Cyclic phosphonate ester inhibitors of microsomal triglyceride t

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...

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544157, 546 22, 548113, 558 83, A61K 31675, A61K 3166, C07F 96574, C07F 96541

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active

059624400

ABSTRACT:
Novel cyclic phosphonate ester inhibitors of MTP are provided which have the structure ##STR1## wherein R.sup.2, L.sup.2, A, B, L.sup.1, R.sup.1 and R.sup.5a are as set out herein. These compounds are useful in lowering serum cholesterol and triglycerides.

REFERENCES:
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Cairns, M. et al, "Photorearrangements of Benzyl Phosphites Stereochemistry at Phosphorus", Tetrahedron Letters, vol. 30, No. 9, pp. 1025-1028, 1989.
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Yamashita, M. et al, "Nucleophilic Substitution with Phosphide Anions Prepared by an Action of Sodium Dihydridobis(2-methoxyethanolato)aluminate on Phosphorus Compounds", Bull. Chem. Soc. Jpn., 46,219-222 (1983).
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Bentrude, W.G. et al, "Conformations of Saturated Phosphorus Heterocycles. IV. .sup.1 H, .sup.13 C, and .sup.31 P Nuclear Magnetic Resonance Studies of Geometrical Isomers of 2-Z-4-Methyl-and 4-tert-Butyl-1,3,2-dioxaphospholanes", J. of the Amer. Chem. Soc. 98:7, Mar. 31, 1976, pp. 1850-1859.
Bentrude, W.G. et al, "Conformations of Saturated Cyclic Phosphorus Heterocycles, II, 5-tert-Butyl-2-amino-1,3,2-dioxaphosphorinanes, Apparent Effects of P-N Vicinal Interactions on the Conformational Energy of Amino Groups on Trivalent Phosphorus . . . ", J. of the Amer. Chem. Soc. 95:14, Jul. 11, 1973, pp. 4666-4675.
Bentrude, W.G. et al, "Free-Radical Chemistry of Organophosphorus Compounds. Free-Radical Arbuzov Reaction Stereochemistries and the Question of Available Permutational Modes for Phosphoranyl Radicals", J. of the Amer. Chem. Soc. 99:13,Jun. 22, 1977, pp. 4383-4390.

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