Antiviral ethers of aspartate protease substrate isosteres

Details Antiviral ethers of aspartate protease substrate isosteres Antiviral ethers of aspartate protease substrate isosteres

1995-10-19

1997-09-02

Ramsuer, Robert W.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

N-c doai

514479, 544168, 546221, 548200, 560 27, A61K 31215, C07C27120

Patent

active

056632002

ABSTRACT:
Antiretroviral compounds (which are effective, for example, against HIV) of the formula I ##STR1## in which R.sub.1 is an acyl radical lower-alkoxyl-lower-alkanoyl whose lower alkoxy radical is unsubstituted or is substituted by halogen, phenyl, lower alkoxy or a heterocyclic radical selected from piperidinyl, pyrrolidinyl, tetrahydropyranyl, tetrahydrofuranyl, thiazolidinyl, thiazolyl, indolyl or 4H-1-benzopyranyl which is unsubstituted or substituted by oxo, hydroxyl, amine, lower alkyl, lower-alkoxycarbonyl and/or phenyl-lower-alkoxycarbonyl; lower alkanoyl which is unsubstituted or is substituted by one of the said unsubstituted or substituted heterocyclic radicals; arylcarbonyl or heterocyclylcarbonyl which are substituted by heterocyclyl or heterocyclyl-lower-alkyl; phenyl-lower-alkanoyl which is substituted by hydroxyl and lower alkyl; or arylsulfonyl;
or the residue of an amino acid which is defined in accordance with the description (and which may be acylated on the amino nitrogen by one of the abovementioned acyl radicals);

REFERENCES:
patent: 4894437 (1990-01-01), TenBrink
patent: 5189017 (1993-02-01), Lukas et al.
Rich et al., J. Med. Chem. 34, 1225-1228 (1991).
de Solms et al, J. Med. Chem. 34, 2852-2857 (1991).

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