Tricyclic compounds and intermediates thereof

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514510, 514562, 514563, 514599, 514616, 514617, 514618, 514619, 514621, 514622, 514824, 546 93, 558 12, 558 13, 558411, 558414, 558415, 558416, 560 10, 560 18, 560 21, 560 22, 560 23, 560 25, 560 28, 562427, 562435, 562437, 562438, 562453, 562455, 564 74, 564154, 564155, 564158, 564162, 564166, 564167, 564168, 564169, 564172, 564180, A61K 3144, A61K 31165, C07C23700, C07C20700

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active

054788358

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 -S(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 et al.
patent: 4489090 (1984-12-01), DeVries et al.
patent: 4868210 (1989-09-01), Trivedi
Abou-Gharbia et al., Chemical Abstracts, vol. 91 (1979) 39211y.
J. Am. Chem. Soc. (1984) 106, 4175-80.
Heterocycles, vol. 12, No. 5 (1979) 637-45.
Chemical Abstracts, vol. 98 (1983) 89198q.
Chemical Abstracts, vol. 91 (1979) 39211y.

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