Sankyo Company, Limited

Kazuhiko Sasagawa

Tomowo Kobayashi

Masakatsu Kaneko

Yasuo Shimoji

Yo Takiguchi

Makoto Kamokari

Tomoyuki Shibata

Norio Nakamura

Mitsuo Yamazaki

Yukio Sugimura

Takafumi Kohama

Jun Ohsumi

Kiyoshi Sakai

Takashi Yusa

Fusaaki Shimizu

Kazuhiko Tamaki

Osamu Oda

Hideki Miyazaki

Akio Shiraishi

Shinwa Kurihara

Naomi Shimazaki

Masaaki Sasaki

Jun Ohsuri

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

Rhizoxin and rhizoxin-2-ene derivatives of formula (I): ##STR1## in which: n is 1 to 25: A is an extra bond or oxygen, X is oxygen, sulfur, nitrogen or carbonyl; and R is hydrogen, carboxylic acyl having from 1 to 25 carbon atoms, alkoxycarbonyl group having from 2 to 26 carbon atoms, phosphono, alkylphosphono group in which the alkyl part has from 1 to 25 carbon atoms, dialkylphosphono group in which each alkyl part has from 1 to 25 carbon atoms, alkyl group having from 1 to 25 carbon atoms, aralkyl, cycloalkyl, heterocyclic, alkylthio group in which the alkyl part has from 1 to 25 carbon atoms, aralkylthio, or heterocyclylthio, or when X represents a nitrogen atom, R is R.sup.1 and R.sup.2, where R.sup.1 and R.sup.2 are hydrogen, alkyl, acyl, alkoxycarbonyl, phosphono, alkylphosphono or dialkylphosphono have valuable anti-tumor activity. They may be prepared by acylation of rhizoxin or rhizoxin-2-ene.

Rhizoxin derivatives and their use as anti-tumor agents

Rhizoxin and rhizoxin-2-ene derivatives of formula ##STR1## in which: n is 1 to 25; A is an extra bond or oxygen, X is oxygen, sulfur, nitrogen or carbonyl; and R is hydrogen, carboxylic acyl having from 1 to 25 carbon atoms, alkoxycarbonyl group having from 2 to 26 carbon atoms, phosphono, alkylphosphono group in which the alkyl part has from 1 to 25 carbon atoms, dialkylphosphono group in which each alkyl part has from 1 to 25 carbon atoms, alkyl group having from 1 to 25 carbon atoms, aralkyl, cycloalkyl, heterocyclic, alkylthio group in which the alkyl part has from 1 to 25 carbon atoms, aralkylthio, or heterocyclylthio, or when X represents a nitrogen atom, R is R.sup.1 and R.sup.2, where R.sup.1 and R.sup.2 are hydrogen, alkyl, acyl, alkoxycarbonyl, phosphono, alkylphosphono or dialkylphosphono, have valuable anti-tumor activity. They may be prepared by acylation of rhizoxin or rhizoxin-2-ene.

Compounds of formula (I): ##STR1## [in which: Y represents a group of formula ##STR2## the dotted line is a double of single bond; R.sup.1 is hydrogen, alkyl or aryl; R.sup.2 is hydrogen or halogen; R.sup.3 is alkyl or cycloalkyl; R.sup.4 is hydrogen, alkyl, hydroxy or halogen; and R.sup.6 is hydrogen, optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or aralkyl;] and pharmaceutically acceptable salts thereof are valuable in the treatment of cachexia. Certain of these compounds are novel.

Method of treating cachexia and certain new compounds for use in this

Compounds of formula (I): ##STR1## and pharmaceutically acceptable salts thereof are valuable in the treatment of cachexia.

Method of treating cachexia

Compounds of formula (I): ##STR1## [wherein: m is 1-3; A and B are oxygen or sulfur; and one of R.sup.1 and R.sup.2 is C.sub.10 -C.sub.22 alkyl and the other is a group of formula (II). ##STR2## where: n is 2 or 3; and --NR.sup.3 R.sup.4 R.sup.5 is an amino group] and salts thereof are effective anti-cancer agents.

Certain tetrahydro-furan or pyran phosphate-ethylene or propylene

Prostanoic acid derivatives having the formula ##STR1## wherein A represents a straight or branched alkylene group having from one to 5 carbon atoms, R.sup.1 represents a straight or branched alkyl group having from 4 to 10 carbon atoms and R.sup.2 represents hydrogen atom or a straight or branched alkyl group having from one to 6 carbon atoms and pharmaceutically acceptable salts thereof. The compounds are useful as oxytocic agents and agents inhibiting the secretion of gastric acid and may be prepared by oxidizing a compound having the formula ##STR2## wherein A, R.sup.1 and R.sup.2 are the same as above, R.sup.3 and R.sup.4 are the same or different and each represents a protecting group for the hydroxyl group to give a compound having the formula ##STR3## wherein A, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same as above, removing the hydroxyl-protecting group from the latter compound and, if appropriate, salifying the product thus obtained.

16,16-Dimethyl

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Tokyo, Japan

Kazuhiko Sasagawa