Kaken Pharmaceutical Company, Ltd.

The Green Cross Corporation

Masao Tohno

Katsuhiro Uchida

Makoto Okumura

Mitsuo Mimura

Shozo Masumoto

Kazumasa Yokoyama

Tadakazu Suyama

Yutaka Mizushima

Hiroyuki Okamoto

Kiyonoshin Ichikawa

Misako Matsumura

Yoshinobu Hashimoto

Shigetoshi Sugio

Kiichiro Nabeta

Yoshiaki Konishi

Shozoh Masumoto

Biphenylylpropionic acid derivatives of the formula: ##STR1## wherein R is an alkylcarbonyloxyalkyl group or an alkenylcarbonyloxyalkyl group having the formula: ##STR2## wherein R.sup.1 is a lower alkyl group having 1 to 5 carbon atoms and R.sup.2 is an alkyl group having 1 to 15 carbon atoms or an alkenyl group having 2 to 8 carbon atoms, or a lactone having the formula: ##STR3## wherein R.sup.3 and R.sup.4 are hydrogen atom or a lower alkyl group having 1 to 2 carbon atoms, and n is an integer of 1 or 2. The compounds have excellent anti-inflammatory, analgesic and antipyretic activities. Moreover, the compounds have no irritation, rapid and long-acting, and high safety margin.

Biphenylylpropionic acid derivative, process for preparing the same and

There is provided an ophthalmic preparation comprising a fat emulsion containing flurbiprofen or its derivative such as ester as an active ingredient.

Flurbiprofen derivative ophthalmic preparation

Biphenylylpropionic acid derivative and pharmaceutical composition

Biphenylylpropionic acid derivatives of the formula: ##STR1## wherein R is an alkylcarbonyloxyalkyl group or an alkenylcarbonyloxyalkyl group having the formula: ##STR2## wherein R.sup.1 is an alkyl group having 1 to 15 carbon atoms or an alkenyl group having 2 to 8 carbon atoms and m is 0 or an integer of 1. The compounds have excellent anti-inflammatory, analgesic and antipyretic activities. Moreover, the compounds have no irritation, rapid and long-acting, and high safety margin.

There is provided a fat emulsion of an ester of flurbiprofen having the formula ##STR1## wherein R is a group of the formula ##STR2## wherein R.sub.1 is a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group, R.sub.2 is a C.sub.1 -C.sub.15 alkyl group or a C.sub.2 -C.sub.8 alkenyl group, and m is zero or an integer of 1; or a lactone group of the formula ##STR3## wherein R.sub.3 and R.sub.4 are same as or different from each other and are a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group, and n is an integer of 1 or 2. The emulsion containing particles of a vegetable oil dissolving the ester can be orally or parenterally administered to human or animal for analgesia, antiphlogosis and antipyresis in various diseases and exhibits a high activity with small amounts in terms of flurbiprofen as compared with flurbiprofen itself.

Ester of flurbiprofen and emulsion containing the same

A novel anti-inflammatory drug, which exhibits rapidly a pharmacological activity, maintains the activity for a long time, and is free from a side effect such as a gastrointestinal disorder or a central nervous disturbance is disclosed. The drug comprises a compound of an alkylcarbonyloxyalkylester or alkenylcarbonyloxyalkylester derivative of indolylacetic acid or anilinophenylacetic acid. The compound is prepared by an esterification reaction.

Ester substituted alkyl-2-(2,6-dichloroanilino)phenyl acetates

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Otsu, Japan

Masao Tohno