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Details for Patent: 5,886,034

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Details for Patent: 5,886,034

Title: Prostaglandins E and anti ulcers containing same
Abstract:The novel 13,14-dihydro-15-keto prostaglandins E of the invention have remarkable preventive effects against ulcers. Further, the novel 13,14-dihydro-15-keto-prostaglandins E of the invention have an advatage that they have none of side effects which prostaglandin E intrinsically has, or can remarakably reduce such effects of the prostaglandin E. Therefore, the novel 13, 14-dihydro-15-keto prostaglandins E of the invention are effective for animal and human use for treatment and prevention of ulcers, such as duodenal ulcer and gastric ulcer.
Inventor(s): Ueno; Ryuzo (Nishinomiya, JP), Ueno; Ryuji (Nishinomiya, JP), Kato; Ichie (Kawanishi, JP), Oda; Tomio (Sanda, JP)
Assignee: Kabushiki Kaisha Ueno Seiyaku Kenkyujo (Osaka-Fu, JP)
Filing Date:Mar 10, 1995
Application Number:08/401,675
Claims:1. Prostaglandin E of general formula I:

wherein X is ##STR48## R.sub.1 is a hydrogen atom, a physiology acceptable salt residue, or an ester residue selected from the group consisting of alkyl, benzyl, hydroxyalkyl, alkoxyalkyl, alkylsilyl and tetrahydropyranyl group;

R.sub.2 is a hydrogen atom or a methyl group;

R.sub.3 is a hydroxyl or hydroxymethyl group;

R.sub.4 is a hydrogen atom;

R.sub.5 is a hydrogen atom; and

R.sub.6 is a C.sub.6 -C.sub.9 straight alkyl group which may have a double bond,

wherein the C.sub.2 -C.sub.3 bond is a single bond.

2. The prostaglandin E of claim 1, wherein R.sub.6 is a C.sub.6 straight alkyl group.

3. The prostaglandin E of claim 1, wherein the general formula is. ##STR49##

4. The prostaglandin E of claim 1, which is 13,14-dihydro-15-keto-20-ethyl-PGE.sub.2 or alkyl ester thereof.

5. An anti-ulcer composition comprising an anti-ulcer effective amount of prostaglandin E of general formula I: ##STR50## wherein X is ##STR51## R.sub.1 is a hydrogen atom, a physiologically acceptable salt residue, or an ester residue selected from the group consisting of alkyl, benzyl, hydroxyalkyl, alkoxyalkyl, alkylsilyl and tetrahydropyranyl group;

R.sub.2 is a hydrogen atom or a methyl group;

R.sub.3 is a hydroxyl or hydroxymethyl group;

R.sub.4 is a hydrogen atom;

R.sub.5 is a hydrogen atom; and

R.sub.6 is a C.sub.6 -C.sub.9 straight alkyl group which may have a double bond,

wherein the C.sub.2 -C.sub.3 bond is a single bond.

6. The anti-ulcer composition of claim 5, wherein R.sub.6 is a C.sub.6 straight alkyl group.

7. The anti-ulcer composition as described in claim 5, wherein the general formula is. ##STR52##

8. The anti-ulcer composition of claim 5, which is 13,14-dihydro-15-keto-20-ethyl-PGE.sub.2 or alkyl ester thereof.
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