Dainippon Pharmaceutical Company, Limited

Kunihiko Takeyama

Kanoo Hosoki

Tadahiro Sawayama

Masanao Shimizu

Haruki Nishimura

Yoshinobu Masuda

Kazuya Nishimura

Naonobu Hatano

Takashi Sasagawa

Masahisa Hashimoto

Hiroaki Kinugasa

Kiyoshi Nakamura

Akihisa Ikeno

Kouji Hayashi

Hisao Minato

Masatoshi Tsukamoto

Ameliorant for blood lipid metabolism

There are provided tripeptide compounds represented by the following formula ##STR1## wherein R.sub.1 represents a C.sub.1-10 alkyl group, a C.sub.4-7 cycloalkyl or C.sub.5-7 cycloalkyl-lower alkyl group, a phenyl or phenyl-lower alkyl group in which the benzene ring may optionally be substituted by a substituent selected from halogen, lower alkyl, lower alkoxy, phenyl, methylenedioxy, ethylenedioxy, amino, di(lower alkyl)amino and hydroxy, a naphthyl or naphthyl-lower alkyl group in which the naphthalene ring may optionally be substituted by a substituent selected from halogen, lower alkyl, lower alkoxy and hydroxy, a heterocyclic or heterocyclic-lower alkyl group in which the heterocycle is a saturated or unsaturated 5- or 6-membered ring containing a nitrogen, oxygen or sulfur atom as the hetero atom, and may optionally be substituted by a substituent selected from halogen, lower alkyl, lower alkoxy, amino, di(lower alkyl)amino, hydroxy, oxo and saturated 5- or 6-membered nitrogen-containing heterocyclic group, and further may optionally be fused to a benzene ring, or an imidazolylvinyl group; R.sub.2 represents a hydrogen atom, a C.sub.1-10 alkyl group or a benzyl group; R.sub.3 represents a group of the formula ##STR2## represents a benzene, cyclopentane or cyclohexane ring, R.sub.4 represents a hydrogen atom, a C.sub.1-10 alkyl group or a benzyl group, p is 0 or 1, q is 1, 2, or 3, and X represents a phenyl group which may optionally be substituted by a substituent selected from halogen, lower alkoxy and hydroxy, a C.sub.4-8 cycloalkyl group, or a C.sub.5-7 cycloalkyl group which is fused to a benzene, and Y represents a hydrogen atom or a lower alkyl group, or X and Y, together with the nitrogen and carbon atoms to which they are bonded, forms a 5- or 6-membered heterocycle which may contain a nitrogen, oxygen or sulfur atom, W represents a single bond, --O-- or --NH--, T represents a single bond, ##STR3## and m is 2 or 3, or salts thereof and processes for production thereof. The compounds are useful as antihypertensive agents.

Tripeptide derivatives

1-(3-Mercapto-2-methylpropanoyl)prolyl amino acid derivatives of the formula ##STR1## wherein R represents a hydrogen atom, a lower alkyl group, a phenyl-lower alkyl group or a substituted phenyl-lower alkyl group, R.sub.1 represents a hydrogen atom, R.sub.4 CO--, R.sub.5 S--, or ##STR2## R.sub.2 represents a hydrogen atom or a lower alkyl group, R.sub.3 represents a hydrogen atom, a phenyl group, a lower alkyl group, or a substituted lower alkyl group, or R.sub.2 and R.sub.3 form a heterocyclic ring together with the nitrogen and carbon atoms to which they are respectively bonded; salts of these compounds; compositions comprising these compounds or salts; and processes for preparing these compounds or salts. These compounds and salts have excellent antihypertensive activity.

1-(3-Mercapto-2-methylpropanoyl)prolyl amino acid derivatives and salts

New .omega.-(N-acylamino)alkylphosphoryl ethanolamines and their pharmaceutically acceptable acid addition salts have superior renin-inhibitory activities, antihypertensive activities and cholesterol-lowering activities. The .omega.-(N-acylamino)alkylphosphoryl ethanolamines are prepared by (1) reacting an .omega.-(N-acylamino) alkanol with a 2-(N-substituted amino)ethyl phosphate or its derivative, hydrolyzing the resulting product or splitting off the phosphoric acid-protective group of the resulting product thereby to form an .omega.-(N-acylamino) alkyl 2-(N-substituted amino) ethyl phosphate, and splitting off the amino-protective groups of the resulting phosphate, or (2) reacting an .omega.-(N-acylamino) alkanol with a phosphorus oxyhalide, reacting the resulting .omega.-(N-acylamino)alkyl dichlorophosphate with a 2-(N-substituted amino) ethanol, hydrolyzing the reaction product to form an .omega.-(N-acylamino) alkyl 2-(N-substituted)ethyl phosphate, and splitting off the amino-protective groups of said phosphate.

.omega.-(N-acylamino)alkylphosphoryl ethanolamines, pharmaceutical

Growing community of inventors

Ikoma, Japan

Kunihiko Takeyama