Otsuka Pharmaceutical Company, Limited

Ss Pharmaceutical Co., Ltd.

Ssp Co. Ltd

Sumitomo Metal Industries, Inc.

Boehringer Ingelheim International Gmbh

Sankin Industry Company, Limited

D. Western Therapeutics Institute, Inc.

Ludwig Institute for Cancer Research Limited

Astellas Pharma Gmbh

Hisamitsu Pharmaceutical Company, Inc.

Imperial Cancer Research Technology, Ltd.

Minoru Okada

Akira Iwasa

Shuichi Kasai

Tetsuyuki Uno

Kenji Ono

Katsumi Imamori

Masaya Kato

Norifumi Sato

Syuichi Kasai

Makoto Suzuki

Yoshiaki Shida

Kenji Ishigaki

Nobuaki Ito

Takao Nishi

Mitsuaki Ohta

Wataru Takahashi

Hiroyuki Kaizawa

Koyo Matsuda

Mayumi Yamano

Tomonobu Koizumi

Ken-Ichi Kawaguchi

Hirohisa Okuyama

Mutsuo Nakanishi

Yasuhiro Takeji

Hisashi Shinohara

Hidetaka Hiyama

Junpei Haruta

Hideki Kitagaki

Yoshihito Sugimoto

Toshiaki Horie

Tomonori Shibata

Masahiro Fuwa

Masahiko Hayakawa

Hiroyuki Moritomo

Noriyuki Koyama

Yoshihiro Murakami

Hiroyoshi Hidaka

Hitoshi Matsushita

Yasuo Ikeda

Yasuo Koga

Noriko Ishikawa

Katsumi Tamura

Yoshihiro Inoue

Toshiaki Kurazumi

Naohiko Kanai

Norio Fukuda

Yoshio Shu

Yohei Yuki

Yoshito Kihara

Yukio Kimura

Shigeo Fujieda

Tomio Nishikawa

Kazuyuki Nakano

Isamu Kato

Ryozo Isomura

Kazuki Matsumoto

Tetsuo Hayashi

Koichi Takahashi

Kenji Masuda

Nao Koseki

Takashi Kabuki

Kengo Matsumoto

Katsuhiro Omichi

An ointment is provided. The ointment stably comprises an oxazole compound that has specific inhibitory activity against PDE4 and that is represented by the following formula (11). The ointment can be efficiently absorbed into the skin. 

Ointment containing an oxazole compound

The present invention provides a oxazole compound represented by Formula (1), or a salt thereof: wherein Ris an aryl group which may have one or more substituents; Ris an aryl group or a nitrogen atom-containing heterocyclic group each of which may have one or more substituents; and W is a divalent group represented by &#x2014;Y-A- or or &#x2014;Y&#x2014;C(&#x2550;O)&#x2014; wherein Yis a group such as &#x2014;C(&#x2550;O)&#x2014;, Ais a group such as a lower alkylene group, and Yis a group such as a piperazinediyl group. The oxazole compound has a specific inhibitory action against phosphodiesterase 4.

Oxazole compound and pharmaceutical composition

An object of the present invention is to provide a novel method for producing an oxazole compound. The invention relates to a method for producing a compound represented by formula (1): wherein Ris lower alkyl group or halogen substituted lower alkyl group, Ris lower alkyl group, Ris lower alkyl group, Ris lower alkyl group, halogen substituted lower alkyl group or a group represented by formula: &#x2014;CYCOOR, wherein Y is a halogen atom, Ris an alkali metal atom or lower alkyl group, Aris phenyl group substituted with lower alkyl group, etc., or pyridyl group substituted with lower alkyl group, etc., X, Xand Xare the same or different and are halogen atoms, Xis a leaving group, and M is an alkali metal atom. 

Method for producing oxazole compound

The present invention provides a oxazole compound represented by Formula (1), or a salt thereof: wherein Ris an aryl group which may have one or more substituents; Ris an aryl group or a nitrogen atom-containing heterocyclic group each of which may have one or more substituents; and W is a divalent group represented by &#x2014;Y-A- or &#x2014;Y&#x2014;C(&#x2550;O)&#x2014; wherein Yis a group such as &#x2014;C(&#x2550;O)&#x2014;, Ais a group such as a lower alkylene group, and Yis a group such as a piperazinediyl group. The oxazole compound has a specific inhibitory action against phosphodiesterase 4.

The present invention provides 4-amino-5-cyanopyrimidine derivatives of the formula: wherein R, Rand Rare defined herein, or pharmaceutically acceptable salts thereof, having a safe and potent adenosine A2a receptor agonistic activity; and also provides an adenosine A2a receptor agonist, an intraocular pressure reducing agent, or a medicine for treating glaucoma, etc., which comprises the compound as an active ingredient. 

4-amino 5-cyanopyrimidine derivatives

4-amino-5-cyanopyrimidine derivatives

This invention relates to a new composition containing the effective concentration of an aqueous extract of red vine leaves (1) and an anti-inflammatory agent (2) for preventing or alleviating the discomfort associated with mild-to-moderate chronic venous insufficiency of the legs. The compositions according to this invention may also contain pharmaceutically or cosmically acceptable additives.

External composition comprising an aqueous extract of red vine leaves and an anti-inflammatory agent

An orally administrable uncompressed rapidly dissolving molded dosage form comprises a drug and either one or more saccharides or one saccharide and polyvinylpyrrolidone. Saccarides are chosen and used in proportion based on their solubilities. Methods for producing uncompressed rapidly dissolving solid preparations comprise mixing a drug and carriers according to the present invention and charging the mixture in a mold. Rapidly dissolving oral dosage forms facilitate administration of drugs to patients having a difficulty in swallowing such as children and the elderly.

Quickly soluble solid preparations

This invention relates to an intra-articular preparation for the treatment of arthropathy, which comprises microcapsules of (a) a high-molecular substance, which has biodegradability and biocompatibility, and (b) a drug. When applied directly to a joint area, this preparation can achieve a high drug concentration at the target area, can inhibit occurrence of general side effect, and can maintain drug efficacy over a long term. The preparation can therefore alleviate the burden on the patient.

Intra-articular preparation for the treatment of arthropathy

Drug composition with controlled drug release rate

Carbostyril derivatives

A controlled release-initiation and controlled release-rate pharmaceutical composition in which a drug-containing composition is coated with a membrane layer comprising a water insoluble high polymer and silicone. The starting time for the release of drugs from the controlled release-initiation and controlled release-rate pharmaceutical composition of this invention and the drug-releasing rate thereafter can be controlled at will.

Controlled release-initiation and controlled release-rate pharmaceutical

Compressed molded preparations are disclosed. In the preparation coated granules of a pharmaceutical composition are compressed and molded together with non-coated component(s) containing 10% or more by weight of non-swelling polymers. According to the preparation there is little breakdown of the coating of coated granules at the time of compressing and molding, and the rate of disintegration, and in turn, the release rate of the pharmaceutical component, can be freely controlled or modulated.

Compressed-molded preparations

Growing community of inventors

Inzai, Japan

Minoru Okada