Sankyo Company, Limited

Taisho Pharmaceutical Co., Ltd.

Kabushiki Kaisha Toshiba

Daiichi Pharmaceutical Co., Ltd.

Alps Electric Co., Ltd.

Kazuo Hasegawa

Yoshio Iizuka

Atsusuke Terada

Kazuyuki Wachi

Keiichi Tabata

Hachio Miyazawa

Takao Yoshioka

Masao Kuroda

Hiroshi Kogen

Masaaki Kurabayashi

Hideshi Kurihara

Hiroshi Kadokawa

Takashi Fujita

Toshiaki Nakajima

Kenji Tsunoda

Tohru Nagahama

Hiroshi Nakano

Yuji Ito

Akira Yoshida

Shigeo Tanaka

Yuichi Aizawa

Hiroyoshi Horikoshi

Mitsuo Yamazaki

Teiichiro Koga

Eiichi Kitazawa

Yasunori Miyahara

Takashi Kasai

Kozo Oda

Tsutomu Kanai

Tadashi Shiotani

Hideaki Kitajima

Fumio Urushizaki

Toyonori Takebayashi

Takako Fujii

Eiichi Otomo

Yoshiyuki Takasu

Jyoji Maeda

Akira Honma

Yomoyuki Kurumada

Mayumi Naito

Hachio Miyazwa

Takayuki Onodera

Takako Ishii

Akiko Yoneda

Ichiro Okudaira

Toshihiro Sudo

A microemulsion containing (A) a highly polar and fat-soluble oil drug, a highly polar oil and a lowly polar oil, (B) a polyglycerol mono-fatty acid ester and (C) a water-soluble polyhydric alcohol, wherein the amount of (B) is 0.3 to 3 parts by weight based on one part by weight of (A) and the amount of (C) is 0.1 to 3 parts by weight based on one part by weight of the total amount of (A) and (B). The present invention makes it possible to make a microemulsion containing a highly polar and fat-soluble drug which is highly stable.

Microemulsion

A suspension of a sparingly water-soluble acidic drug, especially, a nonsteroidal anti-inflammatory analgesic agent, which is stable for a prolonged period of time and is highly dissolvable, and a process for simply and easily producing the suspension. This suspension has a pH value of 2 to 5 and comprises a sparingly water-soluble acidic drug whose average particle size ranges from 1 to 15 &mgr;m, a polyglycerol fatty acid ester, a water-soluble polyhydric alcohol and water, optionally, together with an inorganic powder having an average particle size of 1 to 15 &mgr;m. This process is characterized by carrying out pulverization and dispersion of a sparingly water-soluble acid drug, a polyglycerol fatty acid ester, a water-soluble polyhydric alcohol and water by means of a pulverizer comprising a main shaft adapted to rotate in a casing and a plurality of layshafts adapted to revolve in relationship interlocked with the rotation of the main shaft, each of the layshafts being fitted with a multiplicity of annular griding media.

Suspension of sparingly water-soluble acidic drug

Remedy for dermatitis

The present invention aims at providing a drug which is highly effective in improving decline of mental functions such as disorientation, which are the major symptoms of dementia such as Alzheimer type dementia or cerebrovascular dementia, as well as general side symptoms such as decreased spontaneity, contact disturbances, motivation, emotional disturbances, abnormal behaviors and disturbances in activity of daily living. The agent for improving dementia of the present invention comprises N-(2,6-dimethylphenyl)-2-(2-oxo-1-pyrrolidinyl)acetamide or a salt thereof as an active ingredient.

Agent for improving dementia

Dermatologic composition

Described herein are of formula (I): ##STR1## and pharmaceutically acceptable salts thereof are analgesics and anti-inflammatory agents as well having anti-ulcer and 5-lipoxygenase inhibitory activities.

Use of imidazopyrazole derivatives as analgesics and anti-inflammatory

Described herein are compounds of formula (I): ##STR1## �in which: R.sup.1 and R.sup.2 are hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl, aralkyl, arylalkenyl, aryl, aromatic heterocyclic, cyano or halogen; R.sup.3 is hydrogen, optionally substituted alkyl, aralkyl or acyl; R.sup.4 and R.sup.5 are hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl, aralkyl, arylalkenyl, aryl or aromatic heterocyclic!; and pharmaceutically acceptable salts thereof are analgesics and anti-inflammatory agents as well having anti-ulcer and 5-lipoxygenase inhibitory activities.

Use of imidazopyrazole derivatives as analgesics anti-inflammatory agents

Described herein are compounds of formula (I): ##STR1## and pharmaceutically acceptable salts thereof are analgesics and anti-inflammatory agents as well having anti-ulcer and 5-lipoxygenase inhibitory activities.

Compounds of formula (I): ##STR1## in which: R represents hydrogen, methyl or hydroxy; X represents an alkyl, alkenyl, cycloalkyl, aryl, aralkyl, or heterocyclic group; A represents a single bond, or an alkylene, alkenylene, alkynylene or alkadienylene group; Y represents hydrogen, or an aryl, cycloalkyl or heterocyclic group; have valuable antihypercholesteremic activities and may be used in the treatment of disorders arising from a blood cholesterol imbalance in humans and other animals.

Octahydronaphthalene oxime compounds for cholesterol synthesis inhibition

Tricyclic heterocyclic compound

Compounds of formula (I): ##STR1## in which R is hydrogen, methyl or hydroxy; X is alkyl, alkenyl, cycloalkyl, aryl or aralkyl; A is a single bond or alkylene, alkenylene, alkynylene or alkadienylene and Y is aryl. The compounds have valuable antihypercholesteremic activities and can be used in the treatment of disorders arising from a blood cholesterol imbalance in humans and animals.

Benzylidenethiazolidine compounds of formula (I): ##STR1## [in which R.sup.1, R.sup.2 and R.sup.5 are each hydrogen or alkyl; R.sup.3 and R.sup.4 are each hydrogen, alkyl, formyl, alkylcarbonyl, arylcarbonyl, carboxy, alkoxycarbonyl, aryloxycarbonyl, hydroxy, alkylcarbonyloxy, formyloxy, arylcarbonyloxy, optionally substituted alkoxy or halogen; W is methylene, carbonyl or a group of formula &gt;C.dbd.N--OV, wherein V is hydrogen, alkylcarbonyl, arylcarbonyl or optionally substituted alkyl; and n is an integer of from 1 to 3] and salts thereof have the ability to inhibit the formation of lipid peroxide in the mammalian body, and can therefore be used for the treatment of arteriosclerosis and other diseases and disorders arising from an imbalance in the lipid peroxide level. They can also be used for the preparation of the corresponding benzylthiazolidine compounds, which have a generally greater hypoglycemic activity. Processes for the preparation of these compounds of formula (I) are also provided.

Benzylidenethiazolidine derivatives and their use for the inhibition

Compounds of formula (I): ##STR1## [in which: R.sup.1 and R.sup.2 are hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl, aralkyl, arylalkenyl, aryl, aromatic heterocyclic, cyano or halogen; R.sup.3 is hydrogen, optionally substituted alkyl, aralkyl or acyl; R.sup.4 and R.sup.5 are hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl, aralkyl, arylalkenyl, aryl or aromatic heterocyclic]; and pharmaceutically acceptable salts thereof are analgesics and anti-inflammatory agents as well having anti-ulcer and 5-lipoxygenase inhibitory activities.

Compounds of formula (I): ##STR1## and pharmaceutically acceptable salts thereof are analgesics and anti-inflammatory agents as well having anti-ulcer and 5-lipoxygenase inhibitory activities.

Growing community of inventors

Tokyo, Japan

Kazuo Hasegawa