Indoleacetic acid derivatives, process for their preparation, an

Details Indoleacetic acid derivatives, process for their preparation, an Indoleacetic acid derivatives, process for their preparation, an

1990-04-24

1993-01-05

Springer, David B.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

546201, 548501, C07D40312, C07D40112, A61K 3141, A61K 31445

Patent

active

051772230

DESCRIPTION:

BRIEF SUMMARY
DESCRIPTION

1. Technical Field
The present invention relates to an indoleacetic acid derivative which has an anti-inflammatory action, an antirheumatic action and an anti-ulcer action, and particularly to an indoleacetic acid derivative and a salt thereof which have a reduced adverse effect than that of conventional non-steroidal anti-inflammatory drugs, a method of preparing them and an anti-inflammatory drug, antirheumatic drug and anti-ulcer drug each of which contains one of them as an active ingredient.
2. Background Art
Anti-inflammatory drugs are classified into steroid hormones, non-steroidal anti-inflammatory drugs, antiphlogistic enzymes and immunosuppression agents. Of these drugs, non-steroidal anti-inflammatory drugs are most important drugs and, in recent, they have been actively developed all over the world. However, such non-steroidal anti-inflammatory drugs have many problems in the clinical field. The most critical problem is adverse effects such as damages to the digestive organs and the kidneys. Indomethacin, which is a typical indoleacetic acid-type compound having the strongest anti-inflammatory action among non-steroidal anti-inflammatory drugs, is a first choice drug as a remedy for rheumatism. Although indomethacin has a great curative effect, it has adverse effects such as injuries to the gastrointestine and the kidneys and thus has a critical problem in use. Such adverse effects are serious since indomethacin must be continuously administered to the rheumatics for a long period and a large amount of indomethacin must be used as an anti-inflammatory drug. As this type of anti-inflammatory drugs manifest curative effects and adverse effects which are much different depending upon patients, it is necessary to use various types of drugs.
There is thus demand for an anti-inflammatory drug which has reduced adverse effects such as injuries to the gastrointestine and the kidneys and which is effective with excellent persistence.
On the other hand, a group of anticholinergic drugs and histamine H2 receptor blockers such as Cimetidine are generally used as drugs effective for controlling the gastric-acid secretion in the clinical field.
Anticholinergic drugs have adverse effects of controlling the gastric excretory movement and controlling the thirs, mydriasis and sudation, and also have a limit to the use for inhibiting the aggravation of ulcer and preventing the recurrence thereof even if the drugs are used in amounts which allow the gastric-acid secretion to be substantially inhibited. Cimetidine exhibits adverse effects such as an undesirable central action and an antiandrogen action, and particularly has a problem with respect to the lowering in defensive factors in gastric mucosa, which is observed in curing treatment for a long period. It is said that this mainly causes the recurrence of ulcer after the use of cimetidine has been stopped.
There has been arisen a demand for a compound capable of effectively controlling the secretion of the gastric acid serving as an aggressive factor, capable of reinforcing the defensive factor (cytoprotection action) and also having an excellent anti-ulcer action.
Considering the above-mentioned situation, the inventors energetically researched with a view to developing an excellent anti-inflammatory drug, antirheumatic drug, and anti-ulcerative drug. As a result, the inventors found that novel indoleacetic acid derivatives expressed by the formula (I) below and salts thereof have an excellent anti-inflammatory action, antirheumatic action and anti-ulcer action and exhibit extremely reduced adverse effects. This led to the achievement of the present invention.


DISCLOSURE OF INVENTION

The present invention provides indoleacetic acid derivatives expressed by the following formula (I) and salts thereof: ##STR4## [wherein X denotes a piperidino group, 1-pyrrolidinyl group or 3-hydroxy-1-pyrrolidinyl group; Y denotes ##STR5## (wherein R.sup.1 denotes a hydrogen atom or a lower alkyl group, 1 denotes 0, 1 or 2) or ##STR6## (wherein R.sup.2 denotes a

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