# US 12,594,261 B2 · Use of heterocyclic derivatives with cardiomyocyte proliferation activity for treatment of heart diseases

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- Number: US 12,594,261 B2
- Document ID: US12594261B2
- Status: Granted
- Kind: B2
- Application number: 17/755,399
- Filed: 2019-12-14
- Published: 2022-12-01
- Granted: 2026-04-07
- Earliest claimed: 2019-12-14
- Assignees: Shanghai East Hospital (East Hospital, Tongji University School of Medicine)
- Applicants: Shanghai East Hospital (East Hospital, Tongji University School of Medicine)
- Inventors: Yihan Chen; Dandan Liang; Yi Liu; Subas Man Sakya; Li Li; Fulei Zhang; Huixing Zhou; Xiaoyu He
- Web page: https://patentgrep.com/patent/US12594261B2

## CPC

- A61K 31/4178: not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
- A61K 31/5377: not condensed and containing further heterocyclic rings, e.g. timolol
- A61K 31/4166: having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
- A61K 31/4439: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465)
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Provided herein is the use of heterocyclic derivatives with cardiomyocyte proliferation activity for treatment of heart diseases. Specifically, disclosed is the use of compounds of formula (I) or a pharmaceutically acceptable salt, a solvate, a stereoisomer or a prodrug thereof; and application thereof. Definition of each group in the formula can be found in the specification for details.

## Claims

### Claim 1

A method for promoting growth of cardiomyocytes in vitro, which comprises a step of:
culturing cardiomyocyte in the present of a compound, or a pharmaceutically acceptable salt, a solvate, a stereoisomer or a prodrug;
wherein,
the compound has a structure of Formula I:
wherein
Lb, ring B1 and La together form
ring A1 is selected from the group consisting of C3-C10 heterocyclic group, C4-C10 heteroaryl, and C6-C10 aryl, wherein the heterocycle and heteroaryl each independently have 1-4 heteroatoms selected from N, O, and S;
ring A2 is
Rc is selected from the group consisting of halogen, —OH, nitro, cyano, sulfonyl, R″, —N(R″)2—, R″—O—, R″—S—, R″—S(O)2—, R″—S(O)—, R″—C(O), R″—C(O)O—, and R″—OC(O)—; wherein each R″ is independently selected from the group consisting of H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, C6-C10 aryl, 4- to 7-membered heterocycloalkyl, 5- to 7-membered heteroaryl, —C1-C4 alkylene-C3-C6 cycloalkyl, —C1-C4 alkylene-C6-C10 aryl, —C1-C4 alkylene-4 to 7-membered heterocycloalkyl, and —C1-C4 alkylene-5 to 7-membered heteroaryl; and
Rd is selected from the group consisting of halogen, R″, and R″—O—; wherein each R″ is independently selected from the group consisting of H and C1-C6 alkyl;
n1 is 1, 2, 3, 4 or 5;
n2 is 0, 1, or 2;
or, the compound is selected from the group consisting of:
or, the compound is selected from the following table:
Compound
ID
Name
TJU-B004
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-
{[2-(morpholin-4-yl)ethyl]amino}-4,5-dihydro-1H-
imidazol-5-one
TJU-B005
4-[(2H-1,3-benzodioxol-5-yl)methyl]-2-(phenylamino)-
4,5-dihydro-1H-imidazol-5-one
TJU-B006
(4Z)-4-[(2,3-dihydro-1,4-benzodioxin-6-yl)methylidene]-
2-[(4-methoxyphenyl)amino]-4,5-dihydro-1H-imidazol-
5-one
TJU-B007
(4Z)-4-[(2,3-dihydro-1,4-benzodioxin-6-yl)methylidene]-
2-(phenylamino)-4,5-dihydro-1H-imidazol-5-one
TJU-B009
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-
[(4-methoxyphenyl)amino]-4,5-dihydro-1H-imidazol-
5-one
TJU-B011
(4Z)-4-[(6-chloro-2H-1,3-benzodioxol-5-yl)methylidene]-
2-(phenylamino)-4,5-dihydro-1H-imidazol-5-one
TJU-B013
(4Z)-4-[1-(2H-1,3-benzodioxol-5-yl)ethylidene]-2-
(phenylamino)-4,5-dihydro-1H-imidazol-5-one
TJU-B014
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-1-
methyl-2-(phenylamino)-4,5-dihydro-1H-imidazol-5-one
TJU-B016
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-1-
methyl-2-[(propan-2-yl)amino]-4,5-dihydro-1H-imidazol-
5-one
TJU-B019
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-
(benzylamino)-4,5-dihydro-1H-imidazol-5-one
TJU-B021
(4Z)-2-[(4-aminophenyl)amino]-4-[(2H-1,3-benzodioxol-
5-yl)methylidene]-4,5-dihydro-1H-imidazol-5-one
TJU-B026
(4Z)-4-[(2,3-dihydro-1,4-benzodioxin-6-yl)methylidene]-
2-{[2-(morpholin-4-yl)ethyl]amino}-4,5-dihydro-1H-
imidazol-5-one
TJU-B027
(4Z)-2-[(2H-1,3-benzodioxol-5-yl)amino]-4-[(2H-1,3-
benzodioxol-5-yl)methylidene]-4,5-dihydro-1H-imidazol-
5-one
TJU-B028
(4Z)-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-
yl)methylidene]-2-(phenylamino)-4,5-dihydro-1H-
imidazol-5-one
TJU-B029
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-
[(cyclopropylmethyl)amino]-4,5-dihydro-1H-imidazol-5-
one
TJU-B031
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(pyridin-
3-yl)amino]-4,5-dihydro-1H-imidazol-5-one
TJU-B033
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-
(methylamino)-4,5-dihydro-1H-imidazol-5-one
TJU-B034
(4Z)-2-amino-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-
4,5-dihydro-1H-imidazol-5-one
TJU-B036
(4Z)-2-amino-4-[(3-methoxyphenyl)methylidene]-1-methyl-
4,5-dihydro-1H-imidazol-5-one
TJU-B038
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(propan-
2-yl)amino]-4,5-dihydro-1H-imidazol-5-one
TJU-B039
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-phenyl-
4,5-dihydro-1H-imidazol-5-one
TJU-B040
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-
(ethylamino)-4,5-dihydro-1H-imidazol-5-one
TJU-B043
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-
(phenylamino)-4,5-dihydro-1H-imidazol-5-one
TJU-B045
(4Z)-2-amino-1-methyl-4-(phenylmethylidene)-4,5-dihydro-
1H-imidazol-5-one
TJU-B049
(4Z)-2-amino-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-
yl)methylidene]-4,5-dihydro-1H-imidazol-5-one
TJU-B050
(4Z)-2-amino-4-[(4-fluorophenyl)methylidene]-1-methyl-
4,5-dihydro-1H-imidazol-5-one
TJU-B051
(4Z)-4-[(7-methoxy-2H-1,3-benzodioxol-5-yl)methylidene]-
2-(phenylamino)-4,5-dihydro-1H-imidazol-5-one
TJU-B052
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-
[(cyclopropylmethyl)amino]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B056
(4Z)-2-amino-4-[(3-chlorophenyl)methylidene]-1-methyl-
4,5-dihydro-1H-imidazol-5-one
TJU-B057
(4Z)-2-amino-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-
1-methyl-4,5-dihydro-1H-imidazol-5-one
TJU-B058
4-{[(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-5-oxo-
4,5-dihydro-1H-imidazol-2-yl]amino}benzonitrile
TJU-B059
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-
cyclopropyl-4,5-dihydro-1H-imidazol-5-one
TJU-B060
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(4-
chlorophenyl)amino]-4,5-dihydro-1H-imidazol-5-one
TJU-B063
(4Z)-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-
yl)methylidene]-2-phenyl-4,5-dihydro-1H-imidazol-5-one
TJU-B064
(4Z)-2-amino-4-[(6-chloro-2H-1,3-benzodioxol-5-
yl)methylidene]-4,5-dihydro-1H-imidazol-5-one
TJU-B065
(4Z)-2-amino-4-[(7-methoxy-2H-1,3-benzodioxol-5-
yl)methylidene]-4,5-dihydro-1H-imidazol-5-one
TJU-B066
(4Z)-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-
yl)methylidene]-2-{[2-(morpholin-4-yl)ethyl]amino}-4,5-
dihydro-1H-imidazol-5-one
TJU-B067
(4Z)-2-amino-4-[(2-fluorophenyl)methylidene]-1-methyl-
4,5-dihydro-1H-imidazol-5-one
TJU-B070
(4Z)-2-amino-4-[(3,4-dimethoxyphenyl)methylidene]-1-
methyl-4,5-dihydro-1H-imidazol-5-one
TJU-B085
(4Z)-4-[(3,4-dimethoxyphenyl)methylidene]-2-
(phenylamino)-4,5-dihydro-1H-imidazol-5-one
TJU-B088
(4Z)-2-[(2H-1,3-benzodioxol-5-yl)amino]-4-[(2H-1,3-
benzodioxol-5-yl)methylidene]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B097
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-
[(pyridin-2-yl)amino]-4,5-dihydro-1H-imidazol-5-one
TJU-B110
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(4-
methylphenyl)amino]-4,5-dihydro-1H-imidazol-5-one
TJU-B253
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-
(cyclohexylamino)-4,5-dihydro-1H-imidazol-5-one
TJU-B254
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(2-
methoxyphenyl)amino]-4,5-dihydro-1H-imidazol-5-one.

### Claim 2 (depends on 1)

The method of claim 1, wherein the compound is L41, a pharmaceutically acceptable salt, a solvate, a stereoisomer or a prodrug, or a derivative compound thereof:

### Claim 3

A method for promoting cardiomyocyte proliferation and/or regeneration of cardiomyocyte in vitro, which comprises a step of:
contacting cardiomyocyte with a compound, or a pharmaceutically acceptable salt, a solvate, a stereoisomer or a prodrug, thereby promoting cardiomyocyte proliferation and/or regeneration;
wherein
the compound has a structure of Formula I:
wherein
Lb, ring B1 and La together form
ring A1 is selected from the group consisting of C3-C10 heterocyclic group, C4-C10 heteroaryl, and C6-C10 aryl, wherein the heterocycle and heteroaryl each have 1-4 heteroatoms selected from N, O, and S;
ring A2 is
Rc is selected from the group consisting of halogen, —OH, nitro, cyano, sulfonyl, R″, —N(R″)2—, R″—O—, R″—S—, R″—S(O)2—, R″—S(O)—, R″—C(O), R″—C(O)O—, and R″—OC(O)—; wherein each R″ is independently selected from the group consisting of H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, C6-C10 aryl, 4- to 7-membered heterocycloalkyl, 5- to 7-membered heteroaryl, —C1-C4 alkylene-C3-C6 cycloalkyl, —C1-C4 alkylene-C6-C10 aryl, —C1-C4 alkylene-4 to 7-membered heterocycloalkyl, and —C1-C4 alkylene-5 to 7-membered heteroaryl; and
Rd is selected from the group consisting of halogen, R″, and R″—O—; wherein each R″ is independently selected from the group consisting of H and C1-C6 alkyl;
n1 is 1, 2, 3, 4 or 5;
n2 is 0, 1, or 2;
or, the compound is selected from the group consisting of:
or, the compound is selected from the following table:
Compound ID
Name
TJU-B004
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-{[2-(morpholin-4-yl)
ethyl]amino}-4,5-dihydro-1H-imidazol-5-one
TJU-B005
4-[(2H-1,3-benzodioxol-5-yl)methyl]-2-(phenylamino)-4,5-dihydro-1H-
imidazol-5-one
TJU-B006
(4Z)-4-[(2,3-dihydro-1,4-benzodioxin-6-yl)methylidene]-2-[(4-
methoxyphenyl)amino]-4,5-dihydro-1H-imidazol-5-one
TJU-B007
(4Z)-4-[(2,3-dihydro-1,4-benzodioxin-6-yl)methylidene]-2-(phenylamino)-
4,5-dihydro-1H-imidazol-5-one
TJU-B009
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(4-methoxyphenyl)
amino]-4,5-dihydro-1H-imidazol-5-one
TJU-B011
(4Z)-4-[(6-chloro-2H-1,3-benzodioxol-5-yl)methylidene]-2-(phenylamino)-
4,5-dihydro-1H-imidazol-5-one
TJU-B013
(4Z)-4-[1-(2H-1,3-benzodioxol-5-yl)ethylidene]-2-(phenylamino)-4,5-
dihydro-1H-imidazol-5-one
TJU-B014
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-1-methyl-2-(phenylamino)-
4,5-dihydro-1H-imidazol-5-one
TJU-B016
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-1-methyl-2-[(propan-2-yl)
amino]-4,5-dihydro-1H-imidazol-5-one
TJU-B019
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(benzylamino)-4,5-
dihydro-1H-imidazol-5-one
TJU-B021
(4Z)-2-[(4-aminophenyl)amino]-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-
4,5-dihydro-1H-imidazol-5-one
TJU-B026
(4Z)-4-[(2,3-dihydro-1,4-benzodioxin-6-yl)methylidene]-2-{[2-(morpholin-4-
yl)ethyl]amino}-4,5-dihydro-1H-imidazol-5-one
TJU-B027
(4Z)-2-[(2H-1,3-benzodioxol-5-yl)amino]-4-[(2H-1,3-benzodioxol-5-yl)
methylidene]-4,5-dihydro-1H-imidazol-5-one
TJU-B028
(4Z)-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-yl)methylidene]-2-
(phenylamino)-4,5-dihydro-1H-imidazol-5-one
TJU-B029
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(cyclopropylmethyl)
amino]-4,5-dihydro-1H-imidazol-5-one
TJU-B031
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(pyridin-3-yl)amino]-4,5-
dihydro-1H-imidazol-5-one
TJU-B033
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(methylamino)-4,5-
dihydro-1H-imidazol-5-one
TJU-B034
(4Z)-2-amino-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-4,5-dihydro-1H-
imidazol-5-one
TJU-B036
(4Z)-2-amino-4-[(3-methoxyphenyl)methylidene]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B038
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(propan-2-yl)amino]-4,5-
dihydro-1H-imidazol-5-one
TJU-B039
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-phenyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B040
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(ethylamino)-4,5-dihydro-
1H-imidazol-5-one
TJU-B043
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(phenylamino)-4,5-
dihydro-1H-imidazol-5-one
TJU-B045
(4Z)-2-amino-1-methyl-4-(phenylmethylidene)-4,5-dihydro-1H-imidazol-5-
one
TJU-B049
(4Z)-2-amino-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-yl)methylidene]-4,5-
dihydro-1H-imidazol-5-one
TJU-B050
(4Z)-2-amino-4-[(4-fluorophenyl)methylidene]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B051
(4Z)-4-[(7-methoxy-2H-1,3-benzodioxol-5-yl)methylidene]-2-(phenylamino)-
4,5-dihydro-1H-imidazol-5-one
TJU-B052
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(cyclopropylmethyl)
amino]-1-methyl-4,5-dihydro-1H-imidazol-5-one
TJU-B056
(4Z)-2-amino-4-[(3-chlorophenyl)methylidene]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B057
(4Z)-2-amino-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-1-methyl-4,5-
dihydro-1H-imidazol-5-one
TJU-B058
4-{[(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-5-oxo-4,5-dihydro-1H-
imidazol-2-yl]amino} benzonitrile
TJU-B059
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-cyclopropyl-4,5-dihydro-
1H-imidazol-5-one
TJU-B060
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(4-chlorophenyl)amino]-
4,5-dihydro-1H-imidazol-5-one
TJU-B063
(4Z)-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-yl)methylidene]-2-phenyl-4,5-
dihydro-1H-imidazol-5-one
TJU-B064
(4Z)-2-amino-4-[(6-chloro-2H-1,3-benzodioxol-5-yl)methylidene]-4,5-
dihydro-1H-imidazol-5-one
TJU-B065
(4Z)-2-amino-4-[(7-methoxy-2H-1,3-benzodioxol-5-yl)methylidene]-4,5-
dihydro-1H-imidazol-5-one
TJU-B066
(4Z)-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-yl)methylidene]-2-{[2-
(morpholin-4-yl)ethyl]amino}-4,5-dihydro-1H-imidazol-5-one
TJU-B067
(4Z)-2-amino-4-[(2-fluorophenyl)methylidene]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B070
(4Z)-2-amino-4-[(3,4-dimethoxyphenyl)methylidene]-1-methyl-4,5-dihydro-
1H-imidazol-5-one
TJU-B085
(4Z)-4-[(3,4-dimethoxyphenyl)methylidene]-2-(phenylamino)-4,5-dihydro-
1H-imidazol-5-one
TJU-B088
(4Z)-2-[(2H-1,3-benzodioxol-5-yl)amino]-4-[(2H-1,3-benzodioxol-5-yl)
methylidene]-1-methyl-4,5-dihydro-1H-imidazol-5-one
TJU-B097
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(pyridin-2-yl)amino]-4,5-
dihydro-1H-imidazol-5-one
TJU-B110
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(4-methylphenyl)
amino]-4,5-dihydro-1H-imidazol-5-one
TJU-B253
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(cyclohexylamino)-4,5-
dihydro-1H-imidazol-5-one
TJU-B254
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(2-methoxyphenyl)
amino]-4,5-dihydro-1H-imidazol-5-one

### Claim 4 (depends on 3)

The method of claim 3, wherein the compound is L41, a pharmaceutically acceptable salt, a solvate, a stereoisomer or a prodrug, or a derivative compound thereof:

### Claim 5

A method for treating a cardiovascular disease, which comprises a step of: administering a compound or a pharmaceutically acceptable salt, a solvate, a stereoisomer or a prodrug to a subject in need;
wherein
the compound has a structure of Formula I:
wherein
Lb, ring B1 and La together form
ring A1 is selected from the group consisting of C3-C10 heterocyclic group, C4-C10 heteroaryl, and C6-C10 aryl, wherein the heterocycle and heteroaryl each have 1-4 heteroatoms selected from N, O, and S;
ring A2 is
Rc is selected from the group consisting of halogen, —OH, nitro, cyano, sulfonyl, R″, —N(R″)2—, R″—O—, R″—S—, R″—S(O)2—, R″—S(O)—, R″—C(O), R″—C(O)O—, and R″—OC(O)—; wherein each R″ is independently selected from the group consisting of H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, C6-C10 aryl, 4- to 7-membered heterocycloalkyl, 5- to 7-membered heteroaryl, —C1-C4 alkylene-C3-C6 cycloalkyl, —C1-C4 alkylene-C6-C10 aryl, —C1-C4 alkylene-4 to 7-membered heterocycloalkyl, and —C1-C4 alkylene-5 to 7-membered heteroaryl; and
Rd is selected from the group consisting of halogen, R″, and R″—O—; wherein R″ is each independently selected from the group consisting of H, C1-C6 alkyl;
n1 is 1, 2, 3, 4 or 5;
n2 is 0, 1, or 2;
or, the compound is selected from the group consisting of:
or, the compound is selected from the following table:
Compound ID
Name
TJU-B004
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-{[2-(morpholin-4-yl)ethyl]
amino}-4,5-dihydro-1H-imidazol-5-one
TJU-B005
4-[(2H-1,3-benzodioxol-5-yl)methyl]-2-(phenylamino)-4,5-dihydro-1H-
imidazol-5-one
TJU-B006
(4Z)-4-[(2,3-dihydro-1,4-benzodioxin-6-yl)methylidene]-2-[(4-methoxyphenyl)
amino]-4,5-dihydro-1H-imidazol-5-one
TJU-B007
(4Z)-4-[(2,3-dihydro-1,4-benzodioxin-6-yl)methylidene]-2-(phenylamino)-4,5-
dihydro-1H-imidazol-5-one
TJU-B009
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(4-methoxyphenyl)amino]-
4,5-dihydro-1H-imidazol-5-one
TJU-B011
(4Z)-4-[(6-chloro-2H-1,3-benzodioxol-5-yl)methylidene]-2-(phenylamino)-4,5-
dihydro-1H-imidazol-5-one
TJU-B013
(4Z)-4-[1-(2H-1,3-benzodioxol-5-yl)ethylidene]-2-(phenylamino)-4,5-dihydro-
1H-imidazol-5-one
TJU-B014
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-1-methyl-2-(phenylamino)-4,5-
dihydro-1H-imidazol-5-one
TJU-B016
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-1-methyl-2-[(propan-2-yl)
amino]-4,5-dihydro-1H-imidazol-5-one
TJU-B019
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(benzylamino)-4,5-dihydro-
1H-imidazol-5-one
TJU-B021
(4Z)-2-[(4-aminophenyl)amino]-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-4,5-
dihydro-1H-imidazol-5-one
TJU-B026
(4Z)-4-[(2,3-dihydro-1,4-benzodioxin-6-yl)methylidene]-2-{[2-(morpholin-4-yl)
ethyl]amino}-4,5-dihydro-1H-imidazol-5-one
TJU-B027
(4Z)-2-[(2H-1,3-benzodioxol-5-yl)amino]-4-[(2H-1,3-benzodioxol-5-yl)
methylidene]-4,5-dihydro-1H-imidazol-5-one
TJU-B028
(4Z)-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-yl)methylidene]-2-(phenylamino)-
4,5-dihydro-1H-imidazol-5-one
TJU-B029
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(cyclopropylmethyl)amino]-
4,5-dihydro-1H-imidazol-5-one
TJU-B031
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(pyridin-3-yl)amino]-4,5-
dihydro-1H-imidazol-5-one
TJU-B033
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(methylamino)-4,5-dihydro-
1H-imidazol-5-one
TJU-B034
(4Z)-2-amino-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-4,5-dihydro-1H-
imidazol-5-one
TJU-B036
(4Z)-2-amino-4-[(3-methoxyphenyl)methylidene]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B038
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(propan-2-yl)amino]-4,5-
dihydro-1H-imidazol-5-one
TJU-B039
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-phenyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B040
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(ethylamino)-4,5-dihydro-1H-
imidazol-5-one
TJU-B043
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(phenylamino)-4,5-dihydro-
1H-imidazol-5-one
TJU-B045
(4Z)-2-amino-1-methyl-4-(phenylmethylidene)-4,5-dihydro-1H-imidazol-5-one
TJU-B049
(4Z)-2-amino-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-yl)methylidene]-4,5-
dihydro-1H-imidazol-5-one
TJU-B050
(4Z)-2-amino-4-[(4-fluorophenyl)methylidene]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B051
(4Z)-4-[(7-methoxy-2H-1,3-benzodioxol-5-yl)methylidene]-2-(phenylamino)-
4,5-dihydro-1H-imidazol-5-one
TJU-B052
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(cyclopropylmethyl)amino]-
1-methyl-4,5-dihydro-1H-imidazol-5-one
TJU-B056
(4Z)-2-amino-4-[(3-chlorophenyl)methylidene]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B057
(4Z)-2-amino-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-1-methyl-4,5-dihydro-
1H-imidazol-5-one
TJU-B058
4-{[(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-5-oxo-4,5-dihydro-1H-imid
azol-2-yl]amino}benzonitrile
TJU-B059
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-cyclopropyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B060
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(4-chlorophenyl)amino]-4,5-
dihydro-1H-imidazol-5-one
TJU-B063
(4Z)-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-yl)methylidene]-2-phenyl-4,5-
dihydro-1H-imidazol-5-one
TJU-B064
(4Z)-2-amino-4-[(6-chloro-2H-1,3-benzodioxol-5-yl)methylidene]-4,5-dihydro-
1H-imidazol-5-one
TJU-B065
(4Z)-2-amino-4-[(7-methoxy-2H-1,3-benzodioxol-5-yl)methylidene]-4,5-
dihydro-1H-imidazol-5-one
TJU-B066
(4Z)-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-yl)methylidene]-2-{[2-(morpholin-
4-yl)ethyl]amino}-4,5-dihydro-1H-imidazol-5-one
TJU-B067
(4Z)-2-amino-4-[(2-fluorophenyl)methylidene]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B070
(4Z)-2-amino-4-[(3,4-dimethoxyphenyl)methylidene]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B085
(4Z)-4-[(3,4-dimethoxyphenyl)methylidene]-2-(phenylamino)-4,5-dihydro-1H-
imidazol-5-one
TJU-B088
(4Z)-2-[(2H-1,3-benzodioxol-5-yl)amino]-4-[(2H-1,3-benzodioxol-5-yl)
methylidene]-1-methyl-4,5-dihydro-1H-imidazol-5-one
TJU-B097
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(pyridin-2-yl)amino]-4,5-
dihydro-1H-imidazol-5-one
TJU-B110
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(4-methylphenyl)amino]-4,5-
dihydro-1H-imidazol-5-one
TJU-B253
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(cyclohexylamino)-4,5-
dihydro-1H-imidazol-5-one
TJU-B254
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(2-methoxyphenyl)amino]-
4,5-dihydro-1H-imidazol-5-one

### Claim 6 (depends on 5)

The method of claim 5, wherein the subjects comprises human and non-human mammal.

### Claim 7 (depends on 5)

The method of claim 5, wherein the compound is L41, a pharmaceutically acceptable salt, a solvate, a stereoisomer or a prodrug, or a derivative compound thereof:

### Claim 8 (depends on 1)

The method of claim 1, wherein the compound is selected from the group consisting of
or
the compound is selected from the following table
Compound ID
Name
TJU-B004
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-{[2-(morpholin-4-yl)ethyl]
amino}-4,5-dihydro-1H-imidazol-5-one
TJU-B005
4-[(2H-1,3-benzodioxol-5-yl)methyl]-2-(phenylamino)-4,5-dihydro-1H-
imidazol-5-one
TJU-B006
(4Z)-4-[(2,3-dihydro-1,4-benzodioxin-6-yl)methylidene]-2-[(4-methoxyphenyl)
amino]-4,5-dihydro-1H-imidazol-5-one
TJU-B007
(4Z)-4-[(2,3-dihydro-1,4-benzodioxin-6-yl)methylidene]-2-(phenylamino)-4,5-
dihydro-1H-imidazol-5-one
TJU-B009
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(4-methoxyphenyl)amino]-
4,5-dihydro-1H-imidazol-5-one
TJU-B011
(4Z)-4-[(6-chloro-2H-1,3-benzodioxol-5-yl)methylidene]-2-(phenylamino)-4,5-
dihydro-1H-imidazol-5-one
TJU-B013
(4Z)-4-[1-(2H-1,3-benzodioxol-5-yl)ethylidene]-2-(phenylamino)-4,5-dihydro-
1H-imidazol-5-one
TJU-B014
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-1-methyl-2-(phenylamino)-4,5-
dihydro-1H-imidazol-5-one
TJU-B016
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-1-methyl-2-[(propan-2-yl)
amino]-4,5-dihydro-1H-imidazol-5-one
TJU-B019
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(benzylamino)-4,5-dihydro-
1H-imidazol-5-one
TJU-B021
(4Z)-2-[(4-aminophenyl)amino]-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-
4,5-dihydro-1H-imidazol-5-one
TJU-B026
(4,54Z)-4-[(2,3-dihydro-1,4-benzodioxin-6-yl)methylidene]-2-{[2-(morpholin-4-
yl)ethyl]amino}-4,5-dihydro-1H-imidazol-5-one
TJU-B027
(4Z)-2-[(2H-1,3-benzodioxol-5-yl)amino]-4-[(2H-1,3-benzodioxol-5-yl)
methylidene]-4,5-dihydro-1H-imidazol-5-one
TJU-B028
(4Z)-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-yl)methylidene]-2-(phenylamino)-
4,5-dihydro-1H-imidazol-5-one
TJU-B029
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(cyclopropylmethyl)amino]-
4,5-dihydro-1H-imidazol-5-one
TJU-B031
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(pyridin-3-yl)amino]-4,5-
dihydro-1H-imidazol-5-one
TJU-B033
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(methylamino)-4,5-dihydro-
1H-imidazol-5-one
TJU-B034
(4Z)-2-amino-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-4,5-dihydro-1H-
imidazol-5-one
TJU-B036
(4Z)-2-amino-4-[(3-methoxyphenyl)methylidene]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B038
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(propan-2-yl)amino]-4,5-
dihydro-1H-imidazol-5-one
TJU-B039
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-phenyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B040
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(ethylamino)-4,5-dihydro-
1H-imidazol-5-one
TJU-B043
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(phenylamino)-4,5-dihydro-
1H-imidazol-5-one
TJU-B045
(4Z)-2-amino-1-methyl-4-(phenylmethylidene)-4,5-dihydro-1H-imidazol-5-one
TJU-B049
(4Z)-2-amino-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-yl)methylidene]-4,5-
dihydro-1H-imidazol-5-one
TJU-B050
(4Z)-2-amino-4-[(4-fluorophenyl)methylidene]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B051
(4Z)-4-[(7-methoxy-2H-1,3-benzodioxol-5-yl)methylidene]-2-(phenylamino)-
4,5-dihydro-1H-imidazol-5-one
TJU-B052
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(cyclopropylmethyl)amino]-
1-methyl-4,5-dihydro-1H-imidazol-5-one
TJU-B056
(4Z)-2-amino-4-[(3-chlorophenyl)methylidene]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B057
(4Z)-2-amino-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-1-methyl-4,5-
dihydro-1H-imidazol-5-one
TJU-B058
4-{[(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-5-oxo-4,5-dihydro-1H-
imidazol-2-yl]amino}benzonitrile
TJU-B059
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-cyclopropyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B060
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(4-chlorophenyl)amino]-
4,5-dihydro-1H-imidazol-5-one
TJU-B063
(4Z)-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-yl)methylidene]-2-phenyl-4,5-
dihydro-1H-imidazol-5-one
TJU-B064
(4Z)-2-amino-4-[(6-chloro-2H-1,3-benzodioxol-5-yl)methylidene]-4,5-dihydro-
1H-imidazol-5-one
TJU-B065
(4Z)-2-amino-4-[(7-methoxy-2H-1,3-benzodioxol-5-yl)methylidene]-4,5-
dihydro-1H-imidazol-5-one
TJU-B066
(4Z)-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-yl)methylidene]-2-{[2-(morpholin-
4-yl)ethyl]amino}-4,5-dihydro-1H-imidazol-5-one
TJU-B067
(4Z)-2-amino-4-[(2-fluorophenyl)methylidene]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B070
(4Z)-2-amino-4-[(3,4-dimethoxyphenyl)methylidene]-1-methyl-4,5-dihydro-
1H-imidazol-5-one
TJU-B085
(4Z)-4-[(3,4-dimethoxyphenyl)methylidene]-2-(phenylamino)-4,5-dihydro-1H-
imidazol-5-one
TJU-B088
(4Z)-2-[(2H-1,3-benzodioxol-5-yl)amino]-4-[(2H-1,3-benzodioxol-5-yl)
methylidene]-1-methyl-4,5-dihydro-1H-imidazol-5-one
TJU-B097
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(pyridin-2-yl)amino]-4,5-
dihydro-1H-imidazol-5-one
TJU-B110
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(4-methylphenyl)amino]-
4,5-dihydro-1H-imidazol-5-one
TJU-B253
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(cyclohexylamino)-4,5-
dihydro-1H-imidazol-5-one
TJU-B254
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(2-methoxyphenyl)amino]-
4,5-dihydro-1H-imidazol-5-one

### Claim 9 (depends on 3)

The method of claim 3, wherein the compound is selected from the group consisting of
or
the compound is selected from the following table
Compound ID
Name
TJU-B004
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-{[2-(morpholin-4-yl)ethyl]
amino}-4,5-dihydro-1H-imidazol-5-one
TJU-B005
4-[(2H-1,3-benzodioxol-5-yl)methyl]-2-(phenylamino)-4,5-dihydro-1H-
imidazol-5-one
TJU-B006
(4Z)-4-[(2,3-dihydro-1,4-benzodioxin-6-yl)methylidene]-2-[(4-methoxyphenyl)
amino]-4,5-dihydro-1H-imidazol-5-one
TJU-B007
(4Z)-4-[(2,3-dihydro-1,4-benzodioxin-6-yl)methylidene]-2-(phenylamino)-4,5-
dihydro-1H-imidazol-5-one
TJU-B009
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(4-methoxyphenyl)amino]-
4,5-dihydro-1H-imidazol-5-one
TJU-B011
(4Z)-4-[(6-chloro-2H-1,3-benzodioxol-5-yl)methylidene]-2-(phenylamino)-4,5-
dihydro-1H-imidazol-5-one
TJU-B013
(4Z)-4-[1-(2H-1,3-benzodioxol-5-yl)ethylidene]-2-(phenylamino)-4,5-dihydro-
1H-imidazol-5-one
TJU-B014
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-1-methyl-2-(phenylamino)-4,5-
dihydro-1H-imidazol-5-one
TJU-B016
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-1-methyl-2-[(propan-2-yl)
amino]-4,5-dihydro-1H-imidazol-5-one
TJU-B019
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(benzylamino)-4,5-dihydro-
1H-imidazol-5-one
TJU-B021
(4Z)-2-[(4-aminophenyl)amino]-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-
4,5-dihydro-1H-imidazol-5-one
TJU-B026
(4Z)-4-[(2,3-dihydro-1,4-benzodioxin-6-yl)methylidene]-2-{[2-(morpholin-4-
yl)ethyl]amino}-4,5-dihydro-1H-imidazol-5-one
TJU-B027
(4Z)-2-[(2H-1,3-benzodioxol-5-yl)amino]-4-[(2H-1,3-benzodioxol-5-yl)
methylidene]-4,5-dihydro-1H-imidazol-5-one
TJU-B028
(4Z)-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-yl)methylidene]-2-(phenylamino)-
4,5-dihydro-1H-imidazol-5-one
TJU-B029
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(cyclopropylmethyl)amino]-
4,5-dihydro-1H-imidazol-5-one
TJU-B031
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(pyridin-3-yl)amino]-4,5-
dihydro-1H-imidazol-5-one
TJU-B033
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(methylamino)-4,5-dihydro-
1H-imidazol-5-one
TJU-B034
(4Z)-2-amino-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-4,5-dihydro-1H-
imidazol-5-one
TJU-B036
(4Z)-2-amino-4-[(3-methoxyphenyl)methylidene]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B038
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(propan-2-yl)amino]-4,5-
dihydro-1H-imidazol-5-one
TJU-B039
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-phenyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B040
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(ethylamino)-4,5-dihydro-
1H-imidazol-5-one
TJU-B043
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(phenylamino)-4,5-dihydro-
1H-imidazol-5-one
TJU-B045
(4Z)-2-amino-1-methyl-4-(phenylmethylidene)-4,5-dihydro-1H-imidazol-5-one
TJU-B049
(4Z)-2-amino-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-yl)methylidene]-4,5-
dihydro-1H-imidazol-5-one
TJU-B050
(4Z)-2-amino-4-[(4-fluorophenyl)methylidene]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B051
(4Z)-4-[(7-methoxy-2H-1,3-benzodioxol-5-yl)methylidene]-2-(phenylamino)-
4,5-dihydro-1H-imidazol-5-one
TJU-B052
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(cyclopropylmethyl)amino]-
1-methyl-4,5-dihydro-1H-imidazol-5-one
TJU-B056
(4Z)-2-amino-4-[(3-chlorophenyl)methylidene]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B057
(4Z)-2-amino-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-1-methyl-4,5-dihydro-
1H-imidazol-5-one
TJU-B058
4-{[(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-5-oxo-4,5-dihydro-1H-
imidazol-2-yl]amino} benzonitrile
TJU-B059
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-cyclopropyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B060
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(4-chlorophenyl)amino]-
4,5-dihydro-1H-imidazol-5-one
TJU-B063
(4Z)-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-yl)methylidene]-2-phenyl-4,5-
dihydro-1H-imidazol-5-one
TJU-B064
(4Z)-2-amino-4-[(6-chloro-2H-1,3-benzodioxol-5-yl)methylidene]-4,5-dihydro-
1H-imidazol-5-one
TJU-B065
(4Z)-2-amino-4-[(7-methoxy-2H-1,3-benzodioxol-5-yl)methylidene]-4,5-
dihydro-1H-imidazol-5-one
TJU-B066
(4Z)-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-yl)methylidene]-2-{[2-(morpholin-
4-yl)ethyl]amino}-4,5-dihydro-1H-imidazol-5-one
TJU-B067
(4Z)-2-amino-4-[(2-fluorophenyl)methylidene]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B070
(4Z)-2-amino-4-[(3,4-dimethoxyphenyl)methylidene]-1-methyl-4,5-dihydro-
1H-imidazol-5-one
TJU-B085
(4Z)-4-[(3,4-dimethoxyphenyl)methylidene]-2-(phenylamino)-4,5-dihydro-1H-
imidazol-5-one
TJU-B088
(4Z)-2-[(2H-1,3-benzodioxol-5-yl)amino]-4-[(2H-1,3-benzodioxol-5-yl)
methylidene]-1-methyl-4,5-dihydro-1H-imidazol-5-one
TJU-B097
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(pyridin-2-yl)amino]-4,5-
dihydro-1H-imidazol-5-one
TJU-B110
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(4-methylphenyl)amino]-
4,5-dihydro-1H-imidazol-5-one
TJU-B253
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(cyclohexylamino)-4,5-
dihydro-1H-imidazol-5-one
TJU-B254
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(2-methoxyphenyl)amino]-
4,5-dihydro-1H-imidazol-5-one

### Claim 10 (depends on 5)

The method of claim 5, wherein the compound is selected from the group consisting of
or
the compound is selected from the following table
Compound ID
Name
TJU-B004
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-{[2-(morpholin-4-yl)ethyl]
amino}-4,5-dihydro-1H-imidazol-5-one
TJU-B005
4-[(2H-1,3-benzodioxol-5-yl)methyl]-2-(phenylamino)-4,5-dihydro-1H-
imidazol-5-one
TJU-B006
(4Z)-4-[(2,3-dihydro-1,4-benzodioxin-6-yl)methylidene]-2-[(4-methoxyphenyl)
amino]-4,5-dihydro-1H-imidazol-5-one
TJU-B007
(4Z)-4-[(2,3-dihydro-1,4-benzodioxin-6-yl)methylidene]-2-(phenylamino)-4,5-
dihydro-1H-imidazol-5-one
TJU-B009
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(4-methoxyphenyl)amino]-
4,5-dihydro-1H-imidazol-5-one
TJU-B011
(4Z)-4-[(6-chloro-2H-1,3-benzodioxol-5-yl)methylidene]-2-(phenylamino)-4,5-
dihydro-1H-imidazol-5-one
TJU-B013
(4Z)-4-[1-(2H-1,3-benzodioxol-5-yl)ethylidene]-2-(phenylamino)-4,5-dihydro-
1H-imidazol-5-one
TJU-B014
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-1-methyl-2-(phenylamino)-4,5-
dihydro-1H-imidazol-5-one
TJU-B016
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-1-methyl-2-[(propan-2-yl)
amino]-4,5-dihydro-1H-imidazol-5-one
TJU-B019
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(benzylamino)-4,5-dihydro-
1H-imidazol-5-one
TJU-B021
(4Z)-2-[(4-aminophenyl)amino]-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-
4,5-dihydro-1H-imidazol-5-one
TJU-B026
(4Z)-4-[(2,3-dihydro-1,4-benzodioxin-6-yl)methylidene]-2-{[2-(morpholin-4-
yl)ethyl]amino}-4,5-dihydro-1H-imidazol-5-one
TJU-B027
(4Z)-2-[(2H-1,3-benzodioxol-5-yl)amino]-4-[(2H-1,3-benzodioxol-5-yl)
methylidene]-4,5-dihydro-1H-imidazol-5-one
TJU-B028
(4Z)-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-yl)methylidene]-2-(phenylamino)-
4,5-dihydro-1H-imidazol-5-one
TJU-B029
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(cyclopropylmethyl)amino]-
4,5-dihydro-1H-imidazol-5-one
TJU-B031
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(pyridin-3-yl)amino]-4,5-
dihydro-1H-imidazol-5-one
TJU-B033
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(methylamino)-4,5-dihydro-
1H-imidazol-5-one
TJU-B034
(4Z)-2-amino-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-4,5-dihydro-1H-
imidazol-5-one
TJU-B036
(4Z)-2-amino-4-[(3-methoxyphenyl)methylidene]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B038
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(propan-2-yl)amino]-4,5-
dihydro-1H-imidazol-5-one
TJU-B039
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-phenyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B040
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(ethylamino)-4,5-dihydro-
1H-imidazol-5-one
TJU-B043
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(phenylamino)-4,5-dihydro-
1H-imidazol-5-one
TJU-B045
(4Z)-2-amino-1-methyl-4-(phenylmethylidene)-4,5-dihydro-1H-imidazol-5-one
TJU-B049
(4Z)-2-amino-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-yl)methylidene]-4,5-
dihydro-1H-imidazol-5-one
TJU-B050
(4Z)-2-amino-4-[(4-fluorophenyl)methylidene]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B051
(4Z)-4-[(7-methoxy-2H-1,3-benzodioxol-5-yl)methylidene]-2-(phenylamino)-
4,5-dihydro-1H-imidazol-5-one
TJU-B052
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(cyclopropylmethyl)amino]-
1-methyl-4,5-dihydro-1H-imidazol-5-one
TJU-B056
(4Z)-2-amino-4-[(3-chlorophenyl)methylidene]-1-methyl-4,5-dihydro-1H-
zimidaol-5-one
TJU-B057
(4Z)-2-amino-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-1-methyl-4,5-dihydro-
1H-imidazol-5-one
TJU-B058
4-{[(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-5-oxo-4,5-dihydro-1H-
imidazol-2-yl]amino } benzonitrile
TJU-B059
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-cyclopropyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B060
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(4-chlorophenyl)amino]-4,5-
dihydro-1H-imidazol-5-one
TJU-B063
(4Z)-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-yl)methylidene]-2-phenyl-4,5-
dihydro-1H-imidazol-5-one
TJU-B064
(4Z)-2-amino-4-[(6-chloro-2H-1,3-benzodioxol-5-yl)methylidene]-4,5-dihydro-
1H-imidazol-5-one
TJU-B065
(4Z)-2-amino-4-[(7-methoxy-2H-1,3-benzodioxol-5-yl)methylidene]-4,5-
dihydro-1H-imidazol-5-one
TJU-B066
(4Z)-4-[(2,2-difluoro-2H-1,3-benzodioxol-5-yl)methylidene]-2-{[2-(morpholin-
4-yl)ethyl]amino}-4,5-dihydro-1H-imidazol-5-one
TJU-B067
(4Z)-2-amino-4-[(2-fluorophenyl)methylidene]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B070
(4Z)-2-amino-4-[(3,4-dimethoxyphenyl)methylidene]-1-methyl-4,5-dihydro-1H-
imidazol-5-one
TJU-B085
(4Z)-4-[(3,4-dimethoxyphenyl)methylidene]-2-(phenylamino)-4,5-dihydro-1H-
imidazol-5-one
TJU-B088
(4Z)-2-[(2H-1,3-benzodioxol-5-yl)amino]-4-[(2H-1,3-benzodioxol-5-yl)
methylidene]-1-methyl-4,5-dihydro-1H-imidazol-5-one
TJU-B097
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(pyridin-2-yl)amino]-4,5-
dihydro-1H-imidazol-5-one
TJU-B110
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(4-methylphenyl)amino]-4,5-
dihydro-1H-imidazol-5-one
TJU-B253
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-(cyclohexylamino)-4,5-
dihydro-1H-imidazol-5-one
TJU-B254
(4Z)-4-[(2H-1,3-benzodioxol-5-yl)methylidene]-2-[(2-methoxyphenyl)amino]-4,
5-dihydro-1H-imidazol-5-one