Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-06-26
1997-11-11
Grumbling, Matthew V.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
544284, A61K 31505, C07D40302
Patent
active
056864582
DESCRIPTION:
BRIEF SUMMARY
This is a 371 of PCT/KR93/00096 filed Oct. 29, 1993.
FIELD OF THE INVENTION
The present invention relates to novel quinazoline derivatives and pharmaceutically acceptable salts thereof which possess an excellent anti-secretory activity, pharmaceutical compositions containing the same as an active ingredient, their novel intermediates, and processes for the preparation thereof.
BACKGROUND OF THE INVENTION
For the treatment of peptic ulcer disease, various drugs such as antacid, anticholinergic agent and H.sub.2 -receptor antagonist have been used. Recently, the advent of omeprazole useful as a proton pump inhibitor has rekindled research activities in this field.
However, it has been pointed out that the proton pump inhibition by omeprazole is irreversible, which may induce side effects. Accordingly, various attempts to develop a reversible proton pump inhibitor are being actively made. For example, European Patent Nos. 322133 and 404322 disclose quinazoline derivatives involving a reversible proton pump inhibitor.
SUMMARY OF THE INVENTION
The present inventors have carried out extensive research to develop a reversible proton pump inhibitor with improved efficacy; and, as a result, have discovered that quinazoline derivatives having a tetrahydroisoquinoline group at the 4-position of the quinazoline nucleus exhibit excellent proton pump inhibition effects and have the ability to attain a reversible proton pump inhibition.
Accordingly, it is an object of the present invention to provide novel quinazoline derivatives having a tetrahydroisoquinoline group at the 4-position of the quinazoline nucleus, and pharmaceutically acceptable salts thereof.
It is another object of the present invention to provide processes for preparing said compounds.
It is a further object of the present invention to provide pharmaceutical compositions containing the same as active ingredients.
It is still another object of the invention to provide novel intermediate compounds useful for the preparation of the inventive quinazoline derivatives.
BRIEF DESCRIPTION OF THE DRAWINGS
The present invention may be more fully understood with reference to the following drawings, wherein:
FIGS. 1 to 3 depict the Lineweaver-Burk plots of the specific activities obtained from an exemplary inventive compound, omeprazole and SK&F96067.
DETAILED DESCRIPTION OF THE INVENTION
In accordance with the present invention, there is provided novel quinazaline derivatives of formula(I) and their pharmaceutically acceptable salts: ##STR2## wherein, R.sub.1 and R.sub.2 are each hydrogen or a C.sub.1 -C.sub.4 alkyl group; same or different, are each hydrogen, a C.sub.1 -C.sub.4 alkyl group, a cyclopropyl group, or a C.sub.1 -C.sub.4 alkyl group substituted with a halogen;
Among the compounds of the present invention, preferred are those wherein; same or different, hydrogen, a C.sub.1 -C.sub.4 alkyl group or a C.sub.1 -C.sub.4 alkyl group substituted with a halogen.
Particularly, preferred compounds of the present invention are listed below: inazoline; inazoline; nazoline; nazoline; e-2-yl)quinazoline; ine-2-yl)quinazoline; e; azoline; inazoline; ne-2-yl)quinazoline; ne-2-yl)quinazoline; e-2-yl)quinazoline; soquinoline-2-yl)quinazoline; droisoquinoline-2-yl)quinazoline; droisoquinoline-2-yl)quinazoline; -tetrahydroisoquinoline-2-yl)quinazoline; quinoline-2-yl)quinazoline; 4-tetrahydroisoquinoline-2-yl) quinazoline; e-2-yl)quinazoline; oquinoline-2-yl)quinazoline; e-2-yl)quinazoline; inoline-2-yl)quinazoline; ydroisoquinoline-2-yl) quinazoline; -2-yl)quinazoline; quinoline-2-yl)quinazoline; droisoquinoline-2-yl) quinazoline; e-2-yl)quinazoline; oquinoline-2-yl)quinazoline; oline-2-yl)quinazoline; roisoquinoline-2-yl)quinazoline; oline-2-yl)quinazoline; roisoquinoline-2-yl)quinazoline; oline-2-yl)quinazoline; roisoquinoline-2-yl)quinazoline; oline-2-yl)quinazoline; roisoquinoline-2-yl)quinazoline; ine-2-yl)quinazoline; isoquinoline-2-yl)quinazoline; and oquinoline-2-yl)quinazoline.
The quinazoline derivatives of formula(I) in the present invention may
REFERENCES:
patent: 3956495 (1976-05-01), Lacefield
patent: 3960861 (1976-06-01), Danilewicz et al.
patent: 4044136 (1977-08-01), Danilewicz et al.
patent: 5064833 (1991-11-01), Ife et al.
patent: 5444062 (1995-08-01), Coe et al.
Chae Jeong Seok
Jo Dae Woong
Kim Chang Seop
Kim Jae Kyu
Lee Jeong Won
Grumbling Matthew V.
Yuhan Corporation
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