Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-07-25
1998-12-15
Dentz, Bernard
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546118, A61K 31435, C07D47104
Patent
active
058497536
DESCRIPTION:
BRIEF SUMMARY
This applicaton is a 371 of PCT/KR95/00009 filed Feb. 8, 1995.
FIELD OF THE INVENTION
The present invention relates to novel substituted pyridyl imidazole derivatives, processes for preparing them and pharmaceutical compositions containing same as active ingredients.
DESCRIPTION OF THE PRIOR ART
Various pyridyl imidazole derivatives, which can inhibit the action of angiotensin II, have been used for the treatment of hypertension caused by angiotensin II. Angiotensin II is produced, by an angiotensin converting enzyme, from angiotensin I, which is formed from angiotensinogen in blood plasma .alpha.-globin by the action of renin. Angiotensin II, which is a potent vaso-constrictor interacting with specific receptors on cell membrane, has been reported to cause hypertension in mammals including human beings.
Many studies have been made to search for an antagonist which inhibits the action of angiotensin II on the receptors of its target cell in order to suppress the elevation of blood pressure. As a result, many imidazole derivatives have been developed(see A. T. Chiu et al., Eur. J. Pharm., 157, 13(1981); P. C. Wong et al., J. Pharmacol. Exp. Ther., 247, 1(1988); P. C. Wong et al., Hypertension, 13, 489(1989), etc.).
For example, D. J. Carini et al. reported in J. Med. Chem., 34, 2525(1990) imidazole derivatives of the following formula(A): ##STR2##
Further, EP No. 400,974 discloses imidazole derivatives of the following formula(B): ##STR3## wherein: --A'--B'--C'--D'-- represents a 6-membered heterocycle having 1 to 3 nitrogen atoms such as --C(R.sup.7)=C(R.sup.7)--C(R.sup.7)=N-- wherein each of R.sub.7 's is independently a hydrogen atom, or a substituted alkyl or aryl group or heterocycle(e.g., --C(CH.sub.3)=CH--C(CH.sub.3)=N--).
However, needs have continued to exist for the development of imidazole derivatives which inhibit more effectively the activity of angiotensin II.
SUMMARY OF THE INVENTION
Accordingly, an object of the present invention is to provide novel substituted pyridyl imidazole derivatives of formula(I), and pharmacologically acceptable salts thereof, having an enhanced ability to suppress the activity of angiotensin II: ##STR4## wherein: A is a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl group, OR.sub.1, or NR.sub.2 R.sub.3 wherein R.sub.1, R.sub.2 and R.sub.3 are independently a hydrogen, or a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl group; B is a hydrogen, or a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl group; D is a hydrogen, a halogen, or a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl group, or ##STR5## wherein Z is a hydrogen, R.sub.1, NO.sub.2, (CH.sub.2).sub.p OR.sub.5, (CH.sub.2).sub.p NR.sub.2 R.sub.3 or a halogen, n is 0 or an integer of 1 to 3, R.sub.1, R.sub.2 and R.sub.3 are the same as defined above, p is 0 or an integer of 1 to 3, and R.sub.5 is a hydrogen, a C.sub.1 -C.sub.6 alkyl group or a phenyl group substituted with a C.sub.1 -C.sub.4 alkyl; and W is ##STR6## wherein X and Y are independently O or S, m is an integer of 1 to 4, n is the same as defined above and R.sub.4 is a straight, branched or cyclic C.sub.1 -C.sub.4 alkyl group.
It is another object of the present invention to provide processes for preparing the derivatives, and provide pharmaceutical compositions containing same as active ingredients.
DESCRIPTION OF THE DRAWING
FIG. 1 is a HPLC chart showing the result of the enzyme digestion test of the Merck compound(FIG. 1A) and the present compound prepared in Example 8(FIG. 1B), respectively.
DETAILED DESCRIPTION OF THE INVENTION
The present compound of formula(I) is characterized in that the substituent W has the structure of: ##STR7## wherein R.sub.4, X, Y, n and m have the same meanings as defined previously.
Among the compounds of formula(I), preferred are those wherein A is a straight, branched or cyclic C.sub.2 -C.sub.4 alkyl group or OR.sub.1 wherein R.sub.1 is a straight, branched or cyclic C.sub.1 -C.sub.4 alkyl group; B is a hydrogen or a straight, branched or cyclic C.sub.1 -C.sub.4 alkyl group; D is
Cha Ok-Ja
Jung Yi-Sook
Kim Hye-Ryung
Kim Nak-Jeong
Kim Seon-Ju
Dentz Bernard
Korea Research Institute of Chemical Technology
LandOfFree
Pyridyl imidazole derivatives and processes for the preparation does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Pyridyl imidazole derivatives and processes for the preparation , we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Pyridyl imidazole derivatives and processes for the preparation will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1458270