Kowa Company Limited

Takeo Deushi

Toshihito Mori

Akio Iwasaki

Masami Shiratsuchi

Kazuhiro Kamiya

Masahito Nakayama

Masahiro Tamura

Yoshio Takahashi

Toshimi Mizoguchi

Toshiaki Oda

Hisakatsu Ito

Isamu Watanabe

Mitsuteru Hirata

Takeshi Ohshima

Takeshi Oda

Hiroyuki Sonoki

Takafumi Kunieda

Hisakatsu Itoh

Hiroyuki Ishiwata

Yasushi Wada

Kazuhiro Onogi

Hendrik Timmerman

Toru Kanke

Jiro Matsumoto

Tsutomu Tohma

Mingqiang Zang

Yukihiro Okuno

Tetsuya Ishikawa

Katsuhiro Yamamoto

Masahoto Nakayama

Pyrimidine derivatives

The present invention is directed to a tetrazole derivative represented by the following formula (1) or a salt thereof: ##STR1## wherein R.sup.1 and R.sup.2 independently represent a hydrogen atom, a hydroxyl group, a lower alkyl group, a substituted or unsubstituted alkoxy group, or a substituted or unsubstituted alkanoyloxy group; R.sup.3 represents a hydrogen atom or a substituted or unsubstituted lower alkyl group; A represents a methyleneoxy group or a vinylene group; B represents a substituted or unsubstituted quinolyl group, a substituted or unsubstituted quinazolyl group, or a substituted or unsubstituted benzimidazolyl group; and a broken line indicates that there may be a double bond; and to a medicine containing the compound as an active ingredient. The medicine according to the present invention is endowed with excellent antileukotriene activity and antihistaminic activity, and is useful for the prevention and treatment of, for example, asthma.

Tetrazole derivatives

The present invention is directed to a tetrazole derivative represented by the following formula (1) or a salt thereof: ##STR1## wherein R.sup.1 and R.sup.2 independently represent a hydrogen atom, a hydroxyl group, a lower alkyl group, a substituted or unsubstituted alkoxy group, or a substituted or unsubstituted alkanoyloxy group; R.sup.3 represents a hydrogen atom or a substituted or unsubstituted lower alkyl group; A represents a methyleneoxy group or a vinylene group; Z represents a substituted or unsubstituted benzimidazolyl group; and a broken line indicates that there may be a double bond; and to a medicine containing the compound as an active ingredient. The medicine according to the present invention is endowed with excellent antileukotriene activity and antihistaminic activity, and is useful for the prevention and treatment of, for example, asthma.

Pyrimidine derivatives as endothelin antagonists

Azoxy compound

A compound expressed by the formula: ##STR1## in which R.sub.11, R.sub.21 and R.sub.31 are identical with or different from each other and each denotes a hydrogen atom, a halogen atom, an alkyl group, an alkenyl group, a haloalkyl group, an alkoxy group, an alkylthio group, an aryl or an aralkyl group which aromatic ring is optionally substituted appropriately by one to three substituents or a heterocyclic group optionally substituted appropriately by one to three substituents, or R.sub.11 and R.sub.21 may together form an alkylene group, Y denotes O or NOH, with a proviso that where R.sub.21 (or R.sub.11) and R.sub.31 denote a hydrogen atom at the same time, R.sub.11 (or R.sub.21) cannot represent an n-butyl group. This compound is useful as an antifungal agent.

Azoxy compounds

A process for producing an antibiotic, which comprises cultivating an antibiotic KA-6606-producing strain of the genus Saccharopolyspora in a nutrient culture medium, isolating an antibiotic KA-6606-containing substance from the culture broth, and separating from the resulting antibiotic KA-6606-containing substance at least one antibiotic selected from the group consisting of antibiotic KA-6606 VII, KA-6606 VIII, KA-6606 IX, KA-6606 X, KA-6606 XI, KA-6606 XII, KA-6606 XIII, KA-6606 XIV, KA-6606 XV, KA-6606 XVI and KA-6606 XVII; and novel antibiotics KA-6606 XII, XIII and XV to XVII.

Antibiotics KA-6606 XII, XIII, XV, XVI and XVII

A process for producing an antibiotic, which comprises cultivating an antibiotic KA-6606-producing strain of an genus Saccharopolyspora in a nutrient culture medium, isolating the antibiotic KA-6606-containing substance from the culture broth, and separating from the resulting antibiotic KA-6606-containing substance at least one antibiotic selected from the group consisting of antibiotic KA-6606 VII, KA-6606 VIII, KA-6606 IX, KIA-6606 X, KA-6606 XI, KA-6606 XII, KA-6606 XIII, KA-6606 XIV, KA-6606 XV, KIA-6606 XVI and KA-6606 XVII; and novel antibiotics KA-6606 XII, XIII and XV to XVII.

Process for production of antibiotics and novel antibiotics produced

Novel antibiotics of the following structure ##STR1## wherein R represents a moiety selected from the group consisting of hydrogen, --COCH.sub.2 NH.sub.2, --COCH.sub.2 NHCONH.sub.2 and --COCH.sub.2 NHCHO; process for preparation thereof; and biologically pure culture for use therein.

Biologically pure culture

An antibiotic substance KA-7038 selected from the group consisting of the compounds having formulae I to VII described in claim 1, mixtures thereof and acid addition salts thereof; an antibiotic composition composed of (i) antibiotically effective amount of aforesaid antibiotic substance KA-7038, and (ii) a pharmaceutically acceptable diluent or carrier. The antibiotic substance KA-7038 can be produced by cultivating an antibiotic substance KA-7038-producing strain belonging to genus Streptomyces, for example Streptomyces sp. KC-7038, and isolating the antibiotic substance KA-7038 from the culture broth.

Process for preparation of antibiotics and biologically pure culture for

Novel antibiotics, process for preparation thereof and biologically pure

Antibiotic KA-7038 and compositions containing same

Antibiotics of the KA-6606 series and pharmaceutical compositions thereof

Growing community of inventors

Sayama, Japan

Takeo Deushi