Mitsubishi Kasei Corporation

Mitsubishi Chemical Industries Limited

Kohei Umezu

Shinya Inoue

Kazuo Suzuki

Tetsuo Sekiya

Masao Taniguchi

Tadashi Shirasaka

Hiromi Okushima

Mayumi Hirata

Chiaki Hyodo

Yoshiharu Morita

Koichiro Hirayama

Masayuki Mitsuka

Tetsuro Shinpuku

Hiroshi Terayama

A novel 1-phenylalkyl-3-phenylurea derivative represented by the following formula (I): ##STR1## wherein R.sup.1 and R.sup.5 represent independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.5 alkoxyl or halo; R.sup.2 represents hydrogen or C.sub.1 -C.sub.15 alkyl; R.sup.3 represents C.sub.1 -C.sub.15 alkyl or R.sup.3 represents together with R.sup.2 C.sub.2 -C.sub.9 alkylene; R.sup.4 and R.sup.5 represent independently C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxyl or halo; X represents oxygen or sulfur; Y represents --O--(CH.sub.2).sub.l --O-- wherein l is an integer of 1 to 3 or --(CH.sub.2).sub.p -- wherein p is an integer of 3 to 5; m is 0 or an integer of 1 to 5; and n is 0 or an integer of 1 to 3, is provided. The 1-phenylalkyl-3-phenylurea derivative (I) have the action of reducing cholesterol in blood by ACAT inhibition, and therefore, useful for treating hyperlipemia and atherosclerosis.

1-phenylalkyl-3-phenylurea derivative

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

Novel 1-phenylakyl-3-phenylurea derivatives represented by the following formula (I): ##STR1## wherein R.sup.1 is an alkyl group of 1 to 8 carbon atoms, an alkoxy group of 1 to 5 carbon atoms or a halogen atom, R.sup.2 is an alkyl group of 1 to 15 carbon atoms, each of R.sup.3 and R.sup.4 is independently an alkyl group of 1 to 5 carbon atoms, m is an integer of 1 to 3, and n is 0 or 1, are provided. The compounds are potent in reducing the cholesterol level in serum, and useful for treating hyperlipemia and atherosclerosis.

1-phenylalkyl-3-phenylurea derivatives

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

The present invention provides lysosome liberation inhibitors comprising, as effective ingredients, cembrane-type diterpene compounds represented by the general formula (I) or (II): ##STR1## wherein R is a hydrogen atom or an acyl group. Also provided is histamine release inhibitors comprising the cembrane-type diterpene compounds represented by the general formula (I) or (II) above as effective ingredients.

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Yokohama, Japan

Kohei Umezu