Hiv protease inhibitors and processes for their preparation

C - Chemistry – Metallurgy – 07 – K

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C07K 5/02 (2006.01) A61K 38/04 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2043603

4-18105/A HIV protease inhibitors and processes for their preparation Abstract The invention relates to compounds of formula Image (I), wherein R1 is di-lower alkylamino, pyrrolidino, piperidino, morpholino, thiomorpholino, S,S-dioxothiomorpholino, piper- azino, N-lower alkylpiperazino, benzyloxy or benzyloxy substituted in the phenyl ring by lower alkyl or by lower alkoxy, A1 is a bivalent radical of one of the amino acids valine and asparagine that is bonded N-terminally to the group -(C=0) and C-terminally to the group -NH, A2 is a bivalent radical of one of the amino acids tyrosine and phenylalanine that is bonded N-terminally to the group -(C=0) and C-terminally to the group -NH, and R3 is OR2 or NHR2 wherein R2 is hydrogen or lower alkyl, and also to salts of those compounds insofar as one or more salt-forming groups is (are) present. The compounds are gag protease inhibitors and are suitable for the treatment of retroviral diseases.

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