Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-12-21
1996-06-11
Rollins, John W.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
424451, 424464, A61K 31505, A61K 948, A61K 920
Patent
active
055256058
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The present invention relates to a remedy for inflammatory intestinal diseases which contains as the active ingredient 9-(4-acetyl-3-hydroxy-2-n-propylphenoxymethyl)-3-(1H-tetrazol-5-yl)-4H-pyr ido[1,2-a]pyrimidine-4-one (hereinafter referred to as Compound 1) or a physiologically acceptable salt thereof.
BACKGROUND ARTS
Inflammatory intestinal diseases are spontaneous and chronic diseases of which typical examples are ulcerative colitis and Crohn's disease, and the numbers of the patients suffering therefrom have been steadily increasing in recent years. Many principal and clinical investigations have been vigorously carried out by investigating groups such as the special diseases investigating group on refractory inflammatory intestinal disorders of the Ministry of Health, Japan; however, the cause and the morbidity of the diseases involved have not been discovered.
For the treatment of inflammatory intestinal diseases, only several attempts such as the administration of an immunosuppressive agent, 6-mercaptopurine, the voluminous administration of an antibacterial agent, sulfasalazine, and oral, intravenous, topical and intracolonic administration of steroid hormones, such as prednisolone acetate, have been made. However, these pharmaceutical treatments can play a role only as symptomatic therapy for the diseases and are not of the type which can quickly remove the symptoms arising from digestive organs, such as diarrhea, bloody stool, and abdominal pain. Furthermore, these drugs mentioned above give side effects in a high rate and are required to be administered voluminously for a long period, and therefore, such drugs have a disadvantage in terms of the maintenance of the quality of life of the patients. Moreover, it is known that non-steroid anti-inflammatory agents such as indomethacin, which is commonly used for the treatment for inflammatory diseases, normally make the condition of the patients suffering from the inflammatory intestinal diseases worse, providing difficulty in the maintenance of remission of the diseases.
It is an object of the present invention to remedy inflammatory reactions, which is the cause of the disease, in a short time and to provide a highly safe remedy for the inflammatory intestinal diseases by removing the symptoms deriving from digestive organs, such as diarrhea, bloody stool, and abdominal pain, therewith.
DISCLOSURE OF THE INVENTION
In the course of pharmacological study on pyridopyrimidine compounds known as having suppressive action on the central nervous system (Japanese Patent Laid-opened No. Sho 49-14495 Gazette), suppressive action on allergic reaction (Japanese Patent Laid-opened No. Sho 54-36294 Gazette) and antagonistic action on SRS-A (Japanese Patent Laid-opened No. Sho 62-24262 Gazette and No. Sho 63-183581 Gazette), the inventors of the present patent application found that either compound 1 represented by the formula: ##STR2## or a physiologically acceptable salt thereof (hereinafter referred to as Pyridopyrimidine compound I) has remedial action on inflammatory intestinal diseases, which has not been known in the past, and thereby accomplishing the present invention.
The compound 1, the active ingredient specified in the present invention, can be prepared, for example, by forming a tetrazol ring in reacting 9-(4-acetyl-3-hydroxy-2-n-propylphenoxymethyl)-3-cyano-4H-pyrido[1,2-a]pyr imidine-4-one with aluminium azide, then converting the resulting compound to a potassium salt thereof by using potassium hydroxide/ethanol solution and letting it precipitate by neutralizing it with chloric acid or sulfuric acid.
For the physiologically acceptable salt of the compound 1, a sodium or potassium salt thereof can be exemplified.
The compound 1 showed distinct remedial effect on intestinal impairment when it was administered into guinea pigs having intestinal impairment which was induced by the intracolonic injection of acetic acid (intestine-impaired guinea pigs), or rats and mice both having intestinal impairment which was induce
REFERENCES:
patent: 4816459 (1989-03-01), Matsuishi et al.
Rollins John W.
Tokyo Tanabe Company Limited
LandOfFree
Remedy for inflammatory intestinal diseases does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Remedy for inflammatory intestinal diseases, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Remedy for inflammatory intestinal diseases will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-351779