Merck + Co., Inc.

Mitsubishi Kasei Corporation

Mitsubishi Chemical Industries Limited

Masao Taniguchi

Arthur A Patchett

William H Parsons

William R Schoen

Shinya Inoue

Tadashi Shirasaka

Kohei Umezu

Yoshiharu Morita

Kazuo Suzuki

Mayumi Hirata

Tetsuo Sekiya

Tetsuo Jikihara

Shuzo Hayakawa

Yasuo Hoshide

Osamu Kawashima

Ryoichi Ando

Hiroko Suzuki

Masayuki Mitsuka

Tetsuro Shinpuku

Carboxamide derivatives of the following general formula (I): ##STR1## (wherein R.sup.1 and R.sup.2 are C.sub.1 -C.sub.3 alkyl group or both taken together C.sub.1 -C.sub.3 alkylene group,

Carboxamide derivatives

A novel pyrrolealdehyde derivative represented by the following formula (I): ##STR1## wherein R represents C.sub.10 -C.sub.16 alkyl unsubstituted or substituted by at least one substituent selected from the group consisting of halo, hydroxy, amino, carbamoyl, C.sub.1 -C.sub.5 alkylamino, C.sub.2 -C.sub.6 dialkylamino, C.sub.2 -C.sub.6 acylamino, C.sub.1 -C.sub.5 alkylthio, mercapto, C.sub.2 -C.sub.6 acyloxy, carbamoyloxy, C.sub.6 -C.sub.12 aryl and C.sub.3 -C.sub.7 cycloalkyl; or C.sub.10 -C.sub.16 alkenyl having at least one vinyl, and a pharmaceutically acceptable salt thereof are provided. The compounds are highly effective in reducing the level of triglyceride and cholesterol in serum, and useful as an active ingredient of a pharmaceutical composition for treating hyperlipemia and arteriosclerosis.

Pyrrolealdehyde derivative

New 3-(1-aminoalkylphosphinyl)-(2-substituted)propionic acids are described which display antibacterial activity and potentiate carbapenem antibiotics.

Antibacterial agents and potentiators of carbapenem antibiotics

Certain phosphinic acid derivatives having antibacterial activity

Novel pyrrolecarboxylic acid derivatives represented by the following formula: ##STR1## where R.sup.1 is a hydrogen atom, an alkyl group of 5 to 25 carbon atoms or an alkenyl group of 5 to 25 carbon atoms, R.sup.2 is a hydrogen atom, a phenyl group or an optionally substituted alkyl group of 1 to 10 carbon atoms, and R.sup.3 is a hydrogen atom, an alkyl group of 5 to 25 carbon atoms or an alkenyl group of 5 to 25 carbon atoms, or pharmaceutically acceptable salts thereof are provided. The compounds are highly effective in reducing the level of triglyceride or cholesterol in serum, and useful as an active ingredient of a pharmaceutical composition for treating hyperlipemia and arteriosclerosis.

Pyrrolecarboxylic acid derivatives

Novel diphenylurea derivatives represented by the following formula (I): ##STR1## wherein R.sub.1 is an alkyl group of 5 to 18 carbon atoms, each of R.sub.2 and R.sub.3 is independently an alkyl group of 1 to 5 carbon atoms, an alkoxy group of 1 to 5 carbon atoms or a halogen atom, R.sub.4 is hydrogen atom, an alkyl group of 1 to 5 carbon atoms, an alkoxy group of 1 to 5 carbon atoms or a halogen atom, and X is oxygen atom or sulfur atom, are provided. The compounds are potent in reducing the cholesterol level in serum, and useful for treating hyperlipemia and atherosclerosis.

Diphenylurea derivatives

Disclosed are some new aminoethylphosphinic acid derivatives useful as antibacterial agents.

Aminoethylphosphinic acid derivatives

Novel antibacterial agents and potentiators of carbapenem antibiotics

Disclosed herein is a process for preparing phthalide derivatives represented by the general formula (IV): ##STR1## wherein R.sup.1 to R.sup.7 are herein defined, comprising (i) reacting a nitrophthalide of the general formula (I) defined herein with an isoquinoline of the general formula (II) defined herein, and (ii) reducing the resultant phthalideisoquinoline of the general formula (III) defined herein. The process is characterized in (A) that the reaction defined in (i) is carried out in methanol, and/or (B) that the nitrophthalide of the general formula (I) is a nitrophthalide obtained by a reaction of a phthalide of the general formula (V) defined herein with copper nitrate or zinc nitrate.

Process for preparation of phthalide derivatives

Growing community of inventors

Machida, Japan

Masao Taniguchi