Asahi Kasei Pharma Corporation

Asahi Kasei Kogyo Kabushiki Kaisha

Takehiko Sasahara

Mitsunobu Mohri

Yukio Suzuki

Daisuke Mochizuki

Tetsu Saito

Takeo Higashino

Ken-Ichi Kasahara

A pharmaceutical useful as a therapeutic agent and a preventive agent for hyperlipemia, and a pharmaceutical useful as a therapeutic agent and a preventive agent for hepatic disorders associated with cholestasis, particularly, primary biliary cirrhosis and primary sclerosing cholangitis, and a pharmaceutical useful as a therapeutic agent and a preventive agent for obesity, fatty liver and steatohepatitis are provided. A benzothiazepine or benzothiepine compound represented by the following formula (1A) having a thioamide bond and a quaternary ammonium substitutent: 

Benzothiazepine and benzothiepine compounds

A method for inhibiting ileal bile acid transporter activity in a subject, comprising administering to said subject an effective amount of a compound represented by formula (1): 

Quaternary ammonium compounds

Drugs useful for the treatment and prevention of hyperlipidemia, moreover drugs useful for the treatment and prevention of cholestasis-caused hepatopathy, particularly primary biliary cirrhosis and primary sclerosing cholangitis, and drugs for the treatment and prevention of obesity, fatty liver and steatohepatitis, containing as active ingredients benzothiazepine compounds having a thioamide bond and a quaternary ammonium substituent, represented by formula (1) below are provided. Also, drugs containing ileal bile acid transporter inhibiting compounds as active ingredients for the treatment and prevention of cholestasis-caused hepatopathy are provided.

Described herein are pyrazolo[1,5-a]pyridine-3-carboxylic acid derivatives represented by the following formula (I): ##STR1## wherein R.sub.1 and R.sub.2 individually mean a hydrogen atom or a lower alkyl group, R.sub.3 denotes an azabicyclo group containing a tertiary nitrogen atom, and Y stands for --O-- or --NH--, or salts thereof. Their preparation process and serotonin receptor antagonists containing them as active ingredients are also described.

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Numazu, Japan

Takehiko Sasahara