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Details for Patent: 6,265,440

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Details for Patent: 6,265,440

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 advantage that they have none of side effects which prostaglandin E intrinsically has, or can remarkably 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: R-Tech Ueno, Ltd. (Osaka-fu, JP)
Filing Date:May 06, 1998
Application Number:09/073,253
Claims:1. Prostagelandin E of general formula I: ##STR78##

wherein X is ##STR79##

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 or a methyl group; R.sub.5 is a hydrogen atom or a methyl group; and R.sub.6 is a C.sub.5 -C.sub.9 alkyl group which may have a branch or 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.5 is a methyl group.

3. The prostaglandin E of claim 1, wherein R.sub.6 is a C.sub.6 -C.sub.9 alkyl group.

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

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

6. An anti-ulcer composition comprising an anti-ulcer effective amount of prostaglandin E of general formula I: ##STR80##

wherein X is: ##STR81##

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 or a methyl group;

R.sub.5 is a hydrogen atom or a methyl group; and

R.sub.6 is a C.sub.5 -C.sub.9 alkyl group which may have a branch or a double bond, wherein the C.sub.2 -C.sub.3 bond is a single bond.

7. The anti-ulcer composition of claim 6, wherein R.sub.5 is a methyl group.

8. The anti-ulcer composition of claim 6, wherein R.sub.6 is a C.sub.6 -C.sub.9 alkyl group.

9. The anti-ulcer composition of claim 6, which is 13,14-dihydro-15-keto-20-methyl-PGE.sub.1 or alkyl ester thereof.

10. The anti-ulcer composition of claim 6, which is 13,14-dihydro-15-keto-20-ethyl-PGE.sub.1 or alkyl ester thereof.
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