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US 5,010,087 AGranted
Tricyclic compounds and TXA.sub.2 antagonistic compositions thereof
AssigneeKyowa Hakko Kogyo Co., Ltd.
InventorsEtsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
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Abstract
Novel tricyclic compounds having a TXA.sub.2 -antagonizing activity represented by formula (I): ##STR1## which strongly antagonize an action of thromboxane A.sub.2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.
Claims10
A tricyclic compound of the formula:
- ##STR144## wherein:
- X.sub.1 --X.sub.2 is selected from the group consisting of --CH.sub.2 --O-- or ##STR145## (wherein l represents 0, 1, or 2);
- L is selected from the group consisting of --CH.dbd.CH-- or --S--;
- is a single or double bond;
- W is selected from the group consisting of --S--, --O--, --NH--, --CH.sub.2 --, --NHCO-- or .dbd.CH--, and the left side of each formula is bound to the tricyclic nucleus;
- n is 0,1,2, or 3;
- Z is selected from the group consisting of --NR.sup.1 CO--, --NR.sup.1 SO.sub.2 --, --NR.sup.1 CONH--, --NR.sup.1 CSNH--, --NR.sup.1 NHCONH--, --NR.sup.1 NHCSNH--, --NR.sup.1 COO-- or --NR.sup.1 COS--, wherein R.sup.1 is hydrogen or lower alkyl, and the right side of each formula is bound to Q;
- Q is selected from the group consisting of optionally substituted, N-substituted or unsubstituted pyrrolyl, (wherein the N-substituent is lower alkyl, phenyl or benzyl), pyridyl, quinolyl or isoquinolyl wherein substitution means 1 to 3 substituents on the aromatic ring, independently selected from lower alkyl, phenyl, benzyl, halogen, triflouromethyl, nitro, OR.sup.2 or SR.sup.2, (wherein R.sup.2 represents hydrogen, lower alkyl, phenyl or benzyl);
- one of R.sup.A and R.sup.B is hydrogen and the other is --Y--M-- wherein Y is selected from the group consisting of a single bond, --CR.sup.3 R.sup.4 --(CH.sub.2).sub.m -- and --CR.sup.3 .dbd.CR.sup.4 --(CH.sup.2).sub.m)-- and each of R.sup.3 and R.sup.4 are independently hydrogen or lower alkyl and m is 0, 1, 2, 3, or 4, wherein the left side of each formula is bound to the tricyclic nucleus;
- M is --COOR.sup.5 and R.sup.5 is hydrogen, lower alkyl or --CONR.sup.5a R.sup.5b and each of R.sup.5a and R.sup.5b independently are hydrogen or lower alkyl;
- each of G.sup.A and G.sup.B are independently lower alkyl, halogen or OR.sup.6 and R.sup.6 represents hydrogen, lower alkyl, phenyl or benzyl;
- each of g.sup.A and g.sup.B are independently 0, 1, 2 or 3;
- or a pharmaceutically acceptable salt thereof.
10 more elements
Dependencies are inferred from the claim text.