Phosphinic acid derivatives, their preparation and their use

Details Phosphinic acid derivatives, their preparation and their use Phosphinic acid derivatives, their preparation and their use

1995-06-28

1998-01-13

Ambrose, Michael G.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Phosphorus containing other than solely as part of an...

558 81, 562 9, 562 15, 564 12, A61K 31675, C07F 96584

Patent

active

057079790

ABSTRACT:
Compounds of the formula I, ##STR1## in which the symbols or substituents A, B, D, D*, E and E* have the meanings given in the specification, inhibit aspartyl proteases and are suitable for controlling viral diseases.

REFERENCES:
J.A. Martin, "Recent Advances in the Design of HIV Proteinase Inhibitors," Antiviral Research, 17, pp. 265-278 (1992).
S.S. Abdel-Mequid, "Inhibitors of Aspartyl Proteinases," Medicinal Research Reviews, vol. 3, No. 6, pp. 731-778 (1993).
M. Lang et al., "HIV-1 Protease Inhibitors: Development, Status, and Potential Role in the Treatment of AIDS," Arch Phar., vol. 326, pp. 921-924 (1993).
P.Y.S. Lam et al., "Rational Design of Potent, Bioavailable, Nonpeptide Cyclic Ureas as HIV Protease Inhibitors," Science, vol. 263, pp. 380-384 (1994).
D.N. Srivastva et al., "Bioreversible Phosphate Protective Groups: Synthesis and Stability of Model Acyloxymethyl Phosphates," Bioorganic Chemistry, vol. 12, pp. 118-129 (1984).
Christian Perigaud et al., "Rational Design for Cytosolic Delivery of Nucleoside Monophosphates: Sate and DTE as Enzyme-Labile Transient Phosphate Protecting Groups," Bioorganic & Medicinal Chemistry Letters, vol. 3, No. 12, pp. 2521-2526 (1993).
A. Peyman et al., "C.sub.2 -symmetrische Inhibitoren der HIV-Protease auf Phosphinsaurebasis," Angew. Chem, vol. 105, No. 12, pp. 1852-1854 (1993).
B. Stowasser et al., "New Hybrid Transition State Analog Inhibitors of HIV Protease with Peripheric C.sub.2 -Symmetry," Tetrahedron Letters, vol. 33, No. 44, pp. 6625-6628 (1992).
L. Maier, "Organic Phosphorus Compounds. LXXI, Preparation, Properties, and Structure of Bis(Aminomethyl)phosphinic Acid, (H.sub.2 NCH.sub.2) P(O)OH," J. of Organometallic Chem., vol. 178, pp. 157-169 (1979).
A. Peyman et al., "Non-Peptide-Based Inhibitors of Human Immunodeficiency Virus-1 Protease", Bioorganic & Medicinal Chemistry Letters, vol. 4, No. 21, (1994), pp. 2601-2604.

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