Otsuka Pharmaceutical Factory, Inc.

Yoshiaki Tsuda

Makoto Inoue

Shizuo Nakamura

Kinji Hashimoto

Masatoshi Inai

Kiyoto Goto

Yoshihiko Tsuda

Kenichi Kanai

Kazushi Nagao

Ken-ichi Kanai

This invention provides thiazole derivative of the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and A are as defined above, and salts thereof. These compounds have particularly potent angiogenesis inhibiting activity.

Thiazole derivatives

Disclosed is a proline derivative of the formula ##STR1## or a pharmaceutically acceptable salt thereof. These derivatives have useful utilities such as activity of inhibiting angiotensin converting enzyme.

Proline derivatives

Disclosed are phenol derivatives of the formula ##STR1## wherein R.sup.1 is a substituted phenyl group, R.sup.2 and R.sup.3 are C.sub.1 -C.sub.6 alkyl group and of the formula ##STR2## wherein R.sup.8, R.sup.9 and R.sup.10 are C.sub.1 -C.sub.6 alkyl and the like and A is H, C.sub.1 -C.sub.6 alkylsulfonyl and the like substituents. These compounds and some related compounds have anti-inflammatory activity and lipoxygenase inhibitory activity.

Phenol derivatives, their preparation and the use thereof

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

This invention provides a proline derivative represented by the formula ##STR1## wherein: R.sub.1 is C.sub.5 -C.sub.14 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.6 alkyl or a group ##STR2## (wherein R.sub.5 is hydrogen, C.sub.1 -C.sub.14 alkyl or phenyl and R.sub.6 is hydrogen or C.sub.1 -C.sub.6 alkyl);

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Anan, Japan

Yoshiaki Tsuda