Ono Pharmaceutical Co., Ltd.

Takashi Muryobayashi

Katsuhiro Imaki

Yoshiki Sakai

Hisao Nakai

Masayasu Kurono

Hajimu Miyake

Takashi Yamato

Akiyoshi Kawasaki

A novel prostaglandin analogue of the formula: ##STR1## [wherein the symbol  represents .beta.-configuration, the dotted line ---------- represents .alpha.-configuration, and the double bond between C.sub.13 -C.sub.14 represents transconfiguration] and cyclodextrin clathrates thereof, and non-toxic salts thereof are useful for the treatment and/or prevention of diseases induced by platelet aggregation, such as thrombosis, or induced by cytodamage.

Prostaglandin analogue

Use of prostaglandin analogues to treat cytodamage

Prostaglandin E.sub.1 analogues of the general formula: ##STR1## (wherein R.sup.1 represents a single bond or a straight- or branched-chain alkylene group of from 1 to 5 carbon atom(s), R.sup.2 represents a cycloalkyl group of from 4 to 7 carbon atoms either unsubstituted or substituted by at least one straight- or branched-chain alkyl group of from 1 to 8 carbon(s), and the double bond between C.sub.13 and C.sub.14 is trans) and cyclodextrin clathrate thereof, are useful in the prevention or treatment of cytodamage associated with digestive system disease, especially liver damage.

Prostaglandin E.sub.1 analogues

Prostaglandin analogue of the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atom(s), R.sup.2 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 6 carbon atom(s), the symbols------X--Y--Z-- in formula VB represent one of the groups: ##STR2## wherein in formulae (ii) and (iv), the configuration on C.sub.6 is S- or R-configuration or a mixture thereof and in formulae (iii) and (v) the double bond between C.sub.5 and C.sub.6 is in E- or Z-configuration or a mixture thereof) and n represents an integer of from 3 to 5 non-toxic salts thereof when R.sup.1 represents a hydrogen atom and cyclodextrin clathrates thereof are useful in the prevention or treatment of cytodamage associated with many diseases, especially liver damage.

Prostaglandin E.sub.1 analogues of general formula: ##STR1## [wherein R.sup.1 represents a bond or a straight- or branched-chain alkylene group containing from 1 to 5 carbon atom(s), and R.sup.2 represents a hydrogen atom, a straight- or branched-chain alkyl group containing from 1 to 8 carbon atom(s), a cycloalkyl group containing from 4 to 7 carbon atoms in the ring and unsubstituted or substituted by at least one stright- or branched-chain alkyl group containing from 1 to 8 carbon atom(s) or a phenyl or phenoxy group unsubstituted or substituted by at least one halogen atoms, trifluoromethyl group or straight- or branched-chain alkyl group containing from 1 to 4 carbon atom(s), with the proviso that, when R.sup.1 represents a bond, R.sup.2 does not represent a phenoxy group,] possess inhibitory activity or gastric ulceration and cytoprotective activity.

Prostaglandin analogues

Prostaglandin analogues of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## X represents trans-vinylene or ethylene and Y represents cis-vinylene or ethylene, R represents hydrogen or alkyl of 1 through 12 carbon atoms, R.sup.1, R.sup.2 and R.sup.3 represent hydrogen, or alkyl of 1 through 12 carbon atoms or an aryl group, with the proviso that at least one of the symbols R.sup.1, R.sup.2 and R.sup.3 represents an alkyl or aryl group, are new compounds possessing useful pharmacological properties; they are especially useful for the treatment of gastric ulceration.

Growing community of inventors

Takatsuki, Japan

Takashi Muryobayashi