Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-04-28
1996-11-05
Springer, David B.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546126, C07D45104, A61K 3146
Patent
active
055718205
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP 93/01484 filed Oct. 15, 1993.
TECHNICAL FIELD
The present invention relates to a heterocyclic compound. More particularly, the present invention relates to a novel quinolone compound, which has an action for stimulating a serotonin 4 receptor and is therefore useful for the treatment of chronic gastritis or for improving digestive tract conditions accompanied by postoperative gastroparesis. The present invention also relates to a pharmaceutical use of such a quinolone compound.
BACKGROUND ART
Serotonin is a nurotransmitter which is widely distributed in human and has a remarkable variety of physiological effects. It is hitherto known that a serotonin receptor includes three subtypes of serotonin 1 receptor, serotonin 2 receptor and serotonin 3 receptor. In addition to these receptors, it is reported by Dumuis, A., et al., Molecular Pharmacology, 34, 880, 1988 that serotonin 4 receptor is existent.
Serotonin 4 receptor is considered to take a part in contraction of the ileum or ascending colon of guinea pig or relaxation of rat esophagus. Cisapride and renzapride, which are stimulants of serotonin 4 receptor, accelerate gastrointestinal motor functions and improve gastrointestinal conditions such as chronic gastritis, heartburn accompanied by postoperative gastroparesis, anorexia, bowel pain, abdominal distension, etc., and are thus considered to be effective for the treatment of gastro-esophagal reflux, intestinal pseudo-obstruction and constipation [Alimentary Pharmacology and Therapeutics, 6, 273, 1992].
As heterocyclic compounds having an activity of antagonizing or stimulating serotonin receptors, European Patent No. 0458636A1 discloses quinolone derivatives which exert on a serotonin 3 receptor antagonizing activity.
On the other hand, U.S. Pat. No. 5,106,851 discloses quinazoline-carboxylic acid derivatives as heterocyclic compounds effective for the treatment of gastrointestinal disorders. However, the compounds are merely known to show an affinity to muscarinic receptors but remain unknown about any action of serotonin receptors.
As stated above, no research has been reported on any heterocyclic compound having an excellent antagonizing or stimulating activity particularly on serotonin 4 receptor.
Accordingly, the .object of the present invention is to provide a novel heterocyclic compound having a potent stimulating activity especially on serotonin 4 receptor and a pharmaceutical use thereof.
DISCLOSURE OF INVENTION
An object of the present invention is to provide endo-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-1-isopropyl-2(1H)-quinolone- 3-carboxamide represented by formula (I): ##STR2## as well as a pharmaceutically acceptable salt thereof.
Another object of the present invention is to provide a pharmaceutical composition comprising as an effective ingredient the compound of formula (I) or its pharmaceutically acceptable salt and a pharmaceutically acceptable carrier, particularly for stimulating serotonin 4 receptor.
A further object of the present invention is to provide a method for stimulating serotonin 4 receptor which comprises administering to human an effective dose of the compound of formula (I) or a pharmaceutically acceptable salt thereof.
A still further object of the present invention is to provide the compound of formula (I) or a pharmaceutically acceptable salt thereof, for use as an active ingredient of the pharmaceutical composition particularly for stimulating serotonin 4 receptor.
A still further object of the present invention is to provide use of said compound or a salt thereof for the preparation of a pharmaceutical composition comprising as an effective ingredient the compound of formula (I) or a pharmaceutically acceptable salt thereof and for stimulating serotonin 4 receptor.
BEST MODE FOR CARRYING OUT THE INVENTION
As the pharmaceutically acceptable salts of the compound of formula (I) in accordance with the present invention, there are acid addition salts. These acid addition salts are those obtained by adding pharmacologi
REFERENCES:
patent: 5106851 (1992-04-01), Turconi et al.
patent: 5248684 (1993-09-01), Suzuki et al.
Asanuma Hajime
Hatayama Katsuo
Isobe Yoshihiko
Ito Chika
Muramatsu Makoto
Springer David B.
Taisho Pharmaceutical Co. Ltd.
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