Substituted benzylurea derivatives and medicine containing the s

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...

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514357, 514438, 514471, 514522, 514534, 514539, 514598, 514563, 546286, 546329, 549 60, 549 71, 549 72, 549474, 549496, 558417, 560 39, A61K 3117, C07C27506, C07C27528

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059227672

ABSTRACT:
Disclosed herein are substituted benzylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 are independently H, a halogen atom, or an alkyl or alkoxyl group, R.sup.3 is a phenyl or heterocyclic group which may be substituted, n is an integer of 1-6, and R.sup.4 is a phenyl group which may be substituted, or salts thereof, and medicines comprising such a derivative as an active ingredient. The derivatives or salts thereof strongly inhibit only ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.

REFERENCES:
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patent: 4623662 (1986-11-01), De Vries
patent: 5030653 (1991-07-01), Trivedi
Corwin Hansch, et al., vol. 64, No. 7, pp. 1186-1191, Jul. 1975, "Formulation of De Novo Substituent Constants in Correlation Analysis: Inhibition of Dihydrofolate Reductase by 2,4-Diamino-5(3,4-Dichlorophenyl)-6-Substituted Pyrimidines".
B. R. Baker, et al., Journal of Medicinal Chemistry, vol. 12, No. 1, pp. 86-88, 1969, "Irreversible Enzyme Inhibitors. CXXXVII. Active-Site-Directed Irreversible Inhibitors of Dihydrofolic Reductase Derived From 6-(.rho.-Aminomethylphenoxymethyl)-2,4-Dimino-5-(3,4-Dichlorophenyl)Pyrimi dine Bearing a Terminal Sulfonyl Fluoride".
B.R. Baker, et al., Journal of Medicinal Chemistry, vol. 12, No. 4, pp. 680-683, 1969, "Irreversible Enzyme Inhibitors. CLVII. Effect of Bridge Modification of the Selective Irreversible Inhibition of Dihydrofolic Reductase From L1210 Mouse Leukemia and Liver by 2, )Phenoxymethyl!Pyrimidine. I".
B.R. Baker, et al., Journal of Medicinal Chemistry, vol. 12, No. 4, pp. 684-688, 1969, "Irreversible Enzyme Inhibitors. CLVIII. Effect of Bridge Modification on the Selective Irreversible Inhibition of Dihydrofolic Reductase From l1210 Mouse Leukemia and Liver by l)Phenoxymethyl!Pyrimidine. II".

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