Mitsubishi Tanabe Pharma Corporation

Ryo Sakakibara

Wataru Sasaki

Fumihiko Akahoshi

Hideki Ushirogochi

Yuichi Onda

Takafumi Yamagami

Tomofumi Setsuta

Yosuke Matsumura

Souta Yamasaki

Minami Yamaguchi

The present invention provides an industrially advantageous method for producing a 3,5-disubstituted triazine compound that is useful as an active pharmaceutical ingredient. More specifically, the present invention provides a production method, whereby it becomes possible to efficiently produce a 3-oxo-5-substituted triazine in water without the need to isolate an intermediate that may have mutagenicity, and it also becomes possible to perform the production without the need to isolate a product in each of multiple steps. Namely, the present invention provides a method for producing a compound represented by formula I or a salt thereof, the method including a step of reacting a compound represented by the following formula IV or a salt thereof with a base in water, and optionally including a step of forming a salt thereof. Specifically, the present invention provides a method for producing a compound represented by formula I or a salt thereof, the method including a step of derivatizing a compound represented by formula II or a salt thereof into a corresponding compound represented by formula III, a salt thereof, or a derivative thereof, then a step of reacting the resulting compound, a salt thereof, or a derivative thereof with aminourea or a salt thereof in water to produce a compound represented by formula IV or a salt thereof, and then a step of reacting the resulting compound or a salt thereof in the presence of a base. (wherein ring A represents an optionally substituted aryl group or an optionally substituted heteroaryl group)

Method for producing triazine compound

A compound represented by general formula [I] wherein X represents N or the like, Y represents CH or the like; Rrepresents a cycloalkyl group which may be substituted or the like, Rrepresents an alkyl group or the like, Rrepresents an alkyl group which may be substituted or the like, Rrepresents a hydrogen atom or an alkyl group, or a pharmaceutically acceptable salt thereof has an inhibitory activity on aldosterone synthetase, and is useful as a prophylactic and/or therapeutic agent for various diseases or symptoms associated with aldosterone.

Nitrogen-containing aromatic heterocyclic compound

This invention provides a novel disubstituted 1,2,4-triazine compound or a pharmaceutically acceptable salt thereof, which has an aldosterone synthetase inhibitory activity and is useful for preventing and/or treating various diseases or conditions associated with aldosterone; a method for preparing it; use of it; as well as a pharmaceutical composition comprising it as an active ingredient. A compound of the general formula [I]: wherein Ris, for example, a group of the following formula (A-1): wherein ring Ais, for example, a cycloalkyl group which may be substituted,and Ris, for example, a monocyclic cycloalkyl group,or a pharmaceutically acceptable salt thereof.

Disubstituted 1, 2, 4-triazine compound

This invention provides a novel disubstituted 1,2,4-triazine compound or a pharmaceutically acceptable salt thereof, which has an aldosterone synthetase inhibitory activity and is useful for preventing and/or treating various diseases or conditions associated with aldosterone; a method for preparing it; use of it; as well as a pharmaceutical composition comprising it as an active ingredient. A compound of the general formula [I]: wherein Ris, for example, a group of the following formula (A-1): wherein ring Ais, for example, a cycloalkyl group which may be substituted, and Ris, for example, a monocyclic cycloalkyl group,or a pharmaceutically acceptable salt thereof.

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Osaka, Japan

Ryo Sakakibara