IP Library › Granted Patent US 12,404,268

Granted Patent B2

US 12,404,268 · App. 17/433,193 · Granted Sep 2, 2025

2-heteroaryl aminoquinazolinone derivative

Inventors: Kazuto Mori (Osaka, JP); Hiroyuki Kitano (Osaka, JP); Tomoyuki Furuta (Osaka, JP); Hajime Seki (Osaka, JP); Yohei Kobayashi (Osaka, JP)

Assignee: Sumitomo Pharma Co., Ltd.

C07D413/12 A61K31/506 A61K45/06 A61P25/08 A61P25/28 C07D401/12 C07D401/14 C07D403/12 C07D471/04

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Patent No.: US 12,404,268
App. No.: 17/433,193
Granted: Sep 2, 2025
Kind: B2

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Abstract

Provided is a 2-heteroaryl aminoquinazolinone derivative, which is a compound represented by formula (1): or a pharmaceutically acceptable salt thereof wherein X 1 represents CR 1 or N, X 2 represents CR 2 or N, X 3 represents CR 3 or N, X 4 represents CR 4 or N, Y represents optionally substituted C 1-6 alkyl, an optionally substituted C 3-10 alicyclic group, an optionally substituted 4- to 10-membered nitrogen-containing non-aryl heterocycle, optionally substituted C 6-10 aryl, or optionally substituted 5- to 10-membered heteroaryl, Z represents optionally substituted 6- to 10-membered heteroaryl, and R 1 , R 2 , R 3 , and R 4 each independently represent a hydrogen atom, halogen, cyano, optionally substituted C 1-6 alkyl, optionally substituted C 1-6 alkoxy, or the like.

Claims (118)

1. A compound represented by formula (1):

or a pharmaceutically acceptable salt thereof,

wherein

X 1 represents CR 1 or N,

X 2 represents CR 2 or N,

X 3 represents CR 3 or N,

X 4 represents CR 4 or N,

wherein (1) if X 1 is N, X 2 is CR 2 , X 3 is CR 3 , and X 4 is CR 4 , (2) if X 2 is N, X 1 is CR 1 , X 3 is CR 3 , and X 4 is CR 4 , (3) if X 3 is N, X 1 is CR 1 , X 2 is CR 2 , and X 4 is CR 4 , and (4) if X 4 is N, X 1 is CR 1 , X 2 is CR 2 , and X 3 is CR 3 ,

Y represents optionally substituted C 1-6 alkyl, an optionally substituted C 3-10 alicyclic group, an optionally substituted 4- to 10-membered non-aryl heterocycle, optionally substituted C 6-10 aryl, or optionally substituted 5- to 10-membered heteroaryl,

Z represents optionally substituted 5- to 10-membered heteroaryl, wherein when Z is substituted, it is substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, cyano, dimethylamino, C 1-6 alkoxy, and C 1-6 alkyl (wherein the alkoxy and the alkyl are each independently optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, hydroxy, and C 1-6 alkoxy),

wherein Z does not attach to a nitrogen atom to which the heteroaryl attaches at a nitrogen atom on a ring of the

heteroaryl group

R 1 , R 2 , R 3 , and R 4 each independently represent a hydrogen atom, halogen, cyano, C 1-6 alkylsulfonyl, —SO 2 —NR 5 R 6 , —NR 7 R 8 , —NR 9 —C(═O)R 10 , —NR 11 —SO 2 —R 12 , —C(═O)NR 13 R 14 , —C(═O)OR 15 , optionally substituted C 1-6 alkyl, or optionally substituted C 1-6 alkoxy,

R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , R 14 , and R 15 are the same or different, each independently, and if there are multiple instances, they each independently represent a hydrogen atom, a C 3-6 alicyclic group, or C 1-6 alkyl (wherein the alicyclic group and the alkyl are each independently optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, a hydroxyl group, a C 3-10 alicyclic group, C 1-6 alkoxy, and a 4- to 6-membered non-aryl heterocyclic group), wherein R 5 and R 6 , R 7 and R 8 , and R 13 and R 14 , together with the nitrogen atom to which they are attached, may form a 4- to 10-membered nitrogen-containing non-aryl heterocyclic group (wherein the ring is optionally substituted with 1 to 5 of the same or different substituents selected from the group consisting of halogen, hydroxy, C 1-6 alkyl, and C 1-6 alkoxy),

provided that the compound is not:

a compound represented by formula (W-1):

wherein

Z a is optionally substituted 5- to 10-membered heteroaryl;

a compound represented by formula (W-2):

wherein

X a is O or S, and Y b is ethyl, unsubstituted phenyl, 4-chlorophenyl, or 4-methoxyphenyl;

a compound represented by formula (W-3):

wherein

X c is —S— or —SO 2 —, and Y c is unsubstituted phenyl, 4-chlorophenyl, or 4-methoxyphenyl;

a compound represented by formula (W-4):

wherein

X d is methoxy, chloro, or dimethylamino, and Y d is ethyl, unsubstituted phenyl, 4-chlorophenyl, or 4-methoxyphenyl;

2-{(4,6-dimethylpyrimidin-2-yl)amino}-3-isopentylquinazolin-4 (3H)-one;

3-(pyridin-2-yl)-2-(pyridin-2-ylamino) quinazolin-4 (3H)-one;

3-methyl-2-{[2-((1-methylpiperidin-4-yl) methoxy)pyridin-3-yl]amino}pyrido[3,4-d]pyrimidin-4 (3H)-one; or

3-methyl-2-{[2-((1-methylpiperidin-4-yl) methoxy)pyridin-3-yl]amino}pyrido[2,3-d]pyrimidin-4 (3H)-one.

2. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein X 1 is CR 1 .

3. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein X 2 is CR 2 .

4. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein X 3 is CR 3 .

5. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein X 4 is CR 4 .

6. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein R 1 , R 2 , R 3 , and R 4 are each independently a hydrogen atom, halogen, cyano, C 1-6 alkoxy, or C 1-6 alkyl (wherein the alkoxy and the alkyl are each independently optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, hydroxy, and C 1-6 alkoxy).

7. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein R 1 , R 3 , and R 4 are all hydrogen atoms, and R 2 is a hydrogen atom, halogen, cyano, C 1-6 alkyl (wherein the alkyl is optionally substituted with 1 to 3 fluorine or a methoxy group), or C 1-6 alkoxy.

8. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein R 1 , R 3 , and R 4 are all hydrogen atoms, and R 2 is a hydrogen atom, fluorine, chloro, cyano, or C 1-6 alkyl (wherein the alkyl is optionally substituted with 1 to 3 fluorine or a methoxy group).

9. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein R 1 , R 3 , and R 4 are all hydrogen atoms, and R 2 is fluorine or cyano.

10. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein Y is

(1) C 1-6 alkyl optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, hydroxy, amino, dimethylamino, a C 3-6 alicyclic group, a 4- to 10-membered nitrogen-containing non-aryl heterocyclic group, C 1-6 alkoxy, C 6-10 aryl (wherein the alicyclic group, the nitrogen-containing non-aryl heterocyclic group, the alkoxy, and the aryl group are each independently optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, cyano, a C 3-6 alicyclic group, C 1-6 alkyl optionally substituted with 1 to 5 fluorine, and C 1-6 alkoxy), and 5- to 10-membered heteroaryl (wherein the heteroaryl group is optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, cyano, a C 3-6 alicyclic group, C 1-6 alkyl optionally substituted with 1 to 5 fluorine, and C 1-6 alkoxy),

(2) a C 3-10 alicyclic group optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, hydroxy, amino, dimethylamino, C 1-6 alkyl optionally substituted with 1 to 5 fluorine, a C 3-6 alicyclic group, a 4- to 10-membered nitrogen-containing non-aryl heterocyclic group, C 1-6 alkoxy, C 6-10 aryl (wherein the alicyclic group, the nitrogen-containing non-aryl heterocyclic group, the alkoxy, and the aryl group are each independently optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, cyano, a C 3-6 alicyclic group, C 1-6 alkyl optionally substituted with 1 to 5 fluorine, and C 1-6 alkoxy), and 5- to 10-membered heteroaryl (wherein the heteroaryl group is optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, cyano, a C 3-6 alicyclic group, C 1-6 alkyl optionally substituted with 1 to 5 fluorine, and C 1-6 alkoxy),

(3) a 4- to 10-membered non-aryl heterocyclic group optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, hydroxy, amino, dimethylamino, C 1-6 alkyl optionally substituted with 1 to 5 fluorine, a C 3-6 alicyclic group, C 1-6 alkoxy, and C 6-10 aryl (wherein the alicyclic group, the alkoxy, and the aryl group are each independently optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, cyano, a C 3-6 alicyclic group, C 1-6 alkyl optionally substituted with 1 to 5 fluorine, and C 1-6 alkoxy),

(4) C 6-10 aryl optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, cyano, dimethylamino, C 1-6 alkoxy, and C 1-6 alkyl (wherein the alkoxy and the alkyl are each independently optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, hydroxy, and C 1-6 alkoxy), or

(5) 5- to 10-membered heteroaryl optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, cyano, dimethylamino, C 1 -6 alkoxy, and C 1-6 alkyl (wherein the alkoxy and the alkyl are each independently optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, hydroxy, and C 1-6 alkoxy).

11. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein Y is

(1) C 1-3 alkyl optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of fluorine, a C 3-6 alicyclic group, a 5- or 6-membered nitrogen-containing non-aryl heterocyclic group, phenyl (wherein the alicyclic group, the nitrogen-containing non-aryl heterocycle, and the phenyl group are each independently optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of fluorine, cyano, C 1-3 alkyl optionally substituted with 1 to 3 fluorine, and methoxy), and 5- to 6-membered heteroaryl (wherein the heteroaryl group is optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of fluorine, cyano, C 1-3 alkyl optionally substituted with 1 to 3 fluorine, and methoxy),

(2) a C 3-6 alicyclic group optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of fluorine, amino, dimethylamino, C 1-3 alkyl optionally substituted with 1 to 3 fluorine, a 5- to 6-membered nitrogen-containing non-aryl heterocyclic group, phenyl (wherein the phenyl group is optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of fluorine, cyano, C 1-3 alkyl optionally substituted with 1 to 3 fluorine, and methoxy), and 5- to 6-membered heteroaryl (wherein the heteroaryl group is optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of fluorine, cyano, C 1-3 alkyl optionally substituted with 1 to 3 fluorine, and methoxy),

(3) a 5- or 6-membered nitrogen-containing non-aryl heterocyclic group optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of fluorine, amino, dimethylamino, and C 1-3 alkyl optionally substituted with 1 to 3 fluorine,

(4) phenyl optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, cyano, dimethylamino, C 1-3 alkoxy, and C 1-3 alkyl optionally substituted with 1 to 3 fluorine, or

(5) 5- or 6-membered heteroaryl optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, cyano, dimethylamino, C 1-3 alkoxy, and C 1-3 alkyl optionally substituted with 1 to 3 fluorine.

12. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein Y is

(1) C 1-3 alkyl optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of fluorine, a C 3-6 alicyclic group, a 5- or 6-membered nitrogen-containing non-aryl heterocyclic group, phenyl (wherein the alicyclic group, the nitrogen-containing non-aryl heterocycle, and the phenyl group are each independently optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of fluorine, cyano, C 1-3 alkyl optionally substituted with 1 to 3 fluorine, and methoxy), and 5-membered heteroaryl (wherein the heteroaryl group is optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of fluorine, cyano, C 1-3 alkyl optionally substituted with 1 to 3 fluorine, and methoxy),

(2) a C 5-6 alicyclic group or phenylcyclopropyl wherein the C 5-6 alicyclic group or phenylcyclopropyl is optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of fluorine, amino, dimethylamino, C 2-3 alkyl optionally substituted with 1 to 3 fluorine, a 5- to 6-membered nitrogen-containing non-aryl heterocyclic group, phenyl (wherein the phenyl group is optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of fluorine, cyano, C 1-3 alkyl optionally substituted with 1 to 3 fluorine, and methoxy), and 5- to 6-membered heteroaryl (wherein the heteroaryl group is optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of fluorine, cyano, C 1-3 alkyl optionally substituted with 1 to 3 fluorine, and methoxy),

(3) a 4- to 6-membered nitrogen-containing non-aryl heterocyclic group, phenyloxetanyl, or tetrahydropyranyl wherein the 4- to 6-membered nitrogen-containing non-aryl heterocyclic group, phenyloxetanyl, or tetrahydropyranyl is optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of fluorine, amino, dimethylamino, C 2-3 alkyl optionally substituted with 1 to 3 fluorine, and phenyl (wherein the phenyl group is optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of fluorine, cyano, C 1-3 alkyl optionally substituted with 1 to 3 fluorine, and methoxy),

(5) 6-membered heteroaryl optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, cyano, C 1-3 alkoxy, and C 1-3 alkyl optionally substituted with 1 to 3 fluorine.

13. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein Y is

(1) C 1-3 alkyl optionally substituted with 1 to 3 fluorine,

(2) a C 5-6 alicyclic group optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of fluorine, amino, dimethylamino, and C 1-3 alkyl optionally substituted with 1 to 3 fluorine,

14. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein Y is

(1) a C 5-6 alicyclic group optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of fluorine, amino, dimethylamino, and C 1-3 alkyl optionally substituted with 1 to 3 fluorine,

(2) a 5- or 6-membered nitrogen-containing non-aryl heterocyclic group optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of fluorine, amino, dimethylamino, and C 1-3 alkyl optionally substituted with 1 to 3 fluorine,

(3) phenyl optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, cyano, methoxy, and C 1-3 alkyl optionally substituted with 1 to 3 fluorine, or

(4) 5- or 6-membered heteroaryl optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, cyano, methoxy, and C 1-3 alkyl optionally substituted with 1 to 3 fluorine.

15. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein Y is

(1) phenyl optionally substituted with 1 to 2 of the same or different substituents selected from the group consisting of fluorine, cyano, methoxy, and methyl, or

(2) 5- or 6-membered heteroaryl optionally substituted with 1 to 2 of the same or different substituents selected from the group consisting of fluorine, cyano, methoxy, and methyl.

16. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein Y is

(1) phenyl optionally substituted with 1 to 2 of the same or different substituents selected from the group consisting of fluorine, cyano, methoxy, and methyl, or

(2) 6-membered heteroaryl optionally substituted with 1 to 2 of the same or different substituents selected from the group consisting of fluorine, cyano, methoxy, and methyl.

17. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein Z is 6- to 10-membered heteroaryl optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, cyano, C 2-6 alkoxy, and C 1-6 alkyl (wherein the alkoxy and the alkyl are each independently optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, hydroxy, and C 1-6 alkoxy).

18. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein Z is 6- to 10-membered heteroaryl, thienyl, pyrrolyl, thiazolyl, isothiazolyl, isoxazolyl, or thiadiazolyl wherein the 6- to 10-membered heteroaryl, thienyl, pyrrolyl, thiazolyl, isothiazolyl, isoxazolyl, or thiadiazolyl is optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of fluorine, cyano, C 2-6 alkoxy, and C 1-6 alkyl (wherein the alkoxy and the alkyl are each independently optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of halogen, hydroxy, and C 1-6 alkoxy).

19. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein Z is 6- to 10-membered heteroaryl optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of fluorine, chloro, cyano, C 1-6 alkoxy, and C 1-3 alkyl optionally substituted with 1 to 3 fluorine.

20. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein Z is pyridyl, pyrimidinyl, indazolyl, or imidazopyridyl wherein the pyridyl, pyrimidinyl, indazolyl, or imidazopyridyl is optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of fluorine, chloro, cyano, methoxy, and C 1-3 alkyl optionally substituted with 1 to 3 fluorine.

21. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein Z is pyridyl optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of fluorine, chloro, cyano, and C 1-3 alkyl optionally substituted with 1 to 3 fluorine.

22. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , selected from the following compounds:

4-oxo-3-phenyl-2-(pyridin-3-ylamino)-3,4-dihydroquinazoline-6-carbonitrile,

6-fluoro-2-((5-fluoropyridin-3-yl)amino)-3-(o-tolyl) quinazolin-4 (3H)-one,

6-chloro-2-((2-methoxypyridin-3-yl)amino)-3-phenylquinazolin-4 (3H)-one,

6-fluoro-3-phenyl-2-(pyridin-3-ylamino) quinazolin-4 (3H)-one,

3-phenyl-2-(pyridin-3-ylamino) quinazolin-4 (3H)-one,

6-chloro-3-(2-chlorophenyl)-2-(pyridin-3-ylamino) quinazolin-4 (3H)-one,

6-chloro-3-phenyl-2-(pyridin-3-ylamino) quinazolin-4 (3H)-one,

6,8-difluoro-3-phenyl-2-(pyridin-3-ylamino) quinazolin-4 (3H)-one,

6-fluoro-3-(pyridin-3-yl)-2-(pyridin-3-ylamino) quinazolin-4 (3H)-one,

6-chloro-3-phenyl-2-(pyrazin-2-ylamino) quinazolin-4 (3H)-one,

6-fluoro-3-phenyl-2-(pyrazin-2-ylamino) quinazolin-4 (3H)-one,

6-fluoro-2-((5-fluoropyridin-3-yl)amino)-3-phenylquinazolin-4 (3H)-one,

5-((6-chloro-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)amino) nicotinonitrile,

6-methyl-3-phenyl-2-(pyridin-3-ylamino) quinazolin-4 (3H)-one,

2-((5-chloropyridin-3-yl)amino)-6-fluoro-3-phenylquinazolin-4 (3H)-one,

6-chloro-3-(2-fluorophenyl)-2-(pyridin-3-ylamino) quinazolin-4 (3H)-one,

2-((1-methyl-1H-indazol-6-yl)amino)-3-phenylquinazolin-4 (3H)-one,

2-(imidazo [1,5-a]pyridin-8-ylamino)-3-phenylquinazolin-4 (3H)-one,

3-(4-methoxy-2-methylphenyl)-4-oxo-2-(pyridin-3-ylamino)-3,4-dihydroquinazoline-6-carbonitrile,

3-(5-fluoro-2-methylphenyl)-4-oxo-2-(pyridin-3-ylamino)-3,4-dihydroquinazoline-6-carbonitrile,

6-fluoro-2-(pyridin-3-ylamino)-3-(p-tolyl) quinazolin-4 (3H)-one,

6-fluoro-2-(pyridin-3-ylamino)-3-(o-tolyl) quinazolin-4 (3H)-one,

6-fluoro-3-(2-fluorophenyl)-2-(pyridin-3-ylamino) quinazolin-4 (3H)-one,

4-oxo-2-(pyridin-3-ylamino)-3-(o-tolyl)-3,4-dihydroquinazoline-6-carbonitrile,

6-fluoro-3-(2-fluorophenyl)-2-((5-fluoropyridin-3-yl)amino) quinazolin-4 (3H)-one,

2-((5-fluoropyridin-3-yl)amino)-4-oxo-3-phenyl-3,4-dihydroquinazoline-6-carbonitrile,

3-(2-fluorophenyl)-2-((5-fluoropyridin-3-yl)amino)-4-oxo-3,4-dihydroquinazoline-6-carbonitrile,

2-((5-fluoropyridin-3-yl)amino)-4-oxo-3-(o-tolyl)-3,4-dihydroquinazoline-6-carbonitrile,

6-fluoro-2-((4-fluoropyridin-2-yl)amino)-3-phenylquinazolin-4 (3H)-one,

6-fluoro-2-((5-methylpyridin-2-yl)amino)-3-phenylquinazolin-4 (3H)-one,

6-fluoro-2-((2-fluoropyridin-4-yl)amino)-3-phenylquinazolin-4 (3H)-one,

6-fluoro-3-(2-methoxyphenyl)-2-(pyridin-3-ylamino) quinazolin-4 (3H)-one, and

3-(2-chlorophenyl)-6-fluoro-2-(pyridin-3-ylamino) quinazolin-4 (3H)-one.

23. A medicament comprising the compound or the pharmaceutically acceptable salt thereof according to claim 1 as an active ingredient and at least one pharmaceutically acceptable excipient.

24. A pharmaceutical composition comprising the compound or the pharmaceutically acceptable salt thereof according to claim 1 .

25. A method for treating or preventing a disorder or disease associated with an abnormal nerve excitation, comprising administering a therapeutically or prophylactically effective amount of the compound or the pharmaceutically acceptable salt thereof according to claim 1 to a patient in need thereof.

26. A pharmaceutical composition comprised of the compound or the pharmaceutically acceptable salt thereof according to claim 1 in combination with at least one agent selected from agents classified as an antiepileptic medicament, an antidepressant, an anxiolytic, or an antipsychotic medicament.

27. A pharmaceutical kit comprising the compound or the pharmaceutically acceptable salt thereof according to claim 1 and at least one agent selected from agents classified as an antiepileptic medicament, an antidepressant, an anxiolytic, or an antipsychotic medicament.

Assignments (3)

CORRECTIVE ASSIGNMENT TO CORRECT THE THE ERRONEOUS PROPERTY NUMBER PREVIOUSLY RECORDED AT REEL: 059969 FRAME: 0017. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Oct 31, 2022

From: SUMITOMO DAINIPPON PHARMA CO., LTD.

To: SUMITOMO PHARMA CO., LTD.

Reel/Frame 062029/0341 →

CHANGE OF NAME Recorded May 12, 2022

From: SUMITOMO DAINIPPON PHARMA CO., LTD.

To: SUMITOMO PHARMA CO., LTD.

Reel/Frame 059969/0017 →

ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 23, 2021

From: MORI, KAZUTO; KITANO, HIROYUKI; FURUTA, TOMOYUKI; SEKI, HAJIME; KOBAYASHI, YOHEI

To: SUMITOMO DAINIPPON PHARMA CO., LTD.

Reel/Frame 057261/0051 →

Priority Claims (1)

JP 2020-077487 · Apr 24, 2020 · national

Continuity (1)

Related Publication 20220340553A1 · Oct 27, 2022

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Database Registry, Database accession No. 2199676-12-3: Pyrido[2,3-d]pyrimidin-4(3H)-one, 3-methyl-2-[[2-[(1-methyl-4-piperidinyl)methoxy]-3-pyridinyl]amino]-, Mar. 27, 2018, XP093151764. [cited by applicant]

D3 Database Registry, Database accession No. 2198334-25-5: Pyrido[3,4-d]pyrimidin-4(3H)-one, 3-methyl-2-[[2-[(1-methyl-4-piperidinyl)methoxy]-3-pyridinyl]amino]-, Mar. 25, 2018, XP093151767. [cited by applicant]

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