclyl; R3 is C 1-6 Alkyl, C 6-10 Aryl C 1-6 Alkyl, C 1-6 Alkyl-substituted C 6-10 Aryl C 1-6 Alkyl, halogen-substituted C 6-10 Aryl C 1-6 Alkyl, C 1-6 Haloalkoxy-substituted C 6-10 Aryl C 1-6 Alkyl, C 1-6 Alkoxy-substituted C 6-10 Aryl C 1-6 Alkyl, hydroxy-substituted C 6-10 Aryl C 1-6 Alkyl, C 1-6 C substituted with alkyl-substituted amino 6-10 Aryl C 1-6 Alkyl, C 6-10 Aryl, C 1-4 Alkyl-substituted C 6-10 Aryl or halogen-substituted C 6-10 It is aryl.

[0157] In one embodiment, R and R are each independently methyl, n-propyl, isobutyl, isopentyl, benzyl, methyl- or t-butyl-substituted benzyl, fluoro- or chloro-substituted benzyl, methoxy- or ethoxy-substituted benzyl, trifluoromethoxy-substituted benzyl, hydroxy-substituted benzyl, dimethylamino-substituted benzyl, cyclohexyl, methyl-substituted cyclohexyl, tetrahydro-2H-pyran-4-yl, or 2,2,6,6-tetramethylpiperidin-4-yl; R3 is methyl, n-propyl, isobutyl, isopentyl, benzyl, methyl or t-butyl substituted benzyl, fluoro or chloro substituted benzyl, methoxy or ethoxy substituted benzyl, trifluoromethoxy substituted benzyl, hydroxy substituted benzyl, dimethylamino substituted benzyl, or phenyl.

[0158] In one embodiment, R1 and R2 are each independently methyl, ethyl, n-propyl, isopropyl, isobutyl, isopentyl, benzyl, 4-methylbenzyl, 4-(t-butyl)benzyl, 4-fluorobenzyl, 3-chlorobenzyl, 4-chlorobenzyl, 4-methoxybenzyl, 4-ethoxybenzyl, 4-hydroxybenzyl, 3-hydroxybenzyl, 4-(dimethylamino)benzyl, 4-(trifluoromethoxy)benzyl, cyclohexyl, trans-4-methylcyclohexyl, tetrahydro-2H-pyran-4-yl, or 2,2,6,6-tetramethylpiperidin-4-yl; R3 is methyl, ethyl, n-propyl, isopropyl, isobutyl, isopentyl, benzyl, 4-methylbenzyl, 4-(t-butyl)benzyl, 4-fluorobenzyl, 3-chlorobenzyl, 4-chlorobenzyl, 4-methoxybenzyl, 4-ethoxybenzyl, 4-hydroxybenzyl, 3-hydroxybenzyl, 4-(dimethylamino)benzyl, 4-(trifluoromethoxy)benzyl, or phenyl.

[0159] In one embodiment, R and R each independently represent a C optionally substituted with a hydroxyl group, a carboxyl group, a carbamoyl group, an amino group, or an amidinoamino group. 1-6 Alkyl, optionally substituted C 3-6 Cycloalkyl 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 4- to 6-membered heterocycloalkylC 1-6 It is alkyl.

[0160] In one embodiment, R and R each independently represent a C optionally substituted with a hydroxyl group, a carboxyl group, a carbamoyl group, an amino group, or an amidinoamino group. 1-6 Alkyl, optionally substituted C 3-6 Cycloalkyl C 1-6 Alkyl or optionally substituted C 6-10 Aryl C 1-6 It is alkyl.

[0161] In one embodiment, R1 and R2 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, amidinoamino substituted C 1-6 Alkyl, carboxy-substituted 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, 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 1-4Alkoxycarbonyl-substituted C 1-6 Alkyl, C 1-4 C substituted with alkyl-substituted amino 6-10 Aryl C 1-6 Alkyl, or C 3-6 Cycloalkyl C 1-6 It is alkyl.

[0162] In one embodiment, R2 is optionally substituted C 6-10 Aryl C 1-6 In one embodiment, R2 is an optionally substituted C6 arylC 1-6 In one embodiment, R2 is optionally substituted benzyl.

[0163] In one embodiment, each R2 is independently a hydroxy-substituted C 1-6 Alkyl, carbamoyl 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 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, C 1-4 Alkoxycarbonyl-substituted C 1-6 Alkyl, C 1-4 C substituted with alkyl-substituted amino 6-10 Aryl C 1-6 Alkyl, or C 3-6 Cycloalkyl C 1-6 It is alkyl.

[0164] In one embodiment, R2 is C 6-10 Aryl C1-6 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, or C 1-4 C substituted with alkyl-substituted amino 6-10 Aryl C 1-6 It is alkyl.

[0165] In one embodiment, R2 is C6 arylC 1-6 Alkyl, C 1-6 Alkyl-substituted C6 aryl C 1-6 Alkyl, C 1-6 Alkoxy-substituted C6 aryl C 1-6 Alkyl, C 1-6 Haloalkoxy-substituted C6 arylC 1-6 Alkyl, hydroxy-substituted C6 arylC 1-6 Alkyl, halogen-substituted C6 arylC 1-6 Alkyl or C 1-6 C6 aryl C substituted with alkyl-substituted amino 1-6 It is alkyl.

[0166] In one embodiment, R2 is benzyl, methyl or t-butyl substituted benzyl, methoxy or ethoxy substituted benzyl, trifluoromethoxy substituted benzyl, hydroxy substituted benzyl, fluoro or chloro substituted benzyl, or dimethylamino substituted substituted benzyl.

[0167] In one embodiment, R2 is isobutyl, isopentyl, benzyl, 4-fluorobenzyl, 4-chlorobenzyl, 4-hydroxybenzyl, 3-hydroxybenzyl, cyclohexyl, tetrahydro-2H-pyran-4-yl, or 2,2,6,6-tetramethylpiperidin-4-yl.

[0168] In one embodiment, R2 is benzyl, 4-fluorobenzyl, 4-chlorobenzyl, 4-hydroxybenzyl, or 3-hydroxybenzyl.

[0169] In one embodiment, R2 is a 5- or 6-membered heteroaryl substituted C 1-6 In one embodiment, the 5- or 6-membered heteroaryl group in the 5- or 6-membered heteroaryl-substituted alkyl of R2 may be selected from the group consisting of thienyl, pyrrolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, furanyl, oxazolyl, isoxazolyl, oxadiazolyl, thiadiazolyl, triazolyl, tetrazolyl, pyridyl, pyridazinyl, pyrimidinyl, and pyrazinyl. In one embodiment, R2 is pyridyl-substituted methyl or thienyl-substituted methyl.

[0170] In one embodiment, C 10 Aryl-substituted C 1-6 In one embodiment, R2 is 1-naphthylmethyl or 2-naphthylmethyl. In one embodiment, R2 is 1-naphthylmethyl.

[0171] In one embodiment, R1 is alkyl or optionally substituted benzyl, wherein said alkyl is unsubstituted.

[0172] In one embodiment, R1 is a C optionally substituted with a hydroxyl group, a carboxyl group, a carbamoyl group, an amino group, or an amidinoamino group. 1-6 Alkyl, optionally substituted C 3-6 Cycloalkyl C 1-6Alkyl, optionally substituted C6 arylC 1-6 alkyl, or optionally substituted 5- or 6-membered heteroarylC 1-6 It is alkyl.

[0173] In one embodiment, R1 is a C optionally substituted with a hydroxyl group, a carboxyl group, a carbamoyl group, an amino group, or an amidinoamino group. 1-6 alkyl, or optionally substituted benzyl.

[0174] In one embodiment, R is C 1-6 Alkyl, C6 aryl C 1-6 Alkyl, C 1-6 Alkyl-substituted C6 aryl C 1-6 Alkyl, C 1-6 Alkoxy-substituted C6 aryl C 1-6 Alkyl, C 1-6 Haloalkoxy-substituted C6 arylC 1-6 Alkyl, hydroxy-substituted C6 arylC 1-6 Alkyl, halogen-substituted C6 arylC 1-6 Alkyl, or C 1-6 C6 aryl C substituted with alkyl-substituted amino 1-6 It is alkyl.

[0175] In one embodiment, R1 is methyl, isobutyl, isopentyl, benzyl, methyl or t-butyl substituted benzyl, methoxy or ethoxy substituted benzyl, trifluoromethoxy substituted benzyl, hydroxy substituted benzyl, fluoro or chloro substituted benzyl, or dimethylamino substituted benzyl.

[0176] In one embodiment, R1 is methyl, isobutyl, isopentyl, benzyl, 4-methylbenzyl, 4-(t-butyl)benzyl, 3-chlorobenzyl, 4-chlorobenzyl, 4-methoxybenzyl, 4-ethoxybenzyl, 4-hydroxybenzyl, 4-(dimethylamino)benzyl, cyclohexyl, or trans-4-methylcyclohexyl.

[0177] In one embodiment, R1 is methyl, isobutyl, isopentyl, benzyl, 4-methylbenzyl, 4-(t-butyl)benzyl, 3-chlorobenzyl, 4-chlorobenzyl, 4-methoxybenzyl, 4-ethoxybenzyl, 4-hydroxybenzyl, or 4-(dimethylamino)benzyl.

[0178] In one embodiment, R is C 3-6 Cycloalkyl C 1-6 It is alkyl. In one embodiment, R1 is C 3-6 Cycloalkyl C 1-6 C in alkyl 3-6 The cycloalkyl group may be selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl, 1-6 The alkyl group may be selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, tert-butyl, sec-butyl, n-pentyl, isopentyl, neopentyl, tert-pentyl, 1,2-dimethylpropyl, n-hexyl. In one embodiment, R1 is cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, cyclopropylethyl, cyclobutylethyl, cyclopentylethyl, or cyclohexylethyl. In one embodiment, R1 is cyclopropylmethyl or cyclohexylmethyl.

[0179] In one embodiment, R3 is alkyl optionally substituted with hydroxyl, carboxyl, carbamoyl, amino or amidinoamino group, optionally substituted C 6-10 Arylalkyl, optionally substituted C 2-6 Alkenyl, or optionally substituted C 6-10 It is aryl.

[0180] In one embodiment, R3 is alkyl optionally substituted with hydroxyl, carboxyl, carbamoyl, amino or amidinoamino group, or optionally substituted C 6-10 It is arylalkyl.

[0181] In one embodiment, R3 is optionally substituted alkyl. In one embodiment, R3 is alkyl, wherein the alkyl is unsubstituted. In one embodiment, R3 is optionally substituted C 1-6 R3 is C 1-6 It is alkyl.

[0182] In one embodiment, R3 is a C optionally substituted with a hydroxyl group, a carboxyl group, a carbamoyl group, an amino group, or an amidinoamino group. 1-6 Alkyl or optionally substituted C 6-10 Aryl C 1-6 It is alkyl.

[0183] In one embodiment, R3 is C 1-6 Alkyl, hydroxy-substituted C 1-6 Alkyl, carbamoyl 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 Alkyl-substituted C 6-10 Aryl C 1-6 Alkyl, hydroxy-substituted C 6-10 Aryl C1-6 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 C substituted with alkyl-substituted amino 6-10 Aryl C 1-6 Alkyl, or C 3-6 Cycloalkyl C 1-6 It is alkyl.

[0184] In one embodiment, R3 is C 1-6 Alkyl, hydroxy-substituted C 1-6 Alkyl, carbamoyl substituted C 1-6 Alkyl, amidinoamino substituted C 1-6 Alkyl, carboxy-substituted C 1-6 Alkyl, C 1-4 Alkoxycarbonyl-substituted C 1-6 Alkyl, or C 3-6 Cycloalkyl C 1-6 It is alkyl.

[0185] In one embodiment, R3 is C 1-6 Alkyl, C6 aryl C 1-6 Alkyl, C 1-6 Alkyl-substituted C6 aryl C 1-6 Alkyl, halogen-substituted C6 arylC 1-6 Alkyl, C 1-6 Haloalkoxy-substituted C6 arylC 1-6 Alkyl, C 1-6 Alkoxy-substituted C6 aryl C 1-6 Alkyl, hydroxy-substituted C6 arylC 1-6 Alkyl, or C 1-6 C6 aryl C substituted with alkyl-substituted amino 1-6 It is alkyl.

[0186] In one embodiment, R3 is n-propyl, isobutyl, isopentyl, benzyl, methyl or t-butyl substituted benzyl, fluoro or chloro substituted benzyl, methoxy or ethoxy substituted benzyl, trifluoromethoxy substituted benzyl, hydroxy substituted benzyl, or dimethylamino substituted benzyl.

[0187] In one embodiment, R3 is C 1-6 Alkyl, C6 aryl C 1-6 Alkyl or halogen substituted C6 arylC 1-6 It is alkyl.

[0188] In one embodiment, R3 is n-propyl, isobutyl, isopentyl, benzyl, or chloro-substituted benzyl.

[0189] In one embodiment, R3 is C 1-6 It is alkyl.

[0190] In one embodiment, R3 is n-propyl, isobutyl, isopentyl, benzyl, 4-chlorobenzyl, or phenyl.

[0191] In one embodiment, R3 is n-propyl, isobutyl, or isopentyl.

[0192] In one embodiment, R3 is C 3-6 Cycloalkyl C 1-6 It is alkyl. In one embodiment, R3 C 3-6 Cycloalkyl C 1-6 C in alkyl 3-6 The cycloalkyl group may be selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl, 1-6The alkyl group may be selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, tert-butyl, sec-butyl, n-pentyl, isopentyl, neopentyl, tert-pentyl, 1,2-dimethylpropyl, n-hexyl. In one embodiment, R3 is cyclopropylmethyl.

[0193] In one embodiment, R3 is C 2-6 It is alkenyl. In one embodiment, R3 may be selected from the group consisting of 1-propenyl, 1-butenyl, 1-pentenyl, 1-hexenyl, 2-methyl-1-propenyl, 2-methyl-1-butenyl, 2-ethyl-1-butenyl, and 2-methyl-1-pentenyl. In one embodiment, R3 is 2-methyl-1-propenyl.

[0194] In one embodiment, R2 is benzyl, R1 is isobutyl, methoxy-substituted benzyl, methyl-substituted benzyl, t-butyl-substituted benzyl, or chloro-substituted benzyl, and R3 is isobutyl.

[0195] In one embodiment, R2 is benzyl, R1 is methoxy-substituted benzyl or chloro-substituted benzyl, and R3 is isobutyl.

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

[0197] In one embodiment, R2 in the compound of formula IF is benzyl, R1 is 4-methoxybenzyl, and R3 is isobutyl.

[0198] In one embodiment, R2 in the compound of formula IB is benzyl, R1 is 4-methoxybenzyl, and R3 is isobutyl.

[0199] In one embodiment, R2 is benzyl or chloro-substituted benzyl, and R1 and R3 are each independently isobutyl or isopentyl.

[0200] In one embodiment, R2 is benzyl, R1 is isopentyl, and R3 is isobutyl.

[0201] In one embodiment, R2 in the compound of formula IB is benzyl or 4-chlorobenzyl, and R1 and R3 are both isobutyl.

[0202] In one embodiment, R2 in the compound of formula IB is benzyl, R1 is isobutyl, and R3 is isopentyl.

[0203] Preferred combinations of substituents R1, R2, and R3 in compounds of formula IF and IB of the present disclosure are shown in the table below. [Table 1]

[0204] Preferred combinations of substituents R1, R2, R3 and X in compounds of formula IF and IB of the present disclosure are shown below in the form of (R1, R2, R3) = (M, N, Q), where R1(M) is selected from M1 to M15, R2(N) is selected from N1 to N11, and R3(Q) is selected from Q1 to Q6. [Table 2] Preferred combinations of substituents R1, R2 and R3 (R1,R2,R3)=(M1,N1,Q1),(M1,N1,Q2),(M1,N1,Q3),(M1,N1,Q4),(M1,N1,Q5),(M1,N1,Q6),(M1,N2,Q1),(M1,N2,Q2),(M1,N2,Q3),(M1,N2,Q4),(M1, N2,Q5),(M1,N2,Q6),(M1,N3,Q1),(M1,N3,Q2),(M1,N3,Q3),(M1,N3,Q4),(M1,N3,Q5),(M1,N3,Q6),(M1,N4,Q1),(M1,N4,Q2),(M1,N4,Q3),(M1,N4,Q ( M1,N6,Q4),(M1,N6,Q5),(M1,N6,Q6),(M1,N7,Q1),(M1,N7,Q2),(M1,N7,Q3),(M1,N7,Q4),(M1,N7,Q5),(M1,N7,Q6),(M1,N8,Q1),(M1,N8,Q2),(M1,N 8,Q3),(M1,N8,Q4),(M1,N8,Q5),(M1,N8,Q6),(M1,N9,Q1),(M1,N9,Q2),(M1,N9,Q3),(M1,N9,Q4),(M1,N9,Q5),(M1,N9,Q6),(M1,N10,Q1),(M1,N10,Q2),(M1,N10,Q3),(M1,N10,Q4),(M1,N10,Q5),(M1,N10,Q6),(M2,N1,Q1),(M2,N1,Q2),(M2,N1,Q3),(M2,N1,Q4),(M2,N1,Q5),(M2,N1,Q6),(M2,N2, Q1),(M2,N2,Q2),(M2,N2,Q3),(M2,N2,Q4),(M2,N2,Q5),(M2,N2,Q6),(M2,N3,Q1),(M2,N3,Q2),(M2,N3,Q3),(M2,N3,Q4),(M2,N3,Q5),(M2,N3,Q6),(M2,N4,Q1),(M2,N4,Q2),(M2,N4,Q3),(M2,N4,Q4),(M2,N4,Q5),(M2,N4,Q6),(M2,N5,Q1),(M2,N5,Q2),(M2,N5,Q3),(M2,N5,Q4),(M2,N5,Q5),(M2,(N5,Q6),(M2,N6,Q1),(M2,N6,Q2),(M2,N6,Q3),(M2,N6,Q4),(M2,N6,Q5),(M2,N6,Q6),(M2,N7,Q1),(M2,N7,Q2),(M2,N7,Q3),(M2,N7,Q4),(M2,N7,Q5),(M2,N7,Q6),(M2,N8,Q1),(M2,N8,Q2),(M2,N8,Q3),(M2,N8,Q4),(M2,N8,Q5),(M2,N8,Q6),(M2,N9,Q1),(M2,N9,Q2),(M2,N9,Q3),(M2,N9,Q4),( (M2,N9,Q5), (M2,N9,Q6), (M2,N10,Q1), (M2,N10,Q2), (M2,N10,Q3), (M2,N10,Q4), (M2,N10,Q5), (M2,N10,Q6), (M3,N1,Q1), (M3,N1,Q2), (M3,N1,Q3), (M3,N1,Q4), (M3,N1,Q5), (M3,N1,Q6), (M3,N2,Q1), (M3,N2,Q2), (M3,N2,Q3), (M3,N2,Q4), (M3,N2,Q5), (M3,N2,Q6), (M3,N3,Q1), (M3,N3,Q2), (M3 (M3,N3,Q4), (M3,N3,Q5), (M3,N3,Q6), (M3,N4,Q1), (M3,N4,Q2), (M3,N4,Q3), (M3,N4,Q4), (M3,N4,Q5), (M3,N4,Q6), (M3,N5,Q1), (M3,N5,Q2), (M3,N5,Q3), (M3,N5,Q4), (M3,N5,Q5), (M3,N5,Q6), (M3,N6,Q1), (M3,N6,Q2), (M3,N6,Q3), (M3,N6,Q4), (M3,N6,Q5), (M3,N6,Q6), (M3,N7,Q1) (M3,N7,Q2),(M3,N7,Q3),(M3,N7,Q4),(M3,N7,Q5),(M3,N7,Q6),(M3,N8,Q1),(M3,N8,Q2),(M3,N8,Q3),(M3,N8,Q4),(M3,N8,Q5),(M3,N8,Q6),(M3,N9,Q1),(M3,N9,Q2),(M3,N9,Q3),(M3,N9,Q4),(M3,N9,Q5),(M3,N9,Q6),(M3,N10,Q1),(M3,N10,Q2),(M3,N10,Q3),(M3,N10,Q4),(M3,N10,Q5),(M3,N10,Q6),(M4,N1,Q1),(M4,N1,Q2),(M4,N1,Q3),(M4,N1,Q4),(M4,N1,Q5),(M4,N1,Q6),(M4,N2,Q1),(M4,N2,Q2),(M4,N2,Q3),(M4,N2,Q4),(M4,N2,Q5),(M4,N2,Q6),(M4,N3,Q1),(M4,N3,Q2),(M4,N3,Q3),(M4,N3,Q4),(M4,N3,Q5),(M4,N3,Q6),(M4,N4,Q1),(M4,N4,Q2),(M4,N4,Q3),(M4,N4,Q4),(M4,N4,Q5),(M4,N4,Q6),(M4,N5,Q1),(M4,N5,Q2),(M4,N5,Q3),(M4,N5,Q4),(M4,N5,Q5),(M4,N5,Q6),(M4,N6,Q1),(M4,N6,Q2),(M4,N6,Q3),(M4,N6,Q4),(M4,N6,Q5),(M4,N6,Q6),(M4,N7,Q1),(M4,N7,Q2),(M4,N7,Q3),(M4,N7,Q4),(M4,N7,Q5),(M4,N7,Q6),(M4,N8,Q1),(M4,N8,Q2),(M4,N8,Q3),(M4,N8,Q4),(M4,N8,Q5),(M4,N8,Q6),(M4,N9,Q1),(M4,N9,Q2),(M4,N9,Q3),(M4,N9,Q4),(M4,N9,Q5),(M4,N9,Q6),(M4,N10,Q1),(M4,N10,Q2),(M4,N10,Q3),(M4,N10,Q4),(M4,N10,Q5),(M4,N10,Q6),(M5,N1,Q1),(M5,N1,Q2),(M5,N1,Q3),(M5,N1,Q4),(M5,N1,Q5),(M5,N1,Q6),(M5,N2,Q1),(M5,N2,Q2),(M5,N2,Q3),(M5,N2,Q4),(M5,N2,Q5),(M5,N2,Q6),(M5,N3,Q1),(M5,N3,Q2),(M5,N3,Q3),(M5,N3,Q4),(M5,N3,Q5),(M5,N3,Q6),(M5,N4,Q1),(M5,N4,Q2),(M5,N4,Q3),(M5,N4,Q4),(M5,N4,Q5),(M5,N4,Q6),(M5,N5,Q1),(M5,N5,Q2),(M5,N5,Q3),(M5,N5,Q4),(M5,N5,Q5),(M5,N5,Q6),(M5,N6,Q1),(M5,N6,Q2),(M5,N6,Q3),(M5,N6,Q4),(M5,N6,Q5),(M5,N6,Q6),(M5,N7,Q1),(M5,N7,Q2),(M5,N7,Q3),(M5,N7,Q4),(M5,N7,Q5),(M5,N7,Q6),(M5,N8,Q1),(M5,N8,Q2),(M5,N8,Q3),(M5,N8,Q4),(M5,N8,Q5),(M5,N8,Q6),(M5,N9,Q1),(M5,N9,Q2),(M5,N9,Q3),(M5,N9,Q4),(M5 (M5, N9, Q6), (M5, N10, Q1), (M5, N10, Q2), (M5, N10, Q3), (M5, N10, Q4), (M5, N10, Q5), (M5, N10, Q6), (M6, N1, Q1), (M6, N1, Q2), (M6, N1, Q3), (M6, N1, Q4), (M6, N1, Q5), (M6, N1, Q6), (M6, N2, Q1), (M6, N2, Q2), (M6, N2, Q3), (M6, N2, Q4), (M6, N2, Q5), (M6, N2, Q6), (M6, N3, Q1), (M6, N3, Q2), (M6, N 3,Q3),(M6,N3,Q4),(M6,N3,Q5),(M6,N3,Q6),(M6,N4,Q1),(M6,N4,Q2),(M6,N4,Q3),(M6,N4,Q4),(M6,N4,Q5),(M6,N4,Q6),(M6,N5,Q1),(M6,N5,Q ( M6,N7,Q2),(M6,N7,Q3),(M6,N7,Q4),(M6,N7,Q5),(M6,N7,Q6),(M6,N8,Q1),(M6,N8,Q2),(M6,N8,Q3),(M6,N8,Q4),(M6,N8,Q5),(M6,N8,Q6),(M6,N9,Q1),(M6,N9,Q2),(M6,N9,Q3),(M6,N9,Q4),(M6,N9,Q5),(M6,N9,Q6),(M6,N10,Q1),(M6,N10,Q2),(M6,N10,Q3),(M6,N10,Q4),(M6,N10,Q5),(M6(N10,Q6),(M7,N1,Q1),(M7,N1,Q2),(M7,N1,Q3),(M7,N1,Q4),(M7,N1,Q5),(M7,N1,Q6),(M7,N2,Q1),(M7,N2,Q2),(M7,N2,Q3),(M7,N2,Q4),(M7,N2,Q5),(M7,N2,Q6),(M7,N3,Q1),(M7,N3,Q2),(M7,N3,Q3),(M7,N3,Q4),(M7,N3,Q5),(M7,N3,Q6),(M7,N4,Q1),(M7,N4,Q2),(M7,N4,Q3),(M7,N4,Q4) (M7,N4,Q5),(M7,N4,Q6),(M7,N5,Q1),(M7,N5,Q2),(M7,N5,Q3),(M7,N5,Q4),(M7,N5,Q5),(M7,N5,Q6),(M7,N6,Q1),(M7,N6,Q2),(M7,N6,Q3),(M7,N6,Q4),(M7,N6,Q5),(M7,N6,Q6),(M7,N7,Q1),(M7,N7,Q2),(M7,N7,Q3),(M7,N7,Q4),(M7,N7,Q5),(M7,N7,Q6),(M7,N8,Q1),(M7,N8,Q2),(M7,N8,Q 3),(M7,N8,Q4),(M7,N8,Q5),(M7,N8,Q6),(M7,N9,Q1),(M7,N9,Q2),(M7,N9,Q3),(M7,N9,Q4),(M7,N9,Q5),(M7,N9,Q6),(M7,N10,Q1),(M7,N10,Q2),(M7,N10,Q3),(M7,N10,Q4),(M7,N10,Q5),(M7,N10,Q6),(M8,N1,Q1),(M8,N1,Q2),(M8,N1,Q3),(M8,N1,Q4),(M8,N1,Q5),(M8,N1,Q6),(M8,N2,Q1 ,(M8,N2,Q2),(M8,N2,Q3),(M8,N2,Q4),(M8,N2,Q5),(M8,N2,Q6),(M8,N3,Q1),(M8,N3,Q2),(M8,N3,Q3),(M8,N3,Q4),(M8,N3,Q5),(M8,N3,Q6),(M8 (M8,N5,Q5),(M8,N5),Q6),(M8,N6,Q1),(M8,N6,Q2),(M8,N6,Q3),(M8,N6,Q4),(M8,N6,Q5),(M8,N6,Q6),(M8,N7,Q1),(M8,N7,Q2),(M8,N7,Q3),(M8,N7,Q4),(M8,N7,Q5),(M8,N7,Q6),(M8,N8,Q1),(M8,N8,Q2),(M8,N8,Q3),(M8,N8,Q4),(M8,N8,Q5),(M8,N8,Q6),(M8,N9,Q1),(M8,N9,Q2),(M8,N9,Q3),(M8,N9,Q4),(M8 (M8, N9, Q6), (M8, N10, Q1), (M8, N10, Q2), (M8, N10, Q3), (M8, N10, Q4), (M8, N10, Q5), (M8, N10, Q6), (M9, N1, Q1), (M9, N1, Q2), (M9, N1, Q3), (M9, N1, Q4), (M9, N1, Q5), (M9, N1, Q6), (M9, N2, Q1), (M9, N2, Q2), (M9, N2, Q3), (M9, N2, Q4), (M9, N2, Q5), (M9, N2, Q6), (M9, N3, Q1), (M9, N3, Q2), (M9, N 3,Q3),(M9,N3,Q4),(M9,N3,Q5),(M9,N3,Q6),(M9,N4,Q1),(M9,N4,Q2),(M9,N4,Q3),(M9,N4,Q4),(M9,N4,Q5),(M9,N4,Q6),(M9,N5,Q1),(M9,N5,Q ( (M9,N7,Q2), (M9,N7,Q3), (M9,N7,Q4), (M9,N7,Q5), (M9,N7,Q6), (M9,N8,Q1), (M9,N8,Q2), (M9,N8,Q3), (M9,N8,Q4), (M9,N8,Q5), (M9,N8,Q6), (M9,N9,Q1), (M9,N9,Q2), (M9,N9,Q3), (M9,N9,Q4), (M9,N9,Q5), (M9,N9,Q6), (M9,N10,Q1), (M9,N10,Q2), (M9,N10,Q3), (M9,N10,Q4), (M9,N10,Q5), (M9(N10,Q6),(M10,N1,Q1),(M10,N1,Q2),(M10,N1,Q3),(M10,N1,Q4),(M10,N1,Q5),(M10,N1,Q6),(M10,N2,Q1),(M10,N2,Q2),(M10,N2,Q3),(M10,N2,Q4),(M10,N2,Q5),(M10,N2,Q6),(M10,N3,Q1),(M10,N3,Q2),(M10,N3,Q3),(M10,N3,Q4),(M10,N3,Q5),(M10,N3,Q6),(M10,N4,Q1),(M10,N4,Q2),( M10,N4,Q3),(M10,N4,Q4),(M10,N4,Q5),(M10,N4,Q6),(M10,N5,Q1),(M10,N5,Q2),(M10,N5,Q3),(M10,N5,Q4),(M10,N5,Q5),(M10,N5,Q6),(M10,N 6,Q1),(M10,N6,Q2),(M10,N6,Q3),(M10,N6,Q4),(M10,N6,Q5),(M10,N6,Q6),(M10,N7,Q1),(M10,N7,Q2),(M10,N7,Q3),(M10,N7,Q4),(M10,N7,Q5) (M10,N7,Q6), (M10,N8,Q1), (M10,N8,Q2), (M10,N8,Q3), (M10,N8,Q4), (M10,N8,Q5), (M10,N8,Q6), (M10,N9,Q1), (M10,N9,Q2), (M10,N9,Q3), (M10,N9,Q4), (M10,N9,Q5), (M10,N9,Q6), (M10,N10,Q1), (M10,N10,Q2), (M10,N10,Q3), (M10,N10,Q4), (M10,N10,Q5), (M10,N10,Q6), (M11,N1,Q1), (M 11,N1,Q2),(M11,N1,Q3),(M11,N1,Q4),(M11,N1,Q5),(M11,N1,Q6),(M11,N2,Q1),(M11,N2,Q2),(M11,N2,Q3),(M11,N2,Q4),(M11,N2,Q5),(M11,N2,Q6),(M11,N3,Q1),(M11,N3,Q2),(M11,N3,Q3),(M11,N3,Q4),(M11,N3,Q5),(M11,N3,Q6),(M11,N4,Q1),(M11,N4,Q2),(M11,N4,Q3),(M11,N4,Q4)(M11,N4,Q5),(M11,N4,Q6),(M11,N5,Q1),(M11,N5,Q2),(M11,N5,Q3),(M11,N5,Q4),(M11,N5,Q5),(M11,N5,Q6),(M11,N6,Q1),(M11,N6,Q2),(M11 (M11,N7,Q6),(M11,N8,Q) 1),(M11,N8,Q2),(M11,N8,Q3),(M11,N8,Q4),(M11,N8,Q5),(M11,N8,Q6),(M11,N9,Q1),(M11,N9,Q2),(M11,N9,Q3),(M11,N9,Q4),(M11,N9,Q5),(M11,N9,Q6),(M11,N10,Q1),(M11,N10,Q2),(M11,N10,Q3),(M11,N10,Q4),(M11,N10,Q5),(M11,N10,Q6),(M12,N1,Q1),(M12,N1,Q2),(M12,N1,Q3),( M12,N1,Q4),(M12,N1,Q5),(M12,N1,Q6),(M12,N2,Q1),(M12,N2,Q2),(M12,N2,Q3),(M12,N2,Q4),(M12,N2,Q5),(M12,N2,Q6),(M12,N3,Q1),(M12, N3,Q2),(M12,N3,Q3),(M12,N3,Q4),(M12,N3,Q5),(M12,N3,Q6),(M12,N4,Q1),(M12,N4,Q2),(M12,N4,Q3),(M12,N4,Q4),(M12,N4,Q5),(M12,N4,Q6 ),(M12,N5,Q1),(M12,N5,Q2),(M12,N5,Q3),(M12,N5,Q4),(M12,N5,Q5),(M12,N5,Q6),(M12,N6,Q1),(M12,N6,Q2),(M12,N6,Q3),(M12,N6,Q4),(M1 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Q5),(M13,N8,Q6),(M13,N9,Q1),(M13,N9,Q2),(M13,N9,Q3),(M13,N9,Q4),(M13,N9,Q5),(M13,N9,Q6),(M13,N10,Q1),(M13,N10,Q2),(M13,N10,Q3),(M13,N10,Q4),(M13,N10,Q5),(M13,N10,Q6),(M14,N1,Q1),(M14,N1,Q2),(M14,N1,Q3),(M14,N1,Q4),(M14,N1,Q5),(M14,N1,Q6),(M14,N2,Q1)(M14,N2,Q2),(M14,N2,Q3),(M14,N2,Q4),(M14,N2,Q5),(M14,N2,Q6),(M14,N3,Q1),(M14,N3,Q2),(M14,N3,Q3),(M14,N3,Q4),(M14,N3,Q5),(M14,N3,Q6),(M14,N4,Q1),(M14,N4,Q2),(M14,N4,Q3),(M14,N4,Q4),(M14,N4,Q5),(M14,N4,Q6),(M14,N5,Q1),(M14,N5,Q2),(M14,N5,Q3),(M14,N5,Q4),(M14,N5,Q5),(M14,N5,Q6),(M14,N6,Q1),(M14,N6,Q2),(M14,N6,Q3),(M14,N6,Q4),(M14,N6,Q5),(M14,N6, Q6),(M14,N7,Q1),(M14,N7,Q2),(M14,N7,Q3),(M14,N7,Q4),(M14,N7,Q5),(M14,N7,Q6),(M14,N8,Q1),(M14,N8,Q2),(M14,N8,Q3),(M14,N8,Q4),(M14,N8,Q5),(M14,N8,Q6),(M14,N9,Q1),(M14,N9,Q2),(M14,N9,Q3),(M14,N9,Q4),(M14,N9,Q5),(M14,N9,Q6),(M14,N10,Q1),(M14,N10,Q2),(M14,N10,Q3),(M14,N10,Q4),(M14,N10,Q5),(M14,N10,Q6),(M15,N1,Q1),(M15,N1,Q2),(M15,N1,Q3),(M15,N1,Q4),(M15,N1,Q5),(M15,N1,Q6),(M15,N2,Q1),(M15,N2,Q2),(M15,N2,Q3),(M15,N2,Q4),(M15,N2,Q5),(M15,N2,Q6),(M15,N3,Q1),(M15,N3,Q2),(M15,N3,Q3),(M15,N3,Q4),(M15,N3,Q5),(M15,N3,Q6),(M15,N4,Q1),(M15,N4,Q2),(M15,N4,Q3),(M15,N4,Q4),(M15,N4,Q5),(M15,N4,Q6),(M15,N5,Q1),(M15,N5,Q2),(M15,N5,Q3),(M15,N5,Q4),(M15,N5,Q5),(M15,N5,Q6),(M15,N6,Q1),(M15,N6,Q2),(M15,N6,Q3),(M15,N6,Q4),(M15,N6,Q5),(M15,N6,Q6),(M15,N7,Q1),(M15,N7,Q2),(M15,N7,Q3),(M15,N7,Q4),(M15,N7,Q5),(M15,N7,Q6),(M15,N8,Q1),(M15,N8,Q2),(M15,N8,Q3),(M15,N8,Q4),(M15,N8,Q5),(M15,N8,Q6),(M15,N9,Q1),(M15,N9,Q2),(M15,N9,Q3),(M15,N9,Q4),(M15,N9,Q5),(M15,N9,Q6),(M15,N10,Q1),(M15,N10,Q2),(M15,N10,Q3),(M15,N10,Q4),(M15,N10,Q5),(M15,N10,Q6),

[0205] 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, and X is -NH-.

[0206] 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.

[0207] The present disclosure is also intended to encompass various hydrates, solvates and crystalline polymorphs.

[0208] 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.

[0209] The present disclosure also encompasses prodrugs of the compounds of the present disclosure. In the present disclosure, prodrugs refer to derivatives that are decomposed in vivo, for example, by acid hydrolysis or enzymatically, to yield compounds represented by formula IF, IB, IIF, IIB, XXIF, XXIB, XXIIF, XXIIB, XXIIIF, or XXIIIB described herein. For example, if a compound represented by formula IF, IB, IIF, IIB, XXIF, XXIB, XXIIF, XXIIB, XXIIIF, or XXIIIB described herein contains a hydroxyl group, an amino group, or a carboxyl group, these groups can be modified using conventional methods to produce a prodrug. Prodrug technology is described, for example, in C.G. Wermuth, "The Practice of Medicinal Chemistry," 4th Ed., Academic Press, (2015), Chapter 28.

[0210] 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.

[0211] 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.

[0212] 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 becomes a phosphate ester, or a compound which becomes an alkanoyloxymethyloxy group.

[0213] 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:

[0214] 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.

[0215] 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.

[0216] The phrase "a compound or its enantiomer or a salt thereof or a solvate thereof" means a compound, an enantiomer of said compound, a salt of said compound, a salt of said enantiomer, a solvate of said compound, a solvate of said enantiomer, a solvate of a salt of said compound, or a solvate of a salt of said enantiomer.

[0217] As used herein, a therapeutic agent that "prevents" rabies refers to a compound that reduces the appearance of a disorder or condition in a treated subject compared to an untreated subject, or that delays the onset of or reduces the severity of one or more symptoms of rabies in a subject compared to an untreated subject.

[0218] The term "treating" includes prophylactic and / or therapeutic treatment. The term "prophylactic or therapeutic" treatment is art-recognized and includes administration to a host of one or more compounds or pharmaceutical compositions of the present invention. When administered prior to clinical manifestation of an undesirable condition (e.g., disease or other undesirable condition in a host animal), the treatment is prophylactic (i.e., protects the host from the onset of the undesirable condition), whereas when administered after the manifestation of the undesirable condition, the treatment is therapeutic (i.e., intended to attenuate, ameliorate, or stabilize an existing undesirable condition or its side effects).

[0219] The term "prodrug" is intended to encompass compounds that are converted under physiological conditions into therapeutically active agents of the present disclosure (e.g., compounds of Formula I). ​​A common method for making prodrugs is to include one or more selected moieties that are hydrolyzed under physiological conditions to reveal the desired molecule. In other embodiments, the prodrug is converted by enzymatic activity in the host animal. For example, esters or carbonates (e.g., esters or carbonates of alcohols or carboxylic acids) are preferred prodrugs of the present disclosure. In certain embodiments, some of the compounds in the formulations depicted above or all of the compounds of Formulae IF, IB, XXIF, and XXIB can be replaced with the corresponding appropriate prodrug, for example, where a hydroxyl in the parent compound is provided as an ester or carbonate, or a carboxylic acid present in the parent compound is provided as an ester.

[0220] Pharmaceutical Composition The compositions and methods of the present disclosure can be used to treat individuals in need thereof. In certain embodiments, the individual is a mammal, such as a human, or a non-human mammal. When administered to an animal, such as a human, the composition or compound is preferably administered as a pharmaceutical composition, for example, comprising a compound of the present disclosure and a pharmaceutically acceptable carrier. Pharmaceutically acceptable carriers are well known in the art and include, for example, aqueous solutions, such as water or buffered saline, or other solvents or vehicles, such as glycols, glycerol, oils, such as olive oil, or injectable organic esters. In preferred embodiments, when such pharmaceutical compositions are intended for administration to humans, particularly via an invasive route (i.e., a route such as injection or implantation that avoids transport or diffusion through an epithelial barrier), the aqueous solution is pyrogen-free or substantially pyrogen-free. The excipient can be selected, for example, to effect delayed release of the agent or to selectively target one or more cells, tissues, or organs. The pharmaceutical composition may be in unit dosage form, such as tablets, capsules (including sprinkle capsules and gelatin capsules), granules, lyophilized for reconstitution, powder, liquid, syrup, suppository, or injection. The composition may also be present in a transdermal delivery system, such as a skin patch. The composition may also be present in a liquid suitable for topical administration, such as eye drops.

[0221] A pharmaceutically acceptable carrier can contain a physiologically acceptable agent that acts, for example, to stabilize, increase the solubility, or increase the absorption of a compound, such as a compound of the present disclosure. Such physiologically acceptable agents include, for example, carbohydrates such as glucose, sucrose, or dextran, antioxidants such as ascorbic acid or glutathione, chelating agents, low-molecular-weight proteins, or other stabilizers or excipients. The choice of a pharmaceutically acceptable carrier, including a physiologically acceptable agent, depends, for example, on the route of administration of the composition. The preparation or pharmaceutical composition may be a self-emulsifying drug delivery system or a self-microemulsifying drug delivery system. The pharmaceutical composition (preparation) may also be a liposome or other polymer matrix, into which, for example, a compound of the present disclosure may be incorporated. Liposomes, such as liposomes containing phospholipids or other lipids, are non-toxic, physiologically acceptable, and metabolizable carriers that are relatively easy to prepare and administer.

[0222] The phrase "pharmaceutically acceptable," as employed herein, refers to compounds, materials, compositions, and / or dosage forms that are, within the scope of sound medical judgment, suitable for use in contact with the tissues of human beings and animals without excessive toxicity, irritation, allergic response, other problem or complication, commensurate with a reasonable benefit / risk ratio.

[0223] The phrase "pharmaceutically acceptable carrier" as used herein means a pharmaceutically acceptable material, composition, or vehicle, such as a liquid or solid filler, diluent, excipient, solvent, or encapsulating material. Each carrier must be "acceptable" in the sense of being compatible with the other ingredients of the formulation and not harmful to the patient. Some examples of materials that can function as pharmaceutically acceptable carriers include: (1) sugars, such as lactose, glucose, and sucrose; (2) starches, such as corn starch and potato starch; (3) cellulose and its derivatives, such as sodium carboxymethylcellulose, ethylcellulose, and cellulose acetate; (4) powdered tragacanth; (5) malt; (6) gelatin; (7) talc; (8) excipients, such as cocoa butter and suppository wax; (9) oils, such as peanut oil, cottonseed oil, safflower oil, sesame oil, olive oil, (10) glycols, such as propylene glycol; (11) polyols, such as glycerin, sorbitol, mannitol, and polyethylene glycol; (12) esters, such as ethyl oleate and ethyl laurate; (13) agar; (14) buffers, such as magnesium hydroxide and aluminum hydroxide; (15) alginic acid; (16) pyrogen-free water; (17) isotonic saline; (18) Ringer's solution; (19) ethyl alcohol; (20) phosphate buffer; and (21) other non-toxic, compatible substances employed in pharmaceutical formulations.

[0224] Pharmaceutical compositions (preparations) can be administered to a subject by any of several routes of administration, including, for example, orally (e.g., drenches, tablets, capsules (including sprinkle capsules and gelatin capsules), boluses, powders, granules, pastes for application to the tongue, etc., in aqueous or non-aqueous solutions or suspensions); absorption through the oral mucosa (e.g., sublingually); anally, rectally, or vaginally (e.g., as a pessary, cream, or foam, etc.); parenterally (e.g., as a sterile solution or suspension, including intramuscularly, intravenously, subcutaneously, or intrathecally); nasally; intraperitoneally; subcutaneously; transdermally (e.g., as a patch applied to the skin); and topically (e.g., as a cream, ointment, or spray applied to the skin, or as eye drops). The compounds can also be formulated for inhalation. In certain embodiments, the compounds may simply be dissolved or suspended in sterile water. Details of suitable routes of administration and compositions suitable therefor can be found, for example, in U.S. Pat. Nos. 6,110,973, 5,731,000, 5,541,231, 5,427,798, 5,358,970 and 4,172,896, and the patents cited therein.

[0225] The formulations may conveniently be presented in unit dosage form and may be prepared by any methods well known in the art of pharmacy. The amount of active ingredient which can be combined with a carrier material to produce a single dosage form will vary depending upon the host being treated and the particular mode of administration. The amount of active ingredient which can be combined with a carrier material to produce a single dosage form will generally be that amount of the compound which produces a therapeutic effect. Generally, this amount will range from about 1 percent to about 99 percent of the active ingredient, preferably from about 5 percent to about 70 percent of the active ingredient, and most preferably from about 10 percent to about 30 percent of the active ingredient, out of one hundred percent.

[0226] Methods of preparing these formulations or compositions include the step of bringing into association an active compound, such as a compound of the present disclosure, with the carrier and, optionally, one or more accessory ingredients. In general, the formulations are prepared by uniformly and intimately bringing into association a compound of the present disclosure with liquid carriers, or finely divided solid carriers, or both, and then, if necessary, shaping the product.

[0227] Formulations of the present disclosure suitable for oral administration may be in the form of capsules (including sprinkle capsules and gelatin capsules), cachets, pills, tablets, lozenges (using a flavored base, usually sucrose and acacia or tragacanth), lyophilized forms, powders, granules, or as a solution or suspension in an aqueous or non-aqueous liquid, or as an oil-in-water or water-in-oil liquid emulsion, or as an elixir or syrup, or as a pastille (using an inert base, such as gelatin and glycerin, or sucrose and acacia), and / or as a mouthwash, each of which contains a predetermined amount of a compound of the present disclosure as an active ingredient. The composition or compound may also be administered as a bolus, electuary, or paste.

[0228] To prepare solid dosage forms for oral administration, such as capsules (including sprinkle capsules and gelatin capsules), tablets, pills, dragees, powders, and granules, the active ingredient is mixed with one or more pharmaceutically acceptable carriers, such as sodium citrate or dicalcium phosphate, and / or any of the following: (1) fillers or extenders, such as starch, lactose, sucrose, glucose, mannitol, and / or silicic acid; (2) binders, such as carboxymethylcellulose, alginate, gelatin, polyvinylpyrrolidone, sucrose, and / or acacia; (3) humectants, such as glycerol; (4) disintegrating agents. Disintegrating agents, such as agar-agar, calcium carbonate, potato or tapioca starch, alginic acid, certain silicates, and sodium carbonate; (5) solution retarding agents, such as paraffin; (6) absorption accelerators, such as quaternary ammonium compounds; (7) wetting agents, such as cetyl alcohol and glycerol monostearate; (8) absorbents, such as kaolin and bentonite clay; (9) lubricants, such as talc, calcium stearate, magnesium stearate, solid polyethylene glycol, sodium lauryl sulfate, and mixtures thereof; (10) complexing agents, such as modified and unmodified cyclodextrins; and (11) coloring agents. In the case of capsules (including sprinkle capsules and gelatin capsules), tablets, and pills, the pharmaceutical compositions may also contain buffering agents. Solid compositions of a similar type may also be employed as fillers in soft and hard-filled gelatin capsules using such excipients as lactose or milk sugar, as well as high molecular weight polyethylene glycols and the like.

[0229] Tablets can be made by compression or molding, optionally with one or more accessory ingredients. Compressed tablets can be prepared using binders (e.g., gelatin or hydroxypropylmethylcellulose), lubricants, inert diluents, preservatives, disintegrants (e.g., sodium starch glycolate or cross-linked sodium carboxymethylcellulose), surfactants, or dispersing agents. Molded tablets can be made by molding a mixture of the powdered compound moistened with an inert liquid diluent in a suitable machine.

[0230] Tablets and other solid dosage forms of pharmaceutical compositions, such as sugar-coated tablets, capsules (including sprinkle capsules and gelatin capsules), pills, and granules, may be optionally scored or prepared with coatings and shells, such as enteric coatings and other coatings well known in the pharmaceutical formulation art. They may also be formulated to provide sustained or controlled release of the active ingredient therein, for example, using hydroxypropylmethylcellulose, other polymer matrices, liposomes, and / or microspheres in different proportions to provide the desired release profile. They may be sterilized, for example, by filtration through a bacteria-retaining filter or by incorporating a sterilizing agent in the form of a sterile solid composition that can be dissolved in sterile water or some other sterile injectable medium immediately before use. These compositions may also optionally contain emulsifying agents, and may be composed to release the active ingredient(s) only, or preferentially, in a certain part of the digestive tract, optionally in a delayed manner. Examples of embedding compositions that can be used include polymeric substances and waxes. The active ingredient can also be in micro-encapsulated form, if appropriate, with one or more of the excipients described above.

[0231] The liquid dosage form useful for oral administration includes pharmaceutically acceptable emulsion, freeze-dried for reconstitution, microemulsion, solution, suspension, syrup and elixir.In addition to active ingredient, liquid dosage form can contain the inert diluent commonly used in this field, such as water or other solvent, cyclodextrin and its derivatives, solubilizer and emulsifier, such as ethyl alcohol, isopropyl alcohol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1,3-butylene glycol, oil (especially cottonseed oil, peanut oil, corn oil, germ oil, olive oil, castor oil and sesame oil), glycerol, tetrahydrofuryl alcohol, polyethylene glycol and fatty acid ester of sorbitan, etc., and their mixtures.

[0232] Besides inert diluents, the oral compositions can also include adjuvants such as wetting agents, emulsifying and suspending agents, sweetening, flavoring, coloring, perfuming and preservative agents.

[0233] Suspensions may contain, in addition to the active compound, suspending agents such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol and sorbitan esters, microcrystalline cellulose, aluminum metahydroxide, bentonite, agar-agar, and tragacanth, and mixtures thereof.

[0234] Formulations of pharmaceutical compositions for rectal, vaginal, or urethral administration may be presented as suppositories, which can be prepared by mixing one or more active compounds with one or more suitable non-irritating excipients or carriers including, for example, cocoa butter, polyethylene glycol, a suppository wax, or a salicylate, which are solid at room temperature but liquid at body temperature and therefore will melt in the rectum or vaginal cavity and release the active compound.

[0235] Formulations of the pharmaceutical composition for administration to the mouth may be presented as a mouthwash, or an oral spray, or an oral ointment.

[0236] Alternatively or additionally, the compositions can be formulated for delivery via a catheter, stent, wire, or other intraluminal device, which may be particularly useful for delivery to the bladder, urethra, ureter, rectum, or intestine.

[0237] Formulations which are suitable for vaginal administration also include pessaries, tampons, creams, gels, pastes, foams or spray formulations containing such carriers as are known in the art to be appropriate.

[0238] Dosage forms for topical or transdermal administration include powders, sprays, ointments, pastes, creams, lotions, gels, solutions, patches, and inhalants. The active compound can be mixed under sterile conditions with a pharmaceutically acceptable carrier, and any preservatives, buffers, or propellants that may be required.

[0239] The ointments, pastes, creams and gels may contain, in addition to the active compound, excipients such as animal and vegetable fats and oils, waxes, paraffin, starch, tragacanth, cellulose derivatives, polyethylene glycols, silicones, bentonite, silicic acid, talc and zinc oxide, or mixtures thereof.

[0240] Powders and sprays can contain, in addition to the active compound, excipients such as lactose, talc, silicic acid, aluminum hydroxide, calcium silicates and polyamide powder, or mixtures of these substances. Sprays can additionally contain customary propellants, such as chlorofluorohydrocarbons and volatile unsubstituted hydrocarbons, such as butane and propane.

[0241] Transdermal patch has the added advantage of providing controlled delivery of the compound of the present disclosure to the body.Such dosage forms can be prepared by dissolving or dispersing active compound in a suitable medium.The flux of compound across the skin can also be increased by using an absorption enhancer.The rate of such flux can be controlled by providing a rate-controlling membrane or dispersing compound in a polymer matrix or gel.

[0242] Ophthalmic preparations, eye ointments, powders, solutions, etc. are also contemplated within the scope of the present disclosure.Exemplary ophthalmic preparations are described in U.S. Patent Application Publication Nos. 2005 / 0080056, 2005 / 0059744, 2005 / 0031697 and 2005 / 004074 and U.S. Patent No. 6,583,124 (the contents of which are incorporated herein by reference).If desired, liquid ophthalmic preparations have properties similar to those of tears, aqueous humor or vitreous humor, or are compatible with such fluids.Preferred administration route is local administration (e.g., topical administration, such as eye drops, or administration via implant).

[0243] The phrases "parenteral administration" and "parenterally administered" as used herein refer to modes of administration other than enteral and topical administration, usually by injection, and include, without limitation, intravenous, intramuscular, intraarterial, intrathecal, intracapsular, intraorbital, intracardiac, intradermal, intraperitoneal, transtracheal, subcutaneous, subcuticular, intraarticular, subcapsular, subarachnoid, intraspinal, and intrasternal injection and infusion. Pharmaceutical compositions suitable for parenteral administration contain one or more active compounds in combination with one or more pharmaceutically acceptable sterile, isotonic, aqueous or non-aqueous solutions, dispersions, suspensions, or emulsions, or sterile powders that can be reconstituted into a sterile injectable solution or dispersion immediately before use, which may contain antioxidants, buffers, bacteriostats, solutes that render the formulation isotonic with the blood of the intended recipient, or suspending or thickening agents.

[0244] Examples of suitable aqueous and non-aqueous carriers that can be employed in the pharmaceutical compositions of the present disclosure include water, ethanol, polyols (e.g., glycerol, propylene glycol, polyethylene glycol, and the like) and suitable mixtures thereof, vegetable oils such as olive oil, and injectable organic esters such as ethyl oleate, etc. Proper fluidity can be maintained, for example, by the use of coating materials such as lecithin, by the maintenance of the required particle size in the case of dispersions, and by the use of surfactants.

[0245] These compositions can also contain adjuvants, such as preservatives, wetting agents, emulsifying agents, and dispersing agents. Prevention of microbial action can be ensured by including various antibacterial and antifungal agents, such as parabens, chlorobutanol, and phenol sorbic acid. It is also desirable to include isotonic agents, such as sugars and sodium chloride, in the composition. In addition, prolonged absorption of injectable pharmaceutical forms can be achieved by including agents that delay absorption, such as aluminum monostearate and gelatin.

[0246] In some cases, in order to prolong the effect of a drug, it is desirable to delay the absorption of the drug from subcutaneous injection or intramuscular injection.This can be achieved by using a liquid suspension of crystalline or amorphous material with poor water solubility.Therefore, the absorption rate of the drug depends on its dissolution rate, and the rate can also depend on the crystal size and crystalline form.Alternatively, the delayed absorption of parenterally administered drug forms can be achieved by dissolving or suspending the drug in an oil vehicle.

[0247] Injectable depot forms are made by forming microencapsulated matrices of the subject compounds in biodegradable polymers such as polylactide-polyglycolide. The rate of drug release can be controlled depending on the drug-to-polymer ratio and the nature of the particular polymer employed. Examples of other biodegradable polymers include poly(orthoesters) and poly(anhydrides). Depot injectable formulations are also prepared by entrapping the drug in liposomes or microemulsions that are compatible with body tissues.

[0248] For use in the methods of the present disclosure, the active compound may be provided per se, or may be provided as a pharmaceutical composition containing, for example, 0.1 to 99.5% (more preferably, 0.5 to 90%) of the active ingredient in combination with a pharmaceutically acceptable carrier.

[0249] The method of introduction can also be provided by a rechargeable or biodegradable device. In recent years, various sustained release polymeric devices have been developed and tested in vivo for the controlled delivery of drugs, including proteinaceous biologics. Various biocompatible polymers (including hydrogels), including both biodegradable and non-degradable polymers, can be used to form implants for the sustained release of compounds at a specific target site.

[0250] The actual dosage level of the active ingredient in the pharmaceutical composition can be varied to obtain an amount of the active ingredient that is effective to achieve the desired therapeutic response for a particular patient, composition, and mode of administration without being toxic to that particular patient.

[0251] The selected dosage level will depend upon a variety of factors, including the activity of the particular compound or combination of compounds employed, or their esters, salts, or amides, the route of administration, the time of administration, the rate of excretion of the particular compound(s) employed, the duration of treatment, other drugs, compounds, and / or substances used in combination with the particular compound(s) employed, the age, sex, weight, condition, general health, and prior medical history of the patient being treated, and similar factors well known in the medical arts.

[0252] A physician or veterinarian skilled in the art can easily determine and prescribe the therapeutically effective amount of the pharmaceutical composition required. For example, a physician or veterinarian can start the dosage of the pharmaceutical composition or compound at a level lower than that required to achieve the desired therapeutic effect and gradually increase the dosage until the desired effect is achieved. A "therapeutically effective amount" refers to the concentration of the compound sufficient to elicit the desired therapeutic effect. It is generally understood that the effective amount of a compound varies according to the subject's weight, sex, age, and medical history. Other factors that affect the effective amount include, but are not limited to, the severity of the patient's condition, the disorder being treated, the stability of the compound, and, if desired, other types of therapeutic agents being administered together with the compound of the present disclosure. A larger total dose can be delivered by multiple administrations of the agent. Methods for determining efficacy and dosage are known to those skilled in the art (Isselbacher et al. (1996) Harrison's Principles of Internal Medicine, 13th ed., pp. 1814-1882, incorporated herein by reference).

[0253] Generally, the appropriate daily dose of the active compound used in the compositions and methods of the present disclosure will be the amount of compound that is the lowest effective dose that produces a therapeutic effect.This effective dose will generally depend on the factors listed above.

[0254] If desired, the effective daily dose of active compound can be administered as 1, 2, 3, 4, 5, or 6 or more than 6 divided doses, which are administered separately at appropriate intervals throughout the day, if necessary, in unit dosage form.In certain embodiments of the present disclosure, active compound can be administered twice or three times a day.In a preferred embodiment, active compound is administered once a day.

[0255] The patient for this treatment may be any animal in need of treatment, including primates, particularly humans, and other mammals such as horses, cattle, pigs and sheep; as well as poultry and pets in general.

[0256] In certain embodiments, the compounds of the present disclosure may be used alone or may be administered in combination with another type of therapeutic agent. As used herein, the phrase "administered in combination" refers to any form of administration of two or more different therapeutic compounds, such that a second compound is administered while a previously administered therapeutic compound is still effective in the body (e.g., the two compounds are effective in the patient's body simultaneously, which may involve a synergistic effect of the two compounds). For example, different therapeutic compounds can be administered either simultaneously or sequentially, either in the same formulation or in separate formulations. In certain embodiments, different therapeutic compounds can be administered within 1 hour, 12 hours, 24 hours, 36 hours, 48 ​​hours, 72 hours, or within 1 week of each other. Thus, individuals receiving such treatment can benefit from the combined effects of different therapeutic compounds.

[0257] In certain embodiments, co-administration of a compound of the present disclosure with one or more additional therapeutic agent(s) (e.g., one or more additional chemotherapeutic agent(s)) provides improved efficacy compared to the individual administration of a compound of the present disclosure (e.g., a compound of Formula IF, IB, XXIF, or XXIB) or the one or more additional therapeutic agent(s). In certain such embodiments, the co-administration provides an additive effect, where additive effect refers to the sum of the effects of the individual administration of a compound of the present disclosure and one or more additional therapeutic agent(s).

[0258] 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.

[0259] 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.

[0260] 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.

[0261] 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.

[0262] 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.

[0263] 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, and such pharmaceutical compositions are also within the scope of the present disclosure.

[0264] 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 drug...

Claims

[Claim 1] The invention described in the examples.

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