IP Library Granted Patent US 12,679,813
Granted Patent B2
US 12,679,813 · App. 18/025,932 · Granted Jul 14, 2026

Triazine compound salt, crystal form thereof, and production method therefor

Inventors: Takafumi Yamagami (Osaka, JP); Tomofumi Setsuta (Osaka, JP); Yoshihiro Sugiura (Osaka, JP); Naoko Ueda (Osaka, JP)
Assignee: TANABE PHARMA CORPORATION
C07D253/07C07B2200/13
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Quick Facts
Patent No.
US 12,679,813
App. No.
18/025,932
Filed
Mar 13, 2023
Granted
Jul 14, 2026
Kind
B2
Art Unit
1621
USPC
514/242
Abstract

The present invention provides a salt of a triazine compound which has an inhibitory action against aldosterone synthase and is useful as a drug, and especially as a drug for preventing or treating primary aldosteronism and the like, a crystal thereof, and a method for producing the same. Specifically, the present invention provides a pharmaceutically acceptable salt of 3-[4-[[trans-4-(acetamino)cyclohexyl]carbamoylmethyl]piperazin-1-yl]-5-(p-tolyl)-1,2,4-triazine, wherein the salt is hydrobromide, sulfate, succinate, or tosylate, and the like.

Claims (15)

1 . A crystal of pharmaceutically acceptable salt of 3-[4-[[trans-4-(acetamino)cyclohexyl]carbamoylmethyl]piperazin-1-yl]-5-(p-tolyl)-1,2,4-triazine, wherein the salt is hydrobromide, sulfate, succinate, or tosylate.

2 . The crystal according to claim 1 , wherein the salt is hydrobromide.

3 . The crystal according to claim 2 , having peaks at 8.8° 0.2°, 18.1°±0.2°, 20.9°±0.2°, and 25.6°±0.2° as diffraction angles expressed in 2θ in a powder X-ray diffraction spectrum.

4 . The crystal according to claim 2 , having an endothermic peak at 265 to 275° C. in a differential scanning calorimetry analysis.

5 . An aldosterone synthase inhibitor comprising the crystal according to claim 1 as an active ingredient.

6 . A pharmaceutical composition comprising the crystal according to claim 1 and a pharmaceutically acceptable additive.

7 . An aldosterone synthase inhibitor comprising the crystal according to claim 2 as an active ingredient.

8 . A pharmaceutical composition comprising the crystal according to claim 2 and a pharmaceutically acceptable additive.

9 . An aldosterone synthase inhibitor comprising the crystal according to claim 3 as an active ingredient.

10 . A pharmaceutical composition comprising the crystal according to claim 3 and a pharmaceutically acceptable additive.

11 . An aldosterone synthase inhibitor comprising the crystal according to claim 4 as an active ingredient.

12 . A pharmaceutical composition comprising the crystal according to claim 4 and a pharmaceutically acceptable additive.

13 . The crystal according to claim 3 further having peaks at 15.1°±0.2°, 17.5°±0.2°, 21.5°±0.2°, and 25.0°±0.2° as diffraction angles expressed in 2θ in a powder X-ray diffraction spectrum.

14 . An aldosterone synthase inhibitor comprising the crystal according to claim 13 as an active ingredient.

15 . A pharmaceutical composition comprising the crystal according to claim 14 and a pharmaceutically acceptable additive.

Assignments (2)
CHANGE OF NAME Recorded Mar 5, 2026
From: MITSUBISHI TANABE PHARMA CORPORATION
To: TANABE PHARMA CORPORATION
Reel/Frame 073977/0840 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 13, 2023
From: YAMAGAMI, TAKAFUMI; SETSUTA, TOMOFUMI; SUGIURA, YOSHIHIRO; UEDA, NAOKO
To: MITSUBISHI TANABE PHARMA CORPORATION
Reel/Frame 062960/0609 →
Priority Claims (1)
JP 2020-154875 · Sep 15, 2020 · national
Continuity (1)
Related Publication 20230365513A1 · Nov 16, 2023
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