Otsuka Pharmaceutical Company, Limited

Tetsuyuki Uno

Minoru Okada

Masaya Kato

Norifumi Sato

Takao Nishi

Nobuaki Ito

Yasuo Koga

Yasuhiro Takeji

Hisashi Shinohara

Hidetaka Hiyama

Junpei Haruta

Hideki Kitagaki

Masahiro Fuwa

Tomonori Shibata

Gil-Namg Chu

Kazuyuki Nakagawa

Hisashi Miyamoto

Hiroshi Ishikawa

Katsumi Tamura

Yoshio Shu

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

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

Carbostyril derivatives

Carbostyril derivatives and salts thereof represented by the general formula (1a), including some known compounds, possess activities for inhibiting adhesion of thrombocytes. ##STR1## Z, A, X, R, R.sup.1 and R.sup.2 are defined in the specification. Some carbostyril derivatives having chemical structural formulas similar to those of carbostyril derivatives and salts thereof represented by the general formula (1a) have been known in prior art references, however the above-mentioned pharmacological activities have not been known to the present date.

Carbostyril derivatives and salts thereof and pharmaceutical

A carbostyril derivative or pharmaceutically acceptable salt thereof represented by the following general formula: ##STR1## wherein Z, A, XN, R, R.sup.1, and R.sup.2 are as defined in the specification. These carbostyril derivatives are useful in pharmaceutical compositions for inhibiting adhesion of thrombocytes.

Carbostyril derivatives and salts thereof and pharmaceutical composition

Benzo-heterocyclic compounds of the formula: ##STR1## wherein R.sup.1 is a lower alkyl group; R.sup.2 is a halogen atom or a group of the formula ##STR2## (wherein R.sup.4 and R.sup.5 combine together with the nitrogen atom to which they bind to form a 5- or 6-membered saturated heterocyclic group which may optionally contain an oxygen atom or nitrogen atom within the ring as an additional hetero atom and may also optionally have a substituent selected from a lower alkyl or hydroxy group on the hetero ring); R.sup.3 is an amino or nitro group; X is a halogen atom; and n is an integer of 1 or 2, and a salt thereof, which have excellent antimicrobial activities and are useful as an antimicrobial agent, or as an intermediate for the preparation of an active compound.

Pyrrolo [3,2,1-ij]-quinoline carboxylic acid compound

Growing community of inventors

Soja, Japan

Tetsuyuki Uno