Kaneka Corporation

Kanegafuchi Kagaku Kogyo Kabushiki Kaisha

Kanegafuchi Chemical Industry Co., Ltd.

Activbiotics Pharma, LLC

Katsuji Yamashita

Kazunori Hosoe

Kiyoshi Watanabe

Takehiko Yamane

Takayoshi Hidaka

Kenji Fujii

Hideo Kondo

Takuji Hashizume

Ikuo Katsumi

Yutaka Ariki

Toshiaki Yamashita

Fumiyuki Kuze

Yasuhiro Saka

Jeffrey L Watts

Shinichi Sakashita

Robert J Yancey, Jr

Fumihiko Kanoo

George Todaro

Ribhi M Shawar

Fumihiko Kano

Use of rifamycin derivative for treating mastitis in a domestic animal

Antibacterial compositions comprising (1) a rifamycin derivative represented by the formula (I) or its physiologically acceptable salt, and (2) a proton pump inhibitor (a) or a bismuth preparation (b) wherein the components (1) and (2) are used in such amounts as producing a synergistic effect against drugs and remedies for digestive organ diseases which contain the antibacterial compositions, process for producing them, and pharmaceutical preparations related to the antibacterial compositions. The compositions can be administered to patients with digestive diseases caused by infection of in a smaller dose and at a lower administration frequency as compared with conventional remedies.

Antibacterial compositions with synergistic effect, drugs and remedies for digestive diseases containing the same, process for the production thereof and preparations associated therewith

A method for treating a digestive organ disease caused by the infection of Helicobacter, comprising administering a rifamycin derivative expressed by the formula (I), or a physiologically acceptable salt thereof ##STR1##

Treatment of disease caused by infection of Helicobacter

A method for treatment of diseases caused by Chlamydia infection is disclosed comprising administering a rifamycin of the formula (I): ##STR1## wherein R.sup.1 is hydrogen atom or acetyl, and X is oxygen, sulfur or a group NR, in which R is hydrogen, an alkyl group having 1 to 7 carbon atoms or a group of the formula (II): ##STR2## in which n is an integer of 1 to 3; or a physiologically acceptable salt thereof.

Method for treating chlamydia infectious diseases by rifamycin derivative

A rifamycin derivative having the formula (I): ##STR1## wherein A is a group having the formula: ##STR2## in which R.sup.1 is an alkyl group having 4 or 5 carbon atoms or an alkenyl group having 3 to 5 carbon atoms, or a group having the formula: in which n is 3 or 4; or a pharmaceutically acceptable salt thereof. The rifamycin derivative (I) exhibits a strong antibacterial activity against Gram-positive bacteria and acid-fast bacteria, and also exhibits a strong antibacterial activity against tubercle bacilli.

3'-hydroxybenzoxazinorifamycin derivative, process for preparing the

A rifamycin derivative having the formula (I): ##STR1## wherein R.sup.1 is hydrogen atom, methyl group or ethyl group, R.sup.2 is an alkyl group having 1 to 4 carbon atoms, and A is a group having the formula: ##STR2## in which n is an integer of 3 to 5, or group having the formula: ##STR3## in which R.sup.3 is a alkyl group having 1 to 5 carbon atoms; or a salt thereof. The rifamycin derivative (I) exhibits a strong antibacterial activity against Gram-positive bacteria and acid-fast bacteria, and also exhibits a strong antibacterial activity against tubercle bacilli.

Substituted benzoxazinorifamycin derivative and antibacterial agent

A novel rifamycin derivative having the formula (I): ##STR1## wherein X.sup.1 is an alkyl group with 1 to 6 carbon atoms or a cycloalkyl group with 3 to 8 carbon atoms; X.sup.2 is a hydrogen atom or an alkyl group with 1 to 4 carbon atoms; R.sup.1 is hydrogen atom or acetyl group; A is a group represented by the formula: ##STR2## wherein R.sup.2 is an alkyl group with 1 to 4 carbon atoms or an alkoxyalkyl group with 2 to 6 carbon atoms and R.sup.3 is an alkyl group with 1 to 6 carbon atoms or an alkoxyalkyl group with 2 to 6 carbon atoms, or a group represented by the formula ##STR3## wherein ##STR4## is a 3 to 9 membered cyclic amino group with 2 to 8 carbon atoms, R.sup.4 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, or salts thereof, a process for preparing the same and antibacterial agents containing the same as an effective ingredient. The rifamycin derivative of the present invention having the formula (I) shows a strong antibacterial activity against the Gram-positive bacteria and the acid-fast bacteria.

Alkyl-substituted benzoxazinorifamycin derivative, process for preparing

A novel rifamycin derivative having the general formula (I): ##STR1## or salts thereof, a process for preparing the same and antibacterial agents containing the same as an effective component. The rifamycin derivative of the present invention having the general formula (I) shows a strong antibacterial activity against the Gram-positive bacteria and the acid-fast bacteria.

Benzoxazinorifamycin derivative, process for preparing the same and

A new anti-inflammatory, analgesic, and antipyretic pharmaceutical composition is disclosed which contains a 3,5-di-tert-butyl-4-hydroxystyrene derivative of the formula: ##STR1## wherein R.sup.1 stands for a group represented by COR.sup.3 [R.sup.3 denotes a group of OR.sup.4 (R.sup.4 is a hydrogen atom or an alkyl group with C.sub.1 .about.C.sub.4), an alkyl group with C.sub.1 .about.C.sub.3, a phenyl group, or an amino group], a nitro group, or an alkylsulfonyl group represented by SO.sub.2 R.sup.5 (R.sup.5 is an alkyl group with C.sub.1 .about.C.sub.3); and R.sup.2 stands for a hydrogen atom, an alkyl group with C.sub.1 .about.C.sub.4, a hydroxyalkyl group with C.sub.1 .about.C.sub.4, a cyano group, or an acyl group represented by COR.sup.6 (R.sup.6 is an alkyl group with C.sub.1 .about.C.sub.3), or its pharmaceutically acceptable salt as an active ingredient in association with pharmaceutical excipients. The pharmaceutical composition has excellent anti-inflammatory, analgesic, and antipyretic activities and low toxicity.

Anti-inflammatory, analgesic, and antipyretic pharmaceutical composition

Novel compounds, 3,5-di-tert-butylstyrene derivatives and their salts, are disclosed, which derivatives are represented by the general formula: ##STR1## wherein R.sup.1 stands for an acyloxy group represented by R.sup.3 COO (R.sup.3 is a hydrogen atom or an alkyl group with C.sub.1 -C.sub.6), an alkoxyl group of R.sub.4 O (R.sup.4 is an alkyl group with C.sub.1 -C.sub.4), a hydroxyl group, or a hydrogen atom; R.sup.2 stands for ##STR2## (R.sup.5 is a hydrogen atom or an alkyl group with C.sub.1 -C.sub.3 and X.sup.1 is CH.sub.2 or an oxygen atom), ##STR3## (R.sup.5 and X.sup.1 are each the same as defined above), or ##STR4## (X.sup.2 is an oxygen or sulfur atom). There are also disclosed an anti-inflammatory, analgesic, and antipyretic pharmaceutical composition and an anti-platelet aggregation pharmaceutical composition, both pharmaceutical compositions comprising the foregoing 3,5-di-tert-butylstyrene derivative or its pharmaceutically acceptable salt as an active ingredient in association with pharmaceutical excipients.

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Kobe, Japan

Katsuji Yamashita