Mitsubishi Tanabe Pharma Corporation

Mitsubishi Pharma Corporation

Fumihiko Akahoshi

Hiroshi Sakashita

Yoshiharu Hayashi

Wataru Sasaki

Hiroshi Kitajima

Tomohiro Yoshida

Hideki Ushirogochi

Ryo Sakakibara

Yuichi Onda

Naoko Ueda

Shinji Kirihara

Satoru Uemori

Reiko Tsutsumiuchi

Masahiro Takeuchi

Yuji Abe

Yoshihito Tanaka

Takuya Yoshimura

Jun Anabuki

Minami Yamaguchi

Aki Kusunoki

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.

A concomitant agent to be used simultaneously or separately, comprising a combination of (a) 3-{(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl}thiazolidine, a salt of the compound with an organic or inorganic and mono- or di-basic acid or a solvate thereof, and

Concomitant pharmaceutical agents and use thereof

The present invention provides 3-{(2S,4S)-4-[4-(3-methyl -1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2 -ylcarbonyl}thiazolidine (compound I) useful as a dipeptidyl peptidase-IV inhibitor, which has superior properties of stability and hygroscopicity, and reproducible crystal structure, and a production method thereof.

Salt of proline derivative, solvate thereof, and production method thereof

The present invention provides 3-{(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl}thiazolidine (compound I) useful as a dipeptidyl peptidase-IV inhibitor, which has superior properties of stability and hygroscopicity, and reproducible crystal structure, and a production method thereof.

A thiazolidine derivative represented by the formula (I) wherein each symbol is as defined in the specification, and a pharmaceutically acceptable salt thereof exhibit a potent DPP-IV inhibitory activity, and can be provided as an agent for the prophylaxis or treatment of diabetes, an agent for the prophylaxis or treatment of obesity and the like.

Thiazolidine derivatives and medicinal use thereof

Compounds represented by the &#x3b1;-amino acid derivative or a pharmaceutically acceptable salt thereof of the present invention have a therapeutic effect due to a DPP-IV inhibitory action and useful as pharmaceutical agents for the treatment and/or prophylaxis of diseases relating to a DPP-IV inhibitor.

&#x3b1;-amino acid derivatives and use thereof as medicines

The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the &#x3b3;-position of proline represented by the formula (I)wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.

Proline derivatives and the use thereof as drugs

The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the &#x3b3;-position of proline represented by the formula (I) wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.

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Tokyo, Japan

Fumihiko Akahoshi