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US 5,629,431 AGranted
Inhibitors of retroviral proteases
AssigneeHoechst Aktiengesellschaft
InventorsKarl-Heinz Budt, Anuschirwan Peyman
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Abstract
The present invention relates to compounds of the formula I ##STR1## in which A, Q, R.sup.2, R.sup.3, R.sup.4 and the corresponding radicals with an * are defined as indicated in the description, a process for the preparation thereof, and the use thereof for inhibiting retroviral proteases.
Claims2
A compound of the formula I ##STR8## wherein:
- Q is a radical of the formula IIa;
- ##STR9## in which:
- Y is oxygen;
- R.sup.5 is hydrogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.6 -C.sub.10)-aryl, (C.sub.7 -C.sub.20)-arylalkyl, which may be substituted by alkoxy, or glyceryl or is a residue of a phosphate prodrug, or acyl-oxyalkyl;
- A is a radical of the formula (IV):
- D--(E).sub.n --(F).sub.o --(G).sub.p (IV)
- in which:
- E, F or G is Gly, Ala, Val, Leu, lle, Nva, Nle, Phe, Tyr, Asp or Glu;
- D is R.sup.1 or a radical of the formula (VI):
- ##STR10## and n+o+p is 1;
- R.sup.1 is hydrogen, (C.sub.1 -C.sub.6)-alkylsulfonyl, (C.sub.8 -C.sub.10)-aryl-(C.sub.1 -C.sub.2)-alkyl, triphenylmethyl, (C.sub.1 -C.sub.6)-alkoxycarbonyl or (C.sub.6 -C.sub.10)-aryl-(C.sub.1 -C.sub.2)-alkoxycarbonyl;
- R.sup.2 is hydrogen, phenyl or benzyl;
- R.sup.3, R.sup.4 and R.sup.11 are hydrogen and
- R.sup.9 is hydrogen, n-propyl, isopropyl, n-butyl, sec.-butyl, isobutyl, benzyl, carboxymethyl, carboxyethyl, 1-naphthylmethyl, 2-napthylmethyl, 2-(methylthio)ethyl, 2-(methylsulfinyl)ethyl, 2-(methylsulfonyl)ethyl, indol-2-yl-methyl or indol-3-yl-methyl;
- or a physiologically tolerated salt thereof.
12 more elements
A compound of the formula I ##STR11## wherein:
- Q is radical of the formula IIa ##STR12## in which:
- Y is oxygen;
- R.sup.5 is hydrogen or (C.sub.1 -C.sub.4)-alkyl;
- A is a radical of the formula (IV):
- ti D--(E).sub.n --(F).sub.o --(G).sub.p (IV)
- in which:
- E, F or G is Val, Phe, lle or Asp;
- D is R.sup.1 or a radical of the formula (VI):
- ##STR13## and n+o+p is 1;
- R.sup.1 is hydrogen, (C.sub.1 -C.sub.6)-alkylsuifonyl, phenyl-(C.sub.1 -C.sub.2)-alkyl, triphenymethyl, (C.sub.1 -C.sub.6)-alkoxycarbonyl or phenyl-(C.sub.1 -C.sub.2)-alkoxycarbonyl;
- R.sup.2 is hydrogen, phenyl or benzyl;
- R.sup.3, R.sup.4 and R.sup.11 are hydrogen;
- and
- R.sup.9 is hydrogen, isopropyl, sec.-butyl, benzyl, carboxymethyl, 1-napthylmethyl, 2-(methylthio)ethyl or indol-2-yl-methyl;
- or a physiologically tolerated salt thereof.
12 more elements
Dependencies are inferred from the claim text.