Morpholin- and thiomorpholin-4-ylamides

C - Chemistry – Metallurgy – 07 – K

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C07K 5/027 (2006.01) A61K 38/06 (2006.01) C07K 1/06 (2006.01) C07K 5/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2093109

4-19041/A Abstract Morpholin- and thiomorpholin-4-ylamides There are described compounds of formula I Image (I), wherein R1 is hydrogen or lower alkyl, R2 is hydrogen, lower alkyl, lower alkoxycarbonyl, phenyl- or naphthyl-lower alkoxy- carbonyl, heterocyclylcarbonyl wherein heterocyclyl contains 5 or 6 ring atoms, is saturated and is bonded to the carbonyl group via a ring nitrogen atom and, in addition to the bonding nitrogen atom, contains as ring member one or more further heteroatoms selected from unsubstituted or C1-C4alkyl-substituted NH, O, S, S=O and SO2, or is lower alkanoyl, phenyl- or naphthyl-lower alkanoyl or lower alkanesulfonyl, R3 is morpholino, thiomorpholino, S-oxothiomorpholino or S,S-dioxothiomorpholino, the heterocyclyl radical in heterocyclylcarbonyl R2 having the same definition as R3 or having a definition other than R3, and R4 is hydrogen, hydroxy, C1-C4alkoxy, cyano, trifluoromethyl or fluorine, and salts of those compounds where salt-forming groups are present. These compounds are inhibitors of HIV-protease and are used in the treatment of AIDS.

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