Prostaglandins E and anti ulcers containing same

Details Prostaglandins E and anti ulcers containing same Prostaglandins E and anti ulcers containing same

1998-05-06

2001-07-24

Gerstl, Robert (Department: 1626)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

C514S573000, C560S121000, C562S503000

Reexamination Certificate

active

06265440

ABSTRACT:

BACKGROUND OF THE INVENTION
The present invention relates to a novel type of prostaglandin E and ulcer preventive agents containing the same.
Prostaglandin is a generic term for various prostanoic acids and is classified into various groups, such as E, F, A, B, C, D, and H, according to the manner in which keto and/or hydroxyl groups are introduced in five-membered ring portions. Prostaglandins will stimulate the uterine muscle and, in addition, they have various physiological and pharmacological actions, such as vasodilation, inhibition of platelet aggregation, and inflammatory action.
Prostaglandin E (hereinafter referred to as PGE), as a substance with a five-membered ring structure, has a group represented by:
Broadly, there are known two types of PGE, namely, PGE
1
in which the carbon-carbon bond at the 5- and 6-positions (C
5
-C
6
bond) is a single bond:
and PGE
2
in which the C
5
-C
6
bond is a double bond:
PGE
2
, for example, is known as having antiulcer activity on one hand, but on the other hand it has such actions as uterine contraction, intestine contraction, and vasodilation; further it is recognized as having side effects, such as severe alvine flux. Therefore, it is unsuitable or impossible to use PGE
2
as antiulcers.
Whilst, it has been recognized that in human or animal metabolites there are present free substances similar to prostaglandin E in which C
13
-C
14
bond is saturated and in which the carbon at the 15-position forms a carbonyl group. These substances, or species of 13,14-dihydro-15-keto prostaglandin E are:
These corresponds to PGE
1
, PGE
2
, and 6-keto PGE
1
respectively, and they are known as substances which are naturally metabolically produced in vivo through enzymic metabolic reaction. These species of 13,14-dihydro-15-keto PGE have been reported as physiologically and pharmacologically inactive metabolic products which exhibit little of the various physiological activities of PGE (Acta Physiologica Scandinavica, Vol 66, p. 509~, 1966), and has been regarded as such. Therefore, little has been expected of the pharmacological effect of these metabolic products and compounds similar to them.
SUMMARY OF THE INVENTION
While evaluating the pharmacological activities of derivatives of the aforesaid metabolic products, the present inventor found that the derivatives, such as esters salts, one having a protective group on the carboxyl group as well as one having free carboxyl group, one having substituent groups at the 16-, 17-, 19-, and/or 20-positions, one in which the carbon at the 11-position has a methyl group or a hydroxymethyl group, and one having an alkoxy group at the terminal of a &ohgr; chain, exhibited antiulcer activities, and that they showed no trace or a significantly reduced degree of such central and peripheral physiological effects as were simultaneously appeared as a side effect and were inherent to known or common PGE which had been recognized as having antiulcer activities.


REFERENCES:
patent: 3836578 (1974-09-01), Samuelson
patent: 5166174 (1992-11-01), Ueno
Erik Anggard, “The Biological Activities of Three Metabolites of Prostaglandin1” Acta Physiol. Scand. (1966) 66:509-510.

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