Otsuka Pharmaceutical Factory, Inc.

Yoshihiko Tsuda

Yasuhide Inoue

Kazuyoshi Miyata

Kazuhiko Tsutsumi

Yasuo Shoji

Yasuhisa Kurogi

Yasuhiro Sakai

Chieko Naba

Keigo Sato

Takeshi Iwamoto

Jun Kanaya

Eiji Uesaka

Shinya Miki

Kayoko Shinomiya

Atsushi Shima

Norihiro Yoshinaga

Masako Doi

Akifumi Hagi

Yoshiaki Tsuda

Shizuo Nakamura

Chieko Yoshida

Seiichirou Kanou

Yauso Shoji

Tagui Sugimoto

Kenichi Kawamura

Takahiro Tomoyasu

Mitsuyoshi Kondo

Akiyoshi Kuroda

Yasuhisa Kuroki

The present invention provides a phosphonic acid diester compound represented by General Formula wherein R, R, Rand Rare the same or different, and represent hydrogen, halogen, lower alkyl or lower alkoxy; Ris phenyl having on the phenyl ring 1&#x2013;3 substituents selected from the group consisting of lower alkyl, halogen-substituted lower alkyl, lower alkoxy, halogen-substituted lower alkoxy, phenoxy, benzyloxy, hydroxyl, halogen, nitro, lower alkylthio, di(lower alkyl)amino, lower alkanolyamino, pyrrolidinyl and phenyl, or the like, provided that Ris not mono(lower alkoxy)pheny; and Ris lower alkyl;and an ACAT-1 inhibitor containing the compound as an active ingredient.

Phosphonic diester derivatives

Phosphonic acid diester derivatives

Process for preparing quinazolin-4-one derivatives

Phosphonic ester derivatives of quinazolinones

The present invention provides an agent for preventing and treating cataract comprising, as an active ingredient, a carboxylic acid amide derivative represented by the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X are as defined above. The present invention has a marked preventive and therapeutic effect on the cataract belonging to various classifications and particularly on the diabetic cataract.

Composition for preventing and treating cataract

The invention provides a phosphonic diester derivative of the formula: ##STR1## wherein the variables are as defined in the specification. The derivative of the invention has excellent hypolipidemic and hypoglycemic activities and little side effects and hence is useful as therapeutic and prophylactic agents for hyperlipidemic diseases and diabetes and as a therapeutic agent for cataract.

A pharmaceutical composition for treating hyperlipidemia containing, as the active ingredient, at least one carboxamide compounds represented by the formula (1) which possess excellent activities in lowering serum lipid, as well as having low toxicity with high safety. Said carboxamide compounds represented by the formula (1) are known compounds developed by the present inventors, but the pharmacological activities for treating hyperlipidemia have not been found yet.

Method for treating hyperlipidemia

Novel carboxamide compounds represented by the general formula (I) possess excellent activities for lowering lipids and thus they are useful as agents for treating and preventing various diseases (hyperlipidemia) such as hypercholesterolemia, hypertriglyceridemia, hyperphospholipidemia, hyperlipacidemia, and the like.

Carboxamide compounds, processes for preparing the same and a

A carboxamide compound of the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X are as defined and pharmaceutically acceptable salts thereof, and composition containing the compound are disclosed. The compound is useful as a calcium antagonistic agent and an antiinflammatory agent.

Carboxamide compounds

Growing community of inventors

Naruto, Japan

Yoshihiko Tsuda