Kaken Pharmaceutical Company, Ltd.

The Green Cross Corporation

Katsuhiro Uchida

Makoto Okumura

Masao Tohno

Mitsuo Mimura

Shozo Masumoto

Kazumasa Yokoyama

Tadakazu Suyama

Yutaka Mizushima

Hiroyuki Okamoto

Michiko Nagahara

Kiyonoshin Ichikawa

Misako Matsumura

Jun Nakano

Yoshinobu Hashimoto

Kiyoharu Ukai

Terutake Nakagawa

Kazuhiko Kimura

Kiichiro Nabeta

Shigetoshi Sugio

Michio Nakanishi

Soichiro Sato

Chikara Ieda

Shozoh Masumoto

Yoshiaki Konishi

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

A 1,4-dihydropyridine derivative having the formula (I): ##STR1## wherein X is oxygen atom or nitrogen atom; when X is oxygen atom, R.sup.1 is hydrogen atom, a lower alkyl group, a lower cycloalkyl group, a lower alkenyl group or magnesium atom, when X is nitrogen atom, X-R.sup.1 group is NH.sub.2, NHR.sup.1', NR.sup.1' R.sup.1' or ##STR2## in which R.sup.1' is a lower alkyl group or a lower alkoxyalkyl group, R.sup.1' is a lower alkyl group and n is an integer of 2 to 6; R.sup.2 is a lower alkyl group, a lower cycloalkyl group or a lower alkoxyalkyl group and R.sup.3 is a lower alkyl group, formyl group, dimethoxymethyl group, cyano group or amino group, when X is oxygen atom and R.sup.1 is hydrogen atom or magnesium atom, R.sup.3 is methyl group, when X is nitrogen atom, R.sup.3 is methyl group, or a pharmaceutically acceptable salt thereof, some processes for preparing the same and a pharmaceutical composition containing the same. According to the present invention, a superior cerebral function improver can be provided.

1-4-dihydropyridine derivative, process for preparing the same and

An azaazulene derivative having the general formula (I): ##STR1## wherein R.sup.1 is hydrogen atom or isopropyl group; the bond C N between C at the 2-position and N at the 1-position is single bond or double bond; when the bond C N is single bond, R.sup.2 is 5-tetrazolyl group, R.sup.3 is taken together with carbon atom to form carbonyl group at the 2-position, and R.sup.4 is hydrogen atom, an alkyl group having 1 to 18 carbon atoms, a lower alkenyl group, a lower alkyl group having oxygen atom or sulfur atom in carbon chain, a lower alkyl group having a halogen atom or cyano group, a lower alkyl group having heteroaromatic ring, a diphenyl lower alkyl group, or a lower alkyl group having hydrocarbon-aromatic ring with the general formula: ##STR2## in which W is single bond or carbonyl group, oxygen atom, sulfur atom or --CH.dbd.CH--, n is an integer of 1 to 6, and R.sup.1', R.sup.2' and R.sup.3' are the same or different and each is hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxyl group, trifluoromethyl group, hydroxyl group, a lower alkoxycarbonyl group, carboxyl group, acetyl group or cyano group; when the bond C N is double bond, N at the 1-position has no substituent R.sup.4, R.sup.2 is cyano group, and R.sup.3 is amino group or a salt thereof, azido group, a diphenyl lower alkyl amino group, a substituted phenyl amino group, a substituted piperazinyl group, a substituted homopiperazinyl group, an amino acid residue bonded by N terminal group in which C terminal group is carboxyl group or a lower alkyl ester thereof, or a lower alkyl amino group which may have an alkyl amino group that may be cyclic one, or a salt thereof, which is useful as an active ingredient of an antiallergic agent and an antiinflammatory agent and has also an inhibitory activity against histamine release, 5-lipoxygenase inhibiting activity, relaxing activity of smooth musculus trachealis and inhibitory activity against carrageenin edema, and further, is useful as medicine for prevention and treatment of bronchial asthma, allergic coryza, allergic conjunctivitis, urticaria, atopic dermatitis, other inflammatory diseases or the like.

Azaazulene compounds which are useful as antiallergic and

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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Kyoto, Japan

Katsuhiro Uchida