Sankyo Company, Limited

Yukio Sugimura

Kimio Iino

Tomoyuki Shibata

Toshihiko Hashimoto

Tomowo Kobayashi

Teruo Tanaka

Shinichi Sugawara

Tetsuo Miyadera

Yoshio Tsujita

Shigeki Muramatsu

Takeshi Kagasaki

Tetsuo Hiraoka

Kazuhiko Tamaki

Yukiko Kameyama

Yoko Shimada

Masayuki Iwata

Takafumi Kohama

Kazuhiko Sasagawa

Kazuhiko Tanzawa

Akio Shiraishi

Naomi Shimazaki

Shinwa Kurihara

Radicicol derivatives in which one or both hydroxy groups are acylated have valuable anti-tumor activity or may be used as chemical intermediates.

Radicicol derivatives, their preparation and their anti-tumor activity

Collagenase inhibitor

Compounds of formula (I): ##STR1## in which: A and B are separately monoamines or together diamines; and Z is a group of formula (II) or (III): ##STR2## (in which R.sup.1, R.sup.2 and R.sup.7 are various organic groups, n is 0, 1 or 2 and X is a direct carbon-carbon bond or lower alkylene) show valuable anti-tumor activity and may be prepared by reacting an amine-platinum complex with a compound providing the group represented by Z.

Anti-tumor platinum complexes, their preparation and their therapeutic

A compound of the formula ##STR1## in which: R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen atoms and groups of formula R.sup.3 --CO--, wherein R.sup.3 represents a group selected from the group consisting of unsubstituted alkyl groups having from 9 to 20 carbon atoms; substituted alkyl groups having from 10 to 20 carbon atoms; unsubstituted alkenyl groups having from 9 to 20 carbon atoms; substituted alkenyl group having from 10 to 20 carbon atoms; unsubstituted alkynyl groups having from 8 to 10 carbon atoms; and substituted alkynyl groups having from 8 to 10 carbon atoms wherein R.sup.1 and R.sup.2 are not both hydrogen atoms or acetyl groups. The compounds have antitumor activity.

A new compound, which we have named Leustroducsin H, has formula (I): ##STR1## and pharmaceutically acceptable salts thereof. This compound may be prepared by hydrolysis of naturally occurring Leustroducsins and the compound may be used for the treatment or prophylaxis of thrombocytopenia.

Leustroducsin H, its preparation and its therapeutic use

Compounds of formula (I): ##STR1## wherein: one or both of R.sup.1 and R.sup.2 are selected from a variety of organic groups;

2-(1-aceti

Compounds of formula (I): ##STR1## (wherein R.sup.1 is carboxy, --CONR.sup.4 R.sup.5, cyano or hydroxymethyl, and R.sup.2 and R.sup.3 are hydrogen, alkyl or substituted alkyl, R.sup.4 and R.sup.5 being hydrogen or a variety of groups) have good antibiotic activity and reduced renal toxicity.

Carbapenem compounds and use

Compounds of formula (I): ##STR1## in which: R.sup.1 represents a hydrogen atom, an alkyl group, an alkoxy group or various substituted alkyl groups;

2-penem-3-carboxylic acid derivatives and use

Compounds of formula (I): ##STR1## (wherein R.sup.1 represents a C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.3 alpha-hydroxyalkyl group;

Penem derivatives, and composition containing them

Compounds of formula (I): ##STR1## [wherein: R.sup.1 represents a hydrogen atom, an alkyl group, an alkoxy group or various substituted alkyl groups;

Carbapenem compounds, and compositions containing them

A 7.beta.-acylamino-7.alpha.-alkoxycephalosporin is prepared by reacting a 7-acylaminocephalosporin with a halogenating agent to give an iminohalide, reacting the latter compound with a base to give a keteneimine, reacting the latter compound with a halogen to give an .alpha.-halogeno iminohalide, reacting the latter compound with an alkali metal alkoxide and consecutively either subjecting the resulting compound to hydrolysis, or reacting the resulting compound with an acid or a halogenosilyl compound followed by treating the resulting compound with water. The 7.beta.-acylamino-7.alpha.-alkoxycephalosporin is useful as an antibacterial agent.

Process for preparing 7.beta.-acylamino-7.alpha.-alkoxycephalosporins

A process for preparing a 7.beta.-acylamino-7.alpha.alkoxycephalosporin or 6.beta.-acylamino-6.alpha.-alkoxypenicillin which comprises either (a) reacting a 7.beta.-(.alpha.'-halogeno or .alpha.'-hydroxyacylamino)cephalosporin or 6.beta.-(.alpha.'halogeno or .alpha.'-hydroxyacylamino)penicillin with a halogenating agent to give a .alpha.-halogeno-iminohalide, reacting the latter compound with an equimolar amount of an alkali metal alkoxide in the presence of one equivalent amount of a base to give a 7.alpha.-alkoxyketeneimine and subjecting the latter compound to hydration; or (b) reacting the 7.beta.-(.alpha.'-halogeno or .alpha.'hydroxyacylamino)cephalosporin or 6.beta.-(.alpha.'-halogeno or .alpha.'-hydroxyacylamino) penicillin with the halogenating agent to give the .alpha.-halogeno-iminohalide, reacting the latter compound with two equimolar amounts of the alkali metal alkoxide in the presence of one equivalent amount of the base to give a dialkoxyimino compound, reacting the latter compound with a halogeno-silyl compound or an acid and treating the resulting product with water. The final products are useful as antibacterial agents or intermediates thereof.

Growing community of inventors

Tokyo, Japan

Yukio Sugimura