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US 5,707,979 AGranted
Phosphinic acid derivatives, their preparation and their use
AssigneeHoechst Aktiengesellschaft
InventorsAnuschirwan Peyman, Wilhelm Stahl, Karl-Heinz Budt, Dieter Ruppert, Henning Schussler, Konrad Wagner
Life of this patent
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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.
Claims8
A compound of the formula I ##STR9## in which A is a radical of the formula IIa, ##STR10## in which Y is oxygen;
- R.sup.1 is oxygen;
- R.sup.2 is
- hydrogen,
- (C.sub.1 -C.sub.6)-alkyl,
- (C.sub.7 -C.sub.13)-arylalkyl,
- (C.sub.6 -C.sub.12)-aryl,
- all of which are unsubstituted or substituted by hydroxyl,
- (C.sub.1 -C.sub.10)-alkyl, (C.sub.1 -C.sub.3)-alkoxy, F, Cl or Br;
- an equivalent of a physiologically tolerated salt, or
- a residue of a phosphinic acid prodrug;
- B is a radical of the formula IIIa ##STR11## where L is oxygen;
- D and D* are, independently of each other,
- R.sup.6 {(C.sub.1 -C.sub.6)-alkyl},
- where the alkyl is saturated or unsaturated, branched or unbranched,
- where R.sup.6 is
- (C.sub.6 -C.sub.12)-aryl, unsubstituted or substituted by R.sup.7 ;
- or
- (C.sub.3 -C.sub.12)-cycloalkyl, unsubstituted or substituted by R.sup.7 ;
- where R.sup.7 is, independently of each other,
- --R.sup.8
- where R.sup.8 is
- hydrogen, or
- (C.sub.1 -C.sub.6)-alkyl, unsubstituted or substituted by hydroxyl;
- E and E* are benzyl.
21 more elements
Dependencies are inferred from the claim text.