IP Library Granted Patent US 9,453,021
Granted Patent B2
US 9,453,021 · App. 14/116,702 · Granted Sep 27, 2016

Pyrimidodiazepinone compound

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Quick Facts
Patent No.
US 9,453,021
App. No.
14/116,702
Granted
Sep 27, 2016
Kind
B2
Abstract

Provided are a compound represented by general formula (I), or the pharmaceutically acceptable salt thereof, (wherein R a represents a hydrogen atom or the like, R 1 and R 2 may be the same or different, and each represents a hydrogen atom, optionally substituted lower alkyl or cycloalkyl, or R 1 and R 2 are combined together with the adjacent nitrogen atom thereto to form nitrogen-containing heterocyclic group, and Z represents a bicyclic heterocyclic group in which optionally substituted two six-membered rings are fused to each other, or the like) and the like.

Claims (26)

1. A compound represented by formula (I), or a pharmaceutically acceptable salt thereof,

wherein R a represents a hydrogen atom, halogen, hydroxy, or lower alkoxy, R 1 and R 2 may be the same or different, and each represents a hydrogen atom, optionally substituted lower alkyl or cycloalkyl, or R 1 and R 2 are combined together with the adjacent nitrogen atom thereto to form a nitrogen-containing heterocyclic group, and Z represents a bicyclic heterocyclic group in which optionally substituted two six-membered rings are fused to each other.

2. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein R a is a hydrogen atom.

3. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein the bicyclic heterocyclic ring moiety of the bicyclic heterocyclic group in which two six-membered rings are fused to each other is a heterocyclic ring represented by any one of the following formulae (A) to (R)

4. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein the bicyclic heterocyclic ring moiety of the bicyclic heterocyclic group in which two six-membered rings are fused to each other is a heterocyclic ring represented by the following formula (A), (B), (D), (E), (J), or (L)

5. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein the bicyclic heterocyclic ring moiety of the bicyclic heterocyclic group in which two six-membered rings are fused to each other is a heterocyclic ring represented by the following formula (E), (J), or (L)

6. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein the bicyclic heterocyclic group in which two six-membered rings are fused to each other is a group represented by the following formula (A1), (A2), (B1), (B2), (D1), (D2), (E1), (E2), (J1), (J2), (L1), or (L2)

7. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein the bicyclic heterocyclic group in which optionally substituted two six-membered rings are fused to each other is a group represented by the following formula (L1a), (J1a), (J2a), or (E1a),

wherein R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , and R 11 may be the same or different, and each represents a hydrogen atom, or optionally substituted lower alkyl.

8. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein the bicyclic heterocyclic group in which optionally substituted two six-membered rings are fused to each other is a group represented by the following formula (L1a) or (J1a),

wherein R 3 , R 4 , R 5 , and R 6 may be the same or different, and each represents a hydrogen atom, or optionally substituted lower alkyl.

9. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein R 1 is lower alkyl or cycloalkyl, and R 2 is a hydrogen atom.

10. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein R 1 is lower alkyl, and R 2 is a hydrogen atom.

11. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein the compound represented by formula (I) is selected from the group consisting of:

(S)-6-(2,3-dimethyl-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl)-2-ethylamino-6,7,7a,8,9,10-hexahydro-5H-pyrimido[5,4-f]pyrrolo[1,2-a][1,4]diazepin-5-one (compound 7),

(S)-6-(2,3-dimethyl-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl)-2-methylamino-6,7,7a,8,9,10-hexahydro-5H-pyrimido[5,4-f]pyrrolo[1,2-a][1,4]diazepin-5-one (compound 8),

(S)-6-(3-methyl-4-oxo-3,4-dihydroquinazolin-8-yl)-2-methylamino-6,7,7a,8,9,10-hexahydro-5H-pyrimido[5,4-f]pyrrolo[1,2-a][1,4]diazepin-5-one (compound 10),

(S)-2-ethylamino-6-(2,3-dimethyl-4-oxo-3,4-dihydroquinazolin-8-yl)-6,7,7a,8,9,10-hexahydro-5H-pyrimido[5,4-f]pyrrolo[1,2-a][1,4]diazepin-5-one (compound 11),

(S)-6-(3-ethyl-4-oxo-3,4-dihydroquinazolin-8-yl)-2-methylamino-6,7,7a,8,9,10-hexahydro-5H-pyrimido[5,4-f]pyrrolo[1,2-a][1,4]diazepin-5-one (compound 14),

(S)-2-ethylamino-6-(3-methyl-4-oxo-3,4-dihydroquinazolin-5-yl)-6,7,7a,8,9,10-hexahydro-5H-pyrimido[5,4-f]pyrrolo[1,2-a][1,4]diazepin-5-one (compound 15),

(S)-6-(3-(3-(dimethylamino)propyl)-4-oxo-3,4-dihydroquinazolin-8-yl)-2-(methylamino)-6,7,7a,8,9,10-hexahydro-5H-pyrimido[5,4-f]pyrrolo[1,2-a][1,4]diazepin-5-one (compound 38),

(S)-6-(3-(3-(dimethylamino)propyl)-4-oxo-3,4-dihydroquinazolin-8-yl)-2-(ethylamino)-6,7,7a,8,9,10-hexahydro-5H-pyrimido[5,4-f]pyrrolo[1,2-a][1,4]diazepin-5-one (compound 39),

(S)-2-ethylamino-6-(2-(methoxymethyl)-3-methyl-4-oxo-3,4-dihydroquinazolin-8-yl)-6,7,7a,8,9,10-hexahydro-5H-pyrimido[5,4-f]pyrrolo[1,2-a][1,4]diazepin-5-one (compound 65), and

(S)-6-(3-methyl-4-oxo-3,4-dihydroquinazolin-8-yl)-2-propylamino-6,7,7a,8,9,10-hexahydro-5H-pyrimido[5,4-f]pyrrolo[1,2-a][1,4]diazepin-5-one (compound 71).

12. A method of treating diabetic pain, which comprises administering an effective amount of the compound or the pharmaceutically acceptable salt thereof according to claim 1 .

13. A method of treating pain, which comprises administering an effective amount of the compound or the pharmaceutically acceptable salt thereof according to claim 1 .

Assignments (2)
CHANGE OF NAME AND ADDRESS Recorded Oct 23, 2019
From: KYOWA HAKKO KIRIN CO., LTD.
To: KYOWA KIRIN CO., LTD.
Reel/Frame 050797/0533 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 11, 2014
From: OTSUBO, NOBUMASA; OKAZAKI, SHUKO; TSUKUMO, YUKIHITO; IIDA, KYOICHIRO; NAKOJI, MASAYOSHI
To: KYOWA HAKKO KIRIN CO., LTD.
Reel/Frame 032192/0455 →