Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1992-12-11
1994-08-23
Ivy, C. Warren
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514217, 514431, 514450, 540489, 549 12, 549268, 549354, A01N 4346, C07D27302, C07D31306, C07D33712
Patent
active
053408071
ABSTRACT:
Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6 alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 --O, CH.sub.2 --(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.14 represents hydrogen or C1-6 alkyl) and Z represents oxygen or sulfur, or a pharmaceutically acceptable salt thereof. The compound possesses an acyl coenzyme A: cholesterol acyltransferase-inhibiting activity, and thus are expected to have preventive and therapeutic effects on hyperlipemia and arteriosclerosis.
REFERENCES:
patent: 4136197 (1979-01-01), Hubner
patent: 4489090 (1984-12-01), DeVries et al.
patent: 4868210 (1989-09-01), Trivedi
Chemical Abstract, vol. 91, No. 39211y, 1979, Abou-Gharbia et al, "Synthesis of tricyclic arylspiro comp. as potential antileukemic and anticonvulsant agents".
J. Am. Chem. Soc. (1984) 106, 4175-80.
Heterocycles, vol. 12, No. 5, (1979) 637-45.
Chem. Abst., 98 (1983) 89198q.
Harakawa Hiroyuki
Kubo Kazuhiro
Kumazawa Toshiaki
Obase Hiroyuki
Oda Shoji
Covington Raymond
Ivy C. Warren
Kyowa Hakko Kogyo Co. Ltd.
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